Zopiclone Flashcards

Drug Class

• Zopiclone is classified as a Z drug, which are non-benzodiazepine hypnotics and sedatives.

Indications

• Primarily used for the short-term treatment of debilitating or distressing insomnia, although non-pharmacological treatments are preferred.

Mechanism of Action (MOA)

• Z drugs act on the GABA type A receptor, similar to benzodiazepines.
• They facilitate GABA binding, enhancing inhibitory effects in the brain, leading to reduced anxiety, sleeplessness, and sedation.
• Not effective as anticonvulsants and have a shorter duration of action compared to most benzodiazepines.

Adverse Effects

• Common effects include daytime sleepiness, which can impair driving and complex tasks.
• Possible rebound insomnia after cessation of use.
• Other neurological issues include headaches, confusion, nightmares, and rarely amnesia.
• Unique adverse effects: Zopiclone may cause taste disturbance; Zolpidem is more likely to cause gastrointestinal upset.
• Prolonged use beyond four weeks can lead to dependence and withdrawal symptoms such as headaches and anxiety.
• Overdose can cause severe drowsiness, coma, and respiratory depression.

Warnings

• Use with caution in the elderly due to increased sensitivity to neurological effects.
• Contraindicated in patients with obstructive sleep apnoea or respiratory depression as it may exacerbate conditions.

Interactions

• Z drugs can amplify the sedative effects of alcohol, antihistamines, and benzodiazepines.
• Enhance hypotensive effects of antihypertensive medications.
• Metabolism through CYP450 enzymes: Inhibitors (e.g., macrolides) increase sedation, while inducers (e.g., phenytoin, rifampicin) may reduce sedation.

Prescription Guidelines

• Prescribed at the lowest effective dose for the shortest duration, typically no longer than two weeks.
• Common doses include Zopiclone 7.5 mg or Zolpidem 10 mg taken at bedtime.
• Starting doses for elderly patients should be halved.

Administration

• Available for oral use only, in the form of tablets or capsules.

Patient Counselling

• Emphasize that sleeping tablets are a short-term solution for insomnia.
• Discuss underlying reasons for insomnia and provide sleep hygiene advice.
• Advise against regular use due to potential dependency; maximum usage should be 2-4 weeks.
• Warn about the risk of drowsiness affecting driving or operating heavy machinery the following day.

Monitoring

• Clinical monitoring for efficacy and safety is essential during treatment.