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HD > Pharmacology 1: Therapeutic Approach To Infectious Diseases (HIV) > Flashcards

Pharmacology 1: Therapeutic Approach To Infectious Diseases (HIV) Flashcards

1
Q

What is the first anti-retroviral agent to be discovered?

A

Zidovudine.

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2
Q

How many anti-retrovirals is the standard of care?

A

3 anti-retrovirals.

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3
Q

The most important measure of ART efficacy is what?

A

Viral load.

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4
Q

1- HIV enters the CD4 cells after fusion of viral ____ with ______ or _____ receptors on human cells.

A

HIV enters the CD4 cells after fusion of viral Gp41 with CCR5 or CXCR4 receptors on human cells.

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5
Q

2- After entry, viral RNA is converted to DNA with the help of __________________.

A

After entry, viral RNA is converted to DNA with the help of reverse transcriptase (RNA dependent DNA polymerase).

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6
Q

3- Viral DNA integrates with human DNA to form ______, with the help of enzyme _______.

A

Viral DNA integrates with human DNA to form provirus, with the help of enzyme integrase.

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7
Q

4- The proviral DNA replicates and transcripts to form ____, which forms proteins via _________.

A

The proviral DNA replicates and transcripts to form RNA, which forms proteins via translation.

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8
Q

5- ___________ cleaves the proteins and allows their assembly as __________.

A

Protease enzyme cleaves the proteins and allows their assembly as new virion.

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9
Q

List the 4 targets of anti-retroviral drug action?

A

1- fusion/entry inhibitors.
2- reverse transcriptase inhibitors.
3- integrase inhibitors.
4- protease inhibitors.

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10
Q

List the 5 classification of anti-retrovirals?

A

1- reverse transcriptase inhibitors: nucleoside/tide reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs).
2- protease inhibitors.
3- integrase inhibitors.
4- entry/fusion inhibitors.
5- CCR5 receptor antagonist.

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11
Q

NRTIs are ______ - activated by what?

A

Prodrugs - activated by host cell kinases to form triphosphates.

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12
Q

NRTIs _______ _____ reverse transcriptase.

A

NRTIs competitively inhibit reverse transcriptase.

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13
Q

All NRTIs are excreted by _______, except _____ which is metabolized by ______ ___________.

A

All are excreted by kidneys (dose adjustment in renal failure), except abacavir which is metabolized by alcohol dehydrogenase.

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14
Q

All NRTIs may cause which side effects?

A

Lactic acidosis, hepatomegaly and steatosis.

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15
Q

List NRTIs?

A

• Abacavir
• Didanosine
• Emtricitabine
• Lamivudine
• Stavudine
• Tenofovir
• Zalcitabine
• Zidovudine

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16
Q

Which NRTI is a nucleotide (instead of nucleoside) reverse transcriptase inhibitor?

A

Tenofovir.

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17
Q

Which NRTIs need to be converted?

A
  • Zalcitabine.
  • Zidovudine.
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18
Q

List the uses for zidovudine?

A

1-prophylaxis of needle stick injury.
2- prevention of vertical transmission.

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19
Q

List the adverse effects of zidovudine?

A

BM suppression, myopathy, lipodystrophy syndrome, nail hyperpigmentation and lipoatrophy.

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20
Q

Which NTRI’s oral bioavailability increases with food?

A

Tenofovir.

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21
Q

What happens to didanosine’s oral bioavailability with food?

A

Reduced.

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22
Q

List the adverse effects of didanosine?

A

Dose-limiting pancreatitis (max chance), hyperuricemia, optic neuritis, painful sensory peripheral neuropathy, neutropenia, diarrhea.

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23
Q

List the AE of stavudine?

A
  • causes dose limiting peripheral neuropathy.
  • max chance of causing lactic acidosis.
  • most strongly associated with lipodystrophy syndrome.
  • also causes pancreatitis.
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24
Q

What happens in lipodystrophy syndrome?

A
  • hyperlipidemia.
  • hypercholesterolemia.
  • glucose intolerance, and fat redistribution,
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25
Q

What are the best tolerated NRTIs?

A

Lamivudine and Emtricitabine.

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26
Q

What are the advantages of Lamivudine and Emtricitabine?

A

Not associated with peripheral neuropathy or pancreatitis, also effective against Hep B.

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27
Q

List the AE of abacavir?

A

Increases risk of MI, may cause severe hypersensitivity reaction > esp in patients having HLA B5701allele (testing should be done before starting abacavir).

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28
Q

Max risk of pancreatitis is seen with which NRTI?

A

Didanosine.

29
Q

Max risk of peripheral neuropathy is seen with which NRTI?

A

Stavudine.

30
Q

Max risk of lipodystrophy is seen with which NRTI?

A

Stavudine.

31
Q

List NNRTIs?

A

• Delavirdine
• Efavirenz
• Nevirapine
• Etravirine

32
Q

NNRTIs are ________ inhibitors of reverse transcriptase?

A

Non-competitive

33
Q

NNRIs are selective for which type of HIV?

A

HIV-1.

34
Q

List the disadvantages to NNRTIs?

A
  • Resistance develops rapidly.
  • Skin rash is seen with all NNRTIs.
35
Q

List an advantage of NNRTIs?

A

Do not cause lipodystrophy.

36
Q

_____________ and ____________ are CYP450 inducers, whereas _________ is an enzyme inhibitor.

A

Nevirpine and Efavirenz are CYP450 inducers, whereas Delavirdine is an enzyme inhibitor.

37
Q

List protease inhibitors?

A

• Atazanavir
• Darunavir
• Fosamprenavir
• Indinavir
• Lopinavir
• Saquinavir
• Ritonavir
• Nelfinavir
all end with “navir”.

38
Q

How do protease inhibitors work?

A

Inhibit post-translational modification of viral proteins.
PIs inhibit CYP3A4, thus inhibit metabolism of several drugs.

39
Q

List another application of Ritonavir?

A

In low doses can be used with other PIs to increase their plasma concentration > ‘Ritonavir boosting’.

40
Q

List an AE of PIs?

A

Metabolic abnormalities (including lipodystrophy syndrome) because all PIs are metabolized in the liver.

41
Q

Which PI is devoid of metabolic abnormalities?

A

Atazanavir, because it’s metabolized by alcohol dehydrogenase.

42
Q

List an entry inhibitor?

A

Efuvirtide.

43
Q

How can Enfuvirtide works?

A

Binds to Gp41 subunit of HIV envelope protein and inhibits fusion of viral and host cell membranes, prevents entry of the virus in the host cells.

44
Q

List disadvantages of Enfuvirtide?

A

Used SC and can cause injection site reactions, hypersensitivity and pneumonia.
Not effective against HIV-2.

45
Q

List a CCR5 co-receptor antagonist?

A

Maraviroc.

46
Q

What is the first CCR5 co-receptor antagonist to be approved for use?

A

Maraviroc.

47
Q

What is the route of administration of Maraviroc?

A

Given orally.

48
Q

What is Maraviroc used for?

A

Only effective against CCR5-tropic virus, this type of HIV-1 virus tends to predominate early in infection.

49
Q

List integrase inhibitors?

A

• Raltegravir
• Elvitegravir
• Dolutegravir

50
Q

___________ is a new drug that inhibits the metabolism of ____________. It is approved as a booster for this drug.

A

Cobicistat is a new drug that inhibits the metabolism of Elvitegravir. It is approved as a booster for this drug.

51
Q

List the WHO guidelines for Anti-retroviral therapy (ART)?

A

ART should be started in all HIV patients regardless of WHO clinical stage and at any CD4 cell count.

52
Q

Which type of therapy is recommended for HIV patients?

A

Highly active anti-retroviral therapy (HAART) , it’s recommended with the primary goal of complete suppression of viral replication (viral copies < 50 copies/mL).

53
Q

What is the standard combination ART regimens?

A

standard combination ART regimens: 2 NRTI + NNRTI/Protease inhibitor (PI)/ integrase inhibitor (II).

54
Q

What is the preferred first line ART for adults?

A

Tenofovir + Lamivudine (or Emtricitabine) + Efavirenz
( 2 NRTI + 1 NNRTI/II).

55
Q

What is the second line ART for adults?

A

2 NRTI + PI.

56
Q

What is the preferred first line ART for adolescents?

A

Tenofovir + Lamivudine (or Emtricitabine) + Efavirenz
Or
Tenofovir + Lamivudine (or Emtricitabine) + Dolutegravir
(2 NRTI + 1 NNRTI/II)

57
Q

What is the second line ART for adolescents?

A

2 NRTI + PI

58
Q

What is the preferred first line ART for children (3-10 years)?

A

Abacavir + Lamivudine + Efavirenz
(2 NRTI + 1 NNRTI)

59
Q

What is the second line ART for children (3-10 years)?

A

2 NRTI + PI (or RAL(Raltegravir))

60
Q

What is the preferred first line ART for children (<3 years)?

A

Abacavir + Lamivudine + Lopnivair + Ritonavir (ritonavir boosting)
(2 NRTI + 1 PI/II)

61
Q

What is the second line ART for children (<3 years)?

A

2 NRTI + RAL (Raltegravir)

62
Q

Post-exposure prophylaxis for HIV is continued for ____ days and should start within ___ hours of exposure

A

Continued for 28 days and should start within 72 hours of exposure.

63
Q

What is preferred post-exposure prophylaxis of HIV for adults and adolescents?

A

Tenofovir + Lamivudine + PI

64
Q

What is alternative post-exposure prophylaxis of HIV for adults and adolescents?

A

Raltegravir or Efavirenz are alternatives to PI.
So it becomes (Tenofovir + Lamivudine + Raltegravir or Efavirenz)

( preferred is T + L + PI).

65
Q

What is preferred post-exposure prophylaxis of HIV for children <10 years?

A

Zidovudine + Lamivudine + Lopinavir.

66
Q

What is alternative post-exposure prophylaxis of HIV for children < 10 years?

A

Abacavir can be used for zidovudine.
So it becomes (Zidovudine + Lamivudine + Abacavir)

67
Q

What if prophylaxis of HIV for infants?

A

Zidovudine + Nevirapine for 6 weeks.

68
Q

List anti-HIV combinations that should not be used? And why?

A

1- Zidovudine + Stavudine: pharmacological antagonism (compete for the intracellular phosphorylation).
2- Atazanavir + Indinavir: additive unconjugated hyperbilirubinemia.
3- Didanosine/Stavudine + Zalcitabine: additive peripheral neuropathy.

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