Central Nervous System Pharmacology Practice Questions

Q: All of the following about thiopentone are true except which one?

IV injection is painless. ***IV injection is painless*** - Thiopentone is a **barbiturate anesthetic** that is known to cause **pain on injection** due to its **alkaline pH** and propensity to cause local irritation. - This characteristic makes the statement that its IV injection is painless incorrect, as pain and venous irritation are common side effects. *It decreases ICP* - Thiopentone, like other barbiturates, causes **cerebral vasoconstriction**, leading to a decrease in **cerebral blood flow** and **intracranial pressure (ICP)**, making it useful in neurosurgical settings. - This effect is due to a reduction in **cerebral metabolic rate for oxygen (CMRO2)**, which couples with cerebral blood flow. *It has anticonvulsant action* - Thiopentone is a potent **anticonvulsant** because it enhances the inhibitory effects of **GABA** in the central nervous system, which helps to suppress seizure activity. - It is used to terminate **status epilepticus** that is refractory to other treatments. *It can cause reflex tachycardia* - Thiopentone can cause **peripheral vasodilation** and a decrease in **blood pressure**, which may trigger a **reflex tachycardia** as the body attempts to compensate for the reduced systemic vascular resistance. - This effect is generally mild but can be more pronounced in hypovolemic patients or at higher doses.

Q: Which of the following antiepileptic drugs is associated with causing congenital heart disease in the fetus?

Valproate. ***Valproate*** - **Valproate** is associated with the **highest overall risk of major congenital malformations** among antiepileptic drugs, affecting **10-20%** of exposed fetuses - While **neural tube defects** (spina bifida) are the most characteristic malformation, **cardiac defects** (including atrial septal defects, ventricular septal defects, and coarctation of aorta) occur in approximately **2-3%** of exposed pregnancies - The teratogenic risk is **dose-dependent**, with higher doses (>1000 mg/day) carrying substantially greater risk - Valproate is classified as **FDA Category X** (contraindicated in pregnancy) due to its high teratogenic potential *Phenytoin* - **Phenytoin** is associated with **fetal hydantoin syndrome**, which includes craniofacial abnormalities, limb defects, nail hypoplasia, and growth restriction - Cardiac defects do occur with phenytoin exposure (particularly septal defects), with an estimated risk of **2-3%** - However, the **overall rate of major malformations** is lower than valproate (approximately 6-10%) - While cardiac defects are part of the phenytoin teratogenicity spectrum, valproate carries a higher absolute risk *Carbamazepine* - **Carbamazepine** is primarily associated with **neural tube defects** (0.5-1% risk), particularly spina bifida - The overall risk of major congenital malformations is **approximately 4-6%**, lower than both valproate and phenytoin - Cardiac defects can occur but are less frequently reported compared to other malformations *Barbiturates* - **Barbiturates** (such as phenobarbital) have teratogenic potential including cardiac defects and cleft palate - The overall risk of major malformations is **estimated at 5-7%** - While cardiac defects have been reported, the evidence base is less robust than for valproate, and the absolute risk is lower

Q: Which drug is the first-line treatment for absence seizures?

Ethosuximide. ***Ethosuximide*** - **Ethosuximide** is the **first-line drug** of choice for treating **absence seizures** due to its specific mechanism of action in inhibiting **T-type calcium channels** in the thalamus. - Its efficacy is highly specific to **absence seizures**, meaning it is primarily effective for this type of seizure and generally not for other seizure types. *Lamotrigine* - While effective for various seizure types, including **generalized tonic-clonic seizures** and **focal seizures**, **lamotrigine** is considered a **second-line agent** for absence seizures. - It is often used when **ethosuximide** or **valproic acid** is not tolerated or ineffective, or when there are co-existing seizure types. *Carbamazepine* - **Carbamazepine** is a first-line treatment for **focal seizures** and **generalized tonic-clonic seizures**, but it is generally **contraindicated** for absence seizures. - In some cases, **carbamazepine** can paradoxically **worsen absence seizures** or precipitate them due to its distinct mechanism of action involving **sodium channel blockade**. *Phenytoin* - **Phenytoin** is primarily used for **focal seizures** and **generalized tonic-clonic seizures** by stabilizing neuronal membranes and reducing neuronal excitability via **sodium channel blockade**. - It is **not effective** for absence seizures and, like carbamazepine, can sometimes **exacerbate** them or has no beneficial effect.

Q: What is the classification of Rotigotine?

Dopamine agonist. ***Dopamine agonist*** - Rotigotine is classified as a **non-ergoline dopamine agonist**, meaning it directly stimulates dopamine receptors in the brain. - It is used in the treatment of **Parkinson's disease** and **restless legs syndrome** by mimicking the effects of dopamine. *Dopamine antagonist* - **Dopamine antagonists** block dopamine receptors and are typically used as antipsychotics or antiemetics. - This classification would have opposite pharmacological effects to what is seen with rotigotine. *GABA agonist* - **GABA agonists** enhance the effects of the inhibitory neurotransmitter GABA, leading to sedation or seizure control. - This mechanism of action is unrelated to rotigotine's primary effects on dopamine pathways. *GABA antagonist* - **GABA antagonists** block GABA receptors, which can lead to increased neuronal excitability and seizures. - This is not the mechanism of action for rotigotine, which targets the dopaminergic system.

Q: Which drug is used in amytrophic lateral sclerosis?

Riluzole. ***Riluzole*** - **Riluzole** is an **NMDA receptor antagonist** that is approved for the treatment of **amyotrophic lateral sclerosis (ALS)**. - It works by reducing **glutamate-mediated excitotoxicity**, which is thought to contribute to neuronal damage in ALS, thereby extending survival time and delaying the need for tracheostomy. *Glatiramer acetate* - **Glatiramer acetate** is an immunomodulating drug used in the treatment of **multiple sclerosis (MS)**. - It is believed to work by inducing and activating **T-suppressor cells** specific for myelin basic protein, thus reducing the frequency of relapses in MS. *Tacrine* - **Tacrine** is an **acetylcholinesterase inhibitor** that was previously used for the treatment of **mild to moderate Alzheimer's disease**. - Its use has largely been replaced by newer, better-tolerated drugs due to its significant **hepatotoxicity** and frequent dosing schedule. *Olanzapine* - **Olanzapine** is an **atypical antipsychotic** medication used to treat conditions such as **schizophrenia** and **bipolar disorder**. - It primarily exerts its effects by blocking **dopamine D2** and **serotonin 5-HT2A** receptors.

Q: Which of the following drugs does not potentiate the effect of NMDA at NMDA receptors?

Ketamine. ***Ketamine*** - **Ketamine** is an **NMDA receptor antagonist**, meaning it blocks the activity of NMDA receptors rather than potentiating it. - It binds to a site within the **NMDA receptor channel**, preventing ion flow and neuronal excitation. - Used clinically as a dissociative anesthetic and for treatment-resistant depression. *Aspartic acid* - **Aspartic acid** functions as an **excitatory neurotransmitter** and is an **agonist** at NMDA receptors. - It readily activates these receptors by binding to the glutamate-binding site, thereby potentiating their effects. *D-serine* - **D-serine** acts as an **endogenous co-agonist** at the NMDA receptor by binding to the **glycine regulatory site** (also called the glycine-B site). - Its binding is essential for the full activation and potentiation of NMDA receptor activity. - Along with glycine, it is one of the primary physiological co-agonists required for NMDA receptor function. *Homocysteic acid* - **Homocysteic acid** is an **endogenous excitatory amino acid** that acts as an **agonist** at NMDA receptors. - It directly binds to and activates NMDA receptors at the glutamate-binding site, thus potentiating their effects.

Q: Patient on treatment with carbidopa + levodopa for 10 years now has wearing-off effect. What should be added to restore action?

Tolcapone. ***Tolcapone*** - **Tolcapone** is a **catechol-O-methyltransferase (COMT) inhibitor** that prevents the peripheral breakdown of levodopa, increasing its availability to the brain. - Adding a COMT inhibitor is the **primary strategy** to mitigate the **wearing-off effect** in patients receiving chronic levodopa therapy by prolonging levodopa's half-life and duration of action. - COMT inhibitors directly extend the duration of each levodopa dose, making them first-line adjuncts for wearing-off phenomenon. *Rasagiline* - **Rasagiline** is a **monoamine oxidase-B (MAO-B) inhibitor** used in Parkinson's disease to reduce the breakdown of dopamine in the brain. - It is also effective as an adjunct in treating **wearing-off** and can reduce daily off-time, though COMT inhibitors are typically preferred as first-line agents for this specific indication. - MAO-B inhibitors work by increasing central dopamine levels rather than directly extending levodopa's duration. *Benzhexol* - **Benzhexol** (also known as trihexyphenidyl) is an **anticholinergic agent** primarily used to treat tremor and dystonia in Parkinson's disease, especially in younger patients. - It does not address the aetiology of the **wearing-off phenomenon**, which is due to fluctuating levodopa levels and dopamine deficiency. *Amantadine* - **Amantadine** is an **NMDA receptor antagonist** used primarily to reduce **dyskinesias** associated with long-term levodopa therapy in Parkinson's disease. - While it has some efficacy in early Parkinson's and improving motor fluctuations, it is not the primary intervention for the **wearing-off effect** where reduced duration of benefit from levodopa is the main issue.

Q: Which of the following statements about oxcarbazepine is incorrect?

Less chances of hyponatremia than carbamazepine. ***Correct Answer: Less chances of hyponatremia than carbamazepine*** - This statement is **incorrect** because oxcarbazepine has a **higher incidence of hyponatremia** (up to 25% of patients) compared to carbamazepine (5-10%). - Hyponatremia is a well-known and dose-related adverse effect of oxcarbazepine, often requiring monitoring of serum sodium levels. - This is the most definitively incorrect statement among the options. *Incorrect: Metabolises itself* - While this statement is somewhat ambiguous, it likely refers to **autoinduction of metabolism**, which is a characteristic of **carbamazepine** [1]. - **Oxcarbazepine** is a prodrug that is rapidly converted to its active metabolite monohydroxy derivative (MHD), but it **does not autoinduce its own metabolism** to a significant extent like carbamazepine does [1]. - However, if interpreted literally, oxcarbazepine does undergo metabolism, making this statement potentially confusing. *Incorrect: Less chances of hepatotoxicity than carbamazepine* - This statement is **correct** about oxcarbazepine. It is generally associated with a **lower risk of severe hepatotoxicity** [1] compared to carbamazepine. - While liver enzyme elevations can occur, serious liver damage is much less common with oxcarbazepine. *Incorrect: It is less enzyme inducer than carbamazepine* - This statement is **correct** about oxcarbazepine. Its active metabolite MHD is a **weaker inducer of cytochrome P450 enzymes** (especially CYP3A4) than carbamazepine. - This translates to fewer and less significant drug-drug interactions with oxcarbazepine.

Q: What is the drug of choice for treating restless leg syndrome in a woman who developed pain and crawling sensation on her legs at night?

Pramipexole. ***Pramipexole*** - **Pramipexole** is a **dopamine agonist** (D2/D3 receptor agonist) that is highly effective in treating **restless leg syndrome (RLS)** and is FDA-approved for moderate-to-severe RLS. - It helps alleviate the characteristic **pain, crawling sensations (paresthesias)**, and the urge to move the legs, especially at night. - **First-line treatment** along with other dopamine agonists like ropinirole and rotigotine. - **Preferred in many guidelines** as a primary pharmacological option for RLS. *Gabapentin* - **Gabapentin** (and gabapentin enacarbil) is an **alpha-2-delta ligand** that is also considered a **first-line treatment option** for RLS per recent guidelines. - Particularly useful in patients with **comorbid insomnia, neuropathic pain**, or when there is concern about **augmentation** (worsening of symptoms with long-term dopamine agonist use). - While equally effective, **dopamine agonists like pramipexole** are more traditionally recognized as the primary choice in conventional teaching and previous exam questions. *Vitamin B12* - **Vitamin B12 deficiency** can cause **neurological symptoms** like numbness or tingling, but supplementation is **not a direct treatment for primary RLS** unless a specific deficiency is identified and contributing to symptoms. - No direct evidence supporting **Vitamin B12 supplementation** as a primary treatment for RLS itself. *Iron tablets* - **Iron deficiency** (ferritin <75 μg/L) is a common and important cause of **secondary RLS**, and **iron supplementation** should be considered when low iron stores are identified. - However, for primary RLS or without confirmed iron deficiency, iron tablets are **not the primary pharmacological treatment**, and dopamine agonists like pramipexole remain the preferred initial option.

Q: Which dopamine receptor blocker is commonly used for intractable Sydenham chorea?

Haloperidol. ***Haloperidol*** - Haloperidol is a **typical antipsychotic** and **dopamine D2 receptor blocker** commonly used for severe or intractable Sydenham chorea due to its efficacy in controlling **hyperkinetic movements**. - Its mechanism of action involves reducing dopaminergic overactivity in the **basal ganglia**, which is implicated in the pathogenesis of chorea. - While effective, it carries a risk of **extrapyramidal side effects** and requires monitoring. *Valproate* - Valproate is an **anticonvulsant** and **mood stabilizer** that IS actually used as a **first-line treatment** for Sydenham chorea, often preferred due to better tolerability compared to typical antipsychotics. - However, valproate is **not a dopamine receptor blocker** - it works through GABAergic mechanisms and sodium channel blockade. - The question specifically asks for a dopamine receptor blocker, making haloperidol the correct answer. *Warfarin* - Warfarin is an **anticoagulant** prescribed to prevent **thromboembolic events**, and has no role in the treatment of Sydenham chorea. - Its mechanism involves inhibiting **vitamin K-dependent clotting factors**, which is unrelated to neurological movement disorders. *Risperidone* - Risperidone is an **atypical antipsychotic** that blocks both **dopamine D2** and **serotonin 5-HT2A receptors**. While it can be effective for chorea, it is generally considered a **second-line agent**. - It may be used when typical antipsychotics are poorly tolerated, offering potentially lower risk of **extrapyramidal side effects** compared to haloperidol, though it still carries risks.

Question 1

All of the following about thiopentone are true except which one?

Accepted Answer

IV injection is painless

Answer

It has anticonvulsant action

Answer

It can cause reflex tachycardia

Answer

It decreases ICP

Question 2

Which of the following antiepileptic drugs is associated with causing congenital heart disease in the fetus?

Accepted Answer

Valproate

Answer

Carbamazepine

Answer

Phenytoin

Answer

Barbiturates

Question 3

Which drug is the first-line treatment for absence seizures?

Accepted Answer

Ethosuximide

Answer

Carbamazepine

Answer

Phenytoin

Answer

Lamotrigine

Question 4

What is the classification of Rotigotine?

Accepted Answer

Dopamine agonist

Answer

Dopamine antagonist

Answer

GABA agonist

Answer

GABA antagonist

Question 5

Which drug is used in amytrophic lateral sclerosis?

Accepted Answer

Riluzole

Answer

Tacrine

Answer

Olanzapine

Answer

Glatiramer acetate

Question 6

Which of the following drugs does not potentiate the effect of NMDA at NMDA receptors?

Accepted Answer

Ketamine

Answer

Aspartic acid

Answer

D-serine

Answer

Homocysteic acid

Question 7

Patient on treatment with carbidopa + levodopa for 10 years now has wearing-off effect. What should be added to restore action?

Accepted Answer

Tolcapone

Answer

Benzhexol

Answer

Rasagiline

Answer

Amantadine

Question 8

Which of the following statements about oxcarbazepine is incorrect?

Accepted Answer

Less chances of hyponatremia than carbamazepine

Answer

Metabolises itself

Answer

Less chances of hepatotoxicity than carbamazepine

Answer

It is less enzyme inducer than carbamazepine

Question 9

What is the drug of choice for treating restless leg syndrome in a woman who developed pain and crawling sensation on her legs at night?

Accepted Answer

Pramipexole

Answer

Gabapentin

Answer

Vitamin B12

Answer

Iron tablets

Question 10

Which dopamine receptor blocker is commonly used for intractable Sydenham chorea?

Accepted Answer

Haloperidol

Answer

Warfarin

Answer

Risperidone

Answer

Valproate

Central Nervous System Pharmacology — MCQs

Central Nervous System Pharmacology — MCQs

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