Bromazepam


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Anxiety
Adult: Initially, 6-18 mg daily in divided doses. Doses up to 60 mg daily have been used.
Elderly: Max initial dose: 3 mg daily in divided doses.
Special Patient Group
Debilitated patients: Max initial dose: 3 mg daily in divided doses.
Renal Impairment
No dosage adjustment needed.
Hepatic Impairment
Mild to moderate: Initiate therapy conservatively; adjust cautiously. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Patient w/ myasthenia gravis, severe resp insufficiency including chronic obstructive airways disease w/ incipient resp failure, sleep apnoea syndrome. Severe hepatic impairment.
Thận trọng
Patient w/ CV or cerebrovascular disease, pre-existing or chornic resp disease, acute narrow-angle glaucoma, impaired gag reflex, history of alcohol or drug abuse; at risk of falls. Not intended as primary therapy of depression, anxiety and/or psychosis. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly, debilitated patients. Pregnancy and lactation.
Phản ứng phụ
Drowsiness, dizziness, headache, ataxia, decreased alertness, seizures, tremor, incontinence, anterograde amnesia, confusional state, emotional disturbances, libido disorders, muscle weakness and spasm, depression; behavioural, speech and sleep disorders, restlessness, agitation, delusion, irritability, aggressiveness, nightmares, anger, psychoses, hallucinations, diplopia, pruritus and rash, fatigue, cardiac failure, resp depression, anorexia, GI disturbances (e.g. nausea, vomiting).
Thông tin tư vấn bệnh nhân
May impair ability to perform activities requiring mental alertness and motor coordination (e.g. operating machinery, driving).
Monitoring Parameters
Monitor resp, CV and mental status. Periodic monitoring of CBC and LFTs.
Quá liều
Symptoms: Drowsiness, mental confusion, lethargy, areflexia, apnoea, ataxia, hypotonia, hypotension, cardio-resp depression and coma. Management: Symptomatic and supportive treatment. Admin activated charcoal if taken w/in 1-2 hr. May admin flumazenil cautiously for severe CNS depression.
Tương tác
May enhance the activity w/ CYP450 inhibitor (e.g. azole antifungals, macrolides, HIV protease inhibitors, Ca channel blockers). Elevated plasma levels w/ disulfiram or cimetidine. Additive CNS depressant effects w/ barbiturates, sedatives, anaesth, anxiolytics, hypnotics, phenothiazines, other antipsychotics, skeletal muscle relaxants. May potentiate anticholinergic effects of atropine, antihistamines and antidepressants. Increased psychic drug dependence w/ narcotic analgesics.
Food Interaction
Food may decrease systemic exposure and delay onset of clinical effects. Additive CNS depressant effect w/ alcohol. May increase serum level w/ grapefruit juice.
Tác dụng
Description: Bromazepam increases neuronal membrane permeability to Cl ions by binding to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron w/in the CNS (including the limbic system, reticular formation) and enhancing the GABA inhibitory effects resulting in hyperpolarisation and stabilisation.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Serum concentration may be decreased by food. Bioavailability: 60%. Time to peak plasma concentration: ≤2 hr.
Distribution: Volume of distribution: 50 L. Plasma protein binding: 70%.
Metabolism: Undergoes hepatic metabolism. 3-hydroxy-bromazepam and 2-(2-amino-5-bromo-3-hydroxybenzoyl) pyridine are the predominant metabolites.
Excretion: Via urine (69% as metabolites). Elimination half-life: Approx 20 hr.
Đặc tính

Chemical Structure Image
Bromazepam

Source: National Center for Biotechnology Information. PubChem Database. Bromazepam, CID=2441, https://pubchem.ncbi.nlm.nih.gov/compound/Bromazepam (accessed on Jan. 21, 2020)

Bảo quản
Store below 30°C.
Phân loại MIMS
References
Anon. Bromazepam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/04/2014.

Buckingham R (ed). Bromazepam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/04/2014.

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