Roxatidine

• N- { -3 [3 - ( piperidinomethyl ) phenoxy] - propyl} glycolamid
• N- { -3 [( α - piperidino - m- tolyl) oxy] - propyl} glycolamid
• 2-hydroxy- N-(3 - [3 - (1- piperidinylmethyl ) - phenoxy]- propyl) -acetamide

A02BA06

Gastric acid blocker

H2 - antagonist

755-787 mg · kg -1 ( LD50, rat, oral)

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Roxatidine ( Roxatidinacetat ) (trade name: Roxit ) is a drug from the group of H2 - antagonists for the treatment of gastric and duodenal ulcers.

Effect

Roxatidine acts as a competitive antagonist of histamine on parietal cells in the stomach and thus inhibits acid secretion. It has a four times greater antisecretory effect than cimetidine.

Pharmacokinetics

Roxatidine is taken in the form of Roxatidinacetat, a prodrug that is metabolized by the organism to the actual drug. Roxatidinacetat is rapidly absorbed following oral administration and deacylated in the body to roxatidine. The max. Plasma levels is reached after 2-3 h. Within 24 hours, more than 90 % of the administered acetate roxatidine appear in the urine. The major metabolite of the acetate is 55% roxatidine, and there are at least 9 more.

Dosage

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

Contraindications

• Anuria
• Children under 14 years
• Hepatic impairment ( no ther. Experience)

Roxatidine passes into the central nervous system and into breast milk in small part.

Adverse effects

Rarely, allergic reactions such as itching and rash occur, continue headache ( 1%), insomnia, restlessness, fatigue, tachycardia (rare), diarrhea ( 1%), constipation ( 0.5%).

There is no evidence of mutagenic, teratogenic or carcinogenic effects.