Anxiolytics Flashcards
1
Q
What binds to GABAa receptors orthosteric and allosteric sites?
A
Orthosteric- agonist= muscimol a.agonist= bicuculline, picrotoxin Allosteric- agonist= diazepam a.agonist= flumazenil
2
Q
GABAa receptors show ‘constitutive acitivity’ what does this mean?
A
The channel can open randomly without activation
3
Q
What are the agonists and a.agonists of GABAb receptors?
A
Agonist= baclofen A.agonist= phaclofen
4
Q
Where do anxiolytics bind?
A
The allosteric site on GABAa receptors -
enhancing the activity of the receptor to GABA
5
Q
What are 5 physiological effects of benzodiazepine agonist?
A
- Sedation/anxiolytic
- Hypnosis
- Anterograde amnesia
- Anti-convulsant
- Reduction in muscle tone
6
Q
How do barbiturates differ from b.pines in their modulation of GABAa receptors?
A
Barbiturates increase the mean open time of the receptors channels, whereas b.pines increase the frequency of the channels opening
7
Q
What are the 2 main factors which determine the therapeutic use of d.pine
A
- Lipid solubility- redistribution and onset of action
2. Drug half life
8
Q
What are 4 adverse effects of b.pine agonists
A
- Sleepiness
- (Mixed with other CNS depressants) fatal overdose
- Tolerance
- Withdrawal symptoms
