✓ Misbranded drug – low quality drug Ex: PCM 650 contains only PCM 300

✓ Adultered drug – has additional unwanted substances

Correct format of prescription: Complete name of drug, dose, frequency (no abbreviations)
Ex: Tablet azithromycin 500 mg once a day for 5 days

26
1
 Defecation
Urination
Miosis + Accomodation
B.C
Bradycardia ( )
Emesis
Lacrimation
Salivation

Cholinergic agonists
❖ Direct agonist

 Tertiary amines
✓ Pilocarpine: DOC in CAG, Also used in Xerostomia
SE: Brow ache, Retinal detachment

 Quarternary amines
✓ Bethenechol: Rx of post-op ileus and urinary retention

❖ Indirect agonists (Carbamates-Reversible)

 Tertiary amines
✓ Donepazil (DOC) Gallantamine Rivastigmine Tacrine: Rx of
✓ Physostigmine: Rx of Atropine/Dathura/Belladona toxicity

 Quarternary amines
✓ Edrophonium: Dx of Myasthenia Gravis
✓ Neostigmine: Rx of
✓ Pyridostigmine: Rx of Myasthenia Gravis

Organophosphates & Carbamates

MOA:

C/F:
+ M: Diarrhea, Urination, Miosis, B.C, Bradycardia, Emesis, Lacrimation, Salivation
+ Nm: Initially contractions later SMR

Rx:
OP:
Carbamate
Atropine (DOC): every 5 minutes until “Signs of Atropinization i.e Mydriasis,↑H.R,
↓Secretions seen
Anti-cholinergics

✓ Botox:
Used in Rx of Blepharospasm, Wrinkles, Cervical dystonia, Achalasia cardia
✓ Onabotulinum toxin A: Rx of Prophylaxis of Migraine

2
 Muscarinic antagonists

✓ Bronchi: SAMA- Ipratropium, LAMA- Tiotropium SE: Dry mouth (MC)

✓ Anti-secretory: Glycopyrrolate ( BBB)

✓ Heart: Atropine – DOC for bradycardia, AV block

✓ Eyes (Mydriatics + Cycloplegics): Cyclopentolate, Atropine, Tropicamide

✓ CNS: Benzhexol (Trihexyphenidyl)

✓ Urinary system: Rx for overactive bladder (Detrusor instability, urge incontinence)

Solifenacin, Oxybutynin, Fesoterodine, Flavoxate, Tolterodine, Trospium ( BBB), Detrusor:
Darifenacin
STD(tolterodine) are uroselective, others are Non-selective

✓ GIT:

Anti-emetic:
Also used in Narcoanalysis (DOC: Thiopentone)

Sympathetic Nervous System

⍺1 ⍺2
⍺1a: mydriasis, urethra constriction ⍺2a: ↓ symp func, ↓ functions in CNS
(prostate) ⍺2b(postsynaptic): vasoconstriction
⍺1b: vasoconstriction

β1 β2 β3
↑ Dromo, Chrono, Inotropy B.D, V.D, Uterine relax ↓ Urination
↑glycemia Lipolysis
↑ renin production ↓kalemia

3
 Sympathomimetics

✓ Adrenaline:
DOC: …………………shock (I.m> S.C) 0.5 ml of 1:1000 if NR → 0.25 ml iv (1.10000)
Treatment of Cardiac arrest: i.v (1:10000), Bradycardia
Bronchial asthma 0.5 ml of 1:1000
Given along with
Also used in glaucoma (prodrug: dipivefrine)
Shows Vasomotor reversal of Dale/ Epinephrine reversal

✓ Dopamine:
DOC for Cardiogenic shock with Oliguria

✓ Nor-Adrenaline:
DOC in vasodilatory shock & cardiogenic shock

✓ Dobutamine:
DOC -Inotrope in Acute CHF, also used in stress echocardiography

Indirectly acting sympathomimetics

❖ Reuptake ⊖: Cocaine
❖ Release enhancers or drugs causing displacement of NT:
✓ Tyramine:
✓ Methylphenidate:
✓ Modafinil:

Non-catecholamines

❖ Alpha-1 agonist:

4
✓ Phenylephrine: Mydiatric, Decongestant, DOC for Hypotension d/t Spinal anesthesia +
bradycardia, Priaspism. SE: Bradycardia
✓ Midodrine (DOC) for Rx of Orthostatic hypotension
✓ Oxymetazoline
SE: Rhinitis medicamentosa/Rebound rhinitis

❖ Alpha-2 agonist:
✓ Methyldopa: Rx of PIH
✓ Clonidine: DOC in Rx of HTN urgency, Tourette’s syndrome, diarrhea in Diabetic patients
SE:

❖ Beta-3 agonist:
✓ Mirabegron,Vibegron

❖ Beta-2 agonist:
✓ SABA(<4 hr, fast acting)- Salbutemol, Terbutaline
✓ LABA(12 hr)- Salmeterol & Formeterol

SE: Tremors, Tachycardia (Palpitations), Hypokalemia

Sympatholytics

❖ Alpha blockers:
Non-selective:
✓ Phenoxybenzamine: Rx of Phaeochromocytoma
✓ Phentolamine, Tolazoline: Rx of Cheese Rxn & Rebound HTN

Alpha-1 blockers:
✓ Prazosin: Rx of HTN + BPH, HTN + Dyslipidemia, Scorpion sting
SE: 1st dose hypotension, Postural hypotension

Selective Alpha-1a blockers: Tamsulosin, Sildosin

❖ Beta blockers:
1st gen (Non-selective): …………………………….., Timolol, Nadolol

2nd gen (Cardioselective): Celiprolol, Metoprolol, Betoxolol, Esmolol (metabolized by

Esterases), Atenolol, Nebivolol (most cardiosel)

3rd gen: additional properties like Alpha block (Labetolol, Carvedilol), CCB(Carvedilol), NO
release (Nebivolol, Nipradilol), K channel open (Tilisolol), K channel close (Sotalol)

Uses:
Rx of HTN (2nd line), Angina, Chronic CHF, MI, Arrythmia, HOCM, Aortic dissection, Glaucoma
(avoid in asthmatics), DOC in Perfomance anxiety and prophylaxis of migraine, Thyroid
storm
C/I: Asthma, Vasospastic disorders, Diabetes Mellitus, Acute CHF

5
 Antidote: Glucagon

CARDIOVASCULAR SYSTEM

Anti Hypertensives

Drugs acting through NO

✓ Hydralazine -  TPR via arteriolar dilation. SE –
✓ Nitroprusside -  TPR via arteriolar & venous dilation SE – ………………… toxicity

K channel openers: Minoxidil, Diazoxide, Hydralazine

✓ Topical Minoxidil is used in
✓ Diazoxide is used in

CCB (Dihydropyridines):
✓ Nicardipine:
✓ Nifedipine:
✓ Nimodipine is cerebroselective so its used to reverse compensatory v.c (ischemia) after SAH
Side effects: Reflex tachycardia, Gingival hyperplasia, Constipation

Drugs acting on RAAS

✓ Beta-blockers
✓ Direct Renin ⊖: Aliskiren, Enalkiren

✓ ACEI: Capto(shortest), Lisino, Perindopril (longest acting)

✓ ARB’s: Epro (shortest), Telmisartan(longest acting)

• All are prodrugs except capto & lisinopril, olme & candesartan
• Uses of ACEI’s and ARB’s: HTN, Diabetic nephropathy, CKD, MI, Heart failure
• Losartan has Q anti-platelet, uricosuric activity whereas Telmisartan has PPAR- agonist
activity

SE: ACEI cause ………………………… (MC), ……………………………

All RAAS inhibitors can cause hyperkalemia
• C/I in pregnancy ,they are also C/I in bilateral renal artery stenosis
✓ Spironolactone: DOC in Rx of Resistant HTN

HTN with comorbidities :

▪ DM,CKD –
▪ Angina, Previous MI, Hyperthyroidism, Migraine, Anxiety, Tremors -
▪ Osteoporosis –
▪ Heart failure –
▪ BPH, dyslipidemia –
▪ Raynauds disease -

Diuretics

6
❖ Loop diuretic/ High ceiling diuretics:
▪ They act on thick part of ascending limb of loop of henle, ………………… symporter system
Uses:
▪ DOC for……..………………… edema
▪ Furosemide is diuretic of choice in Renal failure (Thiazides – ineffective)
Side effects:
▪ Hypo (Na, K, Cl, Ca, MG) emia
▪ Hyperuricemia, Hyperglycemia, Hyperlipidemia
▪ Metabolic alkalosis, Ototoxicity (Ethacrynic acid is the most ototoxic)

❖ Thiazide diuretics: Moderate efficacy diuretics

Ex: Hydrochlorothiazide, Chlorthalidone, Indapamide, Metolazone
▪ Act on proximal part of DCT by ⊖ Na+cl- symporter
Uses: Rx of HTN, Calcium stones, Rx of nephrogenic DI
Side effects: Same as loops except Hypercalcemia

❖ K+ sparing diuretics:
▪ Act on CD and ⊖ Na - K antiport system which is under the influence of aldosterone
Uses:
▪ Spironolactone is DOC for edema in …………………, Conn syndrome and Resistant HTN. Its also
used in CHF and adjunct to diuretics causing hypokalemia
▪ Amiloride is DOC for Rx of……………………………………, also used for Liddle’s syndrome
SE: Hyperkalemia, Metabolic…………………, Gynecomastia (Spironolactone)

Gynecomastia drugs: Digoxin, INH, Spironolactone, Cimetidine, Ketoconazole, Oestrogen

❖ Carbonic anhydrase ⊖:
▪ They act on PCT, ⊖ carbonic anhydrase ⊖ Na+ - H+ antiport system causing loss of Na+ &
bicarbonate in urine
Uses: Rx of mountain sickness (DOC), acute congestive glaucoma, alkanization of urine
Side effects: Hypokalemia (max among diuretics), hypersensitivity reaction (sulphonamide
derivative), Metabolic acidosis, Renal stones

❖ Osmotic diuretics: works on LOH>PCT

Mannitol is DOC for Cerebral edema, Acute congestive glaucoma

Anti-Diuretic hormone / Vasopressin

Vasopressin agonists
✓ Terlipressin: selective V1 ⊕ - DOC for bleeding esophageal varices
✓ Desmopressin: selective V2 agonist
DOC for Rx of Central Diabetes insipidus & Nocturnal enuresis

Vasopressin antagonists
✓ Selective V2 – Mozavaptan, Tolvaptan (most potent but hepatotox) is DOC for SIADH
Congestive Heart Failure

7
 Acute CHF
Inotropes: Dobutamine (DOC)
Pulmonary edema: furosemide(DOC)

Chronic CHF
✓ ACEI/ARBS: Candesartan & Valsartan are preferred
✓ -blockers: Carvedilol, Metoprolol, Bisoprolol
✓ Vasodilators: Nitrates, Hydralazine, CCB (Non-DHP), Vericiguat
✓ Aldosterone ⊖: Spironolactone, Eplerenone
✓ Ivabradine
✓ Neutral endopeptidase (neprilysin) ⊖: Sacubitril
(Sacubitril + Valsartan combo known as ARNI )
✓ Vasopeptidase ⊖: Omapatrilat, Sampatrilat ⊖ both ACE & Neprilysin

❖ Drugs ↓ mortality: Sacubitril, B⊖, Hydralazine+IDN, ACEI/ARB, Ivabradine, Spironolactone

✓ Cardiac glycosides (Digoxin, Digitoxin, Oubain)

▪ MOA: It ⊖ Na-K ATPase (inotrope), vagomimetic action (anti-arrhythmic) so it 
contractility  H.R
▪ SE: Earliest & MC – Nausea, Vomitting, Gynecomastia, Xanthopsia, Hyperkalemia,
Arrhythmia (MC-Ventricular bigeminy, Most characteristic- Non-paroxysmal atrial
tachycardia with AV block
▪ Digoxin toxicity Rx – Mild (K+), Severe (Digibind), Ventricular arrhythmia – Lidocaine (DOC)
▪ Cautions: Renal & Thyroid dysfuntion, Myocarditis, MI, WPW synd, ↓(K,Mg), ↑Ca,

Anti-anginal drugs

Nitrates→ …………………→ …………………→ Smooth muscle relaxation (v.d)

❖ Nitrates: NTG (GTN), Isosorbide mono/dinitrate, Amyl nitrite, pentaerythritol tetranitrate

✓ Nitroglycerin (s.l) is DOC for ………………… of angina
✓ Amylnitrate by inhalational route (shortest)
Uses: CHF, Angina, MI, Biliary colic pain, Achalasia, Cyanide tox (CAM BAC)
SE: Orthostatic hypotension, Headache, Tolerance

❖ -blockers:
• Used in the long-term prophylaxis of angina and this class of drugs decrease mortality
• C/I in vasospastic/variant angina (DOC -CCB)

✓ Dipyridamole: it ⊖ PDE & adenosine agonist. SE: Coronary steal phenomenon

Anti-arrhythmic drugs

❖ Class I ( Na channel blockers)

❖ Class II ( Beta blockers)

8
❖ Class III (Potassium channel blockers)
❖ Class IV (CCB – Non-dihydropyridines)

Class Ia Drugs: They are useful in V.tach and fibrillation

As they ⊖ K channels risk of Prolonged QT interval ( Torsades )
✓ Procainamide –
✓ Quinidine-
Its derived from Cinchona plant (Cinchonism is the specific side effect)
It also has anti-malarial effects

Class Ib drugs:
✓ Lidocaine – DOC for MI & Digitalis induced Ventricular arrhythmias
✓ Mexilitine, Phenytoin

Class Ic drugs: Flecainide (DOC- Rx of WPW)

Class II drugs: -blockers – DOC for rate control in A.fib & flutter, catecholamine induced
arrhythmia (ex – phaeochromocytoma)

Class III drugs: Bretylium (defibrillator), Sotalol, Ibutilide, Amiodarone

Class III drugs can cause Torsades (Max with Ibutilide, Min with Amiodarone)

✓ Amiodarone:
▪ It has an longest acting antiarrythmic
▪ It also ⊖ Na, β, calcium receptors so it’s the wide-spectrum antiarrythmic (DOC for
Ventricular arrhythmias, rhythm control in A.fib & flutter)
Side effects:
Better: blue skin discoloration
Check: corneal deposits (whorl like)
PFT: pulmonary fibrosis
TFT: thyroid (Hypo>Hyper)

Class IV drugs: Non dihydropyrdines (Verapamil and Diltiazem)

Class V (Miscellaneous) drugs: ADAM

✓ Adenosine: has t1/2 of 5 sec. It’s the DOC for Rx of Acute SVT/PSVT (In Asthma/COPD:
Verapamil is DOC for Acute SVT/PSVT)
SE: Hypotension, Bronchoconstriction
✓ Digoxin
✓ Atropine: DOC for bradycardia and AV block
✓ Magnesium sulphate: DOC for Torsade de pointes and eclampsia in pregnant women

Anti-hyperlipidemics

❖ HMG-CoA reductase ⊖: Atorva/Rosuva/Prava/Pitavastatin

▪ MOA: ⊖ the rate-limiting enzyme for cholesterol synthesis. They also have pleiotropic
effects (Anti-platelet/coagulant, Vasodilatory and Anti-inflammatory)

9
▪ They are DOC for dyslipidemia with raised LDL ( LDL, HDL, TG)
▪ Rosuvastatin is the longest acting, Atorvastatin is safe in renal failure
Side effects: Hepatotoxic, Myalgia, myopathy (max with simvastatin)
▪ C/I in pregnancy and children

❖ Fibric acid derivatives (fibrates): Gemfibrozil, clofibrate, fenofibrate, bezafibrate

▪ Stimulate PPAR-α and  LPL→  TGL
▪  TGL,  LDL,  HDL (DOC for hypertriglyceridemia)
Side effects: Myopathy and also  statin induced myopathy, Cholesterol gallstones

❖ Niacin (nicotinic acid-Vit B3):

▪  LDL, HDL,  TGL
Side effects: PG mediated flushing and pruritis (use NSAIDS)

❖ Bile acid resins(sequestrants): Cholestyramine, colestipol, colesevelam

▪ They ⊖ the enterohepatic circulation of bile acids, decreasing the same in liver →  in bile
acid synthesis from cholesterol in the liver
▪ DOC to  LDL in pregnancy & children ( cholesterol →  LDL receptors →  LDL and  HDL)
Side effects: GI upset, absorption of other drugs and fat-soluble vitamins

ENDOCRINOLOGY

❖ Insulin

• All insulins are given by s.c route except Regular insulin (i.v), Afrezza (inhalational)
• MC side effect is hypoglycaemia & lipodystrophy at the site of injection
Types:
 Ultra-short (mealtime): Glulisine, Aspart, Lispro
 Short: Regular human insulin (DOC for DKA)
 Ultra-long acting (peakless insulins): Glargine, Detemir, Degludec

Anti- hyperglycemic agents

❖ Sulfonylureas (SFU): MOA: increase insulin release by inhibiting ATP sensitive K channels
▪ 2nd gen (more potent): Glyburide (Glibenclamide), Glipizide, Glicazide, Glimipride are more
preferred
MC side effect of these drugs is wt gain & hypoglycemia

❖ Meglitinides: MOA: same as SFU but short acting Ex: Rapaglinide and Nateglinide
▪ They are used for PP-hyperglycemia
SE: Weight gain & hypoglycemia (less risk)

❖GLP-1 analogues: stimulate insulin release, delay gastric emptying inducing satiety and are
given s.c. Ex: Exanatide, Liraglutide, Albiglutide & Dulaglutide
Side effects: Nausea, vomiting, wt loss, pancreatitis

GLP-2 agonist: Teduglutide

10
❖ DPP (Dipeptidyl peptidase) 4 ⊖:
▪ MOA:  GLP-1 activity by inhibiting DPP-4 but is devoid of GLP-1 related side effects Ex:
Sita, Saxa, Alo, Tedi, Vilda, Linagliptin
SE: Pancreatitis, angioedema, Nasopharyngitis
Primarily excreted by Kidney so dose should be decreased in renal failure

❖Biguanide: stimulate AMPK leading to gluconeogenesis inhibition,  insulin resistance

▪ Metformin is DOC for type II DM Rx
SE: At high dose  B12 absorption (Megaloblastic anemia)
▪ C/I in renal failure (GFR<30) as risk of lactic acidosis increases more

❖ Thiazolidinediones
▪ MOA: stimulate PPAR , a nuclear receptor that  GLUT 4 production Ex: Pioglitazone,
Rosiglitazone
▪ They are C/I in CHF, weight gain, Osteoporosis (↑ risk of fractures)
▪ They are metabolized from liver hence they are safe in renal failure

Other drugs safe in RF: GLP-1 agonist (Dula/Albiglutide), DPP-4 ⊖ (Lina/Tedigliptin)

❖ Alpha - glucosidase ⊖Acarbose, Miglitol

▪ MOA: This enzyme metabolises starch & disaccharides into glucose
Side effects: Flatulence and Diarrhea (C/I in IBD)

❖ SGLT-2 ⊖: These receptors present in PCT absorb glucose & Na

Ex:Cana, Dapa, Sotagliflozin
SE: UTI & Vaginal infections, ↑ risk of fractures (canagliflozin), wt loss

❖ Amylin analogue: Pramlintide

▪ MOA:  glucagon release, delays gastric emptying and induces satiety given along with
insulin s.c in both DM type I & II SE: Nausea, Vomitting

Anti – thyroid drugs

❖ Thyroid peroxidase (TPO) ⊖

✓ Carbimazole (prodrug), Methimazole – DOC for hyperthyroidism & Grave’s disease and also
in last two trimesters of pregnancy
▪ It causes esophageal/choanal atresia, cutis aplasia

✓ Propythiouracil: It ⊖TPO & also ⊖ peripheral T4 to T3 conversion by inhibiting

deiodinase
DOC for 1st trimester & thyroid storm (TOC –Beta-blockers + PTU). It is hepatotoxic

❖ Iodides: KI & Lugol’s iodine (5% iodine + 10% KI)

▪ They decrease release also decrease size of the gland. They are used to make patient
euthyroid prior to Sx to  the risk of thyroid storm and to make gland firm

11
❖ Peripheral conversion⊖: Amiodarone, Propranolol, Steroids and PTU

Thyroid hormone replacement

❖Levothyroxine (T4): longer acting drug that is used for Rx of hypothyroidism

❖Liothyronine (T3): short acting

Bone Drugs
❖Bisphoshonates: MOA: apoptosis of osteoclast & inhibit osteoclastic mediated bone
resorption
▪ DOC for Rx of Osteoporosis, Rx of hypercalcemia associated with malignancies, Paget’s
disease
▪ Side effects: Esophagitis, Osteonecrosis of jaw, Hypo/hypercalcemia, increased risk of bone
fractures

❖Teriparatide: MOA: incomplete PTH analog that activates osteoblasts for bone formation
❖Strontium Ranealate: only class of drug that acts both on bone formation & resorption

Drugs of Reproductive system

❖ Selective Estrogen Receptor Modulators (SERM)

▪ Tamoxifen is DOC for breast cancer (premenopausal)
▪ Raloxifene is used in Px & Rx of postmenopausal osteoporosis

❖ Clomiphene citrate: estrogen antagonist at anterior pituitary preventing feedback

▪ Its DOC for Rx of infertility d/t anovulation & oligospermia SE: Multiple gestation

❖ Aromatase ⊖: Anastrozole, Letrozole

▪ DOC for Rx of postmenopausal Breast cancer

❖ Mifepristone:
▪ Mifepristone + Misoprostol is used for abortion. MC side effect is bleeding

❖ Anti-androgens
▪ 5-alpha reductase ⊖: Finasteride, Dutasteride used for Rx of BPH, hirsutism & androgenic
aloplecia

GH & Somatostatin Drugs

❖ GH2 receptor antagonist- Pegvisomant is used in acromegaly

❖Somatostatin analogues: Octreotide, Lanreotide, Paseriotide

▪ Used in Rx of Acute Esophageal Variceal bleeding, Glucagonoma, VIPoma, GFRoma,
Carcinoid tumor, Acromegaly, Insulinoma, Gastrinoma
SE: Nausea, vomiting, hyperglycemia

12
 AUTOCOIDS

Histamine

❖ 1st gen H1 antagonist:

Highly sedative- Diphenhydramine, Doxylamine, Promethazine

❖ 2nd gen H1 antagonist: Cetirizine (derivative of Hydroxyzine), Levocetrizine, Loratadine

(long), Fexofenadine

USES: Urticaria, Pruritus, Insect bites, Allergic rhinitis d/t H1 block.

D/t Muscarinic block: Rx of Parkinsonism (EPS), Acute muscular dystonia, Common cold, Px
of motion sickness
▪ Meniere’s disease(Vertigo): Betahistine (Vertin)-histamine analogue,

Serotonin

❖ 5HT1:

o 5HT1A agonist: decreases anxiety Ex: Bus, Ipsa, Gepirone (Anxiolytics)

o 5HT1B/1D agonist: v.c of cranial vessels Ex: Suma (DOC), Riza(fastest), Frova(longest),
Naratriptan

❖ 5HT3: Na/K ion coupled that causes Nausea and Vomitting

o 5HT3 Antagonists –Ondan (shortest), Palono (longest & most potent)setron

❖ 5HT4: Increase GI peristalsis

o 5HT4 Agonist –Mosapride, Prucalopride used in
SE: QT-prolongation (Tegaserod, Cisapride)

Migrane management

❖ Acute:
 5HT1b/d ⊕: Triptans are C/I in ischemic heart disease, HTN, pregnancy, liver & renal
impairment
 5HT1f ⊕: Lasmiditan. It has lesser risk of coronary vasospasm
 Ergot derivatives (non-selective 5HT): Ergotamine, Dihydroergotamine SE: gangrene of end
arteries especially in limbs, precipitate MI and angina

❖ Prophylaxis:
A: Anti-epileptics (Topiramate, Gabapentin, Valproate), Anti-depressants (Nortriptylline)
B: Beta-blocker- Propranolol (DOC)
Migraine in Preg: PCM (DOC), Sumatriptan

Eicosanoids

13
❖ Prostaglandin E1 analog:
✓ Misoprostol is used as gastroprotective agent, to maintain the patency of ductus arteriosus,
and for medical abortion
✓ Alprostadil is DOC maintain patency of ductus arteriosus

❖ Prostaglandin F2α analog:

✓ Carboprost is used for abortion in 2nd trimester
✓ Latano, Bimato, Travo, Tafluprost is used for glaucoma

NSAID’S

• NSAIDS (anti-inflammatory, analgesic and antipyretic properties) can be classified as

Nonselective (COX1=COX2):
Preferential COX II ⊖: Ace/Diclofenac
Selective COX II ⊖: Etori & Lumira (longest, fastest & most selective), Celecoxib (least
selective, shortest)

Non-selective COX ⊖
❖ Acetaminophen:
It’s used as an antipyretic & analgesic but no anti-inflammatory properties
▪ Extra analgesic effect due to Cannabinoid agonism → ⊕ TRPV1 receptor
▪ It causes hepatotoxicity due to a toxic metabolite NAPQI that causes glutathione depletion
▪ N-acetyl cysteine ⊖ NAPQI and replenishes glutathione

❖ Aspirin:
▪ It’s a salicylate which is non-competitive irreversible ⊖ of COX
▪ The anti-inflammatory effect is seen at high dose (325-625 mg) and the antiaggregant effect
is seen with lower doses (40-325 mg)
▪ No antidote is present so forced alkaline diuresis is done to enhance excretion of the drug

❖ Indomethacin: It’s the DOC for acute gout & used in closure of PDA (DOC: Ibuprofen)

Side effects of NSAIDS: GI effects like nausea and vomiting are mc seen.
They can also cause Peptic ulcer disease. No GI side effects seen with Selective COX II ⊖ but
risk of MI d/t thrombosis

Gout

Acute Gout:

▪ NSAIDS (except aspirin) are the DOC

▪ Colchicine ⊖ the migration of neutrophils to joints by inhibiting tubulin required for their
movement and also decreases inflammatory mediators

Chronic Gout:

❖ Xanthine Oxidase ⊖ - Allopurinol (DOC), Febuxostat

14
 Allopurinol is also used in Lesch-Nyhan syndrome and Tumor lysis syndrome
Side effects- Xanthine stones can form in the urine

❖ Uricosuric drugs: Probenecid

Probenecid increases uric acid excretion so C/I in patients with renal stones Losartan also
has uricosuric effects

❖ Uricase analogs: Rasburicase (DOC), Pegloticase is used Rx of tumor lysis syndrome

Rheumatoid Arthritis

Acute attack: NSAIDS (Aspirin, Ace/diclofenac, Celecoxib) and steroids (Triamcinolone,

Prednisolone)
Chronic: DMARDS
SAARDS

 Methotrexate: It’s the DOC and mostly the treatment is started with MTX later HCQS is
added
 Sulfasalazine an Amino-salicylic acid derivative (also used in UC)
 Hydroxychloroquine SE: Bull’s eye maculopathy
 IL-6⊖: Tocilizumab, Sarilumab

CENTRAL NERVOUS SYSTEM

Anti – epileptic drugs

❖ Phenytoin: MOA:⊖ …………………

➢ Uses: Focal seizures, Digoxin induced VT
➢ It shows both 1st order and zero order kinetics & belongs to class Ib anti-arrythmics
Side effects:
▪ Vit K,D,Folate (B9) (hemorrhagic disease of new born, Osteomalacia, Meg Anemia)
▪ Hypertrophy of gum, Hirsutism, Hyperglycemia (⊖insulin release)
▪ Teratogenic (Fetal-hydantion syndrome) characterized by cleft lip & palate, hypoplastic
phalanges, microcephaly

❖ Carbamazapine: MOA:⊖ Na channel

➢ DOC for Focal seizure/Trigeminal neuralgia
Side effects:
Agranulocytosis so C/I with Clozapine, ADH ↑ (SIADH), Hypersensitivities like SJS

❖ Sodium valproate: Wide spectrum anti-epileptic that ⊖ Na⁺, T-type of Ca⁺ channels,
↑GABA, Glutamate
➢ DOC for GTCS, Myoclonic, Atonic, Absence seizures, Lennox Gastaut & Dravet syndrome
➢ Also used in BPD (Rapid cyclers), Acute mania, Px of migraine
Side effects: V:Vomitting, Nausea (MC), A:Aloplecia/curling L:Liver tox (C/I < 2 years of age),
Pr:Pancreatitis, PCOS, O:Obesity, T:Teratogenic (NTD)

15
 ❖ Lamotrigine: Wide spectrum anti-epileptic that ⊖ Na⁺, Ca⁺ channels and glutamate,
↑GABA
➢ SE: Steven-Johnson Sydrome

❖ Ethosuximide: MOA:⊖ only T type of Ca⁺ channels so used in absence seizures

❖ Topiramate: ⊖Na+/opens K channels, Glutamate receptors (AMPA, Kainate), ⊕ GABA-A

receptors
➢ Other Uses: Craving of alcohol, Obesity
➢ SE: Nephrolithiasis, weight loss

❖ Zonisamide - ⊖ Na+ and Ca+ channels approved only for partial seizures, SE: Nephrolithiasis

❖ Gabapentin & Pregabalin

➢ MOA: exocytosis of GABA, DOC for Post-Herpetic Neuralgia, Diabetic neuropathy &
Restless leg syndrome

❖ Levetiracetam: binds to SV2A, 1st line in GTCS, Focal seizures, JME and is DOC in pregnancy

Status epilepticus & alcohol withdrawal seizures …………………

Febrile seizures Rectal ......................... , Intranasal midazolam

Pregnancy, Eclampsia (MgSo4) Lamotrigine/Levetiracetam (DOC)

GTCS, Absence, Myoclonic, Atonic, LGS, Dravet …………………

Focal/Partial seizures Carbamazepine/Oxcarbamazepine

Infantile spasms/Salaam seizures/West syndrome ACTH

Barbiturates (GABA mimetic) Benzodiazepines (GABA facilitatory)

Enzyme inducers Not enzyme inducer

C/I in Acute intermittent porphyria No C/I

Dont have any specific antidote Flumazenil is the specific antidote

❖ Benzodiazepines
➢ Long acting (C/I in liver failure) – Diazepam, Clonazepam, Flurazepam, Flunitrazepam,
Nitrazepam
➢ Short acting (Safe in liver failure) – Estazolam, Oxazepam, Temezepam, Lorazepam
Uses: Antiepileptic,Hypnosis, Anxiolytic, Muscle relaxation, Anesthetic
▪ Alcohol withdrawal – Chlordiazepoxide (DOC) except seizures- Lorazepam

❖ Barbiturates

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✓ Phenobarbitone –used for Rx of seizures in neonates & Criggler-Najjar syndrome
✓ Thiopentone –redistribution phenomenon, used as i.v anesthetic (for induction)
✓ Methohexitone – used in Electroconvulsive therapy

Insomnia treatment

❖ Z drugs: selective 1 agonist at GABA-A receptor used for hypnosis & sedation
✓ Zaleplon, Eszopiclone
Antidote for Benzodiazepines & Z drugs is Flumazenil

❖ Melatonin agonists (MT1 – sleep, MT2 – circadian rhythm)

✓ Ramelteon – DOC for sleep induction in insomnia & jet lag

❖ Dual Orexin (promotor for wakefulness) receptor antagonist (DORA):

➢ Suvorexant/Daridorexant: DOC for sleep maintanence

Anti-depressants

❖ TCA
(⊖ uptake of NA& 5HT)
➢ Amitryptalline, Nortryptalline – Rx of peripheral neuropathy & also used in smoking
dependence and migraine prophylaxis
➢Imipramine is used in nocturnal enuresis
Side effects: TCAs additionally block α1, H1 and M (HAM)

• TCA toxicity produces cardiac arrhythmias (Rx-Lidocaine) & convulsions (Rx-Diazepam) and
acidosis (Rx- Sodium Bicarbonate)

❖ SNRI (Serotonin NE reuptake ⊖)

➢ Venlafexine
➢ Duloxetine and Milnacipran for Fibromyalgia

❖ Selective Serotonin Reuptake ⊖ (SSRI)

➢ They are first line for mild to moderate depression, OCD, phobias, PTSD, eating disorders
like bulimia nervosa & anorexia nervosa, premenstrual tension syndrome (PTS), panic
attacks, GAD

✓ Fluoxetine is the longest SSRI so preferred in most cases

✓ Fluvoxamine shortest SSRI. Others are Paroxetine, Citalopram, Escitalopram, Sertraline
Side effect:
▪ Delayed ejaculation so SSRI can be used in Rx of premature ejaculation
▪ Nausea vomiting (MC)

❖ Atypical antidepressants
5HT2 ⊖: Trazodone SE: Priapism
NDRI: Bupropion – used in smoking cessation

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 Bipolar Disorder

Mania – Lithium is DOC for Px, Anti-psychotics (DOC in preg), Anti-epileptics like Valproate
(DOC for rapid cyclers in BPD)

❖ Lithium
➢ MOA: ⊖ IMP which IP3 required for BDNF synthesis, also ⊖ GSK-3 pathway (⊖
metabolism)
➢ It acts as mood stabilizer (controls both depression and mania)
Side effects: Leukocytosis, Tremors, Hypothyroidism, Inc urine (Nephrogenic DI), Mother c/I
(Ebstein’s anamoly)
➢ It is a drug with low T.I so regular TDM is required
Therapeutic range: 0.5- 1.2 mEq/L
Toxicity: >1.5 mEq/L Dialysis: >4 mEq/L

Anti-Psychotics [Neuroleptics]

❖ Typical antipsychotics: D2 ⊖
Low potency: Chlorpromazine, Thioridazine (Minimum EPS)
High potency: Fluphenazine, Haloperidol (Max EPS)

Other receptor block (HAM): Thioridazine>Haloperidol

▪ Hyperprolactinemia is seen with potent typicals & Atypical (Risperidone)

EPS (extrapyramidal side-effects) are seen mostly with potent Typicals, Atypicals
 Acute muscular dystonia (<1 week): (Rx –Benzhexol, Benztropine-DOC, Antihistaminics like
Promethazine, Diphenhydramine)
 Drug induced parkinsonism (5d-1month): Rx – central anticholinergic
 Akathasia (MC EPS – 5d-2month): Rx- DOC-Propanolol, BZD
 Tardive dyskinesia: Rx- VMAT2 ⊖ like Valbenazine, Deutetrabenazine
❖ Neuroleptic malignant syndrome –Rx –i.v Dantrolene (DOC), Bromocriptine (D2 agonist) is
also used

❖ Atypical anti-psychotics (5HT-2A⊖ + D2 ⊖):

Ex: Aripiprazole, Clozapine, Risperidone

✓ Aripiprazole is also partial agonist at D2 receptors, 5HT1A receptors

✓ Clozapine is DOC for resistant schizophrenia and side effect is agranulocytosis (dose
independent), convulsions (high dose), strong anti-cholinergic effects like low potency
typicals so sedation (MC-SE), Wet- pillow syndrome

Anti Parkinsons drugs

Dopamine precursor: Levodopa

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➢ Levodopa is always combined with peripheral DD ⊖ (Carbidopa & Benserzide) but
Pyridoxine (B6) is C/I
SE: On-Off phenomenon (Rx: MAO-B⊖, COMT⊖,D2⊕), Vomitting (Rx:Domperidone)

✓ COMT ⊖: Tolcapone, Entacapone

✓ MAO- B ⊖: Rasageline, Safinamide (For On-Off effect)

✓ D2 agonists
❖ Ergot derivates – Cabergoline, Bromocriptine cause side effects like peripheral
vasocontriction that leads to gangrene, fibrosis

❖ Non-Ergot derivatives – Pramipexole, Ropinirole, Rotgotine DOC for Parkinsons (<65 years of
age), used in Restless leg syndrome

✓ Central anti-cholinergic’s: Benztropine, Benzhexol, Bipiridin are DOC for drug induced
parkinsonism

Rx of Alzheimer’s disease
➢ Cholinergic drugs – Donepezil (DOC), Rivastigmine, Galantamine, Tacrine (no longer used as
it is hepatotoxic, Adacanumab, Lecanemab (⊖ β amyloid)

Opioids
➢ The opioid receptors are of 3 subtypes i.e μ, κ, δ acted upon by endogenous opioids called
as endorphins, dysnorphins, enkephalins respectively

➢ μ: Miosis, Urinary retention, Sedation, Constipation, Analgesia, Respiratory depression,

Increased muscle rigidity, Euphoria (Mnemonic: MUSCARInE)

Classification based on receptor interactions:

➢ Full agonists – Morphine, Meperidine (Pethidine), Methadone, Codeine, Tramadol,

Loperamide

➢ Pure antagonist – Naloxone, Naltrexone

❖ Morphine
➢ It’s used by both oral and parenteral routes as an analgesic in labour, cancer patients, MI. Its
also useful in pulmonary edema as it also produces v.d (d/t Histamine release)
➢ S/E: NV (⊕ CTZ), Hypotension, B.C and Pruritis (d/t Histamine), Resp depression,
Constipation
➢ Its C/I in head injuries ( ICT), bronchospastic disorders, Renal failure, Biliary colic pain

✓ Loperamide is DOC for diarrhea associated with IBS

✓ Methadone: Its used to decrease withdrawal symptoms in opioid addicts

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✓ Dextromethorphan/Noscapine/Codein: used as an antitussives

✓ Tramadol/ Tapentadol: analgesic for moderate pain, it also ⊖ reuptake of NA & 5HT

✓ Fentanyl group: Alfentanyl, Fentanyl (100x morphine), Sufentanyl (1000x) are used in
anesthesia SE: Truncal rigidity (Wooden Chest syndrome)

Pure Antagonist
✓ Naloxone is DOC for opioid toxicity as it’s the shortest acting, Naltrexone for maintanence

Smoking dependence
➢ Varenicline (most effective drug) ,Cytisinicline(cytisine), Nicotine inhalers (most effective
form of nicotine replacement) & Bupropion are 1st line drugs
➢ Clonidine & Nortriptyline are 2nd line drugs

Alcohol
➢ Toxicity – DOC is Fomepizole (⊖ alcohol dehydrogenase), Ethanol for Methanol poisoning
➢ Withdrawal – Benzodiazepines are DOC (Diazepam, Lorazepam, Chlordiazepoxide)
➢ Dependance – Disulfiram (aldehyde dehydrogenase ⊖)

HEMATOLOGY

Blood forming drugs

➢ Iron is absorbed in ferrous form from Duodenum, Ferrous Suphate is the oral agent of
choice
➢ Substances which ↑iron absorption are Ascorbic acid (Vit C), Gastric acid (Hcl), Amino acids
➢ Substances which ↓ iron absorption are Tetracycline (Chelating agent), Alkalis → Convert
Fe2 to Fe3
➢ In acute iron poisoning Rx is done by iron chelating agents like Desferroxamine (i.m)
➢ Chronic iron overload and thalassemia → Desferroxamine, Deferiprone (resistant cases)

Growth Factors required for blood formation

1) RBC: Epo is the growth factor. Drugs: EPOIETIN α, EPOIETIN β

2) Platelets: Thrombopoietin & IL 11 are Growth factor for platelets. Drugs: Oprelvekin,
Romiplostim, Eltrombopag

3) WBC: G-CSF & GM-CSF are growth factors. Drugs: Recombinant G-CSF = Leno & Filgrastim,
GMCSF = Mol & Sargramostim

Anti – platelet drugs

 Anti – PLT drugs are used in prophylaxis of TIA, Stroke, MI, Angina, Per Vascular diseases

✓ TXA2 ⊖ →Aspirin (40-325mg)

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 ✓ ADP (P2Y12) ⊖ → Irreversible (Clopidogrel, Prasugrel, Ticlopidine), Reversible (Ticagrelor,
Cangrelor).
Omeprazole (....................................... ) is C/I with Clopidogrel

✓ GP IIb/IIIa ⊖ → Abciximab(safe in renal failure), Eptifibatide, Tirofiban (Strongest anti PLT

drug as they block aggregation induced by all agonists)

✓ Phosphodiesterase ⊖ → Dipyridamole, Cilastazol (used in PVD, Intermittent claudication)

▪ Dipyridamole causes QCoronary steal phenomenon (not used in MI)

 SE: Bleeding is the main side effect with all anti – PLT drugs

Anti-Coagulants
USES: DVT, Pulm embolism, Cancer induced thromboembolism, PCI, A.Fib, Prosthetic Valves
etc

Oral:
❑ Vit K ⊖ , Dicumarol (coumarin)

 Direct oral anti-coagulants (DOAC):

❑ Factor Xa ⊖ – Rivaroxaban Antidote for Xa ⊖: Andexanet alfa
❑ Direct thrombin ⊖– Dabigatran (Antidote:Idarucizumab)

❖ Parenteral:
❑ Direct thrombin ⊖ – Lepirudin, Bivalirudin, Argatroban
❑ Indirect thrombin ⊖ – Heparin, LMWH (Enoxaparin, Dalteparin, Tinzaparin), Fondaparinux
▪ UFH → ⊕ AT3 → ⊖Xa = ⊖IIa
▪ LMWH → ⊕ AT3 → ⊖Xa >⊖IIa
▪ Fondaparinux → ⊕ AT3 → ⊖Xa

Heparin (i.v or subcutaneous) Warfarin (Oral)

⊕ AT3 → ⊖Xa, ⊖Iia ⊖vit K dependent factors (II, VII, IX, X, Prot C, S)

Rapid onset of action Delayed onset (4-5 days)

Monitored by aPTT (~30 sec) PT (~15 sec) or INR (Target:2~3)

Around 5: Stop warfarin and restart at low dose
>10: Stop warfarin, give vit K
Does not cross placenta (DOC in pregnancy) C/I: Fetal Warfarin syndrome – growth retardation,
hypoplastic nose, and hand bones
Side effects: Bleeding, HIT (DOC – Argatroban), Bleeding, dermal vascular necrosis (Purple toe synd)
Osteoporosis, Alopecia, Hyperkalemia

Antidote – Inj Vit K, 4-factor complex, if NA then FFP if NA then

Whole blood

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 Fibrinolytic/Thrombolytic agents
USES: thrombolysis in acute MI, severe pulmonary embolism, DVT, Stroke

1) Streptokinase- It is antigenic, causes allergic reactions, produces neutralizing Abs

2) Recombinant tissue plasminogen activators: Alte, Rete, Dute, Tenecte…………………
▪ They are non – antigenic and preferred fibrinolytics
SE: Bleeding

Anti-fibrinolytics: Epsilon Amino Caproic Acid (EACA) & Tranexemic acid

GENERAL PHARMACOLOGY

❖ ABSORPTION: Movement of drug from site of administration to blood

Lipid Soluble drugs (Non – ionized drug) ....................................... cross the membrane easily
Water soluble drugs (Ionized drug) ...................................... cross the membrane
▪ Whenever the medium is same the drug will cross membranes (Acidic drugs in acidic media,
Basic drugs in basic media)

❖ ELIMINATION: Stoppage of action of drug

1) Metabolism – breaking down
2) Excretion – Removing the drug from the body
▪ Metabolism and excretion is together called as elimination

Most of the drugs are inactivated by metabolism but some may be activated from inactive
drug (pro drugs)
Metabolism – make a drug water soluble
PHASE – 1 reaction: Oxidation(MC)
PHASE – 2 reaction aka conjugation reaction: Glucoronidation (MC)

▪ Aspirin toxicity- acidic drug so makes urine alkaline (basic) by NaHCo3 so all the drug can be
excreted completely
▪ Amphetamine toxicity- basic drug so make the urine acidic by NH4Cl

 Cytochrome 3A4 are responsible for metabolism of most drugs followed by CYP2D6 (Codein

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 to morphine, most CNS & CVS drugs)

Enzyme ⊖: Valproate, INH, Protease ⊖, Cimetidine, Ciprofloxacin, Omeprazole,

Ketoconazole, Erythromycin, Grapefruit juice, Quinidine (VIP COKE & Grapefruit juice)
They cause drug toxicity Ex: Erythromycin causing Theophylline toxicity

Enzyme Inducers: St.Johns wort, Carbamazepine, Cigarrette smoke, Rifampicin, Alcohol

(chronic), Phenytoin, Phenobarbital Griseofulvin (So CRAP)
They cause drug failure

• It takes 4-5 half lives to remove most of the drug out of the body and to achieve Q. steady
state concentration

ORDER OF PHARMACOKINETICS

First order (T ½ constant) ZERO ORDER (T1/2 variable)

Fraction eliminated per unit time is constant Ex: Amount is constant Ex: 500 mg drug removed
500 mg of a drug removed at 50% /hour 500 – 250 at the rate of 50 mg/hour
– 125 – 62.5 – 31.25 –15 – 7.5 500 – 450 – 400 – 350 – 300 – 250 – 200 – 150
Around 95% is cleared in 4-5 half lives

Rate of elimination Plasma Concentration Rate of elimination is constant or independent

of plasma concentration
↑ concentration - ↑ Rate of elimination
Clearance is constant Clearance is inversely proportional to plasma
concentration

Q. Zero order kinetics drugs: W – Warfarin, A- Alcohol / Aspirin, T – Theophylline, T-

Tolbutamide (Anti diabetic),
POWER – Phenytoin
Patients are more prone to have toxicity with zero order drug

PHARMACODYNAMICS

▪ This is what the drug does to the body to produce an effect by binding to a target like
receptor, enzymes, ion channels, transporters

▪ Potency: ability of a drug to bind to the target. Its related to dose of the curve
▪ Efficacy: ability of a drug to produce an effect after binding to the target

In DRC (dose response curve) X axis is potency(dose) and Y axis (height) is efficacy

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 Signal transduction mechanisms

Therapeutic Index, Window

❖ Therapeutic Index:

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▪ It’s a measure of drug safety calculated as Q.T.I = LD50/ ED50 (Mnemonic: TILE)

▪ LD 50: minimum dose required to kill 50 % of population (measure of drug toxicity)

▪ ED50: minimum dose required to produce clinical effect in 50 % population (measure of
drug potency)

▪ For the drugs with Low T.I, therapeutic drug monitoring (TDM) should be done
Q. Ex: LoW: (Lithium, Warfarin), Therapeutic: (Theophylline), Drug: (Digoxin)

Clinical trials for New Drug development:

❖ Phase 0: Microdosing (100 mcg), to determine PK & PD

Size: 1-5
❖ Phase 1: drug tested on normal human volunteers (efficacy can’t be measured as they
aren’t patients). Mainly to test toxicity (max tolerable dose) and pharmacokinetics of the
drug
Size: 10-100

❖ Phase 2: drug tested in small number of patients. This phase is to establish both efficacy and
dose in patients
Size: 100-500

❖ Phase 3: drug tested in large group of patients with different genetic & ethnic backgrounds
to confirm efficacy. If safe application is filed with FDA/CDSCO and if approved the drug is
marketed
Size: 1000-5000

❖ Phase 4: Post marketing surveillance of drug to know rare or long-term use adverse effects
❖ Phase 5: Pharmacoepidemology – to check new indications of drugs and confirm SE found in
Phase 4

Schedule of drugs
✓ Schedule H – only available on prescription by registered medical practitioner
✓ Schedule H1 – antibiotics
✓ Schedule G – given only under medical supervision
✓ Schedule X – Narcotic and Psychotic drugs (NRx) Ex: Morphine, Opioid, Benzodiazepine,
Barbiturates
✓ Schedule Y – NDCTR (New drugs & clinical trial rules)

Pregnancy category
✓ Category A>B>C : safe in pregnancy
✓ Category D: Benefit > teratogenic risk
✓ Category X: Teratogenic risk > Benefit (absolutely contraindicated)
Ex: Warfarin (Contradi syndrome), Misoprostol (Moebius syndrome), Diethylstilbestrol
(Vaginal adenocarcinoma)

✓ Spurious / Counterfeit drug – doesn’t contain active ingredient

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✓ Misbranded drug – low quality drug Ex: PCM 650 contains only PCM 300
✓ Adultered drug – has additional unwanted substances

Correct format of prescription: Complete name of drug, dose, frequency (no abbreviations)
Ex: Tablet azithromycin 500 mg once a day for 5 days

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