Showing posts with label Biomedicine-pro. Show all posts
Showing posts with label Biomedicine-pro. Show all posts

Tuesday, June 5, 2012

Clinical Efficacy of Nevirapine


Nevirapine, also marketed under the trade name Viramune (Boehringer Ingelheim), is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS. As with other antiretroviral drugs, HIV rapidly develops resistance if nevirapine is used alone, so recommended therapy consists of combinations of three or more antiretrovirals.

Nevirapine in triple combination therapy has been shown to suppress viral load effectively when used as initial antiretroviral therapy (i.e., in antiretroviral-naive patients). Some clinical trials have demonstrated comparable HIV suppression with nevirapine-based regimens to that achieved with protease inhibitors (PIs) or efavirenz. Although concerns have been raised about nevirapine-based regimens in those starting therapy with high viral load or low CD4 count, some analyses suggest that nevirapine may be effective in these patients.

Nevirapine may also form a useful component of salvage regimens after virological failure, usually in combination with one or more PIs as well as nRTIs, especially in those who have not previously taken an NNRTI.

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Ritonavir's Method of Action

Ritonavir, with trade name Norvir (Abbott Laboratories), is an antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS.

Ritonavir is frequently prescribed with HAART, not for its antiviral action, but as it inhibits the same host enzyme that metabolizes other protease inhibitors. This inhibition leads to higher plasma concentrations of these latter drugs, allowing the clinician to lower their dose and frequency and improving their clinical efficacy.

Ritonavir was originally developed as an inhibitor of HIV protease. It is one of the most complex inhibitors. It is now rarely used for its own antiviral activity, but remains widely used as a booster of other protease inhibitors. More specifically, ritonavir is used to inhibit a particular liver enzyme that normally metabolizes protease inhibitors, cytochrome P450-3A4 (CYP3A4). The drug's molecular structure inhibits CYP3A4, so a low dose can be used to enhance other protease inhibitors. This discovery, which has drastically reduced the adverse effects and improved the efficacy of PI's and HAART, was first communicated in an article published in the AIDS Journal in 1997 by the University of Liverpool. This effect does come with a price: it also affects the efficacy of numerous other medications, making it difficult to know how to administer them concurrently. In addition it can cause a large number of side-effects on its own.

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Sunday, June 3, 2012

Saquinavir's Mode of Action

Saquinavir







Saquinavir is an antiretroviral drug used in HIV therapy. It falls in the protease inhibitor class. Two formulations have been marketed:
  • a hard-gel capsule formulation of the mesylate, with trade name Invirase, which requires combination with ritonavir to increase the saquinavir bioavailability;
  • a soft-gel capsule formulation of saquinavir, with trade name Fortovase.
Both formulations are generally used as a component of highly active antiretroviral therapy (HAART).
 
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell. Saquinavir inhibits both HIV-1 and HIV-2 proteases.

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Wednesday, May 30, 2012

Side Effects of Saquinavir Mesylate



Item name: Saquinavir Mesylate
CAS: 149845-06-7
Molecular Formula: C39H54N6O8S
Formula Weight: 766.95g/mol
Description: Saquinavir mesylate (SQV) is a commonly prescribed protease inhibitor that is recommended to be boosted with a subtherapeutic dose of RTV.

Check with your doctor if any of these most common side effects persist or become bothersome when using Saquinavir Mesylate:
Anxiety; blurred vision; body fat changes; changes in sexual desire; constipation; diarrhea; dizziness; dry lips or skin; gas; headache; heartburn; mouth sores; nausea; night sweats; sleeplessness; stomach discomfort; taste changes; tenderness or bleeding of the gums; tiredness; vomiting; warts; weight gain
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Tuesday, May 29, 2012

The History of Stavudine

Stavudine







Stavudine (2'-3'-didehydro-2'-3'-dideoxythymidine, d4T, brand name Zerit) is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV. Stavudine is used in combination with other medicines for the treatment of human immunodeficiency virus (HIV) infection.

Stavudine was first synthetized in the sixties by Jerome Horwitz. It was subsequently reconsidered as an anti-HIV agent by the Rega Institute for Medical Research in Belgium. Stavudine was approved by the U.S. Food and Drug Administration (FDA) on June 24, 1994 for adults and on September 6, 1996 for pediatric use and again as an extended-release version for once-a-day dosing in 2001. The fourth antiretroviral drug on the market, its patent expired in the United States on 2008-06-25.

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Friday, May 25, 2012

Something About Valacyclovir Hydrochloride

Valacyclovir Hydrochloride






Item name:Valacyclovir Hydrochloride
CAS:124832-27-5
Molecular Formula:C13H21ClN6O4
Formula Weight:360.8g/mol

Valaciclovir (INN) or valacyclovir (USAN) is an antiviral drug used in the management of herpes simplex, herpes zoster (shingles), and herpes B. It is a prodrug, being converted in vivo to aciclovir. It is marketed by GlaxoSmithKline under the trade names Valtrex and Zelitrex. As of November 25, 2009 (2009 -11-25)[update], valacyclovir is marketed in generic form in the United States by Ranbaxy Laboratories.

Valtrex is offered in 500 mg and 1 gram tablets, the active ingredient being valacyclovir hydrochloride, with the inactive ingredients carnauba wax, colloidal silicon dioxide, crospovidone, FD&C Blue No. 2 Lake, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, povidone, and titanium dioxide.

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