Drugs with CNS effects act of what receptors (neurotransmitters) - Answer-GABA
Acetylcholine
Seratonin
Dopamine
Norepinephrine
Anti- anxiety drugs, and sedative hypnotic drug classes - Answer-Benzodiazapimes, atypical anxiolytics,
sedative hypnotics, barbituates
Benzodiazepine drugs - Answer-All the "pams" plus librium
Alprazolam (Xanax)
Chlordiazepoxide (Librium)
Clonazepam (Klonopin)
Diazepam (Valium)
Lorazepam (Ativan)
Oxazepam (Serax)
,Benzodiazepine like drugs - Answer-Eszopiclone (Lunesta)
Zolpidem (Ambien)
Mechanism of action of benzodiazepine - Answer-increases the action of GABA (an inhibitory
neurotransmitter) thereby decreasing neuronal excitation. Benzos bind to the benzodiazepine receptor.
When GABA increases, it decreases neuronal excitation=reduction in anxiety, muscle relaxation, and
anticonvulsant.
Metabolized in the liver- highly lipid soluble & protein bound
Adverse effects of benzodiazepines - Answer-Major effects due to action as CNS depressant- sedation,
cardiac and resp depressant, depression, confusion, hypotention
May also see paradoxical anxiety, agitation, and acute rage
Psychological and physical dependence
Considerations with benzodiazepines - Answer-Development of dependence- must taper off as it can
cause physical and psychological withdrawal symptoms
Xanax and Ativan are more likely to develop dependence. Prescribe Clonazepam (Klonopin) is less likely
for dependence due to its long action.
Benzos are for *short-term* treatment of anxiety
Atypical Anxiolytic - Answer-Buspirone (Buspar)
, Benzodiazepines interact with - Answer-MAOI's, SSRI's, etoh, antihistamines, pregnancy category D
Buspirone (Buspar) MOA - Answer-Buspirone (BuSpar) - approved for the treatment of GAD
Full agonist at the pre-synaptic serotinin-1A (5-HT 1a) receptor, also has action at dopamine receptors
Short half-life, but slow onset of action
Metabolized by oxidation, excreted in urine
Buspirone (Buspar) considerations - Answer-Absorbed well orally
Should be taken with food to decrease first-pass effect
NOT to be used in individuals with liver or renal disease
Takes 1 to 2 weeks for onset of anxiolytic effects. Up to 6 weeks for maximum effects.
Buspirone (buspar) interacts with - Answer-Anti psychotics such as haldol- compete for metabolism site.
Buspirone is used in conjuction with - Answer-SSRI's-augements the response in individuals with
agitated or anxious depression
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