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药品详细

Ranitidine(雷尼替丁)

化学结构式图
中文名
雷尼替丁
英文名
Ranitidine
分子式
C13H22N4O3S
化学名
dimethyl[(5-{[(2-{[(E)-1-(methylamino)-2-nitroethenyl]amino}ethyl)sulfanyl]methyl}furan-2-yl)methyl]amine
分子量
Average: 314.404
Monoisotopic: 314.14126128
CAS号
66357-35-5
ATC分类
A02B 未知;A02B 未知
药物类型
small molecule
阶段
approved
商品名
Alquen;Alter-H2;Alvidina;Apo-Ranitidin;Artomil;Azuranit;Coralen;Digestosan;Ergan;Esofex;Fendibina;Gastrial;Gastridina;Gastrolav;Gastrosedol;Kuracid;Label;Lake;Logat;Melfax;Microtid;Mideran;Neugal;Noctone;Noktome;Normon;Novo-Radinine;Nu-Ranit;Pep-Rani;Ptinolin;Quadrin;Quantor;Radin;RAN;Ran H2;Ran Lich;Rani 2;Rani AbZ;Rani-BASF;Rani-nerton;Rani-Puren;Rani-Q;Rani-Sanorania;Raniben;Raniberl;Raniberta;Ranibloc;Ranic;Ranicux;Ranidil;Ranidin;Ranidine;Ranidura;Ranifur;Ranigasan;Ranigast;Ranigen;Ranilonga;Ranimerck;Raniogas;Raniplex;Ranisan;Ranitab;Ranitic;Ranitidin;Ranitidin 1A Pharma;Ranitidin AL;Ranitidin Arcana;Ranitidin Atid;Ranitidin AWD;Ranitidin Basics;Ranitidin Duncan;Ranitidin Dyna;Ranitidin Helvepharm;Ranitidin Heumann;Ranitidin Hexal;Ranitidin Merck;Ranitidin Millet;Ranitidin NM;Ranitidin Normon;Ranitidin PB;Ranitidin Stada;Ranitidin von ct;Ranitidin-Cophar;Ranitidin-Isis;Ranitidin-ratiopharm;Ranitidina predilu Grif;Ranitidina Tamarang;Ranitiget;Ranitin;Ranitine;Ranobel;Rantacid;Ranuber;Raticina;Regalil;Renatac;Rozon;Rubiulcer;Santanol;Serviradine;Sostril;Tanidina;Taural;Terposen;Toriol;Trigger;Ulcecur;Ulcex;Ulcirex;Ulcodin;Ulcolind Rani;Ulsaven;Ultidine;Viserul;Zandid;Zantac;Zantac 150;Zantac 75;Zantac In Plastic Container;Zantarac;Zantic;
同义名
Ranitidine Base;Ranitidine HCL;Ranitidine hydrochloride;Rantidine HCL;
基本介绍

A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers. [PubChem]

生产厂家
  • Alpharma us pharmaceuticals division
  • Amneal pharmaceuticals
  • Amneal pharmaceuticals ny llc
  • Apotex inc
  • Aurobindo pharma usa inc
  • Bedford laboratories div ben venue laboratories inc
  • Ben venue laboratories inc
  • Boehringer ingelheim
  • Boehringer ingelheim corp
  • Boehringer ingelheim pharmaceuticals inc
  • Contract pharmacal corp
  • Cypress pharmaceutical inc
  • Dr reddys laboratories inc
  • Dr reddys laboratories ltd
  • Genpharm inc
  • Glaxosmithkline
  • Glenmark generics inc usa
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • L perrigo co
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pharmaceutical assoc inc div beach products
  • Ranbaxy laboratories ltd
  • Ranbaxy pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Torpharm inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • Wockhardt americas inc
  • Wockhardt ltd
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Furans
Substructures
  • Ethers
  • Oxoazaniums
  • Nitro compounds
  • Aliphatic and Aryl Amines
  • Heterocyclic compounds
  • Aromatic compounds
  • Furans
适应症
gastric acid RELATED DISORDERS 中和胃酸;
药理
Indication Used in the treatment of peptic ulcer disease (PUD), dyspepsia, stress ulcer prophylaxis, and gastroesophageal reflux disease (GERD).
Pharmacodynamics Ranitidine is a histamine H2-receptor antagonist similar to cimetidine and famotidine. An H2-receptor antagonist, often shortened to H2 antagonist, is a drug used to block the action of histamine on parietal cells in the stomach, decreasing acid production by these cells. These drugs are used in the treatment of dyspepsia, however their use has waned since the advent of the more effective proton pump inhibitors. Like the H1-antihistamines, the H2 antagonists are inverse agonists rather than true receptor antagonists.
Mechanism of action The H2 antagonists are competitive inhibitors of histamine at the parietal cell H2 receptor. They suppress the normal secretion of acid by parietal cells and the meal-stimulated secretion of acid. They accomplish this by two mechanisms: histamine released by ECL cells in the stomach is blocked from binding on parietal cell H2 receptors which stimulate acid secretion, and other substances that promote acid secretion (such as gastrin and acetylcholine) have a reduced effect on parietal cells when the H2 receptors are blocked.
Absorption Approximately 50% bioavailability orally.
Volume of distribution
  • 1.4 L/kg
  • 1.76 L/kg [clinically significant renal function impairment (creatinine clearance 25 to 35 mL/min)]
Protein binding 15%
Metabolism
Hepatic. Ranitidine is metabolized to the N-oxide, S-oxide, and N-desmethyl metabolites, accounting for approximately 4%, 1%, and 1% of the dose, respectively.
Route of elimination The principal route of excretion is the urine (active tubular excretion, renal clearance 410mL/min), with approximately 30% of the orally administered dose collected in the urine as unchanged drug in 24 hours.
Half life 2.8-3.1 hours
Clearance
  • 29 mL/min [clinically significant renal function impairment]
  • 3 mL/min/Kg [neonatal patients]
Toxicity LD50=77mg/kg (orally in mice). Symptoms of overdose include muscular tremors, vomiting, and rapid respiration.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00230 Ranitidine Pathway SMP00230
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 69-70 °C PhysProp
water solubility 24.7 mg/mL Not Available
logP 0.27 SANGSTER (1993)
Caco2 permeability -6.31 ADME Research, USCD
Predicted Properties
Property Value Source
water solubility 7.95e-02 g/l ALOGPS
logP 0.79 ALOGPS
logP 0.98 ChemAxon
logS -3.6 ALOGPS
pKa (strongest basic) 8.08 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 86.26 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 95.15 ChemAxon
polarizability 33.58 ChemAxon
药物相互作用
Drug Interaction
Acenocoumarol Ranitidine may increase the anticoagulant effect of acenocoumarol. (Conflicting evidence)
Anisindione Ranitidine may increase the anticoagulant effect of anisindione. (Conflicting evidence)
Atazanavir Ranitidine may decrease the levels/effects of atazanavir.
Cefditoren H2-Antagonists such as ranitidine may decrease the serum concentration of cefditoren. Cefditoren prescribing information recommends to avoid concomitant use with H2-antagonists (eg, famotidine, ranitidine) and antacids as well. Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of H2-antagonists can not be avoided.
Dabrafenib H2-receptor antagonists may alter the solubility of dabrafenib and reduce its bioavailability.
Dasatinib Ranitidine may decrease the serum level of dasatinib.
Dicumarol Ranitidine may increase the anticoagulant effect of dicumarol. (Conflicting evidence)
Itraconazole The H2-receptor antagonist, ranitidine, may decrease the absorption of itraconazole.
Ketoconazole The H2-receptor antagonist, ranitidine, may decrease the absorption of ketoconazole.
Procainamide The histamine H2-receptor antagonist, ranitidine, may increase the effect of procainamide.
Rilpivirine Histamine-2 receptor antagonists increase gastric pH which causes a decrease in the exposure of rilpivirine thus reducing efficacy.
Tolazoline Anticipated loss of efficacy of tolazoline
Vismodegib Vismodegib serum concentrations may be decreased by histamine 2 receptor antagonists such as ranitidine.
Warfarin Ranitidine may increase the anticoagulant effect of warfarin. (Conflicting evidence)
食物相互作用
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.
  • Take without regard to meals.

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