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Look Up > Drugs > Oxazepam
Oxazepam
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Pharmacological Index
Use
Restrictions
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Administration
Monitoring Parameters
Reference Range
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(oks A ze pam)

U.S. Brand Names
Serax®

Generic Available

Yes


Canadian Brand Names
Apo®-Oxazepam; Novo-Oxazepam; Oxpam®; PMS-Oxazepam; Zapex®

Pharmacological Index

Benzodiazepine


Use

Treatment of anxiety and management of alcohol withdrawal


Restrictions

C-IV


Pregnancy Risk Factor

D


Contraindications

Hypersensitivity to this drug or any component of its 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 contains tartrazine; use is not recommended in pediatric patients <6 years of age; dose has not been established between 6-12 years of age.

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 (ie, 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

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

Miscellaneous: Drug dependence


Overdosage/Toxicology

Symptoms of overdose include somnolence, confusion, coma, hypoactive reflexes, dyspnea, hypotension, slurred speech, impaired coordination

Treatment for benzodiazepine overdose is supportive. Rarely is mechanical ventilation required. 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 the respiratory depression due to toxicity.


Drug Interactions

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

Oral contraceptives may increase the clearance of oxazepam

Oxazepam may decrease the antiparkinsonian efficacy of levodopa

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

Phenytoin may increase the clearance of oxazepam


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

Peak serum concentration: 1-2 hours

Absorption: Oral: Almost completely

Protein binding: 86% to 99%

Metabolism: In the liver to inactive compounds (primarily as glucuronides)

Half-life: 2.8-5.7 hours

Time to peak serum concentration: Within 2-4 hours

Elimination: Excretion of unchanged drug (50%) and metabolites; excreted without need for liver metabolism


Usual Dosage

Oral:

Adults:

Anxiety: 10-30 mg 3-4 times/day

Alcohol withdrawal: 15-30 mg 3-4 times/day

Hypnotic: 15-30 mg

Hemodialysis: Not dialyzable (0% to 5%)


Dietary Considerations

Alcohol: Additive CNS effect, avoid use


Administration

Give orally in divided doses


Monitoring Parameters

Respiratory and cardiovascular status


Reference Range

Therapeutic: 0.2-1.4 mg/mL (SI: 0.7-4.9 mmol/L)


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

>10% of patients experience dry mouth which disappears with cessation of drug therapy


Patient Information

Take exactly as directed (do not increase dose or frequency); may take 2-3 weeks to achieve desired results; may cause physical and/or psychological dependence. Do not use excessive alcohol or other prescription or OTC medications (especially pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, lightheadedness, impaired coordination, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, or dry mouth (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help); altered sexual drive or ability (reversible); or photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). Report persistent CNS effects (eg, confusion, depression, increased sedation, excitation, headache, agitation, insomnia or nightmares, dizziness, fatigue, impaired coordination, changes in personality, or changes in cognition); changes in urinary pattern; muscle cramping, weakness, tremors, or rigidity; ringing in ears or visual disturbances; chest pain, palpitations, or rapid heartbeat; excessive perspiration, excessive GI symptoms (cramping, constipation, vomiting, anorexia); or worsening of condition. Pregnancy/breast-feeding precautions: Do not get pregnant while taking this medication; use appropriate barrier contraceptive measures. Breast-feeding is not recommended.


Nursing Implications

Provide safety measures (ie, side rails, night light, and call button); remove smoking materials from area; supervise ambulation


Dosage Forms

Capsule: 10 mg, 15 mg, 30 mg

Tablet: 15 mg


References

Hicks R, Dysken MW, Davis JM, et al, "The Pharmacokinetics of Psychotropic Medication in the Elderly: A Review," J Clin Psychiatry, 1981, 42(10)374-85.

Moshkowitz M, Pines A, Finkelstein A, et al, "Skin Blisters as a Manifestation of Oxazepam Toxicity," J Toxicol Clin Toxicol, 1990, 28(3):383-6.

Zileli MS, Teletar F, Deniz S, et al, "Oxazepam Intoxication Simulating Nonketo-Acidotic Diabetic Coma," JAMA, 1971, 215(12):1986.


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