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
What kind of receptors are GPCRs?
Metabotropic receptors
26
Where is a GPCR found?
Part of it is outside the cell, part of it is inside the cell
27
What determines the activity of a G protein?
Whether or not a diphosphate or triphosphate is bound to it
28
How many subunits does the G protein have?
3 (alpha, beta, gamma)
29
The A subunit binds to _______. It activates effectors when ________ is bound; dissociated from BY subunits
guanine; GTP
30
The B and Y subunits activate upon dissociation from _______ subunit. It activates effectors when ________.
alpha; free
31
What are the 3 possible effectors?
adenylate cyclase PI3-kinase protein kinase C
32
Have enzymatic activity that is part of the receptor itself
receptor with intrinsic enzyme activity
33
Have enzymatic activity that is separate from the ligand binding domain
receptor with associated enzyme activity
34
Which receptor has the following enzyme activities: tyrosine kinase tyrosine phosphate serine/threonine kinase guanylyl cyclase
receptor with intrinsic enzyme activity
35
Which receptor has the following enzyme activities: janus kinase (JAK) signal transducers and activators of transcription (STAT)
receptor with associated enzyme activity
36
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.
single stretch of amino acids outside; inside
37
Where are intracellular receptors found?
inside the cell
38
Ligand for intracellular receptors must be _______ so it can pass through the membrane to bind to the receptor
lipophilic
39
Intracellular receptors mediate _____ ________
DNA transcription
40
Activation time of ion channel
milliseconds
41
Activation time of GPCR
seconds to minutes
42
Activation time of receptor with intrinsic and associated enzyme activity
minutes to hours
43
Activation time of intracellular receptor
hours to days
44
Get _______ affinity from multiple points of interaction
higher
45
Hydrophobic bonds are ________
weakest
46
Hydrogen bonds _______ and mediated by ______
weak; H+
47
Ionic bonds are most _________. They are also ______ and _______
common intermediate, reversible
48
Covalent bonds are _________ and __________
strongest, irreversible
49
What are the results of drug binding?
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
What are some small molecules that can be produced as a result of drug binding?
cAMP/cGMP PIP2 IP3 PKC intracellular Ca2+
51
Elicits max. effect
full agonist
52
Elicits less than max. effect (therefore less efficacious)
partial agonist
53
Competes with ligand (agonist) for binding to receptor
competitive antagonist
54
Binds to receptor with high affinity; there is no dissociation
non-competitive/irreversible antagonist
55
Emax = no change EC50 = increases
competitive anatagonist
56
Emax = decreases EC50 = no change
non-competitive/irreversible antagonist
57
Acts like an antagonist, blocks tonic activity of a receptor, and reduces basal activity of a receptor
inverse agonist
58
What describes the principal that not every receptor needs to be occupied to achieve maximal effect?
spare receptor theory
59
What describes the physiology of amplification of signal transduction pathways
spare receptor theory
60
Attenuated response that occurs with sustained stimulation with a drug (physiological)
tolerance
61
Modifications of the receptor to minimize signaling (cellular)
desensitization
62
Process by which the number of receptors is decreased (molecular)
downregulation