Pharmacokinetics

Zopiclone is
rapidly absorbed following administration by mouth and widely
distributed. It has an elimination half-life of 3.5 to 6.5 hours and is
reported to be about 45 to 80% bound to plasma proteins. Zopiclone is
extensively metabolised in the liver; the 2 major metabolites, the less
active zopiclone N-oxide and the inactive N-desmethylzopiclone are
excreted mainly in the urine. About 50% of a dose is converted by
decarboxylation to inactive metabolites which are partly eliminated via
the lungs as carbon dioxide. Only about 5% of a dose appears unchanged
in the urine and about 16% appears in the fasces. Excretion of zopiclone
in the saliva may explain reports of a bitter taste. It is also
distributed into breast milk.

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Indication
& Dosage

INSOMNIA:
7.5mg at night. Some patient may need 15mg.
Elderly patients may be given 3.75mg at night. Severe hepatic
insufficiency: 3.75mg at night. Duration of treatment not to exceed 28
days.

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Action

Hypotic and sedative actions, anticonvulsant
and muslcle relaxant
properties similar to benzodiazepines. Bind to a site in the
GABA-A-benzodiazepine-chloride channel macro-molecular receptor complex,
but different from that of the benzodiazephine binding site. Zopiclone
does not alter REM sleep but prolongs stages 3 & 4. Psychomotor
functions are impaired to some extent.

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Interactions
Metoclopramide: Concomitant administration may increase the plasma
concetration of zopiclone.
Atropine: May decrease its plasma concentration, when given
concurrently.
Trimipramine: If given along with Zopiclone may result in lessened
antidepressant effect of the former.

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Adverse
Effects & Precaution

Metallic or
bitter after-taste, nausea, vomiting, allergic skin reactions,
irritability, hallucinations, depression, amnesia and confusion.

Precaution: Patients of severe hepatic insufficiency.
Pregnancy:  Use with caution
Breast Feeding: Contraindicated
Man : May be given in reduced dose

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Brand
available in market

LYZOP

 

 

Lyka

TAB

7.5mg

10

38.00

SOMNA

 

 

Brown & Burk

TAB

7.5mg

10

38.00

ZICLONE

 

 

Bal Pharma

TAB

7.5mg

10

48.00

ZOLINOX

 

 

Solus

TAB

7.5mg

10

45.50

ZOLIUM

 

 

FDC

TAB

7.5mg

10

36.50

ZONAP

 

 

Unisearch

TAB

7.5mg

10

45.25

ZOPICON

 

 

Intas

TAB

7.5mg

10

50.75

 

Pharmacokinetics

Zopiclone is rapidly absorbed following administration by mouth and widely distributed. It has an elimination half-life of 3.5 to 6.5 hours and is reported to be about 45 to 80% bound to plasma proteins. Zopiclone is extensively metabolised in the liver; the 2 major metabolites, the less active zopiclone N-oxide and the inactive N-desmethylzopiclone are excreted mainly in the urine. About 50% of a dose is converted by decarboxylation to inactive metabolites which are partly eliminated via the lungs as carbon dioxide. Only about 5% of a dose appears unchanged in the urine and about 16% appears in the fasces. Excretion of zopiclone in the saliva may explain reports of a bitter taste. It is also distributed into breast milk.

Top

Indication & Dosage

INSOMNIA: 7.5mg at night. Some patient may need 15mg. Elderly patients may be given 3.75mg at night. Severe hepatic insufficiency: 3.75mg at night. Duration of treatment not to exceed 28 days.

Top

Action

Hypotic and sedative actions, anticonvulsant and muslcle relaxant properties similar to benzodiazepines. Bind to a site in the GABA-A-benzodiazepine-chloride channel macro-molecular receptor complex, but different from that of the benzodiazephine binding site. Zopiclone does not alter REM sleep but prolongs stages 3 & 4. Psychomotor functions are impaired to some extent.

Top

Interactions
Metoclopramide: Concomitant administration may increase the plasma concetration of zopiclone.
Atropine: May decrease its plasma concentration, when given concurrently.
Trimipramine: If given along with Zopiclone may result in lessened antidepressant effect of the former.

Top

Adverse Effects & Precaution

Metallic or bitter after-taste, nausea, vomiting, allergic skin reactions, irritability, hallucinations, depression, amnesia and confusion.

Precaution: Patients of severe hepatic insufficiency.
Pregnancy: Use with caution
Breast Feeding: Contraindicated
Man : May be given in reduced dose

Top

Brand available in market

LYZOP

Lyka

TAB

7.5mg

10

38.00

SOMNA

Brown & Burk

TAB

7.5mg

10

38.00

ZICLONE

Bal Pharma

TAB

7.5mg

10

48.00

ZOLINOX

Solus

TAB

7.5mg

10

45.50

ZOLIUM

FDC

TAB

7.5mg

10

36.50

ZONAP

Unisearch

TAB

7.5mg

10

45.25

ZOPICON

Intas

TAB

7.5mg

10

50.75