Alprazolam is a potent, short-acting benzodiazepine anxiolytic a minor tranquilizer. It is commonly used for the treatment of anxiety disorders, especially of panic disorder, but also in the treatment of generalized anxiety disorder (GAD) or social anxiety disorder.
Class of Drug
Antianxiety agent, hypnotic.
Mechanism of Action
Potentiates effects of GABA in limbic system and reticular formation.
Indications / Dosage / Route
Routes of Administration: Oral only.
Condition: Anxiety disorder
Dose: Adults:Initial: 0.25-0.5 mg t.i.d. Maximum: 4 mg/d.
Elderly or debilitated: Initial: 0.25 mg b.i.d. to t.i.d.
Condition: Panic disorder
Dose: Adults: 0.5 mg t.i.d., increase to maximum of 10 mg/d.
Adjustment of Dosage
Kidney disease: Use caution.
Liver disease: Initial: 0.25 mg, b.i.d. or t.i.d.
Elderly: See above.
Pediatric: Safety and efficacy have not been established in children under 18 years.
Food and Drug Interactions
Food: No restrictions.
Pregnancy: Category D.
Lactation: Appears in breast milk. Potentially toxic to infant. Avoid breastfeeding.
Contraindications: Hypersensitivity to benzodiazepines, pregnancy
Warnings / Precautions
> Use with caution in patients with the following conditions: history of drug abuse, severe renal and hepatic impairment, elderly, neonates, infants.
> Benzodiazepines may cause psychologic and physical dependence.
> These drugs may cause paradoxical rage.
> It is best not to prescribe this drug for more than 6 months. If there is a need for long-term therapy, evaluate patient frequently.
> Use only for patients who have significant anxiety without medication, do not respond to other treatment, and are not drug abusers.
Clinically Important Drug Interactions
> Drugs that increase effects/toxicity of benzodiazepines: CNS depressants (alcohol, antihistamines, narcotic analgesics, tricyclic antidepressants, SSRIs, MAO inhibitors), cimetidine, disulfiram.
> Drugs that decrease effects/toxicity of benzodiazepines: flumazenil (antidote for overdose), carbamazepine.
> Common: Drowsiness, lightheadedness, Depression, Headache.
> Serious: Depression, respiratory Depression, Apnea, Hallucinations, Hepatitis, Seizures, Hostile behavior, Stevens-Johnson syndrome.
Parameters to Monitor
> Signs of chronic toxicity: ataxia, vertigo, slurred speech.
> Monitor dosing to make sure amount taken is as prescribed particularly if patient has suicidal tendencies.
> Monitor patient for efficacy of treatment: reduced symptoms of anxiety and tension, improved sleep.
> Signs of physical/psychologic dependence, particularly if patient is addiction-prone and requests frequent renewal of prescription or is experiencing a diminished response to the drug.
> Patient’s neurologic status including the following: memory (anterograde amnesia), disturbing thoughts, unusual behavior.
> Possibility of blood dyscrasias: fever, sore throat, upper respiratory infection. Perform total and differential WBC counts.
Advice to Patient
> Avoid driving and other activities requiring mental alertness or that are potentially dangerous until response to drug is known.
> Avoid alcohol and other CNS depressants such as narcotic analgesics, alcohol, antidepressants, antihistamines, and barbiturates when taking this drug.
> Use OTC medications only with approval from the treating physician.
> Cigarette smoking will decrease drug effect. Do not smoke when taking this drug.
> Do not stop drug abruptly if taken for more than 1 month. If suddenly withdrawn, there may be recurrence of the original anxiety or insomnia. A full-blown withdrawal may occur consisting of vomiting, insomnia, tremor, sweating, muscle spasms. After chronic use, decrease drug dosage slowly, i.e, over a period of several weeks at a rate of 25% per week.
> Avoid excessive use of xanthine-containing foods (regular coffee, tea, chocolate) as these may counteract the action of the drug.
Further Useful Info
> Alprazolam appears to have some antidepressant effects and is indicated for anxiety associated with depression.
> The side effect profile of alprazolam appears better than that of some other benzodiazepines.
> Seizures may occur if flumazenil is given after long term use of benzodiazepines.