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anxiolytics
anxiolytics
30
Pharmacology
Professional
11/12/2012

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Term
anxiety
Definition
fear or apprehension of something dreadful
Term
treatment of anxiety
Definition
when it interferes with normal life
when it interferes with part of another disease
Term
physiological effects of anxiety
Definition
restlessness
tachycardia
tension
hypertension
sweating
dyspnea without identifiable cause
avoidance behavior
arousal
decrease in concentration
Term
types of anxiety
Definition
generalized anxiety disorder (GAD)
panic disorder
obsessive compulsive disorder (OCD)
social anxiety disorder or social phobia
post-traumatic stress disorder (PTSD)
social phobias
anxiety associated with other medical issues
Term
induced anxiety
Definition
drugs: cocaine, beta agonists, psychostimulants
diseases: CHF, COPD, diagnosis of terminal diseases
withdrawal: antidepressants, anxiolytics, drugs of abuse
Term
norepinephrine in anxiety
Definition
over firing of locus ceruleus
Term
GABA in anxiety
Definition
counteracts stimulatory effects of excess NE
GAD, panic
Term
serotonin
Definition
5HT1a receptors targeted in treatment
GAD, panic, OCD, social anxiety
Term
corticotropin-releasing factor (CRF) and HPA axis
Definition
hyperregulation
suppression after treatment of PTSD
Term
drug treatments for anxiety
Definition
benzodiazepines
buspirone (BuSpar)
antidepressants
beta blockers
Term
norepinephrine in anxiety
Definition
over-firing in locus ceruleus
GAD, panic, PTSD, OCD, social anxiety
Term
benzodiazepines (receptor, SE's, tolerance)
Definition
bind to the receptor on GABAa: increases Cl- influx, decreased neuronal firing
side effects: sedation, anterograde amnesia, confusion
tolerance: occurs with sedative and anticonvulsant effects, NOT seen with anxiolytic effects
Term
GABA in anxiety
Definition
counteracts stimulatory effects of excess NE
GAD, panic
Term
serotonin in anxiety
Definition
5HT1a receptors targeted in treatment
GAD, panic, OCD, social anxiety
Term
corticotropin-releasing factor (CRF) and HPA axis
Definition
hyperregulation
suppression after treatment in PTSD
Term
anxiolytic benzodiazepines
Definition
alprazolam (Xanax)
Chlordiazepoxide (Librium(
clonazepam (klonopin)
diazepam (valium)
lorazepam (ativan)
oxazepam (serax)
Term
considerations for benzodiazepines
Definition
pharmacokinetics:
short half-life: reach steady state faster, more likely to have rebound anxiety
long half-life: active metabolites, accumulation, drowsiness, amnesia
potential for dependence and/or abuse
short-term use preferred
Term
buspirone (BuSpar)
Definition
partial agonist on brain 5HT1a receptors
moderate affinity for brain dopamine D2 receptors
longer onset of action than BZD
little abuse potential
Uses: GAD, social anxiety, or cormorbid depression; adjunct use with OCD, PTSD
not good for panic disorders
Term
advantages of buspirone
Definition
little or no sedation
no CNS depression
no muscle relaxation
little abuse, tolerance, or withdrawal
Term
disadvantages of buspirone
Definition
slow onset: 1-2 weeks for onset, 2-3 weeks for full effect
not for severe anxiety
not for panic attacks
best in naive patients
Term
SSRIs
Definition
1st line treatment for OCD and panic
other uses: social anxiety, PTSD, GAD
doses are usually higher than ones used for treatment of depression
panic disorders: start with very low doses, titrate doses up slowly
SE's: nausea, diarrhea, sweating, decreased libido, anorexia
Term
anxiolytic SSRIs
Definition
fluoxetine (Prozac)
paroxetine (paxil)
sertraline (zoloft)
fluvoxamine (Luvox)--only FDA-approved for OCD
citalopram (Celexa)--unlabeled use for OCD
escitalopram (lexapro)--only FDA-approved for GAD
Term
clomipramine (Anafranil)
Definition
TCA
primarily inhibits serotonin reuptake
2nd line therapy for OCD
often used in combination with SSRIs
SE's: may be the same or slightly more severe than other TCAs
Term
venlafaxine (Effexor)
Definition
FDA-approved uses: GAD, social anxiety disorder, panic disorder
unlabeled/investigation use: OCD
drug interactions: CYP2D6 substrate
only SSRI up to 150mg/day
SNRI once 150mg/day exceeded
dosage range-75-300mg/day
Term
duloxetine (cymbalta)
Definition
FDA-approved use: GAD
drug interactions: CYP1A2 and CYP2D6 substrate/inhibitor
SNRI across all doses
dosage range-60-120mg/day
Term
propranolol
Definition
beta blocker
uses: social anxiety, PTSD-nightmares
CNS penetration-lipophilic
decreased peripheral symptoms of anxiety
monitor cardiovascular effects: HR, BP
SE's: hallucinations, vivid dreams, lethargy, impotence
Term
hydroxyzine (Vistaril)
Definition
histamine H1 antagonist
Term
doxepin (Sinequan, discontinued)
Definition
TCA
unlabeled/investigational anxiolytic activity
Term
clonidine (catapres)
Definition
alpha2 agonist
uses: panic attacks, anxiety associated with drug withdrawal
Term
investigational anxiolytics
Definition
serotonin receptor antagonists, GABA uptake blocker, partial benzodiazepine receptor agonists
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