pharmacology notes

Apr 16th, 2015
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OTHER ANTI-HIV/AIDSaggieFUSION INHIBITORSAka Entry inhibitorsInclude:EnfluvirtideMaravirocENFLUVIRTIDEFuzeonFormely called T-20Available formulation: P/E90mg/ml for injection-binds to gp41 and interferes with its ability to approx. the twomembranes.Enfuvirtide is a 36-amino-acid peptide that binds to gp41,preventing the conformational change.Enfuvirtide, in combination with other antiretrovirals, is approved fortherapy of treatment-experienced patients with evidence of viralreplication despite ongoing antiretroviral drug therapy.As a peptide, it must be given subcutaneously.Most of the adverse effects are related to the injection i.e pain,erythema, induration, and nodules, which occur in almost all patients.However, only 3 percent discontinue treatment because of them.Enfuvirtide must be reconstituted prior to administration.It is an expensive medication.92% plasma protein boundMetabolism: proteolytic hydrolysis?Elimination t1/2 : 3.8 hrPeak conc. 8 hrsMARAVIROC [MA-RA-VI-ROC]Selzentry/ CelsentriOften ref to as a chemokine receptor antagonist-binds to CCR5 preventing an interaction with gp120it is well absorbed orally therefore formulated as an oral tablet.Maraviroc blocks the CCR5 coreceptor that works together with gp41to facilitate HIV entry through the membrane into the cell.HIV may express either the CCR5 coreceptor or the CXCR4coreceptor, or both.A test to determine tropism is required to distinguish the CCR

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