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Flashcards in Drugs Five Last Time Deck (31)
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1
Q

5 drug classes to act on HIV

A

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

2
Q

Drug interactions with anti HIV drugs

A

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

3
Q

Nucleoside/nucleotide reverse transcriptase inhibitors mech of action

A

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

4
Q

Nucleoside/nucleotide reverse transcriptase inhibitors ADRS

A
  • Lactic acidosis (rare accumulation)

- hepatic steatosis (fatty degeneration of liver)

5
Q

Abacavir

A

Analog of guanine commonly used in antiretrovirals

6
Q

Abacavir mech of action

A

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

7
Q

HLA-B 5701

A

Specific genetic variation that makes patients susceptibe to abacavir hypersensitivity

8
Q

Zidovudine (ZDV or AZT)

A

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

9
Q

Zidovudine mech of action

A

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

10
Q

Zidovudine ADRs

A

Anemia and neutropenia

11
Q

Non nucleoside reverse transcriptase inhibitors

A

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

12
Q

Non nucleoside reverse transcriptase inhibitors mech of action

A

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

13
Q

Efavirenz

A

NNRTI for treating HIV

14
Q

Efavirenz ADRs

A

CNS compications
Rash, steven johnson
Teratogenicity

15
Q

Protease inhibitors

A

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

16
Q

Protease inhibtors mech of action

A

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

17
Q

Protease inhibitors ADRs

A
  • Hyperglycemia
  • Diabetes
  • hyperlipidemia
  • decreased cardiac conductio velocity
18
Q

Ritanovir boosting

A

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

19
Q

Fusion inhibitors

A

Prevent entracnce of HIV into CD4T cells

20
Q

Enfuviritide aka T-20

A

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

21
Q

Enfuviritide aka T-20 resistance

A

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

22
Q

HIV-1 Integrase strand transfer inhibitors

A

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

23
Q

Example of HIV-1 Integrase strand transfer inhibitor

A

Raltegravir

24
Q

Raltegravir mech of action

A

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

25
Q

Other examples of HIV-1 Integrase strand transfer inhibitors

A
  • Elvitegravir

- Dolutegravir

26
Q

CCR5 antagonists

A

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

27
Q

CCR5 antagonist mech of action

A

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

28
Q

Zidovudine/iamivudine

A

2 nucleoside reverse transcriptase inhibitors administered togethers

29
Q

Juluca (dolutgravir and rilpivirone)

A

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

30
Q

Ilbazumab-uiyk

A

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

31
Q

ART therapy

A

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