Peringatan Keamanan

Oral doses of 1,000 mg/kg in mice and rats were not found to be lethal. Intravenous LD50 values in mice and rats were 77 and 83 mg/kg, respectively.L10821

Overdose information

There has been limited experience with ranitidine overdose. Reported acute ingestions of up to 18 grams orally were followed by temporary adverse effects similar to the normal adverse effects of this drug, including tachycardia, bradycardia, dizziness, diarrhea, nausea, and vomiting, among other effects.L10821 Gait abnormalities and hypotension have also been observed. When an overdose with ranitidine is suspected, remove unabsorbed ranitidine from the gastrointestinal tract if possible, and monitor the patient and provide supportive therapy as required.L10818,L10923

Ranitidine

DB00863

small molecule approved withdrawn

Deskripsi

Ranitidine is a commonly used drug, classified as a histamine H2-receptor antagonist, and belongs to the same drug class as cimetidine and famotidine. This drug helps to prevent and treat gastric-acid associated conditions, including ulcers, because of its ability to decrease gastric acid secretion.A176759,L10818 Ranitidine is often referred to as Zantac, and is available in various forms, including tablet, injection, and effervescent tablet preparations.L10818,F4253

The prevalence of GERD is thought to be 10-20% in western countries.A176843 Ranitidine has proven to be an effective treatment for relieving uncomfortable symptoms of gastric acid associated conditions and is therefore widely used in GERD and other gastric-acid related conditions.A176849,L10818

Struktur Molekul 2D

Berat 314.4
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 or ranitidine is about 2.5-3 hours.[A188817,L10818] It may be longer after oral administration versus injection.[A188817] The plasma half-life is longer for elderly patients population due to a decrease in renal function, and is measured at 3-4 hours.[A188817,L10818]
Volume Distribusi The volume of distribution is higher than body volume, and measures at approximately 1.4 L/kg.[A188817,L10818] It concentrates in breast milk, but does not readily distribute into the cerebrospinal fluid.[A188817]
Klirens (Clearance) Renal clearance is about 410 mL/min according to FDA prescribing information.[L10818] Another resource mentions a plasma clearance of approximately 600 ml/min.[A188817] Clearance is decreased in the elderly and those with impaired or hepatic renal function.[A188817,L10818] It is recommended to decrease the dose of ranitidine by one-half in patients with renal impairment.[L10818]

Absorpsi

Ranitidine is rapidly absorbed with peak concentrations reached within 1-3 hours after administration, and varying greatly among patients. Bioavailability is about 50%-60% due to hepatic metabolism.A188817,L10923 In a pharmacokinetic study of healthy males, the AUC 0-infinity was about 2,488.6 ng x h/mL and the median Tmax was 2.83 hours.A188829 Food or antacids have limited effects on absorption. One clinical study found that the administration of a potent antacid (150 mmol) in subjects in the fasted state led to decreased absorption of ranitidine.L10818

Metabolisme

The major metabolite in the urine is N-oxide, which represents less than 4% of the dose. Other metabolites of ranitidine include S-oxide (1%) and desmethyl ranitidine (1%).L10818,L10923 The feces contain the remainder of the excreted ranitidine dose. Liver dysfunction has been shown to cause small, but clinically insignificant, changes in various ranitidine pharmacokinetic parameters.L10818

Rute Eliminasi

This drug is mainly excreted in the urine but also excreted in the feces.A188817,L10923 About 30% of a single oral dose has been measured in the urine as unchanged drug within 24 hours of ingestion.L10818

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1320 Data
Deferasirox The serum concentration of Ranitidine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Ranitidine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Ranitidine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Ranitidine can be decreased when it is combined with Teriflunomide.
Atazanavir Ranitidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Ranitidine can cause a decrease in the absorption of Bosutinib 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 Ranitidine.
Dabigatran etexilate Ranitidine can cause a decrease in the absorption of Dabigatran etexilate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dabrafenib Ranitidine can cause a decrease in the absorption of Dabrafenib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Erlotinib Ranitidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Ranitidine can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pazopanib Ranitidine can cause a decrease in the absorption of Pazopanib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Riociguat Ranitidine can cause a decrease in the absorption of Riociguat resulting in a reduced serum concentration and potentially a decrease in efficacy.
Glimepiride The serum concentration of Glimepiride can be increased when it is combined with Ranitidine.
Acetohexamide The serum concentration of Acetohexamide can be increased when it is combined with Ranitidine.
Chlorpropamide The serum concentration of Chlorpropamide can be increased when it is combined with Ranitidine.
Tolazamide The serum concentration of Tolazamide can be increased when it is combined with Ranitidine.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Ranitidine.
Glipizide The serum concentration of Glipizide can be increased when it is combined with Ranitidine.
Gliclazide The serum concentration of Gliclazide can be increased when it is combined with Ranitidine.
Tolbutamide The serum concentration of Tolbutamide can be increased when it is combined with Ranitidine.
Gliquidone The serum concentration of Gliquidone can be increased when it is combined with Ranitidine.
Glisoxepide The serum concentration of Glisoxepide can be increased when it is combined with Ranitidine.
Glibornuride The serum concentration of Glibornuride can be increased when it is combined with Ranitidine.
Carbutamide The serum concentration of Carbutamide can be increased when it is combined with Ranitidine.
Metahexamide The serum concentration of Metahexamide can be increased when it is combined with Ranitidine.
Benzylpenicilloyl polylysine Ranitidine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Ranitidine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Ranitidine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Ranitidine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Ranitidine.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Ranitidine.
Bupropion The excretion of Ranitidine can be decreased when combined with Bupropion.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Ranitidine.
Aspartame The excretion of Ranitidine can be decreased when combined with Aspartame.
Valproic acid The excretion of Ranitidine can be decreased when combined with Valproic acid.
Oxytetracycline The excretion of Ranitidine can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Ranitidine can be decreased when combined with Leucovorin.
Mercaptopurine The excretion of Ranitidine can be decreased when combined with Mercaptopurine.
Novobiocin The excretion of Ranitidine can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Ranitidine can be decreased when combined with Benzylpenicillin.
Ouabain The excretion of Ranitidine can be decreased when combined with Ouabain.
Liotrix The excretion of Ranitidine can be decreased when combined with Liotrix.
Cilastatin The excretion of Ranitidine can be decreased when combined with Cilastatin.
Tazobactam The excretion of Ranitidine can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Ranitidine can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Ranitidine can be decreased when combined with Topiroxostat.
Cholic Acid The excretion of Ranitidine can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Ranitidine can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Ranitidine can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Ranitidine can be decreased when combined with Caprylic acid.
Ataluren The excretion of Ranitidine can be decreased when combined with Ataluren.
Cabotegravir The excretion of Ranitidine can be decreased when combined with Cabotegravir.
Pradigastat The excretion of Ranitidine can be decreased when combined with Pradigastat.
Cefotiam The excretion of Ranitidine can be decreased when combined with Cefotiam.
Cefalotin The excretion of Ranitidine can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Ranitidine can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Ranitidine can be decreased when combined with Cefotaxime.
Piroxicam The excretion of Ranitidine can be decreased when combined with Piroxicam.
Cephalexin The excretion of Ranitidine can be decreased when combined with Cephalexin.
Acyclovir The excretion of Ranitidine can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Ranitidine can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Ranitidine can be decreased when combined with Cefaclor.
Salicylic acid The excretion of Ranitidine can be decreased when combined with Salicylic acid.
Ketoprofen The excretion of Ranitidine can be decreased when combined with Ketoprofen.
Cefadroxil The excretion of Ranitidine can be decreased when combined with Cefadroxil.
Cefamandole The excretion of Ranitidine can be decreased when combined with Cefamandole.
Cefazolin The excretion of Ranitidine can be decreased when combined with Cefazolin.
Ceftizoxime The excretion of Ranitidine can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Ranitidine can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Ranitidine can be decreased when combined with Ceftibuten.
Cefaloridine The excretion of Ranitidine can be decreased when combined with Cefaloridine.
Liothyronine The excretion of Ranitidine can be decreased when combined with Liothyronine.
Pravastatin The excretion of Ranitidine can be decreased when combined with Pravastatin.
Pantoprazole The excretion of Ranitidine can be decreased when combined with Pantoprazole.
Conjugated estrogens The excretion of Ranitidine can be decreased when combined with Conjugated estrogens.
Indomethacin The excretion of Ranitidine can be decreased when combined with Indomethacin.
Lansoprazole The excretion of Ranitidine can be decreased when combined with Lansoprazole.
Zidovudine The excretion of Ranitidine can be decreased when combined with Zidovudine.
Methotrexate The excretion of Ranitidine can be decreased when combined with Methotrexate.
Diclofenac The excretion of Ranitidine can be decreased when combined with Diclofenac.
Esomeprazole The excretion of Ranitidine can be decreased when combined with Esomeprazole.
Tetracycline The excretion of Ranitidine can be decreased when combined with Tetracycline.
Acetylsalicylic acid The excretion of Ranitidine can be decreased when combined with Acetylsalicylic acid.
Ibuprofen The excretion of Ranitidine can be decreased when combined with Ibuprofen.
Ceftriaxone The excretion of Ranitidine can be decreased when combined with Ceftriaxone.
Cefoperazone The excretion of Ranitidine can be decreased when combined with Cefoperazone.
Taurocholic acid The excretion of Ranitidine can be decreased when combined with Taurocholic acid.
Dolutegravir The excretion of Ranitidine can be decreased when combined with Dolutegravir.
Lenvatinib The excretion of Ranitidine can be decreased when combined with Lenvatinib.
Baricitinib Ranitidine may decrease the excretion rate of Baricitinib which could result in a higher serum level.
Apalutamide The excretion of Ranitidine can be decreased when combined with Apalutamide.
Rucaparib The metabolism of Rucaparib can be decreased when combined with Ranitidine.
Favipiravir The excretion of Ranitidine can be decreased when combined with Favipiravir.
Cimetidine The excretion of Ranitidine can be decreased when combined with Cimetidine.
Tafamidis The excretion of Ranitidine can be decreased when combined with Tafamidis.
Linezolid The excretion of Ranitidine can be decreased when combined with Linezolid.
Cefpodoxime Ranitidine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime Ranitidine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dasatinib Ranitidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.

Target Protein

Histamine H2 receptor HRH2
Acetylcholinesterase ACHE

Referensi & Sumber

Synthesis reference: John W. Clitherow, "Intermediates in the preparation of ranitidine." U.S. Patent US4413135, issued November, 1981.
Artikel (PubMed)
  • PMID: 27083385
    Mauran A, Goze T, Abadie D, Bondon-Guitton E, Chevrel P, Schmitt L, Montastruc JL, Montastruc F: Mania associated with ranitidine: a case report and review of literature. Fundam Clin Pharmacol. 2016 Aug;30(4):294-6. doi: 10.1111/fcp.12201. Epub 2016 May 5.
  • PMID: 2667937
    Grant SM, Langtry HD, Brogden RN: Ranitidine. An updated review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in peptic ulcer disease and other allied diseases. Drugs. 1989 Jun;37(6):801-70. doi: 10.2165/00003495-198937060-00003.
  • PMID: 16341949
    Pettit M: Treatment of gastroesophageal reflux disease. Pharm World Sci. 2005 Dec;27(6):432-5. doi: 10.1007/s11096-005-4798-7.
  • PMID: 25133039
    Badillo R, Francis D: Diagnosis and treatment of gastroesophageal reflux disease. World J Gastrointest Pharmacol Ther. 2014 Aug 6;5(3):105-12. doi: 10.4292/wjgpt.v5.i3.105.
  • PMID: 3307670
    Sontag S, Robinson M, McCallum RW, Barwick KW, Nardi R: Ranitidine therapy for gastroesophageal reflux disease. Results of a large double-blind trial. Arch Intern Med. 1987 Aug;147(8):1485-91.
  • PMID: 6323334
    Vezzadini P, Bonora G, Tomassetti P, Pazzaglia M, Labo G: Medical treatment of Zollinger-Ellison syndrome with ranitidine. Int J Tissue React. 1983;5(4):339-43.
  • PMID: 6329583
    Roberts CJ: Clinical pharmacokinetics of ranitidine. Clin Pharmacokinet. 1984 May-Jun;9(3):211-21. doi: 10.2165/00003088-198409030-00003.
  • PMID: 17688076
    Gschwend MH, Guserle R, Erenmemisoglu A, Martin W, Tamur U, Kanzik I, Hincal AA: Pharmacokinetics and bioequivalence study of ranitidine film tablets in healthy male subjects. Arzneimittelforschung. 2007;57(6):315-9. doi: 10.1055/s-0031-1296625.
Textbook
  • Caitlin C. Nugent; Jamie M. Terrell (2018). H2 Blockers- StatPearls. StatPearls Publishing.

Contoh Produk & Brand

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