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2H. Pharmacology > chapter2 pharmacodynamics > Flashcards

chapter2 pharmacodynamics Flashcards

1
Q

Receptor function

A
  1. Determinants quanti relation2. Regulatory proteins3. Therapeutic and toxic effects
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2
Q

Emax

A

Maximal response produced by a drug

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3
Q

Ec50

A

50% maximal effect

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4
Q

Bmax

A

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

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5
Q

Kd

A

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

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6
Q

Coupling

A

Transduction process that links drug occupancy of receptors and pharmacologic respnse

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7
Q

Spare receptors

A

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

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8
Q

Example spare receptors

A

Irreversible antagonist

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9
Q

90% quasi-irreversible antagonist

A

B- adrenoceptors

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10
Q

Types of antagonist

A
  1. Chemical 2. Functional3. Competitive A. Eq B. Nonequilibrium4. Noncompetitive
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11
Q

Antagonist property

A

+ affinity- efficacy

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12
Q

Other type of antagonism

A

PhysiologicalChemicalPharmacokinetic

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13
Q

Pharmacokinetic antagonist

A

One drug accelerates/ eliminates other drug

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14
Q

2 properties agonist

A

AffinityEfficacy

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15
Q

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

A

Potency

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16
Q

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

A

Dose-resp rel

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17
Q

Interaction of two agonist that act independently but cause opposite effects

A

FUNCTIONAL ANTAGONISM

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18
Q

Example func anatagonist

A

ACTHEPINEPHRINE

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19
Q

Eq competitive

A

Band is loose

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20
Q

Noneq competitive

A

Bond is covalent

21
Q

PHARMACODYNAMICS

A

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

22
Q

PHARMACOKINETICS

A

what the body does to the drug

23
Q

Examples of drugs of chem interaction

A

PROTAMINE SULFATE

24
Q

MOA: membrane surfactants

A

Amphotericin B- antifungal grrr

25
Q

MOA: denature proteins

A

ASTRINGENTS

26
Q

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

A

Therapeutic window

27
Q

Cumulative distribution of a population response to a drug

A

Quantal dose

28
Q

Uses of quantal dose

A

TD 50LD 50

29
Q

TD 50

A

Dose produce a toxic effect in 50% of population

30
Q

LD50

A

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

31
Q

Therapeutic index

A

Ratio of TD50 and ED50If ⬆️ = safer

32
Q

Propranolol

A

Competitive B- adrenoceptor antagonist

33
Q

2 therapeutic implication for competitive antagonist

A
  1. Conc of antagonist2. Conc of agonist in competition
34
Q

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

A

Phenoxybenzamine

35
Q

Types of agonist

A
  1. Partial2. Full
36
Q

Many clinical antagonist are actually

A

Weak partial agonist

37
Q

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

A

Ibuprenorphrine

38
Q

Inhibitors of tyrosine kinase for neoplastic do

A

TrastuzumabCeruximab

39
Q

Other tyrosine inhibitors in the cytoplasm that are “small mol”

A

GefitinibErlotinib

40
Q

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

A

Verapamil

41
Q

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

A

Milerinone

42
Q

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

A

Sildenafil

43
Q

PhosphorylAtion: Common theme2 func

A

AmplificationFlexible regulation

44
Q

Tx for breast ca that antagonizes GF receptor signaling

A

Trastuzumab

45
Q

Small molecule inhibitor cytoplasmic tyrosine kinaseTx CML

A

Imatinib

46
Q

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

A

Tamoxifen

47
Q

Responsiveness diminish rapidly after administration of drug

A

Tachyphylaxis

48
Q

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

A

Saralasin

2H. Pharmacology (17 decks)

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