pharmacology notes

Apr 16th, 2015
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ANTIRETROVIRALSNONNUCLEOSIDE REVERSE TRANCRIPTASEINHIBITORS(NNRTIs)BYTOBIAS OMONDIMBchB IVUEEXAMPLES1. Efavirenz2. Nevirapine3. Delavirdine4. Etravirine: Is the newest NNRTI approved for treatmentof experienced HIV patients May be effective against HIV strains resistantto other drugs in this groupMODE OF ACTIONThey inhibit HIV-reverse transcriptase by binding at asite remote from the active site(this site is differentfrom the binding site of NRTIs)They produce conformational change in theenzyme that prevents substrate bindingNNRTIs do not require phosphorylation to beactive and do not compete with nucleosidetriphosphatesThere is no cross-resistance with NRTIsRESISTANCEResistance emerges rapidly by single pointgene mutations(mutations occur in the polgene, and is rapid if these agents are used asmonotherapy)PHARMACOKINETICSEFAVIRENZ:Oral absorption is less goodFatty foods may enhance its oralbioavailabilityCan be given once daily because of its longhalf life of two daysEFV is metabolized by hepatic cytochromeP450PharmacokineticsNEVIRAPINE:Oral absorption is very good with good oralbioavailabilityPenetrates most tissues including the CNSHas a half life of more than 24hoursMetabolized by the hepatic cytochrome P450cyp3A4 isoformUsed in combination regimensIs effective in prevention of vertical HIVtransmission when given as a single dose tomothers at the ons

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