NRTIs Flashcards
What is the mechanism of action of the Nucleoside Reverse Transcriptase inhibitors (NRTIs)
- They mimic DNA bases,
- Acting as false substrates for reverse transcriptase
Which 2 NRTIs act as Thymidine?
Zidovudine (AZT) + Stavudine (d4T)
Which NRTI act as Guanosine?
Abacavir (ABC)
Which 2 NRTIs act as Cytidine?
- Lamivudine (3TC) + emtricitabine (FTC)
Which 2 NRTIs act as Adenosines?
- Tenofovir (TDF) + Dedanosine (ddI)
Which NRTI well penetrates CSF?
Zidovudine (AZT)
How do the NRTIs result to lactic acidosis in host cells?
They all inhibit mitochondrial DNA gamma, which is an enzyme that replicates the mitochondria of a host cell.
How does lactic acidosis manifest itself in the human body? How do you know u are having lactic acidosis?
- Nausea
- Vomiting
- Abdominal pain
- Extreme tiredness
What are the side effects from using Zidovudine (AZT)?
- Anemia
-Myelosuppression - Neutropenia
-leucopenia - peripheral neuropathy (damage to peripheral nerves)
Wha are side effects of using stavudine (d4T)?
- Neutropenia
- Lipoatrophy
What are the side effects from using abacavir (ABC)?
- Hypersensitivity reactions
What are the side effects from using Tenofovir (TDF)
- Nephrotoxicity
- Bone loss
What are side effects from using lamivudine (3TC) and Emtricitabine (FTC)?
Peripheral neurophathy
What’s the metabolism pathway of the NRTIs?
Zidovudine (AZT) and Abacavir (ABC) undergo glucuronidation in the liver.
Which drugs does Zidovudine interact with?
- Ganciclovir
- Valproate
- Probenecid
What is the possible outcome from Zidovudine interaction with ganciclovir?
- increased
hematological toxicity
What is the possible outcome from Zidovudine interaction with valproate?
increase
AZT levels
What is the possible outcome from Zidovudine interaction with probenecid?
delayed
AZT excretion
When to not use Zidovudine? (The drug’s CI)
- Anemiac or patients with neutropenia
What drugs does tenofovir interact with? And what are the outcomes?
- ddI- increases levels of
didanosine - ATV- decrease levels of
atazanavir - Kaletra®- Increase TDF
levels
When is Tenofovir contraindicated?
On patients with nephrotoxicity
What are the adverse effects from Tenofovir use?
- Nephrotoxic,
- Hepatomegaly-enlargement of the liver beyond its normal size,
- HBV exacerbationswhen you stop using the drug
