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Pharmacology I > Lecture 4/5 - Pharmacodynamics > Flashcards

Lecture 4/5 - Pharmacodynamics Flashcards

1
Q

What is different about how corticosteroids interact with the cell?

A

Act on nuclear receptors, altering genes expressed. this causes its effects to be expressed for several weeks even with the drugs gone

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2
Q

What is an electrostatic interaction?

A

Attraction between functional groups w/ opposite charges

Can be either strong or weak depending on the charge strength

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3
Q

Describe hydrogen bonds.

A

Hydrogen covalently bonded to an electronegative atom

Weak

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4
Q

What tends to act on intracellular receptors?

A

Hormone/drug crosses plasma membrane

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5
Q

What is commonly the effect of intracellular receptor activation?

A

As a complex, stimulates gene transcription OR removes an inhibtion

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6
Q

What is the typical characteristics of intracellular receptor reaction time?

A

Normally has a lag period but will persist over time

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7
Q

What five examples given in lecture activate intracellular receptors?

A 
Corticosteriods 
Mineralcorticoids 
Sex steroids 
Vitamin D 
Thyroid hormone
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8
Q

What is the structure of a transmembrane protein?

A

Polypeptides w/ extracellular hormone binding domain + cytoplasmic enzyme domain

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9
Q

What are the three kinds of enzymes involved with the transmembrane proteins?

A

Tyrosine kinase + Serine kinase + Guanylyl cyclase

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10
Q

What happens to the transmembrane protein receptors once stimulated?

A

They are down regulated

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11
Q

What are three examples given in lecture of protein tyrosine kinase receptors?

A

Insulin + Epidermal GF + PDGF

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12
Q

Describe ligand-gated channels.

A

Receptor is linked to an ion channel, when ligand binds channel is opened and ions rush in or out of the cell

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13
Q

What ion is paired with acetylcholine/nicotinic receptors?

A

Na

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14
Q

What ion is paired with GABA receptors?

A

Cl-

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15
Q

What ion is paired with benzodiazepine receptors?

A

Cl

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16
Q

What ion is paired with the glutamate receptor?

A

Ca or Na

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17
Q

Describe a G-protein coupled receptor.

A

Coupled with G-protein to intracellular second messengers, spans the whole membrane

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18
Q

What do G proteins interact with?

A

GTP, stimulate binding + hydrolysis = GDP

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19
Q

What do Gs receptors do?

A

Stimulation the formation of cAMP

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20
Q

What do Gi receptors do?

A

Inhibit the formation of cAMP

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21
Q

What does cAMP do if it is activated?

A

PDE breaks down cAMP

cAMP also binds to intracellular protein kinases = phosphorylation of PKA + CREB

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22
Q

What is a major Gs receptor?

A

Beta1

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23
Q

What is a major Gi receptor?

A

Alpha 2

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24
Q

What compounds stimulate Gs?

A

EPI - NE - Isoproterenol - Dobutamine - Histamine - FSH - ACTH

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25
Q

What compounds stimulate Gi?

A

NE - EPI - Dexmedetomidine - Acetylcholine - Morphine - Serotonin

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26
Q

What does Gq activate?

A

Phospholipase C

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27
Q

What does PLC do?

A

Hyrolyze PIP2 into
IP3
DAG

28
Q

What does IP3 do?

A

release calcium stores

29
Q

What does DAG do?

A

Stimulate PKC

30
Q

What compounds stimulate Gq?

A

Acetylcholine - NE/EPI - Phenylephrine - Serotonin

31
Q

How does the amount of drugs bound to receptors compare to the amount of free drug?

A

Negligible

32
Q

What is response directly related to?

A

Number of receptors occupied

33
Q

When do you get a maximal response?

A

When all receptors are being used, at this point no matter how much drug you introduce into the system it will do nothing

34
Q

What does a sigmoid dose response curve allow you to do?

A

Determine EC50 (effective concentration)

35
Q

What direction are more potent drugs on dose-response curves?

A

Left

36
Q

What does the slope tell you on a dose-response curve?

A

How fast response changes with dose

37
Q

What does the quantal dose-response curve show you?

A

Frequency of desired effect with each dose (a yes or no response)
use frequency distribution plot

38
Q

What are the two components to therapeutic ratio?

A

ED50 + LD50

39
Q

What is Kd?

A

Concentration needed to produce half the maximal binding

40
Q

What is affinity ?

A

Measures the binding of drug to receptor

41
Q

What is Potency?

A

Dose require to produce a given effect

42
Q

What tells you potency?

A

EC50

43
Q

What is efficacy?

A

Degree of biological response via the binding of the drug to the receptor. NOT POTENCY

44
Q

What is intrinsic activity?

A

= efficacy, ability of the drug to initiate response

Number btwn 1 and 0

45
Q

What type of activity do agonist have?

A

Affinity + Intrinsic

46
Q

What type of activity do antagonists have?

A

Affinity + no intrinsic

47
Q

What type of activity do partial agonist have?

A

Affinity + lower intrinsic

48
Q

What is an agonist?

A

Bind to receptor and cause a response

49
Q

What is an antagonist?

A

Binds to receptor but does not cause a response, blocking the agonist from doing it’s job

50
Q

What is a partial agonist?

A

Binds to receptor and causes response but not as good on one, will block the max effect of the agonist

51
Q

What are the four types of antagonists?

A

Competitive
Non-competitive
Functional
Chemical

52
Q

What is a competitive antagonist?

A

Compete for binding site w/ agonist but with zero activity

53
Q

What effects does the competitive antagonist have?

A

Decrease affinity
NO EFFECT on maximal dose response
Shift curve to the right

54
Q

Can the agonist overcome the competitive antagonist?

A

Yes, in high enough doses

55
Q

What are non-competitive antagonist?

A

Bind irreversibly to receptor so agonist cannot bind, can also bind to a secondary site preventing the agonist from acting

56
Q

What are the effects of a non-competitive antagonist?

A

Max response is decreased

EC50 may or may not change

57
Q

What is a functional antagonist?

A

Acts through different receptor mechanisms to alter response, less specific and harder to control

58
Q

What is a chemical antagonist?

A

Neutralizes drug or compound

59
Q

What is a partial agonist?

A

Partial agonist produce response but w/ lower efficacy than full agonist

60
Q

For most drugs, what is the duration of activity linked to?

A

Time that drug is bound to receptor, meaning once drug is cleared from the blood stream action is terminated

61
Q

What happens when a partial agonist combines with a full agonist?

A

Competition for the receptor will occur causing a decrease in the response, causing them to look like antagonists

62
Q

What is an inverse agonist?

A

Does the opposite, physiologically, of what the Agonist does
Example: if the agonist increases heart rate the inverse will decrease it

63
Q

What causes tolerance?

A

Chronic administration of drugs

64
Q

How is pharmacokinetic tolerance?

A

Drug induces its own metabolism

Drug increase metabolism of another drug

65
Q

What is pharmacodynamic tolerance?

A

Up or Down regulation of receptor

Pharmacology I (21 decks)

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