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Disease and Defense- Pharm > Pharmacodynamics and Drug Receptors > Flashcards

Pharmacodynamics and Drug Receptors Flashcards

1
Q

What is D?

A

drug

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1
Q

Pharmacologic ______ largely determines the dose necessary to administer to the patient.

A

potency

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2
Q

Name 2 hormone receptors.

A

glucocorticoid; estrogen

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2
Q

The size, shape, and electrical charge of a drug determine its ______ to a particular receptor.

A

binding affinity

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2
Q

What is an agonist?

A

binds to and activates the receptor

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2
Q

Receptor antagonists refer to antagonists that _____.

A

bind to the same receptor as the agonist

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3
Q

_____ are drugs that occupy receptors and bring about a full or maximal response.

A

Full agonists

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4
Q

______ refers to the concentration (EC50) or dose (ED50) required to produce 50% of that drug’s individual maximal effect.

A

Potency

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4
Q

Physiological antagonists bind to _____.

A

a different receptor

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5
Q

What are specialized receptors?

A

membrane proteins or ion channels designed to detect chemical signals and initiate a response using signal transduction pathways

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6
Q

_____ are the components of the biologic system that accomplish the biologic effect after being activated by the receptor, i.e., they are molecules that translate the drug-receptor interaction into a change in cellular activity.

A

Effectors

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6
Q

These are membrane proteins or ion channels designed to detect chemical signals and initiate a response using signal transduction pathways.

A

specialized receptors

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8
Q

What does opening or closing a ligand gated ion channel do?

A

changes the membrane potential

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9
Q

What is an agonist to norepinephrine in the heart?

A

Dobutamine

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9
Q

What is e?

A

the specific response

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9
Q

What are EC50 and ED50?

A

Kd, or the concentration of drug at which 50% of the receptors are occupied by drug

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10
Q

The potency of a drug provides information on _____ will be required to produce a given effect.

A

how much drug (dose)

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11
Q

What is efficacy, simply stated?

A

maximum effect

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11
Q

____ is physiologic antagonist to histamine in the treatment of anaphylactic shock.

A

Epinephrine

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12
Q

______ relates the dose of drug to the drug concentration in the target organ over time.

A

Pharmacokinetics

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13
Q

Name 3 enzymes that act as receptors.

A

angiotensin converting enzyme, carbonic anhydrase, Na+-K+-ATPase

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15
Q

Effectors are ______; ie, _____.

A

the components of the biologic system that accomplishes the biologic effect after being activated by the receptor, i.e., they are molecules that translate the drug-receptor interaction into a change in cellular activity.

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15
Q

What is an antagonist?

A

prevents binding by blocking the receptor

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16
Q

______ relates the drug concentration in the target organ over time to the mechanism and magnitude of the drug effect.

A

Pharmacodynamics

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17
Q

Name 4 chemical antagonists.

A

1) EDTA to lead 2) antacids 3) osmotic diuretics 4) protamine to heparin

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18
Q

Name 3 major mechanisms of transduction and amplification.

A

1) ligand gated ion channels 2) GPCRs 3) kinase-linked or hormone receptors

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19
Q

The _____ of a drug provides information on how much drug (dose) will be required to produce a given effect.

A

potency

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20
Q

An ______ is a drug that inhibits the action of an agonist but has no effect in the absence of an agonist.

A

antagonist

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21
Q

The _____ of a drug is the most important determinant of its clinical utility.

A

efficacy

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22
Q

What are generalized receptors?

A

biological molecules with any function including enzymes, lipids, or nucleic acids

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23
Q

In noncompetitive antagonists, increasing the concentration of agonist _____.

A

can not overcome the antagonism.

24
Q

______ refers to the extent a given clinical effect can be achieved in an intact patient.

A

Efficacy

25
Q

Name 2 neurotransmitter receptors.

A

norepinephrine or dopamine

25
Q

What does a dose-response curve tell?

A

the relationship between dose or concentration of a drug and its effect

27
Q

What is the rate of response of kinase linked or hormone receptors?

A

slow (hours)

28
Q

What is a competitive reversible antagonist?

A

binds reversibly to the active site but does not activate it; blocks agonist binding

29
Q

Partial agonists are drugs that _____ but _____.

A

occupy the same receptor as the full agonist; bring about less than the maximum response, even at full dosage levels.

29
Q

What is a noncompetitive antagonist?

A

binds irreversibly or pseudoirriversibly to the active site of the receptor OR binds to an allosteric site

30
Q

The majority of drug binding sites are _____.

A

proteins

32
Q

Pharmacodynamics relates _____ to ______.

A

the drug concentration in the target organ over time; the mechanism and magnitude of the drug effect

32
Q

Name a transport protein that act as a receptor.

A

carrier molecules like the kidney Na+-K+-2Cl- cotransporter

33
Q

Pharmacologic potency largely determines ______.

A

the dose necessary to administer to the patient

35
Q

Name a norepinephrine antagonist.

A

Metoprolol

36
Q

Efficacy refers to ________.

A

the extent a given clinical effect can be achieved in an intact patient

38
Q

_____ and _____ can also act as receptors but have lower specificity.

A

Nucleic acids; membrane lipids

40
Q

What does binding to a kinase linked or nuclear receptor do?

A

change gene transcription and protein synthesis

41
Q

The _____ and _____ structural features of proteins allow for greatest specificity of drug fit.

A

secondary; tertiary

43
Q

What is potency, simply stated?

A

dose

44
Q

In _____, increasing the concentration of agonist can not overcome the antagonism.

A

noncompetitive antagonists

45
Q

An antagonist is a drug that _____ but ______.

A

inhibits the action of an agonist; has no effect in the absence of an agonist

46
Q

These are biological molecules with any function including enzymes, lipids, or nucleic acids.

A

generalized receptors

47
Q

What is the rate of response of ligand-gated ion channels?

A

very fast (msec)

48
Q

______ refer to antagonists that bind to the same receptor as the agonist.

A

Receptor antagonists

49
Q

_____ bind the agonist molecule directly and do not involve any receptor binding.

A

Chemical antagonists

51
Q

Name a structural protein that act as a receptor.

A

tubulin

52
Q

The secondary and tertiary structural features of proteins allow for ______.

A

greatest specificity of drug fit

54
Q

Pharmacokinetics relates _____ to _____.

A

the dose of drug; the drug concentration in the target organ over time

55
Q

Antagonists can be divided into ______ and _____ antagonists.

A

receptor; non-receptor

57
Q

What is the rate of response of GPCRs?

A

fast (sec)

58
Q

The more _____ a drug, the less that is needed for any given effect.

A

potent

60
Q

Nucleic acids and membrane lipids can also act as receptors but have ______.

A

lower specificity

61
Q

Nonreceptor antagonists include _____ that bind to a different receptor and ______ that bind the agonist molecule directly and do not involve any receptor binding.

A

physiological antagonists; chemical antagonists

62
Q

______ bind to a different receptor.

A

Physiological antagonists

63
Q

The ____, _____, and ______ of a drug determine its binding affinity to a particular receptor.

A

size; shape; electrical charge

64
Q

Chemical antagonists bind _____.

A

the agonist molecule directly and do not involve any receptor binding

65
Q

What is R?

A

receptor

66
Q

Name 2 receptor or voltage gated ion channels that act as receptors.

A

nicotinic cholinergic or 5HT3-serotoninergic

68
Q

Potency refers to the concentration (EC50) or dose (ED50) required to ______.

A

produce 50% of that drug’s individual maximal effect

69
Q

The glucocorticoid and estrogen receptors are types of ______.

A

hormone receptors

70
Q

In choosing between 2 drugs the prescriber considers their relative _____ rather than relative _____.

A

efficacies; potencies

71
Q

Full agonists are drugs that _____.

A

occupy receptors and bring about a full or maximal response

72
Q

_____ are drugs that occupy the same receptor as the full agonist but bring about less than the maximum response, even at full dosage levels.

A

Partial agonists

73
Q

_______ include physiological antagonists that bind to a different receptor and chemical antagonists that bind the agonist molecule directly and do not involve any receptor binding.

A

Nonreceptor antagonists

74
Q

What is Emax?

A

the maximum response possible

75
Q

Name 3 second messengers associated with GPCRs.

A

1) cAMP 2) cGMP 3) IP3

Disease and Defense- Pharm (12 decks)

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