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93 Cards in this Set

  • Front
  • Back
What are four characteristics of etomidate?
1. Hypnosis
2. No analgesic properties
3. CV stability
4. Carboxylated imidazole derivative
What are three side effects of etomidate?
1. pain on injection
2. myoclonus
3. adrenal cortical suppression
Which isomer has hypnotic properties?
+
How is etomidate metabolized?
in the liver by hepatic microsomal enzymes and plasma esterases
What is etomidates primary mode of metabolism?
ester hydrolysis
What accounts for the extremely short duration of action?
The rapid distribution half-life
Is etomidate lipid soluble? Characteristics of Vd.
Yes, has a volume of distribution several times greater than its body weight
The total body clearance of etomidate is rapid, how many times greater than thiopental?
5x
WHat is the hepatic extraction ratio of etomidate?
67%
Awakening occurs how many minutes after initial bolus administration?
7-14 min
What % protein bound is etomidate?
76%
What receptor does etomidate work at?
GABA a
Does etomidate cause histamine release?
yes
What is the induction dose of etomidate?
0.2-0.4 mg/kg
What effects does etomidate have on the CNS?
decrease CRMO2, CBF, ICP
Although ICP is reduced what is maintained?
CPP
What may myoclonus may be caused by?
uneven drug distribution into the brain stem or deep cerebral structures and not to CNS stimulation
Myoclonus is decreased with pretreatment of what two drugs?
fentanyl and diazepam
Does etomidate decrease IOP?
yes
Why is etomidate not used with SSEPs?
increases wave amplitude
Although, etomidate has no effect on CV, when has a decrease in BP been caused by?
aortic and mitral valve disease
What is the order of cardiorespiratory depression?
Propofol>thiopental>etomidate
What are the respiratory effects of etomidate?
reduction in minute ventilation while respiratory rate is increased
What may be blunted by etomidate?
response to CO2, may cause brief periods of apnea followed by a period of hyperventilation
Etomidate causes what else?
Adrenocortical suppression
How long does the adrenalcortical suppression last?
4 days
Does etomidate cause pain on injection?
yes
With etomidate what is common on onset?
myoclonia
Does etomidate increase N/V?
yes
3 features of ketamine
1. pKa of 7.5
2. partially water soluble
3. slightly acidic
Chemical structure of ketamine
Optically active drug with chiral center. It exists as two optical isomers
Which isomer has less side effects?
S(+) isomer
What is the primary site of analgesic action of ketamine?
thalamoneocortical system
What is the mechanism of action of ketamine?
antagonism at N-methyl-D-aspartate amino acid (NMDA) receptors in the brain
Characteristics of NMDA receptor
ligand-gated ion channel where anions Ca+2 and Na+ are voltage dependent
What is the most important excitatory NT in the CNS?
L-glutamate
What does L-glutamate do at the NMDA receptor?
it causes opening of the channel causing rapid influx of NA+, Ca2+ and K+ cause depolarization of normally negative postsynaptic membrane that initiates action potential
With ketamine the cortical area are depressed what is still stimulated?
limbic system (causes excitatory behavior)
Ketamine also induces electrophysiologic changes that reduce _________ turnover
acetylcholine
What drug can reverse ketamine sedative effects but not analgesic?
Physostigmine
Ketamine may act as an agonist at which receptors?
opiate
What biotransform ketamine?
Hepatic microsomal enzymes
Primary pathway for ketamine metabolism by P-450 is?
demethylation to form metabolite I, norketamine
Pharmacological activity of the metabolite norketamine is approx?
20-30%
With IV ketamine peak plasma concentrations are reached within?
5 min of IV injection
Termination of ketamine is ____ min.
10-15
Which drug does not have cumulative effects?
etomidate
Hepatic extraction of ketamine is ____. Ketamine is dependent on what for its extraction?
high (therefore ketamine extraction is dependent on hepatic blood flow)
Ketamine IM reaches peak plasma concentrations at ?
22min
What is the IM dose of ketamine?
4-6mg/kg to 5-10mg/kg
What is the onset of ketamine IM?
2-3 minutes
What analgesic dose is required for ketamine?
0.44 mg/kg
Does ketamine cross the placenta?
yes, highly lipid soluble
What dose of ketamine does not cause CNS depression in the newborn?
0.2 to 1mg/kg
Ketamine causes?
dissociative anesthesia
CNS effects of ketamine?
Increase CRMO2, CBF, CSP
What can attenutate the CNS effects of ketamine?
hyperventilation
What EEG waves are seen?
alpha waves transition to theta waves
What reduce the occurrence of emergence delerium associated with ketamine?
benzo's
What are the CV effects of ketamine?
-↑BP, HR, CO, CVP
--↑PVR(42%), PAP(47%), right ventricular stroke work.
Ketamine activates?
the SNS, results in endogenous catecholamine release
What may blunt cardiac stimulation?
inhalational anesthetics and benzos
Respiratory effects from ketamine
Respiratory depression which is reflected in decrease in tidal volume over respiratory rate. Begins 2-3 minutes after parental administration
What positive effect does ketamine produce related to respiratory system?
bronchodilation
Ketamine is a ________ derivative.
Phencyclidine
Use caution in these patients when using ketamine. 7
HTN, angina, CHF, ↑ICP and IOP, psychiatric disease and airway problems
Ketamine may be used for induction of anesthesia what 5 high risk patients?
-Shock
-Severe dehydration
-Severe anemia
-Bronchospasm
-One-lung ventilation
Onset of ketamine is....
slow
What is the chemical structure of propofol?
2,6-diisopropyl phenol
Propofol is prepared in a milky white emulsion of?
10% soybean oil, 2.25% glycerol, and 1.2% purified egg lecithin
Rapid distribution to the central to the peripheral compartments produces a?
rapid awakening after sedative and anesthetic doses
What characteristic of propofol differentiates from thiopental?
its rapid metabolic clearance, which actually exceeds hepatic blood flow
What disease may prolong effects of propofol?
liver disease
Elderly require what type of doses of propofol?
reduced
Children require what type of doses?
larger
What is the mechanism of action of propofol?
Acts on GABA inhibitory neurotransmitter and GABAa receptor
Does intraarterial injection of propofol cause injury?
no
What are the CNS effects of propofol?
↓CMRO2, CBF, ICP and CPP
-cerebral autoregulation and reactivity change in CO2 are intact
EEG shows?
delta waves, burst suppression with higher doses
Propofol may produce spontaneous excitatory movements secondary to?
selective disinhibition of subcortical areas
Does propofol reduce IOP?
yes
What else has been associated with propofol?
Opisthotonos
CV effects from propofol?
Produces significant cardiac depression
Respiratory effects of propofol?
↓ in TV are more prominent than ↓ in respiratory rate, apnea is common on initial administration of induction doses.
What are contraindication of propofol?
a. Hypersensitivity reactions
b. Caution with elderly, debilitated, cardiac-compromised
c. Generic contains sodium metabisulfite, sulfite sensitivitymore common in asthmatic patients.
What is the induction dose of propofol?
0.5 to 2.5mg/kg
What is the induction dose of propofol for a child?
2.5-3mg/kg
What is the common denominator of propofol infusion syndrome?
impaired systemic microcirculation with tissue hypoperfusion and hypoxia
What occurs in propofol infusion syndrome?
Fatty acid metabolism and mitochondrial activity is impaired which creates an oxygen supply-demand mismatch that results in cardiac and peripheral muscle necrosis
What are the symptoms of propofol infusion syndrome? 7
metabolic acidosis, refractory cardiac failure, persistent bradycardia refractory to treatment, fever, lipemia, rhabdomyolysis and possible renal failure
Reformulation of propofol that retards bacterial growth?
EDTA
Is propofol a bronchodilator?
no
Does propofol have antiemetic properties?
yes