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SBL - Exam 2 > HIV Pharmacology > Flashcards

HIV Pharmacology Flashcards

(70 cards)

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1
Q

what is the life cycle of HIV (8 steps)?

A
  1. entry
  2. fusion and uncoating
  3. reverse transcription
  4. integration
  5. transcription
  6. translation
  7. virion assembly
  8. budding and maturation
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2
Q

MOA of miraviroc

A

binds specifically to CCR5 to prevent viral entry into the host cell

  • miraviroc is not efficatious in viruses with a tropism for CCR5 and CXCR4 or just CXCR4
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3
Q

what surface receptors are usually seen in advanced HIV?

A

CXCR4

  • this means miraviroc may not be useful in patients with advanced HIV (it only binds CCR5)
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4
Q

what are the pharmacokinetics of miraviroc?

A
  • oral administration
  • CYP450 metabolism
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5
Q

mechanisms of resistance to miraviroc

A
  1. mutations in the V3 loop of gp120
  2. emergence of CXCR4-tropic virus
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6
Q

what stage of the life cycle does miraviroc act on?

A

fusion

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7
Q

MOA of enfuvirtide

A

binds gp41, preventing the conformational changes needed for fusion of the viral envelope with the host cell membrane

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8
Q

what are the pharmacokinetics of enfuvirtide?

A
  • subcutaneous injection
  • metabolized by proteolytic hydrolysis, without involvement of CYP450
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9
Q

mechanisms of resistance of enfuvirtide

A
  • mutations in gp41 to prevent enfuvirtide binding
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10
Q

adverse effects of enfuvirtide

A
  • local injection site reactions
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11
Q

can NRTIs eradicate virus from cells that are already infected?

A

no, once the cells are infected the virus’ genetic material is integrated into the host cell DNA

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12
Q

what is the mechanism of action of nucleoside/tide reverse transcriptase inhibitors (NRTIs)?

A

competitive inhibition of HIV reverse transcriptase

  • the NRTI is incorporated into the growing DNA, leading to premature chain termination
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13
Q

mechanisms of resistance to NRTIs

A
  • point mutations in HIV reverse transcriptase
  • impaired kinase activity to prevent phosphorylation and subsequent activation (only for nucleosides)
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14
Q

abacavir

A

guanosine nucleoside RT inhibitor

  • drug combinations inculde
    • abacavir + lamivudine
    • abacavir + zidovudine
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15
Q

pharmacokinetics of abacavir

A

metabolized by alcohol dehydrogenase

  • serum levels of abacavir can be increased with concurrent ingestion of EtOH
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16
Q

adverse effects of abacavir

A

hypersensitivity (consitutional sx, respiratory sx, skin rash)

  • do not reintroduce abacavir if hypersensitivity occurs; may cause death
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17
Q

didanosine

A

adenosine nucleoside RT inhibitor

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18
Q

adverse effects of didanosine

A
  • dose-dependent pancreatitis
    • contraindicated in alcoholism and hypertrigyceridemia
  • retinal changes
    • mandated periodic retinal exams
  • lactic acidosis and hepatic steatosis when combined with stavudine
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19
Q

lamivudine

A

cytosine nucleoside RT inhibitor

  • active against HIV and HBV
    • discontinuation could exacertbate HBV symptoms
  • should not be used in conjuction with emtricitabine; since they are related, they select for the same point mutation in HIV reverse transcriptase
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20
Q

emtricitabine

A

cytosine nucleoside RT inhibitor

fluorinated analog of lamivudine

  • active against HIV and HBV
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21
Q

pharmacokinetics of emtricitabine

A

has a long intracellular half-life that allows for once daily dosing

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22
Q

adverse effects of emtricitabine

A
  • constitutional sx
  • hyperpigmentation of the palms and soles
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23
Q

stavudine

A

thymidine nucleoside RT inhibitor

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24
Q

adverse effects of stavudine

A
  • dose-dependent peripheral neuropathy
  • dyslipidemia
  • lactic acidosis and hepatic steatosis when combined with didanosine
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25
zidovudine
deoxythymidine **nucleoside** RT inhibitor
26
adverse effects of **zidovudine**
* macrocytic anemia * neutropenia * constitutional symptoms
27
tenofovir
adenosine **nucleoTide** RT inhibitor * active against HIV and HBV
28
what drugs enhance absorption of **tenofovir**?
**disoproxil** and **alafenamide**
29
MOA of non-nucleoside reverse transcriptase inhibitors **(NNRTIs)**?
binds HIV reverse transcriptase at a site _distant from the active site_ * binding leads to reduced activity * **non-competitive inhibitor**
30
mechanisms of resistance to **NNRTIs**
* point mutations in **HIV reverse transcriptase** that alter NNRTI binding * there is no cross resistance between NNRTIs and NRTIs since they bind such different sites
31
pharmacokinetics of **NNRTIs**
metabolized by CYP450 system
32
delavirdine
first generation NNRTI
33
adverse effects of **delavirdine**
* skin rash * constitutional symptoms * increased aminotransferase levels
34
efavirenz
first generation NNRTI
35
pharmacokinetics of efavirenz
can only be given once daily d/t **increased t1/2**
36
adverse effects of efavirenz
* **CNS symptoms** - dizziness, drowsiness, insomnia, nightmares, HA * skin rash
37
nevirapine
first generation NNRTI * used in preventing transmission of HIV from mother to child * single dose to mother at onset of labor, and a dose to the baby within 3 days after birth
38
adverse effects of **nevirapine**
* rash (can be dose-limiting) * liver toxicity
39
etravirine
second generation NNRTI * increased potency, increased t1/2, and less adverse effects * has a higher genetic barrier to resistance; designed to overcome resistance to first generation NNRTIs
40
pharmacokinetics of **etravirine**
metabolized by CYP450 system * _induces_ CYP3A4 * _inhibits_ CYP2C9 and CYP2C19
41
rilpivirine
second generation NNRTI * increased potency, increased t1/2, and less adverse effects * coformulated with **emtricitabine** + **tenofovir**; allows for once daily oral administration
42
adverse effects of **rilpivirine**
* rash, depression, HA, insomnia, **increased serum aminotransferases** * high doses associated with **QT prolongation**
43
what stage of the HIV life cycle do integrase strand transfer inhibitors **(INSTIs)** work at?
integration
44
MOA of integrase strand transfer inhibitors **(INSTIs)**
bind HIV integrase to inhibit strand transfer and ligation of reverse-transcribed HIV DNA into the chromosomes of the host cell
45
dolute**_gravir_**
integrase strand transfer inhibitor (INSTI) * used for treatment of naïve patients in combination with: * tenofovir + emtricitabine * abacavir + lamivudine
46
elvite**_gravir_**
integrase strand transfer inhibitor (INSTI) * only available as a combination pill * elvitegravir + cobicistat + emtricitabine + tenofovir * requires **boosting** with cobicistat
47
ralte**_gravir_**
integrase strand transfer inhibitor (INSTI) * preferred treatment for treatment naïve patients
48
what stage of the HIV life cycle do **protease inhibitors** work on?
budding and maturatino
49
MOA of **protease inhibitors**
competitively inhibit **HIV aspartyl protease** to prevent maturation of final structural proteins that make up the mature virion core * prevents production of gag and pol polypeptides
50
adverese effects of **protease inhibitors**
* GI intolerance (can be dose-limiting) * **lipodystrophy** * **​**metabolic - hyperglycemia + hyperlipidemia * morphologic - lipoatrophy + fat depositino * redistribution and accumulation of body fat * central obesity, buffalo hump, facial wasting, breast enlargment, cushingoid appearance
51
pharmacokinetics of **protease inhibitors**
* metabolized by CYP450 system * **ritonavir** has the _strongest_ inhibitory effect on CYP3A4 * **saquinavir** has the weakest
52
ataza**_navir_**
protease inhibitor * **once daily** dosing
53
adverse effects of **atazanavir**
* diarrhea and nausea * skin rash * **not associated with dyslipidemia or hyperglycemia** (unlike most protease inhibitors)
54
pharmacokinetics of **atazanavir**
_inhibits_ CYP3A4, CYP2C9, UGT1A1
55
daru**_navir_**
protease inhibitor * must be boosted with **ritonavir** or **cobicistat**
56
adverse effects of **darunavir**
sulfa drug
57
fosampre**_navir_**
protease inhibitor
58
adverse effects of **fosamprenavir**
sulfa drug * personal parasthesias * depression
59
indi**_navir_**
protease inhibitor
60
adverse effects of **indinavir**
**un**conjugated _hyperbilirubinemia_ and _nephrolithiasis_ * consuming 1.5L of water each day helps prevent kidney stones
61
pharmacokinetics of **indinavir**
boosting with **ritonavir** allows for _twice daily dosing_ * this carries increased risk for kidney stones--drink lots of water!
62
lopi**_navir_**
protease inhibitor * available only in combination with low-dose **ritonavir**
63
nelfi**_navir_**
protease inhibitor
64
rito**_navir_**
protease inhibitor
65
pharmacokinetics of **ritonavir**
* at standard dosing for protease inhibitors, it has a high rate of GI side effects * very potent CYP450 _inhibitor_; used primarily as a **booster** * lower doses are used for _inhibition_ of CYP3A4
66
saqui**_navir_**
protease inhibitor * formulated for **once daily** dosing with **ritonavir**
67
tipra**_navir_**
protease inhibitor * **_indicated in patients resistant to other protease inhibitors_** * combined with **ritonavir**
68
adverse effects of **tipranavir**
sulfa drug
69
what is highly active antiretroviral therapy **(HAART)**?
combinations of 3-4 drugs used to treat HIV and prevent resistance by inhibiting various steps of the life cycle
70
what drug combinations are used in HAART?
**2 NRTIs** plus either: * 1 protease inhibitor (sometimes 2 for boosting) * 1 NNRTI * 1 INSTI

SBL - Exam 2 (5 decks)

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