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| CAS No.: | 66357-59-3 |
|---|---|
| Name: | Ranitidine Hydrochloride |
| Molecular Structure: | |
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| Formula: | C13H22N4O3S.HCl |
| Molecular Weight: | 350.87 |
| Synonyms: | 1,1-Ethenediamine,N-[2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-N'-methyl-2-nitro-,monohydrochloride (9CI);AH 19065;Achedos;Acloral;Aldin;Anistal;Antagonin;Axoban;Azantac;Consec;Coralen;Curan;Ezopta;Gastrial;Gastrosedol;Histac;Histak;Lydin;Melfax;Noctone;Ptinolin;Quicran;Radinat;Ranacid;Randin;Rani 2;Ranial;Raniben;Ranidine;Ranigast;Ranimex;Raniogas;Raniplex;Ranitab;Ranitidine hydrochloride;Ranitidine-akri;Ranitiget;Ranitin;Ranix;Rantac;Rantidol;Rantin;Ranuber;Raticina;Simetac;Sostril;Taural;Terposen;Trigger;Ul-Pep;Ulcex;Ulsal;Ultidine;Urantac;Verlost;Vesyca;Weichilin;Weidos;Xanidine;Zantab;Zintac; |
| EINECS: | 266-333-0 |
| Melting Point: | 134 °C (dec.) |
| Solubility: | Soluble in water, 2-hydroxypropyl-beta-cyclodextrin, acetic acid, methanol, ethanol and dimethyl sulfoxide. Insoluble in chloroform. |
| Appearance: | Off-white crystalline solid |
| Hazard Symbols: | F,T |
| Risk Codes: | 20/21/22 |
| Safety: | 22-24/25 |
| PSA: | 111.56000 |
| LogP: | 3.56600 |
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Chemistry
Product Name: Ranitidine hydrochloride (CAS NO.66357-59-3)
Molecular Formula: C13H23ClN4O3S
Molecular Weight: 350.86g/mol
Mol File: 66357-59-3.mol
Einecs: 266-332-5
Appearance: Off-White Crystalline Solid
Melting Point: 134°C (dec.)
Boiling point: 437.1 °C at 760 mmHg
Flash Point: 218.2 °C
Water Solubility: H2O: 1.8 mg/mL
Sensitive: Hygroscopic
Enthalpy of Vaporization: 69.37 kJ/mol
Vapour Pressure: 7.66E-08 mmHg at 25°C
Product Categories: Inhibitors; Intermediates & Fine Chemicals; Pharmaceuticals; Sulfur & Selenium Compounds; AntagonistsEPA; NeatsCell Signaling Enzymes; 1694 Pharmaceuticals&Personal Care Products; Histaminergics; Neurotransmitters; Substrates; Xenobiotics and Drug Metabolism
History
Ranitidine hydrochloride (CAS NO.66357-59-3) was developed by Glaxo in an effort to match the success of Smith, Kline & French (prior to the merger of the two companies into GlaxoSmithKline) with the first histamine H2-receptor antagonist cimetidine. Ranitidine was the result of a rational drug-design process using what was by then a fairly refined model of the histamine H2-receptor and quantitative structure-activity relationships.
Glaxo refined the model further by replacing the imidazole-ring of cimetidine with a furan-ring with a nitrogen-containing substituent, and in doing so developed ranitidine. Ranitidine was found to have a far-improved tolerability profile, longer-lasting action, and ten times the activity of cimetidine. Ranitidine has 10% the affinity that cimetidine has to CYP450 so it causes fewer side effects, but other H2 blockers famotidine and nizatidine have no CYP450 significant interactions.
Ranitidine was introduced in 1981 and was the world's biggest-selling prescription drug by 1988. It has since largely been superseded by the even more effective proton pump inhibitors, with omeprazole becoming the biggest-selling drug for many years. When omeprazole and ranitidine were compared in a study of 144 people with severe inflammation and erosions or ulcers of the esophagus, 85 percent to those treated with omeprazole healed within eight weeks, compared to 50 percent of those given ranitidine. In addition, the omeprazole group reported earlier relief of heart burn symptoms.
Uses
Ranitidine hydrochloride (CAS NO.66357-59-3) is a histamine H2-receptor antagonist that inhibits stomach acid production. It is commonly used in treatment of peptic ulcer disease and gastroesophageal reflux disease . Ranitidine is also used alongside fexofenadine and other antihistamines for the treatment of skin conditions such as hives. Ranitidine HCl is marketed under the brand name Zinetac or Zantac.
Outside of the United States, ranitidine is combined with bismuth as a citrate salt , to treat Helicobacter pylori infections. This combination is usually given with clarithromycin, an antibiotic.
Toxicity Data With Reference
| Organism | Test Type | Route | Reported Dose (Normalized Dose) | Effect | Source |
|---|---|---|---|---|---|
| child | TDLo | oral | 2400mg/kg/43W (2400mg/kg) | BEHAVIORAL: COMA CARDIAC: PULSE RATE SKIN AND APPENDAGES (SKIN): SWEATING: OTHER | American Journal of Diseases of Children. Vol. 139, Pg. 442, 1985. |
| dog | LDLo | oral | 3gm/kg (3000mg/kg) | BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: ATAXIA GASTROINTESTINAL: NAUSEA OR VOMITING | Journal of Toxicological Sciences. Vol. 8(Suppl, |
| man | TDLo | intravenous | 714mg/kg/5M-C (714mg/kg) | CARDIAC: CHANGE IN RATE | American Journal of Gastroenterology. Vol. 83, Pg. 332, 1988. |
| man | TDLo | oral | 8571ug/kg/2D- (8.571mg/kg) | KIDNEY, URETER, AND BLADDER: "CHANGES IN TUBULES (INCLUDING ACUTE RENAL FAILURE, ACUTE TUBULAR NECROSIS)" KIDNEY, URETER, AND BLADDER: INTERSTITIAL NEPHRITIS BLOOD: EOSINOPHILIA | American Journal of Kidney Diseases. Vol. 22, Pg. 337, 1993. |
| man | TDLo | oral | 30mg/kg/1W-I (30mg/kg) | BEHAVIORAL: HEADACHE | New England Journal of Medicine. Vol. 310, Pg. 1602, 1984. |
| man | TDLo | oral | 87mg/kg/4D-I (87mg/kg) | BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: EXCITEMENT CARDIAC: PULSE RATE | Annals of Internal Medicine. Vol. 108, Pg. 493, 1988. |
| mouse | LD50 | intramuscular | 400mg/kg (400mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| mouse | LD50 | intraperitoneal | 300mg/kg (300mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| mouse | LD50 | intravenous | 60mg/kg (60mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD LUNGS, THORAX, OR RESPIRATION: CYANOSIS | Journal of Toxicological Sciences. Vol. 8(Suppl, |
| mouse | LD50 | oral | 1100mg/kg (1100mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) LUNGS, THORAX, OR RESPIRATION: CYANOSIS BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Journal of Toxicological Sciences. Vol. 8(Suppl, |
| mouse | LD50 | subcutaneous | 630mg/kg (630mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| rabbit | LD50 | intravenous | 109mg/kg (109mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| rabbit | LD50 | oral | 2500mg/kg (2500mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| rat | LD50 | intramuscular | 1530mg/kg (1530mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| rat | LD50 | intraperitoneal | 441mg/kg (441mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| rat | LD50 | intravenous | 85mg/kg (85mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) LUNGS, THORAX, OR RESPIRATION: CYANOSIS BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Journal of Toxicological Sciences. Vol. 8(Suppl, |
| rat | LD50 | oral | 4190mg/kg (4190mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) LUNGS, THORAX, OR RESPIRATION: DYSPNEA BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Oyo Yakuri. Pharmacometrics. Vol. 26, Pg. 147, 1983. |
| rat | LD50 | subcutaneous | 1700mg/kg (1700mg/kg) | Yakkyoku. Pharmacy. Vol. 36, Pg. 521, 1985. | |
| women | TDLo | intravenous | 27mg/kg/8D-I (27mg/kg) | BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" | Archives of Internal Medicine. Vol. 152, Pg. 2325, 1992. |
| women | TDLo | multiple routes | 174mg/kg/33D- (174mg/kg) | KIDNEY, URETER, AND BLADDER: "CHANGES IN TUBULES (INCLUDING ACUTE RENAL FAILURE, ACUTE TUBULAR NECROSIS)" KIDNEY, URETER, AND BLADDER: INTERSTITIAL NEPHRITIS | American Journal of Kidney Diseases. Vol. 22, Pg. 333, 1993. |
| women | TDLo | oral | 3mg/kg (3mg/kg) | LUNGS, THORAX, OR RESPIRATION: DYSPNEA SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE" | New England Journal of Medicine. Vol. 310, Pg. 1601, 1984. |
| women | TDLo | oral | 9mg/kg/36H-I (9mg/kg) | BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" | American Journal of Psychiatry. Vol. 143, Pg. 257, 1985. |
| women | TDLo | oral | 12mg/kg/2D-I (12mg/kg) | SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE" | Allergy. Vol. 51, Pg. 659, 1996. |
Safety Profile
Safety Information of Ranitidine hydrochloride (CAS NO.66357-59-3):
Risk Statements: 20/21/22
20: Harmful by inhalation
21: Harmful in contact with skin
22: Harmful if swallowed
Safety Statements: 22-24/25
22: Do not breathe dust
24: Avoid contact with skin
25: Avoid contact with eyes
Specification
Ranitidine hydrochloride ,its CAS NO. is 66357-59-3,the synonyms is 1,1-Ethenediamine, N-(2-(((5-((dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-, monohydrochloride ; Alvidina ; Apo-Ranitidin ; Coralen ; Digestosan ; Ergan ; Esofex ; Fendibina ; Gastridina ; Gastrolav ; Kuracid ; Label ; Mideran ;N-(2-(((5-((Dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine, hydrochloride ; Neugal ; Noktome ; Normon ; Novo-Radinine ; Ranitidin Helvepharm ; Ulcolind Rani ; Zantac in plastic container .