SM_90b: Sedatives and Hypnotics Flashcards
Sedative reduces ___ and produces a ___ effect
Sedative reduces excitatory response to external stimuli and produces a calming effect
Hypnotic causes ____ and ____
Hypnotic causes drowsiness and sleep
Sedative hypnotics cause ____ in lower doses and ____ in higher doses
Sedative hypnotics cause sedation in lower doses and sleep in higher doses
Most sedative-hypnotics act on the ____ receptor
Most sedative-hypnotics act on the GABAA receptor
- Ligand gated Cl- channel
- Bind between alpha and gamma subunits
Benzodiazepines bind between the ____ and ____ subunits of the GABAA receptor at the ____ site
Benzodiazepines bind between the alpha and gamma subunits of the GABAA receptor at the BDZ site
Benzodiazepines ____ GABA channel openings and ____
Benzodiazepines increase the frequency of GABAA channel openings and require GABA to open channels before acting
General anesthetics (propofol, etomidate) act by ____
General anesthetics (propofol, etomidate) act by increasing the duration of GABAA channel openings
- Act on beta subunit
- Higher doses can open channel without GABA
Barbiturates act by ____
Barbiturates act by increasing the duration of GABAA channel opening
- Act on alpha subunit
- Higher doses can open channel without GABA
Picrotoxin is a ____
Picrotoxin is a non-competitive GABAA antagonist that binds to the channel part of all subunits
Convulsant
Bicuculline is a ___
Bicuculline is a competitive GABAA antagonist that binds to GABA binding site
Convulsant
Penicillin is an ____
Penicillin is an uncompetitive GABAA antagonist
Convulsant
(blocks open channels, so needs agonist to work)
Benzodiazepines max out at causing ____ due to a ____
Benzodiazepines max out at causing anesthesia due to a ceiling effect
-azepams and -azolams are ____
-azepams and -azolams are benzodiazepines
____ is used for immediate relief of anxiety or aggression
Diazepam is used for immediate relief of anxiety or aggression
____ or ____ are used for immediate relief of panic
Alprazolam or clonazepam are used for immediate relief of panic
(severe anxiety with strong autonomic overactivity)
____ is used to treat REM sleep behavior disorder in which muscle atonia is absent
Clonazepam is used to treat REM sleep behavior disorder in which muscle atonia is absent
____ or ____ are used for sedation/amnesia during medical procedures and in balanced anesthesia
Midazolam or diazepam are used for sedation/amnesia during medical procedures and in balanced anesthesia
____, ____, or ____ are used as anticonvulsants
Diazepam, lorazepam, and clonazepam are used as anticonvulsants
____ are ____ used for muscle spasms
Diazepam and clonazepam are used for muscle spasms
____ are used to treat ethanol withdrawal
Benzodiazepines are used to treat ethanol withdrawal
____ can create anterograde amnesia
All benzodiazepines can create anterograde amnesia
____ may cause breakthrough panic attacks, while ____ may prevent breakthrough panic attacks
Short-acting agents such as alprazolam may cause breakthrough panic attacks, while long-acting agents such as clonazepam may prevent breakthrough panic attacks
After several months, stopping benzodiazepines will cause ___
After several months, stopping benzodiazepines will cause withdrawal symptoms
- Low to moderate dose: anxiety, agitation, muscle cramps (myoclonic jerks), sleep disturbances, dizziness, increased sensitivity to light and sound, paresthesias and strange sensatiosn
- High dose: seizure and delirium
Benzodiazepines are well-absorbed ___
Benzodiazepines are well-absorbed orally
(peak plasma concentrations generally achieved in 1 hour)
Majority of benzodiazepines are metabolized by ____ in Phase I and all are ____ in Phase II
Majority of benzodiazepines are metabolized by CYP3A4 in Phase I and all are glurcuronidated in Phase II
(excreted in urine)
____, ____, and ____ are benzodiazepines without active metabolites and do NOT need to be metabolized by CYPs
Lorazepam, oxazepam, and temazepam (LOTs) are benzodiazepines without active metabolites and do NOT need to be metabolized by CYPs