Peringatan Keamanan

The oral LD50 of buspirone is 196 mg/kg in rat, 655 mg/kg in mouse, 586 mg/kg in dog, and 356 mg/kg in monkey. The intraperitoneal LD50 is 136 mg/kg in rat and 146 mg/kg in mouse.L4478,L7381

In clinical pharmacology trials, administration of buspirone at the dose of 375 mg/day resulted in symptoms of nausea, vomiting, dizziness, drowsiness, miosis, and gastric distress. Few cases of overdosage that have been reported usually resulted in complete recovery. In case of overdose, the use of general symptomatic and supportive treatment is recommended along with immediate gastric lavage and monitoring of respiration, pulse, and blood pressure.L4478

Buspirone

DB00490

small molecule approved investigational

Deskripsi

Buspirone is a novel anxiolytic agent with a unique structure and a pharmacological profile. Belonging to the azaspirodecanedione drug class,A180991 buspirone is a serotonin 5-HT1A receptor agonist that is not chemically or pharmacologically related to benzodiazepines, barbiturates, and other sedative/anxiolytic drugs.L4478 Unlike many drugs used to treat anxiety, buspirone does not exhibit anticonvulsant, sedative, hypnotic, and muscle-relaxant properties. Due to these characteristics, buspirone been termed 'anxioselective'.A180985 First synthesized in 1968 then patented in 1975,L7375 it is commonly marketed under the brand name Buspar®. Buspirone was first approved in 1986 by the FDA A181751 and has been used to treat anxiety disorders, such as generalized anxiety disorder (GAD), and relieve symptoms of anxiety. It has also been used as a second-line therapy for unipolar depression when the use of selective serotonin reuptake inhibitors (SSRIs) is deemed clinically inadequate or inappropriate.L7375 The potential use of buspirone in combination with melatonin in depression and cognitive impairment via promoting neurogenesis has also been investigated.A181751

Struktur Molekul 2D

Berat 385.5031
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In a single-dose pharmacokinetic study of 14C-labeled buspirone, the average elimination half-life of unchanged buspirone following administration of single doses ranging from 10 to 40 mg was about 2 to 3 hours.[L4478]
Volume Distribusi In a pharmacokinetic study assessing buspirone over the dose range of 10 to 40 mg, the volume of distribution was 5.3 L/kg.[A181027]
Klirens (Clearance) In a pharmacokinetic study assessing buspirone over the dose range of 10 to 40 mg, the systemic clearance was 1.7 L/h/kg.[A181027]

Absorpsi

Buspirone is rapidly absorbed following oral administration.L4478 Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism. While absorption of buspirone is decreased with concomitant food intake, the first-pass metabolism of the drug is also decreased, resulting in an increased bioavailability L7375 as well as increased Cmax and AUC.L4478 Following oral administration of single oral doses of 20 mg, the Cmax ranged from 1 to 6 ng/mL and the Tmax ranged from 40 to 90 minutes.L4478

Metabolisme

Buspirone is extensively metabolized upon administration, where it primarily undergoes hepatic oxidation mediated by the CYP3A4 enzyme. Hydroxylated derivatives are produced, including a pharmacologically active metabolite 1-pyrimidinylpiperazine (1-PP). In animal studies, 1-PP possessed about one quarter of the pharmacological activity of buspirone.L4478

Rute Eliminasi

A single-dose pharmacokinetic studies using 14C-labeled buspirone demonstrated that about 29-63% of the dose administered was excreted in the urine within 24 hours, primarily in the form of metabolites. About 18% to 38% of the dose was eliminated via fecal excretion.L4478

Interaksi Makanan

4 Data
  • 1. Avoid alcohol. Alcohol may cause additive CNS depressant effects.
  • 2. Avoid grapefruit products. Grapefruit increases the plasma concentrations of the drug.
  • 3. Take at the same time every day. Take consistently at the same time in regard to meals.
  • 4. Take with or without food. Take drug always with or always without food in a consistent manner.

Interaksi Obat

1858 Data
Valsartan Buspirone may decrease the antihypertensive activities of Valsartan.
Ramipril Buspirone may decrease the antihypertensive activities of Ramipril.
Remikiren Buspirone may decrease the antihypertensive activities of Remikiren.
Guanadrel Buspirone may decrease the antihypertensive activities of Guanadrel.
Olmesartan Buspirone may decrease the antihypertensive activities of Olmesartan.
Atenolol Buspirone may decrease the antihypertensive activities of Atenolol.
Minoxidil Buspirone may decrease the antihypertensive activities of Minoxidil.
Treprostinil Buspirone may decrease the antihypertensive activities of Treprostinil.
Trandolapril Buspirone may decrease the antihypertensive activities of Trandolapril.
Benazepril Buspirone may decrease the antihypertensive activities of Benazepril.
Candoxatril Buspirone may decrease the antihypertensive activities of Candoxatril.
Moexipril Buspirone may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Buspirone may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Buspirone may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Buspirone may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Buspirone may decrease the antihypertensive activities of Eprosartan.
Quinapril Buspirone may decrease the antihypertensive activities of Quinapril.
Telmisartan Buspirone may decrease the antihypertensive activities of Telmisartan.
Deserpidine Buspirone may decrease the antihypertensive activities of Deserpidine.
Pentolinium Buspirone may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Buspirone may decrease the antihypertensive activities of Trimethaphan.
Bretylium Buspirone may decrease the antihypertensive activities of Bretylium.
Terazosin Buspirone may decrease the antihypertensive activities of Terazosin.
Cilazapril Buspirone may decrease the antihypertensive activities of Cilazapril.
Saprisartan Buspirone may decrease the antihypertensive activities of Saprisartan.
Spirapril Buspirone may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Buspirone may decrease the antihypertensive activities of Dexpropranolol.
Diethylnorspermine Buspirone may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Buspirone may decrease the antihypertensive activities of Temocapril.
Trimazosin Buspirone may decrease the antihypertensive activities of Trimazosin.
Rauwolfia serpentina root Buspirone may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Buspirone may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Buspirone may decrease the antihypertensive activities of Imidapril.
BQ-123 Buspirone may decrease the antihypertensive activities of BQ-123.
Dihydralazine Buspirone may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Buspirone may decrease the antihypertensive activities of Zofenopril.
Guanoxan Buspirone may decrease the antihypertensive activities of Guanoxan.
Delapril Buspirone may decrease the antihypertensive activities of Delapril.
Vincamine Buspirone may decrease the antihypertensive activities of Vincamine.
Linsidomine Buspirone may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Buspirone may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Buspirone may decrease the antihypertensive activities of Tolonidine.
Endralazine Buspirone may decrease the antihypertensive activities of Endralazine.
Cadralazine Buspirone may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Buspirone may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Buspirone may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Buspirone may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Buspirone may decrease the antihypertensive activities of Guanoclor.
Candesartan Buspirone may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Buspirone may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Buspirone may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Buspirone may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Buspirone may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Buspirone may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Buspirone may decrease the antihypertensive activities of Quinaprilat.
Enalapril Buspirone may decrease the antihypertensive activities of Enalapril.
Captopril Buspirone may decrease the antihypertensive activities of Captopril.
Nimodipine Buspirone may decrease the antihypertensive activities of Nimodipine.
Carvedilol Buspirone may decrease the antihypertensive activities of Carvedilol.
Nebivolol Buspirone may decrease the antihypertensive activities of Nebivolol.
Pinacidil Buspirone may decrease the antihypertensive activities of Pinacidil.
Riociguat Buspirone may decrease the antihypertensive activities of Riociguat.
Aliskiren Buspirone may decrease the antihypertensive activities of Aliskiren.
Lacidipine Buspirone may decrease the antihypertensive activities of Lacidipine.
Niguldipine Buspirone may decrease the antihypertensive activities of Niguldipine.
Naftopidil Buspirone may decrease the antihypertensive activities of Naftopidil.
Dexniguldipine Buspirone may decrease the antihypertensive activities of Dexniguldipine.
Prazosin Buspirone may decrease the antihypertensive activities of Prazosin.
Bosentan Buspirone may decrease the antihypertensive activities of Bosentan.
Losartan Buspirone may decrease the antihypertensive activities of Losartan.
Irbesartan Buspirone may decrease the antihypertensive activities of Irbesartan.
Sitaxentan Buspirone may decrease the antihypertensive activities of Sitaxentan.
Selexipag Buspirone may decrease the antihypertensive activities of Selexipag.
Amlodipine Buspirone may decrease the antihypertensive activities of Amlodipine.
Azilsartan medoxomil Buspirone may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Buspirone may decrease the antihypertensive activities of Diazoxide.
Buprenorphine Buspirone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
Hydrocodone Buspirone 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 Buspirone.
Magnesium sulfate The therapeutic efficacy of Buspirone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Buspirone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Buspirone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
Orphenadrine Buspirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Buspirone 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 Buspirone.
Rotigotine Buspirone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Buspirone.
Sodium oxybate Buspirone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Buspirone 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 Buspirone.
Thalidomide Buspirone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Buspirone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Sirolimus The metabolism of Buspirone can be decreased when combined with Sirolimus.
Dirithromycin The metabolism of Buspirone can be decreased when combined with Dirithromycin.
Telithromycin The metabolism of Buspirone can be decreased when combined with Telithromycin.

Target Protein

5-hydroxytryptamine receptor 1A HTR1A
D(2) dopamine receptor DRD2
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
Alpha-1 adrenergic receptors ADRA1A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2874976
    Goa KL, Ward A: Buspirone. A preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic. Drugs. 1986 Aug;32(2):114-29. doi: 10.2165/00003495-198632020-00002.
  • PMID: 3041384
    Jann MW: Buspirone: an update on a unique anxiolytic agent. Pharmacotherapy. 1988;8(2):100-16.
  • PMID: 10320950
    Mahmood I, Sahajwalla C: Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug. Clin Pharmacokinet. 1999 Apr;36(4):277-87. doi: 10.2165/00003088-199936040-00003.
  • PMID: 26535760
    Howland RH: Buspirone: Back to the Future. J Psychosoc Nurs Ment Health Serv. 2015 Nov;53(11):21-4. doi: 10.3928/02793695-20151022-01.
  • PMID: 2870639
    Eison AS, Temple DL Jr: Buspirone: review of its pharmacology and current perspectives on its mechanism of action. Am J Med. 1986 Mar 31;80(3B):1-9. doi: 10.1016/0002-9343(86)90325-6.
  • PMID: 1796057
    Tunnicliff G: Molecular basis of buspirone's anxiolytic action. Pharmacol Toxicol. 1991 Sep;69(3):149-56.
  • PMID: 1973941
    Yocca FD: Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. J Clin Psychopharmacol. 1990 Jun;10(3 Suppl):6S-12S.
  • PMID: 24337875
    Garcia-Garcia AL, Newman-Tancredi A, Leonardo ED: 5-HT(1A) corrected receptors in mood and anxiety: recent insights into autoreceptor versus heteroreceptor function. Psychopharmacology (Berl). 2014 Feb;231(4):623-36. doi: 10.1007/s00213-013-3389-x. Epub 2013 Dec 12.
Textbook
  • ISBN: 978-0-7020-3471-8
    43. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 538-539). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 535 • International brands: 11
Produk
  • Amb-buspirone
    Tablet • 10 mg • Oral • Canada • Approved
  • Apo-buspirone
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Auro-buspirone
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Buspar
    Tablet • 5 mg/1 • Oral • US • Approved
  • Buspar
    Tablet • 10 mg/1 • Oral • US • Approved
  • Buspar
    Tablet • 15 mg/1 • Oral • US • Approved
  • Buspar
    Tablet • 30 mg/1 • Oral • US • Approved
  • Buspar
    Tablet • 5 mg/1 • Oral • US • Approved
Menampilkan 8 dari 535 produk.
International Brands
  • Ansial — Rontag
  • Anxiron — Valeant
  • Anxut — Eisai
  • Bespar
  • Buscalm — Wockhardt
  • Busp — Hexal
  • Buspon — Deva
  • Dalpas — Biotech
  • Epsilat — Coup
  • Pasrin — Aspen Pharmacare

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