Antivirals

Question 0

What does long term HAART therapy often result in?

Answer 0

HIV lipodystrophy syndrome with redistribution of fatty tissue, altered lipoprotein profile, and insulin resistance

Question 1

Typical HAART combo?

Answer 1

Protease inhibitor or NNRTI coupled with two NRTIs

Question 2

Enfuvirtide

Answer 2

Binds gp41 preventing fusion and cell entry

Lacks cross resistance with other agents

Question 3

Zidovudine

Answer 3

NRTI
orally - absorption through GI tract
Good distribution- therapeutic levels reached in the brain
Glucoronidated in the liver
Most common side effect is myelosuppression, CNS toxicity, lactic acidosis, liver damage
Use with probenecid increases concentration

Question 4

Lamivudine

Answer 4

NRTI
synergizes with lamivudine
Also treats hep b

Question 5

Emtricitabine

Answer 5

NRTI

low side effects, good bioavailability

Question 6

Tenofovir

Answer 6

NRTI
First nucleotide RTI
concentration high, also used for hep b

Question 7

NNRTIs

Answer 7

Don’t require activation
Not incorporated into DNA
Nevirapine - single dose prevents transmission to newborn, life threatening rash
Efavirenz - long half life, taken once a day

Question 8

Protease inhibitors

Answer 8

Oral drugs
Many drug drug interactions, often inhibit p450
Mimic transition state during proteolysis
Fecal elimination
Ritonavir - inhibits metabolism of other protease inhibitors, given as boost
Saquinavir - drug can crystallize in liver and kidney, drink water

Question 9

Acyclovir

Answer 9

Absorbance after oral dose fair but adequate
Given IV in serious infections
Distribution wide including CSF
Eliminated by kidney

Question 10

Valacyclovir

Answer 10

Higher absorption after oral dose and quickly converted of acyclovir

Question 11

Ganciclovir

Answer 11

Agent against CMV
virus kinase prefers over acyclovir
Used IV or intraocular implants
IV admin can lead to myelosuppression

Question 12

Foscarnet

Answer 12

Agent against CMV
needs no activation
Used in acyclovir resistant CMV
Side effects include renal dysfunction, hypocalcemia, and chromosomal damage

Question 13

Drug therapies against flu

Answer 13

Zanamivir - inhaled, more side effects
Oseltamivir - taken orally
Inhibits viral neuraminidase - cant cleave sialic acids for virus release

Question 14

Interferon alpha

Answer 14

Treats hep b and c
SC or IM - not orally
Activate JAK STAT antiviral pathways
Cleared by liver and kidney quickly but conjugation with PEG chains increases half life tenfold
Flu like symptoms follow as well as possible neurotoxicity and bone marrow suppression

Question 15

Ribavirin

Answer 15

Guanine nucleoside analog
Against hep c orally
Aerosol against respiratory syncytial virus in children
Teratogen