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severe respiratory depression; teratogenic; depress liver and kidney function; reduce GI motility; lower body temperature
What are the 5 adverse effects of barbiturates?
zolpidem (ambien); zaleplon; eszopiclone
What are the 3 Z compounds?
aloprazolam (xanax); clonazepam (klonopin); lorazepam (ativan)
What are the 3 most prescribed anti-anxiety drugs in the U.S. (all 3 are benzodiazepines)?
-zolam; -zepam
What are the 2 suffixes for benzodiazepines?
klonopin
What is the trade name for clonazepam?
sedation
- decrease activity
- moderates excitement
- calms the recipient
- increase respiratory depression (caution)
hypnosis
- drowsiness
- facilitates the onset and maintenance of sleep that resembles natural sleep
cause membrane hyper-polarization (makes it more negative which leads to neuronal inhibition because it makes it hard to cause action potential)
How does benzodiazepines change the membrane potential of neurons?
cns depression; anterograde amnesia; respiratory effects (apnea); visual and dental effects (contraindicated in narrow angle glaucoma; xerostomia, swollen tongue and bitter/metallic tase); thrombophlebitis (blood clot)
What are the 5 adverse effects of benzodiazepines
myathenia gravis; obstructive sleep apnea; acute angle closure glaucoma
What are the 3 contraindications of benzodiazepines?
flumazenil
What is benzodiazepine antagonist?
acute barbiturate poisoning (overdose)
How did Marilyn Monroe die?
thiopental
What is the ultra short acting barbiturate?
zolpidem (ambien)
Z compound:
- quick onset of action
- sife effects: headache, drowsiness, dizziness and diarrhea
- ambien: a controlled release dose form
anxiolytic; sedative; hypnosis; sleep; amnesia
What are the 5 effects of sedative-hypnotic agents?
benzodiazepines
What is the most popular class of medication is used for anti-anxiety?
xanax
What is the trade name for alprazolam?
ativan
What is the trade name for lorazepam?
yes
Can a drug produce both sedation and hypnotic effects?
GABA
What receptors do benzodiazepines activate?
NMDA; AMPA
What 2 receptors cause excitatory neurosignaling?
GABA
What receptor causes inhibitory neurosignaling?
balance; inhibitory
NMDA/AMPA (excitatory receptors) and GABA (inhibitory receptors) are in _______________ but when drugs activate GABA ______________ signaling occurs
decreased excitatory neurosginaling
What would happen if you blocked NMDA receptors?
enhance
Do benzodiazepines enhance or inhibit the GABA activity?
chloride
What ion is involved with GABA receptors?
less likely
Is the neuron more or less likely to fire action potential after a patient take a benzodiazepine?
wider therapeutic range; less addictive
In what 2 ways are benzodiazepines "better" (or safer) than barbiturates?
yes
Can you be addicted to benzodiazepines?
seizures (so must taper off)
What can happen if patient abruptly stops taking benzodiazepines?
yes
Can you develop tolerance to benzodiazepines?
Benzodiazepine overdose (do not use when a patient has been taking benzos for a long time; Xanax + flumazenil = withdrawal symptoms and seizures)
When is flumazenil used?
decrease (by increasing metabolism which decreases bioavailability since rifampin induces CYP3A4)
Does rifampin (for TB) increase or decrease the therapeutic effect of benzodiazepines?
increase (by decreasing metabolism which increases bioavailability since GF juice inhibits CYP3A4)
Does grapefruit juice increase or decrease the therapeutic effects benzodiazepines?
high rates of abuse; complete cardiovascular and respiratory depression with overdose; narrow therapeutic range
What 3 things makes barbiturates more unsafe compared to benzodiazepines?
respiratory depression
decrease in depth and rate of breathing
Barbiturates
MOA of _________________:
- prolongs the period of Cl- ion channel opening
Benzodiazepines
MOA of _________________:
- increases frequency of Cl- ion channel opening
alprazolam; clonazepam
Which 2 benzodiazepines are subject to CYP3A4-mediated metabolism?
lorazempam
What benzodiazepine is not subject to CYP3A4-mediated metabolism?
false
True or False?
You can combine benzos and barbiturates (sedatives) with other CNS depressants
benzodiazepine receptors
What receptor do z compounds act on?
insomnia
What are z compounds mainly prescribed for?
can cause breathing problems
Why is it not a good idea to mix benzos or z compounds with alcohol?