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

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
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Alprazolam.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Alprazolam.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Alprazolam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Alprazolam is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Alprazolam is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Alprazolam is combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The metabolism of Alprazolam can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 6-O-benzylguanine.
7-Deazaguanine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 7-Deazaguanine.
7-ethyl-10-hydroxycamptothecin
The metabolism of Alprazolam can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Alprazolam is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Alprazolam is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
7,9-Dimethylguanine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 7,9-Dimethylguanine.
8-azaguanine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 8-azaguanine.
8-chlorotheophylline
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 8-chlorotheophylline.
9-aminocamptothecin
The metabolism of Alprazolam can be decreased when combined with 9-aminocamptothecin.
9-Deazaguanine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 9-Deazaguanine.
9-Methylguanine
The therapeutic efficacy of Alprazolam can be decreased when used in combination with 9-Methylguanine.
Abacavir
Alprazolam may decrease the excretion rate of Abacavir which could result in a higher serum level.
9 References
  1. 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. 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. 3 . George TT, Tripp J: Alprazolam .PubMed: 30844192
  4. 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. 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. 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. 7 . FDA Approved Drug Products: Xanax Link
  8. 8 . FDA Pregnancy Categories Link
  9. 9 . Flockhart Table of Drug Interactions Link