Peringatan Keamanan

Reported oral TDLO (woman) is 400 mg/kg and subcutaneous LD50 in rat is 160 mg/kg.MSDS The lowest acute dose of butalbital alone associated with death in adults is 2.0 g.A177754 Symptoms of acute barbiturate poisoning include drowsiness, confusion, coma, respiratory depression, hypotension, and shock. Due to the CNS depressant effects, an overdose of barbiturates may lead to death.L10370 Barbiturates are also associated with withdrawal reactions, which may lead to death if severe.A177754

Butalbital

DB00241

small molecule approved illicit

Deskripsi

Butalbital, or 5-allyl-5-isobutylbarbituric acid, is a derivative of barbituric acid which the hydrogens at position 5 are substituted by an allyl group and an isobutyl group. It is a short-to-intermediate acting member of barbiturates that exhibit muscle-relaxing and anti-anxiety properties that produce central nervous system (CNS) depression that ranges from mild sedation to general anesthesia.A177754 Butalbital has a low degree of selectivity and a narrow therapeutic index.A177754 Typically indicated to manage tension (or muscle contraction) headaches, butalbital is often combined with one or more therapeutic agents, such as acetylsalicylic acid, acetaminophen, aspirin, and caffeine. There have not been clinical trials that evaluate the clinical efficacy of butalbital in migraines A177754 thus it is not indicated for such condition. As with other barbiturates, butalbital carries a risk of abuse or misuse potential, intoxication, hangover, tolerance, dependence, and overdosage possibly leading to death.L10370 Butalbital?containing analgesics can also produce a drug?induced headache in addition to tolerance and dependence. Due to these risks, the use of butalbital-containing combination products is typically limited for use only in cases where other medications are deemed ineffective and such usage is advised to be carefully monitored.A177754

Struktur Molekul 2D

Berat 224.2563
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life is about 35 hours. In a study of 5 healthy volunteers receiving 100 mg butalbital in combination with aspirin and caffeine, the mean plasma elimination half-life of butalbital was 61 hours, with the range of 35 to 88 hours.[A177838, T598]
Volume Distribusi The volume of distribution of butalbital is reported to be approximately 0.8?L/kg.[T598] Butalbital is expected to distribute to most of the tissues in the body [F4561], including the mamillary glands and placenta.[F4561] The plasma-to-blood concentration ratio was almost unity indicating that there is no preferential distribution of butalbital into either plasma or blood cells.[L10370]
Klirens (Clearance) There is limited data on the clearance of butalbital.

Absorpsi

Butalbital gets readily and rapidly absorbed from the gastrointestinal tract.F4561 The time to reach the peak plasma concentrations is reported to be approximately 2 hours.A177754 Typical blood concentrations of butalbital peaked at 2.1 mg/L and declined to 1.5 mg/L at 24 hr.A177838 Plasma concentrations of 10 to 20 ?g/mL have been associated with toxicity; coma and fatalities have occurred with concentrations of 25 to 30 ?g/mL.A177754

Metabolisme

Butalbital is expected to undergo nearly complete hepatic metabolism.A177754 It primarily undergoes C5 oxidation to form 5-isobutyl-5-(2,3-dihydroxypropyl) barbituric acid, which is the major metabolite. Butalbital may also undergo omega-hydroxylation to form 5-allyl-5(3-hydroxy-2-methyl-1-propyl) barbituric acid.A177835, L10370, T598

Rute Eliminasi

Butalbital predominantly undergoes renal elimination with 59 to 88% of the total dose administered being excreted from the kidneys as unchanged parent drug or metabolites.L6121,L10370 Urinary excretion products included parent drug (about 3.6% of the dose), 5-isobutyl-5-(2,3-dihydroxypropyl) barbituric acid (about 24% of the dose), 5-allyl-5(3-hydroxy-2-methyl-1-propyl) barbituric acid (about 4.8%), products with the barbituric acid ring hydrolyzed with excretion of urea (about 14% of the dose), as well as unidentified materials.L10370 Of the material excreted in the urine, 32% is conjugated.L10370 Elimination is not complete within 24 hours, and the drug accumulates with frequent administration.A177754

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Profound CNS depression can occur.

Interaksi Obat

1342 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Butalbital.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Butalbital.
Buprenorphine Butalbital 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 Butalbital.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Hydrocodone Butalbital 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 Butalbital.
Magnesium sulfate The therapeutic efficacy of Butalbital can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Butalbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Butalbital may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Mirtazapine Butalbital may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Orphenadrine Butalbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Butalbital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Butalbital may increase the sedative activities of Pramipexole.
Ropinirole Butalbital may increase the sedative activities of Ropinirole.
Rotigotine Butalbital may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Butalbital.
Suvorexant Butalbital 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 Butalbital.
Thalidomide Butalbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Butalbital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Butalbital.
Mefloquine The therapeutic efficacy of Butalbital can be decreased when used in combination with Mefloquine.
Orlistat Orlistat can cause a decrease in the absorption of Butalbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Propacetamol The metabolism of Propacetamol can be increased when combined with Butalbital.
Chloramphenicol The metabolism of Butalbital can be decreased when combined with Chloramphenicol.
Doxycycline The serum concentration of Doxycycline can be decreased when it is combined with Butalbital.
Felbamate The serum concentration of Butalbital can be increased when it is combined with Felbamate.
Griseofulvin The serum concentration of Griseofulvin can be decreased when it is combined with Butalbital.
Lamotrigine The serum concentration of Lamotrigine can be decreased when it is combined with Butalbital.
Mianserin The therapeutic efficacy of Butalbital can be decreased when used in combination with Mianserin.
Primidone The risk or severity of adverse effects can be increased when Primidone is combined with Butalbital.
Methylphenobarbital The risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Butalbital.
Pyridoxine The metabolism of Butalbital can be increased when combined with Pyridoxine.
Teniposide The serum concentration of Teniposide can be decreased when it is combined with Butalbital.
Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Butalbital.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Butalbital.
Prilocaine The risk or severity of methemoglobinemia can be increased when Butalbital is combined with Prilocaine.
Topotecan Butalbital may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Butalbital.
Sodium oxybate Butalbital may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Butalbital.
Perampanel The metabolism of Perampanel can be increased when combined with Butalbital.
Warfarin The metabolism of Warfarin can be increased when combined with Butalbital.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Butalbital.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Butalbital.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Butalbital.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Butalbital.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Butalbital.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Butalbital.
Aminophylline The therapeutic efficacy of Butalbital can be decreased when used in combination with Aminophylline.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Butalbital is combined with Botulinum toxin type A.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Butalbital is combined with Botulinum toxin type B.
Meperidine Butalbital may increase the hypotensive and central nervous system depressant (CNS depressant) activities of Meperidine.
Somatostatin The risk or severity of adverse effects can be increased when Somatostatin is combined with Butalbital.
Ethanol Butalbital may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Butalbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Fluvoxamine The risk or severity of adverse effects can be increased when Butalbital is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Butalbital is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Butalbital is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Butalbital is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Butalbital is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Butalbital is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Butalbital is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Butalbital is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Butalbital is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Butalbital is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Butalbital is combined with Dapoxetine.
Desvenlafaxine The risk or severity of adverse effects can be increased when Butalbital is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Butalbital is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Butalbital is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Butalbital is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Butalbital is combined with Alaproclate.
Naltrexone The risk or severity of adverse effects can be increased when Butalbital is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Butalbital is combined with Bezitramide.
Morphine The risk or severity of adverse effects can be increased when Butalbital is combined with Morphine.
Hydromorphone The risk or severity of adverse effects can be increased when Butalbital is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Butalbital is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Butalbital is combined with Butorphanol.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Butalbital is combined with Dextropropoxyphene.
Pentazocine The risk or severity of adverse effects can be increased when Butalbital is combined with Pentazocine.
Sufentanil The risk or severity of adverse effects can be increased when Butalbital is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Butalbital is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Butalbital is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Butalbital is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Butalbital is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Butalbital is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Butalbital is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Butalbital is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Butalbital is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Butalbital is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Butalbital is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Butalbital is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Butalbital is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Butalbital is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Butalbital is combined with Carfentanil.

Target Protein

Gamma-aminobutyric acid receptor subunit alpha-2 GABRA2
Gamma-aminobutyric acid receptor subunit alpha-3 GABRA3
Gamma-aminobutyric acid receptor subunit alpha-4 GABRA4
Gamma-aminobutyric acid receptor subunit alpha-5 GABRA5
Gamma-aminobutyric acid receptor subunit alpha-6 GABRA6
GABA(A) Receptor GABRA1
Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Glutamate receptor 2 GRIA2
Glutamate receptor ionotropic, kainate 2 GRIK2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11903523
    Silberstein SD, McCrory DC: Butalbital in the treatment of headache: history, pharmacology, and efficacy. Headache. 2001 Nov-Dec;41(10):953-67.
  • PMID: 12173787
    Wenzel RG, Sarvis CA: Do butalbital-containing products have a role in the management of migraine? Pharmacotherapy. 2002 Aug;22(8):1029-35.
  • PMID: 23011802
    Bryczkowski C, Geib AJ: Combined butalbital/acetaminophen/caffeine overdose: case files of the Robert Wood Johnson Medical School Toxicology Service. J Med Toxicol. 2012 Dec;8(4):424-31. doi: 10.1007/s13181-012-0261-z.
  • PMID: 27378845
    Puthenkalam R, Hieckel M, Simeone X, Suwattanasophon C, Feldbauer RV, Ecker GF, Ernst M: Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What? Front Mol Neurosci. 2016 Jun 16;9:44. doi: 10.3389/fnmol.2016.00044. eCollection 2016.
  • PMID: 29124988
    Poyant JO, Albright R, Clain J, Pandompatam G, Barreto EF: Extracorporeal elimination of butalbital in acute aspirin-butalbital-caffeine-codeine (Fiorinal with Codeine) poisoning. Clin Toxicol (Phila). 2018 Jun;56(6):439-441. doi: 10.1080/15563650.2017.1400554. Epub 2017 Nov 10.
  • PMID: 6105059
    Dain JG, Bhuta SI, Coombs RA, Talbot KC, Dugger HA: Metabolism of butalbital, 5-allyl-5-isobutylbarbituric acid, in the dog. Drug Metab Dispos. 1980 Jul-Aug;8(4):247-52.
  • PMID: 3244271
    Drost ML, Walter L: Blood and plasma concentrations of butalbital following single oral doses in man. J Anal Toxicol. 1988 Nov-Dec;12(6):322-4.
Textbook
  • ISBN: 978-0-471-72760-6
    23. (2012). In Medical Toxicology of Drug Abuse: Synthesized Chemicals and Psychoactive Plants. (pp. 474-476). Hoboken, N.J: John Wiley & Sons.

Contoh Produk & Brand

Produk: 322 • International brands: 1
Produk
  • Acetaminophen, Butalbital and Caffeine
    Tablet • - • Oral • US • Generic • Approved
  • Alagesic LQ
    Syrup • - • Oral • US • Generic • Approved
  • Allzital
    Tablet • - • Oral • US • Generic • Approved
  • Allzital
    Tablet • - • Oral • US • Generic • Approved
  • Allzital
    Tablet • - • Oral • US • Generic • Approved
  • Allzital
    Tablet • - • Oral • US • Generic • Approved
  • Ascomp with Codeine
    Capsule • - • Oral • US • Generic • Approved
  • Ascomp with Codeine
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Menampilkan 8 dari 322 produk.
International Brands
  • Sandoptal — Sandoz Pharmaceuticals Corporations

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