Sedatives and Hypnotics Flashcards
What do Benzodiazepines do to the EC50 for the GABA-induced Cl- influx
decreases it ie LEFT SHIFT (slide 18 of sedatives)
Actions of the benzodiazepines
1) reduction of anxiety
2) sedative and hypnotic actions
3) anticonvulsant
4) muscle relaxant
5) anesthesia
Name the short acting benzodiazepines please
Diazepam
Flurazepam
Name the intermediate acting benzodiazepines please
Alprazolam
Lorazepam
Temazepam
Name the long acting benzodiazepines please
Oxazepam
Triazolam
Name the benzodiazepines that are directly conjugated and are not metabolized at P450
oxazepam - short acting
lorazepam - intermediate acting
temezepam - intermediate acting
(TO < LAT < DF)
Which benzodiazepines are P450’d to intermediate active metabolites before being conjugated
diazepam
flurazepam
LONG ACTING
Treat me: I have skeletal muscle spasms from MS and cerebral palsy ie degenerative disorders
Dizepam - long acting
Treat me: seizures
clonazepam
Treat me: status epilepticus
diazepam - long acting
lorazeaom - intermediate
Treatm me: OH withdrawl
diazepma - long acting
oxazepam - short acting
Treat me: sleep disroders
flurazepma - long
temazepam - intermediate
triazolam - short
A/se of Benzoa
drowsy, confusion
ataxia
cognitive impairment
PARADOXICALs: anxiety, irritabiliyt, hostility, rage, paranoia, depression, suicidal ideation (dose related)
Withdrawal sxs of Benzos
confusion, anxiety, agitation, restlessness, insomnia, tension
MOA benzos
increase FREQUENCY of channel opening
MOA barbituates
increase DURATION of GABAa opening
inhibit glutamate receptors centrally
inhibit sodium receptors centrally
Actions of barbituates ie things to watch out for
respiratory depression - stops hypoxic chemoreceptor response to CO2
induceds p450s
Thiopental use
barbituate used IV to induce anesthesia - short duration
Phenobarbital use
barbituate long term management of a) tonic clonic seizures b) status epiliepticus and c) Eclampsia
N-phenylbarbital and phenobarbital use
kernicterus and hyperbilirubinemia
A/se of barbituates
times five million
CNS - drowsy, impaired concentrcation, mental and phys sluggy
paradoxical excitement
hypersensitivity
hang over
increased porphryin synthesis***
increases perception of pain***
dependence
poisoning - resp and CNS depression***
Differentiate between the three non-benzo benoz receptor agonists used for treatment of insomnia
ZOLPIDEM - short t 1/2, used if cxtzd by difficulty in sleep initiation (also ramelteon - 5HT1a agonist)
ZALEPLON - short t1/2 and rapid onset
ESZOPICLONE - longer 1/2; decreases sleep latency and improves sleep maintenance
What is Buspirone and who cares a bout it?
only anxiolytic (not hypnotic, not anticonvulsant or muscle relaxant)
used for ANXIETY
takes 2-3 weeks to work
5HT1 a receptor agonist
works like antidepressants
What is Ramelteon and who cares about it?
MT1 and MT2 melatonin receptor agonist
used @ insomnia with difficulty with sleep onset just like zolpidem (not zoleplon be careful zolpIdem with an i for insomnia)
Hydroxyzine as a sed/hyp
antihistamine with antiemetic activity
used for SYMPTOMATIC RELIEF OF ANXIERTY (kind of like clonidine)
Propanolol as a sed/hyp
Propanolol for Performance anxiety
Clonidine as a sed/hyp
modifiers autonomic expression of anxiety (kind of liek hydroxyzine)
Diphenhydramine and doxylamine
mild types of situational insomnia
