Principles of Pharmacology- Lecture 1

Question 1

Affinity

Answer 1

potential for drug receptor binding

“receptor binding”

Question 2

Receptor

Answer 2

binding site with biological effect

“site”

Question 3

Intrinsic activity

Answer 3

capacity to produce biological effect

Question 4

Agonists

Answer 4

substances that stimulate a receptor to produce a physiologic reaction; have both affinity and intrinsic activity

Question 5

Antagonists

Answer 5

substances that oppose or interfere with the activity of a receptor and its endogenous substrate without producing a physiologic effect itself; antagonists have affinity but lack intrinsic activity

Question 6

Allostery

Answer 6

a stereospecific phenomenon whereby a bound ligand influences specificity of a second site

Question 7

Efficacy

Answer 7

Affinity x Intrinsic activity ; dose independent

Question 8

EC50

Answer 8

effective concentration in 50% of subjects

Question 9

ED50

Answer 9

effective dose in 50% of subjects

Question 10

IC50

Answer 10

inhibitory of 50% of subjects

Question 11

Hypersensitivity

Answer 11

result of chronic antagonism

Question 12

Maximum Dose

Answer 12

min. amount of drug producing maximum therapeutic effect

Question 13

Partial Agonist

Answer 13

low intrinsic activity with potency and affinity within therapeutic range

Question 14

Pharmacodynamics

Answer 14

Drug-> Body
focuses on biochemical and physiological effects of drugs and their mechanisms of action; potency, efficacy, affinity and toxicity are key measures

Question 15

Pharmacokinetics

Answer 15

Body → Drug (ADME)

Question 16

Pharmacotherapeutics

Answer 16

Drug—> Disease

Question 17

Posology

Answer 17

study of drug dosing

Question 18

Potency

Answer 18

biological response to a given dose

Question 19

Resistance

Answer 19

loss of pharm. effect

Question 20

Selectivity

Answer 20

ability to produce a desired effect versus adverse effect

Question 21

Specificity

Answer 21

ability to act at a specific receptor

Question 22

Tachyphylaxis

Answer 22

rapidly decreasing therapeutic response

Question 23

Teratogenesis

Answer 23

congenital malformation

Question 24

Bioavailability

Answer 24

amount of active drug reaching target tissue ; does not directly relate to drug potency

Question 25

Therapeutic index:

Answer 25

: LD50:ED50 or TD50:ED50

Question 26

DPA

Answer 26

diagnostic pharmaceutical agent

Question 27

TPA

Answer 27

therapeutic pharmaceutical agent

Question 28

Drug Types

Answer 28

``` Supportive: glucose Supplemental: Insulin Prophylactic: low dose aspirin Symptomatic: olopaptidane Diagnostic: florescein Therapeutic: methotrexate ```

Question 29

PHYSIOLOGIC RECEPTOR MOTIFS

Answer 29

Nuclear: e.g. steroids, hormones G-protein-coupled: e.g. AChM, rhodopsin This is the MOST COMMON receptor type targeted by ophthalmic drugs Ion channels: e.g. GABAA, AChN, glutamate Enzymatic: e.g. insulin, epidermal growth factor Calcium release: calcineurin, nitric oxide synthase

Question 30

Types of Agonists

Answer 30

``` Direct Indirect Mixed Inverse Partial ```

Question 31

Antagonists Binding Integrity

Answer 31

Reversible | Irreversible

Question 32

Antagonists binding site selectivity

Answer 32

Competitive (same as endogenous agonist) Non-competitive (allosteric) Uncompetitive (allosteric binding in presence of substrate slows ligand dissociation and response rate) (requires presence of agonists)

Question 33

Antagonists Mode of Action

Answer 33

Biological: e.g. PCN Chemical: e.g. Alka Seltzer, chelators Physiological: e.g. ACh, E, His