오셀타미비르

오셀타미비르 속성

오셀타미비르 C화학적 특성, 용도, 생산

용도

Oseltamivir is an orally active inhibitor of influenza virus neuraminidase; converted in vivo to the active acid metabolite. An antiviral drug. It is a COVID19-related research product.

정의

ChEBI: A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.

Indications

Oseltamivir phosphate (Tamiflu) is the ethyl ester prodrug of oseltamivir carboxylate, an analogue of neuraminic (sialic) acid that is a reversible competitive antagonist of influenza A and B neuraminidase.Influenza virus resistant to oseltamivir has not been found in naturally acquired isolates but has been isolated from influenza patients who have undergone treatment with this drug.These resistant strains contain mutations in the active site of neuraminidase and are generally less virulent and infective than nonresistant virus. In vitro passage of influenza virus in the presence of oseltamivir carboxylate can produce mutations in hemagglutinin that decrease the overall dependence of viral replication on neuraminidase; however, the clinical relevance of this resistance mechanism is unknown.

Antimicrobial activity

Oseltamivir is active against influenza A and B, but no other virus.

원료

Mutations in the neuraminidase (H274Y) have been detected in treated patients with seasonal H1N1 infection. Cross-resistance with zanamivir has been described in vitro.

Pharmaceutical Applications

A selective neuraminidase inhibitor, formulated as the phosphate salt of the ethyl ester for oral administration.

Pharmacokinetics

Oral absorption: c. 75%
C_max 75 mg oral: 0.35–0.55 mg/L after 4 h
Plasma half-life: 7–9 h
Plasma protein binding: Not known
The ethyl ester prodrug is hydrolyzed by hepatic esterases to release the active compound, oseltamivir carboxylate. Drug is excreted in the urine as the carboxylate derivative.

Clinical Use

Oseltamivir is approved for the treatment of uncomplicated acute influenza in patients aged 1 year and older. It decreases the duration of illness by 1 to 1.5 days when treatment is initiated within 48 hours of the onset of symptoms. Oseltamivir is also indicated for the prophylaxis of influenza in individuals aged 13 and older. It reduces infection rates to approximately 10 to 25% of that found in untreated populations; however, it is not intended to substitute for the early vaccination recommended by the CDC. Oseltamivir can be used as postexposure prophylaxis in household contacts of infected patients, with infection rates of treated patients around 10% of placebo control levels.

부작용

The most frequently reported adverse effects of oseltamivir are nausea and vomiting.These events are usually mild to moderate, occur during the first 1 to 2 days of treatment, and can be lessened by taking the drug with food. Bronchitis, insomnia, and vertigo may also occur. Oseltamivir may not be indicated for use in certain individuals. Its efficacy in patients with chronic cardiac or respiratory disease has not been established. In clinical trials, no difference in the incidence of complications was seen between treatment and control groups. The efficacy of oseltamivir has not been demonstrated in immunocompromised patients, patients who begin treatment after 40 hours of symptoms, or patients given repeated prophylactic courses of therapy. Dosage adjustment is recommended for individuals with renal insufficiency; the drug’s safety in patients with hepatic insufficiency is unknown.

오셀타미비르 준비 용품 및 원자재

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오셀타미비르 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Henan Tengmao Chemical Technology Co. LTD	+8615238638457	salesvip2@hntmhg.com	China	415	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	994	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1811	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9352	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Nanjing Dolon Biotechnology Co.,Ltd.	18905173768	sales@dolonchem.com	CHINA	2972	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
Casorganics US Corp	+17326109938	sales@casorganics.com	CHINA	174	58
Shanghai Yingrui Biopharma Co.,Ltd	21-33585366	export01@shyrchem.com	CHINA	1320	58

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