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Pharmacology — MBBS Complete Overview

Pharmacology for MBBS is divided into General Pharmacology and Systemic Pharmacology. Here is a structured, high-yield breakdown of the entire subject.

UNIT 1 — General Pharmacology

1. Basic Concepts

TermDefinition
Pharmacokinetics (PK)What the body does to the drug (ADME)
Pharmacodynamics (PD)What the drug does to the body
Bioavailability (F)Fraction of drug reaching systemic circulation unchanged
Volume of Distribution (Vd)Apparent volume in which drug distributes
Half-life (t½)Time for plasma concentration to fall by 50%
Clearance (Cl)Volume of plasma cleared of drug per unit time
Steady stateAchieved after ~5 half-lives

2. Pharmacokinetics (ADME)

Absorption
  • Routes: oral, sublingual, transdermal, IM, IV, inhalation
  • First-pass effect: hepatic metabolism before systemic circulation (e.g., GTN, morphine, propranolol have high first-pass)
  • Factors: lipid solubility, ionization (Henderson-Hasselbalch), surface area, blood flow
Distribution
  • Plasma protein binding (albumin for acidic drugs; α₁-acid glycoprotein for basic drugs)
  • Blood-brain barrier: only lipid-soluble, un-ionized, non-protein-bound drugs cross
  • Vd = Dose / Plasma concentration
    • High Vd → tissue binding (e.g., chloroquine, digoxin)
    • Low Vd → confined to plasma (e.g., heparin, warfarin)
Metabolism
  • Phase I: Oxidation (CYP450), reduction, hydrolysis → may activate or inactivate
  • Phase II: Conjugation (glucuronidation, sulfation, acetylation) → mostly inactivation
  • Enzyme induction: Rifampicin, phenytoin, carbamazepine, barbiturates → reduce drug effect
  • Enzyme inhibition: Ketoconazole, erythromycin, cimetidine, grapefruit juice → increase drug toxicity
Excretion
  • Renal: glomerular filtration + tubular secretion − tubular reabsorption
  • Acidifying urine → traps basic drugs (amphetamine poisoning)
  • Alkalinizing urine → traps acidic drugs (aspirin poisoning)
  • Also: bile (enterohepatic circulation), lungs (volatile agents), milk, sweat

3. Pharmacodynamics

Receptor Types
TypeMechanismExample
Ionotropic (Type I)Ligand-gated ion channelNicotinic ACh, GABA-A
G-protein coupled (Type II)2nd messengerβ-adrenoceptors, M receptors
Enzyme-linked (Type III)Tyrosine kinaseInsulin receptor, growth factors
Intracellular (Type IV)Gene transcriptionSteroids, thyroid hormones
Drug-Receptor Interactions
  • Agonist: Binds + activates receptor
  • Antagonist: Binds but does not activate (competitive/non-competitive)
  • Partial agonist: Submaximal response even at full receptor occupancy (e.g., buprenorphine)
  • Inverse agonist: Reduces basal activity below baseline
  • Efficacy: Maximal effect a drug can produce (Emax)
  • Potency: Dose needed to produce a given effect (EC50) — lower EC50 = more potent
Dose-Response Curve
  • Graded DRC: individual response vs. dose
  • Quantal DRC: population response — used to derive ED50, LD50, Therapeutic Index (TI = LD50/ED50)
  • High TI = safer drug (e.g., penicillin); Low TI = narrow therapeutic index (e.g., digoxin, lithium, warfarin, aminoglycosides, phenytoin)

UNIT 2 — Autonomic Nervous System (ANS) Pharmacology

Neurotransmitters & Receptors

DivisionNTReceptorsEffects
Sympathetic (adrenergic)Norepinephrine, Epinephrineα₁, α₂, β₁, β₂, β₃Fight or flight
Parasympathetic (cholinergic)AcetylcholineM₁, M₂, M₃, Nicotinic (Nm, Nn)Rest & digest

Cholinergic Pharmacology

Cholinomimetics (Direct)
  • Muscarinic: Pilocarpine (glaucoma), Bethanechol (urinary retention), Carbachol
  • Nicotinic: Nicotine (no therapeutic use)
Anti-ChE (Indirect cholinomimetics)
  • Reversible: Neostigmine (myasthenia gravis, reversal of NMB), Physostigmine (glaucoma, atropine poisoning), Pyridostigmine, Edrophonium (diagnosis of MG — Tensilon test)
  • Irreversible: Organophosphates (DDVP, malathion) — inhibit AChE permanently; treat with Atropine + Pralidoxime (2-PAM)
Anticholinergics (Antimuscarinic)
  • Atropine: mydriasis, cycloplegia, antisecretory, tachycardia, antidote for organophosphate poisoning
  • Scopolamine: motion sickness
  • Ipratropium: COPD (inhaled)
  • Tropicamide, Homatropine: ophthalmology
  • Oxybutynin, Tolterodine: overactive bladder (M₃ blockers)
  • Benztropine, Trihexyphenidyl: Parkinson's disease
Ganglion Blockers: Mecamylamine, Trimethaphan (hypertensive emergency, rarely used)
Neuromuscular Blocking Agents (NMBAs)
TypeExamplesReversal
DepolarizingSuccinylcholine (SCh)None (spontaneous)
Non-depolarizingVecuronium, Rocuronium, Atracurium, PancuroniumNeostigmine + Atropine / Sugammadex

Adrenergic Pharmacology

Adrenergic Agonists
DrugReceptorsUses
Adrenaline (Epinephrine)α, βAnaphylaxis, cardiac arrest, with LA
Noradrenalineα₁, α₂, β₁Vasopressor in septic shock
DopamineD₁, β₁ (low dose); α (high dose)Shock, heart failure
Dobutamineβ₁Cardiogenic shock, cardiac stress test
Isoprenalineβ₁, β₂AV block, bradycardia (historical)
Salbutamolβ₂Bronchial asthma (SABA)
Salmeterol/Formoterolβ₂COPD/asthma (LABA)
Clonidineα₂ centralHypertension, opioid withdrawal
Phenylephrineα₁Nasal decongestant, hypotension
Adrenergic Antagonists
Alpha blockers:
  • Non-selective: Phentolamine (pheochromocytoma), Phenoxybenzamine (irreversible)
  • α₁-selective: Prazosin, Tamsulosin (BPH), Doxazosin
Beta blockers:
DrugSelectivitySpecial Feature
PropranololNon-selective (β₁+β₂)Also: migraine, thyrotoxicosis, anxiety
Atenolol, Metoprololβ₁-selective (cardioselective)Preferred in asthma/COPD
Carvedilolα₁ + β (non-selective)HF with reduced EF
Labetalolα₁ + βHypertension in pregnancy
Esmololβ₁-selective, ultra-shortSVT in ICU
TimololNon-selectiveGlaucoma (topical)

UNIT 3 — CNS Pharmacology

Sedative-Hypnotics & Anxiolytics

Benzodiazepines — enhance GABA-A (increase frequency of Cl⁻ channel opening)
  • Short-acting: Triazolam, Midazolam (procedural sedation)
  • Intermediate: Lorazepam, Temazepam
  • Long-acting: Diazepam, Clonazepam, Chlordiazepoxide
  • Antidote: Flumazenil
Barbiturates — enhance GABA-A (increase duration of Cl⁻ channel opening)
  • Thiopentone: IV induction of anesthesia
  • Phenobarbitone: epilepsy
  • Antidote: None specific (supportive care)
Non-BZD Hypnotics (Z-drugs): Zolpidem, Zaleplon, Zopiclone — GABA-A (BZD site)

Antiepileptics

DrugMechanismSeizure Type
PhenytoinNa⁺ channel blockadePartial, GTCS (not absence)
CarbamazepineNa⁺ channel blockadePartial, GTCS, trigeminal neuralgia
ValproateNa⁺ block + GABA ↑ + T-Ca²⁺ blockBroad spectrum, drug of choice in absence
EthosuximideT-type Ca²⁺ channel blockAbsence (petit mal) only
PhenobarbitoneGABA-A enhancerNeonatal seizures, GTCS
BenzodiazepinesGABA-A enhancerStatus epilepticus (IV lorazepam/diazepam)
LamotrigineNa⁺ channel blockPartial, GTCS, bipolar
LevetiracetamSV2A proteinBroad spectrum, well-tolerated
Gabapentin/Pregabalinα₂δ Ca²⁺ channelNeuropathic pain, anxiety

Antidepressants

ClassExamplesMechanism
TCAImipramine, AmitriptylineBlock 5-HT + NE reuptake; anticholinergic, antihistamine
SSRIFluoxetine, Sertraline, EscitalopramSelective serotonin reuptake inhibition
SNRIVenlafaxine, Duloxetine5-HT + NE reuptake inhibition
MAOIPhenelzine, TranylcypromineIrreversible MAO inhibition (tyramine interaction)
Mirtazapineα₂ block + 5-HT₂/₃ blockSedation, appetite ↑
BupropionNE + DA reuptake inhibitionAlso smoking cessation, ADHD

Antipsychotics

Typical (1st generation) — D₂ blockade
  • Low potency: Chlorpromazine (sedation, anticholinergic effects)
  • High potency: Haloperidol, Fluphenazine (more EPS)
  • EPS: Parkinsonism, Akathisia, Acute dystonia, Tardive dyskinesia
  • NMS: Neuroleptic Malignant Syndrome (fever, rigidity, ↑CK) — treat with Dantrolene + Bromocriptine
Atypical (2nd generation) — D₂ + 5-HT₂ block
  • Clozapine: most effective; risk of agranulocytosis (monitor WBC)
  • Olanzapine: weight gain, metabolic syndrome
  • Risperidone: highest prolactin ↑ among atypicals
  • Quetiapine: sedation, used in dementia
  • Aripiprazole: partial D₂ agonist; minimal metabolic effects

Opioid Analgesics

Receptors: μ (analgesia, euphoria, respiratory depression, constipation), κ, δ
DrugTypeNotes
MorphineFull agonistGold standard; release histamine
CodeineProdrug (→ morphine)Mild pain, antitussive
Pethidine (Meperidine)Full agonistAvoid in renal failure (norpethidine); Serotonin syndrome with MAOIs
FentanylFull agonist100× morphine; transdermal patch
BuprenorphinePartial μ agonistOpioid dependence, chronic pain
TramadolWeak μ agonist + SNRISeizure risk
Naloxoneμ antagonistOpioid overdose antidote (IV)
Naltrexoneμ antagonist (oral)Opioid/alcohol dependence

UNIT 4 — Cardiovascular Pharmacology

Antihypertensives

ClassExamplesMechanism
ACE InhibitorsEnalapril, Lisinopril, RamiprilBlock ACE → ↓ Angiotensin II; cough (bradykinin ↑)
ARBsLosartan, Valsartan, TelmisartanBlock AT₁ receptor; no cough
CCBs (Dihydropyridines)Amlodipine, NifedipineL-type Ca²⁺ block (vascular) → vasodilation
CCBs (Non-DHP)Verapamil, DiltiazemCa²⁺ block (cardiac + vascular) → ↓HR, ↓contractility
Beta-blockersAtenolol, Metoprolol↓HR, ↓CO, ↓renin
Thiazide diureticsHydrochlorothiazide, Indapamide↓Na reabsorption in DCT
Aldosterone antagonistsSpironolactone, EplerenoneK⁺-sparing; used in HF, hyperaldosteronism
Direct vasodilatorsHydralazine (arterial), MinoxidilRefractory HTN; hydralazine in pregnancy

Anti-Anginal Drugs

DrugMechanismNotes
GTN (Nitroglycerin)NO → cGMP → vasodilationSublingual; tolerance with continuous use
Isosorbide dinitrate/mononitrateSame as GTNOral; prevent tolerance with nitrate-free intervals
Beta-blockers↓HR, ↓contractility, ↓O₂ demandStable angina; avoid in Prinzmetal's
CCBs (Verapamil/Diltiazem)↓HR + vasodilationStable angina; drug of choice in Prinzmetal's
RanolazineLate Na⁺ current inhibitorChronic stable angina
IvabradineHCN channel block (If)↓HR without affecting contractility

Antiarrhythmics (Vaughan-Williams Classification)

ClassMechanismExamples
IaNa⁺ block (moderate) + K⁺ blockQuinidine, Procainamide, Disopyramide
IbNa⁺ block (weak/fast dissociation)Lidocaine, Mexiletine
IcNa⁺ block (strong)Flecainide, Propafenone
IIBeta-blockersPropranolol, Metoprolol
IIIK⁺ channel block (↑ AP duration)Amiodarone, Sotalol, Ibutilide
IVCa²⁺ channel blockVerapamil, Diltiazem
OtherAdenosineDrug of choice for SVT (IV)
Amiodarone: most effective antiarrhythmic; toxicities — pulmonary fibrosis, thyroid dysfunction, corneal microdeposits, photosensitivity, blue-grey skin.

Heart Failure Drugs

  • ACEi/ARBs: ↓afterload, ↓remodeling — reduce mortality
  • Beta-blockers (Carvedilol, Metoprolol succinate, Bisoprolol): ↓mortality in HFrEF
  • Diuretics: Furosemide (loop) — relieve congestion
  • Spironolactone/Eplerenone: aldosterone antagonism — reduce mortality
  • Digoxin: ↑contractility (Na⁺/K⁺-ATPase inhibitor); narrow TI; toxicity: arrhythmias, nausea, visual disturbances (xanthopsia); antidote: Digibind (anti-digoxin Fab)
  • ARNI (Sacubitril/Valsartan): neprilysin inhibitor + ARB; superior to ACEi in HFrEF
  • SGLT2 inhibitors (Empagliflozin, Dapagliflozin): significant CV mortality reduction in HFrEF

UNIT 5 — Diuretics

ClassSiteExamplesKey Points
Loop diureticsThick ascending loop of HenleFurosemide, BumetanideMost potent; cause hypokalemia, ototoxicity
ThiazidesDCTHCTZ, ChlorthalidoneHypokalemia, hyperuricemia, hyperglycemia
K⁺-sparingCollecting ductSpironolactone (aldosterone antagonist), Amiloride, TriamtereneHyperkalemia risk
Carbonic anhydrase inhibitorsPCTAcetazolamideGlaucoma, altitude sickness, metabolic alkalosis
OsmoticProximal tubule + loopMannitol↑ICP, acute glaucoma, oliguric renal failure

UNIT 6 — Respiratory Pharmacology

Asthma/COPD
  • SABA: Salbutamol (albuterol), Terbutaline — first-line for acute attack
  • LABA: Salmeterol, Formoterol — maintenance (always with ICS in asthma)
  • ICS: Beclomethasone, Budesonide, Fluticasone — reduce airway inflammation
  • LAMA: Tiotropium, Ipratropium — COPD (preferred); muscarinic antagonists
  • Methylxanthines: Theophylline — phosphodiesterase inhibitor; narrow TI (arrhythmias, seizures)
  • Leukotriene antagonists: Montelukast, Zafirlukast — aspirin-sensitive asthma
  • Cromoglicate/Nedocromil: mast cell stabilizers — prophylaxis only
  • Biologics: Omalizumab (anti-IgE), Mepolizumab (anti-IL-5) — severe allergic/eosinophilic asthma
Antitussives: Codeine, Dextromethorphan Expectorants: Guaifenesin, Ambroxol, Bromhexine Mucolytics: Acetylcysteine (NAC — also antidote for paracetamol toxicity)

UNIT 7 — GIT Pharmacology

DrugUseMechanism
PPIs (Omeprazole, Pantoprazole)PUD, GERDIrreversible H⁺/K⁺-ATPase inhibition
H₂-blockers (Ranitidine, Famotidine)PUDH₂ receptor block → ↓acid
Antacids (Mg(OH)₂, Al(OH)₃)Symptomatic reliefNeutralize acid
SucralfatePUD (especially with NSAID)Mucosal protective barrier
MisoprostolNSAID-induced ulcer preventionPGE₁ analogue → ↓acid, ↑mucus
MetoclopramideGERD, vomitingD₂ block + 5-HT₄ agonist (prokinetic)
OndansetronNausea/vomiting (chemotherapy)5-HT₃ antagonist
LoperamideDiarrheaPeripheral opioid receptor agonist
LactuloseConstipation, hepatic encephalopathyOsmotic laxative

UNIT 8 — Antimicrobial Pharmacology

Antibiotics by Mechanism

MechanismDrug ClassExamples
Cell wall synthesis inhibitionPenicillins, Cephalosporins, Carbapenems, VancomycinAmoxicillin, Ceftriaxone, Meropenem
DNA gyrase/Topoisomerase II inhibitionFluoroquinolonesCiprofloxacin, Levofloxacin
RNA polymerase inhibitionRifampicinAnti-TB
30S ribosome inhibitionAminoglycosides, TetracyclinesGentamicin, Doxycycline
50S ribosome inhibitionMacrolides, Chloramphenicol, Clindamycin, LinezolidAzithromycin, Erythromycin
Cell membrane disruptionPolymyxinsColistin
Folate synthesis inhibitionSulfonamides, TrimethoprimCo-trimoxazole

Key Antibiotic Toxicities

DrugToxicity
AminoglycosidesOtotoxicity (irreversible), nephrotoxicity
TetracyclinesTeeth discoloration in children, photosensitivity; avoid in pregnancy
ChloramphenicolGrey baby syndrome, aplastic anemia
FluoroquinolonesTendon rupture (Achilles), QT prolongation, avoid in children
RifampicinOrange-red body secretions, enzyme induction, hepatotoxicity
VancomycinRed man syndrome (infusion-related), nephrotoxicity
LinezolidMAO inhibition → serotonin syndrome; thrombocytopenia
MetronidazoleDisulfiram-like reaction with alcohol

Anti-TB Drugs (RIPE)

DrugMechanismKey Toxicity
RifampicinRNA pol inhibitionHepatotoxicity, enzyme inducer
Isoniazid (INH)InhA inhibition (mycolic acid)Peripheral neuropathy (↓ pyridoxine/B6), hepatitis
PyrazinamideDisrupts membrane potentialHyperuricemia, hepatotoxicity
EthambutolArabinosyltransferase inhibitionOptic neuritis (↓ visual acuity, green-red color)
Streptomycin30S inhibitionOtotoxicity, nephrotoxicity

Antifungals

DrugClassMechanismUse
Amphotericin BPolyeneBinds ergosterol → membrane disruptionSevere systemic fungal infections
FluconazoleAzoleInhibits 14α-demethylase → ↓ergosterolCandida, Cryptococcus
ItraconazoleAzoleBroader spectrum than fluconazoleAspergillus, dermatophytes
TerbinafineAllylamineSqualene epoxidase inhibitorDermatophytes (nail)
CaspofunginEchinocandinβ-1,3-glucan synthase inhibitorInvasive Aspergillus, Candida
GriseofulvinDisrupts microtubulesDermatophytes (oral)

Antivirals

DrugUseMechanism
AcyclovirHSV, VZVThymidine kinase-activated; inhibits viral DNA polymerase
GanciclovirCMVSame mechanism; more toxic
OseltamivirInfluenzaNeuraminidase inhibitor
RibavirinRSV, HCV, viral hemorrhagic feversPurine analogue
Zidovudine (AZT)HIVNRTI (nucleoside reverse transcriptase inhibitor)
TenofovirHIV, HBVNRTI
EfavirenzHIVNNRTI
Lopinavir/RitonavirHIVProtease inhibitor
RaltegravirHIVIntegrase inhibitor
Interferon-αHBV, HCVImmunomodulator + antiviral

UNIT 9 — Endocrine Pharmacology

Diabetes Mellitus

DrugMechanismKey Points
Regular insulinBinds insulin receptorShort-acting; IV use
Glargine/DetemirSlow absorptionBasal insulin (no peak)
Metformin↓hepatic gluconeogenesis (AMPK activation)First-line T2DM; no weight gain; lactic acidosis risk
Sulfonylureas (Glibenclamide)Close K_ATP channel → insulin ↑Hypoglycemia risk
DPP-4 inhibitors (Sitagliptin)↑GLP-1 and GIPWeight neutral; risk of pancreatitis
GLP-1 agonists (Liraglutide)Incretin mimeticWeight loss; CV benefit
SGLT2 inhibitors (Empagliflozin)↓glucose reabsorption in PCTCV and renal protection; genital infections
Thiazolidinediones (Pioglitazone)PPAR-γ activation → insulin sensitizationWeight gain, edema, bladder cancer risk
Acarboseα-glucosidase inhibitorFlatulence

Thyroid Pharmacology

  • Hypothyroidism: Levothyroxine (T4) — synthetic; narrow TI
  • Hyperthyroidism:
    • Carbimazole / Propylthiouracil (PTU): inhibit thyroid peroxidase; PTU also inhibits peripheral T4→T3 conversion; teratogenic (carbimazole — aplasia cutis)
    • Propranolol: symptomatic relief of thyroid storm
    • Radioiodine (¹³¹I): ablative therapy
    • Lugol's iodine (KI): pre-operative (Wolff-Chaikoff effect)

Corticosteroids

  • Glucocorticoids: Hydrocortisone > Prednisolone > Methylprednisolone > Dexamethasone (increasing potency)
  • Mineralocorticoid: Fludrocortisone
  • Side effects: hyperglycemia, hypertension, osteoporosis, Cushing's syndrome, adrenal suppression, peptic ulcer, immunosuppression

UNIT 10 — Chemotherapy (Anticancer Drugs)

ClassExamplesMechanism
Alkylating agentsCyclophosphamide, ChlorambucilCross-link DNA
AntimetabolitesMethotrexate, 5-FU, 6-MPInhibit nucleotide synthesis
Vinca alkaloidsVincristine, VinblastineInhibit microtubule polymerization
TaxanesPaclitaxel, DocetaxelStabilize microtubules
AnthracyclinesDoxorubicin, DaunorubicinIntercalate DNA; free radical generation; cardiotoxicity
Topoisomerase inhibitorsIrinotecan (I), Etoposide (II)Block DNA unwinding
Platinum compoundsCisplatin, CarboplatinCross-link DNA; nephrotoxic
Hormonal agentsTamoxifen (SERM), Letrozole (aromatase inhibitor)Breast cancer
Targeted therapyImatinib (BCR-ABL), Trastuzumab (HER2), Rituximab (CD20)Targeted molecular inhibition

UNIT 11 — Key Antidotes (High-Yield)

Poison/DrugAntidote
OrganophosphatesAtropine + Pralidoxime (2-PAM)
OpioidsNaloxone
BenzodiazepinesFlumazenil
Paracetamol (Acetaminophen)N-Acetylcysteine (NAC)
HeparinProtamine sulfate
WarfarinVitamin K, Fresh Frozen Plasma
DigoxinDigibind (anti-digoxin Fab)
CO poisoning100% O₂, Hyperbaric O₂
CyanideSodium nitrite + Sodium thiosulfate / Hydroxocobalamin
IronDeferoxamine (IM); Deferasirox (oral)
LeadEDTA, BAL (dimercaprol), Penicillamine
Methanol/Ethylene glycolFomepizole (4-MP) or Ethanol + Folate/Pyridoxine
MethemoglobinemiaMethylene blue
TCA overdoseSodium bicarbonate
Beta-blocker overdoseGlucagon, Calcium
CCB overdoseCalcium gluconate, Glucagon, Insulin-dextrose

High-Yield One-Liners for Exams

  • Drug of choice for status epilepticus: IV Lorazepam → IV Phenytoin → General anesthesia
  • Drug causing Lupus-like syndrome: Hydralazine, Procainamide, INH
  • Safest antihypertensive in pregnancy: Methyldopa, Labetalol, Nifedipine (avoid ACEi/ARBs)
  • Drug causing pulmonary fibrosis: Amiodarone, Bleomycin, Busulfan, Methotrexate, Nitrofurantoin
  • Enzyme inducer mnemonic (GRAPCS): Griseofulvin, Rifampicin, Alcohol (chronic), Phenytoin, Carbamazepine, Sulphonylureas
  • Narrow Therapeutic Index drugs: Digoxin, Lithium, Phenytoin, Warfarin, Aminoglycosides, Theophylline (mnemonic: DWPALT)
  • First-line in bipolar disorder: Lithium (monitor: Na⁺, TFT, renal function, levels)
  • Disulfiram-like reaction: Metronidazole, Tinidazole, Cephalosporins (Cefoperazone), Chlorpropamide
  • Drug of choice in Prinzmetal's (Variant) angina: CCBs (Verapamil, Diltiazem, Nifedipine)
  • Drug of choice in SVT (acute): Adenosine IV

This covers the full MBBS pharmacology curriculum. Let me know if you want a deep dive into any specific unit, practice MCQs, or a topic explained with mechanisms and clinical correlations.
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