Trade Names:Alprazolam Intensol- Oral solution 1 mg/mL
Trade Names:Xanax- Tablets 0.25 mg- Tablets 0.5 mg- Tablets 1 mg- Tablets 2 mg
Trade Names:Xanax XR- Tablets, extended-release 0.5 mg- Tablets, extended-release 1 mg- Tablets, extended-release 2 mg- Tablets, extended-release 3 mg
Trade Names:Niravam- Orally disintegrating tablets 0.25 mg- Orally disintegrating tablets 0.5 mg- Orally disintegrating tablets 1 mg- Orally disintegrating tablets 2 mgApo-Alpraz (Canada)Apo-Alpraz TS (Canada)Gen-Alprazolam (Canada)Xanax TS (Canada)
Potentiates action of GABA, an inhibitory neurotransmitter, resulting in increased neuronal inhibition and CNS depression, especially in limbic system and reticular formation.
Readily absorbed; T max is 1 to 2 h; C max is 8 to 37 ng/mL (0.5 to 3 mg doses).
80% protein bound. Crosses the placenta and is excreted in breast milk.
Metabolized in the liver to alpha-hydroxy-alprazolam (activity is approximately 50% that of alprazolam) and a benzophenone derivative (inactive).
The t ½ is approximately 16.3 h. Excreted in the urine.
The t ½ is approximately 19.7 h in those with alcoholic liver disease.Elderly
The t ½ is approximately 16.3 h.Obese
The t ½ is approximately 21.8 h.
Treatment of panic disorders with or without agoraphobia ( Niravam , Xanax , Xanax XR ); management of anxiety disorders or for short-term relief of symptoms of anxiety, including anxiety associated with depression ( Niravam , immediate-release tablets and oral solution).
Treatment of irritable bowel syndrome, depression, PMS.
Hypersensitivity to other benzodiazepines; acute narrow-angle glaucoma; patients receiving itraconazole or ketoconazole.
PO Immediate-release tablets: 0.5 mg 3 times daily; if needed, increase by max 1 mg/day every 3 to 4 day. May require more than 4 mg/day. Extended-release tablets: start with 0.5 to 1 mg daily (suggested daily dose ranges between 3 and 6 mg).Anxiety Disorder (Immediate-Release Tablets and Oral Solution)Adults
PO Immediate-release tablets and oral solution: 0.25 to 0.5 mg 3 times daily (max, 4 mg/day in divided doses). Extended-release tablets: Start with 0.5 mg daily and gradually increase if needed (suggested total daily dose range 3 to 6 mg/day).Elderly/Debilitated PatientsAdults
PO Immediate-release tablets: 0.25 mg 2 to 3 times daily; may increase dose gradually. Extended-release tablets: 0.25 mg 2 to 3 times daily. May increase dose gradually.
Store immediate-release tablets below 77°F. Store extended-release tablets, orally disintegrating tablets, and oral solution at controlled room temperature (59° to 86°F). Protect orally disintegrating tablets from moisture.
Produce additive CNS depressant effects.Cimetidine, disulfiram, oral contraceptives
May increase effects of alprazolam, producing excessive sedation and impaired psychomotor function.Desipramine, imipramine
Plasma concentrations of these agents may be increased by alprazolam.Digoxin
Serum digoxin concentrations may increase.Drugs that affect salivary flow and stomach pH
May slow dissolution or disintegration, resulting in slowed or decreased Niravam absorption.Drugs that induce CYP3A4 metabolism (eg, carbamazepine, rifamycins)
May decrease alprazolam plasma levels.Drugs that inhibit CYP3A4 metabolism (eg, diltiazem, fluoxetine, fluvoxamine, grapefruit juice, isoniazid, macrolide antibiotics [eg, erythromycin], nefazodone, nonnucleoside reverse transcriptase inhibitors [eg, delavirdine, efavirenz], protease inhibitors [eg, indinavir])
May increase alprazolam plasma concentrations.Itraconazole, ketoconazole
Concurrent use with alprazolam is contraindicated.Omeprazole
May increase serum levels of alprazolam and enhance alprazolam's effects.Theophyllines
May antagonize sedative effects of alprazolam.
None well documented.
Tachycardia (15%); hypotension (5%); palpitation (at least 1%).
Drowsiness (77%); fatigue/tiredness (49%); sedation (45%); irritability, memory impairment (33%); cognitive disorder (29%); somnolence (23%); light-headedness (21%); decreased libido (14%); depression (12%); dysarthria (11%); confusional state (10%); abnormal coordination (9%); ataxia, mental impairment (7%); disturbed attention, impaired balance, disinhibition (3%); disorientation, paresthesia, dyskinesia, talkativeness, derealization, abnormal dreams, lethargy (2%); anxiety, hypesthesia, hypersomnia, fear, warm feeling (1%); malaise, weakness, headache, dizziness, tremor, irritability, insomnia, nervousness, increased libido, restlessness, agitation, depersonalization, nightmare (at least 1%).
Rash (11%); increased sweating (at least 1%); Stevens-Johnson syndrome (postmarketing).
Nasal congestion (17%); allergic rhinitis (1%); vertigo, blurred vision (at least 1%).
Constipation (26%); nausea/vomiting (22%); diarrhea (21%); abdominal distress (18%); dry mouth (15%); increased salivation (6%); dyspepsia, abdominal pain (at least 1%).
Micturition difficulties (12%); menstrual disorders (10%); dysmenorrhea (4%); sexual dysfunction, PMS, incontinence (2%); gynecomastia (postmarketing).
Increased liver enzymes, hepatitis, hepatic failure (postmarketing).
Increased appetite (33%); decreased appetite (28%); weight gain (27%); weight loss (23%); edema (5%); anorexia (2%).
Rigidity (4%); arthralgia, myalgia (2%); limb pain (1%); back pain, muscle cramps, muscle twitching (at least 1%).
Upper respiratory tract infection (4%); dyspnea (2%); hyperventilation (at least 1%).
Chest pain (at least 1%); hyperprolactinemia (postmarketing).
Frequently assess patient for response to treatment. Notify health care provider if condition does not appear to be improving or worsens. Ensure therapy is periodically reviewed to determine if it needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated.
Category D .
Excreted in breast milk.
Safety and efficacy in children younger than 18 yr of age not established.
Use smallest effective dose to preclude development of ataxia or overdosage.
Caution is needed to avoid accumulation of drug.
Caution is needed to avoid accumulation of drug.
Prolonged use can lead to physical and psychological dependence. Withdrawal syndrome has occurred within 4 to 6 wk of treatment, especially if abruptly discontinued. Cautious use and tapering of dosage are necessary.
There is a risk of fetal harm (eg, congenital abnormalities) when used during pregnancy.
Death has been reported in patients with pulmonary disease shortly after starting alprazolam treatment.
Early morning anxiety and emergence of anxiety symptoms have been reported between doses in patients with panic disorder.
Hypomania and mania have been reported.
Not intended for patients with primary depressive disorder, psychoses, or disorders in which anxiety is not prominent.
May occur during abrupt drug discontinuation or dose reduction.
Use with caution in patients with suicidal tendencies; do not allow access to large quantities of drug.
If treatment is to be discontinued or the dose reduced, gradually taper the dose (eg, no more than 0.5 mg every 3 days). Monitor patient for withdrawal symptoms (eg, increased anxiety, tremor, muscle or abdominal cramps, sweating). If significant withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.
Somnolence, confusion, impaired coordination, diminished reflexes, coma, death.
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