Anti-anxiety Agents (Exam 5)

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?