Benzodiazepines Flashcards
MOA of benzos
- bind to GABA receptors in the synapse
- decrease the excitability of neurons by increasing efficiency of GABA
metabolism of benzos
CYP450
side effects of benzos
- MC: sedation, impaired concentration
- dizziness, ataxia, muscle twitching
what side effects of benzos should you be alert to?
disinhibition with paradoxical agitation and/or aggression
overdose sx of benzos
respiratory depression (esp if combined with ETOH)
what determines the severity of withdrawal symptoms from benzos
the faster the serum levels of the drug falls, the worse the sx
which benzo is known for its withdrawal?
xanax
symptoms of withdrawal from benzos
increased anxiety, tremor or shakiness, muscle twitching, sweating, tachycardia, HTN, zeizures
pros of long acting benzos
provide less symptom fluctuation and less severe withdrawal
cons of long acting benzos
higher potential for drug accumulation and therefore sedation
how should you start dosing benzos?
LOW and go SLOW
how long until a patient can develop tolerance/dependence from benzos?
3 weeks
what is the biggest mistake when it comes to benzos?
continuing them indefinitely
safest and efficient strategy of benzos
- start with a short/intermediate acting benzo at a low dose to begin, then titrate up
- continue for 2-6 weeks followed by a 1-2 week taper
- during those 6 weeks, start SSRI
alprazolam
xanax
indications for xanax
panic d/o, GAD, social phobia
onset of xanax
fast
how many times is xanax taken a day?`
can be multiple
why is there an abuse potential with xanax?
fast euphoria commonly reported
how sedating is xanax?
less than other benzos`
diazepam
valium
indications for valium
anxiety, ETOH w/d, adjunct tx of muscle spasm and movement disorders
half-life of valium
a really really long time (100 hours)
downside of valium
longer half life leads to accumulation of active metabolites, especially in elderly
lorazepam
ativan
indications for ativan
anxiety, ETOH w/d, adjunct in acute psychotic agitation
are there active metabolites in ativan?
NO
metabolism of ativan
NOT CYP450 - good choice if pt on other meds or has comorbid conditions
how is ativan excreted?
renally - unique!
special quality of ativan
ONLY benzo in IM form that has a rapid, predictable and complete absorption
chlordiazepoxide
librium
indications for librium
anciety and ETOH w/d
half life of librium
> 100 hours
what is the caution with librium and the elderly?
since the long half life ensures drug will accumulate with multiple dosing, they may become suddenly obtunded
metabolism of librium
CYP450
clonazepam
klonopin
indication for klonopin
initially an anticonvulsant, NOW for panic d/o, social phobia and GAD
half like of klonopin
long, but has a rapid onset & is very potent
metabolism of klonopin
CYP450
triazolam
halcion
onset of halcion
rapid after oral administration
half life of halcion
shortest of all benzos
indication for halcion
initiation of sleep issues
estazolam
prosom
action of prosom
intermediate
temazepam
restoril
action of restoril
intermediate
flurazepam
dalmane
action of dalmane
long
quazepam
doral
action of doral
long
Oxazepam
Serax - short
