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Neuroscience > Transmitters and receptors > Flashcards

Transmitters and receptors Flashcards

1
Q

What must drugs do in order to access the CNS?

A

Cross the blood brain barrier

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2
Q

What effect do drugs that cross the blood brain barrier have?

A

Interfere with chemical neurotransmission within CNS

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3
Q

Which processes of chemical neurotransmission can drugs that enter the CNS affect?

A

Synthesis

Storage

Release

Inactivation (reuptake and metabolism)

Receptor interactions

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4
Q

Describe the effects of cocaine and amphetamine on noradrenergic nerves?

A

Both increase NA in synaptic cleft

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5
Q

How can excitatory input be reduced to treat epilepsy?

A

Phenytoin

Limits excitatory nerve activation

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6
Q

Describe the action of phenytoin?

A

Decreases excitatory fibre activity (glutamate) by inhibiting Na channels

Only binds Na channel while it is open

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7
Q

How can inhibitory input be enhanced to treat epilepsy?

A

Benzodiazepines

Enhance GABA receptor activity

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8
Q

Which neurotransmitters are implicated in the use of sedative, hypnotic and anxiolytic agents?

A

GABA (sedation and anxiety)

Serotonin (sedation and anxiety)

NA (anxiety)

NPY (anxiety)

HA (sedation)

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9
Q

What are the clinical applications of benzodiazepines?

A

Epilepsy

Anxiety

Sleep disorders

Premedication (sedation for procedures)

Acute alcohol withdrawal

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10
Q

Why can beta-andrenoceptor antagonists be useful in the treatment of anxiety?

A

Can block the physical symptoms

(sweating, tremor, tachycardia)

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11
Q

Which drug class is now obsolete as hypntoic/anxiolytics?

A

Barbiturates

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12
Q

What are barbiturates?

A

General depressants

Produce all levels of CNS depression

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13
Q

Why are barbiturates no longer used?

A

Exceedingly toxic

Highly addictive

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14
Q

Why are benzodiazepines more favourable than barbiturates?

A

Wider therapeutic index

Less depression of resp and cardio centres

Less dependence

Safe in overdose

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15
Q

Describe the effects of benzodiazepines?

A

Elicit sedation and induction of sleep

Reduce anxiety and aggression

Reduce muscle tone

Obliterate memory

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16
Q

How do benzodiazepines exert their effect?

A

Interact with GABA A receptor and interfere with GABAergic transmission

GABA A receptors are ligand-gated ion channels that let Cl into cell

17
Q

Where do benzodiazepines bind to the GABA A receptor?

A

Allosteric site

18
Q

What do benzodiazepines modulate on the GABA A receptor?

A

Orthosteric ligand affinity

Orthosteric ligand efficacy

Receptor activation level

19
Q

Describe the effect that benzodiazepines have when they bind the GABA A receptor?

A

Bind > increase in receptor affinity for GABA > increases frequency of Cl channel opening > increased sensitivity, no change in maximum response

20
Q

Describe the effect that barbiturates have when they bind the GABA A receptor?

A

Bind receptor > prolong opening of Cl channel > increased sensitivity and maximum response

21
Q

Why are benzodiazepines considered safe in overdose, whereas barbiturates are not?

A

Benzodiazepines increase the frequency of Cl channel opening, and do not change the maximum response. Therefore, they have a celing effetc.

Barbiturates prolong the opening of Cl channels, and increase the maximum response. Therefore, there is no ceiling effect.

22
Q

Describe the advantages of allosteric modulators?

A

Celing effect of inhibitors

Positive modulation of endogenous agonist effect, rather than continuous effect of exogenous agonist

Great receptor subtype selectivity possible

23
Q

Describe some of the disadvantages of usinjg benzodiazepines?

A

Unwanted effects: drowsiness, confusion, impaired coordination

Interaction with alcohol, antihistamines and barbiturates

Long lasting hangover effects

Withdrawal symptoms

Dependence

24
Q

Describe the tolerance effect of benzodiazepines?

A

Gradual escalation of dose needed

25
Q

Describe the dependence effect of benzodiazepines?

A

Signs of physical and psychological withdrawal

26
Q

What determines the route of administration of benzodiazepines?

A

Pharmacokinetic profile

Active orally, but differ in duration

27
Q

Describe the differences in characterisitcs and usage between short and medium/long acting benzodiazepines?

A

Short: no daytime anxiety, can be used by elderly and drivers

Medium/long: 3-4 daily doses needed, fast onset, muscle tension

28
Q

Is low potency a disadvantage in drugs?

A

Only if the dose is so large that it is awkward to administer

29
Q

Describe the difference between pharmacological efficacy and clinical efficacy?

A

Pharmacological efficacy: strength of receptor activation

Clinical efficacy: strength of beneficial effect

30
Q
A

Neuroscience (51 decks)

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