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Pharma 1- Semmelweis > Topic 6-Antiretroviral agents > Flashcards

Topic 6-Antiretroviral agents Flashcards

1
Q

Indications of starting the antiretroviral therapy (cART : Combined Antiretroviral Therapy)

A
  1. ) in case of clinical HIV related symptoms (opportunistic infections) or HBV coninfection
  2. )CD4+ is lower than 200/ul
  3. )If viral load (HIV RNA count) is above 5000-10000/mL
  4. )During pregnancy (except efavirenz)
  5. )Post exposition prophylaxis for medical staff
  6. )For children, more aggressive treatment
  7. ) For HIV discordant sexual partners
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2
Q

What is the cART?

A

2NRTI and Integrase inhibitors or 1 NNRTI or PI or maraviroc
Life long treatment is need, hold application
Very few examples of total eradication (once after bone marrow transplant and once in a connate case)

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3
Q

Antiretroviral agent mechanisms

A
  1. )Entry/Fusion/Attachment inhibitors
  2. )Nucleoside/Nucleotide and Non-Nucleoside Reverse Transcriptase inhibitor
  3. )Integrase inhibitor
  4. )Maturation inhibitor
  5. )Protease inhibitor
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4
Q

Nucleoside/nucleotide RT inhibitors (NRTI)

Thymidine analogue:?

A

Thymidine analogue: Zidovudine

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5
Q

Nucleoside/nucleotide RT inhibitors (NRTI)

Cytidine analogues:?

A

Cytidine analogues: Lamivudine, Emtricitabine

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6
Q

Nucleoside/nucleotide RT inhibitors (NRTI)

Purine analogues:?

A

Purine analogues: Abacavir, tenofovir

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7
Q

Mechanism of action of the NRTI (nuceoside/nucleotide RT inhibitors)

A

RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replication of HIV and other retroviruses.

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8
Q

What is the resistance like for NRTIs?

A

Lots of mutations are needed and no cross resistance between drugs

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9
Q

Which NRTI penetrates the CNS

A

tenofovir

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10
Q

Which NRTIs excreted through kidneys

A

zidovudin, abacavir, and didanosin

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11
Q

Which NRTIs are active agaisnt HBV

A

Lamivudin, emtricitabin, and tenofovir

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12
Q

Main adverse effects of NRTIs

A

GI issues, headache, fatigue, lactic acidosis, hepatomegalia, lypodystrophy, hepatitis, transaminase elevation

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13
Q

Main adverse effect of zidovudin?

A

anemia, leukopenia

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14
Q

Stavudin and Didanosin side effects?

A

Pancreatitis and peripheral neuropathy (these drugs aren’t used anymore)

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15
Q

Main adverse effect of abacavir?

A

Hypersensitivity reaction for HLA-B*5701

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16
Q

Main adverse effect of tenofovir?

A

Nephrotoxicity and bone abnormality (given with disoproxil and alafenamide to lower toxicity)

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17
Q

Initial treatment with NRTIs?

A

one cytidine and one purine are combined and identical analogues should not be combined

18
Q

1st generation non-nucleoside RT inhibitors (NNRTI)

A

1st generation Nevirapin, Efavirenz

19
Q

2nd generation non-nucleoside RT inhibitors

A

2nd generation Etravirin, Rilpivirin

20
Q

NNRTIs are effective against

A

HIV-1

21
Q

A single point-mutation can cause resistance in which generation of NNRTIs

A

1st generation

22
Q

NNRTIs are metabolized where?

A

liver

23
Q

Which NNRTI penetrates well into the CNS

A

Efavirenz

24
Q

Which NNRTIs have low penetration

A

etravirin and rilpivirin, but enough to control HIV

25
Q

General adverse effects of NNRTIs

A

liver and GI issues, rash (Steven Johnson syndrome)

Efavirenz can cause CNS issues and is teratogenic

26
Q

What are the protease inhibitors

A 
Ritonavir
Lopinavir
Atazanavir
Darunavir
Tipranavir
27
Q

Mechanism of protease inhibitors

A

Cleaves Gag and Gag-Pol polyproteins of HIV, that have key role in maturation of HIV (no cross reaction with human proteases)

28
Q

Adverse effects of protease inhibitors? Resistance?

A

insulin resistance, hyperlipidemia, abdominal fat uptake, transaminase elevation, GI, and neurological issue, and allergic reactions
No cross resistance between PIs

29
Q

Kinetics of PI

A

Oral availability
Don’t enter CNS
Metabolized by CYP3A4 in liver
Half life is variable

30
Q

Which PI is metabolized by CYP2C19?

A

nelfinavir

31
Q

Which PI blocks CYP3A4?

A

Ritonavir

32
Q

What are the three integrase inhibitors

A

Raltegravir
Elvitegravir
Dolutegravir

33
Q

Mechanism of action of Raltegravir?

Kinetics?

A 
Inhibits the integration of NA transcripted HIV into the human DNA chain
oral administration (twice a day), conjugated by glururonic acid
34
Q

Adverse effects of Raltegravir

A

GI issues, headache, dizziness, skin rash CK elevation, myopathy

35
Q

Details of Elvitegravir

A

Administered once with „booster” (CYP3A inhibitor: ritonavir or cobicistat)

  • Cross- resistance with raltegravir
  • Combined tablet: elvitegravir(+cobicistat)+emtricitabin+ tenofovir
  • Side effects: similar to raltegravir
  • Simple administration but many interactions
36
Q

Details of Dolutegravir

A
  • Low cross-resistance, higher genetic barrier

- Side effects: Sever hypersensitive reactions, insomnia, headache

37
Q

Entry inhibitor for HIV

A

Enfuvirtid

38
Q

Details of Enfuviritd

A 
Binds to Gp41 of HIV and inhibits the binding to the cells
Polypeptide structure,subcutaneous administered
Well tolerated (local rxn, headache, nausea, bacterial pneumonia)
Used for multidrug resistant cases
39
Q

CCR5 coreceptor antagonist

A

Maraviroc

40
Q

Maraviroc is effective in which case

A

macrophage infecting viruses, not effective on CXCR4 and mixed trop viruses
CCR5 viruses are mainly present in earlier stages of the diseases
CXCR4 viruses, which prefer T-cells, mainly appear later

41
Q

Adverse effects of Maraviroc

A

Headache, dizziness, orthostatic hypotension, airway infections, allergic liver disorder, increased prevalence of malignancies

42
Q

Kinetics of Maraviroc? Initial treatment?

A

Orally administered, metabolzed in liver (CYP3A4 interactions)
Not recommended as initial treatment

Pharma 1- Semmelweis (16 decks)

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