NEET-PG 2015 - Pharmacology Practice Questions

Q: Which of the following is not a known side effect of amiodarone?

Hyperglycemia. ***Hyperglycemia*** - **Hyperglycemia** is generally **not recognized** as a direct or common side effect of amiodarone. - Amiodarone's primary action is on cardiac ion channels, and its metabolic effects typically involve thyroid function, not glucose regulation. *Hyperthyroidism* - Amiodarone contains **iodine**, which can induce **thyroid dysfunction**, including both hypo- and hyperthyroidism. - **Amiodarone-induced hyperthyroidism (AIH)** can occur due to increased thyroid hormone synthesis or destructive thyroiditis. *Peripheral neuropathy* - **Neurological side effects**, including **peripheral neuropathy**, are known to occur with chronic amiodarone use. - Symptoms often include **paresthesias**, weakness, and sensory loss in the extremities. *Skin discoloration* - Prolonged use of amiodarone can lead to **bluish-gray skin discoloration**, particularly in sun-exposed areas. - This is due to the **accumulation of amiodarone** and its metabolites in the skin.

Q: Alkaline diuresis in drug poisoning is not done in?

Morphine. ***Morphine*** - **Morphine** is an **alkaline drug**, so its elimination is actually enhanced by **acidification of the urine**, not alkalinization. - Alkaline diuresis would decrease the ionization of morphine in the renal tubules, leading to **increased reabsorption** and reduced excretion. *Aspirin* - **Aspirin (acetylsalicylic acid)** is an **acidic drug**, and **alkaline diuresis** is effective in increasing its excretion by trapping the ionized form in the renal tubules. - This process prevents reabsorption and promotes clearance, which is a standard treatment for aspirin overdose. *Methotrexate* - **Methotrexate** is a **weak organic acid**, and **alkaline diuresis** is crucial in reducing its toxicity, especially in high-dose therapy. - By increasing urine pH, the renal elimination of methotrexate is significantly enhanced, preventing kidney damage and systemic accumulation. *Phenobarbitone* - **Phenobarbitone** is a **weak acid**, and **alkaline diuresis** is a well-established method to increase its renal excretion in cases of overdose. - Alkalinization of the urine promotes the ionization of phenobarbitone, reducing its reabsorption by the renal tubules and accelerating its elimination.

Q: Permission from DCGI [Drug controller general, India] is needed before which phase of drug trial?

Phase 3. ***Phase 3*** - Permission from the **DCGI (Drug Controller General of India)** is mandatory before initiating **Phase 3** clinical trials as per **Schedule Y** of the Drugs and Cosmetics Rules. - Phase 3 trials involve **large-scale studies in Indian patients** to establish efficacy and safety in the target population, requiring explicit regulatory approval. - This is the critical regulatory checkpoint where DCGI evaluates the Phase 1 and 2 data before allowing widespread testing in Indian subjects. *Phase 1* - Phase 1 trials can be conducted after approval from the **Institutional Ethics Committee (IEC)** without requiring prior DCGI permission. - These trials in healthy volunteers focus on safety, pharmacokinetics, and dose-ranging studies. - DCGI is informed but explicit permission is not mandatory at this stage. *Phase 2* - Phase 2 trials also proceed with **IEC approval** and do not require prior DCGI permission. - These trials evaluate therapeutic efficacy and dose determination in a limited number of patients. - Results from Phase 2 are submitted to DCGI when seeking Phase 3 approval. *Phase 4* - Phase 4 trials are **post-marketing surveillance** studies conducted after drug approval. - These are conducted under the Post-Marketing Surveillance (PMS) framework. - While regulatory oversight exists, these are not pre-market trials requiring permission to initiate.

Q: Which of the following are CYP3A inhibitors?

Both a and c. ***Both a and c (Ritonavir and Verapamil)*** - **Ritonavir** is a **potent CYP3A4 inhibitor**, one of the strongest known, commonly used as a pharmacokinetic booster for other protease inhibitors to increase their bioavailability - **Verapamil** is a **calcium channel blocker** that acts as a **moderate CYP3A4 inhibitor**, leading to clinically significant drug interactions requiring dose adjustments - Both drugs have **clinically relevant and well-established** CYP3A4 inhibitory effects *Ritonavir alone* - While correct that Ritonavir is a potent CYP3A4 inhibitor, this option is incomplete as it excludes Verapamil - Ritonavir's inhibitory effect is so strong that it can increase plasma concentrations of co-administered CYP3A4 substrates by several-fold *Amiodarone* - Amiodarone is primarily a **potent inhibitor of CYP2C9, CYP2D6, and P-glycoprotein** - While it does have **weak to moderate CYP3A4 inhibitory activity**, this effect is **less clinically significant** compared to its effects on other CYP enzymes - In the context of clinically important CYP3A4 inhibitors, Ritonavir and Verapamil are more relevant examples *Verapamil alone* - While correct that Verapamil is a CYP3A4 inhibitor, this option is incomplete as it excludes Ritonavir - Verapamil can increase plasma concentrations of drugs like simvastatin, cyclosporine, and other CYP3A4 substrates

Q: Regarding the concepts of efficacy and potency of a drug, which of the following statements is FALSE?

ED50 of the drug corresponds to efficacy. ***ED50 of the drug corresponds to efficacy*** - **ED50** (median effective dose) is the dose at which 50% of individuals exhibit the specified effect; it quantifies **potency**, not efficacy. - **Efficacy** refers to the maximum effect a drug can produce, while potency refers to the amount of drug needed to produce an effect. *In a clinical setup, efficacy is more important than potency* - **Efficacy** determines the maximal therapeutic benefit a drug can achieve for a patient, making it crucial for clinical outcomes. - While **potency** influences the dose required, a highly potent drug that is not very efficacious may not be clinically useful. *Drugs that produce a similar pharmacological effect can have different levels of efficacy* - Two drugs might act on the same receptor but elicit different maximal responses, indicating varying **efficacy**. - For example, a **partial agonist** and **full agonist** interacting with the same receptor will have different efficacies. *In the log dose response curve, the height of the curve corresponds with efficacy* - The **maximal response** or plateau of the dose-response curve represents the **efficacy** of a drug. - A higher plateau on the curve indicates a drug with greater intrinsic activity achieving a larger effect.

Q: Volume of distribution of a drug is 500 ml and target concentration of drug in blood is 5 g/L. 20% of administered drug is reached to systemic circulation. What will be the loading dose of that drug -

12.5 gm. ***12.5 gm*** - The formula for loading dose (LD) is: LD = (Target Concentration × Volume of Distribution) / Bioavailability. - Given: Target Concentration = 5 g/L, Volume of Distribution = 500 mL = 0.5 L, Bioavailability = 20% = 0.2. - So, LD = (5 g/L × 0.5 L) / 0.2 = 2.5 g / 0.2 = **12.5 g**. *1 gm* - This value would be obtained if the target concentration was 2 g/L with 100% bioavailability, or if the calculation incorrectly handled the volume or bioavailability factor. - It does not account for the specified **bioavailability of 20%** or the given target concentration and volume of distribution. *5 gm* - This result would be obtained if the bioavailability was assumed to be 50% (LD = 2.5 g / 0.5 = 5 g), or if the volume of distribution was incorrectly used in the calculation. - This option does not correctly factor in the **20% bioavailability** of the administered drug. *25 gm* - This value would result from mistakes such as dividing by bioavailability of 10% instead of 20% (LD = 2.5 g / 0.1 = 25 g), or by multiplying bioavailability instead of dividing by it. - This answer significantly **overestimates** the required dose, which could lead to drug toxicity.

Q: High volume of distribution is primarily determined by:

High lipid solubility. ***High lipid solubility***- Highly **lipid-soluble** drugs readily cross biological membranes and distribute extensively into tissues, including adipose tissue, CNS, and intracellular compartments, leading to a **high volume of distribution (Vd)** [1, 2].- This property allows the drug to move out of the bloodstream and into various body compartments, increasing the apparent volume in which the drug is dissolved [1].*High plasma protein binding*- **High plasma protein binding** generally **restricts** drug distribution to tissues because only the **unbound (free) fraction** can diffuse across capillary membranes into interstitial fluid and cells [1].- This typically leads to a **lower Vd**, as the drug is largely retained within the plasma compartment.*Elimination rate*- The **elimination rate** determines how quickly the drug is removed from the body, affecting the **duration of action** rather than the extent of distribution.- It influences drug concentration changes over time but does not directly determine the physical space (volume) into which the drug distributes.*Half-life of the drug*- The **half-life (t½)** is the time required for drug concentration to reduce by half, and it is **determined by** both Vd and clearance (t½ = 0.693 × Vd/CL).- Half-life is a **consequence** of Vd and clearance, not a primary determinant of how widely a drug distributes [3].

Q: What is the best method for treating methanol poisoning?

Fomepizole. ***Fomepizole*** - **Fomepizole** (Antizol) is a potent inhibitor of **alcohol dehydrogenase**, the enzyme responsible for metabolizing methanol into toxic metabolites like formic acid [1]. - By inhibiting this enzyme, fomepizole prevents the formation of these harmful metabolites, thus halting the progression of methanol toxicity and reducing mortality [1]. - It is the **gold standard** antidote for methanol poisoning. *Calcium gluconate* - **Calcium gluconate** is primarily used to treat **hypocalcemia** and magnesium toxicity. - It has no role in the direct treatment or detoxification of methanol poisoning. *Deferoxamine* - **Deferoxamine** is a **chelating agent** used to treat **iron toxicity** by binding to iron and facilitating its excretion [3]. - It is not effective for methanol poisoning as it does not interact with methanol or its toxic metabolites. *BAL* - **BAL** (British Anti-Lewisite, dimercaprol) is a chelating agent primarily used for poisoning by **heavy metals** such as arsenic, mercury, and gold [2]. - It has no therapeutic role in methanol poisoning, which involves a different toxicological mechanism.

Q: Interstitial nephritis is associated with all of the following medications except:

INH. ***INH*** - **Isoniazid (INH)** is primarily associated with **hepatotoxicity** (liver damage) and **peripheral neuropathy**, not typically interstitial nephritis. - While many drugs can rarely cause various adverse effects, INH is not a recognized common cause of **drug-induced interstitial nephritis**. *Beta-lactam antibiotics* - **Beta-lactam antibiotics**, including penicillins and cephalosporins, are among the most common causes of **drug-induced acute interstitial nephritis (AIN)**. - AIN is an **allergic hypersensitivity reaction** characterized by inflammation of the kidney's tubules and interstitium. *Diuretics* - Certain **diuretics**, particularly **thiazide diuretics** and **loop diuretics**, have been implicated in causing **acute interstitial nephritis**. - The mechanism is thought to be an **allergic or hypersensitivity reaction** within the renal tubules and interstitium. *Allopurinol* - **Allopurinol**, used to treat gout and hyperuricemia, is a known cause of **drug-induced acute interstitial nephritis**. - Renal involvement with allopurinol can range from mild tubular dysfunction to severe **acute kidney injury** due to AIN.

Q: What is the classification of Lorcaserin?

Anti-obesity. ***Anti-obesity*** - Lorcaserin is a selective **serotonin 5-HT₂C receptor agonist** that works by promoting satiety and reducing food intake. - It is prescribed as a long-term treatment for **weight management** in adults who are obese or overweight with at least one weight-related comorbidity. *Anti-anxiety* - Anti-anxiety medications, such as **benzodiazepines** or **SSRIs**, primarily target neurotransmitters like GABA or serotonin 5-HT₁A receptors to reduce anxiety symptoms. - Lorcaserin's primary mechanism of action is distinct, focusing on the 5-HT₂C receptor for appetite regulation, not anxiety. *Anti-smoking* - Anti-smoking medications, like **varenicline** or **bupropion**, are designed to reduce nicotine cravings and withdrawal symptoms. - Their mechanisms often involve nicotinic acetylcholine receptors or dopamine and norepinephrine reuptake inhibition, which differs from lorcaserin's action. *Anti-helminthic* - Anti-helminthic drugs are used to treat **parasitic worm infections** by paralyzing or killing the worms. - Common examples include **albendazole** or **mebendazole**, which have no relation to appetite control or obesity treatment.

Question 1

Which of the following is not a known side effect of amiodarone?

Accepted Answer

Hyperglycemia

Answer

Peripheral neuropathy

Answer

Hyperthyroidism

Answer

Skin discoloration

Question 2

Alkaline diuresis in drug poisoning is not done in?

Accepted Answer

Morphine

Answer

Aspirin

Answer

Phenobarbitone

Answer

Methotrexate

Question 3

Permission from DCGI [Drug controller general, India] is needed before which phase of drug trial?

Accepted Answer

Phase 3

Answer

Phase 1

Answer

Phase 2

Answer

Phase 4

Question 4

Which of the following are CYP3A inhibitors?

Accepted Answer

Both a and c

Answer

Ritonavir

Answer

Amiodarone

Answer

Verapamil

Question 5

Regarding the concepts of efficacy and potency of a drug, which of the following statements is FALSE?

Accepted Answer

ED50 of the drug corresponds to efficacy

Answer

Drugs that produce a similar pharmacological effect can have different levels of efficacy

Answer

In a clinical setup, efficacy is more important than potency

Answer

In the log dose response curve, the height of the curve corresponds with efficacy

Question 6

Volume of distribution of a drug is 500 ml and target concentration of drug in blood is 5 g/L. 20% of administered drug is reached to systemic circulation. What will be the loading dose of that drug -

Accepted Answer

12.5 gm

Answer

1 gm

Answer

5 gm

Answer

25 gm

Question 7

High volume of distribution is primarily determined by:

Accepted Answer

High lipid solubility

Answer

High plasma protein binding

Answer

Elimination rate

Answer

Half-life of the drug

Question 8

What is the best method for treating methanol poisoning?

Accepted Answer

Fomepizole

Answer

Calcium gluconate

Answer

BAL

Answer

Deferoxamine

Question 9

Interstitial nephritis is associated with all of the following medications except:

Accepted Answer

INH

Answer

Diuretics

Answer

Allopurinol

Answer

Beta-lactam antibiotics

Question 10

What is the classification of Lorcaserin?

Accepted Answer

Anti-obesity

Answer

Anti-anxiety

Answer

Anti-smoking

Answer

Anti-helminthic

NEET-PG 2015 — Pharmacology