Term
| anxiolytics therapeutic rationale |
|
Definition
-interact with limbic system
-blunt anxiety by depressing the RAS
-may reduce anxiety associated with some eating disorders |
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Term
| sedatives/hypnotics therapeutics rationale |
|
Definition
-depress the RAS
-help fall asleep quicker/longer |
|
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Term
| anxiety disorders general |
|
Definition
-most prevalent psychiatric disorder
-significant comorbidity |
|
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Term
| panic disorder/PTSD/GAD more common in |
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Definition
|
|
Term
| what brain regions are responsible for anxiety |
|
Definition
-amygdala
-hippocampus
-medial frontal cortex
-RAS |
|
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Term
|
Definition
-processes incoming sensory signals and send them to high brain regions to interpret
-can trigger fear or anxiety
-emotional memories are stored in central part of amygdala |
|
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Term
|
Definition
-external stimuli
-cortex
-amygdala
-emotional memory/hippocampus/hypothalmus/midbrain/medulla (clinical manifestations) |
|
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Term
|
Definition
| -emotional aspects of fear |
|
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Term
|
Definition
|
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Term
|
Definition
| -inc. respiration, shortness of breath, feeling smothered |
|
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Term
|
Definition
| -endocrine responses (cortisol) |
|
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Term
|
Definition
-cardiovascular
-inc HR, BP, etc |
|
|
Term
|
Definition
| -alertness and arousal (vigilance) |
|
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Term
|
Definition
-NE (excitatory)
-serotonin (inhibitory)
-GABA (excitatory)
(overstimulated) |
|
|
Term
|
Definition
-benzos
-busiprone (non benzo)
-barbituates
-antidepressants
-b-adrenergic blocking agents |
|
|
Term
|
Definition
-most commonly prescribed anxiolytics
-action on GABA receptor
-4 most common
-diazepam
-lorazepam
-clonazepam
-alprazolam |
|
|
Term
|
Definition
-ligand gated
-stimulation leads to influx of Cl-
-contain a binding site for GABA and multiple sites that can be occupied by pharmacological compounds
-composed of 5 subunits
-anxiolytic effects thought to be mediated by receptors containing alpha 2 subunits |
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Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
-bind to "benzo receptor" on GABA A receptor
-induces conformational change
-increases frequency of Cl ion channels opening when stimulated by GABA
-positive allosteric modulator (inc effect of natural agonist) |
|
|
Term
|
Definition
-well absorbed after oral administration
-reach peak blood and brain concentration within 1-2 hours
-variable onset of action
-presence of food delays absorption
-metabolized by CYPs
-benzos and active metabolites are highly bound to plasma proteins |
|
|
Term
|
Definition
-CIV
-potential for dependence
-more likely with high does and LT tx
-more likely with short acting
-taping of doses |
|
|
Term
|
Definition
-used for chronic and or acute situations (PRN dosing)
-risk for relapse
-many clinicians favor combined tx |
|
|
Term
|
Definition
-withdrawal and seizures
-drowsiness/sedation
-irritability
-memory impairment
-anterograde amnesia
-depression
-rare-hypotension, blurred vision, skin rash, nausea, hypersensitivity |
|
|
Term
|
Definition
-hypersensitivity
-glaucoma
-pregnancy/breast feeding (D or X)
-caution in renal/hepatic, task requiring CNS alertness, suicidal pts |
|
|
Term
|
Definition
CNS depressants
CYP inhibitors |
|
|
Term
|
Definition
-Tx GAD, panic disorder, anxiety ass. with depression
-preg D
-CYP34A
-short half life
-halogen or nitro group yields sedative activity |
|
|
Term
|
Definition
-Tx panic disorder
-preg D
-CYP3A4
-long half life |
|
|
Term
|
Definition
-Tx anxiety, ethanol withdrawal
-preg D
-CYP3A4, CYP2C19
-long half life |
|
|
Term
|
Definition
-Tx anxiety disorders (off label insomnia, ethanol withdrawal)
-preg D
-inactivated by glucuronidation
-interm. half life |
|
|
Term
|
Definition
-tx anxiety disorder, ethanol withdrawal
-SE ataxia
-preg D
-long half life
-CYP34A |
|
|
Term
|
Definition
-tx GAD, ethanol withdrawal
-SE GI, nervousness
-preg D
-CYP3A4
-long half life
-short acting |
|
|
Term
|
Definition
-tx anxiety disorders, ethanol widthdrawal
-preg D
-glucuronidation metabolism
-50% excreted unchanged
-multiple daily doses |
|
|
Term
|
Definition
-tx benzo overdose
-anatagonist
-only has effect on drugs which bind the benzo site on GABA A
-may result in seizures
-short half life
-multiple daily doses
-IV form |
|
|
Term
|
Definition
-serotonin partial agonist
-anxiolytic
-not habit forming
-good safety profile
-freq. adjunct to SSRIs
-does not block panic attackes or tx OCD/PTSD
-takes 4-6 weeks for effects |
|
|
Term
|
Definition
-tx GAD (no sedative/hypnotic effects)
-preg B
-not recc. with hepatic/renal, or with SSRI/MAOI
-CYP3A4
-inter. half life |
|
|
Term
|
Definition
-major action on GABA receptors
-some action as an inhibitor of excitatory AMPA receptors
-commonly used before benzos
-inc sedation, toleration
-high risk of overdose
-more profound withdrawal
-rarely used for insomnia now
-thiopental
-pentobarbital
-methohexital
-phenobarbital |
|
|
Term
|
Definition
-antidepressants-SSRIs, TCA, MAOI
-B adrenergic antagonists |
|
|
Term
|
Definition
-difficulty falling asleep
-assoc. with anxiety disorders |
|
|
Term
|
Definition
| -assoc. with pain disorders |
|
|
Term
|
Definition
-early morning waking
-characteristic of clinical depression |
|
|
Term
|
Definition
-benzos
-benzo receptor agonists
-melatonin receptor agonists
-barbituates |
|
|
Term
| FDA warning for insomnia tx |
|
Definition
-all sedative hypnotic drugs including benzos
-requiring stronger warnings on product labeling
-possibility of severe allergic rxns
-complex sleep related behaviors |
|
|
Term
| non pharm tx for insomnia |
|
Definition
-reduce stress, anxiety
-avoid caffeine, alcohol, nicotine before bed
-dont take naps |
|
|
Term
|
Definition
-tx insomnia
-pregnancy x
-CYP3A4
-interm half life |
|
|
Term
|
Definition
-insomnia
-preg x
-CYP3A4
-long half life |
|
|
Term
|
Definition
-tx insomnia
-preg x
-CYP3A4
-interm half life |
|
|
Term
|
Definition
-bind to GABA A
-diff affinity and structure
-higher affinity for alpha 1
-CIV |
|
|
Term
|
Definition
-tx insomnia
-preg c
-CYP3A4
-interm half life
-long acting |
|
|
Term
|
Definition
-tx insomnia
-preg c
-CYP3A4
-short half life |
|
|
Term
|
Definition
-tx insomnia
-preg c
-CYP3A4
-longer half life than other benzo recp. agonists |
|
|
Term
| melatonin receptor agonist general |
|
Definition
-ramelteon
-melatonin
-produced in pineal gland
-regulated by SCN-hypothalamus)
-via light dark
-determines circadian rhythm
-sleep wake cycle |
|
|
Term
|
Definition
-doesnt bind GABA
-binds and activates melatonin (MT1 and MT2)
-has not shown abuse potential
-no withdrawal or rebound insomnia (typical of GABA drugs) |
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