Benzodiazepines (2) Exam 1 Flashcards
Differentiate sedatives and hypnotics.
- Sedatives: induce calm/sleep
- Hypnotics: induce hypnosis/sleep
When is anesthesia awareness most common?
- During sedation cases and during emergence.
- 1:1000 (or 1:10,000 per some studies)
What is the mechanism for less EEG activity seen during anesthesia/sedation?
Less cerebral blood flow (CBF) and cerebral metabolic requirement of oxygen (CMRO₂) = less metabolism = less EEG activity.
What was the first compressed EEG?
- Bispectral analysis
- 1500 subjects w/ 5000 hours of EEG signaling
What drugs were utilized in the bispectral analysis study?
- Isoflurane/ O₂
- Propofol/nitrous
- Propofol/alfentanil
Which drug exhibited a strong correlation between BIS change and patient movement?
Which drug had less correlation?
- Hypnotic drugs strong correlation
- Narcotics less correlation
In the BIS study, what reading indicated that a patient was for sure unconscious?
<58
In the BIS study, a reading of <65 indicated a ___% of return to consciousness within the minute.
5%
What is a normal BIS range?
40-60
What are the four parameters (other than the BIS itself) noted on a BIS monitor?
- SQI (signal quality index)
- EMG (electromyogram)
- EEG (electroencephalogram)
- SR (suppression ratio)
What is the SR noted on a BIS monitor?
Suppression Ratio (percentage of time that the EEG is flat)
Name drugs that could suppress EEG activity.
Hypnotics, volatiles, NMBDs, Opioids
β-blockers
Name drugs that could enhance EEG activity.
Ketamine, epinephrine
What are the five main functions of a benzodiazepine?
- Anxiolysis
- Sedation
- Anterograde amnesia
- Anticonvulsant
- Spinal-cord mediated muscle relaxation
What is the only “thing” that can cause retrograde amnesia?
ECT (electroconvulsive therapy)
Why are written instructions given to a patient after waking up from benzodiazepine sedation?
Anterograde amnesia effects last longer than sedative effects.
Can benzodiazepines be substituted for NMBs due to their spinal-cord mediated skeletal muscle relaxation?
No; not adequate for true paralysis
__________ drugs can induce CYP450’s.
Barbiturates
What is the mechanism of action of benzodiazepines?
Enhancement of GABA affinity to GABA-A receptor. Allows for greater Cl⁻ influx and thus hyperpolarization.
Which GABA site do benzodiazepines bind to?
Trick question. Benzo’s do not bind directly to GABA sites, they bind to BZD sites which activate GABA sites.
How many subunits are present in a GABA receptor?
Five
In-between the α1 & β2 subunits
What subunits do Benzodiazepines bind to on the GABA receptor?
In-between α1 & γ2
GABA receptors with α1 subunits exhibit what properties when bound?
- Sedation, amnesia, & anticonvulsion
- Most abundant: cerebral cortex, cerebellar cortex, & thalamus.
GABA receptors with α2 subunits exhibit what properties when bound?
Anxiolysis & skeletal muscle relaxation
Less abundant: hippocampus & amygdala
What other drugs bind to GABA receptors besides benzodiazepines? (4)
Barbiturates, Etomidate, Propofol, & EtOH
Risk of overdose & cross-tolerance
Benzodiazepines are highly _____ soluble and highly _______ bound.
Lipid; protein
What factors cause differing effects amongst benzodiazepines?
- Potency
- Lipid solubility
- Redistribution (to peripheral tissues)
- Pharmacokinetics
List EEG waves from greatest activity to least activity.
Gamma → Βeta → Αlpha → Theta → Delta
What general effect(s) do benzodiazepines have on EEG activity?
Decreased αlpha activity
What platelet effects do benzodiazepines have?
Inhibitory towards platelet aggregation (very slight, only in vitro studies)