Drugs for Anxiety Flashcards
What is the MOA of Barbiturates?
bind GABA receptor and enhance duration of GABA mediated Chloride flux, causing hyperpolarization of neuron= neuronal inhibition
at higher concentrations, directly open GABA Cl- channels
What is the use of sedative-hypnotics at low-doses?
anxiolytic and sedative
What is the use of sedative-hypnotics at high doses?
anesthesia, but also may cause coma and death
What drugs are Benzodiazepines?
-alprazolam
-clonazepam
-diazepam
-lorazepam
-midazolam
-triazolam
-remimazolam
Which benzodiazepine is used as a sleep aid?
triazolam
Which benzodiazepine is used for seizure control and muscle relaxation?
diazepam and clonazepam
What is the MOA of benzodiazepines?
increase the frequency of GABA mediated channel opening and Cl- influx causing hyperpolarization of the neuron and neuronal inhibition
Where are benzodiazepine binding sites?
-alpha 1: mediates sedation
-alpha 2/3: mediates anxiolysis
-alpha 5: mediates cognitive impairment
What is the difference of benzodiazepines from barbiturates?
benzos do not have direct effect and cannot directly open channels= no response without GABA which limits toxicity
Which benzodiazepines are full agonists?
diazepam and zolpidem
What is the selectivity of zolpidem?
alpha1
What drug is a benzodiazepine is an antagonist?
flumazenil
What is the use of flumazenil?
competitively inhibits the effects of full agonist benzodiazepines (no effects when given alone!)
What are the therapeutic indications of Benzodiazepines?
-anxiety (short term only (2-4 weeks), long term treatment is antidepressants)
-anesthesia (midazolam)
-muscle relaxation
-sleep disorders
-epilepsy
Which benzodiazepine is associated with abuse potential?
alprazolam, due to rapid absorption and CNS entry
