anxiolytic drugs Flashcards
Describe the general mechanism of action of the sedative-hypnotic agents.
Produce graded dose-dependent CNS depressant effects
Distinct mechanism of depressant action: augment GABA inhibition and/or inhibit glutamate excitation
Discuss the relation between drug effects on GABA vs glutamate function and their clinical uses and safety margins.
We don’t use glutamate blockers because they are too dangerous
Relate differences in the pharmacokinetic disposition of benzodiazepines to their clinical uses.
A
Describe the unique pharmacodynamic profile of buspirone and its role in the treatment of anxiety.
5HT1A partial agonist - NOT a benzodiazepine
Some D2 receptor block monitor for possibility of extrapyramidal system side effects
NO sedation - additive CNS depression, anticonvulsant, or myorelaxant action
Requires 2 weeks for onset of anxiolytic effect and 4-6 weeks for maximal efficacy
More useful and effective in chronic anxiety
Less patient acceptance
Must be administered on routine schedule - not prn use
List additional clinical indications for benzodiazepines (Benzodiazepines: Diazepam, Alprazolam, Lorazepam, Oxazepam, Flumazenil, Midazolam; Barbiturates: Pentobarbital, Phenobarbital)
Can use benzos for alcohol withdrawal, and use both for seizures, muscle relaxant sleep
Diazepam is drug of choice for status epilepticus
Describe the side effect profile of the benzodiazepines as it relates to their limited utility in treatment of anxiety.
Daytime sedation and performance impairment
tolerance, psychological dependence, physiological dependence, withdrawal, additive effects with other CNS depressants Alcohol, opioid analgesics, TCADs, antipsychotic agents, anticonvulsants, antihistamines, Anterograde Amnesia
Benzodiazepines and barbiturates share which of the following pharmacologic properties?
A. Augment GABA action at the GABA receptor-chloride channel complex at low doses
B. Ability to maintain surgical anesthesia (stage III) when administered intravenously
C. Inhibition of GABA neurotransmission
D. Efficacy in the treatment of seizure disorders
E. High therapeutic index
F. Agonist action at benzodiazepine receptors
G. Addiction potential with prolonged use
Efficacy in the treatment of seizure disorders
Augment GABA action at the GABA receptor-chloride channel complex at low doses
Addiction potential with prolonged use
Which of the following properties is shared by both inhalational general anesthetics and oral benzodiazepine anti-anxiety agents?
A Maintenance of Stage III surgical anesthesia
B Potentiation of GABAA receptor activity
C Low margin of safety
D Relatively low potency
E Inhibition of excitatory synaptic transmission
B Potentiation of GABAA receptor activity
BDZs or barbiturates enhance channel opening only in presence of GABA
BDZ’s
Administration of flumazenil (Romazicon) will reverse the toxicities associated with an overdose of: Alcohol Barbiturates Benzodiazepines Morphine All of the above A, B, and C only
benzos
which benzos are nice on the liver
oxazepam, lorezapam
Side effects associated with the use of benzodiazepines in treatment of anxiety disorders could include all of the following EXCEPT: A Development of physical dependence B Development of psychologic dependence C Ataxia and risk of falls in the elderly D Retrograde amnesia E Excessive daytime drowsiness F Impaired judgment G Exacerbation of porphyria H Could include all of the above
D Retrograde amnesia
G Exacerbation of porphyria
what is 1st and second line for anxiety?
SSRIs or SNRIs first line medication treatment
Especially patients with comorbid depression
If response, duration should be at least 6-12 months
Second line medications
TCADs: not preferred cardiotoxicity in OD + tolerability
BDZs: efficacious w/i min-hr - concerns with abuse - adjunct to SSRI-SNRI for acute management while SSRI take effect
Buspirone: time to onset longer and weaker anxiolytic effect than BDZs; used as augmentation to SSRIs
what do u take for acute panic attack?
benzo
