HIV Pharm Flashcards
(27 cards)
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
