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Neuro Pharmacology > Transmitters and Receptors > Flashcards

Transmitters and Receptors Flashcards

1
Q

What do drugs in the CNS affect?

A

synthesis, storage, inactivation of NTs (reuptake or metabolism or bind to receptor)

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2
Q

What is the action of Phenytoin?

A

blocks the AP activation of glutamate-releasing nerves to limit excitatory activation of motor nerves in epilepsy; it binds to and inhibits OPEN Na+ channels and is therefore enhanced in high frequency firing

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3
Q

What is the action of benzodiazepines on GABA?

A

enhance GABA receptor activity by binding at an allosteric site

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4
Q

For sedation and anxiety tx we want to target

A

GABA - main inhibitory transmitter of the CNS

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5
Q

To treat anxiety alone we want to target

A

Serotonin (prejunctional CNS receptors); NA (peripheral tachycardia); NPY (1 receptor activation reduces anxiety)

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6
Q

To sedate alone we want to target

A

Histamine - H1 receptor antagonists are sedative

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7
Q

Benzodiazepines are used in

A

epilepsy, anxiety, sleep disorders, sedation for medical procedures, and acute alcohol withdrawal

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8
Q

Sedative-hypnotic and anxiolytic agents are used in

A

sleep disorders (insomnia), anxiety

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9
Q

Barbiturates are used for

A

anaesthesia and anticonvulsants

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10
Q

Why are barbiturates no longer routinely prescribed?

A

toxic - low therapeutic index, induce liver enzymes, withdrawal can cause death; highly addictive

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11
Q

Barbiturates cause

A

general depressants, cause CNS depression - mild sedation, surgical anaesthesia, coma, death

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12
Q

Why are benzodiazepines considered safer than barbiturates?

A

Wider therapeutic index, less depression, safe in overdose

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13
Q

Benzodiazepines elicit

A

sedation and induction of sleep (reduced time to fall asleep/increased duration of sleep), reduced anxiety and agression, reduction of muscle tone (anticonvulsant but decreased coordination), obliterate memory

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14
Q

GABA A receptors are

A

ligand-gated ion channels

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15
Q

GABA B receptors are

A

GPCRs

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16
Q

Benzodiazepines interact with which receptor?

A

GABA A only

17
Q

What is the function of GABA A receptors?

A

lets Cl- into cell; hyperpolarizes cell decreasing activation

18
Q

What is the main action of benzodiazepines?

A

Interfere with GABAergic transmission: binding to the GABA A receptor allosteric site increases affinity for GABA which increases frequency of channel opening (lets in more Cl_)

19
Q

Benzodiazepines bind to which site on the GABA A receptor?

A

allosteric site, not orthosteric site

20
Q

Binding at the allosteric site can modulate

A

orthostatic ligand affinity and efficacy, and receptor activation level

21
Q

How do barbiturates act differently on the GABA A receptor to benzodiazepines?

A

Barbiturates prolong opening of channel (letting more Cl- in) where benzodiazepines increase frequency of opening - this is why you can OD on barbiturates and die, but be ok ODing on benzodiazepines

22
Q

What are the unwanted effects of benzodiazepines?

A

drowsiness, confusion, impaired coordination

23
Q

What are the disadvantages in using benzodiazepines?

A

interactions with alcohol, antihistamines, and barbiturates; long lasting hang over effects; withdrawal symptoms; dependence/abuse potential

24
Q

What is potency?

A

relative position of the dose-effect curve along the dose axis - more potency does not mean a drug is superior

25
Q

What is efficacy?

A

The ability of a drug to do the right thing

26
Q

What is pharmacological efficacy?

A

Strength of receptor activation ie full agonists have high efficacy, partial agonists have low efficacy

27
Q

What is clinical efficacy?

A

The strength of the beneficial effect

28
Q

Benzodiazepines increase the ________ of GABA

A

potency; increase the frequency of the Cl- channel opening at the GABA A receptor

29
Q

Barbiturates increase the _______ of GABA

A

efficacy; increase the duration of Cl- channel opening at the GABA A receptor

30
Q

Non-benzodiazepine hypnotics

A

zolipidem, zopiclone

31
Q

Non-nenzodiazpine anxiolytics

A

buspirone

32
Q

Zolpidem

A

non-BDZ hypnotic for short term tx of insomnia; binds GABA A at BDZ site, short duration

33
Q

Zopiclone

A

non-BDZ hypnotic for short term tx of insomnia; binds GABA A at different site to BDZ site

34
Q

Buspirone

A

non-BDZ anxiolytic; partial agonist at 5HT 1A receptors (inhibitory autoreceptors regulating transmitter release)

Neuro Pharmacology (4 decks)

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