TD

CHOLINERGICS

DIRECT INDIRECT

NEOSTIGMINE RIVASTIGMINE
NON SELECTIVE MUSCARINIC NICOTINIC EDROPHONIUM
PYRIDOSTIGMINE GALANTAMINE
PYSOSTIGMINE DONEPEZIL
AMBENONIUM TACRINE
BETANECHOL PILOCARPINE NICOTINE
ACETYLCHOLINE DEMECARIUM (Carbamates)
CARBACHOL CIVEMELINE VARENICLINE
ECHOTHOPHATE (Organophosphate)

MOA: Activates M1-M3 MOA: Activates nicotinic Ach

-primary NT in all
autonomic gangla at the
synpases between
parasympathetic
postganglion
-primary NT at the somatic
(voluntary) skeletal muscle
NMJ
MOA: Act on both M & N
receptors. Activates M1 -
M3 receptiors in all
peripheral tissues
USES:
Miotic during ocular
surgery
SE: DUMB BELSS
Notes:
-Short lived DOA: 5-30sec
-Rapidly hydrolyzed by AchE
-Results to increased secretion,
smooth muscle contraction (except in
vascular smooth muscle where it
causes relaxation) and changes in
heart rate
receptors
Uses: Bladder and Bowel
Atony (post surgery or
spinal cord injury)
SE: Cyclospasm,
Diarrhea, Urinary
Urgency, Vasodilation,
Reflex tachycardia,
Sweating
Notes:
-Results to increased
secretion, smooth
muscle contraction
(except in vascular
smooth muscle where it
causes relaxation)
-Resistant to AchE, orally
active, act on M
receptors only
CARBACHOL - for
glaucoma, used as miotic
MOA: Activates M3 receptors
on ciliary muscle (increasing
aqueous humor outflow) &
salivary glands (increasing
salivation)
Uses: Glaucoma, Sjogren
syndrome, Sicca Syndrome
SE: DUMB BELSS
Notes:
-Good lipid solubility
compared to choline esters
receptors (Nn & Nm)
Uses: Smoking cessation
SE: Generalized ganglionic
stimulation (hypertension,
tachycardia, nausea,
vomiting, diarrhea)
Notes:
-OVERDOSE leads to
convulsions, paralysis &
coma
-Activates autonomic post
ganglionic neurons (both
sympa & parasymp) &
skeletal muscle
neuromuscular end plates
-DOA: 1-6 hr only
VARENICLINE - Selective
partial agonist at nicotinic
receptors; DOA 12-24h
MOA: Inhibits AchE
MOA: Inhibits AchE
Uses: Alzheimer's Disease
MOA: Inhibitis AchE
Uses:
-Myasthenia gravis (treatment) SE: DUMB BELSS
Uses:
-Reversal of nondepolarizing NM blockade
-Myasthenia gravis
-Glaucoma (physostigmine, echothiophate, Notes:
demecarium) (diagnosis - Tensilon Test)
RIVASTIGMINE is
-Differentiation of cholinergic
available at transdermal
SE: DUMB BELSS crisis & myasthenic crisis
patch
DONEPEXIL is combined
Notes: SE: DUMB BELSS with Memantine (NMDA
-Muscarinic effects are blocked by ATROPINE
antagonist) for Alzhemer's
-NEOSTIGMINE: poor lipid solubility, oral, DOA Dementia)
30min-2hr Notes:
-PYRIDOSTIGMINE: poor lipid solubility, oral, DOA 4-8hr IV, short lived, DOA 5-15mins
-PHYSOSTIGMINE: good lipid solubility, able to enter
CNS, DOA 4-8hr
-ECHOTHIPATE: moderate lipid solubility, DOA 2-7days
-Other organophosphates:
MALATHION (Scabicide), and PARATHION
(Insectidide): high lipid solubility, DOA 7-30 days
SARIN, TABUN, SOMAN: Nerve Gases

 TD
ANTI CHOLINERGICS

CHOLINESTERASE
ANTI MUSCARINIC ANTI NICOTINIC REGENERATOR

NEUROMUSCULAR GANGLION
SELECTIVE NON SELECTIVE BLOCKER BLOCKER
PRALIDOXIME

IPRATROPIUM DICYCLOMINE OXYBUTYNIN ATROPINE BENZTROPINE MOA: Binds

Tiotropium NON
Hyoscyamine Darifenacin, Solifenacin, Homatropine, Biperiden SCOPOLAMINE DEPOLARIZING DEPOLARIZING
HEXAMEHTHONIUM phosphorus of
Tolteradine, Trospium, Cyclopentolate, organophosphate.
Umeclidinium Glycopyrrolate Imidafenacin Tropicamide Trihexyphenidyl
BReask
Glycoyrronium organophosphate
bond with
PROTOTYPE MOA: Competitively cholinesterase.
MOA: Blocks MOA: Slightly blocks NONSELECTIVE blocks all muscarinc SUCCINYLCHOLINE 1) TUBOCURARINE Regenerate active
M3 MOA: Completitvely M3 receptors.
blocks M3 receptors MUSCULAR BLOCKER
MOA: Competitvely receptors. 2) PANCURONIUM AchE.
(bronchial Reduces detrusor Antagonize MOA:
blocks all muscarinic Competively
smooth muscle tone. histamine & 3) ATRACURONIUM
MOA: Competitvely receptors. Restores NT blocks Nn
muscle). Uses: IBS, minor balance in basal serotonin 4) VEROCURONIUM Uses: Antidote for
Prevents blocks all muscarinic nicotinic early stage
diarrhea, decreased receptors ganglia. 5) ROCURONIUM receptors
vagal acid secretion in cholinesterase
stimulated Uses: Urge Uses: Motion inhibitor poisoning
GIT
brochoconstri incontinence, Post Uses: Parkinsons Dse sickness; (organophosphate &
Uses: Mydriatic, decreased acid Uses: nerve gas poisoning);
ction operative spasms Hypertension
Cycloplegic, 1st secretion in GIT; N/ can relieve skeletal
SE: Alice in choice for (obsolete),
Wonderland SE: Alice in Wonderland V muscle & endplate
USES: Acute Organophosphate Hypertensive block
SE: Alice in
Asthma, Wonderland poisoning, emergencies
COPD Available in PO & IV Bradycardia, Notes: Reduces tremors SE: Alice in
forms, relatively Hypersalivation more than bradykinesia Wonderland SE: muscle weakness
Available as patch SE: Postural
short half life or ridgidity
SE: Alice in (may cause pruritus) hypotension,
(6hrs). Other SE: Atropine Toxicity Sexual
Wonderland Notes: Applied as Notes: must be
name: (Alice in Wonderland) Dysfunction,
Dicycloverine transdermal patch administered before
Constipation, Dry 6-8 hours of
mouth, Blurred organophosphate
vission bond with
cholinesterase occurs;
has oxime group
which has high
affiniity for phosphate

 TD

ADRENERGICS/ SYMPATHOMIMETICS
DIRECT INDIRECT
REUPTAKE
NON SELECTIVE ALPHA BETA INHIBITOR RELEASERS

EPINEPHRINE NOREPINEPHRINE DOPAMINE ISOPROTERENOL ALPHA 1 ALPHA 2 BETA 1 BETA 2 PHENYLPROPA

NOLAMINE
MOA: CLONIDINE METHYLDOPA DOBUTAMINE SALBUTAMOL
APRACLONIDINE
A1: MOA: PHENYLEPHRINE Guanfacine, ALBUTEROL
Brimonidine
vasocontricstion, Pseudoephedrine, Guanabenz,
increase BP Alpha 1: TERBUTALINE
vasoconstriction, Oxymetazoline, MOA: Dexmedetomidine,
MOA: B1: increase HR, MOA: non Tetrahydrozoline, Tizanidine ISOXUPRINE
increase BP Midodrine, A2: decrease
A1: conduction & selective beta RITODRINE
vasocontricstion, contractility B1: increase HR, Naphazoline, central
adrenegric Xylometazoline
increase BP B2: bronchodilation conducion & receptors sympathetic MOA: B1: increase
contractility outflow HR & contractility
B1: increase HR, (not so much B2 activator; MOA: Act mainly
activity) D1: vasodilation in MOA: MOA: by causing
conduction & B1: increased HT, release of NE,
splanchnic & renal Uses: Acute heart
contractility conduction & Uses: HPN, Cancer A2: decrease failure, Cardiogenic
B2: bronchodilation but also has
blood vessels MOA: central
B2: bronchodilation Uses: Neurogenic contractility pain, Opioid shock direct agonist
shock, Cardiogenic A1: vasoconstriction, sympathetic activity at some
B2: increase BP
withdrawal USES:
shock (last resort) outflow adrenegic
Uses: Cardiogenic bronchodilation MOA: decreases SE: Tachycardia, SALBUTAMOL: Acute receptors;
Uses: Cardiac shock, heart secretion of arrhythmias, Asthma attach DOC activates A & B
arrest, Anaphylaxis SE: Extreme Uses: Nasal SE: Sedation, aqueous humor tachyphylaxis, HPN,
failure congestin, mydriatic, rebound HPN, dry Uses: adrenegic
(DOC), Asthma, vasospalsm, Tissue Uses: Asthma eosinophilic receptors in respi
drug-induced mouth Preecmplasia, TERBUTALINE,
COPD, Hemostasis necrosis, Excessive
hypotension,
myocarditis, mucosa
BP increase, GHPN, Uses: Glaucoma premature RITODRINE,
SE: CVS orthostatic sedative ISOXUPRINE:
Arrythmias, SE: CVS ventricular beats,
infarction, Reflex disturbance, hypotension, spinal Taper use prior to (Dexmedetomi Tocolysis for preterm Uses: nasal
SE: Hypertension, disturbance, angina, dysnea,
Bradycardia arrhytmias shock
d/c to avoid dine), muscle fever, HA, nausea
labor vasoconstrictor,
Tachycardia, arrhythmias SE: Blurring of
rebound HPN; relaxant appetite
Ischemia, vision, dry mouth, supressant
Hyperglycemia Notes: Notes: Inactive SE: Rebound nasal Treat rebound HPN (Tizanidine) hyperemia, SE: tachycardia, tremors,
Notes: synthetic congestion (Rhinitis nervousness,
Compensatory PO; do not enter with pruritus, eye restllessness, arrhythmias
catecholamine, medicamentosa);supi May preciptate
vagal reflexes tend CNS significantly; PHENTOLAMINE; discomfort when used excessively,
Notes: Inactive PO; to overcoe the ne HPN, stroke, MI, SE: Sedation, Hemorrhagic
short DOA; very not readily taken piloerection, urinary
loss of responsiveness
direct positive When taken PO, Hemolytic (tolerance) stroke esp in
do not enter CNS effective in renal up into nerve retention
chronotropic there is initial Anemia (+) women
significantly; short failure associated endings
effects; increase in BP Coomb's test
DOA; can cross Alpha>Beta; with shock
May precipiate
placenta (may Avoid then will go down arrhythmias in COPD and
Inactive PO; do not PSEUDOEPHEDRINE heart disease
cause fetal anoxia) enter CNS once the drug
in 1st term, may enters the CNS
significantly; short cause Gastroschisis ISOXUPRINE: used as
DOA vasodilator in Reynaud's
phenomenon; may cause
maternal pulmonary
edema


NON SELECTIVE
IRREVERSIBLE
PHENOXYBENZAMINE
MOA: blocks A1>A2 irrerversibly
Uses: Pheochromocytoma
(presurgical)
SE: Orthostatic hypotension, Reflex
tachycardia, GI irritation, MI
Forms covalent bond w alpha
receptors (effects last for several
days)
ALPHA
REVERSIBLE
PHENTOLAMINE
Tolazoline
MOA:MOA: blocks A1>A2
rerversibly
Uses: Pheochromocytoma
(presurgical), Antidote to A1
agonist overdose, Rebound HPN
SE: Orthostatic hypotension,
Reflex tachycardia, GI irritation
ADRENERGIC ANTAGONISTS
ALPHA 1
PRAZOSIN
Doxazosin, Terazosin, Tamsulosin,
Silodosin, Alfuzosin
MOA: Blocks A1 adrenergic receptors
Uses: BPH, HPN
SE: First dose orthostatic hypotension, Reflex
tachycardia (less chance), dizziness, drowsiness,
headache, weakness, asthenia, nausea, edema
TAMSULOSIN - most selective for prostatic
smooth muscle
DOXAZOSIN, TAMSULOSIN, SILODOSIN
& ALDUZOSIN - not indicated in females for tx of
HPN
INTRINSIC SYMPATHOMIMETIC ACTIVITY:
-partial agonist activity
-lowers BP with modest reduction in HR
-advantage in treating patients with asthma bec these
drugs are less likely to cause bronchospasm
-Acebutolol, Pindolol, Carteolol, Bopindolol, Oxprenolol,
Celiprolol, Penbutolo
BETA BLOCKERS IN DM:
-masking of premonitory symptoms of hypoglycemia from
insulin overdosage (tachycardia, tremor, anxiety)
-impaired hepatic mobilization of glucose
BETA
NON SELECTIVE
PROPANOLOL
Pindolol, Timolol, Labetalol, Carvedilol,
Nadolol, Levobunolol, Metipranolol,
Carteolol
MOA:blocks B1 & B2 receptors. Blocks
sympathetic effects on heart & BP. Reduces renin
release
Uses: Angina prophylaxis, HPN, Arrythmias,
migraine, performance anxiety, hyperthyroidism,
glaucoma
SE: bronchospasm, AV block, heart failure, CNS
sedation, erectile dysfunction
Notes:
May mask symptoms of hypOglycemia in DM
CARVEDILOL & LABETALOL - combined A
& B blockade (may used in pheochromocytoma
PROPANOLOL - IUGR, small placenta &
congenital abnormalities have been reported with
use, but no adequate & well-contracted studies
conducted
METIPRANOLOL - used as ophthalmic drops
for Glaucoma
TD
BETA 1
ATENOLOL
Betaxolol, Esmolol, Acebutolol,
Metoprolol, Alprenolol, Nebivolol,
Bisoprolol
MOA: selectively blocks B1 receptors.
Blocks sympathetic effects on heart & BP
Uses: Angina, HPN, heart failure, SVT
(Esmolol only)
SE: Bronchospasm (less chance), AV block,
heart failure, CNS sedation, erectile
dysfunction
Notes:
Masks symptoms of hypOglycemia in DM
ESMOLOL - shortest half life
(Esmall-LOL)
BETAXOLOL - may aslso be used as
ophthalmic solution for glaucoma
ATENOLOL - use of this cardioselective
BB during pregnancy has been shown to
lower birthweights & impair fetal growth
 TD
DRUGS FOR GLAUCOMA

FLOW OF AQUEOUS HUMOR

Ciliary body à Posterior chamber à
Alpha 2 Agonist Apraclonidine Anterior chamber angle à Pupil à Anterior
chamber à Trabecular meshwork à Canal
Decrease of Schlemm à Uveosacral veins

secretion of Beta blocker Timolol Reciprocal control of Pupil:

aqueous SANS – pupillary dilator muscle
PANS – pupillary constrictor

humor from Carbonic Anhydrase Acetazolamide Ciliary Muscle

ciliary Inhibitor Dorzolamide
(controls accommodation)
PANS (primary control of muscarinic

epithelium receptors)
Insignificant contributions from SANS

Osmotic agents Mannitol Ciliary Epithelium

Important receptors with permissive effect
on aqueous humor secretion

Canal of Schlemm Prostaglandins Latanoprost

Increasae
outflow of Uveosacrall veins Alpha agonist Epinphrine
aqueous humor
Pilocarpine
Trabecular meshwork Cholinergic
Physostigmine

 TD
ANTI HPN
ANGIOTENSIN RENIN VASODILATOR
SYMPATHOPLEGICS ANTAGONISTS DIURETICS INHIBITOR
CNS Sympathetic Adrenergic Nerve Terminal ACE
Outflow Blockers Ganglion ARBs Thiazides Loop Diuretics Aliskerin
CCB Older Oral Parenteral
Blockers Blockers Blockers Inhibitors
METHYL LOSARTAN Non
MOA: inhibits MINOXIDIL NITROPRUSSIDE
CLONIDINE -DOPA Candesartan, HYDROCHLORTHI Dihydropyridine Dihydropyri HYDRALAZINE FENOLDOPAM
Alpha 1 Selective Beta Non Selective RESERPINE AZIDE FUROSEMIDE renin. Prevents Diazoxide
CAPTORPRIL Valsartan, conversion of dine
HEXAMETHON Chlorthalidone, Bumetanide,
GUANETHI- Irbesartan, Torsemide, angiotensinogen
DINE IUM Enalapril, Indapamide, to angiotensin I MOA: relaxes
MOA: Benazepril, Eprosartan, Metalazone Ethacrynic acid VERAPAMIL venouse &
PRAZOSIN Timethaphan MOA: D1
activates A2 PROPANOLOL Guanadrel Fosinopril, Telmisartan, Diltiazem
arteriolar smooth agonist; causes
adrenergic Doxazosin, NIFEDIPINE MOA: alters MOA: opens K
Terazosin, Pindolol, Timolol, Mecamylamine Lisinopril, Azilsartan, Usesu: HPN
intracellular Ca
muscle by arteriolar
recetors Labetalol, Carvedilol, MOA: Valsartan Amlodipine, channels in increasing NO -->
Tamsulosin, irreversibly Quinapril, Ramipril, Felodipine, metabolism. vascular smooth vasodilation of
Nadolol, Levobunolol, increases cGMP the afferent&
Silodosin, blocks the Trandolapril, SE: HA, diarrhea, Nicardipine, MOA: relaxes muscle cuaisng causing smooth
Metipranolol, MOA: inhibits Na-Cl efferant
MOA: Use: Alfuzosin VMAT Moexipril, cough, rash, Nisoldipine, blocks arteriolar hyperpolarization muscle relaxation
Betaxolol, Bisoprolol, trasnporter in DCT; smooth muscle; , muscle arterioles;
activates A2 Preeclamps Nebivolol cause moderate MOA: inhibit Na- hyperK, increase Clevidipine, voltage
adrenergic ia Perindopril, in serum Crea, Isradipine, gated L- decreases relaxtaion &
increases renal
diuresis & reduced K-2Cl transporter
recetors Uses: HPN Imidapril in TAL of Henle. renal impariment, Levamlopidine type Ca afterload vasodilation Uses: HPN blood flow
(obsolete) MOA: blocls AT1 excretion of Ca
Cause powerful angioedema , Lacidipine, channels emergency, acute
SE: sedation, MOA: inhibit receptors in diuresis & Lercanidipine (cardiac > HF, cardiogenic
MOA: vascular smooth -Fetal harm may Uses: HPN, HF Uses: HPN
Uses: HPN, hemolytic vesicular release competitively Uses: HPN (1st increased Ca vascular) Uses: HPN, shock, controlled
MOA:blocks B1 & B2 SE: sedation, cocur when given emergency
cancer pain, anemia, receptors. Blocks of NE from the blocks Nn Ach muscle & renal (in combination alopecia hypotension
MOA: Blocks A1 severe line), HF, excretion during pregnancy with ISDN)
opioid (+) coombs sympathetic effects post synaptic cortex. Decreases
adrenergic psychiatric receptors aldosterone hypercalciuria,
withdrawal test on heart & BP. neuron renal Ca stones, of drugs that act Uses: SE:
receptors depression, MOA: inhibits ACE & secretion. SE: edema, reflex SE: hypotension,
Reduces renin nephrogenic DI SE: hypoK met on RAAS during angina, hypotension,
suicidal formation of angiotensin HPN, SVT SE: edema, tachycardia, HA, cyanide
release Uses: HPN II. Decrease aldosterone alka, K wasting, the 2nd & 3rd hypoK -
SE: sedation, ideation Uses: HPN (obsolete), HPN term reduces renal migraine reflex angina, toxicity
rebound Uses: BPH, secretion dehydration, tachycardia,
(obsolete) Uses: HPN, HF, DM ototoxicity, sulfa MOA: blocks pericarditis,
HPN emergencies nephropathy SE: hypoK met function & MI, drug-
HPN, dry voltage pulmo HPN, short duration
Uses: Angina Avoid in px alka, dilutional allergy, increases fetal & gatedL-type
mouth prophylaxis, HPN, neonatal morbidity SE: induced lupus hypertrichosis, -not commonly of action: 10
with hx of SE: sedation, Uses: HPN, HF, post-MI, hypoNa, K wasting, hyperuricemia, used bec it is very
Arrythmias, SE: postural hypomagnesemia, Ca channels costipatio hirsutism, salt & mins
SE: First dose derpression severe psychiatric DM nepropathy SE: hypotension, hyperGLUC, sulfa & death (vascular >
orthostatic migraine, hypotension, allergy n, pretibial water retention light sensitive, has
Taper use depression, teratogen, hyperK, nephritis, hypoCa cardiac) -Combination short duration of
hypotension, performance anxiety, dry mouth, edema,
prior to d/c suicidal ideation hypoglycemia, nausea, tx w ISDN for action; given as
Reflex hyperthyroidism, blurred vision, SE: cough, taste
to avoid constipation, anemia, diarrhea METOLAZONE - flushing, HF is more -requires continuous
rebound HPN tachycardia glaucoma disturbance, angioedema, ETHACRYNIC effective than
sexual ACID - a loop Uses: dizzinesss, concomitant use infusion
(less chance), Avoid in px with hypotension, teratogen, appears in cord Angina, HPN ACEi in blacks
dysfunction blood & crosses gingival of diuretics & BBs
dizziness, hx of depression hyperK -ARBs are as diuretic that is not
SE: bronchospasm, plaenta & may a sulfur derivative hyperplasi to block
Antidote: drowsiness, effective as ACEi but compensatory
headache, AV block, heart has less cough cause hypoK, & can be given in SE: a, HF, AV
PHENTOLA responses
MINE weakness, failure, CNS -slows ventricular hypoNa, px with sulfur constipation, block,
sedation, erectile remodelling & increases -Slows ventricular hypoglycemia, allergy sinus
asthenia, remodelling & pretibial
nausea, edema dysfunction survival in HF jaundice & edema, depressio
increases survival in thrombocytopenia n
-delays progression of HF nausea,
DM nephropathy flushing,
TAMSULOSIN Notes: -delays progression dizziness
- most selective May mask symptoms -use of drugs that act on of DM nephropathy -excessive
for prostatic of hypOglycemia in RAAS during 2nd & 3rd cardiac
trim reduces renal use of drugs that depressio
smooth muscle DM -greater
function & increases fetal act on RAAS during n may
2nd & 3rd trim vasodilator
& neonatal morbidity & effect than occur
DOXAZOSIN, CARVEDILOL & death. D/c as soon as reduces renal
function & increases cardiodepres
TAMSULOSIN LABETALOL - pregnancy is detected sant effect
, SILODOSIN (fetal hypotension, fetal & neonatal
combined A & B
& blockade (may used neonatal skull hypoplasia, morbidity & death.
ALDUZOSIN - in anuria, renal failure, renal D/c as soon as
not indicated in pheochromocytoma dysplasia) pregnancy is
females for tx detected (fetal
-may further decrease hypotension,
of HPN GFR in px w renal artery
PROPANOLOL - neonatal skull
IUGR, small placenta stenosis bec of dilation of hypoplasia, anuria,
the efferent arterioles renal failure, renal
& congenital
abnormalities have dysplasia)
been reported with CAPTOPRIL - short t -may further
use, but no 1/2. necessitating 2-4x a decrease GFR in px
adequate & well- day administration w renal artery
contracted studies stenosis bec of
conducted dilation of the
efferent arterioles
METIPRANOLOL -
used as ophthalmic
drops for Glaucoma

 TD

DRUGS FOR ANGINA PECTORIS

VASODILATORS CARDIAC DEPRESSANT OTHERS

METABOLISM
CCBs BETA BLOCKERS MODIFIERS
NITRATES CCBS

TRIMETAZIDINE RANOLAZINE IVABRADINE

ULTRA SHORT
AMYL NITRITE
MOA: release NO,
increases cGMP & relaxes
smooth muscle esp
vascular
Uses: Cyanide Poisoning
SE: reflex tachycardia,
orthostatic hypotension,
headache,
methemoglobinemia
ROA: inhalational
DIHYDRO- PROPANOLOL
SHORT LONG PYRIDINE NON DIHYDROPYRIDINE
Pindolol, Timolol, Labetalol, Carvedilol,
Nadolol, Levobunolol, Metipranolol
MOA: reduces a late,
NITROGLYCERINE prolonged Na current in
TRANS- VERAPAMIL DILTIAZEM MOA: inhibit beta myocardial cells -->
DERMAL
ISDN, ISMN NIFEDIPINE oxidation of FA by increase Ca expulsion via
Amlodipin
inhibiting 3-ketoacyl-coA Na-Ca exchanger --> MOA: increase funny Na
thiolase which enhances decrease intracellular Ca -- current in SA node,
Felodipin glucose oxidation.
MOA:blocks B1 & B2 receptors. Blocks > decrease cardiac force & decreases
Nicardipin Prevents decrease in ATP
MOA: release NO, increases cGMP sympathetic effects on heart & BP. work load. May also modify hyperpolarization, induces
Nisoldipin
Reduces renin release in ischemic/hypoxic state FA oxidation inward pacemaker current
& relaxes smooth muscle esp Clevidipin
vascular --> decrease HR & cardiac
Isradipine work
Uses: Angina prophylaxis, HPN, Uses: angina pectoris, Uses: prophylaxis of
Arrythmias, migraine, performance tinnitus, dizziness angina
Uses: Angina, acute coronary MOA: blocks voltage
syndrome gated L-type Ca anxiety, hyperthyroidism, glaucoma Uses: prophylaxis of
MOA: blocks voltage angina, HF
gated L-type Ca channels (cardiac > SE: EPS, gait instability,
SE: QT prolongation,
channels (cardiac > vascular) restless leg syndrome I
SE: reflex tachycardia, orthostatic SE: bronchospasm, AV block, heart nausea, constipation,
vascular) failure, CNS sedation, erectile dizziness SE: bradycardia, HPN,
hypotension, headache, tolerance
(transdermal) Uses: angina, HPN, dysfunction atrial fibrillation
Interacts with MAO
Uses: angina, HPN, SVT migraine inhibitors CYP3A4 inhibitors increase
MOA: blocks voltage SVT migraine May mask symptoms of hypOglycemia Ranolazine concentration &
Dangerous hypotension with PDE
inhibitors such as Sildenafil gatedL-type Ca channels SE: costipation, in DM DOA
(vascular > cardiac)
SE: costipation, pretibial edema,
nausea, flushing,
pretibial edema,
First pass effect is ~90% (NTG) nausea, flushing, dizzinesss, gingival
Uses: Angina, HPN
dizzinesss, gingival hyperplasia, HF, AV
hyperplasia, HF, AV block, sinus
NTG also decrease plt depression
aggregation SE: constipation, pretibial block, sinus
edema, nausea, flushing, depression
dizziness
Excessive cardiac
Nitrate-induced headache: due to depression may
meningeal blood vessel Excessive cardiac
Greater vasodilator effect depression may occur occur
vasodilation
than cardiodepressant
effect

Complex IV MONDAY DISEASE: due to occupational exposure

(cytochrome to nitrates; alternating development of tolerance (during work
oxidase) of the week) & loss of tolerance (over the weekend) every Monday
ETS is affected
by cyanide.

Antidote for
cyanide
THERAPEUTIC STRATEGIES IN ANGINA: DRUGS THAT CAN CAUSE GINGIVAL HYPERPLASIA:
NapaCa-Pangit ng gingiVa mo!
poisoning: -defect that causes angina pain is inadequate coronary
Lilly Cyanide Kit: oxygen delivery relative to the myocardial oxygen Nifedipine
inhaled amyl
nitrite + IV
requirement Cyclosporine
sodium nitrite + -can be corrected in 2 ways:
IV sodium - increasing oxygen delivery Phenytoin
thiosfulate
- reducing oxygen requirement Verapamil
 TD

DRUGS USED IN HEART FAILURE

POSITIVE INOTROPES VASODILATORS MISCELLANEOUS

Dramatically effective in CHF due to increased afterload
(eg: continuing HPN in an individual who has just had an infarct)

HYDRALAZINE ACE
NITROPRUSSIDE
INHIBITORS & BETA
CARDIAC BETA PDE BNP ANALOG DIURETICS BLOCKERS
SACUBITRIL
AGONIST INHIBITORS NITROGLYCERIN ISDN ARBS
GLYCOSIDE

Used in
For acute combination
Have been shown to NESIRITIDE - CARVEDILOL
DIGOXIN DOBUTAMINE INAMIRINONE severe failure
reduce mortality in increase cGMP; may LABETALOL with Valsartan
with FIRST LINE therapy for HF
(B1 seletive); African Americans BISOPROLOL
Digitoxin MILRINONE congestion be used for acute
decompensated
for both systolic &
FIRST LINE NEBIVOLOL
diastolic failure
DOPAMINE failure but has not DRUGS for Chronic METOPROLOL
It is a prodrug
been shown to Heart Failure
that is
reduce mortality FUROSEMIDE - activated to
MOA: inhibits immediate reduction of Sacubitrilat,
Increase cAMP by Reduced aldosterone
Na/K ATPase; inhibiting its pulmonary congestion secretion, salt & which inhibiits
& severe edema Reduced
Increase breakdown by water retention and progression of the enzyme:
Not appropriate for associated with acute
intracellular Ca chronic failure phosphodiesterase; vascular resistance chronic heart Neprilysin
increasing cardiac HF (responsible for
because of increase intracellular failure B
contractility tolerance, lack of Ca; vasodilation blockers are the degradation
Decrease morbidity & not of value in of ANP & BNP -
orak efficacy & SPIRINOLACTONE &
significant mortality in chronic acute failure & two BP
Uses: HF, nodal Should not be used EPLERENONE - have heart failure lowerong
arrhythmogenic significant long-term may be
arrhythmias in chronic failure peptides that
effects benefits & can reduce detrimental if
because they work mainly by
mortality in chronic systolic
increase morbidity & dysfunction is reducting blood
SE: narrow failure volume. This
therapeutic index, mortality marked
enzyme also
arrythmias, degrades
vomiting, Bradykinin - an
diarrhea, visual inflammatory
changes mediator
exerting potent
Reduced clerance DIGITALIS TOXICITY NARROW THERAPEUTIC INDEX vasodilatory
with Quinidine, -Increase by hypoK, hypoMg & hyperCa action
WALA C PaPa V DiTo
Amiodarone, - Loop diuretics & thiazides may significantly
Cyclosporine, Warfarin
reduce serum K & precipitate Digitalis Toxicity What drugs have
Diltiazem &
Digitalis-induced vomiting may deplete serum Mg
Aminoglycosides
Verapamil. - been shown to
& similarly facilitate toxicity Lithium improve SURVIVAL
Amphotericin B in cases of HF?
Arrythmogenesis
increased by
Carbamazepine ABA, buhay kappa!
CORRECTION OF DIGITALIS TOXICITY
Phenobarbital
hypoK, hypoMg &
hyperCa
-Correction of K/Mg deficiency
-Antiarrhythmic drugs Phenytoin
ACE inhibitors
-drug of choice: LIDOCAINE Vancomycin Beta blockers
-electronic pacemaker may be required in severe cases
-Digoxin Antibodies Digoxin Aldosterone
-Fab fragments; Digibind Theophylline
-may save patients who would otherwise die antagonist

 TD

ANTI
ARRHYTHMICs

1 CLASS 1
SODIUM CHANNEL
BLOCKERS
acts on phase 0

2 CLASS 2
BETA BLOCKERS
acts on phase 4

primarily cardiac beta-adrenoceptor

3 CLASS 3
K CHANNEL BLOCKERS
acts on phase 3

Hallmark: prolongation of AP duration

4 CLASS 4
CALCIUM CHANNEL
BLOCKERS

a b c
blockade & reduction in cAMP: reduction AV conduction velocity is decreased & ERP
-caused by blockade of K influx that are responsible for increased
A B C in both Na & Ca currents, suppression of repolarization of AP
prolong AP shortens AP no effect on AP duration abnormal pacemakers
-results in increase ERP & reduces the ability of the heart to
AV node is particularly sensitive to respond to rapid tachycardia ECG: PR interval is consistently increased
blockers, PR interval usually prolonged

ECG: increase QT interval Effective in arrhythmias that must traverse

Ca-dependent cardiac tissues (AV node)
Cause a state- & use- dependent selective
MOA: Use- & state- dependect

block of Na channels influx;
some block K channels influx.
Slowed conduction velocity &
pacemaker activity; prolonged
AP duration & refractory
period Ibutilide
Mnemonic: Double Quarter Pounder
PROCAINAMIDE DISOPYRAMIDE
Uses: Atrial &
ventricular arrhythmias, Uses: Atrial &
ventricular arrhythmias
esp after MI
SE: arrythmias,
SE: arrythmias,
hypotension, marked
hypotension, lupus-like
syndrome antimuscarinic effects,
HF
HyperK exacerbates
HyperK exacerbates
cardiac toxicity
cardiac toxicity
Crosses into breast milk
Crosses into breast milk
Treatment of Class 1A Overdose:
Mnemonic: Tomato Lettuce Mayo Please
QUINIDINE
Uses: Atrial &
ventricular arrhythmias,
Malaria
SE: arrythmias
(torsades),
hypotension,
Cinchonism (headache,
vertigo, tinnitus),
cardiac depression, GI
upset, autoimmune
reactions (ITP),
hemolytic anemia
HyperK exacerbates
cardiac toxicity
Crosses into breast
milk. Use with extreme
caution in pregnant
LIDOCAINE FLECAINIDE
Mexilentine Propafenone
Tocainide Encainide
Phenytoin Moricizine
More Extra Fries Please
Grp 1B - slows recovery of Na Grp 1C - powerful
channels from inactivation depressant of Na current
leading to prolonged ERP Can markedly slow
Selectively affects ischemic or conduction velocity in
atrial & ventricular cells
depolarized Purkinje &
ventricular tissue (little effect
ECG effects: no effect on
on ECG) ventricular AP duration or
QT interval; increase QRS
duration
MOA: Highly seletive use &
state- dependent Na influx
block; minimal effect in normal
tissue; no effect on K influx MOA: Selective use &
state- dependent block of
Na influx; slowed
Uses: DOC for ventricular
conduction velocity &
arrhythmias post MI, Digoxin-
induced arrythmias pacemaker activity
SE: CNS stimulation, Uses: refractory
arrhythmias
cardiovascular depression,
arrythmias, allergy,
agranulocytosis (Tocainide) SE: increased
arrhythmias
(proarrhythmic effects),
Only affect ischemic tissue
CNS excitation
HyperK exacerbates cardiac
toxicity HyperK exacerbates
cardiac toxicity
S A D
Mnemonic: K, SAD ! depression of Ca currents
PROPANOLOL
Metoptolol ESMOLOL
AMIODARONE
Timolol DOFETILIDE
SOTALOL Dronedarone
Vernakalant
NON DHYDROPYRIDINE
MOA: Blocks Beta MOA: Selectively blocks
receptors; slowed beta 1 receptors;
pacemaker activity slowed pacemaker
MOA: K influx block &
activity beta adrenoceptor MOA: Strong K influx
block
Uses: Post MI block produces marked MOA: Selectively K
prolongation of AP &
prophylaxis against Uses: Acute influx block; prolonged
sudden death, perioperative & refractory period. Grp 1 AP & QT interval
Uses: Ventricular
Thyrotoxicosis thyrotoxic arrhythmias, activity slows condution
arrhythmias, AFib, SVT velocity; grp2 & 4
SVT DILTIAZEM VERAPAMIL
activity confers Uses: Treatment &
SE: bronchospasm, SE: dose-related additional antiarrythmic prophylaxis of AFib
cardiac depression, AV SE: bronchospasms, activity
torsades de pointes,
block, hypotension cardiac depression, AV
excessive beta blockade SE: torsades de pointes
block, hypotension (sinus bradycardia,
Uses: refractory
In CHF, reduces asthma)
arrhythmias, used off-
progression and label in many
decreases incidence of arrhythmias
Drug present in breast MOA: blocks voltage MOA: blocks voltage
potentially fatal gated L-type Ca gated L-type Ca
milk
arrhythmias channels (cardiac > channels (cardiac >
SE: microcrystalline
vascular) vascular)
deposits in cornea &
SOTALOL is a beta skin, thyroid
blocker anti arrhythmic dysfunction (hyper or Uses: angina, HPN, SVT Uses: angina, HPN, SVT
that has Class 3 migraine migraine
hypo), paresthesia,
properties. Sotalol & tremor, pulmonary
Amiodarone aslo have fibrosis
group 2 effects SE: costipation, SE: costipation,
pretibial edema, pretibial edema,
MOST EFFICACIOUS of nausea, flushing, nausea, flushing,
METOPROLOL & all anti arrhythmics dizzinesss, gingival dizzinesss, gingival
TIMOLOL is
hyperplasia, HF, AV hyperplasia, HF, AV
concentrated in breast block, sinus depression block, sinus depression
milk Drugs that cause Has the longest t1/2

-Sodium Lactate to reverse drug- patients LIDOCAINE is the least

cardiotoxic among Contraindicated for post Agranulocytosis: Excessive cardiac Excessive cardiac
Can cause fetal harm
induced arrhythmias conventional anti arrhythmics; MI arrhythmias CCCAPPIT Me! (cardiac, thyroid,
depression may occur depression may occur
Reduces clearance of never given PO due to
-Pressor sympathomimetics to reverse Digoxin significant first pass effect Enters breast milk Clozapine neurodev, neurological
& growth defects in Should be avoided in Should be avoided in
neonates) ventricular tachycardia ventricular tachycardia
drug-induced hypotension if indicated
PHENYTOIN - increased
CoTrimozaxole
incidence of major
malformations (orofacial clefts,
Colchicine
cardiac defects, fetal hydantoin
syndrome effect) & cognitive
Aminopyrine Amiodarone
defects has been reported for Phenylbutazone Toxicity:
pregnant who use it for Pulmonary fibrosis
epilepsy; also secreted in
human milk
PTU Paresthesias
Indomethacin Tremors
Tocainide Thyroid dysfxn
Corneal deposits
Methimazole Skin deposits
 DIURETICS TD

SALT EXCRETION WATER EXCRETION

PCT TAL DCT CCD OSMOTIC ADH

-last tubular site of Na reabsorption

-carries out isoosmotic reabsorption of
amino acids, glucose & numerous cations
-major site for NaCl & NaHCO3
reasbsorption (60-70%)
-site of uric acid transport
-responsible for a significant % of NaCL
reabsorption via Na-K-2CL transporter
-site of Ca & Mg reabsorption
-Prostaglandins are important in
maintainung glomerular filtration
-actively pumps Na & Cl out of the lumen of -responsible for reabsorbing 2-5% of total filtered Na MANNITOL
the nephron via Na-Cl transporter -under te influence of aldosterone, reasbsoption of Na Glycerin
-responsible for ~5-8% of Na reabsorption occurs via channels, accompanied by an equivalent AGONIST ANTAGONIST
-Ca is also reabsorbed in this segment under loss of K or H+ Isosorbide
the contol of PTH -primary site of acidification of urine
Urea
-last site of K excretion

CARBONIC ANHYDRASE MOA: osmotically retains water in VASOPRESSIN CONIVAPTAN Tolvaptan

INHIBITORS LOOP DIURETICS THIAZIDE K SPARING tubule by reducing reabsorption in
PCT, descending loop of Henle & CD; Desmopressin Lixivaptan
in the periphery, mannitol extracts
water from cells Terlipressin Demeclocycline Lithium

Uses: rhabdomyolysis, hemolysis,

increased ICP, acute glaucoma
ACETALOZAMIDE FUROSEMIDE HYDROCHLORTHIAZIDE
Dorzolamide Bumetanide Chlorthalidone SE: transient volume expansion
ALDOSTERONE
Indapamide ANTAGONISTS ENACS INHIBITORS (hypoNa, pulmonary edema, followed
by HyperNa), headache, N/V, MOA: agonists at V1 & V2 ADH receptors; MOA: antagonist at V1 & V2
Brinzolamide Torsemide activate insertion of aquporin in water receptors
dehydration
Dichlorphenamide Ethacrynic acid Metolazone channles in collecting tubule;
vasoconstricton Uses: SIADH, hypoNa
Methazolamide Bendroflumethiazide Used to maintain high urine flow

MOA: inhibits carbonic anhydrase; in
glaucoma, secretion of aqueous humor
is reduced; in mountain sickness,
metabolic acidosis increases
respiration
Uses: glaucoma, mountain sickness,
edema with alkalosis
SE: drowsiness, paresthesias, sulfa
allergy, renal Ca stones, K wasting,
hyperCl NAGMA, hepatic enceph in
cirrhotic px
Enters the breast milk
Diuresis is self limiting after 2-3 days
Hydroflumethiazide Uses: central DI, nocturnal enuresis, SE: infusion site rxns, hyperKa,
hemophilia, von Willerbrand's dse nephrogenic DI, renal filaure
MOA: inhibit Na-K-2Cl transporter; cause Methyclothiazide (lithium, demeclocycline), bone &
powerful diuresis & increase Ca excretion SE: hypoNa, HPN teeth abnormalities
Polythiazide SPIRINOLACTONE AMILORIDE (demeclocycline)
Uses: HF, pulmonary edema, HPN, Quinethazone Eplerenone Triamterene Increses the Factor VIII activity in mild
hyperCa, acute renal failure, anion hemophilia A or von Willerbrand dse Central Pontine Myelinolysis
overdose Trichlormethiazide may occur with rapid correction of
hypoNa
TERLIPRESSIN:not recommended during
SE: hypoK metab alkalosis, K wasting, pregnancy as it can cause uterine contrxn &
dehydration , ototoxicity, sulfa allergy, may decrease uterine blood flow; may have LIXIVAPTAN is considered an
hyperuricemia, hypoCa, hypoMg, MOA: inhibit Na-Cl transporter; cause harmful effects on pregnany & fetus Orphan Drug
nephritis moderate diuresis & reduced Ca MOA: inhibits ENaC epithelial
excretion MOA: steroid inhibitors of sodium channels; reduces Na
cytoplasmic aldosterone receptor; reabsorption & K excretion
reduce K exretion
Synergistic ototoxicity with
Aminoglycosides Uses: HPN, HF, hypercalciuria, renal Ca
stones, nephrogenic DI Uses: hypoK
Efficacy decreased by NSAIDS Uses: hyperaldosteronism, HPN, HF,
hypoK
SE: hypoK metab alka, dilutional SE: hyperK, acute renal failure (with
hypoNa, K wasting, sulfa allergy, indomethacin), kidney stones,
hyperGLUC SE: hyperK, gynecomastia metabolic acidosis
LOOP (spiriniolactone), impotence, BPH,
hypoC metab acidosis
DIURETICS Synergistic effect with Loop diuretics Should never be given with K
supplements
TOXICITY Efficacy decreased by NSAIDS EPLERENONE - reduces
progression of DM nephropathy &
OH DANG! reduces mortality in post MI
Ototoxicity
Hypokalemia
GYNECOMASTIA
Dehydration Spirinolactone
Allergy to Sulfa Digoxin
Cimetidine
Nephritis Alcohol
Gout Ketoconazole
 TD

DYSLIPIDEMIA DRUGS

STATINS BILE ACID RESINS CHOLESTEROL ABSORPTION BLOCKERS

NIACIN FIBRATES
D OC FO R HIG H CHO LES T EROL D OC FOR HIGH T Gs
D OC FOR LO W HDL
CHOLESTYRAMINE
SIMVASTATIN EZETIMIDE SITOSTEROL
Colesevelam GEMFIBROZIL
Atorvastatin, Rosuvastatin, Fluvastatin,
Pravastatin, Lovastatin, Pitavastatin Colestipol FenoHibrate
MOA: decreases catabolism
of apoA1; decreases VLDL BezaHibrate
syntheis & secretion from
MOA: selective inhibitor of MOA: Cholesterol analog, takes the liver; decreases LDL
NPC1L1 transporter, decreasing the place of dietary & biliary cholesterol concentrations;
MOA: binds bile acids, preventing their interstinal absorption of increases HDL cholesterol
reabsorption & increasing cholesterol cholesterol, decreasing intestinal
MOA: inhibits rate-limiting enzyme in cholesterol cholesterol & other phytosterols absorption of cholesterol & other MOA: activates PPAR-alpha & increases
biosynthesis. Increased hepatic cholesterol uptake. utilization for replacement --> upregulates --> decreases choleterol hepatic
phytosterols expression of lipoprotein lipase &
Increased high-afHinity LDL receptors. Decreased LDL LDL receptors ---> modestly lowers LDL pool, increases hepatic LDL Uses: hypercholesterolemia
apolipoproteins (apo-AI, apo-AII); lowers
levels. Causes modest reduction in triglycerides. levels receptors --> decreases LDL & (low HDL, high LDL/VLDL) TGs; decreases secretion of VLDL;
phytosterols Uses: hypercholesterolemia increases HDL

(high LDL), phytosterolemia
Uses: Hypercholesterolemia (high LDL), ACS/ Uses: Hypercholesterolemia (high LDL), SE: Hlushing, pruritus, rashes,
atherosclerotic vascular dse (primary & secondary pruritus in cholestasis, digitalis toxicity Uses: hypercholesterolemia acathosis nigricans, GI Uses: DOC for hyperTGs;
prevention), Ischemic stroke (high LDL), phytosterolemia SE: GI upset, bloating, impotence irritation, hepatotoxicity hypercholesterolemia (low HDL, high
SE: constipation, bloating, gritty tase, (rare), coronary events (mild), hyperuricemia, IGT, LDL), fat redistribution syndrome
arrythmias, amblyopia
SE: hepatotoxicity, myopathy, rhabdomyolysis, GI steatorrhea, gallstones (rare), malabsorption SE: hepatotoxicty (increased
distress (vit K) with statin use), myositis
SE: nausea, rashes, leukopenia,
Avoid in patients with PUD. hemoconcentration, incrreased risk of
Increased risk of mupotahy & rhabdomyolysis when Increases TGs & VLDL in patients with high Potentiates effects of anti cholesterol gallstones
Synergistic LDL-lowering effect
used with Hibrates. TGs. with statins. DRUGS THAT CAUSE hypertensives (vasodilators,
ganglion blockers).
Given before bedtime bec cholesterol synthesis Treat constipation with Hiber supplements/ Considered a prodrug. CUTANEOUS Increased risk of myopathy &
predominantly occurs at night. psyllium. Decreases Hibrinogen and rhabdomyolysis when used with statins.
FLUSHING: increase t-PA
Contraindicated for use in pregnant bec safety is not Avoid in patients with diverticulitis. Avoided in px with hepatic or renal
established and no appraent beneHit. Interferes with absorption of some drugs & dysfunction.
vitamins. V Vancomycin May increase LDL in px with familial
Shoudl be taken with meals. combined hyperlipoproteinemia.
SIMVASTATIN & LOVASTATIN - prodrugs; all the rest
are active form Non-absorbable polymers that bind bile acids
A Adenosine Higher risk of gallstine formation if given
w/ resins

ROSUVASTATIN, ATORVASTATIN & SIMVASTATIN -
& similar steroids in the intestines preventing
their absorption N Niacin
greater maximal effect that other statins

C CCBs
If given with resins, give at least 1hour before or 4 hours

Other Anti-Dyslipidemic:
after resin administration (resins decreases the
DISADVANTAGEOUS ANTI DYSLIPIDEMIC COMBINATIOS: ASPIRIN PROBUCOL
absorption of statins).
pretreatment Antioxidant that inhibit the oxidation of LDL & lowers
Has CYP450 dependent metabolism. FIBRATE + RESIN = increased risk of cholelithiasis reduces flushing. cholesterol in the blood by increasing rate of LCL
catabolism in cholesterol elimination from the body. It
STATIN + RESIN = impaired statin absorption may inhibit early states of cholesterol biosynthesis &
slightly inhibit dietary cholesterol absorption. May also

inhibit the oxidation & tissue deposition of LDL, thereby
STATIN + FIBRATE = increased risk of myopathy & rhabdomyolysis inhibiting atherogenesis; Used to lower LDL & HDL
cholesterol, yet has little feect on serum TG or VLDL.
 TD

histaminergic agents

H1 BLOCKERS H2 BLOCKERS

1st generation 2nd generation

CIMETIDINE
Ranitidine, Famotidine, Nizatidine

DIPHENHYDRAMINE CETIRIZINE
Brompheniramine, Chlorpheniramine, Cyclizine, Meclizine, Loratadine, Fexofenadine,
Buclizine, Hydroxyzine, Promethazine, Cyproheptadine, Desloratadine, MOA: competitive pharmacologic block of H2 receptors
Clemastine, Tripelennamine Levocetirizine, Terfenadine,
Astemizole, Ebastine, Uses: PUD, Zollinger-Ellison syndrome, GERD; For nocturnal
Azelastine, Bilastine, acid secretions
Rupatadine
SE: CPY450 inhibitor & antiadrogen effects like gynecomastia
(Cimetidine only); decreases hepatic blood \low
MOA: competitive pharmacologic block of peripheral & CNS H1
receptor plus alpha & muscarinic receptor block. Anti motion sickness
Used in ICU setting to prevent gastric erosion & hemorrhage.
effect.
Reduction of nocturnal acid secretion in gastric & duodenal
ulcer, accelerate heaing & prevent recurrences.
Uses: hay fever, angioedema, motion sickness, insomnia, dystonia, MOA: competitive pharmacologic
anti-emetic (Promethazine), for serotonin syndrome block of peripheral H1 receptors;
(Cyproheptadine) No autonomic or anti motion Usual half life: 1-3 hours
sickness
SE: drowsiness, ALICE in wonderland, anorexia, orthostatic
hypotension Uses: hay fever, angioedema,
urticaria
More likley to block autonomic receptors, also has alpha1 blocking &
local anesthetic effect. SE: None

CYCLIZINE - more anti motion sickness action, less sedative & Fatal arrhythmias from interaction
autonomic effects. between azoles/erythromycin &
terfenadine/astemizole.
PROMETHAZINE - less antimotion sickness, more sedative &
autonomic effects. Usual half life: 12-24hours

Usual half life: 4-12hours

 TD

SEROTONIN: 5HT)

5HT1D 5HT2 5HT3 5HT4

Gq; increase IP3, DAG

Smooth muscle, platelets Ligand gated ion channel Gs, increase cAMP
Gi; decrease cAMP
Effects: CNS excitation, smooth Area postrema (CNS), sensory Presynaptic nerve terminals
Brain
muscle contraction/relaxation, & enteric nerves in enteric nervous system
Effect: Synaptic inhibition
vasodilation, diarrhea, Effect: vomiting Effect: intestinal motility
brochoconstriction

SUMATRIPTAN
ONDANSETRON
Almotriptan, Eletriptan, VASOSELECTIVE UTEROSELECTIVE
Frovatriptan, Naratriptan, Granisetron, Dolasetron,
Palonosetron, Alosetron
Rizatriptan, Zolmitriptan

ERGOTAMINE ERGONOVINE
Dihydroergotamine Methylsergide Methylergonovine MOA: 5HT3 receptor antagonist; blocks
chemoreceptor trigger zone & enteric nervous
system 5HT3 receptors
MOA: 5HT1D receptor agonist; cause
vasoconstriction; modulates neurotransmitter
release Uses: chemotherapy & postoperative vomiting;
irritable bowel disease (Alosetron only)
MOA: partial agonist at alpha & 5-HT receptors,
Uses: DOC for acute migraine, cluster headache some have potent agonist effect at dopamine
MOA; partial agonist at alpha and 5HT2
receeptors, some have potent agonist effect receptors SE: diarrhea, headache, malaise, QRS & QT
at Dopamine receptors prolongation (Dolasetron only), constipation
SE: paresthesia, dizziness, chest pain, coronary
(Alosetron only)
vasospasm, injection site rxn Uses: postpartum bleeding, migraine
Uses: migraine, cluster headache
All are per orem except for Sumatriptan which SE: GI upset (nausea, vomiting, diarrhea),
can also be given intranasally, trandersmal, & uterine spasm, abortion
SE: GI upset, vasospasm, gangrene, uterine
IV.
spasm, retroperitoneal \ibrosis
(Methysergide only) The uterus becomes more sensitive to ergots during
All has 2-27 hrs DOA excet for Sumatriptan pregnancy, produce very powerful & long-lasting
DOA: 2-4h contraction, leading to decreased bleeding.
Antidote: NITROPRUSSIDE
Nevery give before delivery of placenta.
Can cause epinephrine reversal due to
partial agonist effect on alpha receptors. Methylergometrine/ Methylerobasin (other name of
Methylergonovine) is a homolg of ergonovine.

 TD

vertigo drugs

betahistine cinnarizine dimenhydrinate

DRUGS USED FOR MIGRAINE

FLUNARIZINE
Selective calcium entry blocker with
MOA: strong antagonist of H3 receptor (leads MOA: an anti histamine & CCB; calmodulin binding properties and H1
to increased levels of NT: histamine, Ach, NE, promotes cerebral blood Llow
serotonin & GABA), and weak agonist of H1 antagonistic activity.
receptor (causes local vasodilation &
increased permeability in the inner ear)
Uses: cerebral apoplexy, post First generation anti histamine used Effective in the prophylaxis of
trauma cerebral symptoms & for nausea, vomiting, and dizziness
cerebral atherosclerosis; more caused by motion sickness. migraine, occlusive peripheral vascular
Uses: balance disorders or to alleviate vertigo commonly prescribed for nausea
symptoms associated with Meniere's disease & vomiting due to motion disease, vertigo and as adjuvant
sickness, chemotherapy, vertigo
or Meniere's disease therapy for epilepsy

 TD

prostaglandins

pge1 pge2 pgf2alpha pgi2

Gs, Gq
Gs,
Vascular smooth muscle Gs, Gq
Gq Vascular smooth muscle
relaxataion, protective effects Vascular smooth muscle relaxation,
on gastric mucosa, maintains Increases uterine tone, decreases IOP relaxation (peripheral,
maintains PDA, increase uterine tone pulmonary, coronary)
PDA

CARBOPROST LATANOPROST
MISOPROSTOL DINOPROSTONE EPOPROSTENOL
ALPROSTADIL Bimatoprost, Travoprost, Bimatoprost, Travoprost,
Gemeprost Sulprostone Unoprostone Beraprost, Iloprost, Treprostinil
Unoprostone

MOA: Activates EP receptors. Causes MOA: Low concentrations: contract; Higher

increased HCO3 & mucus secretion in MOA: Activates EP receptors, causes concentration: relax uterine & cervical
stomach. Uterine contraction. vascular smooth muscle relaxation smooth muscle; soften cervix at term before MOA: activates FP receptors; increase
& vasodilation. induction with oxytocin outWlow of aqueous humor, reduces MOA: activates IP receptors. Causes
Uses: PUD, prevention of NSAID-induced
MOA: activates F2alpha receptors intraocular pressure vasodilation. Reduces platelet
gastric mucosal injury, abortifacient Uses: Maintenance of PDA, erectile
aggregation.
Uses: induction of labor (cervical ripening),
dysfunction abortifacient Uses: control of postpartum hemorrhage, for Uses: glaucoma
refractory postpartum bleeding, abortifacient
SE: abdominal pain, diarrhea, uterine Uses: pulmo HPN, reduces platelt
cramping, miscarriage, teratogenic effect
SE: apnea, hypotension, arrhythmia, SE: cramping, fetal trauma SE: alters color of the iris causing permanent aggregation in dialysis machines
(Moebius syndrome) priapism, lightheadedness SE: vomiting, diarrhea, transient eye color change
bronchoconstriction

Approved abortifacient in the 2nd SE: hypotension, Wlushing, headache
May also be used together with Given as injection into the trimester. Although effective in inducing May cause vomiting, diarrhea, transient
Mifepristone or Methotrexate as safe cavernosa for erectile dysfunctiion labor, it produces more SE than other bronchoconstriction if given systematically
abortifacient. oxytocins

 TD

ASTHMA DRUGS

BRONCHODILATORS ANTI INFLAMMATORY LEUKOTRIENE ANTAGONIST ANTI-IgE ANTIBODY

LEUKOTRIENE LEUKOTRIENT
MUSCARINIC MAST CELL SYNTHESIS RECEPTOR
BETA AGONIST ANTAGONIST METHYLXANTHINE STABILIZER CORTICOSTEROIDS OMALIZUMAB
INHIBITOR ANTAGONIST

FLUTICASONE MOA: binds IgE antibodies on

IPRATROPIUM
THEOPHYLLINE Beclomethasone, mast cells; reduces reaction to
Tiotropium, CROMOLYN MONTELUKAST inhaled antigen
SABA LABA Aminophylline, Budesonide, Ciclesonide, ZILEUTON
Umeclinidium, Nedocromil, Lodoxamide Flunisolide, Mometasone, ZaXirlukast, Pranlukast
Glycoyrronium Pentoxifylline, Doxofylline
Triamcinolone Uses: prophylaxis of severe,
refractory asthma not
responsive to all other drugs

SE: fever, angioedema,
anaphylactin reactions,
SALBUTAMOL FORMOTEROL MOA: blocks muscarinic MOA: inhibitor of
idiopathic severe
receptors in bronchial smooth thrombocytopenia,
ALBUTEROL Arformoterol, phospholipase A2; reduces
muscle; prevents vagal- expression of cyclooxygenase MOA: inhibitor of 5- nasopharyngitis, upper
Bambuterol, Cleneterol, lipooxygenase; reduces MOA: blocks cysteinyl abdominal pain
Levalbuterol, Terbutaline, stimulared MOA: phosphodiesterase leukotriene-1 receptor for
Vilanterol, Indacaterol, inhibition; adenosine receptor MOA: prevents calcium inXlux synthesis of leukotrienes;
Metaproterenol, bronchoconsstriction and stabilize mast cells --> leukotrienes C4, D4 & E4;
Olodaterol, Salmeterol antagonist; causes Uses: asthma prophylaxis preevnts airway inXlammation
Pirbuterol, Procaterol, preventing degranulation and & bronchoconstriction prevents airway inXlammation Binds IgE antibodies on
bronchodilation (DOC), COPD, allergic rhinitis, & bronchoconstriction
Fenoterol, Bitolterol mnemonic: FAB C VIOS Uses: acute asthma, COPD release of histamine, sensitized mast cells &
leukotrienes and other Xirst line treatment for
prevents activation by BA
Uses: asthma (prophylaxis mediators moderate to severe BA, anti Uses: asthma prophylaxis; triggers & subsequent release
inXlammatory for auto immune Uses: asthma prophylaxis,
SE: dry mouth, blurred vision, against nocturnal attacks); exercise-, antigen- & aspirin- of inXlammatory mediators.
diseases & cancer, for immune exercise-, antigen-, and aspirin-
anti cholinergic effects intermittent claudication induced bronchospam Humanized murine monoclonal
Uses: asthma prophylaxis, suppresion induced bronchospasm
(Pentoxifylline only) antibody, very expensive &
allergies (ophthalmic,
MOA: activates beta2 receptors nasopharyngeal, only administered IV.
Less toxic than beta agonists in SE: Xlulike synrome, headache,
in bronchial smooth uscle, gastrointestinal) SE: oropharyngeal candidiasis, drowsiness, dyspepsia, SE: GI upset, insomnia,
aptients with COPD. SE: CNS stimulation (insomnia, neuropyschiatric effects,
causes bronchodilation MOA: activates beta2 receptors seizure, anorexia), cardiac minimal systemic steroid
Tiotropium & Umeclidinium hepatitis, elevation of liver
in bronchial smooth muscle, toxicity (ex. adrenal enzymes, hepatotoxic Churg-Strauss syndrome (rare)
causes bronchodilation. stimulation (arrhythmias),
have longer DOA than tremors, increased BP, diuresis, SE: cough, airway irritation suppression), mild growth
Uses: acute asthma attacks Potentiation of corticosteroid Ipratropium. retardation
increase GI motility No bronchodilator action.
(DOC) action. No bronchodilayor action.
Ipratropium given as aerosol
has little systemic effects. No bronchodilator action but Not recommended for acute BA
can prevent Inhibit synthesis of arachidonic Not recommended for acute BA
Antidote in overdosage: BETA attack attack.
SE: tachycardia, tremors, Uses: asthma prophylaxis (not Has no effect on the chronic bronchoconstriction caused by acid by inhibiting
BLOCKERS
nervousness, restlessness, for acute relief) inXlammation aspect of atntigens (both in the early and phospholipase A2. REduces
arrhythmias when used bronchial asthma. late BA responses). expression of COX and LT.

excessively, loss of Glycopyrronium does not cross Higher clearance in Unusually insoluble chemicals Increase responsiveess of beta
responsiveness (tolerance, SE: tachycardia, tremors, adolescents & smokers. receptos in the airway.
nervousness, restlessness, the BBB, and consequently has so rarely used.
tachyphylaxis) no to few central effects. It may
arrhythmias when used Narrow therapeutic window. May be given as ophthalmic Bind to intracellular receptors
excessively, loss of be used as a monotherapy as and activate glucocorticoid
maintenance for COPD. It may Usual DOA: 12hrs solution for allergic
May precipitate arrhytmias in responsiveness (tolerance, conjunctivitis. response elements in the
patients with concurrent COPd tachyphylaxis) also be used as an anti- Causes bronchodilation & nucleus leading to sythesis if
spasmodic & reduce salivation increased strength of May also be given (Off-label) substances that prevent full
and heart disease. for Food allergy and IBD.
with some anesthetics. contraction of diaphragm expression of inXlammation &
Usual DOA: 204 hrs Increase asthma mortality allergy.

All are given inhalational. when used alone.
For status asthmaticus: use IV
Salbutamol & Terbutaline is May precipitate arrhythmias. Prednisolone or
also available PO.
Usual DOA: 12hrs Hydrocortisone.
Terbutaline can also be given Prednisolone is the active
IV. metabolite of Prednisone.
Ciclesonide has lowest
systemic steroid toxicity.

 TD
DRUGS FOR COUGH

MUCOLYTIC EXPECTORANT ANTITUSSIVES OTHERS

N-ACETYLCYSTEINE VITEX
CENTRALLY PERIPHERALLY NEGUNDO
Carbocisteine, Ambroxol, GUIAFENESIN ACTING ACTING
Bromhexine, Erdosteine (LAGUNDI)

MOA: may act as irritant to gastric vagal OPIOID NON OPIOID LEVODROPOPIZINE
receptors, & recruit efferent
MOA: decrease sputum activity; usually parasympathetic reFlexes that cause
derivatives of cysteine; reduce disulFide glandular exocytosis of a less viscous mucus
bridges that bind glycoproteins to other mixture Inhibits PDE III & inhibits
proteins such as albumin; act as antioxidant Ca2+ entry (acts as CCB),
& may reduce airway inFlammation which partly explain its
Uses: cough bronchodilatory effects.

DEXTROMETHORPHAN BUTAMIRATE MOA: non opioid drug
with a peripheral action
Uses: cough (available as IV, PO, IM &
inhalational forms) SE: drowsiness, incomplete or infrequent Codeine CITRATE by inhibiting the afferent Considered a potent anti
bowel movements, inducing of a relaxed pathways that generate
inFlammatory agent & acts
easy state, stomach cramps, headache, rash, the cough reFlex via inhibition of COX2
SE: chest tightness, disagreeable odor, nausea, vomiting, stomach upset (modulates C-Fiber
without much interfering
drowsiness, fever, hemoptysis, increased activity) COX1 pathways.
volume of bronchial secretions, irritation of
tracheal or bronchial tract, nausea, Are often emetics (Ipecac, Guiafenesin) MOA: decreased sensitivity of the
rhinorrhea, stomatitis, vomiting medullary/ CNS cough centers to Uses: cough Traditionally used in
peripheral stimuli & decreased MOA: act through receptors in
the brainsteam to inhibit hyperactive respiratory
mucosal secretion disorder, has medicinal
Orally avaialble drugs are well-tolerated, but cough SE: nausea, vomiting,
heartburn, diarrhea, importance in asthma.
of little beneFit in acute respiratory condition
Uses: cough fatigue, weakness,
Uses: cough drowsiness, dizzines,
headache, palpitations

SE: decrease secretions in the
SE: somnolence, nausea,
bronchioles, thickens sputum &
inhibit ciliary activity, reducing vomiting, diarrhea, dizziness, Doses not cause side
clearance of thickened sputum; hypotension effects such as
constipation constipation or
respiratory depression
Centrally acting antitussive but which can be produced by
MORPHINE may be effective but is neither chemically or
opioid antitussive.
indicated only in intractable cough pharmacologically related to
opioids
from bronchial carcinoma,

DEXTROMETHROPHAN has no
addictive potential, no analgesic
effect, produces less constipation
and inhibition of mucociliary
clearance.

 TD

HEMATOPOIETIC DRUGS

RBC PLATELET GRANULOCYE

IRON VITAMIN EPO OPRELVEKIN MYELOID

(IL-11) PERIPHERALLY
GROWTH
ACTING
Thrombopoietin, FACTOR
Eltrombopag,
FOLIC ACID
CYANOCOBALAMIN EPOETIN ALFA Romiplastim
Folacin (Pteroglutamic
FERROUS Hydroxocobalamin acid), Folinic acid/ Darbepoetin alfa, FILGRAMSTIM
SULFATE Methylcobalamin Leucovorin, L- Methoxypolyethylene glycol-
epooetin alfa Sargramostim,
methylfolate MOA: recombinant form of an PLERIXAFOR
endogenous cytokine; PegGilgramstim, Plerixafor,
oral: Ferrous gluconate, Ferrous
activates IL-11 receptors Lenogramstim
fumarate, Ferrous carbonate
parenteral: Iron dextran, MOA: cofactor required for Uses: secondary prevention of
essential enzymatic rxns to MOA: precursor of an MOA: agonist of erythropoietin thrombocytopenia in px
Sodium ferric gluconate receptors expressed by red cell
complex, Iron sucrose methionine, & metabolize essential donor of methyl undergoing cytotoxic
methylmalonyl-CoA groups used for synthesis of progenitors chemotherpay for non myeloid
amino acids, purines, & cancers MOA: binds receptors on myeloid
deoxynucleotide A hematopoetic stem cell mobilizer;
Uses: Vit B12 deGiciency, Uses: anemia esp associated with progenitor & stimulates cell blocks binding of stromal cell-
megaloblastic anemia chronic renal failure, HIV infection, maturation & proliferation; derived factor-1-alpha, found on
SE: fatigue, headache, accelerates neutrophil recovery &
(pernicious anemia, gastric Uses: megaloblastic anemia, cancer, prematurity, for dizziness, anemia, Gluid bone marrow stromal cells, to the
resection) prevention of neural tube prevention of the need for reduces incidenceof infection CXC chemokine receptor 4 (CXCR4).
accumulation in the lungs,
defects (spina biGida), transfusion in px undergoing
MOA: required for the biosynthesis of certain types of elective surgery transient atrial arrhythmias
heme & heme-containing proteins, prevention of coronary artery Uses: neutropenia assoc with
including hemoglobin & myoglobin SE: no signiGicant toxicity The inhibition results in the
disease chemotherapy, myelodysplasia,
Given SC OD. mobilization of progenitor &
SE: HPN, thrombosis, pure red cell aplastic anemia; mobilization of hematopoietic stem cells from the
Uses: iron deGiciency anemia, iron Parenteral form is required for aplasia peripheral blood ells in bone marrow into peripheral blood.
SE: no signiGicant toxicity
supplementation pernicious anemia & other preparation for hematopoietic

malabsorption syndrome. stem cell transplantation
SE: black stools (may obscure acute GI Folic acid is not toxic in Hemoglobin levels hould be ELTROMBOPAG Used for mobilization of

loss) overdose but large amounts maintained <12g/dL. Small- molecule thormbopoietin hematopoietic stem cells to
Hydroxocobalamin has a longer can partially compensate for
(TPO)-receptor agonist that SE: bone pain (arthralgia), fever, peripheral blood for collection and
interacts with human TPO edema, splenic rupture
ACUTE OVERDOSE: necrotixing
t1/2 than cyanocobalamin. Vit B12 deGiciency & put receptor transmembrane domain subsequent autologous
Performance-enhancing drug in
gastroenteritis, abdominal pain, bloody people with unrecognized Vit athlete (prohibited use) of human TPO-receptor & initiates transplantation in patients with NHL
diarrhea, shock, lethargy, dyspnea B12 deGiciency (which are not signaling cascades that induce
PegGilgrastim has a longer t1/2. & Multiple Myeloma.
Has a storage of up to 5yrs in the proliferation & differentiation of
liver. compensated by folic acid).
megakaryocytes from bone
CHRONIC IRON OVERDOSE: Darbepoietin is once a week marrow progenitor cells; used for
hemochromatosis, organ failure (heart, administration, while Methoxy treatment of thrombocytopenia in
liver, pancreas, etc), death Mecobalamin is the shorter term Only modest amounts are Polyethylene Glycol -Epoetin Beta adults & pediatric px >5yr with
for Methylcobalamin. stored in the body. is 1-2x per month administration. chronic ITP with insufficient
response to corticosteroids, Ig or
splenectomy.

IRON CONTENT DEFEROXAMINE (Deferasirox, Deferiprone)

Class: Heavy Metal Chelator

Fe carbonate / Carbonyl Iron – 100%
MOA: Chelates excess iron ROMIPLASTIN
Fe fumarate – 33 %
Uses: Acute iron poisoning, hemochromatosis not adequately treated by Fusion antibody-peptide that is a
Fe sulfate, dried – 30% phlebotomy
thrombopoietin receptor agonist;
stimulates proliferation,
Fe sulfate, hydrated – 20% SE: hypotension, ARDS, neurotoxicity, increased susceptibility to infections differentiation, & activity of
Ferric ammonium sulfate – 18% DEFEROXAMINE is used for acute intoxication (IV dorm) while DEFERASIROX
monocytes, neutrophils eosinophils,
& macrophages; Used for
Fe gluconate – 12% & DEFERIPRONE are for chronic (oral) thrombocytopenia

 TD
DRUGS USED IN COAGULATION DISORDERS

ANTIPLATELET ANTICOAGULANT THROMBOLYTIC PRO CLOTTING

ASPIRIN GPIIb/IIIa INHIBITORS ADP INHIBITORS PDE INHIBITORS INDIRECT DIRECT T-PA DERIVATIVES
ANTIPLASMIN /
VITAMIN K ADH AGONIST
SERINE PROTEASE
Acetylsalicylic acid/ ASA AMINOCAPROIC ACID INHIBITOR

ABCIXIMAB LEPIRUDIN ATEPLASE

CLOPIDOGREL Vit K1 (Phytonadione), Vit
DIPYRIDAMOLE WARFARIN Desirudin, Bivalrudin, Anistreplase, Reteplase, DESMOPRESSIN
EptiNibatide Ticlopidine, Prasugrel, HEPARIN LMW HEPARIN TRANEXAMIC ACID K2 (Menadione), Vit K3 APROTININ
Cilostazol Dicumarol, Anisindione Argatroban, Streptokinase, Tenecteplase, (Phytomenadione) Vasopressin, Telipressin
MOA: nonselective, TiroNiban Ticagrelor
Dabigatran Urokinase
irreversible COX 1&2
inhibitor; reduces platelet
production of
thromboxane A2, a potent
stimulator of plt MOA: irreversibly MOA: activates MOA: binds to
inhibits binding of ADP MOA: inhibits ENOXAPARIN thrombin's active site MOA: competitively
aggregation antithrombin III MOA: increases supply of MOA: inhibits plasmin &
to plt receptors, phosphodiesterase III & (inactivates thrombin of Dalteparin, and inhibits its inhibits plasminogen reduced Vit K, which is plasmin-streptokinase
reducing plt increases cAMP in plt & MOA: inhibits Vit K Tinzaparin, enzymatic action MOA: tissue plasminogen activation by inhibiting required for synthesis of MOA: vasopressin V2 complex in px who have
MOA: inhibits plt FIIa, FIXa, FXa by epoxide reductase activator analog; converts
Uses: prevention of aggregation by aggregation blood vessels; inhibits plt forming a stable complex Danaparoid, tPA functional Vit K- receptor agonist received Streptokinase
aggregation & causes (responsible for y- Fondaparinux, plasminogen to plasmin, which
arterial thrombosis (MI, interfering with GPIIb/ with them) dependent clotting &
vasodilation; inhibit carboxylation of the Vit Nadroparin USES: anticoagulation degrades the Nibrin & anticlotting factors
TIA, CVD), inNlammatory IIIa binding to -dependent clotting Nibrinogen causing
disorders (rhematic Uses: prevention & uptake of adenosine by in px with heparin- Uses: prevention & Uses: hemophilia A, von Uses: post-op or intra-op
fribrinogen & other factors II, VII, IX, X, thrombolysis treatment of acute Willerbrand dse, central
fever, Kawasaki dse, ligands treatment of arterial endothelial cells & RBC, Uses: DVT, PE, MI, induced- bleeding
thrombosis (stroke, thus increasing adenosine unstable angina, Protein C & Protein S thrombocytopenia, bleeding episodes in px Uses: Vit K deNiciency, DI
Juvenile RA)
TIA, unstable angina), levels leadings to adjuvant to PCI & percutaneous with high risk of antidote to warfarin,
prevention of coronary angioplasty Uses: acute MI, ischemic stroke, bleeding (hemophilia, prevention of SE: increased risk of
Uses: used during PCI to inhibition of plt thrombolytics, ANib, DOC Uses: chronic PE
SE: GI toxicity, tinnitus, restenosis after PCI, aggregation for anticoagulation (with aspirin) intracranial aneurysms, hemorrhagic diatheses in SE: headache, Nlushing, renal failure, heart
prevent thrombosis; anticoagulation (DVT, nausea, hyponatremia,
hypersensitivity, adjunct to ACS) menstrual, obstetrics, newborns attack & stroke
during pregnancy, given ANib, valve replacement) MOA: binds &
hyperventilation, with thrombolytics for thrombolytics, seizures
thrombolysis, acute EXCEPT IN PREGNANCY potentiates effects of SE: bleeding, cerebral
HAGMA, increased coronary syndrome Uses: prevention of revascularization SE: bleeing, effect- postoperative)
antithrombin III on hemorrhage, reperfusion May reduce bleeding by
bleeding time, SE: bleeding, nausea, thromboembolic prolonging antibodies, SE: severe infusion rxn
(unstable angina, procedures, given with factor Xa (more arrhthmias Increases the factor VIII as much as 50% (in
nephrotoxicity (AKI, dyspepsia, hematologic complications of cardiac GPIIb-IIIa inhibitors for anaphylaction rxnx when administered too
NSTEMI) (neutropenia, SE:bleeding, warfarin- selective). Less effect SE: thrombosis, activity of px with mild
interstitial nephritis) valve replacement, fast (dyspnea, chest & many types of surgeries)
angioplasty & stent induced necrosis (for px on thrombin. hypotension, myopathy, back pain) hemophilia A or vWdse
leukopenia, thrombotic secondary prevention of placement Loss of effectiveness (on 2nd
thrombocytopenia with protein C & S Monitor effect with diarrhea
SE: bleedung, ischemic stroke (with deNiciency), teratogen use) and allergic rxn may be
Associated with Reye thrombocytopenia purpura - Ticlopidine) aspirin), intermittent aPTT Removed from the
(bone defects, Uses: DVT, PE, MI, observed with Streptokinase market in 2007 due to
Syndome in children. claudication (Cilostazol Vit K3 (menadione)
SE: bleeding, heparin- hemorrhage) unstable angina, Contraindicated in DIC
only) induced should NEVER be used in mortality
Do not use as NSAID for GI & hematologic SE adjuvant to PCI & No reversal agents therapeutics (ineffective)
Prevents vessel thrombocytopenia, Antidote: AMINOCAPROIC
gout. are more common with thrombolytics, ANib exist
restenosis, reinfarction osteoporosis with Monitor effects with PT. ACID
TRIFLUSAL ia a salicyclic and death. Ticlopidine. SE: headache (bec it is a
chronic use
acid derivative. Additive effects with vasodilator), palpitations
SE: bleeding, less risk Used with caution for
Aspirin. Antidote: VITAMIN K of thrombocytopenia px with renal Tx shoudl be done within 6hrs,
Monitor with aPTT (slow) or FFP (fast) better if within 3hrs
TICAGRELOR DYIRIDAMOLE, by itself, insufNiciency
speciNically inhibits has little or no beneNit.
ADP subtype P2Y; in Does not require
Antidote: PROTAMINE Narrow therapeutic STREPTOKINASE forms a
contrast to other aPTT monitoring. DABIGATRAN is P,
SULFATE window. while all the rest are complex with endogenous
antiplt drugs, it has a CILOSTAZOL is plasminogen, thus catalyzing
contraindicated in heart parenteral
binding site different Protamine sulfate is the conversion of plasminogen
from ADP, making it an failure Administered IV or SC. Active ingredient in only partially to plasmin
allosteric antagonist most rat poisons effective in reversing BIVALIRUDIN also
SULODEXIDE: a effects. inhibits platelet
activation tPA is selective for Nibrin-bound
heparinoid consisting of Highly protein-bound plasminogen
80% heparin & 20% Advantage over
dermatan sulfate regular heparin is
higher bioavailability
and t1/2

FONDAPARINUX is
given SC OD

OTHER DRUGS USED FOR

COAGULATION DISORDERS:
ŸAnti Hemophilic factor CONTRAINDICATIONS TO THROMBOLYSIS:
Ÿ History of CVD hemorrhage at any time
ŸAnti-inhibitor coagulant complex
Ÿ Non hemorrhagic stroke or other cerebrovascular event within
ŸAnti-thrombin III the past year
ŸFactor VIIa, VIII, IX complex Ÿ Marked hypertension (>180/110 mmHg) at any time during
ŸSomatostatin: Tx of intestinal & pancreatic the acute presentation
fistulae, excessive secretion from endocrine tumors of Ÿ Suspicion of aortic dissection
the GIT, acutre severe GI hemorrhage, ERCP Ÿ Active internal bleeding (excluding menses)

 TD
NSAIDS

SALICYLATES NON SELECTIVE NSAIDS COX2 SELECTIVE PARACETAMOL

Phenacetin

ASPIRIN CELECOXIB
KETOROLAC
Salsalate, Sodium Salicylate, IBUPROFEN INDOMETHACIN Etoricoxib, Parecoxib, Rofecoxib,
Dexketoprofen
Choline Salicylate, Magnesium Diclofenac, DiMlunisal, Etodolac, Valdecoxib
Salicylate INTRAVENOS NSAID
Fenoprofen, Flurbiprofen, Ketoprofen,
Nabumetone, Naproxen, Oxaprozin, MOA: selectively inhibits COX3;
weak COX1 & COX2 inhibitor;
Piroxicam, Sulindac, Tolmentin, inhibits prostaglandin synthesis
Mefenamic acid, Bromfenac, MOA: nonselective
MOA: selective COX2 inhibitor; inhibits prostaglandin

synthesis
Meclofenamate, Suprofen, Aceclofenac reversible COX1 & COX2
Uses: analgesica (mild),
MOA: nonselective, irreversible COX 1 & 2 inhibitor; inhibit antipyretic
inhibitor; reduce platelet production of MOA: nonselective prostaglandin synthesis Uses: analgesiam antipyretic, anti inMlammatory
thromboxaneA2, a potent stimulator of platelet reversible COX1 & COX2

aggregation inhibitor; inhibit SE: hepatotoxicity, renal
prostaglandin synthesis Uses: anti inMlammatory SE: GI bleeding (reduced risk), nephrotoxicity, MI &
papillary necrosis & interstitial
(gout, arthritis, stroke (rofecoxib & valdecoxib only), rash
nephritis (phenacetin only),
Uses: prevention of arterial thrombosis (MI, MOA: nonselective reversible COX1 & COX2 ankylosing spondylitis), methemoglobinemia, hemolytic
closure of PDA
TIA, CVD), inMlammatory disorders (rheumatic inhibitor; inhibits prostaglandin synthesis Uses: post-surgical anemia
fever, Kawasaki dse, juvenile rheumatoid analgesic control Coxibs are 10-20x COX2> COX1

arthritis) (moderate to to severe,
Uses: analgesia (musculoskeletal, headache, short term), mainly used SE: GI toxicity,
50% less GI SE compared to nonselective NSAIDs Increased hepatotoxicity with
dysmenorrhea), antipyretic, anti-inMlammatory for analgesia, not for anti pancreatitis,
alcohol use.
SE: GI toxicity, nephrotoxicity, tinnitus, inMlammatory effect nephrotoxicity, serious
hematologic rxns
hypersensitivity, hyperventilation, HAGMA ROFECOXIB & VALDECOXIB - withdrawn due to
SE: GI bleeding (less than aspirin), nephrotoxicity (aplastic anemia,
increased incidence of thrombosis Preferred antipyretic in children
(AKI & interstitial nephritis), hypersensitivity rxn SE: high risk for GI thrombocytopenia), BM (does NOT cuse Reye's
Uncoupler of oxidative phosphorylation. toxicity & nephrotoxicity, suppression syndrome)
allergic rxns MELOXICAM is a preferentially COX2 selective
Long term use reduces the risk of colon cancer.
Associated with REYE SYNDROME in children. Inhibits COX1>COX2 inhibitor
Antidote: N-ACETYLCYSTEINE
MISOPROSTOL prevents NSAID-induced gastritis. Use generaly restricted

to 72hrs only (due to GI
Prevents uric acid excretion (don't use in gout). & renal damage) Indomethacin has Half life: 2-3hrs
NSAIDS (in general) may cause premature closure of ductus greater anti
arteriosus. inMlammatory effect
Low doses undergo Mirst order kinetics, while compared to other
high doses undergo zero order reaction. NSAIDs
IBUPROFEN & INDOMETHACIN can be used to close PDA. PARACETAMOL OVERDOSE:
ŸDOSAGE
ŸToxic Dose: 150mg/kg (21 Paracetamol 500mg tab)
Long term use reduces the risk of colon cancer IBUPROFEN & NAPROXEN have moderate effectiveness. ŸLethal Dose: 15g (30 Paracetamol 500mg tab)
(unknown/ not well understood mechanism) ŸTREATMENT
Antidote is N-acetylcysteine
IBUPROFEN is relatively safe but with short half-life of 2 Supportive management
hrs. Gastric decontamination with activated charcoal

NAPROXEN & PIROXICAM have longer half-lives NSAIDs
may interfere with ASA's antithrombotic action.

 TD
ANTI GOUT

MICROTUBULE
uricosuric xanthine oxidase inhibitor others
ASSEMBLY INHIBITOR

COLCHICINE PROBENECID ANAKIMURA,

ALLOPURINOL FEBUXOSTAT PEGLOTICASE CANAKINUMAB,
SulNinpyrazone RILONACEPT

MOA: compete with uric acid for

reabsorption in the proximal tubules; IL-1 pathway inhibitor
MOA: inhibits microtubule assembly and increase uric acid excretion MOA: active metabolite A novel urate-
LTB4 production leading to decreased (alloxanthine) irreversibly lowering
MOA: non purine reversible inhibitot of
macrophage migration and phagocytosis inhibits xanthine oxidase and xanthine oxidase (more selective than recombinant Used for acute gout in
Uses: gout lowers production of uric acid allopurinol); lowers production of uric mammalian urate px with
acid oxidase enzyme (an contraindication to, or
Uses: gout, familial mediterranean fever
enzyme absent in who are refractory to
SE: GI irritation, rashes, nephrotic Uses: 1st line for chronic gout, humans which traditional therapies
syndrome (probenecid only), aplastic tumor lysis syndrome Uses: chronic gout, tumor lysis syndrome, converts uric acid to like NSAIDs and/or
SE: diarrhea, nauses, vomiting, abdominal anemia, sulfa allergy allopurinol tolerance allantoin) Colchicine
pain, hepatic necrosis, acute renal failure, DIC,
seizure, hair loss, bone marrow depression SE: GI upset, rash, peripheral
(aplastic anemia), peripheral neuritis, May precipitate acute gout during neuritis, vasculitis, bone SE: liver function abnormalities,
myopathy early phase of drug action (prevent by marrow dysfunction, aplastic headache, GI upset, rash, liver dysfuncion
coadministering with colchicine or anemia, cataracts (febuxostat) NSAIDs in Gout: INDOMETHACIN
indomethacin). ŸIndomethacin & other NSAIDs also inhibits urate crystal phagocytosis
Diarrhea is the adverse effect which signals ŸIndomethacin is commonly used in the initial treatment of gout as the
toxicity from colchicine Inhibits metabolism of replacement for colchicine
Witheld for 1-2 wk after an acute episode
Inhibit secretion of other weak acids mercaptopurine and of gouty arthritis (coadministered with
ŸAspirin is not used due to its renal retention of uric acid at low doses
(penicillin, methotrexate). azathioprine. colchicine or indomethacin to avoid an
acute attack)
Consider HYPOURICEMIC DRUG THERAPY:
May be given together with Witheld for 1-2 wk after an ŸAfter 2 episodes of acute attack
GOAL OF TREATMENT: antimicrobial agents (particularly acute episode of gouty Febuxostat is a newer non-purine ŸSerum uric acid >9mg/dl
Prompt alleviation of pain & disability penicillins) to prolong therapeutics arthritis (coadministered inhibitor of xanthine oxidase; more Ÿ (+) Uric acid stones
ŸBed Rest effects by inhibiting renal tubular with colchicine or effective than allopurinol Ÿ (+) Tophi or chronic gout
ŸMainstay treatment during Acute Attack: secretion of antibiotics indomethacin to avoid an
NSAIDs (first line), Colchicine, Glucocorticoids
acute attack)

 Anti bacterial
TD

BACTERIAL CELL WALL SYNTHESIS INHIBITORS

BETA LACTAM PEPTIDE

PENICILLINS CEPHALOSPORINS CARBAPENEMS MONOBACTAMS INHIBITORS GLYCOPEPTIDE ANTIBIOTICS CYCLOSERINE DAPTOMYCIN FOSFOMYCIN

BACTERIAL protein SYNTHESIS INHIBITORS

aminoglycosides tetracyclines chloramphenicol macrolide lincosamide oxazolidinone streptogramin

nucleic acid SYNTHESIS INHIBITORS

sulfonamides trimethoprim Fluoroquinolones

miscellaneous

nitroimidazole nitrofurantoin pseudomonic acid polymyxins macrocyclic

 TD

penicllins

isoxazolyl amino anti pseudomonal

natural PENICILLINS
penicillins penicillins penicillins

Methicillin
AMPICILLIN PIPERACILLIN
PENICILLIN G, V Nafcillin, Oxacillin, Cloxacillin,
Dicloxacillin AMOXICILLIN Ticarcillin, Carbenicllin

MOA: binds to penicillin-binding proteins; inhibits

transpeptidation in bacterial cell walls
MOA: binds to penicillin-binding proteinsl
Uses: DOC for syphilis, for streptococcal, pneumococcal, inhibits transpeptidation in bacterial cell walls
meningococcal, G(+) bacilli, spirochete infection MOA: binds to penicillin-binding proteins; inhibits MOA: binds to penicillin-binding proteins; inhibits
transpeptidation in bacterial cell walls Uses: infections due to enterococci, Listeria transpeptidation in bacterial cell walls
SE: hypersensitivity, complete cross-allergenicity with other monocytogenes, E.coli, Proteus mirabilis,
penicillins, GI disturbances, seizures H.inSluenzae, Moraxella catarrhalis (HELPSE) Uses: greater activity against G(-) infections; infections due to
Uses: staphylococcal infections
Pseudomonas, Enterobacter & Klebsiella

Renal tubular reabsorption inhibited by Probenecid. SE: hypersensitivity, cross-allergenicity, GI upset,
SE: hypersensitivity, complete cross-allergenicity with other
pseudomembranous colitis & rash (Ampicillin) SE: hypersensitivity, complete cross-allergenicity with other
penicillins, GI disturbances, interstitial nephritis (methicillin),
neutropenia (nafcillin) penicillins, GI disturbances
Inactivated by beta-lactamase (penicillinase)
Inactivated by beta-lactamse (penicillinase).

Resistant to inactivation by beta lactamase (penicillinase). Inactivated by beta lactamse (penicillinase).
Benzathine Penicillin & Procaine Penicillin: long acting IM
preparations. Enhanced effect when used with beta-lactamase
Biliary clearance. inhibitors (Clavulanic acid, Sulbactam) Enhanced effect when used with beta lactamase inhibitors

(Clavulanic acid, Tazobactam).
Given IM but Pen V can be given PO.
Synergistic effect with Aminoglycosides.
Very narrow spectrum.
Synergistic with Aminoglycosides against Pseudomonas
Increased activity against enterococci when given together
with aminoglycosides. Ampicillin undergoes enterohepatic
recirculation.

Narrow spectrum.


cephalosporins TD

1st gen 2nd gen 3rd gen 4th gen

cefazolin, cefadroxil, cefaclor, cefamandole, cefmetazole, cefoperazone, cefotaxime, ceftazidime,

cefonicid, cefuroxime, cefprozil, cefepime, ceftaroline,
cephalexin, cephalothin, ceftizoxime, ceftriaxone, cefixime, cefpirome
cephaprin, cephradine ceforanide, cefoxitin, cefotetan, cefpodoxime, proxetil, cefdinir, cefditoren
loracarbef pivoxil, ceftibuten, moxalactam
MOA: binds to penicillin-binding proteins;
inhibits transpeptidation in bacterial cell
MOA: binds to penicillin-binding proteins; inhibits MOA: binds to penicillin-binding proteins; inhibits walls
transpeptidation in bacterial cell walls transpeptidation in bacterial cell walls MOA: binds to penicillin-binding proteinsl inhibits transpeptidation in bacterial
cell walls

Uses: wide coverage against gram (+) & gram
Uses: surgical prophylaxis, bone infections, infections Uses: added coverage for infections due to Haemophilus, (-) bacteria, MRSA (Ceftaroline)
due to gram (+) cocci (staphylococci & common Enterobacter & Neisseria Uses: decreased gram (+) coverage; increased gram (-) activity (Pseudomonas,
streptococci(, E.coli & Klebsiella pneumoniae, skin & Bacteroides, against Providencia, Serratia, Neisseria, Haemophilus; DOC for
gonorrhea (Ceftriaxone & CeRixime)
soft tissue infections, UTI SE: hypersensitivity, cross-allergenicity
SE: hypersensitivity, cross-allergenicity (partial with penicilins, (partial with penicilins, complete with
complete with cephalosporins), injection site reactions, phlebitis,
SE: SE: hypersensitivity, cross-allergenicity (partial with penicilins, complete with cephalosporins), GI upset
SE: hypersensitivity, cross-allergenicity (partial with GI upset, disulRiram reaction (Cefamandole, Cefotetan)
penicillins, complete with cephalosporins), injection cephalosporins), GI upset, disulRiram reaction (Cefoperazone)

site reactions, phlebitis, GI upset Resistant to beta-lactamase.
Increases nephrotoxicity of Aminoglycosides.
Synergistic effect with Aminoglycosides.

Increases nephrotoxcity of Aminoglycosides. Broad gram (-) activity.
Do not cross the BBB.
All hvae renal excretion except CEFOPERAZONE & CEFTRIAXONE.

Do not cross the BBB. In some sources, Ceftaroline belongs to the
Slight less activity against gram (+) but extended gram (-) activity. 5th gen Cephalosporins.
All can penetrate the BBB except CEFOPERAZONE & CEFIXIME.

Minimal activity against gram (-) cocci, enterococci,
MRSA & most gram (-) CEFUROXIME has improved action against pneumococcus & More resistant to beta-lactamase produced by
H.inRluenza CEFTRIAXONE & CEFOTAXIME are the most active Cephs against Penicillin-
Enterobacter, Hemophilus, Neisseria, &
resistant Streptococcus pneumoniae.
Pneumococcal.

Cephalosporins CEFOTETAN & CEFOXITIN have good activity against B.fragilis &
causing disulfiram
thus are used for abdominal & pelvic infections. CEFTIZOXIME is commonly used against Bacteroides.
reaction: Has improved stability to chromosomal
Cefamandole
Cefmetazole
CEFTRIAXONE lactamse.
Best CNS penetrance!
Cefotetan All are pregnancy category B. Should be reserved against serious infection except Ceftriaxone & CeRixime.
Cefoperazone
Ceftaroline used for MRSA.
CEFTRIAXONE has a very good CNS penetration.
1st Gen Cephalosporins: 2nd Gen Cephalosporins: 3rd Gen Cephalosporins:
FADer, help me FAZ my PHarmacology boards!
In a FAMily gathering you see your FOXy cousin wearing a
FEnge PO ng PERA to FIX my TTTTTv! CEFT OLOZ AN E
ceFADroxil
FUR coat & drinking TEa
ceFEtamet ŸA novel cephalosporin, usually combined with
ceFAMandole CEFTAZIDIME has a very good action on Pseudomonas. Tazobactam, used for the treatment of complicated
ceFAZolin ceFOXitin cefPOdoxin
urinary tract & intraabdominal infections;
cePHalothin ceFURoxime cefoPERAzone
ŸVery good activity against gram (-) organisms
cePHapirin cefoTEtan ceFIXime All are pregnancy category B. including Pseudomonas aeruginosa, most
cePHradine FAC! LORA the PROfessional AZhOLE is still on the FONe. cefTazidime
ceFAClor extended-spectrum-beta-lactamase-producing
cePHalexin cefoTaxime
LORAcarbef organisms & some anaerobes.
cefoTizoxime
cefPROzil cefTibuten
cefmetAZOLE cefTriaxone
ceFONicid
 TD

BACTERIAL CELL WALL SYNTHESIS INHIBITORS

BETA LACTAM PEPTIDE

CARBAPENEMS MONOBACTAMS INHIBITORS GLYCOPEPTIDE ANTIBIOTIC CYCLOSERINE DAPTOMYCIN FOSFOMYCIN

IMIPENEM- CLAVULANIC VANCOMYCIN MOA: blocks MOA: binds to cell

incorporation of D-Ala MOA: inactivates the
CILASTIN ASTREONAM ACID Teicoplanin, Dalbavancin, BACITRACIN into the pentapeptide
membrane causing enxyme UDP-N-
depolarization & rapid acetylglucosamine-3-
Ertapenem, Sulbactam, Telavancin side chain of cell death enolpyruvyltransfera
peptidoglycan
Meropenem, Tazobactam se which is
important in
Doripenem Uses: infections caused
Uses: drug-resistant peptidoglycan
MOA: inhibits cell wall synthesis by binding by G(+) bacteria
tuberculosis (2nd line synthesis (very early
MOA: binds to penicillin- to D-Ala-D-Ala terminus of nascent including sepsis &
MOA: interferes with drug) endocarditis stage of bacterial cell
binding proteins; inhibits peptidoglycan --> inhibit transglycosylation the late stage in gram wall sythesis) -->
MOA: inhibits inactivation --> prevents elongation & crosslinking of
transpeptidation in of penicillins by bacterial (+) organisms prevents formation
bacterial cell walls peptidoglycan chain SE: neurotoxicity of N-acetylmuramic
beta-lactamase SE: myopathy
MOA: binds to penicillin- (penicillinase) (tremors, seizures, acid.
binding proteins; inhibits
Uses: infections due to psychosis)
trasnspeptidation in Uses: infections resistant Uses: serious infections caused by drug- gram (+) bacteria
More rapidly
bacterial cell walls to beta lactamses Uses: infections against resistant organisms (MRSA), sepsis, Uses: uncomplicated
endocarditis & meningitis, bactericidal than
produced by gram (-) rods beta-lactamase produding Only used as a second- Vancomycin. UTI
including Klebsiella, pseudomembranous colitis SE: nephrotoxicity line agent in TB.
Uses: wide coverage gonococci, streptococci,
Pseudomonas & Serratia E.coli & H.inVluenzae
against gram (+) & gram (-)
Inactivated by Safe for pregnant px.
bacteria; for serious SE: red man syndrome, nephrotoxicity, Reserved for topical pulmonary surfactant
infections such as SE: GI upsaet, SE: hypersensitivity, ototoxicity, chills, fever, phlebitis use only due to marked so cannot be used
pneumonia & sepsis superinfection, vertigo, cholestatic jaundice nephrotoxicity. Renal excretion.
against pneumonia.
headache, hepatoxicity,
Reserved for serious life-threatening infections.
skin rash
SE: hypersensitivity, cross- Usual combinations: Resistance emerges
Monitor creatine rapidly.
allergenicity (partial with Amoxicillin-Clavulanate, Treat red man syndrome by slowing the rate of phosphokinase weekly
penicillins), GI upset, CNS Resistant to beta- Ampicillin-Sulbactam, infusion.
to check for severity of
toxicity (confusion, lactamase. Piperacillin-Tazobactam. myopathy.
encelopathy, seizures) Synergistic with Beta
Narrow spectrum. Lactam & Quinolones
No cross-allergenicity
Most active against NOT bactericidal (only
Reserved for serious life- with penicillins. plasmid encoded beta VRSA & VRE are due to D-Ala-D-Lactate formation. destabilizes bacterial
threatening infections.
lactamases (gonococci, cell membrane).
streptococci, E.coli & Teicoplanin & Telavancin are not absorbed in the
No activity against gram H.inVluenzae).
CILASTIN inhibits renal (+) bacteria or anaerobes. GIT thus used for bacterial enterocolitis; they are

Drugs of last resort

also eliminated unchanged in the urine.
metabolism (hydrolysis) of I aM your Last Shot at Victory
imipenem by
Not good inhibitor of
DIHYDROPEPTIDASE. Given IV. Renal excretion. inducible chromosomal Decrease dose for renally impaired patients. Imipenem
beta lactamases
(Enterobacter,
Amikacin
Synergistic with AG. Dalbavancin has very long t1/2 (6-11 days) which
Given IV.
Pseudomonas, Serratia) permits once-weekly dosing & is more active han Meropenem
Vancomycin.
Linezolid
Streptogramins
Vancomycin
 TD

BACTERIAL PROTEIN SYNTHESIS INHIBITORS

aminoglycosides tetracyclines chloramphenicol macrolides lincosamide oxazolidinone streptogramin Fusidane

GENTAMICIN NEOMYCIN DOXYCYCLINE ERYTHROMYCIN CLINDAMYCIN LINEZOLID Quinupristin Fusidic Acid,

STREP- SPECTI- MOA: inhibits
-Dalfopristin Na Fusidate
AMIKACIN TOMYCIN Kanamycin, NOMYCIN Minocycline, transpeptidation (catalyzed Azithromycin, Lincomycin Tedizolid
Tobramycin by peptidul in\luenzae) at
Paromomycin Tigecycline, 50S subunit. Static. Clarithromycin,
Demeclocycline, Telithromycin,
MOA: binds to 23s
MOA: inhibit protein Lymecycline Uses: meningitis Roxithromycin MOA: binds to 50s subunit. ribosomal RNA of 50s
MOA: inhibit protein synthesis by synthesis by binding MOA: inhibit (S.pneumoniae, Static. subunit. Static. MOA: binds 50s
MOA: inhibit subunit. Cidal. MOA: inhibits
binding to 30S subunit; proetin synthesis to 30s subunit. Cidal. MOA: inhibit protein protein H.in\luenzae, transloction
bactericidal by binding to 30s synthesis by binding to synthesis by N.meningitidis), backup for process during
Uses: skin & soft tissue Uses: infections caused
subunit. Cidal. 30s subunit. Cidal. binding to 30s Salmonella, Rickettsia & protein
Uses: TB, Tularemia, MOA: binds 30s ribosomal Bacteroides MOA: binds to 50s ribosomal infection, anaerobic by drug-resistant Uses: infections
Uses: infections caused by subunit. Cidal. caused by drug- synthesis
Bubonic plague, subunit. Static. subunit. Static. infections, backup drug gram(+) cocci such as
aerobic gram (-) bacteria (E.coli, against gram (+) cocci, resistant gram(+)
Uses: infections Brucellosis, Uses: skin infections, Staphylococci &
Enterobacter, Klebsiella, Proteus, Enterococcal Uses: drug- SE: GI disturbances, endocardititis prophylaxis Enterococcus (MRSA, cocci such as
caused by bowel preparations for Uses: infections caused by Uses: CAP, Pertussis, Diphtheria, Uses: topical
Providencia, Pseudomonas, endocarditis elective surgery (to resistant aplastic anemia (penicillin-allergy), PCP VRSA, VRE), Listeria, Staphylococci &
aerobic gram (-) M.pneumoniae, chlamydiae, Chlamydial infections, MAC E.faecium (MRSA, antimicrobial
Serratia), Endocartitis (caused by bacteria (E.colim decrease aerobic gonorrhea, (idiosyncratic), gray baby pneumonia, toxoplasmosis Corynebacteria against most
rickettsiae & Vibrio; PUD, lyme VRSA, VRE)
staphylococci, streptococci, Enterobacter, \lora), hepatic gonorrhea in syndrome, dose-related common skin
enterococci), ocular infections SE: hypersensitivity, disease, Malaria prophylaxis, anemia
Klebsiella, encephalopathy, penicillin- SE: GI upset, cholestatic hepatitis, pathogens
nephrotoxicity Amoebiasis, SIADH SE: GI disturbances, skin SE: bone marrow
Proteus, visceral leishmaniasis allergic px (demeclocycline), acne, CAP, hepatotoxicity, QT prolongation, SE: injection site including
(reversible), rash, neutropenia, hepatic suppresion,
SE: nephrotoxicity (reversible), Providencia, (Paromomycin) bronchitis (doxycycline) drug interactions, rare fulminant reactions, severe S.aureus
ototoxicity Inhibits hepatic drug- dysfunction, thrombocytopenia,
ototoxicity (irreversible), Pseudomonas, (vestibulotoxic metabolizing enzymes hepatic failure (Telithromycin) pseudomembranous colitis neutropenia, serotonin arthalgia-myalgia
Serratia), TB 2nd SE:
neuromuscular blockade irreversible), nephrotoxicity causing many drug (C.def\icile overgrowth) syndrome (when given syndrome
line drug SE: hypersensitivity, SE: GI disturbance, teratogen An antibiotic
neuromuscular nephrotoxicity (reversible), interactions. All macrolides inhibit CYP450 together with isolated from the
(tooth enamel) dysplasia/ serotonergic drugs
blockade, teratigen (reversible), ototoxicity EXCEPT Azithromycin. Inhibits CYP450 fermentation
Synergistic effect with cell wall (congenital discoloration), hepatotoxicity, Cross-resistance bertween such as SSRIs),
SE: ototoxicity (irreversible), nephrotoxicity, enzymes, causing broth of
synthesis (beta lactam & deafness), injection Given PO and IV. clindamycin & macrolide is neuropathy, optic
vancomycin) inhibitors due to nephrotoxicity (irreversible), neuromuscular multiple drug Fusidum
site rxns photosensitivity, reversible common. neuritis
(reversible), neuromuscular blockade, vestibulotoxicity (esp Azithromycin has the highest Vd & interactions. coccineum
enhancement of transport to the
inside of the bacterial cell. ototoxicity blockade anemia Able to cross the placenta & slowest elimination.
minocycline)
(irreversible), Syngergistic effect BBB. Resistance is due to Resistance is due to
neuromuscular methylation of binding
with beta lactam Limited to topical & No cross- Telithromycin is used for decreased af\inity of
Given IM or IV only. blockade antibiotics.
Divalent cations impair oral sites & enzymatic drug to binding site.
oral use (Neomycin). resistance with absorption (minimal for Resistance is due to the macrolide-resistance.
inactivation.
other drugs Doxycycline). formation of
Have concetraion dependent Synergistic effect used in acetyltransferase that
Given IM. Reverse gonorrhea. Good oral bioavailability but
killing. with beta lactam Tigecycline has the broadest inactivates drug. G(-) aerobes are resistant
antibiotics. neuromuscular spectrum & has the longest t1/2 Azithromycin absorption is
blockade with calcium impeded by food. because of poor
(30-36hrs).
Has widespread penetration through the
Are not capable of penetrating gluconate & Given IM. Usually caused as topical
resistance. neostigmine. outer membrane.
the BBB. Least resistance Do not drink with milk (decreased agent: Chloramphenicol
but narrowest Half-lives: Erythromycin (2hrs),
absorption with divalent cations like Palmitate & Clarithromycin (6hrs),
therapeutic For Streptomycin, Calcium). Chloramphenicol Na
Low tissue penetration. window. Kanamycin is the most Azithromycin (24-48hrs).
resistance is due to ototoxic.
Succinate
changes in the High Vd, cross the placenta,
ribosomal binding enterohepatic recycling. Resistanace is due to development
Mechanism of Resistance:
plasmid-meadiated formation of site. of ef\lux pumps & production of AMINOGLYCOSIDES
inactivating enzymes "group
transferase" --> catalyze the
acetylation of amine functions &

If given together
All are excreted renally EXCEPT
Doxycycline (bile).

methylase enzyme.

TETRACYCLINE 30S
with Pens, can be Cross-resistance among
the transfer of phosphoryl or used for Resistance is due to development of
adenylyl grps to the oxygen ef\lux pumps for active extrusion of macrolides: complete ore partial
enterococcal Tetracyclines & the formation of resistance with drugs acting on the
atoms of the hydroxyl grps of AG.

endocarditis, TB
plague & Tularemia
ribosomal protection proteins that
interfere with Tetracycline binding
(but not present with Tigecycline
50s.
CHLORAMPHENICOL
Gentamicin & Tobramycin are the
most vestibulotoxic &
except in Proteus & Pseudomonas).
ERYTHROMYCIN
nephrotoxic.

Tigecycline is given IV only & is
unaffected by common Tetracycline
resistance mechanisms. LINCOSAMIDES
50S

Group Pregnancy Category D
LINEZOLID
STREPTOGRAMINS

Sulfonamides
SILVER
SULFADIAZINE
Mafenide Acetate
MOA: inhibits dihyropteorate
synthase. Static.
Uses: burn infections
SE: GI upset, acute hemolysis in
G6PD deBiciency, nephrotoxicity, DNA gyrase & topoisomerase IV. Cidal.
hypersensitivity (assume cross-
hypersensitivity, SJS/TEN),
hematotoxicity, drug interactions, Cholera (backup), Typhoid Uses: UTI & GIT infections, gram (-) rods (such
kernicterus SE: GI distress, CNS effects (dizziness, headache), tendinitis, QTc prolongation
Displaces protein binding of other atypical pneumonia, tuberculosis (2nd line Avoid use in young children & pregannat women. MOA: inhibits DNA
drugs/bilirubin in G6PD deBiciency, drug), infections of soft tissue, bones & joints; replication by binding to
TD
nucleic acid synthesis inhibitors
TRIMETHOPRIM Fluoroquinolones
CO- 1st generation 2nd generation 3rd generation 4th generation
TRIMOXAZOLE
Nalidixic acid, LEVOFLOXACIN
CIPROFLOXACIN, Ofloxacin,
MOA: sequential blockade of
dihydropteroate synthase
Cinoxacin, Norfloxacin, Lomefloxacin, Gemifloxacin, Moxifloxacin, Sparfloxacin, Grepafloxacin, Gatifloxacin, TROVAFLOXACIN
(SULFAMETHOXAZOLE) and
dihydrolate reductase
Rosoxacin, Enoxacin Pazufloxacin, Tosufloxacin, Balofloxacin Alatrofloxacin,
(TRIMETHOPRIM). Cidal.
Oxolinic acid Prulifloxacin,
Uses: urinary tract, MOA: inhibits DNA replication by binding to DNA gyrase & topoisomerase IV. Cidal.
respiratory, ear & sinus
infections (Haemophilus,
MOA: inhibits DNA replication by binding to Clinafloxacin
Moraxella, Aeromonas), Uses: lung infections caused by gram (+) cocci, atypical pnuemonia (Chlamydia, Mycoplasma), TB (2nd line drug)
P.jiroveci pneumonia,
Toxoplasmosis, Nocardiosis,
fever, Shigellosis as Shigella, Salmonella, ETEC &
Campylobacter), gonococc, gram (+) cocci,
SE: GI upset, acute henolysis
intraabdominal MDR organisms (such as
nephrotoxicity, DNA gyrase &
hypersensitivity (assume Pseudomonas, Enterobacter) Enhance toxicity of methylxanthines (Theophylline).
topoisomerase IV. Cidal.
cross-hypersensitivity, SJS/
TEN), hematotoxicity, drug
GrepaBloxaxin withdrawn due to severe cardiotoxicity (arrhythmias); GatiBloxacin has also been withdrawn due to DM.
interactions, kernicterus SE: GI distress, CNS effects (dizziness, Uses: broad spectrum
headache), insomnia, skin rash, abnormal
activity gram (-) & (+),
LFTs, tendonitis & tendon rupture MoxiBloxacin has hepatic clearance --> lower urinary levels. so use in UTI is not recommended.
Dipslaces protein binidng of enhanced activity against
other drugs/bilirubin.
anaerobes
High resistnance esp for C.jejuni, gonococci, G(+) cocci like MRSA, pseudomonas & serratia.
Avoid use in young children & pregnant
Low solubility in acidic urine women.
causeing formation of stones. Are used as alternative to Ceftriaxone & CeBixime in gonorrhea. SE: GI distress, CNS effects
(dizziness, headache),
Enhance toxiicty of methylxanthine tendinitis, QTc
Resistance is duet to plasmin- OBloxacin can be used against C.trachomatis. Respiratory quinolones.
mediated (decreased (Theophylline). prolongtaion,
intracellular accumulation of hepatotoxicity
the drug, increased MoxiBloxacin & GemiBloxacin are the newest members of this family & are considred to have the broadest sprectrum of activity with (TrovaBloxacin)
production of PABA by CiproBloxacin is the most active agent against increased activity against anaerobes & atypical agents.
bacteria, decreased
gram(-) organisms esp Pseudomonas.
sensitivity of dihydropteroate Avoid use in young children
synthetase to sulfas and Elimination is via the kidneys by tubular secretion (may compete with probenecid for excretion) except MoxiBloxacin.
& pregnant women.
production of dihydrofolate
reductase that has decreased General properties of quinolones: good oral
afBinity for the drug). bioavailability, high Vd, t1/2 3-8hrs, Never use MoxiBloxacin in UTI.
absorption is impeded by antacids, elimination Enhance toxicity of
methylxanthine
is via kidneys by tubular secretion (may LevoBloxacin is used in CAP cause by Chlamydia, Mycoplasma, & Legionella.
Sulfonamides are formulated
compete probenecid for excretion) except (theophylline).
in a 5:1 ratio with
Trimethoprim. MoxiBloxain.
GemiBloxacin, LevoBloxacin, & MoxiBloxacin can prolong Q
Widest spectrum of activity
NorBloxacin does not achieve adequate plasma among FQ.
LevoBloxacin has superior activity against gram(+) bacteria inclusing S.pnuemoniae
levels for use in systemic infections.
All have relaibely long t1/2 permitting once daily dosing.
Oral absorption is impared by cations.
GatiBloxacin can cause hyperglycemia in DM px, & hypoglycemia in px receiving OHA.
 TD

miscellanous antibiotics

PSEUDOMONIC
NITROIMIDAZOLE NITROFURAN POLYMYXINS MACROCYCLIC
ACID

METRONIDAZOLE POLYMYXIN B
NITROFURATOIN MUPIROCIN FIDAXOMICIN
Tinidazole, Secnidazole Polymyxin E

MOA: inhibits staphylococcal isoleucyl MOA: inhibits bacterial protein

MOA: forms multiple reactive tRNA synthetase. Cidal. MOA: attach to and disrupt bacterial cell synthesis by binding to the sigma
MOA: reactive reduction by ferredoxin forming intermediates when acted upon by membrane, bind & inactivate endotoxin. subunit of RNA polymerase. Static.
free radicals that disrupt free electron transport Cidal.
bacterial nitrofuran reductase --> disrupt
chain. Cidal. protein, RNA & DNA synthesis. Cidal. Uses: gram(+) cocci including
methicillin-susceptible & MRSA, for Uses: gram (+) bacteria only,
minor skin infections such as Impetigo Uses: gram (-) bacteria; for salvage C.defIicili in adults
Uses: anaerobic or mixed intra-abdominal Uses: uncomplicated UTI (exceot Proteus therapy of Acinetobacterm
infections, vaginitis (Trichomonas, Gardnerella),
& Pseudomonas) Enterobacteriaceae & Pseudomonas
pseudomembranous colitis, brain abscess, SE: epistaxis, stinging or burning aeroginosa SE: nausea, vomiting, abdominal pain,
protozoal infections sensation on the skin, mild skin rash, GI bleeding, anemia, neutropenia

SE: anorexia, nausea, vomiting, skin headache
rashes, pulmonary inIiltrates, SE: eosiophilia, fever, nephrotoxicity,
SE: GI irritation, metallic taste, headache, dark neurotoxicity, rash, urticaria Granted Orphan Drug Status for
phototoxicity, neuropathies, hemolysis in
urine, leukopenia, dizziness, ataxia, neuropathy, patients with G6PD deIiciency Only used topically (available as C.difIicile in children.

seizures, disulIiram rxn intranasal ointment).
Proteus & Neisseria are resistant.

Proteus & Pseudomonas are resistant. Narrow spectrum.
DOC for Amoebiasis, Giardiasis & Do not used over large infected areas
For topical use only (to limit toxicity).
Pseudomembranous colitis such as decubitus ulcers or open
Contraindicated in renal insufIiciency. surgical wound (may lead to resistance).

Single OD dose can prevent recurrent
UTI.

AcidiIication of urine enhances activity.

Adjust dose in renal patients.


ANTI TB DRUGS TD

RIFAMPICIN
ISONIAZID PYRAZINAMIDE ETHAMBUTOL STREPTOMYCIN
Rifabutin, Rifapentine, Rifaximin
MOST HEPATOTOXIC

MOA: unknown; converted to active

MOA: inhibits DNA-dependent RNA polymerase --> inhibits RNA PYRAZINOIC ACID under acidic condition of MOA: inhibits arabinosyl transferases
involved in the synthesis of MOA: inhibit protein synthesis by
production. Cidal. macrophage lysosomes; Static but can be cidal binding to S12 ribosomal subunit.
MOA: inhibits mycolic acid synthesis. Cidal. on actively dividing mycobacteria arabinogalactan in mycobacterial cell
wall. Static Cidal.

Uses: TB (active, latent), atypical mycobacterial infections, leprosy,
Uses: TB (active, latent, prophylaxis)
prophylaxis for meningococcal & staphylococcal carriers states, drug- Uses: TB (active) Uses: TB (for drug-resistant strains),
resistant infections (MRSA, PRSP) Uses: TB (active), atypical mycobacterial
infections tularemia, bubonic plague, brucellosis
SE: hepatitis, neurotoxicity (seizures, neuritis,
SE: hepatotoxicity, non gouty polyarthralgia,
insomia), acute hemolysis in G6PD deHicienct, SE: red-orange body Hluids, light chain proteinuria, skin rash, asymptomatic hyperuricemia, myalgia, GI SE: hypersensitivity, nephrotoxicity
drug-induced lupus, drugs interactions thrombocytopenia, nephritis, hepatotoxicity, Hlulike syndrome, irritation, rash, porphyria, photosensitivity SE: visual disturbances (decreased visual
acuity, red-green color blindness, (reversible), ototoxicity
anemia, cholestasis (vestivulotoxic, irreversible).
retrobulbar neuritis, retinal damage),
Most important drug used in TB (Hirst line headache, confusion, hyperuricemia, neuromuscular blockade, teratogen
Also known as "sterilizing agent" used during (congenital deafness), injection site
agent). Also considered a Hirst line agent for PTB. peripheral neuritis
the Hirst 2months of therapy. rxns

Prevent neurotoxicity by co-administering
Potent CYP450 inducer. Most hepatotoxic anti TB drug. Perform base ophthalmologic
PYRIDOXINE (Vit B6). examination before starting Synergistic effect with beta lactam
antibiotics.
antimycobacterila therapy.
Rapid development of resistance if used alone. Require metabolic conversion via
Liver metabolism by acetylation (Filipinos are
Pyrazinamide in MTb.
fast acetylators.) Resistance is due to mutation in emb Given IM.
Delays the emergence of resistance to dapsone. gene.

Resistance is via mutation in pncA gene which
Potent CYP450 inhibitor.
codes for pyrazinamidase & increased efHlux
RIFAXIMIN is a Rifampin derivative that is not absorbed in the GIT, Dose adjustment is needed in renal px.
systems.
and so is used for the prevention of hepatic encephalopathy, for
Less active against other mycobacteria. treatment of traveler's diarrhea (off-label use: for IBS &
pseudomembranous colitis). Decreased dose in hepatic & renal patients. Always used in combination with other
drugs for TB.
Structural congener of pyridoxine.
Resistance is due to changes of drug sensitivity of the polymerase
Take with meals.
enzyme. Taken with meals.
High level resistance due to deletion of KatG
gene which codes for catalase-peroxidase
enzyme involved in bioactivation of INH, low Undergoes enterohepatic recirculation.
level resistatnce due to deletion of inhA gene
which encodes the target enzyme which is an
acyl protein reductase. Orange-colored metabolites.
ALTERNATIVE ANTI MYCOBACTERIAL DRUGS:
Best taken 1 hr before or 2hrs after meals. AMIKACIN: streptomycin-resistant or MDR mycobacterial strains
Delay emergence of resistance to Dapsone.

CIPROFLOXACIN, OFLOXACIN: active against strains of M.tuberculosis resistant to first line agents
ETHIONAMIDE: no cross resistance with INH; SE: severe GI irritation & neurotoxicity
Rigabutin equally effective as anti-mycobacterial agent with less drug
interaction and it is the preferred anti-TB for AIDS patients. p-AMINODSALICYLIC ACID(PAS): rarely used bec primary resistance is common; SE: GI irritation,
PUD, hypersensitivity rxns, effects on kidney, liver, & thyroid function
Best taken 1 hr before or 2hrs after meal. CAPREOMYCIN: SE: ototoxicity, renal dysfunction
CYCLOSERINE: peripheral neuropathy, CNS dysfunction

TD

drugs for leprosy drugs for ATYPICAL MYCOBACTERIA

LEPROMATOUS
TUBERCULOID LEPROSY PROPHYLAXIS TREATMENT
LEPROSY

DAPSONE AND DAPSONE, RIFAMPICIN,

RIFAMPICIN AND CLOFAZIMINE
CLARITHROMYCIN or AZITHROMYCIN with or
without RIFABUTIN in patients with CD4 countt AZITHROMYCIN or CLARITHROMYCIN with
ETHAMBUTOL and RIFABUTIN
less than 50/L

DAPSONE
CLOFAZIMINE
ACEDAPSONE

MOA: inhibititon of folic acid synthesis. Static.

MOA: binds to guanine bases in bacterial DNA. Cidal.


Uses: leprosy, PCP pneumonia (backup)
Uses: leprosy (sulfone-resistance)


SE: GI irritation, fever, skin rashes, methemoglobinemia, acute hemolysis
in px with G6PD deJiciency SE: GI irritation, skin discoloration (ranging from orange to red brown to
nearly black)

Most active drug against M.leprae.

Usually used in combination with Rifampicin & Clofazimine.

Acedapsone is a a respiratory form of dapsone which has drug action that
can last for several months.

TD

ANTI FUNGAL AGENTS

BLOCKS
ALTER CELL NUCLEIC DISRUPTS
MEMBRANE MICROTUBULE
ACID
FUNCTIONS
SYNTHESIS

POLYENES AZOLES ALLYLAMINE ECHINOCANDIN

FLUCYTOSINE GRISEOFULVIN

FLUCONAZOLE CASFOFUNGIN
AMPHOTERICIN TERBINAFINE
B NYSTATIN KETOCONAZOLE Vorixconazole, ITRACONAZOLE CLOTRIMAZOLE Anidulafungin,
Posaconazole Butenafine, Naftifine Micafungin
MOA: accumulated in fungal
cells by the action of permease MOA: interferes with microtubule
& converted by cytosine function; inhibits synthesis &
polymerization of nucleci acids.
deaminase to 5-FU, which
inhibits thimidylate synthase. Static.
Static.
MOA: inhibits fungal P-450- Uses: dermatophytosis
MOA: binds to regosterol in fungal MOA: inhibits fungal P450- MOA: inhibits b-glucan synthase
cell membranes, foming arti7icial MOA: binds to ergosterol dependent enzymes blocking
in fungal cell MOA: inhibit fungal P-450-dependent dependent enzymes blocking decreasing fungal cell wall Uses: cryptococcosis, systemic
pores. Cidal. enzymes blocking ergosterol ergosterol synthesis. Static. MOA: interfere with ergosterol synthesis. Static. candidal infections,
membranes, forming ergosterl synthesis. Static. MOA: inhibit fungal P450- SE: headachem mental confusion,
synthesis. Static. dependent enzymes blocking synthesis by inhibiting fungal chromoblastomycosis GI irritation, photosensitivity,
arti7icial pores. Cidal. squalene oxidase. Cidal.
Uses: candidiasis (esophageal, ergosterol synthesis. Static. hepatotoxicity, disul7iram rxn,
Uses: systemic fungal infections Uses: blastomycosis, Uses: disseminated &
Uses: chronic mucocutaneous oropharyngeal, vulvovaginitis), SE: myelosuppression, alopecia, drug interactions
(Aspergillus, Blastomyces, Candida sporotrichosis, dermatophytosis, mucocutaneous candidiasis,
albicans, Cryptococcus, Uses: candidiasis cocccidiodomycosis, Uses: dermatophytosis,
(oropharyngeal, candidiasis, dermatophytosis chromoblastomycosis, Uses: mucocutaneous salvage therapy for invasive hepatotoxicity
Histoplasma, Mucor) cryptococcal meningitis onychomycosis aspergillosis
esophageal, vaginal) (treatment & prophylaxis) alternative for infections due to candidiasis, dermatophytosis, Accumulates in keratin.
aspergillus, coccidiodes, seborrheic dermatitis, pityriasis
SE: GI disturbances (vomiting, cryptococcus & histoplasma, Selective toxicity occurs bec
diarrhea), rash, hepatotoxicity, drug versicolor SE: GI upset, rash, headache, taste mammalian cells have low
SE: infusion rxns (chills, fever, candida SE: headache, GI distress, fever, Potent CYP450 inducer.
muscle spasms, hypotension), SE: nephrotoxicity SE: GI disturbances (vomiting, disturbances, hepatotoxicity
(severe) interactions rash, 7lushing (histamine release), levels of permease & deaminase.
nephrotoxicity (RTA with Mg & K diarrhea), rash, hepatotoxicity elevated liver enzymes
SE: none signi7icant when
wasting) SE: GI disturbances (vomiting, administered topically Contraindicated in porphyria.
Narrow antifungal spectrum. Accumulated in keratin. Syngergistic with Amphotericin.
Minimal mucocutaneous Alternative to Ampho B in the diarrhea), rash, hepatotoxicity
absorption. All are given IV.
Control infusion rxns by slowing tx of C.neoformans Given PO.
Limited to topical use because of Given PO & topical.
rate of infusion & premedication Potent CYP450 inhibitor (affect Much more selective for fungal systemic toxicity. Decrease dose in renal px.
phase I metabolism). MICAFUNGIN can increase levels of
with antihistamines. Available as a siwh and cells than ketoconazole but with
As effective as Ampho B in cyclosporine & tacrolimus. Absorption is increased by intake
swallow preparation. candidemia. poor entry into CNS. More effective than griseofulvin in Resistance is due to decreased of fatty meal.
Additive nephrotoxicity with other Interferes with steroid hormone onchomycosis. activity of fungal permease &
synthesis.
nephrotoxic drugs deaminase.
Has a good CNS permeability. May also be used for
(aminoglycosdies). subcutaneous Resiatnce is due to decreased
chromoblastomycosis. transport of drug into the fungal
Resistance is due to changes in the Has synergistic effect when cell wall.
Lipid formulations: Ambisome, sensitivity of target enzyme. POSACONAZOLE - broadest given with Ampho B & Triazoles
Amphotec, Abelcet. spectrum triazole (the only
azole with activity against
Rarely used due to drug interaction & Rhizopus sp /mucormycosis).
Highly lipid soluble, poorly narrow spectrum.

absorbed in the GIT.
Potent CYP450 inhibitor.

High Vd except in the CNS with a
t1/2 of 2weeks.

Resistance is due to decreased
level of ergosterol or change in
membrane structure.

Has the widest antifugal spectrum.

ANTIVIRAL AGENTS TD

FOR HERPES FOR HIV FOR INFLUENZA FOR HBV & HCV

ACYCLOVIR OSELTAMIVIR LAMIVUDINE

GANCYCLOVIR PROTEIN ENTRY AMANTADINE INTERFERON
Valacyclovir, Peniciclovir, Famciclovir,
Valganciclovir
CIDOFOVIR FORCARNET NRTI NNRTI INHIBITORS INHIBITORS Rimantadine
Zanamivir, ALPHA
Adefovir dipivoxil,
Entecavir, Telbivudine,
RIBAVIRIN
Docosanol, Trifluridine Peramivir Tenofovir, Clevudine

MOA: inhibits viral MOA: degrades

RNA polymerase, INDINAVIR CCR5 MOA: inhibits
MOA: inhibits viral DNA polymerase &
ZIDOVUDINE FUSION RECEPTOR MOA: inhibit earl
viral RNA via
MOA: inhibits HBV guanosine
DNA polymerase
HIV reverse Amprenavir, Atazanavir,
INHIBITOR RALTEGAVIR step replication & MOA: inhibits activation of host
MOA: activated by viral thymidine causing chain DELAVIRINE Darunavir, Indinavir, prevent uning by neuraminidase; ce RNAase DNA polymerase triphosphate
kinase (TK ) to form the inhibitor viral termination
transcriptase;
binds to
Abacavir, Didanosine,
Emtricitabine, Lopinavir, Nelfinavir, ANTAGONIST binding to M2 decreases release (ribonuclease) formation;
prevents capping
DNA polymerase Efevirenz, Etravirine, of progeny virus
pyrophosphate Nevirapine, Rilpivirine Ritonavir, Saquinavir, proton channels Uses: Hep B of viral mRNA;
Lamivudine, Stavudine, infection, HIV
Uses: infections due MOA: inhibits viral binding site Tenofovir, Zalcitabine Tipranavir, Uses: HBV blocks RNA-
Uses: infections due to HSV1, HSV2, VZV to CMV, HSV1, HSV2, DNA polymerase, Fosamprenavir, infection, HCV infection dependent RNA
causing chain Boceprevir, Telaprivir Uses: inTluenza A Uses: inTluenza A & (Lamivudine)
VZV B, shortens infection, Kaposi polymerases
termination Uses: CMV retinitis, only sarcoma, genital
SE: nausea, diarrhea, headache,
acyclovir- ENFUVIRTDE MARAVIROC Integrase inhibitor
duration of
symptoms warts

SE: ADEFOVIR -

delirium, tremor, seizures, hypotension, SE: leukopenia, resistance, HSV Uses: HCV
(an enzyme SE: GI irritation,
nephrotoxicity (crystalluria) thrombocytopenia, Uses: CMV retinitis, infections in px MOA: inhibit HIV essential for lactic acidosi, rena infection, RSV
mucocutaneous with AIDS reverse MOA: inhibit viral dizziness, SE: alopecia, & hepatic toxicity
mucositis, proetin processing replication of HIV) cerebellar SE: OSELTAMIVIR - infection
HSV infections, transcriptase after myalgia, ENTECAVIR -
hepatotoxicity, leading to dyfunction(ataxia, GI effects
No activity against strains of HSV with seizures, acyclovir- phosphorylation inhibition of strand depression, Tlu-like headache,
resistance, SE: nephrotoxicity, by cellular dysarthria), livedo ZANAMIVIR - syndrome, thyroid SE: hemolytic
absent thymidine kinase activity. neutropenia Uses: HIV infection transfer dizziness, fatigue,
ganciclovir- electrolyte enzymes MOA: binds to reticularis bronchospasm in dysfunction, anemia,
MOA: inhibit HIV nausea
resistance, genital abnormalities reverse gp41 subunit of asthmatics hearling loss conjunctival &
DOCOSANOL inhibits the fusion warts, molluscum (hypocalcemia), viral envelope MOA: blocks viral
No activity against transcriptase, no SE: hyperlipidemia, DI: avoid usuing bronchial
between the HSV envelope & plasma contagiosum genitourinary attachment via Virtually obsolete irritation,
strains of HSC with Uses: HIV inefction, phosphorylation fat redistribution, glycoproetin, transmembrane Rifampicin Coinfection
membranes. ulceration, CNS prevention of in terms of usage. OSELTAMIVIR - Contraindications
absent TK activity. required hyperglycemia, preventing fusion concomitantly between HBV & teratogen
effects (headache, maternal-fetal HIV of viral & cellylar chemokine presently the drug include HIV may increase
insulinr resistance, receptor CCR5 (lowered blood of choice for
SE: nephrotoxicity hallucinations, transmission membranes autoimmune the risk of
TRIFLURIDINE is a Tluorinated acanthosis levels) Amantadine is also inTluenza
Given as IV of seizures) Uses: HIV infection nigricans, used in treating disease, history of pancreatitis with Early IV
pyrimidine nucleoside. (including H1N1)
intraocular implant cardiac Lamivudine use. administration of
Active against ATAZANAVIR, Uses: HIV infection Parkinsonism. Ribavirin
(for CMV retinitis). SE: lactic acidosis Uses: HIV infection arrhythmias &
strains of HSV with Active against with hepatic SE: DELAVIRDINE, FOSAMOPRENAVI pregnancy decreases
VALOMACICLOVIR is an investigational absent TK activity.
strains of HSV with steatosis NEVIRAPINE -rash, R, LOPINAVIR, mortality in viral
agent which acts as an inhibitor of viral SE: cough,
CMV resistance is absent TK activity. increased AST/ALT NELFINAVIR, SE: injection site hemorrhagic
DNA polymerase for shingles & EBV. ZIDOVUDINE - rxns, diarrhea, muscle &
due to mutation in bone marrow SAQUINAVIR -GI fevers.
Resistance is due EFAVIRENZ - distress & diarrhea joint pain,
viral DNA hypersensitivity, increased hepatic
polymerase & in the to mutation in DNA Does not require suppresion teratogenicity, increased
Given PO, topical & IV. polymerase. phosphorylation ABACAVIR - ETRAVIRINE - ATAZANAVIR - transaminases
gens that code for peripheral incidence of Other drugs for
the activating viral for antiviral hypersensitivity increased bacterial RSV: Pavilizumab
activity. cholesterol, neuropathy pneumonia
phosphotransferase. DIDANOSINE - Minimal cross- (monoclonal
Dose adjustment in renal px. Dose adjustment in triglycerides AMPRENAVIR - antibody against
renal px. pancreatitis resistance with
rash RSV antigen)
VALGANCICLOVIR is Resistance is due STAVUDINE, No cross-resiatnce other anti HIV
Resistance is due to changes in viral to mutation in DNA INDINAVIR - drugs
DNA polymerase. a prodrug of ZALCITABINE - with other anti HIV
polymerase gene. peripheral hyperbilirubinemia drugs
Gangciclovir with & nephrolithiasis
increased oral neuropathy
VALACYCLOVIR is a prodrug that is bioavailability.
Dose adjustment in
converted to Acyclovir and reached renal px.
plasma levels 3-5x (longert t1/2) more
than acyclovir.

PENICICLOVIR does not cause chain
termination.

FAMCICLOVIR is a prodrug which is
converted to Penciclovir in vivo. MISC ELLA NEOUS ANTIVIR ALS:

IMIQUINOD –an immune response modifier

effective for external genital & perianal warts

INO SINE A CE DOB EN

DIME PR ANOL –licensed for the tx of cell
mediated immune deficiencies assoc with viral
infections; used for genital warts, herpes virus
infection, subacute sclerosing panecephalitis &
other conditions

SOFO SB UVIR –a nucleotide prodrug that

undergoes metabolism to the active uridine
analog triphosphate, an inhibitor of Hep C virus
RNA-dependent polymerase; used for Hep C
 TD

ANTI MALARIA

BLOOD TISSUE
SCHIZONTIZIDE SCHIZONTIZODE GAMETOCIDE SPORONTICIDE OTHERS

CHLOROQUINE ARTEMISIN ATOVAQUONE- SULDADOXINE-

PROGUANIL MEPACRINE
QUININE HALOFANTRINE PRIMAQUINE PROGUANIL PYRIMETHAMINE
ATOVAQUONE- SULFADOXINE-
Hydroxychloroquine, MEFLOQUINE PROGUANIL DOXYCYLINE Artesunate, Artemether, PYRIMETHAMINE
Quinidine gluconate Lumefantrine QUINACRINE-
Amodiaquine, Piperaquine Dihydroartemisinin
ATABRINE
MOA: forms
electron-
MOA: unknown MOA: MOA: unknown MOA: forms toxic free transferring
MOA: prevents MOA: complexes with Atovaquone redox
DNA to prevent strand radicals in malarial food
polymerization of heme into disrupts MOA: sequential compounds that
separation; blocks DNA MOA: impairs vacuole blockade of folic
hemozoin Uses: mitonchondri Uses: malaria acts as cellular
replication & al electron progeny of malarial (chloroquine- acid synthesis,
chemoprophyla apociplast genes, oxidants
transcription transport resistance), Uses: malaria blood
Uses: malaria (non- xis resulting in
(chloroquine- (blood & severe (uncomplicated schizonticide; Used in the tx
falciparum, chloroquine- tissue abnormal cell falciparum sporonticide Uses: malaria & prevention
Uses: malaria resistant areas), division falciparum, quinine-
sensitive), chemoprophylaxis schizonticide); malaria resistant) (pyrimethamine) (radical cure of of malaria.
(chloroquine-sensitive areas), (chloroquine-resistance), alternative to
quinune in Proguanil (quinidine) P.vivax &
RA, amebic liver abscess severe falciparum malaria inhibits folate
(quinidine) acute attacks of Uses: ovale), terminal May also be
synthesis SE: nausea, vomiting, Uses: malaria prophylaxis
falciparum chemoprophylaxis (chlorine- used as an
(sporonticide) SE: abdominal diarrhea (vivax, ovale),
SE: GI irritation, skin rash, malaria (MDR) pain, diarrhea, resistant immunodular
headaches, peripheral SE: cinchonism PCP, yory agaent.
vomiting, cough, P.falciparum)
neuropathies, myocardial (headache, tinnitus, pneumonia
SE: GI distress, Uses: tx and SE: GI disturbance, rash, headache, ARTEMETHER-
depression, retinal damage, vertigo), hemolysis in chemoprophyl pruritus, LUMEFANTRINE is the
auditory impairment, G6PD dePiciency, skin rash, teratogen (tooth SE: skin rashes, GI
headache, axis elevated liver DOC for uncomplicated SE: GI distress,
psychosis blackwater fever enamel dysplasia/ enzymes, distress,
dizziness, (chloroquine- discoloration), falciparum malaria in the pruritus,
resistant cardiotoxicity Philippines. hemolysis, kindey headaches,
cardiac hepatotoxicity, damage, drug
conduction P.falciparum) (prolongs PR & methemoglobin
May precipitate porphyria. Quinine is commonly nephrotoxicity, interactions, folic
used with doxycyline or defects, QT interval), emia,
photosensitivity, teratogen Artemisinin-based acid dePiciency
clindamycin to limit psychiatric vestibulotoxicity hemolysisin
SE: abdominal combination therapy is (pyrimethamine) G6PD
toxicities. disorders
pain, nausea, currently the Pirst line of dePiciency
(psychosis), Lumefantrine
neurologic vomiting, Do not drink with malaria tx recommended
diarrhea, used in by WHO for children, adult Competition for
DOC for malaria in symptoms, milk (decreased plasma protein
pregnant px seizures headaches, absorption). combination & pregannct women in 2nd Should be used
rash, with or 3rd trimester. binidng sites with with a blood
increased Artemether (Co- other drugs. schizonticide.

liver enzymes Artem)
Due to potential
embryotoxicity of Pyrimethamine is Eradicates
Artemisinin identiPied in a long-acting hypnozoites in
animal studies, it is not folate antagonist. the liver,
considered safe for use in preventing
1st trimester. malarial
relapse.

TD
DRUGS FOR AMEBIASIS

TISSUE AMEBICIDE luminal AMEBICIDE

METRONIDAZOLE
EMETINE
CHLOROQUINE Tinidazole, NITAZOXANIDE DILOXANIDE FUROATE IODOQUINOL PAROMOMYCIN
Dehydroemetine Secnidazole

MOA: inhibit protein MOA: reactive reduction by

synthesis; blocks ribosomal ferredoxin forming free MOA: unknown
movement along mRNA radicals that disrupt ETC
MOA: reactive reduction by MOA: inhibits protein
ferredoxin forming free Uses: mild to severe intestinal sysnthesis; binds to 16s
Uses: backup drug for severe Uses: severe intestinal & MOA: unknown amebiasis
radicals that disrupt ETC ribosomal subunit
intestinal & extraintestinal extraintestinal amebiasis

amebiasis (DOC), trichomoniasis,
giardiasis, bacterial vaginosis, Uses: asymptomatic cyst of SE: GI distress, thyroid
Uses: metronidazole- E.histolytica (DOC) Uses: asymptomatic cyst
anaerobic infections resistatnt amebiasis, enlargement, skin rxns due to carriers (backup), intestinal
SE: GI distress, muscle (B.fragilis, C.difRicile), PUD giardiasis, cryptosporidiosis iodine toxicity, neurotoxicity amebiasis, cryptosporidiosis
weakness, CVS dysfunction (DOC) SE: Rlatulence, nausea, (peripheral neuropathy,

(arrhythmias & CHF) visual dysfunction)
SE: GI irritation, metallic abdominal cramps
SE: headache, dizziness,
SE: GI distress rashes, arthralgia
taste, headache, dark urine,
Reserved only for situations leukopenia, dizziness, ataxia, Usually used in combination
when metronidazole cannot neuropathy, seizures, with Metronidazole
be used. disulRiram rxn

TD

DRUGS FOR PNEUMOCYTOSIS AMD TOXOPLASMOSIS

SULFADIAZINE-
PYRIMETHAMINE
CO TRIMOXAZOLE PENTAMIDE
Pyrimethamine
+Clindamycin

MOA: sequential blockade of

dihydropteroate synthase
(Suldamethoxazole) and
dihydrofolate reductase MOA: unknown; probably MOA: sequential blockade of
(Trimethoprim) inhibits glycolysis or interferes dihydropteroate synthase
with nucleic acid metabolism (Sulfadiazine) and dihydrofolate

reductase (Pyrimethamine)
Uses: prophylaxis & treatment of
penumocytosis (DOC), prophylaxis Uses: prophylaxis & treatment
(T.gondii, I.belli) of pneumocytosis (backup), Uses: prophylaxis & treatment
trypanosomiasis of Toxoplasmosis (DOC)


SE: GI upset, acute hemolysis in
G6PD deLiciency, nephrotoxicity, SE: respiratory stimulation SE: gastric irritation, glossitis,
hypersensitivity (assume cross- followed by depression, neurologic symptoms
hypersensitivity, SJS/TEN), hypotension, hypoglycemia, (headache, insomnia, tremors,
hematatoxicity, drug interactions, anemia, neutropenia, hepatitis, seizures), hematotoxicity
kernicterus pancreatitis (megaloblastic anemia,
thrombocytopenia),
Displaces protein binding of other Administered by nasal spray pseudomembranous colitis
(aerosol). (clindamycin)
drugs/bilirubin.

Recommended at CD4 count <200

TD

DRUGS FOR TRYPANOSOMIASIS

TRYPANOSOMA BRUCEI TRYPANOSOMA BRUCEI TRYPANOSOMA

LEISHMANIA
RHODIENSE, EAST AFRICAN GAMBIENSE, WEST AFRICAN CRUZI, AMERICAN

SODIUM STIBOGLUCONATE
SURAMIN MELARSOPROL PENTAMIDINE ELORNITHINE Meglumine antimonate, NIFURTIMOX
Amphotericin, Miltefosine

MOA: unknown; probably

inhibits glycolysis or interfres
with nucleic acid metabolism MOA: organic arsenical; inhibits MOA: unknown; probably
ezyme sulGhydryl groups in inhibits glycolysis or interfere MOA: unknown; probably inhibits glycolysis or
MOA: suicide inhibitor of
trypanosomes with nucleic acid metabolism ornithine decarboxylase interferes with nucleic acid metabolism
Uses: african sleeping sickness MOA: inhibits trypanothione reductase
(hemolymphatic stage),
Uses: african sleeping sickness Uses: african sleeping sickness Uses: Na Stibogluconate (DOC except in India)
onchocerciasis (backup) Uses: advanced West African
(DOC) (hemolymphatic stages), sleeping sickness (DOC) Uses: Chaga's disease (DOC), African sleeping

prophylaxis for pneumocytosis, sickness (backup), mucocutaneous
SE: fatigue, nausea, vomiting, SE; GI symptoms, fever, headache, myalgias,
Kala-azar (visceral leishmaniasis
seizures, shock, fever, rash, SE: GI irritation, reactive SE: diarrhea, vomiting, anemia, arthralgias, rash, sterile abscesses, cardiotoxicity
leishmaniasis
headache, paresthesia, encephalopathy thrombocytopenia, leukopenia, (T-wave changes, QT prolongation)

neuropathies, renal seizures SE: nausea, vomiting, abdominal pain, fever,
abnormalities (proteinuria), SE: respiratory stimulation rash, restlessness, insomia, neuropathies,
Crosses the BBB. Alternative drugs include:
chronic diarrhea, hemolytic followed by depression, seizures
anemia, agranulocytosis hypotension, hypoglycemia, Crosses the BBB. VISCERAL (KALA-AZAR): Pentamidine,
Given IM. anemia, neutropenia, hepatitis, Miltefosine
pancreatitis Does not cross the BBB.
Does not cross the BBB. Considerably less toxic than CUTANEOUS: Fluconazole, Metronidazole
Melarsoprol. MUCOCUTANEOUS: Amphotericin B
Considerably administered with
Suramin. Do not cross the BBB>
Used in combination with
Melarsoprol
 SEDATIVE - HYPNOTIC DRUGS LM

BENZODIAZEPINES BARBITURATES
[Binds GABA-A receptor subunits to increase FREQUENCY of Cl‫ ﹶ‬ OTHERS
[Binds GABA-A receptor sites; increases DURATION of Cl‫ ﹶ‬channel opening;
channel opening; membrane hyperpolarizaDon] blocks glutamic acid neurotransmission; at high doses blocks Na channels]

SHORT ACTING INTERMEDIATE ACTING LONG ACTING ULTRA SHORT SHORT-INTERMEDIATE LONG ACTING MELATONIN RECEPTOR
IMIDAZOPYRINE AGONIST ANXIOLYTIC
[T½: 1.5 - 2.5h ] [T½: 12h ] [T½: 100h ] [T½: 4-9m ] [T½: 15 - 50h ] [T½: 118h ]

MIDAZOLAM (Bro%zolam, THIOPENTAL PENTOBARBITAL (Secobarbital, PHENOBARBITAL ZOLPIDEM
Triazolam, Oxazepam, E%zolam) LORAZEPAM (Alprazolam, DIAZEPAM ( Chlorazepate, Amobarbital, Butalbital, RAMELTEON BUSPIRONE
Estazolam, Clonazepam, Chlordiazepoxide, Flurazepam, (Methohexital, Thiamylal) (Mephobarbital, Primidone) (Zaleplon, Eszopiclone)
Butabarbital, Talbutal,
Lormetazepam, Nitrazepam, Quazepam, Flunitrazepam)
Aprobarbital)
Uses: Anesthesia inducDon Temazepam) MOA: AcDvates Melatonin receptors MOA: ParDal agonist at 5HT1A
Uses: Anesthesia inducDon Uses: Status epilepDcus MOA: Binds selecDvely to a subroup
and possibly D2 receptors
Preop sedaDon Uses: Status EpilepDcus (MT1 and MT2) in the suprachiasma-
Increased ICP Uses: Insomnia Seizure d/o of GABA-A receptors to enhance
Acute Anxiety Uses: Status epilepDcus Dc nuclei thus decreasing latency of
Skeletal muscle relaxant Insomnia membrane hyperpolarizaDon
Preop sedaDon Uses: Generalized anxiety d/o
Panic aOacks Skeletal muscle relaxant Anesthesia sleep onset
SE: Acute intermiOent Hyperbilirubinemia
Insomnia [Triazolam] Tranquilizers
Anxiety/Seizure d/o porphyria; Extension of CNS (Gilbert Syndrome) Uses: Insomnia
SE: Acute intermiOent SE: Non-specific chast pain
Seizure d/o [Clonazepam] Alcohol withdrawal Uses: Insomnia
depressant acDons; dependence porphyria; Extension of CNS Delayed sleep onset
SE: Anterograde amnesia Bipolar d/o [Clonazepam] Tachycardia/palpitaDons
Insomnia [Flurazepam] liability greater than Benzos SE: Severe Cardio/respi
depressant acDons; dependence Dizziness/nervousness
Rebound insomnia/anxiety Anxiety d/o [Clonazepam] SE: Dizziness
liability greater than Benzos depression; Extension of CNS SE: Few amnesDc effects
Dec. psychomotor skills Panic d/o [Clonazepam] FaDgue Tinnitus/GI distress
SE: Anterograde amnesia Notes: AddiDve CNS depression depressant acDons; dependence Dependence liability (less)
Paresthesia
Dependence liability Insomnia [Estazolam] Dec. psychomotor skills Decreased testosterone
if taken with ethanol; CYP450 Notes: AddiDve CNS depression liability greater than Benzos
Unwanted dayDme Increased prolacDn Pupillary constricDon
Dependence liability inducer Notes: Lack anD-convulsant, anD-
if taken with ethanol; CYP450
sedaDon SE: Anterograde amnesia Respiratory depression anxiety and muscle relaxant
inducer Notes: May be excreted
Dec. psychomotor skills Notes: Minimal rebound insomnia Notes: No anDconvulsant effect
Unwanted dayDme unchanged effects; very rapid onset of acDon;
Notes: Decreased REM sleep Dependence liability Minimal abuse liability No muscle relaxant effect
sedaDon in the urine; AddiDve CNS effects reversed by FLUMAZENIL
Avoid during 1st trimester Respiratory depression Minimal withdrawal s/sx Minimal CNS depression
depression if taken with ethanol;
Floppy infant syndrome Unwanted dayDme
Notes: Flunitrazepam (Rohypnol) CYP450 inducer
Inceased oral cleX risk sedaDon used as a Date-rape drug (odorless
colorless, tasteless, anterograde
Notes: Lorazepam preferred over amnesia effect)
Diazepam in Status epilepDcus
due to its long distribuDon T½

FLUMAZENIL [T½: 30m] MNEMONICS:

BENZodiazepines = Mercedes Benz (Fast Frequency)
MOA: Antidote; antagonist at benzodiazepine sites on GABA-A receptor BARBiturates = Barbed wire (Duration)
Uses: Benzodiazepine overdose TAYOpental = TAYO agad (shortest acting)
SE: Agitation, Confusion, Precipitates benzodiazepine withdrawal syndrome
for those with benzodiazepine dependence
Chlordiazepoxide = longest spelling (longest T½: 36-200h)
Notes: Seizure and arrhythmias may occur for those who took TCAs and
benzodiazepines Most catastrophic symptom of sedative-hypnotic withdrawal?
- REBOUND SUICIDE
 ANTI-SEIZURE DRUGS
LM

TONIC-CLONIC & PARTIAL MYOCLONIC ABSENCE ADJUNCTS

VALPROIC ACID
(Sodium Valproate)
PHENOBARBITAL
MOA: Blocks Na channels, enhances K channel permeability
(Primidone)
Uses: Bipolar d/o Acute Mania (DOC); GTC seizure (DOC); VALPROIC ACID VALPROIC ACID
MOA: Binds to GABA-A receptor sites and increases DURATION of
Absence (Sodium Valproate) (Sodium Valproate)
Cl channel opening
seizure (DOC); Partial seizure; Myoclonic seizure
Uses: GTC seizure; Partial seizure; Status epilepticus; Insomnia;
SE: NTD, Spina biNida, Hepatotoxicity (esp. in infants), [SAME] [SAME]
Hyperbilirubinemia (Gilbert syndrome)
wt. gain,
SE: Acute intermittent porphyria, extended CNS depressant
GI upset, drowsiness, nausea, tremor, alopecia
actions, tolerance, dependence liability
Notes: CYP450 inhibitor; same effect on Ca channels as
Notes: Primary anticonvulsant in infants, children, and pregnant
Ethosuximide

DIAZEPAM
LAMOTRIGINE
LAMOTRIGINE CLONAZEPAM (Lorazepam, Clorazepate)
(Zonisamide)
(Zonisamide) MOA: Binds to GABA-A receptor sites and increases FREQUENCY of

MOA: Blocks Na and Ca channels, decreases Glutamate [same] Cl channel opening
[SAME]
Uses: Partial seizure (DOC); GTC seizure; Myoclonic & Uses: Status epilepticus
absence seizure; Bipolar d/o SE: Anterograde amnesia, unwanted daytime sedation, respiratory
SE: SJS/TEN [Lamotrigine], severe skin reaction depression, dec. psychomotor skills, tolerance, dependence
[Zonisamide], Dizziness, ataxia, nausea, rash liability
Notes: Undergoes glucuronidation reaction

ETHOSUXIMIDE GABAPENTIN
CLONAZEPAM (Phensuximide, Methsuximide) (Pregabalin)
MOA: Binds GABA-A receptors to increase frequency of Cl MOA: Decreases Ca currents (T-type) in thalamus
PHENYTOIN MOA: Binds Ca channels; Inc GABA release; inhibits neuronal
channel opening; membrange hyperpolarization Uses: Absence seizures
(Fosyphenytoin, Mephenytoin, Ethotion) discharge from seizure foci
Uses: Absence seizure; Myoclonic seizure; Infantile spasms SE: GI distress, lethargy, headache, behavioral changes
MOA: Blocks voltage gated Na channels Uses: Absence seizure; Neuropathic pain (post herpetic neuralgia);
SE: Anterograde amnesia, decreased psychomotor skills. Notes: long half-life
Uses: Generalized tonic-clonic seizure (DOC); Partial seizure Migraine
unwanted daytime sedation, respiratory depression,
(DOC); Status Epilepticus; Arrhythmias (Grp 1B action) SE: Dizziness, sedation, ataxia, nystagmus, tremor
tolerance, dependence liability
SE: Nystagmus, diplopia, sedation, Gingival hyperplasia, Notes: Eliminated in the kidneys in the unchanged form
Hirsutism, Fetal hydantoin syndrome
Notes: Phenytoin preferred in prolonged therapy for Status
epilepticus because it is less sedating; Fostomycin is a LEVETIRAZETAM
water-soluble prodrug MOA: Binds synaptic vesicular protein 2 (SV2A) inhibiting hyper
synchronisation of epileptiform burst Niring; modiNies
synaptic release of Glutamate and GABA
Uses: Juvenile myoclonic epilepsy; GTC seizure; Partial seizure
CARBAMAZEPINE SE: Hallucination, psychosis, irritability, dizziness, sedaation
(Oxcarbazepine, Eslicarbazepine) Notes: Minimal drug interactions, eliminated in kidneys unchanged
MOA: Blocks voltage gated Na channels; dec. Glutamate release
Uses: Trigeminal neuralgia (DOC); GTC seizure (DOC); Partial
seizure (DOC); Bipolar d/o TOPIRAMATE
SE: SJS, Spina biNida, craniofacial anomalies, hyponatremia (Felbamate)
[Oxcar], Diplopia, cognitive dysfunction, drowsiness, MOA: Actions on phosphorylation (Na, Ca, GABA, Glutamate,
bloody dyscrasias FETAL HYDANTOIN SYNDROME Carbonic anhydrase)
Notes: CYP450 inducer; can cause auto-induction - Upturned nose Uses: Lennox-gestaut syndrome; West syndrome; Migraine;
Oxcarbazepine has less drug interactions - Mild mid facial hypoplasia GTC seizure; Refractory seizures [Felbamate]
- Long upper lip with thin vermillion border SE: Psychomotor slowing, Memory impairment, Acute myopia
- Lower distal digital hypoplasia
glaucoma, urolithiasis, Hepatic and hematoxicity [Felbamate]
 GENERAL ANESTHESIA LM

INHALED INTRAVENOUS
[Facilitate GABA mediated inhibition; block brain
NMDA and ACh-N receptors]

BARBITURATES BENZODIAZEPINES DISSOCIATIVE OPIOIDS MISCELLANEOUS

GAS VOLATILE LIQUIDS

FENTANYL
THIOPENTAL MIDAZOLAM (Brotizolam, Triazolam, KETAMINE ETOMIDATE
Oxazepam, Etizolam, Lorazepam) (Morphine, Alfentanyl, Remifentanil)
(Methohexital, Thiamylal) MOA: Blocks glutamate and NMDA MOA: Modulates GABAa receptors
DESFLURANE MOA: Interact with µ (mu) or δ (sigma), and
NITROUS OXIDE MOA: Increases DURATION of Cl channel MOA: Inceases FREQUENCY of Cl channel receptors (β3 subunit)
Uses: General anesthesia κ (kappa) receptors for endogenous
Uses: Anesthesia for minor OR and opening opening Uses: Dissociative anesthesia (Analgesia, Uses: General anesthesia (in patients with
SE: Bronchospasm opioid peptide
dental procedures Uses: Anesthesia induction Uses: Anesthesia induction amnesia and catatonia but with limited cardiorespiratory reserve)
Peripheral vasodilation Uses: General anesthesia
SE: Euphoria, Megaloblastic anemia Inceased ICP Preop sedation retained consciousness) SE: Pain on injection, myoclonus
Notes: All other inhaled anesthetic SE: Respiratory depression
bronchodilation SE: Dependence liability Anxiety/panic attacks SE: Emergence delirium (Post-op effects: Post-op N/V, Adrenocortical
causes bronchodilation Chest wall deformity, constipation
Notes: Lowest potency (highest MAC) Acute intermittent porphyria SE: Anterograde amnesia, unwanted disorientation, hallucination, suppression
daytime sedation, dependency Notes: Antidote is NALOXONE
least cardiotoxicity Tolerance excitation), cardiovascular Notes: Minimal effect on Cardiorespi function
SEVOFLURANE liability, post-op Respi depression Neuroleptanesthesia (analgesia +
Extension of CNS depression stimulation, HPN, inc. ICP No analgesic property
Uses: General anesthesia Notes: Antidote is FLUMAZENIL anesthesia) happens when given with
Notes: Additive CNS depression w/ ethanol Notes: Reduce Emergence delirium with
SE: Renal insufPiciency Adjucnt with inhalational Droperidol and NO
CYP450 inducer pretreatment of Benzodiazepine PROPOFOL
Peripheral vasodilation anesthetics and IV opioids Faster recovery [Remifentanyl]
Rapid entry into the brain (<1min) (Fospropofol)
Slow onset but longder DOA MOA: Potentiates GABA-A receptors
ISOFLURANE Blocks Na channels
Uses: General anesthesia Uses: General anesthesia for prolonged
SE: Catecholamine induced sedation esp. in ICU/OPD patients
arrhythmias, peripheral SE: Bradycardia, hypotension,
vasodilation vasodilation, priapism
paresthesia [Fospropofol]
Notes: Milk of amnesia
ENFLURANE
Uses: General anesthesia
DEXMETOMIDINE
SE: Spike and wave activity in EEG,
MOA: A2 receptor agonist, decrease
muscle twiitching, breath
sympathetic tone with attenuation
holding
of neuroendocrine and hemo-
Notes: Has pungent odor limiting use
dynamic response to anesthesia
and surgery and cause sedation
HALOTHANE and analgesia
Uses: General anesthesia
SE: Malignant hyperthermia (if used
with Succinylcholine), Post-
operative hepatitis

METHOXYFLURANE
Uses: General anesthesia
SE: Renal insufPiciency
 LM

LOCAL ANESTHETICS
[Blockade of Na channels slow, then prevents
axon potential propagation]

ESTERS AMIDE

SHORT ACTING LONG ACTING SURFACE ACTING MEDIUM ACTING LONG ACTING

PROCAINE BENZOCAINE LIDOCAINE BUPIVACAINE

TETRACAINE
(Novocaine, Chloroprocaine) (Butamben) Uses: Antiarrhythmic (1B) used (Levobupivacaine)
Uses: Local/spinal/epidural/
Uses: Extravasation complications Uses: Local/topical anesthesia post-MI, digitalis toxicity Uses: Local/epidural/intrathecal
topical/ophthalmic anesth
from venipuncture, inadvert- SE: Light headedness, sedation, SE: Light headedness, sedation, SE: Severe cardiotoxicity
SE: Most allergenic among LAs
ent intraarterial inections Restlessness, nystsagmus, Restlessness, nystsagmus, Hypotension, arrhythmias
Notes: Primarily for spinal (2-3h)
SE: Light headedness, sedation, Cardiorespiratory depression Cardiorespiratory depression Notes: Treat cardiotoxicity with
Restlessness, nystsagmus, Skin irritation Notes: Topical, inTiltration, spinal, INTRALIPID/LIPOSOMAL
forms (Fat emulsion in TPN)
Cardiorespiratory depression Antibody formation (allergy) epidural, IV, peripheral
Antibody formation (allergy) Notes: Topical use only Give with EPI to decrease
Notes: Shortest T½ among LAs systemic absorption
COCAINE ROPIVACAINE
MOA: Intrinsic sympathometic PRILOCAINE (Mepivacaine) Uses: Local/epidural anesthesia
activity; vasoconstriction Uses: Local/dental anesthesia SE: Cardiotoxicity (less than
Uses: Local/topical anesthesia SE: Methemoglobinemia Bupivacaine)
MNEMONICS:
ESTERS have only 1 ‘i’ in their names SE: Severe HPN, cerebral Light headedness, sedation, Notes: Longest T½ among LAs
AMIDES have 2 ‘i’s in their names hemorrhage, arryhthmias, Restlessness, nystsagmus, Treat cardiotoxicity with
MI, stroke, abuse liability Cardiorespiratory depression INTRALIPID/LIPOSOMAL
PROCAINE = shortest T½
Notes: Only LA that vasoconstricts Notes: Administer methylene blue forms (Fat emulsion in TPN)
- a PRO finishes the race fastest
ROPIVACAINE = longest T½ Topical use only for methemoglobinemia
- at the end of a long ROPE

Why NOT to inject LA into an abscess? Lidocaine won’t work in an acidic environment (below pKa =
charged form will predominate), thus will not be able to cross the cell membrane and excert its action
 LM

SKELETAL MUSCLE RELAXANTS

NEUROMUSCULAR BLOCKERS OTHERS

NON-DEPOLARIZING DEPOLARIZING CENTRALLY ACTING DIRECT ACTING MUSCLE OTHERS

[Competitive antagonists at skeletal muscle SPASMOLYTICS RELAXANTS
nicotinic acetylcholine receptors] SUCCINYLCHOLINE
BACLOFEN
MOA: Agonist at ACh-N causing initial
MOA: GABA-B agonist; facilitate spinal
twitch then persistent repolarization, DANTROLENE EPERISONE
inhibition of motor neurons
followed by long Wlaccid paralysis MOA: Blocks RyR1 Ca-release channels in Class: Antispasmodic
Uses: Cerebral palsy spasticity; stroke
Uses: Malignant hyperthermia, hyperK, the skeletal muscles MOA: Relaxes both skeletal and vascular
Multiple sclerosis
SHORT ACTING INTERMEDIATE ACTING LONG ACTING Inc. IOP, regurgitation (aspiration)
SE: Sedation, weakness, dizziness
Uses: Malignant hyperthermia; spasm smooth muscles
Arryhthmia, muscle pain due to CP, MS, and SCI Uses: Reduces myotonia, improves
Confusion, nausea, headache
Notes: DANTROLENE for malignant SE: Muscle weakness circulation, suppresses pain relfex
MIVACURIUM ATRACURIUM (Cisatracurium) hyperthermia; metabolized by
Uses: Intubation; General anesthesia Uses: Intubation; General anesthesia; TUBOCURARINE pseudocholinesterase (plasma)
ORPHENADRINE (Chlorphenesin,
SE: Respiratory paralysis, apnea Mechanical ventillation facilitation Uses: Prolonged relaxation during OR; a.k.a SUXAMETHONIUM Methocarbamol, Cyclobenzapirine)
Histamine release (moderate) SE: Bronchospasm; seizures; Intubation; General anesthesia MOA: Inhibits muscle stretch reWlex
Notes: Metabolized by Respiratory paralysis; apnea SE: Ganglion block (hypotension), Uses: Acute spasm from muscle injury;
pseudocholinesterase Histamine release Recurarization, Respi paralysis InWlammation
Short DOA (10-20m) Notes: Undergoes HOFFMAN elimination Prolonged apnea, histamine release SE: Strong antimuscarinic effects
(rapid spontaneous breakdown) Notes: C/i in myocardial ischemia

DIAZEPAM
VECURONIUM
PANCURONIUM MOA: Facilitates GABAergic transmission
Uses: Intubation; General anesthesia
MOA: Moderate block on cardiac in the CNS
SE: Respiratory paralysis, apnea
muscarinic Uses: Cerepbral palsy spasm; stroke
Minimal cardiovascular effects
receptors Spinal Cord injury; acute spasm
Notes: Undergoes elimination in BILE
Uses: Euthanasia; lethal injection; SE: Anterograde amnesia, unwanted
Muscle relaxation potentiated by
Strychnine poisoning; intubation daytime sedation, respiratory
inhaled anesth, aminogly, quinidines
General anesthesia depression, tolerance
SE: Recurarization, tachycardia, apnea
ROCURONIUM Respiratory paralysis, HPN
Uses: Intubation; General anesthesia Notes: May cause heart block TIZANIDINE
SE: Hypersensitivity, apnea MOA: α2 adrenoreceptor agonist in the SC
Respiratory depression Uses: Multiple sclerosis spasm; stroke;
Notes: SUGAMMADEX is a novel reversal MALIGNANT HYPERTHERMIA Amyotropic lateral sclerosis
agent; slight antimuscarinic effect - Rare interaction between succinylcholine with inhaled SE: Weakness, sedation, hypotension
Used in patients w/ renal anesthetics
impairment - Life-threatening condition characterized by massive Ca release
Most rapid onset (60-120s) from sarcoplasmic reticulum to skeletal muscle
- Early sign: Trismus (contraction of jaw muscles)
- Tx: DANTROLENE
 LM
ANTI-PARKINSONISM

DOPA-PRECURSOR DOPA-AGONIST MAO INHIBITORS COMT INHIBITORS ANTICHOLINERGICS OTHERS

LEVODOPA-CARBIDOPA SELEGILINE (Rasagiline) ENTACAPONE (Tolcapone) BENZTROPINE (Biperiden,

Trihexyphenidyl, Procyclidine) AMANTADINE
MOA: L is a dopa precursor, while C MOA: Selectively inh MAO-B decreasing MOA: Blocks L-dopa metabolism by
inhibits peripheral metabolism ERGOT NON-ERGOT degradation of dopamine; inhibiting COMT in periphery and
MOA: Decreases excitatory actions of
cholinergic neurons by blocking
MOA: Potentiates dopaminergic function
(synthesis, release, reuptake)
via dopa decarboxylase Inc response to Levo-Carbidopa CNS; prolong L-dopa response
muscarinic receptors Uses: Parkinson's dse; InRluenza
Uses: Parkinson Dse. (DOC) Uses: Only as adjunct to Levodopa; Uses: Wearing-off phenomena
Uses: Adjunct for Parkinson's dse. and SE: Livedo reticularis, behavioral
SE: GI upset, dyskinesia, behavioral Can be given alone [Rasagiline] Adjunct to Levodopa
BROMOCRPITINE (Pergolide, PRAMIPEXOLE (Ropinirole) EPS caused by antipsychotics changes, GI disturbances, urinary
changes, On-off phenomena Cabergoline, Piribedil) SE: Insomnia, mood changes, SE: Orange urine, NMS, sleep
MOA: Partial agonist at D2 and D3 SE: Atropine-like effects, confusion retention, peripheral edema
Wearing-off phenomena, MOA: Partial agonist at D2 receptors, Dyskinesia, GI distress, hypoTN disturbance, rhabdomyolysis,
receptors; smooths out Rluctuations Inattention, drowsiness, Notes: Improves bradykinesia, tremor,
Postural HPN, arrhythmia leading to inh of prolactin release Notes: May cause agitation, delirium, and Hepatotoxicity [Tolcapone]
in Levodopa response Delusions, hallucinations and rigidity; anti-muscarinic action
Notes: C/i in px with hx of PSYCHOSIS Uses: Levodopa intolerance, Hyper- death if used with Meperidine Notes: Entacapone (periphery)
Uses: Restless leg syndrome Notes: Improves tremor and rigidity
Use with COMT to prolong DOA prolactinema, intermittent Serotonin syndrome if used with Tolcapone (periphery + CNS)
On-off phenomenon Exacerbate tardive dyskinesia
HPN crisis if used with MAOIs claudication, tremors SSRIs, TCSs, and Meperidine
SE: Behavioral changes, confusion ROTIGOTINE
SE: Pulmonary inRiltrate/Ribrosis, Compulsive gambling, overeating, MOA: Dopamine agonist
Eryhthromelalgia, anorexia, hypersexuality, uncotrollable Uses: Restless leg syndrome
N/V, Dyskinesia, behavioral change tendency to fall asleep Notes: Used as OD transdermal patch
Notes: PRIBEDIL can act as D3 agonist and Notes: C/i with active PUD, recent MI, providing slow and constant doses
as A2 adrenergic antagonist or psychotic illness

APOMORPHINE
MOA: Partial agonist at D3 receptors;
Antagonist at 5HT3 and Alpha
adrenoreceptors
Uses: Off-periods, erectile dysfunction,
Alcoholism, Opiate addiction,
Alhzeimer's Disease ON-OFF PHENOMENA
SE: Severe nausea, dyskinesia, - Alternating periods of improved mobility and akinesia,
Hypotension, drowsiness, occurring a few hours to days during treatment
sweating
Notes: Use TRIMETHOBENZAMIDE to WEARING-OFF PHENOMENA
prevent severe nausea
- Deterioration of drug effect in between doses
- Due to progressive destruction of nigrostriatal neurons
that occurs with disease progression

DRUGS for HUNTINGTON’S DISEASE

DRUGS for TOURETTE’S SYNDROME MNEMONICS:


TETRABENZAMINE / RESERPINE
HALOPERIDOL / PIMOZIDE LIVEDO RETICULARIS
MOA: Deplete amine transmitters esp Dopa from nerve endings
MOA: Blocks central D2 receptor Drugs that cause LR: “A MAN reads fHM and GQ”
by reversibly inhibiting VMAT2, resulting in decreased uptake
Uses: Reduces vocal and motor tic frequency and severity Amantadine Gemcitabine
of monoamines
SE: Parkinsonism, dyskinesia, sedation, blurred vision, dry Hydroxyurea Quinidine
Uses: reduces chorea severity
mouth, visual disturbance, arrhythmia [Pimozide] Minocycline
SE: hypoTN, sedation, depression, diarrhea
 ANTI-PSYCHOTICS LM

TYPICALS / CLASSICAL ATYPICALS LITHIUM [Mood stabilizer]

MOA: Uncertain; Decreases cAMP
[Block of D2 receptors >> 5HT2 receptors] [Block of 5HT2 receptors >> D2 receptors] Uses: Recurrent depression, BPD, schizoaffective
SE: EBSTEIN ANOMALY, tremor, sedation,
CHLORPROMAZINE (Thiothexene, aphasia, thyroid enlargement, Neprogenic DI
Flupentixol, Promethazine, Levomepromazine) Bradycardia, renal dysfunction, dysrhythmia
Uses: Shizophrenia, manic phase of BPD Notes: C/i in sick sinus syndrome,
SE: CORENAL and LENS deposits, failure of treat overdose with HEMODIALYSIS
CLOZAPINE
ejaculation, EPS, tardive dyskinesia, narrow therapeutic index
Uses: Refractory and suicidal schizophrenia
Hyperprolactinemia, marked seadtion, NMS
SE: DM, weight gain, myocarditis, ileus,
Notes: May also block α and histamine receptor,
Agranulocytosis, hypersalivation, seizure
Protoype antipsychotic [Promethazine]
Notes: REDUCES SUICIDE RISK
Prominent wt. gain, hyperglycemia,
THIORIDAZINE (Fluphenazine, Perphenazine, Agarnulocytosis, and seizures OLANZAPINE
Prochlorperazine, Tri9luoperazine)
Uses: Schizophrenia, BPD, anorexia, depression
Uses: Schizophrenia, antiemesis and preop
SE: Weight gain, hyperglycemia,
sedation [Prochlorperazine]
Hyperlipidemia, agranulocytosis
SE: RETINAL deposits [Thioridazine], failure
Notes: Prominent wt. gain and hyperglycemia
of ejaculation, EPS, tardive dyskinesia, QUETIAPINE
Safe in pregnancy
Hyperprolactinemia, Cardiotoxicity Uses: Schizophrenia, BPD manic phase
Notes: Strongest autonomic effects [Thioridazine] SE: Somnilence, fatigue, sleep, paralysis,
Only antipsychotic w/ FATAL OVERDOSE Hypnagogic hallucinations, cataracts,
Priapism, Prolonged QT (TDP)
Notes: Safe in pregnancy RISPERIDONE (Paliperidone)
Uses: Schizophrenia, BPD, depression,
HALOPERIDOL (Droperidol)
Intractable hiccups, Tourette's syndrome
Uses: Schizophrenia, manic phase of BPD,
SE: Hyperprolactinemia, photosensitivity,
Huntington's dse, Tourette's syndrome
EPS, insomnia
SE: Neuroleptic Malignant Syndrome,
Notes: Only antipsychotic used for the
Extrapyramidal symptoms (major),
Tardive dyskinesia, Hyperprolactinemia YOUTH and ELDERLY
ZIPRAZIDONE
Notes: Causes the MOST EPS of all typicals Uses: Schizophrenia, BPD manic phase
Weakest autonomic effects, least sedating SE: EPS, QT prolongation (TDP)
among aypicals Notes: Inc mortality in elderly with dementia-
related psychosis
ARPIPRAZOLE
Uses: MDD, cocainde dependence, autism,
Schizophrenia, BPD manic phase
SE: LEAST SEDATING atypical
 ANTI-DEPRESSANTS LM

TETRACYCLIC/UNICYCLIC

TRICYCLIC-ANTIDEPRESSANTS SSRI SNRI
ANTIDEPRESSANTS
SEROTONIN ANTAGONISTS MAOI

FLUOXETINE (Paroxetine, Citalopram, VENLAFAXINE (Duloxetine, AMOXAPINE (Maprotiline) TRAZODONE (Nefazodone, Vortioxetine) PHENELZINE (Tranylcypromine,
IMIPRAMINE (Clomipramine, Desipramine,
Amitryptiline, Nortriptyline, Doxepin, Escitalopram, Sertraline, Fluvoxamine, Desvenlafaxine, Milnacipran) Isocarboxazid, Selegiline)
Vilazodone) MOA: Strong NE reuptake inhibitor, weak MOA: Blocks 5-HT2A receptors, weak inhibitor
Protriptyline, Trimipramine) MOA: Inhibits MAO A and B; Inc CNS levels
MOA: Inhibits neuronal reuptake of serotonin serotonin reuptake inhibitor, blocks of NE and 5HT transporters
MOA: Block NE and 5-HT transporters MOA: Inhibits neuronal reuptake of serotonin by
and NE by binding to both transporters Dopamine D2 receptors Blocks SERT [Nefazodone], blocks of NE and Serotonin
Like SNRis + signi@icant ANS blockade inhibiting Serotonin Transporter (SERT)
Uses; MDD, Fibromyalgia, Perimenopausal Uses: Major depression 5-HT2C receptors [Trazodone] Uses: Major depression unresponsive to other
Uses: MDD , Bipolar disorders, Acute panic Uses: OCD (DOC), MDD (@irst line), Anxiety,
symptoms, Diabetic neuropathy, SE: Akathisia, Parkinsonism, seizures, Uses: Major depression, Hypnosis/sleeping drugs, Anxiety, Phobic features,
attacks, Phobias, Enuresis, ADHD, Panic attacks, Anxiety, PTSD, Bulimia,
Neuropathic pain, Chronic pain DOs Amenorrhea-galactorrhea syndrome, aid [Trazodone] Hypochondriasis
OCD [Clomipramine] Premenstrual dysphoria, Alcohol
SE: Dizziness, insomnia, sedation, GI distress, Cardiotoxicity SE: Sedation, GI disturbance, Ortho hypo, SE: Dizziness, insomnia, orthohypo, blurred
SE: Excessive sedation, fatigue, confusion, dependence, Premature ejaculation
HPN and CNS stimulation [Venlafaxine], Notes: Lowers seizure threshold [Amoxapine] Priapisim [Trazodone], Hepatotoxicity vision, arrhythmia, diarrhea, seizure,
α-blocking effects, sympathomimetic [Dapoxetine]
Hepatotoxicity [Duloxetine], Withdrawal [Nefazodone], Hyperprolactinemia hyperthermia, CNS stimulation
effects, ortho hypo, cardiomyopathy, SE: N/V, headache, anxiety, agitation,
syndrome even in just 1 missed dose, Notes: May cause arrhythmias in Px with Notes: HYPERTENSIVE CRISIS when taken
arrhythmia, tremors, weight gain Drowsiness, insomnia, Erectile dysfxn,
Anticholinergic effects MIRTAZAPINE pre-existing cardiac diseases with tyramine
Notes: Additive depression of the CNS with other EPS, QT prolongation [Citalopram],
Notes: Differ from TCA in lacking blockade of MOA: Inc amine release from nerve endings by Modest α1 and H1 receptor blockade SEROTONIN SYNDROME when taken
central antidepressants Withdrawal syndrome
H1, M, and Alpha receptors antagonism of presynaptic α2 adreno- Short T½ to be given BID or TID with SSRIs
3Cs of overdose: Coma, Convulsions, Notes: CYP 450 inhibitors - Fluoxetine, Fluvox- Nonselective MAOI [ Tranylcypromine]
Inc risk for suicide in children and adoles receptors
Cardiotoxicity amine, and Paroxetine
Venlafaxine has less af@inity for NE Uses: Major depression, Appetite stimulation, MAO-B Selective [Selegiline]
Imipramine metabolized to Despiramine Serotonin syndrome when used w MAOIs
transporters, Milnacipram more selective Sedation/sleeping aid
Amitriptyline metabolized to Nortriptylin May decrease appetite = weight loss
for NE reuptake SE: Weight gain, marked sedation, diizziness,
Inc. risk for suicide in children and/or
blurred vision, nightmares
adolescents
Notes: Significant muscarinic receptor and
α2 blocking effect

BUPROPION
MOA: Inhibits neuronal reuptake of dopamine
and NE; Inc. Dopa and NE activity
Uses: Major depression, smoking cessation,
Alcohol dependence, improves mood
SE: Weigh loss, agitation, dizziness, dry
mouth, aggravation of psychosis, priapism
Notes: Lowers seizure threshold
Resembles amphetamine in chem struct.

MNEMONICS: SEROTONIN SYNDROME:

- Severe muscle rigidity, myoclonus, hyperthermia, MNEMONICS:
DRUGS for causing ERECTILE DYSFUNCTION Cardiovascular instability, seizures
“SOREE, Sore Penis can’t Fuck Hard” - Drugs implicated: MAOIs, TCAs, MDMA (ecstasy) Drugs causing PRIAPISM
SSRI Spironolactone Dextromethorphan, meperidine, St. Johns Wort “Tigas PeniS Qu, AyaW Bumaba”
Opiates Propanolol Trazodone Alprostadil
Risperidone Finasteride “FAT CHilD” Papaverine Warfarin
Ethanol Hydrocholothiazide Fever Clonus Sildenafil Bupoprion
Estrogen Agitation Hyperreflexia QUetiapine
Tremor Diaphoresis
 OPIOID ANALGESICS / ANTAGONISTS LM

AGONIST MIXED ANTAGONIST DUAL ACTING

NALBUPHINE (Buprenorphine, NALOXONE (Naltrexone, Nelmefene, TRAMADOL (Tapentadol)

Butorphanol, Pentazocine, Alvimopan, Methylnaltrexone)
MOA: Weak agonist at μ receptor
FULL PARTIAL WEAK Levallorphan) MOA: Competitively blocks μ, δ, and κ Uses: Moderate pain, chronic pain syndromes,
MOA: Strong agonist at κ receptors receptors; Rapidly reverses effects Gibromyalgia, neuropathic pain
Weak antagonist at μ receptors of opioid agonists
MORPHINE (Hydromorphone, SE: Seizures, nausea, dizziness,
Oxymorphone) HYDROCODONE (Oxycodone) PROPOXYPHENE (Levopropoxyphene, Uses: Mod - sev pain, opioid dependence/ Uses: Opioid overdose, opioid and alcohol pruritus, constipation
MOA: Strong agonist at κ and μ receptors Dextropropoxyphene) withdrawal, balanced anesthesia dependence [Naltrexone]
MOA: Strong agonist at μ receptors Notes: Lowers seizure threshold
Uses: Mod - sev pain, Cancer pain, Neuropathic MOA: Weak agonist at κ and µ receptors SE: Sedation, dizziness, sweating, SE: Pruritus, nausea, vomiting
Uses: Severe pain, pain associated with C/i in patients with Hx of epilepsy
pain, Opioid dependence/wiithdrawal Uses: Mild - mod pain, Opioid withdrawal, nausea, anxiety, hallucinations, Notes: Precipitates abstinence syndrome
Acute MI, Inc. Pulmonary edema, Serotonin syndrome when used w SSRI
SE: Hypogonadism, hearing loss, Restless leg syndrome nightmares, tolerance, dependence, in patients with opioid dependence
adjunct in anesthesia
+ other [Morphine] SEs SE: Seizures, pulmonary edema, fatal respiratory depression, Reduces craving in alcohol, nicotine,
SE: Miosis, restlessness, respiratory
depression, postural hypotension, inc. Notes: There is genetic variation in the arrhythmias + other [Morphine] SEs
Notes: Withdrawn due to fatal cardiotoxicity
Notes: Reduces craving in alcohol
dependence, effect resistant to
and opioid dependence [Naltrexone]

ICP, constipation, urinary retention, metabolism of codeine and its derivative
(group 1C antiarrhythmic activity) Naloxone reversal
pruritus, addiction liability
[Levopropoxyphene] as antitussive
Notes: Exerts hemodynamic effects on the
pulmonary circulation
DEXTROMETHORPHAN (Codeine)
SigniGicant 1st pass effect
MOA: Decreases sensitivity of cough receptors
depressing the medullary cough center
FENTANYL (Sufentanil, Alfentanil, through sigma receptor stimulation
Remifentanil, Ohmefentanyl) Uses: Cough suppression
MOA: Strong agonist at μ receptors SE: Hallucinations, confusion, excitation,
Uses: Severe pain, adjunct in anesthesia, inc or dec pupil size, nystagmus, seizure,
Breakthrough Cancer pain coma, respiratory depression, addiction
SE: Same w [Morphine] except Miosis Notes: Serotonin syndrome when used with
Notes: May be given Transdermal / Lollipop SSRIs or MAOIs
[Ohmefentanyl] most potent (18000x)

MEPERIDINE
MOA: Strong agonist at κ and μ receptors
Uses: Moderate - severe pain, Labor
analgesia, Spasmodic pain (biliary,
renal), Preop sedation
SE: Seizures, less addiciton liability +
[Morphine] SE except Miosis
Notes: HYPERTENSIVE CRISIS when
taken with Tyramine

METHADONE (Levomethadyl
Acetate, Levorphanol)
MOA: Strong agonist at μ receptors
Uses: Moderate - severe pain,
Opioid dependence/withdrawal
SE: Same w [Morphine] except Miosis
Notes: Used in Methadone Maintenance
Therapy (MMT) for opioid dependence

HYPOTHALAMUS
GNRH
ANALOGUE
LEUPROLIDE
Gonadorelin,
Goserelin, Histrelin,
Nafarelin, Triptorelin
MOA: Inc. LH/FSH secretion
with intermittent dose, but
reduces LH/FSH secretion
with prolonged
administration
Uses: Ovarian suppression,
Endometriosis, Myoma Uteri,
Precocious puberty,
Advanced Prostate cancer
SE: Hot flushes, sweats,
headache, light headedness,
nausea, osteoporosis,
gynecomastia, reduced
libido, dec. Hematocrit
Temporary exacerbation of
precocious puberty/
prostateCA
Apoplexy/blindness during
the 1st few wks of therapy
(Tx: coadminister
FLUTAMIDE)
ANRH
ANTAGONIST
GANIRELIX
Cetrorelix, Abarelix,
Degarelix
MOA: Blocks GnRH
receptors, reducing LH/FSH
production
Uses: Prevents premature
LH surgeduring
controlledovarian
hyperstimulation, Prostate
CA
SE:nausea, headache, Hot
flushes, gynecomastia, Dec
libido/Hct
Des NOT cause a tumor
flare-up if used for Prostate
CA
DEGARELIX for Prostate CA
GANIRELIX prevents LH
surge
AGONIST
SOMATROPIN
MOA: increases release if IGF-1 in the
liver & cartilage; stimulates skeletal
muscle growth, amino acid transport,
protein synthesis & cell proliferation
Uses: growth hormone deficiency,
genetic dses assoc with short stature
(Turner, Noonan, Prader-Willi), failure
to thrive due to chronic renal failure
or SGA, AIDS wasting, improve GI
function in px who underwent
intestinal resection that led to
malabsorption syndrome
SE: peripheral edema, myalgia,
arthralgia, intracranial HPN,
pseudotumor cerebri, slipped capital
femoral epiphysis, progression of
scoliosis, hyperglycemia
Performance-enhancing drug
(increases muscle mass) that is
banned by athletics committees.
Given SC
GROWTH
HORMONE
MECASERMIN
MOA: a recombinant IGF-1
agonist; stimulates skeletal
muscle growth, amino acid
transport, protein synthesis
& cell proliferation
Uses: for children
unresponsive to GH therapy
SE: hypoglycemia, increased
LFT, intracranial HPN
Remedy to hypoglycemia:
give px some snacks prior
to dose
HYPOTHALAMIC AND
PITUITARY HORMONES
ANTAGONIST
PEGVISOMANT
MOA: a GH receptor
antagonist (blocks GH
receptor)
Uses: acromegaly
SE: diarrhea, nausea, flu-
like symptoms, elevated
LFTs, hypersensitivity rxn
Onset of action is expected
within 2 wks of use
OCTREOTIDE
Lanreotide
MOA: somatostatin analog;
suppresses the release of GH,
glucagon, insulin, IGF-1, serotonin
& GI peptides
Uses: acromegaly, pituitary
adenoma (GH-secreting),
carcinoid, gastrinoma,
glucagonoma, variceal bleeding,
gigantism
SE: GI disturbances, gallstones,
arrhythmias/ cardinal conduction
abnormality
Can alter requirements for
antidiabetic agents
Regular release: given BID-QID SC
If slow release: every 4wks IM
Are long acting synthetic analogs
of somatostatin
ANTERIOR
PITUITARY
GONADOTROPINS
FSH
FOLLITROPIN ALFA
Menotropins,
Urofollitropin,
Follitropin Beta
MOA: activates FSH
receptors; mimics effects of
endogenous FSH
Uses: controlled ovarian
hyperstimulation, infertility
due ro hypogonadotropic
hypogonadism in men
SE: headache, depression
syndrome (ovarian
enlargement, ascites,
hypovolemia, shock),
multiple pregnancies in
women, gynecomastia in
mean
FOLLITROPIN ALFA & BETA
are recombinant FSH forms
while UROFOLLITROPIN is a
purified preparation from
urine of postmenopausal
women
LH
CHORIOGONDO-
TROPIN ALFA
HCG, Menotropins,
Lutropin Alfa
MOA: gonadotrophin analog;
actives LH receptors;
mimics effects of
endogenous LH
Uses: initiation of ovulation
during controlled ovarian
hyperstimulation (ovulation
induction), ovarian follicle
development in women with
hypogonadotropic
hypogonadism, male
hypogonadotric
hypogonadism
SE: headache, depression,
edema, ovarian
hyperstimulation syndrome,
multiple pregnancies in
women, gynecomastia in
men, hypersensitivity
CHORIOGONADOTROPIN
ALFA is arecombinat hCG
while LUTROPIN os a
recombinant LH
hCG given IM
PROLACTIN
BROMOCRIPTINE
MIXED Pergolide,
Cabergoline,
Quinagolide
MENOTROPINS
MOA: dopamine agonist; inhibits
prolactin release from the
pituitary gland; also slightly
inhibits GH release (in high
doses); dopaminergic effects on
CNS motor control & behavior
Mixture of FSH & LH from
postmenopausal women
Uses: hyperprolactinemia,
pituitary adenoma (prolactin-
secreting), acromegaly,
Parkinsons dse
SE: GI disturbance, nausea,
headache, lightheadedness,
orthostatic hypotension, fatigue,
behavioral change,
erythromelalgia, Raynauds
phenomenon (vasospasm),
pulmonary infiltrates (in high
doses)
Given PO or vaginally (for
hyperprolactinemia).
Contraindicated in px with
history of psychotic illness
POSTERIOR
PITUITARY
OXYTOCIN
OXYTOCIN
Desmoxytocin
MOA: activates oxytocin
receptors; stimulates
utreine contraction & labor;
stimulates mammary glands,
lactation & milk let-down
Uses: labor induction, labor
augmentation, control of
postpartum hemorrhage
SE: fetal distress, placental
abruption, uterine ruptue,
fluid retention (water
intoxication), hyponatremia,
heart failure,seizures,
hypotension
Contraindications: fetal
distress, prematurity,
abnormal presentation, CPD
& predispositions for uterine
rupture
ATOSIBAN is an oxytocin
receptor blocker; not yet
FDA approved since there is
concern about increased
rates of infant death
CARBETOCIN is an agonist
of peripheral Oxytocin
receptors
TD
VASOPRESSIN
AGONIST ANTAGONIST
CONIVAPTAN
DESMOPRESSIN Tolvaptan,
Lixivaptan
MOA: ADH agonist; relatively
MOA: antagonist at V1a, V2
selective for V2 receptors; receptors; reduces renal
Vasopression V2 receptor excretion of water in
agonist which causes conditions assoc with
insertion of water channels
increased vasopressin
in the collecting duct leading
to more water reabsorption
--> decrease the excretion Uses: SIADH, hyponatremia
of water; act on extra renal in hospitalized px, offset
V2 receptors to increase fluid retention in acute heart
FVIII and vWF failre & SIADH which causes
hyponatremia (dilutional)
Uses: central DI, hemohilia
A, vWdse, esophageal SE: infusion site rxns,
variceal bleeding, primary hyperK
nocturnal enuresis
(pediatric px), colon
Central Pontine Myelinolysis
diverticula
may cocur with rapid
correction of hypoNatremia
SE: GI disturbance,
headaches, flushing,
nausea, hyponatrremia, TOLVAPTAN is more
seizures, allergic rxns selective for V2 receptors
May be given intranasally,
PO or IV
Also contracts vascular
smooth muscle via V1
receptor leading to
vasoconstriction (used as a
tx for esophageal varices or
colon diverticula)
 TD
THYROID DRUGS

HYPOTHYROIDISM HYPERTHROIDISM

BETA
T4 T3 MIXED THIOAMIDE IODINE IODIDE
BLOCKERS

METHIMAZOLE POTASSIUM IODIDE PROPANOLOL RADIOACTIVE IODINE

LEVOTHYROXINE LIOTHYRONINE LIOTRIX PROPYLTHIOURACIL Lugol's Solution/ Potassium Iodide 131
Carbimazole Esmolol, Metoprolol, Atenolol
Saturated Solution [KISS]

MOA: inhibits thyroid peroxidase MOA: emits beta rays causing

Same MOA with rxns; blocks iodine organiSication; MOA: inhibit iodine organiSication & MOA: blocks beta receptors
MOA: activation of nuclear Same MOA. MOA: inhibits thyroid peroxidase rxns; blocks (control HR & other cardiac destruction of thyroid parenchyma
receptors results in gene Levothyroxine. inhibits peripheral conversion of T4 hormone release; reduce size &
iodine organiSication vascularity of thyroid gland abnormalities of severe
expression with RNA formation & into T3
thyrotoxicosis); slows pacemaker
protein synthesis Liotrix is a 4:1 ratio of activity; inhibits peripheral Uses: hyperthyroidism
Liothyronine has a faster
onset but shorter half life. T4:T3 Uses: hyperthyroidism, thyroid storm Uses: hyperthyroidism, thyroid storm, conversion of T4 into T3 (Only
Uses: hyperthyroidism, thyroid
Uses: hypothyroidism, myxedema storm preparations for surgical thyroidectomy Propanolol) SE: hypothyroidism (permanent),
coma to reduce the size & vascularity of the sore throat, sialitis
SE: maculopapular pruritic rash, GI distress, thyroid gland, radiation prophylaxis
cholestatic jaundice, agranulocytosis, urticaria, Uses: hyperthyroidism esp
SE: maculopapular pruritic rash, GI
SE: dry skin, sweating, tachycardia,
nervousness, tremor, weight loss,
MYXEDEMA COMA TREATMENT distressm fulminant hepatitis,
agranulocytosis, urticaria, vasculitis,
vasculitis, lupus-like syndrome,
lymphadenopathy, hypoprothrombinemia,

SE: iodism, acneiform rash, swollen
thyroid storm, adjunct to control
tachycardia, HPN & AFib, post MI
Preferred treatment for most patients.

exfoliative dermatitis, polyserositis, arthralgia, salivary glands, mucus membrane prophylaxis against sudden death
weakness, heat intolerance ŸIV loading dose of Levothyroxine (300-400 mcg), followed lupus-like syndrome, hypothyroidism, altered sense of taste or smell Permanent cure of thyrotoxicosis without
lymphadenopathy, ulcerations, conjunctivitis, rhinorrhea, surgery & no effect on other tissues.
by 50-100mcg daily hypoprothrombinemia, exfoliative drug fever, metallic taste, bleeding
T4 dose must be lowered in px ŸIV Hydrocortisone is indicated if the px has associated dermatitis, polyserositis, arthralgia, disorders, anaphylactoid rxns SE: bronchospasm, cardiac
DOC for nonpregnant hyperthyroid px bec longer depression, AV block, Advantages include easy administration,
with CVS dse or longstanding adrenal or pituitary insufficiency hypothyroidism DOC (24h). effectiveness, low expenses & absence of
hypothyroidism (increased hypotension, bradycardia
Should not be used alone (escape 2-8wks). pain.
cardiosensitivity).

DOC for pregant hyperthyroid px Cross the placenta (teratogen). ESMOLOL may be uase to treat
(does not enter placenta & Prevent radiation-induced thyroid damage. Contraindicated in pregnant women or
thyrotoxicosis-related arrhythmias. nursing mothers.
Thyrotropin (a recombinant breastmilk). Prenatal exposure causes APLASTIA CUTIS CONGENITA.
human TSH) is also available. Prenatal exposure causes fetal goiter.
Causes clinical improvement Patient should be euthyroid or on BB
Slow onset of action (3-4 wks for full effect). WITHOUTaltering thyroid hormone before RAI.
Shorter DOA 6-8hrs Onset is faster compared to Thionamides levels.
Maximum effect is seen after 6-8
(2-7days) but effect is transient (thyroid gland
wks of therapy. Thiamazole is the other name of Methimazole. escapes iodine block after several weeks of Onset of action is 6-12wks.
Onset is within hours but DOA is also
Slow onset of action (3-4 wks for full treatment)
short (4-6hrs)
effect)
Maximym effect sen in 3-6months

ANTI THYROID DRUGS INHIBITING THYROID STORM TREATMENT WOLFF-CHAIKOFF EFFECT

PERIPHERAL CONVERSTION OF T4 INTO T3 1) PTU – blocks thyroid hormone synthesis
2) IODIDE (KISS) – retards release of thyroid hormone
!IODI NE IN GE ST ION CAU SE H YP OT HYROI DISM!
!HY DROCORTI SON E!PT U!PROP ANOLOL! 3) PROPANOLOL – controls CVS manifestations JOD-BASEDOW PHENOMENON
4) HYDROCORTISONE – protects against shock & blocks
!IODI NE IN GE ST ION CAU SE H YP ERTH YROIDI SM !
DRUG-INDUCED HYPERTHYROIDISM peripheral conversion of T4 to T3

CAM

! C LOFIB RATE ! A MI OD ARONE ! M ET HA DON E!

 TD

CORTICOSTEROIDS

AGONIST ANTAGONIST

GLUCOCORTICOIDS MINERALOCORTICOIDS SYNTHESIS INHIBITORS RECEPTOR INHIBITORS

INTERMEDIATE RELEASE, DELAYED FLUDROCORTISONE

SHORT ACTING RELEASE Dexoycortisone
AMINOGLUTETHIMIDE KETOCONAZOLE METYRAPONE GLUCOCORTICOID MINERALOCORTICOID

HYDROCORTISONE/
CORTISOL
MOA: activates glucocorticoid receptors
leading to altered gene transcription;
suppreses inflammtaion; replaces cortisol
when deficient
Uses: adrenal insufficiency associated with
life threatening shock, chronic adrenal
insufficiency (Addisons Dse), congenital
adrenal hyperplasia, insect bites, contact
dermatitis, status asthmaticus, thyroid
storm
SE: none common when used topically or
at physiologic replacement doses
Low potency: Desonide
Medium potency: Fluticasone,
Mometasone
High potency: Desoximetasone, Clobetasol
PREDNISONE
Prednisolone, Methylprednisolone,
Meprednisone, Dexamethasone,
Betamethasone, Triamcinolone
MOA: suppresses inflammation & immune response
Uses: wide variety of inflammatory, allergic, autoimmune (collagen &
rheumatic dse etc), & neoplastic dses (hematopoeitic cancers),
prevention of organ transplant rejection, asthma, lung maturation in
preterm labor (Betamethasone & Dexamethasone), chemotherapy-
induced vomiting, hypercalcemia, mountain sickness)
SE: adrenal suppression, growth inhibition, muscle wasting,
osteoporosis, salt retention, glucose intolerance, behavioral changes
(psychosis)
BETAMETHASONE hastens fetal lung maturation.
PREDNISOLONE is the active metabolite of Prednisone.
This group has a long t1/2, reduced salt-retaining effect & better
penetration of lipid barriers
MOA: strong agonist of mineralocorticoid receptors; increase Na
reabsorption, K & H excretion
Uses: chronic adrenal insufficiency (Addisons Dse), congenital adrenal
hyperplasia, adrenal replacement therapy post adrenalectomy
SE: salt & fluid retention, hypoK, CHF, muscle wasting, osteoporosis,
glucose intolerance, behavioral changes
Additive hypoK with loop diuretics & thiazides.
DEOXYCORTICOSTERONE is the precursor of aldosterone.
FLUDROCORTISONE also has significant glucocorticoid activity.
Aldosterone is implicated in myocardial & vascular fibrosis &
baroreceptor function.
MOA: inhibits desmolase, blocking conversion of
cholesterol to pregnenolone; reduces synthesis
of all hormonally active steroids
Uses: breast cancer, Cushing sydnrome
SE: skin rash, hepatotoxicity, hypothyroidism
Abused by body builders to lower circulating
levels of cortisol in the body & prevent muscle
loss.
MOA: inhibits cholesterol side-chain cleavage,
cytochrome P450 enzymes & other enzymes
necessary for synthesis of all steroids
Uses: adrenal carcinoma, hirsutism, breast
cancer, prostate cancer, Cushing syndrome,
fungal infections
SE: hepatotoxicity, many drug interactions,
androgenuc effect
Potent inhibitory of CYP450 enzymes
MOA: selective inhibitor of steroid 11-
hydroxylation, interfering with cortisol &
corticosterone synthesis
Uses: diagnostic testing for adrenal
function, Cushing syndrome
SE: dizziness, GI disturbances
DOC for pregnant px with Cushing
syndrome.
SPIRONOLACTONE
MIFEPRISTONE (RU486)
MOA: competitive inhibitor at the GC receptor as well
as progesterone receptor
MOA: blocks aldosterone receptors
Uses: Cushing syndrome
Uses: for hypoK due to ther diuretics, for post MI, hyperaldosteronism
SE: abdominal pain & cramping, uterine cramping,
nausea, headache, vomiting, diarrhea, dizziness, SE: hyperK, anti-androgenic effect (gynecomastia)
vaginal bleeding
Also with weak antagnist effect at the androgen receptor
Also used as an approved abortifacient for medical
abortion (usually together with Misoprostol).
 TD

GONADAL HORMONES and INHIBITORS

PART1

ESTROGENS PROGESTINS

AGONIST ANTAGONIST AGONIST ANTAGONIST

ETHINYL ESTRADIOL NORGESTREL

SYNTHETIC ESTROGEN AROMATASE OVARIAN
Mestranol, Estradiol Cypionate, (NONSTEROID) SERM INHIBITOR INHIBITOR Norethindrone, Ethylnodiol, MIFEPRISTONE (RU-468)
Premarin, Estriol Megestrol, Desogestrel,
Norelgestromin, Norgestimate,
Etonogestrel, Progesterone,
ANASTROZOLE Levonorgestrel, Dydrogesterone,
TAMOXIFENE MOA: pharmacologic antagonist of glucocorticoid &
MOA: activates estrogen receptors; leads to changes in rates of
transcription of estrogen-regulated genes
DIETHYLSTILBESTROL Toremifene RALOXIFENE CLOMIPHENE FULVESTRANT Letrozole, DANAZOL Ulipristal, Tibolone, Norethisterone, progesterone receptors

Exemestane Dienogest
Uses: medical abortion, Cushings syndrome
Uses: primary hypogonadism, postmenopausal hormonal
replacement therapy, osteoporosis, contraception, intractable
dysmenorrhea SE: vaginal bleeding, abdl pain, GI upset (vomiting,
diarrhea), uterine cramping, nausea, headache, dizziness
SE: breakthrough bleeding, nausea, breast tenderness, migraine, MOA: activates progesterone receptors; changes rates of trancription
thromboembolism (DVTs), gallbladder dse, hypertriglyceridemia, MOA: estrogen antagonist MOA: estrogen antagonist MOA: partial agonist of MOA: weak cytochrome P450 of progesterone-regulated genes Combination with Misoprostol results in abortion of 95%
MOA: activates estrogen receptors; leads to MOA: reduces estrogen
HPN, premature closure of epiphysis in young females, increased changes in rates of trancription of estrogen- actions in breast tissue & CNS; actions in breast tissue, uterus estrogen receptors in pituitary; inhibitor & partial agonist of of early pregnancies.
risk of breast & endometrial cancer (remedy: add progesterone to estrogen agonist effects in & CNS; estrogen agonist effects reduces negative feedback by synthesis by inhibiting progestin & androgen
regulated genes aromatase
the preparation) uterus, liver & bone in liver & bone; increase bone Estradiol; increases FSH & LH receptors Uses: HRT (given together with Estrogen, to prevent Estrogen-induced
mineral density output endometrial cancer), contraception, assisted reproduction (for As abortifacient in early pregnancy (may be used up to
Uses: atrophic vaginitis, HRT, prevention of Uses: breast cancer, precocious maintenance of pregnancy), anovulation induction (given in high doses 49days after menses).
ETHINYL ESTRADIOL has low bioavailability PO/ TD/ IM/ intravaginal Uses: hormone-responsive Uses: endometriosis, fibrocystic to suppress FDH & LH)
adverse pregnancy outcomes, metastatic puberty
prostate cancer breast cancer, prophylaxis of Uses: osteoporosis, breast Uses: induction of ovulation for dse, hemophilia, angioneurotic
breast CA esp in high risk cancer prevention women who want to get edema Complication: failure to induce complete abortion. May
ESTRADIOL CYPIONATE is IM with longer t1/2. pregnant Pure estrogen receptor SE: HPN, decreased HDL, weight gain, reversible decrease in bone cause sepsis due to unusual organisms (Clostridium
SE: hot flushes, musculoskeletal
SE: breakthrough bleeding, nausea, breast antagonist in all tissues usedin mineral density, delayed resumption of ovulation after use sordelli)
disorders, osteoporosis, joint
tenderness, migraine, thromboembolism SE: hot flushes, SE: hot flushes, breast CA resistant to SE: acne, hirsutism, weight
PREMARIN is a mixture of conjugated estrogen used in HRT thromboembolism (DVTs), thromboembolism (DVTs) SE: hot flushes, eye symptoms pains gain, menstrual disturbances,
(DVTs), gallbladder dse, hypertriglyceridemia, Tamoxifen
HPN, premature closure of epiphysis in young endometrial hyperplasia, (afterimages), headache, hepatic dysfunction MEGESTROL is used as an appetite stimulant.
Effects of estrogen: growth of genital stuctures & secondary sexual females, increased risk of breast & endometrial endometrical cancer constipation, reversible hair Effective against breast cancers
cancer (remedy: add progesterone to the Reduces incidence of breast loss, ovarian enlargement,
characteristics, modifies serum protein level & decrease bone cancer in women who are very that have become resistant to Contraindicated during
multiple pregnancy (10%) Tamoxifen. Given PO or as vaginal cream.
resorption, enhances coagulability of blood, increases TG & HDL preparation) Prevents osteoporosis in post high risk. pregnancy & breastfeeding.
levels while decreasing LDL, if given as continuous infusion will menopausal women &
inhibit FSH & LH decreases risk of Increased risk of low-grade MEDROXYPROGESTERONE has a better oral bioavailability.
Associated with infertility, ectopic pregnacy, EXEMESTANE is an irreversible
clear cell vaginal adenocarcinoma in daughters atherosclerosis at the risk of No estrogenic effects on ovarian cancer with long term May also act on glucocorticoid
endometrial tissue. inhibitor receptors.
of mothers who took DES. causing Endometrial cancer. use.
L-NORGESTERL & NORETHINDRONE has more androgenic effect.

FLUVESTRANT is full estrogen

receptor antagonist (no agonist NORGESTREL undergoes enterohepatic recirculation.
effect) used in hormone
receptor positive metastatic Effects of Progesterone: induces secretory changes in the
breast cancer. endometrium, stabilize the endometrium, affect carbohydrate
metabolism & stimulate deposition of fat, high doses suppress FSH &
TORIMEFENE is structurally LH secretion.
related to Tamoxifen
TIBOLONE is a synthetic steroid with weak estrogenic, proestrogenic &
androgenic activity, and hence is an agonist of the estrogen,
progesterone & androgen receptor. It is primarily used in menopausal
hormone therapy, postmenopausal osteoporosis & endometriosis.

GNRH
AGONIST
LEUPROLIDE Gonadorelin,
Goserelin, Histrelin,
Nafarelin, Triptorelin
MOA: agonist of GnRH receptors; increased LH
& FSH secretion with INTERMITTENT
administration; reduced LH & FSH secretion
with PROLONGED CONTINUOUS administration
(due to downregulation of GnRH receptors in
the pituitary cells that normally release LH &
FSH)
Uses: ovarian suppression, controlled ovarian
hyperstimulation, endometriosis, myoma uteri,
central precocious puberty, advanced prostate
cancer
SE: hot flushes, sweats, headache, light
headedness, injection site rxns, nausea,
osteoporosis, gynecomastia, reduced libido,
decreased hematocrit
Symptoms of hypogonadism with continuous
treatment.
Temporary exacerbation of precocious puberty
or prostate cancer.
Apoplexy & blindness during the first few wks of
therapy (remedy: co-administer Flutamide, an
androgen receptor antagonist)
May be given intranasally, depot formulation
also available.
LEUPROLIDE has a long agonist activity.
ANTAGONIST
GANIRELIX
Cetrorelix, Abarelix,
Degarelix
MOA: blocks GnRH receptors;
reduced endogenous production of
LH & FSH
Use: prevents premature LH surge
during controlled ovarian
hyperstimulation, advanced prostate
cancer
SE: nausea, headache,
hypersensitivity (Abarelix), hot
flushes, gynecomastia, decreased
libido, decreased hematocrit,
osteoporosis
Does not cause a tumor flare-up
when used for treatment of
advanced prostate cancer
Also less likely to cause ovarian
hyperstimulation syndrome
DEGARELIX is used for prostate CA
while GANIRELIX prevent LH surge in
controlled ovulation.
GONADAL HORMONES and INHIBITORS
AGONIST
TESTOSTERONE
Fluoxymesterone,
Methyltestosterone,
Testosterone Cypionate,
Oxymetholone,
Mesterolone
MOA: activates androgen receptors; promotes
development of male characteristics;
increases body muscle bulk & RBC production
Uses: male hypogonadism, delayed puberty,
wasting syndromes, certain types of anemia
SE: virilization & menstrual irregularities in
females, paradoxical feminization in males,
cholestatic jaundice, elevated LFTs, premature
closure of epiphysis
Contraindicated in pregnant women & px with
prostate cancer.
Effects of Androgen: secondary sexual
characteristics, fertility & libido, male pattern
baldness, increases muscle mass, increased
RBC production, decreased urea nitrogen
excretion, maintains normal bone density
Used illegally by athletes as performance
enhancer
ANDROGENS
OXANDROLONE
Nandrolone
Deacnoate
MOA: activate androgen receptors;
promotes development of male
characteristics; increases body
muscle bulk & RBC production;
increases ratio of anabolic-to-
androgenic activity
Uses: illegal performance
enhancement drugs in athletes
SE: virilization in females,
paradoxical feminization in males,
cholestatic jaundice, elevated liver
enzymes, HCC
This group is called ANABOLIC
STEROIDS
TD
PART2
OCPs
ANTAGONISTS COMBINED PROGESTIN ONLY POST-COITAL
ESTRADIOL + LEVONORGESTREL
RECEPTOR MEDROXYPROGEST Ethinyl Estradiol +
ANTAGONISTS SYNTHESIS INHIBITORS NORETHINDRONE (Ethinyl ERONE ACETATE
Estradiol + Desogestrel/ Levonorgestrel
Norgestrel/ Drospirenone/
Norgestimate/
Norethisterone)
MOA: activates estrogen &/or
FLUTAMIDE CYPROTERONE progesterone receptors; thicken
cervical mucus; inhibits ovulation
Bicalutamide, Cyproterone FINASTERIDE Dutasteride MOA: activates progesterone
Nilutamide Acetate receptors; prevents contraception
by altering cervical mucus & creating
Uses: emergency contraception
a hostile endometrium
MOA: combined oral contraceptive, activates SE: severe nausea, vomiting, breast
estrogen & progesteron receptors, inhibits tenderness, irregular bleeding,
Uses: contraception, HRT headache, dizziness (fewer SE
ovulation, effects on cervical mucus gland, uterine
compared to estrogen alone &
tubes & endometrium lead to decreased affinity,
inhibit ovulation when given before LH surge SE: breakthrough bleeding, hair loss, combination contraceptives)
MOA: competitive antagonist MOA: inhibits 5alpha-reductase enzyme that
dysmenorrhea, delayed return of
androgen receptor converts testosterone to dihydrotestosterone
MOA: antagonist at androgen fertility, osteoporosis Must be taken within 72hrs of
receptor; marked progestational Uses: contraception, hypogonadism, acne,
unprotected sexual intercourse (not
effect that suppresses the feedback hirsutism, dysmenorrhea, endometriosis
Uses: prostate cancer, surgical Uses: BPH, male-pattern baldness, hirsutism effective once implantation has
castration (Nilutamide) enhancement of LH & FSH IM depot preparation (DEPO-
PROVERA). occured).
SE: breakthrough bleeding, nausea, breast
SE: impotence (rare), gynecomastia, tenderness, skin pigmentation, thromboembolism
SE: gynecomastia, hot flushes, Uses: hirsutism, component of OCPs, depression YUZPE regimen for combination
decreases sexual drive in men (DVTs), breast cancer (earlier onset), headache, Does not protect against STDs.
impotence, hepatotoxicity depression, weight gain & hirsutism for older OCPs emergency contraception.
Controversial use in prevention of prostate
SE: hepatotoxicity, adrenal cancer.
Less hepatotoxicity with Bicalutamide Lifetime risk of breast cancer is not changed. Doe not protect against STDs
& Nilutamide. suppression, depression,
gynecomastia, galactorrhea,
thromboembolism DUTASTERIDE is newer with longer t1/2 Does not protect against STDs
GnRH analogs (Leuprolide) must be
co-administered with Flutamide to
Orphan drug status This group is less likely to cause impotence,
prevent acute flare-up of prostate NORETHINDRONE is a testosterone derivative
cancer infertility & decreased libido while DROSPIRENONE is a spirinolactone
derivative that is anti adrogrenic
NORGESTIMATE & DESOGESTREL are newer
progestins
Combined OCPs may be used for androgen-
induced hirsutism
MESTRANOL (Estrogen) may also be used in OCPs

SULFONYLUREAS
1ST GEN
CHLORPROPRAM
IDE Tolbutamide,
Tolazamide
MOA: increases insulin secretion
from the pancreatic beta cells by
closing ATP-sensitive K+ channels
Uses: T2 DM
SE: hypoglycemia, weight gain,
disulfiram rxn, hyperemic flush
after alcohol ingestion, dilutional
hyponatermia, hematologic toxicity
TOLBUTAMIDE &
CHLORPROPAMIDE are highly
protein bound drugs --> drugs
that compete for protein bindng
may enhance hypoglycemic effects
Lower potency, greater toxicity.
May also cause allergic rxns &
rash
INSULIN
SECRETAGOGUES
MEGLITINIDES
REPAGLINIDE
Nateglinide,
2ND GEN
Mitiglinide
GLIPIZIDE Glimepiride, MOA: increases insulin secretion
from pancretic beta cells by
Glyburide, Glibenclamide, closing ATP-sensitive K+ channels;
insulin secretagogue, smular to SU
Gliclazide with some overlap in binding sites,
reduces circulating glucose,
increases glycogen, fat & protein
formation & gene regulation
Uses: T2DM (postprandial
hyperglycemia)
MOA: increases insulin secretion from pancreatic beta SE: hypoglycemia (least),
cells by closing ATP-sensitive Kchannels -->
headache, URTI
depolarizarion of beta cells of the pancreas
Used in diabetics with Sulfa
Uses: T2DM, in px with functioning beta cells, reduces allergies.
circulating glucose, increase glycogen, fat & protein
formation, regulates gene expression
NATEGLINIDE has the least
incidence of hypoglycemia & may
SE: hypoglycemia (less), weight gain, photosensitivity, be used in CKD px.
hematologic toxicity, cholestatic jaundice
(Glibenclamide)
Requires islet cell function.
Contraindicated in px with hepatic impairment & renal
insufficiency. Very shory DOA (4-8hrs only)
Require islet cell function. May come in combination with
Metformin
May come in combination with Metformin.
INSULIN
SENSITIZERS
BIGUANIDES
METFORMIN
MOA: reduced hepatic & renal
gluconeogenesis with decreased
endogenous glucose production,
activates AMP-stimulated protein
kinase leading to inhibition of
gluconeogenesis/ endogenous
glucose production
Uses: T2DM (first line), diabetes
prevention, PCOS
SE: GI disturbance, weight loss,
lactic acidosis (esp in renally &
hepatically impaired px), Vit B12
malabsorption
DOC for obese diabetics.
Contraindicated in px with renal
dse, alcoholism, hepatic dse, CHF,
or conditions predisposing to
tissue anoxia (hypoxic or acidotic
states)
May also caused slowing of
glucose absorption from GIT,
decreased plasma glucagon.
Causes a decrease in endogenous
insulin production by increasing
insulin sensitivity of tissues "Insulin
Sparing Effect" therefore does not
have weight gain as SE.
Does not cause hypoglycemia
ANTI DIABETIC AGENTS
THIAZOLEDI
NEDIONES
PIOGLITAZONE
Rosiglitazone,
Troglitazone
MOA: regulates gene expression
by binding to PPAR-gamma &
PPAR-alpha --> increases tissue
sensitivity, increases glucose
uptake in muscle & adipose tissue,
inhibits hepatic gluconeogenesis,
effects on lipid metabolism &
distribution of body fat, conrtol of
fasting & postprandial glucose;
decreased risk of DM in high rish
px
Uses: T2DM, DM prevention
SE: fluid retention, anemia, weight
gain, CHF, bone fractures esp in
women, CVS events
(Rosiglitazone), hepatotoxicity
(Troglitazone), macular edema,
dyslipidemia, (increase HDL & LDL,
decrease TG), incresed risk of MI
(Rosiglitazone)
Contraindicated in pregnancy,
chronic liver dse & CHF.
PIOGLITAZONE reduces mortality &
macrovascular events (MI &
stroke) bec of its TG lowering
effects.
ROSIGLITAZONE binds to PPAR-
gamma only.
PPAR regulates transcription of
genes encoding proteins involved
in carbohydrate & lipid
metabolism.
May increase risk for developing
bladder cancer.
NON-INSULIN
ALPHA
GLUCOSIDASE
INHIBITORS
ACARBOSE
Miglitol,
Voglibose
MOA: inhibits intestinal alpha
glucosidases --> reduce
conversion of starch &
dissacharides to monosaccharide
--> reduce post prandial
hyperglycemia
Uses: T2DM, DM prevention
SE: GI disturbance (flatulence,
diarrhea, abdl pain), hypoglycemia
(when taken with SU), increased
liver enzymes
Relatively minor glucose-lowering
benefit.
Treat hypoglycemia with oral
glucose (Dextrose) NOT Sucrose,
bec absorption is impaired.
Impaired absorption of Sucrose.
Taken immediately before a meal.
Contraindicated in px with renal &
hepatic impaiement & intestinal
disorders
AMYLIN
ANALOG
PRAMLINTIDE
MOA: activates amylin receptors;
reduce post-meal glucose
excursions; suppresses glucagon
release; delays gastric emptying;
stimulates CNS to reduce appetite
(anorectic effect)
Uses: T1 & T2 DM
SE: hypoglycemia, GI disturbances,
nausea, anorexia, headache
Administered as an injectable
preparation (SC) together with
insulin to control post prandial
glucose
Short t1/2 of 48 mins
TD
INCRETIN
MODULATO
SGLT2 BILE ACID
RS
INHIBITORS SEQUESTRANT
DAPAGLIFLOZIN
GLP1 DPP4 Empagliflozin,
ANALOG INHIBITOR COLESEVELAM
Canagliflozin
SITAGLIPTIN MOA: inhibits SGLT2 transporter --
EXENATIDE > inhibits reabsorption of glucose
Liraglutide Saxagliptin, in the kidneys back to the blood --
> excretion of glucose out in the
Linagliptin, urine MOA: binds bile acids; lowers
glucose through unknown
Vildagliptin, Uses: T2DM
mechanism
Tenegliptin Uses: T2DM
SE: dizziness, strong smell of
urine, edema, weakness, nausea,
vomiting, decrease in the amount SE: constipation, dyspepsia,
MOA: activates GLP-1 receptors --
> reduction of post-meal glucose
of urine myalgia, asthenia
excursopns; augments glucose-
stimulated insulin release from
Do not use among renally impaired
px
pancreatic B cells; retards gastric
emptying; inhibits glucagom MOA: inhibits dipeptidyl
secretion; produces satiety peptidase-4 (DPP4) that degrades
GLP-1 & other incretins --> raises
circulating GLP-1 levels; augments
Uses: T2DM glucose-stimulated insulin release
from pancreatic B cells; retards
gastric emptying; inhibits glucagon
SE: hypoglycemia, acute
secretion; produces satiety;
pancreatitis, nausea, vomiting,
reduces post-meal glucose
headache, anorexia, mild weight excursions
loss
Uses: T2DM
Administered as an injectable
preparation (SC), used in
combination with Metformin or a
SE: headache, nasopharyngitis,
SU
URTI, hypersensitivity rxns,
pancreatitis
LIRAGLUTIDE has possible thyroid
CA risk Administered orally as
monotherapy or in combination
with Metformin
Long actinf injectables
 TD

PANCREATIC HORMONES AND ANTIOBESITY DRUGS

INSULIN GLUCAGON DRUGS FOR OBESITY

RAPID: Lispro, Aspart, Glulisine

SHORT: Regular (Humulin R) ORLISTAT SIBUTRAMINE RIMONABANT PHENTERMINE
INTERMEDIATE: NPH, Lente (Humulin N)
LONG: UltraLente, Glargine, Detemir, Insulin Degludec MOA: activates glucagon receptors

PREMIXED INSULIN: Humulin 70NPH/ 30 Regular

Uses: severe hypoglycemia, diagnosis of endocrine
disorders, beta blocker overdose, radiology of the bowels
MOA: inhibits GI & pancreatic MOA: selectively blocks
lipases; reduces absorption of fats An appetite suppressant
cannabinoid-1 (CB-1) which is an amphetamine
MOA: activates insulin receptors --> reduces circulating glucose by increasing glucose uptake; promote glucose SE: nausea, vomiting, hypotension receptors; reduces derivative
transport & oxidation, glycogen lipid & protein synthesis & regulates gene expression Uses: obesity, T2DM MOA: inhibits NE & serotonin reuptake in the appetite (anorectic effect)
CNS; reduces appetite (anorectic effect)
Glucagon-secreting tumors (Glucagonomas) present with SE: similar with
Uses: T1 & T2 DM, diabetic emergencies (DKA, HHS -rapid acting), hyperK decreased amino acids in blood, anemia, diarrhea, weight SE: weight loss, flatulence, Uses: obesity, smoking Amphetamine
loss & necrolytic migratory erythema Uses: obesity cessation, drug addiction
steatorrhea, fecal incontinence,
malabsorption of fat-soluble
SE: hypoglycemia, insulin allergy, immune insulin resistance, lipodystrophy at injection site, weight gain, increased
vitamins (A,D,E,L), hepatotoxicity SE: dry mouth, GI disturbance, tachycardia, SE: suicidality,
cancer risk (linked to insulin resistance & hyperinsulinemia in px with prediabetes & T2DM)
HPN, CVS events (MI, arrhythmias), stroke depression, nausea
Rebound weight gain upon
Beta blockers may mask signs of hypOglycemia. discontinuation.
Withdrawn due to increased risk of CVS events Withdrawn because of
& stroke increased risk of suicides,
All insulin preparations contain Zinc. Contraindicated in pregnancy, depression & other
reduced hepatobiliary function & serious psychiatric
malabsorption states problems
Parenteral (IV or SC)

Effects of insulin: increased glycogen & protein synthesis, decreased protein catabolism, increased TG storage
MOA of Insulin: TRANSPORTER TISSUES FUNCTION
RAPID ACTING INSULINS are injected a few mins prior to meals & they are the preferred insulin for continuous SC -binds to a tyrosine kinase receptor, which
infusion devicees. phosphorylayed itself & a variety of intracellular
GLUT1 All tissues, esp red cells, brain Basal uptake of glucose; transport across
proteins when activated by the hormone
the BBB
SHORT ACTING INSULINS are injected more than an hour before a meal -activation of phosphatidulinositol-3-kinase
pathway & MAP kinase pathway
-translocation of glucose transporter (esp GLUT 4)
INTERMEDIATE ACTING INSULINS are often combined with regular & rapid acting insulins GLUT2 Beta cells of pancreas; liver, kidney, gut Regulation of insulin release, other
to the cell membrane
aspects of glucose homeostasis
-increase in glucose uptake
LONG ACTING INSULINS are called PEAKLESS insulins -increased glycogen synthase activity
-increased glycogen formation
GLUT3 Brain, kidney, placenta, other tissues Uptake in neurons & other tissues

GLUT4 Muscle, adipose Insulin-mediated uptake of glucose

GLUT5 Gut, kidney Absorption of Fructose


PTH
TERIPARATIDE
MOA: act through PTH
receptors to produced a net
increase in bone formation,
stimulates bone turnover
Uses: osteoporosis
SE: hypercalcemia,
hypercalciuria, arthralgia,
rhinitis, nausea, weakness,
dizziness, pharyngitis,
dyspepsia, rash
Must be administered in low
intermittent doses to
stimulate bone formation.
Used IV for osteoporosis.
TD
BONE AND MINERAL HOMEOSTASIS
HORMONAL NON-HORMONAL
THYROID PHOSPHATE MONOCLONAL
HORMONE VIT D BISPHOSPHONATE BINDING RESIN SERM ANTIBODY MINERALS
ALENDRONATE CALCIUM
CALCITONIN ERGOCALCIFEROL CALCITRIOL
SEVELAMER RALOXIFENE DENOSUMAB Phosphate,
Salcatonin Cholecalciferol Doxercalciferol, Paricalcitol, Calcipotriene Wtidronate, Ibandronate,
Pamidronate, Risedronate, Strontium
Tiludronate, Zoledronic Acid
MOA: regulates gene transcription via the Vit D MOA: binds to dietary MOA: interacts
MOA: acts through receptors; stimulates intestinal Ca absorption, MOA: regulates gene transcription via the Vit D receptor; phosphate & prevents selectively with estrogen MOA: binds to RANKL & MOA: multiple
calcitonin receptors to bone resorption, renal Ca & phosphate stimulates intestinal Ca absorption, bone resorption, renal its absorption receptors leading to prevents it from physiologic actions
inhibit bone resoprtion reabsorption; decrease PTH, promote innate calcium & phosphate reabsorption, decrease PTH MOA: suppresses the activity of osteoclasts in inhibition of bone stimulating osteoclast through regulation of
immunity part via inhibition of farnesyl pyrophosphate resorption without differentiation & multiple enzymatic
synthesis; inhibits bone resorption & Uses: stimulating breast or function --> inhibit pathways; Sr
Uses: Pagets dse of Uses: secondary hyperparathyroidism in CKD, hypocalcemia in secondarily, bone formation by acting on the hyperphosphatemia in endometrial hyperplasia bone resorption
bone, hypercalcemia, suppresses bone
Uses: Vit D deficiency (rickets, osteomalacia, hypoparathyroidism (Calcitriol), psoriasis (Calcipotriene) basic hydroxyapatite crystal structure CKD,
osteoporosis, tumor resorption & increase
intestinal ostedystrophy, CKD, chronic liver dse, hypoparathyroidism, vit bone formation; Ca &
marker for thyroid hypoparathyroidism, nephrotic syndrome), D intoxication Uses: osteoporosis Uses: osteoporosis
cancer SE: hypercalcemia, hyperphosphatemia, hypercalciuria Uses: Pagets dse of bone, hyoercalcemia esp PO4 are required for
osteoporosis, psoriasis, renal failure,
in malignancies, osteoporosis, bone bone mineralization
malabsorption
metastases SE: hypo/hypertension, SE: increased risk of SE: increased risk of
SE: rhinitis, nausea, The active form Calcitriol is preferred in px with CKD, chronic GI disturbance venous infection
Uses: osteoporosis,
vomiting, facial flushing, SE: hypercalcemia, hyperphosphatemia, liver dse, & hypoparathyroidism. thromboembolism
tingling SE: adynamic bone, osteonecrosis of the jaw, osteomlacia,
hypercalciuria deficiencies in Ca & PO4
renal impairment, GI irritation Can significantly reduce
DOXERCALCIFEROL is a prodrug that is converted in the liver uric acid levels
Administered as a nasal Commonly added to dairy products & other food to 1,25-dihydroxyvitamin D
SE: ectopic calcification
spray. products Take drugs with large quantities of water &
avoid situations that permit esophageal reflux. Contraindicated in
PARICALCITOL, CALCIPOTRENE are analogs of Calcitriol & are
hypophosphatemia &
Used for osteoporosis Given topically for psoriasis, given with Calcium used topically for psoriasis & are being investigated for bowel obstruction
malignancies & inflammatory disorders.
but is less effective than supplements for osteoporosis Remedy for GI irritation & prevent reflux; take
Biphosphonates & lots of water & keep px in an upright position
Teriparatide for 30mins after intake of drug.
DOXERCALCIFEROL, PARICALCITOL & CALCIPOTRIENE cause lss
hypercalcemia & hypercalciuria
Contraindicated in those with renal
impairment, esophageal motility disorders &
peptic ulcers


Hope this helps you!

This is a tabulated notes of Topnotch Pharmacology.
This is helpful while studying the Pearls J
God Bless!

-
TD Trix Dones LM Leo Magpantay