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propofol (Diprivan)

Tradename: Diprivan. Indications: 1) induction or maintenance of anesthesia 2) short-term sedation (24 hours or less) for intubated intensive care patients Contraindications: 1) when general anesthesia is contraindicated 2) NOT for obstetrical anesthesia 3) NOT for neurosurgical anesthesia Dosage: 1) 40 mg IV every 10 sec until induction 2) 2-2.5 mg/kg IV drip 3) initial bolus dose of 0.5-1.0 mg/kg for adults or 1.5-2.0 mg/kg for children - titrate every 1-3 minutes to effect with boluses of 0.25-0.5mg/kg (adults) or 0.5-1.0 mg/kg (children) - infusions may avoid the "peak & trough" effect of boluses - use 100-150 ug/kg/min (adults) & up to 250 ug/kg/min (children) [7] * one provider should be dedicated to administering propofol, monitoring vital signs (cardiac monitoring, pulse oximetry, capnography, & blood pressure & respiratory rate every 5 minutes), & performing any needed resuscitation [7] * optimize volume status prior to propofol administration to avoid hypotension * propofol provides sedation & amnesia without analgesia; thus coadminister ketamine, fentanyl, or a local anesthetic [7] Injection: 10 mg/mL (20 mL) Pharmacokinetics: 1) rapid onset of action (within 30 seconds of IV bolus) 2) 3 compartment model describes disposition & elimination a) plasma b) rapidly equilibrating compartment c) slowly equilibrating compartment 3) equilibration dependent upon rate & duration of infusion - long infusions result in tissue accumulation & increased time awakening when the drug is stopped 4) metabolized by liver; conjugation to inactive metabolites 5) eliminated by the kidney 6) duration of action 3-10 minutes (variable) 7) terminal 1/2life for a 10 day infusion is 1-3 days Adverse effects: 1) common (> 10%) - nausea 2) less common (1-10%) - fever, hypotension, bradycardia, apnea, vomiting, abdominal cramping, cough, flushing 3) uncommon (< 1%) - chest pain, dry mouth, somnolence, tachycardia, syncope, agitation, bronchospasm, diarrhea, ear pain, pruritus, dyspnea, tremor, confusion, twitching 4) propofol-associated infusion syndrome (rare) - lactic acidosis - rhabdomyolysis - hypertriglyceridemia - J point elevation on electrocardiogram - occurs at doses >4 mg/kg/hour for > 48 hours 5) other [2] - decreased systemic vascular resistance - anaphylactic reactions - withdrawal symptoms with longer infusions - contamination & risk of secondary infection* - immune suppression - tolerance - delayed seizures - green urine - arrhythmias 6) patients < 6 months of age & > 75 years of age have higher rates of complications [7] * Tubing must be changed every 12 hours to decrease risk of bacterial contamination Drug interactions: 1) CNS depressants 2) cardio-respiratory depressants Laboratory: - propofol in serum/plasma - propofol glucuronide in urine - urine appearance: may be green [6] Mechanism of action: 1) IV sedative hypnotic 2) sedative general anesthetic 3) diisopropylphenol in a lipid emulsion 4) NOT an analgesic 5) 1.1 kcal of fat/mL (1 g of fat/10 mL)

Related

fospropofol (Lusedra, Aquavan)

General

general anesthetic injectable

Properties

MISC-INFO: elimination route LIVER pregnancy-category B safety in lactation -

Database Correlations

PUBCHEM cid=4943

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Medical Knowledge Self Assessment Program (MKSAP) 16, American College of Physicians, Philadelphia 2012
  5. Roberts RJ, Barletta JF, Fong JJ et al Incidence of propofol-related infusion syndrome in critically ill adults: a prospective, multicenter study. Crit Care. 2009;13(5):R169. doi: 10.1186 PMID: 19874582
  6. Atalla AS, Palka J 12 Causes of Discolored Urine. Medscape. Nov 15, 2017 https://reference.medscape.com/slideshow/discolored-urine-6008332
  7. Miller KA, Andolfatto G, Miner JR et al. Clinical practice guideline for emergency department procedural sedation with propofol: 2018 update. Ann Emerg Med 2019. Feb 4 PMID: 30732981 https://www.annemergmed.com/article/S0196-0644(18)31576-2/fulltext