Oseltamivir (oseltamivir, oseltamivir ) is a medicine for treating influenza .
| Oseltamivir | |
|---|---|
 | |
 | |
| Chemical compound | |
| IUPAC | ethyl (3R, 4R, 5S) -5-amino-4-acetamido-3- (pentan-3-yloxy) -cyclohex-1-ene-1-carboxylate |
| Gross formula | C 16 H 28 N 2 O 4 |
| Molar mass | 312.4 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| ATX | |
| Pharmacokinetics | |
| Bioavailable | 75% |
| Metabolism | in the liver |
| The half-life. | 6-10 hours |
| Excretion | the kidneys |
| Dosage Forms | |
| capsules and powder for suspension | |
| Route of administration | |
| orally | |
| Other names | |
| Tamiflu, Tamiflu, Nomides | |
Oseltamivir is an antiviral agent , belongs to the group of neuraminidase inhibitors , blocks the replication of influenza viruses type A and B.
In Russia, it is known under the brand name Tamiflu . In Belarus, it is produced under the trademark Flustop [1] .
Received approval from the FDA in 1999 [2] , later the FDA described the effectiveness of the drug as a whole, as "modest" [3] .
Content
Performance and Safety Information
Performance Evaluation
According to the World Health Organization and the United States Centers for Disease Control ( CDC ), published in the fall of 2009, test results for influenza A / H1N1 viruses (California / 04/2009) from patients in Mexico and the United States showed that new viruses are sensitive to neuraminidase inhibitors (oseltamivir and zanamivir ), but resistant to another class - adamantanes ( amantadine , rimantadine ) [4] [5] [6] .
On the official website of the drug Tamiflu [7] it is reported that the effectiveness of the drug in the treatment of influenza in patients with chronic heart and / or respiratory diseases has not been established.
Studies published by 2009 show that oseltamivir reduces the duration of symptoms in healthy patients by an average of 0.5 days, and by 0.74 days in patients at risk if treatment is started in the first hours after contact with the patient [8] .
There is no reliable information about whether taking oseltamivir affects the frequency of complications, for example, the risk of hospitalization or pneumonia [9] .
In December 2010, the World Health Organization reported 314 samples of H1N1 influenza that were common in 2009, resistant to oseltamivir [10] .
Among circulating influenza viruses, strains resistant to oseltamivir were identified, including in people not treated with this drug [11] .
Possible side effects
- Nausea , vomiting , insomnia , dizziness , diarrhea , lethargy, headaches , sore throat , cough , abdominal pain [12] . Also, the use of oseltamivir was associated with renal and psychiatric events [3] .
- The data of post-marketing studies of the drug in 2006 (mainly obtained in Japan) indicate a high risk, especially in children, of the development of impaired consciousness ( psychotic reactions , delirium ). In this regard, the US Food and Drug Administration ( FDA ) and the drug manufacturing company ( Roche Laboratories, Inc. ) informed health workers about changes to the drug annotation [13] .
Criticism
In 2006 [14] and 2014 [15] [16] , mass purchases of the drug by individual countries were criticized, in particular, those made in 2005 (“bird flu” H5N1) by Britain, Canada, Israel, the USA, and Australia. Several billion dollars were spent on purchases.
Since 2009, Cochrane Collaboration has attempted to obtain complete clinical trial protocols from Roche (the manufacturer of oseltamivir) [17] [18] [19] [20] . In 2014, the Acute Respiratory Infections Group of collaboration published a meta-review [21] [22] [23] , which concluded that oseltamivir and zanamivir had a small effect in reducing the duration of flu-like symptoms in adults, and noted a decrease in the risk of cold use. The use of oseltamivir increases the chances of side effects in adults and children. It was also noted that the mechanism of specific interaction with the influenza virus suggested by manufacturers is not confirmed by clinical studies [24] .
Cochrane publications disagreed with Tamiflu manufacturer Roche [25] .
Patent
Patents covering the invention of oseltamivir belong to the biopharmaceutical company of California, Gilead Sciences (for example, US patent No. 5763483 [26] was filed in 1996 and is valid until 2016). Gilead transferred the rights to further development and production of the drug to Roche in 1996 [27] .
Notes
- ↑ Flustop - Academpharm
- ↑ Drug Approval Package . Tamiflu (Oseltamivir Phosphate) Capsule FDA - "Approval Date: 10/27/1999." Date of treatment February 6, 2016.
- ↑ 1 2 Jefferson T. Neuraminidase inhibitors for preventing and treating influenza in adults and children : [trans. from English ] / Jefferson T, Jones MA, Doshi P ... [et al. ] // Cochrane Database of Systematic Reviews . - 2014 .-- No. April 4 (April 10). - DOI : 10.1002 / 14651858.CD008965.pub4 .
- ↑ WHO | Use of antiviral drugs against influenza A (H1N1)
- ↑ CDC H1N1 Flu | Questions and Answers: Antiviral Drugs, 2009—2010 Flu Season
- ↑ CDC - Seasonal Influenza (Flu) - Weekly Report: Influenza Summary Update
- ↑ Tamiflu Influenza Treatment Information for Healthcare Professionals - Limitations of Populations Studied / Genentech (Roche)
- ↑ Burch J. , Corbett M. , Stock C. , Nicholson K. , Elliot AJ , Duffy S. , Westwood M. , Palmer S. , Stewart L. Prescription of anti-influenza drugs for healthy adults: a systematic review and meta -analysis. (English) // The Lancet. Infectious diseases. - 2009. - Vol. 9, no. 9 . - P. 537-545. - DOI : 10.1016 / S1473-3099 (09) 70199-9 . - PMID 19665930 .
- ↑ Ebell MH , Call M. , Shinholser J. Effectiveness of oseltamivir in adults: a meta-analysis of published and unpublished clinical trials. (English) // Family practice. - 2013 .-- Vol. 30, no. 2 . - P. 125-133. - DOI : 10.1093 / fampra / cms059 . - PMID 22997224 .
- ↑ Update on oseltamivir resistance to influenza H1N1 (2009) viruses . World Health Organization (WHO) (December 15, 2010). Date of treatment December 30, 2010. Archived March 4, 2012.
- ↑ Antiviral Agents for the Treatment and Chemoprophylaxis of Influenza : Recommendations of the Advisory Committee on Immunization Practices: Recommendations and Reports: [ eng. ] : pdf / Prepared by Anthony E. Fiore (MD), Alicia Fry (MD), David Shay (MD), Larisa Gubareva (PhD), Joseph S. Bresee (MD), Timothy M. Uyeki (MD), Influenza Division , National Center for Immunization and Respiratory Diseases. - Morbidity and Mortality Weekly Report. - Centers for Disease Control and Prevention , 2011. - Vol. 60, No. 1 (21 January). - P. 6−7. - ISSN 1546-0738 .
- ↑ Medicines: 5000 names of medicines and their forms: Reference book / Ed. M.A. Klyueva. - Ed. 13th - M .: ICTC “Lada”, 2008. - S. 373. - 637 p. - 1000 copies. - ISBN 978-5-94832-271-1 .
- ↑ Tamiflu - making changes to the annotation to the drug . Antibiotics and antimicrobial therapy . Research Institute of Antimicrobial Chemotherapy (NIIAH), Smolensk State Medical University, Ministry of Health of the Russian Federation (December 25, 2006). - "Tamiflu May Be Linked to Risk for Self-Injury and Delirium." Date of treatment February 17, 2019.
- ↑ Jefferson TO , Demicheli V. , Di Pietrantonj C. , Jones M. , Rivetti D. Neuraminidase inhibitors for preventing and treating influenza in healthy adults. (Eng.) // The Cochrane database of systematic reviews. - 2006. - No. 3 . - P. 001265. - DOI : 10.1002 / 14651858.CD001265.pub2 . - PMID 16855962 .
- ↑ Butler D. Tamiflu report comes under fire. (Eng.) // Nature. - 2014 .-- Vol. 508, no. 7497 . - P. 439-440. - DOI : 10.1038 / 508439a . - PMID 24759392 .
- ↑ Spending on Tamiflu Flu Remedy is a “Waste” , BBC Russian Service (April 10, 2014). Date of treatment February 6, 2016.
- ↑ Kate Kelland. Researchers, regulators and Roche row over stockpiled drug Tamiflu . Reuters (April 9, 2014). Date of treatment February 6, 2016.
- ↑ Oliver Staley. Flu Drugs May Do More Harm Than Good, Researchers Find . Bloomberg (April 10, 2014). Date of treatment February 17, 2019.
- ↑ Jefferson T. , Doshi P. Multisystem failure: the story of anti-influenza drugs. (English) // BMJ (Clinical research ed.). - 2014 .-- Vol. 348. - P. 2263. - DOI : 10.1136 / bmj.g2263 . - PMID 24721793 .
- ↑ Jefferson T. , Jones M. , Doshi P. , Spencer EA , Onakpoya I. , Heneghan CJ Oseltamivir for influenza in adults and children: systematic review of clinical study reports and summary of regulatory comments. (English) // BMJ (Clinical research ed.). - 2014 .-- Vol. 348. - P. 2545. - DOI : 10.1136 / bmj.g2545 . - PMID 24811411 .
- ↑ Regulatory information on trials of oseltamivir (Tamiflu) and zanamivir (Relenza) for influenza in adults and children , Cochrane, April 10, 2014
- ↑ UPDATED: Cochrane study: Stockpiling Tamiflu, Relenza was $ 2B 'thrown down the drain' // fiercepharma, April 10, 2014
- ↑ “Tamiflu” proved to be toxic to “big farm” . Home Baby (2014). - log. Date of treatment February 17, 2019.
- ↑ Jefferson T. Neuraminidase inhibitors for preventing and treating influenza in adults and children : [trans. from English ] / Jefferson T, Jones MA, Doshi P ... [ et al. ] // Cochrane Database of Systematic Reviews. - 2014 .-- No. April 4 (April 10). - DOI : 10.1002 / 14651858.CD008965.pub4 .
- ↑ Roche disagrees with criticism of Tamiflu , Russian BBC Service (April 23, 2014). Date of treatment February 6, 2016.
- ↑ Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, Matthew A. Williams. Carbocyclic compounds . US 5763483 A (English) . Date of treatment February 6, 2016.
- ↑ Avian Flu Drugs: Patent Questions . World Intellectual Property Organization (April 2006). - “A quick search of patent databases shows that the patents covering the invention of oseltamivir are owned by the California-based biopharmaceutical company, Gilead Sciences. (See eg US patent no 5763483, for a "novel carbocyclic compound", filed in 1996 and in force in principle until at least 2016.) Rather than further develop and manufacture the drug within the company, Gilead opted in 1996 to license to Roche certain of the exclusive rights conferred by the patents. ”. Date of treatment February 6, 2016.
Links
- Oseltamivir (English) . Drugs.com . Date of treatment February 6, 2016.
- Tamiflu (oseltamivir phosphate) Information . FDA Date of treatment February 6, 2016.
- Oseltamivir (Oseltamyvir) . Encyclopedia of medicines and pharmaceutical products . Radar Patent. - Instruction, application and formula.