Pharmacology of Antiretroviral Agents An Emphasis on Drug ...

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Integrase Inhibitors• Raltegravir: few drug interactions• Metabolized via UGT1A1 mediated glucuronidation• Rifampin: strong inducer <strong>of</strong> UGT1A1• Avoid combination• PB & Phenytoin also induce this pathway• Elvitegravir• Metabolism: CYP3A4 substrate (combined with cobicistatpharmacoenhancerfor activity)• Single tablet regimen cannot be used in renal failure
Pharmacoenhancers• Cobicistat• CYP3A4 inhibitor devoid <strong>of</strong> antiretroviral activity• Combination with other ARVs as booster• Potential for interactions (similar to PIs)• Only affects CYP3A4 (not others)• Decreases tubular secretion <strong>of</strong> creatinine
Page 1 and 2: PHARMACOLOGY OFANTIRETROVIRAL AGENT
Page 3 and 4: Introduction- Patient Case• SY is
Page 5 and 6: 1. Centers for Disease Control and
Page 7 and 8: 3. Luther VP, Wilken AL. HIV Infect
Page 9 and 10: Incident cases in 2009 approx 48,00
Page 11 and 12: ANTIRETROVIRALTHERAPYPharma
Page 13 and 14: 7. Pomerantz RJ and Horn DL. 20 Yea
Page 15 and 16: Step 1: Binding & Attachment9. AIDS
Page 17 and 18: Enfuvirtide- Mechanism of</
Page 19 and 20: NRTI Mechanism of
Page 21 and 22: Integration12. Pommier Y, Johnson A
Page 23 and 24: Protease Inhibitors11. Brunton, L.
Page 25 and 26: When to Start ART in Older Adults
Page 27 and 28: OLDER ADULTSPharmacokineticsAdverse
Page 29 and 30: Drug MetabolismCytochrome P450 Enzy
Page 31 and 32: P-glycoprotein• Efflux transporte
Page 33 and 34: Risk Factors for Drug Interactions
Page 39 and 40: 19. Marzolini C, Back D, Weber R, e
Page 45 and 46: 21. Rastegar DA, Knight AM, and Mon
Page 47 and 48: RECOGNIZINGPREVENTABLE ADVERSEEVENT
Page 49 and 50: Preventable Adverse Events:CCR5 Inh
Page 51: Preventable Adverse EventsNNRTIs•
Page 55 and 56: Drug Interactions Involving Proteas
Page 57 and 58: Pharmacokinetic Interactions withPr
Page 59 and 60: HMG-CoA Reductase Inhibitors andPro
Page 61 and 62: Lipid-Lowering Agents</stro
Page 63 and 64: Neuropsychiatric• An</str
Page 65 and 66: Other P450 interactions•
Page 67 and 68: PREVENTING DRUGINTERACTIONS
Page 69 and 70: Back to our patient case…• SY i
Page 71 and 72: Patient Case• Drug Interactions
Page 73 and 74: References1. Centers for Disease Co

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