HIV/AIDS

Question 1

Abacavir

Answer 1

IND: NRTI
MOA: NRTI
BOX: N/A
CON: HLA-B5701; Genetic hypersensitivity, all pts must be screened. Hepatic impairment
ADR: Hypersensitivity rxn. Lipodystrophy; weird distribution of fat “buffalo hump”. Alcohol increases levels of Abacavir

Question 2

HAART

Answer 2

3-4 drugs in combination. 2 NRTIs + others
Decrease plasma HIV so low that it is undetectable; basically gets rid of disease but very expensive, lifelong, and lots of drug interactions

Question 3

Overview of AIDS treatment

Answer 3

Managed for life now, rather than a death sentence
Complex
Typically only utilize drugs from 2 classes

Question 4

Recommended Regimens

Answer 4

Bictegravir/Tenofovir Alafenamide/Emtricitabine
Dolutegravir/Abacavir/Lamivudine: No HLA B5701 or Hep B
Dolutegravir + (Emtricitabine or Lamivudine) + (Tenofovir Alafenamide or Tenofovir Disoproxil Fumarate)
Dolutegravir/Lamivudine

Question 5

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors

Answer 5

IND:
MOA: Substrates for reverse transcriptases, suppresses HIV replication.
BOX: Lactic acidosis d/t disrupting mitochondrial DNA synthesis (more likely w/Stavudine and Didanosine; no longer recommended in US)
CON: n/a
ADR: Lactic acidosis. Hepatic Steatosis from fatty deposits in the liver.

Question 6

Lamivudine

Answer 6

IND: NRTI
MOA: NRTI
BOX: Exacerbation of Hep B. Important differences among products. Risk of HIV resistance in Hep B treated pts
CON: Hep B
ADR: GI. CNS.

Question 7

Tenofovir

Answer 7

Viread and Vemlidy
IND: NRTI
MOA: NRTI. Once weekly for dialysis pts
BOX: Exacerbation of Hep B
CON: Hep B
ADR: Hypercholesterolemia. Decreased bone mineral density. Rash/pruritis

Question 8

Emtricitibine

Answer 8

IND: NRTI
MOA: NRTI
BOX: Exacerbation of Hep B
CON: Hep B
ADR: HYPERPIGMENTATION on palms and soles. GI

Question 9

Zidovudine is

Answer 9

For short term use in pregnant pts

Question 10

INSTI

Answer 10

IND: Used in combination as first line agents with 2 NRTIs
MOA: Inhibit the enzyme integrase which integrates HIV into human DNA

Dolutegravir
Bictegravir: Only as a combo agent; Biktarvy
Raltegravir
Elvitegravir: old. Only as a combo agent and rarely used d/t resistance

Question 11

Dolutegravir

Answer 11

IND: INSTI
MOA: INSTI
BOX: N/A
CON: Pts on Dofetalide (antiarrhythmic agent)
ADR: Increase LFTs and serum lipase. Hyperglycemia

Question 12

Bictegravir

Answer 12

IND: INSTI
MOA: INSTI +NRTI+NRTI
BOX: Exacerbation of Hep B
CON: Dofetalide or Rifampin. Renal/hepatic dysfunction. Difficult to dose. Hep B
ADR: Increased LFTs/serum bilirubin,

Question 13

Raltegravir

Answer 13

IND: INSTI
MOA: INSTI. Resistance develops more with Raltegravir v Dolutegravir
BOX: N/A
CON: n/a
ADR: Increased LFTs. SJS and Toxic Epidermal Necrolysis

Question 14

Non-nucleoside Reverse Transcriptase Inhibitors (NNRTI)

Answer 14

Combined with an NRTI and an additional agent when used.
Only agent listed as a preferred HIV treatment is Efavirenz
MOA: Inhibit reverse transcriptase activity by blocking nucleoside ability to bind; prevents viral replication
ADR: None

Question 15

Efavirenz

Answer 15

IND:
MOA: NNRTI. Crosses BBB well, can reduce viral load in CNS
BOX: N/A
CON: Administration with Zepatier (Hep C treatment)
ADR: Rash. Increased cholesterol, HDL, triglycerides. Significant CNS. Liver damage

Question 16

Protease Inhibitors

Answer 16

IND:
MOA: Block HIV protease enzyme; prevents maturation of HIV and renders it non-infectious. Good when resistance to other drugs occurs
BOX: N/A
CON:
ADR: Hyperglycemia/diabetes. Hyperlipidemia. LFT elevation. Decreased cardiac conduction speed.

Ritonavir is used INTENTIONALLY to inhibit CYP enzymes, to increase levels of other PIs to increase the anti-viral activity.

Question 17

Enfuvirtide

Answer 17

IND: Pts with resistance or persistent viral load despite ART
MOA: HIV fusion inhibitor. Blocks entry of HIV into CD4 T Cells. 2x/day subQ.
BOX: N/A
CON:
ADR: Injection site rxn

Question 18

Maraviroc CCR5 Antagonist

Answer 18

IND:
MOA: Blocks CCR5 to prevent HIV into the CD4 T Cells. Last line, reserved for drug resistant HIV