CCR5, Fusion, Integrase Inhibitors - Anti - HIV

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Enfuvirtide (Fuzeon ®)

Fusion protein inhibitor.
Dosing (Adults): 90 mg SQ twice daily. (Administer subcutaneously into upper arm, abdomen, or anterior thigh.)

Supplied: Injection (powder for reconstitution): 108 mg (90 mg/ml following reconstitution).

maraviroc (Selzentry™)
INDICATIONS AND USAGE:   SELZENTRY™ is a CCR5 co-receptor antagonist indicated for combination antiretroviral treatment of adults infected with only CCR5-tropic HIV-1detectable, who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents. Tropism and treatment history should guide the use of SELZENTRY.

MOA:  selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Blocking this interaction prevents CCR5-tropic HIV-1 entry into cells.

Recommended Dosing Regimen
Concomitant Medications SELZENTRY Dose
CYP3A inhibitors (with or without a CYP3A inducer)including:
  • protease inhibitors (except tipranavir/ritonavir)
  • delavirdine
  • ketoconazole, itraconazole, clarithromycin,
  • other strong CYP3A inhibitors (e.g., nefazadone, telithromycin)
 150 mg twice daily
Other concomitant medications, including tipranavir/ritonavir, nevirapine, all NRTIs and enfuvirtide 300 mg twice daily
CYP3A inducers (without a strong CYP3A inhibitor) including:
  • efavirenz
  • rifampin
  • carbamazepine, phenobarbital, and phenytoin
 600 mg twice daily

Supplied: 
Tablets: 150 mg and 300 mg

raltegravir (Isentress ®)
INDICATIONS AND USAGE: 
ISENTRESS™ is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) indicated:
• In combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents
.
The safety and efficacy of ISENTRESS have not been established in treatment-naïve adult patients or pediatric patients

Dosing (Adults): 
400 mg administered orally, twice daily with or without food

Supplied: 
Tablets: 400 mg

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Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.

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