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2S PC & TC > U2.1 DRG PHARMACODYNAMICS & RECEPTORS > Flashcards

U2.1 DRG PHARMACODYNAMICS & RECEPTORS Flashcards

1
Q

Actions or effects of the drug on the body

A

Pharmacodynamics

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2
Q

plays a major role in deciding whether a group is appropriate therapy for a particular symptom or disease

A

Pharmacodynamics

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3
Q

Specific molecules/target molecules of the drug so that they could interact with the body that produce changes in the function of the system

A

Receptors

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4
Q

Determine the quantitative relations between dose or concentration of drug and pharmacologic effects

A

Receptors

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5
Q

measurable to its pharmacologic effects

A

Dose

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6
Q

Drugs are _______ in choosing a drug molecule to bind to avoid constant activation or inhibition by promiscuous binding of many different molecules

A

Selective

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7
Q

Drugs have _______ binding and _________ with receptors

A

Selective binding and specificity

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8
Q

Changes its function upon binding in such a way that the function of the biologic system is altered in order to have pharmacologic effect

A

Receptors

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9
Q

Receptors are ___________ in ligand binding characteristics (respond to proper chemical signals and not to meaningless ones)

A

selective

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10
Q

Mediate the actions of both pharmacologic agonists and antagonists

A

Receptors

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11
Q

Most receptors are ______ which provide the necessary diversity and specificity of shape and electrical charge

A

proteins

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12
Q

Specific binding region of the macromolecule

A

Receptor Site or Recognition Site

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13
Q

happens to the drug when there is an interaction between the drug and the receptor

A

initiates the action of the drug

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14
Q

Receptor sites have _______ and _______ affinity to the drug molecule.

A

High and selective affinity

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15
Q

T/F Even if the drug enters the body, but it cannot reach the target receptor, it will still take effect

A

F; it will not take effect

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16
Q

Classification of Receptors

Best characterized drug receptors

A

Regulatory Proteins

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17
Q

Classification of Receptors

Mediates the action of endogenous chemical signals like neurotransmitters, autacoids, and hormones

A

Regulatory Proteins

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18
Q

Classification of Receptors

Mediates the effects of the most useful therapeutic agents as it takes effect immediately

A

Regulatory Proteins

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19
Q

Classification of Receptors

Inhibited (or less commonly, activated) by binding a drug

A

Enzymes

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20
Q

Classification of Receptors

Na+/K+ ATPase Pump, the membrane
receptor for digitalis

A

Transport Proteins

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21
Q

Classification of Receptors

Stabilizes Tubulin

A

Structural Proteins

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22
Q

Molecules that translate the drug-receptor interaction into a change in cellular activity

A

Effectors

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23
Q

T/F Some receptors are also effectors

A

True

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24
Q

Signaling Mechanism

________ drug that crosses the plasma membrane and acts on intracellular receptors

A

Lipid-soluble

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24
Q

T/F A single molecule may incorporate both the drug binding
site and the effector mechanism

A

True

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25
Q

Signaling Mechanism

Steroids

A

Lipid-soluble drugs

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26
Q

Signaling Mechanism

Where steroid attaches to alter genetic transcription

A

hsp90

27
Q

Signaling Mechanism

Transmembrane receptor protein-intracellular enzymatic activity is regulated by a _________ that binds to the proteins’ extracellular domain

A

ligand

28
Q

Signaling Mechanism

Transmembrane Receptors that binds and stimulates a ____________

A

Tyrosine kinase

29
Q

Signaling Mechanism

Other term for Protein Tyrosine Kinase Associated receptors

A

JAK - Janus Kinase

30
Q

Signaling Mechanism

Type of receptor that causes dimerization

A

Transmembrane receptors that stimulates protein tyrosine kinase

31
Q

Signaling Mechanism

Insulin

A

Transmembrane receptors that bind and stimulates protein tyrosine kinase

32
Q

Signaling Mechanism

_______________ transmembrane ion channel: which regulates the opening of the ion channel

A

Ligand-gated

33
Q

Signaling Mechanism

causes drug to mimic or block the
action of agonists

A

ligand-gated ion channels

34
Q

Signaling Mechanism

Type of receptor that is similar to our neurotransmitter receptors

A

Ligand-gated transmembrane ion channel

35
Q

Signaling Mechanism

GABA, excitatory acetylcholine

A

ligand-gated transmembrane ion channel

36
Q

Signaling Mechanism

Receptors transmit its signal across the plasma membrane by (increasing/decreasing) transmembrane conductance of the relevant ion

A

Increasing transmembrane conductance

37
Q

Signaling Mechanism

Binding site of Acetylcholine outside to allow opening of a central aqueous transmembrane ion channel where sodium enters

A

α biding sites

38
Q

Signaling Mechanism

Catecholamine / epinephrine

A

Transmembrane receptor coupled with G protein

39
Q

Signaling mechanism

Increasing the intracellular concentrations of second messengers

A

Transmembrane receptor coupled with G protein

40
Q

modulate the production of intracellular messengers

A

G protein

41
Q

Type of G protein

↑ Adenylyl cyclase → ↑ cAMP

A

Gs, Golf

42
Q

Type of G protein

Receptor for
- β-Adrenergic amines
- Histamine
- Serotonin
- Glucagon
- Many other hormones

A

Gs

43
Q

Type of G protein

↓ Adenylyl cyclase → ↓ cAMP

A

Gi1, Gi2, Gi3

44
Q

Type of G protein

Open cardiac K+ channels → ↓ heart rate

A

Gi1, Gi2, Gi3

45
Q

Type of G protein

receptor for
- α2-Adrenergic amines
- Acetylcholine (muscarinic)
- Opioids Serotonin
- Many others

A

Gi1, Gi2, Gi3

46
Q

Type of G protein

Receptor for Odorants (olfactory epithelium)

A

Golf

47
Q

Type of G protein

Receptors for Neurotransmitters in brain (not yet specifically identified)

A

Go

48
Q

Type of G protein

↑ Phospholipase C → ↑ IP3, diacylglycerol, cytoplasmic Ca2+

A

Gq

49
Q

Type of G protein

Receptors for
- Acetylcholine (muscarinic)
- Bombesin
- Serotonin (5-HT2)
- Many others

A

Gq

50
Q

Type of G protein

Receptors for Photons (rhodopsin and color opsins in retinal rod and cone cells)

A

Gt1, Gt2

51
Q

Type of G protein

↑ cGMP phosphodiesterase → ↓ cGMP (phototransduction)

A

Gt1, Gt2

52
Q

Intracellular Second Messengers

Mediates hormonal responses

A

cAMP (Cyclic adenosine monophosphate)

53
Q

Intracellular Second Messengers

cAMP mobilizes stored energy (breakdown of carbohydrates in the liver stimulated by _____________

A

catecholamines

54
Q

cAMP

Conservation of water by the kidneys mediated by ___________

A

vasopressin

55
Q

cAMP

Calcium homeostasis

A

Parathyroid hormone

56
Q

cAMP

Heart rate and contraction by

A

beta-adrenomimetic catecholamines

57
Q

T/F cAMP is a product of the enzyme adenylyl cyclase and it converts ATP to cAMP

A

T

58
Q

stop the effect of your cAMP

A

Phosphatase

59
Q

Intracellular Second Messengers

Bind to receptors linked to G proteins while other bind to receptor tyrosine kinases

A

Calcium and Phosphoinositides

60
Q

Intracellular Second Messengers

Calcium and Phosphoinositides stimulates the membrane enzyme __________

A

phospholipase C

61
Q

Intracellular Second Messengers

phospholipase C cleaves PIP2 into

A

diacylglycerol (DAG) and Inositol Triphosphate (IP3)

62
Q

Calcium and Phosphoinositides

release the Calcium (Ca2+)

A

Inositol Triphosphate (IP3)

63
Q

Intracellular Second Messengers

Few signaling roles in a few cell types like the intestinal mucosa and vascular smooth muscle cells

A

cGMP (Cyclic guanosine monophosphate)

64
Q

Intracellular Second Messengers

Causes Relaxation of vascular smooth muscles by a kinase-mediated mechanism

A

cGMP (Cyclic guanosine monophosphate)

2S PC & TC (17 decks)

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