Alparazolam (Xanax)

Today's med: Alprazolam (al PRAY zoe lam) 

(brand names: Alprazolam Intensol, Xanax, Niravam)

Drug Class: Benzodiazepine

Other Drugs in this class:  Clonazepam,Lorazepam, Diazepam, Temazepam,Oxazepam, 

Triazolam, Clorazepate,Chlordiazepoxide, Midazolam, Estazolam,Clozapine, Clobazam, Flurazepam,

Flumazenil, Chlordiazepoxide hydrochloride,Clorazepate Dipotassium,Chlordiazepoxide/Amitriptyline,

Chlordiazepoxide/Clidinium bromide,Flurazepam hydrochloride

Indications: Treatment of anxiety disorder (GAD); short-term relief of symptoms of anxiety; panic disorder, with or without agoraphobia; anxiety associated with depression

Use: Unlabeled: Anxiety in children

Actions: Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.

Contraindications: Hypersensitivity to alprazolam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist); narrow-angle glaucoma; concurrent use with ketoconazole or itraconazole

Adverse Effects: >10%:

Central nervous system: Abnormal coordination, cognitive disorder, depression, drowsiness, fatigue, irritability, lightheadedness, memory impairment, sedation, somnolence

Endocrine & metabolic: Libido decreased

Gastrointestinal: Appetite increased/decreased, constipation, weight gain/loss, xerostomia

Genitourinary: Micturition difficulty

Neuromuscular & skeletal: Dysarthria

Respiratory: Nasal congestion

1% to 10%:

Cardiovascular: Chest pain, hypotension, palpitation, sinus tachycardia

Central nervous system: Agitation, akathisia, ataxia, attention disturbance, confusion, depersonalization, derealization, disorientation, disinhibition, dizziness, dream abnormalities, fear, hallucination, headache, hypersomnia, hypoesthesia, insomnia, lethargy, malaise, mental impairment, nervousness, nightmares, restlessness, seizure, syncope, talkativeness, vertigo

Dermatologic: Dermatitis, rash

Endocrine & metabolic: Dysmenorrhea, libido increased, menstrual disorders, sexual dysfunction

Gastrointestinal: Abdominal pain, anorexia, diarrhea, dyspepsia, nausea, salivation increased, vomiting

Genitourinary: Incontinence

Hepatic: Bilirubin increased, jaundice, liver enzymes increased

Neuromuscular & skeletal: Arthralgia, back pain, dyskinesia, dystonia, muscle cramps, muscle twitching, myalgia, paresthesia, tremor, weakness

Ocular: Blurred vision

Respiratory: Allergic rhinitis, dyspnea, hyperventilation, upper respiratory infection

Miscellaneous: Diaphoresis

<1% (Limited to important or life-threatening): Amnesia, angioedema, bilirubin increased, diplopia, falls, homicidal ideation, galactorrhea, gynecomastia, hepatic failure, hepatitis, hyperprolactinemia, hypomania, jaundice, liver enzymes increased, mania, peripheral edema, sleep apnea syndrome, Stevens-Johnson syndrome, suicidal ideation, syncope, tinnitus

Standard Dosing: 

Oral: Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug

Children: Anxiety (unlabeled use): Immediate release: Initial: 0.005 mg/kg/dose or 0.125 mg/dose 3 times/day; increase in increments of 0.125-0.25 mg, up to a maximum of 0.02 mg/kg/dose or 0.06 mg/kg/day (range of doses reported in one study: 0.375-3 mg/day) (Pfefferbaum, 1987). See "Dose Reduction" comment below.

Adults:

Anxiety: Immediate release: Initial: 0.25-0.5 mg 3 times/day; titrate dose upward every 3-4 days; usual maximum: 4 mg/day. Patients requiring doses >4 mg/day should be increased cautiously. Periodic reassessment and consideration of dosage reduction is recommended.

Panic disorder:

Immediate release: Initial: 0.5 mg 3 times/day; dose may be increased every 3-4 days in increments ≤1 mg/day. Mean effective dosage: 5-6 mg/day; some patients may require much as 10 mg/day

Extended release: 0.5-1 mg once daily; may increase dose every 3-4 days in increments ≤1 mg/day (range: 3-6 mg/day)

Switching from immediate release to extended release: Patients may be switched to extended release tablets by taking the total daily dose of the immediate release tablets and giving it once daily using the extended release preparation.

Preoperative anxiety (unlabeled use): 0.5 mg 60-90 minutes before procedure (De Witte, 2002)

Dose reduction: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg every 3 days; however, some patients may require a slower reduction. If withdrawal symptoms occur, resume previous dose and discontinue on a less rapid schedule.

Elderly: Note: Elderly patients may be more sensitive to the effects of alprazolam including ataxia and oversedation. The elderly may also have impaired renal function leading to decreased clearance. Titrate gradually, if needed and tolerated.

Immediate release: Initial: 0.25 mg 2-3 times/day

Extended release: Initial: 0.5 mg once daily

Administration

Immediate release preparations: Can be administered sublingually if oral administration is not possible; absorption and onset of effect are comparable to oral administration (Scavone,1987; Scavone, 1992)

Extended release tablet: Should be taken once daily in the morning; do not crush, break, or chew.

Orally-disintegrating tablets: Using dry hands, place tablet on top of tongue and allow to disintegrate. If using one-half of tablet, immediately discard remaining half (may not remain stable). Administration with water is not necessary.

Dietary Considerations

Extended release tablet should be taken once daily in the morning.

Drug interactions: Link: http://www.drugs.com/drug-interactions/alprazolam,xanax-xr.html

A total of 823 drugs (4656 brand and generic names) are known to interact with Xanax XR (alprazolam).

• 17 major drug interactions (56 brand and generic names)
• 705 moderate drug interactions (3789 brand and generic names)
• 101 minor drug interactions (811 brand and generic names)

Show all medications in the database that may interact with Xanax XR (alprazolam).

Concerns related to adverse effects:

• Anterograde amnesia: Benzodiazepines have been associated with anterograde amnesia.

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Paradoxical reactions: Paradoxical reactions, including hyperactive or aggressive behavior, have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients.

Disease-related concerns:

• Depression: Use caution in patients with depression, particularly if suicidal risk may be present; episodes of mania or hypomania have occurred in depressed patients treated with alprazolam.

• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use (generally >10 days).

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Renal impairment: Use with caution in patients with renal impairment or predisposition to urate nephropathy; has weak uricosuric properties.

• Respiratory disease: Use with caution in patients with respiratory disease.

Concurrent drug therapy issues:

• CNS depressants/psychoactive medications: Use with caution in patients receiving other CNS depressants or psychoactive medication; effects with other sedative drugs or ethanol may be potentiated.

• High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.

Other warnings/precautions:

• Appropriate use: Does not have analgesic, antidepressant, or antipsychotic properties.

• Breakthrough anxiety: At the end of dosing interval, breakthrough anxiety may occur.

• Withdrawal: Rebound or withdrawal symptoms, including seizures, may occur following abrupt discontinuation or large decreases in dose (more common in patients receiving >4 mg/day or prolonged treatment); the risk of seizures appears to be greatest 24-72 hours following discontinuation of therapy. Use caution when reducing dose or withdrawing therapy; decrease slowly (eg, ≤0.5 mg every 3 days) and monitor for withdrawal symptoms. Flumazenil may cause withdrawal in patients receiving long-term benzodiazepine therapy.

Monitoring Parameters

Respiratory and cardiovascular status

Al-pray for a Xanax....