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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
Name 4 chemical antagonists.
1) EDTA to lead 2) antacids 3) osmotic diuretics 4) protamine to heparin
18
Name 3 major mechanisms of transduction and amplification.
1) ligand gated ion channels 2) GPCRs 3) kinase-linked or hormone receptors
19
The _____ of a drug provides information on how much drug (dose) will be required to produce a given effect.
potency
20
An ______ is a drug that inhibits the action of an agonist but has no effect in the absence of an agonist.
antagonist
21
The _____ of a drug is the most important determinant of its clinical utility.
efficacy
22
What are generalized receptors?
biological molecules with any function including enzymes, lipids, or nucleic acids
23
In noncompetitive antagonists, increasing the concentration of agonist \_\_\_\_\_.
can not overcome the antagonism.
24
\_\_\_\_\_\_ refers to the extent a given clinical effect can be achieved in an intact patient.
Efficacy
25
Name 2 neurotransmitter receptors.
norepinephrine or dopamine
25
What does a dose-response curve tell?
the relationship between dose or concentration of a drug and its effect
27
What is the rate of response of kinase linked or hormone receptors?
slow (hours)
28
What is a competitive reversible antagonist?
binds reversibly to the active site but does not activate it; blocks agonist binding
29
Partial agonists are drugs that _____ but \_\_\_\_\_.
occupy the same receptor as the full agonist; bring about less than the maximum response, even at full dosage levels.
29
What is a noncompetitive antagonist?
binds irreversibly or pseudoirriversibly to the active site of the receptor OR binds to an allosteric site
30
The majority of drug binding sites are \_\_\_\_\_.
proteins
32
Pharmacodynamics relates _____ to \_\_\_\_\_\_.
the drug concentration in the target organ over time; the mechanism and magnitude of the drug effect
32
Name a transport protein that act as a receptor.
carrier molecules like the kidney Na+-K+-2Cl- cotransporter
33
Pharmacologic potency largely determines \_\_\_\_\_\_.
the dose necessary to administer to the patient
35
Name a norepinephrine antagonist.
Metoprolol
36
Efficacy refers to \_\_\_\_\_\_\_\_.
the extent a given clinical effect can be achieved in an intact patient
38
\_\_\_\_\_ and _____ can also act as receptors but have lower specificity.
Nucleic acids; membrane lipids
40
What does binding to a kinase linked or nuclear receptor do?
change gene transcription and protein synthesis
41
The _____ and _____ structural features of proteins allow for greatest specificity of drug fit.
secondary; tertiary
43
What is potency, simply stated?
dose
44
In \_\_\_\_\_, increasing the concentration of agonist can not overcome the antagonism.
noncompetitive antagonists
45
An antagonist is a drug that _____ but \_\_\_\_\_\_.
inhibits the action of an agonist; has no effect in the absence of an agonist
46
These are biological molecules with any function including enzymes, lipids, or nucleic acids.
generalized receptors
47
What is the rate of response of ligand-gated ion channels?
very fast (msec)
48
\_\_\_\_\_\_ refer to antagonists that bind to the same receptor as the agonist.
Receptor antagonists
49
\_\_\_\_\_ bind the agonist molecule directly and do not involve any receptor binding.
Chemical antagonists
51
Name a structural protein that act as a receptor.
tubulin
52
The secondary and tertiary structural features of proteins allow for \_\_\_\_\_\_.
greatest specificity of drug fit
54
Pharmacokinetics relates _____ to \_\_\_\_\_.
the dose of drug; the drug concentration in the target organ over time
55
Antagonists can be divided into ______ and _____ antagonists.
receptor; non-receptor
57
What is the rate of response of GPCRs?
fast (sec)
58
The more _____ a drug, the less that is needed for any given effect.
potent
60
Nucleic acids and membrane lipids can also act as receptors but have \_\_\_\_\_\_.
lower specificity
61
Nonreceptor antagonists include _____ that bind to a different receptor and ______ that bind the agonist molecule directly and do not involve any receptor binding.
physiological antagonists; chemical antagonists
62
\_\_\_\_\_\_ bind to a different receptor.
Physiological antagonists
63
The \_\_\_\_, \_\_\_\_\_, and ______ of a drug determine its binding affinity to a particular receptor.
size; shape; electrical charge
64
Chemical antagonists bind \_\_\_\_\_.
the agonist molecule directly and do not involve any receptor binding
65
What is R?
receptor
66
Name 2 receptor or voltage gated ion channels that act as receptors.
nicotinic cholinergic or 5HT3-serotoninergic
68
Potency refers to the concentration (EC50) or dose (ED50) required to \_\_\_\_\_\_.
produce 50% of that drug’s individual maximal effect
69
The glucocorticoid and estrogen receptors are types of \_\_\_\_\_\_.
hormone receptors
70
In choosing between 2 drugs the prescriber considers their relative _____ rather than relative \_\_\_\_\_.
efficacies; potencies
71
Full agonists are drugs that \_\_\_\_\_.
occupy receptors and bring about a full or maximal response
72
\_\_\_\_\_ are drugs that occupy the same receptor as the full agonist but bring about less than the maximum response, even at full dosage levels.
Partial agonists
73
\_\_\_\_\_\_\_ 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.
Nonreceptor antagonists
74
What is Emax?
the maximum response possible
75
Name 3 second messengers associated with GPCRs.
1) cAMP 2) cGMP 3) IP3

Disease and Defense- Pharm (12 decks)

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