Peringatan Keamanan

The oral LD50 is 4049 mg/kg in rats and 4686 mg/kg in mice.L11157 The subcutaneous LD50 is 800 mg/kg in rats and mice.L11157 The intraperitoneal LD50 is 800 mg/kg in rats and 778 mg/kg in mice.L11157 The intravenous LD50 is 204 mg/kg in rats and 254 mg/kg in mice.L11157 The lowest published toxic dose (TDLo) in man following oral administration is 4 mg/kg/7D.L11157

Symptoms of overdose resemble the adverse events seen with the use of recommended doses, and they should be responded with supportive and symptomatic treatment. Any unabsorbed drug should be removed from the gastrointestinal tract, and the patient should be monitored accordingly. The use of hemodialysis to eliminate the drug from the systemic circulation is effective, but the experience of using hemodialysis in response to famotidine overdose is limited in clinical settings.L11139

Famotidine

DB00927

small molecule approved

Deskripsi

Famotidine is a competitive histamine-2 (H2) receptor antagonist that works to inhibit gastric acid secretion. It is commonly used in gastrointestinal conditions related to acid secretion, such as gastric ulcers and gastroesophageal reflux disease (GERD), in adults and children.L11166 Compared to other H2 receptor antagonists, famotidine displays high selectivity towards this receptor; in a study consisting of healthy volunteers and patients with acid hypersecretory disease, famotidine was about 20 to 50 times more potent at inhibiting gastric acid secretion than cimetidine and eight times more potent than ranitidine on a weight basis.A189462 Famotidine is used in various over-the-counter and off-label uses.L11166 While oral formulations of famotidine are more commonly used, the intravenous solution of the drug is available for use in hospital settings.L11142

Struktur Molekul 2D

Berat 337.445
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life is about 2 to 4 hours.[A189474] The half-life is expected to increase nonlinearly in patients with decreased renal function.[A189459]
Volume Distribusi The steady-state volume of distribution ranges from 1.0 to 1.3 L/kg.[A189474] Famotidine is found in breast milk; however, it is found in breast milk at the lowest concentrations compared to other H<sub>2</sub> receptor antagonists.[L11166]
Klirens (Clearance) Renal clearance is 250-450 mL/min, indicating some tubular excretion. Because the renal clearance rate exceeds the glomerular filtration rate, famotidine is thought to be mainly eliminated via both glomerular filtration and renal tubular secretion.[A189474]

Absorpsi

Following oral administration, the absorption of famotidine is dose-dependent and incomplete.A189474 The oral bioavailability ranges from 40-50%, and the Cmax is reached in 1-4 hours post-dosing.A189459,A189474 While the bioavailability can be slightly increased with the intake of food and decreased by antacids, there is no clinical significance.L11139

Metabolisme

Famotidine undergoes minimal first-pass metabolism. About 25-30% of the drug is eliminated through hepatic metabolism. The only metabolite identified in humans is the S-oxide.L11139

Rute Eliminasi

About 65-70% of the total administered dose of famotidine undergoes renal elimination, and 30-35% of the dose is cleared by metabolism.L11139 Following intravenous administration, about 70% of the drug is eliminated in the urine as an unchanged drug.A189474

Interaksi Makanan

3 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol increases the risk of gastric irritation.
  • 2. Limit caffeine intake. Caffeine and other acidic beverages increases the risk of gastric irritation.
  • 3. Take with or without food. Food slightly increases bioavailability, but not to a clinically significant extent.

Interaksi Obat

740 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Famotidine.
Atazanavir Famotidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren The serum concentration of Cefditoren can be decreased when it is combined with Famotidine.
Dabigatran etexilate Famotidine can cause a decrease in the absorption of Dabigatran etexilate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dabrafenib Famotidine can cause a decrease in the absorption of Dabrafenib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Erlotinib Famotidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pazopanib Famotidine can cause a decrease in the absorption of Pazopanib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Riociguat Famotidine can cause a decrease in the absorption of Riociguat resulting in a reduced serum concentration and potentially a decrease in efficacy.
Benzylpenicilloyl polylysine Famotidine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Famotidine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Famotidine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Famotidine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Famotidine.
Aspartame The excretion of Famotidine can be decreased when combined with Aspartame.
Pravastatin The excretion of Famotidine can be decreased when combined with Pravastatin.
Pantoprazole The excretion of Famotidine can be decreased when combined with Pantoprazole.
Cefotiam The excretion of Famotidine can be decreased when combined with Cefotiam.
Liothyronine The excretion of Famotidine can be decreased when combined with Liothyronine.
Conjugated estrogens The excretion of Famotidine can be decreased when combined with Conjugated estrogens.
Indomethacin The excretion of Famotidine can be decreased when combined with Indomethacin.
Aminohippuric acid The excretion of Famotidine can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Famotidine can be decreased when combined with Lansoprazole.
Cefalotin The excretion of Famotidine can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Famotidine can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Famotidine can be decreased when combined with Cefotaxime.
Zidovudine The excretion of Famotidine can be decreased when combined with Zidovudine.
Guanidine The excretion of Famotidine can be decreased when combined with Guanidine.
Piroxicam The excretion of Famotidine can be decreased when combined with Piroxicam.
Methotrexate The excretion of Famotidine can be decreased when combined with Methotrexate.
Cephalexin The excretion of Famotidine can be decreased when combined with Cephalexin.
Diclofenac The excretion of Famotidine can be decreased when combined with Diclofenac.
Oxytetracycline The excretion of Famotidine can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Famotidine can be decreased when combined with Leucovorin.
Furosemide The excretion of Famotidine can be decreased when combined with Furosemide.
Esomeprazole The excretion of Famotidine can be decreased when combined with Esomeprazole.
Tetracycline The excretion of Famotidine can be decreased when combined with Tetracycline.
Acyclovir The excretion of Famotidine can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Famotidine can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Famotidine can be decreased when combined with Cefaclor.
Bumetanide The excretion of Famotidine can be decreased when combined with Bumetanide.
Dinoprostone The excretion of Famotidine can be decreased when combined with Dinoprostone.
Succinic acid The excretion of Succinic acid can be decreased when combined with Famotidine.
Citrulline The excretion of Citrulline can be decreased when combined with Famotidine.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Famotidine.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Famotidine.
Piperacillin The excretion of Piperacillin can be decreased when combined with Famotidine.
Trifluridine The excretion of Trifluridine can be decreased when combined with Famotidine.
Allopurinol The excretion of Allopurinol can be decreased when combined with Famotidine.
Cefdinir The excretion of Cefdinir can be decreased when combined with Famotidine.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Famotidine.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Famotidine.
Fluorescein The excretion of Fluorescein can be decreased when combined with Famotidine.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Famotidine.
Estradiol The excretion of Estradiol can be decreased when combined with Famotidine.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Famotidine.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Famotidine.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Famotidine.
Cefazolin The excretion of Cefazolin can be decreased when combined with Famotidine.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Famotidine.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Famotidine.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Famotidine.
Tazobactam The excretion of Tazobactam can be decreased when combined with Famotidine.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Famotidine.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Famotidine.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Famotidine.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Famotidine.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Famotidine.
Doripenem The excretion of Doripenem can be decreased when combined with Famotidine.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Famotidine.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Famotidine.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Famotidine.
Avibactam The excretion of Avibactam can be decreased when combined with Famotidine.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Famotidine.
Silibinin The excretion of Silibinin can be decreased when combined with Famotidine.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Famotidine.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Famotidine.
Relebactam The excretion of Relebactam can be decreased when combined with Famotidine.
Tenofovir The excretion of Tenofovir can be decreased when combined with Famotidine.
Salicylic acid The excretion of Famotidine can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Famotidine can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Famotidine can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Famotidine can be decreased when combined with Ketoprofen.
Minocycline The excretion of Famotidine can be decreased when combined with Minocycline.
Probenecid The excretion of Famotidine can be decreased when combined with Probenecid.
Novobiocin The excretion of Famotidine can be decreased when combined with Novobiocin.
Melatonin The excretion of Famotidine can be decreased when combined with Melatonin.
Ouabain The excretion of Famotidine can be decreased when combined with Ouabain.
Cefadroxil The excretion of Famotidine can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Famotidine can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Famotidine can be decreased when combined with Cefamandole.
Cefoperazone The excretion of Famotidine can be decreased when combined with Cefoperazone.
Liotrix The excretion of Famotidine can be decreased when combined with Liotrix.
Cilastatin The excretion of Famotidine can be decreased when combined with Cilastatin.
trans-2-hydroxycinnamic acid The excretion of Famotidine can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Famotidine can be decreased when combined with Topiroxostat.
Benzoic acid The excretion of Famotidine can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Famotidine can be decreased when combined with Caprylic acid.
Ataluren The excretion of Famotidine can be decreased when combined with Ataluren.
Teriflunomide The excretion of Famotidine can be decreased when combined with Teriflunomide.
Cabotegravir The excretion of Famotidine can be decreased when combined with Cabotegravir.

Target Protein

Histamine H2 receptor HRH2

Referensi & Sumber

Synthesis reference: Montserrat Ballester-Rodes, Francisco E. Palomo-Nicolau, Antonio L. Palomo-Coli, "Famotidine polymorphic forms and their preparation process." U.S. Patent US5021582, issued March, 1987.
Artikel (PubMed)
  • PMID: 2887616
    Chremos AN: Clinical pharmacology of famotidine: a summary. J Clin Gastroenterol. 1987;9 Suppl 2:7-12. doi: 10.1097/00004836-198707002-00003.
  • PMID: 2573505
    Langtry HD, Grant SM, Goa KL: Famotidine. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in peptic ulcer disease and other allied diseases. Drugs. 1989 Oct;38(4):551-90. doi: 10.2165/00003495-198938040-00005.
  • PMID: 1764869
    Echizen H, Ishizaki T: Clinical pharmacokinetics of famotidine. Clin Pharmacokinet. 1991 Sep;21(3):178-94. doi: 10.2165/00003088-199121030-00003.
Textbook
  • ISBN: 978-0-7020-3471-8
    29. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 360-363). Edinburgh: Elsevier/Churchill Livingstone.

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