Introduction to ADME LO

Question 1

Identify the portions of a concentration vs. time cure that are associated with onset, duration, and intensity of a pharmacologic effect.

Answer 1

Onset is how quickly is acts. It is the first time we see an effect on the graph.
Duration is how long it acts.
Intensity is the peak effect, the maximum effective concentration. (Other things to know are LogC means concentration and sometimes peak effect happens before peak concentration)

Question 2

Provided a route of administration, identify barrier that may reduce the amount of drug that reaches the site of action.

Answer 2

The GI tract may present barriers during absorption.

Question 3

Define disposition, pharmacokinetics, and pharmacodynamics

Answer 3

Disposition is what happens to the drug once it gets into the body. The fate of a drug after is has entered the systemic circulation. Pharmacokinetics is how the drug moves through the body. This is best represented in the liver and excretion and distribution. Pharmacodynamics what the body does to the drug which is essentially the pharmacological effect.

Question 4

Identify what percent of drugs currently fail in clinical trials due to problems with ADME.

Answer 4

Less than 10% of attrition in clinical trials of new drugs is due to ADME.

Question 5

Identify the primary routes of administration.

Answer 5

Ingestion, inhalation, dermal, parenteral (intravenous, subcutaneous, intramuscular, intraperitoneal)

Question 6

Describe the four potential consequences of drug metabolism as it relates to pharmacologic activity.

Answer 6

Active drug to inactive metabolite (hydroxylation), active drug to active metabolite (acetylation), inactive drug to active metabolite (demethylation) , active drug to reactive metabolite