EXAM 5 - Metabolic Drug Interactions Flashcards
What are the two major types of drug interactions?
Enzyme inhibition
* reversible (most common)
* slowly reversible or irreversible
Enzyme induction
* transcriptional activation (more likely)
* protein (or mRNA) stabilization (less likely)
What are the two major types of drug interactions?
Enzyme inhibition
* reversible (most common)
* slowly reversible or irreversible
Enzyme induction
* transcriptional activation (more likely)
* protein (or mRNA) stabilization (less likely)
Explain why P450s are often involved in drug interactions.
P450s are often involved because so mamy drugs get metabolized by P450 enzymes.
* P450 enzymes can also be inhibited and induced by many other drugs.
Explain why P450s are often involved in drug interactions.
P450s are often involved because so mamy drugs get metabolized by P450 enzymes.
* P450 enzymes can also be inhibited and induced by many other drugs.
Describe the different effects of Rifampin and Troleandomycin on IV Midazolam.
Midazolam is an anesthetic metabolized by P4503A4 to form midazolam-OH.
Rifampin induces the effects of midazolam
* increases metabolism of midazolam which can result in uneffective dose bc it falls below the theraputic window
Troleandomycin inhibits the effects oif midazolam
* slows down the metabolism of midazolam –> concentration is too high –> fully anesthetized for longer than usual
Explain the clinical significance of metabolic drug interactions.
- Changes the outcomes of drugs
- Predicting risk in specific patients
What are the types of outcomes of metabolic drug interactions?
- no effect
- toxicity
- reduced therapeutic effect
How do metabolic drug interactions predict risk in specific patients?
- patient related risk factors - pharmacogenetics, disease, habits, age
- dose - most DIs are related but not all (e.g. potent inhibitors)
- route of administration
- duration of administration - long half-life drugs are less effected
- sequence of administration - induction usually takes longer to occur than inhibition
What are some ways pharmacists can manage drug interactions?
- identification of patients - computerized screening
- actions to reduce risk of adverse drug interactions
- computerized prevention of adverse interactions
What are actions to reduce risk of adverses drug interactions?
a. Use of alternative noninteracting medications. Almost always
possible to do this
b. Adjust the dose based off response, rather than prophylactically
c. Adjust dosing times
d. Monitor for altered response