HIV Flashcards
Examples of NRTIs
Abacavir
Didanosine
Emtricitabine
Lamivudine
Stavudine
Tenofovir
Zidovudine
Mechanism of action of NRTIs
Act as nucleoside analogs –> competitively blocks nucleoside binding to reverse transriptase –> inhibits formation of 3’ to 5’ phosphodiester linkages –> termination of DNA chain –> inhibition of RNA to DNA reverse transcription
General adverse effects of NRTIs
Mitochondrial toxicity
Lactic acidosis
HIV associated lipodystrophy
Abacavir specific adverse effects
Increase cardiovascular events
Hypersensitivity reactions
Avoid in HLA B5701 positive patients
What HIV medication causes pancreatitis
Didanosine
Stavudine
What HIV medication is associated with cardiovascular disease/increased risk of MI
Abacavir
What HIV medication is associated with nephrotoxicity
Tenofovir
TDF > TAF
What HIV medication is associated with OP
Tenofovir
TDF > TAF
What HIV medication is associated with bone marrow suppression
Zidovudine
What HIV medications cause peripheral neuropathy
Stavudine
Didanosine
Zalcitabine
Examples of protease inhibitors
ends with “navir”
Atazanavir
Darunavir
Lopinavir
Indanavir
MOA of protease inhibitors
Inhibits viral HIV-1 protase –> production of immature virions (non-infectious)
Adverse effects of protease inhibitors
GI upset
Nephrolithiasis, crystal-induced nephropathy, haematuria
Metabolic abnormalities - hyperglycaemia, dyslipidemia, lipodystrophy
Increased risk of bleeding in patients with haemophilia
Changes to hair e.g. thinning
Advantage of ritonavir
Ritonavir is CYP450 inhibitor
Can be used in subtherapeutic doses to increase concentrations of other HIV drugs
Which HIV medication with teratogenic?
Efavirenz
Which HIV medication causes indirect hyperbilirubinaemia
Atazanavir
Specific adverse effect of nevirapine
Severe hepatotoxicity in higher doses
CD4 200-500
Tuberculosis
CD4 < 200
PJP
Cryptosporidium
Candida
Fungal pneumonia
CD4 < 100
Toxoplasmosis
Candida, HSV, CMV oesophagitis
CD4 < 50
CMV
Cryptococcus
MAC
Primary CNS lymphoma
Pathophysiology of HIV
1) HIV enters body and attaches to CD4 receptor with gp120 glycoprotein binding
2) Viral envelope fuses with host cell and capsid enters the cell
- for fusion, CD4 receptor and coreceptor (CCR5 in macrophages and CCR5 or CXCR4 in T cells) must be present
- CCR5 mainly occurs during early stages, CXCR4 occurs in later stages
3) Virion’s RNA transcribed into dsDNA vy viral reverse transcriptase and then integrated into host’s DNA by viral intergrase
4) Viral DNA is replicated and virions are assembled
MOA of NNRTIs
Nonnucleoside reverse transcriptase inhibitors
Binds to reverse transcriptase at different location
Examples of NNRTIs
Efavirenz
Nevirapine
General adverse effects of NNRTIs
Hypersensitivity reactions
SJS
MOA of integrase inhibitors
Inhibition of viral integrase –> blockade of viral DNA integration into host’s DNA –> inhibition of viral replication
Examples of inegrase inhibitors
Ends with “-gravir”
Bictegravir
Dolutegravir
Raltegravir
Examples of entry inhibitors and MOA
Enfuvirtide - fusion inhibitor, competitively binds to gp41
Maraviroc - CCR5 antagonist, inhibition of gp120 interaction
