Alprazolam


Description

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 tre...

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Pharmacology

Indication

Alprazolam is indicated for the management of anxiety disorder, anxiety associated with depression,... Read more

Pharmacodynamic

Alprazolam is indicated to treat anxiety and panic disorders.[Label] The mechanism by which its cell... Read more

Mechanism of action

Alprazolam is a triazolobenzodiazepine used to treat certain anxiety and panic disorders.[Label] Alp... Read more

Absorption

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

Protein binding

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

Route of elimination

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

Toxicity

Alprazolam overdose can present as sleepiness, confusion, poor coordination, slow reflexes, coma, an... 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.
    • Avoid excessive quantities of coffee or tea (Caffeine).
    • Avoid taking with grapefruit juice.
    • Take with food.

    Interactions

    Type in a drug name to check for interaction with Alprazolam

    The metabolism of Alprazolam can be decreased when combined with (R)-warfarin.
    The metabolism of Alprazolam can be decreased when combined with (S)-Warfarin.
    The risk or severity of adverse effects can be increased when Alprazolam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The therapeutic efficacy of Alprazolam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
    The metabolism of Alprazolam can be decreased when combined with 3,5-diiodothyropropionic acid.
    The risk or severity of adverse effects can be increased when Alprazolam is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Alprazolam.
    The risk or severity of adverse effects can be increased when Alprazolam is combined with 4-Methoxyamphetamine.
    The metabolism of Alprazolam can be decreased when combined with 5-androstenedione.
    The risk or severity of adverse effects can be increased when Alprazolam is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Alprazolam can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Alprazolam can be decreased when combined with 6-O-benzylguanine.
    The therapeutic efficacy of Alprazolam can be decreased when used in combination with 7-Deazaguanine.
    The metabolism of Alprazolam can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Alprazolam is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when Alprazolam is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    The therapeutic efficacy of Alprazolam can be decreased when used in combination with 7,9-Dimethylguanine.
    The therapeutic efficacy of Alprazolam can be decreased when used in combination with 8-azaguanine.
    The therapeutic efficacy of Alprazolam can be decreased when used in combination with 8-chlorotheophylline.
    The metabolism of Alprazolam can be decreased when combined with 9-aminocamptothecin.

    References

    • 1 . Dangkoob F, Housaindokht MR, Asoodeh A, Rajabi O, Rouhbakhsh Zaeri Z, Verdian Doghaei A: Spectroscopic and molecular modeling study on the separate and simultaneous bindings of alprazolam and fluoxetine hydrochloride to human serum albumin (HSA): with the aim of the drug interactions probing. Spectrochim Acta A Mol Biomol Spectrosc. 2015 Feb 25;137:1106-19. doi: 10.1016/j.saa.2014.08.149. Epub 2014 Oct 7. [PubMed: 25300043]
    • 2 . Greenblatt DJ, Wright CE: Clinical pharmacokinetics of alprazolam. Therapeutic implications. Clin Pharmacokinet. 1993 Jun;24(6):453-71. doi: 10.2165/00003088-199324060-00003. [PubMed: 8513649]
    • 3 . George TT, Tripp J: Alprazolam . [PubMed: 30844192]
    • 4 . Verster JC, Volkerts ER: Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature. CNS Drug Rev. 2004 Spring;10(1):45-76. [PubMed: 14978513]
    • 5 . Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed: 19515014]
    • 6 . Williams JA, Ring BJ, Cantrell VE, Jones DR, Eckstein J, Ruterbories K, Hamman MA, Hall SD, Wrighton SA: Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos. 2002 Aug;30(8):883-91. [PubMed: 12124305]
    • 7 . FDA Approved Drug Products: Xanax [Link]
    • 8 . FDA Pregnancy Categories [Link]
    • 9 . Flockhart Table of Drug Interactions [Link]

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