Pharmacology Chapter 49 - Antivirals

8/10/2019 Pharmacology Chapter 49 - Antivirals

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Pharmacology Chapter 49: Antivirals Page % of 4

o pancreatitis, especially with stavudine, zalcitabine, ribavirin, hydro0yureao neuropathy with stavudine, isoniazid, vincristine, ribavirino hyperuricemia1 levels o ddI may increase with allopurinol1 increased /I risk emtricita&ine ! "orinated analog of TC (ith high &ioavaila&ility and half#lifeo I in children, pregnancy, renal#hepatic ailure, metronidazole, or disulframo given (ith tenofovir$ helps prevent ac"isition of H'V also. also (ith efaviren6o avoid conc"rrent "se (ith TCo hyperpigmentation of palms and soles$ especially in AA

o 51D4V resistance$ also (ith TC lamiv"dine TCB ! cytosine analog often "sed (ith AT and stav"dine d4TB or a&aciviro 51D4V resistance$ same as emtricita&ineo good bioavailability, increases with T/&6"/7o avoid with zalcitabine, inhibit each others phosphorylation stav"dine d4TB ! thymidine analog (ith e-cellent &ioavaila&ilityo ne"ropathy$ increased (ith dd'$ 6alcita&ine$ vincristine$ isonia6id$ or ri&avirino increased acidosis or hepatic steatosis1 pancreatitis, arthralgia, 2 *"T#*To avoid with ddI and *$T tenofovir ! acyclic n"cleoside phosphonate analog of adenosineo only requires two phosphorylations1 inhibits reverse transcriptase and chain terminationo EF=7 m"tationo combination with emtricitabine or eavirenzo osteomalacia$ calci"m and phosphate loss$ pro-imal renal t"&"lar to-icity 6alcita&ine ddCB ! cytosine analog (ith high &ioavaila&ility. avoid (ith food and antacidso ne"ropathy$ avoid other dr"gs. pancreatitiso

oral and esophageal ulcerationo avoid with 4T 6idov"dine ATB ! deo-ythymidine analog (ith good &ioavaila&ility and CS penetrationo renal e-cretion$ gl"c"ronidated in the livero administered typically with 4T and abacaviro reduces vertical transmission 38495o decreases !IV6associated dementia and thrombocytopeniao myelosuppression with macrocytic anemia and neutropenia. increases (ith ganciclovir$ ri&avirino avoid with stavudine pregnancyo +7T's ! TC or AT. a&acavir$ dd'$ emtricita&ine$ stav"dineo ++7T' ! nevirapineo P's ! lopinavir8ritonavir. ata6anavir8ritonavir$ indinavir8ritonavir$ nel0navir$ ritonavir$ sa"inavir

nonnucleoside reverse transcriptase inhibitors (NNRTIs) &ind directly to reverse transcriptase res"lting in allosteric inhi&ition of 7+A and *+A#dependent *+A polymerase do not compete with nucleoside triphosphates nor require phosphorylation to be active no cross#resistance &et(een +7T's and ++7T's E1?+ and G1D1C confer resistance across all ++7T's :I intolerance, rash 3";"5, ? metabolism 3


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Pharmacology Chapter 49: Antivirals Page of 4

o avoid (ith proton#p"mp inhi&itors and other acid#red"cing agentso n8v8d$ headache$ ne"ropathy$ hyper&ilir"&inemia and Ia"ndice dar"navir ! must be co6administered with ritonaviro @ liver and pancreatic en6ymes$ hepatitiso a s"lfa dr"g$ avoid in allergy fosamprenavir ! prodr"g of amprenavir "ndergoing hydrolysis in intestinal epitheli"mo mostly administered (ith ritonaviro red"ced levels (ith high fat meals

o SJS$ n8v8d$ perioral paresthesiao C' in children$ pregnancy$ renal or hepatic fail"re$ metronida6ole$ or dis"l0ramo avoid supplemental vitamin Do give at diAerent times than ritonavir indinavir ! re"ires acidic environment$ typically re"ires empty stomacho hyper&ilir"&inemia$ nephrolithiasis (ater m"st &e ingested to avoidBo hemolytic anemia, thrombocytopenia, insomnia, n#v#d lopinavir ! only with ritonavir, reduced pill burden with good complianceo ritonavir inhi&its A4$ (hich increases lopinavir half#lifeo I with riampin, metronidazole, disulfram nel0navir ! diarrhea and at"lence ritonavir ! high &ioavaila&ility active form after meta&olism via A4 and %*Fo potent A4 inhi&itor and th"s increases half#life of other P's$ (hich is goodo saquinavir and ritonavir increase CT and &B sa"inavir ! enhanced a&sorption (ith fatty meal tipranavir ! high#fat meal increases &ioavaila&ilityo

avoid in head trauma or intracranial bleed, avoid combination with ritonaviro statin levels are increased causing rhabdomyolysis and myopathyo sula

entry inhibitors enf"virtide ! s"&c"taneo"s inIection$ &inds to and inhi&its gp41 action maraviroc ! &inds to CC7=$ "sed for 7=#tropic H'V#1 patientso I in end6stage renal diseaseo resistance due to mutation o gpE8? V4 loopo meta&oli6ed via A4: m"st increase (ith ind"cers and decrease (ith inhi&itors

integrase strand transfer inhibitor raltegravir ! pyrimidinone analog that &loc,s integrase preventing integration into host genomeo no CGP interaction$ ho(ever$ sho"ld &e increased if given (ith rifampino avoid with antacids, metals will bindo increased F, rhabdomyolysis, myopathy

Anti#hepatitis Agents interferon#K ! inhi&ition of viral penetration$ translation$ transcription$ processing$ mat"ration$ and release.

increased 5HC e-pression$ increased phagocytosiso s"&c"taneo"s or '5 inIection. pegylated given SL onlyo pegylation increases hal6lie and slower clearanceo Gu6like symptoms, increased HTs, alopecia, myelosuppression, autoimmune e0acerbationo I in autoimmune, cardiac disease, hepatic and renal insuciency

HBV treatment goal is viral s"ppression +7T's ! TC$ adefovir dipivo-il$ tenofovir$ entecavir$ tel&iv"dine$ '+#Ko ac"te e-acer&ation of H


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o increased availa&ility (ith high#fat mealso I in anemia, BH, vascular disease, and pregnancy, mutagenic

Anti#'n"en6a Agents classi0cation via core protein A$

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Pharmacology Chapter 49 - Antivirals