Intro to Drug Metabolism Flashcards
Which principle describes: what does the drug do to the body
Pharmacodynamics
What is the goal behind the minimum effective concentration (MEC)?
To keep concentration above it
When does onset occur in terms of the therapeutic window?
The moment concentration reaches MEC
When does termination occur in terms of the therapeutic window?
After concentration goes down and just dips below MEC
What is the therapeutic window?
Area between toxicity and MEC
Which principle describes: what does the body do to the drug?
Pharmacokinetics
Which occurs first, pharmacokinetics or pharmacodynamics?
Pharmacokinetics
Which principle describes: How the body absorbs, distributes, and eliminates the drug
Pharmacokinetics
Which principle describes: Plasma concentration (dose) needed to produce effect-
Pharmacodynamics
What are some other terms used interchangeably with metabolism?
Biotransformation & Inactivation
Do all drugs undergoing metabolism inactivate the drug itself?
No, not all
Some actually get activated like L-Dopa to dopamine
Some stay active and transform to another active form like diazepam to oxazepam
Metabolism of drugs make it more (hydrophilic/hydrophobic)
Hydrophilic
Metabolism of drugs make it more (hydrophobic/hydrophilic)
Hydrophilic
Once a drug is metabolized, where is it eliminated?
Kidneys & GI tract
Where is the primary location of metabolism?
Liver (hepatic)
What is found in phase I rxns?
p450
Which rxn requires energy?
Phase II
What is found in phase II rxns?
Conjugation rxns
Which rxn does NOT require energy?
Phase I
Once metabolized, what exactly is being removed?
- Parent (starting) compound
2. Metabolites
Which phase makes the compound more hydrophilic?
Both phase I & II
What specific rxns occur in phase I?
- Hydroxylation
- Dealkylation
- N-oxidation
What specifically do phase II rxns add to the compound?
Endogenous substrates (glucuronides, sulfates & acetates)
What is a pro-drug? How does it cycled through?
Inactive form; bioactivated via enzymatic action
