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25 Cards in this Set

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What is the primary use of benzodiazepines?
Primarily used for generalized anxiety disorder (GAD)

Also to relieve transient anxiety

(Antidepressant venlafaxine also now used to treat GAD)
Clomipramine is effective in treating…?
TCA
-- effective in treating OCD
SSRIs are effective in treating…?
PTSD in non-combat veterans

Social anxiety disorder

Also effective in treating OCD
Buspirone is effective in treating…?
GAD

Takes about 1 wk
Beta blockers are effective in treating…?
Performance related anxiety
-- musical performances
How do we treat General Anxiety Disorder?
BENZODIAZEPINES
-- alprazolam
-- clonazepam
-- diazepam
-- flurazepam
-- oxazepam
-- triazolam

Most commonly prescribed b/c of efficacy and favorable side effect profiles
What do benzodiazepines do?
Produce a general DEPRESSION of neuronal systems w/ more potent effects at polysynaptic connections

Clinically relevant CNS sites of action include brain stem (reticular activating system), diencephalons (limbic system) and cerebral cortex. Fxnally responsible for:
1. sedative hypnotic properties
-- decrease duration of stage 1, ¾, and REM
-- decrease latency to persistent sleep
-- increase stage 2 and total sleep time
2. anti-anxiety effects
3. anti-convulsant properties
4. muscle relaxant effects (at spinal cord level)
5. conscious sedation
6. pre-op med
Which meds are used for seizures?
Clonazepam (Klonopin)
Diazepam (Valium)
Which benzodiazepine is the DOC for the elderly?
Oxazepam

Glucuronidation and renal secretion
Which benzodiazepine is the shortest acting?
Triazolam (Halcion)
Which benzodiazepine has the highest potency w/ little sedation?
Alprazolam (Xanax)
Which is the preferred benzodiazepine for panic disorder?
Clonazepam
What are the new hypnotics (non-BZs)?
“Z drugs”

Zolpidem (Ambien)

Zaleplon (Sonata)

Eszopiclone (Lunestra)
NonBZ new hypnotics?
Act through the GABAa receptor
-- BZ receptor agonists
-- less abuse potential
-- mild side effects (drowsiness, dizziness, headache)
-- little effect on sleep stages
-- no alcohol potentiation
-- half-life

AMNESTIC!

NOT an anxiolytic, anticonvulsant, or muscle relaxant
What is the half-life of the non-BZs?
Zolpidem = 2.6hr

Zaleplon = 1hr

Exzoplicone = 6.5hr
BZ metabolism?
Primarily metabolized by oxidative reactions or by conjugation to flucuronic acid.

Conjugation tends NOT to be affected by aging whereas oxidation is decreased

Oxazepam is metabolized by conjugation – thus DOC for elderly
BZ side effects?
1. In general , SEs are modest and readily managed
-- little organ toxicity
-- minimal capacity to induce hepatic enzymes

2. Main SEs are
-- sedation, dizziness
-- uncoordination, paradoxical agitation
-- impairment of cognitive fxn

3. minimal suicide potential w/ overdose by themselves, although combo w/ alcohol may be more problematic
BZ antagonist?
FLUMAZENIL
-- Acts at the BZ receptor to prevent the binding of BZ to it
Clinical uses of Flumazenil?
LIMITED

1. BZ overdosage
-- short half-life is a problem

2. to reverse rapidly the effects of BZ when they are used as an adjunct w/ anesthesia in outpatient surgery

TestQ: Reverse respiration depression due to BZ
Buspirone use?
ANTI-ANXIETY AGENT

1. slower onset of action than BZs
-- takes ~1wk to work

2. appears to have minimal w/d potential

NON-BZ
Buspirone side effects?
Dizziness and nausea
Buspirone MOA?
Appears to involve direct action of serotonin receptors (probably the 5-HT1A receptor)

Hyperpol cells via K+ conductance
Treatment of Panic Disorder?
BZs may help minimize the “anticipatory anxiety” associated w/ panic attacks, but may be relatively ineffective against the condition itself
1. in general, high potency BZs used (too much sedation w/ lower potency drugs)
-- alprazolam
-- clonazapam
2. It may be necessary to use higher doses of alprazolam to treat PD than are generally used to treat GAD
3. Be aware of increased risk of seizures and severe w/d rxns upon cessation of trtmt w/ high doses of alprazolam

TCAs and MAOIs represent standard treatment for PD
1. demonstrated efficacy in controlled studies
2. necessary to use the same doses for the usual periods of time in order to obtain effective control of symptoms of PD as is needed in the treatment of depressive disorders
3. same S/E profiles and dietary limitations apply w/ regard to their use in the treatment of PD
4. SSRIs are also effective in PD
Treatment of OCD?
CLOMIPRAMINE

Norepi reuptake blocking effects, but most distinctive among the TCAs for being a very potent inhibitor of serotonin reuptake.
-- serotonin reuptake seems necessary for efficacy in OCD

SSRIs are also effective in OCD
-- fluoxetine
-- fluvoxamine
-- paroxetine
-- sertraline
Summary…?
GAD
1. BZ
-- differ in pharmacokinetic profiles
-- rapidly acting, effective, relatively safe
-- carry risk of w/d rxns
-- MOA involves BZ-GABAa receptor complex and Cl ion influx to produce mbrn hyperpolarization
-- CNS depressants
2. buspirone
3. venlafaxine
4. SSRIs


BUSPIRONE is effective also in GAD, but slow in onset of action
-- appears to have no abuse potential
-- MOA is speculated to involve serotonin receptors (partic 5-HT1A receptors)