ALPRAZOLAM

ALPRAZOLAM
(al-pray'zoe-lam)
Niravam, Xanax, Xanax XR
Classifications: anxiolytic; sedative-hypnotic; benzodiazepine;
Therapeutic: antianxiety
; sedative-hypnotic
Prototype: Lorazepam
Pregnancy Category: D
Controlled Substance: Schedule IV

Availability

0.25 mg, 0.5 mg, 1 mg, 2 mg tablets; 0.5 mg, 1 mg, 2 mg, 3 mg sustained-release tabs; 1 mg/mL oral solution; 0.25 mg, 0.5 mg, 1 mg, 2 mg orally disintegrating tabs

Action

A CNS depressant that appears to act at the limbic, thalamic, and hypothalamic levels of the CNS.

Therapeutic Effect

Has antianxiety and sedative effects with addictive potential.

Uses

Management of anxiety disorders or for short-term relief of anxiety symptoms. Also used as adjunct in management of anxiety associated with depression and agitation, and for panic disorders, such as agoraphobia.

Unlabeled Uses

Alcohol withdrawal.

Contraindications

Sensitivity to benzodiazepines; acute narrow angle glaucoma; pulmonary disease; use alone in primary depression or psychotic disorders, bipolar disorders, organic brain disorders; myasthenia gravis; pregnancy (category D), lactation; children <18 y.

Cautious Use

Impaired hepatic function; history of alcoholism; renal impairment, hepatic disease; geriatric and debilitated patients. Effectiveness for long-term treatment (>4 mo) not established.

Route & Dosage

Anxiety Disorders
Adult: PO 0.25–0.5 mg t.i.d. (max: 4 mg/d)
Geriatric: PO 0.125–0.25 mg b.i.d.

Panic Attacks
Adult: PO 1–2 mg t.i.d. (max: 8 mg/d); sustained release: initiate with 0.5 mg to 1 mg once/d. Depending on the response, the dose may be increased at intervals of 3 to 4 days in increments of no more than 1 mg/d. Target range 3–6 mg/d (max: 10 mg/d).

Hepatic Impairment
Reduce dose by 50% in hepatic impairment.
Do not discontinue abruptly.

Administration

Oral
  • Reduce drug gradually when discontinuing drug.
  • Store in light-resistant containers at 15°–30° C (59°–86° F), unless otherwise directed.

Adverse Effects (≥1%)

CNS: Drowsiness, sedation, light-headedness, dizziness, syncope, depression, headache, confusion, insomnia, nervousness, fatigue, clumsiness, unsteadiness, rigidity, tremor, restlessness, paradoxical excitement, hallucinations. CV: Tachycardia, hypotension, ECG changes. Special Senses: Blurred vision. Respiratory: Dyspnea.

Interactions

Drug: Alcohol and other cns depressants, anticonvulsants, antihistamines, barbiturates, narcotic analgesics, benzodiazepines, compound CNS depressant effects; cimetidine, disulfiram, fluoxetine, tricyclic antidepressants increase alprazolam levels (decreased metabolism); oral contraceptives may increase or decrease alprazolam effects. Herbal: Kava, valerian may potentiate sedation; St. John's wort decreases serum level of alprazolam. Cigarette smoking may decrease serum level of alprazolam by 50%.

Pharmacokinetics

Absorption: Rapidly absorbed. Peak: 1–2 h. Distribution: Crosses placenta. Metabolism: Oxidized in liver to inactive metabolites by CYP3A4. Elimination: Renal elimination. Half-Life: 12–15 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for S&S of drowsiness and sedation, especially in older adults or the debilitated; they may require supervised ambulation and/or side rails.
  • Lab tests: Monitor periodic blood counts, urinalyses, and blood chemistry studies, particularly during continuing therapy.

Patient & Family Education

  • Note: Adverse reactions that may occur during early high-dose therapy. These usually disappear with continuing therapy, but dosage adjustments may be indicated.
  • Make position changes slowly and in stages to prevent dizziness.
  • Do not use alcohol, other CNS depressants, or OTC medications containing antihistamines (e.g., sleep aids, cold, hay fever, or allergy remedies) without consulting physician.
  • Do not drive or engage in potentially hazardous activities until response to drug is known.
  • Taper dosage following continuous use; abrupt discontinuation of drug may cause withdrawal symptoms: nausea, vomiting, abdominal and muscle cramps, sweating, confusion, tremors, convulsions.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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