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Nervous System > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What are the 4 receptor families?

A

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

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2
Q

How do ligand-gated ion channels work

A

Ligand bind

Facilitate movement of ion across membrane- depolarisation or hyper polarisation which bring effect

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3
Q

How do G-protein coupled receptors work?

A

GalpaS and I work with same enzyme but AlphaI inhibit adenylyl cyclase
Adenylyl cyclase convert aMp to cAMP, influence PKA bring cellular event
G
GalphaQ activates phospholipase C, convert PIP2 to DAG (influence PKC) and IP3 (calcium regulator)
Or affect ion channel

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4
Q

How do nuclear receptors work?

A

Receptor inside cell in cytosol, binding to it causes it to bind to DNA, to increase or decrease gene expression

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5
Q

Which receptors are fastest?

A

Ligand gated- millisecond
G protein- seconds
Kinase-linked receptor - hours
Nuclear receptors- hours

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6
Q

How do kinase-linked receptors work?

A

Lead to protein phosphorylation
Gene transcription
Protein synthesis
Cellular effects

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7
Q

Agonist drugs

A

Activate receptors

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8
Q

Antagonist drugs

A

Block receptors

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9
Q

Affinity

A

How well a drug binds to receptor

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10
Q

Efficacy

A

How well it causes a recordable response

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11
Q

2 phases an agonist works

A

Drug binding- affinity
Receptor activation- efficacy
Biological effect

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12
Q

What is a full agonist?

A

elicit 100% effect on endogenous agonist

High efficacy

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13
Q

Partial agonist

A

Elicit<100% effect of endogenous agonist

Low efficacy, not full response

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14
Q

Super agonist

A

100% endogenous effect- bring greater effect

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15
Q

Inverse agonist

A

Reduce basal receptor activity

Lower basal rate

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16
Q

Potency meaning

A

Product of affinity and efficacy

Conc or amount of drug to produce desired effect

17
Q

Antagonists have how much efficacy

A

0

18
Q

Different non-receptor antagonists and explanation

A

Chemical antagonist- binding an inactivating unbound drug in solution, allow to be excreted
Physiological antagonist- produce opposite physiological effects of another agonist, indirectly oppose action of that original agonist
Pharmacokinetic- drug influence action of another

19
Q

A full agonist doesn’t need to bind to all receptors in tissues to bring about max response

True or false?

A

True

20
Q

A partial agonist will be at 100% receptor occupancy and still not get 100% effect

True or false?

A

True

21
Q

Dissociation constant

A

Conc of drug required to occupy 50% of available receptors

22
Q

Desensitization

A

A drug effectiveness may decrease rapidly when given repeatedly or continuously

23
Q

Tolerance

A

Decrease in drugs effectiveness over days/weeks

24
Q

Resistance

A

Adaptive changes making body less response and so less effective

Nervous System (7 decks)

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