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IOS 11 Exam 4

Drug Interactions

QuestionAnswer
Nucleoside reverse trasncriptase inhibitors excretion Renal excretion and do not participate in drug interactions involving the liver
Efuvirtide excretion Cleared by peptide catabolism and amino-acid recycling, drug interactions are not expected
Non nucleoside reverse transcriptase metabolism Extensive hepatic metabolism
Protease inhibitors metabolism Extensive hepatic metabolism
3A4 inhibition is caused by Ritonavir>Delaviridine>Nelfivavir>Indinavir>amprenavir?saquinavir
3A4 enzyme induction Lopinavir/r > Tipranavir/r = Darunavir/r > Nelfinavir =Indinavir=Delaviridine=Atazanavir
Therapeutic failure is Viral load increases and the CD4 count declines. Resistance can occur to drug and class
Pharmacodynamic activity maybe Additive, Antagonastic,Synergistic
Ritonavir is a potent inhibitor of 3A4 and P-gP in the intestanal tract and Liver
Boosting dose of Ritonavir is 100-200mg
Benefit of Indinivar/Ritonavir Indinivar no longer has to be given on empty stomach
Efavirenz is an inducer and Kaletra (lopinavir/ritonavir) an inhibitor what happens Efavirenz induces the metabolism of lopinavir AUC 40%. If give this combination take 3 tablets BID of Kaletra rather than 2BID=PK interaction. This occurs with many protease inhibitors and Efavarinz in a lot of the cases boost with 100mg of ritonavir PK
Tenofovir and Atazanavir interaction MOA Do not known but Boost with Ritononavir
Fos-Amprinavir and Lopinavir Both induce the metabolism of the other and boosting does not help. Do not use together PK
Tipranavir and other Protease inhibitors Saquanavir,Amprinavir,lopinavir should not be used Tipranavir induces PK
Zidovudine and Stavudine Thymidine analogs should not be used together-antagonism PD
Didanosine and tenofovir Should not be used together they are adenosine analogs antagonism=PD also a Didanosine AUC is increased 48-64% so there is also a PK interaction if patient is >60Kg 250mg and 200mg if <60kg
Atazanavir + Rifampin Decreased concentration of Atazanavir boosting does not work- PK
Efavarinz +Rifampin AUC of Efavarinz is decreased 25% so increase does to 800mg monitor level in 2-4 weeks PK
Rifabutin + Ritonavir boosted Decrease Rifabutin to 150mg 2-3 times a week PK
Efavarinz +Rifabutin Remember Efavarinz is an inducer so must increase Rifabutin 450-600mgday
Bactrium(cotrimoxazole) +zidovudine Overlapping bone marrow suppression=PD Monitor WBC
Didanosine +Ribavarin Coadministration is not recommended due to pancretitis and lactic acidosis-PD
Ribavarin increases levels of DDAPT so when there is an accumulation This can increase pancrititis and lactic acidosis
Atazanavir +omeprazole Atazanavir is acid dependant for absorption and cannot be taken with a PPI can use H2 blocker is space 10 hours then 2 or take boosted with ritonavir and H2- PK
Tipranavir and PPI or H2 Not recommended PK
INdinavir and PPI There is a decrease in AUC must take with booster of Ritonavir
Lopinavir/ritonavir + Simvastatin or Lovastatin They are contraindicated since high AUC- Choose Pravstatin or FLuvastatin- PK
Ritonavir + Sidenafi Decrease Sildenafil to 25mg q48 hr PK
Ritonavir +Vardinafil Vardinafil must be decreased to 2.5mg q72 hrs-PK
Ritonavir + Tadalafil Tadalafil must be decreased to 10 mg q 72 hr-PK
Atazanavir + oral contraceptives Increases the oral contraceptions concentrationIndinavir + Oral Contraceptive NC
Lopinavir/ritonavir + Phenytoin Both drugs induce each other monitor drug levels-PK
St. Johns Worts + Protease inhibitor Do not use Higly decrease protease concentration- PK
Secondary Adrenal Suppression Weight gain, fatigue- Cushings this occurs from steroids- Protease inhibitors increase concentration so must monitor when give even an inhaled steroid- PD
Protease Inhibitors have increased rates of Glucose and lipid abnormalities
Efavirenz is contraindicated in Pregnancy
Pregant women should avoid Efavarinz, Zalcitabine, Delaviridine
Need dose adjustment for renal dysfunction emtricitabine, lamivudine,zidovidine,didanosine,tenovir,stavudine,abacavir
Treat HIV and HBV Lamivudine,Tenofovir,emtricitabine Travuda=emtricitabine+tenofovir
Cytosine analogs are Zalcitibine,emtricitabine,lamivudine
Thymidine analogs are Stavudine, zidovudine
Adenosine analogs are Didanosine and Tenofovir
Guanosine analogs are Abacavir
Created by: liza001
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