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Pharmacology > ARVS > Flashcards

ARVS Flashcards

1
Q

ARV classes and key names?

A
  1. Nucleoside.nucleotide reverse transcriptase inhibitors(NRTI)-“Dine”, “Bine”, “vir”(@ the end)
  2. Non-nucleoside reverse transcriptase inhibitors (NNRT)-“vir” in the middle
  3. Protease inhibitors(PIs)-“navir”
  4. Intergrase inhibitors-“Teger”
  5. Fusion inhibitor
  6. CCR5 Antagonist
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2
Q

Nucleoside nucleotide reverse transcriptase inhibitors(NRTI) drugs`/

A

D-E-A-L-S–T-Z

Didanosine

Emtricitabine (FTC)

Abacavir (ABC)

Lamivudine
(3TC)

Stavudine

  1. Tenofovir (TDF)
  2. Zidovudine (AZT, ZDV)
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3
Q

NRTI MOA?

A

Resemble nucleosides/nucleotides naturally used in DNA synthesis

Compete with host nucleotides to serve as the substrate for chain elongation by reverse
transcriptase

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4
Q

NRTI activation?

A

Must undergo intracellular activation to become active

Nucleoside analogs=Triphosphorylation

Nucleotide analog=Diphosphorylation

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5
Q

NRTI S/E?

Specify for Tenofovir(3), Zidovudine(1), Abacavir(1) and others(4)?

A

Tenofovir:
1. Nephrotoxicty
2. Fanconi syndrome
3. Bone demineralization disorders

Zidovudine:
1. Anemia

Abacavir:
1. Fatal hypersensitivity
(HLA-B*5701 gene)

All others:
1. Peripheral neuropathy
2. Lactic acidosis
3. Pancreatitis
4. LIpodystrophy,

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6
Q

NNRTIs drugs?

A

“vir”

  1. Efavirenz,
  2. Nevirapine
  3. Etravirine
  4. Rilpivirine
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7
Q

NNRTIs MOA?

A

1.Binding site of NNRTIs is different from that of NRTIs. Inhibit HIV reverse transcriptase

  1. Do not compete with nucleoside triphosphates.
  2. Do not require intracellular activation
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8
Q

NNRTIs A/E-3?

Specify three drugs!

A

EFV: abnormal dreams, psychosis, gynaecomastia, headache, mild to moderate
maculopapular rash

NVP: rash (may be severe or life-threatening - SJS), hepatitis

ETR: rash (may be severe or life-threatening - SJS), triglyceridaemia

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9
Q

Integrase Inhibitors drugs-3?

A

“teger”

  1. Dolutegravir
  2. Raltegravir
  3. Carbotegravir
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10
Q

Integrase Inhibitors drugs MOA?

A
  1. Inhibit viral integrase enzyme
  2. Prevent the transfer of viral DNA strand into host-cell genome
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11
Q

Raltegravir

  1. PK
  2. DI
  3. A/E
  4. Tolerance
A

PK: bioavailability enhanced by food

DI: Rifampicin  ↓ raltegravir plasma levels

A/E: headaches, nausea, fatigue, myopathy, rhabdomyolysis

Tolerance:well-tolerated

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12
Q

Integrase Inhibitors MOA-2?

A
  1. Inhibit viral integrase enzyme
  2. Prevent the transfer of viral DNA strand into host-cell genome
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13
Q

Dolutegravir CI?

A
  • DTG may increase the risk of neural tube defects  avoid preconception
    and in the first 6 weeks of pregnancy
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14
Q

Dolutegravir A/E?-6

A
  1. Tetratogenic
  2. insomnia
  3. weight gain
  4. headache
  5. neuropsychiatric effects
  6. diarrhea
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15
Q

Integrase Inhibitors DI?

A
  1. Antacids & iron supplements → ↓ Decreased DTG plasma conc. → Dose spacing
  2. Anticonvulsants (carbamazepine, phenobarbital, phenytoin) →↓ DTG
    plasma conc. →→ Avoid co-admin if possible
  3. Metformin → ↑↑↑Metforminplasma conc.→Limit metformin dose to max 500 mg 12-hourly
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16
Q

PIs drug-5?

A

“navir”

  1. Lopinavir
  2. Atazanavir
  3. Dorunavir
  4. Saquinavir
  5. Ritonavir
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17
Q

Ritonavir

A

Inhibits CYP3A4 at subtherapeutic doses

Inhibits metabolism of PIs

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18
Q

PIs MOA?

A

Inhibits HIV protease. Prevents cleavage of viral precursor & non-infectious virions

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19
Q

Lopinavir/ritonavir (LPV/r) A/E-4?

A
  1. Hyperglycaemia
  2. diarrhea
  3. dyslipidemia
  4. atherosclerosis
20
Q

Atazanavir/ritonavir (ATV/r) A/E?

A
  1. Jaundice
  2. abdominal pain
21
Q

Atazanavir/ritonavir (ATV/r) usauge?

A

Used if LPV/r is not well tolerated

22
Q

Atazanavir/ritonavir (ATV/r) DI?

A

warfarin→↓ INR→↑ Coagulation

23
Q

Darunavir/ritononavir (DRV/r) DI?

A

warfarin→↓ INR→↑ Coagulation

24
Q

Darunavir/ritononavir (DRV/r) A/E?

A
  1. abdominal pain
  2. fatigue
  3. headache
25
Q

Saquinavir/ritonavir (SQV/r) A/E?

A

Prolonged QT and PR intervals

26
Q

Distinguish differences between DTG and EFV for HIV regimes

A

Check notes

27
Q

First-line regimens formula?

A

2 NRTI + NNRTI or INSTI

28
Q

Preferred first-line regimen?

A

2 NRTI + NNRTI or INSTI

Tenofovir + Lamivudine + Dolutegravir (TLD)
TDF + 3TC + DTG

29
Q

Alternative first-line regimens for patients with TB?

A

Formula: 2 NRTI + NNRTI or INSTI

TDF + FTC + EFV (TEE)

30
Q

Alternative first-line regimens for patients who are pregnant?

A

Formula: 2 NRTI + NNRTI or INSTI

TDF + FTC + EFV (TEE)

31
Q

Alternative first-line regimens for patients who are Contraindications and intolerance to EFV?

A

Normal Formula: 2 NRTI + NNRTI or INSTI

TDF + FTC + DTG (TLD

32
Q

Alternative first-line regimens for patients who are Contraindications with EFV & DTG?

A

Normal Formula: 2 NRTI + NNRTI or INSTI

TDF + 3TC/FTC + LPV/r

33
Q

Second-line Regimens ususage?

A

When Failing on first-line regimen

34
Q

Second-line Regimens formula?

A

Replace with DTG or PI

Zidovudine + (L/e) + Replacement (DTG or PI)

35
Q

Second-line Regimens on Failing on NNRTI-based (TDF+3TC/FTC+EFV/NVP) 1st line regimen?

A

AZT + 3TC + DTG

Zidovudine + Lamivudine + Dolutegravir

36
Q

Second-line Regimens if HBV positive?

A

Continue TDF because withdrawl may cause a fatal hepatitis flare

TDF + 3TC + DTG

Tenofovir+Lamivudine+ DTG

37
Q

Second-line Regimens if HBV positive Contraindication/intolerance to DTG?

A

AZT + 3TC +LPV/r

Zidovudine + Lamivudine + Lopanavir
But,

if HBsAg positive:
TDF + 3TC +LPV/r

38
Q

Second-line Regimens Contraindication/intolerance to TDF & AZT?

A

ABC + 3TC + LPV/r

Abacavir + Lamivudine + Lopinavir/Ritonavir

39
Q

Second-line Regimens failing a InSTI-based (TDF+3TC+DTG) 1st line regimen (>2 years)

A

AZT + 3TC +LPV/r
But,
if HBsAg positive:
TDF + 3TC/FTC +LPV/r

40
Q

Third-line Regimens?

A

Genotypic resistance test

resistance to LPV/r or ATV/r and/or DTG

41
Q

3RD line regime drugs available?

A
  1. PI =Darunavir (DRV)
  2. Integrase inhibitor =Raltegravir (RAL)
  3. NNRTIs= Etravirine (ETR), Rilpivirine (RPV)(MVC)
  4. CCR5 blocker = Maraviroc (MVC)
42
Q

Other drugs for 3rd regime drugs?

MOA

A/E

A

Efuvirtide(Fusion inhibitor)

MOA: Binds gp41 envelope glycoprotein thus preventing viral entry

A/E: Wheezing cough, numbness or tingling sensation

43
Q

PrEP?

A

-2 NRTI

Tenofovir + Emtriceitabine

OR

Tenofovir + Lamivudine

Hepatitis combination with tenofovir

44
Q

Post-exposure Prophylaxis (PEP)

A

TDF + 3TC + DTG

But,

If DTG contraindicated:
TDF + 3TC + ATV/r or LPV/r

If TDF contraindicated or source patient fails on TDF regimen:
AZT + 3TC + DTG
28-day Rx

45
Q

Revise the below:

  1. Combinations to avoid
  2. Mitochondrial toxicity

3.

A

CHECK NOTES

46
Q

Resistance in ART?

A
  1. K103N mutation
    * reduces NVP and EFV susceptibility by about 50 and 20-fold,
    respectively
  2. K103S mutation
    * usually occurs in samples from patients who previously had K103N
    * causes intermediate to high-level resistance to EFV and NVP
  3. K101P mutation
    * Affects all NNRTIs
    WHO, 2022
47
Q

Co-trimoxazole Preventative Therapy(CPT)?

A

Prophylaxis of PJP adn toxoplamisis in HIV patients

Pharmacology (44 decks)

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