Question

A drug ‘X’ is more selective for the 1 subunit of BZD receptors. It lacks effect on slow-wave sleep, minimum residual daytime sedation, no rebound insomnia on discontinuation, low abuse potential. Which of the following can be ‘X’?

• A. Flurozepam
• B. Flumazenil
• C. Melatonin
• D. Zolpidem

Answer 1

The Correct Option is D

The question asks us to identify a drug that fits the specified profile based on its selectivity and effects on sleep and sedation. Let's break down the question and options to determine the correct answer.

1. Understanding BZD Receptors and Selectivity:
   • Benzodiazepine (BZD) receptors are associated with GABA_A receptors in the central nervous system and have various subunits. The α1 subunit is particularly linked to sedative and hypnotic actions.
   • Drugs that are more selective for the α1 subunit are likely to have strong hypnotic effects but with fewer anxiolytic and muscle relaxant properties than those affecting other subunits.
2. Characteristics of Drug 'X':
   • No effect on slow-wave sleep – indicates the drug doesn't disrupt the most restorative phase of sleep.
   • Minimum residual daytime sedation – suggests a short half-life or low sedative potency during the day.
   • No rebound insomnia on discontinuation – important for short-term insomnia treatments without withdrawal effects.
   • Low abuse potential – indicates a profile that doesn't lead to dependency or misuse.
3. Analyzing the Options:
   • Flurozepam: A long-acting benzodiazepine often associated with hangover effects and residual sedation.
   • Flumazenil: Not a hypnotic; it is an antagonist used to reverse benzodiazepine effects and has no sedative properties.
   • Melatonin: A sleep-regulating hormone supplement; not selective for BZD receptors.
   • Zolpidem: A non-benzodiazepine hypnotic that selectively binds to the α1 subunit of GABA_A receptors, promoting sleep with minimal disruption of sleep architecture and a low risk of abuse.
4. Conclusion:
   • Based on the properties described, Zolpidem fits the criteria for drug 'X'. It is known for effectively inducing sleep with minimal adverse effects on the sleep cycle and low risk of dependency.

Thus, the correct answer is Zolpidem.