HIV Drugs

Question 1

Zidovudine

Answer 1

MOA: nucleoside RTI (incorporation into host genome terminates polymerization)

PK: requires phosphorylation by host enzymes

Resistance: occurs across the class

Adverse: granulocytopenia, anemia, CNS distrubances, mitochondial activity inhibitor (lactic acidosis), hepatic steatosis (fatty liver), hyperlipidemia, change in fat distribution, drug-drug

Question 2

Lamivudine

Answer 2

MOA: nucleoside RTI (incorporation into host genome terminates polymerization)

PK: requires phosphorylation by host enzymes

Resistance: occurs across the class

Adverse: mitochondial activity inhibitor (lactic acidosis), hepatic steatosis (fatty liver), hyperlipidemia, change in fat distribution, drug-drug

*most tolerated, also used to treat HepC

Question 3

Emtricitabine

Answer 3

MOA: nucleoside RTI (incorporation into host genome terminates polymerization)

PK: requires phosphorylation by host enzymes

Resistance: occurs across the class

Adverse: mitochondial activity inhibitor (lactic acidosis), hepatic steatosis (fatty liver), hyperlipidemia, change in fat distribution, drug-drug

*most tolerated, also used to treat HepC

Question 4

Abacavir

Answer 4

MOA: nucleoside RTI (incorporation into host genome terminates polymerization)

PK: requires phosphorylation by host enzymes

Resistance: occurs across the class

Adverse: mitochondial activity inhibitor (lactic acidosis), hepatic steatosis (fatty liver), hyperlipidemia, change in fat distribution, drug-drug, hypersensitivity

Question 5

Tenofovir

Answer 5

MOA: nucleotide reverse transcriptase inhibitor

Toxicity: nephrotoxicity, nausea, vomiting, diarrhea, mitochondial toxicity (lactic acidosis), hepatic steatosis (fatty liver)

Question 6

Efavirenz

Answer 6

MOA: non-nucleotide RTI (binds allosteric site)

Resistance: no cross resistance with nucleotide RTIs

Adverse: CNS, GI intolerance, rash, CYP450 metabolized

Question 7

Etravirine

Answer 7

MOA: non-nucleotide RTI (binds allosteric site)

Resistance: no cross resistance with nucleotide RTIs

Adverse: peripheral neuropathy, rash, CYP450 metabolized

Question 8

Atazanavir

Answer 8

MOA: protease inhibitor, viral assembly/maturation

Resistance: no cross resistance with nucleotide RTI or non-nucleotide RTI

Toxicity: peripheral lipoatrophy and central fat accumulation (skinny arms fat trunk), GI, hepato, hyperglycemia + insulin resistance, dyslipidemia, cardiac conduction abnormalities, CYP3A4 metabolism

Question 9

Ritonavir

Answer 9

MOA: protease inhibitor, viral assembly/maturation

Resistance: no cross resistance with nucleotide RTI or non-nucleotide RTI

Toxicity: peripheral lipoatrophy and central fat accumulation (skinny arms fat trunk), GI, hepato, hyperglycemia + insulin resistance, dyslipidemia, cardiac conduction abnormalities, CYP3A4 metabolism

_**CYP3A4 inhibitor ==> boosting!!*_

Question 10

Darunavir

Answer 10

MOA: protease inhibitor, viral assembly/maturation

Resistance: no cross resistance with nucleotide RTI or non-nucleotide RTI

Toxicity: peripheral lipoatrophy and central fat accumulation (skinny arms fat trunk), GI, hepato, hyperglycemia + insulin resistance, dyslipidemia, cardiac conduction abnormalities, CYP3A4 metabolism

Question 11

Enfuvirtide

Answer 11

MOA: fusion inhibitor, binds gp41 and prevents conformational change

Admin: SubQ q12hr

Adverse: local reactions, systemic hypersensitivity, pneumonia

Question 12

Raltegravir

Answer 12

MOA: integrase inhibitor, inhibits provirus integration into host genome (inhibits strand transfer)

Toxicity: less

Question 13

Maraviroc

Answer 13

MOA: CCR5 antagonist, blocks HIV “receptor”

Toxicity: pyrexia, rash, postural dizziness, no increased risk of malignancy/infection