Pharmacodynamic Principles - 1 Flashcards

1
Q

the study of what the drug does to the body

A

pharmacodynamics.

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2
Q

what does pharmacodynamics include? “HINT:3”

A

1- the action of the drug on the body (beneficial and harmful).
2- influence of drug concentrations on the magnitude of response.
3- modification of the action of one drug by another drug.

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3
Q

how do antacids work?

A

neutralization of gastric HCL

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4
Q

how do chelating agents work?

A

chelation of heavy metals.

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5
Q

give examples of chelating agents?

A

EDTA and dimercaprol.

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6
Q

when are chelating agents used?

A

in cases of heavy metal poisoning.

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7
Q

give an example diuretic?

A

mannitol.

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8
Q

give an example of a laxative?

A

mag. sulphate.

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9
Q

how do diuretics and laxatives work?

A

osmotic activity.

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10
Q

how does activated charcoal work?

A

adsorptive property.

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11
Q

give an example of a radioisotope?

A

l-131

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12
Q

how do radioisotopes work?

A

radioactivity.

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13
Q

majority of drugs act by binding to their _____ or _____________

A

targets or specific receptors.

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14
Q

a macromolecule or binding site located on the surface or inside the cell that serves to recognize the signal molecule/drug and initiate response to it, but itself has no other function.

A

receptor.

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15
Q

list the 4 receptor families?

A

1- ligand - gated ion channels.
2- G-protein coupled receptors.
3- enzyme linked receptors.
4- cytosolic (nuclear) receptors.

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16
Q

where are receptors found in ligand-gated ion channels?

A

coupled directly to membrane ion channels

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17
Q

speed of response in ligand-gated ion channels is?

A

millisecond.

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18
Q

give an example of a drug that acts on ligand-gated ion channels?

A

neurotransmitters.

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19
Q

where are receptors in G-protein coupled receptors found?

A

bound to cell membrane and coupled intracellular effector system by a g-protein.

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20
Q

speed of response in g-protein coupled receptors?

A

seconds.

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21
Q

give an example of a drug that acts on GPCR?

A

catecholamines.

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22
Q

binding of a drug to an enzyme linked receptor results in?

A

increased enzymatic activity.

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23
Q

speed of response in an enzyme linked receptor is?

A

minutes to hours.

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24
Q

give an example of a drug that acts on enzyme linked receptors?

A

receptors for growth hormone and insulin

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25
Q

what is the function of a cytosolic (nuclear) receptors?

A

regulate DNA transcription and protein synthesis.

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26
Q

speed of response in a cytosolic (nuclear) receptors?

A

hours to days.

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27
Q

give an example of a drugs that act on cytosolic (nuclear) receptors?

A

steroid receptors, thyroid receptors.

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28
Q

list the 4 different G proteins based on alpha subunit?

A

1- Gs
2- Gi
3- Go
4- Gq

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29
Q

what is the function of Gs?

A

adenylyl cyclase activation, Ca2+ channel opening.

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30
Q

what is the function of Gi?

A

adenylyl cyclase inhibition, K+ channel opening.

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31
Q

what is the function of Go?

A

Ca2+ channel inhibition.

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32
Q

what is the function of Gq?

A

phospholipase C activation.

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33
Q

list 5 examples of GPCRs?

A

1- muscarinic receptor (M2): Gi,Go.
2- muscarinic (M1): Gq.
3- B adrenergic: Gs.
4- Alpha 1 adrenergic: Gq.
5- alpha 2 adrenergic: Gi.

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34
Q

list the 4 mechanisms of drug action?

A

1- enzyme inhibition.
2- transporters.
3- alter microbial processes.
4- incorporation into larger molecules.

35
Q

list 2 examples of drugs that inhibit enzymes?

A

1- aspirin inhibits cyclooxygenase enzyme.
2- allopurinol inhibits xanthine.

36
Q

give an example of drug that uses transporters?

A

blockade of anion transport in renal tubule by probenecid increases uric acid excretion.

37
Q

give an example of a drug that alters microbial processes?

A

penicillin interferes with formation of bacterial cell wall.

38
Q

give an example of a drug that incorporates into larger molecules?

A

5-flurouracil, an anticancer drug, is incorporated in place of uracil.

39
Q

list the 3 types of therapeutic biologics?

A

1- genetically engineered enzymes and monoclonal antibodies.
2- genetically modified viruses and microbes.
3- gene therapy products.

40
Q

give an example of generically modified viruses and microbes?

A

genetically modified live oncolytic herpes virus to treat melanoma.

41
Q

give an example of gene therapy products?

A

using viruses as vectors to replace genetic mutations.

42
Q

Number of drug receptor complexes determines ______?

A

Amount of response

43
Q

Receptors are responsible for _______?

A

Selectivity of drug action

44
Q

Any molecule which attaches selectively to particular receptors or sites?

A

Ligand

45
Q

List the 4 types of ligands?

A

1- agonist.
2- antagonist.
3- partial agonist.
4- inverse agonist.

46
Q

Agent which activates the receptor to produce an effect similar to the psychological signal molecule?

A

Agonist

47
Q

Which ligand has both affinity and a maximal intrinsic activity (IA=1)?

A

Agonist

48
Q

Give an example of a drug and which receptor is it an agonist to?

A

Salbutamol (B2 agonist).

49
Q

Which drug produces longer bronchodilation than adrenaline?

A

Salbutamol

50
Q

An agent which prevents the action of an agonist on a receptor but does not have any effect of its own?

A

Antagonist

51
Q

Which ligand has affinity and zero intrinsic activity (IA=0)?

A

Antagonist

52
Q

Give an example of a drug and which receptor are they an antagonist to?

A

Propanol is a B antagonist (B blocker)

53
Q

An agent which activates the receptor to produce submaximal effect but antagonizes the action of a full antagonist?

A

Partial agonist

54
Q

Which ligand has affinity and submaximal intrinsic activity (IA between 0 and 1)?

A

Partial agonist

55
Q

Give an example of a partial and which receptor?

A

Pindol is a partial agonist at B receptor.

56
Q

An agent which activates a receptor to produce an effect in the opposite direction to that of the agonist?

A

Inverse agonist

57
Q

Which ligand has affinity and intrinsic activity (IA = between 0-1)

A

Inverse agonist

58
Q

Give an example of an agonist, their inverse agonist , which receptor do they work on, and their effects?

A

Benzodiazepines, produce sedation, anxiolysis and control convulsions (GABA receptor agonist).
B-Carbolines (inverse agonist of GABA receptor), produce stimulation, anxiety and convulsions.

59
Q

Increase in number of receptors

A

Up regulation of receptors

60
Q

Decrease in number of receptors

A

Down regulation of receptors

61
Q

Up regulation happens by continued presence of an ______ or absence of _______

A

Presence of Antagonist.
Absence of Agonist.

62
Q

MI can be precipitated on abrupt withdrawal of which drugs?

A

Beta-blockers

63
Q

How can abrupt cessation of B-blockers cause MI?

A

Continuous use of beta-blockers, up regulation of beta receptors, on abrupt cessation, endogenous epinephrine acts on large number of beta receptors, MI

64
Q

Down regulation of receptors happiness because of a continued presence of an _____

A

Presence of an agonist

65
Q

List the 2 factors that can bring about down regulation of receptors?

A

1- internalization of the receptor.
2- decreased synthesis/ increased destruction of the receptor.

66
Q

Asthma patients treated continuously with ______ become ______ responsive to them

A

Beta agonist.
Less.

67
Q

Dose response curve is which shape?

A

Rectangular hyperbola

68
Q

When response is plotted again log(dose), the curve becomes which shape?

A

Sigmoid.

69
Q

Linear response is seen in the ______% response zone

A

30-70%

70
Q

Amount of drug needed to produce the same response

A

Potency

71
Q

Potency is important for what?

A

Choosing the dose of the drug

72
Q

10 mg of morphine = 100 mg of pethidine as an analgesic.
Which drug is more potent?

A

Morphine

73
Q

The maximal response that can be elicited by the drug

A

Efficacy

74
Q

Efficacy is important for what?

A

Choosing the drug

75
Q

10 mg of morphine can relive chest pain of MI. Very high dose of aspirin is not able to relieve the same chest pain.
Which drug has higher efficacy?

A

Morphine

76
Q

Small increase is dose will markedly increase the response

A

Steep slope.

77
Q

Little increase in response occurs over a wide dose range?

A

Flat slope

78
Q

Gap between therapeutic effect DRC and the adverse effect of DRC

A

therapeutic index

79
Q

Therapeutic index is expressed by what?

A

TI = LD50/ED50
LD50 = dose which kills 50% of recipients.
ED 50= dose which produces specified effect in 50% recipients.

80
Q

List the 2 factors that bound the therapeutic window/ range?

A

1- dose which produces minimal therapeutic effect.
2- dose which produces maximal acceptable adverse effect

81
Q

Drugs with wide therapeutic range are _____ at high doses?

A

Safe

82
Q

Give an example of a drug with wide therapeutic range which are safe at high doses

A

Paracetamol

83
Q

Drugs with a narrow therapeutic range can be _____ at slight increase in dose

A

Toxic

84
Q

Give an example of a drug with a narrow therapeutic range which can be toxic at slight increase in dose?

A

Theophylline.