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PHA112 > Drug & Receptor Interactions > Flashcards

Drug & Receptor Interactions Flashcards

1
Q

What is a receptor?

A

A protein that responds to a stimulus and transmits chemical signals to produce a response

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2
Q

What is a ligand?

A

An ion/molecule that forms a complex with a another molecule

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3
Q

What is a prodrug?

A

A compound that must undergo chemical conversion by metabolic processes before becoming an active pharmacological agent.

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4
Q

Give an example of a prodrug and how it works

A

Diamorphine - when it enters the brain it is converted into morphine which binds to mu opioid receptors

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5
Q

Define bioavailability

A

Extent and rate at which the active drug enters systemic circulation

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6
Q

Define affinity

A

How tightly a drug binds to its receptor

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7
Q

Define efficacy

A

The capacity of a drug to produce a change in a target cell/organ after binding to a receptor

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8
Q

Define potency

A

A measure of the amount of drug required to produce an effect of given intensity

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9
Q

What is an agonist?

A

A neurotransmitter/drug that mimics the action of a neurotransmitter and binds to its receptor

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10
Q

Agonists have a _____ affinity for its own receptor and can produce an _______ or ______ effect of the post-synaptic neuron

A

high
excitation
inhibition

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11
Q

Partial agonists produce a higher/lower response than a partial/full agonist after binding

A

lower

full

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12
Q

What is an inverse agonist?

A

A ligand that binds to the same receptor binding site as an agonist

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13
Q

An agonist increases/decreases the activity of a receptor above its basal level.
An inverse agonist increases/decreases the activity of a receptor below its basal level.

A

increases

decreases

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14
Q

What can block the effects of agonists and inverse agonists?

A

antagonists

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15
Q

What is an antagonist?

A

A drug that has affinity for a neurotransmitter receptor and prevents the action of a neurotransmitter to bind to its own receptor

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16
Q

What is an inhibitor?

A

A molecule that binds to another e.g. enzyme and decreases its activity.

17
Q

Give 2 ways in which some drugs inhibit activity of a neuron

A
  • hyperpolarization of neuron

- blockade of binding of a neurotransmitter to its own receptor

18
Q

Give an example of agonists that inhibit the postsynaptic neuron

A

GABA
Diazepam
Morphine

19
Q

Give an example of an antagonist that inhibits the influx of Ca2+ ions

A

Nifedipine

20
Q

Give an example of an antagonist that inhibits the B1-adrenergic receptor

A

atenolol - beta blocker

21
Q

What causes disinhibition?

A

The inhibition of the inhibitor

22
Q

Describe how the release of endorphin can cause the excitation of synaptic transmission through disinhibition of GABAergic inputs

A
  • opioidergic neuron is depolarised
  • endorphin is released which binds to opioid receptors on GABA
  • The activation of the receptors causes hyperpolarisation of GABA
  • GABA neuron stops exerting an inhibitiory control over dopamine
  • The dopamine neuron can fire and release dopamine
23
Q

What is the collective name of the 3 protective membranes that cover the skull?

A

meninges

24
Q

What are the 3 layers of the meninges called?

A
  • dura mater
  • arachnoid layer
  • pia mater
25
Q

List the 3 main functions of the meninges

A
  • protection
  • blood supply
  • gives space for the flow of cerebrospinal fluid
26
Q

Describe how the blood brain barrier maintains a neutral environment

A
  • regulates passage of molecules in/out

- protects brain from microorganisms and toxins circulating in the blood

27
Q

What are the 2 main pairs of arteries that the brain relies on for its blood supply?

A
  • internal carotid arteries

- vertebral arteries

28
Q

What part of the brain do the internal carotid arteries supply blood to?

A

anterior brain

29
Q

What part of the brain do the vertebral arteries supply blood to?

A

posterior brain

brainstem

30
Q

What happens to the brain when it is without O2 and important nutrients?

A
  • brain cells are damaged/ die within minutes

- damage leading to physical/cognitive/mental disabilities

31
Q

What term refers to the blood flow in the brain?

A

Cerebrovascular

32
Q

Define Cerebral blood flow (CBF)

A

the blood supply to the brain in a given time

33
Q

What is an adults typical CBF?

A

750mL/min
or
15% of CO

34
Q

What term describes too much blood flow?

A

hyperemia

35
Q

What can hyperemia lead to?

A

intracranial pressure (ICP)

36
Q

List the 3 purposes of the cerebrospinal fluid (CSF)

A
  • buoyancy against gravity
  • protection - from brain striking cranium when jolted
  • chemical stability
37
Q

The brain and CSF are similar in ________, which makes the brain float in neutral ________ suspended in CSF

A

density

buoyancy

38
Q

What cells of the choroid plexus produce the CSF ?

A

ependymal cells

PHA112 (16 decks)

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