TDM & Toxicology
No description yet. This curated deck is ready for daily study.
Card preview (24)
Serum concentration is not equivalent to the concentration of ___________
Receptors [could be correlated with physiological responses in certain cases]
Why do we monitor TDM?***
-to guard against overdoes or underdoses -check for compliance
Study of the rate of process of absorption, distribution, and biotransformation (metabolism, and excretion)
pharmacokinetics
Study of biochemical physiological effects of drugs and their mechanisms of action
pharmacodynamics
A discipline concerned with the study of adverse effects of agents on living systems.
toxicology
What is the pharmacokinetics order of biotransformation?
LADME** -liberation -absorption -distribution -metabolization -excretion
Absorption: Rate and extent of drug absorption vary from different ________& _______
sites, drugs
What is the first-pass effect?
***after ORAL administration, drug is absorbed by small intestine and carried via portal vein to liver where the drug is extensively metabolized.
Mechanisms of pharmacokinetics?
-passive diffusion (95% of drugs) -active diffusion (needs carrier protein, against conc. gradient) -facilitated transport -convective (pore) transport -pinocytosis (fat soluble cells)
The drug must be in true ________ solution at the site of absorption.
aqueous
weak acid pKa: ______in H2O Strong acid pKa:_____ in H2O
-2 ~12 < -2
upon entering the circulatory system, most drugs will quickly equilibrate between a ______ and _______ state
free, bound
Only ______ drug is available for distribution beyond the vascular compartment.
free
physiological response of drugs is dependent only the _____ form of the drug (active)
free
Bound drug distribution is dependent on kinetic binding and physiological ________ parameters.
filtration
major sites for biotransformation and drug metabolism?
major: liver minor: kidneys, brain, lungs, skin, and GI tract
metabolism may affect the drug in what three ways?
-Increase activity (prodrug) -decrease activity (inactivation or detoxication) -no effect on activity
metabolites are generally more…
soluble -some metabolites may still be pharmacologically active* (needs to be factored into the half-life) *****on test, trick question
biotransformation changes the _______ of the drug
shape
what happens after a prodrug is metabolized?
activity increases
What are the two major metabolic pathways of drugs?
-phase 1- inactivation- reactions metabolize lipophilic drugs to more polar forms to facilitate renal excretion -phase 2- Excration
-accomplished by oxidative or deductive processes -Cytochrome P-450 enzymes on microsomal membranes oxidize to inactive drugs -metabolites can be metabolically active compounds
Phase 1- Innactivation
what enzyme metabolises most drugs?
Cytochrome P-450 (polar drugs)
-redactions involve conjugation of drugs with compounds such as glutathione, glucuronic acid, sulfate, and phosphate -conjugates produced are water-soluble and can be excreted by the kidneys
Phase 2-Exreation