Flashcards in Sleep Pharm Deck (27)
Describe the 2 arousal pathways
1) Cholinergic neurons from the upper pons, PPT, and LDT activate the Thalamus
2) Monoaminergic: Dopaminergic (ventral tegmental nucleus), histaminergic (tuberomamilary), serotonergic (raphe nucleus), activate the cortex to process thalamic input followng cholinergic activation
What the hell does orexin do?
Orein activates all of the wakeful state pathways listed above. Mediates the rapid transition between sleep and awake.
Remember the safety issues with barbiturates:
They work by modulating GABA receptors to make GABA last longer. At very high doses can activate GABA itself. Remember the graph, the effects of larger doses just keep increasing. You'll first feel sedated, then hypnotic, then completely out (anesthetized, then hit coma and it can kill you.
How do you recognize a barbiturate drug by its name?
They all end in -barbital
Benzos are much safer than barbiturates, remember their mech and how they shift the dose response curve to the left
All benzos are excreted how?
Al Benzos end in
Benzo with the longest half life
Short half life benzos? (will not accumulate)
Estazolam and Lorazepam
All the benzos are contraindicated in
LIVER dz , COPD, Depression, Driving, other CNS drugs, Glaucoma, Category x
All the benzodiazepines are metabolized via CYP3A4 except for
Quazepam which is CYP2B6
Quaepam and Flurezepam accumulate
KNOW....along with Diazepam
What the hell are the benzodiazepine receptor agonists?
- Important to note that they are all similar to benzo in their MOA. Include the same side effects like sedation, cognitive impairment, rebound insomnia with the short acting drugs
Which can be used in pregnancy? Benzos or benzo receptor agonists?
Benzo receptor agonists- these are category c drugs
Benzos are category x
Benzo receptor agonists we should know
most prescribed insominia drug on the market. comes in a sublingual form and a spray so that it can be used in the middle of the night and acts fast.
variability in asians
FLUMAZENIL IS IMPORTANT WHY?
It is a benzo antagonist. reverses sedation from benzos quickly. IV agent.
Can cause abrupt awakening with agitation and potentially increase adverse effects.
Melatonin receptor agonist (MT-1 receptor)
Adverse effect of sedation comes in handy when you're treating ppl who can;t sleep.
AEs of antidepressants
- Cyps interactions
- Interaction with alcohol
anti-H1 at low dose, muscarinic blocker
significant alpha 2 antagonism
1st gen antihistamines work how
Cross the BBB easily and produce rapid sedation through central H1 block
WHat must you watch for with 1st gen antihistamines
blurred vision, INCREASED OCULAR PRESSURE therefore they are contraindicated in old ppl and glaucoma pts