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Concepts & terms Flashcards

(31 cards)

1
Q

activates the receptor as a direct result of binding to it

A

agonist

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2
Q

produces a lower response at full receptor occupancy; concentration curve resembles that of the full agonist with some antagonist bound to the receptor sites

A

partial agonist

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3
Q

binds to the receptor but doesn’t activate generation of a signal; primary action is to interfere with the action of the agonist

A

antagonist

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4
Q

competes with the agonist for the receptor site

A

competitive antagonist

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5
Q

duration of action of irreversible antagonist

A

largely determined by the rate of turnover of the receptors and not its rate of elimination

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6
Q

the concentration of drug that produces 50% of max effect

A

EC50

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7
Q

the transduction process that links drug occupancy of receptors and pharm response

A

coupling

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8
Q

helps elicit a maximal biological response at a concentration of agonist that does not result in occupancy of the full complement of available receptors

A

spare receptors

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9
Q

can cross the plasma membrane and act on an intracellular receptor

A
corticosteroids
mineralocorticoids
sex steroids
vitamin D
thyroid hormone
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10
Q

endogenous ligands that regulate the flow of ions through the plasma membrane

A

acetylcholine
serotonin
GABA
glutamate

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11
Q

G protein-coupled receptor NTs/ligands

A
adrenergic amines
serotonin
muscarinic ACh
peptide hormones
odorants
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12
Q

degrades cAMP and IP3, respectively

A
caffeine (cAMP)
lithium ion (IP3)
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13
Q

the dose of drug required to produce 50% of maximal effect of the drug; refers to the potency

A

ED50 = median effective dose

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14
Q

dose required to produce a toxic effect in 50% of animals

A

TD50 = median toxic dose

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15
Q

toxic dose required to produce death in 50% of animals

A

LD50 = lethal toxic dose

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16
Q

the ratio of the TD50 to the LD50

A

therapeutic index

17
Q
what the body does to a drug:
absorption
distribution
metabolism
excretion
A

pharmacokinetics

18
Q

what the drug does to the body:
side effects
toxicity
withdrawal reactions

A

pharmacodynamics

19
Q

mimic actions of epinephrine or NE

A

sympathomimetics

20
Q

directly interact with and activate adrenoreceptors

A

direct agonists

21
Q

actions depend on the abilities to enhance the actions of endogenous catecholamines

A

indirect agonists

22
Q

intracellular signaling pathway that promotes release of sequestered Ca2+ increasing intracellular calcium and activating calcium-dependent kinases

23
Q

activates protein kinase C

24
Q

enzyme that increases cAMP
beta receptors and D1 receptors activate this enzyme
alpha 2 and D2 receptors inhibit it

A

adenylyl cyclase

25
primary location of beta 1 receptors
heart | activation increases contractility and direct activation of the SA node
26
mediate urinary continence
alpha receptors in bladder base, urethral sphincter and prostate Note: alpha1 receptor activation causes constriction
27
receptor that plays a role in normal ejaculation
alpha
28
agonist at both alpha and beta receptors - potent vasoconstrictor & cardiac stimulant - increases HR and contractility
epinephrine
29
agonist of both alpha and beta1 receptors - increases peripheral vascular resistance in both systolic and diastolic bp - compensatory baroreflex of heart overcomes the chronotropic effects, but positive inotropic effects are maintained
norepinephrine
30
immediate precursor to NE
dopamine
31
action of indirect-acting sympathomimetics
they are "amphetamine-like" because they displaced stores catecholamine NT and interfere with NET