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Pharmacology > Antiretrovirals > Flashcards

Antiretrovirals Flashcards

1
Q

What are Nucleoside/Nucleotide Reverse Transcriptase Inhibitors NRTIs

A

Analogues of nucleotides/nucleosides that inhibit Reverse transcriptase Enzymes

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2
Q

Name the NRTIs

A

Abacavir: ABC
Emtricitabine: FTC
Lamivudine: 3TC
Tenofovir: TDF
Zidovudine: AZT,ZDV

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3
Q

MOA of NRTIs

A

compete with original host nucleotides binding on active site of reverse transcriptase
–>serve as false substrate–> viral DNA chain elongation and viral replication stops
*require activation

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4
Q

Activation of NRTIs

A

Nucleotide analogue: Diphosphorylation
Nucleoside analogue Triphosphorylation

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5
Q

AEs of Nucleotide analogues

A

TDF: nephrotoxicty
Fanconi’s syndrome
Bone mineralisation disorder

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6
Q

AEs of Nucleoside analogues

A

AZT: anemia
ABC: rash
Peripheral neuropathy
Lactic acidosis
Pancreatitis
Lipdystrophy
NH

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7
Q

Imp. AE of ABC in people wirh HLA-B*5701 gene

A

fatal hypersensitivity rxns

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8
Q

Name the Non-Nucleoside Reverse Transcriptase Inhibitors NNRTIs

A

Efavirenz: EFV
Nevirapine: NVP
Etravirine: ETR
Rilpivirine: RPV

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9
Q

MOA of NNRTIs

A

inhibit HIV Reverse Transcriptase by binding to allosteric site of enzyme

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10
Q

Diff. between NNRTIs and NRTIs

A

NNRTIs bind at different site than NRTIs
NNRTIs do not compete with nucleoside triphosphates
NNRTIs do not require intracellular activation

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11
Q

AEs of EFV

A

Psychosis
abnormal dreams
Gynecomastia
Maculopapular rash

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12
Q

AEs of NVP

A

rash: sever or life threatening- SJS
Heaptitis

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13
Q

AEs of ETR

A

rash: severe or life threatening-SJS
Triglyceridaemia

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14
Q

Which are the Integrase Inhibitors IIs

A

Dolutegravir: DTG
Raltegravir: RAL
Cabotegravir: CAB

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15
Q

MOA of IIs

A

inhibit viral integrase enzyme
–> prevent transfer of viral DNA strand into host-cell genome

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16
Q

AEs of DTG

A

Teratogenic: not used in 1st trimester
Insomnia
weight gain
diarrhea
CNS effects

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17
Q

DIs of DTG

A

Antacids and Fe supplements: decr DTG [plasma]
Anticonvulsants: decr DTG [plasma]
Metformin: incr Metformin conc.

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18
Q

DIs of RAL

A

Rifampicin: decr. RAL plasma levels

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19
Q

AES of RAL

A

generally well tolerated
Headaches
nausea
fatigue
myopathy
rhabdomyolysis

20
Q

Name the Protease Inhibitors PIs

A

Atazanvir: ATV
Lopinavir: LPV
Ritonavir: RTV
Darunavir: DRV
Saquinavir: SQV

21
Q

MOA of PIs

A

inhibit HIV protease
–> prevent cleavage of viral precursor proteins
–> results in immature and non0infectious virions

22
Q

General DIs of PIs

A

drugs metabolised by CYP3A4: ketoconazole, Carbamazepine, diazepam, midazolam, sildenafil= incr. plasma conc.

23
Q

AEs of Lopinavir/ritonavir LPV/r

A

Dyslipidemia
Hyperglycaemia
diarrhea
Atherosclerosis

24
Q

When is Atazanavir/ritonavir ATV/r used

A

if LPV/r is not well tolerated

25
Q

DIs of ATV/r

A

warfarin–> decr. INR–> potential anticoagulant effect

26
Q

AEs of ATV/r

A

jaundice
abdominal pain

27
Q

DIs of Darunavir/ritonavir DRV/r

A

warfarin–> decr. INR

28
Q

AEs of DRV/r

A

abdominal pain
fatigue
headache

29
Q

AEs of Saquinavir/ritonavir SQV/r

A

Prolonged QT and PR intervals

30
Q

1st line Regimen of ARV

A

2NRTIs + NNRTI or IIs
TLD= tenofavir+ Lamivudine/Emtricibine + Dolutegravir
*TLD: fixed once dail dose
*patients >_30 kg and >_10yrs

31
Q

Alternative 1st line Regimen in TB patients and in Pregnant women

A

Rifampicin decr DTG in TB and its Teratogenic
*Tenofovir+ L/E+ EFV(TEE)

32
Q

What to replace EFV is TB patients 1st line regimen

A

TDF+ L/E+ LPV/r

33
Q

Alternative 1st line if EFV is CIed

A

T+ L/E + DTG

34
Q

Alternative 1st line if EFV AND DTG are CIed

A

T+ L/E + LPV/R

35
Q

Alternative 1st line if TDF is CIed

A

ABC + L
OR
AZT+ L

36
Q

Alternative 1st line if TDF & ABC are CIed

A

AZT+ L+ DTG/EFV

37
Q

When are 2nd line Regimens used

A

if patient is failing on 1st regimne

38
Q

2nd line regimen if patient failed on NNRTIs

A

AZT + L + DTG
*if HBsAg (HBV) +ive: T+L+DTG
*stopping TDF in chroni HBV patient leads to fatal hepatitis flare

39
Q

2nd line regimen if DTG is CIed

A

AZT + L + LPV/R
*HBsAg +ive: TDF + L + LPV/R

40
Q

2nd line regimen if TDF & AZT is CIed

A

ABC + L + LPV/R

41
Q

2nd line regimen if patients is failing IIs 1st line regimen

A

AZT + L + LPV/R
*HBsAg +ive: TDF+ L/E + LPV/R

42
Q

What to do in 2nd line regimens if Dyslipidemia/diarrhea associated with LPV/r occures

A

Replace with ATV/r

43
Q

Which drugs are available for 3rd line regimens

A

PI: DRV
IIs: RAL
NNRTIs: ETR, RPV, MVC
CCR5 blocker: Maraviroc MVC

44
Q

Pre-exposure Prophylaxis

A

PrEP: TDF/ L OT TDF/E
*continued risk of aquiring HIV

45
Q

Post-exposure Prophylaxis

A

PEP: TDF+ L+ DTG
*if DTG is CIed: T+L/E+ ATV/r OR LPV/r
*if TDF CIed or failing: replace with AZT
** HIV -ive people 72 hrs after substantial exposure

46
Q

Combinations to avoid

A

Didanosine+stavudine
Zidovudine+stavudine
L+E
Didanosine+TDF

Pharmacology (50 decks)

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