Maknotte (Zopiclone)

Zopiclone is indicated for insomnia, a sleep disorder characterized by difficulty initiating or maintaining sleep.

• Insomnia (difficulty falling asleep): helps patients initiate sleep more quickly.
• Insomnia (difficulty maintaining sleep): reduces nocturnal awakenings and prolongs sleep duration.
• Generalized insomnia: improves overall sleep quality and next‑day functioning.

• Zopiclone acts as a positive allosteric modulator at the GABA‑A receptor complex. By binding to a distinct site on the receptor, it enhances the inhibitory effect of GABA, increasing chloride ion influx into neurons. This potentiation leads to reduced neuronal excitability and central nervous system depression, facilitating the onset and maintenance of sleep without the benzodiazepine binding profile.

Zopiclone may cause a range of adverse reactions, varying from mild to serious.

Common Side Effects

• Bitter or metallic taste: transient alteration in oral sensation.
• Drowsiness or fatigue: feeling sleepy during daytime.
• Dry mouth: reduced salivary flow.
• Headache: mild to moderate cranial pain.
• Nausea: upset stomach or urge to vomit.

Serious or Rare Side Effects

• Complex sleep behaviours: sleepwalking, sleep‑driving, or performing other activities while not fully awake.
• Allergic reactions: rash, itching, swelling, or difficulty breathing.
• Mood changes: depression, anxiety, or suicidal thoughts.
• Respiratory depression: slowed breathing, especially when combined with other depressants.
• Memory impairment: amnesia for events occurring after dosing.

Before prescribing Zopiclone, clinicians should consider several safety precautions to minimize risks.

• Avoid alcohol: concurrent use can intensify sedation and respiratory depression.
• Use caution in elderly: increased sensitivity may lead to falls and cognitive impairment.
• Do not operate machinery: impaired alertness can affect driving or use of hazardous equipment.
• Pregnancy category B: limited data suggest relative safety, but use only if clearly needed.
• Renal or hepatic impairment: dose adjustment may be required due to altered metabolism.
• Store at ambient temperature: keep below 25 °C in the original packaging, protected from moisture and light.

Zopiclone can interact with other medicines, altering its effectiveness or increasing adverse effects.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole): may raise plasma concentrations and heighten sedation.
• Opioids (e.g., morphine, oxycodone): additive central nervous system depression can be dangerous.
• Other hypnotics or sedatives (e.g., benzodiazepines, barbiturates): risk of profound sedation and respiratory compromise.

Moderate Interactions (Monitor Closely)

• Alcohol and CNS depressants: enhance drowsiness and impair coordination.
• CYP3A4 inducers (e.g., rifampicin, carbamazepine): may reduce therapeutic effect.
• Antidepressants (e.g., fluoxetine, sertraline): can increase sedation or affect metabolism.