Autonomic Drugs Cholinomimetics: Drug Moa and Indication Adverse Effects Notable Properties

DRUG MOA and INDICATION ADVERSE EFFECTS NOTABLE PROPERTIES
1. AUTONOMIC DRUGS
Cholinomimetics
A. Direct Acting Choline Esters
Muscarinic agonist; activates M1 through M3 receptors in all peripheral
tissues. Results to increased secretion, smooth muscle contraction (except CNS stimulation, miosis, cyclospasm, brochoconstriction,
in vascular smooth muscles where it causes relaxation) and changes in excessive GI and GU smooth muscle contraction, increased very short lived DOA: 5-30sec, apidly hydrolyzed by AChE; acts
i. Acetylcholine heart rate secretory activity of sweat gland, airways etc, vasodilation on both M and N receptors
Results in smooth muscle contraction except in vascular smooth
Muscarinic agonist; activates M1 through M3 receptors in all peripheral Cylospasm, diarrhea, urinary urgency, vasodilation, reflex muscles where it causes relaxation; resistant to AChE, orally
ii.Betanechol tissues (same as Ach) ; for Bladder and bowel atony tachycardia, sweating active, act on M receptors only
Nonselective muscarinic and nicotinic agonist; similar to betanechol; used Cylospasm, diarrhea, urinary urgency, vasodilation, reflex
iii. Carbachol topically for glaucoma treatment tachycardia, sweating acts on both M and N receptors, DOA: 30mins-2hrs
B. Direct Acting Muscarinic Alkaloids
Partial muscarinic agonist; used for treatment of Glaucoma, Sjogren's
i. Pilocarpine syndrome and Sicca syndrome Miosis, blurring of vision good lipid solubility compared to choline esters
C. Direct Acting Nicotinic Agonists
Agonist at both NN and NM receptos; activates autonomic post ganglionic
neurons (both sympathetic and parasympathetic) and skeletal muscle Generalized ganglionic stimulation (hypertension, tachycardia, Able to enter the CNS and activates NN receptors ; DOA: 1-6h
i. Nicotine neuromuscular end plates ; for Smoking Cessation nausea, vomiting, diarrhea) only
Selective partial agonist at nicotinic receptors; used exclusively for smoking Generalized ganglionic stimulation (hypertension, tachycardia,
ii. Varenicline cessation nausea, vomiting, diarrhea) longer DOA than nicotine: 12-24h
D. Short Acting Cholinesterase
Inhibitor (Alcohol)
Binds briefly to active site of acetylcholinesterase (AChE) and prevents
access of acetylcholine (Ach); Amplifies all actions of Ach; increases
parasympathetic activity and somatic neuromuscular transmission ; for
i. Edrophonium Myasthenia gravis diagnosis (Tensilon test) Miosis, salivation, nausea, vomiting, diarrhea, bradycardia parenteral, very short lived DOA: 5-15min
E. Intermediate Acting Cholinesterase
Inhbitors (Carbamates)
Forms covalent bonds with AChE, but is hydrolyzed and released; Longer
acting than Edrophonium ; for Myasthenia gravis treatment; reversal of
i. Neostigmine nondepolarizing muscular blockade, Ogilvie syndrome Miosis, salivation, nausea, vomiting, diarrhea, bradycardia poor lipid solubility, oral, DOA: 30min-2h
ii. Pyridostigmine Longer acting effect compared to Neostigmine Miosis, salivation, nausea, vomiting, diarrhea, bradycardia poor lipid solubility, oral, DOA: 4-8h
iii. Physostigmine Natural alkaloid tertiary amine, similar to neostigmine Miosis, salivation, nausea, vomiting, diarrhea, bradycardia good lipid solubility: able to enter the CNS, DOA: 4-8h
F. Long Acting Cholinesterase
Inhibitors (Organophosphates)
i. Echothiophate Similar to neostigmine but with slower release Miosis, salivation, nausea, vomiting, diarrhea, bradycardia moderate lipid solubiliy, DOA: 2-7days
ii. Malathion, Parathion malathion: scabicide, parathion: insecticide Miosis, salivation, nausea, vomiting, diarrhea, bradycardia high lipid solubiliy, DOA: 7-30 days
Cholinoceptor Blocking Drugs
Competitively blocks all muscarinic receptors, antagonizes histamine and Drowsiness, blurring of vision, dry eyes, constipation, dry mouth,
i. Scopolamine serotonin ; for motion sickness, dec. acid secretion in the GIT urinary retention known as Hyoscine-N-Butyl-Bromide (Buscopan)
Nonselective competitive antagonism at all muscarinic receptors in the CNS

and peripheral tissues; causes mydriasis and cycloplegia; mandatory
antidote for severe cholinesterase inhibitor poisoning ; Mydriatic, cycloplegic,
antidote for organophosphate poisoning (DOC), for bradycardia, DOC for organophosphate poisoning; notorious for causing
ii. Atropine hypersalivation and to decrease airway secretion during general anesthesia hyperthermia
Similar to atropine but with a shorter duration of action (12-24h) ; Mydriatic,
iv. Homatropine cycloplegic in eye examinations Mydriatic, cycloplegic
Similar to atropine but with a shorter duration of action (3-6h), Mydriatic,
v. Cyclopentolate cycloplegic in eye examinations Mydriatic, cycloplegic
Similar to atropine but with the shortest duration of action (15-60min); Tachycardia, mydriasis, cyloplegia, skin flushing, delirium,
vi. Tropicamide Mydriatic, cycloplegic in eye examinations hallucinations, urinary retention, constipation shorter DOA among cholineceptor blockers (15-60min)
Competitive nonselective antagonist at muscarinic receptors ; for BA and not as effective as SABAs but less tachycardia and arrhythmia ;
vii. Ipratropium COPD Dry mouth, cough, nasal dryness few muscarinic effects outside the lungs
not as effective as SABAs but less tachycardia and arrhythmia ;
Similar to Ipratropium but with longer duration of action
viii. Tiotropium Dry mouth, cough, nasal dryness few muscarinic effects outside the lungs
Nonselective muscarinic antagonist which reduces detrussor smooth muscle
tone spasms ; for decreasing urgency in mild cystitis and dec. bladder Tachycardia, mydriasis, cyloplegia, skin flushing, delirium,
ix. Oxybutinin spasm after urologic surgery hallucinations, urinary retention, constipation for urinary urgency and incontinence
Regenerates active acetylcholinesterase; can relieve skeletal muscle and Must be administered before 6-8 hours of organophosphate bond
endplate block ; Usual antidote for early stage cholinesterase inhibitor with cholinesterase occurs ; has oxime group which has high
x. Pralidoxime poisoning muscle weakness affinity for phosphorus
xi. Hexamethonium, Competitively blocks all Nn nicotinic Ach receptors ; for Hypertensive Postural hypotension, dry mouth, blurred vision, constipation,
Mecamylamine, Trimethaptan emergencies (obsolete) sexual dysfunction first successful agents in treating HTN
Sympathomimetics
Non-selective, direct acting sympathomimetic; activates A and B adrenergic
receptors; A1 - vasoconstriction and increased BP; B1 - increased HR,
conduction and contractility; B2 - bronchodilatation ; used for Cardiac arrest, DOC for Anaphylaxis ; inactive per orem ; do not enter CNS
i. Epinephrine anaphylaxis, asthma, COPD, Hemostasis Hypertension, tachycardia, ischemia, hyperglycemia significantly ; short DOA
Non-selective, direct acting sympathomimetic; activates A and B adrenergic

receptors; A1 - vasoconstriction and increased BP; B1 - increased HR, Compensatory vagal reflexes tend to overcome the direct postive
conduction and contractility; B2 - bronchodilatation ; used for Neurogenic Extreme vasospasm, tissue necrosis, excessive BP increase, chronotropic effects ; alpha activity > beta activity; inactive per
ii. Norepinephrine shock, cardiogenic shock arrhythmias, infarction, reflex bradycardia orem ; do not enter CNS significantly ; short DOA
Non-selective, direct acting sympathomimetic; activates A, B and D1

adrenergic receptors; A1 - vasoconstriction and increased BP; B1 -
increased HR, conduction and contractility; D1 - vasodilation in splanchnic inactive per orem ; do not enter CNS significantly ; short DOA;
iii. Dopamine and renal blood vessels ; for cardiogenic Shock and heart failure Cardiovascular disturbances, arrhythmias very effective in renal failure associated with shock
Beta nonselective sympathomimetic; nonselectively activates B adrenergic
receptors; B1 - increased HR, conduction and contractility; B2-
iv. Isoproterenol bronchodilatation ; for Asthma Cardiovascular disturbances, arrhythmias synthetic catecholamine, not readily taken up into nerve endings
A1 agonist used for short term maintenance of BP in acute hypotension; also

used intranasally to produce local vasoconstriction as a decongestant ; Rebound nasal congestion (Rhinitis medicamentosa),
vi. Phenylephrine mydriatic, for drug-induced hypotension, spinal shock hypertension, stroke, MI Mydriasis without cycloplegia
A2 agonist that inhibits adenylyl cyclase and interacts with other intracellular
pathways; marked vasodilation by central sympatholytic effect ; for When taken per orem, there is initial inc in BP then will go down
vii. Clonidine Hypertension, Cancer pain, opioid withdrawal Sedation, rebound hypertension, dry mouth once the drug enters the CNS
viii. Methyldopa, Guanfacine and Central sympatholytics analogous to clonidine ; Methyldopa is used for Pre-
Guanabenz eclampsia Sedation, positive Coomb's test (Hemolytic anemia) Methyldopa - positive Coomb's test (Hemolytic anemia)
A2 agonist; reserved for ophthalmologic use in glaucoma for reduction of
xi. Apraclonidine, Brimonidine intraocular pressure eye discomfort, hyperemia and pruritus, blurred vision NONE
B1 agonist that activates adenylyl cyclase, increasing myocardial Tachyarrhythmia, Hypertension, Eosinophilic myocarditis,
contractility; with positive inotropic effect ; Clinically used for cardiogenic Premature ventricular beats, Angina, Dyspnea, Fever,
xii. Dobutamine shock and acute heart failure Headache, Nausea, Palpitation Beta1 selective
B2 agonist with adenylyl cyclase activation; results to bronchial smooth Nausea , Fever, Bronchospasm, Vomiting, Headache, Dizziness,
xiii. Albuterol/Salbutamol muscle dilation ; for Bronchial Asthma Cough, Allergic reactions Rapid development of tolerance; DOC as Asthma reliever
D1 agonist that activates adenylyl cyclase; results to vascular smooth Angina, Cardiac dysrhythmia, Dizziness, Flushing, Heart failure,
xiv. Fenoldopam muscle relaxation ; for Hypertension Hypotension, Myocardial infarction, Tachycardia D1 agonist
D2 agonist that inhibits adenylyl cyclase and interacts with other intracellular
pathways; restores dopamine actions in the CNS for Parkinson's disease,
xv. Bromocriptine prolactinemia Nausea, Hypotension, Headache, Dizziness D2 agonist
Sympatholytics
Irreversibly blocks A1 and A2 receptors resulting to indirect baroreflex
activation. Decreases blood pressure but increases heart rate due to
i. Phenoxybenzamine baroreflex activation ; for Pheochromocytoma Orthostatic hypotension, Reflex tachycardia, GI irritation Irreversible blockade
Reversible A1 and A2 receptor antagonist with low half life ; for
ii. Phentolamine Pheochromocytoma and Rebound hypertension Orthostatic hypotension, Reflex tachycardia, GI irritation Reversible blockade
Blocks A1 but not A2 receptors; leads to reduction in blood pressure ; for Dizziness, Drowsiness, Headache, Weakness, Asthenia,
iii. Prazosin, Doxazosin, Terazosin Benign Prostatic Hyperplasia, Hypertension Nausea, Palpitation, Edema, Orthostatic hypotension Used in patients with HTN and BPH at the same time
Slightly selective A1a blockade causing relaxation of prostatic smooth Headache, Orthostatic hypotension, Rhinitis, Abnormal Slightly selective A1a blockade causing relaxation of prostatic
iv. Tamsulosin muscles > vascular smooth muscle ; for BPH ejaculation, Dizziness, Arthralgia, Infection smooth muscles > vascular smooth muscle
Beta blockade > A1 blockade; still with BP depressant effects and limited HR
vi. Labetalol increase safe in pregnant patients
Blocks B1 and B2 receptors; lowers both HR and BP and reduces the
release of renin ; for Angina prophylaxis, hypertension, arrhythmias,
vii. Propranolol, Nadolol, Timolol migraine, performance anxiety, hyperthyroidism Propranolol has local anesthetic effect
B1 > B2 blockade; lowers both HR and BP, reduces the release of renin
viii. Metoprolol, Atenolol, Alprenolol, BUT is considered safer for patients with asthma ; for Angina prophylaxis, Nebivolol has vasodilating effect ; metoprolol reduce moratlity in
Betaxolol, Nebivolol hypertension, arrhythmias, migraine, performance anxiety, hyperthyroidism heart failure
x. Pindolol, Acebutolol, Carteolol,
Bopindolol, Oxprenolol, Celiprolol, B1, B2 with intrinsic sympathomimetic (partial agonist) effect; lowers BP with
Penbutolol modest reduction in HR Pindolol is a partial agonist, therefore safer in bronchial asthma
xi. Carvedilol, Medoxalol, Beta blockade > A1 blockade; still with BP depressant effects and limited HR
Bucindolol, Labetalol increase ; for Heart Failure Carvedilol reduce mortality in heart failure
Bronchospasm, cardiac depression, AV block, hypotension,
B1 > B2 blockade; for rapid control of BP and arrhythmias, thyrotoxicosis dizziness, headache; Use in caution with DM Px: Masks
xii. Esmolol and myocardial ischemia intraoperatively ; for Supraventricular tachycardia symptoms of hypoglycemia in diabetics Used in for perioperative thyroid storm
2. CARDIOVASCULAR-RENAL DRUGS
Antihypertensives
lower BP by decreasing volume and a direct vascular effect that is not yet
A. Diuretics fully understood
Inhibit Na/Cl transporter in distal convoluted tubule. Cause moderate
i.Thiazide: Hydrochlorothiazide, diuresis and reduced excretion of calcium; for mild to moderate hypertension Hypokalemic metabolic alkalosis, Dilutional hyponatremia,
Chlorthalidone, Metolazone, (FIRST LINE), Heart failure, Nephrogenic Diabetes Insipidius, Renal calcium Potassium wasting, hyperlipidemia, hyperuricemia, sulfa allergy, causes hypercalcemia in contrast with loop diuretics which cause
Indapamide stones hyperglycemia, hypercalcemia hypocalcemia ; FIRST LINE for mild to moderate hypertension
Inhibit Na/K/2Cl transporter in thick ascending limb of loop of Henle, Cause Hypokalemic metabolic alkalosis, Potassium wasting, ototoxicity,
ii. Loop: Furosemide, Torsemide, powerful diuresis and increased CA excretion; for heart failure, hypertension, hyperuricemia, nephrotoxicity, dehydration, hypomagnesemia, causes hypocalcemia in contrast with thiazide diuretics which
Bumetanide, Ethacrynic Acid acute renal failure, Pulmonary edema, hypercalcemia, Anion overdose sulfa allergy cause hypercalcemia
decrease venous return, decrease HR, decrease contractile force, decrease
B. Sympathoplegics cardiac output, decrease TPR
i.Sympathetic Outflow Blocker: activates a2 adrenergic receptors ; for hypertensive urgency (clonidine), pre dry mouth, sedation, rebound hypertension, hemolytic anemia: Taper use prior to discontinuation to avoid rebound hypertension
Clonidine, Methyldopa eclampsia (methyldopa) (+) Coomb's test (methyldopa), sedation ; readily enter the CNS
ii. Ganglion blockers: competetively blocks Nn nicotinic Ach receptors; for hypertension (obsolete), Postural hypotension, blurred vision, constipation, dry mouth,
Hexamethonium,Trimethaphan hypertensive emergencies sexual dysfunction NONE
Reserpine Irreversibly blocks the vesicular monoamine transporter (VMAT)

iii. Nerve terminal blockers: while Guanethidine and Guanadrel inhibit the vesicular release of NE from
Reserpine, Guanethidine, Guanadrel the presynaptic neuron; for Hypertension (obsolete) Sedation, suicidal ideation, severe psychiatric depression NONE
iv. Adrenergic antagonists: Tamsulosin is most selective for prostatic smooth muscle ;
Prazosin,Doxazosin, Terazosin, selectively blocks a1 adrenergic receptors; for hypertension, benign prostatic Reflex tachycardia (less chance), first dose orthostatic Doxazosin and Terazosin has longer duration of action than
Tamsulosin, Silodosin hyperplasia hypotension prazosin
C. Vasodilators
Release NO from endothelial cells, Relaxes arteriolar smooth muscle,
causing vasolidation. Decreases afterload ; for pre-eclampsia, hypertension, Edema, myocardial ischemia, drug induced lupus (hydralazine), combination treatment with ISDN for heart failure is more
i. Oral Vasolidator: Hydralazine heart failure reflex tachycardia effective than ACEIs in blacks
Opens K+ channels in vascular smooth muscle, causing hyperpolarization,
muscle relaxation and vasolidation; for alopecia / male pattern baldness, Edema, Angina, Reflex tachycardia, Pulmonary hypertension, require concomitant use of diuretics and BBs to block
Minoxidil hypertension Pericarditis, Hirsutism, salt and water retention compensatory responses
ii. Calcium Channel Blockers
Non-dihydropyridine calcium block voltage-gated L-type calcium channels (cardiac > vascular); for Constipation, Nausea, flushing,gingival hyperplasia, AV block,
channel blocker: Verapamil, Diltiazem Angina, Supraventricular tachycardia, migraine, hypertension sinus node depression, Pretibial edema, dizziness excessive cardiac depression may occur
Dihydropyridine calcium
channel blocker: Nifedipine,
Amlodipine, Nicardipine, Nisoldipine, block voltage-gated L-type calcium channels (vascular > cardiac); for
Isradipine, Felodipine Angina, hypertension Nausea, Flushing, dizziness, pretibial edema, constipation greater vasodilator effect that cardiodepressant effect
iii. Parenteral Vasodilators
relaxes venous and arteriolar smooth muscle; for acute heart failure, not commonly used because it is very light sensitive, has short
Nitroprusside controlled hypotension, cardiogenic shock, hypertensive emergency hypotension, headache, CN toxicity Duration of action ; given as continuous infusion
a thiazide derivative without a diuretic effect ; also reduces
Opens K+ channels in vascular smooth muscle, causing hyperpolarization, insulin release (can be used to treat hypoglycemia in insulin-
Diazoxide muscle relaxation and vasolidation; for hypertension hypotension, headache producing tumors)
causes arteriolar vasolidation of the afferent and efferent arterioles.

Fenoldopam Increases renal blood flow; for hypertensive emergency hypotension, hypokalemia short duration of action: 10mins
D. Angiotensin antagonists and renin
inhibitor
cough, hyperkalemia, rash, hypotension, palpitations, renal
i. ACE inhibitors: Captopril, damage in patients with preexisting renal vascular disease but is slows down the progression of DM nephropathy and cardiac
Enalapril, Lisinopril, Benazepril inhibit angiotensin converting enzyme ; for hypertension, heart failure protective for DM nephropathy ; CI in pregnancy remodelling in heart failure
ii. Angiotensin receptor blocker:
Losartan, Valsartan, Irbesartan, fatigue / weakness, hypoglycemia, anemia, diarrhea, cough, CI in
Candesartan competetively blocks Angiotensin 1 receptor site ; for hypertension pregnancy as effective as ACEi but less cough
diarrhea, cough, rash, hyperkalemia, increase in serum no reproductive toxicity but is also CI because of the toxicity of
iii. Renin inhibitor: Aliskerin inhibitor of renin's action on its substrate angiotensinogen creatinine, renal impairment, angioedema ACEi and ARBs
Vasodilators and anti-Angina Pectoris
A. Nitrates
i. Ultrashort-acting nitrate: Amyl releases nitric oxide (NO), relaxes smooth muscle, especially vascular,
Nitrite increases cGMP (cyclic guanosine monophosphate); for cyanide poisoning Reflex tachycardia, Orthostatic hypotension, methemoglobinemia inhalational route, but now rarely used
ii. Short-acting nitrate: Nitroglycerin, releases nitric oxide (NO), increases cGMP (cyclic guanosine Dangerous hypotension with PDE inhibitors such as Sildenafil ;
Isosorbide Dinitrate, Isosorbide monophosphate) and relaxes smooth muscle especially vascular; for Reflex tachycardia, orthostatic hypotension, headache, tolerance First Pass effect is ~90% (NTG), NTG also decrease platelet
Mononitrate Angina, acute coronary syndromes (transdermal) aggregation
B. Calcium Channel Blockers
i. Non-dihydropyridine calcium block voltage-gated L-type calcium channels (cardiac > vascular); for Constipation, Nausea, flushing,gingival hyperplasia, AV block,
channel blocker: Verapamil, Diltiazem Angina, Supraventricular tachycardia, migraine, hypertension sinus node depression, Pretibial edema, dizziness excessive cardiac depression may occur
ii. Dihydropyridine calcium channel
blocker: Nifedipine, Amlodipine,
Nicardipine, Nisoldipine, Isradipine, block voltage-gated L-type calcium channels (vascular > cardiac); for
Felodipine Angina, hypertension Nausea, Flushing, dizziness, pretibial edema, constipation greater vasodilator effect that cardiodepressant effect
Drugs used in Heart Failure
Other drugs for heart failure include Diuretics (Furosemide is the DOC for
acute heart failure), Angiotensin Antagonists (ACEi is the DOC for chronic
heart failure), Beta1 blockers (dopamine and dobutamine), Non-selective
Beta Blockers (Carvedilol, Labetalol, Metoprolol), PDEi (Inamrinone,
A. Cardiac Glycoside Milrinone), Vasodilators (Nitroprusside, Nitroglycerin)
inhibits Na/K ATPase; increases intracellular Ca, increasing cardiac Narrow therapeutic index, Arrhythmias, diarrhea, vomiting, visual Arrhythmogenesis increased by hypokalemia, hypercalcemia,
i. Digoxin contractility; for heart failure, Nodal arrythmias changes hypomagnesemia
Anti-Arrhythmics
A. Class 1 Antiarryhtmics
Use- and state-dependent block of INa channels; some block of Ik channels. Arrhythmias, lupus-like syndrome (procainamide), hypotension,
Slowed conduction velocity and pacemaker activity; prolonged action cinchonism (quinidine), thrombocytopenia (quinidine),
i. Class 1A: Procainamide, potential duration and refractory period; for atrial and ventricular arrhythmias antimuscarinic effect (disopyramide), quinidine reduces digoxin
Disopyramide, Quinidine, especially after myocardial infarction clearance Hyperkalemia exacerbates cardiac toxicity
highly selective use and state-dependent INa block; minimal effect in normal Hyperkalemia, exacerbates cardiac toxicity. Lidocaine is the least
tissue; no effect on IK; DOC for ventricular arrhythmia post-myocardial cardiotoxic among conventional anti-arrhythmics ; only affect
ii. Class 1B: Lidocaine, Mexiletene, infarction, Digoxin-induced arrhythmia ; Mexilitine can be used for CNS stimulation, Allergy, Arrhythmias, depression, ischemic tissue; lidocaine is never given P.O due to significant
Tocainide, Phenytoin neuropathic pain Agranulocytosis first pass effect
iii. Class 1C: Flecainide, Selective use and state-dependent block of INa; slowed conduction velocity hyperkalemia exacerbates cardiac toxicity contraindicated for
Propafenone, Encainide, Moricizine and pacemaker activity; for refractory arrhythmias Increased arrhythmias (proarrhythmic effect), CNS excitation post MI arrhythmias
B. Class 2 Antiarrythmics
Block of beta-receptors, decrease in cAMP results to decreased Na and Ca

current and suppression of cardiac pacemaker activity; for Post MI In CHF, reduces progression and decreases incidence of
prophylaxis against sudden death, thyrotoxicosis, acute perioperative and potentially fatal arrhythmias. Sotalol is a beta-blocker anti
i. Propranolol, Esmolol thyrotoxic arrhythmias, Supraventricular tachycardia Bronchospasm, AV block, Hypotension, Cardiac depression arrhythmic that has class 3 properties
C. Class 3 Arrhythmics Group with the greatest risk for TDP

Selective Ik block ; prolonged action potential and QT interval; for treatment
i. Dofetilide, Ibutilide, and prophylaxis of atrial fibrillation Torsade de pointes NONE
Ik block and beta-adrenoceptor block; for ventricular arrhythmias, Dose-related torsade de pointes, excessive beta-blockade (sinus
ii. Sotalol Supraventricular tachycardia, Atrial fibrillation bradycardia, asthma) NONE
Strong Ik block produces marked prolongation of action potential and
refractory period. Group 1 activity slows conduction velocity; groups 2 and 4 Microcrystalline deposits in cornea and skin, paresthesias, Amiodarone has Class 1, 2 3 and 4 activity therefore is the
activity confer additional anti arrhythmic activity; for refractory arrhythmia, Pulmonary fibrosis, Tremor, Thyroid dysfunction (hyper- or hypo- MOST EFFICACIOUS of all anti-arrhythmics, amiodarone has
iii. Amiodarone, Dronedarone used off label in many arrhythmia ) longest among all anti-arrhythmics (1-10 weeks)
D. Class 4 Antiarrythmatics
Block voltage-gated L-type calcium channels (cardiac >vascular), decreased Constipation, Pretibial edema, Nausea, Flushing, Gingival
i. Non-dihydropyridine calcium AV conduction velocity ; for Angina, Hypertension, Supraventricular hyperplasia, heart failure, AV block, dizziness, sinus node
channel blocker: Verapamil, Diltiazem tachycardia, migraine, Raynaud's Phenomenon, Vasospasm depression should be avoided in Ventricular tachycardia
E.Miscellaneous Antiarrythmics
Increase in diastolic Ik of AV node that causes marked hyperpolarization and
conduction block; reduced ICa; For AV nodal arrhythmias, DOC for DOC for paroxysmal supraventricular tachycardia, Duration of
i. Adenosine paroxysmal supraventricular tachycardia Flushing, Transient chest pain, Dyspnea, Hypotension action is only 15sec
Diuretics
A. Carbonic Anhydrase Inhibitors
i. Acetazolamide, Dorzolamide, Inhibits carbonic anhydrase. In proximal tubule, In glaucoma, secretion of Drowsiness, Sulfa Allergy, Renal calcium stones, Paresthesias,
Brinzolamide, Dichlorphenamide, aqueous humor is reduced and in mountain sickness, metabolic acidosis hyperchloremic metabolic acidosis, hepatic encephalopathy in
Methanolamide increases respiration; for glaucoma, diuresis for edema with alkalosis. cirrhotic patients, potassium wasting diuresis is self-limiting after 2-3 days
B. Loop Diuretic
Inhibit Na/K/2Cl transporter in thick ascending limb of loop of Henle, Cause
powerful diuresis and increased Ca excretion; for Heart failure, Hypokalemic metabolic alkasis, dehydration, Ototoxicity, Synergistic ototoxicity with aminoglycosides. Efficacy decreased
i.Furosemide, Bumetanide, Hypertension, Pulmonary Edema, Hypercalcemia, Acute renal failure, Anion Potassium wasting, Sulfa allergy, Hyperuricemia, Hypocalcemia, by NSAIDs ; causes hypocalcemia in contrast with thiazide
Torsemide overdose Hypomagnesemia, Nephritis diuretics which cause hypercalcemia
C. Thiazide Diuretics
i. Hydrochlorothiazide, Inhibit Na/Cl transporter in distal convolutes tubes. Causes moderate Hypokalemic metabolic alkalosis, Potassium wasting, dilutional Synergistic effect with loop diurectics. Efficacy decreased by
Chlorthalidone, Indapamide, diuresis and reduced excretion of calcium; For hypertension Hypercalciuria, hyponatremia, Hyperglycemia, hyperuricemia, sulfa allergy, NSAIDs ; causes hypercalcemia in contrast with loop diuretics
Metolazone Heart failure, Nephrogenic diabetes insipidius, renal calcium stones hyperlipidemia which cause hypocalcemia
D. Potassium-Sparing Diuretics
Steroid inhibitors of cytoplasmic aldosterone receptor in cortical collecting Hyperkalemia, impotence, Benign prostatic hyperplasia,
i. Spironolactone, Eplerenone ducts. Reduce K excretion; for Hyperaldosteronism, Heart failure, Hyperchloremic metabolic acidosis, anti-androgenic effect Eplerenone reduces progression of DM nephropathy and
(Aldosterone Antagonist) Hypokalemia, Hypertension (Spironolactione) reduces mortality post MI
Hyperkalemia, kidney stones, metabolic acidosis, Acute renal
ii. Amiloride, Triamterene (Na Inhibitor of ENaC (Epithelial sodium channels) in cortical collecting duct, failure (with indomethacin), should never be given with potassium
channel Blocker) reduces Na reabsorption and K excretion; for hypokalemia supplements should never be given with potassium supplements
E. Osmotic Diuretics
Osmotically retains water in tubule by reducing reabsorption in proximal
tubule, descending limb of Henle's loop, and collecting ducts; in the Transient volume expansion (hyponatremia, pulmonary edema;
i. Mannitol, Glycerin, Isosorbide, periphery, mannitol extracts water from cells; for Rhabdomyolysis, followed by hypernatremia) nausea, headache, dehydration,
Urea Hemolysis, Increased intracranial pressure, Acute glaucoma vomiting used to maintain high urine flow
F. ADH Agonists/ Antagonists
Agonists at V1 and V2 ADH receptors. Activate insertion of aquaporin water

i. Antidiuretic hormone, channels in collecting tubule. Vasoconstriction; For central diabetes Increases the factor VIII activity of patients with mild hemophilia
Desmopressin, Vasopressin insipidus, hemophilia, Nocturnal enuresis, von Willebrand's disease Hypertension, Hyponatremia A or von Willebrand disease
G. ADH Antagonists: Conivaptan, Infusion site reactions, hyperkalemia, Nephrogenic diabetes

Tolvaptan, Lixivaptan, insipidus, Bone and Teeth abnormalities(demeclocycline), Renal Central Pontine Myelinosis may occur with rapid correction of
Demeclocycline, Lithium Antagonist at V1, V2 receptors; for SIADH and Hyponatremia failure (Lithium, demeclocycline) hyponatremia
3. DRUGS WITH IMPORTANT ACTION ON SMOOTH MUSCLES

Histamine, Serotonin and the Ergot Alkaloids
Possess antimuscarinic, adrenaline-antagonising, serotonin
diminish or abolish the major actions of histamine in the body by competitive, antagonising, and local anaesthetic effects. Some have calcium-
reversible blockade of histamine H1-receptor sites on tissues ; used channel blocking activity ; Sedating antihistamines may enhance
primarily for the alleviation of conditions such as urticarial rashes and nasal the sedative effects of CNS depressants including alcohol,
allergy that are characterised by type I hypersensitivity ; are of value in barbiturates, hypnotics, opioid analgesics, anxiolytic sedatives,
preventing urticaria and are used to treat urticarial rashes and mild Sedation, should not be given to neonates because they are and antipsychotics ; all are PO but can be given topical (nose
A. H1 antagonists angioedema more susceptible to antimuscarinic effects and eyes) ; negligible effect on H2 receptors
more likely to block autonomic receptors, also has alpha1

Reversible blockade of histamine H1-receptor sites on tissues ; anti-nausea blocking and local anesthetic effect ; Cyclizine (more anti-motion
i. 1st Generation: Diphenhydramine, and antiparkinsonism effect, for allergic reactions, for sedation and motion sickness action less sedative and and autonomic effects);
Dimenhydrinate, Chlorpheniramine, sickness (Diphenhydramine Dimenhydrinate, Cyclizine, Meclizine, Anticholinergic effects, orthostatic hypotension (promethazine), Promethazine (less anti-motion sickness, more sedative and
Meclizine, Promethazine Promethazine), for chemotherapy-induced vomiting (Diphenhydramine) sedation autonomic effects ; Usual half-life: 4-12h
ii. 2nd Generation: Loratadine, headache, dry mouth, hyperkinesia, malaise, may cause
Desloratadine, Cetirizine, Reversible blockade of histamine H1-receptor sites on tissues ; for allergic arrhythmia due to blockade of cardiac potassium channels
Levocertirizine, Fexofenadine reactions (acrivastine, astemizole, cetirizine, loratadine, and terfenadine) No sedation and antimuscarinic effects ; usual half-life: 12-24h
B. H2 antagonists No blocking action on H1 receptor
Surmountable competitive pharmacologic block of H2 receptors, reduction of

i. Cimetidine, Ranitidine, nocturnal acid secretion in gastirc and duodenal ulcer, accelerate healing CYP450 inhibitor, antiandrogen effects, decreased hepatic blood used in the ICU setting to prevent gastric erosion and
Famotidine, Nizatidine and prevent recurrences ; for PUD, GERD and ZES flow (cimetidine), weak enzyme inhibitory effect (Ranitidine) hemorrhage ; usual half-life: 1-3h
C. Serotonin Agonists
i. 5HT1D receptor agonist:
Sumatriptan, Naratriptan, Almotriptan, all are per orem only except for Sumatriptan which can also be
Eletriptan, Frovatriptan, Rizatriptan, Agonist at the 5HT1D receptor in the blood vessels causing vasocontriction ; Injection site reaction, paresthesia, dizziness, warm/hot given intranasally, transdermal and IV ; All has 2-27hrs DOA exc
Zolmitriptan 1st line treatment for Acute migraine and cluster headache attacks sensation, chest pain, coronary vasospasm for sumatriptan DOA: 2-4h
D. Serotonin Antagonists
i. 5HT3 receptor antagonist:
Ondansetron, Granisetron, Selectively block 5HT3 receptors ; For antiemesis in patients post- Dolasetron can increase QRS and QT (proarrhythmic effect)
Dolasetron, Alosetron chemotherapy or post-operation Constipation, headache, malaise duration so never use in patients with heart disease
most are partial agonists at alpha receptors and 5HT receptors but some are
E. Ergot Alkaloids potent agonist at dopamine receptors
gangrene (secondary to ischemia) in overdose, unusual
hyperplasia of the retroperitoneal, retropleural or subendocardial can cause epinephrine reversal due to partial agonist effect on
Mixed partial agonist effects at 5-HT2 and a-adrenoceptors, causes cavity --> hydronephrosis, cardiac valvular and conduction alpha receptors (REMEMBER: All partial agonist will act as
i. Vasoselective: Ergotamine vasoconstriction; For Migraine attacks (but 5HT1D are preferred) system malfunction antagonist in the present of a full agonist)
uterus becomes more sensitive to ergots during pregnancy,

Mixed partial agonist effects at 5-HT2 and a-adrenoceptors, causes produce very powerful and long-lasting contraction leading to
ii. Uteroselective: Ergonovine vasoconstriction; For control of post-partum bleeding marked uterine contraction, GI upset (nausea, vomiting, diarrhea) decreased bleeding, Never give before delivery of placenta
The Eicosanoids: Prostaglandins, Thromoboxanes, Leukotrienes and related compounds

A. Prostaglandin E1 analog
PGE1 analogue, activated EP receptor, causes increased HCO3 and
mucus secretion in stomach and uterine contraction; For prevention of Misoprostol's intended use is for NSAID-induced gastritis, may
ulcer in patients who take high doses of NSAIDs due to arthritis, also be used together with Mifepristone or Methotrexate as safe
i. Misoprostol, Gemeprost abortifacient Abdominal pain, Uterine cramping, teratogen, miscarriage abortifacient
PGE1 analogue, causes vascular smooth muscle relaxation and
vasolidation; For Maintenance of patent ductus arteriosus (PDA),
ii. Alprostadil Erectile dysfunction Apnea, hypotension, priapism, lightheadedness, arrhythmia given as injection into the cavernosa for erectile dysfunction
B. Prostaglandin E2 analog
Low concentrations contract, higher concentrations relax uterine and
cervical smooth muscle, soften cervix at term before induction with approved abortifacient in the 2nd trimester, although effective in
i. Dinoprostone, Sulprostone oxytocin; For cervical ripening, induction of labor, abortifacient Cramping, Fetal trauma inducing labor, it produces more SE than other oxytocics
C. Prostaglandin F2a analog
i. Latanoprost, Arboprost,
Bimatoprost, Travoprost, PGF2a analogue, increases outflow of aqueous humor thus reduces Latanoprost may cause changes in the color of the iris and may
Unoprostone intraocular pressure; For glaucoma vomiting, diarrhea, transient bronchoconstriction lengthen eyelashes
D. Prostaglandin I2 analog
PGI2 analogue, activates IP receptor, causes vasolidation and reduces
i. Epoprostenol, Beraprost, Iloprost, platelet aggregation; For severe pulmonary Hypertension and reducing
Treprostinil platelet aggregation in dialysis machines Hypotension, headache, flusing used primarily for pulmonary hypertension (esp Treprostinil IV)
E. Leukotriene antagonists
i. Lipoxygenase inhibitor: Zileuton see entry on Drugs used for Asthma
ii. LT receptor blocker: Montelukast,
Zafirlukast see entry on Drugs used for Asthma
F. Corticosteroids see entry on Drugs used for Asthma
G. Non-steroidal anti-inflammatory
drugs see entry on Analgesics
Drugs used in Asthma
A. Beta2-selective agonist
(shortacting)
i. Albuterol/Salbutamol, Increase toxicity when used for COPD (May precipitate
Levalbuterol, Terbutaline, arrythmias) and in patients with heart disease; usual DOA: 2-
Metaproterenol, Pirbuterol, Activates beta2-receptors in bronchial smooth muscle leading to Tachycardia, Nervousness, tremors, restlessness, arrhythmias when 4hrs, all are given inhalational, Salbutamol and terbutaline is also
Procaterol, Fenoterol bronchodilation ; DOC for acute asthma attacks used excessively, loss of responsiveness (tolerance, tachyphylaxis) available PO, terbutaline can also be given IV
B. Beta2-selective agonist (long
acting)
Activates beta2-receptors in bronchial smooth muscle leading to
ii. Salmeterol, Formoterol, bronchodilation, potentiates corticosteroid action; For Asthma Tachycardia, Nervousness, tremors, restlessness, arrhythmia when Increase asthma mortality when used alone; May precipitate
Cleneterol, Bambuterol prophylaxis used excessively, loss of responsiveness (tolerance, tachyphylaxis) arrhythmias; usual DOA: 12hrs
C. Muscarinic receptor agonist
More effective and less toxic than beta agonists for COPD,
Blocks muscarinic receptors in bronchial smooth muscle and prevent Tiotropium has longer DOA than Ipratropium, Ipratropium given
bronchoconstriction mediated by vagal discharge; For acute BA attack as aerosol has little systemic effects, has no effect on the chronic
i. Ipratropium, Tiotropium and COPD anti-muscarinic effects (dry mouth, blurred vision etc.) inflammation aspect of BA
C. Methylxanthine
Phosphodiesterase inhibitor, Adenosine receptor antagonist, causes
bronchodilation and increased strength of contraction of diaphragm; For
i. Theophylline, Aminophylline, asthma especially in nocturnal attacks, Intermittent claudication CNS stimulation (Insomnia, seizure, Anorexia), Cardiac stimulation Antidote in overdosage is BB. Higher clearance in adolescents
Pentoxifylline (pentoxifylline), very useful in COPD (Arrhythmias), Tremors, increased BP, diuresis, inc GI motility and smokers. Narrow therapeutic window; usual DOA: 12hrs
D. Mast cell Stabilizer
Prevents calcium influx and stabilizes mast cells, preventing No bronchodilator action but can prevent bronchoconstriction
i. Cromolyn, Nedocromil, degranulation and release of histamine, leukotrienes and mediators; for caused by antigens (both in the early and late BA responses),
Lodoxamide Asthma prophylaxis and allergies (oral, nasal and ophthalmic drops) Cough, Airway irritation unusually insoluble chemicals so rarely used
E. Corticosteroid
Inhibit synthesis of arachidonic acid by inhibiting Phospholipase A2,
Reduces expression of COX and LT, inc responsiveness of Beta
receptors in the airway, bind to intracellular receptors and activate
Glucocorticoid response elements in the nucleus leading to synthesis of
substances that prevent full expression of inflammation and allergy ;
i. Fluticasone, Beclomethasone, DOC for Asthma prophylaxis, First line treatment for moderate to
Budesonide, Flunisolide, severe BA, COPD, Allergic rhinitis, also used as anti-inflammatory for Oropharyngeal candidiasis, mild growth retardation observed in
Mometasone, Triamcinolone, other conditions such as auto-immune diseases and cancer, also for children, Minimal systemic steroid steroid toxicity (eg, adrenal For status asthmaticus: use IV prednisolone or hydrocortisone ;
Ciclosenide immune suppression suppression), Mild growth retardation prednisolone is the active metabolite of prednisone
F. Leukotriene synthesis inhibitor
Inhibitor of 5-lipoxygenase. Reduces synthesis of leukotrienes.
Prevents airway inflammation and bronchoconstriction; For asthma Flulike syndrome, headache, drowsiness, dyspepsia, hepatitis,
i. Zileuton prophylaxis elevation of liver enzymes (more than LT receptor blockers) No bronchodilator action, not recommended for acute BA attack
G. Leukotriene Antagonist
i. Montelukast, Zafirlukast, Blocks leukotriene-1 receptor, prevents airway inflammation and
Pranlukast bronchoconstriction; For asthma prophylaxis Gastrointestinal upset, Insomnia, elevation of liver enzymes No bronchodilator action, not recommended for acute BA attack
H. Anti-IgE antibody
Binds IgE antibodies on sensitized mast cells and prevents activation
by BA triggers and subsequent release of inflammatory mediators; For
prophylaxis of severe, refractory asthma not responsive to all other humanized murine monoclonal antibody, very expensive and
i. Omalizumab drugs Long term toxicity not yet well documented only administered IV
4. DRUGS THAT ACT ON THE CENTRAL NERVOUS SYSTEM

Sedative-Hypnotics
A. Short-acting benzodiazepines
bind GABA-A receptor subunits to increase frequency of chloride
channel opening which causes membrane hyperpolarization ; For acute causes anterograde amnesia, decreased psychomotor skills, additive CNS depression if used with ethanol, antihistamines,
i. Midazolam, brotizolam, triazolam, anxiety, panic attacks, anesthesia induction and preoperative sedation unwanted daytime sedation, tolerance, dependence liability and antipsychotics, opioids and TCAs, decreased REM sleep, use
oxazepam, etizolam (esp Midazolam), insomnia (Triazolam) rebound insomnia or anxiety. lower doses in the elderly when used for insomnia
B. Intermediate-acting
benzodiazepines
bind GABA-A receptor subunits to increase frequency of chloride additive CNS depression if used with ethanol etc, decreased
channel opening which causes membrane hyperpolarization; For REM sleep, High dose BZD and Barbs may suppress seizure but
i. Lorazepam, Alprazolam, anxiety disorders even panic disorders (Alprazolam and Clonazepam), at the expenses of marked sedation EXCEPT Clonazepam and
Estazolam, Clonazepam, insomnia (Estazolam), skeletal muscle relaxation, seizure disorders causes anterograde amnesia, decreased psychomotor skills, Phenobarbital, Lorazepam is preferred over Diazepam in Status
Lormetazepam, Nitrazepam, (Clonazepam), status epilepticus (Lorazepam), tranquilizers, Bipolar unwanted daytime sedation, tolerance, dependence liability and Epilepticus due to its long distribution halflife, use lower doses in
Temazepam disorder (Clonazepam), infantile spasm (Clonazepam) unwanted daytime sedation. the elderly when used for insomnia
C. Long-acting Benzodiazepine
bind GABA-A receptor subunits to increase frequency of chloride
channel opening which causes membrane hyperpolarization; For
anxiety disorders, insomnia (Flurazepam), skeletal muscle relaxation
i. Diazepam, chlorazepate, (e.g. cerebral palsy - Diazepam), seizure disorders, tranquilizers, for causes anterograde amnesia, decreased psychomotor skills (esp additive CNS depression if used with ethanol etc., decreased
chlordiazepoxide, flurazepam, status epilepticus (Diazepam), anesthesia (Diazepam), alcohol Diazepam and Flurazepam), unwanted daytime sedation, tolerance, REM sleep, Flunitrazepam is used as a date-rape drug, use
quazepam, flunitrazepam withdrawal (Diazepam and Chlordiazepoxide) dependence liability and rebound insomnia or anxiety. lower doses in the elderly when used for insomnia
D. Benzodiazepine antagonist
antagonist at benzodiazepine sites on GABA-A receptor ; for agitation, confusion, and precipitates benzodiazepine withdrawal Seizures and arrhythmias may occur when administered in
i. Flumazenil benzodiazepine overdose. syndrome for those with benzodiazepine dependence. patients who took both TCAs and benzodiazepines
E. Ultrashort-acting barbiturates
bind to GABA-A receptor sites (distinct from benzodiazepines) to
increase duration of chloride channel opening, block glutamic acid
i. Thiopental, Methohexital, neurotransmission, at high doses can block NA channels ; For dependence liability is greater than benzodiazepine, acute intermittent additive CNS depression if used with ethanol etc., CYP450
Thiamylal anesthesia induction (esp Thiopental) porphyria. inducer, Thiopental has highest lipid solubility
F. Short and intermediate-acting
barbiturates
increase duration of chloride channel opening, block glutamic acid
i. Pentobarbital, secobarbital, neurotransmission, at high doses can block Na channels ; For insomnia
amobarbital, butalbital, butabarbital, and preoperative sedation (Secobarbital), for status epilepticus dependence liability is greater than benzodiazepine, acute intermittent additive CNS depression if used with ethanol etc., CYP450
talbutal, aprobarbital (Phenobarbital) porphyria. inducer
G. Long-acting barbiturate
increase duration of chloride channel opening, block glutamic acid additive CNS depression if used with ethanol, CYP450 inducer,
neurotransmission, at high doses can block Na channels ; For Phenobarbital may be excreted unchanged in the urine, High
i. Phenobarbital, mephobarbital, insomnia, seizure disorders (Phenobarbital), status epilepticus dependence liability is greater than benzodiazepine, acute intermittent dose BZD and Barbs may suppress seizure but at the expenses
primidone (Phenobarbital) porphyria, severe respiratory and cardiovascular depression of marked sedation EXCEPT Clonazepam and Phenobarbital
H. Imidazopyridine sedative-hypnotics
lack anti-convulsant, anti-anxiety and muscle relaxant effects,
effects are reversed with Flumazenil, very rapid onset of action,
bind selectively to a subgroup of GABA-A receptors, acting like may dec. REM sleep, rebound inc on withdrawal from chronic
benzodiazepines to enhance membrane hyperpolarization, only interact day-after psychomotor depression, few amnestic effects; tolerance, use, increasing use due to rapid onset with minimal effects on
with GABA-A receptors with alpha-1 subunit ; For insomnia and sleep dependence liability and withdrawal symptoms is less than that of the sleep pattern and cause less daytime cognitive impairment
i. Zolpidem, Zaleplon, Eszopiclone disorder esp. when sleep onset is delayed benzodiazepines as compared to BZD
I. Atypical Sedative-Hypnotics
minimal abuse liability, minimal CNS depressant effects,
non-specific chest pain, tachycardia, palpitations, dizziness, tolerance and withdrawal ; no anticonvulsant or muscle relaxant
i. Partial Serotonin Agonist: partial agonist at 5-HT1A receptors and possibly D2 receptors, precise nervousness, tinnitus, GI distress, paresthesias, dose-dependent property ; slow onset of action (>1week), metabolized by
Buspirone MOA of anxiolytic effect is unkown ; For generalized anxiety disorders pupillary constriction CYP3A4, safe for pregnant patients
minimal rebound insomnia or withdrawal symptoms, minimal
ii. Melatonin receptor agonist: activates melatonin receptors (MT1 and MT2 receptors) in the abuse liability, metabolized by CYP450 (increased levels in the
Ramelteon suprachiasmatic nuclei in the CNS --> decreased latency of sleep onset Dizziness, fatigue, decreased testosterone, increased prolactin presence of CYP1A2 or CYP2D6 inhibitors
Antiseizure Drugs
CYP450 inducer , metabolism is non-linear (elimination shift from

1st order to zero order at moderate to high dose levels) ,
block voltage-gated Na channel ; DOC for generalized tonic-clonic nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, Fosphenytion is a water-soluble prodrug of phenytoin ; phenytoin
i. Phenytoin, Fosyphenytoin, seizures, DOC for partial seizures, status epilepticus, arrhythmias, anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal is preferred in prolonged therapy for status epilepticus because it
Mephenytoin, Ethotoin migraine hydantoin syndrome, abnormalities in Vit D metabolism is less sedating.
CYP450 inducer, Oxcarbazepine has less drug interactions,
block voltage-gated Na channels and decreases glutamate release ; diplopia, cognitive dysfunction, drowsiness, ataxia, blood dyscrasias, metabolism may be inhibited by other drugs such as
DOC for trigeminal neuralgia, DOC for generalized tonic-clonic Stevens-Johnson syndrome, erythematous rash, teratogen (spina Propoxyphene and valproic acid ; may be used for acute manic
ii. Carbamazepine, Oxcarbazepine seizures, DOC for partial seizures, for bipolar disorders bifida and craniofacial anomalies), hyponatremia (Oxcarbazepine) phase and as prophylaxis in the depressive phase
blocks high-frequency firing of neurons which modifies amino acid CYP450 inhibitor ; also have the same effect on Ca currents like
metabolism ; DOC for bipolar disorder (acute mania), DOC for Ethosuximide ; Other MOA include enhancing K channel
generalized tonic-clonic seizures and absence seizure, partial seizures, drowsiness, nausea, tremor, alopecia, weight gain, hepatotoxicity (esp permeability ; BZDs are commonly required at initiation therapy
iii. Valproic acid myoclonic seizures, also used for Bipolar disorders in infants), neural tube defects of valproic acid ; DOC for acute manic illness
May also act on Na channels and as antagonist at some
glutamate receptors ; primary anticonvulsant in infants, children
iv. Phenobarbital see notes above ; For status epilepticus in children cognitive dysfunction, dependence and pregnant patients
v. Ethosuximide, Phensuximide, inhibit low threshold (T-type) Ca currents esp in thalamic neurons ;
Methsuximide DOC for absence seizure GI distress, lethargy, headache and behavioural changes. Long half-life
vi. Diazepam see entry on Sedative-Hypnotics
eliminated in the kidneys in their unchanged form ; structural
blocks Ca++ channels, increases GABA release ; For neuropathic pain analogues of GABA but does not activate GABA receptor directly
vii. Gabapentin, Pregabalin such as postherpetic neuralgia, partial seizures, migraine dizziness, sedation, ataxia, nystagmus, tremor ; also have the same effect on Ca currents like Ethosuximide
blocks Na and Ca++ channels and decreases glutamate , Zonisamide
only blocks Na channels ; For generalized tonic-clonic seizures, DOC primarily undergoes glucuronidation reaction ; Lamotrigine may
for partial seizures, myoclonic seizures, absence seizures, bipolar dizziness, ataxia, nausea, rash, SJS / TEN (lamotrigine), severe skin be used for acute manic phase and as prophylaxis in the
viii. Lamotrigine, Zonisamide disorder. reaction (Zonisamide) depressive phase
Bind synaptic protein selectively inhibiting hypersynchronization of
epileptiform burst firing ; For generalized tonic-clonic seizures, partial It is not metabolized by CYP450 enzymes, eliminated in the
ix. Levetiracetam seizures dizziness, sedation, weakness, irritability, hallucinations, psychosis kidneys in their unchanged form
multiple actions on synaptic function, probably via actions on
phosphorylation (Na, Ca, GABA, AMPA-glutamate, carbonic
anhydrase), Felbamate also facilitate the inhibitory actions of GABA but drowsiness, dizziness, ataxia, psychomotor slowing, memory Antiseizure drugs with the most number of MOA, undergo both
its exact MOA is still unknown ; For generalized tonic-clonic seizures, impairment, paresthesias, weight loss, acute myopia, glaucoma, hepatic and renal metabolism, Topiramate can also block Na
partial seizures, absence seizures, migraine ; Felbamate is only for myopia, urolithiasis ; felbamate causes hepatic failure and channels and potentitae action of GABA and block glutamate
x. Topiramate, Felbamate severe refractory seizure states hematotoxic (can cause ITP, aplastic anemia) receptor, Felbamate may also block glutamate receptors
Irreversibly inactivates GABA aminotransaminase (GABA-T) which
xi. Vigabatrin terminates the action of GABA ; For GTC seizure visual field defects None
Inhibits GABA transporter (GAT-1) in neurons and glia thus inhibiting its
xii. Tiagabine reuptake, leading to prolongation of GABA effects ; For partial seizures asthenia or weakness, dizzines None
General Anesthetics
A. Inhalational General Anesthetics This group in general increase the threshold for firing of CNS neurons
Lowest Potency (highest MAC) and least cardiotoxic; additive
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N megaloblastic anemia on prolonged exposure; Euphoria (laughing CNS depression with many agents especially opioids and
i. Nitrous Oxide receptors; used as anesthesia for minor surgery and dental procedures gas), bronchodilation sedative-hypnotics
additive CNS depression with many agents especially opioids
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N and sedative-hypnotics ; all inhaled anesthetcis cause
ii. Desflurane receptors ; For general anesthesia bronchospasm, peripheral vasodilation bronchodilation except Desflurane
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N peripheral vasodilation, renal insufficiency (due to Flourine release), additive CNS depression with many agents especially opioids
iii. Sevoflurane receptors; For general anesthesia bronchodilation and sedative-hypnotics
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N catecholamine-induced arrhythmias, peripheral vasodilation, additive CNS depression with many agents especially opioids
iv. Isoflurane receptors ; For general anesthesia bronchodilation and sedative-hypnotics
spike-and-wave activity in EEG, muscle twitching, breath-holding,
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N myocardial depression, renal insufficiency (due to Flourine release), additive CNS depression with many agents especially opioids
v. Enflurane receptors ; For general anesthesia dec cardiac output, bronchodilation and sedative-hypnotics ; has pungent odor which limits its use
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N catecholamine-induced arrhythmias, myocardial depression, post- additive CNS depression with many agents especially opioids
vi. Halothane receptors ; For general anesthesia operative hepatitis, dec cardiac output, bronchodilation and sedative-hypnotics
Highest potency and lowest MAC (very slow onset and recovery);
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N additive CNS depression with many agents especially opioids
vii. Methoxyflurane receptors ; For general anesthesia renal insufficiency (due to Flourine release), bronchodilation and sedative-hypnotics
B. Intravenous General Anesthetics
i. Barbiturates: Thiopental, are respiratory and circulatory depressants --> dec cerebral blood flow
Methohexital, Thiamylal see notes above --> dec ICP rapid entry into the brain (<1min)
ii. Benzodiazepine: Midazolam,
Brotizolam, Triazolam, Oxazepam, Midazolam is a usual adjunct with inhalational anesthetics and IV
Etizolam see notes above see notes above opioids, has a slow onset but longer DOA
Blocks excitation by glutamate at NMDA receptors; For dissociative
iii. Phencyclidine derivative: anesthesia (analgesia, amnesia and catatonia but with retained CV stimulation, hypertension, increased ICP, delirium, Dissociative Reduces delirium by pretreatment with benzodiazepine,
Ketamine consciousness) anesthesia, post-op effects: disorientation, hallucination, excitation congener of Phencyclidine / angel dust
Modulates GABA-A receptors containing beta3 subunits; For general pain at injection site, myoclonus, postoperative nausea and vomiting, Minimal effects on CV and respiratory functions, no analgesic
iv. Imidazole derivative: Etomidate anesthesia to patients with limited cardiac or respiratory reserve adrenocortical suppression (on prolonged administration) properties, short DOA
Antidote is Naloxone / Naltrexone ; Neuroleptanesthesia

Interacts with mu, sigma, kappa receptors for endogenous opioid (analgesia + amnesia) happens when Fentanyl, Droperidol and
v. Opioid analgesics: Fentanyl, peptides ; For high risk patients who might not survive general respiratory depression, chest wall rigidity (which may cause impaired Nitrous oxide are given together ; faster recovery with
morphine, alfentanil, remifentanil anesthesia ventilation) and constipation remifentanil ; these drugs have fast onset of action
"milk of anesthesia", additive effects with sedative-hypnotic drugs

bradycardia, vasodilation, hypotension, negative inotropism, pain at ; as rapid as thiopental and also with fast recovery ; antiemetic
Potentiates GABA-A receptors, blocks Na channels; For prolonged injection site, anterograde amnesia, dystonia, priapism, paresthesia action ; Fospropofol is the water-soluble prodrug form of propofol
vi. Propofol, Fospropofol sedation esp in ICU patients and also in OPD surgeries (Fospropofol) but with slower onset and recovery
Local Anesthetics
A. Ester Local Anesthetics this group can cause antibody formation in some patients
Blockade of Na channels slows which prevents axon potential light-headedness, sedation, restlessness, nystagmus, seizures,
i. Procaine propagation; For local anesthesia respiratory, CV depression Shortest half-life among local anesthetics
ii. Benzocaine propagation; For local anesthesia, topical anesthesia respiratory, CV depression Use cautiously in sunburns, Topical only
with intrinsic sympathomimetic activity so it does not need an
Blockade of Na channels slows which prevents axon potential light-headedness, sedation, restlessness, nystagmus, seizures, alpha agonist (like epinephrine) to limit its systemic absorption;
propagation, with intrinsic sympathomimetic activity; For local respiratory, CV depression, abuse liability, severe hypertension, causes mood elevation due to action on dopamine receptor ; All
iii. Cocaine anesthesia, topical anesthesia cerebral hemorrhage, cardiac arrhythmia, MI local anesthetics are vasodilators EXCEPT cocaine ; Topical only
Blockade of Na channels slows which prevents axon potential

propagation; For local anesthesia, spinal anesthesia, epidural light-headedness, sedation, restlessness, nystagmus, seizures,
iv. Tetracaine anesthesia, topical ophthalmic anesthesia respiratory, CV depression also available as Ophthalmic solution
B. Amide Local Anesthetics
Blockade of Na channels slows which prevents axon potential
propagation; For local anesthesia, antiarrhythmia (group 1B activity), light-headedness, sedation, restlessness, nystagmus, seizures, Frequently administered with Epinephrine to avoid systemic
i. Lidocaine used for post-MI and for digitalis toxicity respiratory, CV depression absorption
ii. Prilocaine propagation; For local anesthesia, dental anesthesia respiratory, CV depression causes methemoglobinemia (antidote: methylene blue)
propagation; For local anesthesia, epidural anesthesia, intrathecal respiratory, CV depression, severe CV toxicity, hypotension and Use with caution in pregnant women and patients with cardiac
iii. Bupivacaine anesthesia arrhythmias disease (may cause heartblock, arrhyhtmia and hypotension)
iv. Ropivacaine propagation; For local anesthesia, epidural anesthesia respiratory, CV depression, cardiotoxicity Longest half-life among local anesthesia
Skeletal Muscle Relaxant
A. Depolarizing Neuromuscular
Blocker
Agonist at Ach-N receptors causing initial twitch then persistent muscle pain, hyperkalemia, increased intragastric pressure leading to
depolarization ; For skeletal muscle relaxation during intubation and regurgitation (aspiration), increased intraocular pressure, malignant Metabolized by pseudocholinesterase ; may cause malignant
i. Succinylcholine general anesthesia hyperthermia hyperthermia if given together with inhaled anesthetics
B. Non-Depolarizing Neuromuscular effects are easily reversed by giving AChE inhibitors such as
Blocker a common SE for this group is Histamine release Neostigmine
i. Mivacurium (short-acting: 10- Metabolized by pseudocholinesterase; reverse effects with
20mins DOA) respiratory paralysis, apnea, and moderate histamine release Neostigmine
Undergoes Hoffman elimination (rapid spontaneous breakdown);

respiratory paralysis, apnea, and moderate histamine release and reverse effects with Neostigmine ; converted to Laudanosine
ii. Atracurium (intermediate-acting) bronchospasm which can cause seizures
iii. Vecuronium (intermediate-acting) respiratory paralysis and apnea Undergoes elimination in bile; reverse effects with Neostigmine
reverse effects with Neostigmine; Suggamadex is a novel
iv. Rocuronium (intermediate- reversal agent for rocuronium; most rapid onset time (60-120
acting) Competitive antagonists at skeletal muscle nicotinic acetylcholine respiratory paralysis and apnea, hypersensitivity sec)
receptors; For skeletal muscle relaxation during intubation and general Relatively contraindicated in myocardial ischemia; reverse effects
v. Tubocurarine (long-acting) anesthesia respiratory paralysis, apnea, hypotension and recurarization with neostigmine
Competitive antagonists at skeletal muscle nicotinic acetylcholine
receptors; For skeletal muscle relaxation during intubation and general
vi. Pancuronium (long-acting) anesthesia, euthanasia, lethal injection, strychnine poisoning respiratory paralysis, apnea, tachycardia, hypertension, recurarization Reverse effects with Neostigmine, may cause heart block
Anti-Parkinsonism and other drugs for movement disorders
A. Dopamine Precursor
Contraindicated in patients with history of psychosis;
hypertensive crisis occurs when used with MAO inhibitors,
Levodopa is a dopamine precursor, carbidopa inhibits peripheral GI upset (emesis), dyskinesia (choreoathetosis), behavioural changes ameliorates signs of parkinsonism and decreases mortality rate ;
metabolism via dopa decarboxylase; Drug of choice for parkinson’s (anxiety, agitation, confusion, delusion), on-off phenomena, wearing- patient response decreases with time but is improved when given
i. Levodopa-carbidopa disease off phenomena, postural hypotension, tachycardia together with COMT inhibitors
B. Dopamine Agonist
anorexia, nausea, vomiting, dyskinesia, postural hypotension,
Partial agonist at dopamine D2 receptors in brain; For Parkinson’s behavioural changes, erythromelalgia (Bromocriptine), pulmonary
i. Bromocriptine, Pergolide disease which is levodopa intolerance, hyperprolactinemia infiltrate (Bromocriptine) Ergot alkaloids
Contraindicated for patients with active peptic ulcer disease,
psychotic illnesss or recent MI ; decrease dose in renal
Partial agonist at dopamine D3 receptors in brain, Roprinole is a D2 anorexia, nausea, vomiting, dyskinesia, postural hypotension, dysfunction ; Neuroprotective ; Ropirinole is metabolized by
ii. Pramipexole, Ropinirole agonist; For Parkinson’s disease behavioural changes (more prominent compared to levodopa) CYP1A2
Partial agonist at dopamine D3 receptors, antagonist at 5-HT and alpha
adrenoceptors; For off-periods of Parkinson’s disease, alcoholism,
iii. Apomorphine opiate addiction, erectile dysfunction, alzheimer’s disease severe nausea, dyskinesia, hypotension, drowsiness and sweating Premedicate with Trimethobenzamide to prevent severe nausea
C. MAO type B inhibitor
Selective inhibitors of MAO type B leading to decreased degradation of
dopamine, increases response to levodopa/carbidopa; Only as adjunct serotonin syndrome occurs when used with SSRI and Meperidine
to levodopa for parkinson’s disease but Rasigiline can be given alone ; Selegiline is hepatically metabolized into desmethyl selegiline
i. Selegiline, Rasagiline (more potent) insomnia, mood changes, dyskinesias, GI distress and hypotension (which is neuroprotective) and amphetamine
D. COMT inhibitor
Block L-dopa metabolism by inhibiting catechol-O-methyltransferase in dyskinesias, GI distress, postural hypotension, sleep disturbance,
periphery and CNS, prolongs response to levodopa; used in the orange discoloration of urine, hepatotoxicity (tolcapone only), Entacapone only acts in the periphery while Tolcapone acts both
i. Entacapone, Tolcapone wearing-off phenomena of parkinson’s disease, as adjuncts to levodopa neuroleptic malignant syndrome, rhabdomyolysis in the periphery and CNS.
E. Antiviral
enhances dopaminergic transmission by unknown mechanism, maybe behavioural changes (restlessness, agitation, insomnia, hallucination,
by influencing the synthesis, release or reuptake of dopamine; For psychosis), livedo reticularis, GI disturbances, urinary retention, May improve bradykinesia, rigidity and tremor ; has
i. Amantadine Parkinson’s disease and influenza postural hypotension, peripheral edema antimuscarinic action
F. Anticholinergic
Decrease the excitatory actions of cholinergic neurons on cells in the Exacerbate tardive dyskinesias that result from prolonged use of
i. Benztropine, Biperiden, striatum by blocking muscarinic receptors; as adjunct for parkinson’s drowsiness, inattention, confusion, delusions, hallucinations, atropine- antipsychotic drugs; improve tremor and rigidity with little effect
Trihexyphenidyl, Orphenadrine disease and extrapyramidal symptoms caused by antipsychotics like effects on bradykinesia
Antipsychotics and Lithium
A. Typical Antipsyhotics may also be used for pruritus and as sedatives has no effect on negative symptoms
extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia,

atropine-like effects, failure of ejaculation, postural hypotension,
Blocks D2 receptors >> 5-HT2 receptors; For schizophrenia and other marked sedation, corneal and lens deposits, neuroleptic malignant
i. Phenothiazine: Chlorpromazine psychotic disorders syndrome, contact dermatitis prototype of all typical antipsychotics
Thioridazine has the Strongest autonomic effects; only
ii. Other Phenothiazines: extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia, antipsychotic with fatal overdose ; Fluphenazine and
Thioridazine, Fluphenazine, atropine-like effects, failure of ejaculation, postural hypotension, Trifluoperazine have very significant parkinson-like effect ;
Perphenazine, Prochlorperazine, Blocks D2 receptors >> 5-HT2 receptors; For schizophrenia and other retinal deposits (thioridazine), cardiotoxicity (arrhythmias - Fluphenazine has less sedation compared to other anti-
Trifluoperazine psychotic disorders, antiemesis (prochlorperazine) thioridazine) psychotics
iii. Butyrophenol: Haloperidol, Blocks D2 receptors >> 5-HT2 receptors; For schizophrenia and other extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia, causes the most extrapyramidal symptoms of all typical anti-
Droperidol psychotic disorders, huntington’s disease and tourette’s syndrome neuroleptic malignant syndrome psychotics ; has the weakest autonomic effects
may be used for mania and psychotic symptoms in Alzheimer's
B. Atypical Antipsychotics dementia and Parkinsons disease cure both negative and positive symptoms
Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural Only antipsychotic that reduces the risk of suicide ; may be
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia (refractory, hypotension, weight gain, hyperglycemia, hyperlipidemia, myocarditis, effective for drug-resistant types ; weight gain, agranulocytosis,
i. Clozapine suicidal) and other psychotic disorders agranulocytosis, seizures, ileus, hypersalivation (sialorrhea) seizure and hyperglycemia is prominent
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, bipolar Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural
ii. Olanzapine disorders, anorexia nervosa and depression hypotension, weight gain, hyperglycemia, hyperlipidemia weight gain and hyperglycemia is prominent, safe in pregnancy
Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, bipolar hypotension, weight gain, somnolence, fatigue, sleep paralysis,
iii. Quetiapine disorders (manic) hypnagogic hallucinations, cataracts, priapism, QT prolongation (TDP) can cause TDP, safe in pregnancy
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, bipolar Extrapyramidal dysfunction (less), hyperprolactinemia (marked),
iv. Risperidone disorders, depression, intractable hiccups, tourette syndrome insomnia, photosensitivity Only antipsychotic approved for schizophrenia in the youth
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, bipolar Extrapyramidal dysfunction (less), postural hypotension, QT Increased mortality in elderly patients with dementia-related
v. Ziprasidone disorders (acute mania) prolongation (TDP) psychosis ; can cause TDP
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, bipolar Extrapyramidal dysfunction (less), GI upset, tremor, hypersensitivity
vi. Aripiprazole disorders, depression, autism, cocaine dependence (rare) Least sedating atypical antipsychotics
Uncertain MOA but the proposed MOA is by inhibiting the enzyme Tremor, sedation, ataxia, aphasia, thyroid enlargement, Contraindicated in sick sinus syndrome; treat overdose with
involved in the recycling of neuronal membrane phosphoinositides hypothyroidism, reversible nephrogenic diabetes insipidus, edema, hemodialysis ; high volume of distribution ; clinical benefit is seen
which causes depletion of phosphatidylinositol bisphosphate, thus acneiform skin eruption, leukocytosis, teratogen (ebstein’s anomaly), only after weeks of use ; antipsychotic agents or BZDs are
consequently decreasing IP3 and DAG --> decrease in bradycardia, some drugs (NSAIDs, ACEi, diuretis etc) can increase commonly required at initiation therapy of Li and valproic acid ;
neurotransmission ; For bipolar disorder, recurrent depression, Lithium toxicity while caffeine and theophylline can decrease its Contraindicated in lactation ; Natriuresis stimulates reflex
vii. Lithium (mood stabilizer) schizoaffective disorder toxicity increase in the reabsorption of Li and Na in the PCT
Antidepressants
A. Tricyclic Antidepressants
Additive depression of the CNS with other central depressants ;
Imipramine is metabolized to desipramine while amitriptyline is
Block NE and 5-HT transporters leading to potentiation of NT action at metabolized to nortriptyline ; longterm use may lead to down-
postsynaptic receptors; For MDD (most effective), bipolar disorder, excessive sedation, fatigue, confusion, sympathomimetic effects, regulation of Beta receptors leading to a decrease in BP and
i. Imipramine, Clomipramine, acute panic attacks, ADHD, chronic pain states, as sleeping aid, OCD atropine-like effects, orthostatic hypotension, cardiomyopathies, depression of cardiac conduction ; has significant muscarinic
Desipramine, Amitryptyline, (Clomipramine) ; this group is very useful for patients with psychomotor arrhythmias, tremors, paresthesias, weight gain ; 3Cs of overdose: receptor blocking effect esp Amitriptyline ; lower seizure
Nortryptiline retardation, sleep disturbance, poor appetite and weight loss Coma, Cardiotoxicity, Convulsions threshold ; may interfere with antihypertensive action of Clonidine
B. SSRI
Serotonin syndrome when used with MAOIs ; minimal inhibitory

Inhibits neuronal reuptake of serotonin by inhibiting Serotonin effect on cholinergic or adrenergic receptors ; lower seizure
i. Fluoxetine, Paroxetine, Transporter (SERT); DOC for OCD, for MDD, anxiety, panic attacks, nausea, vomiting, headache, anxiety, agitation, drowsiness, insomnia, threshold ; this group can decrease appetite leading to weight
Citalopram, Escitalopram, Sertraline, phobias, PTSD, GAD, bulimia, premenstrual dysphoric disorder, alcohol erectile dysfunction, EPS, QT prolongation (citalopram), withdrawal loss ; Increased risk for suicide in children and adolescents ;
Fluvoxamine dependence syndrome Fluoxetine, Fluvoxamine and Paroxetine are CYP450 inhibitors
C. SNRI
dizziness, insomnia, sedation, GI distress, hypertension (venlafaxine), venlafaxine has less affinity for NE transporter than
Inhibits neuronal reuptake of serotonin and norepinephrine by binding hepatotoxicity (duloxetine), withdrawal syndrome even in just one desvenlafaxine and duloxetine ; differ from TCA in lacking
i. Venlafaxine, Duloxetine, to transporters for both 5HT and NE; For MDD, fibromyalgia, missed dose, CNS stimulation (Venlafaxine), liver dysfunction blockade of H1, M and alpha receptors ; Increased risk for
Desvenlafaxine neuropathic pain, menopausal symptoms (Duloxetine) suicide in children and adolescents
D. Serotonin antagonist
May cause arrhythmias in px with pre-existing cardiac disease ;
short t1/2 so given BID to TID, has significant muscarinic
Blocks 5-HT2A receptors, weak inhibitor of NE and 5HT transporters; sedation, GI disturbance, orthostatic hypotension, priapism, receptor blocking effect esp Nefazodone ; CYP450 inhibitors ;
i. Trazodone, Nefazodone For MDD, as sleeping aid (trazodone) hyperprolactinemia, liver dysfunction (nefazodone) Trazodone also has significant alpha1 and H1 blocking effect
E. Tetracyclics Increased risk for suicide in children and adolescents
Strong norepinephrine reuptake inhibitor and weak serotonin reuptake autonomic effects, akathisia, parkinsonism (due to dopamine receptor Lowers seizure threshold, has significant muscarinic receptor
i. Amoxapine inhibitor, blocks dopamine D2 receptors; For MDD blockade), seizures, cardiotoxicity blocking effect
Increases amine release from nerve endings by antagonism of
presynaptic a2 adrenoceptors, also blocks serotonin 5-HT2A receptors; weight gain, marked sedation, dizziness, blurred vision and
ii. Mirtazapine For MDD, appetite stimulation, as sleeping aid nightmares has significant muscarinic receptor and alpha2 blocking effect
Inhibits neuronal reuptake of dopamine and norepinephrine, increase

dopamine and norepinephrine activity; For MDD and smoking weight loss, agitation, anxiety, dizziness, dry mouth, aggravation of Lowers seizure threshold, for smoking cessation ; no effect on
iii. Bupropion cessation, alcohol dependence psychosis, seizures, priapism 5HT or NE receptors or amine transporters ; CYP450 inhibitor
F. MAO Inhibitors
Hypertensive crisis when taken with tyramine-rich food, serotonin
Inhibits MAO type A and type B, increases CNS levels of NE and syndrome when taken with SSRI ; this group is structurally
serotonin, Phenelzine and Tranylcypromine are nonselective MAO related to amphetamine ; CYP450 inhibitors ; longterm use may
inhibitors while Selegiline is a MAO-B selective inhibitor; For MDD lead to down-regulation of Beta receptors (leading to decrase in
i. Phenelzine, tranylcypromine, unresponsive to other agents ; useful in patients with significant anxiety, dizziness, insomnia, orthostatic hypotension, blurred vision, BP) ; lower seizure threshold ; selegiline may be given as skin
selegiline phobic features and hypochondriasis arrhythmia, diarrhea, hyperthermia, CNS stimulation, seizure patch
Opioid Analgesics and Antagonists
A. Full Agonist TRIAD: miosis, coma, respiratory depression Additive CNS depression with other depressants
Exerts hemodynamic effects on the pulmonary circulation ;
Strong agonist at u receptors; For severe pain, pain associated with miosis, restlessness, respiratory depression, increased ICP, postural significant first-pass effect ; metabolized in the body to morphine-
i. Morphine acute MI, for pulmonary edema hypotension, urinary retention, pruritus, addiction liability 6-glucuronide which has equal analgesic activity as morphine
Strong agonist at u receptors; For severe pain, adjunct in anesthesia, restlessness, respiratory depression, increased ICP, postural May be given transdermally or via lollipop; ohmefentanyl is the
ii. Fentanyl chronic pain and breakthrough cancer pain hypotension, urinary retention, pruritus, addiction liability most potent opioid
Only opioid that does not cause miosis and biliary contraction ;
opioid of choice for pain relief in pancreatitis ; metabolized to
Strong agonist at u and k receptors, inhibits pain neurotransmission, normeperidine which can cause seizure therefore contraindicated
muscarinic blocking actions; For moderate to severe pain, labor restlessness, respiratory depression, increased ICP, postural in patients with seizure disorder ; if given with MAOi -->
iii. Meperidine analgesia, spasmodic pain (biliary, renal), preoperative sedation hypotension, urinary retention, pruritus, addiction liability, seizures Hyperpyrexic coma, if given with SSRI --> Serotonin syndrome
Strong agonist at u receptors, inhibits pain neurotransmission, binds Used in methadone maintenance therapy (MMT) for opioid
NMDA receptors and antagonizes the effects of glutamate; For miosis, restlessness, respiratory depression, increased ICP, postural dependence; currently being investigated as a novel treatment
iv. Methadone moderate to severe pain, opioid dependence, opioid withdrawal hypotension, urinary retention, pruritus, addiction liability for leukemia
B. Partial Agonist / Moderate Agonist
Strong agonist at u receptors, inhibits pain neurotransmission, binds

NMDA receptors and antagonises the effects of glutamate; For miosis, restlessness, respiratory depression, increased ICP, postural there is genetic variation in the metabolism of codeine and its
i. Hydrocodone, oxycodone moderate to severe pain, opioid dependence, opioid withdrawal hypotension, urinary retention, pruritus, addiction liability derivatives
Decreases sensitivity of cough receptors, depressing the medullary
cough center through sigma receptors stimulation; For cough hallucination, confusion, excitation, increased or decreased pupil size,
ii. Dextrometorphan, codeine suppression nystagmus, seizures, coma, respiratory depression, addiction liability codeine is metabolized by CYP2D6 to morphine
C. Weak Agonist
i. Propoxyphene,
levopropoxyphene, Weak agonist at u receptors, inhibits pain neurotransmission; For mild miosis, respiratory depression, increased ICP, postural hypotension,
dextropropoxyphene to moderate pain, restless leg syndrome urinary retention, pruritus, addiction liability, fatal arrythmias Withdrawn because of fatal cardiotoxicity
D. Mixed Agonist-Antagonist
Strong agonist at k receptors, weak antagonist activity at u receptors; sedation, dizziness, sweating, nausea, anxiety, hallucinations,
i. Nalbuphine, buprenorphine, For moderate to severe pain, opioid dependence, alcohol dependence, nightmares, respiratory depression (less), tolerance, dependence Buprenorphine reduces craving in alcohol dependence,
butorphanol, pentazocine balance anesthesia, for opioid withdrawal states (buprenorphine) liability buprenorphine and nalbuphine is resistant to Naloxone
E. Opioid Antagonist
Competitively blocks u, sigma and k receptors, rapidly reverses effects Precipitates abstinence syndrome in Px with opioid dependence ;
of opioid agonists; For opioid overdose, opioid and alcohol dependence Naloxone and Nalmefene is IV (DOA: 12-24 hrs) while
i. Naloxone, naltrexone, nalmefene (naltrexone) pruritus, nausea, vomiting Naltrexone is PO (DOA: 48h)
F. Dual-acting
Weak agonist at u receptors, inhibits neuronal reuptake of serotonin
and norepinephrine; For moderate pain, chronic pain syndrome, Lower seizure threshold ; CI in Px taking SSRI and those with
i. Tramadol neuropathic pain seizures, nausea, dizziness, pruritus, constipation history of seizure
5. DRUGS USED TO TREAT DISEASES OF THE BLOOD, INFLAMMATION, & GOUT
Agents Used in Anemias and Hematopoietic Growth Factors
A. Hematopoietic growth factor
i. Ferrous sulfate, Ferrous
gluconate, Ferrous Fumarate, Iron Required for the biosynthesis of heme and heme containing proteins, Black stools, shock, lethargy, dyspnea, abdominal pain, necrotizing
dextran, Sodium Ferric Gluconate including hemoglobin and myoglobin; For Iron deficiency anmia, iron gastroenteritis, death, organ failure, hemochromatosis, metabolic
complex, Iron sucrose supplementation acidosis None
B. Heavy metal chelator
Hypotension, Neurotoxicity, ARDS, Increased susceptibility to
i. Deferoxamine, Deferasirox Chelates excess iron; For acute and chronic iron poisoning infections None
C. Hematopoietic growth factor
Cofactor required for essential enzymatic reactions that form

i. Cyanocobalamin, tetrahydrofolate, convert homocysteine to methionine and metabolize Hydroxocobalamin has a longer t1/2 than cyanocobalamin ; has
Hydroxocobalamin methylmalonyl-CoA; For vitamin B12 deficiency, megaloblastic anemia No significant toxicity a storage of up to 5yrs in the liver
D. Hematopoietic growth factor
Precursor of an essential donor of methyl groups used for synthesis of
amino acids, purines and deoxynucleotide; For Megaloblastic anemia,
i. Folic acid, Folacin prevention of neutral tube defects (spina bifida), prevention of coronary
(Pteroylglutamic acid), Folinic acid artery disease No significant toxicity only modest amounts are stored in the body
E. Hematopoietic growth factor
i. Epoetin Alfa, Darbepoetin alfa, Agonist of erythropoietin receptors expressed by red cell progenitors; Performance-enhancing drug in athletes ; darbepoietin is once a
Methoxy Polyethylene Glycol- Epoetin For Anemia, associated with chronic renal failure, cancer, HIV infection week administration, while Methoxy Polyethylene Glycol- Epoetin
Beta and prematurity Hypertension, Thrombosis, Pure red cell aplasia Beta is 1-2x per month administration
F. Myeloid growth factor
Binds receptors on myeloid progenitors and stimulates cell maturation
and proliferation ; Accelerates neutrophil recovery and reduces
i. (G-CSF) Filgrastim, Sargamostim incidence of infection; For neutropenia associated with chemotherapy,
(GM-CSF), Pegfilgrastim myelodysplasia, and aplastic anemia Edema, Fever, Arthralgia Pegfilgrastim has longer t1/2
G. Megakaryocyte growth factor
Recombinant form of an endogenous cytokine; activates IL -11
receptors ; For secondary prevention of thrombocytopenia in patients fatigue, headache, anemia, fluid accumulation in the lungs, dizziness,
i. Oprelvekin(IL-11), Thrombopoietin undergoing chemotheraphy transient atrialarrythmias given SC OD
Agents Used in Dyslipidemia
has direct anti-atherosclerotic effect, and can prevent bone loss ;
Increased risk of myopathy and rhabdomyolysis when used with
fibrates ; Given before bedtime because cholesterol synthesis
predominantly occurs at night ; simvastatin and lovastatin are
prodrugs, all the rest are in their active form already ;
A. HMG-CoA Reductase Inhibitors: Inhibits rate-limiting enzyme in cholesterol biosynthesis (HMG-CoA Rosuvastatin, Atorvastatin and Simvastatin have greater maximal
Simvastatin, Atorvastatin, reductase), Increased hepatic cholesterol uptake, Increased high effect than other statins ; if given together with resins give at
Rosuvastatin, Fluvastatin, affinity LDL receptors which leads to decreased LDL levels ; DOC for least 1hr before or 4hrs after resin administration (resins
Pravastatin, Lovastatin, Pitavastatin, hypercholesterolemia (high LDL), decreases risk of acute coronary Hepatoxicity, Myopathy, Rhabdomyolysis, Gastrointestinal distress, decrease the absorption of statins) ; has CYP450 dependent
Cerivastatin, syndromes, ischemic stroke Teratogen metabolism
non-absorbable polymers that bind bile acids and similar steroids in the
intestines preventing their reabsorption, increases cholesterol utilization
B. Bile Acid Binding Resin: for replacement, modestly lowers LDL levels by increasing hepatic LDL Increases TGs and VLDL in patients with high TGs and
Colesevelam, Colestipol, receptors ; For hypercholesterolemia (high LDL), pruritus in cholestasis, Constipation, Bloating, Gritty taste, Gallstone formation, steatorrhea, combined hyperlipidemia ; Treat constipation with fiber
Cholestyramine digitalis toxicity malabsortion of fat soluble substances (vitamin k, folate) supplements/psyllium ; Avoid in patients with diverticulitis
Selective inhibitor of the NPC1L1 transporter decreasing intestinal

absorption of cholesterol and other phytosterols, decreases cholesterol
C. NPC1L1 transporter inhibitor: hepatic pool, increases hepatic LDL receptors ; For
Ezetimibe Hypercholesterolemia (High LDL), phytosterolemia Hepatoxicity (increased with statin use), Myositis Synergistic LDL-lowering effect with statins ; is a prodrug
Cholesterol analog, takes the place of dietary and billiary cholesterol,

D. Sterol absorption blocker: decreasing intestinal absorption of cholesterol and other phytosterols ;
Sitosterol For Hypercholesterolemia (high LDL), phytosterolemia Gastrointestinal upset, bloating, impotence (rare), coronary events NONE
Decreases VLDL synthesis and LDL cholesterol concentrations,
decreases hormone-sensitive lipase activity leading to decreased LDL decreases fibrinogen and increases t-PA ; NSAIDs pre-treatment
levels, Increases HDL cholesterol by decreasing its catabolism ; DOC Flushing, nausea, vomiting, Pruritus, Acanthosis nigricans, Rashes, reduces flushing ; Avoid in patients with peptic ulcer disease ;
for increasing HDL levels, for Hypercholesterolemia (low HDL, high Gastrointestinal irritation, Hepatoxicity (mild), Hyperuricemia, Impaired Potentiates effects of antihypertensives (vasodilators, ganglion
E. Nicotinic Acid derivatives: Niacin LDL/VLDL), hypertriglyceridemia glucose tolerance, Arrhythmias, Ambylopia blockers)
Increased risk of myopathy and rhabdomyolysis when used with

Activates PPAR-α and increases expression of lipoprotein lipase and statins ; Avoided in patients with hepatic or renal dysfunction ;
apolipoproteins (apoA-I, apoA-II) leading to enhanced clearance of TG- may increase LDL in patients with familial combined
F. Fibrates: Gemfibrozil, Fenofibrate, rich lipoproteins, Lowers triglycerides, Increases HDL ; DOC for Nausea, Rashes, Leukopenia, nausea, vomiting, increased risk of hyperlipoproteinemia ; has little or no effect on LDL ; higher risk
Bezafibrate hypertriglyceridemia cholesterol gallstones of gallstone formation if given together with resins
Drugs for Coagulation
A. Antiplatelet For arterial thrombosis only
Nonselective, irreversible COX 1&2 inhibitor. Reduces platelet
production of thromboxane A2, temporarily inhibit Prostacyclin
synthesis ; For prevention or arterial thrombosis (MI, TIA, CVD), Gastrointestinal toxicity, nephrotoxicity, tinnitus, hyperventilation,
Inflammatory disorders (rheumatic fever, juvenile rheumatoid arthritis, hypersensitivity, HAGMA, Increased bleeding time, Nephrotoxicity Uncoupler of oxidative phosphorylation, associated with Reye
i. Aspirin kawasaki disease) (AKI and Interstitial Nephritis) syndrome in children ; Do not use as NSAID for gout
Reversbily inhibits the binding of fibrin and other ligands to the platelet
ii. GPIIb-IIIa inhibitor: Abciximab, GPIIb-IIIa receptor ; For antithrombosis during PCI, Acute coronary
Eptifibatide,Tirofiban syndromes (unstable angina, NSTEMI) Bleeding, Thrombocytopenia Adjunct to thrombolysis
Inhibits phosphodiesterase III and increases cAMP in platelets and

blood vessels, Inhibits platelet aggregation and causes vasolidation ; additional MOA: inhibit uptake of adenosine by endothelial cells
For prevention of thromboembolic complications of cardiac valve and RBC, thus increasing adenosine levels leading to inhibition
iii. PDE III inhibitor: Dipyridamole, replacement (as adjunct to warfarin), secondary prevention of ischemic of platelet aggregation ; Cilostazol is contraindicated in heart
Cilostazol stroke (with aspirin), Intermittent claudication (Cilostazol only) Headache, palpitations failure
Irreversibly inhibits binding of ADP to platelet receptors,thus reducing
platelet aggregation ; For prevention and treatment of arterial
iv. ADP inhibitor: thrombosis (stroke, TIA, unstable angina), Acute coronary syndromes, Bleeding, nausea, hematologic (neutropenia, leukopenia), thrombotic GI & Hematologic SE are more common with ticlopidine. Additive
Clopidogrel,Ticlopidine, Prasugel Prevention of re-stenosis after PCI thrombocytopenic purpura (Ticlopidine), dyspepsia effects with aspirin
B. Anticoagulant For both venous and arterial thrombosis
Activates antithrombin III which Inactivates thrombin or factor IIa, factor
IXa & factor Xa by forming stable complexes with them ; For deep
venous thrombosis, myocardial dysfunction, Pulmonary embolism,
adjuvant to percutaneous coronary intervention (PCI) and
thrombolytics, Atrial fibrillation, Pulmonary embolism, given with
i. Heparin (indirect thrombin thrombolytics for revascularization procedures, given with GPIIb-IIIa Bleeding, transient Heparin-induced thrombocytopenia, Osteoporosis DOC for anticoagulation during pregnancy ; administered IV or
inhibitor) inhibitors for angioplasty and stent placement with chronic use SC ; Monitor with aPTT, Antidote: Protamine Sulfate
Binds and potentiates effect of antithrombin III on factor Xa (more Does not require aPTT monitoring, Protamine sulfate is only
selective for Xa); For Deep venous thrombosis, Pulmonary embolism, partially effective in reversing effects ; advantage over regular
ii. LMWH: Enoxaparin, Dalteparin, unstable angina, myocardial infarction, adjuvant to percutaneous heparin is higher bioavailability and t1/2 ; Fondaparinux is given
Tinzaparin, Fondaparinux coronary intervention (PCI) and thrombolytics, Atrial fibrillation Bleeding, less risk of thrombocytopenia SC OD
iii. Direct Thrombin Inhibitors: Binds to thrombin's ative site and inhibits its enzymatic action; For Monitor with aPTT. No reversal agents exist ; Dabigatran is PO
Lepirudin, Desirudin, Bivalirudin, anticoagulation in patients with heparin induced thrombocytopenia while all the rest are parenteral ; Bivalirudin also inhibits platelet
Argatroban, Dabigatran (HIT), percutaneous coronary angioplasty (Bivalirudin with aspirin) Bleeding, Anaphylactic reactions, Effect-prolonging antibodies activation
iv. Direct Oral Factor Xa inhibitor: bind to free and bound factor Xa ; For prevention of Venous
Rivaroxaban, Apixaban thrombosis, in stroke patients with Afib bleeding No reversal agent
Inhibits vitamin K epoxide reductase (responsible for y-carboxylation of
the vitamin K- dependent clotting (factors II, VII, IX, X, Protein C &
Protein S) ; For chronic anticoagulation (DVT, atrial fibrillation, valve Bleeding, Teratogen (bone defects, hemorrhage), warfarin-induced Monitor effects with PT-INR. Antidote is vitamin K or FFP. Narrow
v. Warfarin, Dicumarol replacement) EXCEPT in pregnancy skin necrosis (transient hypercoagulability) therapeutic window ; 99% protein-bound
C. Antidote
Chemical antagonist of heparin. Reverses excessive anticlotting activity
i. Protamine Sulfate of unfractionated heparin; For heparin overdosage hypotension, flushing, bradycardia, dyspnea, hypersensitivity Partially reverses effect of LMWHs
Increases supply of reduced vitamin K, which is required for synthesis
ii. Endogenous Vitamin: Vitamin K1, of functional vitamin K-dependent clotting and anticlotting factors ; For
K2, K3 (Phytonadione, Menaquinone, Vitamin K deficiency, Antidote to warfarin, prevention of hemorrhagic Severe infusion reaction when administered at a fast rate (dyspnea,
Menadione) diatheses in newborns chest and back pain) Vit K1 may be given PO or IV
Tx should be done within 6 hrs, better if within 3hrs ; Antidote is
D. Thrombolytic: Alteplase, AMINOCAPROIC ACID ; Streptokinase forms a complex with
Anistreplase, Reteplase, Tissue plasminogen activator analog. Converts plasminogen to endogenous plasminogen, thus catalyzing the conversion of
Streptokinase, Tenecteplase, plasmin, which degrades the fibrin and fibrinogen, causing thrombolysis Bleeding, Reperfusion, Cerebral hemorrhage, Arrhythmias ; Loss of plasminogen to plasmin ; tPA is selective for fibrin-bound
Urokinase ; For acute myocardial infarction, pulmonary embolism, Ischemic stroke effectiveness (on 2nd use) and allergic reactions (streptokinase) plasminogen
Competitively inhibits plasminogen activation thus inhibiting fibrinolysis ;
For prevention and treatment of acute bleeding episodes in patients
with high risk of bleeding (hemophilia, intracranial aneurysms, Contraindicated in disseminated intravascualr coagulation (DIC)
E. Antiplasmin drug: Tranexamic acid menstrual, obstetrics, thrombolytics, postperative) Thrombosis, hypotension, Myopathy, Diarrhea and genitourinary bleeding
Vasopressin V2 receptor agonist, Increases factor VIII activity of
patients with mild hemophilia A or VWD; For hemophillia A, von
F. ADH agonist: Desmopressin Willebrand's disease, central diabetes insipidus headaches, nausea, flushing, seizures, hyponatremia may cause immunologic reactions and infections
Non-steroidal Anti-Inflammatory Drugs, Disease-Modifying Anti-rheumatic Drugs, Non-opioid Analgesics & Drugs Used in Gout
A.Non-selective NSAID
low doses undergo first order kinetics while high doses undergo
zero order reaction ; Long term use reduces the risk of colon
i. Aspirin, Sodium Salicylate See entry on Drugs for caogulation Disorder See entry on Drugs for caogulation Disorder cancer
Ibuprofen and Indomethacin can be used to close PDA ;
ii. Ibuprofen, Diclofenac, Diflunisal, Ibuprofen and naproxen have moderate effectiveness ; Ibuprofen
Etodolac, Fenoprofen, Flurbiprofen, is relatively safe but with short half-life of 2hrs ; Naproxen and
Ketoprofen, Meloxicam, Nabumetone, Piroxicam have longer half-lives ; Ketorolac has significant
Naproxen, Oxaprozin, Piroxicam, Nonselective reversible COX-1 and COX-2 inhibitor. Inhibits analgesic effect but not anti-inflammatory effect ; use Ketorolac
Sulinidac, Tolemtin, Mefenamic acid, prostaglandin and thromboxane synthesis ; For analgesia, fever and as Gastrointestinal bleeding (less than aspirin), Nephrotoxicity (AKI and only for 72hrs due to GI and renal damage ; NSAIDs may
Ketorolac anti inflammatory Interstitial Nephritis), Hypersensitivity reaction interfere with ASA's antithrombotic action
Nonselective reversible COX-1 and COX-2 inhibitor. Inhibits
prostaglandin synthesis and inhibit crystal phagocytosis by
macrophages ; For anti inflammatory (gout arthritis, ankylosing Gastrointestinal toxicity, pancreatitis, Nephrotoxicity, Serious Indomethacin has greater anti-inflammatory effect compared to
iii. Indomethacin spondylitis), for closing PDA hematologic reactions, BM suppression other NSAIDs
B. COX-2 Selective NSAID: Selective COX-2 inhibitor. Inhibits prostaglandin synthesis ; For Gastrointestinal bleeding, Nephrotoxicity (same risk as nonselective Rofecoxib and Valdecoxib withdrawn due to incereased
Celecoxib, Etoricoxib, Parecoxib Analgesia, Anti inflammatory, Antipyretic NSAIDs), Myocardial infarction and stroke incidence of thrombosis
C. Non-opioid Analgesic (COX3 Selectively inhibits COX-3 in the CNS, Weak COX-1 and COX-2
inhibitor) Paracetamol inhibitor in the periphery, Inhibits prostaglandin synthesis ; For Hepatoxicity (antidote: NAC), Renal papillary necrosis and Interstitial Preferred antipyretic in children (does not cause reye's
(Acetaminophen) Analgesia and antipyretic nephritis, Methemoglobinemia, Hemolytic anemia syndrome) ; t1/2 is only 2-3h
D. Disease Modifying Anti-Rheumatic
Drug
Inhibits AICAR transformylase and thymidylate synthase, with
secondary effects on polymorphonuclear chemotaxis ; For rheumatoid
arthritis, SLE, JRA, psoriatic arthritis, Ankylosing spondylitis, Nausea, Mucosal ulcers, hepatoxicity, hypersensitivty, DMARD of choice for Rheumatoid arthritis, Rescue agent:
i. Methotrexate Polymyositis Pseudolymphomatous reaction, teratogen, hematotoxicity Leucovorin (Folinic acid)
Bacterial infections (URTIs), reactivation of latent tuberculosis,
lymphoma, Demyelination, Reactivation of Hepatitis B, Auto antibody
ii. TNF-alpha inhibitor: Infliximab, Binds or inhibits to TNF-a ; For Crohn's disease, rheumatoid arthritis, formation (ANA, anti dsDNA), infusion reactions, hepatoxicity,
Adalimumab, Etanercept other rheumatic disease hematotoxicity, cardiotoxicity Synergistic effects with methotrexate
Forms 6-thioguanine, suppressing inosinic acid synthesis, B-cell and T-
cell function, Immunoglobulin production and interleukin-2 secretion ; Cannot give allopurinol with azathioprine (allopurinol reduces
For rheumatoid arthritis, psoriatic arthritis, reactive arthritis, Bone marrow supression, increased risk of infections, increased xanthine oxidase catabolism of purine analogs, increasing 6-
iii. Azathioprine polymyositis, SLE incidence of lymphoma, Fever, rash, hepatotoxicity, allergic reactions thioguanine nucleotides, leading to severe leukopenia)
Suppression of T-lymphocyte leading to decreased leukocyte
chemotaxis, stabilization of lysosomal enzymes, inhibition of DNA and
RNA synthesis, trapping of free radicals ; For rheumatiod arthritis, SLE, Ocular toxicity, Dyspepsia, Nausea, vomiting, abdominal pain, rashes,
iv. Chloroquine, Hydroxychloroquine Sjogren's syndrome, Malaria nightmares, myopathy, neuropathy, ocular toxicity safe for pregnant women
Forms phospharamide mustard, which cross links DNA to prevent cell
replication, Supresses T-cell and B-cell function ; For Rheumatoid
arthritis, SLE vasculitis, Wegener's granulomatosis, severe rheumatic
v. Cyclophosphamide diseases Hemorrhagic cystitis Hemorrhagic cystitis, Rescue agent is Mesna
Inhibits interleukin-1 and iterleukin-2 receptor production and
secondarily inhibits macrophage-T-cell interaction and T-cell Nephrotoxicity, hypertension, hyperkalemia, hepatoxicity, Gingival
vi. Cyclosporine responsiveness ; For rheumatoid arthritis, SLE, Tissue transplantation hyperplasia, hirsutism NONE
active product inhibits inosine monophosphate dehydrogenase and
inhibits T-cell lymphocyte proliferation ; For SLE nephritis, vasculitis, Gastrointestinal disturbances, headache, hypertension, reversible
vii. Mycophenolate Mofetil Wegener's granulomatosis, rheumatoid arthritis myelosupression NONE
Nausea, vomiting headache,rash, hemolytic anemia,
active metabolite inhibits the release of inflammatory bowel cytokines; methemoglobinemia, neutropenia, leukopenia, thrombocytopenia,
For rheumatoid arthritis, inflammatory bowel disease, JRA, ankylosing pulmonary toxicity, autoantibody formation (anti dsDNA), Reversible
viii. Sulfasalazine spondylitis infertility in men anti-IBD drugs
E. Antigout drugs
Diarrhea, nausea, vomiting, abdominal pain, hepatic necrosis, acute a general mitotic poison, may also be used for Familial
i. Microtubule assembly inhibtor: Inhibits microtubule assembly and LTB4 production leading to renal failure, disseminated intravascular coagulation, seizures, hair Mediterranean Fever ; diarrhea is the adverse effect which
Colchicine decreased macrophage migration and phagocytosis ; For gout loss, bone marrow depression, peripheral neuritis, myopathy signals toxicity from colchicine
May precipitate acute gout during early phase of drug action

(prevent by coadministering with colchicine or indomethacin) ;
may be given together with antimicrobial agents (particularly
ii. Uricosuric agent: Probenecid, are weak acids that compete with uric acid for reabsorption in the PCT Gastrointestinal irritation, rashes, nephrotic syndrome, aplastic Penicillins) to prolong therapeutic effect by inhibiting renal tubular
Sulfinpyrazone leading to increased uric acid excretion ; For gout anemia ; sulfa allergy secretion of antibiotics
Inhibits metabolism of mercaptopurine and azathioprine. Witheld
for 1-2 wk after an acute episode of gouty arthritis
Active metabolite (alloxanthine) irreversibly inhibits xanthine oxidase (coadministered with colcichine or indomethacin to avoid an
iii. Xanthine oxidase inhibitor: and lowers production of uric acid; 1st line treatment of chronic gout, Gastrointestinal upset, Rash, Peripheral neuritis, Vasculitis, bone acute attack) ; Feboxustat is a newer non-purine inhbitor of
Allopurinol, Febuxostat tumor lysis syndrome marrow dysfunction, Aplastic anemia, liver dysfunction (Febuxostat) Xanthine Oxidase ; Febuxostat is more effective than Allopurinol
6. ENDOCRINE DRUGS
Hypothalamic and Pituitary Hormones
Recombinant Growth hormone, Increases release of IGF-1 in the liver
and carilage, stimulates skeletal muscle growth, amino acid transport,
protein synthesis and cell proliferation ; For GH deficiency in children
and genetic disease associated with short stature (Turner syndrome, Peripheral edema, Myalgia, Arthralgia, Intracranial hypertension,
Prader-Willi syndrome), failure to thrive due to chronic renal failure or pseudotumor cerebri, slipped capital femoral epiphysis, progression of used as Performance enhancing drug since it increases muscle
i. Somatropin SGA, AIDS wasting scoliosis, hyperglycemia mass
ii. Mecasermin Recombinant IGF-1 ; For children unresponsive to GH therapy Hypoglycemia remedy to hypoglycemia: give patient some snacks prior to dose
Somatstatin analog, suppresses the release of growth hormones,
glucagon, insulin, gastrin, IGF-1, serotonin and gastrointestinal
peptides ; For Acromegaly, pituitary adenoma, carcinoid, gastrinoma, regular release: given BID-QID SC, if slow release: every 4wks
iii. Octreotide, Lanreotide glucagonoma, variceal bleeding GI upset, gallstone, cardiac condution abnormality IM
diarrhea, nausea, flu-like syndrome, elevated LFTs, hypesensitivity
iv. Pegvisomant GH receptor antagonist ; For acromegaly reaction onset of action is expected within 2wks of use
Gonadotropin analog (FSH analog); activates FSH receptors and Headache, depression, edema, ovarian hyperstimulation syndrome Follitropin alfa and beta are recombinant FSH forms while
v. Follitropin alfa, Follitropin beta, mimics effects of endogenous FSH ; For Controlled ovarian (ovarian enlargement, ascites, hypovolemia, shock), multiple Urofollitropin is a purified preparation from urine of
Urofollitropin hyperstimulation, infertility due to hypogonadism in men pregnancies in women, gynecomastia in men postmenopausal women
vi. Menotropins, Human chorionic Gonadotropin analog (LH analog); activates LH receptors and mimics menotropins are mixtures of FSH and LH from postmenopausal
gonadotropin (HCG), effects of endogenous LH ; For Controlled ovarian hyperstimulation Headache, depression, edema, ovarian hyperstimulation syndrome, women ; Choriogondaotropin alfa is a recombinant hCG while
Choriogondaotropin alfa, Lutropin (ovulation induction), hypogonadotripic hypogonadism multiple pregnancies in women, gynecomastia in men Lutropin is a recombinant LH
GnRH analog, increased LH and FSH secretion with intermittent there is exacerbation of symptoms in males with prostate CA and
vii. Leuprolide, Gonadorelin, administration , reduced LH and FSH secretion with prolonged children with precocious puberty during the first few weeks of
Goserelin, Histrelin, Nafarelin, continuous administration ; For Controlled ovarian hyperstimulation, Hot flushes, sweats, headaches, osteoporosis, gynecomastia, therapy (remedy: co-administer Flutamide, an androgen receptor
Triptorelin endometriosis, myoma uteri, precocious puberty, postate CA reduced libido, decreased hematocrit antagonist) ; Gonadorelin is a synthetic human GnRH
GnRH antagonist, blocks GnRH receptors, reduces endogenous Does NOT cause tumor flare-up whe used for treatment of
production of LH and FSH ; For Controlled ovarian hyperstimulation Nausea, headache, hypersensitivity, hot flushes, gynecomastia, advanced prostate cancer, Degarelix is used for prostate CA
viii. Ganirelix, Cetrorelix, Degarelix (prevents premature LH surge), advanced prostate CA decreased libido, decreased hematocrit, osteoporosis while Ganirelix prevent LH surge in controlled ovulation
Dopamine agonist, partial agonist at dopamine D2 receptors in brain,
inhibits prolactin release, Slightly inhibits GH release ; For Nausea, headache, lightheadedness, orthostatic hypotension, fatigue,
Hyperprolactinemia, Pituitary adenoma, acromegaly, Parkinson's behavioral changes, erythromelalgia, Raynaud's phenomenon,
ix. Bromocriptine, Carbegoline disease pulmonary infiltrates CI in patients with history of psychotic illness
Activates oxytocin receptorsl stimulates uterine contraction and labor,
stimulates mammary glands, lactation and milk let-down ; For Labor
induction, labor augmentation, control of uterine hemorrhage post- Fetal distress, placental abruption, uterine rupture, fluid retention,
x. Oxytocin delivery hyponatremia, heart failure, seizures, hypotension ATOSIBAN - an oxytocin antagonist used in preterm labor
ADH agonist, Vasopressin V2 receptor agonist which causes insertion
of water channels in the collecting duct leading to more water
reabsoprtion, also regulates the release of factor VIII and VWF ; For also contracts vascular smooth muscles via V1 receptor leading
Central DI, Hemphilia A, von Willebrand's disease, Variceal bleeding, to vasoconstriction, used as treatment for esophageal varices or
xi. Desmopressin primary nocturnal seizures Headaches, flushing, nausea, hyponatremia, seizures colon diverticula
ADH antagonist, Antagonist at V1a and V2 receptors ; For SIADH,

Hyponatremia, offset fluid retention in acute heart failure and SIADH Central pontine myelinolysis may occur with rapid correction of
xii. Conivaptan, Tolvaptan which causes hyponatremia (dilutional) Infusion site reactions, hyperkalemia hyponatremia, tolvaptan is more selective for V2 receptors
Thryoid & Antithyroid Drugs
Thryoid hormone, activation of nuclear receptors results in gene T4 dose must be lowered in patients with cardiovascular disease
i. Levothyroxine (T4), Liothyronine expression with RA formation and protein synthesis ; For Dry skin, sweatng, tachycardia, nervousness, tremor, weight loss, or longstanding hypothyroidism (increased cardiosensitivity) ;
(T3) Hypothyroidism, myxedema coma weakness, heat intolerance Liothyronine has a faster onset but shorter half-life
Maculopapular pruritic rash, gastrointestinal distress, fulminant
Inhibits thyroid peroxidase reactions, blocks iodine organification, hepatitis, agranulocytosis, urticaria, vasculitis, lupus-like syndrome,
inhibits peripheral conversion of T4 into T3 ; For Hyperthyroidism, lymphadenopathy, hypoprothrombinemia, Exfoliative dermatitis, Drug of choice for pregnant hyperthyroid patients; slow onset of
ii. Propylthiouracil (PTU) thyroid storm polyserositis, arthralgia, hypothyroidism action (3-4 weeks for full effect)
Maculopapular pruritic rash, gastrointestinal distress, fulminant
hepatitis, agranulocytosis, urticaria, vasculitis, lupus-like syndrome,
Inhibits thyroid peroxidase reactions, blocks iodine organification ; For lymphadenopathy, hypoprothrombinemia, Exfoliative dermatitis,
iii. Methimazole, Carbimazole Hyperthyroidism, thyroid storm polyserositis, arthralgia, hypothyroidism Methimazole and Carbimazole are teratogens
Inhibit iodine organification and hormone release leading to reduced Iodism, acneiform rash, swollen salivary glands, mucous membrane onset is more rapid (2-7 days) but effect is transient ; Should not
iv. Lugol Solution (Iodine in size and vascularity of thyroid gland ; For Hyperthyroidism, thyroid ulcerations, conjunctivitis, rhinorrhea, drug fever, metallic taste, be used alone (escape in 2-8 weeks); prevents radiation induced
Potssium Iodide), Potassium Iodide storm, preparation for surgical thyroidectomy, radiation prophylaxis bleeding disorders, anaphylactoid reactions thryoid damage; prenatal exposure causes fetal goiter
Beta blocker control HR and other cardiac abnormalities of severe
thyrotoxicosis, slows pacemaker activity; inhibits peripheral conversion Esmolol may be used to treat thyrotoxicosis-related arrhythmias;
v. Propranolol, Esmolol, Metoprolol, of T4 into T3 ; For Hyperthyroidism, thyroid storm, post MI prophylaxis, causes clinical improvement WITHOUT altering thyroid hormone
Atenolol hypertension Bronchospasm, cardiac depression, AV block, hypotension levels
Iodide, emits beta rays causing destruction of thyroid parenchyma ; For Preferred treatment for most patients due to ease of
hyperthyroidism, permanent cure of thyrotoxicosis without surgery and administration, effectiveness, low expense and absence of pain;
vi. Radioactive Iodine no effect on other tissues Permanent hypothyroidism, sore throat contraindicated in pregnant women or nursing mothers
Adrenocorticosteroids & Adrenocortical Antagonists
i. Low Potency: Desonide Effects: stimulate gluconeogenesis, increased fat deposition,
ii. Med Potency: Fluticasone, Glucocorticoid, activates glucocorticoid receptors, leading to altered protein catabolism, inhibit cell-mediated immunologic functions,
Mometasone gene transcription, Suppresses inflammation, Replaces cortisol when lymphotoxic, increased neutrophils, decreased lymphocytes,
iii. High Potency: Desoximetasone, deficient ; For Acute adrenal insufficiency, insect bites, contact Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, eosinpphils, basophils and monocytes, inhibit leukocyte
Clobetasol dermatitis, status asthmaticus, thyroid storm salt retention, glucose intolerance, behavioral changes migration, inhibit PLA2
iv. Prednisone, Prednisolone, Glucocorticoid; For supressession of inflammation and immune
Methylprednisolone, Meprednisone, response, hematopoeitic cancers, transplant rejection, collagen and
Dexamethasone, Betamethasone, rheumatic disease, lung maturation in preterm labor (betamethasone Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, prednisolone is the active metabolite of prednisone ; this group
Triamcinolone and dexamethasone) salt retention, glucose intolerance, behavioral changes (psychosis) has a long t1/2 and better penetration of lipid barriers
strong agonist of mineralocorticoid receptors and moderate activation of

glucorticoid receptors, Increases Na reabsorption, K and H excretion ;
v. Mineralocorticoid: For Chronic adrenal insufficiency (Addison's disease), Congenital Salt and fluid retention, Hypokalemia, Congestive heart failure, muscle
Fludrocortisone, Deoxycorticosterone adrenal hyperplasia, adrenal replacement therapy post-adrenalectomy wastng, oteoporosis, glucose intolerance, behavioral changes Additive hypokalemia with loop diurectics and thiazides
Glucorticoid synthesis inhibitor, inhibits desmolase activity, blocking
conversion of cholesterol to pregnenolone ; For Breast CA, Cushing
vi. Aminoglutethimide syndrome Skin rash, hepatotoxicity, hypothyroidism Also inhibits synthesis of all hormonally active steroids
Glucorticoid synthesis inhibitor; azole antifungal; inhibits cholesterol
side chain cleavage, cytochrome P450 enzymes and other enzymes
necessary for synthesis of all steroids ; For Adrenal CA, Hirsutism,
Breast CA, steroid-responsive metastatic Prostate CA, Cushing's
vii. Ketoconazole syndrome, Fungal infections, hirsutism Hepatotoxicity, many drug interactions, androgenic effect Potent inhibitor of CYP450 enzymes
Glucorticoid synthesis inhibitor, selective inhibitor of steroid-11
viii. Metyrapone hydroxylatuion, interfering with cortisol and corticosterone synthesis ;
As diagnostic test for adrenal function Dizziness, GI disturbances DOC for pregnant patients with Cushing's syndrome
ix. Mifepristone (RU486) competitive inhibitor at the GC receptor as well as progesterone abdominal pain and cramping, uterine cramping, nausea, headache, also used as an approved abortifacient for medical abortion
receptor ; For Cushing's syndrome vomiting, diarrhea, dizziness, vaginal bleeding (usually together with misoprostol)
x. Spironolactone, Eplerenone
Aldoesterone antagonist - see entry - Aldoesterone antagonist - see entry - also with weak antagonist effect at the androgen receptor
Gonadal Hormones and Inhbitors

A. Estrogen compounds
Increases risk of endometrial cancer and breast cancer ; Ethinyl
Estradiol has low bioavailability, PO/TD/IM/Intravaginal ; Estradiol
cypionate is IM with longer t1/2 ; Premarin is a mixture of
conjugated estrogen used in HRT ; Ethinyl estradiol undergoes
enterohepatic recirculation ; Effects of Estrogen: growth of genital
structures and secondary sexual characteristics, modifies serum
Activates etrogen receptors, leads to changes in rates of trasncription protein levels and decrease bone resorption, enhances
of estrogen-regulated genes ; For Primary hypogonadism, breakthrough bleeding, nausea, breast tenderness, migraine, coagulability of blood, increases TG and HDL levels while
i. Ethinyl Estradiol, Mestranol, Postmenopausal hormonal replacement therapy, Osteoporosis, thromboembolism (DVTs), gallbladder disease, hypertriglyceridemia, decreasing LDL levels, if given as continuous infusion will inhibt
Estradiol cypionate, Premarin Contraception, Intractable dysmenorrhea hypertension, premature closure of the epiphysis in young females FSH and LH release
Synthetic estrogen (nonsteroid); activates estrogen receptors; leads to

ii. Diethylstilbestrol changes in rates of transcription of estrogen-regulated genes ; For
Atrophic vaginitis, hormone replacement therapy, prevention of adverse associated with Infertility, ectopic pregnancy, clear cell vaginal
pregnancy outcomes, metastatic prostate CA Infertility, ectopic pregnancy, clear cell vaginal adenocarcinoma adenocarcinoma in daughters of women treated with DES
B. Progestins
Prevents estrogen induced endometrial cancer when used in

combination with estrogens; Megesterol is used as an appetite
i. Norgestrel, Medroxyprogesterone, stimulant ; given PO or as vaginal cream ; Medroxyprogesterone
Norethindrone, Norgestimate, has a better oral bioavilability ; L-Norgestrel and Norethindrone
Desogestrel,Megestrol has more androgenic effect ; Norgestrel undergoes enterohepatic
recirculation ; Effects of progesterone: induces secretory
activates progesterone receptors, change rates of transcription of changes in the endometrium, stabilize the endometrium, affect
progesterone-regulated genes ; For Hormone replacement therapy, Hypertension, decreased HDL, weight gain, reversible decrease in carbohydrate metabolism and stimulate deposition of fat, high
contraception, assisted reproduction, anovulation induction bone mineral density, delayed resumption of ovulation after use doses suppress FSH and LH secretion
C. Combined Hormonal
Contraceptives maybe PO/IM/TD/vaginal rings/IUD
i. Estradiol + Norethindrone
ii. Ethinyl Estradiol + Desogestrel

Combined oral contraceptive, activates estrogen and progesterone Lifetime risk of breast cancer is NOT changed; Norethindrone is
iii. Ethinyl Estradiol + Drospirenone
receptors, inhibits ovulation, effects on cervical mucus gland, uterine breakthrough bleeding, nausea, breast tenderness, migraine, a testosterone derivative while Drospirenone is a spironolactone
tubesand endometrium lead to decreased fertility, inhibit ovulation when thromboembolism (DVTs), breast cancer (earlier onset), headache, derivative that is antiandrogenic ; Norgestimate and Desogestrel
given before the LH surge ; For Contraception, hypogonadism, acne, skin pigmentation, depression, weight gain acne and hirsutism for are newer progestins ; combined OCPs may be used for
iv. Ethinyl Estradiol + Noregistmate hirsutism, dysmenorrhea, endometriosis older OCPs androgen-induced hirsutism
Progestin-only contraceptive, activates progresterone receptors,
Prevents conception by altering cervical mucus and creating a hostile Breakthrough bleeding, hair loss, dysmenorrhea, delayed return of
v. Medroxyprogesterone Acetate endometrium ; For Contraception, hormone replacement therapy fertility, osteoporosis IM depot preparation
Postcoital contraceptive, activates estrogen and/or progesterone
receptors, thickens cervical mucus, inhibits ovulation ; For Emergency Severe nausea, vomiting, breast tenderness, irregular bleeding,
vi. Levonorgestrel contraception headache, dizziness Must be taken within 72 hours of unprotected sexual intercourse
D. Selective Estrogen Receptor
Modulators (SERMs)
Estrogen antagonist actions in breast tissue and CNS, Estrogen agonist
effects in uterus, liver and bone ; For Hormone responsive breast CA, Hot flushes, thromboembolism, endometrial hyperplasia, endometrial prevent osteoporosis in post-menopausal women ; Torimefene is
i. Tamoxifen, Torimefene prophylaxis of breast CA esp. in those with high risk cancer structurally related to Tamoxifen
Estrogen antagonist actions in breast tissue, uterus, and CNS,
Estrogen agonist effects in liver and bone. Increases bone mineral
ii. Raloxifene density ; For Osteoporosis, breast CA prevention Hot flushes, thromboembolism No estrogenic effect on endometrial tissue unlike tamoxifen
Partial agonist in pituitary, reduces negative feedback by estradiol, Hot flushes, afterimages, headache, constipation, reversible hair loss,
iii. Clomiphene increases FSH and LH output ; For Induction of ovulation ovarian enlargement may cause multiple pregnancies
iv. Anastrozole, Letrozole, Reduces estrogen synthesisby inhibiting aromatase ; For breast CA, Effective against brest CA that have become tamoxifen-resistant
Exemestane precocious puberty Hot flushes, musculoskeletal disorders, osteoporosis, joint pains ; Exemestane is an IRREVERSIBLE inhibitor
Ovarian inhibitor, weak cytochrome P450 inhibitor and partial agonist of
progestin and androgen receptors ; For Endometriosis, Fibrocystic Acne, hirsutism, weight gain, menstrual disturbances, hepatic
v. Danazol disease, Hemophilia, Angioneurotic edema dysfunction May also act on Glucocorticoid receptors
Combined with misoprostol results in abortion of 95% of early

Glucocorticoid receptor antagonist, progesterone receptor antagonist ; Vaginal bleeding, abdominal pain, GI upset (vomiting, diarrhea), pregnancies ; as abortifacient in early pregnancy (may be used
vi. Mifepristone (RU486) For Medical abortion, Cushing's syndrome uterine cramping, nausea, headache, dizziness up to 49days after menses)
vii. Leuprolide and Ganirelix see entry see entry see entry
E. Androgens may be given IV or as TD
Activates androgen receptors, promotes development of male Effects of androgen: secondary sexual characteristics, fertility
characteristics, increases body muscle bulk and RBC production ; For and libido, male pattern baldness, increases muscle mass,
i. Testosterone, Fluoxymesterone, Male hypogonadism, delayed puberty, wasting syndromes (for weight Virilization and menstrual irregularities in females, paradoxical increased RBC production, decreased urea nitrogen excretion ;
Methyltestosterone gain), certain types of anemias feminization in males, cholestatic jaundice, elevated LFTs used illegally by atheletes as performance enhancer
Activates androgen receptors, promotes development of male

ii. Oxandrolone, Stanozolol, characteristics, increases body muscle bulk and RBC production; Virilization in females, paradoxical feminization in males; cholestatic
Nandrolone increased ratio of anabolic-to-androgenic activity in animals jaundice, elevated liver enzymes, hepatocellular CA this group is called "anabolic steroids"
For benign and malignant prostate disease, precocious puberty, hair
F. Anti-androgens loss and hirsutism
GnRH analogs must be coadministered with flutamide to prevent
i. Flutamide, Bicalutamide, Competitive antagonist at androgen receptor ; For Prostate CA, surgical acute flareups of prostate CA ; Bicalutamide and Nilutamide have
Nilutamide castration Gynecomastia, hot flushes, impotence, hepatotoxicity less heaptotoxicity
Antagonist at androgen receptor. Marked progestational effect that
suppresses the feedback enhancement of LH and FSH ; for Hirsutism,
component of combined oral contraceptives, decreased sexual drive in Hepatotoxicity, Adrenal suppression, depression, gynecomastia,
ii. Cyproterone men galactorrhea, thromboembolism Orphan drug status
Androgen synthesis inhibitor, inhibits 5a reducase enzyme that
converts testosterone to dihydrotestosterone ; For BPH, Male pattern Dutasteride is newer with longer t1/2 ; this group is less likely to
iii. Finasteride, Dutasteride baldness. Hirsutism Impotence, gynecomastia, depression cause impotence, infertility and decreased libido
iv. GnRH agonist and antagonists see entry see entry see entry
v. Ketoconazole see entry see entry see entry
P ancreatic Hormones & Antidiabetic Drugs
A. Insulins
i. Rapid Acting Insulin: Lispro, Effects of insulin: increased glycogen and protein synthesis,
Aspart, Glulisine decreased protein catabolism, increased TG storage ; rapid
acting insulins are injected a few mins prior to meals and they are
ii. Short Acting Insulin: Regular the preferred insulin for continuous SC infusion devices ; short-
Activates insulin receptors leading to a reducting of circulating glucose: acting insulins are injected more than an hour before a meal ;
iii. Intermediate Acting: NPH, Lente promotes glucose transport and oxidation; glycogen, lipid, protein Hypoglycemia (antidote: sugar or candy, IV glucose, IM glucagon), intermediate acting insulins are often combined with regular and
iv. Long Acting Insulin: Detemir, synthesis and regulation of gene expression ; For Diabetes mellitus, insulin allergy, immune insulin resistance, lipodystrophy at injection rapid acting insulins ; long acting insulins are called "peakless"
Glargine, Ultralente, Lantus diabetic emergencies like DKA, HHS (rapid-acting), Hyperkalemia site insulins
B. Sulfonylureas
2nd generation sulfonylurea, acts as an insulin secretagogue, increases
insulin secretion from pancreatic beta cells by closing ATP sensitive K+
i. Glipizide, Glibenclamide, channels leading to depolarization of the B cell; For Type 2 Diabetes Less hypoglycemia, weight gain, photosensitivity, cholestatic jaundice
Glimepiride, Gliclazide, Glyburide Mellitus (glibenclamide) Not effective in patients with functional B cells
1st generation sulfonylurea, acts as an insulin secretagogue; increases

ii. Tolazamide, Tolbutamide, insulin secretion from pancreatic beta cells by losing ATP sensitive K+ Hypoglycemia, weight gain, disulfiram reaction, hyperemic flush, tolbutamide and chlorpropamide are highly protein bound drugs,
Chlorpropamide channels ; for Type 2 Diabetes Mellitus dilutional hyponatremia, hematologic toxicity which may also cause allergic reactions and rash
C. Meglitinides
Insulin Secretagogue, similar to sulfonylureas with some overlap in
binding sites, reduces circulating glucose, increases glycogen, fat and
i. Repaglinide protein formation and gene regulation ; For Type 2 Diabetes Mellitus Least hypoglycemia, headache, URTI Least Hypoglycemia, rapid onset and short DOA
Insulin Secretagogue, similar to sulfonylureas with some overlap in

binding sites, reduces circulating glucose, increases glycogen, fat and Has least incidence of hypoglycemia, may be used in CKD
ii. Nateglinide protein formation and gene regulation ; For Type 2 Diabetes Mellitus Least hypoglycemia, headache, URTI patients ; rapid onset and short DOA
D. Biguanides
DOC for obese diabetics ; may also cause slowing of glucose
Reduced hepatic and renal gluconeogenesis with decreased absorption from GIT, decreased plasma glucagon ; causes a
endogenous glucose production, activates AMP-stimulated protein decrease in endogenous insulin production by increasing insulin
kinase leading to inhibition of gluconeogenesis ; For Type 2 DM, GI disturbance, weight loss, lactic acidosis (esp in renally and sensitivity of tissues "Insulin Sparing Effect" therefore does not
i. Metformin Diabetes prevention, PCOS hepatically impaired patients), Vit B12 malabsorption have weight gain as a SE ; do NOT cause hypoglycemia
E. Alpha Glucosidase Inhibitors
Inhibits intestinal alpha-glucosidases , reduces conversion of starch
and disacchardies to monosaccharidea, reduces post prandial GI disturbance, hypoglycemia, increased liver enzymes, flatulence, relatively minor glucose lowering effects ; impaired absoprtion of
i. Acarbose, Miglitol hyperglycemia ; For Type 2 DM, Diabetes prevention diarrhea, abdominal pain sucrose ; taken immediately before a meal
F. Thiazolidinediones
Regulates gene expression by binding to PPAR-gamma and PPAR-
alpha which increases tissue sensitivity, increases glucose uptake in
muscle and adipose tissue, inhibits hepatic gluconeogenesis, effects on
lipid metabolism and distribution of body fat, control of fasting and binds to PPAR-gamma and PPAR-alpha ; PPAR regulates
postprandial glucose, decreased risk of DM in high-risk patients ; For transcription of genes encoding proteins involved in carbohydrate
i. Pioglitazone Type 2 DM, Diabetes prevention Fluid retention, weight gain, congestive heart failure, fractures esp in and lipid metabolism
Regulates gene expression by binding to PPAR-gamma ONLY ; for women, cardiovascular events, hepatotoxicity (Troglitazone), macular
ii. Rosiglitazone Type 2 DM, Diabetes prevention edema, dyslipidemia, increased risk of MI (Rosiglitazone) binds to PPAR-gamma ONLY
G. Novel Antidiabetic Agents
Analog of GLP-1, Binds to GLP-1 receptors which leads to reducetion
of post-meal glucose excursions, increases glucose-mediated insulin
release, lowers glucagon levels, slows gastric emptying time, produces
i. Exenatide satiety ; For Type 2 DM Hypoglycemia, acute pancreatitis, GI upset, nausea, vomiting usually combined with SU or metformin ; long-acting injectables
Dipeptidyl Peptidase-4 Inhibitors, blocks degradation of GLP-1, raises
circulating GLP-1 levels, reduces post-meal glucose excursions,
increases glucose mediated insulin release, lowers glucagon levels,
ii. Sitagliptin, Linagliptin slows gastric emptying time, decreases appetite ; For Type 2 DM Headache, nasopharyngitis, URTI often combined with metformin
Analog of amylin, Binds to amylin receptors, reduce post-meal glucose
excursions, lowers glucagon levels, slows gastric emptying, decreases
iii. Pramlintide appetite ; For Type 2 DM Hypoglycemia, GI disturbances used with insulin to control post-prandial glucose
Bile acid binder, lowers glucose through unknown mechanisms ; For
iv. Colesevelam hydrochloride Type 2 DM constipation, dyspepsia, myalgia, asthenia None
Agents That Affect Bone Mineral Homeostasis
A. Vitamin D Metabolites and Analogs
INACTIVE Vitamin D; Regulates gene tanscription via the vitamin D
receptor; stimulates intestinal calcium absorption, bone resorption,
renal calcium and phosphate reabsorption, decreases PTH, promote
innate immunity ; For Vitamin D deficiency states (intestinal
osteodystrophy, CKD, chronic liver disease, hypoparathyroidism, given topically for psoriasis ; given with calcium supplements for
i. Cholecalciferol, Ergocalciferol nephrotic syndrome) osteoporosis, psoriasis Hypercalcemia, hyperphosphatemia, hypercalciuria osteoporosis
The active form Calcitriol is preferred in patients with CKD,
ACTIVE Vitamin D; Regulates gene tanscription via the vitamin D chronic liver disease and hypoparathyroidism ; Doxercalciferol is
receptor; stimulates intestinal calcium absorption, bone resorption, rena a prodrug that is converted in the liver to 1,25-dihydroxyvitaminD
calcium and phosphate reabsorption, decreases PTH, promote innate Hypercalcemia, hyperphosphatemia, hypercalciuria ; Doxercalciferol, ; Paricalcitol, Calcipotriene are analogs of calcitriol and are used
ii. Calcitriol, Doxercalciferol, immunity ; For Secondary hyperparathyroidism in CKD, hypocalcemia Paricalcitol and Calcipotriene cause less hypercalcemia and topically for psoriasis and are being investigated for malignancies
Paricalcitol, Calcipotriene in hypoparathyroidism, psoriasis hypercalciuria and inflammatory disorders
B. Bisphosphonates
Pamidronate, Zoledronic acid and Etidronate are used IV for
hypercalcemia in Paget's disease and cancer ; all other
preparations and Etidronate can be given PO but with low
i. Alendronate, Risedronate, Suppress the activity of osteoclasts in part via inhibition of farnesyl bioavailability (<10%) ; Treatment regimen: oral OD (alendronate,
Ibandronate, Pamidronate, pyrophosphate synthesis, inhibit resorption and formation of bone by Adynamic bone, Esophagitis, Osteonecrosis of the Jaw, renal risedronate, ibandronate), weekly PO (alendronate, risedronate),
Zoledronate, Etidronate, Tiludronate, acting on the basic hydroxyapatite crystal structure ; For Paget's impairment, GI irritation (remedy: take lots of water and keep patient monthly PO (ibandronate), quarterly injection (ibandronate),
Zoledronic acid disease of the bone, Hypercalcemia esp in malignancies, Osteoporosis in an upright position for 30mins after intake of drug) annual IV (zoledronate)
C. Hormones
Recombinant PTH, Acts via cognate G protein coupled receptors, hypercalcemia, arthralgia, rhinitis, nausea, weakness, dizziness,
i. Teriparatide stimulates bone formation when given in low intermittent doses pharyngitis, dyspepsia, rash used IV for osteoporosis
Acts via cognate G protein coupled receptors; suppresses bone

resorption ; For Paget's disease of the bone, hypercalcemia, given as injection or as nasal spray ; used for osteoporosis but is
ii. Calcitonin osteoporosis, tumor marker for thyroid CA Rhinitis, Nausea, vomiting, facial flushing less effective than bisphosphonates and teriparatide
D. Selective Estrogen Receptor
Modulators (SERMs)
Interacts selectively with estrogen receptors, inhibits PTH-stimulated
bone resorption without stimulating breast or endometrial hyperplasia,
i. Raloxifene delay bone loss in post-menopausal women see entry see entry
E. Rank Ligand (RANKL) Inhibitor
Monoclonal antibody, binds to RANKL and prevents it from stimulating
osteoclast differentiation and function, blocks bone resorption ; For as potent as bisphosphonates ; given SC every 6months which
i. Denosumab postmenopausal osteoporosis increased risk of infection avoid the GI SE
F. Calcium Receptor Antagonist
Activates the calcium sensing receptors in the parathyroid gland,
inhibits PTH secretion ; For secondary hyperparathyroidism in CKD, hypocalcemia, adynamic bone disease (profound decreae in bone cell
i. Cinacalcet hypercalcemia in patients with parathyroid CA activity) considered a Calcimimetic (decreases PTH)
7. CHEMOTHERAPEUTIC DRUGS
Beta-Lactam & Other Cell Wall-Active & Membrane-Active Antibiotics
Bactericidal ; excreted unchanged in the urine ; capable of
A. Penicillin
entering the blood brain barrier
i. Natural Penicillins: Penicillin G, Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial Inactivated by beta-lactamase (penicillinase) ; given IM but Pen
Penicillin V (narrow spectrum cell walls ; DOC for syphillis, for streptococcal, meningococcal, G+ V can be given PO ; increased activity against enterococci when
penicillin) bacilli, spirochete infection hypersensitivity, GI disturbances given together with aminoglycosides
ii. Anti-Staphylococcal Penicillins: Resistant to inactivation by beta-lactamase (penicillinase) ; all
Methicillin, nafcillin, oxacillin, Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial hypersensitivity, GI disturbances, interstitial nephritis (methicillin), penicillins are excreted unchanged in the urine EXCEPT for
cloxacillin (very narrow spectrum) cell walls; For staphylococcal infections neutropenia (nafcillin) Nafcillin which is excreted in the bile
iii. Extended Spectrum Penicillin: Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial
Ampicillin, Amoxicillin cell walls ; For enterococci, Listeria, E. coli, Proteus, H. influenza, hypersensitivity, GI disturbances, pseudomembranous colitis Inactivated by beta-lactamase (penicillinase), enhanced effect
Moraxella (ampicillin), rash (ampicillin) when used with beta-lactamase inhibitors (clavulanic acid,
sulbactam) ; ampicillin undergoes enterohepatic recirculation ;
synergistic effect with aminoglycosides
iv. Antipseudomonal Penicillin:

Piperacillin, ticarcillin, carbenicillin Inactivated by beta-lactamase (penicillinase), enhanced effect
Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial when used with beta-lactamase inhibitors (clavulanic acid,
cell walls ; For Pseudomonas, Enterobacter, Klebsiella hypersensitivity, GI disturbances tazobactam)
B. Cephalosporins Bactericidal ; mostly IV ; all have renal excretion EXCEPT
Cefoperazone and Ceftriaxone
i.First Generation: Cefazolin,
Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial Increases nephrotoxicity of aminoglycosides ; do not cross the
cefadroxil, cephalothin, cephapirin,
cell walls ; For surgical prophylaxis, bone infections, infections due to BBB ; minimal activity against G- cocci, enterococci, MRSA and
cephradine, cephalexin
staph and strep, E. coli, Klebsiella, G+ cocci hypersensitivity, injection site reactions, phlebitis, GI upset most G- rods
ii. Second Generation: Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial
Cefamandole, cefaclor, cefonicid, cell walls ; For surgical prophylaxis, bone infections, infections due to
cefuroxime, cefprozil, loracarbef, staph strep and E. coli, Enterobacter, Neisseria, infections against
ceforanide, cefoxitin, cefmetazole, anaerobes (Bacteroides), sinus ear and respiratory infections by hypersensitivity, injection site reactions, phlebitis, GI upset, Increases nephrotoxicity of aminoglycosides ; do not cross the
cefotetan Klebsiella andHemophilus Hypoprothrombinemia and Disulfiram rection (cefamandole, cefotetan) BBB ; slight less activity against G+ but extended G- activity
Synergistic effect with aminoglycosides ; all have renal excretion
iii. Third Generation: Cefoperazone, EXCEPT Cefoperazone and Ceftriaxone ; all can penetrate the
cefotaxime, ceftizoxime, ceftriaxone, BBB EXCEPT Cefoperazone and Cefixime ; Ceftriaxone and
cefixime, cefpodoxime proxetil, Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial Cefotaxime are the most active Cephs against Penicillin resistant
cefdinir, ceftibuten cell walls ; decreased gram + coverage, increased gram – activity Streptococcus pneumoniae ; Ceftizoxime is commonly used
(pseudomonas, bacteroides), against Providencia, Serratia, Neiserria, hypersensitivity, GI upset, Hypoprothrombinemia and Disulfiram against Bacteroides ; should be reserved against serious
Haemophilus ; DOC for gonorrhea (Ceftriaxone and Cefixime) rection (cefoperazone) infection EXCEPT ceftriaxone and cefixime
iv. Fourth Generation: Cefipime Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial More resistant to beta-lactamase produced by Enterobacter,
cell walls ; wide coverage against gram + and gram - bacteria hypersensitivity, GI upset Haemophilus, Neisseria and Pneumococcal
C. Other Beta-Lactams
Reserved for serious ife-threatening infections; cilastatin inhibits

renal metabolism of imipenem ; given IV ; low susceptibility to B-
i. Carbapenems: Imipenem- lactamases ; active against Pseudomonas and Acinetobacter
cilastatin , ertapenem, meropenem Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial EXCEPT Ertapenem ; Imipenem given with Cilastatin which acts
cell walls, wide coverage against gram + gram - bacteria and as Dehydropeptidase enzyme inhibitor ; Partial cross-allergenicity
anaerobes ; For infections resistant to other antibiotics EXCEPT MRSA, hypersensitivity, GI upset, CNS toxicity (confusion, encephalopathy, with Penicillins ; Ertapenem has longer t1/2 but less active
DOC for Enterobacter, Citrobacter and Serratia seizures) against Enterococci and Pseudomonas
Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial Resistant to beta-lactamase, no activity against gram + bacteria
ii.Monobactam: Aztreonam cell walls ; used against Gram – like klebsiella, pseudomonas and GI upset, superinfection, vertigo, headache, skin rash and or anaerobes ; given IV ; synergistic with AG ; renal excretion ;
Serratia hepatotoxicity No cross-allergenicity with Pens
iii. Beta-Lactamase Inhibitors:
Clavulanic acid , sulbactam,
tazobactam Most active against plasmid encoded B lactamases (Gonococci,
Inhibits inactivation of penicillins by bacterial beta-lactamase Streptococci, E coli and H. Influenzae ; not good inhibitor of
(penicillinase); used against beta-lactamase producing gonococci, inducible chromosomal B lactamases
streptococci, E. coli and H. influenza hypersensitivity and cholestatic jaundice (Enterobacter,Pseudomonas, Serratia)
D. Other Cell Wall Synthesis
Inhibitors
Narrow spectrum Treat red man syndrome by slowing the rate of

i. Glycopeptides: Vancomycin, Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of infusion ; VRSA and VRE are due to D-Ala-D-Lactate formation ;
teicoplanin, telavancin nascent peptidoglycan --> inhibit transglycosylation --> prevent teicoplanin and telavancin are not absorbed in the GIT thus used
elongation and cross-linking of peptidoglycan chain ; For MRSA, PRSP, for bacterial enterocolitis, they are also eliminated unchanged in
as alternative for pseudomembranous colitis red man syndrome, nephrotoxicity, ototoxicity, chills, fever, phlebitis the urine ; decrease dose for renally impaired patients
ii. Peptide Antibiotic: Bacitracin Interferes with a late stage oin cell wall synthesis in gram + organisms ;
For gram + bacteria nephrotoxicity Reserved for topical use only due to marked nephrotoxicity
iii. Antimetabolite: Cycloserine Blocks incorporation of D-Ala into the pentapeptide side chain of the
peptidoglycan ; For drug-resistant TB neurotoxicity (tremors, seizures and psychosis) only used as a second-line agent in TB
iv. Antimetabolite: Fosfomycin inhibits cytosolic enolpyruvate transferase --> prevents formation of N- renal excretion ; resistance emerges rapidly ; synergistic with
acetylmuramic acid (a peptidoglycan precursor molecule) Diarrhea Beta lactam and quinolones
v. Cyclic lipopeptide: Daptomycin same spectrum of activity as Vancomycin ; For VRE, VRSA, for G+ monitoring of CPK is needed, NOT Bactericidal (only destabilizes
acitivity, against endocarditis and sepsis myopathy bacterial cell membrane)
Tetracyclines, Macrolides, Clindamycin, Chloramphenicol, Streptogramins & Oxazolidinones
Inhibits transpeptidation (catalyzed by peptidyl transferase) by blocking given PO and IV ; able to cross the placenta and BBB ; Inhibits
the binding of aminoacyl moiety of the charged tRNA to the acceptor hepatic drug-metabolizing enzymes causing many drug
site o mRNA at 50S subunit, basteriostatic ; For meningitis (Strep interactions ; resistance is due to the formation of
A. Chloramphenicol (broad spectrum pneumonia, H influenza, Neisseria meningitides), back up for acetyltransferase that inactivates drug ; usually used as topical
protein synthesis inhibitor) Salmonella, Rickettsia, Bacteroides, Wide spectrum antibiotic GI disturbance, aplastic anemia, gray baby syndrome agent
Binds 30s ribosomal subunit thus preveting the binding of tRNA to
mRNA, bacteriostatic ; Broad/Wide Spectrum (G+ and G-), For
infections caused by Mycoplasma pneumonia, Chlamydia, Rickettsia, Tigecycline has the broadest spectrum and has the longest t1/2
Vibrio, Spirochetes such as Leptospira, Peptic ulcer disease, Lyme (30-36hrs); do not drink with milk (decreased absorption with
disease, Malaria prophylaxis, Amoebiasis, Acne, Doxycycline is an divalent cations like calcium) ; high Vd, cross the placenta,
alternative to macrolides as initial treatment of CAP, Alternative in enterohepatic recycling ; all are excreted renally EXCEPT
syphilis, treatment of respiratory infection caused by susceptible GI disturbances (enetrocolitis, nausea, diarrhea, vomiting), teratogen Doxycycline (bile) ; Resistance is due to development of efflux
organism, prophylaxis against infection in chronic bronchitis ; Selective (tooth enamel dysplasia/discoloration), hepatotoxicity, nephrotoxicity, pumps for active extrusion of tetracyclines and the formation of
B. Tetracyclines: Tetracycline, uses: Tetracycline (H. Pylori PUD), Doxycycline (Lyme disease and photosensitivity n(esp. demeclocycline), vestibulotoxicity, candidiasis, ribosomal protection proteins that interfere with tetracycline
doxycycline, minocycline, tigecycline, malaria prevention), Minocycline (Meningococcal carrier state), bacterial superinfection with S. aureus and C. difficile, Fanconi binding (but not present with Tigecycline EXCEPT in Proteus and
demeclocycline Demeclocycline (SIADH), Tigecycline (more broad spectrum - MRSA, syndrome Pseudomonas) ; Tigecycline is given IV only
VRE, B-lactamase producing G- bacteria, anaerobes, Chlamydiae,
Mycobacteria)
C. Macrolides
Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; good oral bioavilability but azithromycin absoprtion is impeded by
For community-acquired pneumonia, pertussis, diphtheria, chlamydial food ; All macrolides inhibit CYP450 except azithromycin;
infections ; Eryhthromycin (Campylobacter, Chlamydia, Mycoplasma, azithromycin has highest Vd and slowest elimination;
Legionella, Corynebacterium, Chlamydophila, Legionella, Ureaplasma, telithromycin is used for macrolide-resistance ; Half-lives:
Bordetella, G+ cocci, some G-), Clarithromycin and Azithromycin Erythromycin (2hrs), Clarithromycin (6hrs), Azithromycin (24-
(coverage of Erythromycin plus greater activity against Chlamydia, 48hrs) ; Resistance is due to development of efflux pumps and
Mycobacterium avium, Toxoplasma, Helicobacter, Haemophilus, production of methylase enzyme ; Cross-resistance among
i. Erythromycin, azithromycin, Moraxella, Neiserria) ; Azithromycin is used as an alternative macrolides: complete or partial resistance with drugs acting on
clarithromycin, telithromycin Ceftriaxone in Gonorrhea and to Pen G in syphilis GI disturbance, cholestatic hepatitis, QT prolongation, drug interaction the 50S
a narrow spectrum macrolide, for G+ and anaerobe, low oral GI upset, rashes, eosinophilia, acute cholestatic hepatitis, enzyme as effective as Vancomycin as treatment for C. difficile possibly
ii. Fidaxomicin bioavailability inhibitor with lower relapse rate
Ketolide, structurally related to macrolide, same MOA and spectrum as
erythromycin but macrolide-resistant organisms are susceptible to
iii. Telithromycin telithromycin ; For CAP QT prolongation, enzyme inhibitor, hepatic dysfunction For CAP including multi-drug resistant organisms
Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ;
For anaerobic infections (Bacteroides), alternative against gram + cocci Cross-resistance between clindamycin and macrolides is
(MRSA), endocarditis prophylaxis esp in those allergic to Pens, PCP common ; Resistance is due to methylation of binding sites and
D. Lincosamides: Clindamycin, pneumonia, toxoplasmosis (+ Pyrimethamine), skin and soft tissue GI disturbance, skin rash, neutropenia, hepatic dysfunction, possible enzymatic inactivation ; G- aerobes are resistant because of poor
lincomycin infection superinfection (Pseudomembranous colitis - C. difficile overgrowth) penetration through th eouter membrane
Binds 50s ribosomal subunit, constricting the channel where
polypeptides are extruded thus tRNA synthetase is also inhibited -->
E. Streptogramin: Quinupristin- decreased free tRNA ; For infections caused by drug-resistant gram + Inhibits CYP450 enzymes causing multiple drug interactions ;
Dalfopristin cocci (MRSA, VRSA, PRSP, resistant E. faecium) Injection site reaction, anthralgia-myalgia syndrome BACTERICIDAL
Binds 23S rRNA of 50s ribosomal subunit, inhibit initiation by blockin
formation of the tRNA-ribosome-mRNA ternary complex, bacteriostatic ;
Reserved for infections caused by drug-resistant gram + cocci (MRSA, Thrombocytopenia, neutropenia, serotonin syndrome, neuropathy, Inhibits CYP450 enzymes causing multiple drug interactions ;
F. Oxazolidinone: Linezolid VRE, PRSP), Listeria, Corynebacteria optic neuritis Resistance is due to decreasedaffinity of drug to binding site
Aminoglycosides & Spectinomycin
AG are given IM or IV only, have concentration dependent killing,

General MOA of all aminoglycosides (AG) is by inhibiting is not capabale of penetrating the blood brain barrier, low tissue
protein synthesis by binding to 30s subunit: (1) block penetration, SYNERGISTIC effect with cell wall synthesis
formation of the initiation complex (2) cause misreading of inhibitors due to enhancement of transport to the inside of the
the code on the mRNA template (3) inhibit translocation, nephrotoxicity (reversible - Acute Tubular Necrosis esp in elderly, if bacterial cell ; mechanism of resistance of AG: plasmid-mediated
bactericidal ; For serious infections caused by aerobic gram given with Amphotericin B, Cephalosporin and Vancomycin)), formation of inactivating enzymes "group transferase" -->
– bacteria (E.coli, Enterobacter, Klebsiella, Proteus, ototoxicity (irreversible), neuromuscular blockade (Curare-like block -- catalyze the acetylation of amine functions and the transfer of
Providencia, Pseudomonas, Serratia, Haemophilus, > respiratory paralysis. Remedy: Calcium, Neostigmine and phosphoryl or adenylyl groups to the oxygen atoms of the
Moraxella, Shigella), endocarditis, ocular infections ; If Mechanical Ventilator) ; S. pneumoniae is resistant to Gentamicin, hydroxyl groups of AG, For Streptomycin, resistance is due to
given together with Pens, may be used for Listeria, Enterococci is resistant to amikacin, gentamicin, tobramycin but NOT changes in the ribosomal binding site ; Gentamicin and
A. Gentamycin, tobramycin Enterococcus and G+ cocci streptomycin tobramycin are the most vestibulotoxic and nephrotoxic
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For serious infections caused by aerobic gram
– bacteria (E.coli, Enterobacter, Klebsiella, Proteus,
Providencia, Pseudomonas, Serratia, Haemophilus,
Moraxella, Shigella), endocarditis, ocular infections,
multidrug resistant TB (2nd line) ; If given together with nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular Least resistance and narrowest therapeutic window ; used for
B. Amikacin Pens, may be used for Listeria, Enterococcus and G+ cocci blockade streptomycin-resistant TB
Inhibits protein synthesis by binding to 30s subunit, hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible),
bactericidal ; For TB, tularaemia, bubonic plague, neuromuscular blockade, teratogen (congenital deafness), injection Administered intramuscularly ; if given together with Pens can be
C. Streptomycin brucellosis site reactions used for enterococcal endocarditis, TB plague and tularemia
bactericidal ; For skin infections, bowel preparations for Limited to topical and oral use due to nephrotoxicity, kanamycin
elective surgeries, hepatic encephalopathy, visceral hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible), is most ototoxic ; Neomycin has the most skin reactions (allergic
D. Neomycin, kanamycin, paromomycin leishmaniasis (paromomycin) neuromuscular blockade reactions, contact dermatitis)
bactericidal ; For drug-resistant gonorrhoea, gonorrhoea in nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular
E. Spectinomycin penicillin allergic patients blockade Ototoxcity of AG's can be increased by loop diuretics
bactericidal ; For serious infections caused by aerobic gram hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible), For Treatment of serious infections caused by organisms
F. Netilmicin – bacteria neuromuscular blockade resistant to other aminoglycosides
Sulfonamides, Trimethoprim & Quinolones
A. Sulfonamides: Silver sulfadiazine, mafenide
acetate
i. Short acting: Sulfisoxazole
GI upset, mild hepatic dysfunction, acute hemolysis in G6PD
Inhibits dihydropteroate synthase, bacteriostatic ; For burn deficiency, nephrotoxicity (precipitate in the urine at acidic pH --> low solubility in acidic urine causing formation of stones ;
ii. Intermediate acting: Sulfamethoxazole infections, for G=, G-, Chlamydia and Nocardia, Simple oral crystalluria, hematuria), hypersensitivity (cross-allergenicity with other Resistance is due to plasmin-mediated (decreased intracellular
sulfas (UTI), Sulfacetamide (ocular infection, topical), related drugs such OHAs and diurectics), exfoliative dermatitis, accumulation of the drug, increased production of PABA by
Mafenide and Silver sulfadiazine (burn infection, topical), polyarteritis nodosa, SJS, hematotoxicity (granulocytopenia, bacteria, decreased sensitivity of dihydropteroate synthetase to
Sulfasalazine (Ulcerative colitis and RA, oral), Sulfadizaine thrombocytopenia, aplactis anemia), kernicterus ; Drug Interactions: sulfas and production of dihydrofolate reductase that has
iii. Long acting: Sulfadoxine + Pyrimethamine + Folinic acid (Toxoplasmosis, oral) warfarin, methotrexate, bilirubin decreased affnity for the drug
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; For UTI, respiratory, ear and
sinus infections (Hemophilus, Moraxella, Aeromonas), DOC GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity,
for P. jiroveci pneumonia and Nocardiosis, toxoplasmosis, hypersensitivity, hematotoxicity, kernicterus ; trimethoprim toxicity:
B. Combination: Co-trimoxazole Back-up for cholera typhoid fever shigellosis, G- sepsis, antifolate effects (megaloblastic anemia, leukopenia, Sulfonamides are weakly acidic while Trimethroprim is a weak
(Sulfamethoxazole + Trimethoprim) MRSA, Listeria granulocytopenia) base ; remedy for antifolate effects: Folinic acid supplement
C. Fluoroquinolones
Inhibits DNA replication by binding to DNA gyrase and
topoisomerase IV (G+) and Topoisomerase II (G-),
bactericidal, inhibition of Topoisomerase II results in
blockade of relaxation of supercoiled DNA that is catalyzed General SE: GI distress, skin rashes, HA, dizziness, insomnia,
by DNA gyrase while inhibition of Topoisomerase IV increased LFT, phototoxicity, CNS effects (dizziness, headache),
interferes with the separation of replicated chromosomal tendinitis and tendon rupture, opportunistic infection by Candida and
DNA during cell division ; General use of FQs: For Streptococci ; CI in pregnancy and in children (damage growing
infections of the urogenital and GI tract by G- (gonococci, cartilage --> arthropathy), enhance toxicity of methylxanthines
E. coli, Klebsiela, Campylobacter, Enterobacter, (theophylline) ; Mechanism of resistance for Quinolones: decreased General properties of quinolones: good oral bioavailability, high
Pseudomonas, Salmonella, Shigella), respiratory tract, skin intracellular accumulation via efflux pumps, change in porin structure, Vd, t1/2 3-8hrs, absorption is impeded by antacids, elimination is
and soft tissue infection ; may be used against chnages in sensitivity of target enzyme svia point mutations in the via kidneys by tubular secretion (may compete with probenecid
i. First Generation Fluoroquinolones: meningococcal carrier state, for treatment of TB and antibiotic binding region, mutations in the quinolone resistance for excretion) EXCEPT for MOXIFLOXACIN ; Norfloxacin does
Norfloxacin, Nalidixic acid prophylaxis in neutropenic patients determining region of the gyrA gene that encodes for DNA gyrase not achieve adequte plasma levels for use in systemic infections
Inhibits DNA replication by binding to DNA gyrase and
topoisomerase IV (G+) and Topoisomerase II (G-), GI distress, skin rashes, HA, dizziness, insomnia, increased LFT,
bactericidal, bactericidal ; For UTI and GIT infections (gram phototoxicity, CNS effects (dizziness, headache), tendinitis and high resistance esp for C. jejuni, gonococci, G+ cocci like MRSA,
– rods, gonococci, gram + cocci), atypical pneumonia tendon rupture, opportunistic infection by Candida and Streptococci ; Pseudomonas and Serratia ; are used as alternative to
ii. Second Generation Fluoroquinolones: (Mycoplasma, Chlamydophila), Mycobacteria ; increased CI in pregnancy and in children (damage growing cartilage --> Ceftriaxone and Cefixime in gonorrhea ; Ofloxacin can be used
Ciprofloxacin, ofloxacin activity against G- arthropathy) against C. trachomatis
"Respiratory Quinolones" ; Moxifloxacin and Gemifloxacin are the
newest members of this family and are condisered to have the
broadest spectrum of activity with increased activity aginst
Inhibits DNA replication by binding to DNA gyrase and anaerobes ang atypical agents ; FQ elimination is via kidneys by
topoisomerase IV (G+) and Topoisomerase II (G-), GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, tubular secretion (may compete with probenecid for excretion)
bactericidal, bactericidal ; For lung infections caused by phototoxicity, CNS effects (dizziness, headache), tendinitis and EXCEPT Moxifloxacin ; NEVER use moxifloxacin is UTI ;
gram + cocci, atypical pneumonia (Chlamydia, tendon rupture, opportunistic infection by Candida and Streptococci ; Levofloxacin is used in CAP caused by Chlamydia, Mycoplasma
iii. Third Generation Fluoroquinolones: mycoplasma) ; less G- activity compared to 2nd gen but CI in pregnancy and in children (damage growing cartilage --> and Legionella ; Gemifloxacin, Levofloxacin and Moxifloxacin can
Levofloxacin, Gemifloxacin, Moxifloxacin increased activity against G+ cocci, enterococci, MRSA arthropathy) prolong QT
GI distress, skin rashes, HA, dizziness, insomnia, increased LFT,
Inhibits DNA replication by binding to DNA gyrase and phototoxicity, CNS effects (dizziness, headache), tendinitis and
topoisomerase IV (G+) and Topoisomerase II (G-), tendon rupture, opportunistic infection by Candida and Streptococci ;
iv. Fourth Generation Fluoroquinolones: bactericidal, bactericidal ; has broad spectrum activity CI in pregnancy and in children (damage growing cartilage --> additional SE: diabetes (gatifloxacin), hepatotoxicity
Trovafloxacin, Gatifloxacin (gram – and gram +), enhanced activity against anaerobes arthropathy) QT prolongation (trovafloxacin)
D. Miscellaneous agents
Reactive reduction by ferredoxin forming free radicals that
disrupt electron transport chain, bactericidal ; For anaerobic
or mixed intra-abdominal infections, vaginitis (trichomonas,
gardnerella), pseudomembranous colitis, brain abscess, GI irritation, metallic taste, headache, dark urine, leukopenia,
i. Metronidazole, tinidazole protozoal infections dizziness, ataxia, neuropathy, seizures and disulfiram reaction DOC for amoebiasis, giardiasis and Pseudomembranous colitis
Forms multiple reactive intermediates when acted upon by
bacterial nitrofuran reductase, bactericidal ; For UTI (except GI irritation, skin rashes, pulmonary infiltrates, phototoxicity, single OD dose can prevent recurrent UTI ; acidification of urine
ii. Nitrofurantoin Proteus and Pseudomonas) neuropathies, hemolysis in patients with G6PD deficiency enhances activity ; adjust dose in renal patients
Antimycobacterial Drugs
Most impt drug in TB, prevent neurotoxicity by giving pyridoxine
(vit B6) ; structural congener of pyridoxine ; high level resistance
due to deletion of KatG gene whichh codes for catalase-
peroxidase enzyme involved in bioactivation of INH, low level
Inhibits mycolic acid synthesis, bactericidal ; For TB, for hepatotoxicity, neurotoxicity (seizures, peripheral neuritis, insomnia, resistance due to deletion og inhA gene which encodes the
latent infection, given as a sole drug for prophylaxis of restlessness, muscle twitching), acute hemolysis in G6PD deficiency, target enzyme which is an acyl protein reductase ; Potent
A. Isoniazid (nicotinic acid derivative) close contacts and skin test converters drug-induced lupus CYP450 inhibitor
Potent CYP450 inducer ; rapid development of resistance if used

Inhibits DNA-dependent RNA polymerase, bactericidal ; For alone ; resistance is due to changes of drug sensitivity of the
TB, leprosy, prophylaxis for meningococcal and polymerase enzyme; undergoes enterohepatic recirculation ;
staphylococcal carrier states, drug-resistant infections orange-colored metabolites ; delay emergence of resistance to
(MRSA, PRSP) when given together with Vancomycin, can dapsone ; Rifabutin is equally effective as anti-mycobacterial
be used as sole drug in the treatment of latent TB in INH- red-orange urine, light chain proteinuria, skin rash, thrombocytopenia, agent with less drug interaction and it is the preferred anti-TB for
B. Rifamycin derivatives: Rifampicin, rifabutin, intolerant patient or in close contact of patients with INH- nephritis, hepatotoxicity, flulike syndrome, anemia, impair antibody AIDS patients ; Rifamixin is not absorbed in the GIT and is used
rifapentine, rifamixin resistant strains of the organism response for traveler's diarrhea
Inhibits arabinosyl transferases involved in the synthesis of dose-dependent visual disturbances (decreased visual acuity, red Resistance is due to mutation in emb gene ; dose adjustment id
arabinogalactan in mycobacterial cell wall, bacteriostatic ; green color blindness, retrobulbar neuritis, retinal damage, optic needed in renal patients ; always used in combination with other
C. Ethambutol (butanol derivative) For TB neuritis), headache, confusion, hyperuricemia, peripheral neuritis drugs for TB
Most hepatotoxic anti-TB drug, also known as sterilizing agent ;
require metabolic conversion via pyrazinamidases in MTb ;
Unknow MOA, bacteriostatic but can be bactericidal on hepatotoxicity, nongouty polyarhtralgia, asymptomatic hyperuricemia, resistance is via mutation in pncA gene which codes for
actively dividing mycobacteria, is metabolozed to pyrazinoic myalgia, GIT irritation, maculopapular rash, porphyria, photosensitivity pyrazinamidases and increased efflux systems ; decrease dose
D. Pyrazinamide (pyrazine derivative) acid, t 1/2 is increased in liver and kidney disease ; For TB ; CI in pregnancy in hepatic and renal patients
E. Streptomycin (aminoglycoside) for MDRTB (TB meningitis, miliary TB, severe organ TB) see entry see entry
Drugs for Leprosy
Most active drug against M. leprae ; used in combination with
Inhibition of folic acid synthesis, bacteriostatic ; For leprosy, GI irritation, fever, skin rashes, methemoglobinemia, acute hemolysis rifampicin and clofazimine ; Acedapsone is a repository form of
A. Sulfones: Dapsone, acedapsone alternative for PCP pneumonia in G6PD deficiency patients dapsone which has drug action that can last for several months
Binds to guanine bases in bacterial DNA, bactericidal ; For
B. Clofazimine leprosy GI irritation, skin discoloration a phenazine dye
Antifungal Agents
Control infusion reactions by slowing the rate of infusion and
Binds to ergosterol in fungal cell membranes, forming premedication with antihistamines, additive nephrotoxicity with
artificial pores, fungicidal, WIDEST antifungal spectrum ; other nephrotoxic drugs (aminoglycosides) ; highly lipid soluble,
For systemic fungal infections (aspergillus, blastomyces, infusion reactions (chills, fever, muscle spasms, vomiting, poorly absorbed in the GIT ; high Vd except in the CNS with a
candida, Cryptococcus, histoplasma, mucor), for initial hypotension), dose limiting nephrotoxicity (decreased GFR, ATN with t1/2 of 2weeks ; resistance is due to decreased level of
induction before followup treatment with azoles, can be magnesium and potassium wasting, decreased erythropoietin), ergosterol or change in membrane structure ; has the WIDEST
A. Polyene antifungal: Amphotericin B used topically in mycotic corneal ulcers and keratitis neurotoxicity (seizure, neuronal damage) antifungal spectrum
Accumulated in fungal cells by the action of permease and
converted by cytosine deaminase to 5-FU, which inhibits
thimidylate synthase, pyrimidine antimetabolite, fungistatic ;
given together with ampho B and Triazoles - For decrease dose in renal patients ; resistance is due to decreased
cryptococcal infection, systemic candidal infections, activity of fungal permease and deaminase ; has synergistic
B. Flucytosine chromoblastomycosis reversible myelosuppresion, alopecia, hepatotoxicity effect when given with ampho B and Triazoles.
C. Azole Antifungals
Inhibit 14α-demethylase --> decreased ergosterol Limited to topical use because of systemic toxicity ; narrow
production --> increased permeability of cell membrane, antifungal spectrum ; resistance is due to chnages in the
Inhibits fungal P450-dependent enzymes blocking sensitivity of target enzyme ; Potent CYP450 inhibitor ;
ergosterol synthesis, fungistatic ; For chronic GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, drug Ketoconazole is rarely used due to drug interactions and narrow
i. Ketoconazole (Imidazole) mucocutaneous candidiasis, dermatophytosis interaction, gynecomastia, menstrual irregularities and infertility spectrum
Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell membrane,
Inhibits fungal P450-dependent enzymes blocking
ergosterol synthesis, fungistatic ; DOC for candidiasis
(esophageal, oropharyngeal, vulvovaginitis),
coccidioidomycosis, cryptococcal meningitis (treatment and alternative to Ampho B in the treatment of C. neoformans, as
ii. Fluconazole (Triazole) prophylaxis) GI disturbances (vomiting, diarrhea), rash, hepatotoxicity effective as Ampho B in candidemia
ergosterol synthesis, fungistatic ; DOC for blastomycosis,
sporotrichosis, dermatophytosis esp onchomycosis,
chromoblastomycosis ; alternative for infections due to
Aspergillus, Coccidioides, Cryptococcus and Histoplasma ,
iii. Itraconazole (Triazole) for esophageal candidiasis resistant to fluconazole GI disturbances (vomiting, diarrhea), rash, hepatotoxicity may also be used for subcutaneous chromoblastomycosis
ergosterol synthesis, fungistatic ; co-DOC for invasive
aspergillosis, alternative in candidemia, for fluconazole-
resistant organisms, for candidal esophagitis and stomatitis GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, blurring of
iv. Voriconazole (Triazole) in AIDS patients vision in 30% of patients, CI in pregnancy wider specturm azole
ergosterol synthesis, fungistatic ; For Candida and
Aspergillus, as prophylaxis of fungal infection during cancer BROADEST spectrum triazole ; the only azole with activity
v. Posaconazole (Triazole) chemotherapy, salvage therapy in invasive aspergillosis GI disturbances (vomiting, diarrhea), rash, hepatotoxicity against Rhizopus sp. (mucormycosis) ; Potent CYP450 inhibitor
ergosterol synthesis, fungistatic ; For mucocutaneous
candidiasis, dermatophytosis, seborrheic dermatitis,
vi. Clotrimazole, miconazole, ketoconazole pityriasis versicolor None when administered topically Limited to topical use because of systemic toxicity
Inhibit beta-glucan synthase which produces β(1-->2)
glycan which is a cellwall component, thus decreasing
fungal cell wall synthesis, fungostatic ; For disseminated
and mucocutaneous candidiasis who fail to respond to
D: Echinocandins: Caspofungin, anidulafungin, amphoB, for mucormycosis, salvage therapy for invasive headache, GI distress, rash, fever, flushing (histamine release), all are given IV ; micafungin can increase levels of cyclosporine
micafungin aspergillosis elevated liver enzymes and tacrolimus
Interferes with microtubule function in dermatophytes, headache, mental confusion, GI irritation, photosensitivity, given PO ; Accumulates in keratin ; potent CYP450 inducer ;
inhibits synthesis and polymerization of nucleic acids, hepatotoxicity, disulfiram reaction, drug interactions (decreases absorption is increased by intake of fatty meal ; resistance is due
E. Griseofulvin fungistatic ; For dermatophytosis bioavialability of warfarin) ; contraindicated in porphyria to decreased transport of drug into the fungal cell wall
Inhibits withg ergosterol synthesis by inhibiting fungal
squalene oxidase leading to increased squalene which
interferes with ergosterol synthesis, fungicidal ; For given PO and topical, also accumulates in keratin, more effective
F. Terbinafine dermatophytosis, onchomycosis GI upset, rash, headache, taste disturbances than griseofulvin in onchomycosis
Binds to ergosterol in fungal cell membranes, forming
artificial pores, fungicidal ; For candidiasis ((oropharyngeal,
esophageal and vaginal), for GI fungal infections in patients Minimal mucocutaneous absorption, available as swish and
G. Nystatin (polyene) with impaired defense mechanisms nephrotoxicity (severe) swallow preparation
Antiviral Agents
A. Anti-Herpes
Activated by viral thymidine kinase (TK) to forms that inhibit
viral DNA polymerase, guanosine analog, competitive given PO, topical and IV ; dose adjustment in renal patients ; No
substrate for DNA polymerase, causes chain termination activity against strains of HSV with absent thymidine kinase
after its incorporation into the viral DNA ; For infections due activity ; resistance is due to changes in viral DNA polymerase ;
to HSV1, HSV2, VZV (mucocutaneous and genital herpes, Valacyclovir is a prodrug that is converted to Acyclovir and
prophylaxis in AIDS and in other Immunocompromised reached plams levels 3-5x (longer t1/2) more than acyclovir ;
i. Acyclovir, valacyclovir, penciclovir, famciclovir, states such as organ transplant patients, herpes nausea, diarrhea, headache, delirium, tremor, seizures, hypotension, Penciclovir does not cause chain termination ; Famciclovir is a
docosanol encephalitis, neonatal HSV infection etc. nephrotoxicity prodrug which is converted to Penciclovir in vivo
Inhibits fusion between the HSV envelope and plasma nausea, diarrhea, headache, delirium, tremor, seizures, hypotension,
ii. Docosanol membrane, prevents viral entry and subsequent replication nephrotoxicity topical preparation shortens healing time
given as IV or intraocular implant (for CMV retinitis) ; No activity

Inhibits viral DNA polymerase causing chain termination, against strains of HSV with absent thymidine kinase activity ;
guanosine derivative ; For infections due to CMV, HSV1, CMV resistance is due to mutation in viral DNA polymerase and
HSV2, VZV ; For prohylaxis and treatment of CMV retinitis in the genes that code for the activating viral phosphotransferase
and other CMV infections in the immunocompromised leukopenia, thrombocytopenia, mucositis, hepatotoxicity, seizures, ; Valganciclovir is a prodrug of ganciclovir with increased oral
iii. Ganciclovir, valganciclovir (anti-CMV) patients neutropenia bioavialability
Inhibits viral DNA polymerase causing chain termination ;
For CMV retinitis, mucocutaneous HSV infections, Active against strains of HSV with absent thymidine kinase
acyclovir-resistance, ganciclovir-resistance, genital warts activity ; resistance is due to mutation in DNA polymerase ; dose
iv. Cifodovir (anti-CMV) and molluscum contangiosum nephrotoxicity adjustment in renal patients
Inhibits viral RNA polymerase, DNA polymerase, and HIV
reverse transcriptase, binds to pyrophosphate binding site ; Active against strains of HSV with absent thymidine kinase
as alternative for prophylaxis and treatment of CMV activity ; does not require phosphorylation for antiviral activity ;
retinitis, gancyclovir-resistant strains of CMV, HSV infection nephrotoxicity, electrolyte abnormalities (hypocalcemia), GU resistance is due to mutations in DNA polymerase gene ; dose
v. Foscarnet (anti-CMV) in patients with AIDS, also used in organ transplantation ulcerations, CNS effects (headache, hallucination, seizures) adjusment in renal patients
GI irritation, paresthesia, tremor, convulsion, hepatic dysfunction, CI in used topically only because it is rapidly metabolized into the
vi. Vidarabine adenine analog ; For HSV, VZV, CMV pregnancy inactive form and because it has a toxic potential
vii. Idoxuridine, trifluridine pyrimidine analogs ; For herpes keratitis (HSV-1) irritation, blurred vision, photophobia topical only because it is too toxic fo systemic use
antisense oligonucleotide that binds to mRNA of CMV injected intravitreally ; concurrent systemic use of anti-CMV in
causing inhibition of early protein synthesis ; For CMV threapy is recommended to protect against extraocular and
viii. Fomivirsen retinitis iritis, vitritis, increased IOP, changes in vision contralateral retinal CMV disease
B. Drugs for HIV
Inhibit HIV reverse transcriptase after phosphorylation by these are prodrugs converted by host cell kinases tp
cellular enzymes, acts as chain terminators via insertion triphosphates causing competitive binding of natural nulecotides
into the growing DNA chain ; For HIV infection, prevention to the dNTP-binding site of Reverse Transcriptase ; resistance is
i. NRTI: of maternal-fetal HIV transmission see specific drugs below due to mutation in pol gene
a. Abacavir guanosine analog hypersensitivity reaction good oral bioavailability, T1/2 is 12-24hrs, resistance is slow
acute pancreatitis, peripheral neuropathy, diarrhea, hepatic oral bioavailability is decreased by food and chelating agents ;
b. Didanosine (ddI) NRTI dysfunction, hyperuricemia, CNS effects dose adjustment in renal patients
aesthenia, GI upset, headache, hyperpigmentation of palms of soles,

c. Emtricitabine NRTI CI in pregnancy, children, renal and hepatic and patients per orem once a day treatment, dose adjustment in renal patients
80% oral bioavailability ;may also be used for Hepa B infection ;

d. Lamivudine (3TC) NRTI GI upset, headache, fatigue, insomnia HAART, dose adjustment in renal patients
peripheral neuropathy esp if given together with Zalcitabine, lactic
e. Stavudine (d4T) NRTI acidosis with hepatic steatosis good oral bioavailability, dose adjustment in renal patients
a nucleotide but acts as NRTI, competitively inhibits RT, oral bioavailabilty is 25-40% ; halflife is 60hours ; also used
f. Tenofovir cause chain termination after incorporation into DNA GI upset, asthenia, headache, Fanconi syndrome, AKI against HBV
peripheral neuropathy, pancreatitis, esophageal ulceration, stomatitis,
g. Zalcitabine (ddC) NRTI arthralgias increased oral bioavailability, dose adjustment in renal patients
BM suppression (anemia, neutropenia, thrombocytopenia), acute dose adjustment in uremic patients and cirrhosis ; affected by
h. Zidovudine (ZDV) Azidothymidine or AZT cholestatic hepatitis, agitation, insomnia, myalgia, headache, GI upset enzymes inducers and inhibitors
Inhibits HIV reverse transcriptase, no phosphorylation
ii. NNRTI: Delavirdine, efavirenz, etravirine, required, do not compete with nucleoside triphosphate ; For Delavirdine and Nevirapine (rash, increased AST/ALT, Efavirenz binds to a different binding site ; resistance is due to mutations in
nevirapine HIV infection (teratogenicity), Etravirine (increased cholesterol and triglycerides) pol gene
metabolized by CYP3A4 and CYP2D6, affected by enzyme
a. Delavirdine NNRTI rashes, teratogenic inducer and inhibitor
enhanced absorption by fatty meals, drug interactions are
b. Efavirenz NNRTI CNS dysfunction, skin rash, increased plasma cholesterol, teratogenic common
nausea, vomiting, diarrhea, increased cholesterol, triglycerides and
c. Etravirine NNRTI, for drug-resistant HIV LFTs NEWEST NNRTI
used as a singledose to prevent HIV vertical transmission
d. Nevirapine at the onset of labor and also given to the neonate rash, SJS, TEN good oral bioavailability,t1/2 is >24hours
General SE: hyperglycemia, insulin resistance, hyperlipidemia, altered
body fat distribution (buffalo hump, gynecomastia, truncal obesity,
iii. Protease Inhibitor: Atrazanavir, Darunavir, cleaves precursor polyprotein to form the final structural facial and peripheral lipodystrophy) due to the inhibition of lipid-
Fosamprenavir, Indinavir, Nelfinavir, Lopinavir- protein of the mature virion core, inhibits viral protein regulating proteins which have active sites with structural homology to Resistance is due to mutation in pol gene ; are potent CYP3A4
Ritonavir, Saquinavir, Tipranavir processing ; For HIV infection that of HIV protease inhibitor esp Ritonavir
per orem absorption requires acidic environment ; can penetrate

CSF and seminal fluid ; is not associated with dyslipidemia, fat
a. Atazanavir Protease Inhibitor peripheral neuropathy, skin rash, hyperbilirubinemia, QT prolongation deposition or metabolic syndrome ; CYP3A4 and 2C9 inhibitor
b. Darunavir Protease Inhibitor rash, hepatotoxicity, hypersensitivity ; CI in patients with sulfa allergy Given together with Ritonavir in patients resistant to other PIs
GI upset, paresthesia, rash, CI in pregnant patients and children if

drug uses propylene glycol as solvent ; does not have risk for
hyperlipidemia, fat maldistribution, hyperglycaemia and insulin a prodrug that is converted to the active drug Amprenavir ;
c. Fosamprenavir Protease Inhibitor resistance absorption is impaired by fatty food ; used with lowdose Ritonavir
nausea, vomiting, diarrhea, thrombocytopenia, hyperbilirubinemia, decreased bioavailability in the presence of food ; affected by
d. Indinavir Protease Inhibitor nephrolithiasis, insulin resistance enzyme inhibitors and inducers
used as a combination drug: uses subtherapeutic dose of
ritonavir which inhibits CYP3A4 mediated metabolism of there is increased compliance with this drug ; Ritonavir has
e. Lopinavir-Ritonavir lopinavir GI upset (well-tolerated side effects) “boosting effect” on other PI due to enzyme inhibitory effect
absorption is increased by food, short half-life ; has the most
f. Nelfinavir Protease Inhibitor Diarrhea favorable safety profile for pregnancy
Protease Inhibitor ; subtherapeutic doses inhibit CYP3A4-
mediated metabolism of other Pis (Indnavir, Lopinavir, good oral bioavailability esp when taken with meals ; affected by
g. Ritonavir Saquinavir) which permits lower dose of the other PI GI upset, bitter taste, paresthesia, increased LFT's enzyme inducer and inhibitors
Protease Inhibitor ; given together with low dose Ritonavir
h. Saquinavir to improve compliance and decrease GI upset nausea, vomiting, diarrhea, dyspepsia, rhinitis affected by enzyme inducers and inhibitors
newer drug ; induces P-glycoprotein transporters which leads to
i. Tipranavir Protease Inhibitor ; given with Ritonavir for PI-resistant HIV GI upset, rash, hepatotoxicity alteration of GI absorption of other drugs
iv. Entry inhibitors:
Binds to gp41 subunit of viral envelope glycoprotein,
preventing fusion of viral and cellular membranes ; For
previously drug-treated patients with persistent HIV injection site reaction, hypersensitivity reaction, increased incidence of
a. Fusion Inhibitor: Enfuvirtide, Docosanol replication despite ongoing therapy bacterial pneumonia subcutaneous and usually given together with other HIV agents
Blocks viral attachment by blocking CCR5, a
transmembrane protein involved in the attachment of HIV to good tissue penetration ; affected by enzyme inhibitors and
b. CCR5 receptor antagonist: Maraviroc host cell ; For HIV infection cough, diarrhea, muscle and joint pains, increased LFTs inducers
C. Drugs for Influenza
Amantadine is also used in treating parkinsonism ; should be
given within 48hrs of exposure ; Rimantadine has longer halflife
Inhibit early step replication and prevent uncoating by GI irritation, dizziness, cerebellar dysfunction (ataxia, dysarthria), and doe snot need dose-adjustment for renally-impaired Px ;
i. Uncoating inhibitors: Amantadine, rimantadine binding to M2 proton channels ; For influenza A and rubella livedo reticularis there is increased resistance observed with amantadine
Inhibits neuraminidase which cleaves sialic acid residues
from viral proteins and surface proteins of infected cells ,
ii. Neuraminidase inhibitors: Oseltamivir, decrease release of progeny virus ; For influenza A and B, GI effects (Oseltamivir), bronchospasm in asthmatics and cough with DOC for influenza (including H1N1) ; Oseltamivir is PO while
zanamivir shortens duration of symptoms throat discomfort (Zanamivir ) Zanamivir is intranasal
D. Drug for HBV and HCV
cytokine, increased activity of JAKS leading to
phosphorylation of signal transducers and activation of
transcription (STATS) which causes increased formation of
antiviral proteins , also increases NK cells that destroy
infected liver cells, Degrades viral RNA via activation of
host cell RNAse (ribonuclease) ; For chronic HBV, HCV alopecia, myalgia, severe depression, flu-like syndrome, thyroid
infection, Kaposi sarcoma, genital warts, prevents dysfunction, reversible hearing loss, neutropenia ; Contraindications slow absorption, given IM or SC once a day 3x week but the
dissemination of HZV in cancer patients and decreased include autoimmune disease, history of cardiac arrhythmia and PEG-form is only given once a week, given topically for genital
i. Interferon-α CMV shedding after renal transplantation pregnancy warts
Dipiroxil is a prodrug of Adefovir ; Telbivudine is a newer drug

Inhibits HBV DNA polymerase causing chain termination (nucleoside analog) but develpoment of resistance is rapid, it is
after incorporation into the viral DNA ; For lamivudine- as effective as lamivudine ; Tenofovir is an anti-RT drug that is
resistant Hepatitis B infection, suppresses HBV replication also effective in chronic HBV, it is active against lamivudine and
ii. Adefovir, Dipivoxil, Telbivudine, Tenofovir and improves liver histology and fibrosis Lactic acidosis, renal toxicity, severe hepatomegaly with steatosis entecavir-resistant strains
iii. Entecavir guanosine nucleoside, inhibits DNA polymerase headache, dizziness, fatigue, nausea is as effective as lamivudine, longer t1/2 of 12hrs
Coinfection between HBV and HIV may increase the risk of

see entry, also active for HBV, rapidly suppresses HBV pancreatitis with lamivudine use ; longer t1/2 in HBV infected
iii. Lamivudine (3TC) replication see entry cells than in HIV (lower dose required in HBV than in HIV)
Inhibits guanosine triphosphate formation, prevents
capping of viral mRNA, blocks RNA-dependent RNA
polymerase, inhibit replication of many DNA and RNA
viruses like Influenza A and B, parainfluenza, paramyxo
viruses, HCV and HIV ; For HCV infection (with IFN-α) and given PO, IV or aerosol, avoid concomitant administration of
RSV infection, decreases mortality in viral hemorrhagic anatcids ; Early IV administration of ribavirin decreases mortality
iii. Ribavirin fevers haemolytic anemia, conjunctival and bronchial irritation, teratogen in viral hemorrhagic fevers ; monotherapy is NOT effective
Antiprotozoal Drugs
A. Antimalarial drugs
accumulates in the food vacuole of plasmodia —> Prevents
polymerization of heme into hemozoin —> inc heme
concentration which is toxic to the parasite, Blood
schizonticide ; For malaria (non-falciparum, chloroquine-
sensitive), DOC for acute attacks of non-Falciparum and May precipitate porphyria ; Chloroquine is 4-aminoquinoline
sensitive Falciparum malaria, used as chemoprophylaxis derivative, can be given PO and has high Vd, absorption is
except in regions where P. falciparum is resistant, for GI irritation, skin rash, headache, severe skin lesions, peripheral decrease by antacids ; resistance is due to dec. intracellular
autoimmune diseases such as rheumatoid arthritis, neuropathies, myocardial depression, retinal damage, auditory accumulation via inc activation of membrane pumps, dec
i. Chloroquine, hydroxychloroquine amoebic liver abscess impairment, psychosis intravacuolar accumulation via transporter encoded by pfcrt gene
Complexes with double stranded DNA to prevent strand
separation —> blocks DNA replication and transcription to
RNA, blood schizonticide ; For malaria (chloroquine-
resistant) and severe falciparum malaria (quinidine), given cinchonism (headache, tinnitus, vertigo), hemolysis in G6PD Quinine is commonly used with doxycycline or clindamycin to
together with Doxycycline and or Clindamycin to shorten deficiency, blackwater fever, blurring of vision, GI upset, disturbance n limit toxicities, PO and IV (in severe infection) ; NEVER use as
ii. Quinine, Quinidine gluconate duration of disease cardiac conduction ; CI in pregnancy prophylaxis
Unknown MOA, blood schizonticide ; For
chemoprophylaxis (chloroquine-resistant areas) ; 1st line
drug (weekly administration) for prophylaxis in all areas
with Chloroquine resistance), alternative to quinine in acute GI distress, skin rash, headache, dizziness, cardiac conduction
attacks and uncomplicated infections from falciparum defects, psychiatric disorders (psychosis), neurologic symptoms,
iii. Mefloquine malaria seziures is a 4-quinoline derivatives, PO
8-aminoquinoline, Forms quinoline-quinone metabolites
which are electron-transferring redox compounds that act
as cellular oxidants, tissue schizonticides, gametocides ;
For malaria, eradicates liver stages of P. vivax and P. ovale
(radical cure of P. vivax and P. ovale), alternative as Eradicates hypnozoites in the liver, preventing malarial relapse,
primary prevention, terminal prophylaxis (vivax, ovale), GI distress, pruritus, headaches, methemoglobinemia, hemolysis in PO , should be used with a blood schizonticide, 14-day course of
iv. Primaquine PCP pneumonia G6PD deficient patients ; CI in pregnancy Tx after Tx with choloroquine
Atovaquone disrupts mitochondrial electron transport, blood
and tissue schizonticide, proguanil inhibits folate synthesis,
sporonticide ; For treatment and chemoprophylaxis of also effective against Mefloquine-resistant Falciparum infection ;
chloroquine-resistant falciparum, protective vs. Mefloquine- abdominal pain, nausea, vomiting, diarrhea, headache, rash, Proguanil has a t1/2 12-16h ; Atovaquone is an alternative for P.
v. Atovaquone-proguanil resistant falciparum increased liver enzymes jiroveci infection
Sequential blockade of folic acid synthesis (sulfadoxine
blocks Dihyrodpteroate synthetase, Pyrimethamine blocks GI disturbances, teratogen (enamel dysplasia and discoloration),
Dihydrofolate reductase, blood schizonticide and hepatotoxicity, nephrotoxicity, photosensitivity, vestibulotoxicity, t1/2 is usually >100h, PO, highly protein bound ; pyrimethamine
vi. Sulfadoxine-pyrimethamine (Fansidar) sporonticide ; For malaria (for Chloroquine-resistant) hemolysis is a sporonticide
Impairs progeny of malarial apicoplast genes, resulting in
abnormal cell division, blood schizonticide ; For GI disturbances, teratogen (enamel dysplasia and discoloration),
vii. Doxycycline chemoprophylaxis in multi-drug resistant strains hepatotoxicity, nephrotoxicity, photosensitivity, vestibulotoxicity Do not drink with milk (decreased absorption), PO
Unknown MOA, active vs the erythrocytic stage of all 4 Lumefantrine used in combination with artemether (Co-arthem)
strains including Chloroquine-resistant, blood schizonticide for uncomplicated falciparum infection ; Halofantrine is never
; For chloroquine-resistant malaria and severe falciparum abdominal pain, diarrhea, vomiting, cough, rash, headache, pruritus, used for prophylaxis because of cardiotoxicity and
viii. Halofantrine , lumefantrine malaria elevated liver enzymes, cardiotoxicity, teratogen embryogenecity, Lumefantrine has minimal cardiotoxicity
Co-artem is the DOC for uncomplicated falciparum malaria in the
Philippines ; Combination therapy of artemesinins with one or two
long-acting antimalarial drugs (amodiaquine, mefloquine,
sulfadoxine/pyrimethamine or lumefantrine) is favored to retard
is metabolized in the food vacuole of protozoa —> Forms the development and progression of drug resistance in P.
ix. Artemsinin, artesunate, artemether, toxic free radicals in malarial food vacuole, blood falciparum ; not given as Prophylaxis due to short t1/2 (1-3h) ;
dihydroartemsinin schizonticide ; For malaria (falciparum and MDR strains) nausea, vomiting, diarrhea ; SAFE in pregnancy the only reliably effective meds vs Quinine-resistant strains
MOA same as chloroquine (inhibits the digestion of
x. Amiodaquine hemoglobin) ; For chloroquine-resistant falciparum agranulocytosis, aplastic anemia low-cost, given as combination with Artesunate
B. Anti-amoebiasis
Unknown MOA, converted to Diloxanide freebase (active
amobecide), luminal amebicide ; DOC for asymptomatic converted in vivo into Diloxanide freebase which is the
i. Diloxanide Furoate cyst carrier of E. histolytica flatulence, nausea, abdominal cramps amoebicide
Inhibits protein synthesis by blocking ribosomal movement

along messenger RNA, tissue amebicide ; back up drug for Reserved only for situations where metronidazole can’t be used ,
ii. Emetine, dehydroemetine severe intestinal, hepatic and extraintestinal amebiasis GI distress, muscle weakness, CV dysfunction (arrhythmias and CHF) given SC or IM , usually given together with luminal amebicides
halogenated hydroxyquinoline, Unknown MOA, luminal
amebicide ; Alternative to Diloxanide for mild to severe GI distress, thyroid enlargement, skin reactions due to iodine toxicity,
ii. Iodoquinol intestinal amebiasis neurotoxicity (peripheral neuropathy, visual dysfunction) Usually used in combination with metronidazole, PO
Reactive reduction by ferredoxin forming free radicals that
disrupt electron transport chain, tissue amebicide ; DOC given PO, IV or topical, Metronidazole t1/2 is 6-8h, Tinidazole
for severe intestinal wall disease and in hepatic abscess t1/2 is 12-14h; dose adjustment in renal patients, well distributed
and other extra intestinal amebic disease, DOC for GI irritation, metallic taste, headache, dark urine, leukopenia, even in CSF ; active against protozoan and bacteria (Bacteroides
trichomoniasis, also used for giardiasis, bacterial vaginosis dizziness, ataxia, neuropathy, seizures, disulfiram reaction, and Clostridium, DOC for Pseudomembranous colitis) ; causes
iii. Metronidazole, Tinidazole, Secnidazole (Gardnerella vaginalis), anaerobic infections, H. pylori PUD opportunistic infections, parestheisa, CI in pregnancy potentiation of warfarin action ; bets taken with meals
An aminoglycoside, Inhibits protein synthesis, binds to 16S may be given together with tetracycline in mild intestinal disease
ribosomal subunit, luminal amebicide ; For intestinal ; superior to Diloxanide in asymptomatic carries but SE limits its
iv. Paromomycin amebiasis, cryptosporidiosis headaches, dizziness, rashes, arthralgia use
Reactive reductions by ferredoxin forming free radicals that
disrupt electron transport chain, tissue amebicide ; For
metronidazole-resistant amebiasis, giardiasis,
v. Nitazoxanide cryptosporidiosis (DOC) GI distress may also be used in helminthic infections
C.Drugs for Pneumocystis and Toxoplasmosis
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; DOC for prophylaxis and
treatment of Pneumocystosis, prophylaxis (T. gondii, I. GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity,
i. Co-trimoxazole belli) hypersensitivity, hematotoxicity, kernicterus Recommended at CD4 count < 200, given daily, PO or IV
Unknown MOA but may involve inhibition of glycolysis or
interference with NA metabolism of Protozoans and Fungi ; respiratory stimulation followed by depression, hypotension,
For prophylaxis and treatment of pneumocystosis and hypoglycaemia, anemia, neutropenia, hepatitis, pancreatitis, inhalant Administered by nasal spray/aerosol, given once a month if used
ii. Pentamidine trypanosomiasis route has minimal SE for prophylaxis, IV or IM for 21 days if for Tx of active disease
Sequential blockade of dihydropteroate synthase gastric irritation, glossitis, neurologic symptoms (headache, insomnia, an alternative drug for Toxoplasmosis is Clindamycin ,give daily
(sulfadiazine) and dihydrofolate reductase (pyrimethamine) tremors, seizures), hematotoxicity (megaloblastic anemia, for 3-4 weeks if for Tx of active toxoplasmosis , if for Toxoplasma
iii. Pyrimethamine-sulfadiazine ; DOC for prophylaxis and treatment of toxoplasmosis thrombocytopenia), pseudomembranous colitis (clindamycin) encephalitis, give for at least 6 weeks
Atovaquone disrupts mitochondrial electron transport ; For
mild to moderate PCP, as chemoprophylaxis for abdominal pain, nausea, vomiting, diarrhea, fever, increased liver
iv. Atovaquone Chloroquine resistant malaria (with Proguanil) enzymes has increased absorption in the presence of food, PO
D. Drugs for Trypanosomiasis
Unknown MOA but may involve inhibition of glycolysis or
interference with NA metabolism of Protozoans and Fungi ;
For hemolymphatic stage of T. gambiense and T. respiratory stimulation followed by depression, hypotension,
rhodiense, For prophylaxis and treatment of hypoglycaemia, anemia, neutropenia, hepatitis, pancreatitis, inhalant do not use for latter stages because it does not cross the BBB,
i. Pentamidine pneumocystosis route has minimal SE also used for Kala-azar and PCP
Polyanionic compound, Unknown MOA ; DOC for early fatigue, nausea, vomiting, seizures, shock fever, rash, headache,
hemolymphatic stages of African sleeping sickness, paresthesia, neuropathies, renal abnormalities (proteinuria), chronic Do not cross blood brain barrier , Used in combination with
ii. Suramin Alternative to Ivermectin in onchocerciasis diarrhea, haemolytic anemia and agranulocytosis melarsoprol
Suicide inhibitor of ornithine decarboxylase ; DOC for
iii. Eflornithine advanced west African sleeping sickness diarrhea, vomiting, anemia, thrombocytopenia, leukopenia, seizures Crosses blood brain barrier, PO, IV
Organic arsenical, inhibits enzyme sulfhydryl (-SH) groups Crosses BBB, administered parenterally because it causes GI
iv. Melarsoprol in trypanosomes ; DOC for African sleeping sickness GI irritation, reactive encephalopathy upset
Nitrofurazone derivative, Inhibits trypanothione reductase
which is unique to the parasite ; DOC for Chagas disease /
American Sleeping sickness (Trypanosoma cruzi),
alternative for African sleeping sickness, also for nausea, vomiting, fever, rash, restlessness, insomnia, neuropathies,
v. Nifurtimox mucocutaneous leishmaniasis seizures Does not cross BBB
Drugs for Leishmaniasis
IV ; alternative for leishmaniasis are as follows: Pentamidine or
Miltefosine (for visceral leishmaniasis), Fluconazole or
Pentavalent antimony, Inhibits glycolysis or effects on NA GI symptoms, fever, rash, arthralgia, healdache, myalgia, sterile Metronidazole (for cutaneous leishmaniasis) and Amphotericin B
vi. Sodium Stibogluconate metabolism ; DOC for Leishmaniasis abscesses, cardiotoxicity (for mucocutaneous leishmaniasis)
Anthelmintics
Selectively inhibits microtubule synthesis and glucose
uptake in nematodes, ovicidal ; Also a primary drug
(together with albendazole) for ascariasis, pinworm and
A. Mebendazole whipworm ; alternative for visceral larva migrans GI irritation, agranulocytosis, alopecia ; CI in pregnancy Greatly affected by enzyme inducers and inhibitors
Inhibits microtubule assembly, larvicidal and ovicidal ; DOC
for ascariasis, hookworm, whipworm, hydatid disease ,
alternative for threadworms, filariasis, larva migrans, reversible leukopenia, alopecia, elevation of liver function tests, bone primary drug for ascariasis, ancylostomiasis, trichuriasis ; safety
B. Albendazole cysticercosis, trichuriasis marrow suppression in pregnant and children is not yet established
Immobilizes microfilariae by an unknown mechanism —>
inc susceptibility to host defense mechanism ; DOC for headache, malaise, weakness, anorexia, filarial fever (fever, rashes,
C. Diethylcarbamazine filariasis and eye worm disease (Loa-Loa) ocular damage, joint and muscle pain, lymphangitis) May cause mazzotti reaction when used for onchocerciasis
Intensifies GABA-mediated neurotransmission in
nematodes —> immobilizes parasites —> removal by
reticuloendothelial system ; DOC for onchocerciasis, Mazzotti reaction (fever, headache, dizziness, rashes, pruritus,
cutaneous larva migrans, strongyloidiasis and some form of tachycardia, hypotension, pain in muscles and joints and lymph
D. Ivermectin filariasis glands) ; CI in pregnancy and in Px taking GABA-mediated meds Antidote for Mazzoti reaction is antihistamine and NSAIDs
Stimulates nicotinic receptors at NMJ of nematodes —>
depolarization —> depolarization-induced paralysis, Kills
adult worms not eggs ; DOC for hookworm and roundworm
E. Pyrantel pamoate infections, alternative for pinworm GI distress headache, weakness Contraindicated in patients with hepatic dysfunction
Structural congener of Mebendazole, same MOA as
Mebendazole, Selectively inhibits microtubule synthesis
and glucose uptake in nematodes, ovicidal , has anti-
inflammatory and immunosuppressive action in the host ; GI irritation, headache, dizziness, drowsiness, leukopenia, hematuria,
Used as alternative for Strongyloides and Trichinosis (adult SJS, liver failure, intrahepatic cholestasis, lymphadenopathy,
F. Thiabendazole worms) irreversible liver failure : CI in pregnancy CI in renal and liver disease
Increases membrane permeability to calcium —>
contraction of trematode and cestode muscle —> muscle
paralysis, vacualization and death ; DOC for trematodes
(schistosoma, paragonimus, clonorchis, opistorchis) and
cestodes (taenia, diphyllobothrium) together with Used with steroid when treating neurocysticercosis to dec
Niclosamide ; for infection by small and large intestinal headache, dizziness, nausea, malaise, Inc ICP, seizure swelling , contraindicated in ocular cysticercosis (may cause
G. Praziquantel flukes ; alternative to Albendazole in Cysticerci (neurocystecercosis) ; CI in pregnancy irreparable eye damage)
Uncouples oxidative phosphorylation or by activating
ATPases, scoleces and segments are killed but NOT Ova ;
alternative drug to Praziquantel for cestode infection
(Taenia, Diphyllobotrium), not effective in cystecercosis
(use Albendazole or Praziquantel instead) or Hydatid
disease (use Albendazole), effective in the Tx of infections
H. Niclosamide from small and large intestinal flukes GI distress, headache, rash, fever Avoid ethanol consumption for 48 hours upon drug consumption
GABA agonist —> paralyze ascaris —> expelled by normal
I. Piperazine peristalsis ; As alternative for ascariasis GI upset ; CI in pregnancy CI in renal and liver disease and to Px with seizure disorder
Unknown MOA ; co-DOC (with Triclabendazole) for Tx of
Fascioliasis (sheep liver fluke), as alternative for
J. Bithionol paragonimiasis Nausea,vomiting, diarrhea, abdominal cramps, phototoxicity, rash NONE
an organophosphate prodrug —> Dichlorvos (AchE
inhibitor) -> muscle contraction —> paralysis ; Active vs
K. Metrifonate Schistosoma haemoatobium Excess cholinergic stimulation (DUMBBELSS) ; CI in pregnancy NONE
effective solely in Schistosome mansion (intestinal
bilharziasis) - on male immature forms and adult GI upset, pruritus, eosinophilia, urticaria, pulmonary infiltrates ; CI in
L. Oxamniquine schistosomal forms ; MOA is unknown pregnancy and seizure disorder MOA is unknown but can cause paralysis
Cancer Chemotherapy
all are Cell-cycle non-specific ; Universal MOA: form
reactive molecular species that alkylate nucleophilic groups
on DNA bases, particularly the N-7 of guanine leading to
cross-linking of bases, abnormal base pairing and DNA Resistance is due to increased DNA repair, decreased drug
A. Alkylating agents strand breakage permeability and production of trapping agents such as thiols
Forms DNA cross-links, resulting in inhibition of DNA
synthesis and function, Cell-cycle nonspecific, bone marrow suppression, hemorrhagic cystitis, hepatotoxicity,
Mechlorethamine has additional MOA: converts to a alopecia, SIADH, pulmonary toxicity, cardiac dysfunction ; Rescue therapy is MESNA and hydration; metabolite is acrolein
i. Nitrogen Mustards: Cyclophosphamide, reactive cytotoxic product ; For non-hodgkin’s lymphoma, Mechorethamine SE include marked vesicant action, sterility, which is important for Cyclophosphamide’s anti-cancer effect and
Chlorambucil, Mechlorethamine breast cancer, ovarian cancer, neuroblastoma, CLL myelosuppresion, alopecia also its toxicity
synthesis and function, Cell-cycle nonspecific ; component
of regimen For testicular cancer, ovarian cancer, bladder IV, Rescue therapy is Amifostine, decreased nephrotoxicity by
ii. Platinum Analogs: Cisplatin, Carboplatin, cancer and lung cancer ; Oxaliplatin is used also for nausea, vomiting, nephrotoxicity, neurotoxicity (peripheral neuritis), giving mannitol with forced hydration ; Carboplatin is less
oxaliplatin advanced colon CA ototoxicity (acoustic nerve damage), hematotoxicity nephrotoxic but has more myelosuppression
iii. Alkyl sulfonate: Busulfan synthesis and function, Cell-cycle nonspecific ; For CML pulmonary fibrosis, adrenal insufficiency, skin pigmentation Spares the bone marrow
synthesis and function, Cell-cycle nonspecific ; For brain CNS toxicity (dizziness, ataxia), nausea and vomiting, bone marrow Highly lipophilic allowing ease of passage through BBB into the
iv. Nirtosoureas: Carmustine, lomustine tumors, melanoma, skin cancer suppression, skin flushing CNS
a reactive agent which forms hydrogen peroxide, which
generates free radicals that cause DNA strand scission, cell
cycle non-specific ; component of reigned For Hodgkin’s bone marrow suppression, pulmonary toxicity, hemolysis, disulfiram PO, can pemetrate the CSF, LEUKEMOGENIC, CPY450
v. Others: Procarbazine, Dacarbazine lymphoma, non-hodgkin’s lymphoma, brain tumors reaction,skin reactions, peripheral neuropathy, CNS dysfunction inhibitor, Dacarbazine is phototoxic
all are cell-cycle specific , they also have
B. Antimetabolites immunosuppressant action
Inhibits dihydrofolate reductase, decreases synthesis of PO, IV, Rescue therapy is Leucovorin (Folinic acid) ; cytotoxic
thymidylate, amino acids, purine nucleotides —> interfere due to formation of polyglutamate derivatives ; resistance is due
with NA and CHON metabolism ; cell cycle specific ; For to decreased drug accumulation, changes in drug sensitivity or
choriocarcinoma, acute leukemia, non-hodgkin, primary activity of DHF reductase and decreased formation of
CNS lymphoma, breast cancer, head and neck cancer, polyglutamates ; clearance is dependent on renal function
bladder cancer ; also for psoriasis, rheumatoid arthritis, bone marrow suppression, pulmonary infiltrates and fibrosis, therefore adequate hydration is important to prevent
i. Folate antagonist: Methotrexate ectopic pregnancy mucositis, crystalluria, hepatotoxic crystallization into stones
are activated by hypoxanthie-guanine
phosphoribosyltransferase (HGPRT) to toxic nucleotides 6-MP metabolism inhibited by allopurinol and febuxostat ,
which inhibit enzymes in purine metabolism —> Inhibits de Resistance is due to decreased activity of HGPRT, increased
ii. Purine antagonist: 6-Mercaptopurine, 6- novo purine nucleotide synthesis , cell cycle specific ; For bone marrow suppression, hepatic dysfunction (necrosis, jaundice, alkaline phosphatase activity (which inactivates the toxic
thioguanine, fludarabine, cladribine acute leukemia (AML, ALL), CML cholestasis) nucleotide) , undergo significant FPE (by xanthine oxidase)
converted to 5-fluoro-2’-deoxyuridine-5’-monophosphate (5-
FdUMP) which Inhibits thymidylate synthase, incorporation IV, can distribute to CSF, causes “thymineless” death of cells,
inhibits DNA synthesis and function, cell cycle specific ; For Resistance is due to decreased activation of 5-FU, increase
bladder cancer, breast cancer, colorectal cancer, anal thymidylate synthase activity and decreased sensitivity of this
cancer, head and neck cancer, liver cancer and ovarian enzyme ; another metabolite is 5-florouridine-5’triphosphate
cancer, topically for keratoses and superficial basal cell (FUTP) which incorporates into RNA —> interfere with RNA
iii. Pyrimidine antagonist: 5-Fluorouracil skin cancer bone marrow suppression, GI irritation, alopecia processing and function
a cytosine arabinoside, activated by kinases to Ara-Cytidine
Triphosphate (AraCTP) which Inhibits DNA polymerase —
> inhibition of DNA synthesis and repair, inhibits Most specific for the S-phase of the cell cycle, Resistance is due
ribonucleotide reductase with reduced formation of dNTPs, to decreased uptake and decreased conversion to AraCTP, a
iv. Pyrimidine antagonist: Cytarabine (ARA-C) cell cycle specific ; For AML, ALL, CML GI irritation, bone marrow suppression, neurotoxicity cytosine arabinoside
a deoxycytidine analog, converted to Gemcitabine
diphosphate which inhibits ribonucleotide reductase with
reduced formation of deoxyribonucleotide triphosphate
required for DNA synthesis, Gemcitabine triphosphate is
incorporated into DNA causing chain termination, cell cycle
specific ; For pancreatic cancer, bladder cancer, non-small
v. Pyrimidine antagonist: Gemcitabine cell lung cancer, non-Hodgkins lymphoma bone marrow suppression, neutropenia, pulmonary toxicity a deoxycytidine analog
C. Natural Anticancer Drugs all are cell-cycle specific
Prevents assembly of tubulin dimers into microtubule
assembly blocking the formation of mitotic spindles, causes
cell arrest at metaphase, cell cycle specific ; For acute
leukemias, lymphomas, wilms tumor and neuroblastoma ;
Vinblastine For lymphomas, neuroblastomas, testicular IV, highly distributed except in CSF, Acts primarily in M phase of
i. Vinca alkaloid: Vincristine, Vinblastine, carcinoma and Kaposi sarcoma ; Vinorelbine For non-small cancer cell cycle, Resistance is due to increased efflux of drugs
Vinorelbine cell lung cancer and breast cancer Neurotixicity (areflexia, peripheral neuritis, paralytic ileus) via membrane drug transporter
Induces DNA breakage by inhibiting DNA topoisomerase II,
inhibits mitochondrial electron transport, cell cycle specific ;
Combination regimen For lung cancer, prostate cancer,
testicular cancer, non-hodgkin’s lymphoma, germ cell and PO, high Vd ; dose adjustment in renal patients ; Act on the Late
ii. Podophyllotoxin: Etoposide, Teniposide gastric cancer bone marrow suppression, alopecia, GI distress S and early G2 phase
Inhibits DNA topoisomerase I which cute and relegates
single DNA strands during normal DNA repair, cell cycle
specific; For advanced ovarian cancer (2nd line), small cell
iii. Camptothecins: Topotecan, Irinotecan lung cancer, Irinotecan For metastatic colorectal cancer bone marrow suppression, diarrhea Irinotecan can be used for metastatic colorectal cancer
Interferes with mitotic spindle synthesis by preventing
microtubule disassembly into tubulin monomers, cell cycle
specific ; For solid tumors - advanced breast and ovarian Paclitaxel (neutropenia, thrombocytopenia, peripheral neuropathy,
cancer, lung cancer, gastroesophageal cancer, prostate hypersensitivity),
iv. Taxanes: Paclitaxel, Docetaxel cancer, bladder cancer, head and neck cancer Docetaxel (neurotoxicity, bone marrow suppression) Act on M phase
D. Antitumor antibiotics
Intercalates between base pairs, inhibits topoisomerase II,
generates free radicals, blocks synthesis of RNA and DNA
causing DNA strand scission, causes membrane disruption,
cell cycle non-specific ; Doxorubicin For Hodgkins and Non-
Hodgkins lumphoma, myelomas, sarcomas, breast cancer,
endometrial cancer, lung cancer, ovarian cancer and
thyroid cancer ; Daunorubicin For acute leukemias
Idarubicin For AML, Epirubicin For breast cancer and
gastroesophageal ; Mitoxantrine For acute myeloid
i. Anthracycline: Doxorubicin, Daunorubicin, leukemias, Non-Hodgkins lymphoma, breast and alopecia, nausea, vomiting, Cardiotoxicity (dilated cardiomyopathy, Rescue therapy is Dexrazoxane and liposomal formulation of the
Idarubicin, Epirubicin, Mitoxantrone gastroesophageal cancer CHF) drug
Generated free radicals which bind to DNA and causes
DNA strand breaks leading to inhibition of DNA synthesis,
intercalates with DNA, cell cycle specific ; Component of
regimens in Hodgkins lymphoma and testicular cancer,
lymphomas and squamous cell cancer, head and neck pneumonitis, pulmonary fibrosis, alopecia, mucocutaneous reactions, IV, inactivated by tissue aminopeptidases, Most specific for the
ii. Bleomycin cancer, skin cancer hypersensitivity reactions G2 phase of cell cycle, a glycopeptide
Binds to double stranded DNA, inhibits DNA-dependent
RNA synthesis, cell cycle non-specific ; For melanoma,
iii. Actinomycin D wilm’s tumor, choriocarcinoma, Kaposi sarcoma bone marrow suppression, skin reactions, GI irritation None
Metabolized into an alkylating agent that cross-links DNA ;
In combination regimens for adenocarcinoma of the cervix,
iv. Mitomycin C stomach, pancreas and lungs severe myelosuppression, toxic the heart, liver, lungs and kidneys IV, used for hypoxic tumor cells
E. Miscellaneous Anticancer Drugs
Tyrosine kinase inhibitor of the protein product of bcr-abl
i. TK inhibitor: Imatinib, Dasatinib, Nilotinib oncogene in CML ; For CML, GIST diarrhea, myalgia, fluid retention, CHF Resistance is due to mutation is bcr-abl gene
ii. Growth Factor Receptor Inhibitor
recognizes a surface protein in breast CA cells that
overexpress Her-2-neu receptors for epidermal growth
a. Her-2-neu inhibitor: Trastuzumab factor nausea, vomiting, chills, fever, headache, cardiotoxicity (CHF) None
EGFR (Epidermal Growth Factor Receptor) regulate
signaling involved in cellular proliferation, invasion and
metastasis and angiogenesis, it also inhibits cytotoxic
activity of some anti-cancer and radiation treatment,
Gefitinib and Erlotinib are capable of inhibiting EGFR’s
Tyrosine Kinase domain ; Cetuximab (+ Irinotecan and
Oxalipatin) For metastatic colon cancer and Head and
Neck cancer ; Panitumumab For refractory colorectal
b. EGFR inhibitor: Cetuximab, Panitumumab, cancer ; Gefitinib and Erlotinib as second-line agents for
Gefitinib, Erlotinib non-small cell lung cancer folliculitis, diffuse hair loss, dry skin, paronychia Erlotinib can also be used for advanced pancreatic cancer
VEGF (Vascular Endothelial Growth Factor) has a role in
angiogenesis required for metastasis, Inhibits binding of
VEGF to VEGFR leading to inhibition of VEGF signalling,
inhibits tumor vascular permeability but enhances tumor
blood flow and drug delivery ; Sorefenib Sunitinib and
Pazopanib inhibits multiple receptor Tyrosine Kinase
c. VEGF Inhibitor: Bevacizumab, Sorafenib, including those associated to VEGF ; For metastatic hypertension, arterial thrombosis, impaired wound healing,
Sunitinib, Pazopanib colorectal cancer, breast cancer, diabetic retinopathy proteinuria, GI perforation may also be used in non-small cell lung CA and renal CA
Binds to a surface protein in NHL cells, induces
complement-mediated lysis, direct cytotoxicity and
induction of apoptosis ; For Non-Hodgkin’s lymphoma and
iv. Rituximab other lymphomas hypersensitivity reaction, bone marrow suppression None
Endogenous glycoproteins with antineoplastic,
immunosuppressive and antiviral actions ; For hairy cell alopecia, myalgia, depression, thyroid dysfunction, hearing loss, bone
v. Interferon alpha leukemia, early CML, T-cell lymphoma marrow suppression None
Depletes serum asparagine ; For ALL, T-cell auxotrophic
CA (leukemia and lymphomas) that require asparagine for
vi. Asparaginase growth acute pancreatitis, bleeding, severe hypersensitivity reaction None
Allows DNA transcription and differentiation of immature
leukemic promyelocytes into mature granulocytes ; For retinoic acid syndrome (dyspnea, fever, weight gain, peripheral Only vitamin that can cure cancer, treat retinoic acid syndrome
vii. All-Trans retinoic acid acute promyelocytic leukemia edema) with dexamethasone
a reversible inhibitor of 26s proteasome in mammalian cell ;
viii. Protease Inhibitor: Bortezomib For multiple myeloma peripheral neuropathy, thrombocytoppenia
F. Hormonal Anticancer Agents
Suppresses inflammation and immune response, may
trigger apoptosis and work on nondividing cancer cells ; For adrenal suppression, growth inhibition, muscle wasting, osteoporosis,
i. Prednisone CLL, Hodgkin’s lymphoma, leukemia, lymphoma salt retention see entry
Estrogen antagonist actions in breasts tissue and CNS,
estrogen agonist effects in uterus, liver and bone ; For
hormone-responsive breast cancer, Toremifene For hot flushes, thromboembolism, endometrial hyperplasia, endometrial
ii. SERM: Tamoxifen, Toremifene advanced breast cancer cancer Prevents osteoporosis and decrease risk of atherosclerosis
GnRH analogs (leuprolide) must be co-administered to prevent
iii. Androgen antagonist: Flutamide Androgen antagonist ; For prostate cancer gynecomastia, hot flushes, impotence acute flare-up of prostate cancer
Increased LH, FSH secretion with intermittent
iv. GnRH analog: Leuprolide, Goserelin administration, reduced LH and FSH secretion with hot flushes, sweats, headache, osteoporosis, gynecomastia,
Nafarelin prolonged continuous administration ; For prostate cancer gynecomastia, testicular atrophy, impotence, bone pain see entry
Reduces estrogen synthesis by inhibiting aromatase; For nausea, diarrhea, hot flushes, bone and back pain, dyspnea, Effective againsts breast cancer that have become resistant to
v. Aromatase inhibitor: Anastrazole, Letrozole advanced breast cancer peripheral edema tamoxifen
Drugs Used in the Treatment of Gastrointestinal Diseases

Impairs absorption of tetracyclines, flouroquinolones,itraconazole
Sodium bicarbonate: Belching, metabolic alkalosis. Calcium and iron ; When used regularly in large doses needed to
A. Antacids: Magnesium-Aluminum Hydroxide, Neutralize stomach acid by reacting with protons in the carbonate: hypercalcemia, renal insufficiency, metabolic alkalosis significantly raise the stomach pH, antacids, decrease recurrence
Calcium carbonate, Sodium bicarbonate lumen ; For peptic ulcer disease, Gastroesophagal reflux (milk-alkali syndrome rate of peptic ulcers
Competitive pharmacologic block of H2 receptors ; For Gynecomastia (cimetidine only), Diarrhea, headache, fatigue, Cimetidine is a potent inhibitor of CYP450. Highly effective in
B. H2 receptor antagonist: Cimetidine, Ranitidine, peptic ulcer disease, Zollinger-Ellison syndrome, Myalgias, constipation, Nosocomial pneumonia, Mental status suppressing nocturnal acid secretion but only modest effect on
Famotidine, Nizatidine Gastroesophagal reflux, dyspepsia changes, Bradycardia, Hypotension, Blood dyscrasias meal- stimulated secretion
Irreversible blockade of H/K ATPase in active gastric
parietal cells, Long lasting reduction of meal stimulated and usually enetric coated, t1/2 is 1-2hrs but DOA of is around 24hrs,
C. Proton Pump Inhibitor: Omeprazole, nocturnal acid secretion ; For Peptic ulcer disease(DOC), Diarrhea, headache, abdominal pain, Malabsorption syndrome (Vit needs 3-4 days treatment to achieve full effectiveness ;
Lansopraole, Rabeprazole, Pantoprazole, Zollinger-Ellison syndrome, Gastroesophageal reflux, B12, Ca, Fe, Zn, Digoxin, Ketoconazole), Infections (respiratory, decreases bioavailability drugs that require acidity for GI
Esomeprazole dyspepsia enteric), Hypergastrinemia, Atrophic gastritis absorption
D. Mucosal Protective Agent:
polymerizes in acidic environmet —> polymers bind to
injured tissue and forms a protective covering over ulcer
bed, Accelerates healing of peptic ulcers and reduces Highly insoluble, requiring frequent dosing (QID) ; chemically:
i. Sucralfate recurrence rate ; For Peptic ulcer disease constipation, dizziness, flatulence, dry mouth Aluminum Sucrose Sulfate
forms a protective coating on ulcerated tissue, stimulates
mucosal protective mechanisms, direct antimicrobial effects
and sequestration of enterotoxins ; For Peptic ulcer Black stools, darkening of tongue, Encephalopathy (Atraxia,
ii. Bismuth Salicylate disease, Dyspepsia, Infectious diarrhea headaches, confusion, seizures) Reduces stool frequency and liquidity in infectious diarrhea
PGE1 analog, Activates EP receptors, causes increased
HCO3 and mucus secretion and inhibits acid secretion in
the stomach, causes uterine contraction ; For Peptic ulcer
disease, Prevention of NSAID-induced gastric mucosal
iii. Misoprostol injury, Abortifacient Abdominal pain, Diarrhea, Uterine cramping, Miscarriage see entry, decreases ulcer in NSAIDs induced ulceration
E. Prokinetics
Metoclopramide and domperidone block D2 receptors,
Erythromycin stimulates motilin receptor, Increases gastric
emptying and intestinal motility ; As Antiemetic for post
operative/chemotherapy vomiting, Diabetic gastroparesis
i. Metoclopramide, Domperidone, Erythromycin, (drug of choice), Neostigmine for acute large bowel Domperidone does not cross the BBB (less toxic) ; Increases
Neostigmine distention Parkinsonism, Extrapyramidal effects, Hyperprolactinemia LES pressure (helpful in GERD)
F. Laxatives
Indigestible, hydrophilic colloids that absorb water, forming
i. Bulk-forming: Psyllium, Methylcellulose, a bulky emollient gel that distends the colon and promotes
Polycarbophil peristasis ; For constipation Diarrhea None
ii. Stool-softener: Docusate, Glycerine, Mineral Soften stool material, Permitting water and lipids to Diarrhea, Aspiration,(Lipid pneumonitis), Malaabsorption of fat-soluble
oil penetrate the stool ; For constipation vitamins (A, D, E, K) None
Soluble but nonabsorbable compound that result in
iii. Osmotic: Lactulose, Magnesium oxide, increased stool liquidity due to an obligate increase in fecal Diarrhea, Flatus, Abominal cramps, Electrolyte abnormalities
Magnesium hydroxide, Sorbitol, Magnesium fluid ; For Constipation, Hepatic encephalopathy (hyperphosphatemia, hypocalcemia, hypernatremia, hypokalemia,
citrate, Sodium phosphate, Polyethylene Glycol (lactulose), Preparation for endoscopy (polyethylene glycol) hypermagnesemia) None
iv. Stimulant: Bisacodyl, Aloe, Senna, Cascara, Unknown. Directly stimulate enteric nervous system and
Castor oil colonic electrolyte and fluid secretion Diarrhea can cause melanosis coli
Lubiprostone is a Chloride channel activator which
stimulates Cl secretion into the intestines leading to
increased fecal fluid content, Methylnaltrexone and
v. Miscellaneous: Lubiprostone, Alvimopan are Opioid receptor antagonist that block
Methylnaltrexone, Alvimopan intestinal mu receptors, but not the CNS mild nausea, stomach pain, mild diarrhoea, bloating, headache NONE
Activates opioid receptors in enteric nervous system. Slows Do not use in children less than 4 years of age (increased
motility with negligible CNS effects, Kaolin (+pectin) chance of causing paralytic ileus), Reverse ileus by administering
G. Anti-diarrheals: Diphenoxylate, Loperamide, absorbs bacterial toxin and fluid leading to decreased stool Drowsiness, Nausea, Paralytic ileus, interfere with absorption of other Betanechol. Direct m-agonist, Kaolin is hydrated Magnesium
Kaolin+Pectin, Colloidal Bismuth liquidity ; for Diarrhea (nonspecific, noninfectious) drugs Aluminum Silicate
H. Drugs for IBS
i. laxatives, antidiarrheals and low-dose TCA see entry see entry see entry
see entry ; antispasmodic for abdominal pain, for IBS with
ii. Anticholinergics: Dicylomine, Hyoscyamine prominent diarrhoea see entry see entry
iii. 5HT3 antagonist: Alosteron see entry ; For IBS with severe diarrhoea severe constipation, ischemic colitis see entry
see entry ; activate type2 chloride channels in small
iv. Lubiprostone intestines ; For IBS with predominant constipation see entry see entry
I. Anti-emetics
Blocks chemoreceptor trigger zone and enteric nervous
i. Ondansetron, Granisetron, Dolasetron, system 5-HT3 receptors ; For Vomiting (Post Headache, Dizziness, Constipation, QRS and QT prolongation
Palonosetron chemothereaphy, postoperative) (Dolasetron only) see entry
antagonist of the Neurokinin-1 receptor in the areas
postrema that is activated by substance P and other
ii. Aprepitant tackykinins ; For post-chemotherapy nausea and vomiting fatigue, dizziness, diarrhea an enzyme inhibitor
iii. Scopoloamine see entry ; For motion sickness emesis see entry see entry
J. Drugs for IBD
Unknown. Probably inhibits production of eicosanoid
inflammatory mediators (PG and LT) and interfering with
i. Aminosalicylates: Mesalamine, Balsalazine, cytokines ; For Inflammatory bowel disease (mild to Gastrointestinal upset,Headaches, Arthralgias, Myalgias, Bone
Olsalazine, Sulfasalazine moderate) marrow suppression, Malaise, Hypersensitivity reactions ( severe) Not useful for treating active flare ups of disease
ii. Other agents: Antibiotics,
Immunosuppressibe antimetabolites see entry ; Natalizumab is a Mab that blocks intergrins in
(Azathioprine, 6-MP, Methotrexate), anti-TNF circulating leukocytes, restricted to severe refractory
(Infliximab), Natalizumab Crohn’s disease multifocal leukoencephalopathy see entry
K. Miscellaneous Agents
For pancreatic enzyme replacement, improve digestion of
fats proteins and carbohydrates ; For pancreatic
i. Pancreatic lipase: Pancreatin or insufficiency due to Cystic Fibrosis, pancreatitis and
Pancrealipase pancreatectomy hyperuricemia Taken with every meal
a bile acid derivative that decreases cholesterol content of
bile by decreasing hepatic cholesterol secretion and other
ii. Drugs that inhibit formation of Gallstones: effects on hepatocyte canalicular membrane ; For gallstone headache, dizziness, mild stomach pain, rhinorrhea, sore throat, rash
Ursodiol in patients refusing or not eligible for surgery hair loss None

Autonomic Drugs Cholinomimetics: Drug Moa and Indication Adverse Effects Notable Properties

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Autonomic Drugs Cholinomimetics: Drug Moa and Indication Adverse Effects Notable Properties

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DRUG MOA and INDICATION ADVERSE EFFECTS NOTABLE PROPERTIES

Nonselective competitive antagonism at all muscarinic receptors in the CNS

Non-selective, direct acting sympathomimetic; activates A and B adrenergic

Non-selective, direct acting sympathomimetic; activates A, B and D1

A1 agonist used for short term maintenance of BP in acute hypotension; also

Reserpine Irreversibly blocks the vesicular monoamine transporter (VMAT)

causes arteriolar vasolidation of the afferent and efferent arterioles.

Block of beta-receptors, decrease in cAMP results to decreased Na and Ca

C. Class 3 Arrhythmics Group with the greatest risk for TDP

Agonists at V1 and V2 ADH receptors. Activate insertion of aquaporin water

G. ADH Antagonists: Conivaptan, Infusion site reactions, hyperkalemia, Nephrogenic diabetes

3. DRUGS WITH IMPORTANT ACTION ON SMOOTH MUSCLES

more likely to block autonomic receptors, also has alpha1

Surmountable competitive pharmacologic block of H2 receptors, reduction of

uterus becomes more sensitive to ergots during pregnancy,

The Eicosanoids: Prostaglandins, Thromoboxanes, Leukotrienes and related compounds

4. DRUGS THAT ACT ON THE CENTRAL NERVOUS SYSTEM

CYP450 inducer , metabolism is non-linear (elimination shift from

Antidote is Naloxone / Naltrexone ; Neuroleptanesthesia

"milk of anesthesia", additive effects with sedative-hypnotic drugs

Blockade of Na channels slows which prevents axon potential

Undergoes Hoffman elimination (rapid spontaneous breakdown);

extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia,

Serotonin syndrome when used with MAOIs ; minimal inhibitory

Inhibits neuronal reuptake of dopamine and norepinephrine, increase

Strong agonist at u receptors, inhibits pain neurotransmission, binds

Cofactor required for essential enzymatic reactions that form

Selective inhibitor of the NPC1L1 transporter decreasing intestinal

Cholesterol analog, takes the place of dietary and billiary cholesterol,

Increased risk of myopathy and rhabdomyolysis when used with

Inhibits phosphodiesterase III and increases cAMP in platelets and

May precipitate acute gout during early phase of drug action

ADH antagonist, Antagonist at V1a and V2 receptors ; For SIADH,

strong agonist of mineralocorticoid receptors and moderate activation of

Gonadal Hormones and Inhbitors

Synthetic estrogen (nonsteroid); activates estrogen receptors; leads to

Prevents estrogen induced endometrial cancer when used in

ii. Ethinyl Estradiol + Desogestrel

Combined with misoprostol results in abortion of 95% of early

Activates androgen receptors, promotes development of male

1st generation sulfonylurea, acts as an insulin secretagogue; increases

Insulin Secretagogue, similar to sulfonylureas with some overlap in

Acts via cognate G protein coupled receptors; suppresses bone

iv. Antipseudomonal Penicillin:

Reserved for serious ife-threatening infections; cilastatin inhibits

Narrow spectrum Treat red man syndrome by slowing the rate of

AG are given IM or IV only, have concentration dependent killing,

Potent CYP450 inducer ; rapid development of resistance if used

given as IV or intraocular implant (for CMV retinitis) ; No activity

aesthenia, GI upset, headache, hyperpigmentation of palms of soles,

80% oral bioavailability ;may also be used for Hepa B infection ;

per orem absorption requires acidic environment ; can penetrate

GI upset, paresthesia, rash, CI in pregnant patients and children if

Dipiroxil is a prodrug of Adefovir ; Telbivudine is a newer drug

Coinfection between HBV and HIV may increase the risk of

Inhibits protein synthesis by blocking ribosomal movement

Drugs Used in the Treatment of Gastrointestinal Diseases

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