OXAZEPAM

brands

Class

• Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM)
• Benzodiazepine (anxiolytic)

OXAZEPAM commonly prescribed for

(Bold for FDA approved)

How OXAZEPAM works

• Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex

• Enhances the inhibitory effects of GABA

• Boosts chloride conductance through GABA-regulated channels

• Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders

How long until OXAZEPAM works

• Some immediate relief with first dosing is common; can take several weeks with daily dosing for maximal therapeutic benefit

Notable Side Effects

• Sedation, fatigue, depression

• Dizziness, ataxia, slurred speech, weakness

• Forgetfulness, confusion

• Hyperexcitability, nervousness

• Rare hallucinations, mania

• Rare hypotension

• Hypersalivation, dry mouth

Life Threatening Side Effects

• Respiratory depression, especially when taken with CNS depressants in overdose

• Rare hepatic dysfunction, renal dysfunction, blood dyscrasias

weight gain

unusual

sedation

common

What to do about OXAZEPAM side effects

• Wait

• Wait

• Wait

• Lower the dose

• Take largest dose at bedtime to avoid sedative effects during the day

• Switch to another agent

• Administer flumazenil if side effects are severe or life-threatening

usual dosage range

• Mild to moderate anxiety: 30–60 mg/day in 3–4 divided doses

• Severe anxiety, anxiety associated with alcohol withdrawal: 45–120 mg/day in 3–4 divided doses

Dosage Forms

• Capsule 10 mg, 15 mg, 30 mg

• Tablet 15 mg

long term use

• Risk of dependence, particularly for treatment periods longer than 12 weeks and especially in patients with past or current polysubstance abuse

habit forming

• Oxazepam is a Schedule IV drug

• Patients may develop dependence and/or tolerance with long-term use

Renal Impairment

• Use with caution; oxazepam levels may be increased

Hepatic Impairment

• Use with caution; oxazepam levels may be increased

• Because of its short half-life and inactive metabolites, oxazepam may be a preferred benzodiazepine in some patients with liver disease

Cardiac Impairment

• Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction

Elderly

• Initial 30 mg in 3 divided doses; can be increased to 30–60 mg/day in 3–4 divided doses

Children and Adolescents

• Safety and efficacy not established under age 6

• No clear dosing guidelines for children ages 6–12

• Long-term effects of oxazepam in children/ adolescents are unknown

• Should generally receive lower doses and be more closely monitored

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Possible increased risk of birth defects when benzodiazepines are taken during pregnancy

• Because of the potential risks, oxazepam is not generally recommended as treatment for anxiety during pregnancy, especially during first trimester

• Drug should be tapered if discontinued

• Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects

• Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy

• Seizures, even mild seizures, may cause harm to the embryo/fetus

Breast Feeding

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed

• Effects on infant have been observed and include feeding difficulties, sedation, and weight loss