alprazolam
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alprazolam
[al-pra´zo-lam]alprazolam
😞😴😙 Pharmacologic class: Benzodiazepine
😞😴😙 Therapeutic class: Anxiolytic
😞😴😙 Controlled substance schedule IV
😞😴😙 Pregnancy risk category D
Action
😞😴😙 Unclear. Thought to act at limbic, thalamic, and hypothalamic levels of CNS to produce sedative, anxiolytic, skeletal muscle relaxant, and anticonvulsant effects.
Availability
😞😴😙 Solution: 1 mg/ml
😞😴😙 Tablets (extended-release): 0.5 mg, 1 mg, 2 mg, 3 mg
😞😴😙 Tablets (immediate-release): 0.25 mg, 0.5 mg, 1 mg, 2 mg
😞😴😙 Tablets (orally disintegrating): 0.25 mg, 0.5 mg, 1 mg, 2 mg
Indications and dosages
😞😴😙 ➣ Anxiety disorders
😞😴😙 Adults: Initially, 0.25 to 0.5 mg P.O. t.i.d. Maximum dosage is 4 mg daily in divided doses.
😞😴😙 Elderly patients: Initially, 0.25 mg P.O. two or three times daily. Maximum dosage is 4 mg daily in divided doses.
😞😴😙 ➣ Panic disorders
😞😴😙 Adults:Immediate-release or orally disintegrating tablets-Initially, 0.5 mg P.O. t.i.d. Extended-release tablets-Initially, 0.5 to 1 mg P.O. daily. Usual dosage is 3 to 6 mg daily, with a maximum dosage of 10 mg daily. For all dosage forms, increase by a maximum of 1 mg daily at intervals of 3 to 4 days, with a maximum of 10 mg daily in divided doses.
Dosage adjustment
😞😴😙 • Hepatic impairment
Off-label uses
😞😴😙 • Agoraphobia
😞😴😙 • Depression
😞😴😙 • Premenstrual syndrome
Contraindications
😞😴😙 • Hypersensitivity to benzodiazepines
😞😴😙 • Narrow-angle glaucoma
😞😴😙 • Labor and delivery
😞😴😙 • Pregnancy or breastfeeding
Precautions
😞😴😙 Use cautiously in:
😞😴😙 • hepatic dysfunction
😞😴😙 • history of attempted suicide or drug dependence
😞😴😙 • elderly patients.
Administration
😞😴😙 • Don't give with grapefruit juice.
😞😴😙 • Make sure patient swallows extended-release tablets whole without chewing or crushing.
😞😴😙 • Mix oral solution with liquids or semisolid foods and instruct patient to consume entire amount immediately.
😞😴😙 • Administer orally disintegrating tablets by placing tablet on patient's tongue. If only one-half of scored tablet is used, discard unused portion immediately.
😞😴😙 ☞ Don't withdraw drug suddenly. Seizures and other withdrawal symptoms may occur unless dosage is tapered carefully.
Adverse reactions
😞😴😙 CNS: dizziness, drowsiness, depression, fatigue, light-headedness, disorientation, anger, hostility, euphoria, hypomanic episodes, restlessness, confusion, crying, delirium, headache, stupor, rigidity, tremor, paresthesia, vivid dreams, extrapyramidal symptoms
😞😴😙 CV: bradycardia, tachycardia, hypertension, hypotension, palpitations, CV collapse
😞😴😙 EENT: blurred or double vision, nystagmus, nasal congestion
😞😴😙 GI: gastric disorders, dysphagia, anorexia, increased salivation, dry mouth
😞😴😙 GU: menstrual irregularities, urinary retention, urinary incontinence, libido changes, gynecomastia
😞😴😙 Hematologic: blood dyscrasias such as eosinophilia, agranulocytosis, leukopenia, and thrombocytopenia
😞😴😙 Hepatic: hepatic dysfunction (including hepatitis)
😞😴😙 Musculoskeletal: muscle rigidity, joint pain
😞😴😙 Skin: dermatitis, rash, pruritus, urticaria, increased sweating
😞😴😙 Other: weight loss or gain, hiccups, fever, edema, psychological drug dependence, drug tolerance
Interactions
😞😴😙 Drug-drug.Antidepressants, antihistamines, opioids, other benzodiazepines: increased CNS depression
😞😴😙 Barbiturates, rifampin: increased metabolism and decreased efficacy of alprazolam
😞😴😙 Cimetidine, disulfiram, erythromycin, fluoxetine, hormonal contraceptives, isoniazid, ketoconazole, metoprolol, propoxyphene, propranolol, valproic acid: decreased metabolism and increased action of alprazolam
😞😴😙 Digoxin: increased risk of digoxin toxicity
😞😴😙 Levodopa: decreased antiparkinsonian effect
😞😴😙 Theophylline: increased sedative effect
😞😴😙 Tricyclic antidepressants (TCAs): increased TCA blood levels
😞😴😙 Drug-diagnostic tests.Itraconazole, ketoconazole: increased alprazolam plasma level
😞😴😙 Drug-food.Grapefruit juice: decreased drug metabolism and increased blood level
😞😴😙 Drug-herbs.Chamomile, hops, kava, skullcap, valerian: increased CNS depression
😞😴😙 Drug-behaviors.Alcohol use: increased CNS depression
😞😴😙 Smoking: decreased alprazolam efficacy
Patient monitoring
😞😴😙 • Watch for excessive CNS depression if patient is concurrently taking antidepressants, other benzodiazepines, antihistamines, or opioids.
😞😴😙 • If patient is taking TCAs concurrently, watch for increase in adverse TCA effects.
😞😴😙 • Monitor CBC and liver and kidney function test results.
😞😴😙 • Monitor vital signs and weight.
😞😴😙 • Report signs of drug abuse, including frequent requests for early refills.
Patient teaching
😞😴😙 • Instruct patient to swallow extended- release tablets whole without crushing or chewing.
😞😴😙 ☞ Tell patient that drug may make him more depressed, angry, or hostile. Urge him to contact prescriber immediately if he thinks he's dangerous to himself or others.
😞😴😙 • Inform patient that drug may cause tremors, muscle rigidity, and other movement problems. Advise him to report these effects to prescriber.
😞😴😙 ☞ Caution patient not to stop taking drug suddenly. Withdrawal symptoms, including seizures, may occur unless drug is tapered carefully.
😞😴😙 • Advise patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
😞😴😙 • As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.