NEET-PG 2015 - Pharmacology Practice Questions

Q: Which of the following is an aromatase inhibitor?

Letrozole. ***Letrozole*** - **Letrozole** is a commonly used **aromatase inhibitor**, which works by blocking the enzyme **aromatase** that converts androgens into estrogens [1]. - This reduction in estrogen levels is crucial in treating **hormone-sensitive breast cancers** [1]. *Tamoxifen* - **Tamoxifen** is a **selective estrogen receptor modulator (SERM)**, not an aromatase inhibitor [2]. - It acts by blocking estrogen receptors in breast tissue while potentially stimulating them in other tissues like bone and uterus [2]. *Danazol* - **Danazol** is a synthetic androgen that suppresses the hypothalamic-pituitary-gonadal axis, leading to **decreased estrogen production**. - It works by inhibiting gonadotropin release and directly inhibiting ovarian steroidogenesis, rather than blocking the aromatase enzyme directly. *Taxane* - **Taxanes** are a class of **chemotherapy drugs** that interfere with cell division by stabilizing microtubules. - They are used to treat various cancers, including breast cancer, but do not act as aromatase inhibitors.

Q: Which antithyroid drug is preferred during the first trimester of pregnancy due to relatively lower placental transfer?

Propylthiouracil. ***Propylthiouracil*** - **Propylthiouracil (PTU)** is the preferred antithyroid drug during the **first trimester** of pregnancy because it crosses the placenta less readily than methimazole/carbimazole. - While it still crosses the placenta, its lower placental transfer and association with fewer fetal anomalies in early pregnancy make it a safer initial choice, especially to minimize the risk of **fetal embryopathy** associated with methimazole. *Carbimazole* - **Carbimazole** (which is metabolized to methimazole) can cross the placenta more easily than PTU and has been associated with **fetal anomalies**, particularly in the first trimester. - Its use is generally avoided during the first trimester due to concerns about congenital malformations such as **aplasia cutis** and **esophageal atresia**. *Both* - While both drugs can cross the placenta to some extent, their safety profiles and recommended use during pregnancy differ significantly. - Carbimazole (methimazole) has a higher risk of teratogenicity in the first trimester compared to PTU. *None of the options* - This option is incorrect because propylthiouracil is indeed known to cross the placenta and is commonly used in pregnancy, especially during the first trimester. - The choice of antithyroid drug is a critical consideration in managing hyperthyroidism in pregnancy.

Q: Which of the following oral antidiabetic drugs is an insulin secretagogue?

Nateglinide. **Nateglinide** - **Nateglinide** is a **meglitinide**, which is a type of **insulin secretagogue**. - It stimulates **insulin release** from pancreatic beta cells by blocking ATP-sensitive potassium channels. *Metformin* - **Metformin** is a **biguanide** that primarily works by **decreasing hepatic glucose production** and increasing insulin sensitivity in peripheral tissues. - It does not directly stimulate insulin secretion. *Pioglitazone* - **Pioglitazone** is a **thiazolidinedione** (TZD) that improves insulin sensitivity by activating **PPAR-gamma receptors**. - It does not directly affect insulin secretion but rather enhances the body's response to existing insulin. *Acarbose* - **Acarbose** is an **alpha-glucosidase inhibitor** that delays the digestion and absorption of carbohydrates in the small intestine. - This reduces postprandial glucose excursions and does not directly stimulate insulin secretion.

Q: How do thiazides cause hypercalcemia?

Decreased calcium excretion. ***Decreased calcium excretion*** - Thiazides inhibit the **Na-Cl co-transporter** in the **distal convoluted tubule**, leading to increased reabsorption of calcium [1], [2]. - This increased reabsorption of calcium is mediated by a low intracellular sodium concentration, which enhances the activity of the **Na+/Ca2+ exchanger** on the basolateral membrane [1]. *Increased parathyroid hormone secretion* - Thiazides **do not directly stimulate** parathyroid hormone (PTH) secretion; instead, they *decrease* calcium excretion, which would typically *lower* PTH levels through negative feedback. - Elevated PTH would lead to increased bone resorption and kidney calcium reabsorption, but this is not the **primary mechanism** for thiazide-induced hypercalcemia [2]. *Decreased calcitonin secretion* - **Calcitonin** is a hormone that *lowers* blood calcium levels, and its decrease would theoretically contribute to hypercalcemia. - However, thiazides have **no direct effect** on calcitonin secretion, making this an unlikely primary mechanism. *Increased calcium absorption* - While increased calcium absorption from the gut can contribute to hypercalcemia, thiazides do **not directly increase intestinal calcium absorption**. - Their primary action for influencing calcium levels is within the **kidney**, specifically on reabsorption, not absorption from the GI tract [1], [2].

Q: Which of the following is a PGE1 analogue used in medical treatments?

Alprostadil. ***Alprostadil*** - **Alprostadil** is a synthetic **prostaglandin E1 (PGE1)** analogue. - It is used in neonates to maintain the **patency of the patent ductus arteriosus** and in adults for the treatment of **erectile dysfunction**. *Carboprost* - **Carboprost** is a synthetic analogue of **prostaglandin F2 alpha (PGF2α)**. - It is primarily used to manage **postpartum hemorrhage** due to its potent uterotonic effects. *Epoprostenol* - **Epoprostenol** is a synthetic analogue of **prostacyclin (PGI2)**. - It is known for its potent **vasodilatory** and **antiplatelet** properties, making it useful in treating **pulmonary arterial hypertension**. *Dinoprostone* - **Dinoprostone** is a synthetic form of **prostaglandin E2 (PGE2)**. - It is used to **induce labor** or **cervical ripening** due to its role in uterine contractions and cervical dilation.

Q: Which of the following is a long-acting beta-2 agonist?

Formoterol. ***Formoterol*** - **Formoterol** is a **long-acting beta-2 agonist (LABA)** commonly used in the treatment of asthma and COPD. - It provides **bronchodilation** for up to 12 hours due to its high lipophilicity, allowing it to remain in the cell membrane and continuously activate beta-2 receptors. *Isoprenaline (non-selective adrenergic agonist)* - **Isoprenaline** is a **non-selective beta-adrenergic agonist**, meaning it activates both beta-1 and beta-2 receptors. - It is **short-acting** and primarily used as a vasodilator or to stimulate heart rate, not as a long-acting bronchodilator. *Ephedrine (non-selective adrenergic agonist)* - **Ephedrine** is a **mixed-acting sympathomimetic amine** that increases the release of norepinephrine and directly stimulates alpha and beta receptors. - It has a short duration of action and is primarily used as a decongestant or bronchodilator in emergency situations, not as a long-acting agent. *Salbutamol (short-acting beta-2 agonist)* - **Salbutamol** is a **short-acting beta-2 agonist (SABA)**, providing rapid onset but a short duration of action (typically 4-6 hours). - It is used for **relieving acute bronchospasm** and is not considered a long-acting medication for maintenance therapy.

Q: Which triptan is available in nasal spray form?

Sumatriptan. ***Sumatriptan*** - **Sumatriptan** is available in multiple formulations, including **oral, subcutaneous injection, and nasal spray**, making it versatile for migraine treatment [1], [2]. - The nasal spray formulation allows for **faster absorption** and onset of action, which can be beneficial for patients with nausea or vomiting during migraine attacks [1]. *Rizatriptan* - **Rizatriptan** is primarily available in **oral tablet** and **orally disintegrating tablet** (ODT) forms [2]. - It does not have a commonly available nasal spray formulation for migraine treatment [2]. *Naratriptan* - **Naratriptan** is available as an **oral tablet** and is known for its **longer half-life** and generally milder side effect profile compared to sumatriptan [2]. - It is not available in a nasal spray formulation [2]. *Frovatriptan* - **Frovatriptan** is available exclusively as an **oral tablet** and is notable for having the **longest half-life** among triptans, making it useful for preventing recurring migraines [2]. - There is no nasal spray formulation for frovatriptan [2].

Q: Acetaminophen [Paracetamol] induced liver toxicity is due to which metabolite?

NAPQI. ***NAPQI*** - **N-acetyl-p-benzoquinone imine (NAPQI)** is a highly reactive and toxic metabolite produced during acetaminophen metabolism, especially in overdose situations [1, 3]. - When glutathione stores are depleted due to excessive NAPQI formation, this metabolite covalently binds to hepatic macromolecules, causing **hepatocellular damage and necrosis** [1, 3].*N-acetylcysteine* - **N-acetylcysteine (NAC)** is the antidote for acetaminophen overdose, not the toxic metabolite itself [2, 3]. - NAC works by replenishing hepatic **glutathione stores**, which helps detoxify NAPQI and prevent liver injury [2, 3].*Co-Q* - **Coenzyme Q10 (CoQ10)** is an endogenous antioxidant and electron carrier in the mitochondrial respiratory chain. - It is not a metabolite of acetaminophen and plays no direct role in acetaminophen-induced liver toxicity.*Cytochrome 'C'* - **Cytochrome c** is a protein involved in the electron transport chain in mitochondria and plays a critical role in apoptosis. - While cellular damage from NAPQI can eventually lead to cytochrome c release and apoptosis, cytochrome c itself is not a metabolite of acetaminophen or the direct cause of toxicity.

Q: Which non-selective beta-blocker has sympathomimetic activity?

Pindolol. ***Pindolol*** - **Pindolol** is a **non-selective beta-blocker** that exhibits **intrinsic sympathomimetic activity (ISA)**, meaning it acts as a partial agonist at beta-adrenergic receptors. - Due to ISA, it causes less reduction in resting heart rate and cardiac output compared to beta-blockers without ISA. *Acebutalol* - **Acebutalol** is a **beta-1 selective blocker** (cardioselective) that possesses **intrinsic sympathomimetic activity (ISA)**. - While it has ISA, it is not a non-selective beta-blocker, making it an incorrect answer for this question. *Nadolol* - **Nadolol** is a **non-selective beta-blocker** that does **not** have intrinsic sympathomimetic activity (ISA). - It primarily acts as a pure antagonist at both beta-1 and beta-2 adrenergic receptors. *Metoprolol* - **Metoprolol** is a **beta-1 selective blocker** (cardioselective) and does **not** possess intrinsic sympathomimetic activity (ISA). - Its primary action is blockade of cardiac beta-1 receptors.

Question 1

A 47-year-old woman presents with complaints of nervousness and increased sensitivity to hot weather. She is diagnosed with hyperthyroidism and prescribed propylthiouracil. What is the principal mechanism by which this drug acts?

Accepted Answer

Inhibiting the enzyme thyroid peroxidase, which reduces the synthesis of thyroid hormones.

Answer

Reducing the proteolysis of thyroglobulin.

Answer

Inhibiting the binding of TSH to its receptor.

Answer

Altering the levels of reverse T3 (rT3) in the body.

Question 2

Which of the following is an aromatase inhibitor?

Accepted Answer

Letrozole

Answer

Tamoxifen

Answer

Danazol

Answer

Taxane

Question 3

Which antithyroid drug is preferred during the first trimester of pregnancy due to relatively lower placental transfer?

Accepted Answer

Propylthiouracil

Answer

Carbimazole

Answer

Both

Answer

None of the options

Question 4

Which of the following oral antidiabetic drugs is an insulin secretagogue?

Accepted Answer

Nateglinide

Answer

Metformin

Answer

Pioglitazone

Answer

Acarbose

Question 5

How do thiazides cause hypercalcemia?

Accepted Answer

Decreased calcium excretion

Answer

Increased parathyroid hormone secretion

Answer

Decreased calcitonin secretion

Answer

Increased calcium absorption

Question 6

Which of the following is a PGE1 analogue used in medical treatments?

Accepted Answer

Alprostadil

Answer

Carboprost

Answer

Epoprostenol

Answer

Dinoprostone

Question 7

Which of the following is a long-acting beta-2 agonist?

Accepted Answer

Formoterol

Answer

Isoprenaline

Answer

Ephedrine

Answer

Salbutamol

Question 8

Which triptan is available in nasal spray form?

Accepted Answer

Sumatriptan

Answer

Rizatriptan

Answer

Naratriptan

Answer

Frovatriptan

Question 9

Acetaminophen [Paracetamol] induced liver toxicity is due to which metabolite?

Accepted Answer

NAPQI

Answer

Co-Q

Answer

Cytochrome 'C'

Answer

N-acetylcysteine

Question 10

Which non-selective beta-blocker has sympathomimetic activity?

Accepted Answer

Pindolol

Answer

Nadolol

Answer

Acebutalol

Answer

Metoprolol

NEET-PG 2015 — Pharmacology