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MNI (immuno pharm) > L23- Antiretroviral Drugs, HIV > Flashcards

L23- Antiretroviral Drugs, HIV Flashcards

1
Q

describe the 4 F’s of HIV progression

A

Flu-like Sxs (acute HIV)
Feels fine (chronic latent HIV, asymptomatic)
Falling T cell count (<200 = AIDS)
Final crisis

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2
Q

HIV treatment goals:

  • (1) generally for patient
  • (2) in terms of function and lab values
  • (3) in terms of prevention
A

1- reduce HIV related morbidity, prolong survival, improve quality of life

2- restore/preserve immune function, maximally suppress viral load (<50 copies/mL = undetectable)

3- prevent vertical transmission

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3
Q

(1) % chance of vertical transmission of HIV w/o Tx

(2) % with Tx

A

1- 20-30% (no Tx)

2- <0.5% (w/ Tx)

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4
Q

describe HAART

A

highly active antiretroviral treatment:

-3 active drugs from at least 2 drug classes (of the 6 classes)

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5
Q

anti-HIV therapy is usually initiated when…. (in uncomplicated cases)

A

CD4 T cell count <500 cells/mm^3

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6
Q

list the situations where there is urgency to initiate anti-HIV therapy

A

-Pregnancy- to avoid vertical transmission

  • AIDS defining conditions
  • acute opportunistic infections
  • HIV-associated nephropathy (possible CKD)
  • lower CD4 cell counts
  • acute/early infection
  • HepB or HepC co-infection
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7
Q

HAART:

  • usually undetectable levels of viral load occurs w/in (1) timeframe
  • (2) list the many predictors for successful Tx
A

1- 12-24 wks

2:
-low baseline viral count
ARV therapy:
-high potency
-tolerability
-convenience and excellent adherence to Tx
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8
Q

list the ARV drug classes

A
  • entry / fusion inhibitors
  • NRTIs (nucleoside/tide reverse transcriptase inhibitors)
  • NNRTIs (non-nucleoside/tide RTIs)
  • integrase inhibitors
  • protease inhibitors
  • pharmacokinetic enhancers
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9
Q

list the entry / fusion inhibitors, ARVs

A

Maraviroc- entry

Enfuvirtide- fusion

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10
Q

(1) is the entry inhibitor of HIV by blocking (2) receptor, therefore is only effective in (3) situations.

A

1- maraviroc
2- CCR5 receptor (HIV co-receptor)
3- m-tropic phase // early infection (before transition to t-tropic / CXCR4)

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11
Q

Maraviroc:

  • (1) metabolism
  • (2) route of administration
  • (3) AEs
A

1- CYP3A4
2- oral
3- well-tolerated, some risk for hepatotoxicity

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12
Q

(1) is the fusion inhibitor of HIV by (2) mechanism. It is approved for (3) uses.

A

1- enfuvirtide
2- resembles gp41 structure –> inhibits function
3- treatment experienced adults (previously on ARVs) with evidence of viral replication ++++ only for HIV-1 Tx

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13
Q

______ is the only ARV not given orally

A

enfuvirtide, fusion inhibitor / gp41 analog

-given SQ

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14
Q

Enfuvirtide:

  • (1) AEs
  • (2) importantly absent AE
A

1- Injection related –> hypersensitivituy reactions and eosinophilia rarely occur

2- no drug interactions

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15
Q

list the NRTIs

A

(nucleo-side/tide reverse transcriptase inhibitors) – st. zelda

  • stavudine
  • tenofovir
  • zidovudine
  • emtricitabine
  • lamivudine
  • didanosine
  • abacavir
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16
Q

NRTIs:

  • (1) key structural feature related to function
  • (2) is the key risk with monotherapy (hint- kinda 2 things)
  • (3) general metabolism feature
A

1- lacks 3’-OH –> stops transcription / chain termination

2- rapid resistance —> cross-resistance to other NRTIs

3- most are not metabolized by cytochrome enzymes => no drug interactions

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17
Q

NRTIs stop DNA transcription which importantly includes (1) and can lead to (2) AEs.

  • (3) are the other common AEs
  • (4) are the rare, but fatal AEs
A

1- inhibition of mitochondrial DNA polymerase
2- peripheral neuropathy, myopathy, lipoatrophy, lactic acidosis

3- pancreatitis, myelosuppression, cardiomyopathy

4- hepatotoxicity (lactic acidosis, hepatomegaly w/ steatosis)

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18
Q

______ NRTIs are associated with dyslipidemia and insulin resistance

A
  • zidovudine

- stavudine

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19
Q

NRTI, Stavudine:

  • (1) analog
  • (use/avoid)
  • (3) AEs
A

1- thymidine

2- avoid (‘stabs you in the back with AEs– high mitochondrial DNA polymerases)

3- peripheral neuropathy, lactici acidosis, hyperlipidemia, neuromuscular weakness

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20
Q

______ is the only nucleotide analog (all others are nucleosides)

21
Q

NRTI, Tenofovir:

  • (1) analog
  • (use/avoid)
  • (3) common AEs
  • (4) is monitored
A

1- adenosine (only nucleotide analog)

2- use

3- upset GI (common in lactose intolerant patients)

4- serum creatinine for renal insufficiency

22
Q

______ is the only NRTI with significant drug interactions, describe common interactions with other ARVs

A

tenofovir (only nucleotide analog)

  • inc [didanosine] –> dec dosage
  • dec [atazanavir] –> inc dosage
23
Q

NRTI, Zidovudine:

  • (1) analog
  • (use/avoid)
  • (3) AEs
A

1- thymidine

2- avoid — except 1st line for pregnant Pts (best at preventing vertical transmission

3- neutropenia, macrocytic anemia (bone marrow suppression), lipoatrophy —- avoid with Stavudine

24
Q

NRTI, Lamivudine:

  • (1) analog
  • (use/avoid)
  • (3) AEs
  • (4) importantly absent mechanism
A

1- cytosine

2- avoid

3- HA, dry mouth, high level resistance

4- no effect on mitochondrial DNA polymerase or bone marrow precursor cells

25
Q

NRTI, Emtricitabine:

  • (1) analog
  • (use/avoid)
  • (3) AEs
A

1- cytosine

2- use

3- hyperpigmentation on palms/soles, 1-3% of Pts, more in darker skin

26
Q

NRTI, Didanosine:

  • (1) analog
  • (use/avoid)
  • (3) AEs
A

1- adenosine

2- avoid (high affinity mitochondrial DNA polymerase)

3- *pancreatitis (–> death), peripheral neuropathy, diarrhea, hepatic dysfunction, CNS effects

27
Q

NRTI, Abacavir:

  • (1) analog
  • (use/avoid)
  • (3) AEs
  • (4) is necessary before use
A

1- guanosine

2- use, slow development of resistance — *avoid in cases with HLA-B57.01 => hypersensitivity rxns

3- *hypersensitivity rxns (if predisposed), GI upset, HA, dizziness

4- *genetic testing

28
Q

list the NNRTIs

A

(non-nucleo-side/tide reverse transcriptase inhibitors)

  • rilpivirine
  • efavirenz
  • nevirapine
29
Q

NNRTIs:

  • (1) discuss general usage
  • (2) discuss general AEs
A

1- ONLY for HIV-1, largely avoided but still used b/c cheap

2- skin rash (SJS = steven-johnson syndrome, TEN = toxic epidermal necrolysis), GI intolerance

30
Q

what are the main concerns and disadvantages with usage of NNRTIs

A

1) resistance + cross-resistance with other NNRTIs –> mutations in the NNRTI pocket that bids the drugs
2) drug interactions –> induction and inhibition of CYPs
3) high incidences of hypersensitivity rxns

31
Q

what are the main advantages of with usage of NNRTIs

A
  • lacks effects on blood forming elements (bone marrow precursors)
  • lacks cross-resistance with NRTIs (different binding sites)
32
Q

NNRTI, Nevirapine:

  • (use/avoid)
  • (2) AEs
  • (3) metabolism
  • (4) previous use, explain
A

1- avoid (all NNRTIs) – if used, titrate dose

2- severe hepatotoxicity (not for women T cell count >250, men >400)

3- urine metabolites via CYP3A4, CYP2B6

4- single does to prevent vertical transmission b/c most effective —- but pregnancy is predisposition for hepatotoxicity

33
Q

NNRTI, Efavirenz:

  • (use/avoid)
  • (2) AEs
  • (3) are monitored
A

1- avoid (all NNRTIs)

2:

  • CNS toxicities (50%): dizziness, drowsiness, insomnia, nightmares / vivid dreams, HA
  • Psychiatric disturbances: depression, mania, psychosis, *suicide
  • Rash (25%)

3- TGs, HDL, LDL, total cholesterol

34
Q

NNRTI, Rilpivirine:

  • (use/avoid)
  • (2) AEs
A

1- avoid in general — use in pregnancy

2- rash, depression, HA, insomnia, elevated LFTs + creatinine (reversible)
-QT prolongation at high doses

35
Q

list the integrase inhibitors

A

bictegravir
raltegravir
elvitegravir
dolutegravir

36
Q

describe the AEs of Integrase Inhibitors

A

For All: GI upset, rash

Raltegravir- slight inc in CK (creatinine phosphokinase)

37
Q

Integrase Inhibitors:

  • (1) are metabolized by CYP3A4
  • (2) are metabolized by UGT1A1
A

1- bictegravir, elvitegravir, dolutegravir

2- bicetegravir, *raltegravir, dolutegravir

38
Q

______ integrase inhibitor requires co-administration with PK enhancers

A

elvitegravir

39
Q

(1) integrase inhibitor is recommended for pregnant Pts

(2) integrase inhibitor is contraindicated in pregnancy

A

1- raltegravir

2- dolutegravir (neural tube defects)

40
Q

list protease inhibitors (indicate specific enzyme)

A

*inhibits HIV aspartyl protease

  • lopinavir
  • indinavir
  • nelfinavir
  • darunavir
  • atazanavir
41
Q

Protease Inhibitors:

  • (good/poor) bioavailability
  • high fat meals inc F for (2) and dec F for (3)
  • (4) is a key associated risk
  • (5) is also usually required
A 
1- poor F
2- nelfinavir
3- indinavir
4- drug interactions - high potential
5- requires PK enhancers
42
Q

list the AEs for protease inhibitors

A
  • GI upset
  • paresthesia

-*lipid metabolism disturbances: hypertriglyceridemia, hypercholesterolemia, DM –> contraindications

***Fat redistribution / accumulation – Cushing Syndrome: central obesity, buffalo hump, facial / peripheral wasting, breast enlargement, Cushingoid appearance

43
Q

Protease Inhibitors:

  • (1) is not associated with dyslipidemia and hyperglycemia, but may cause PR prolongation
  • (2) should be avoid with EtOH as it can lead to disulfiram rxn
  • (3) may precipitate a Sulfa allergy
  • (4) can lead to unconjugated hyperbilirubinemia and or nephrolithiasis
A

1- atazanavir
2- lopinavir
3- darunavir
4- indinavir

44
Q

list the pharmacokinetic enhancers

A

cobicistat

ritonavir

45
Q

PK enhancers have (1) activity in order to improve (2) and (3) of other ARVs in order to change (4) in terms of ARV therapy

A

1- inhibits CYP3A4
2- inc ARV plasma concentration
3- inc tolerability
4- lower and less frequent dosing

46
Q

PreP = (1):

-(2) effectiveness

A

Pre-Exposure Prophylaxis- combination NRTIs

  • emtricitabine
  • tenofovir

-99% effective via sex, 74% effective via IV drug use

47
Q

Post-exposure prophylaxis = ______

A

1) emtricitabine + tenofovir + dolutegravir
2) emtricitabine + tenofovir + raltegravir

-given for 28 days or until source is shown to be HIV-negative

48
Q

list the regimens usually used initially in HIV patients

A

[2 NRTIs + 1 integrase inhibitor]

1) emtricitabine + tenofovir + bicetegravir
2) emtricitabine + tenofovir + dolutegravir
3) emtricitabine + tenofovir + raltegravir
4) abacavir + lamivudine + dolutegravir

49
Q

describe the HIV treatment for newborns

A
  • 4-6 wk prophylaxis
  • Nevirapine + Zidovudine

-nevirapine hepatotoxicity not as prevalent in infants

MNI (immuno pharm) (15 decks)

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