Intro to ADME

Question 1

Disposition

Answer 1

The fate of a drug once it enters systemic circulation

Question 2

Onset

Answer 2

How quickly the drug produces an effect

Question 3

Duration

Answer 3

How long it exhibits an effect

Question 4

Intensity

Answer 4

magnitude of effect

Question 5

Barriers that reduce the amount of drug that reaches the site of action

Answer 5

Membranes that limit the movement of certain drugs

enzymes within membranes that can metabolism the parent drug

Tissue barriers such as BBB can reduce the amount of drug that enters the site of action.

Question 6

What percent of drugs currently fail in clinical trials due to problems with ADME?

Answer 6

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

Question 7

What are the primary routes of administration?

Answer 7

intravenous (fastest onset)
inhalation
oral
intramuscular
subcutaneou
rectal
instillation
dermal

Question 8

Consequences of metabolism

Answer 8

active drug–> inactive metabolite (prolonged pharmacologic effect)

active drug–> active metabolite (decrease pharmacologic effect)

Inactive drug–> active metabolite

active drug–> reactive metabolite

Question 9

Major routes of excretion

Answer 9

Renal
Biliary–> feces

other routes: pulmonary, salivary, mammary

Question 10

A reduction in the extent of absorption will impact which of the three measures of pharmacologic effect?

Answer 10

most likely reduce the intensity or duration of effect

Question 11

A reduction in the speed of entry into the systemic circulation will impact which of the three measures of pharmacologic effect?

Answer 11

most likely reduce the onset of effect