Therapeutics - HIV 4
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What are the SE of Tipranavir?
- Hepatic impairment
- Intracranial hemorrhage
- GI effects – N, V, D
PIs have what effect on Azoles?
Increase Azole concentrations
PIs have what effect on Clarithromycin?
Increase Clarithromycin concentrations
PIs have what effect on PPIs?
Decrease PPI concentrations (may be equally effective though)
PIs have what effect on Opioids?
Increase opioid levels
PIs have what effect on antiarrhythmics?
Increase antiarrhythmic levels
PIs have what effect on anticonvulsants?
Reduce concentration of anticonvulsants and PI
What other drugs are CI with PIs?
What effect do PIs have on Warfarin?
What effect do PIs have on statins?
What are the Non-Nucleoside Reverse transcriptase inhibitors?
- Nevirapine - Viramune
- Delavirine - Rescriptor
- Efavirenz – Sustiva
- Atripla (tenofovir + emtricitabine + efavirenz)
- Etravirine - Intelence
- Rilpivirine – Edurant
- Complera (tenofovir + emtricitabine +rilpivirine)
What is the brand name for Nevirapine?
What is the brand name for Delavirine ?
What is the brand name for Efavirenz?
What is the brand name for tenofovir + emtricitabine + efavirenz?
What is the brand name for Etravirine?
What is the brand name for Rilpivirine?
What is the brand name for tenofovir + emtricitabine +rilpivirine?
What is the generic name for Viramune?
What is the generic name for Rescriptor?
What is the generic name for Sustiva?
What is the generic name for Atripla?
Tenofovir + emtricitabine + efavirenz
What is the generic name for Intelence?
What is the generic name for Edurant?
What is the generic name for Complera?
Tenofovir + emtricitabine +rilpivirine
Delavirdine should be separated by 1 hr from what other drugs?
Didanosine or antacids
How is Delavirdine effected by food?
No food effect
How is Delavirdine metabolized?
By P4503A (inhibitor); 51% excreted in urine (as metabolites)
What are the SE of Delavirdine?
rash; elevated LFTs; headache
Use of DLV is not recommended due to:
High pill burden, dose frequency, SE and DDIs
Efavirenz has good or bad bioavailability?
How is Efavirenz metabolized?
By P4503A (mixed inducer/inhibitor)
What are the SE of Efavirenz?
- Rash; CNS symptoms (52%) = Suicide ideation; elevated LFTs; false + cannabinoid test; teratogenic in monkeys (try not to use in 1st trimester)
- Probably shouldn’t use with schizophrenia or depression
Is Efavirenz used as an initial therapy?
Nevirapine has good or bad bioavailability?
What is Nevirapine metabolized by?
What are the SE of Nevirapine?
Rash (37%); S-J syndrome; hepatitis; fatal hepatic necrosis particularly in women (pregnancy)
Entravirine has in vitro activity against what?
Entravirine should be taken with or without food?
- CYP450 3A4 inducer
- Toxicity: rash 9%; S-J syndrome; nausea 13%
Is Entravirine used initially?
Not usually, usually just used in NNRTI-resistant strains
Rilpiverine is usually combined with what other drugs?
Tenofovir + emtricitabine
What group of patients is Rilpiverine usually used in?
- Ttreatment naïve pts
- VL < 100,000
What are the SE of Rilpiverine?
Depression (4%), insominia, headache (3%), and rash (3%)
What drug requires a viral oad of < 100,000?
Cross resistance to efavirenz, etravirine, and/or nevirapine is likely after development of resistance to _________.
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