Immunosuppressant Drug Interactions Flashcards
What are the 4 drugs that are CYP3A4 and P-gp inducers?
Phenytoin
Phenobarbital
Carbamazepine
Rifampin/Rifabutin
What are the 4 drugs that are CYP3A4 and P-gp inhibitors?
Macrolide antibiotics
Non-DHP CCBs (diltiazem and verapamil)
Azole antifungals
Protease inhibitors, cobicistat
(T/F) - Azithromycin is not considered a CYP3AR inhibitor
TRUE - only macrolide antibiotic that is not
Which 3 immunosuppressant drugs should not be used concomitantly with statins?
CSA, SRL, and TAC
(T/F) - Statins are inhibitors of CYP3A4
FALSE - they’re substrates
(T/F) - CSA is an inhibitors of CYP3A4
TRUE - they’re also substrates
(T/F) - SRL is an inducer of CYP3A4
FALSE - weak inhibitor (also substrates)
(T/F) - TAC is an inhibitor of CYP3A4
TRUE - weak inhibitor, however
Why are statins avoided with CSA, SRL, TAC?
Rhabdomyolysis can occur due to statins breaking down more muscle cells and releasing myoglobin, which causes renal injury or failure; this is because statins are substrates and CSA, SRL, and TAC are inhibitors (weak or strong) of CYP3A4
What two food and herbs interact with CSA, TAC, SRL, EVR
Grapefruit juice and St. John’s Wort
Does grapefruit juice induce or inhibit CYP3A4 and P-gp?
Inhibits CYP3A4 and P-gp
In which location (hepatic or gut) does grapefruit juice inhibit CYP3A4 and P-gp? It can be both locations or different locations for each, by the way.
The gut for both CYP3A4 and P-gp
What is the culprit in grapefruit juice?
Metabolite of naringin (naringenin-metabolite)
Does St. John’s Wort induce or inhibit CYP3A4 and P-gp?
Induces CYP3A4 and P-gp
In which location (hepatic or gut) does St. John’s wort affect CYP3A4 and P-gp? It can be both locations or different locations for each, by the way.
CYP3A4 is affected in the liver and gut
P-gp is affected in the gut
