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Year 2 Pharma > Mechanism of drug action > Flashcards

Mechanism of drug action Flashcards

1
Q

What are 4 types of drug antagonism?

A

Receptor blockade
Physiological antagonism
Chemical antagonism
Pharmocokinetic antagonism

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2
Q

What is a physiological antagonism?

A

Drugs interact with different receptors causing opposite effects in same tissue eg NA and histamine on BP

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3
Q

What is a receptor blockade

A

Block receptors, can be a competitive or irreversible antagonist

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4
Q

What is a pharmacokinetic antagonism?

A

Antagonist decreases the concentration of the active drug at the side of action by decreasing the absorption /increasing metabolism/ excretion of the drug

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5
Q

What is drug tolerance

A

Gradual decrease in responsiveness to drug with repeated administration eg benzodiazepines

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6
Q

What are factors that lead to drug tolerance (5)

A 
Pharmacokinetic factors
Loss of receptors
Change in receptors
Exhaustion of mediator stores
Physiological adaption
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7
Q

What is an example of a pharmacokinetic factor that leads to drug tolerance

A

An increase in rate of metabolism eg barbituates or alcohol

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8
Q

What is an example of a loss of receptors leading to drug tolerance

A

Membrane endocytosis - receptor down regulation (beta adrenoceptors)

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9
Q

What is the up regulation of receptors also called?

A

Denervation supersensitivity

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10
Q

What is an example of a change in receptors leading to drug tolerance

A

Receptor desensitization - conformational change eg nAChR at NMJ

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11
Q

What is an example of an exhaustion of mediator stores that leads to drug tolerance

A

Amphetamines

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12
Q

What is an example of a physiological adaption that leads to drug tolerance

A

Homeostatic response - tolerance to drug side effects

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13
Q

What are the 4 types of receptor families?

A

Ion channel linked receptor
G protein coupled receptors
Kinase linked type
Intracellular steroid type receptor

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14
Q

What is the response rate of an ion channel linked receptor and what are examples?

A

Fast responses - m secs

nAChR or GABA A

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15
Q

What is the response rate of a G protein coupled receptor and what are examples?

A

Slower responses - secs

Beta 1 adrenoceptors in the heart

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16
Q

What is the response rate of a kinase linked type receptor and what are examples?

A

Mins

Insulin/Growth Factors

17
Q

What is the response rate of an intracellular steroid type receptor and what are examples? What do they do?

A

Hrs
Steroid/thyroid hormones
Regulate DNA transcription

18
Q

Where is the location of the 4 main types of receptors?

A

Type 1-3 are found in the membrane and type 4 - the ones that control gene transcription are found intracellularly

19
Q

What are the different types of effectors in receptors?

A

Type 1 - Channel
Type 2 - Enzyme or channel
Type 3 - Enzyme
Type 4 - Gene transcription

20
Q

What are the different types of coupling in receptors?

A

Type 1 - Direct
Type 2 - G protein
Type 3 - Direct
Type 4 - Via DNA

21
Q

A 4 year old girl is bitten by a Tiger snake whilst holidaying in Australia. An anti-venom (harvested antibodies) is administered. Which form of antagonism is utilised by the anti-venom?

A: Competitive receptor blockade
B: Physiological antagonism
C: Chemical antagonism
D: Pharmacokinetic antagonism
E: Irreversible receptor blockade
A

C

22
Q 
Tolerance to the euphoric effects of drugs of abuse (e.g. heroin & cocaine) can occur after repeated use. Which form of tolerance would not involve any change in the cells that mediate the euphoric effects?
A: Receptor desensitisation
B: Receptor down-regulation
C: Exhaustion of mediator stores
D: Receptor up-regulation
E: Increased metabolic degradation
A

E

23
Q

What is ‘use dependency’ of an ion channel blocker?

A

The more that the tissue is used, the more active the tissue is, the more active the ion channel is therefore if blocked then will cause a more complete response faster (more effective)

24
Q

What is chemical antagonism?

A

Interaction of drugs in solution - where drugs can negate the effects of each other eg dimercaperol reduces toxicity of heavy metals by forming complexes

Year 2 Pharma (34 decks)

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