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pharmacology

Rapid Revision Reignite Pharmacology: Question-Answer Format

Sep 24, 2025

General Pharmacology

Big Question 1: What are the primary objectives of drug metabolism and the principal organ involved, and how does this process facilitate drug excretion?

Broad Answer: Drug metabolism primarily involves converting lipid-soluble/non-ionic compounds into water-soluble, ionic forms. The liver is the most common organ where this transformation occurs, which is crucial as water-soluble forms are then readily excreted from the body, predominantly via the kidneys through urine.

Detailed Questions

Q1.1: What is the main objective of drug metabolism, and which organ is most commonly involved in this process?

Answer:

Converting lipid soluble/non-ionic/non-polar drug into water-soluble/ionic/polar form
Liver is the most common organ of metabolism.

Q1.2: How do water-soluble drug forms facilitate elimination from the body, and what is the most common route of drug excretion?

Answer: Water soluble forms are easily excreted out of the body through saliva/urine/sweat. Most common route of Excretion - Urine by kidneys.

Q1.3 Describe the Activity of drug after metabolism with examples.

Examples of active drug to another active drug

Examples of prodrug to active drug

Fluoxetine → Nor-ﬂuvoxetine

Longest acting antidepressant
Forms another metabolite that acts for a longer duration

Allopurinol → Oxypurinol

Oxypurinol is developed separately for gout
Oxypurinol AKA: Alloxanthine

Diazepam → Oxazepam

Oxazepam is developed separately
Does not go to the liver
Safer than diazepam

Spironolactone → Canrenone
Codeine → Morphine
Primidone → Phenobarbitone

Prednisone → Prednisolone
Levodopa → Dopamine
ACE inhibitors (-pril) → active form ends with -prilat

Enalapril → Enalaprilat
Fosinopril → Fosinoprilat
Trandolapril → Trandolaprilat

Sulfasalazine → in the intestine converts to
Sulfapyridine

→ Treatment of Rheumatoid arthritis

5 ASA (Amino salicylic acid)

→ Treatment of UC (ulcerative colitis)

Mycophenolate mofetil → Mycophenolate

Immunosuppressive drug

Q1.4: Which ACE inhibitors are not prodrugs?

Answer:

Captopril
Lisinopril

Q1.5: Describe hepatic drug metabolism and phase reaction?

Answer: Hepatic (liver) metabolism transforms drugs into more water-soluble forms for excretion, mainly via urine or bile. It occurs in two phases: 2 chemical reactions are carried out

-	Phase 1 reaction	Phase 2 reaction
Activity of the drug	Drugs convert into Active form Inactive form	Converts into inactive form only Except: Morphine, Minoxidil Converted into an active form Enzymes transfer polar groups
Type of reaction	Oxidation CYP-450 enzyme Reducntion CYP-450 enzyme Hydrolysis Hydrolase enzyme: Esters Deamination Adenosine deaminase: Purines (Adenosine) Dehydrogenation Alcohol dehydrogenase: Alcohols Cyclization Proguanil Decyclization	Glucuronide conjugation Uridine Di-phosphate glucuronyl transferase (UDP- GT) Acetylation (add Acetyl group) Acetyltransferase: SHIP drugs Methylation Methyl transferase Glycination Sulfation Glutathionylation Paracetamol
Most common reaction	Most drugs undergo oxidation and reduction	Most drugs undergo Glucuronide conjugation
Site of reaction	Smooth Endoplasmic Reticulum (SER) Also known as Microsomes Microsomal reactions	Outside SER Non-microsomal reactions Except: Glucuronide conjugation Microsomal reactions

Q1.6: What are the key characteristics of Cytochrome P450 enzymes?

Answer:

Contains heme pigment
Shows genetic variation/polymorphism in high/low amount

Q1.7: What are CYP enzyme inducers and inhibitors?

Answer:

Category	Mnemonic	Drugs
CYP Enzyme Inducers	GRASS	Griseofulvin Rifampicin Alcohol (chronic) All antiepileptics (except valproate): Phenobarbitone Phenytoin Carbamazepine Smoking St John's Wort (plant product)
CYP Enzyme Inhibitors	COKE IVC GAR	Cimetidine Omeprazole Ketoconazole Erythromycin Isoniazid : Inhibits all CYP types, Except CYP2E1 which it induces Valproate Ciprofloxacin Grape-fruit juice Alcohol (acute) Ritonavir (HIV)

Q1.8: Describe the Types of CYP and their substrates.

Answer:

CYP type	Substrate (drugs metabolized by CYP)
CYP1A2	Theophylline, Clozapine
CYP2C9 (earlier known as CYP2C8) Least quantity Dye to genetic polymorphism	Phenytoin, Warfarin Saturation kinetics is seen
CYP2C19	Clopidogrel (Antiplatelet drugs) Azoles (Antifungal drugs) Voriconazole Ketoconazole PPIs (Proton Pump Inhibitors) Omeprazole Pantoprazole
CYP2D6	[3-blockers (Propranolol) Antiarrhythmics (Quinidine) Tamoxifen TCA (Tricyclic Antidepressant) SSRIs (Antidepressants) Opioids (Codeine) Neuroleptics (Antipsychotics) All are metabolized except, Clozapine which is metabolized by diﬀerent CYP
CYP2E1	Paracetamol
CYP3A4 (maximum quantity in our body) Responsible for metabolism of >50% drugs	Most drugs are metabolized Astemizole Antihistaminic drug Benzodiazepine (Midazolam) Cyclosporine/ Tacrolimus Immunosuppressive drugs

Central Nervous System

Big Question 2: What are Atypical Benzodiazepines?

Broad Answer:

Atypical benzodiazepines are drugs that act on benzodiazepine receptors (BZ1/BZ2 on GABA-A) but are structurally different from classical benzodiazepines.
AKA Z drugs

Detailed Questions

Q2.1: What is the difference between normal and atypical Benzodiazepines?

Answer:

Normal Benzodiazepines	Atypical benzodiazepine
Act on alpha and gamma subunits of GABA A receptors Alpha (a) 1: Produce sedation, used to treat insomnia Alpha (a) 2: Muscle relaxant, used to treat seizures	Act on alpha (a) 1 gamma (g) subunit Produce sedation-Treat insomnia Lack of muscle relaxant effect and anti-seizure activity

Q2.2: What are the drugs included under atypical Benzodiazepines?

Answer:

Zopiclone: Longest acting
Zolpidem
Zaleplon: Shortest acting
- Less sleep cycle distortion

Q2.3: What is the main use of atypical benzodiazepines?

Answer:

Atypical Benzodiazepines are DOC in the treatment of Insomnia
- Chronic insomnia
- Transient insomnia
- Sleep onset insomnia

Q2.4: What is the DOC in treating Jet lag?

Answer: Ramelton is DOC in treating Jet lag, but atypical Benzodiazepines are also used. (off label use)

Q2.5: What are the side effects of atypical Benzodiazepines and what is the antidote used in its poisoning?

Answer:

Side effect: Highly addictive
Poisoning: Flumazenil (Antidote)
- Blocks alpha-gamma junction

Q2.6: What are the adverse effects of Barbiturates?

Answer:

Barbiturates distort the sleep cycle (Not used in insomnia)
Nightmare/night tremors
Hangover

Big Question 3: What are the properties, mechanisms, uses and adverse effects of anti-epileptic drugs?

Broad Answer: Anti-epileptic drugs (AEDs) are a diverse group of drugs used to prevent or control seizures in patients with epilepsy or other seizure-related conditions. They act by inhibiting depolarization of neurons.

Detailed Questions

Q3.1: What are the first-line drugs used in the treatment of various types of epilepsy?

Answer:

GTCS (Grand mal epilepsy)	V/L
Absence (Petit mal epilepsy) EEG: 3Hz wave spike pattern	E/V/L
Atypical absence Myoclonic Atonic Tonic seizures	V/L/T
Focal seizures	LOCPL

V: Valproate
L: Lamotrigine
E: Ethosuximide
T: Topiramate
O: Oxcarbazepine/Eslicarbazepine
C: Carbamazepine
P: Phenytoin
L: Levetiracetam

Autacoids

Big Question 4: What are the roles, preparations, and clinical uses of prostaglandins?

Broad Answer: Autacoids are local hormones that produce local effects and include prostaglandins, leukotrienes, and other locally acting agents. Prostaglandins are a major class of autacoids that mediate inflammation, smooth muscle tone, and reproductive functions. Their synthetic analogs are clinically used in abortions, ductus arteriosus management, glaucoma, peptic ulcers, and pulmonary hypertension. The section also covers uterine stimulants and relaxants (tocolytics), along with prostaglandin synthesis pathways and medical abortion protocols. Understanding their mechanisms and applications is essential for therapeutic decision-making.

Detailed Questions

Q4.1: What are autacoids, and what kind of effects do they produce?

Answer: Autocoids are local hormones that produce local effects.

Q4.2: What are the synthetic preparations of prostaglandins and their clinical uses?

Answer:

Prostaglandins	Synthetic Preparation
PGE1	Misoprostol DOC for MTP/Abortions in 1st trimester (63 days) NSAIDs-induced peptic ulcer (DOC: PPIs) S/E of Misoprostol: Diarrhoea (Chloride Secretion) Teratogenic: Moebius syndrome (6th Cranial nerve damage )
-	Alprostadil DOC to open Ductus arteriosus
-	Lubiprostone (chloride secretors have a laxative property) Treat constipation in inflammatory bowel syndrome.
PGE2	Dinoprostone nd DOC for cervical ripening, MTP in the 2nd trimester
PGF2 Alpha	Dinoprost DOC for MTP in the 2nd trimester
-	Carboprost Control PPH resistant to oxytocin MTP in 2 trimester Contraindicated in Asthma Dose: 250microgram injection Maximum dose: 2000mg or 8 injections/day
-	DOC for glaucoma (POAG, ACG) Latanoprost Bimatoprost Travoprost Tafluprost
PGI2 (Prostacyclin) Vasodilation Antiplatelet effect	DOC for PAH Treprostinil Iloprost Epoprostenol

Q4.3: What are the effects of prostaglandins on the uterus?

Answer:

Uterine Stimulant	Uterine Relaxant (Tocolytics)
Oxytocin DOC: Induction and augment labour DOC: controls PPH Carbetocin: Longer-acting alternative of oxytocin. To control PPH in oxytocin resistance cases Contraindicated the induction of the labour as it can lead to fetal hypoxia ● Carboprost (PGF-2 alpha drugs) ● Ergometrine ● Methyl ergometrine	Used in premature labour Atosiban: Blocks oxytocin receptor -Safe for heart disease patients. Beta (b)-2 agonists: Ritodrine, isoxsuprine CCB: Nifedipine GA with maximum tocolytic effect: Halothane Avoid NSAIDS during labour pain: Due to tocolytic effects as it days child delivery

Endocrine System

Big Question 5: What are the additional drugs used in Diabetes Mellitus beyond traditional hypoglycemics, their mechanisms, and the pharmacological management of diabetic complications?

Broad Answer: Several non-traditional drugs and specific therapies are used in diabetes mellitus to target complications or complement glycemic control:

Colesevelam
Bromocriptine
Epalrestat
Imeglimin

Detailed Questions

Q5.1. What are the additional oral drugs used in diabetes and their mechanisms?

Answer:

Drug	Class/Mechanism	Notes
Colesevelam	Bile acid-binding resin → ↓ glucose absorption from GIT	Also used for hyperlipidemia
Bromocriptine	Dopamine D2 receptor agonist (hypothalamic-pituitary axis)	Taken early morning (< 3 hrs of waking)
Epalrestat	Aldose reductase inhibitor → ↓ conversion of glucose to sorbitol	Used in diabetic neuropathy
Imeglimin	Inhibits hepatic gluconeogenesis	Newer agent

Q5.2. What are the drug treatments for specific diabetic complications?

Answer:

Diabetic Complication	Treatment Drug	Mechanism / Use
Gastroparesis	Erythromycin	Stimulates motilin receptors in the stomach
Diabetic diarrhea	Clonidine	Stimulates α2a receptors in intestine
Diabetic retinopathy	Anti-VEGF agents: Bevacizumab, Ranibizumab, Aflibercept, Pegaptanib	Inhibit neovascularization via intravitreal injection
Diabetic neuropathy	Pregabalin	DOC for neuropathic pain
Anti-obesity in DM	Liraglutide, Semaglutide, Tirzepatide	GLP-1 analogues or dual agonists (GLP-1 + GIP)

Q5.3. Which antidiabetic drugs are associated with an increased risk of fractures?

Answer:

Canagliflozin
Dapagliflozin
Pioglitazone

Q5.4. Which drugs used in diabetes mellitus are known to cause hypoglycaemia?

Answer:

Insulin
Sulfonylureas
Meglitinides

Q5.5. Which antidiabetic drug is associated with megaloblastic anaemia and lactic acidosis?

Answer:

Metformin
- Causes ↓ Vitamin B12 absorption → Megaloblastic anemia
- Risk of lactic acidosis, especially in renal failure

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