Peringatan Keamanan

The intraperitoneal LD50 in male mice is 1.87 g/kg.L31813 In reported cases of acute overdosage with acamprosate (doses of up to 56 grams of acamprosate calcium) diarrhea was the only reported symptom attributable to acamprosate. In the case of an overdose, supportive and symptomatic treatment is recommended.L31738

Acamprosate

DB00659

small molecule approved investigational

Deskripsi

Alcohol use disorder is responsible for a large worldwide burden of morbidity, premature mortality, and economic consequences resulting from accidents, violence, incarceration, decreased productivity, and increased healthcare spending.A229073

Acamprosate, also known by the brand name Campral, is a drug used for the maintenance of alcohol abstinence. It is a structural analogue of the neurotransmitter ?-aminobutyric acid (GABA).L31758 Acamprosate is the first medication specifically formulated for the maintenance of alcohol abstinence in ethanol-dependent patients after alcohol detoxificationA997, unlike naltrexone and disulfiram. It was first approved by the FDA in 2004 and initially marketed by Forest Laboratories.L31783

Struktur Molekul 2D

Berat 181.21
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In pharmacokinetic studies, enteric-coated acamprosate tablets demonstrate a terminal elimination half-life 10-fold higher than reported 3 hour half-life after intravenous infusion of acamprosate.[A229033] After two oral doses of acamprosate 333mg, the terminal half-life ranges between 20 - 33 hours.[L31738]
Volume Distribusi At steady state concentrations, the distribution of acamprosate is about 20L.[A229033] Following intravenous administration, the volume of distribution is about 72-109 L (an estimated 1 L/kg).[L31738]
Klirens (Clearance) Severe renal insufficiency decreases the elimination of acamprosate, and is a contraindication.[A229023,A229033] An acamprosate dose of 333mg, three times daily, is recommended for moderate renal impairment (creatinine clearance of 30-50 mL/min).[L31738]

Absorpsi

Acamprosate is absorbed in the gastrointestinal tract. A229023,A229033 The absolute bioavailability of acamprosate after oral administration is about 11%. The effect of food absorption is clinically insignificant and no adjustment of the dose is necessary with regard to meals.L31738 After repeated oral doses of 666 mg 3 times a day, steady-state concentrations are achieved within 5 to 7 days, with plasma concentration ranging between 370 to 650 micrograms/L.A229033

Metabolisme

Acamprosate is not metabolized.A229033,L31738

Rute Eliminasi

Half of acamprosate excretion occurs as unchanged acetyl-homotaurine in urine, and the other half possibly by biliary excretion.A229033 The kidneys are primarily responsible for the elimination of acamprosate.L31738

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food decreases drug absorption, but not to a clinically significant extent.

Interaksi Obat

104 Data
Aspartame The excretion of Acamprosate can be decreased when combined with Aspartame.
Pravastatin The excretion of Acamprosate can be decreased when combined with Pravastatin.
Cefotiam The excretion of Acamprosate can be decreased when combined with Cefotiam.
Valproic acid The excretion of Acamprosate can be decreased when combined with Valproic acid.
Indomethacin The excretion of Acamprosate can be decreased when combined with Indomethacin.
Aminohippuric acid The excretion of Acamprosate can be decreased when combined with Aminohippuric acid.
Cefalotin The excretion of Acamprosate can be decreased when combined with Cefalotin.
Cefotaxime The excretion of Acamprosate can be decreased when combined with Cefotaxime.
Cimetidine The excretion of Acamprosate can be decreased when combined with Cimetidine.
Piroxicam The excretion of Acamprosate can be decreased when combined with Piroxicam.
Methotrexate The excretion of Acamprosate can be decreased when combined with Methotrexate.
Cephalexin The excretion of Acamprosate can be decreased when combined with Cephalexin.
Enalapril The excretion of Acamprosate can be decreased when combined with Enalapril.
Diclofenac The excretion of Acamprosate can be decreased when combined with Diclofenac.
Oxytetracycline The excretion of Acamprosate can be decreased when combined with Oxytetracycline.
Linezolid The excretion of Acamprosate can be decreased when combined with Linezolid.
Furosemide The excretion of Acamprosate can be decreased when combined with Furosemide.
Tetracycline The excretion of Acamprosate can be decreased when combined with Tetracycline.
Acyclovir The excretion of Acamprosate can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Acamprosate can be decreased when combined with Phenylbutazone.
Bumetanide The excretion of Acamprosate can be decreased when combined with Bumetanide.
Dinoprostone The excretion of Acamprosate can be decreased when combined with Dinoprostone.
Salicylic acid The excretion of Acamprosate can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Acamprosate can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Acamprosate can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Acamprosate can be decreased when combined with Ketoprofen.
Minocycline The excretion of Acamprosate can be decreased when combined with Minocycline.
Probenecid The excretion of Acamprosate can be decreased when combined with Probenecid.
Ibuprofen The excretion of Acamprosate can be decreased when combined with Ibuprofen.
Novobiocin The excretion of Acamprosate can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Acamprosate can be decreased when combined with Benzylpenicillin.
Cefadroxil The excretion of Acamprosate can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Acamprosate can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Acamprosate can be decreased when combined with Cefamandole.
Cefazolin The excretion of Acamprosate can be decreased when combined with Cefazolin.
Cefoperazone The excretion of Acamprosate can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Acamprosate can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Acamprosate can be decreased when combined with Cefacetrile.
Cilastatin The excretion of Acamprosate can be decreased when combined with Cilastatin.
Tazobactam The excretion of Acamprosate can be decreased when combined with Tazobactam.
Topiroxostat The excretion of Acamprosate can be decreased when combined with Topiroxostat.
Glutaric Acid The excretion of Acamprosate can be decreased when combined with Glutaric Acid.
Taurocholic acid The excretion of Acamprosate can be decreased when combined with Taurocholic acid.
Caprylic acid The excretion of Acamprosate can be decreased when combined with Caprylic acid.
Ataluren The excretion of Acamprosate can be decreased when combined with Ataluren.
Dabrafenib The excretion of Acamprosate can be decreased when combined with Dabrafenib.
Dolutegravir The excretion of Acamprosate can be decreased when combined with Dolutegravir.
Lenvatinib The excretion of Acamprosate can be decreased when combined with Lenvatinib.
Tafamidis The excretion of Acamprosate can be decreased when combined with Tafamidis.
Cabotegravir The excretion of Acamprosate can be decreased when combined with Cabotegravir.
Favipiravir The excretion of Acamprosate can be decreased when combined with Favipiravir.
Enasidenib The excretion of Acamprosate can be decreased when combined with Enasidenib.
Naltrexone The bioavailability of Acamprosate can be increased when combined with Naltrexone.
Fexinidazole The excretion of Acamprosate can be decreased when combined with Fexinidazole.
Encorafenib The excretion of Acamprosate can be decreased when combined with Encorafenib.
Cyclosporine The excretion of Acamprosate can be decreased when combined with Cyclosporine.
Riboflavin The excretion of Acamprosate can be decreased when combined with Riboflavin.
Folic acid The excretion of Acamprosate can be decreased when combined with Folic acid.
Ethoxzolamide The excretion of Acamprosate can be decreased when combined with Ethoxzolamide.
Codeine The excretion of Acamprosate can be decreased when combined with Codeine.
Piperacillin The excretion of Acamprosate can be decreased when combined with Piperacillin.
Cidofovir The excretion of Acamprosate can be decreased when combined with Cidofovir.
Trifluridine The excretion of Acamprosate can be decreased when combined with Trifluridine.
Chloramphenicol The excretion of Acamprosate can be decreased when combined with Chloramphenicol.
Tolmetin The excretion of Acamprosate can be decreased when combined with Tolmetin.
Caspofungin The excretion of Acamprosate can be decreased when combined with Caspofungin.
Foscarnet The excretion of Acamprosate can be decreased when combined with Foscarnet.
Carbenicillin The excretion of Acamprosate can be decreased when combined with Carbenicillin.
Sulindac The excretion of Acamprosate can be decreased when combined with Sulindac.
Cyclothiazide The excretion of Acamprosate can be decreased when combined with Cyclothiazide.
Nafcillin The excretion of Acamprosate can be decreased when combined with Nafcillin.
Chlorpropamide The excretion of Acamprosate can be decreased when combined with Chlorpropamide.
Fluorescein The excretion of Acamprosate can be decreased when combined with Fluorescein.
Methazolamide The excretion of Acamprosate can be decreased when combined with Methazolamide.
Flurbiprofen The excretion of Acamprosate can be decreased when combined with Flurbiprofen.
Adefovir dipivoxil The excretion of Acamprosate can be decreased when combined with Adefovir dipivoxil.
Nateglinide The excretion of Acamprosate can be decreased when combined with Nateglinide.
Etodolac The excretion of Acamprosate can be decreased when combined with Etodolac.
Nalidixic acid The excretion of Acamprosate can be decreased when combined with Nalidixic acid.
Naproxen The excretion of Acamprosate can be decreased when combined with Naproxen.
Acetazolamide The excretion of Acamprosate can be decreased when combined with Acetazolamide.
Carprofen The excretion of Acamprosate can be decreased when combined with Carprofen.
Cinoxacin The excretion of Acamprosate can be decreased when combined with Cinoxacin.
Diflunisal The excretion of Acamprosate can be decreased when combined with Diflunisal.
Ranitidine The excretion of Acamprosate can be decreased when combined with Ranitidine.
Chlorothiazide The excretion of Acamprosate can be decreased when combined with Chlorothiazide.
Etacrynic acid The excretion of Acamprosate can be decreased when combined with Etacrynic acid.
Meclofenamic acid The excretion of Acamprosate can be decreased when combined with Meclofenamic acid.
Hydrochlorothiazide The excretion of Acamprosate can be decreased when combined with Hydrochlorothiazide.
Glyburide The excretion of Acamprosate can be decreased when combined with Glyburide.
Norfloxacin The excretion of Acamprosate can be decreased when combined with Norfloxacin.
Amoxicillin The excretion of Acamprosate can be decreased when combined with Amoxicillin.
Tolbutamide The excretion of Acamprosate can be decreased when combined with Tolbutamide.
Ofloxacin The excretion of Acamprosate can be decreased when combined with Ofloxacin.
Captopril The excretion of Acamprosate can be decreased when combined with Captopril.
Cefradine The excretion of Acamprosate can be decreased when combined with Cefradine.
Aminophenazone The excretion of Acamprosate can be decreased when combined with Aminophenazone.
Antipyrine The excretion of Acamprosate can be decreased when combined with Antipyrine.
Oxyphenbutazone The excretion of Acamprosate can be decreased when combined with Oxyphenbutazone.
Phenacetin The excretion of Acamprosate can be decreased when combined with Phenacetin.

Target Protein

Glutamate (NMDA) receptor GRIN1
Metabotropic glutamate receptor 5 GRM5
Gamma-aminobutyric acid type B receptor subunit 1 GABBR1

Referensi & Sumber

Synthesis reference: Claudia Cavarischia, Alex Comely, Marta Écijab, Tommaso Iacoangelia, Mireia Pastób, Lavinia Silvestria, Guido Furlotti. A Convenient, Scalable Process for the Preparation and Purification of Calcium Acamprosate. Synthesis. May 2020 DOI: 10.1055/s-0040-1707399
Artikel (PubMed)
  • PMID: 11584875
    Mason BJ: Treatment of alcohol-dependent outpatients with acamprosate: a clinical review. J Clin Psychiatry. 2001;62 Suppl 20:42-8.
  • PMID: 16467406
    Feeney GF, Connor JP, Young RM, Tucker J, McPherson A: Combined acamprosate and naltrexone, with cognitive behavioural therapy is superior to either medication alone for alcohol abstinence: a single centres' experience with pharmacotherapy. Alcohol Alcohol. 2006 May-Jun;41(3):321-7. Epub 2006 Feb 8.
  • PMID: 9509257
    Tsai G, Coyle JT: The role of glutamatergic neurotransmission in the pathophysiology of alcoholism. Annu Rev Med. 1998;49:173-84.
  • PMID: 9179530
    Wilde MI, Wagstaff AJ: Acamprosate. A review of its pharmacology and clinical potential in the management of alcohol dependence after detoxification. Drugs. 1997 Jun;53(6):1038-53.
  • PMID: 23278595
    Kalk NJ, Lingford-Hughes AR: The clinical pharmacology of acamprosate. Br J Clin Pharmacol. 2014 Feb;77(2):315-23. doi: 10.1111/bcp.12070.
  • PMID: 9839087
    Saivin S, Hulot T, Chabac S, Potgieter A, Durbin P, Houin G: Clinical pharmacokinetics of acamprosate. Clin Pharmacokinet. 1998 Nov;35(5):331-45. doi: 10.2165/00003088-199835050-00001.
  • PMID: 9660305
    al Qatari M, Bouchenafa O, Littleton J: Mechanism of action of acamprosate. Part II. Ethanol dependence modifies effects of acamprosate on NMDA receptor binding in membranes from rat cerebral cortex. Alcohol Clin Exp Res. 1998 Jun;22(4):810-4.
  • PMID: 32159228
    Kelly JF, Humphreys K, Ferri M: Alcoholics Anonymous and other 12-step programs for alcohol use disorder. Cochrane Database Syst Rev. 2020 Mar 11;3:CD012880. doi: 10.1002/14651858.CD012880.pub2.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 16 • International brands: 1
Produk
  • Acamprosate Calcium
    Tablet, coated • 333 mg/1 • Oral • US • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
  • Acamprosate Calcium
    Tablet, delayed release • 333 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 16 produk.
International Brands
  • Regtect — Nippon Shinyaku Co., Ltd.

Sekuens Gen/Protein (FASTA)

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