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Imovane (Zopiclone)—Hypnotic Agent for Insomnia (Rx)
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Imovane (zopiclone) is a sleep medication that helps with short-term insomnia, including trouble falling asleep, staying asleep, and waking up too early. It acts on the GABA-A receptor complex, producing sedative, anxiolytic, and muscle-relaxant effects.
Zopiclone binds to the benzodiazepine-binding site of the GABA-A receptor, enhancing the inhibitory effects of gamma-aminobutyric acid (GABA), the primary inhibitory neurotransmitter in the central nervous system. This leads to increased neuronal hyperpolarization, resulting in sedation and facilitation of sleep.
Compared to classical benzodiazepines, zopiclone demonstrates a rapid onset of action and intermediate elimination half-life, making it suitable for both sleep initiation and sleep maintenance.
Pharmacokinetics
- Absorption: Rapid oral absorption with peak plasma concentrations within 1.5–2 hours
- Bioavailability: Approximately 75–80%
- Distribution: Moderate plasma protein binding (~45%)
- Metabolism: Hepatic metabolism primarily via CYP3A4 and CYP2C8
- Elimination Half-Life: ~5 hours (prolonged in elderly and hepatic impairment)
- Excretion: Renal (as metabolites) and fecal routes
Indications
- Short-term treatment of insomnia
- Sleep-onset insomnia
- Sleep-maintenance insomnia
- Nocturnal awakenings
Dosage & Administration
- Adults: 7.5 mg orally immediately before bedtime
- Elderly / hepatic impairment: Initiate at 3.75 mg
- Administer once nightly, ensuring at least 7–8 hours available for sleep
- Duration of therapy typically limited to 2–4 weeks
Vasta-aiheet
- Hypersensitivity to zopiclone
- Severe respiratory insufficiency
- Severe hepatic impairment
- Sleep apnea syndrome
- Myasthenia gravis
Adverse Effects
- Common: Bitter or metallic taste (dysgeusia), dry mouth, drowsiness
- CNS: Dizziness, headache, confusion, amnesia
- Behavioral: Abnormal sleep-related behaviors (rare)
- Residual sedation, particularly in elderly patients
Lääkkeiden yhteisvaikutukset
- CNS depressants (e.g., opioids, alcohol): Enhanced sedation
- CYP3A4 inhibitors (e.g., erythromycin, ketoconazole): Increased plasma levels
- CYP3A4 inducers (e.g., rifampicin): Reduced efficacy
Why Choose Imovane?
Imovane (zopiclone) remains a widely used hypnotic agent due to its effectiveness in both initiating and maintaining sleep. Its drug properties provide a good mix of effectiveness and how long it lasts, making it a popular choice for treating insomnia when short-term medication is needed.