INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo ZOPIMED (tablets)
SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form):

ZOPIMED (tablets)

COMPOSITION:
Each tablet contains 7,5 mg Zopiclone.

PHARMACOLOGICAL CLASSIFICATION:
A: 2.2 Sedatives, hypnotics.

PHARMACOLOGICAL ACTION:
Zopiclone is a member of the cyclopyrrolone group of compounds and acts as a hypnotic agent. It also has sedative, anxiolytic, anticonvulsant, and muscle-relaxant pharmacological properties. These effects are related to a specific agonist action at central receptors in the GABAA macromolecular complex, which modulates the opening of the chloride ion channel.
Zopiclone is rapidly absorbed. After administration of 3,75 mg and 7,5 mg, peak concentrations of approximately 30 to 60 ng/mL respectively are reached within 1,5 to 2 hours. Food intake does not affect absorption.
Zopiclone is rapidly distributed from the vascular compartment. Zopiclone is weakly bound to plasma proteins (approximately 45%) and non-saturable. Risk of drug interactions due to protein binding is very limited. The volume of distribution is 91,8 to 104,6 litres.
No accumulation of zopiclone and its metabolites occurs after repeated administration. Few interindividual variations were observed.
The elimination half-life of unchanged zopiclone at recommended doses, is approximately 5 hours.
Comparison of the low renal clearance value of unchanged zopiclone (mean 8,4 mL/min) and the plasma clearance (232 mL/min) shows that zopiclone clearance is predominantly metabolic. Approximately 80% of zopiclone is eliminated by the urinary route, mainly in the form of free metabolites (N-oxide and N-demethyl derivates), while approximately 16% is eliminated in the faeces.
Various studies conducted with elderly patients have not shown plasma accumulation of the drug substance on repeated dosing, a slight decrease in hepatic metabolism and increase in elimination half-life to approximately 7 hours.
No accumulation of zopiclone or of its metabolites has been found after prolonged administration in patients with renal insufficiency. Haemodialysis is effective in removing zopiclone.
Plasma clearance of zopiclone in patients with cirrhosis is decreased by approximately 40% corresponding to decreased demethylation. Dosage modification is, therefore, recommended in these patients.

INDICATIONS:
Short term treatment of insomnia in adults.

CONTRA-INDICATIONS:
Patients with a hypersensitivity to zopiclone, myasthenia gravis, respiratory failure, severe sleep apnoea syndrome and severe hepatic insufficiency, should not be treated with zopiclone.
Zopiclone is contra-indicated in persons under the age of 18.
Safety in pregnancy and lactation has not been established.

WARNING:
Patients may experience drowsiness and incoordination on waking. Caution patients about driving motor vehicles or operating machinery until it has been established that their performance is not affected by zopiclone.

DOSAGE AND DIRECTIONS FOR USE:
Adults:
One tablet (7,5 mg zopiclone) orally, shortly before retiring. Do not exceed this dose.
Elderly patients, and patients with impaired liver function or chronic respiratory insufficiency:
Initiate treatment with a lower dose of 3,75 mg zopiclone (half a tablet) in these patients. The dose may be increased to 7,5 mg if required.
Renal insufficiency:
No accumulation of zopiclone or its metabolites has been observed during treatment of insomnia in patients with renal insufficiency. However, treatment of patients with impaired renal function should be initiated using 3,75 mg zopiclone.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects:
The most common side-effect with zopiclone is a bitter after-taste. Other side-effects include dizziness, headache, residual somnolence, digestive disturbances such as dyspepsia, nausea and dry mouth, and allergic or cutaneous reactions such as pruritus and rash.
Patients whose sleep is interrupted or those who do not retire to bed promptly after taking the tablet, are more likely to experience anterograde amnesia. By ensuring that they take the tablet strictly when retiring for the night and are able to have a full night's sleep, patients can reduce the possibility of anterograde amnesia.
Psychiatric Reactions:
Psychiatric reactions such as nightmares, irritability, confusion, hallucinations, aggressiveness and inappropriate behaviour possibly associated with amnesia, have also occurred. If such reactions occur, they may be severe. They occur more frequently in elderly patients.
Abrupt discontinuation, especially after prolonged treatment with zopiclone, has led to withdrawal symptoms and transient rebound insomnia. The dosage should be decreased gradually and patients should be advised on how to discontinue this medicine.
Some patients may experience drowsiness and incoordination on waking.
Special Precautions:
Pharmacodependence or abuse may develop and this possibility should be borne in mind when zopiclone is prescribed. Dose and duration of treatment, history of alcohol and/or drug abuse, and use with alcohol or other psychotropics, may increase the risk of dependence or abuse.
Repeated use of zopiclone may reduce its efficacy.
Zopiclone should not be used as a treatment for depression and its use may even mask the symptoms of depression.
Concomitant intake with alcohol should be avoided as this may enhance the sedative effect of zopiclone. If used concomitantly with central depressant medicines such as neuroleptics, hypnotics, anxiolytics/sedatives, antidepressants, narcotic analgesics, anti-epileptic drugs, anaesthetics and sedative antihistaminics, caution is recommended. The central depressive effect of zopiclone may be enhanced in these circumstances.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
In the event of overdose, varying degrees of central nervous system depression ranging from drowsiness to coma, as determined by the quantity ingested, may occur. Overdose may be potentially fatal especially when combined with other CNS depressants (including alcohol). Symptomatic and supportive treatment in an adequate clinical environment should be provided and respiratory and cardiovascular functions must be monitored. Provided that gastric lavage is performed soon after ingestion, it can be beneficial. Haemodialysis is not useful because zopiclone has a large volume of distribution. Flumazenil may be a useful antidote.

IDENTIFICATION:
A white, elliptical, film-coated tablet, scored on one side.

PRESENTATION:
Blister packs of 30 and 300 tablets.

STORAGE INSTRUCTIONS:
Store below 25°C. Do not expose to direct sunlight. Store tablets in the outer carton until required for use.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER:
33/2.2/0450

NAME AND BUSINESS ADDRESS OF APPLICANT:
Parke-Med, Division of
Warner-Lambert S.A. (Pty) Ltd.
241 Main Road,
RETREAT
7945

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
24 September 1999.

904G585

New addition to this site: October 2000
Current: March 2005
Source: Community Pharmacy

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