Peringatan Keamanan

Alprazolam overdose can present as sleepiness, confusion, poor coordination, slow reflexes, coma, and death.L34783, L34788 Taking alprazolam with alcohol lowers the threshold for overdose.L34783, L34788 Patients should have their respiration, pulse, and blood pressure monitored.L34783, L34788 Patients can be treated by gastric lavage and intravenous fluids.L34783, L34788. If hypotension occurs, patients may be treated with vasopressors.L34783, L34788 In known, or suspected overdoses, patients can be given the benzodiazepine receptor antagonist flumazenil in addition to other methods of management.L34783, L34788

Oral LD50 in rats is 331-2171mg/kg.Label

Alprazolam

DB00404

small molecule approved illicit investigational

Deskripsi

Alprazolam is a triazolobenzodiazepine indicated for the treatment of anxiety and panic disorders.L34783, L34788 It is mainly metabolized by CYP3As and so is contraindicated with CYP3A inhibitors like ketoconazole and itraconazole.L34783, L34788 Benzodiazepine treatment should be stopped gradually by tapering down a patient's dose to avoid withdrawal symptoms.A18125 Alprazolam's adverse effects are generally related to the sedation it can cause.A18125 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.A18125 Alprazolam was given FDA approval on October 16, 1981.L6148

Struktur Molekul 2D

Berat 308.765
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Alprazolam has a mean plasma elimination half-life of 11.2 hours in healthy patients (range 6.3-26.9 hours).[L34783] The mean half-life is 16.3 hours (range 9.0-26.9 hours) in the elderly, 21.8 hours (range 9.9-40.4 hours) in obese patients, and 19.7 hours (range 5.8-65.3 hours) in patients with alcoholic liver disease.[L34783] The half-life is 25% higher in Asian patients compared to Caucasians.[L34783] Other studies have shown the half-life to be 9-16h.[A177925] The extended-release formulation has a half-life of 10.7-15.8 hours in healthy adult patients.[L34788]
Volume Distribusi Alprazolam has a volume of distribution following oral administration of 0.8-1.3L/kg.[A177925] Alprazolam crosses the blood-brain barrier.[A18125]
Klirens (Clearance) A 0.8 mg oral dose of alprazolam had a clearance of 0.90 ± 0.21 mL/min/kg, which increased to 2.13 ± 0.54 mL/min/kg when coadministered with the strong CYP3A4 inducer carbamazepine.[L34783, L34788] Other studies have demonstrated a clearance of 0.70-1.5mL/min/kg.[A177925]

Absorpsi

Alprazolam administered orally is rapidly absorbed in the gastrointestinal tract, reaching Cmax in about 1.8 (1-2) hours. Absorption is high, resulting in an oral bioavailability of 84-91%. A 1 mg oral dose results in a Cmax of 12-22 ?g/L.A177925, L34783 The extended-release formulation of alprazolam (XANAX XR) has similar absorption, bioavailability, and pharmacokinetics as the standard release, with the exception that the Tmax is ~10 hours compared to 1-2 hours. Temporal dosing alters these parameters, with Cmax increasing by 30% and Tmax decreasing by one hour when dosed at night as opposed to in the morning.L34788 Food has an effect on alprazolam absorption; a high-fat meal up to two hours before dosing increases the Cmax by ~25% and either a reduction (food consumed immediately prior to dosing) or increase (food consumed after dosing) of ~1/3 in Tmax. Neither the AUC nor half-life are appreciably affected by eating.L34788

Metabolisme

Alprazolam is metabolized to less effective metabolites by various CYPs including CYP3A4, CYP3A5, CYP3A7, and CYP2C9.A415, A14775, L162, L34783, L34788 The majority of alprazolam metabolism is mediated by hydroxylation via CYP3As.A415, A14775, A177925, L162, L34783, L34788 4-hydroxyalprazolam has 20% the binding affinity of the parent drug, alpha-hydroxyalprazolam has 66% the affinity, and the benzophenone metabolite has <1% the affinity.A177925, L34783, L34788

Rute Eliminasi

Alprazolam is mainly eliminated in the urine.L34783, L34788 A large portion of the dose is eliminated as unmetabolized alprazolam.A177925 <10% of the dose is eliminated as alpha-hydroxy-alprazolam and 4-hydroxy-alprazolam.A177925

Interaksi Makanan

4 Data
  • 1. Avoid alcohol. Alcohol may potentiate the CNS depressant effects of this drug.
  • 2. Avoid grapefruit products.
  • 3. Limit caffeine intake.
  • 4. Take with or without food. Food increases the Cmax of extended release alprazolam by 25%, but the AUC and half life are not affected.

Interaksi Obat

1650 Data
Fluvoxamine The serum concentration of Alprazolam can be increased when it is combined with Fluvoxamine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Dronabinol The metabolism of Alprazolam can be decreased when combined with Dronabinol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Hydrocodone Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Magnesium sulfate The therapeutic efficacy of Alprazolam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Alprazolam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Paraldehyde Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Pramipexole Alprazolam may increase the sedative activities of Pramipexole.
Ropinirole Alprazolam may increase the sedative activities of Ropinirole.
Rotigotine Alprazolam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Alprazolam.
Suvorexant Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Thalidomide Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Sodium oxybate Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Alprazolam can be increased when it is combined with Teduglutide.
Yohimbine The therapeutic efficacy of Alprazolam can be increased when used in combination with Yohimbine.
Sirolimus The serum concentration of Alprazolam can be increased when it is combined with Sirolimus.
Temsirolimus The serum concentration of Alprazolam can be increased when it is combined with Temsirolimus.
Miocamycin The serum concentration of Alprazolam can be increased when it is combined with Miocamycin.
Josamycin The serum concentration of Alprazolam can be increased when it is combined with Josamycin.
Clindamycin The serum concentration of Alprazolam can be increased when it is combined with Clindamycin.
Ixabepilone The serum concentration of Alprazolam can be increased when it is combined with Ixabepilone.
Mepartricin The serum concentration of Alprazolam can be increased when it is combined with Mepartricin.
Tilmicosin The serum concentration of Alprazolam can be increased when it is combined with Tilmicosin.
Tylosin The serum concentration of Alprazolam can be increased when it is combined with Tylosin.
Tylvalosin The serum concentration of Alprazolam can be increased when it is combined with Tylvalosin.
Asunaprevir The serum concentration of Alprazolam can be increased when it is combined with Asunaprevir.
Fosamprenavir The serum concentration of Alprazolam can be increased when it is combined with Fosamprenavir.
TMC-310911 The serum concentration of Alprazolam can be increased when it is combined with TMC-310911.
Everolimus The serum concentration of Alprazolam can be increased when it is combined with Everolimus.
Viloxazine The metabolism of Alprazolam can be decreased when combined with Viloxazine.
Etoposide The metabolism of Alprazolam can be decreased when combined with Etoposide.
Aldesleukin The metabolism of Alprazolam can be decreased when combined with Aldesleukin.
Octreotide The metabolism of Alprazolam can be decreased when combined with Octreotide.
Fluconazole The metabolism of Alprazolam can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Alprazolam can be increased when it is combined with Erythromycin.
Citalopram The metabolism of Alprazolam can be decreased when combined with Citalopram.
Nelfinavir The serum concentration of Alprazolam can be increased when it is combined with Nelfinavir.
Indinavir The serum concentration of Alprazolam can be increased when it is combined with Indinavir.
Lovastatin The metabolism of Alprazolam can be decreased when combined with Lovastatin.
Ziprasidone The metabolism of Alprazolam can be decreased when combined with Ziprasidone.
Cabergoline The metabolism of Alprazolam can be decreased when combined with Cabergoline.
Diethylstilbestrol The metabolism of Alprazolam can be decreased when combined with Diethylstilbestrol.
Isradipine The metabolism of Alprazolam can be decreased when combined with Isradipine.
Valproic acid The metabolism of Alprazolam can be decreased when combined with Valproic acid.
Acetaminophen The metabolism of Alprazolam can be decreased when combined with Acetaminophen.
Dihydroergotamine The metabolism of Alprazolam can be decreased when combined with Dihydroergotamine.
Terfenadine The metabolism of Alprazolam can be decreased when combined with Terfenadine.
Diltiazem The metabolism of Alprazolam can be decreased when combined with Diltiazem.
Methylergometrine The metabolism of Alprazolam can be decreased when combined with Methylergometrine.
Mefloquine The metabolism of Alprazolam can be decreased when combined with Mefloquine.
Clozapine The risk or severity of adverse effects can be increased when Alprazolam is combined with Clozapine.
Mirtazapine The metabolism of Alprazolam can be decreased when combined with Mirtazapine.
Sorafenib The metabolism of Alprazolam can be decreased when combined with Sorafenib.
Nitric Oxide The metabolism of Alprazolam can be decreased when combined with Nitric Oxide.
Cerivastatin The metabolism of Alprazolam can be decreased when combined with Cerivastatin.
Teniposide The metabolism of Alprazolam can be decreased when combined with Teniposide.
Chloramphenicol The metabolism of Alprazolam can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Alprazolam can be decreased when combined with Lansoprazole.
Quinine The metabolism of Alprazolam can be decreased when combined with Quinine.
Raloxifene The metabolism of Alprazolam can be decreased when combined with Raloxifene.
Cimetidine The metabolism of Alprazolam can be decreased when combined with Cimetidine.
Haloperidol The metabolism of Alprazolam can be decreased when combined with Haloperidol.
Ritonavir The serum concentration of Alprazolam can be increased when it is combined with Ritonavir.
Erlotinib The metabolism of Alprazolam can be decreased when combined with Erlotinib.
Ciprofloxacin The metabolism of Alprazolam can be decreased when combined with Ciprofloxacin.
Zafirlukast The metabolism of Alprazolam can be decreased when combined with Zafirlukast.
Vinblastine The metabolism of Alprazolam can be decreased when combined with Vinblastine.
Fluticasone propionate The metabolism of Alprazolam can be decreased when combined with Fluticasone propionate.
Thiopental The metabolism of Alprazolam can be decreased when combined with Thiopental.
Imatinib The metabolism of Alprazolam can be decreased when combined with Imatinib.
Nicardipine The metabolism of Alprazolam can be decreased when combined with Nicardipine.
Efavirenz The metabolism of Alprazolam can be decreased when combined with Efavirenz.
Astemizole The metabolism of Alprazolam can be decreased when combined with Astemizole.
Dextropropoxyphene The metabolism of Alprazolam can be decreased when combined with Dextropropoxyphene.
Verapamil The metabolism of Alprazolam can be decreased when combined with Verapamil.
Epinephrine The metabolism of Alprazolam can be decreased when combined with Epinephrine.
Aprepitant The metabolism of Alprazolam can be decreased when combined with Aprepitant.
Tamoxifen The metabolism of Alprazolam can be decreased when combined with Tamoxifen.
Midazolam The metabolism of Alprazolam can be decreased when combined with Midazolam.
Daunorubicin The metabolism of Alprazolam can be decreased when combined with Daunorubicin.
Ergotamine The metabolism of Alprazolam can be decreased when combined with Ergotamine.
Amprenavir The serum concentration of Alprazolam can be increased when it is combined with Amprenavir.
Delavirdine The metabolism of Alprazolam can be decreased when combined with Delavirdine.
Paroxetine The metabolism of Alprazolam can be decreased when combined with Paroxetine.
Tranylcypromine The metabolism of Alprazolam can be decreased when combined with Tranylcypromine.
Tetracycline The metabolism of Alprazolam can be decreased when combined with Tetracycline.
Methimazole The metabolism of Alprazolam can be decreased when combined with Methimazole.
Roxithromycin The metabolism of Alprazolam can be decreased when combined with Roxithromycin.
Phenelzine The metabolism of Alprazolam can be decreased when combined with Phenelzine.
Propofol The metabolism of Alprazolam can be decreased when combined with Propofol.

Target Protein

GABA(A) Receptor GABRA1
Translocator protein TSPO
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Synthesis reference: Hester, J.B., Jr.; US. Patent 3,681,343; August 1,1972; assigned to The Upjohn Company. Hester, J.B., Jr.; US.Patent 3,781,289; December 25,1973;assigned to The Upjohn Company. Hester, J.B., Jr.; U S . Patent 3,709898; January 9,1973; assigned to The Upjohn Company.
Artikel (PubMed)
  • PMID: 25300043
    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.
  • PMID: 8513649
    Greenblatt DJ, Wright CE: Clinical pharmacokinetics of alprazolam. Therapeutic implications. Clin Pharmacokinet. 1993 Jun;24(6):453-71. doi: 10.2165/00003088-199324060-00003.
  • PMID: 30844192
    George TT, Tripp J: Alprazolam .
  • PMID: 14978513
    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.
  • PMID: 19515014
    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.
  • PMID: 12124305
    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.
  • PMID: 28777203
    Ait-Daoud N, Hamby AS, Sharma S, Blevins D: A Review of Alprazolam Use, Misuse, and Withdrawal. J Addict Med. 2018 Jan/Feb;12(1):4-10. doi: 10.1097/ADM.0000000000000350.
  • PMID: 31129381
    Scott S, Aricescu AR: A structural perspective on GABAA receptor pharmacology. Curr Opin Struct Biol. 2019 Feb;54:189-197. doi: 10.1016/j.sbi.2019.03.023. Epub 2019 May 23.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 609 • International brands: 15
Produk
  • Alprazolam
    Tablet, extended release • 0.5 mg/1 • Oral • US • Approved
  • Alprazolam
    Tablet, extended release • 1 mg/1 • Oral • US • Approved
  • Alprazolam
    Tablet, extended release • 2 mg/1 • Oral • US • Approved
  • Alprazolam
    Tablet, extended release • 3 mg/1 • Oral • US • Approved
  • Alprazolam
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Alprazolam
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Alprazolam
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Alprazolam
    Tablet • 0.25 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 609 produk.
International Brands
  • Alplax
  • Alprazolan
  • Alpronax
  • Alprox
  • Alviz
  • Cassadan
  • Esparon
  • Ralozam
  • Restyl
  • Solanax

Sekuens Gen/Protein (FASTA)

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