Anxiolytics & Sedatives [4] Flashcards
Anxiolytics treat _
Anxiety
Sedatives treat _
Insomnia
2 animal models of anxiety
Conflict test (smaller box but with food)
Elevated cross (rats subside in path with walls and become immobilised in new environment)
Evaluation of anxiety in man (3)
Diagnostic & statistic manual of mental disorders
Galvanic skin resistance
Use of placebo
Current anxiolytics/sedatives (5)
Benzodiazepines
Z-drugs
5-HT1A agonists
Barbiturates
Beta-adrenergic antagonists
What are Z-drugs
Non-benzodiazepine drugs for insomnia
What is the most important anxiolytic/sedative
Benzodiazepine
Benzodiazepine structure
Benzene ring (6c & 3 double bonds)
Attached to diazepam ring
Addition of phenyl & halogen for pharmacology
How many groups of benzodiazepine is there
4
R1 R2 R3 R4
What are benzodiazepines similar in structure to
Chlorodiazepoxide which was synthesised by accident
What is used for a benzodiazepine overdose
Antagonist: Flumazenil
- blocks binding to GABA
4 things that benzodiazepines do
Reduce anxiety and depression
Increase sleep duration (decrease REM sleep)
Reduces muscle tone and coordination
Anticonvulsant effects (for epilepsy)
Where are GABA receptors
Chloride channels with binding sites for endogenous GABA and exogenous BDZ
What does GABA binding do
Opens Cl- channel
Influx of Cl-
Hyperpolarisation of cell
Where does BDZ bind and what does it do
An independent site on the same Cl- channel-receptor complex
Increases GABAs affinity to receptor
Enhances inhibitory effect
