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D1 Spring > Pharm Exam 1 > Flashcards

Pharm Exam 1 Flashcards

1
Q

What term refers to an exogenous chemical agent used to modify physiology?

A

Drug

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2
Q

What term refers to the study of the use of chemical agents for therapeutic purposes?

A

Pharmacology

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3
Q

What term refers to adverse effects of a drug?

A

Toxicology

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4
Q

What term refers to a site of action/target of a drug?

A

Receptor

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5
Q

What is a drug that mimics/stimulates a biological effect called?

A

Agonist

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6
Q

What is a drug that inhibits a biological effect called?

A

Antagonist

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7
Q

What term describes what the drug does to the body?

A

Pharmacodynamics

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8
Q

What are examples of pharmacodynamics?

A

Therapeutic effect and toxic effect

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9
Q

What term describes what the body does to the drug?

A

Pharmacokinetics

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10
Q

What are examples of pharmacokinetics?

A

Absorption, distribution, metabolism, and elimination

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11
Q

What term refers to the study of how a drug acts to achieve a response by altering or modifying existing physiologic or pathologic processes?

A

Pharmacodynamics

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12
Q

Drug actions are ___________

A

Specific

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13
Q

Basic principle: drugs have _______ molecular targets/receptors in the body

A

Specific

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14
Q

What are the 5 classifications of receptors?

A
  1. Ion channel-linked receptor
  2. G-protein coupled receptor (GPCR)
  3. Receptor with intrinsic enzyme activity
  4. Receptor with associated enzyme activity
  5. Intracellular receptor
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15
Q

What are the 2 types of ion channel-linked receptors?

A
  1. Voltage gated ion channel
  2. Ionotropic (ligand-gated) ion channel
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16
Q

What do ion channel-linked receptors control?

A

Flow of ions from outside cell to inside cell

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17
Q

Where are ion channel-linked receptors found?

A

On cell surface

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18
Q

What determines if the ion channel is open or closed?

A

Whether or not the ligand is bound to the ion channel-linked receptor

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19
Q

What are ion-channel linked receptors made up of?

A

Multiple subunits

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20
Q

How does binding of the ligand to an ion channel-linked receptor effect the cell membrane?

A

The membrane either depolarizes or hyperpolarizes

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21
Q

What mediates the signaling of a G protein-coupled receptor (GPCR)e?

A

G proteins

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22
Q

How many times does a GPCR span the membrane?

A

7 times (it has 7 transmembrane domains)

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23
Q

What is the largest family of receptors?

A

GPCR

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24
Q

What kind of receptor is a target for 50-70% of drugs?

A

GPCR

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25
Q

What kind of receptors are GPCRs?

A

Metabotropic receptors

26
Q

Where is a GPCR found?

A

Part of it is outside the cell, part of it is inside the cell

27
Q

What determines the activity of a G protein?

A

Whether or not a diphosphate or triphosphate is bound to it

28
Q

How many subunits does the G protein have?

A

3 (alpha, beta, gamma)

29
Q

The A subunit binds to _______. It activates effectors when ________ is bound; dissociated from BY subunits

A

guanine; GTP

30
Q

The B and Y subunits activate upon dissociation from _______ subunit. It activates effectors when ________.

A

alpha; free

31
Q

What are the 3 possible effectors?

A

adenylate cyclase
PI3-kinase
protein kinase C

32
Q

Have enzymatic activity that is part of the receptor itself

A

receptor with intrinsic enzyme activity

33
Q

Have enzymatic activity that is separate from the ligand binding domain

A

receptor with associated enzyme activity

34
Q

Which receptor has the following enzyme activities:

tyrosine kinase
tyrosine phosphate
serine/threonine kinase
guanylyl cyclase

A

receptor with intrinsic enzyme activity

35
Q

Which receptor has the following enzyme activities:

janus kinase (JAK)
signal transducers and activators of transcription (STAT)

A

receptor with associated enzyme activity

36
Q

For both receptors with intrinsic and associated enzyme activity, these receptors span the membrane with a ______________. The ligand binding domain is _______ the cell; the signaling domain is __________ the cell.

A

single stretch of amino acids

outside; inside

37
Q

Where are intracellular receptors found?

A

inside the cell

38
Q

Ligand for intracellular receptors must be _______ so it can pass through the membrane to bind to the receptor

A

lipophilic

39
Q

Intracellular receptors mediate _____ ________

A

DNA transcription

40
Q

Activation time of ion channel

A

milliseconds

41
Q

Activation time of GPCR

A

seconds to minutes

42
Q

Activation time of receptor with intrinsic and associated enzyme activity

A

minutes to hours

43
Q

Activation time of intracellular receptor

A

hours to days

44
Q

Get _______ affinity from multiple points of interaction

A

higher

45
Q

Hydrophobic bonds are ________

A

weakest

46
Q

Hydrogen bonds _______ and mediated by ______

A

weak; H+

47
Q

Ionic bonds are most _________. They are also ______ and _______

A

common

intermediate, reversible

48
Q

Covalent bonds are _________ and __________

A

strongest, irreversible

49
Q

What are the results of drug binding?

A
  1. change in intracellular ions (thru ion channels)
  2. produce small molecules (thru GPCRs)
  3. protein phosphorylation (activates proteins)
  4. DNA transcription (intracellular receptors)
50
Q

What are some small molecules that can be produced as a result of drug binding?

A

cAMP/cGMP
PIP2
IP3
PKC
intracellular Ca2+

51
Q

Elicits max. effect

A

full agonist

52
Q

Elicits less than max. effect (therefore less efficacious)

A

partial agonist

53
Q

Competes with ligand (agonist) for binding to receptor

A

competitive antagonist

54
Q

Binds to receptor with high affinity; there is no dissociation

A

non-competitive/irreversible antagonist

55
Q

Emax = no change
EC50 = increases

A

competitive anatagonist

56
Q

Emax = decreases
EC50 = no change

A

non-competitive/irreversible antagonist

57
Q

Acts like an antagonist, blocks tonic activity of a receptor, and reduces basal activity of a receptor

A

inverse agonist

58
Q

What describes the principal that not every receptor needs to be occupied to achieve maximal effect?

A

spare receptor theory

59
Q

What describes the physiology of amplification of signal transduction pathways

A

spare receptor theory

60
Q

Attenuated response that occurs with sustained stimulation with a drug (physiological)

A

tolerance

61
Q

Modifications of the receptor to minimize signaling (cellular)

A

desensitization

62
Q

Process by which the number of receptors is decreased (molecular)

A

downregulation

D1 Spring (47 decks)

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