Flashcards in General Principles 2 Deck (27):
Mention 2 plasma proteins with significant drug binding capacity.
Mention the 9 most common routes of drug administration.
2. Buccal/ Sublingual
6. Rectal (Suppository)
What is a graded dose-response curve?
When the response of a receptor-effector system is measured against increasing concentrations of a drug.
What is the Kd?
The concentration of drug required to bind 50% of the receptor sites.
What does Kd mean?
It is a useful measure of the affinity of a drug molecule for its binding site on the receptor molecule.
The smaller the Kd ---> The GREATER the affinity of the drug for the receptor.
What is a quantal-dose response curve?
When the minimum dose required to produce a specified response is determined in each member of the population.
What is the importance of the quantal dose-response curve?
The median effective ED50, median toxic TD50, and (in animals) median lethal LD50 doses are derived.
What information do the quantal dose-response curves provide?
About the variation in sensitivity to the drug in a given population.
If the sensitivity is small, the curve is steep.
What is the main difference between the graded dose-response and the quantal dose-response?
No attempt is made to determine the maximal effect of the drug.
What is the definition of efficacy?
The greatest effect (Emax) an agonist can produce if the dose is taken to the highest tolerated level.
Measured by graded dose-response curve.
What is the definition of potency?
Denotes the amount of drug needed to produce a given effect.
What determines mainly the potency of a drug?
1. The affinity of the receptor for the drug.
2. The number of receptors available.
How can potency of a drug be measured?
From either graded or quantal dose-response curves.
When do we suspect the existence of spare receptors?
If the maximal drug response (Emax) is obtained at less than 100% occupation of the receptors (Bmax).
Mention 2 common examples of chemical antagonism.
What curve does determine the therapeutic index?
The quantal dose-response curves - Calculate the TD50, ED50, LD50.
What drug has a greater first-pass metabolism in men than in women?
What does smoking do in the enzymes of liver and lung?
Induces them and may increase the metabolism of some drugs.
Mention some important inducers of CYP450 1A2.
Mention some important inducers of CYP450 2C9.
1. Barbiturates (phenobarbital)
Mention some important inducers of CYP450 2C19.
Mention some important inducers of CYP450 2E1.
Mention some important inducers of CYP450 3A4.
What are the 4 most common strong inducers of drug metabolism?
What are the 5 most important inhibitors of drug metabolism?
3. Furanocoumarins in grapefruit.
4. Azole antifungals
5. Ritonavir - HIV antiprotease inhibitor.
Mention 3 important inhibitors of P-glycoprotein.
3. Furanocoumarins in grapefruit juice.