Roxatidine

Structural formula
General
Non-proprietary name	Roxatidine
other names	N - {3- [3- (piperidinomethyl) phenoxy] propyl} glycolamide; N - {3 - [(α-piperidino- m -tolyl) -oxy] -propyl} glycolamide; 2-hydroxy- N - (3- [3- (1-piperidinylmethyl) phenoxy] propyl) acetamide;
Molecular formula	C 17 H 26 N 2 O 3
External identifiers / databases
PubChem	91276
ChemSpider	82423
Wikidata	Q415039
Drug information
ATC code	A02 BA06
Drug class	Gastric acid blockers
Mechanism of action	H 2 antagonist
properties
Molar mass	306.4 g · mol -1
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling ; no classification available
Toxicological data	755–787 mg kg −1 ( LD 50 , rat , oral )
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Roxatidine ( Roxatidine Acetate) (trade name: Roxit) is a drug from the group of H ₂ antagonists for the treatment of gastric and duodenal ulcers .

effect

Roxatidine acts as a competitive histamine antagonist on the parietal cells of the stomach and thus inhibits acid secretion. As an acetate, it has a four times stronger antisecretory effect than cimetidine .

Pharmacokinetics

Roxatidine acetate

Roxatidine is taken in the form of roxatidine acetate, a prodrug that is metabolized by the body to the actual active ingredient. Roxatidine acetate is quickly absorbed after oral intake and deacylated to roxatidine in the body. The maximum plasma level is reached after 2–3 hours. Within 24 hours, more than 90% of the administered acetate appears as roxatidine in the urine. The main metabolite of acetate is 55% roxatidine, there are at least 9 others.

dosage

The usual daily dose is 150 mg, with an application period of 4 to 8 weeks.

Contraindications

Anuria
Children under 14 years
Liver dysfunction (no thermal experience)

A small amount of roxatidine passes into the central nervous system and into breast milk .

unwanted effects

Allergic effects such as itching and rash can occur rarely, as well as headache (1%), sleep disorders, restlessness, fatigue, tachycardia (rarely), diarrhea (1%), constipation (0.5%).

There is no evidence of a mutagenic , teratogenic or carcinogenic effect.

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ ^a ^b ^c ^d ^e ^f ^g F. von Bruchhausen et al .: Hager's handbook of pharmaceutical practice . Vol. 9, fabrics P – Z, 1994, p. 535 ff. ( Limited preview in the Google book search).

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[hager-2] ↑ ^a ^b ^c ^d ^e ^f ^g F. von Bruchhausen et al .: Hager's handbook of pharmaceutical practice . Vol. 9, fabrics P – Z, 1994, p. 535 ff. ( Limited preview in the Google book search).