Exam 2; Anti-Anxiety and Hypnotics Flashcards
What are the definitions of anxiolytics, sedatives, and hypnotics
anxiolytics; reduce anxiety
sedatives; induce calmness without drowsiness
hypnotics; induce normal sleep
True or False
anxiolytics, sedatives, and hypnotics are all derived to treat diseases
False; they only treat symptoms
Most of these drugs target what
GABA; the major inhibitory neuron
**activating the receptor
These are the major anti-anxiety drugs; the “‘-pam’s” and “-lam’s” long duration, low dose
benzodiazepines
+ chlorodiazepoxide
The beginning letters; D, A, C, C, O, L
These are used primarily for the treatment of insomnia; shorter duration, higher dose
flurazepam temazapam estrazolam Quazepam triazolam F, T, E, Q, T
This is used in general anesthesia; given IV
midazolam
What is the effect of a low dose of benzodiazepines
decrease aggressive behavior and anxiety
What is the effect of a high dose of benzodiazepines
sedation and hypnosis
anesthesia
amnesia
What kind of mechanisms cause muscle relaxation, involving the benzodiazepines
central and spinal cord mechanisms; anti-spastics
benzodiazepines are also used for what
anti-convulsant effects
Where are the active benzodiazepine receptor sites on the brain
close to or on the GABA receptor of neurons
not where GABA binds directly
What is the activity of benzodiazepine on its receptors
it enhances the effect of GABA on its receptor; makes the receptor more sensitive to GABA
What are the two metabolitic paths of benzodiazepines
absorbed from the GI if given orally
metabolized in the liver; not induce P450
What causes tolerance of benzodiazepines
down regulation of the benzodiazepine binding sites
What could the result be from withdrawal of benzodiazepines
seizures
hyperactivity of the brain due to loss of inhibitory action
What is habituation
not the same as addiction
become psychological dependent; you THINK you need it
What is the therapeutic index of benzodiazepines
very high; it is virtually impossible to kill yourself with solely these; low toxicity
What are five side effects of benzodiazepines
drowsiness ataxia impaired judgment confusion; especially in the elderly decreased ability to learn new material
benzodiazepines can interact with this CNS depressant
ethanol
What are two visual disturbances of benzodiazepines
diplopia
nystagmus
This is a benzodiazepine receptor blocker; given IV due to 1st pass metabolism
flumazenil
These act by binding to α subunits of benzodiazepine receptor
non-benzodiazepine hypnotics
What are three non-benzodiazepine hypnotics
zolpidem
zaleplon
eszopiclone
the “z” drugs
What are four behavioral changes that can occur with non-benzodiazepine hypnotics
decreased inhibitions
bizarre behaviors
sleep driving
hallucinations
This is an α2 agonist non-benzodiazepine hypnotic which induces sleep, causing sedation without respirator depression
Dexmedetomidine
What are two symptoms of dexmedetomidine
decreased blood pressure
bradycardia
This is an slow onset anti-anxiety non-benzodiazepine hypnotic that is a partial serotonin agonist with no sedative or hypnotic effects
buspirone
These barbiturates have a 3-4 hour duration
pentobarbital
secobarbital
These barbiturates have a 6-8 hour duration
butaberbital
amobarbital
These barbiturates have a 10-16 hour duration
phenobarbital
what is the mechanism of action behind barbiturates
enhance the action of GABA; much more efficient that benzodiazepines
barbiturates act on which who places
reticular activating system
acts on sensory cortex leading to unconsciousness
are barbiturates more or less potent that benzodiazepines
less potent; use a higher dose
True or False
barbiturates are not analgesics
True
barbiturates act on this center; which if there is an OD of barbiturates it will lead to death due to respiratory depression
medullary respiratory center
What other use besides hypnosis are barbiturates used for
epilepsy
What are two contraindications of barbiturates
decreases respiration
TI = 10; used in suicides
What can barbiturates interact with regarding other drugs
ethanol
synergistic CNS depression
What can occur when someone who is dependent on barbiturates, stops taking them
they suppress REM sleep, so when you stop, you have a large increase in REM leading to nightmares
These are melatonin receptor agonists; no effect of GABAergic pathways
rameltheon
tasimeltheon
rameltheon and tasimeltheon help maintain what
normal circadian sleep rhythms; reduces the time to fall asleep
What are two side effects of rameltheon and tasimeltheon
somnolence (sleepiness)
fatigue
What are two long term symptoms of rameltheon and tasimeltheon
decreased testosterone synthesis
synergistic with ethanol
What OTC can interact with rameltheon and tasimeltheon
anti-histamines; drowsiness
