Anti-Retroviral Drugs

Front 1

Abacivir
major adverse effect?
Contra?

Back 1

*NRTI
-hypersensitivity reactions, skin rash (50%), elevated serum aminotransferase and CK (pts should be screened for HLA-B allele)
-cardiac risk factor (inc risk of Myocardial effects)

Front 2

Didanosine
phamacokinetic?
major adverse effect?
Contra?

Back 2

*NRTI
-lowest oral bioavailability, should be taken on empty stomach (gastric acid inactivates)
-pancreatitis, hyperuricemia, retinal changes and optic neuritis (requires periodic examinations)
-use with pancreotoxic drugs, cardiac risk factors, concomitant use w other drugs can block their absorption

Front 3

Emtricitabine
viral spectrum?
adverse effect?
contra?

Back 3

*NRTI
-HIV and HBV
-hyperpigmentation of palms and/or soles
-kids, preggos, renal & hepatic failure, combo w lamivudine causes viral resistance

Front 4

Lamivudine
viral spectrum?
viral resistance?
contra?

Back 4

*NRTI
-HIV and HBV
-cross resistance to emtricitabine/enecavir
-concomitantly w zalcitabine (inhibits intracellular phosph)

Front 5

Stavudine
Adverse effect?
contra?

Back 5

*NRTI
-peripheral sensory neuropathy- lactic acidosis w/ hepatic steatosis more freq than other NRTI's
-advanced immunosuppression, concomitant use with neuropathy inducing drugs and zidovudine

Front 6

Zidovudine "AZT"
pharmacodynamic?
clinical pharmacology?
adverse?
contra?

Back 6

*NRTI
-oral & parenteral admin.
-dec dz progression, and prolongs HIV pt survival
-HIV assoc dementia, thrombocytopenia, HIV transmission from mom to newborn, post occupational exposure
-myelosuppression (macrocytic anemia), high doses=confusion
-concomitant admin w. lots of other drugs

Front 7

Delavirdine
pharmacokinetic?
Adverse?
contra?

Back 7

*NNRTI
-oral bioavailability reduced by antacids and H2 receptor antagonists
-skin rash, Stevens Johnson syndrome, inc serum aminotransferase levels
-preggos, CYP450 inhibitor, given with fosamprenavir and rifabutin dec its levels

Front 8

Efavirenz
Adverse?
Contra?

Back 8

*NNRTI
-dizziness, drowsiness, (CNS effects), crystalluria, inc serum CE, elevated liver enzyme
-high fat meals (should be taken on empty stomach, preggos, inducer AND inhibitor of CYP450)

Front 9

Nevirapine
uses?
adverse?
contra?

Back 9

*NNRTI
-given to mom to prevent HIV transmission or at labor onset and 3 days after birth to neonate
-rash w maculopapular eruption, steven johnson syndrome, hepatitis
-induces CYP450

Front 10

Atazanavir
-pharmacokinetic?
-adverse?
contra?

Back 10

*PI
-take with light meals; requires acidic medium for absorption
-PR interval prolongation, inc in QT interval, **NOT assoc with cushingoid appearance
-taking with acid reducing agents, severe hepatic insufficiency

Front 11

Indinavir
pharmacokinetic?
adverse?
contra?

Back 11

*PI
-MUST be taken on empty stomach for max absorption
-indirect hyperbilirubinemia, and nephrolithiasis, thrombocytopenia
-hepatic insufficiency (reduce dose), inhibits CYP450s

Front 12

Lopinavir
pharmacokinetic?
adverse?
contra?

Back 12

*PI
-given in combo with ritonavir, food helps
-diarrhea, elevated serum CE and triglycerides
-concomitant admin w some drugs

Front 13

Ritonavir
pharmacokinetic?
uses?
adverse?
contra?

Back 13

*PI
-metabolized by CYP450s
-potent inhibitor of CYP3A4 (given w other PIs to decrease their freq dosing and viral resistance)
-GI disturbances, paresthesias, elevated aminotransferase levels
-impaired hepatic funct, co-administration with digoxin and theophylline

Front 14

Saquinavir
pharmacokinetic?
adverse?
contra?

Back 14

*PI
-given after fatty meal usually in combo w ritonavir; extensively metabolized by CYP3A4
-abdominal discomfort
-monitor when given w: omeprazole (GI), digoxin, delavirdine (liver), rifampin (liver)

Front 15

Enfuvirtide
pharmacokinetic?
viral spectrum?
adverse?

Back 15

*Entry inhibitor
-parenteral admin (SC)
-HIV 1 (none on HIV-2); binds gp41
-hypersensitivity, local site injection, eosinophilia, inc risk of bact pneumonia

Front 16

Maraviroc
pharmacokinetic?
viral spectrum?
adverse?
contra?

Back 16

*entry inhibitor
-R5 HIV-1 (CCR5 tropic HIV-1) SPECIFIC! block viral attachment
-cough, upper resp tract inf, muscle /joint pain
-same drugs as NNRTI, co admin w CYP3A inhibitors/inducers, liver dysfunction

Front 17

Raltegravir
pharmacokinetic?
viral spectrum?
uses?
contra?

Back 17

*integrase inhibitor
-no interaction w P450, but metabolized by glucuronidation
-HIV-1, HIV-2
-tx experienced pts w multidrug resistant HIV-1 strains
-concurrent use w rifampin and antacids