1. DSA Intro To Pharmacodynamics

Question 1

Pharmacokinetics is the effecs of the body on drugs (absorption, distribution, metabolism) while pharmacodynamics is?

Answer 1

the effects of drugs on the body ( drug receptors, dose-response curves, MOA)

Question 2

What is a component of the biologic system to which a drug binds without changing any function?

Answer 2

inert binding site

Question 3

A type of drug-receptor interaction is covalent bond, which are irreversible while non-covalent bonds are?

Answer 3

reversible, most drugs bind to receptors via this

Question 4

List the following from strong to weakest non covalent bonds…
Hydrogen bonds
Hydrophobic interactions
Ionic Bonds

Answer 4

Ionic bonds- electrostatic between pos/neg ion
Hydrogen bonds- H to NOF
Hydrophobic Interactions

Question 5

From highest to lowest affinity, list the affinities of the following for the mu receptor…
fentanyl, meperidine, morphine

Answer 5

Fentanyl, Morphine, Meperidine

Question 6

Kd or equilibrium dissociation constant is the drug concentration at which?

Answer 6

50% of the drug receptor binding sites are occupied by the drug (lower Kd = higher affinity of drug for receptor)

Question 7

What is a property of a drug determined by its affinities at various binding sites?

Answer 7

Drug Selectivity

Question 8

What describes the ability of a drug to change a receptor function and produce a physiological response upon its binding to a receptor?

Answer 8

intrinsic activity (agonists have this and antagonists do not)

Question 9

An antagonist will cause no activation of a receptor, what does an inverse agonist do?

Answer 9

produces an effect opposite to a full or partial agonist

Question 10

Pharmacologic or receptor antagonism occurs at the same receptor as endogenous ligands or agonist drugs. Some examples include?

Answer 10

Competitive Antagonists
Non-competitive Antagonists (irreversible and allosteric)
NOTE: allosteric binds to another site to alter agonist site

Question 11

What are two types of nonreceptor antagonists?

Answer 11

chemical and physiologic

Question 12

What is the relationship between a drug and its effects described quantitatively?

Answer 12

dose response curve- usually hyperbolic with a linear and plateau phase

Question 13

If you take the log of a dose response cruve, what will you see instead of hyperbolic curve?

Answer 13

Sigmoidal curve

Question 14

What is the dose of drug that produces 50% of its maximal effect?

Answer 14

ED50 (effective dose 50)

NOTE: maximal effect a drug can produce is Emax

Question 15

Graded response answers how much, while quantal response answers what?

Answer 15

does the response occur or not, in how many? Yes or No

Question 16

What represents the number or % of individuals responding at a dose of a drug and only that dose?

Answer 16

Non-cumulative quantal dose response curve

Question 17

What represents the number or % of individuals responding at a dose of a drug AND at all doses lower than that dose?

Answer 17

Cumulative quantal dose response curve

Question 18

ED means effective dose, TD means toxic dose, LD meas?

Answer 18

Lethal dose

Question 19

What is equal to TD50/ED50?

Answer 19

TI or therapeutic index

Question 20

What is the range of doses of a drug or of its concentration in a bodily system that provides for the safe and effective therapy?

Answer 20

Therapeutic window

Question 21

What is described as the amount of drug required to produce a specific effect, represented by the ED50?

Answer 21

Potency, Lower ED50 = more potent drug

Question 22

What describes the maximal pharmacological effect that aa drug can produce, represented by the Emax?

Answer 22

Efficacy, greater Emax, more efficacious drug

Question 23

What modify proteins by covalently attaching phosphate groups to an amino acid residue?

Answer 23

protein kinases