Psych: Sedatives/Hypnotics Flashcards
Definition: producing relaxation, calmness, and decreased motor activity w/o LOC?
Sedation
Definition: inducing drowsiness and a depressed state of consciousness resembling natural sleep, along with impaired sensory responsiveness from which a person is easily aroused
Hypnosis
What schedule of drugs are barbituates and benzos?
Barbs: class II
Benzos: class IV
MOA of alpazolam, clonazepam, diazepam?
GABAa agonists
-increase frequency of Cl channel opening
MOA of lorazepam, midazolam, and temazepam?
GABAa agonists
-increase frequency of Cl channel opening
MOA of eszopiclone and zolpidem
Binds selectively to BZ1 receptors, located on GABA-a receptors
MOA of flumazenil
Antagonist at benzo binding site of GABAa
-reverse adverse effects and OD of benzos
MOA of ramelteon
Melatonin agonist at MT1 and MT2 receptors
What are the high potency benzodiazepines?
Clonazepam, alprazolam, lorazepam
MOA of suvorexant
Blocks binding of orexins
-orexins produce wakefulness, so if they are blocked=ZZZ (promotes sleep)
MOA of doxepin
H1 antagonist and inhibits reuptake of NE and 5HT
Who is most susceptible to the side effects of benzodiazepines and who is resistant?
Elderly are most, alcoholics and barbiturate drug users are resistant
How do benzos change sleep patterns?
More stage II, less stage I, III, and REM
What side effect is more common with the short acting benzos?
Amnesia
How is diazepam metabolised?
CYP3A4 is major contrbuter
What is the black box warning for taking benzos with opiates?
Major sedation, respiratory depression, coma and death
Clinical use of benzos?
Anxiolytic and sedation
Do eszopiclone and zolpidem reduce anxiety?
No
ROI of eszopiclone and zolpidem
IR, sublingual tablets, and oral spray
Clinical use of eszopiclone and zolpidem
Insomnia patients with difficulty with onset of sleep
-eszopiclone can be used for maintenance too
Black box warning of eszopiclone and zolpidem
Complex sleep disorders
-sleep walking, sleep driving, and other activities
What is the black box warning of flumazenil?
Seizures, espcially in those with TCA use
-contraversal use due to the fact that benzos are relatively safe
What is the black box warning of flumazenil?
Seizures, espcially in those with TCA use
-contraversal use due to the fact that benzos are relatively safe
Which group of sedatives are classic inducers of CYP3A4?
Barbituates
-monitor doses of other meds
Clinical use of the barbituates?
Sedation and anxiolytic
MOA of buspirone?
Partial agonist at 5HT
-mostly unsure of mechanism
Clinical use of buspirone?
Nonbenzodiazepine anxiolytic
Does buspirone cause sedation? What about when combined with alcohol?
Nope
-nor does it make sedation worse with alcohol
Clinical use of doxepin?
-causes sedation and anxiolytic
What should you do when taking patients off benzos?
Taper
-25-50% every 1 to 2 weeks over 6-10 weeks
