Alprazolam
Indications
Alprazolam is used for:
Anxiety disorders, Panic disorders, Nausea due to chemotherapy
Adult Dose
Oral
Short-term management of anxiety
Adult: 0.25-0.5 mg tid, increased to 3-4 mg daily if necessary.
Elderly: Initially, 0.25 mg bid/tid.
Panic attacks
Adult
Immediate-release
0.5 mg PO q8hr; may increase q3-4Days by ?1 mg/day
Average dose: 5-6 mg/day PO
May require up to 10 mg/day PO divided q8hr
Extended-release
0.5-1 mg PO qDay; may increase q3-4Days by <1 mg/day
Average dose: 3-6 mg PO qDay
Anxiety Associated With Depression
1-4 mg/day PO divided q8hr
Hepatic impairment: Avoid in severe impairment.
Child Dose
<18 years old: Not recommended
Renal Dose
Renal impairment: Use caution; not studied
Administration
Administration May be taken with or without food. Side effects eg sleepiness/drowsiness may be reduced if taken immediately after meals.
Contra Indications
Acute narrow-angle glaucoma, preexisting CNS depression or coma, resp depression, acute pulmonary insufficiency or sleep apnoea; severe hepatic impairment; pregnancy, lactation.
Precautions
Dosage reduction or gradual withdrawal. Dependence. Geriatric or debilitated patients. Muscle weakness, impaired hepatic or renal function; arteriosclerosis; obesity; depression particularly suicidal tendency; chronic pulmonary insufficiency. May impair ability to drive or operate machinery. Children <18 yr.
Lactation: Enters breast milk/not recommended
Pregnancy-Lactation
Interactions
Potentiates action of alcohol and CNS depressants. Reduced conc with cigarette smoking by 50%.
Potentially Fatal: Cimetidine and fluoxetine reduce the clearance of alprazolam. Alprazolam enhances activity of imipramine and desipramine.
Adverse Effects
Side effects of Alprazolam :
>10% (4 mg dose)
Drowsiness (41%),Depression (10-15%),Headache (10-15%),Constipation (10-15%),Diarrhea (10-15%),Dry mouth (10-15%)
>10% (10 mg dose)
Drowsiness (77%),Impaired coordination (40-50%),Increased appetite (30-35%),Fatigue (30-35%),Memory impairment (30-35%),Irritability (30-35%),Decreased salivation (30-35%),Cognitive disorders (20-30%),Insomnia (20-30%),Dcreased appetite (20-30%),Headache (20-30%),Lightheadedness (20-30%),Dysarthria (20-30%),Diarrhea, constipation, and nausea/vomiting (20-30%),Weight change (20-30%),Nasal congestion (15-20%),Decreased or increased libido (10-15%),Menstrual disorder (10-15%),Difficult micturition (10-15%)
1-10% (4 mg dose)
Tachycardia (5-10%),Confusion (5-10%),Insomnia (5-10%),Nausea/vomiting (5-10%),Blurred vision (5-10%),Nasal congestion (5-10%),Hypotension (1-5%),Syncope (1-5%),Akathisia (1-5%),Dizziness (1-5%),Increased salivation (1-5%),Nervousness (1-5%),Tremor (1-5%),Weight change (1-5%)
1-10% (10 mg dose)
Increased salivation (5-10%),Talkativeness (1-5%),Incontinence (1-5%)
Potentially Fatal: Blood dyscrasias.
Mechanism of Action
Alprazolam has anxiolytic, muscle-relaxant, anticonvulsant, antidepressant and sleep-modifying effects. It binds to the ? aminobutyric acid (GABA)-specific sites throughout the CNS, leading to an increase in the inhibitory effect of GABA on neuronal excitability. Increased neuronal permeability to chloride ions thus results in hyperpolarisation and stabilisation.