drugs

Question 1

Fusion inhibitors 2

Answer 1

Enfuvirtide-GP41 inhibitor taken orally with rash

Maraviroc-CCR5 receptor inhibitor-orally with URT infection/rash and possibly MI

Question 2

NRTIs 2.5 and general

Answer 2

Emticitabine-binds to RT polymerase

Tenofovir-HIV/HBV-Adenosine analog with 1 phosphate

• disproxide-loses protecting group so loses P easily so less stable
• alafenamide-only lose protecting group @ lymph nodes
• -nephrotoxic and deceased bone mineral density

Prodrugs that can cause lactic acidosis

Question 3

NNRTIs 2

Answer 3

Efavirenz-both bind to place close to RT polyermase active site to change conformation

Etravirenz-wiggles and jiggles

elevated liver enzymes and nephrotoxic

Question 4

Viral Integrase Inhibitors 3+1

Answer 4

Raltegravir-first line trx with low tax

Dolutegravir-longer half life

Elvitegravir-1x day

Need colbicastat to inhibit CYP3A4 to increase half life

inhibits strand transfer by binding to Mg in active site of integrate-dna complex-displaces 3’ OH from reactive center

Question 5

Protease Inhibitors 3

mech/side fx

Answer 5

Darunavir-newsest
Atazanavir-fewer lipid side fx
Riotnavir

All reversibly inhibit HIV protease that cleaves gag-pol

Changed body fat distribution, hyperlipidemia, and worsening glycemic control

Question 6

Conformations 4

Answer 6

Truvada-emticiabine and tenofovir

Trimmeq-dolutegravir/abacavir/lamivudine

Stribild=elivitegravir/cobicistat/emtricitabine/tenofovir disproxil

Genvoya=elvitegravic/colbicatat/emtricabine/tenofovor alafenamide