Drug - Receptor Interactions Flashcards

1
Q

What is a drug

A

Chemical substance that interacts with a biological system to create a physiological effect

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2
Q

Drug target sites (4)

A

Receptors, Ion channels, transport systems, enzymes

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3
Q

What is a receptor

A

Proteins within the cell membrane

Activated by neurotransmitters/hormones

Defined by agonists & antagonists

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4
Q

Examples of agonist and antagonist drugs targeting receptors

A

Agonist = acetylcholine

Antagonist = atropine

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5
Q

What is an ion channel

A

Selective pores allowing ion transfer down the electrochemical gradient

Either voltage sensitive or receptor linked

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6
Q

Examples of drugs targeting ion channels

A

Calcium channel blockers + LAs

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7
Q

Examples of ion channels

A

Voltage sensitive = VSCC

Receptor linked = nAChR

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8
Q

What are transport systems

A

Work against concentration gradients (glucose, ions and NTs) Specificity for certain species

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9
Q

Examples of transport systems

A

Na+/K+ ATPase

NA ‘uptake 1’

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10
Q

Examples of drugs targeting transport systems

A

Tricyclic anti-depressants (TCAs)

Cardiac glycosides

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11
Q

What are enzymes

A

Catalytic proteins that increase rate of reaction

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12
Q

Examples of drugs targeting enzymes/ classes

A

Enzyme inhibitors = anticholinesterase (neostigmine)

False substrates = methyldopa

Prodrugs = Chloral hydrate (trichloroethanol)

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13
Q

State none specific drug action

A

Physiochemical properties

> Antacids/osmotic purgatives (↑ water in stool)

Plasma protein binding

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14
Q

How do osmotic purgatives work

A

Draw water into the stool in order to make it softer

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15
Q

What does the potency of a drug depend on

A

Affinity (forces involved in the binding of the drug) and Efficacy (activation of the receptor/Intrinsic activity) = conformational change of the receptor

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16
Q

Describe the dose-response curve

A

↑ Agonist concentration = ↑ tissue response

Greater and steeper curve with a full agonist compared to partial agonists as they have a lower maximum

17
Q

Describe the log dose-response curve

A
18
Q

A key difference between an agonist and antagonists

A

AFFINITY but no efficacy

Types include competitive and irreversible

19
Q

Describe the action of a competitive receptor antagonist

A

SAME site as the agonist

Surmountable (can be overcome)

Shift the dose-response curve to the RIGHT

20
Q

Examples of competitive receptor antagonists (2)

A

Atropine

Propranolol

21
Q

What is the action of irreversible receptor antagonists

A

Binds TIGHTLY or at a DIFFERENT site

Insurmountable (can’t be overcome)

22
Q

Example of an irreversible receptor antagonist (1)

A

Hexamethonium

23
Q

Describe the graph showing the effects of both types of antagonists

A