Antiretrovirals and antianemic agents Flashcards Preview

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Flashcards in Antiretrovirals and antianemic agents Deck (17)
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Name the four different types of HIV treatments?

- RT inhibitors
- Protease inhibitors
- Fusion inhibitors
- Integrase inhibitors


Describe the mechanism of action for nucleoside RT inhibitors

- Must be phosphorylated in the cell in order to become active
- Inhibit by being incorporated into the DNA preventing further transcription
- This is done by lacking 3' OH


What are common NRTI's and how are they excreted?

- Most excreted renally except
- Zidovudine (AZT) - glucuronidation
- Abacavir (ABC) - alcohol dehydrogenased
- No P450 drug interactions


What is the toxicity concern with NRTI's and there effects clinically?

- Mitochondrial toxicity
- Hepatic failure with steatosis (fatty liver) and lactic acidosis.


What are the 2 NRTI resistance mechanisms?

- Nulceoside analog descrimination
- Primer nucleoside unblocking- excision


What is the mechanism of non-nulceoside RT inhibitors?

- Bind directly to RT enzyme preventing transcription


What are the 5 NNRTI's?

- Efavirenz
- Delavirdine
- Etravirine
- Nevirapine
- Rilpivirine


What are the advantages and disadvantages of NNRTI's?

- Adv- long half-life, Hepatic metabolism no renal function adjustments required
- Disadv -resistance and cross resistance
- Skin rash, increased transaminase levels and P450 interactions


Protease inhibitor info

- All end in navir
- Ritonavir induces own metabolism (most potent 3A4 INH) and is often use along with other PI's to reduce metabolism


What are the PI advantages and disadvantages?

- Adv - higher barrier to resistance
- Disadv - Dyslipidemia, insulin resistance, and hepatotoxicity, GI effects, drug interactions


What is the mechanism of action of fusion inhibitors?

- Bind to CD4 on cell surface (MIraviroc) or surface of the HIV envelop (Enfuvirtide)


What are the adverse effects of Miraviroc?

- Hepatotoxicity preceded by allergic reaction (rash and eosinophilia)
- CV adverse effects
- Dizziness and postural hypotension


What is the mechanism of action for integrase inhibitors?

- Binds pre-integration complex to the host DNA
- Terminating integration of viral DNA to the host genome


Name two integrase inhibitors

- Raltegravir (BID)
- Elvitegravir (Q day)


What is cobistat?

- CYP3A4 inhibitor given with elvitegravir to allow single dose.


What are the common side effects of Raltegravir?

- Myositis and rhabdomyolisis
- Increase creatine kinase
- Rare skin reactions and hyper sensitivity rxns


What are the side effects of elvitegravir?

- Nausea, diarrhea and UTI
- Back and joint pain
- Upper respiratory tract infections and bronchitis