Pharmacodynamics Flashcards

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

A

binding affinity

22
Q

If a drug has a low ED50 it means

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

A

9 out of 10

24
Q

What other forms of antagonism are there

A

chemical
physiologic
pharmacokinetic

25
Q

What is chemical antagonism

A

two drugs reacting with each other to diminish the effect of one drug

26
Q

What is a physiologic antagonist

A

two drugs with opposite effects

27
Q

What are the two types of pharmacokinetic antagonism

A

One drug induces or inhibits metabolism or another drug

Receptor changes

28
Q

What are common receptor changes

A

desensitization

decreased receptor #

29
Q

What is a common cause for receptor changes

A

long term drug use

30
Q

What does a Quantal-dose response curve measure

A

Safety

% or # of population who achieve a particular response at a given dose

31
Q

What are the steps to make a quantal-dose response curve

A

Determine dose of beneficial effect
determine dose of harmful effect
plot on bell-shaped curve
convert to sigmoid curve

32
Q

What is therapeutic index

A

ratio of TD50 to ED50

narrow = increased likelihood of ADRs.

33
Q

How is therapeutic index calculated

A

TD50/ED50

34
Q

What is TD50

A

the dose at which 50% of the population have a toxic response

35
Q

Define adverse drug reaction

A

response to a medicine which is noxious and unintended, and which occurs at doses normally used in man

36
Q

Define side effect

A

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
Q

Define medication error

A

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
Q

Define adverse event/experience

A

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
Q

Define serious adverse event

A
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
Q

Define black box/boxed warning

A

a warning designated by the FDA to call attention to serious or life-threatening risk
highest level of warning

41
Q

What is the Naranjo Scale used for

A

to identify an adverse drug reaction

42
Q

What are common causes of ADRs

A

Patient specific factors
Drug-drug interactions
Healthcare provider error
Nonadherence (intentional or unintentional)

43
Q

What is a drug-drug interaction (DDI)

A

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
Q

Synergistic DDI

A

produce a response greater than the sum of the responses to both drugs
Ex:
(+) HIV cocktail
(-) CNS depression

45
Q

Antagonistic DDI

A

produce an effect less than the response produced by each drug alone
Ex:
(+) naloxone for opioid overdose
(-) diuretic + NSAID

46
Q

PK DDI - Absorption

A

slowed GI motility = increased absorption of other drugs

increased GI motility = decreased absorption of other drugs

47
Q

PK DDI - Distribution

A

Changes in plasma protein binding

Two drugs competing for protein

48
Q

PK DDI - Metabolism

A

CYP interactions

49
Q

PK DDI - Elimination/Excretion

A

Occurs mostly in kidneys

50
Q

Drug-Food Interaction

A
Occurs in:
absorption
metabolism
vitamin K foods
Chelation
Enteral tube feeds