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modified on 29 April 2009 at 07:49 ••• 4,798 views

Oxazepam

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Oxazepam is a benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia. Oxazepam possesses relatively weak anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.

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Oxazepam
Systematic (IUPAC) name
9-chloro-4-hydroxy-6-phenyl-
2,5-diazabicyclo[5.4.0]undeca-
5,8,10,12-tetraen-3-one
Identifiers
CAS number 604-75-1
ATC code N05BA04
PubChem 4616
DrugBank APRD01152
ChemSpider 4455
Chemical data
Formula C15H11ClN2O2 
Mol. mass 286.71
Pharmacokinetic data
Bioavailability 95.5%
Metabolism Hepatic
Half life 4-14 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

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Legal status

Schedule IV(US)

Routes Oral


Contents

Contraindications

Hypersensitivity to oxazepam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist); narrow-angle glaucoma (not in product labeling, however, benzodiazepines are contraindicated); not indicated for use in the treatment of psychosis; pregnancy


Warnings/Precautions

May cause hypotension (rare) - use with caution in patients with cardiovascular or cerebrovascular disease, or in patients who would not tolerate transient decreases in blood pressure. Serax® 15 mg tablet contains tartrazine; use is not recommended in pediatric patients <6 years of age; dose has not been established between 6-12 years of age.

Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Use with caution in patients with respiratory disease or impaired gag reflex. Avoid use in patients with sleep apnea.

Causes CNS depression (dose-related) resulting in sedation, dizziness, confusion, or ataxia which may impair physical and mental capabilities. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Use with caution in patients receiving other CNS depressants or psychoactive agents. Effects with other sedative drugs or ethanol may be potentiated. Benzodiazepines have been associated with falls and traumatic injury and should be used with extreme caution in patients who are at risk of these events (especially the elderly).

Use caution in patients with depression, particularly if suicidal risk may be present. Use with caution in patients with a history of drug dependence. Benzodiazepines have been associated with dependence and acute withdrawal symptoms on discontinuation or reduction in dose. Acute withdrawal, including seizures, may be precipitated after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

Benzodiazepines have been associated with anterograde amnesia. Paradoxical reactions, including hyperactive or aggressive behavior have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Does not have analgesic, antidepressant, or antipsychotic properties.

Adverse Reactions

Frequency not defined.

Cardiovascular: Syncope (rare), edema

Central nervous system: Drowsiness, ataxia, dizziness, vertigo, memory impairment, headache, paradoxical reactions (excitement, stimulation of effect), lethargy, amnesia, euphoria

Dermatologic: Rash

Endocrine & metabolic: Decreased libido, menstrual irregularities

Genitourinary: Incontinence

Hematologic: Leukopenia, blood dyscrasias

Hepatic: Jaundice

Neuromuscular & skeletal: Dysarthria, tremor, reflex slowing

Ocular: Blurred vision, diplopia


Overdosage/Toxicology

Symptoms of overdose include somnolence, confusion, coma, hypoactive reflexes, dyspnea, hypotension, slurred speech, and impaired coordination. Treatment for benzodiazepine overdose is supportive. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced CNS depression, but not respiratory depression due to toxicity.


Drug Interactions

Ethanol and other CNS depressants may increase the CNS effects of oxazepam

Levodopa: Therapeutic effects may be diminished in some patients following the addition of a benzodiazepine; limited/inconsistent data

Theophylline and other CNS stimulants may antagonize the sedative effects of oxazepam

Zidovudine: Increased incidence of headache with concurrent use. Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may increase CNS depression).

Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression). Mechanism of Action: Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.


Pharmacodynamics/Kinetics

Absorption: Almost complete Protein binding: 86% to 99% Metabolism: Hepatic to inactive compounds (primarily as glucuronides) Half-life elimination: 2.8-5.7 hours Time to peak, serum: 2-4 hours Excretion: Urine (as unchanged drug (50%) and metabolites)

Dosage, Oral

Children

Anxiety: 1 mg/kg/day has been administered

Adults

Anxiety: 10-30 mg 3-4 times/day Ethanol withdrawal: 15-30 mg 3-4 times/day Hypnotic: 15-30 mg


Elderly

Oral: Anxiety: 10 mg 2-3 times/day; increase gradually as needed to a total of 30-45 mg/day. Dose titration should be slow to evaluate sensitivity. Hemodialysis: Not dialyzable (0% to 5%)

Brand names for Oxazepam

  • Adumbran® (AT, DE, ES, SI)
  • Alepam® (AU)
  • Alopam® (DK, NO)
  • Anxiolit® (AT, CH)
  • Apo-Oxazepam® (CA)
  • Azutranquil® (DE)
  • Benzotran® (NZ)
  • durazepam® (DE)
  • Enidrel® (AR)
  • Limbial® (IT)
  • Medopam® (ZA)
  • Mirfudorm® (DE)
  • Murelax® (AU)
  • Nesontil® (AR)
  • Noctazepam® (DE)
  • Noripam® (ZA)
  • Novoxapram® (CA)
  • Nozepam® (RU)
  • Oksazepam® (HR, PL, SI)
  • Opamox® (FI)
  • Oxa 1A Pharma® (DE)
  • Oxabenz® (DK)
  • Oxahexal® (AT)
  • Oxamin® (FI)
  • Oxapax® (DK)
  • Oxaphar® (BE)
  • Oxascand® (SE)
  • oxa von ct® (DE)
  • Oxazepam 1A Pharma® (DE)
  • Oxazepam AL® (DE)
  • Oxazepam Efeka® (BE, LU)
  • Oxazepam EG® (BE)
  • Oxazepam-Eurogenerics® (LU)
  • Oxazepam Hexal® (DE)
  • Oxazepam Leciva® (CZ)
  • Oxazepam-neuraxpharm® (DE)
  • Oxazepam® (PL, RO, RU)
  • Oxazepam-ratiopharm® (DE, LU)
  • Oxazepam SAD® (DK)
  • Oxazepam Sandoz® (DE)
  • Oxazepam Stada® (DE)
  • Oxepam® (FI)
  • Ox-Pam® (NZ)
  • Oxpram® (CA)
  • PMS-Oxazepam (CA)
  • Praxiten® (AT, DE, HR, SI)
  • Purata® (ZA)
  • Serax® (HK)
  • Serenal® (PT)
  • Serepax® (AU, CL, DK, IN, NO, NZ, ZA)
  • Seresta® (BE, CH)
  • Séresta® (FR)
  • Seresta® (LU, NL)
  • Serpax® (IT)
  • Sigacalm® (DE)
  • Sobril® (NO, SE)
  • Tranquo® (BE, LU)
  • Uskan® (DE)


U.S. Brand Names

  • Serax®

Canadian Brand Names

  • Apo-Oxazepam®
  • Novoxapram®
  • Oxpram®
  • PMS-Oxazepam