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PHAR2220 > L18 antixoyltic > Flashcards

L18 antixoyltic Flashcards

1
Q

optogenetic and pharmacogenetic tools,
together with novel imaging techniques
* visualisation and functional analysis of
cellular networks

A
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2
Q

optogenetics

A

channelrhodopsin-2 (a light-gated ion channel)

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3
Q

electrophysiology

A
  • glutamatergic and GABAergic
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4
Q

anxiogenic pathway

A

glutamatergic - increase anxiety

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5
Q

anxiolytic pathway -

A

GABAergic - decrease anxiety

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6
Q

Amygdala and BNST (bed nucleus of the stria terminalis) both have which pathways

A
  • BLA-vHC - anxiogenic
  • BLA-CEA - anxiolytic
  • anxiogenic pathway - glutamatergic
  • anxiolytic pathway - GABAergic
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7
Q

Tests used in anxiolytic drug discovery

A
  • open field test
  • elevated plus maze
  • light/dark box
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8
Q

Approach-avoidance conflict tests

A

generate a conflict between a drive to approach novel areas and to avoid potential threat simultaneously

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9
Q

Measuring anxiety in animals (Measure behavioural and physiological effects in experimental animals)

A
  • behavioural inhibition, e.g., immobility or suppression of a behavioural response
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10
Q

GABA

A
  • g-aminobutyric acid.
  • the primary inhibitory neurotransmitter in the brain
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11
Q

GABA(A) receptor

A
  • native: two a subunits, two b subunits and one subunit of a third type (e.g., g)
  • most abundant: alpha-1 beta-2 gamma-2
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12
Q

Benzodiazepines can work on GABA receptors w/o GABA (t/f)

A

False

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12
Q

benzodiazepines as positive allosteric modulator (PAM)

A
  • binding site at the α/γ interface
  • affinity for GABA and the frequency of channel opening ↑
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13
Q

Benzodiazepines and efficacy and potentiation

A

No effect on efficacy but increases potentiation

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14
Q

If GABA receptor has a1/a2/a3/a5 subunits

A

Sensitive to benzodiazepines

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15
Q

If GABA receptor has a4/a6 subunits

A

Insensitive to Benzodiazepine

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16
Q

Why are some GABA receptors insensitive to Benzodiazepine

A
  • histidine at position 101 (α1 numbering) is crucial for the action of benzodiazepines
  • introduction of point mutation (histidine to arginine, H to R)
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17
Q

Sedation GABA subunit involved

A

sedation - decreased motor activity in wild-type but not a1

18
Q

Memory impairment GABA subunit involved

A

absent in a1 Mutatant mice

19
Q

anticonvulsant effects GABA subunit involved

A
  • reduced in a1 H101R mice
20
Q

anxiolytic GABA subunit involved

A
  • absent in a2
  • but not a3
  • involvement of the a2 subunit
21
Q

α1 subunit-mediated effects

A
  1. Hypnotic and sedative effects
  2. Anticonvulsant effects
  3. Anterograde amnesia
22
Q

Hypnotic and sedative effects

A

[a1] ↓ sleep latency and ↑ sleep duration; short acting preferred; long-acting drugs lead to drowsiness

23
Q

Anticonvulsant effects

A

[a1] anticonvulsant activity is common to benzodiazepines

24
Q

Anterograde amnesia

A

[a1] prevent memory of events experienced under the influence of drugs; can also be α5-mediated

25
Q

α2 subunit-mediated

A
  1. Anxiolytic effects
  2. Muscle relaxant effects
26
Q

Anxiolytic effects

A

[a2] short acting drugs may paradoxically increase aggression due to withdrawal syndromes

27
Q

Muscle relaxant effects

A

[a2] act through the GABA(A) receptor in the spinal cord; facilitates anxiolytic effects (↑ muscle tone is common to anxiety)

28
Q

Benzodiazepines info

A
  • short, intermediate, and long acting
  • orally active and well absorbed
  • fast onset of therapeutic effects
29
Q

Benzodiazepines treat

A
  • acute anxiety
  • behavioural emergencies
  • premedication for surgery and procedures
  • alcohol withdrawal
30
Q

Undesirable effects during therapeutic use of Benzodiazepines

A
  • drowsiness, amnesia and impaired coordination
  • duration of action of drugs is important
31
Q

Name two Benzodiazepines drugs

A

Diazepam and oxazepam both active

32
Q

Benzodiazepines Tolerance and dependence

A
  • therapeutic effects ↓ when given the same dose
  • use < 2 weeks
  • withdrawal on abrupt cessation e.g., rebound anxiety, tremor, sleep disturbance, loss of appetite
  • short-acting drugs are more problematic
33
Q

Benzodiazepines Acute overdose

A
  • relatively safe
  • treated with i.v. flumazenil (compete with benzodiazepines-binding site)
  • short DoA
  • long-acting *benzodiazepine overdose - repeated flumazenil injection
  • combined with other CNS depressants (alcohol/opioids) - severe respiratory depression
34
Q

Diazepam and oxazepam phase metabolism

A

D= 1 and 2
O= just 2
2= glucuronidation

35
Q

diazepam and oxazepam DoA

A
  • both can be prescribed
  • duration of action - long vs. short
36
Q

Benzodiazepines for elderly

A

PK consideration
* e.g., metabolism
PD consideration
* sensitivity to drugs: sedation ↑ > anxiolytic ↑

37
Q

Buspirone as anxioltyic

A
  • delayed anxiolytic effects - somatodendritic 5-HT1A
    receptor desensitisation
  • generalised anxiety disorder
  • no sedation or impaired motor coordination
  • no tolerance or withdrawal effects
38
Q

Buspirone action

A

a 5-HT1A
receptor partial agonist

39
Q

Buspirone adverse

A

nausea, dizziness, headache, and restlessness

40
Q

Selective serotonin reuptake inhibitors* as anxiolytic

A
  • preferred due to better adverse effect profile
  • slow onset of therapeutic effects
  • generalised, social, and/or panic disorder
  • FDA approved or off-label use
  • reduce depression associated with anxiety
  • do not produce hypnotic effect
41
Q

Extrasynaptic GABA receptors

A

Continuous and independent of NT to synapse (s-gp-B)

42
Q

Synaptic GABA receptors

A

respond to GABA released during neurotransmission (ms-ion-a)

PHAR2220 (20 decks)

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