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Topics, trends & technologies in pharmacology > Recap > Flashcards

Recap Flashcards

1
Q

affinity

A

tendency of a drug to bind to receptors

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2
Q

efficacy

A

tendency (once bound) to switch receptor into active conformation

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3
Q

intermediate efficacy

A

when 100% of receptors are occupied, response is submaximal

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4
Q

Bmax

A

maximum binding capacity (density of receptors in tissues)

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5
Q

Emax

A

maximum response of a drug

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6
Q

EC50

A

conc. needed to produce 50% max. response

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7
Q

what can’t dose-response curves measure?

A

affinity of agonist drugs

response produced is not directly proportional to receptor occupancy

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8
Q

dose-response curves - POTENCY

A

location of curve along dose axis

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9
Q

dose-response curves - MAXIMAL EFFICACY

A

greatest response

reduced efficacy = reduced max. response + slope of curve

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10
Q

dose-response curves - SLOPE

A

change in response

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11
Q

spare receptors

A

pool of receptors is larger than number needed to evoke full response

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12
Q

competitive antagonism

A

agonist occupancy = reduced

raising agonist conc. resolves this (summountable)

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13
Q

competitive antagonism - curve shift

A

fixed conc. shifts curve to right w/o change in slope or maximum

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14
Q

dose ratio (r)

A

ratio by which agonist conc. has to be raised in presence of antagonist in order to restore given level of response

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15
Q

relationship between dose ratio + antagonist concentration

A

linear

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16
Q

irreversible antagonism

A

slow dissociation

17
Q

intrinsic efficacy

A

drug-dependent component

ability of agonist drug molecule, once bound, to activate receptor protein

18
Q

tissue-dependent component of efficacy

A

no. of receptors it expresses + efficiency of receptor coupling activation to the measured tissue response

19
Q

what happens to graph if a partial agonist is competing with a full agonist?

A

acts as antagonist

shifts curve to right

20
Q

constitutive receptor activity

A

activation of receptor without binding of agonist

21
Q

inverse agonist

A

binds to same receptor as agonist but induces opposite response

22
Q

neutral antagonist

A

blocks effects of both an agonist or inverse agonist

23
Q

orthosteric

A

primary binding site

24
Q

allosteric modulators - effects it may have

A

increase/decrease affinity of agonists

modifying efficacy

produce response

25
Q

chemical antagonism

A

2 substances combine in solution + effect of active drug is lost

26
Q

pharmacokinetic antagonism

A

antagonist decreases conc. of active drug at its site of action

-> metabolic degradation increases
-> rate of absorption decreases
-> rate of renal excretion increases

27
Q

physiological antagonism

A

interaction of 2 drugs whose opposing actions in the body cancel each other out

28
Q

desensitisation/tachyphylaxis

A

effect of drug diminishes when given continuously or repeatedly

29
Q

tolerance

A

gradual decrease in responsiveness to a drug

30
Q

refractoriness

A

loss of therapeutic activity

31
Q

resistance

A

loss of effectiveness of antimicrobial/antitumour drugs

32
Q

reasons for desensitisation/tolerance - CHANGE IN RECEPTORS

A

conformational change

tight binding of agonist w/o opening ionic channel

phosphorylation of intracellular regions in receptor protein - interferes with ability to activate 2nd messenger cascades

33
Q

reasons for desensitisation/tolerance - TRANSLOCATION OF RECEPTORS

A

prolonged exposure = reduction in no. of receptors expressed on cell surface

due to internalisation -> receptors taken into cell by endocytosis

34
Q

reasons for desensitisation/tolerance - EXHAUSTION OF MEDIATORS

A

due to depletion of essential intermediate substances

35
Q

reasons for desensitisation/tolerance - ALTERED DRUG METABOLISM

A

same dose = reduced plasma concentration due to increased metabolic degradation

36
Q

Law of Mass Action

A

rate of chemical reaction is proportional to product of concentration of R

37
Q

Ka

A

concentration of drug required to occupy 50% of sites at eq

increased affinity = decreased Ka

38
Q

PA2

A

-ve log of molar conc. of antagonist required to produce agonist dose ratio equal to 2

Topics, trends & technologies in pharmacology (7 decks)

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