Central Nervous System Pharmacology — MCQs
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Buprenorphine is a partial agonist at which opioid receptor?
Which of the following drugs is not used in the treatment of akathisia?
All are symptoms of morphine withdrawal except?
Which of the following is a benzylisoquinoline muscle relaxant?
Botulinum toxin acts on
Which anxiolytic acts through 5-HT1A receptor partial agonism without exhibiting significant anticonvulsant or muscle relaxant properties?
Botulinum toxin type B is used in which disease?
Which is a GABA transaminase inhibitor?
Which of the following drugs is used for Smoking Cessation?
Which dopamine receptor is known for its inhibitory action in the central nervous system?
Central Nervous System Pharmacology Indian Medical PG Practice Questions and MCQs
Question 831: Buprenorphine is a partial agonist at which opioid receptor?
- A. Mu (Correct Answer)
- B. Kappa
- C. Delta
- D. ORL-1
Explanation: ***Mu*** - Buprenorphine primarily acts as a **partial agonist** at the **mu opioid receptor**, providing analgesic effects with a ceiling effect on respiratory depression. - Its partial agonism at the mu receptor contributes to its lower potential for respiratory depression and overdose compared to full mu agonists. *Kappa* - While buprenorphine has some antagonist activity at the kappa receptor, its primary therapeutic action is not at this receptor. - **Kappa receptor agonists** like pentazocine can produce dysphoria and psychotomimetic effects. *Delta* - The delta opioid receptor is involved in analgesia and emotional responses, but buprenorphine has very low affinity and activity at this receptor. - **Delta receptor agonists** are not widely used clinically due to limited efficacy and side effects. *ORL-1* - The ORL-1 (Opioid Receptor-like 1) receptor, also known as the nociceptin receptor, is distinct from classical opioid receptors. - Buprenorphine has **no significant activity** at the ORL-1 receptor, which primarily mediates pain, anxiety, and learning.
Question 832: Which of the following drugs is not used in the treatment of akathisia?
- A. Benzodiazepine
- B. Propranolol
- C. Trihexyphenidyl
- D. Haloperidol (Correct Answer)
Explanation: ***Haloperidol*** - **Haloperidol** is a typical antipsychotic drug known to **cause** or worsen **akathisia**, rather than treat it. - Akathisia is an extrapyramidal symptom, and **first-generation antipsychotics** like haloperidol are frequent culprits due to their strong **D2 receptor blockade**. *Benzodiazepine* - **Benzodiazepines** like lorazepam or clonazepam are often used to treat akathisia due to their **sedative** and **anxiolytic** properties. - They act by enhancing **GABAergic transmission**, which can help calm the motor restlessness associated with akathisia. *Propranolol* - **Propranolol**, a **beta-blocker**, is a first-line treatment for akathisia, particularly effective for its objective motor symptoms. - It works by reducing **adrenergic activity**, which is thought to contribute to the motor restlessness. *Trihexyphenidyl* - **Trihexyphenidyl** is an **anticholinergic** agent primarily used to treat **parkinsonian-like extrapyramidal symptoms** (e.g., dystonia, pseudoparkinsonism). - While sometimes used for generalized EPS, it is **less effective** for the specific motor restlessness of akathisia compared to beta-blockers or benzodiazepines.
Question 833: All are symptoms of morphine withdrawal except?
- A. Yawning
- B. Lacrimation
- C. Mydriasis
- D. Fall in BP (Correct Answer)
Explanation: ***Fall in BP*** - **Hypotension (fall in BP)** is **not** typically a symptom of opioid withdrawal; rather, **hypertension** can occur due to sympathetic overdrive. - Opioid withdrawal symptoms are primarily characterized by **hyperactivity** and increased sympathetic nervous system activity. *Mydriasis* - **Mydriasis (dilated pupils)** is a classic symptom of opioid withdrawal, resulting from reduced parasympathetic tone and increased sympathetic activity. - In contrast, opioid intoxication causes **miosis (pinpoint pupils)**. *Yawning* - **Yawning** is a very common and early symptom of opioid withdrawal, often accompanied by feelings of fatigue and restlessness. - It reflects generalized **autonomic dysregulation** during withdrawal. *Lacrimation* - **Lacrimation (tearing)** is another prominent autonomic symptom of opioid withdrawal. - This, along with rhinorrhea, contributes to the **"flu-like" symptoms** experienced during withdrawal.
Question 834: Which of the following is a benzylisoquinoline muscle relaxant?
- A. Rocuronium
- B. Doxacurium (Correct Answer)
- C. Pancuronium
- D. Vecuronium
Explanation: ***Doxacurium*** - **Doxacurium** is a long-acting, non-depolarizing neuromuscular blocker classified as a **benzylisoquinoline** compound [1]. - These agents are known for their minimal cardiovascular effects and lack of histamine release in therapeutic doses [1]. *Vecuronium* - **Vecuronium** is an **aminosteroid** non-depolarizing neuromuscular blocker [2]. - It is known for its intermediate duration of action and minimal cardiovascular effects [1]. *Rocuronium* - **Rocuronium** is also an **aminosteroid** non-depolarizing neuromuscular blocker [2]. - It has a rapid onset of action, making it suitable for rapid sequence intubation, and can be reversed by **sugammadex**. *Pancuronium* - **Pancuronium** is an **aminosteroid** non-depolarizing neuromuscular blocker with a long duration of action [1]. - It is associated with a vagolytic effect that can cause an increase in **heart rate** and **blood pressure** [1].
Question 835: Botulinum toxin acts on
- A. Synapse (Correct Answer)
- B. Smooth muscle of intestine
- C. Central nervous system
- D. Sensory nerves
Explanation: ***Synapse*** - **Botulinum toxin** acts by inhibiting the release of **acetylcholine** at the **neuromuscular junction**, which is a type of synapse. - This blockade of neurotransmitter release at the **presynaptic terminal** prevents muscle contraction, leading to paralysis. *Smooth muscle of intestine* - While botulinum toxin can affect smooth muscle indirectly by paralyzing the motor nerves innervating them, its primary site of action is the **synapse** itself, not directly on the muscle fibers. - The toxin primarily targets the nerve endings, rather than the mechanical contractility of the muscle cell. *Central nervous system* - **Botulinum toxin** does not readily cross the **blood-brain barrier**, meaning its primary effects are peripheral. - Its therapeutic and toxic effects are localized to the **peripheral nervous system** and neuromuscular junctions. *Sensory nerves* - **Botulinum toxin** specifically targets **motor nerve endings** to inhibit acetylcholine release, leading to muscle paralysis. - It does not directly affect the function of **sensory nerve transmission** or pain perception in the same way.
Question 836: Which anxiolytic acts through 5-HT1A receptor partial agonism without exhibiting significant anticonvulsant or muscle relaxant properties?
- A. Diazepam
- B. Zolpidem
- C. Phenobarbitone
- D. Buspirone (Correct Answer)
Explanation: ***Buspirone*** - **Buspirone** is a unique anxiolytic that primarily acts as a **partial agonist at 5-HT1A receptors**. - Unlike benzodiazepines, it lacks significant **anticonvulsant**, **muscle relaxant**, or **sedative-hypnotic properties** and does not lead to physical dependence or withdrawal. *Diazepam* - **Diazepam** is a **benzodiazepine** that acts by enhancing the effect of **GABA** at GABA-A receptors, leading to significant anxiolytic, sedative, muscle relaxant, and anticonvulsant effects. - It does not primarily act via **5-HT1A receptor partial agonism**. *Zolpidem* - **Zolpidem** is a **non-benzodiazepine hypnotic** that selectively binds to the **GABA-A receptor** subunit, primarily mediating sedative effects. - While it's used for insomnia, it doesn't primarily act as a **5-HT1A partial agonist** and is not typically used for its anxiolytic properties in the same way as buspirone. *Phenobarbitone* - **Phenobarbitone** is a **barbiturate** that acts by prolonging the opening of **chloride channels** associated with GABA-A receptors, leading to strong sedative, hypnotic, and anticonvulsant effects. - Its mechanism of action is distinct from **5-HT1A receptor partial agonism**, and it carries a high risk of dependence and overdose.
Question 837: Botulinum toxin type B is used in which disease?
- A. Cervical dystonia (Correct Answer)
- B. Blepharospasm
- C. Strabismus
- D. Glabellar lines
Explanation: ***Cervical dystonia*** * **Botulinum toxin type B (Myobloc/NeuroBloc)** is specifically approved for the treatment of **cervical dystonia**, which involves involuntary contractions of neck muscles. * It works by blocking the release of **acetylcholine** at the neuromuscular junction, leading to muscle relaxation. *Strabismus* * **Botulinum toxin type A (Botox, Dysport, Xeomin)** is the preferred and most commonly used form for treating **strabismus** by temporarily weakening specific extraocular muscles. * Type B is generally not indicated for strabismus due to differences in potency and duration of action. *Blepharospasm* * **Botulinum toxin type A** (e.g., Botox) is the primary treatment for **blepharospasm**, an involuntary forceful closure of the eyelids. * While both types inhibit acetylcholine release, type A has a more established and concentrated use in treating localized muscle spasms like blepharospasm. *Glabellar lines* * **Botulinum toxin type A** is widely used for cosmetic applications such as reducing **glabellar lines** (frown lines between the eyebrows). * Its efficacy and safety for cosmetic indications are well-established, making type A the standard choice over type B.
Question 838: Which is a GABA transaminase inhibitor?
- A. TCA
- B. Valproate (Correct Answer)
- C. Gabapentin
- D. Sertraline
Explanation: ***Valproate*** - Valproate is known to inhibit **GABA transaminase**, an enzyme responsible for the breakdown of **gamma-aminobutyric acid (GABA)**. - By inhibiting this enzyme, valproate increases the concentration of **GABA** in the brain, enhancing its inhibitory effects and contributing to its anticonvulsant properties. *TCA* - **Tricyclic antidepressants (TCAs)** primarily work by inhibiting the reuptake of **norepinephrine** and **serotonin** in the brain. - They do not directly inhibit GABA transaminase but rather modulate monoamine neurotransmission. *Sertraline* - **Sertraline** is a **selective serotonin reuptake inhibitor (SSRI)** that works by blocking the reabsorption of **serotonin** into presynaptic neurons. - Its primary mechanism of action is focused on serotonin pathways, not on GABA metabolism. *Gabapentin* - **Gabapentin** is an anticonvulsant that is thought to exert its effects by modulating **calcium channels** and increasing **GABA synthesis**, but it is not a direct inhibitor of GABA transaminase. - Its mechanism of action is distinct from directly preventing GABA breakdown.
Question 839: Which of the following drugs is used for Smoking Cessation?
- A. Bupropion (Correct Answer)
- B. Methadone
- C. Buprenorphine
- D. Naltrexone
Explanation: ***Bupropion*** - **Bupropion** is an antidepressant that is also approved as a smoking cessation aid. It works by inhibiting the reuptake of **dopamine** and **norepinephrine**, which can help reduce nicotine cravings and withdrawal symptoms. - It is often prescribed as a first-line pharmacotherapy for smoking cessation, with a typical treatment duration of 7-12 weeks. *Buprenorphine* - **Buprenorphine** is a partial opioid agonist primarily used to treat opioid addiction. It is not indicated for smoking cessation. - While it can help manage withdrawal symptoms from opioids, it has no direct mechanism of action that would reduce nicotine dependence or cravings. *Methadone* - **Methadone** is a full opioid agonist primarily used for the treatment of opioid use disorder (OUD) and chronic pain management. It is not used for smoking cessation. - Its mechanism involves binding to opioid receptors to prevent withdrawal symptoms and reduce cravings for other opioids. *Naltrexone* - **Naltrexone** is an opioid antagonist used primarily for the treatment of alcohol dependence and opioid use disorder. It is not indicated for smoking cessation. - It blocks the effects of opioids and reduces alcohol cravings, but does not affect nicotine pathways or dependence.
Question 840: Which dopamine receptor is known for its inhibitory action in the central nervous system?
- A. Dopamine Receptor D5
- B. No inhibitory dopamine receptor present
- C. Dopamine Receptor D2 (Correct Answer)
- D. Dopamine Receptor D1
Explanation: ***Dopamine Receptor D2*** - The **D2 receptor** is a member of the D2-like family (D2, D3, D4), which are **G-protein coupled receptors** that inhibit adenylyl cyclase activity. - Its activation typically leads to a **decrease in neuronal excitability** and neurotransmitter release, providing an inhibitory effect in the CNS. *Dopamine Receptor D5* - The **D5 receptor** belongs to the D1-like family (D1, D5), which are **G-protein coupled receptors** that stimulate adenylyl cyclase activity. - Activation of D5 receptors typically leads to **excitatory effects** rather than inhibitory ones in the CNS. *No inhibitory dopamine receptor present* - This statement is incorrect as specific dopamine receptor subtypes, particularly the **D2-like family**, are well-established to exert inhibitory actions in the CNS. - These inhibitory effects are crucial for various physiological processes, including motor control and reward pathways. *Dopamine Receptor D1* - The **D1 receptor** is part of the D1-like family (D1, D5) and is known for its **excitatory effects** in the CNS. - Activation of D1 receptors leads to an **increase in intracellular cAMP** and generally enhances neuronal activity.
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