Propofol Flashcards
Please note that the drug card information is for Educational Use ONLY, and the source is from Carrie Bowman's glossary of drug cards permitted by use of Georgetown NAP students. No permission is given to use these cards for anything other than as a study resource for our program.
What are the trade names for Propofol?
Ampofol or Diprivan
What is the formal drug classification of Propofol?
Substituted isopropylphenol (2,6-diisopropylphenol)
General Anesthetic
What are the clinical uses for Propofol? (8)
- Induction and maintenance of GA
- IV sedation
- Same day surgery due to a fast onset and fast recovery and absence of “hangover effect”
- Anticonvulsant activity
- Useful for decreasing ICP and IOP
- Antiemetic
- Antipruritic
- Attenuation of bronchoconstriction
What is the MOA of Propofol?
Exerts sedative-hypnotic effects by discouraging dissociating of the Neurotransmitter GABA from the GABAa receptor, thus increasing transmembrane chloride conductance resulting in hyperpolarization of the POSTsynaptic cell membrane and functional inhibition of the postsynaptic neuron
- Effect is modulation of GABA at the GABAa receptor–specificallythe Beta subunits 1-3
- Dr. E says also NMDA inhibition
What is a secondary MOA of Propofol?
a secondary MOA of propofol is via inhibition of glutamate action at NMDA receptors
What receptor does propfol exert its effects? pre or post synaptically?
GABAa; postsynaptically! functional inhibition of the postsynaptic neuron
What is the onset of action of Propofol?
Fast onset within 20 - 30 seconds
What is the Elimination 1/2 life of Propofol?
4 - 7 hours or 0.5 - 1.5 hours(Dr. E says 0.5-1.5hrs)? depending on the text……
context sensitive 1/2 time for infusions up to 8 hrs is <40 minutes
How is propofol metabolized?
- Rapidly metabolized in the liver by conjugation to glucuronide and sulfate by CPY450 to produce water-soluble compounds which are excreted by the kidneys
- because clearance exceeds hepatic blood flow (1.5-2.2 L/min), extrahepatic metabolism or extra renal elimination is suggested
- lungs play a role in extrahepatic metabolism and are responsible for uptake and first pass elimination
How is Propofol redistributed?
- Initial distribution 2-8 minutes
- whole blood propofol levels decrease rapidly after a single bolus injection
What is the elimination route of propofol?
Less than 0.3% of a dose is excreted unchanged in the urine
What is the volume of distribution of Propofol?
3.5 - 4.5 L/kg
What are the side effects of Propofol? (4)
- Pain on injection, MYOCLONUS, Apnea, Hypotension, Propofol infusion syndrome
- Severe Bradycardia and asystole, risk of infection, Hypertriglyceridemia with prolonged administration, PE, Allergic rxns, Seizures, lactic acidosis, proconvulsant activity, antioxidant properties, abuse potential: amorous behavior, intense dreams, and hallucinations during recovery
- CV and Resp depression
- Dose-dependent reduction of CBF and CMRO2, capable of producing an isoelectric EEG and decreases CPP dependent on decreases in BP
What are the symptoms of propofol infusion syndrome?
- Poor oxygen delivery
- Sepsis
- Serious cerebral injury
- Lipemia
What are contraindications to the use of Propofol?
- Patients that have multiple drug allergies should use with caution; allergies to EGG or SOYBEAN oil
- use extreme caution in patients with poor myocardial function and in patients with predicted difficult airways before artificial a/w established