Anxiolytics Flashcards
How do benzodiazepines work?
They potentiate GABAminergic stimulation. They regulate chloride channels that result in hyperpolarization of the cells in the CNS, making them less likely to fire.
How are BDZs and barbituates similar?
Barbs prolong, rather than potentiate GABAminergic stimulation, and at higher doses have a direct effect on chloride channels (more toxic).
BDZs have a wide/narrow therapeutic range.
What is the antidote for BDZ?
Wide - so death from OD is rare unless combined with another CNS depressant
Flumazenil.
T or F. All BDZs are the same in onset, duration and metabolism.
F - different
What are the clinical uses for BDZs?
- anxiety
- Antiemetic (chemo patient)
- Insomnia
- break Seizure
- anesthetic induction
- ETOH withdrawal
- Muscle relaxation
T or F. BDZs should be tapered due to a withdrawal phenomenon.
T
What are some common AEs of BDZs?
Drowsiness
confusion
sluggishness
retrograde amnesia
What C-Classification are BDZs?
4
Name two short acting BDZs.
Lorazepam and Oxazepam
Which BDZs are preferred in hepatic disease due to lack of active metabolites and short half life?
Lorazepam and Oxazepam
What is the final metabolite of Diazepam?
Oxazepam
What is the generic name for xanax?
Alprazolam
What drug has specific efficacy in the management of panic attacks (fear of flying, stage fright, etc)
Alprazolam
What is the generic name from Valium?
Diazepam
Why is Valium not a good option for the elderly?
It is Long-acting w/ multiple acting agents
What anxiolytic used to be used for insomnia but has since then been replaced with other meds?
Temazepam (Restoril)
Which anxiolytics are approved for panic attacks?
Alprazolam
Temezepam
Which anxiolytic is not a benzo, and acts as a serotonin agonist?
Buspirone (BuSpar)
What are the pros of Buspar?
Non sedating
No confusion or buzz
No street value bc it is not a benzo
“Good for a bus driver”
What are the cons for Buspar?
Takes a few weeks to show effect so it cannot be used PRN or for acute panic attacks
What drug is indicated for the short-term treatment of insomnia (should not be used for greater than 7-10 days). Why is it not typically used long-term?
Zolipedem (Ambien)
C4 schedule, bad hangover
Name the non-benzos benzos.
Ambien - Zolipidem
Zaleplon (Sonata)
Eszopiclone (Lunesta)
Which has a shorter half life - Zolipdem or Zaleplon?
Zalepon
When will you see effects using Zaleplon?
Rapid onset - peak effect in 1 hour with a duration of 6 hours.
What insomnia drug is best for mid-night awakenings?
Zaleplon
What drug mimics Zaleplon in its rapid onset?
Ambien CR.
How does Ambien CR help someone fall asleep and stay asleep?
It has a rapid onset and gradually releases the drug throughout the night.
What is the L for in Lunesta (Eszopiclone)? What is it indicated for?
long half life
Chronic insomnia
Can Ambien break a seizure?
Cannot break a sz and has no effect on skeletal muscle
How does Ramelteon work? Does it have affinity for GABA?
Melatonin receptor agonist (MT1, 2).
No affinity for GABA.
Which drug mimics normal sleep-wake cycles and is approved for long-term use of insomnia?
Ramelteon (Rozerem)
A patient known for drug-seeking complains of insomnia. What may be a good option here?
Rozerem - non scheduled
What is the main con of Ramelteon?
CYP metabolism - drug reactions
What is typical dose of Ambien?
10 mg at bedtime in adults, reduce to 5mg in elderly or in patients with hepatic dysfunction
Name the orexin receptor antagonist that suppress the wake drive? It is cheap or expensive?
Suvorexant (Belsomra)
expensive
What is the dosing regimen for Suvorexant?
10 mg 30 min prior to bed time and allot 7h of sleep time
When should you dose down Suvorexant?
WHen patients have hepatic dysfunction or are on strong CYP inhibitors.
What happens when you combine alcohol and Belsomra?
Sleep-waking behavior
What highly sedating drug is known as a Mickey Finn?
Choral Hydrate
What are some other sleep aiding drugs?
- Diphenhydramine - Benadryl
- TCAs
- Trazadone and Mirtazepine - sedating antidepressants
- Low dose Seroquel - antipsychotic
- Melatonin
