Pharmacology 1: principles Flashcards

1
Q

What is Pharmacodynamics

A

What a drug does to the body

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2
Q

What is Pharmacokinetics

A

The body does to a drug

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3
Q

Describe Affinity

A

The binding step. The strength of association between ligand and receptor

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4
Q

Describe high vs low affinity

A

High affinity agonists have a slow dissociation rate and Low affinity agonists have a fast dissociation rate

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5
Q

Describe Efficacy

A

The activation step. The ability of an agonist to evoke a response.

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6
Q

Do antagonists have affinity or efficacy or both

A

Antagonists have affinity but no efficacy

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7
Q

How do antagonists bind

A

To orthosteric (competitive) or allosteric (non-competitive) sites

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8
Q

What is the EC50?

A

The concentration of agonist which elicits a half-maximal response

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9
Q

What type of plot do we use for the EC50?

A

Semi-logarithmic.

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10
Q

How is the relationship between concentration and response described?

A

Sigmoidal

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11
Q

Describe the graph of a Potent agonist, Less Potent agonist, and a partial agonist

A
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12
Q

In competitive antagonists, in which direction is the response curve shifted?

A

Parallel to the Right.

Becomes less potent but with higher conc. of agonist the antagonist can be out-competed to produce the same maximal response

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13
Q

In non-competitive antagonists, in thich direction is the response curve shifted?

A

Slope Flattened.

When the agonist binds, it cannot contribute to maximal response.

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14
Q

With which type of antagonist does EC50 and therefore potency increase

A

Competitive

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15
Q

What is drug disposition?

A

The fate of drugs in the body
Absorption, distribution, metabolism, excretion

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16
Q

What are the physiochemical factors controlling absorption

A
  1. Solubility
  2. Chemical stability
  3. Lipid to water partition coefficient
  4. Degree of ionisation
17
Q

What factors affect GI absoption?

A

GI motility
pH
Blood flow
Physiochemical interactions
Presence of Transporters

18
Q

Are ionised or unionised drugs more freely able to distribute

A

Only unionised drugs can freely diffuse. Ionised drugs require transporters to move

19
Q

What is the Vd?

A

The apparent volume which a drug is dissolved in

20
Q

What does Vd <5L imply?

A

Drug is contained within the vascular component
eg. bound to protein or too large to cross the capillary wall

21
Q

What does Vd <15L imply

A

Drug is restricted to extracellular water

22
Q

What does Vd >15L imply?

A

distribution throughout total body water
eg. highly lipid soluble drugs