Английская Википедия:Fosamprenavir

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Fosamprenavir (FPV), sold under the brand names Lexiva and Telzir, is a medication used to treat HIV/AIDS.[1][2] It is a prodrug of the protease inhibitor and antiretroviral drug amprenavir.[3] It is marketed by ViiV Healthcare as the calcium salt.[1][2]

Fosamprenavir was approved for medical use in the United States in October 2003,[4] and in the European Union in July 2004.[2] The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient.[1]

A head-to-head study with lopinavir showed the two drugs to have comparable potency, but patients on fosamprenavir tended to have a higher serum cholesterol.[5]

Medical uses

Fosamprenavir is used for the treatment of HIV-1 infections, typically but not necessarily in combination with low-dose ritonavir or other antiviral drugs.[6][7]

Adverse effects

The most common adverse effect is diarrhea. Other common side effects include headache, dizziness and exanthema, which is usually transient. Severe allergic reactions (Stevens–Johnson syndrome) are rare.[6]

Interactions

Amprenavir (the active metabolite of fosamrenavir, which is found in blood plasma, liver and other organs) is metabolized via the liver enzyme CYP3A4 and also weakly inhibits this enzyme. This means that combination with drugs that are also metabolized by CYP3A4 can increase their plasma concentrations and thus side effects; and combination with drugs that inhibit CYP3A4 can increase amprenavir concentrations.[6]

When combining fosamprenavir with low doses of the CYP3A4 inhibitor ritonavir, this interaction is intended as it allows for application of lower fosamprenavir doses.[6]

Pharmacology

Fosamprenavir is quickly activated to amprenavir, even before it reaches the circulation. Amprenavir is a HIV protease inhibitor.[6]

Файл:3nu3 478.png
HIV-1 protease dimer with amprenavir (sticks) bound in the active site. PDB entry Шаблон:PDBe[8]

References

Шаблон:Reflist

External links

Шаблон:Antiretroviral drug Шаблон:Portal bar

  1. 1,0 1,1 1,2 Ошибка цитирования Неверный тег <ref>; для сносок Lexiva FDA label не указан текст
  2. 2,0 2,1 2,2 Ошибка цитирования Неверный тег <ref>; для сносок Telzir EPAR не указан текст
  3. Шаблон:Cite web
  4. Шаблон:Cite web
  5. Шаблон:Cite journal
  6. 6,0 6,1 6,2 6,3 6,4 Шаблон:Cite book
  7. Шаблон:Cite report
  8. Шаблон:Cite journal