---

ANTITUBERCULOSIS DRUGS

First-Line Drugs (HRZE S)

Drug-Specific Points

• Mechanism: Inhibits mycolic acid biosynthesis → mycobacterial cell wall disruption
• Pharmacokinetics: Well absorbed; distributed to CSF, crosses placental barrier; metabolized by acetylation
• Uses: First-line TB; chemoprophylaxis
• Adverse effects: Hepatotoxicity (risk ↑ in chronic alcoholics, elderly, rapid acetylators); Peripheral neuritis (due to pyridoxine competition — give pyridoxine to prevent); fever, skin rashes, anaemia

• Mechanism: Binds bacterial DNA-dependent RNA polymerase → inhibits RNA synthesis
• Kills both intracellular and extracellular bacilli including spurters
• Food reduces absorption; metabolized in liver
• Uses: TB, Leprosy, Meningococcal prophylaxis, Brucellosis (with doxycycline), Staphylococcal infections (with β-lactams)
• Adverse effects: Hepatitis (main AE), Flu-like syndrome, GI disturbances, Skin rashes/flushing

• Active only in acidic pH → effective against intracellular bacilli
• Mechanism: Inhibits mycobacterial mycolic acid biosynthesis (different pathway from INH)
• Adverse effects: Dose-dependent hepatotoxicity (main AE), hyperuricemia, anorexia, nausea

• Bacteriostatic drug
• Used in combination to prevent emergence of resistance
• Main adverse effect: Optic neuritis (decreased visual acuity, colour vision defect — red-green)
• Crosses BBB in meningitis

• Not effective orally → must be given IM
• Active against extracellular bacilli in alkaline pH
• Adverse effects: Ototoxicity, nephrotoxicity, neuromuscular blockade

---

TB Treatment (WHO/RNTCP 2016)

1. Make patient non-infectious as early as possible
2. Prevent drug-resistant bacilli development
3. Prevent relapse
4. Reduce total duration of therapy

• Monoresistance — resistant to only one first-line drug
• Polydrug resistance — resistant to >1 first-line drug, but NOT both INH and Rifampin
• MDR-TB — resistant to both INH and Rifampin ± other first-line drugs
• XDR-TB — MDR + resistant to a fluoroquinolone + a second-line injectable (amikacin/kanamycin/capreomycin)

• Intensive phase (6–9 months): Kanamycin + Levofloxacin + Ethionamide + Cycloserine + Pyrazinamide + Ethambutol + Pyridoxine 100 mg/day
• Continuation phase (18 months): Levofloxacin + Ethionamide + Ethambutol + Cycloserine + Pyridoxine

• INH 300 mg/day (10 mg/kg in children) for 6 months
• Indications: Newborns of mothers with active TB; children <6 years with positive tuberculin test; household contacts; HIV patients with positive tuberculin test

---

ANTILEPROTIC DRUGS

• Oldest, cheapest, most widely used antileprotic
• Mechanism: Structurally similar to PABA → competitively inhibits folate synthetase → prevents THFA synthesis → leprostatic effect
• Pharmacokinetics: Oral; widely distributed; concentrated in infected skin, muscle, liver, kidney; metabolized by acetylation
• Adverse effects: Dose-related haemolytic anaemia (especially in G6PD deficiency); methaemoglobinaemia; anorexia, nausea, vomiting, peripheral neuropathy

Leprosy Treatment Schedules (WHO MDT)

---

ANTIMALARIAL DRUGS

Classification by Stage of Action

1. No agent is effective against sporozoites
2. Most antimalarials act on asexual blood stages except primaquine
3. Only primaquine and tafenoquine are effective against hypnozoites (latent tissue forms)
4. All agents with "quine" (primaquine, chloroquine, quinine) are effective against gametocytes except mefloquine and tafenoquine

---

• 4-aminoquinoline; drug of choice for acute malaria (P. vivax, P. ovale, P. malariae, chloroquine-sensitive P. falciparum)
• Mechanism: Basic drug → taken up by acidic food vacuoles → inhibits heme polymerase → toxic heme accumulates → parasite membrane lysis → death
• Resistance common with P. falciparum
• Safe in pregnancy
• Other uses: Amoebiasis, Rheumatoid arthritis, Discoid lupus erythematosus
• Adverse effects: Nausea, vomiting, headache, visual disturbances; prolonged use → irreversible retinopathy; parenteral → cardiac arrhythmias, cardiac arrest

---

Malaria Treatment Regimens (Summary)

• Chloroquine 600 mg → 600 mg (day 2) → 300 mg (day 3)
• • Primaquine 15 mg/day × 14 days (for radical cure in P. vivax/P. ovale)

• Artesunate 100 mg BD × 3 days + Sulphadoxine/Pyrimethamine (single dose, day 1) — India standard
• OR Artemether + Lumefantrine × 3 days (north-eastern states)
• • Primaquine 0.75 mg/kg single dose on Day 2 (gametocidal)

• Artesunate IV/IM: 2.4 mg/kg at 0h, 12h, 24h → then daily until oral ACT tolerated

📝 PHARMACOLOGY EXAM NOTES

Antituberculosis | Antileprotic | Antimalarial Drugs

---

PART 1: ANTITUBERCULOSIS DRUGS

---

🔷 First-Line Drugs — Remember: "HRZES"

Hisoniazid · Rifampin · Pyrazinamide · Ethambutol · Streptomycin

---

1️⃣ ISONIAZID (INH)

• Kills TB bacteria by stopping mycolic acid production (mycolic acid builds the bacterial cell wall)
• It's a prodrug → gets converted to active form inside the bacteria

• Absorbed easily from gut
• Goes everywhere — CSF, placenta, tubercular cavities
• Broken down by acetylation in liver → excreted in urine

• ✅ First-line TB treatment
• ✅ TB chemoprophylaxis (prevention)

---

2️⃣ RIFAMPIN (Rifampicin)

• Blocks DNA → RNA step (inhibits RNA polymerase)
• Kills both inside-cell and outside-cell bacteria
• Broad spectrum — also works on meningitis, staph, brucella

• Take on empty stomach (food reduces absorption)
• Metabolized in liver
• ⚠️ Turns urine/sweat/tears orange-red (harmless but warn patient)

• ✅ TB (with INH and others)
• ✅ Leprosy
• ✅ Meningococcal prophylaxis
• ✅ Brucellosis (with doxycycline)
• ✅ Staph infections (with β-lactams)

---

3️⃣ PYRAZINAMIDE (PZA)

• Works only in acidic pH (inside cells/caseous lesions)
• Has sterilizing activity — kills remaining hidden bacteria
• Inhibits mycolic acid (different pathway than INH)

• Main: Dose-dependent hepatotoxicity
• Others: Hyperuricemia (gout), anorexia, nausea, fever

---

4️⃣ ETHAMBUTOL

• Bacteriostatic (slows growth, doesn't kill)
• Inhibits arabinosyl transferase → stops cell wall building
• Used in combo to prevent resistance

⚠️ Optic Neuritis — blurred vision + can't see red/green colours → Check eye regularly; stop drug if vision changes

---

5️⃣ STREPTOMYCIN

• Aminoglycoside antibiotic
• Kills bacteria outside cells, in alkaline pH
• Cannot be given orally → must be injected (IM)

• Ototoxicity (hearing damage)
• Nephrotoxicity (kidney damage)
• Neuromuscular blockade

---

🔶 TB TREATMENT REGIMENS (WHO/RNTCP 2016)

4 Goals of TB Treatment (MDT):

1. Make patient non-infectious ASAP
2. Prevent drug resistance
3. Prevent relapse
4. Shorten treatment duration

Treatment Chart:

---

🔴 Drug Resistance Types — Easy to Remember:

MDR-TB Treatment:

• Intensive (6–9 months): Kanamycin + Levofloxacin + Ethionamide + Cycloserine + PZA + Ethambutol + Pyridoxine 100 mg
• Continuation (18 months): Levofloxacin + Ethionamide + Ethambutol + Cycloserine

---

💉 CHEMOPROPHYLAXIS OF TB

• Drug: INH 300 mg/day for 6 months
• Given to:
  1. Newborns of mothers with active TB
  2. Children <6 years with positive tuberculin test
  3. Household contacts of TB patients
  4. HIV patients + positive tuberculin test

---

---

PART 2: ANTILEPROTIC DRUGS

---

Leprosy Basics:

• Caused by Mycobacterium leprae (acid-fast bacillus)
• Chronic infectious disease

---

1️⃣ DAPSONE (Most Important!)

• Looks like PABA → blocks folate synthetase → bacteria can't make folic acid → dies
• Same mechanism as sulphonamides

• Given orally; absorbed well
• Goes to infected skin, muscle, liver, kidney
• Metabolized by acetylation

---

2️⃣ OTHER DRUGS:

• Clofazimine — Phenazine derivative; also anti-inflammatory
• Rifampin — Used in both TB and leprosy
• Ofloxacin, Minocycline, Clarithromycin — Alternative drugs

---

💊 LEPROSY TREATMENT SCHEDULES (WHO MDT)

All drugs are given orally

💡 MBL = More Bacilli → More drugs, More months 💡 PBL = Pauci Bacilli → Less drugs, Less months

---

---

PART 3: ANTIMALARIAL DRUGS

---

Malaria Basics:

• Caused by Plasmodium species
• Transmitted by female Anopheles mosquito
• Species: P. vivax, P. ovale, P. malariae, P. falciparum (most dangerous), P. knowlesi

---

🔶 Classification by Stage They Kill:

⭐ Must-Remember Points:

1. ❌ No drug works against sporozoites
2. Only Primaquine + Tafenoquine kill hypnozoites (prevent relapse in P. vivax/ovale)
3. Drugs with "quine" in name = effective against gametocytes
4. Most drugs work on asexual blood stages except primaquine

---

1️⃣ CHLOROQUINE

• Drug of choice for uncomplicated malaria (P. vivax, P. ovale, P. malariae)
• Mechanism: Goes into parasite's acidic vacuole → blocks heme polymerase → toxic heme builds up → parasite dies
• ⚠️ Resistance common in P. falciparum

• Given orally; well absorbed
• Concentrates in liver, spleen, kidney, lungs, skin
• High affinity for melanin-containing tissues

• ✅ Malaria (drug of choice)
• ✅ Amoebiasis
• ✅ Rheumatoid arthritis
• ✅ Discoid lupus erythematosus
• ✅ Safe in pregnancy

---

🔶 MALARIA TREATMENT REGIMENS (Quick Summary)

Uncomplicated Malaria:

• Chloroquine: 600 mg → 600 mg (day 2) → 300 mg (day 3)
• + Primaquine 15 mg × 14 days (for radical cure — kills liver hypnozoites)

• Option 1: Artesunate 100 mg BD × 3 days + Sulphadoxine/Pyrimethamine (day 1 single dose)
• Option 2: Artemether + Lumefantrine × 3 days (with fatty meal)
• + Primaquine 0.75 mg/kg single dose day 2 (kills gametocytes)

Severe / Cerebral Malaria:

• Artesunate IV/IM: 2.4 mg/kg at 0h → 12h → 24h → then once daily
• Switch to oral ACT once patient can swallow

---

⚡ QUICK REVISION TABLE — All Drugs at a Glance

---

💡 Exam Tips:

• INH peripheral neuritis → always give Pyridoxine (Vit B6)
• Ethambutol → always think eye/optic neuritis
• Streptomycin → never oral, always IM
• Chloroquine → safe in pregnancy, avoid in epilepsy
• Only Primaquine prevents relapse in P. vivax (kills hypnozoites)
• MDR-TB = resistant to H + R (most important drugs)

📝 MCQ PRACTICE SET

Antituberculosis | Antileprotic | Antimalarial Drugs

---

🔷 SECTION A: ANTITUBERCULOSIS DRUGS

(30 Questions)

---

• A) Peptidoglycan
• B) Mycolic acid ✅
• C) RNA polymerase
• D) Folic acid

Explanation: INH inhibits mycolic acid biosynthesis, which is an essential component of the mycobacterial cell wall.

---

• A) Active drug
• B) Prodrug ✅
• C) Slow-release drug
• D) Bacteriostatic drug

Explanation: INH is a prodrug — it is converted to its active form inside mycobacteria.

---

• A) Glucuronidation
• B) Hydroxylation
• C) Acetylation ✅
• D) Sulfation

Explanation: INH is metabolized by acetylation in the liver. Rate of acetylation determines toxicity risk.

---

• A) Vitamin B12
• B) Vitamin C
• C) Pyridoxine (Vitamin B6) ✅
• D) Folic acid

Explanation: INH competitively interferes with pyridoxine utilization → Peripheral neuritis. Pyridoxine supplementation prevents this.

---

• A) Young children
• B) Slow acetylators
• C) Rapid acetylators ✅
• D) Women

Explanation: Risk of hepatotoxicity is more in chronic alcoholics, elderly patients, and rapid acetylators.

---

• A) Inhibits mycolic acid synthesis
• B) Inhibits DNA-dependent RNA polymerase ✅
• C) Inhibits protein synthesis
• D) Inhibits cell wall peptidoglycan

Explanation: Rifampin binds to bacterial DNA-dependent RNA polymerase and inhibits RNA synthesis.

---

• A) Empty stomach
• B) Antacids
• C) Food ✅
• D) Milk

Explanation: Presence of food reduces absorption of Rifampin — should be taken on empty stomach.

---

• A) Tuberculosis
• B) Leprosy
• C) Brucellosis
• D) Typhoid ✅

Explanation: Rifampin is used in TB, Leprosy, Brucellosis (with doxycycline), and meningococcal prophylaxis — NOT typhoid.

---

• A) Optic neuritis
• B) Peripheral neuropathy
• C) Hepatitis ✅
• D) Ototoxicity

Explanation: Hepatitis (hepatotoxicity) is the main adverse effect of Rifampin.

---

• A) Stop the drug immediately
• B) It is a serious side effect
• C) It is harmless and expected ✅
• D) Reduce the dose

Explanation: Rifampin causes orange-red discoloration of urine, sweat, and tears — this is harmless and expected.

---

• A) Alkaline pH
• B) Neutral pH
• C) Acidic pH ✅
• D) All of the above

Explanation: Pyrazinamide is active only in acidic pH — this makes it effective against intracellular bacilli inside macrophages.

---

• A) Optic neuritis
• B) Hepatotoxicity ✅
• C) Ototoxicity
• D) Peripheral neuritis

Explanation: Pyrazinamide causes dose-dependent hepatotoxicity as its main adverse effect.

---

• A) Increases uric acid production
• B) Decreases renal excretion of uric acid ✅
• C) Blocks xanthine oxidase
• D) Increases purine synthesis

Explanation: Pyrazinamide inhibits renal tubular secretion of uric acid → Hyperuricemia → can precipitate gout.

---

• A) Inhibits RNA polymerase
• B) Inhibits mycolic acid synthesis
• C) Inhibits arabinosyl transferase ✅
• D) Inhibits folic acid synthesis

Explanation: Ethambutol inhibits arabinosyl transferases involved in mycobacterial cell wall arabinogalactan synthesis.

---

• A) Hepatotoxicity
• B) Nephrotoxicity
• C) Optic neuritis ✅
• D) Peripheral neuritis

Explanation: Optic neuritis is the main and characteristic adverse effect of Ethambutol — decreased visual acuity and red-green colour vision defect.

---

• A) Bactericidal
• B) Bacteriostatic ✅
• C) Both
• D) Neither

Explanation: Ethambutol is a bacteriostatic drug — it is used in combination to prevent resistance.

---

• A) Macrolides
• B) Tetracyclines
• C) Aminoglycosides ✅
• D) Fluoroquinolones

Explanation: Streptomycin is an aminoglycoside antibiotic used as a first-line antitubercular drug.

---

• A) It causes GI irritation
• B) It is not absorbed from the gut ✅
• C) It is destroyed by stomach acid
• D) It has poor solubility

Explanation: Streptomycin is not absorbed orally — must be given intramuscularly (IM).

---

• A) Intracellular bacilli in acidic pH
• B) Extracellular bacilli in alkaline pH ✅
• C) Both intracellular and extracellular
• D) Latent bacilli in liver

Explanation: Streptomycin kills extracellular bacilli and works best in alkaline pH.

---

• A) Ototoxicity
• B) Nephrotoxicity
• C) Neuromuscular blockade
• D) Optic neuritis ✅

Explanation: Optic neuritis is associated with Ethambutol, NOT Streptomycin. Streptomycin causes ototoxicity, nephrotoxicity, and neuromuscular blockade.

---

• A) 2 HRZ + 4 HR
• B) 2 HRZE + 4 HRE ✅
• C) 2 HRZES + 5 HRE
• D) 3 HRZE + 3 HRE

Explanation: New patients: 2 months HRZE (intensive) + 4 months HRE (continuation).

---

• A) Any two first-line drugs
• B) Isoniazid alone
• C) Both Isoniazid AND Rifampin ✅
• D) Rifampin alone

Explanation: MDR-TB = resistant to both INH and Rifampin with or without resistance to other first-line drugs.

---

• A) Pyrazinamide + Ethambutol
• B) Fluoroquinolone + second-line injectable ✅
• C) Streptomycin + Ethambutol
• D) All first-line drugs

Explanation: XDR = MDR + resistant to a fluoroquinolone AND a second-line injectable (amikacin/kanamycin/capreomycin).

---

• A) Rifampin
• B) Pyrazinamide
• C) Isoniazid ✅
• D) Ethambutol

Explanation: INH 300 mg/day (10 mg/kg in children) for 6 months is used for TB chemoprophylaxis.

---

• A) Newborn of mother with active TB
• B) Children <6 years with positive tuberculin test
• C) Healthy adults with no TB contact ✅
• D) Household contacts of TB patients

Explanation: Chemoprophylaxis is for high-risk groups — not for healthy adults with no exposure or risk factors.

---

• A) Hepatotoxicity
• B) Peripheral neuritis ✅
• C) Optic neuritis
• D) Ototoxicity

---

• A) Streptomycin
• B) Ethambutol ✅
• C) Rifampin
• D) Pyrazinamide

Explanation: Ethambutol crosses the BBB during meningitis (inflamed meninges increase permeability).

---

• A) Rifampin
• B) BCG alone
• C) Isoniazid ✅
• D) Pyrazinamide

---

• A) 3 months
• B) 6 months ✅
• C) 9 months
• D) 12 months

---

• A) Rifampin is safe to take with food
• B) Streptomycin can be given orally
• C) Ethambutol is bactericidal
• D) Pyrazinamide works best in acidic pH ✅

---

---

🟢 SECTION B: ANTILEPROTIC DRUGS

(15 Questions)

---

• A) Mycobacterium tuberculosis
• B) Mycobacterium leprae ✅
• C) Mycobacterium avium
• D) Mycobacterium bovis

---

• A) Macrolide
• B) Sulphone ✅
• C) Fluoroquinolone
• D) Aminoglycoside

---

• A) Inhibits RNA polymerase
• B) Inhibits mycolic acid synthesis
• C) Competitively inhibits folate synthetase ✅
• D) Inhibits arabinosyl transferase

Explanation: Dapsone is structurally similar to PABA → competitively inhibits folate synthetase → prevents THFA synthesis.

---

• A) Hepatotoxicity
• B) Haemolytic anaemia ✅
• C) Optic neuritis
• D) Ototoxicity

Explanation: Dose-related haemolytic anaemia is the most common adverse effect, especially in G6PD-deficient patients.

---

• A) Diabetes mellitus
• B) Hypertension
• C) G6PD deficiency ✅
• D) Renal failure

---

• A) Hydroxylation
• B) Glucuronidation
• C) Acetylation ✅
• D) Oxidation

---

• A) Clofazimine
• B) Rifampin
• C) Dapsone ✅
• D) Ofloxacin

---

• A) 6 months
• B) 9 months
• C) 1 year ✅
• D) 2 years

---

• A) 3 months
• B) 6 months ✅
• C) 1 year
• D) 18 months

---

• A) Ofloxacin
• B) Minocycline
• C) Clofazimine ✅
• D) Ethionamide

---

• A) Daily
• B) Weekly
• C) Once monthly (supervised) ✅
• D) Twice monthly

---

• A) Tetracyclines
• B) Sulphonamides ✅
• C) Aminoglycosides
• D) Beta-lactams

---

• A) Dapsone
• B) Rifampin
• C) Clofazimine
• D) Isoniazid ✅

Explanation: Isoniazid is used for TB, not leprosy. The antileprotic drugs include Dapsone, Rifampin, Clofazimine, and alternatives like Ofloxacin, Minocycline, Clarithromycin.

---

• A) Brain and CSF
• B) Infected skin, muscle, liver, kidney ✅
• C) Bone marrow
• D) Lymph nodes

---

• A) Rifampin
• B) Dapsone ✅
• C) Clofazimine
• D) Ethambutol

---

---

🔴 SECTION C: ANTIMALARIAL DRUGS

(25 Questions)

---

• A) Trypanosoma
• B) Leishmania
• C) Plasmodium ✅
• D) Toxoplasma

---

• A) Male Anopheles mosquito
• B) Female Anopheles mosquito ✅
• C) Female Culex mosquito
• D) Aedes mosquito

---

• A) P. vivax
• B) P. ovale
• C) P. malariae
• D) P. falciparum ✅

---

• A) Chloroquine
• B) Mefloquine
• C) Primaquine ✅
• D) Quinine

Explanation: Primaquine kills hypnozoites (latent liver forms) in P. vivax and P. ovale, which are responsible for relapse.

---

• A) Blood schizonts
• B) Sporozoites
• C) Hypnozoites (latent tissue forms) ✅
• D) Merozoites

---

• A) Chloroquine
• B) Primaquine
• C) Mefloquine
• D) All of the above ✅

Explanation: No available antimalarial drug is effective against sporozoites.

---

• A) 8-aminoquinoline
• B) 4-aminoquinoline ✅
• C) Sesquiterpene lactone
• D) Sulphonamide

---

• A) Inhibits folate synthesis
• B) Inhibits DNA-dependent RNA polymerase
• C) Inhibits heme polymerase → toxic heme accumulation ✅
• D) Disrupts mitochondrial membrane

Explanation: Chloroquine enters acidic food vacuole of parasite → inhibits heme polymerase → toxic heme accumulates → parasite membrane lysis → parasite dies.

---

• A) P. vivax
• B) P. ovale
• C) P. malariae
• D) Chloroquine-resistant P. falciparum ✅

---

• A) Epilepsy
• B) G6PD deficiency
• C) Pregnancy ✅
• D) Retinal disease

---

• A) Hepatotoxicity
• B) Irreversible retinopathy ✅
• C) Optic neuritis
• D) Peripheral neuritis

---

• A) Every month
• B) Every 6–12 months
• C) Every 3–6 months ✅
• D) Every year

---

• A) Pregnancy
• B) Epilepsy ✅
• C) Hypertension
• D) Diabetes

---

• A) Quinine
• B) Mefloquine
• C) Primaquine ✅
• D) Artesunate

---

• A) Anti-Chloroquine Therapy
• B) Artemisinin-based Combination Therapy ✅
• C) Artesunate Combination Treatment
• D) Advanced Combination Therapy

---

• A) Chloroquine + Primaquine
• B) Artesunate + Sulphadoxine/Pyrimethamine ✅
• C) Quinine + Doxycycline
• D) Mefloquine + Primaquine

---

• A) Water only
• B) Empty stomach
• C) Fatty meal ✅
• D) Milk

Explanation: Fat increases absorption of Lumefantrine — always take with a fatty meal.

---

• A) Oral Chloroquine
• B) IV/IM Artesunate ✅
• C) Oral Quinine
• D) IM Primaquine

---

• A) 1.2 mg/kg at 0, 12, 24 hours
• B) 2.4 mg/kg at 0, 12, 24 hours ✅
• C) 4 mg/kg single dose
• D) 1 mg/kg daily

---

• A) Hypertension
• B) G6PD deficiency ✅
• C) Diabetes
• D) Renal failure

Explanation: Primaquine causes haemolytic anaemia in G6PD-deficient patients — check G6PD levels before prescribing.

---

• A) Chloroquine
• B) Quinine
• C) Primaquine ✅
• D) Mefloquine

---

• A) Primaquine
• B) Chloroquine ✅
• C) Artesunate
• D) Pyrimethamine

Explanation: Chloroquine, Mefloquine, and Doxycycline are used for suppressive prophylaxis (suppress erythrocytic phase).

---

• A) Radical cure
• B) Causal prophylaxis ✅
• C) Suppressive prophylaxis
• D) Treatment of cerebral malaria

---

• A) It is effective against all asexual blood stages
• B) It is safe in G6PD deficiency
• C) It is the only drug effective against hypnozoites ✅
• D) It is given IV for severe malaria

---

• A) Artesunate
• B) Primaquine
• C) Chloroquine ✅
• D) Proguanil

---

---

⭐ ANSWER KEY — QUICK REFERENCE

---

💡 Exam Strategy Tips:

• If asked about "main/characteristic" side effect → Ethambutol = Optic neuritis, INH = Peripheral neuritis, Rifampin = Hepatitis
• Any question about relapse prevention → Answer is always Primaquine
• Any question about MDR-TB → must include resistance to both H and R
• Chloroquine + pregnancy = ✅ Safe
• Primaquine + G6PD deficiency = ⚠️ Dangerous

📝 MCQ PRACTICE SET

Antituberculosis | Antileprotic | Antimalarial Drugs

---

🔷 SECTION A: ANTITUBERCULOSIS DRUGS

(30 Questions)

---

• A) Peptidoglycan
• B) Mycolic acid
• C) RNA polymerase
• D) Folic acid

---

• A) Active drug
• B) Prodrug
• C) Slow-release drug
• D) Bacteriostatic drug

---

• A) Glucuronidation
• B) Hydroxylation
• C) Acetylation
• D) Sulfation

---

• A) Vitamin B12
• B) Vitamin C
• C) Pyridoxine (Vitamin B6)
• D) Folic acid

---

• A) Young children
• B) Slow acetylators
• C) Rapid acetylators
• D) Women

---

• A) Inhibits mycolic acid synthesis
• B) Inhibits DNA-dependent RNA polymerase
• C) Inhibits protein synthesis
• D) Inhibits cell wall peptidoglycan

---

• A) Empty stomach
• B) Antacids
• C) Food
• D) Milk

---

• A) Tuberculosis
• B) Leprosy
• C) Brucellosis
• D) Typhoid

---

• A) Optic neuritis
• B) Peripheral neuropathy
• C) Hepatitis
• D) Ototoxicity

---

• A) Stop the drug immediately
• B) It is a serious side effect
• C) It is harmless and expected
• D) Reduce the dose

---

• A) Alkaline pH
• B) Neutral pH
• C) Acidic pH
• D) All of the above

---

• A) Optic neuritis
• B) Hepatotoxicity
• C) Ototoxicity
• D) Peripheral neuritis

---

• A) Increases uric acid production
• B) Decreases renal excretion of uric acid
• C) Blocks xanthine oxidase
• D) Increases purine synthesis

---

• A) Inhibits RNA polymerase
• B) Inhibits mycolic acid synthesis
• C) Inhibits arabinosyl transferase
• D) Inhibits folic acid synthesis

---

• A) Hepatotoxicity
• B) Nephrotoxicity
• C) Optic neuritis
• D) Peripheral neuritis

---

• A) Bactericidal
• B) Bacteriostatic
• C) Both
• D) Neither

---

• A) Macrolides
• B) Tetracyclines
• C) Aminoglycosides
• D) Fluoroquinolones

---

• A) It causes GI irritation
• B) It is not absorbed from the gut
• C) It is destroyed by stomach acid
• D) It has poor solubility

---

• A) Intracellular bacilli in acidic pH
• B) Extracellular bacilli in alkaline pH
• C) Both intracellular and extracellular
• D) Latent bacilli in liver

---

• A) Ototoxicity
• B) Nephrotoxicity
• C) Neuromuscular blockade
• D) Optic neuritis

---

• A) 2 HRZ + 4 HR
• B) 2 HRZE + 4 HRE
• C) 2 HRZES + 5 HRE
• D) 3 HRZE + 3 HRE

---

• A) Any two first-line drugs
• B) Isoniazid alone
• C) Both Isoniazid AND Rifampin
• D) Rifampin alone

---

• A) Pyrazinamide + Ethambutol
• B) Fluoroquinolone + second-line injectable
• C) Streptomycin + Ethambutol
• D) All first-line drugs

---

• A) Rifampin
• B) Pyrazinamide
• C) Isoniazid
• D) Ethambutol

---

• A) Newborn of mother with active TB
• B) Children <6 years with positive tuberculin test
• C) Healthy adults with no TB contact
• D) Household contacts of TB patients

---

• A) Hepatotoxicity
• B) Peripheral neuritis
• C) Optic neuritis
• D) Ototoxicity

---

• A) Streptomycin
• B) Ethambutol
• C) Rifampin
• D) Pyrazinamide

---

• A) Rifampin
• B) BCG alone
• C) Isoniazid
• D) Pyrazinamide

---

• A) 3 months
• B) 6 months
• C) 9 months
• D) 12 months

---

• A) Rifampin is safe to take with food
• B) Streptomycin can be given orally
• C) Ethambutol is bactericidal
• D) Pyrazinamide works best in acidic pH

---

---

🟢 SECTION B: ANTILEPROTIC DRUGS

(15 Questions)

---

• A) Mycobacterium tuberculosis
• B) Mycobacterium leprae
• C) Mycobacterium avium
• D) Mycobacterium bovis

---

• A) Macrolide
• B) Sulphone
• C) Fluoroquinolone
• D) Aminoglycoside

---

• A) Inhibits RNA polymerase
• B) Inhibits mycolic acid synthesis
• C) Competitively inhibits folate synthetase
• D) Inhibits arabinosyl transferase

---

• A) Hepatotoxicity
• B) Haemolytic anaemia
• C) Optic neuritis
• D) Ototoxicity

---

• A) Diabetes mellitus
• B) Hypertension
• C) G6PD deficiency
• D) Renal failure

---

• A) Hydroxylation
• B) Glucuronidation
• C) Acetylation
• D) Oxidation

---

• A) Clofazimine
• B) Rifampin
• C) Dapsone
• D) Ofloxacin

---

• A) 6 months
• B) 9 months
• C) 1 year
• D) 2 years

---

• A) 3 months
• B) 6 months
• C) 1 year
• D) 18 months

---

• A) Ofloxacin
• B) Minocycline
• C) Clofazimine
• D) Ethionamide

---

• A) Daily
• B) Weekly
• C) Once monthly (supervised)
• D) Twice monthly

---

• A) Tetracyclines
• B) Sulphonamides
• C) Aminoglycosides
• D) Beta-lactams

---

• A) Dapsone
• B) Rifampin
• C) Clofazimine
• D) Isoniazid

---

• A) Brain and CSF
• B) Infected skin, muscle, liver, kidney
• C) Bone marrow
• D) Lymph nodes

---

• A) Rifampin
• B) Dapsone
• C) Clofazimine
• D) Ethambutol

---

---

🔴 SECTION C: ANTIMALARIAL DRUGS

(25 Questions)

---

• A) Trypanosoma
• B) Leishmania
• C) Plasmodium
• D) Toxoplasma

---

• A) Male Anopheles mosquito
• B) Female Anopheles mosquito
• C) Female Culex mosquito
• D) Aedes mosquito

---

• A) P. vivax
• B) P. ovale
• C) P. malariae
• D) P. falciparum

---

• A) Chloroquine
• B) Mefloquine
• C) Primaquine
• D) Quinine

---

• A) Blood schizonts
• B) Sporozoites
• C) Hypnozoites (latent tissue forms)
• D) Merozoites

---

• A) Chloroquine
• B) Primaquine
• C) Mefloquine
• D) All of the above

---

• A) 8-aminoquinoline
• B) 4-aminoquinoline
• C) Sesquiterpene lactone
• D) Sulphonamide

---

• A) Inhibits folate synthesis
• B) Inhibits DNA-dependent RNA polymerase
• C) Inhibits heme polymerase → toxic heme accumulation
• D) Disrupts mitochondrial membrane

---

• A) P. vivax
• B) P. ovale
• C) P. malariae
• D) Chloroquine-resistant P. falciparum

---

• A) Epilepsy
• B) G6PD deficiency
• C) Pregnancy
• D) Retinal disease

---

• A) Hepatotoxicity
• B) Irreversible retinopathy
• C) Optic neuritis
• D) Peripheral neuritis

---

• A) Every month
• B) Every 6–12 months
• C) Every 3–6 months
• D) Every year

---

• A) Pregnancy
• B) Epilepsy
• C) Hypertension
• D) Diabetes

---

• A) Quinine
• B) Mefloquine
• C) Primaquine
• D) Artesunate

---

• A) Anti-Chloroquine Therapy
• B) Artemisinin-based Combination Therapy
• C) Artesunate Combination Treatment
• D) Advanced Combination Therapy

---

• A) Chloroquine + Primaquine
• B) Artesunate + Sulphadoxine/Pyrimethamine
• C) Quinine + Doxycycline
• D) Mefloquine + Primaquine

---

• A) Water only
• B) Empty stomach
• C) Fatty meal
• D) Milk

---

• A) Oral Chloroquine
• B) IV/IM Artesunate
• C) Oral Quinine
• D) IM Primaquine

---

• A) 1.2 mg/kg at 0, 12, 24 hours
• B) 2.4 mg/kg at 0, 12, 24 hours
• C) 4 mg/kg single dose
• D) 1 mg/kg daily

---

• A) Hypertension
• B) G6PD deficiency
• C) Diabetes
• D) Renal failure

---

• A) Chloroquine
• B) Quinine
• C) Primaquine
• D) Mefloquine

---

• A) Primaquine
• B) Chloroquine
• C) Artesunate
• D) Pyrimethamine

---

• A) Radical cure
• B) Causal prophylaxis
• C) Suppressive prophylaxis
• D) Treatment of cerebral malaria

---

• A) It is effective against all asexual blood stages
• B) It is safe in G6PD deficiency
• C) It is the only drug effective against hypnozoites
• D) It is given IV for severe malaria

---

• A) Artesunate
• B) Primaquine
• C) Chloroquine
• D) Proguanil

---

💡 Note: Attempt all questions on your own first, then check with your notes. Good luck! 🍀

📊 YOUR MCQ RESULT ANALYSIS

---

---

✅ SECTION A — ANTITUBERCULOSIS DRUGS

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

🟢 SECTION B — ANTILEPROTIC DRUGS

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

🔴 SECTION C — ANTIMALARIAL DRUGS

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

---

📊 FINAL SCORE CARD

---

🔴 YOUR WEAK AREAS — STUDY THESE FIRST

---

⚠️ PRIORITY 1 — ANTIMALARIAL DRUGS (Weakest — 56%)

---

⚠️ PRIORITY 2 — ANTILEPROTIC DRUGS (67%)

---

⚠️ PRIORITY 3 — ANTITUBERCULOSIS DRUGS (77%)

---

📚 REVISION PLAN

💡 Key message: Your basic concepts are strong but you are making mistakes on specific details like doses, durations, drug classifications, and which drug is used for which indication. Revise those specific points and you will easily score 85%+!

🎯 TARGETED REVISION NOTES

Based on YOUR Wrong Answers Only

---

These notes are written specifically for the topics you got wrong. Read carefully — these are your weak points!

---

🔴 PART 1 — ANTITUBERCULOSIS (Your 7 Mistakes)

---

❌ MISTAKE 1 — Rifampin Main Side Effect (Q9)

You thought: Peripheral neuropathy

Correct: Hepatitis

🧠 Easy way to remember: Rifampin → Ruins the River (Liver) → Hepatitis is main AE

⚠️ Peripheral neuropathy/neuritis = INH only, NOT Rifampin

---

❌ MISTAKE 2 — Pyrazinamide Hyperuricemia (Q13)

You thought: Increases uric acid production

Correct: Decreases renal excretion of uric acid

🧠 Think of it this way: PZA blocks kidneys from throwing out uric acid → uric acid stays in blood → Hyperuricemia → Gout

PZA → Blocks renal tubular secretion → Uric acid stays in blood → Gout

The uric acid is NOT being made more — it just cannot come OUT of the body

---

❌ MISTAKE 3 — Streptomycin Why Not Oral (Q18)

You thought: GI irritation

Correct: Not absorbed from the gut

🧠 Remember: Streptomycin is a polar, water-soluble molecule Polar molecules cannot cross the lipid membrane of gut wall So it just passes through without entering blood → MUST be given IM

Streptomycin = Water soluble → Cannot cross gut wall → Not absorbed → Give IM

GI irritation is NOT the reason — absorption failure is the reason!

---

❌ MISTAKE 4 — XDR-TB Definition (Q23)

You thought: MDR + PZA + Ethambutol resistance

Correct: MDR + Fluoroquinolone + Second-line injectable

🧠 Resistance Ladder — Memorize this:

MONORESISTANCE → Resistant to 1 drug only

POLYDRUG → Resistant to >1 drug but NOT both H+R

MDR-TB → Resistant to both H (INH) + R (Rifampin)

XDR-TB → MDR + Fluoroquinolone + Injectable
              (amikacin / kanamycin / capreomycin)

XDR = Xtra Drug Resistance Think: MDR is bad → XDR is when even the backup drugs (FQ + injectable) also fail

---

❌ MISTAKE 5 — TB Chemoprophylaxis Drug (Q24 & Q28)

You thought: Rifampin

Correct: Isoniazid (INH)

🧠 Remember this clearly:

Rifampin is used for meningococcal prophylaxis — NOT TB prophylaxis INH 300 mg/day (10 mg/kg in children) for 6 months = TB prophylaxis

---

❌ MISTAKE 6 — Duration of INH Chemoprophylaxis (Q29)

You thought: 3 months

Correct: 6 months

🧠 Simple memory trick: 6 letters in "ISONIAZID" prophylaxis = 6 months

INH Chemoprophylaxis = 300 mg/day × 6 MONTHS
Children = 10 mg/kg/day × 6 MONTHS

Indications (who gets it):

1. Newborn of mother with active TB
2. Children <6 years with positive tuberculin test
3. Household contacts of TB patients
4. HIV patients + positive tuberculin test

---

❌ MISTAKE 7 — Drug That Crosses BBB in Meningitis (Q27)

You thought: Rifampin

Correct: Ethambutol (as per your notes)

🧠 CNS penetration of TB drugs:

Key point: Ethambutol crosses BBB specifically in meningitis

---

---

🟠 PART 2 — ANTILEPROTIC (Your 5 Mistakes)

---

❌ MISTAKE 8 — Main Adverse Effect of Dapsone (Q34)

You thought: Hepatotoxicity

Correct: Haemolytic anaemia

🧠 Dapsone AE Chart — Must Know:

MAIN AE = Dose-related HAEMOLYTIC ANAEMIA
          (especially dangerous in G6PD deficiency)

OTHER AE = Methaemoglobinaemia
           Anorexia, nausea, vomiting
           Peripheral neuropathy
           Allergic dermatitis

⚠️ Hepatotoxicity is for Rifampin/INH/PZA — NOT Dapsone Dapsone damages RBCs → Haemolysis

---

❌ MISTAKE 9 — Oldest Leprosy Drug (Q37)

You thought: Clofazimine

Correct: Dapsone

🧠 Drug History:

Clofazimine = New addition Dapsone = The OG (original) leprosy drug

---

❌ MISTAKE 10 — Duration of Leprosy Treatment (Q38 & Q39)

You thought: MBL = 6 months, PBL = 3 months

Correct: MBL = 1 year, PBL = 6 months

🧠 Super easy trick:

MBL (More Bacilli = Lepromatous, Borderline Lepromatous, Borderline)
→ MORE drugs + MORE time = 1 YEAR

PBL (Pauci Bacilli = Tuberculoid, Borderline Tuberculoid, Indeterminate)
→ LESS drugs + LESS time = 6 MONTHS

Memory: MBL = More = Months×12 (1 year)

---

❌ MISTAKE 11 — Dapsone Similar to Which Drug Class (Q42)

You thought: Beta-lactams

Correct: Sulphonamides

🧠 Why sulphonamides?

Both Dapsone AND Sulphonamides:
→ Are structurally similar to PABA
→ Inhibit folate synthetase enzyme
→ Block folic acid synthesis
→ Bacteriostatic action

Beta-lactams = work on cell wall peptidoglycan — completely different! Dapsone = Sulphone = Chemical cousin of Sulphonamide

---

---

🔴 PART 3 — ANTIMALARIAL (Your 11 Mistakes — Most Important!)

---

❌ MISTAKE 12 — Primaquine vs Chloroquine for Relapse (Q49 & Q59)

You thought: Chloroquine prevents relapse / Artesunate for radical cure

Correct: Primaquine prevents relapse

🧠 This is the MOST important antimalarial concept:

CHLOROQUINE = Kills blood-stage parasites (merozoites)
              → Terminates clinical attack
              → Does NOT go into liver
              → Does NOT prevent relapse ❌

PRIMAQUINE = Kills hypnozoites in LIVER
             → Prevents relapse ✅
             → Used for RADICAL CURE of P. vivax and P. ovale

Relapse occurs because: P. vivax/P. ovale hide as hypnozoites in liver Only Primaquine and Tafenoquine can kill hypnozoites Artesunate = used for P. falciparum, NOT for radical cure of vivax

---

❌ MISTAKE 13 — Chloroquine Classification (Q52)

You thought: Sulphonamide

Correct: 4-aminoquinoline

🧠 Quinoline Drug Classification — Must Know:

Quick memory: Chloroquine = 4-amino → C has 4 letters? No... just remember Chloro = 4 Primaquine = 8-amino → P comes after C → 8 comes after 4 ✅

---

❌ MISTAKE 14 — ACT for P. falciparum in India (Q61)

You thought: Chloroquine + Primaquine

Correct: Artesunate + Sulphadoxine/Pyrimethamine

🧠 Treatment by Species — CRITICAL TABLE:

Chloroquine + Primaquine = P. vivax radical cure ACT = P. falciparum treatment

---

❌ MISTAKE 15 — Artemether + Lumefantrine with Food (Q62)

You thought: Milk

Correct: Fatty meal

🧠 Why fatty meal? Lumefantrine is highly lipophilic (fat-loving) Fat in food helps it dissolve and get absorbed in gut Without fat → very poor absorption → treatment failure

Artemether + Lumefantrine = ALWAYS take with FATTY MEAL
Examples: Full meal, food with oil/butter/fat
NOT just milk alone

This is a commonly tested clinical point — patient counselling question!

---

❌ MISTAKE 16 — Treatment of Severe/Cerebral Malaria (Q63)

You thought: Oral Chloroquine

Correct: IV/IM Artesunate

🧠 Why NOT oral Chloroquine?

Severe malaria = Patient may be unconscious/vomiting
→ Cannot take oral drugs reliably
→ Need PARENTERAL (IV/IM) treatment
→ Drug of choice = ARTESUNATE IV/IM

Chloroquine parenteral = DANGEROUS → cardiac arrhythmias, cardiac arrest
Artesunate = Safe, fast, effective

Rule: Severe malaria = Always parenteral = Always Artesunate

---

❌ MISTAKE 17 — Artesunate Dose in Severe Malaria (Q64)

You thought: 1 mg/kg daily

Correct: 2.4 mg/kg at 0h, 12h, 24h → then once daily

🧠 Artesunate Dosing — Write it 3 times:

ARTESUNATE (Severe Malaria):
→ 2.4 mg/kg at Hour 0
→ 2.4 mg/kg at Hour 12
→ 2.4 mg/kg at Hour 24
→ Then 2.4 mg/kg ONCE DAILY
→ Until patient can take oral ACT

Remember: 2.4 — think "two point four" — at 0, 12, 24

---

❌ MISTAKE 18 — Gametocidal Drug for ALL Species (Q66)

You thought: Mefloquine

Correct: Primaquine

🧠 Gametocidal Drug Chart:

Mefloquine = NO gametocidal action — common exam trap! Primaquine = kills gametocytes of ALL species + kills hypnozoites

---

❌ MISTAKE 19 — Proguanil Use (Q68)

You thought: Treatment of cerebral malaria

Correct: Causal prophylaxis

🧠 Types of Malaria Prophylaxis:

CAUSAL PROPHYLAXIS = Acts on LIVER stage (pre-erythrocytic)
→ Prevents infection from establishing
→ Drugs: PROGUANIL, Primaquine, Pyrimethamine

SUPPRESSIVE PROPHYLAXIS = Acts on BLOOD stage
→ Suppresses symptoms/clinical attack
→ Drugs: CHLOROQUINE, Mefloquine, Doxycycline

Proguanil = acts on liver (pre-erythrocytic) stage of P. falciparum It is given to travellers visiting malaria zones → causal prophylaxis Cerebral malaria treatment = IV Artesunate (not Proguanil!)

---

❌ MISTAKE 20 — Cardiac Toxicity of Antimalarial (Q70)

You thought: Proguanil

Correct: Chloroquine (parenteral)

🧠 Chloroquine cardiac toxicity:

ORAL Chloroquine (normal doses):
→ Nausea, vomiting, headache, visual disturbances — mild

PARENTERAL Chloroquine (IV/IM):
→ Hypotension
→ Confusion
→ Cardiac ARRHYTHMIAS
→ Convulsions
→ Cardiac ARREST ← most serious!

LONG-TERM high dose (RA treatment):
→ Irreversible retinopathy
→ Myopathy, cardiomyopathy

That is why in severe malaria we use Artesunate — NOT parenteral Chloroquine!

---

---

⚡ MASTER QUICK REVISION — ALL YOUR MISTAKES

---

📌 TOP 5 THINGS TO NEVER FORGET:

1. Primaquine = only drug for hypnozoites = relapse prevention = vivax/ovale
2. INH = TB chemoprophylaxis (NOT Rifampin) for 6 months
3. MBL = 1 year, PBL = 6 months (leprosy)
4. Severe malaria = IV/IM Artesunate 2.4 mg/kg (NOT oral Chloroquine)
5. Dapsone main AE = Haemolytic anaemia (NOT hepatotoxicity)