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Insopin


DESCRIPTION

A yellow colour, oval shaped tablet with marking '861' &'DUO'

 

COMPOSITION

Each tablet contains Zopiclone BP 7.5 mg

PHARMACODYNAMICS

Zopiclone, a cyclopyrrolone derivative, is a short-acting hypnotic agent. Zopiclone belongs to a novel chemical class which is structurally unrelated to existing hypnotics. The pharmacological profile of zopiclone is similar to that of the benzodiazepines. PHARMACOLOGY: In sleep laboratory studies of 1 to 21-day duration in man, zopiclone reduced sleep latency, increased the duration of sleep and decreased the number of nocturnal awakenings. Zopiclone delayed the onset of REM sleep but did not reduce consistently the total duration of REM periods. The duration of stage 1 sleep was shortened, and the time spent in stage 2 sleep increased. In most studies, stage 3 and 4 sleep tended to be increased, but no change and actual decreases have also been observed, The effect of zopiclone on stage 3 and 4 sleep differs from that of the benzodiazepines which suppress slow wave sleep. The clinical significance of this finding is not known.

PHARMACOKINETICS
Absorption, Distribution and Bioavailability: Zopiclone is rapidly absorbed and distributed after oral administration, the time of maximum observed plasma concentration being about 1.75 hours. A study of 16 healthy volunteers receiving a single dose of 7.5 mg of zopiclone intravenously demonstrated the apparent volume of distribution of zopiclone to be 104 15.5 L.


Autoradiographic studies in the rat showed rapid distribution into the blood and peak tissue levels at 0.5 hours in the liver, small intestines, stomach, kidneys and the adrenals. After twenty four hours the total residual radioactivity in the body of the rat was 8%.


The bioavailability of the 7.5 mg tablets in man is 76.3 9.6%, a hepatic first pass effect has been demonstrated. In fresh human plasma, zopiclone is approximately 45% protein bound in the 25-100 ng/mL concentration range.


Metabolism: Zopiclone is extensively and rapidly metabolised by the liver. A large number of metabolites have been isolated and characterised, with the two major ones being the N-oxide, produced by oxidation of the piperazine nitrogen and the N-desmethyl produced by oxidative demethylation of the N-methyl piperazine.


Only the N-oxide analogue has weak pharmacological activity.


Elimination and Excretion: Zopiclone is rapidly eliminated, mainly by means of hepatic metabolism. The elimination half-life after a single oral dose is 5.26 0.76 hours. The elimination half-life for the N-oxide metabolite is 7.28 0.49 hours and that for the N-desmethyl metabolite is 7.28 0.49 hours. Renal clearance is 13.9 7.0 mL/min which further shows that the major elimination pathway is by hepatic metabolism. The amount of renal excretion is also low, unchanged zopiclone 3.6%, the N-oxide metabolites 11.4% and the N-desmethyl metabolite 13.4%.

 

Elderly: In elderly patients, the absolute bioavailability is increased (94% vs 77% in young subjects), and the elimination half-life prolonged (approximately 7 hours).


Hepatic insufficiency: In patients with hepatic insufficiency, elimination half-life is prolonged (11.9) and time to peak plasma levels delayed (3.5 hours).


Renal insufficiency: In patients with mild to moderate renal insufficiency, the pharmacokinetics of zopiclone are not altered. Haemodialysis does not appear to increase the plasma clearance of the drug.

INDICATIONS

Short term treatment of insomnia (2 to 4 weeks).

RECOMMENDED DOSAGE
Adults: 7.5 mg by oral administration shortly before retiring for a maximum of 2-4 weeks. This dose should not be exceeded. Depending on clinical response, the dose may be lowered to 3.75 mg.


Zopiclone is not recommended for long term use (i.e. periods of more than 4 weeks). If used for long periods, treatment should be withdrawn gradually (see Warnings).


Elderly patients: In the elderly and/or debilitated patient an initial dose of 3.75 mg is recommended. The dose may be increased to a maximum of 7.5 mg if the starting dose does not offer adequate therapeutic effect, but in clinical trials, 25% of elderly patients treated with zopiclone experienced CNS side effects at the higher dose. Zopiclone should be used with caution in these patients.


Paediatric: Zopiclone is contraindicated in children. Dosage has not been established.


Hepatic Insufficiency: The recommended dose is 3.75 mg depending on acceptability and efficacy. Up to 7.5 mg may be used with caution in appropriate cases.

 

Alternative therapy: For long term treatment of insomnia, alternative non-pharmacological methods should be considered. Effective practical management of insomnia must respond to the presenting characteristics of the complaint. Giving accurate information is a form of treatment; there is benefit in discussing some simple facts with the patient and relating them to the problem, thereby assisting the patient to place the sleep problem in its context. Sleep hygiene such as reduction of caffeine intake, should be exercised. Programmes designed to establish an optimal sleeping pattern for the patient may also be useful as are relaxation techniques designed to assist the patient deal with tension and intrusive thoughts in bed.

CONTRAINDICATIONS

Patients with known hypersensitivity to zopiclone or any of the excipients, myasthenia gravis, severe impairments of respiratory function, acute cerebrovascular accident, sleep apnoea syndrome. Zopiclone is contraindicated in children.

 

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