chapter2 pharmacodynamics

Question 1

Receptor function

Answer 1

1. Determinants quanti relation2. Regulatory proteins3. Therapeutic and toxic effects

Question 2

Emax

Answer 2

Maximal response produced by a drug

Question 3

Ec50

Answer 3

50% maximal effect

Question 4

Bmax

Answer 4

Total concentration receptor site. (ie. Sites bound to the drug infinitely high conc of free drug)

Question 5

Kd

Answer 5

(Equilibrium dissociation constant)Conc free drug at which half maximal binding.⬇️ Kd : binding affinity is high⬆️ Kd : binding affinity is low

Question 6

Coupling

Answer 6

Transduction process that links drug occupancy of receptors and pharmacologic respnse

Question 7

Spare receptors

Answer 7

Possible to elicit MAXIMAL biological response at conc of agonist that doesnt result in occupancy of full complement of available receptorsEc50< Kd

Question 8

Example spare receptors

Answer 8

Irreversible antagonist

Question 9

90% quasi-irreversible antagonist

Answer 9

B- adrenoceptors

Question 10

Types of antagonist

Answer 10

1. Chemical 2. Functional3. Competitive A. Eq B. Nonequilibrium4. Noncompetitive

Question 11

Antagonist property

Answer 11

+ affinity- efficacy

Question 12

Other type of antagonism

Answer 12

PhysiologicalChemicalPharmacokinetic

Question 13

Pharmacokinetic antagonist

Answer 13

One drug accelerates/ eliminates other drug

Question 14

2 properties agonist

Answer 14

AffinityEfficacy

Question 15

Comparative term for distinguishing which agonist has a higher affinity for given receptor

Answer 15

Potency

Question 16

Response to low doses op a drug usually ⬆️ in direct proportion to dose

Answer 16

Dose-resp rel

Question 17

Interaction of two agonist that act independently but cause opposite effects

Answer 17

FUNCTIONAL ANTAGONISM

Question 18

Example func anatagonist

Answer 18

ACTHEPINEPHRINE

Question 19

Eq competitive

Answer 19

Band is loose

Question 20

Noneq competitive

Answer 20

Bond is covalent

Question 21

PHARMACODYNAMICS

Answer 21

Study of rel drug conc and effects” DRUG does to the body”

Question 22

PHARMACOKINETICS

Answer 22

what the body does to the drug

Question 23

Examples of drugs of chem interaction

Answer 23

PROTAMINE SULFATE

Question 24

MOA: membrane surfactants

Answer 24

Amphotericin B- antifungal grrr

Question 25

MOA: denature proteins

Answer 25

ASTRINGENTS

Question 26

Concentration range over which drug produces a - toxicity-effectivity- ineffectiveness

Answer 26

Therapeutic window

Question 27

Cumulative distribution of a population response to a drug

Answer 27

Quantal dose

Question 28

Uses of quantal dose

Answer 28

TD 50LD 50

Question 29

TD 50

Answer 29

Dose produce a toxic effect in 50% of population

Question 30

LD50

Answer 30

Dose that produce mortality in 50% of population in animal settings

Question 31

Therapeutic index

Answer 31

Ratio of TD50 and ED50If ⬆️ = safer

Question 32

Propranolol

Answer 32

Competitive B- adrenoceptor antagonist

Question 33

2 therapeutic implication for competitive antagonist

Answer 33

1. Conc of antagonist2. Conc of agonist in competition

Question 34

Irreversible a- adrenoceptorControl HTN caused by catecholamine from pheochromocytoma ( tumor adrenal medulla

Answer 34

Phenoxybenzamine

Question 35

Types of agonist

Answer 35

1. Partial2. Full

Question 36

Many clinical antagonist are actually

Answer 36

Weak partial agonist

Question 37

Partial agonistu-opiod receptorsSafer analgesic drug than morphine coz of less RDS in overdoseEffective antianalgesic to morphine individual

Answer 37

Ibuprenorphrine

Question 38

Inhibitors of tyrosine kinase for neoplastic do

Answer 38

TrastuzumabCeruximab

Question 39

Other tyrosine inhibitors in the cytoplasm that are "small mol"

Answer 39

GefitinibErlotinib

Question 40

Inhibits voltage gated channel in d ❤️ and vascular sm mm = antiarrhythmic effects, ⬇️ bp Without mimicking or antagonizing any known endogenous NT

Answer 40

Verapamil

Question 41

Selective inhibitor type 3 phosphodiesterase that are expressed im cardiac mmAdjunctive agent tx acute heart failure

Answer 41

Milerinone

Question 42

Inhibits phosphodiesterase ⬇️Interferes cGMP For the tx erectile dysfunc and pulmo HTN

Answer 42

Sildenafil

Question 43

PhosphorylAtion: Common theme2 func

Answer 43

AmplificationFlexible regulation

Question 44

Tx for breast ca that antagonizes GF receptor signaling

Answer 44

Trastuzumab

Question 45

Small molecule inhibitor cytoplasmic tyrosine kinaseTx CML

Answer 45

Imatinib

Question 46

Drug antagonist to the estrogen mammary receptor " Agonist to the estrogen bone receptor Agonist in uterus which is stimulating endometrial cell proliferation.

Answer 46

Tamoxifen

Question 47

Responsiveness diminish rapidly after administration of drug

Answer 47

Tachyphylaxis

Question 48

A weak partial agonist at angiotensin II receptors:⬇️BP with px with HTN caused by increase angiotensin II production⬆️BP in px who produce normal amount of angiotensin

Answer 48

Saralasin