Rifaximin

Rifaximin 속성

Rifaximin MSDS

Rifaximin

Rifaximin C화학적 특성, 용도, 생산

개요

Rifaximin is an antibiotic structurally related to rifamycin. It is reported to be efficacious in the treatment of gastrointestinal infections and hepatic encephalopathy, being highly active against Gram-positive and -negative aerobic and anaerobic bacteria. Due to poor systemic absorption, rifaximin is effective in presurgical sterilization of the GI tract.It displays good activity against a wide spectrum of bacteria, including Salmonella spp., S. aureus, and E. coli.

화학적 성질

Red-Orange Crystalline Powder

용도

Rifaximin is a non-absorbable semisynthetic Rifamycin antibiotic.

정의

ChEBI: A semisynthetic member of the class of rifamycins and non-systemic gastrointestinal site-specific broad spectrum antibiotic. Used in the treatment of traveller's diarrhoea, hepatic encephalopathy and irritable bowel syndrome.

Antimicrobial activity

The in-vitro activity is slightly inferior to that of rifampicin. The MIC90 for Gram-positive cocci is well below 1 mg/L, with the exception of enterococci (MIC 2–8 mg/L). Among intestinal pathogens C. difficile is sensitive (MIC90 0.8 mg/L), Esch. coli, Salmonella spp. and Shigella spp. are inhibited by 4–8 mg/L. Campylobacter jejuni is mostly insensitive.

Pharmaceutical Applications

A semisynthetic derivative of rifamycin S formulated for oral administration. It is poorly absorbed from the gastrointestinal tract, where its high concentrations are effective against a variety of gastrointestinal pathogens.

Mechanism of action

The mechanism of action of pyrazinamide is unknown, but recent findings suggest that pyrazinamide may be active either totally or in part as a pro-drug. Susceptible organisms produce pyrazinamidase, which is responsible for conversion of pyrazinamide to pyrazinoic acid intracellularly. Mutation in the pyrazinamidase gene (pncA) results in resistant strains of M . tuberculosis. Pyrazinoic acid has been shown to possess biological activity at a pH 5.4 or lower, in contract in vitro tests that show pyrazinoic acid is 8- to 16-fold less active than pyrazinamide . Pyrazinoic acid may lower the pH in the immediate surroundings of the M . tuberculosis to such an extent that the organism is unable to grow, but this physicochemical property appears to account for only some of the activity. The protonated pyrazinoic acid also can permeate the mycobacterial membrane to lower the pH of the cytoplasm. Recent evidence suggests that pyrazinoic acid decreases membrane potential in older, nonreplicating bacilli, thus decreasing membrane transport, and interferes with the energetics of the membrane.

Pharmacokinetics

Oral absorption is very low. However, a fraction of the dose may be absorbed and rapidly eliminated through the bile. A 400 mg oral dose produces a maximum plasma concentration of 3.8 mg/L after 1.2 h. The plasma half-life is 5.8 h. Up to 90% of the administered dose is concentrated in the gut, less than 0.2% in the liver and kidney, and less than 0.01% in other tissues.

Clinical Use

It is used for a variety of gastrointestinal diseases, including the treatment of traveler’s diarrhea. Preliminary results suggest clinical efficacy in the therapy of hepatic encephalopathy and of C. difficile infections.

부작용

Oral doses up to 100 mg/kg for 6 months produced no significant signs of toxicity to rats. Teratogenic effects in rats and rabbits have been reported (pregnancy category C).
Very few adverse effects were reported during human treatment, mostly gastrointestinal discomfort. Prolonged therapy was associated with infrequent urticarial skin reactions.

신진 대사

Pyrazinamide is readily absorbed after oral administration, but little of the intact molecule is excreted unchanged. The major metabolic route consists of hydrolysis by hepatic microsomal pyrazinamidase to pyrazinoic acid, which may then be oxidized by xanthine oxidase to 5-hydroxypyrazinoic acid. The latter compound may appear in the urine either free or as a conjugate with glycine.

Rifaximin 준비 용품 및 원자재

원자재

준비 용품

Rifaximin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12470	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8617865335152	Mandy@hangyubiotech.com	China	11013	58
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	525	58
Henan Suikang Pharmaceutical Co.,Ltd.	+86-18239973690 +86-18239973690	sales@suikangpharm.com	China	186	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21689	55
Hubei XinRunde Chemical Co., Ltd.	+8615102730682	bruce@xrdchem.cn	CHINA	566	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
Casorganics US Corp	+17326109938	sales@casorganics.com	CHINA	174	58

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