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