Oxazepam

Debilitated patient: Initially, 10 mg tid, increase up to 10-20 mg 3 or 4 times daily as necessary.

No dosage adjustment needed.

Oxazepam May be taken with or without food.

Patient w/ CV or cerebrovascular disease, acute narrow-angle glaucoma, suicidal tendencies, history of drug abuse or acute alcoholism, myasthenia gravis, chronic pulmonary insufficiency or sleep apnoea. Not intended for treatment of psychoses. Avoid abrupt withdrawal. Hepatic and renal impairment. Elderly or debilitated patient. Pregnancy and lactation.

Sleep and visual disturbances, drowsiness, dizziness, vertigo, lethargy, headache, tremor, ataxia, mild paradoxical reactions (e.g. excitement, stimulation of affect), minor diffuse skin rashes (e.g. morbilliform, maculopapular and urticarial), nausea, oedema, slurred speech, altered libido, GI symptoms. Rarely, transient anterograde amnesia or memory impairment, syncope, leucopenia and hepatic dysfunction including jaundice.

PO: D

May impair ability to perform hazardous activities requiring mental alertness or physical coordination (e.g. operating machinery, driving).

Monitor resp and CV status. Periodic monitoring of CBC and LFTs.

Symptoms: Drowsiness, mental confusion, lethargy, ataxia, hypotension, hypotonia, resp depression, coma and very rarely, death. Management: Symptomatic and supportive treatment. If ingestion is recent, induce vomiting and/or gastric lavage. Admin of activated charcoal may reduce absorption. Hypotension may be controlled w/ norepinephrine. Flumazenil may be used as an adjunct for proper management but there is a risk of seizure particularly in long-term benzodiazepine users and in TCA overdose.

Additive CNS depressant effects w/ barbiturates, antipsychotics, sedatives/hypnotics, anxiolytics, antidepressants, sedative antihistamines, anticonvulsants, and anaesth. Increased psychic dependence w/ narcotic analgesics. CYP450 inhibitors may enhance benzodiazepine activity.

Enhanced sedative effects w/ alcohol.

Description:
Mechanism of Action: Oxazepam is a short-acting benzodiazepine. It 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: Well absorbed from the GI tract. Time to peak plasma concentration: Approx 2-3 hr.
Distribution: It crosses the placenta and detected in breast milk. Plasma protein binding: Approx 97%.
Metabolism: Undergoes hepatic conjugation to produce the major inactive glucuronide metabolite.
Excretion: Via urine as inactive glucuronide conjugate. Elimination half-life: Approx 4-15 hr.

Source: National Center for Biotechnology Information. PubChem Database. Oxazepam, CID=4616, https://pubchem.ncbi.nlm.nih.gov/compound/Oxazepam (accessed on Jan. 22, 2020)

Store between 15-30°C.

Anxiolytics

Brayfield A, Cadart C (eds). Oxazepam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2014.

Joint Formulary Committee. Oxazepam. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2014.

Oxazepam Capsule (Leading Pharma, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/04/2014.

Oxazepam Tablets BP 10 mg (Accord-UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 23/04/2014.

Oxazepam. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 23/04/2014.

Oxazepam. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 23/04/2014.