(and dosage form):
Each ZOPIVANE tablet contains zopiclone 7.5 mg.
A.2.2. Sedatives, hypnotics.
Zopiclone belongs to the chemical group the cyclopyrrolones, and is reported to have similar amnesic, anxiolytic, muscular relaxant, sedative and anti-convulsant properties to those of the benzodiazepines, although it is chemically distinct from them.
The pharmacological actions of zopiclone are mediated by the enhancement of the activity of aminobutyric acid (GABA) in the brain. It binds to the same receptor component of the GABA receptor in the brain as the benzodiazepines, but at a different site.
Zopiclone is rapidly absorbed following administration by mouth and widely distributed. Peak plasma concentrations are reached within 1.5 to 2 hours. Absorption is not affected by food. Zopiclone is extensively metabolized in the liver and excreted mainly in the urine as the metabolites N-desmethylzopiclone and N-oxide zopiclone, and to a lesser extent in the faeces. A small amount of unchanged zopiclone is excreted in the saliva and this may account for the bitter taste that has been reported.
Zopiclone and its metabolites are excreted in breast milk.
The accumulation of zopiclone or its metabolites on repeat dosing, in the elderly and in renal insufficiency, is not significant.
Plasma clearance is reduced by approximately 40% due to the decrease of the demethylation process in cirrhotic patients. A dose modification is indicated. The elimination half-life of unchanged zopiclone is approximately 5 hours.
Zopiclone is indicated for the short-term treatment of insomnia in adults.
Patients with a hypersensitivity to zopiclone, or suffering from myasthenia gravis, respiratory failure, severe hepatic insufficiency or severe sleep apnoea syndrome, should not use zopiclone.
Safety in pregnancy has not been established. Zopiclone should not be prescribed to nursing mothers.
Zopiclone should not be prescribed to children younger than 18 years old.
Patients with pre-existing CNS depression or coma.
Drowsiness and inco-ordination on waking may occur. Patients should be cautioned about driving motor vehicles or operating machinery, until it has been established that their performance is not affected.
DOSAGE AND DIRECTIONS FOR USE:
7.5 mg (one tablet) taken orally shortly before retiring at night.
This dose should not be exceeded.
Elderly patients and patients with hepatic and chronic respiratory insufficiency:
3.75 mg taken orally shortly before retiring at night, initially. This may be increased to 7.5 mg depending on the effectiveness and tolerance of the tablets.
Although accumulation of zopiclone has not been observed in patients with renal insufficiency, it is recommended that treatment should be initiated with 3.75 mg.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS: SIDE -EFFECTS:
A bitter metallic taste in the mouth has been reported. Sedation, ataxia, drowsiness and inco-ordination on waking, are the most frequent side-effects. They generally decrease on continued administration of zopiclone.
Less frequent side-effects may include headache, visual disturbances; slurred speech or dysarthria, confusion, vertigo, tremor, changes in libido, urinary retention or incontinence, gastro-intestinal disturbances, changes in salivation and mental depression.
Other side-effects may include blood disorders, jaundice and hypersensitivity reactions, such as pruritus and rash.
Respiratory depression and hypotension occasionally occur with high dosages.
Anterograde amnesia may occur, especially when retiring to bed is delayed, after taking ZOPIVANE, or when sleep is interrupted. To reduce the possibility of anterograde amnesia, patients should ensure that they are able to have sufficient sleep and that they take the tablet strictly when retiring for bed.
Some patients may experience paradoxical excitation which may lead to aggression, hostility, inappropriate behaviour, possibly associated with amnesia, nightmares, irritability, and hallucinations.
These reactions are more likely to occur in the elderly and may be severe.
Zopiclone should not be discontinued abruptly after regular use for even a few weeks, as withdrawal symptoms and transient insomnia, may occur. The patient should be advised that treatment should be withdrawn by gradual reduction of the dosage.
The development of dependence or abuse cannot be excluded and should be kept in mind when zopiclone is prescribed. Dependence is particularly likely in patients with a history of alcohol and/or drug abuse and in patients with marked personality disorders. The risk of dependence or abuse increases with dose and duration of treatment and the use with alcohol and other psychotropics. Zopiclone is not appropriate for the treatment of chronic psychosis or for phobic or obsessional states and may mask the symptoms of depression.
Caution is advised when zopiclone is prescribed to patients with personality disorders, organic brain changes, particularly arteriosclerosis, and to patients with muscle weakness, or impaired hepatic and kidney function.
Zopiclone should be given with care to the elderly or debilitated patients who may be more prone to adverse effects.
The sedative effects of zopiclone are most marked during the first few days of administration. Affected patients should be advised not to drive or operate machinery during this time (see "Warnings").
After repeated use, zopiclone may lose some of its efficacy.
The concomitant use of alcohol is not recommended since the sedative effect of zopiclone may be enhanced.
Caution is advised when prescribing zopiclone to patients using central depressant medication such as neuroleptics, anxiolytic/sedatives, hypnotics, antidepressant agents, antiepileptic medication, anaesthetics, narcotic analgesics and sedative antihistaminics as the central depressive effects of zopiclone may be enhanced by these agents.
Erythromycin increases the rate of absorption of zopiclone and prolongs its elimination.
Sedative effects of zoplicone may be enhanced by cisapride.
Zopiclone may be removed by dialysis.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Overdosage usually presents with varying degrees of central nervous system depression, ranging from drowsiness to coma, according to the quantity ingested. When the overdosage is combined with alcohol or other CNS depressants, it may be life-threatening. Symptomatic and supportive treatment in an adequate clinical environment, is recommended, with special attention to respiratory and cardiovascular functions. Gastric lavage is of value only if performed soon after ingestion.
Flumazenil may be useful as an antidote. Haemodialysis is of no value due to the large volume of distribution of zopiclone.
White, barrel-shaped, film-coated, biconvex tablets with a central break-line on one side and plain on the other side.
ZOPIVANE tablets are supplied in blister strips of 10 tablets, packed in 30's.
Store in a cool, dry place below 25°C. Protect from light.
KEEP OUT OF REACH OF CHILDREN.
NAME OF BUSINESS AND ADDRESS OF APPLICANT:
CIPLA MEDPRO (PTY) LTD
Pasita Street, Rosen Heights
Rosen Park, Bellville 7530, RSA
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
© 2002 Cipla Medpro (Pry) Ltd
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New addition to this site: April 2005
Source: Community Pharmacy
Current: June 2006
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