Antivirals Flashcards
Zidovudine
reverse transcriptase inhibitor
watch anemia, neutropenia (G-CSF)
RARE hepatotoxicity and Lactic acidosis
Zidovudine with Tylenol or ganciclovir:
risk of granulocytopenia
Zidovudine with acyclovir
lethargy and somnolence
Lamivudine/Zidovudine
2 choice for HIV combo
Tenofovir/Emtricitabine
#1 choice for HIV combo Well tolerated
Didanosine
Reverse Transcriptase Inhibitor
used in combo with zidovudine
Causes PERIPHERAL NEUROPATHY, Pancreatitis, anemia, granulocytopenia, hyperuricemia
Zalcitaibe
Dideoxycytidine RTI
Causes PERIPHERAL NEUROPATHY and mucosal ulcers
Lamivudine
Cytosine analogue- competitive inhibitor of RT (RTI)
Very well tolerated, MUST USE WITH ANOTHER DRUG (Zidovudine) to prevent resistance
DOC FOR HBV
Stavudine
Dideoxycytidine RTI
Use for ADVANCED HIV if no other therapy tolerated
resistance is uncommon
Causes PERIPHERAL NEUROPATHY, lactic acidosis
DO NOT COMBINE WITH OTHER -VUDINE!
Abacavir
Guansine analogue RTI
5% hypersensitivity reactions– causes fever, malaise, rash, chills, etc. D/C AND DO NOT RESTART
Tenofovir
Adenosine analogue RTI
DOC for naive patients, along with Emtricitabine
Emtricitabine
Cytosine analog (like lamivudine) RTI DOC for naive HIV patients with Tenofovir
Big 4 HIV drugs
Lamivudine, Zidovudine, Tenofovir, Emtricitabine
Protease inhibitors
RAPID RESISTANCE IF USED ALONE
DO NOT INTERRUPT THERAPY
ALWAYS COMBINE WITH RTI
Metabolized BY CYP3A4 (LOTS OF DRUG INTERACTIONS)
DO NOT combine with STATINS OR ST JOHN’S WORT
Protease inhibitor side effects
ALTERED FAT DISTRIBUTION
Buffalo hump, truncal obesity, facial and peripheral atrophy
Insulin resistance
High serum cholesterol
Saquinavir
Protease inhibitor;
GIVE WITH GRAPEFRUIT JUICE or RITONAVIR
Darunavir
2nd choice Protease Inhibitor
Combine with RITONAVIR
More safe and effective, but some SEs:
Rash, HA, BAD DREAMS
Ritonavir
Protease Inhibitor
Use subtherapeutically to inhibit CYP3A4– increases effectiveness of other PIs
CI WITH MANY OTHER DRUGS!
SE: GI, burning, tingling
Indinavir
Protease Inhibitor
Good bioavailability and CSF PENETRATION– Take on empty stomach
DON’T GIVE WITH RIFAMPIN
SE: NEPHROLITHIASIS (Hydrate) and HYPERBILIRUBINEMIA
Nelfanavir
Protease Inhibitor
BETTER ABSORBED WITH FOOD
SE: Asthenia
Amprenavir/Fosamrenavir
PI
Contains PEG– DO NOT GIVE WITH DISULFRAM OR METRONIDAZOLE
SE: SJS or SEVERE RASH
Atazanavir
DOC PI due to low SE
DON’T COMBINE WITH INDINAVIR (increase bilirubin)
Tipranavir
Lopinavir
PI
COMBINE WITH RITONAVIR
Tip: DON’T COMBINE WITH INDUCERS/INHIBITORS OF CYP3A4 (doesn’t this pertain to all PIs?)
Non-nucleoside RTIs
Directly bind RT to prevent RNA to DNA conversion
NO PHOSPHORYLATION NEEDED
RAPID RESISTANCE DEVELOPS
CYP3A4 metabolization= PI INTERACTION!!!
Delavirdine
NNRTI
Inhibits CYP3A4- Antacids decrease efficacy
Nevirapine
DOC NNRTI in PREGNANCY
induces CYP3A4=decreased efficacy of birth control
Efavirenz
NNRTI
DOC EXCEPT IN PREGNANCY
Enfuviritide
FUSION INHIBITOR
Binds to gp41 subunit of viral envelope to prevent fusion
ADVANCED HIV- HAS NO RESISTANCE WITH OTHER ANTIVIRALS
Inject in cheeks
Pneumonia more likely!
Maraviroc
FUSION INHIBITOR
Binds to CCR5 receptor on CD4 Cell
Only use in pts with CCR5 trophic HIV
Raltegravir
INTEGRASE INHIBITOR
Blocks integrase needed to transfer viral DNA to host cell DNA
Advanced HIV