Antiretroviral Drugs Flashcards
List 5 Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Tenofovir (TDF) Emtricitabine Lamivudine (3TC) Zidovudine (AZT) Stavudine (d4T)
List 2 Non-Nuceloside Reverse Transcriptase Inhibitors (NNRTIs)
Efavirenz (EFZ)
Nevirapine (NVP)
Name a Protease Inhibitors (PIs)
Lopinavir-ritonavir (LPV/r)
Name a Integrase inhibitor
Dolutegravir (DTG)
What is the classification of Zidovudine (AZT)?
Nucleoside Reverse Transcriptase Inhibitor
What is the mechanism of action of Zidovudine (AZT)?
Inhibits nucleoside reverse transcriptase, stops the reverse transcription process and halts HIV replication
What are the therapeutic indications of Zidovudine (AZT)? (3)
- selective toxic agent used against HIV
- decrease the perinatal transfer of HIV
- treatment of patients that are HIV-positive
How is Zidovudine (AZT) administered?
orally or IV
Describe the absorption of Zidovudine (AZT)
bioavailability is about 65% and peak plasma concentrations are reached in about 30 min (orally)
What is the half-life of Zidovudine (AZT) and the active triphosphate?
AZT - 1 hour
active triphosphate - 3 hours
Describe the distribution of Zidovudine (AZT)
adequate distribution in CSF
What % of is Zidovudine (AZT) bound to plasma proteins?
30%
Describe the metabolism of Zidovudine (AZT)?
metabolized in the liver to its inactive glucuronide
Describe the excretion of Zidovudine (AZT)?
15% excreted unchanged in urine
What are the adverse effects of Zidovudine (AZT)? (9)
- Anaemia
- Neutropenia
- GIT disturbances
- abnormalities of liver function
- nausea
- headache
- skin rash
- insomnia
- flu-like syndrome
What is the classification of Nevirapine (NVP)?
Non-nucleoside reverse transcriptase inhibitor
What is the mechanism of action of Nevirapine (NVP)?
bind to reverse transcriptase enzyme, blocks reverse transcription process
What is the therapeutic indication of Nevirapine (NVP)?
prevent mother-to-baby transmission of HIV
How is Nevirapine (NVP) administered?
orally
Describe the absorption of Nevirapine (NVP)?
bioavailability is >90% and CSF level is 45% of that in the plasma
Describe the metabolism of Nevirapine (NVP)
metabolized in the liver
Describe the excretion of Nevirapine (NVP)
metabolite is excreted in the urine
What are the adverse effects of Nevirapine (NVP)?
- rash
- Stevens-Johnson syndrome
- toxic epidermal necrolysis
- fulminant hepatitis
- headache
- fever
- lethargy
What is the mechanism of action of integrase inhibitors?
Prevents HIV from integrating its genetic material into the host cell DNA by specifically blocking the action of the viral integrase enzyme
What are the adverse effects of integrase inhibitors?
Can cause increased serum creatine kinase levels
What is the mechanism of action of protease inhibitors?
Blocks the action of HIV protease enzyme, thus preventing cleavage of viral polyproteins into active proteins that are needed for the assembly of new viral particles
What are the adverse effects of protease inhibitors? (8)
- Hyperglycemia
- Gastrointestinal upset
- Cushing-like syndrome
- Renal toxicity (indinavir)
- Thrombocytopenia (indinavir)
- Inhibits cytochrome P450 (ritonavir)
- paraesthesias around the mouth (ritonavir)
- long term use: redistribution of fat (‘buffalo hump’)
