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Zopiclone - Insomnia Medication

Discussion in 'Medications & Substances' started by batgirl, Apr 25, 2007.

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  1. batgirl

    batgirl I'm a VIP

    IMOVANE Aventis

    Generic Name: Zopiclone


    The short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings and/or early morning awakening. As with all hypnotics, long-term continuous treatment is not recommended and a course of treatment should be no longer than 4 weeks in duration.


    Patients with known hypersensitivity to the drug; myasthenia gravis; severe impairment of respiratory function; acute cerebrovascular accident.


    Drug Interactions: Patients should be cautioned against the simultaneous ingestion of zopiclone and alcohol or other CNS depressant drugs because of possible additive effects.

    Abuse and Dependence: In monkeys, zopiclone was self-administered and caused mild to moderate withdrawal signs. In human subjects only limited data are available to-date regarding the dependence liability of zopiclone. In chronic alcoholics, zopiclone elicited similar effects to those of triazolam. In normal subjects, changes in sleep pattern and rebound anxiety appeared upon discontinuation of the drug. Addiction-prone individuals, such as drug addicts and alcoholics, should be under careful surveillance when receiving zopiclone because of the predisposition of such patients to habituation and dependence. Patients with a history of seizures should not be abruptly withdrawn from any CNS depressant drug, including zopiclone.

    Amnesia: Anterograde amnesia of varying severity may occur in rare instances following therapeutic doses of zopiclone. Also prior to falling asleep or during interim periods of wakefulness, memory may be impaired.

    Geriatrics/Debilitated Patients: In elderly and/or debilitated patients, zopiclone should be initiated at a low dose to reduce the possibility of oversedation, dizziness or impaired coordination. The dose should be increased only if necessary.

    Children: Safety and effectiveness in patients under 18 years of age have not been established.

    Pregnancy: The safety of zopiclone in pregnant women has not been established. Therefore, the drug is not recommended during pregnancy.

    Zopiclone is secreted in human milk, and its concentration may reach 50% of the plasma levels. Therefore, the administration of zopiclone to nursing mothers is not recommended.


    Residual effects of zopiclone were assessed by psychomotor and cognitive performance tests in adult and geriatric insomniac patients as well as in young volunteer subjects. The doses ranged from 2.5 mg to 15 mg and drug effect was evaluated between 9 and 13 hours after ingestion. The impairment of performance was dose-related. Doses less than 7.5 mg caused no residual effects. The clinically recommended dose of 7.5 mg caused no or slight impairment in psychomotor performance. Doses above 7.5 mg clearly showed residual effects. The 15 mg dose also produced serious untoward effects that included drowsiness, amnesia, disturbed balance, blurred vision and long-lasting sedation attested by the Multiple Sleep-Latency Test.

    Occupational hazards: Patients should be cautioned against driving an automobile or performing hazardous tasks until they are reasonably certain that treatment with zopiclone does not affect them adversely.

    Caution should be exercised if zopiclone is prescribed to depressed patients, including those with latent depression, particularly when suicidal tendencies may be present and protective measures may be required.

    Zopiclone should be given with caution to patients with impaired hepatic function.

    Adverse Effects

    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.

    The following adverse events were observed in patients receiving zopiclone. In the absence of an established cause-effect relationship those adverse reactions that were observed more frequently with zopiclone than with a placebo are in brackets.

    CNS: (somnolence), (asthenia), dizziness, (confusion), (anterograde amnesia or memory impairment), (feeling of drunkenness), (euphoria), nightmares, agitation, (anxiety or nervousness), hostility, (depression), decreased libido, (coordination abnormality), (hypotonia), tremor, muscle spasms, paresthesia, (speech disorder).

    Cardiovascular: Palpitations.

    Digestive: Dry mouth, (coated tongue), (bad breath), nausea, vomiting, dyspepsia, diarrhea, (constipation), (anorexia or increased appetite).

    Respiratory: Dyspnea.

    Special Senses: Amblyopia.

    Dermatologic: Rash, spots on skin, sweating. Rashes may be a sign of drug hypersensitivity; discontinue if this occurs.

    Metabolic and Nutritional:
    Weight loss.

    Others: (bitter taste), headache, limb heaviness, chills.

    Laboratory Tests: There have been sporadic reports of abnormal laboratory test values including increase in AST (SGOT), ALT (SGPT) or alkaline phosphatase values.

    Geriatrics: Geriatric patients tended to have a higher incidence of palpitations, vomiting, anorexia, sialorrhea, confusion, agitation, anxiety, tremor and sweating than younger patients.


    Drug Class: Hypnotic

    Zopiclone, a cyclopyrrolone derivative, is a short-acting 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 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.

    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.

    In man, zopiclone is rapidly and well absorbed by the oral route. In a dose range of 3.75 to 15 mg, there is a linear relationship between dose and maximum concentration (C(max)) and bioavailability (AUC), while terminal elimination half-life is not dose-dependent and time to peak plasma levels (T(max)) increases only slightly with increasing doses. At the clinically recommended dose of 7.5 mg, peak plasma concentration of 60 ng/mL is achieved within 90 minutes and bioavailability is more than 75%, indicating the absence of a significant first-pass effect.

    The distribution of zopiclone follows a two-compartment model; distribution from the vascular compartment is rapid (distribution half-life: 1.2 hours) while the elimination half-life is approximately 5 hours (range: 3.8 to 6.5 hours). 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.

    In fresh human plasma, zopiclone is approximately 45% protein bound in the 25 to 100 ng/mL concentration range.

    Zopiclone is extensively metabolized by 3 major pathways; only about 4 to 5% of the drug is excreted unchanged in the urine. The metabolic pathways include oxidation to the N-oxide (approx. 12%), demethylation to N-desmethyl zopiclone (approx. 16%) and oxidative decarboxylation to various metabolites. The N-oxide and N-desmethyl analogues are excreted renally, the products of decarboxylation are partly eliminated via the lung as carbon dioxide. Only the N-oxide analogue has weak pharmacological activity. Excretion studies, using (14)C-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.

    In elderly subjects, the absolute bioavailability of zopiclone was increased (94% vs 77% in young subjects) and the elimination half-life prolonged (approx. 7 hours). In patients with hepatic insufficiency, elimination half-life was substantially prolonged (11.9 hours) and time to peak plasma levels delayed (3.5 hours). Mild to moderate renal insufficiency did not alter the pharmacokinetics of zopiclone. Hemodialysis did not appear to increase the plasma clearance of the drug. In lactating women, zopiclone was present in the milk, its concentration paralleled plasma levels but was about 50% lower.

    Source: Internet Mental Health
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  3. batgirl

    batgirl I'm a VIP

    I don't know if I'm supposed to be leaving a comment here, but the main reason I'm posting this medication is it's a relatively new drug and apparently now widely prescribed according to my new psychiatrist. He prescribed it to me 2 days ago for my insomnia, but when we went to the druggists today to fill the prescription, we were told by the druggist suicidal thoughts are common on zopiclone. So obviously I didn't have the prescription filled.
  4. anthony

    anthony Silently Watching Founder

    And people wonder why I have no respect for 90% of physicians. They prescribe a pill with high suicidal ideation to someone with PTSD which encompasses depression and suicidal ideation as it is. They wonder why people fall over the edge and end up killing themselves.

    Nice post Evie...
  5. AmberG

    AmberG New Member

    I actually just made an account here so I could respond to this post.

    I take Zoplicone occasionally because I have trouble getting to sleep and staying asleep. Not sleeping or not staying asleep became a hazard to my health because I would wake up every 30 minutes or so and immediately make myself something to eat. I gained a lot of weight that I have since been able to shed.

    Sometimes I just couldn't get to sleep at all, no matter how tired I was. I have to say, I have never experienced suicidal thoughts. Maybe because I only take half a tablet when needed. I find that once I have taken it at half tab for at least 2 days, I can get to sleep on my own. Unfortunately that only lasts for a few weeks, then I have to do the 2 or 3 day thing again. I don't find it to be a hassle tho.

    The only problem I have with it is the taste. It lingers, sometimes even bottled water will taste bad to me the next day, but honestly that is the only downfall of the pill for me. I had gotten as heavy as 272 pounds due to my "sleep eating" ( I call it that because I wouldn't remember eating unless my husband told me )

    Since I started sleeping properly, I have been able to shed 22 of those pounds in just 2 months, I'm not saying take it to lose weight because you all may not have the same issues as myself, but I don't eat at night anymore because I am sleeping comfortably.. I am saying that sleep is healthy and if you're not getting it then you will suffer. I never feel un-rested after waking up from this Zoplicone, I have never thought of taking my own life while taking Zoplicone. But like I said, it could be because I am taking only half a tab and not on a nightly basis. I am sure it affects every one differently.
    Last edited by a moderator: Sep 6, 2013
  6. cherryblossom

    cherryblossom I'm a VIP Premium Member Donated

    I had the same thing with zopiclone - I switched to zolpidem, which had the same sedative effect, but no nasty taste in my mouth. It might be worth you trying it instead.
  7. cavy

    cavy Active Member

    Hi, I took zopiclone for a couple of years, no side effects at all.

    This drug only works for the first 20 minutes - getting you to sleep. It doesn't keep you asleep.
  8. twopenny

    twopenny Active Member

    Hub was prescribed this to help him sleep, when his nightmares and night time flashbacks were at their worst, and he was getting very little sleep indeed. It gave him major depression and suicidal thoughts (which he'd just got past - this brought them back, and they went away again as soon as he stopped taking it).

    He also said it made him feel groggy for days after taking it. He still has some in reserve, just in case, but hasn't taken any in years - he'd rather take night nurse, or those herbally over the counter sleeping pills (which probably work on the placebo principle). Last time he did take one he said he felt like a zombie for about three days, and as though he couldn't keep up with what was going on around him.

    I'd imagine it's like most drugs - good for some, rubbish for others, but I agree, giving people with PTSD pills that are know to cause suicidal thoughts is insane.
    cavy likes this.
  9. cavy

    cavy Active Member

    I thought we were meant to be the mad ones not the phsychiatrists!!! :joyful:
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