66357-59-3 Usage
Background and overview
Ranitidine Hydrochloride (RHCl) is a kind of histamine H2 receptor antagonist. Since its listing in 1981, ranitidine hydrochloride has been widely used in nearly one hundred countries in the world, including China. It is clinically used for the treatment of duodenal ulcer, reflux esophagitis and Zollinger-Ellison syndrome. It is also used for the prevention of gastrointestinal bleeding caused by stress ulcer and recurrent hemorrhage of peptic ulcer. In recent decade, through the combination of ranitidine and other drugs, it has found that it has high efficiency and remarkable features in the treatment of Helicobacter pylori-positive duodenal ulcer, urticaria and post-cerebral hemorrhage stress ulcer with better efficacy than other similar drugs. Owing to its rapid effect, good potency and low price, ranitidine hydrochloride plays an important role in the anti-ulcer drug market today. Therefore, strict quality control plays important roles in guiding patients with reasonable, safe medication.
Pharmacological effects
This product is a H2 receptor inhibitor, being capable of inhibiting the gastric acid secretion. After oral administration, it is absorbed through the gastrointestinal tract quickly. Synthetic route [4]
The intermediates (3) and (5) were synthesized as follows. The intermediates (3) and (5) were then reacted to produce (6) ranitidine. The (6) is subject to purification and salt formation to generate ranitidine hydrochloride, as shown:
Pharmacokinetics
After oral administration, it is absorbed rapidly from the gastrointestinal tract with a bioavailability (F) of about 50% and peak plasma concentration (tmax) reaching within 1 to 2 hours. Plasma protein binding rate is 15% ± 3%; effective blood concentration is 100ng / ml, widely distributed in the body with the apparent volume of distribution (Vd) of 1.1 ~ 1.9L / Kg. It can penetrate through the blood brain barrier with the drug concentration in cerebrospinal fluid being 1/30 ~ 1 / 20 of blood concentration. 30% is subject to liver metabolism with the metabolites including N-oxide, S-oxide and demethylation metabolites. 50% of the prototype is subject to urine excretion through kidney. Half-life (t1 / 2) is 2 to 3 hours, which is similar to cimetidine. Renal failure causes corresponding increase in the half-life. The goods can be transplanted via the placenta with the milk concentration being higher than the plasma concentration of drugs.
Indications
For the treatment of duodenal ulcer, gastric ulcer, reflux esophagitis, Zollinger-Ellison syndrome and other high acid secretion disorders.
Adverse reactions
Common reactions are: nausea, rash, constipation, fatigue, headache, dizziness and so on.
Light adverse reactions on the renal function, gonadal function and central nervous system.
A small number of patients get mild liver damage after taking the drug with the symptoms disappearing after stopping, liver function returned to normal.
Medicine interactions
Combination with procainamide reduces the clearance rate of the later one.
Drug interactions may occur if used with other medications, consult physician or pharmacist for details.
Precautions
This product mustn’t be used continuously for more than 7 days, the symptom is not relieved, consult your physician or pharmacist.
Elderly patients or patients with liver and kidney dysfunction use with caution.
If overdose or serious adverse reactions, should seek medical treatment immediately.
Disable it for people who are allergic to this product; allergies should use with caution.
This product is not allowed for administration upon change of its traits.
Please put this product where children cannot touch.
Children must be under adult guardianship.?
If you are using other drugs, please consult your physician or pharmacist before using this product.
Contraindication
Children under 8 years should be disabled.
Pregnant and lactating women should be disabled.
Elderly patients medication
The elderly have reduced liver and kidney function; in order to ensure drug safety, dosage should be adjusted.
Chemical Properties
Off-White Crystalline Solid
Uses
Different sources of media describe the Uses of 66357-59-3 differently. You can refer to the following data:
1. A histamine H2-receptor antagonist which inhibits gastric acid secretion. Antiulcerative.
2. antifungal
3. An H-2 histamine receptor antagonistRanitidine hydrochloride is mainly used as an H2-receptor antagonist and helps in the treatment of gastrointestinal lesions because of excessive gastric acid secretion. It also serves as an antiulcer drug.
Brand name
Zantac (GlaxoSmithKline).
Biological Activity
ranitidine is a histamine h2-receptor antagonist that inhibits stomach acid production.ranitidine (zantac) is a histamine h2-receptor antagonist with ic50 of 3.3 ± 1.4 um. it inhibits stomach acid production. it is also used alongside fexofenadine and oth
Biochem/physiol Actions
H2 histamine receptor antagonist; anti-ulcer agent.
Contact allergens
Ranitidine, an H2-receptor antagonist, can cause contact
dermatitis within the pharmaceutical industry and
in health care workers, or may induce systemic drug
reactions in patients.
Check Digit Verification of cas no
The CAS Registry Mumber 66357-59-3 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,6,3,5 and 7 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 66357-59:
(7*6)+(6*6)+(5*3)+(4*5)+(3*7)+(2*5)+(1*9)=153
153 % 10 = 3
So 66357-59-3 is a valid CAS Registry Number.
InChI:InChI=1/C12H20N4O3S.ClH/c1-13-11(8-16(17)18)14-6-7-20-9-10-4-5-12(19-10)15(2)3;/h4-5,8,13-14H,6-7,9H2,1-3H3;1H/b11-8+;
66357-59-3Relevant articles and documents
Preparation method of ranitidine hydrochloride with low NDMA content
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Paragraph 0016-0019, (2020/12/15)
The invention relates to the technical field of ranitidine hydrochloride preparation, in particular to a preparation method of ranitidine hydrochloride with low NDMA content, which comprises the following steps: adding a ranitidine base into ethanol, and stirring until complete dissloving is achieved; cooling the solution to -5 to 5 DEG C; controlling the temperature, adding a hydrochloric acid aqueous solution, adjusting the pH value to 4.5-6.5, and uniformly stirring; adding a seed crystal, preserving heat, stirring and crystallizing for 3-5 hours; and filtering a crystal, washing, drainingand drying to obtain the off-white crystal solid ranitidine hydrochloride. The salifying method disclosed by the invention has the advantages that the steps are simple, the raw material hydrochloric acid aqueous solution is easy to obtain, the product character is good, and the impurity content of the final product NDMA (N-Nitrosodimethylamine) is low.
Preparation of acid addition salts of amine bases by solid phase-gas phase reactions
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Page/Page column 3, (2008/06/13)
A process for the preparation of an acid addition salt of an organic base comprising exposing the organic base in solid form to a gaseous acid, with the proviso that ziprasidone, its acid addition salts and intermediates thereof are excluded.
Aminoalkyl furan derivatives
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, (2008/06/13)
Compounds of the general formula I: STR1 and physiologically acceptable salts thereof and N-oxides and hydrates, in which R1 and R2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group STR2 in which R4 represents hydrogen or lower alkyl or R1 and R2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and STR3 R3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH2 --, O or S; Y represents = S, = O, = NR5 or = CHR6 ; Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms; R5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl; R6 represents nitro, arylsulphonyl or alkylsulphonyl; M is an integer from 2 to 4; and N is 1 or 2; or when X = S, or --CH2 --, n is zero, 1 or 2. These compounds have H2 -antagonist activity. Intermediates in the production thereof are also provided.
