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Zopiclone

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4 sources

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🔗 MergedComparePsychonautWikiTripSitPharmacologyDrugCentral

Collated from PsychonautWiki, TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.

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HallucinogenDepressantCyclopyrroloneHabit-formingCommonPW

Also known as Zimovane, ImovanePW

Fatal overdose may occur when GABAergic substances are combined with other depressants such as opiates, benzodiazepines, barbiturates, gabapentinoids, thienodiazepines or alcohol.[1] It is strongly discouraged to combine these substances, particularly in common to heavy doses.PW

Addiction potentialPW
extremely physically and psychologically addictive
ToxicityPW
low toxicity; potentially lethal when mixed with depressants like benzodiazepines, alcohol or opioids
TolerancePW
full tolerance within a couple of weeks of daily use; baseline after 7 - 14 days
Cross-tolerancePW
benzodiazepines

Oral

Route dataPsychonautWiki

Dose
WeakerStronger
ThresholdLightCommonStrongHeavy
2 mg3.5–5 mg5–7.5 mg7.5–15 mg15 mg+
018.75 mg
LightCommonStrongHeavy
Duration
ShorterLonger
Onset10–30 minutes
Peak3–4 hours
Total3.5–9 hours
OnsetCome-upPeakOffset

🧬 Receptor activityDC

TargetActionAffinitySource
GABA A receptor alpha-3/beta-2/gamma-2 (GABRG2)Positive modulator6.582 KiDRUGCENTRAL
GABA A receptor alpha-3/beta-2/gamma-3 (GABRA3)Positive modulator6.488 KiDRUGCENTRAL
GABA A receptor alpha-5/beta-2/gamma-2 (GABRG2)Positive modulator7.278 KiDRUGCENTRAL
GABA A receptor alpha-5/beta-2/gamma-3 (GABRA5)Positive modulator6.75 KiDRUGCENTRAL
GABA A receptor alpha-5/beta-3/gamma-3 (GABRB3)Positive modulator6.75 KiDRUGCENTRAL
GABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1)Positive modulator7.176 KiDRUGCENTRAL
GABA-A receptor alpha-1/beta-2/gamma-3 (GABRA1)Positive modulator7.155 KiDRUGCENTRAL
GABA-A receptor alpha-5/beta-3/gamma-2 (GABRG2)Positive modulator7.278 KiDRUGCENTRAL
GABA-A receptor; anion channel (Gabrp)—7.54 IC50DRUGCENTRAL
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Mechanism of actionPH

Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex. Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on α1, α2, α3 and α5 GABAA containing receptors as full agonists causing an enhancement of the inhibitory actions of GABA to produce the therapeutic (hypnotic and anxiolytic) and adverse effects of zopiclone.

PharmacodynamicsPH

Zopiclone is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABA<sub>B</sub>Z) receptor complex. Subunit modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.

Pharmacokinetics

Half-lifePH

Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.

AbsorptionPH

Rapidly absorbed following oral administration.

MetabolismPH

Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance.
Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance.
Half Life: Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.

Protein bindingPH

Approximately 45%

Plan when to take Zopiclone — see where onset, peak and comedown land on the clock

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.