Drugs Five Last Time

Question 1

5 drug classes to act on HIV

Answer 1

1) Reverse transcriptase inhibitors (NRTIs and NNRTIs)
2) protease inhibitors
3) HIV fusion inhibitors
4) Integrase strand transfer inhibitors
5) CCR5 antagonists

Question 2

Drug interactions with anti HIV drugs

Answer 2

Many are inducors or inhibitors for one or more CYP450 enzymes and might intensify effects to harmful degree

Question 3

Nucleoside/nucleotide reverse transcriptase inhibitors mech of action

Answer 3

Inhibit ability of virus to use reverse transcriptase to incorportae RNA into host cell’s DNA, preventing replication

Question 4

Nucleoside/nucleotide reverse transcriptase inhibitors ADRS

Answer 4

• Lactic acidosis (rare accumulation)

- hepatic steatosis (fatty degeneration of liver)

Question 5

Abacavir

Answer 5

Analog of guanine commonly used in antiretrovirals

Question 6

Abacavir mech of action

Answer 6

Taken up by host cells and converted to active form, compees for binding reverse transcriptase

Question 7

HLA-B 5701

Answer 7

Specific genetic variation that makes patients susceptibe to abacavir hypersensitivity

Question 8

Zidovudine (ZDV or AZT)

Answer 8

First antiretroviral drug for HIV, not recommended because of adverse effects

Question 9

Zidovudine mech of action

Answer 9

Converted to active form in cell and acts as substrate for reverse transcriptase blocking and terminating further growth

Question 10

Zidovudine ADRs

Answer 10

Anemia and neutropenia

Question 11

Non nucleoside reverse transcriptase inhibitors

Answer 11

Differ from NRTI’s in struture and mech of action,

Question 12

Non nucleoside reverse transcriptase inhibitors mech of action

Answer 12

Active as administered bind directly to reverse transcriptase and cause active inhibition

Question 13

Efavirenz

Answer 13

NNRTI for treating HIV

Question 14

Efavirenz ADRs

Answer 14

CNS compications
Rash, steven johnson
Teratogenicity

Question 15

Protease inhibitors

Answer 15

Active against HIV 1 and 2 most effective especially when used in combo with others

Question 16

Protease inhibtors mech of action

Answer 16

Prevention of HIv maturation by blocking HIV enzyme protease, preventing cleaving of HIV polyproteins

Question 17

Protease inhibitors ADRs

Answer 17

• Hyperglycemia
• Diabetes
• hyperlipidemia
• decreased cardiac conductio velocity

Question 18

Ritanovir boosting

Answer 18

Ritanovir is a Protesase inhibitor routinely combined with other PIs specifically to increase plasma level (one protease inhiibotr can metabolism of the other) to increase therapuetic use

Question 19

Fusion inhibitors

Answer 19

Prevent entracnce of HIV into CD4T cells

Question 20

Enfuviritide aka T-20

Answer 20

First fusion inhibitor, reserved for treatment experienced patients who have evidence of HIV replication despite ongoing ART

Question 21

Enfuviritide aka T-20 resistance

Answer 21

-Structural changes to gp41 (subunit embedded in HIV envelope)

Question 22

HIV-1 Integrase strand transfer inhibitors

Answer 22

PO HIV drugs received accelerated approval for combo therapy for treatment expereinced adults infected wth HIV 1 strains resistant to antiretroviral drugs

Question 23

Example of HIV-1 Integrase strand transfer inhibitor

Answer 23

Raltegravir

Question 24

Raltegravir mech of action

Answer 24

Inhibits enzyme that catylzes the process that results in viral DNA insertion into host genome

Question 25

Other examples of HIV-1 Integrase strand transfer inhibitors

Answer 25

• Elvitegravir

- Dolutegravir

Question 26

CCR5 antagonists

Answer 26

Restricted to use in adults with CCR5 tropic HIV 1 (found in some individuals not others)

Question 27

CCR5 antagonist mech of action

Answer 27

CCR5 tropic HIV-1 strains predominate during early stages of infection, drugs bind CCR5 cco receptor preventing from virus entering host cell

Question 28

Zidovudine/iamivudine

Answer 28

2 nucleoside reverse transcriptase inhibitors administered togethers

Question 29

Juluca (dolutgravir and rilpivirone)

Answer 29

first 2 regimen drug complete regiment approved for treatment of HIV-1 infection

Question 30

Ilbazumab-uiyk

Answer 30

IV treatment for multi drug resistant HIV 1, blocks entry of HIv into CD4 cell

Question 31

ART therapy

Answer 31

Usually contains 3 drugs, attack HIV via 2 different mechanisms, the other 4 are class sparing so if resistance is developed can switch class