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PMHNP > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

Effect of a drug on the body

based on the concept of drug receptor binding

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2
Q

Affinity

A

Kd
D+R <-> DR

Kd= disassociation constant
1. Ratio of rate at which the drug binds to the receptor compared to the rate that a receptor complex disassociates
2. As drug concentration increases the concentration of bound receptors increases and as free receptors inc, bound receptors concentration inc as well

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3
Q

Dose response relationship

A

certain doses are associated with certain responses

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4
Q

Potency (EC50)

A

amount of drug that produces a response in 50% of the population

more potent needs lower dose

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5
Q

Efficacy (Emax)

A

the max response produced by the drug, adding more drug wont produce more response because there is 100% occupancy

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6
Q

Median effective dose (ED50)

A

amount of drug that produces a response in 50% of the population

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7
Q

Median toxic dose (TD50)

A

amount of drug that produces a response in 50% of the population

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8
Q

Median lethal dose (LD50)

A

amount of drug that produces a response in 50% of the population

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9
Q

6 major neurotransmitters

A

Serotonin
Norepinephrine
Dopamine
Acetylcholine
Glutamate
GABA

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10
Q

5 psychotroptic drug targets

A

neurotransmitter reuptake
neurotransmitter receptors
neurotransmitter metabolism
Ion channel neurotransmission (2: ligand and voltage gated)

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11
Q

Neurotransmitter reuptake

A

Prevent recycling of NT like serotonin or dopamine by inhibiting reuptake and storage in neuron and inc levels in the synapse and affect post synaptic neurons

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12
Q

Neurotransmitter receptors

A

Many drugs interact with these by binding on the same receptor as the NT or may bind allosterically and change the receptor to enhance or inhibit the NT

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13
Q

Neurotransmitter metabolism

A

Enzymes are another target of drugs as they convert one molecule into another and the enzyme often affect on NT is to break them down

Basically they could inhibit this and allow NT concentrations to circulate

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14
Q

Ion channel (2)

A

Ligand gated which is opened by NT binding

Voltage gated which opened by charge across the membrane

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15
Q

reuptake

A

NT released during neurotransmission are in many cases transported back into the presynaptic neurons and allows reuse and once back in are put in vescicles for storage and protection and ready to redploy

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16
Q

presynaptic transporter SERT

A

for serotonin

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17
Q

presynaptic transporter NET

A

for norepinephrine and dopamine

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18
Q

presynaptic transporter DAT

A

for dopamine

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19
Q

presynaptic transporter GABA 1-4

A

for GABA

20
Q

presynaptic transporter glycine 1-2

A

for glycine

21
Q

presynaptic transporter: excitatory amino acid transporters 1-5

A

glutamate
aspartate

22
Q

vesicular transporter VMAT 1-2

A

serotonin
NE
DA

23
Q

vesicular transporter VAchT

A

Ach

24
Q

vesicular transporter VIAAT

A

GABA

25
Q

vesicular transporter V GluT 1-3

A

glutamate

26
Q

G-protein linked receptors

A

second messenger system (NT is the first messenger)

drug can act at NT binding sites or allosteric sites

So NT binds first and changes the receptor allowing the g-protein to bind

The G protein makes another change which preps it for the enzyme that synthesizes the second messenger

27
Q

Agonist

A

When a drug binds to the g protein linked receptor it can affect the receptor in different ways than the endogenous NT

Generally produces response similar to the endogenous NT

direct: bind to NT receptor at NT site or allosteric site

indirect: boost levels of NT by blocking inactivation

28
Q

partial agonist

A

stabilizers

Hard to understand

Somewhere on spectrum of agonist that fully activates a receptor and an antagonist that doesn’t change signal transduction

Like a light on a dimmer switch

29
Q

antagonist

A

Usually blocks what an endogenous NT would do to the receptor

True antagonists are neutral and because they have no actions of their own they are often called silent

Maintain baseline activity

30
Q

partial inverse agonist

A

inactivates the receptor
reduces signal transduction
removes baseline activity

Opposite extreme of the agonist in that it neither inc signal transduction or blocks agonist activity like an antagonist

31
Q

dopamine receptors and associated class

A

D1
D2

antipsychotics

32
Q

serotonin receptors and associated class

A

5HT1A, 2A, 1B/D, 2C, 6, 7

antipsychotics
antidepressants
anxiolytics

33
Q

norepinephrine receptors and associated class

A

a-1
a-2
B-2

antidepressant (mirtazapine)
antihypertensives
antipsychotics

34
Q

Acetylcholine receptors and associated class

A

M1
M3/M5

antidepressant
antihistamines
antipsychotics

35
Q

enzymes

A

convert a substrate into a product

Rx can bind to enzyme inhibitors which can be reversible or irreversible

Only a few drugs are enzyme inhibitors

The ones that bind to inhibitors allow the enzyme to inc interaction with substrate because they inhibit the inhibitor

36
Q

Examples of enzyme targets

A

In each case the action of the drug prevents the action of the enzyme that degrades the substrate

Monoamine Oxidase
Acetylcholinesterase
Glycogen synthase kinase (GSK)
Aldehyde Dehydrogenase

37
Q

Ligand gate is regulated by

A

receptor gate keeper that hasd the potential to bind an NT or hormone

38
Q

regulation of a ligand gate produces

A

a confirmation change that opens the channel and allows the flow of charged molecules

39
Q

If agonist occupies a binding site on a ligand gate

A

the frequency at which the channel opens is increased

40
Q

If antagonist binds to the receptor on a ligand gate

A

the channel is locked in resting confirmation and similar to if no NT bound

41
Q

If partial agonist binds to ligand gate

A

will open but less than if full agonist present

42
Q

If inverse agonist binds to ligand gate

A

channel closes and stabilizes it

43
Q

Allosteric site

A

It is a site other than which the endogenous ligand binds

44
Q

Allosteric sites have no activity on their own but when bound at the same time as a ligand

A

they can enhance or block the ligand activity

if enhance they are positive and

if block they are negative allosteric modulator

a. Pos ex is a benzo

45
Q

voltage sensitive

A

Action potential: Electrical impulse in a neuron

Voltage-sensitive sodium channels (VSSCs)
Voltage-sensitive calcium channels (VSCCs)

PMHNP (24 decks)

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