Zopiclone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Insomnia
Adult: 7.5 mg once daily at bedtime for up to 4 weeks. Dose may be reduced to 3.75 mg according to clinical response.
Elderly: Initially, 3.75 mg once daily at bedtime, may increase dose to 7.5 mg once daily if necessary.
Special Patient Group
Patients with chronic respiratory insufficiency; Debilitated patients: Initially, 3.75 mg once daily at bedtime, may increase dose to 7.5 mg if necessary.
Renal Impairment
Initially, 3.75 mg once daily at bedtime.
Hepatic Impairment
Mild to moderate: Initially, 3.75 mg once daily at bedtime. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Respiratory failure, severe sleep apnoea, myasthenia gravis, acute stroke. Severe hepatic impairment. Lactation.
Thận trọng
Patient with psychiatric disorder (e.g. depression), chronic respiratory disease; personal or family history of sleepwalking or disorders that affect sleep (e.g. restless leg syndrome, periodic limb movement); history of drug abuse or alcoholism, risk of falls. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy. Not indicated for long-term treatment of insomnia. Avoid abrupt withdrawal.
Phản ứng phụ
Significant: Psychiatric and paradoxical reactions (e.g. restlessness, aggression, bizarre behaviour, agitation, hallucinations, depersonalisation); rebound insomnia, anterograde amnesia, suicidal ideation and suicide attempts; drug dependence, drug abuse, somnambulism and associated behaviours (e.g. sleep-driving, cooking and eating food, making phone calls while asleep). Rarely, hypersensitivity reactions (e.g. angioedema).
Gastrointestinal disorders: Dysgeusia, dry mouth, nausea, vomiting.
General disorders and administration site conditions: Fatigue.
Nervous system disorders: Somnolence, dizziness, headache.
Thông tin tư vấn bệnh nhân
This drug may impair physical and mental abilities, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor for confusion, excessive drowsiness, and/or respiratory depression.
Quá liều
Symptoms: Drowsiness, confusion, lethargy, ataxia, hypotonia, hypotension, methaemoglobinaemia, respiratory depression, coma. Management: Symptomatic and supportive treatment. Administer activated charcoal within 1 hour of ingestion or gastric lavage within 1 hour of life-threatening overdose. May administer flumazenil in case of severe CNS depression. Maintain clear airway and monitor cardiac and vital signs until patient is stable.
Tương tác
Increased risk of profound sedation, respiratory depression, and coma with concomitant use of opioids. Enhanced central depressive effect with other CNS depressants (e.g. neuroleptics, hypnotics, sedatives, antidepressants, anaesthetics). Increased plasma concentration with CYP3A4 inhibitors (e.g. erythromycin, ketoconazole, ritonavir). Decreased plasma concentrations with CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenobarbital, phenytoin).
Food Interaction
Enhanced sedative effect with alcohol. Decreased plasma concentrations with St. John’s wort.
Tác dụng
Description: Zopiclone is a cyclopyrrolone derivative with pharmacological properties similar to those of benzodiazepines. It binds to the benzodiazepine receptor component of GABA receptor complex, but at a different site to that of benzodiazepines, leading to enhanced GABA activity in the brain.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: 77%. Time to peak plasma concentration: 1.5-2 hours.
Distribution: Rapidly distributed from the vascular compartment. Crosses the placenta, present in breast milk. Volume of distribution: Approx 91.8-104.6 L. Plasma protein binding: Approx 45-80%.
Metabolism: Extensively metabolised in the liver by CYP3A4 and to a lesser extent by CYP2C8 isoenzymes into less active metabolite zopiclone N-oxide and inactive metabolite N-desmethylzopiclone.
Excretion: Via urine (75%, approx 4-5% as unchanged drug); faeces (approx 16%). Elimination half-life: 3.5-6.5 hours.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Zopiclone, CID=5735, https://pubchem.ncbi.nlm.nih.gov/compound/Zopiclone (accessed on Mar. 25, 2020)

Bảo quản
Store below 30°C. Protect from light and moisture.
Phân loại MIMS
Phân loại ATC
N05CF01 - zopiclone ; Belongs to the class of benzodiazepine related agents. Used as hypnotics and sedatives.
References
Anon. Zopiclone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/11/2019.

Buckingham R (ed). Zopiclone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2019.

Joint Formulary Committee. Zopiclone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2019.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Zopiclone từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2021 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi MIMS.com
  • Imovane
  • Phamzopic
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in