ANXIOLYTICS Flashcards
Describe anxiety.
Anxiety is when someone has invasive thoughts of helplessness, worrying, apprehension, difficulty concentrating, irritability and insomnia. Thoughts of impending doomor loss of control. May be accompanied by depression.
What is hypothesized to cause anxiety?
When you lack inhibitory neurons (GABA, glycine, etc.) in your brain.
Describe the GABA receptors.
GABA-A and GABA-C receptors are LGIC’s. They have multiple allosteric sites where drugs can bind. When activated they hyperpolarize the neuron by increasing Cl- influx or inhibiting Ca2+ exchange.
Alprazolam
Benzodiazepine.. Binds to GABA-A receptor at allosteric site, increases Cl- influx by increasing the frequency of the channel opening. Also need GABA to active channel.
Diazepam
Benzodiazepine. Also binds to GABA-A receptor. Inhibitory effect.
When do you use alprazolam and diazepam?
Anxiety, sedative (induction and maintenacne of anesthesia), acute EtOH withdrawal. Can use diazepam for status epilepticus and as a muscle relaxant.
What toxicities are involved with benzodiazepine?
sedation, lihtheadedness, increases total sleep time but decreases REM, anterograde amenesia.
What must you be careful of when giving benzos (diazepam and alprazolam)?
Category D, can overdose if taken with alcohol, grapefruit juice will increase concentrations (p450 metabolism). Diazepam is very quick to act!
Flumazenil
Competitive GABA-A receptor antagonist. Give to people with benzo/alcohol overdose. Can percipitate convulsions. Can be used in hypersomia.
Buspirone
Non-benz anxiolytic. Used over longer periods to treat GAD. 5-HT1A partial agonist and DA agonist. Must be taken fo two weeks to feel effect.
Propanolol
Beta-blocker used in performance anxiety and migrane prevention. Suppresses somatic and autonomic symptoms of anxiety.
