ROXATIDINE ACETATE HYDROCHLORIDE

Synonyms. Roxatidine Acetate Hydrochloride; Roxit; Gastralgin; HOE 062; 2-Acetoxy-N-(3-(m-(1-piperidinylmethyl)phenoxy)propyl)acetamide hydrochloride 2-Hydroxy-N-(3-(m-(piperidinomethyl)phenoxy)propyl)acetamide acetate hydrochloride; Aceroxatidine hydrochloride; 2-(Acetyloxy)-N-(3-(3-(1-piperidinylmethyl)phenoxy)propyl)acetamide monohydrochloride; 2-(Acetyloxy)-N-(3-(3-(1-piperidinylmethyl)phenoxy)propyl-acetamide monohydrochloride; 2-Hydroxy-N-(3-(m-(1-piperidinylmethyl)phenoxy)propyl)acetamide acetate hydrochloride; Altat; N-(3-((alpha-Piperidino-m-tolyl)oxy)propyl)glycolamide acetate monohydrochloride; Other RN: 97744-01-9

ROXATIDINE ACETATE HYDROCHLORIDE

 

PRODUCT IDENTIFICATION

CAS RN

78628-28-1, 93793-83-0 (HCl)

EINECS RN

  

FORMULA

C19H28N2O4·HCl

MOLE WEIGHT

 384.95

H.S CODE

  

SMILES

 c1(cc(ccc1)OCCCNC(COC(C)=O)=O)CN1CCCCC1.Cl

CLASSIFICATION

Anti-ulcerative, Histamine Antagonist

EXTRA NOTES

  

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE.

white powder

MELTING POINT

146 ~ 148 C

BOILING POINT

537 C

DENSITY

 

SOLUBILITY IN WATER

 

SOLVENT SOLUBILITY  

VAPOR DENSITY

 

log P(octanol-water)

  

VAPOR PRESSURE

  

AUTOIGNITION TEMP

  
pKa

 

REFRACTIVE INDEX

 

FLASH POINT

 

 

STABILITY AND REACTIVITY
STABILITY Stable under normal conditions.

INCOMPATIBLE MATERIALS

Strong oxidizing agents
POLYMERIZATION

Has not been reported

NFPA RATINGS

Health: 3, Flammability:0, Reactivity: 0

 

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking - Roxatidine

Google Scholar Search - Roxatidine Acetate

Drug Information Portal (U.S. National Library of Medicine) - Roxatidine Acetate

PubChem Compound Summary - Roxatidine Acetate

Drug Bank -  Roxatidine Acetate

KEGG (Kyoto Encyclopedia of Genes and Genomes) - Roxatidine Acetate

http://www.ebi.ac.uk/ - Roxatidine Acetate

http://www.ncbi.nlm.nih.gov/ - Roxatidine Acetate

http://dmd.aspetjournals.org/
The metabolism of roxatidine acetate hydrochloride (RA), a new histamine-2 receptor antagonist, was studied by GC/MS in rats and dogs in vivo. The co-administration of 14C-RA and RA-d10 labeled with deuterium in the piperidine ring expedited the isolation and identification of 15 urinary metabolites. The major metabolites in both animals were M-1, M-8, M-10, and M-11; M-4 could be found only in the rat. The aromatic and piperidine ring-hydroxylated metabolites were found in small amounts in both species. Following the administration of RA-d10 to rats and dogs, oxygenated metabolites on the piperidine ring, such as M-3 and M-4, were isolated and their analysis indicated the unexpected loss of three or four deuterium atoms from the ring. Also, first and second isotope effects were observed on the conversion rate in vivo and retention time in HPLC, respectively.

http://pubmedcentralcanada.ca/
It is well documented that histamine H2 receptor antagonists decrease gastric acid production by competitively inhibiting the action of histamine on the H2 receptor of gastric parietal cell. Since this drug is efficacious in decreasing gastric juices and increasing gastric pH, several investigators have noted that it would be useful for the prophylaxis of acid aspiration pneumonia, which is one of the most severe perioperative complications. It is thought that handicapped patients' vomiting reflex is easily triggered; they may also have problems with the swallowing mechanism, and some of them suffer from silent regurgitation. In addition, some uncooperative and noncomprehending individuals may eat or drink before anesthesia despite specific instructions about fasting. Therefore, general anesthesia for the handicapped requires careful attention to vomiting and aspiration pneumonia. We evaluated the effect of the long-acting H2 receptor antagonist, roxatidine acetate hydrochloride, on gastric volume and gastric pH when given as an oral preanesthetic.

 

SALES SPECIFICATION

APPEARANCE

white powder

ASSAY

99.0% min

MELTING POINT

146 ~ 148 C

LOSS ON DRYING

0.5% max

ASH

0.1% max

HEAVY METALS

20ppm max

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

Not regulated

HAZARD CLASS

  
PACKING GROUP  

 

SAFETY INFORMATION

HAZARD OVERVIEW

Not known
HAZARD CODES

 

RISK PHRASES

  

SAFETY PHRASES

  

 

PACKING

 

 

PRICE INFORMATION