Description

Simple

A sedative medication used to help with panic attacks and anxiety including anxiety that is related to depression.

Clinical

A long-acting benzodiazepine with intermediate onset commonly used to treat panic disorders and generalized anxiety in addition to anxiety associated with depression.

Overview

Alprazolam is a triazolobenzodiazepine indicated for the treatment of anxiety and panic disorders.[Label] It is mainly metabolized by CYP3As and so is contraindicated with CYP3A inhibitors like ketoconazole and itraconazole.[Label] Benzodiazepine treatment should be stopped gradually by tapering down a patient's dose to avoid withdrawal symptoms.[4] Alprazolam's adverse effects are generally related to the sedation it can cause.[4] Alprazolam has been mixed with alcohol as a drug of abuse to potentiate the sedative effects of the drug which may lead to coma and death.[4] Alprazolam was given FDA approval on October 16, 1981[7].

Pharmacology

Indication

Alprazolam is indicated for the management of anxiety disorder, anxiety associated with depression, panic disorder, and panic disorder with agoraphobia.[Label] Alprazolam may also be prescribed off label for insomnia, premenstrual syndrome, and depression.[ Read more

Pharmacodynamic

Alprazolam is indicated to treat anxiety and panic disorders.[Label] The mechanism by which its cell receptor interactions translate to a clinical effect is not known.[Label,3, Read more

Mechanism of action

Alprazolam is a triazolobenzodiazepine used to treat certain anxiety and panic disorders.[Label] Alprazolam acts on benzodiazepine receptors BNZ-1 and BNZ-2.[Label,3, Read more

Absorption

Oral bioavailability of a standard release tablet of alprazolam is 84-91% with a time to maximum concentration of 1.8 hours.[ Read more

Protein binding

Alprazolam is 80% protein bound in serum.[Label] The majority of this protein binding is to serum albumin.[Label, Read more

Volume of distribution

Volume of distribution following oral administration is 0.8-1.3L/kg.[ Read more

Clearance

Oral clearance is 0.90±0.21mL/min/kg but this increases to 2.13±0.54mL/min/kg when given with CYP3A inducers.[Label] Other studies have demonstrated a clearance of 0.70-1.5mL/min/kg.[ Read more

Half life

11.2 hours in healthy patients.[Label] The half life is 16.3h in the elderly, 5.8-65.3h in patients with alcoholic liver disease, 9.9-40.4h in obese patients.[Label] The half life is 25% higher in Asian patients compared to Caucasians.[Label] Other studies have shown the half life to be 9-16h.[ Read more

Route of elimination

Alprazolam is mainly eliminated in the urine.[Label] A large portion of the dose is eliminated as unmetabolized alprazolam.[ Read more

Toxicity

Alprazolam overdose can present as sleepiness, confusion, poor coordination, slow reflexes, coma, and death.[Label] Taking alprazolam with alcohol lowers the threshold for overdose.[Label] Patients should have their respiration, pulse, and blood pressure monitored.[Label] Patients can be treated by... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Drowsiness US
  • Kind: experimental
    • Percent: 76.8%
  • Kind: placebo
    • Percent: 42.7%
  • Clinical Trial
    Fatigue and tiredness US
  • Kind: experimental
    • Percent: 48.6%
  • Kind: placebo
    • Percent: 42.3%
  • Clinical Trial
    Drowsiness US
  • Kind: experimental
    • Percent: 41%
  • Kind: placebo
    • Percent: 21.6%
  • Clinical Trial
    Impaired coordination US
  • Kind: experimental
    • Percent: 40.1%
  • Kind: placebo
    • Percent: 17.9%
  • Clinical Trial
    Memory Impairment US
  • Kind: experimental
    • Percent: 33.1%
  • Kind: placebo
    • Percent: 22.1%
  • Clinical Trial
    Irritability US
  • Kind: experimental
    • Percent: 33.1%
  • Kind: placebo
    • Percent: 30.1%
  • Clinical Trial
    Increased appetite US
  • Kind: experimental
    • Percent: 32.7%
  • Kind: placebo
    • Percent: 22.8%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 29.5%
  • Clinical Trial
    Cognitive Disorder US
  • Kind: experimental
    • Percent: 28.8%
  • Kind: placebo
    • Percent: 20.5%
  • Clinical Trial
    Decreased appetite US
  • Kind: experimental
    • Percent: 27.8%
  • Kind: placebo
    • Percent: 24.1%
  • Clinical Trial
    Weight Gain US
  • Kind: experimental
    • Percent: 27.2%
  • Kind: placebo
    • Percent: 17.9%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 26.2%
  • Kind: placebo
    • Percent: 15.4%
  • Clinical Trial
    Dysarthria US
  • Kind: experimental
    • Percent: 23.3%
  • Kind: placebo
    • Percent: 6.3%
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: 22.6%
  • Kind: placebo
    • Percent: 16.5%
  • Clinical Trial
    Lightheadedness US
  • Kind: experimental
    • Percent: 20.8%
  • Kind: placebo
    • Percent: 19.3%
  • Clinical Trial
    Lightheadedness US
  • Kind: experimental
    • Percent: 19.3%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 19.2%
  • Clinical Trial
    Fatigue and tiredness US
  • Kind: experimental
    • Percent: 18.4%
  • Clinical Trial
    Nasal Congestion US
  • Kind: experimental
    • Percent: 17.4%
  • Kind: placebo
    • Percent: 16.5%
  • Clinical Trial
    Abnormal involuntary movement US
  • Kind: experimental
    • Percent: 17.3%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 17%
  • Clinical Trial
    Nausea/Vomiting US
  • Kind: experimental
    • Percent: 16.5%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 14.7%
  • Kind: placebo
    • Percent: 13.3%
  • Clinical Trial
    Sweating US
  • Kind: experimental
    • Percent: 14.4%
  • Clinical Trial
    Decreased libido US
  • Kind: experimental
    • Percent: 14.4%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 13.6%
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: 13.3%
  • Clinical Trial
    Decreased appetite US
  • Kind: experimental
    • Percent: 12.8%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: 12.2%
  • Clinical Trial
    Micturition difficulties US
  • Kind: experimental
    • Percent: 12.2%
  • Kind: placebo
    • Percent: 8.6%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 10.8%
  • Kind: placebo
    • Percent: 8.1%
  • Clinical Trial
    Decreased salivation US
  • Kind: experimental
    • Percent: 10.6%
  • Clinical Trial
    Irritability US
  • Kind: experimental
    • Percent: 10.5%
  • Clinical Trial
    Menstrual disorders US
  • Kind: experimental
    • Percent: 10.4%
  • Kind: placebo
    • Percent: 8.7%
  • Clinical Trial
    Confusional state US
  • Kind: experimental
    • Percent: 10.4%
  • Kind: placebo
    • Percent: 8.2%
  • Clinical Trial
    Cognitive Disorder US
  • Kind: experimental
    • Percent: 10.3%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Increased libido US
  • Kind: experimental
    • Percent: 7.7%
  • Kind: placebo
    • Percent: 4.1%
  • Clinical Trial
    Sexual Dysfunction US
  • Kind: experimental
    • Percent: 7.4%
  • Kind: placebo
    • Percent: 3.7%
  • Clinical Trial
    Changes in libido US
  • Kind: experimental
    • Percent: 7.1%
  • Kind: placebo
    • Percent: 5.6%
  • Clinical Trial
    Muscular twitching US
  • Kind: experimental
    • Percent: 6.9%
  • Clinical Trial
    Impaired coordination US
  • Kind: experimental
    • Percent: 6.6%
  • Clinical Trial
    Muscle tone disorders US
  • Kind: experimental
    • Percent: 5.9%
  • Clinical Trial
    Weakness US
  • Kind: experimental
    • Percent: 5.8%
  • Clinical Trial
    Increased salivation US
  • Kind: experimental
    • Percent: 5.6%
  • Kind: placebo
    • Percent: 4.4%
  • Clinical Trial
    Memory Impairment US
  • Kind: experimental
    • Percent: 5.5%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 5.1%
  • Clinical Trial
    Confusional state US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 4.7%
  • Kind: placebo
    • Percent: 2.2%
  • Clinical Trial
    Upper Respiratory Infection US
  • Kind: experimental
    • Percent: 4.3%
  • Kind: placebo
    • Percent: 3.7%
  • Clinical Trial

    Contraindications

    • Hypersensitivity:
      • true
    • Recommended Actions:
      • Avoid
    • Sex Group: all
    • Regions: US
    • Route:
      • Oral
    • Regions: US
    • With Drugs Coadmin:
        • Name: Ketoconazole
        • Drugbank Id: DB01026
    • Route:
      • Oral
    • Regions: US
    • With Drugs Coadmin:
        • Name: Itraconazole
        • Drugbank Id: DB01167

    Food Interactions

    Avoid alcohol. Alcohol may potentiate the CNS depressant effects of this drug.

    Avoid grapefruit products.

    Limit caffeine intake.

    Take with or without food. Food increases the Cmax of extended release alprazolam by 25%, but the AUC and half life are not affected.