HIV Pharm Flashcards
HIV Goals (4)
Lower viral load, improve CD4 counts, prevent resistant, prevent inflammation/infection
Starting Treatment (4)
Emtricitabine + Tenofovir Alafenamide + Bictegravir
Negative HLA-B*5701 & HBV Tx (3)
Abacavir + Lamivudine + Dolutegravir
Only for Low Viral Load, No HBV, and Negative HLA-B*5701 (2)
Dolutegravir + Lamivudine
Other Options (6)
(Doultegravir or Raltegravir) + (Emtricitabine or Lamivudine) + Tenofovir (2)
HIV Cycle (4)
(1) Fuse and Enter the cell
(2) RT (competitive/noncompetitive)
(3) Integrate into genome (integrase)
(4) Cleave and mature (Protelolytic)
Maraviroc
(1) Entry inhibitor: CCR5 blocker
inhibited by CYP3A4, CXCR4 tropism, or GP120 V3 loop mutation
expensive, well tolerated
Enfuvirtide
(1) Fusion inhibitor: mimic gp41 and inhibit 6 helix membrane fusion (ONLY HIV-1)
not effective against, mutant gp41, HIV-2
expensive, parenteral injection
Zidovudine
(2) Thymidine (side) inhibit RT (all HIV and HTLV)
short t1/2, only IV, inhibit mito DNA polymerase (myopathy & hepatic steatosis) suppress bone marrow
Stauvudine
(2) Thymidine (side) inhibit RT (all HIV)
short t1/2, lipodystrophy (Fat wasting) and mito toxicity (peripheral neuropathy, lactic acidosis, hepatic steatosis)
Emtricitabine & Lamivudine
(2) Cytosine (side) inhibit RT (all HIV) Tx HBV
long t1/2, #1 in class, least toxic (E: hyper pigmented palm/soles of POC)
Abacavir
(2) Guanosine (side) inhibit RT
NOT FOR HLA-B*5701, HBV, of CAD hx
Longer t1/2, Fatal hypersensitivity!
Tenofovir (2) +1
(2) Adenosine (tide) inhibit RT Tx HBV
Decent t1/2 (1 day dosing) Disoproxil Fumutrate (nephrotoxicity, falconi kidney dysfxn (malabsoprtion))
Alafendamide: less toxic, well tolerated, lower plasma concentration
Didanosine: (all HIV, HTLV-1) has high mitochondrial toxicity
Nevirapine
(2) NonComp, HIV-1 only, CYP3A4, adult/kid
Decent t1/2, resistance if treated alone, rash
Efavirenz
(2) NonComp, HIV-1 only, CYP3A4, adult/kid
Long t1/2, was considered teratogenic, CNS toxicity, rash,
use with Emtricitabine & Tenofovir
Etravirine
(2) NonComp, HIV-1 only, CYP3A4, adult/kid
High resistance to mutation, decent t1/2, rash, immune reconstitution syndrome (inflammatory disorder
Rilpivirine
(2) NonComp, Naive HIV-1 only, CYP3A4, adult/kid
Decent resistance, long t1/2,
Adverse in kids (CNS, low cortisol, fat redistribution, immune reconstitution)
Doravirine
(2) NonComp, Naive HIV-1 only, CYP3A4, adult/kid
Resistance mutations, decent t1/2, low toxicity
Raltegravir
(3) Integrase, Naive all HIV
short t1/2, well tolerated
Doltegravir
(3) Integrase, Naive all HIV, (-) UGR1A1, NOT FOR PREGNANCY
decent t1/2, high barrier to resistance
Bictegravir
(3) Integrase, Naive all HIV, (-) UGR1A1
good t1/2m, high barrier to resistance, fixed dose, well tolerated
Saquinavir
(4) Competitively inhibit aspartyl protease, all HIV, CYP3A4
NOT USED, short t1/2, high pill burden, Lipodystrophy
Indinavir
(4) Competitively inhibit aspartyl protease, all HIV, CYP3A4
TOXIC crystaluria/renal stones, short t1/2
Darunavir
(4) Competitively inhibit aspartyl protease, all HIV use for 1, #1 when boosted CYP3A4, post exposure prophylaxis
decent t/12, Sulfa drug (rxn), fat redistribution syndrome, immune reconstitution syndrome
Azatanavir
(4) Competitively inhibit aspartyl protease, Naive all HIV, CYP3A4
elevated unconjugated hyperbbilirubinemai, fat redistribution, etc.
Lopinavir
(4) Competitively inhibit aspartyl protease, all HIV, CYP3A4
Use if other PI don’t work
short t1/2, high triglycerides/cholesterol
Ritonavir & Cobicistat
CYP3A4 inhibitors
All protease inhibitors (-avir)
Non-Nucleoside RT inhibitors (-ine)(HIV-1 only)
Entry inhibitor (Maraviroc)
