Pharm Chp 1 FC

Question 1

Pharmacodynamics

Answer 1

study of biochemical and physiologic effects of drugs and the molecular mechanisms by which these effects are produced (drug actions and effects within the body)

Question 2

Law of Mass Action

Answer 2

magnitude of response and rate of reaction is proportional to the number of drug-receptor complexes (efficacy of drug is altered if either changes)

Question 3

Concentration at which no greater effect can be produced

Answer 3

Saturation (all receptors saturated)

Question 4

Simple Occupancy Theory

Answer 4

intensity of response to a drug is proportional to # of receptors occupied by drug (max response when all receptors occupied)

Question 5

Modified Occupany Theory

Answer 5

takes into account affinity and intrinsic activity

Question 6

Strength of attraction between a drug and its receptor

Answer 6

Affinity (if high, drug conc can be low and drug will still bind)

Question 7

Instrinsic Factor

Answer 7

Ability of a drug to activate a receptor following binding (reflected by max efficacy)

Question 8

Mimics the body’s own regulatory molecules (endogenous ligand) and activates a receptor

Answer 8

Agonist (has affinity and high instrinsic activity)

Question 9

Inverse Agonist

Answer 9

An agonist that slows down a physiologic process (due to endogenous ligand already being present in adequate amounts)

Question 10

Full Agonist

Answer 10

Capable of produding max effect produced when drug binds receptor

Question 11

Partial Agonist

Answer 11

Its’ max effect is lower than that of a full agonist (moderate intrinsic activity)

Question 12

Produce pharmacologic effect by preventing the activation of receptors by agonists

Answer 12

Antagonist (has affinity but NO instrinsic activity and response determined by how much agonist is present)

Question 13

Name the 3 types of Antagonists

Answer 13

Competetive Reversible, Competetive Irreversible and Noncompetitive

Question 14

Competitive Irreversible Antagonist

Answer 14

Reduces # of receptors available thus reducing max response agonist can elicit (effects wear off over time as cell adds new receptors)

Question 15

Noncompetitive Antagonist

Answer 15

Does not bind directly to agonist binding site. Reduces affinity for agonist, blocks agonist ability to cause change in receptor or coupling of receptor to signal mechanisms)

Question 16

Major Types of Drug Receptors

Answer 16

4. transmembrane ion channels, transmembrane receptors coupled to G proteins, transmembrane receptors with enzymatic cytosolic domains, intracellular receptors (enzymes and structures))

Question 17

Transmembrane Ion Channels

Answer 17

Allows passage of hydrophilic ions across the plasma membrane (produce AP in cardiac and skeletal muscle)

Question 18

Drugs may affect the function of these ion channels by directly opening or closing the channel

Answer 18

Ligand gated ion channels

Question 19

How many types of transmembrane ions channels are there?

Answer 19

3. Ligand gated, voltage gated and second messenger gated

Question 20

Most abundant call of receptors

Answer 20

G protein coupled receptors

Question 21

Major role of G protein coupled receptors

Answer 21

to activate second messengers

Question 22

Largest group of receptors with enzymatic cytosolic domains

Answer 22

tyrosine kinase family

Question 23

Tyrosine kinase

Answer 23

modifies proteins by phosphorylation (adding or removing a phosphate group)

Question 24

Which type of drug receptors affect transcription?

Answer 24

Intracellular receptors (either increase or decrease transcription of RNA)

Question 25

Intracellular Receptors (including enzyme and structural proteins)

Answer 25

great impact on cellular function, slow process and onset, longer lasting affects (steroid drugs)

Question 26

A drugs ability to induce a certain action at a certain concentration

Answer 26

efficacy

Question 27

Maximal efficacy

Answer 27

largest effect that a drug can produce

Question 28

Dosage needed to produce its effect

Answer 28

potency

Question 29

Minimal effective concentration

Answer 29

lowest plasma concentration that produces the desired effect

Question 30

Effective Dose (ED50)

Answer 30

dose required to produce a therapeutic effect in 50% of the population

Question 31

Range of plasma concentration that produces the desired effect without toxicity

Answer 31

Therapeutic Range (between minimal effective conc and toxic level)

Question 32

Toxic Dose (TD50)

Answer 32

dose of a drug that causes a toxic rxn in 50% of population

Question 33

Plasma concentration at which a drug produces serious side effects

Answer 33

drug toxicity

Question 34

Selective toxicity

Answer 34

eg. Chemotherapy and antimicrobial

Question 35

Lethal Dose (LD50)

Answer 35

dose of a drug that causes death in 50% of population

Question 36

Therapeutic Index or Ratio

Answer 36

LD50:ED50 (the closer the ratio is to 1 the greater the danger)

Question 37

Therapeutic Window

Answer 37

range of doses that elicits a therapeutic response without unacceptable side effects (drugs with small window need close monitoring)

Question 38

A large TI represents a side TW?

Answer 38

TRUE

Question 39

TD50/ED50

Answer 39

Protective index - a measure benefit to risk ratio (more informative about a drug’s relative safety)