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13 Cards in this Set
- Front
- Back
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Does propofol have analgesic activity?
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No
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How does propofol work?
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Propofol inhibits the NMDA subtype glutamate receptors by chanel gating modulation, and has agonistic activity at the GABA receptor. Propofol enhances the amplitude of currents evoked by subthreshold concentrations of GABA. Propofol activates chloride chanels in the B1 subunit of GABA.
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How does propofol compare to benzos in desentitization and deactivation.
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Both drugs slow the rate of deactivation, but only propofol decreases the rate and extent of receptor desentitization in the presence of saturating concentrations of GABA.
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What other uses does propofol have? Why?
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refractory migraine, status epilepticus, and delerium tremens d/t enhanced inhibitory synaptic transmission
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What occurs in propofol w/ hypocarbia?
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It increases cerebrovascular resistance and decreases cerebral blood flow, occular pressure, O2 consumption and ICP. (likely d/t decreased SVR).
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What kind of properties does propofol have that make it ideal for surgery?
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It has antiemetic properties (reduced the amount of seratonin, 5HT in area postrema, possible mediated by GABA), and reduces synaptic transmission in the olfactory cortex. However, propofol does not affect gastric emptying time or Dopamine D2 receptors.
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How fast is the onset of propofol?
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Usually w/in 40 secons.
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Does propofol cross the placenta? Breast milk?
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Yes. Yes.
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How much is propofol protein bound?
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95-99%
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Where is propofol metabolized?
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In the liver, through glucuronide conjugation. However, clearance exceeds hepatic blood flow, making extrahepatic metabolism likely.
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What is the elimination half-life of propofol?
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3-12 hours (d/t slow release from fat stores)
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How fast does recovery from propofol take?
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8-19 minutes after 2 hours of anesthesia. Usually less than 35 minutes for awakening after sedation if less than 3 days. > 3 days, can be > 3.5 hours. Emergence times increased w/ obese patients.
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Describe propofol use in special populations
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Total body clearance and volume of distribution are less in the elderly, similar to adults in children. Clearance/metabolism not affected by chronic hepatic or renal disease.
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