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)
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.
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.
Abatacept
The metabolism of Alprazolam can be increased when combined with Abatacept.
Abiraterone
The metabolism of Alprazolam can be decreased when combined with Abiraterone.
Acalabrutinib
The metabolism of Alprazolam can be decreased when combined with Acalabrutinib.
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