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Pharm Exam 4 > Anti-HIV drugs > Flashcards

Anti-HIV drugs Flashcards

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
nucleotide analogue of adenosine - NRTI?
Tenofovir
26
fluorinated analogue of lamivudine - NRTI?
emtricitabine
27
cytosine analogue NRTI?
lamivudine
28
Post exposure HIV prophylaxis - which drug?
-zidovudine
29
non-Nucleoside reverse transcriptase inhibiors - target? - MOA? - activation? - Activity?
- reverse transcriptase - bind to NON-ACTIVE-site spot on enzyme - NO PHOSPHORYLATION REQUIRED (the NRTIs need phos) - Not helpful against HIV-2
30
NNRTIs | -AE of this class?
* *-Drug-drug interactions due to cytochrome P450 enzymes - Rash - Steven johnson - hep-toxic
31
NRTI vs NNRTI?
- active site vs non active site bindng - phosphorylation vs no phosph needed - active against all HIV vs not good with HIV 2
32
Efavirenz - type? - administration - AE?
- 1,4 dihydro 2h .... NNTRI - 1x daily ORAL-empty stomach - CNS, rash, liver enzymes+,... usual - induces CYP3A4s of P450s - teratogenic!
33
Efavirenz | -Therapeutic indication:
- New and long term HIV+ | - DO NOT GIVE DURING PREGNANCY - teratogenic
34
Nevirapine - type - administration - ae?
- dipyridodiazeinone NNRTI - ORAL - Rash, hepatitis (fulminnant)
35
Nevirapine | -indications?
- new and long term HIV+ | - prevent vertical transmission
36
Drugs that prevent vertical transmission of HIV?
nevirapine | Zidovudine
37
Protease inh - MOA? - AE generaL?
- block maturation of viron particles after budding - drug interactions due to alteration of P450s - NEEDS ACID TO BE ACTIVE - NO PPI or antiacids
38
Atazanavir - type? - administration - AE?
- Protease inh - oral 1x/day - take with food - GI, headache, rash, indirect bilirubinemia, heart - inhibitor of P450s
39
Atazanavir | -therapeurtic indications?
- new and long term HIV+ | - Ok in children 6+
40
Ritonavir - type? - administration - AE?
- protease inh - oral! * **-potent inh of P450s - GI, hepatitis...
41
Ritonavir | -indications for use?
- 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
2 receptors needed for HIV to enter cell?
- CD4 | - CCR5 OR CXCR4
43
Maraviroc - type? - adminisitration? - AE?
- Co-receptor agonist - blocks entry into cell - oral - Cough, URT infection - Allergic Rxn - cardiac in susceptible patients
44
Maraviroc | -Indications?
-patients with CCR5 tropic virus - MUST SCREEN FOR TROPISM
45
Fusion inhibitor drug: - Drug name? - MOA?
- Efuvirtide | - gp41 is fusion protein --> drug binds to gp41 so binding/structural change cant happen
46
Efurvirtide - type? - administration? - AE?
- amino acid fusion inh - ONLY PARENTERAL ANTIRETROVIRAL! - pain at site of inj - insomnia headache,... - bacterial pneumonia
47
Efurvirtide | -indications?
-oNLY for long term HIV+ - experienced patients with HIV replication even with ARV treatemnt (resistance)
48
Integrase inh - MOA? - Drug name?
- binds to HIV integrase and prevents DNA strand transfer | - Ralteravir
49
What is the only antiretroviral drug that is administered via parenteral route?
-Enfuvirtide - fusion inh
50
Which drug is only given to experienced HIV+ patients who still have HIV replcation even with ARV treatment?
-Enfuvirtide - fusion inh
51
Raltegravir - type drug? - administration? - Adverse?
- Integrase INH - ORAL - myopathy, rhabdomyolysis, - creatine kinase inc - headache, insomnia...
52
Raltegravir | -indications?
-new and long term HIV+
53
Standard care for ARV therapy?
-3 ARV drugs - at least 2 from different classes

Pharm Exam 4 (10 decks)

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