Antiretrovirals Flashcards by Aisha Farah

What are Nucleoside/Nucleotide Reverse Transcriptase Inhibitors NRTIs

Analogues of nucleotides/nucleosides that inhibit Reverse transcriptase Enzymes

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Name the NRTIs

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

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MOA of NRTIs

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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Activation of NRTIs

Nucleotide analogue: Diphosphorylation
Nucleoside analogue Triphosphorylation

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AEs of Nucleotide analogues

TDF: nephrotoxicty
Fanconi’s syndrome
Bone mineralisation disorder

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AEs of Nucleoside analogues

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

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

fatal hypersensitivity rxns

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Name the Non-Nucleoside Reverse Transcriptase Inhibitors NNRTIs

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

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MOA of NNRTIs

inhibit HIV Reverse Transcriptase by binding to allosteric site of enzyme

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Diff. between NNRTIs and NRTIs

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

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AEs of EFV

Psychosis
abnormal dreams
Gynecomastia
Maculopapular rash

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AEs of NVP

rash: sever or life threatening- SJS
Heaptitis

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AEs of ETR

rash: severe or life threatening-SJS
Triglyceridaemia

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Which are the Integrase Inhibitors IIs

Dolutegravir: DTG
Raltegravir: RAL
Cabotegravir: CAB

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MOA of IIs

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

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AEs of DTG

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

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DIs of DTG

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

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DIs of RAL

Rifampicin: decr. RAL plasma levels

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AES of RAL

generally well tolerated
Headaches
nausea
fatigue
myopathy
rhabdomyolysis

Name the Protease Inhibitors PIs

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

MOA of PIs

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

General DIs of PIs

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

AEs of Lopinavir/ritonavir LPV/r

Dyslipidemia
Hyperglycaemia
diarrhea
Atherosclerosis

When is Atazanavir/ritonavir ATV/r used

if LPV/r is not well tolerated

DIs of ATV/r

warfarin--> decr. INR--> potential anticoagulant effect

AEs of ATV/r

jaundice abdominal pain

DIs of Darunavir/ritonavir DRV/r

warfarin--> decr. INR

AEs of DRV/r

abdominal pain fatigue headache

AEs of Saquinavir/ritonavir SQV/r

Prolonged QT and PR intervals

1st line Regimen of ARV

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

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

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

What to replace EFV is TB patients 1st line regimen

TDF+ L/E+ LPV/r

Alternative 1st line if EFV is CIed

T+ L/E + DTG

Alternative 1st line if EFV AND DTG are CIed

T+ L/E + LPV/R

Alternative 1st line if TDF is CIed

ABC + L OR AZT+ L

Alternative 1st line if TDF & ABC are CIed

AZT+ L+ DTG/EFV

When are 2nd line Regimens used

if patient is failing on 1st regimne

2nd line regimen if patient failed on NNRTIs

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

2nd line regimen if DTG is CIed

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

2nd line regimen if TDF & AZT is CIed

ABC + L + LPV/R

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

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

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

Replace with ATV/r

Which drugs are available for 3rd line regimens

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

Pre-exposure Prophylaxis

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

Post-exposure Prophylaxis

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

Combinations to avoid

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