Pharmacodynamics

Question 1

Pharmacology

Answer 1

Study of substances interacting with living systems chemically

Question 2

Medical Pharmacology

Answer 2

Study of substances used to prevent, diagnose, and treat disease

Question 3

Toxicology

Answer 3

Study of undesirable effects of chemicals on living systems and ecosystems

Question 4

Pharmacodynamics

Answer 4

what drugs do to the body

Question 5

Pharmacokinetics

Answer 5

what the body does to drugs

Question 6

Properties required for drug to interact chemically with its receptor

Answer 6

Size, electrical charge, shape, atomic composition

Question 7

Shape

Answer 7

drug shape complimentary to receptor ‘site’

Question 8

Size

Answer 8

Varies b/w 100-1000 MW

Question 9

Atomic composition consists of

Answer 9

1. Organic compounds (carbohydrates, proteins, lipids, acids/bases)
2. Inorganic compounds (lithium, iron)

Question 10

ADME

Answer 10

Absorption, distribution, metabolism, excretion

Question 11

Intravenous (IV)

Answer 11

Needles, most rapid onset

Question 12

Intramuscular (IM)

Answer 12

Large volumes, may be painful

Question 13

Subcutaneous (SC)

Answer 13

Skin, smaller volumes than IM, may be painful

Question 14

Oral (PO)

Answer 14

Most convenient, significant first-pass effect

Question 15

Transdermal

Answer 15

Very slow absorption, prolonged duration of action, used for minimal first-pass effect

Question 16

Parenteral Rectal (PR)

Answer 16

Less first-pass effect than PO

Question 17

Inhalation

Answer 17

Often very rapid onset

Question 18

Drug-Receptor Bond types

Answer 18

covalent, electrostatic, hydrophobic

Question 19

Covalent

Answer 19

Very strong bond, not reversible biologically in most cases

Question 20

Electrostatic bonds

Answer 20

Common bond involving charged ionic molecules, H-bonds, dipole

Question 21

Hydrophobic bond

Answer 21

Weak bond involving highly lipid-soluble molecules

Question 22

Rational drug design uses

Answer 22

Computer programs designed to fit 3D structure of receptor site

Question 23

Agonist (def+example)

Answer 23

Binds to and activates receptors
Eg. opening of ion channel, enzyme activation

Question 24

Partial agonist

Answer 24

Agonist with less activation than a full agonist

Question 25

Inverse agonist

Answer 25

Stabilizes receptors in an inactive form, reducing activity

Question 26

Antagonist

Answer 26

Binds to receptor, competes/prevents binding of other molecules

Question 27

Competitive Antagonist

Answer 27

Antagonist that binds to the same site as the natural ligand

Question 28

Noncompetitive Antagonist

Answer 28

Antagonist that binds to a different site on the receptor (allosteric)

Question 29

Irreversible Antagonist

Answer 29

Antagonist that covalently modifies the receptor

Question 30

Best characterized drug receptor is

Answer 30

Regulatory G-protein coupled receptors

Question 31

Duration of Drug Action

Answer 31

Effects last as long as drug occupies receptor

Question 32

If a covalent bond, drug effect:

Answer 32

persists until drug-receptor complex destroyed/new receptors synthesized

Question 33

Concentration-Effect Curves show that

Answer 33

Responses to low dose and dosage are directly proportional

Question 34

Why are drugs reported on a log scale?

Answer 34

Easier to differentiate between 2 drugs you’re comparing

Question 35

Pharmacologic Potency (and what axis is it based on)

Answer 35

Required concentration or dose to create 50% of drug’s maximal effect, based on dose-response curves along dose axis

Question 36

Maximum efficacy (and what axis is it based on)

Answer 36

maximum biological effect, based on dose-response curves along response axis

Question 37

EC50

Answer 37

Concentration of drug required to produce 50% max effect

Question 38

ED50

Answer 38

Dose of drug required for 50% of individuals to exhibit therapeutic effect

Question 39

IC50

Answer 39

Half maximal inhibitory concentration - inhibits specific biological or biochemical function by 50%

Question 40

Kd

Answer 40

Concentration of a free drug where half-maximal receptor binding is observed

Question 41

High Kd means

Answer 41

binding affinity is low

Question 42

Low Kd means

Answer 42

binding affinity is high

Question 43

Spare Receptors

Answer 43

Unbound receptors when an agonist is producing maximal response

Question 44

TD50

Answer 44

Dose where 50% of individuals show a toxic side-effect

Question 45

LD50

Answer 45

Dose where 50% of subjects die

Question 46

TI

Answer 46

Therapeutic index: TD50/ED50

Question 47

TI50

Answer 47

dose of drug required to produce desired effect without undesired effect

Question 48

Drug Signaling Mechanisms (5)

Answer 48

1. Intracellular receptor
2. Extracellular receptor
3. Extracellular receptor activates separate tyrosine kinase
4. Direct regulation of ion channel
5. Cell surface receptor linked to effector enzyme by G-protein

Question 49

Intracellular receptor mechanism

Answer 49

A lipid-soluble ligand crosses the membrane and acts on an intracellular receptor

Question 50

Extracellular receptor/Extracellular receptor activates tyrosine kinase mechanism

Answer 50

A transmembrane receptor protein that has enzymatic activity OR stimulates a protein tyrosine kinase

Question 51

Cell surface receptor linked to effector enzyme by G-protein mechanism

Answer 51

A transmembrane receptor protein stimulates a GTP-binding signal transducer protein (G-protein) that modulates an intracellular second messenger

Question 52

Direct regulation of ion channel mechanism

Answer 52

A ligand-gated transmembrane ion channel can be induced to open or close