Medical  Explorer

Custom Search

Drugs A to Z  :  A  B  C  D  E  F  G  H  I  J  K  L  M  N  O  P  R  S  T  U  V  W  X  Y  Z
Medicinal Ingredients : A  B  C  D  E  F  G  H  I  J  K  L  M  N  O  P  Q  R  S  T  U  V  W  X  Y  Z

Beauty Products : A  B  C  D  E  F  G  I  M  N  O  P  R  S  T  V

Aging      Allergies     Alzheimer's      Arthritis    Asthma      Bacteria   new Cancer    Chickenpox     Colds     Constipation      Diabetes      Epilepsy     Fatigue     Fever     Genetics       Haemorrhoids       newHeadaches      Hepatitis    Immunity      Infection      Insomnia       Leprosy       Menopause      Obesity      Osteoporosis     Other Diseases    Pain      PMS     Parasites     Sinusitis     newStroke     Toxicology    Urology

Arthritis medications
newGeneral Health
Medicinal food
Chinese medicine
OTC Drugs
Health Products


Zopiclone Tablets 7.5 mg

Zopiclone, a cyclopyrrolone derivative, is a shortacting hypnotic agent. Zopiclone belongs to a novel chemical class which is structurally unrelated to existing hypnotics However. the pharmacological profile of zopiclone is similar to that of the benzodiazepines.

In sleep laboratory studies of one 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 differs from that of the benzodiazepines which suppresses slow wave sleep. The clinical significance of this finding is not known. With hypnotic drugs, the duration of hypnotic effect and the profile of unwanted effects may be influenced by the alpha (distribution) and beta (elimination) half-lives of the administered drug and any active metabolites formed. When halt-lives are long, the drug or metabolite may accumulate during periods of nightly administration and be associated with impairments of cognitive and motor performance during waking hours. If half-lives are short, the drug and metabolites will be cleared before the next dose is ingested, and carry-over effects related to sedation or CNS depression should be minimal or absent. If the drug has a very short elimination half-life, it is possible that a relative deficiency (i.e., in relation to the receptor site) may occur at some point in the interval between each night's use. This sequence of events may account for two clinical findings reported to occur after several weeks of nightly use of rapidly eliminated benzodiazepines or benzodiazepine-like hypnotics : 1) increased wakefulness during the last third of the night and 2) the appearance of increased daytime anxiety.

During nightly use and for an extended period, pharmacodynamic tolerance or adaptation to some effects of benzodiazepines or benzodiazepine-like hypnotics may develop. However, in two sleep laboratory studies involving 17 patients, there was an absence of tolerance with zopiclone for treatment periods of more than 4 weeks.


Rebound Insomnia
A transient syndrome whereby the symptoms that led to treatment with a benzodiazepine or benzodiazepine-like agent recur in an enhanced form, may occur on withdrawal of hypnotic treatment.

Some manifestations of rebound insomnia have been reported both in sleep laboratory and clinical studies following the withdrawal of zopiclone. Zopiclone treatment was associated with dose-related residual effects.

Absorption : Zopiclone is rapidly and well absorbed. Bio-availability is more than 75%, indicating the absence of a significant first-pass effect. After the administration of 3.75 and 7.5 mg doses, peak plasma concentrations of 30 and 60 ng/ml, respectively were reached in less than 2 hours. Absorption was similar in males and females. Repeated daily administration of a 7.5 mg oral dose for 14 days did not change the pharmacokinetic characteristics of zopiclone and did not lead to accumulation.


Distribution : Zopiclone is rapidly distributed from the vascular compartment (distribution half-life [ta] : 1.2 hours) while the elimination half-life is approximately 5 hours (range : 3.8 to 6.5 hours). Plasma protein binding is low (approximately 45% in the 25 - 100 ng/ml concentration range) and non saturable. The risk of drug interaction arising from displacement of bound drug is low.


Metabolism : Zopiclone is extensively metabolized by three major pathways; only about 4 to 5% of the drug is excreted unchanged in the urine. The principal metabolites are the N-oxide derivative (~12%) which has weak pharmacological activity in animals, and the N-desmethyl metabolite (~16%) which is pharmacologically inactive. Their apparent halt-lives evaluated from the urinary data are approximately 4.5 and 7.4 hours, respectively. Both metabolites are excreted renally. Other metabolites resulting from oxidative decarboxylation are partly eliminated via the lung as carbon dioxide. In animals, zopiclone did not induce hepatic microsomal enzymes.

Excretion : Excretion studies, using C14-zopiclone have shown that more than 90% of the administered dose was excreted over a period of 5 days, 75% being eliminated in the urine and 16% in the feces. The low renal clearance of unchanged zopiclone (mean 8.4 ml/min) compared with that of plasma (232 ml/min) indicates that zopiclone clearance is mainly metabolic.

Special Patient Population
Elderly Subjects : The absolute bioavailability of zopiclone was increased (94% vs 77% in young subjects) and the elimination half-life prolonged (~7 hours). Accumulation has not been observed on repeated dosing.

Patients with Hepatic Insufficiency : Elimination half-life was substantially prolonged (11.9 hours) and time to peak plasma levels delayed (3.5 hours). Consequently, lower doses are recommended.


Patients with Mild to Moderate Renal Insufficiency : The pharmacokinetics of zopiclone were not affected. Hemodialysis did not appear to increase the plasma clearance of the drug.


Lactating Women : Zopiclone was present in the milk, its concentration paralleled plasma levels but was about 50% lower.

Sleep disturbance may be the presenting manifestation of a physical and/or psychiatric disorder. Consequently, a decision to initiate symptomatic treatment of insomnia should only be made after the patient has been carefully evaluated.

APO-ZOPICLONE (zopiclone) is indicated for the symptomatic relief of transient and short-term insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings and/or early morning awakenings.

Treatment with APO-ZOPICLONE should usually not exceed 7-10 consecutive days. Use for more than 2-3 consecutive weeks requires complete reevaluation of the patient.

Prescriptions for APO-ZOPICLONE should be written for short-term use (7 - 10 days) and it should not be prescribed in quantities exceeding a 1-month supply.

The use of hypnotics should be restricted for insomnia where disturbed sleep results in impaired daytime functioning.

The most common adverse reaction seen with zopiclone is taste alteration (bitter taste). Severe drowsiness and/or impaired coordination are signs of drug intolerance or excessive doses.

1    2    3











Health news
Cardiovascular Guide
Natural Remedies
Treatment of Cancer
Women's Health
Irritable bowel syndrome
Common Childhood Illnesses
Prescribed Drugs