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Pharmacology - Exam 1 > Pharmacodynamics and Drug Receptors > Flashcards

Pharmacodynamics and Drug Receptors Flashcards

1
Q

What is pharmacodynamics?

A
  • action of the drug on the body

- deals with the effects of drugs on biologic systems

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2
Q

receptor

A
  • molecule to which a drug binds to bring about a change in function of the biologic system
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3
Q

receptor site

A
  • specific region of the receptor molecule to which the drug binds
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4
Q

inert binding molecule or site

A
  • molecule to which a drug may bind without changing any function
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5
Q

spare receptor

A
  • receptor that does not bind drug when the [drug] is sufficient to produce maximal effect
  • Kd> EC50
  • receptor may not have a high enough affinity for the drug
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6
Q

effector

A
  • component that accomplishes the biologic effect after the receptor is activated by an agonist
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7
Q

efficacy/ maximal efficacy (Emax)

A
  • maximal effect that can be achieved with a particular drug, regardless of dose
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8
Q

potentcy

A
  • amount of drug needed to elicit desired effect/ produce a given effect
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9
Q

How is potency determined?

A
  • by the affinity of the receptor for the drug and the number of receptors available
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10
Q

graded dose-response curve

A
  • graph of increasing response to increasing [drug] or dose
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11
Q

quantal dose-response curve

A
  • graph of the fraction of a population that shows a specified response at progressively increasing doses
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12
Q

EC50

A
  • [ ] that causes 50% of the maximum effect or toxicity
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13
Q

ED50

A
  • dose that causes 50% of the maximum effect of toxicity
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14
Q

TD50

A
  • median toxic dose ([ ])

- dose ([ ]) at which toxicity occurs in 50% of cases

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15
Q

LD50 (LC50)

A
  • medial lethal dose ([ ])

- dose ([ ]) required to kill half the members of a tested population after a specified test duration

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16
Q

Kd

A
  • [drug] that binds 50% of the receptors in the system
17
Q

Bmax

A
  • maximal number of receptors bound
18
Q

agonist

A
  • drug that fully activates its receptor upon binding
19
Q

partial agonist

A
  • drug that binds to its receptor but produces a smaller effect at full dosage than a full agonist
  • less than full effect even when all the drug available is bound
20
Q

allosteric agonist

A
  • drug that binds to a receptor molecule without interfering with normal agonist binding but alters the response to the normal agonist
21
Q

antagonist

A
  • pharmacologic antagonist that binds without activating its receptor and thereby prevents activation by an agonist
22
Q

competitive antagonist

A
  • pharmacologic antagonist that can be overcome by increasing the concentration of agonist or affinity
23
Q

irreversible antagonist

A
  • pharmacologic antagonist that cannot be overcome by increasing agonist concentration
24
Q

physiological antagonist

A
  • drug that counter effects of another by binding to a different receptor and causing opposing effects
25
Q

chemical antagonist

A
  • drug that counters effects of another by binding the agonist drug ( not the receptor)
26
Q

allosteric antagonist

A
  • drug that binds to a receptor molecule without interfering with normal antagonist binding but alters the response to the normal antagonist
27
Q

TI

A
  • TD50: ED50
28
Q

signaling

A
  • once an agonist drug has bound to its receptor, some effector mechanism is activated
29
Q

What is the classic drug-receptor interactions?

A
  • drug is present in the extracellular space, effector mechanism resides inside the cell, and modifies some intracellular process
  • involves signaling across membranes
30
Q

How many types of signaling are there?

A
  • 5
31
Q

What are the signaling types?

A
  • diffusion
  • transmembrane receptors, outer and inner domain
  • receptor activates cytoplasmic tyrosine kinase molecules (JAKs) to P STATs
  • gated transmembrane channels
  • GPCR with coupling protein
32
Q

How are receptors regulated?

A
  • dynamic

- number, location, and sensitivity

33
Q

How are receptors changed?

A
  • over time
34
Q

tachyphylaxis

A
  • acute decrease in the response to a drug after its administration
35
Q

What causes tachyphylaxis?

A

-frequent or continuous exposure to agonists, resulting in short-term reduction of receptor response

36
Q

downregulation

A
  • long-term reduction in receptor number which occur in response to continuous exposure to agonists
37
Q

upregulation

A
  • increases in receptor number which occur when receptor activation is blocked for prolonged periods by pharmacologic antagonist or by denervation
38
Q

How do you overcome tachyphylaxsis?

A
  • increase dose
  • change drug
  • drug holiday

Pharmacology - Exam 1 (4 decks)

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