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Pharmacodynamics Flashcards

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1
Q

What is pharmacodynamics

A

the effect of a drug on the body

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2
Q

What are the 4 drug receptor types

A

Ligand-gated ion channels
G-protein-coupled receptors
Kinase-linked receptors
Nuclear receptors (DNA coupled)

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3
Q

Attributes of ligand-gated ion channels

A

Milliseconds
Hyperpolarization or depolarization
Nicotinic ACh receptor

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4
Q

Attributes of G-protein-coupled receptors

A

Seconds
Crosses membrane 7 times
Muscarinic ACh receptor

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5
Q

Attributes of Kinase-linked receptors

A

Hours
Joins together for an intracellular response/ binds to impact a different receptor
Cytokine receptors

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6
Q

Attributes of nuclear receptors

A

Hours
occurs intracellularly requires a lipophilic ligand
Estrogen

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7
Q

What is a receptor

A

a component on or in a cell that a substance can bind to

primary location where drugs bind to have their effect

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8
Q

What does a drug target

A

Receptors
Enzymes
Non-human cells

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9
Q

What are all the different drug-receptor interactions

A 
Specific
Selective
Agonist
Antagonist
Competitive antagonist
Non-competitive antagonist
Partial agonist
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10
Q

What is specificity

A

drug only binds to one type of receptor

Ex: A not B

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11
Q

What is selectivity

A

drug prefers to bind to one subtype of a receptor but can still bind to others
Ex: B1 mostly, B2 sometimes

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12
Q

What is an agonist

A

OPTIMUS PRIME DRUG

drugs that occupy receptors and activate them

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13
Q

What is an antagonist

A

MEGATRON DRUG

drugs that occupy receptors and block receptor activation by agonists

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14
Q

What is a competitive antagonist

A

Agonist and antagonist compete to bind to the receptor

highest concentration wins

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15
Q

What is a non-competitive antagonist

A

Near or irreversible binding to receptor

More than one attachment point on the receptor for both the agonist and antagonist so the activation is blocked

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16
Q

What is a partial agonist

A

Doesn’t fit the receptor perfectly but well enough
Lower dose=agonist effect
Higher dose=antagonist effect

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17
Q

Where do opioid receptors and ligand reactions occur

A

mu and kappa receptors

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18
Q

What is a dose response curve based on

A

individual or homogenous population

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19
Q

What is Emax

A

the maximal response from a drug
all receptors are saturated
may cause toxicity

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20
Q

What is ED50

A

the effective dose to get 50% of the expected response

AKA Kd or EC50

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21
Q

What does potency measure

Study These Flashcards
A

binding affinity

22
Q

If a drug has a low ED50 it means

Study These Flashcards
A

it is more potent because it takes less to get the desired response

23
Q

How many receptors will be filled with natural agonists produced by the body

24
Q

What other forms of antagonism are there

Study These Flashcards
A

chemical
physiologic
pharmacokinetic

25
What is chemical antagonism
two drugs reacting with each other to diminish the effect of one drug
26
What is a physiologic antagonist
two drugs with opposite effects
27
What are the two types of pharmacokinetic antagonism
One drug induces or inhibits metabolism or another drug | Receptor changes
28
What are common receptor changes
desensitization | decreased receptor #
29
What is a common cause for receptor changes
long term drug use
30
What does a Quantal-dose response curve measure
Safety | % or # of population who achieve a particular response at a given dose
31
What are the steps to make a quantal-dose response curve
Determine dose of beneficial effect determine dose of harmful effect plot on bell-shaped curve convert to sigmoid curve
32
What is therapeutic index
ratio of TD50 to ED50 | narrow = increased likelihood of ADRs.
33
How is therapeutic index calculated
TD50/ED50
34
What is TD50
the dose at which 50% of the population have a toxic response
35
Define adverse drug reaction
response to a medicine which is noxious and unintended, and which occurs at doses normally used in man
36
Define side effect
any unintended effect of a pharmaceutical product occurring at doses normally used by a patient which is related to the pharmacological properties of the drug
37
Define medication error
any preventable event that may cause or lead to inappropriate medication use or patient harm while the medication is in the control of the health care professional, patient, or consumer
38
Define adverse event/experience
any unintended medical occurrence that may present during treatment with a medicine, but which does not necessarily have a causal relationship with this treatment
39
Define serious adverse event
``` any event that is: fatal or life-threatening permanently/significantly disabling requires or prolongs hospitalization causes a congenital anomaly requires intervention to prevent permanent impairment or damage ```
40
Define black box/boxed warning
a warning designated by the FDA to call attention to serious or life-threatening risk highest level of warning
41
What is the Naranjo Scale used for
to identify an adverse drug reaction
42
What are common causes of ADRs
Patient specific factors Drug-drug interactions Healthcare provider error Nonadherence (intentional or unintentional)
43
What is a drug-drug interaction (DDI)
when a second drug is added to a first drug, resulting in a diminished response to either drug when the combined effect of the two drugs is additive or synergistic
44
Synergistic DDI
produce a response greater than the sum of the responses to both drugs Ex: (+) HIV cocktail (-) CNS depression
45
Antagonistic DDI
produce an effect less than the response produced by each drug alone Ex: (+) naloxone for opioid overdose (-) diuretic + NSAID
46
PK DDI - Absorption
slowed GI motility = increased absorption of other drugs | increased GI motility = decreased absorption of other drugs
47
PK DDI - Distribution
Changes in plasma protein binding | Two drugs competing for protein
48
PK DDI - Metabolism
CYP interactions
49
PK DDI - Elimination/Excretion
Occurs mostly in kidneys
50
Drug-Food Interaction
``` Occurs in: absorption metabolism vitamin K foods Chelation Enteral tube feeds ```

Pharmacology (6 decks)

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