Pharmacodynamics

Question 1

Claudius Galenus

Answer 1

129-200

Theoretical background of drug therapy is important.

Question 2

Paracelsus

Answer 2

Theophrastus von Hohenheim. 1493-1541.

General concept of pharmacokinetics. Importance of dosage.

Question 3

Johann Jakob Wepfer

Answer 3

1620-195.

Animal experiments to verify pharmacological effects.

Question 4

Rudolf Buchheim

Answer 4

1820-1879.
Pharmacology: institute, branch of science.
Chemical properties.

Question 5

Oswald Schmiedeberg

Answer 5

1838-1921.

Widespread acceptance. Journal.

Question 6

3 aspects of pharmacodynamics

Answer 6

1. Drug-receptor interaction
2. Signal transduction
3. Biologic response/toxic effects

Question 7

Requirements for receptors

Answer 7

Binding
Specificity
Effect

Question 8

Major receptor families

Answer 8

Ligand-gated ion channels
GPCR
Enzyme-linked receptors
Intracellular receptors

Question 9

GPCR - process

Answer 9

Extracellular ligand binds > conformation change > exchange of GDP for GTP and G-alpha subunit > signalling cascade

Inactivation: GTP>GDP, beta-arrestin

Question 10

G-alpha subunit types

Answer 10

s/i: > AC > cAMP
y> PLC > IP3 > Ca2+
12/13: Rho-GEF > RhoA

Question 11

Pharmacodynamics - plot

Answer 11

Biological effect as function of log conc of drug

(-> what drug does to organism)

High effect with low toxicity = therapeutic range

Question 12

Def. potency, EC50/IC50, efficacy

Answer 12

Potency: amount of drug needed to cause certain effect
EC50/IC50: conc of drug that causes 50% of max effect/inhibition
(the smaller, the more potent)
Efficacy: magnitude of response caused by drug (depends on number of drug-receptor complexes, ability of drug to activate receptor)

Question 13

Partial agonist vs full agonist

Answer 13

Can have same potency, but partial agonist has lower efficacy.

Question 14

Types of ligands (agonists)

Answer 14

Full agonist
Partial agonist
Super agonist
Inverse agonist
Antagonist

Question 15

Full agonist

Answer 15

Activates receptor (stabilizes active state).

Question 16

Partial agonist

Answer 16

Activates receptor but with lower efficacy

Question 17

Super agonist

Answer 17

Activates receptor with higher efficacy than endogenous agonist

Question 18

Inverse agonist

Answer 18

Stabilises inactive, ligand-bound state of receptor > lower intrinsic receptor activity

Question 19

Antagonist

Answer 19

Does nothing (no efficacy) but prevents agonist from activating receptor.

Question 20

Types of antagonists

Answer 20

Orthosteric/competitive: blocks binding site

Allosteric: binds other site

Question 21

Drug classes?

- olol, -pril, -triptan, -vastatin

Answer 21

Beta-receptor-blocker, ACE-inhibitor, 5-HT-receptor-agonist, HMG-CoA-reductase-inhibitor