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OSELTAMIVIR

Description Indications Contraindications Dosage Interactions Mechanism of Action Pharmacodynamics Elimination Side Effects
OSELTAMIVIR
OSELTAMIVIR structure
CAS No.
196618-13-0
Chemical Name:
OSELTAMIVIR
Synonyms
TaMvir;TAMIFLU;GS 4104;GOP-A-Flu;OSELTAMIVIR;OSTELTAMIVIR;TaMiflu-Free;Oseltamivir (free base);(3R,5S)-ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate;(3R,4R,5S)-Ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
CBNumber:
CB1472402
Molecular Formula:
C16H28N2O4
Formula Weight:
312.4
MOL File:
196618-13-0.mol

OSELTAMIVIR Properties

pka
7.7 (25°); 6.6 (70°)
CAS DataBase Reference
196618-13-0

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OSELTAMIVIR price

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OSELTAMIVIR Chemical Properties,Uses,Production

Description

Oseltamivir is a drug that suppresses the action of influenza A, influenza B, and H1N1 influenza viruses in children and adults. Oseltamivir is administered for the treatment of influenza (flu) for people who are above the age of 2 weeks and have been experiencing flu-like symptoms for less than two days. Oseltamivir may also be prescribed for people who are above 1-year-old as a protective measure to prevent them from contracting influenza due to exposure to the virus without necessarily having indicated any symptoms of infection. The drug may not treat common cold. Oseltamivir goes by the brand name Tamiflu.

Indications

Oseltamivir is prescribed for the treatment of mild or severe illness that results from infection with influenza A or B virus for patients above the age of 2 weeks, and have been experiencing flu-like symptoms for less than 48 hours. The drug is also used for preventive treatment against influenza amongst adolescents above 13 years and adults.

Contraindications

Oseltamivir is contraindicated in patients who may be hypersensitive to the medication or any of the ingredients in its formulation.

Dosage

For best results, Oseltamivir should be administered orally at least within two days of the onset of symptoms or exposure to influenza. The recommended dosage for treatment in adults with influenza is 74mg taken twice per day for 5 days.
In children, the recommended dosage should be 30-75mg (for children between 15kg and 40kg) take twice per day for 5 days, where dosing also depends on the body weight of the patient. For children who are 2 weeks old but <1 year, 3mg/kg should be administered orally two times per day.
For flu prevention in adults, 75mg of Oseltamivir should be administered on a daily basis for 10 days, whereas in children, 30-75mg should be given once per day for 10 days.

Interactions

Drug interactions may influence the effectiveness of certain medications and may increase the risk of exposure to adverse side effects hence the need to consult a doctor with the list of other medications that one might be taking while getting a prescription for Oseltamivir.
A patient should notify their healthcare provider if they have received any nasal flu vaccines within 2 weeks before the administration of the first dose of Oseltamivir.
This drug may reduce protection against flu if the vaccine has been administered through the nose. One should wait for 2 weeks after the treatment with Oseltamivir before nasal administration of the flu vaccine.

Mechanism of Action

The drug is an ethyl ester prodrug that necessitates hydrolysis for modification into the radical form, Oseltamivir carboxylate. The suggested mechanism of action of the drug is suppression of the influenza virus neuraminidase, which increases the probability of modification of the virus molecule, amalgamation and release.
Oseltamivir inhibits the spread of the influenza virus by preventing the action of neuraminidase, the enzyme that allows the spread of the virus from infected cells to those that are not infected. Oseltamivir inhibits the intercellular proliferation of the virus hence the duration and symptoms associated with influenza are also reduced. The length of the presenting symptoms may be reduced by one and a half days if treatment is initiated within 2 days at the onset of the flu symptoms.

Pharmacodynamics

Oseltamivir is an antiviral medication, a neuraminidase suppressor that is used in prophylaxis and treatment of influenza A and B viruses. It is a prodrug that is prescribed as a phosphate, which is hydrolyzed hepatically into the radical metabolite, the unbound carboxylate of the drug (GS4071). Oseltamivir functions as a transitional analog suppressor of influenza neuraminidase.

Elimination

Upon primary absorption, >90% of Oseltamivir is eliminated by transformation into Oseltamivir carboxylate. The converted form of the drug does not undergo further metabolism, and it is excreted in urine. A significant portion, >99% of the Oseltamivir carboxylate is expelled from the body by renal excretion.

Side Effects

Common side effects associated with Oseltamivir include dizziness, headache, abdominal pain, bronchitis, diarrhea, vomiting, and nausea. Taking Oseltamivir after meals may help in reducing nausea. Other adverse side effects may include exacerbation of diabetes, behavioral disturbances, seizures, skin reactions, and allergic reactions.
A patient may need to seek emergency help if they are using Oseltamivir and they experience hallucinations, unusual behavior, shaking/tremors, and sudden confusion.
One should also consult their doctor if they are experiencing signs of an allergic reaction to the drug which may include hives, swelling in the throat or the face, difficulties in breathing, severe skin reactions such as a purple or red skin rash, sore throat, skin pain, peeling, burning eyes, and blistering.

Definition

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.

Antimicrobial activity

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

Acquired resistance

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%
Cmax 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

Treatment and prevention of susceptible influenza A (H3N2) and B infections in adults and young children

Side effects

Adverse events relate to the gastrointestinal tract; the most common is nausea with or without vomiting in 10% of patients. Food alleviates side effects.

OSELTAMIVIR Preparation Products And Raw materials

Raw materials

Preparation Products


OSELTAMIVIR Suppliers

Global( 84)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24196 60
Nanjing Dolon Biotechnology Co.,Ltd.
18905173768
sales@dolonchem.com CHINA 2972 58
Hubei Jusheng Technology Co.,Ltd.
86-188-71490254
peter@hubeijusheng.com CHINA 20095 58
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 141 58
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15884 69
JinYan Chemicals(ShangHai) Co.,Ltd. 13817811078,021-50426030
86-021-50426522,50426273 sales@jingyan-chemical.com China 10012 60
Jia Xing Isenchem Co.,Ltd 0573-85280080,18627885956
0573-85285100 isenchem@163.com,QQ:2446116053 China 9743 66
Chemfun Medical Technology(Shanghai) Co., Ltd. 021-67220633 & 021-37212706
+86-21-67220638 chemfun@chemfun.net China 21815 59
LGM Pharma 1-(800)-881-8210
615-250-9817 inquiries@lgmpharma.com United States 1943 70

196618-13-0(OSELTAMIVIR)Related Search:


  • TAMIFLU
  • OSELTAMIVIR
  • OSTELTAMIVIR
  • Ethyl (3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate
  • (3R,5S)-ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
  • Oseltamivir (free base)
  • ethyl (3R,4R,5S)-5-aMino-4-acetaMido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate
  • GOP-A-Flu
  • GS 4104
  • TaMiflu-Free
  • TaMvir
  • (3R,4R,5S)-Ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
  • -
  • 196618-13-0
  • C16H28N2O4
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