Anxiolytics Flashcards
Describe the mechanism of action of barbiturates.
They bind to sites on the GABA-A receptor which enhances the duration of GABA-mediated Cl- flux. At high doses it can directly open the Cl- channels. This causes hyperpolarization resulting in neuronal inhibition.
Name the barbiturates.
Phenobarbital
Describe the adverse effects associated with barbiturates.
They have a low therapeutic index putting patients at risk for overdose and also have a high rate of dependence/addiction.
What anxiolytics are CYP inducers?
Barbiturates
What are some clinical indications for barbiturates?
Anesthesia and seizure disorders, rarely as a sedative or hypnotic
Describe the mechanism of action of benzodiazepines.
They bind to sites on the GABA-A receptor facilitating GABA-mediated Cl- influx, causing hyperpolarization and thus neuronal inhibition.
Describe the adverse effects associated with benzodiazepines.
Higher doses can cause anterograde amnesia (though this is beneficial for anesthesia purposes), resp depression, decreased BP, increased HR, some tolerance (but less than barbiturates)
Describe the drug interactions of benzodiazepines.
There aren’t any.
Name the clinical indications for benzodiazepines.
Epilepsy tx, anesthesia (e.g. midazolam- Versed), muscle relaxation for neuro disorders
What is a contraindication for benzodiazepines?
Sleep apnea (b/c of resp depression)
Describe the pharmacokinetic properties of benzodiazepines.
They have slower absorption (2-4 hours, but rapid CNS entry), convert to active metabolizes, and are excreted in the urine.
How do benzodiazepines differ from barbiturates?
Benzos can’t directly open the Cl- channel so they have no effect without the presence of GABA, which helps to limit toxicity and have a higher therapeutic index than barbiturates.
Describe the mechanism of action of benzodiazepine receptor agonists.
They are chemically distinct from benzodiazepines but bind to the same benzodiazepine binding site on a subset of the GABA-A receptors
Name the drugs that act at the GABA receptor.
Barbiturates, benzodiazepines, benzodiazepine receptor agonists, and benzodiazepine receptor antagonists
What are the adverse effects associated with benzodiazepine receptor agonists?
Decreased clearance in elderly/hepatic dysfunction, resp depression at high doses, anterograde amnesia, sleep-walking
What are the clinical indications for benzodiazepine receptor agonists?
Middle of the night waking. Has less REM suppression and less tolerance/psychological dependance/abuse than benzos