Drug Study: alprazolam (Apo-Alpraz (CAN), Novo-Alprazol (CAN), Nu-Alpraz (CAN), Xanax, Xanax TS (CAN), Xanax XR)

Generic Name: alprazolam

Brands: Apo-Alpraz (CAN), Novo-Alprazol (CAN), Nu-Alpraz (CAN), Xanax, Xanax TS (CAN), Xanax XR

Pregnancy Category D
Controlled Substance C-IV

Drug classes
Benzodiazepine
Anxiolytic

Therapeutic actions
Exact mechanisms of action not understood; main sites of action may be the limbic system and reticular formation; increases the effects of gamma-aminobutyrate, an inhibitory neurotransmitter; anxiety blocking effects occur at doses well below those necessary to cause sedation, ataxia.

Indications
• Management of anxiety disorders, short-term relief of symptoms of anxiety; anxiety associated with depression.
• Treatment of panic attacks with or without agoraphobia
• Unlabeled uses: Social phobia, premenstrual syndrome, depression

Contraindications and cautions

• Contraindicated with hypersensitivity to benzodiazepines, psychoses, acute narrow-angle glaucoma, shock, coma, acute alcoholic intoxication with depression of vital signs, pregnancy (crosses the placenta; risk of congenital malformations, neonatal withdrawal syndrome), labor and delivery (”floppy infant” syndrome), lactation (secreted in breast milk; infants become lethargic and lose weight).
• Use cautiously with impaired liver or kidney function, debilitation.

Available forms

Tablets—0.25, 0.5, 1, 2 mg; XR tablets—0.5, 1, 2, 3 mg; intensol solution—1 mg/mL

Dosages
Individualize dosage; increase dosage gradually to avoid adverse effects.
ADULTS
• Anxiety disorders: Initially, 0.25–0.5 mg PO tid; adjust to maximum daily dose of 4 mg/day in divided doses or extended-release form once per day in the AM once dosage is established.
• Panic disorder: Initially, 0.5 mg PO tid; increase dose at 3- to 4-day intervals in increments of no more than 1 mg/day; ranges of 1–10 mg/day have been needed; extended-release form once per day in AM once dosage is established.
• Social phobia: 2–8 mg/day PO.
• Premenstrual syndrome: 0.25 mg PO tid.
GERIATRIC PATIENTS OR PATIENTS WITH DEBILITATING DISEASE
Initially, 0.25 mg bid–tid PO; gradually increase if needed and tolerated; ER tablets—0.5 mg PO once each day

Pharmacokinetics

Route

Onset

Peak

Duration

Oral

30 min

1–2 hr

4–6 hr

Metabolism: Hepatic; T1/2: 6.3–26.9 hr
Distribution: Crosses placenta; enters breast milk
Excretion: Urine


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