Selective BZD Receptor Agonists:

Question 1

What are the BZD receptor agonist?

Answer 1

(Schedule IV): Zolipidem (Ambien®, Ambien CR®); Zaleplon (Zonata®); Eszopiclone (Luniest®) Structurally unrelated to BZDs

Question 2

What is the MOA of selective BZD agonists?

Answer 2

All have rapid onset & short duration MOA: Selectively bind to α1 subunits GABAA receptor causing increased neuronal inhibition. - α1 subunits of GABAA: sedation, amnesia.

Question 3

What is the USE, Pharmokenitics, Metabolism, and adverse side effects of Zolipidem (Ambien®, Ambien CR®)?

Answer 3

Minimal anticonvulsant & muscle relaxant activity- Use: Short-Term Insomnia (↓ sleep latency) - Pharmacokinetics: Rapid onset (30 min); Short duration (2.5 hr) - Metabolism: Inactive metabolites via liver P450. - Adverse: CNS (somnolence, dizziness, ataxia,

Question 4

What is the USE, Pharmokenitics, Metabolism, and adverse side effects of Zaleplon (Sonata®)?

Answer 4

Effect on sleep same as Zolipidem. - Half as potent as Zolipidem. - Minimal rebound insomnia; no withdrawal

Question 5

What is the USE, Pharmokenitics, Metabolism, and adverse side effects of Eszopiclone (Lunesta®)

Answer 5

• Minimal anticonvulsant & muscle relaxant activity - Use: Insomnia (↓ sleep latency & night time awakenings, ↑ total sleep time) - PK: Rapid onset (30 min); Short duration (6 hr) - Metabolism: Extensively metabolized by liver CYP3A4. - Adverse: Rebound insomnia can occur; CAUTION: Drug interaction with potent CYP3A4 inhibitors (↑ blood levels: itraconazole, clarithromycin, ritonavir) or inducers (↓ blood levels: rifampin, St John’s wort)

Question 6

Summary Table

Answer 6