Chlordiazepoxide


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Insomnia associated with anxiety
Adult: 10-30 mg before bedtime. Individualise dosage and treatment duration according to patient response and severity of the disorder. Use the lowest effective dose for the shortest possible duration. Treatment duration: Few days to 2 weeks; Max of 4 weeks, including a tapering off process.
Elderly: Dose reduction may be required.

Oral
Anxiety
Adult: For the management of anxiety disorders or the short-term relief of anxiety symptoms: Usual dose range: 5-25 mg 2-4 times daily; may increase gradually. Max: 100 mg daily in divided doses. For the relief of preoperative anxiety and apprehension: 5-10 mg 3-4 times daily for several days preceding surgery. Individualise dosage and treatment duration according to patient response and severity of the disorder. Use the lowest effective dose for the shortest possible duration. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Elderly: Dose reduction may be required. Dosage recommendations may vary among countries and individual products (refer to detailed product guidelines).

Oral
Acute symptoms of alcohol withdrawal
Adult: 25-100 mg, may be repeated, if necessary, after 2-4 hours. Max: 300 mg daily. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Elderly: Dose reduction may be required. Dosage recommendations may vary among countries and individual products (refer to detailed product guidelines).

Oral
Muscle spasms
Adult: 10-30 mg daily in divided doses. Individualise dosage and treatment duration according to patient response and severity of the disorder. Use the lowest effective dose for the shortest possible duration.
Elderly: Dose reduction may be required.
Nhóm bệnh nhân đặc biệt
Debilitated patients: Dose reduction may be required. Dosage recommendations may vary among countries and individual products (refer to detailed product guidelines).
Suy thận
Dose reduction may be required.
Suy gan
Mild to moderate: Dose reduction may be required. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Myasthenia gravis, severe pulmonary insufficiency, respiratory depression, phobic or obsessional states, chronic psychosis, sleep apnoea syndrome. Severe hepatic impairment.
Thận trọng
Patient with depression (particularly if with suicidal risk), porphyria, respiratory disease, history of alcohol or drug abuse; marked personality disorder; at risk of falls. Debilitated patients. Avoid abrupt withdrawal. Not indicated for use alone to treat depression or anxiety associated with depression. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation. Concomitant use with opioids.
Tác dụng không mong muốn
Significant: Anterograde amnesia, paradoxical reactions (including hyperactive or aggressive behaviour), sleep-related activities (e.g. sleep-driving, making phone calls, cooking, and eating food while asleep); physical dependence and withdrawal reactions (prolonged use; high doses), tolerance (prolonged use).
Blood and lymphatic system disorders: Rarely, blood dyscrasias (e.g. agranulocytosis).
Eye disorders: Rarely, visual impairment (including diplopia).
Gastrointestinal disorders: Nausea, constipation, changes in salivation.
General disorders and administration site conditions: Fatigue.
Hepatobiliary disorders: Jaundice.
Investigations: Increased serum bilirubin, transaminases, and alkaline phosphatase; changes in EEG patterns.
Metabolism and nutrition disorders: Increased appetite.
Musculoskeletal and connective tissue disorders: Muscle weakness.
Nervous system disorders: Somnolence, sedation, dizziness, unsteadiness, ataxia, dysarthria, gait disturbance, extrapyramidal symptoms (e.g. tremor, dyskinesia).
Psychiatric disorders: Confusion, hallucinations, restlessness, agitation, delusion, irritability, nightmares, emotional disturbances, psychotic disorder, abnormal behaviour.
Reproductive system and breast disorders: Rarely, changes in libido, minor menstrual irregularities.
Skin and subcutaneous tissue disorders: Rarely, skin eruptions.
Thông tin tư vấn bệnh nhân
This drug may cause sedation, amnesia, impaired concentration, dizziness, drowsiness, and impaired muscular function; if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor respiratory, CV (including orthostasis), and mental status. Evaluate for paradoxical reactions (e.g. acute rage, stimulation, excitement). If indicated for alcohol withdrawal, monitor for signs and symptoms of alcohol withdrawal. Assess the patient's risk for abuse, misuse, and addiction prior to initiation and during treatment.
Quá liều
Symptoms: Drowsiness, mental confusion, lethargy. Severe cases may lead to ataxia, hypotonia, hypotension, respiratory depression, and rarely, coma. Management: Symptomatic and supportive treatment. Initiate IV fluids administration and maintain an adequate airway. Administration of activated charcoal may be given within 1 hour of ingestion, provided that the airway is protected. If hypotension occurs, administer norepinephrine or metaraminol. Flumazenil may be considered as an adjunctive agent for proper overdose management; it is indicated for the complete or partial reversal of the sedative effects. Necessary measures must be instituted to secure airway, ventilation, and IV access prior to flumazenil use.
Tương tác
Potentiated central depressive effects with other centrally-acting agents (e.g. antipsychotics, hypnotics, anxiolytics, antidepressants, analgesics, sedative antihistamines, anaesthetics). Side effects and toxicity may be more evident when used concomitantly with antiepileptic drugs (e.g. phenytoin, barbiturates). May enhance respiratory depression with sodium oxybate. May decrease clearance with CYP450 inhibitors (e.g. cimetidine, erythromycin, omeprazole). May increase clearance with CYP450 inducers (e.g. rifampicin). Increased sedative effect with lofexidine, nabilone, baclofen, tizanidine, and disulfiram. May antagonise the effect of levodopa. Reduced therapeutic effect with theophylline.
Potentially Fatal: Concomitant use with opioids may result in profound sedation, respiratory depression, and coma.
Tương tác với thức ăn
May enhance sedative effect with alcohol; avoid concomitant use.
Tác dụng
Description: Chlordiazepoxide, a benzodiazepine, has antianxiety, sedative, appetite-stimulating, and weak analgesic actions. It binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron. It enhances the inhibitory effect of GABA in different parts of the CNS by increasing the permeability of neuronal membrane to chloride ions, thus resulting in hyperpolarisation and stabilisation.
Pharmacokinetics:
Absorption: Almost completely absorbed. Time to peak plasma concentration: 0.5-2 hours.
Distribution: Crosses the placenta and passes into CSF; enters breast milk. Volume of distribution: 3.3 L/kg. Plasma protein binding: Approx 96%.
Metabolism: Extensively metabolised in the liver to desmethylchlordiazepoxide, desmethyldiazepam (active and long-acting metabolite), and demoxepam.
Excretion: Via urine (1-2% as unchanged drug; 3-6% as metabolite). Elimination half-life: 24-48 hours (chlordiazepoxide); 14-95 hours (demoxepam).
Đặc tính

Chemical Structure Image
Chlordiazepoxide

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2712, Chlordiazepoxide. https://pubchem.ncbi.nlm.nih.gov/compound/Chlordiazepoxide. Accessed July 29, 2020.

Bảo quản
Store between 15-30°C. Protect from light.
Phân loại MIMS
Thuốc giải lo âu
Phân loại ATC
N05BA02 - chlordiazepoxide ; Belongs to the class of benzodiazepine derivatives anxiolytics. Used in the management of anxiety, agitation or tension.
Tài liệu tham khảo
Anon. Chlordiazepoxide (Briggs Drugs in Pregnancy and Lactation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/02/2022.

Anon. Chlordiazepoxide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 16/03/2022.

Anon. Chlordiazepoxide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/02/2022.

Buckingham R (ed). Chlordiazepoxide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/02/2022.

Chlordiazepoxide 5 mg Tablets (Genethics Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 21/02/2022.

Chlordiazepoxide Capsules BP 10 mg (Crescent Pharma Limited). MHRA. https://products.mhra.gov.uk. Accessed 21/02/2022.

Chlordiazepoxide Hydrochloride Capsule (Bryant Ranch Prepack). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/02/2022.

Joint Formulary Committee. Chlordiazepoxide Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/02/2022.

Preston CL (ed). Chlordiazepozide - Sodium Oxybate - Levodopa Drug Interaction. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/02/2022.

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