Imovane (Zopiclone): Dosage, Side Effects, Interactions
The active ingredient zopiclone belongs to the group of active ingredients called Z-substances (also known as Z-drugs) and is used for the short-term treatment of sleep disorders. The hypnotics act as agonists on GABAA receptors and are therefore sleep-inducing.
Zopiclone is indicated for the short-term treatment of insomnia in adults and should only be used for insomnia of clinically significant severity.
The active ingredient zopiclone is approved on the US market in the form of film-coated tablets in strengths of 3.75 and 7.5 mg.
When prescribing Z substances, just like when prescribing benzodiazepines:
- Use only if there is a clear indication.
- Application of the smallest possible dose.
- Application over the shortest possible period.
- No abrupt stop.
- Contraindications must be observed.
How Imovane Zopiclone works
The active ingredient Zopiclone is chemically a cyclopyrrolone derivative. Zopiclone interacts with the α and γ subunits of the GABA A receptor. The consequence of this interaction with the GABA A receptor is the enhancement of the responses to GABA, which could be shown by electrophysiological methods.
- Muscle relaxant
Compared to the benzodiazepines, zopiclone apparently has less of an impact on sleep architecture, and the REM sleep phases in particular seem to be less affected.
After oral administration, zopiclone is rapidly absorbed, reaching maximum plasma levels after 1.5 to 2 hours. The absorption is gender-unspecific and is not influenced by the time of administration or the frequency of administration.
Zopiclone is rapidly distributed from the central compartment in the organism. At around 45 percent, plasma protein binding is relatively low and cannot be saturated. The risk of drug interactions due to plasma protein binding should therefore be very low. During lactation, the pharmacokinetic profiles in blood plasma and breast milk are similar, ie the infant would receive approximately 1 percent of the mother’s daily dose.
Zopiclone does not accumulate after repeated dosing and the inter-individual variation appears to be small. Zopiclone is essentially metabolized into two metabolites: zopiclone N-oxide, which is pharmacologically active in animal models (plasma half-life: 4.4 hours) and non-active N-desmethyl-zopiclone (plasma half-life: 7.3 hours). Results from in vitro studies indicate that metabolism occurs mainly via the isoenzyme cytochrome P450 (CYP) 3A4 . CYP2C8 also seems to be involved in the formation of N-desmethyl-zopiclone .
The elimination half-life is approximately 5 hours. The decrease in the plasma level is dose-independent (in the range of the therapeutic dose). Zopiclone is mainly eliminated in the metabolised form, as shown by the low renal clearance of unchanged zopiclone (mean 8.4 ml/min) and a plasma clearance of 232 ml/min. About 80 percent of the substance and its metabolites are eliminated via the kidneys and about 16 percent with the faeces.
In numerous studies, no accumulation could be observed in elderly patients despite a slightly delayed hepatic metabolism and a longer elimination half-life of zopiclone (approx. 7 hours), even after repeated administration. Even in renal insufficiency, no accumulation of zopiclone or its metabolites was found, even after long-term administration. Zopiclone is also dialysable. In patients with impaired liver function, the plasma clearance of zopiclone is markedly reduced due to a slowing down of demethylation. A dose reduction should therefore be made in these patients.
Dosage of Imovane
The recommended daily dose of zopiclone is 7.5 mg once a day. In general, the lowest effective dose should be used.
Side effects of Imovane Zopiclone
The following side effects occur frequently (≥ 1/100 to < 1/10) when using Zopiclone:
- Taste disturbance (bitter taste)
- Drowsiness the following day
- Dry mouth.
The following interactions exist for the use of zopiclone:
- Opioids ► Risk of sedation, respiratory depression, coma and death due to an additive CNS depressant effect is increased
- Sedatives, hypnotics, analgesics , narcotics, anesthetics, neuroleptics , antiepileptics , anxiolytics, sedative antihistamines , antidepressants , lithium preparations ► mutual reinforcement of the central depressant effect
- Narcotic analgesics ► Intensification of the euphoric effect and thus accelerated development of dependence possible
- Muscle relaxants ► the relaxing effect is increased
- CYP3A4 inhibitors (eg, cimetidine , erythromycin , clarithromycin , ketoconazole , itraconazole , ritonavir ) ► increase in plasma levels of zopiclone
- CYP3A4 inducers (e.g. rifampicin , carbamazepine , phenobarbital , phenytoin , St. John’s wort ) ► Decrease in plasma levels of zopiclone
- Alcohol ► No alcohol should be drunk during treatment with zopiclone, as this can alter and intensify the effect of zopiclone in an unpredictable manner. The ability to drive and use machines is also affected by this combination.
Zopiclone must not be used:
- in case of hypersensitivity to the active substance
- in myasthenia gravis
- with severe respiratory failure
- with severe sleep apnea syndrome
- in severe hepatic insufficiency (due to the risk of encephalopathy)
- in children and adolescents under the age of 18
- during breastfeeding.
When used in the last three months of pregnancy, before or during childbirth, zopiclone can lead to a drop in body temperature, a drop in blood pressure and respiratory depression, reduced muscle tone and poor feeding in the newborn.
Prolonged use late in pregnancy can result in physical dependence in the newborn and the associated risk of postnatal withdrawal symptoms. Zopiclone is not recommended throughout pregnancy.
Zopiclone must not be used during breast-feeding, even if the concentration of zopiclone in breast milk is very low.
Because zopiclone causes sedation and its effects on the central nervous system, there is a risk of amnesia, reduced concentration and impaired muscle function, zopiclone may have an adverse effect on the ability to drive or use machines. Activities such as driving and operating machines should therefore be avoided for at least 12 hours after taking zopiclone.
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