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Pharm Exam 4 > Anti-HIV drugs > Flashcards

Anti-HIV drugs Flashcards

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1
Q

HIV -infection process:

A
  • Attachment
  • Fusion
  • Reverse transcription (ssRNA)
  • Integration
  • Genome replication/Transcription
  • Budding
  • Protein cleavage –> mature viron
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2
Q

NRTI (Nucleoside reverse transcriptase inhibiors) antivirals:

A 
Zidovudine
Lamivudine
Abacavir
Tenofovir
Emtricitabine
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3
Q

NNRTI (non-Nucleoside reverse transcriptase inhibiors) antivirals:

A

nevirapine

efavirenz

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4
Q

Fusion inhibitor antivirals:

A

enfuvirtide

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5
Q

PI (protease inh) antivirals:

A

ritonavir

atazanavir

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6
Q

Co-receptor antagonist antivirals:

A

maraviroc

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7
Q

Integrase inh antivirals:

A

raltegravir

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8
Q

Attachment stage messes with

A

with Co-receptor antagonists (MARAVIROC)

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9
Q

Nucleoside reverse transcriptase inhibiors

  • MOA
  • target
A
  • reverse transcriptase
  • minic nucleotides to inhibit NT binding = chain termination when incorporated into DNA
  • use cellular kinases to convert to triphos form

(also used for HEP B bc it has a reverse transcriptase)

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10
Q

Nucleoside reverse transcriptase inhibiors

-adverse:

A
  • lactic acidosis
  • fatty liver disease
  • lipodystrophy
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11
Q

Abacavir

  • drug type:
  • administration:
  • adverse?
A
  • Nucleoside reverse transcriptase inhibiors
  • ORAL
  • alergic rxn (life threatening) HLA-B5707 - MUST SCREEN PRIOR TO USE
  • cardiac events
  • usual stuff + pancreatitis
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12
Q

Abacavir

  • type?
  • MOA?
  • therapeutic indications?
A

1) Nucleoside reverse transcriptase inhibiors
2) minic nucleotides to inhibit NT binding = chain termination when incorporated into DNA
3) new and long term HIV +

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13
Q

Lamivudine

  • type?
  • administration?
  • Ae?
A

1) cytosine analogue NRTI
2) ORAL - SHORT t1/2
3) least toxic of antiretro drugs
- high doses = GI and CNS effects

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14
Q

Lamivudine

  • therapeutic indication
  • MOA?
A

1) new and long term HIV+
- short term safety in pregnant mothers and neonates
- Chronic HBV (with interferon)
2) minic nucleotides to inhibit NT binding = chain termination when incorporated into DNA

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15
Q

Emtricitabine

  • type
  • administration
  • AE?
A

1) fluorinated analogue of lamivudine - NRTI
2) ORAL - long T1/2
3) Usual + rash ,hyperpigment of palms and soles

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16
Q

hyperpigmentation of palms and soles AE - which drug?

hyperpigmentation of nails AE -which drug?

A
  • palms and soles = emtricitabine

- nails = zidovudine

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17
Q

Emtricitabine

-Therapeutic indication

A
  • new and long term HIV+

- Do not use in children, pregnant women, or renal or hepatic failure

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18
Q

Tenofovir

  • type?
  • administration?
A

1) nucleotide analogue of adenosine - NRTI
2) Oral - but poor bioavailability
- -> must give prodrug (tenofovir + disoproxil)

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19
Q

Lamuvidine vs emtricitabine vs tenofovir

-which is ok for children and pregnant mothers?

A
  • lamivudine is ok short term
  • Zidovudine & Nevirapine = prevents vertical transmission
  • atazanavir - ok for 6+ years

-tenofovir, emtricitabine, and efavirenz are NOT ok.

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20
Q

Tenofovir

  • Ae?
  • Therapeutic indications?
A

1) GI
- renal & bone tox (fanconi synd)
- Crosses placenta - dec bone/fetal growth
2) new and long term HIV+
- chronic HBV

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21
Q

Which HIV drugs are also good for chronic HBV?

A

Tenofovir

Lamuvidine

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22
Q

Zidovudine (AZT)

  • type?
  • administration?
  • AE?
A

1) deoxythymidine analogue - NRTI
2) ORAL - 2x dosing
3) myelosuppression
- usual stuff + hyperpigmentation of nails

23
Q

Zidovudine (AZT)

-Therapeutic indications:

A
  • new and long term HIV+
  • helps prevent vertical transmission
  • post exposure prophylaxis
24
Q

Deoxythymidine analog NRTI?

A

zidovudine

25
Q

nucleotide analogue of adenosine - NRTI?

A

Tenofovir

26
Q

fluorinated analogue of lamivudine - NRTI?

A

emtricitabine

27
Q

cytosine analogue NRTI?

A

lamivudine

28
Q

Post exposure HIV prophylaxis - which drug?

A

-zidovudine

29
Q

non-Nucleoside reverse transcriptase inhibiors

  • target?
  • MOA?
  • activation?
  • Activity?
A
  • reverse transcriptase
  • bind to NON-ACTIVE-site spot on enzyme
  • NO PHOSPHORYLATION REQUIRED (the NRTIs need phos)
  • Not helpful against HIV-2
30
Q

NNRTIs

-AE of this class?

A
  • *-Drug-drug interactions due to cytochrome P450 enzymes
  • Rash
  • Steven johnson
  • hep-toxic
31
Q

NRTI vs NNRTI?

A
  • active site vs non active site bindng
  • phosphorylation vs no phosph needed
  • active against all HIV vs not good with HIV 2
32
Q

Efavirenz

  • type?
  • administration
  • AE?
A
  • 1,4 dihydro 2h …. NNTRI
  • 1x daily ORAL-empty stomach
  • CNS, rash, liver enzymes+,… usual
  • induces CYP3A4s of P450s
  • teratogenic!
33
Q

Efavirenz

-Therapeutic indication:

A
  • New and long term HIV+

- DO NOT GIVE DURING PREGNANCY - teratogenic

34
Q

Nevirapine

  • type
  • administration
  • ae?
A
  • dipyridodiazeinone NNRTI
  • ORAL
  • Rash, hepatitis (fulminnant)
35
Q

Nevirapine

-indications?

A
  • new and long term HIV+

- prevent vertical transmission

36
Q

Drugs that prevent vertical transmission of HIV?

A

nevirapine

Zidovudine

37
Q

Protease inh

  • MOA?
  • AE generaL?
A
  • block maturation of viron particles after budding
  • drug interactions due to alteration of P450s
  • NEEDS ACID TO BE ACTIVE - NO PPI or antiacids
38
Q

Atazanavir

  • type?
  • administration
  • AE?
A
  • Protease inh
  • oral 1x/day - take with food
  • GI, headache, rash, indirect bilirubinemia, heart
  • inhibitor of P450s
39
Q

Atazanavir

-therapeurtic indications?

A
  • new and long term HIV+

- Ok in children 6+

40
Q

Ritonavir

  • type?
  • administration
  • AE?
A
  • protease inh
  • oral!
  • **-potent inh of P450s
  • GI, hepatitis…
41
Q

Ritonavir

-indications for use?

A
  • used in combo!
  • used in low doses asa booster to increase half-ife of co-administered with ARV drugs to prevent metabolism of the active HIV drug - inc halflife (DUE TO POTENT INH OF P450S)
42
Q

2 receptors needed for HIV to enter cell?

A
  • CD4

- CCR5 OR CXCR4

43
Q

Maraviroc

  • type?
  • adminisitration?
  • AE?
A
  • Co-receptor agonist - blocks entry into cell
  • oral
  • Cough, URT infection
  • Allergic Rxn
  • cardiac in susceptible patients
44
Q

Maraviroc

-Indications?

A

-patients with CCR5 tropic virus - MUST SCREEN FOR TROPISM

45
Q

Fusion inhibitor drug:

  • Drug name?
  • MOA?
A
  • Efuvirtide

- gp41 is fusion protein –> drug binds to gp41 so binding/structural change cant happen

46
Q

Efurvirtide

  • type?
  • administration?
  • AE?
A
  • amino acid fusion inh
  • ONLY PARENTERAL ANTIRETROVIRAL!
  • pain at site of inj
  • insomnia headache,…
  • bacterial pneumonia
47
Q

Efurvirtide

-indications?

A

-oNLY for long term HIV+ - experienced patients with HIV replication even with ARV treatemnt (resistance)

48
Q

Integrase inh

  • MOA?
  • Drug name?
A
  • binds to HIV integrase and prevents DNA strand transfer

- Ralteravir

49
Q

What is the only antiretroviral drug that is administered via parenteral route?

A

-Enfuvirtide - fusion inh

50
Q

Which drug is only given to experienced HIV+ patients who still have HIV replcation even with ARV treatment?

A

-Enfuvirtide - fusion inh

51
Q

Raltegravir

  • type drug?
  • administration?
  • Adverse?
A
  • Integrase INH
  • ORAL
  • myopathy, rhabdomyolysis,
  • creatine kinase inc
  • headache, insomnia…
52
Q

Raltegravir

-indications?

A

-new and long term HIV+

53
Q

Standard care for ARV therapy?

A

-3 ARV drugs - at least 2 from different classes

Pharm Exam 4 (10 decks)

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