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Pharmacology (Topic C) > 6. Antiretroviral agents. > Flashcards

6. Antiretroviral agents. Flashcards

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1
Q

What is the MOA of Nucleotide Reverse Transcription Inhibitors (NRTIs).

A

Nucleotide Reverse Transcriptase Inhibitors (NRTIs) also known as HAART (highly active antiretroviral therapy) are nucleotides + nucleosides that lack an OH group necessary for 3’ → 5’ phosphodiester bond formation → chain termination. Nucleoside NRTIs need P-ation by cellular enzymes to be active. Generally, analogs of the same purine/pyrimidine bases (i.e. two cytosine analogs) are not given together.

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2
Q

List the 1st line NNRTIs.

A
  1. Efavirenz
  2. Nevirapine
  3. Delaviridine
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3
Q

List the 2nd line NNRTIs.

A
  1. Ertavirine
  2. Rilpivirine
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4
Q

List the NRTIs.

A
  1. Lamivudine
  2. Tenofovir
  3. Zidovudine - AKA azidothymidine, ZDV or AZT
  4. Stavudine
  5. Didanosine
  6. Abacavir
  7. Emitricitabine
  8. Zalcitabine - cytosine analog, withdrawn in Europe
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5
Q

List the protease inhibitors.

A
  1. Indinavir
  2. Ritonavir
  3. Saquinavir
  4. Atazanavir (newer, least metabolic effects)
  5. Others: Darunavir, Lopinavir, Tipranavir, Indinavir, Nelfinavir, Fosamprenavir.

Most have the “-avir” suffix (remember “guinevere”-based Sketchy scene)

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6
Q

List the integrase inhibitors.

A
  1. Raltegravir
  2. Elvitegravir
  3. Dolutegravir
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7
Q

List the fusion inhibitors.

A
  1. Enfuviritide
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8
Q

List the entry inhibitors.

A
  1. Maraviroc
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9
Q

What are the side effects of NRTIs?

A
  1. Mitochondrial toxicity - all
  2. Lactic Acidosis - all
  3. Lipodystrophy - zidovudine and stavudine
  4. Peripheral Neuropathy - lamivudine, stavudine, didanosine
  5. Headache, Fatigue, GI issues, Liver dysfunction - all
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10
Q

What are the indications for Lamivudine?

A

Lamivudine is a cytosine analog used for Hepatitis B treatment.

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11
Q

What are the side effect of Lamivudine?

A

This is the least toxic, but also least effective NRTI.

  1. Peripheral Neuropathy
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12
Q

What are the indications for Tenofovir?

A

Tenofovir is the only nucleotide NRTI (no P-ation required) and is used for Hepatitis B.

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13
Q

What are the indications of Zidovudine?

A

Zidovudine is used for HIV in pregnancy + breastfeeding to prevent vertical transmission as well as infant prophylaxis.

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14
Q

What are the side effects of Stavudine?

A
  1. Peripheral Neuropathy
  2. Also myelosuppression, but not as bad as AZT.
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15
Q

What are the side effects of Didanosine?

A
  1. Pancreatitis - dose-dependent.
  2. Peripheral Neuropathy - especially ↑ risk if with stavudine.
  3. also hyperuricemia and liver dysfunction.
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16
Q

What are the side effects of Abacavir?

A
  1. Hypersensitivity - type IV → delayed rash; HLA-B57:01 assoc.
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17
Q

What are the side effects of Emtricitabine?

A
  1. Palmoplantar Hyperpigmentation
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18
Q

What is the MOA of Non-Nucleotide Reverse Transcriptase Inhibitors (NNRTIs)?

A

NNRTIs directly bind HIV reverse transcriptase → allosteric inhibition of DNA polymerase activity.

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19
Q

What are the side effects of NNRTI’s?

A

common in NNRTIs:

  1. Flu-like Symptoms: abrupt onset
  2. Hepatic failure: abdominal pain, fever, jaundice (within 6 wks of start)
  3. Skin Rash: sometimes more severe, as Stevens-Johnson syn.
  4. Drug Interactions: CYP450 induction + inhibition
  5. Teratogenicity: both delavirdine and efavirenz
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20
Q

What is the mechanism behind NNRTIs resistance?

A

Resistance is only active for HIV-1; resistance to 1st gen NNRTIs by point mutation in some strains.

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21
Q

What are the side effects of Efavirenz?

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A
  1. CNS effects: dizziness, drowsiness, headache, psychosis, insomnia, nightmares
  2. Teratogenicity
  3. CYP450 induction and inhibition
22
Q

What is the MOA of Protease inhibitors?

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A

Protease Inhibitors inhibit HIV aspartate proteases (encoded by POL gene) necessary for cleavage of HIV polyprotein gene products (no similar protease in humans → selectivity).

23
Q

What is the MOA of Entry Inhibitors?

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A

Entry Inhibitors binds to T-cell surface protein CCR5 → blocks HIV env-encoded gp120 from co-binding CD4/CCR5 during viral entry into cell (does not work for HIV strains with CXCR4 instead of CCR5).

24
Q

What is the MOA of Fusion inhibitors?

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A

Fusion Inhibitors block env-encoded viral gp41, which normally facilitates HIV fusion to T cells.

25
**What is the MOA of Integrase Inhibitors?**
Integrase Inhibitors block pol-encoded viral integrases, which normally allow integration of viral DNA into host genome.
26
**What are the indications for Integrase inhibitors?**
known as cART (combined anti-retroviral therapy) 1. **HIV-related symptoms** - of HIV opportunistic infections / HBV coinfection 2. **CD4+ count \<200** - definite indication, but **\<350 also recommended** 3. **Viral load \> 5000 - 10,000 / ml** 4. **Pregnancy** - all except efavirenz (teratogen) 5. **Prophylaxis in exposed medical staff** 6. **Children** - more aggressive tx bc of faster progression 7. **Sexual Partners**
27
**What are the side effects of Zidovudine?**
1. **Myelosuppression** - causing anemia and neutropenia 2. **Lipodystrophy** - redistribution of fat from limbs to trunk 3. **Headaches** 4. **Asthenia** 5. **Myalgia** and **myopathy** 6. **Peripheral neuropathy**
28
**What are the indications for Emtricitabine?**
Emtricitabine a cytosine analog (a newer form of lamivudine) which is also effective against **hepatitis B.**
29
**What is the mechanism behind integrase inhibitor resitance?**
Resistance happens via pol mutation (affects efficacy of NRTIs, NNRTIs, PIs and integrase inhibitors).
30
**What are the side effects of integrase inhibitors?**
1. **Rhabdomyolysis** - rare; seen as ↑ creatine kinase
31
NNRTIs is also part of which therapy?
Also part of “HAART” therapy. HAART = highly active antiretroviral therapy.
32
**What are the side effects of Delavirdine?**
1. **Teratogenicity** 2. **CYP450 induction and inhibition**
33
**What are the indications for Nevirapine?**
Single dose intrapartum ↓ vertical transmission 50%.
34
What are the kinetics like for Nevirapine?
Penetrates CNS well (others do not) → worse CNS effects!
35
**What are the side effects of Nevirapine?**
**Moderate CYP450 induction**
36
**What are the side effects of Maraviroc?**
1. **HA, dizziness** 2. **Orthostatic hypotension** 3. **Airway infections** 4. **Allergic** 5. **Liver disorders** 6. **Increased malignancy**
37
**What is the mechanism behind protease inhibitors resistance?**
POL gene mutation → resistant proteases
38
What is the mechanism behind Entry inhibitors resistance?
via **env mutation**
39
**What are the side effects of protease inhibitors?**
1. **Hyperglycemia** - via insulin resistance; can → diabetes 2. **Dyslipidemias** - TAGs and LDL ↑ 3. **Lipodystrophy -** ↑ fat on back/abdomen, ↓ on face/limbs 4. **CYP450 Inhibition** - worst with ritonovir 5. **Interactions:** rifampin CYP induction will ↓ protease inhibitor levels; use rifabutin instead!
40
**What is the mechanism behind fusion inhibitors resistance?**
via **env mutation**
41
**How is maraviroc metabolized?**
Metabolized by CYP3A4
42
**What are the side effects of Enfuviritide?**
Enfuvirtide is a polypeptide, administered subcutaneously. It is well tolerated, but may cause **local reactions, HA, nausea, bacterial pneumonia?**
43
What are the indications for Enfurviritide?
They are used for multidrug-resistant cases.
44
What are the side effects of Indinavir?
1. **Nephrolithiasis** - within days of starting; ↓ by hydration
45
What are the side effects of Ritonavir?
Worst CYP inhibition among protease inhibitors. Can be used to ↑ levels of other CYP-metabolized protease inhibitors!
46
**What are some important remarks about Saquinavir?**
Saquinavir is the oldest, least toxic and has↓ oral availability.
47
What are the kinetic parameters of Raltegravir?
1. Raltegravir is given orally 2. Metabolized by glucuronide conjugation
48
**What are the side effects of Raltegravir?**
Chelates bivalent cations, generally well tolerated, but GI, HA, dizziness, rashes may occur.
49
What are the side effects to Elvitegravir?
Elvitegravir has similar sfx to raltegravir; given with CYP inhibiting “booster” (ritonavir or cobicstat).
50
**What are the side effects of Dolutegravir?**
1. **Severe HS rxns** 2. **Insomnia** 3. **Headache**
51
**What are the indications of Dolutegravir?**
Known as cART (combined anti-retroviral therapy) 1. **HIV-related symptoms** - of HIV opportunistic infections / HBV coinfection 2. **CD4+ count \<200** - definite indication, but **\<350 also recommended** 3. **Viral load \> 5000 - 10,000 / ml** 4. **Pregnancy** - all except efavirenz (teratogen) 5. **Prophylaxis in exposed medical staff** 6. **Children** - more aggressive tx bc of faster progression 7. **Sexual Partners**

Pharmacology (Topic C) (20 decks)

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