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Propofol

  • Medical and Pharmacy Editor: John P. Cunha, DO, FACOEP
    John P. Cunha, DO, FACOEP

    John P. Cunha, DO, FACOEP

    John P. Cunha, DO, is a U.S. board-certified Emergency Medicine Physician. Dr. Cunha's educational background includes a BS in Biology from Rutgers, the State University of New Jersey, and a DO from the Kansas City University of Medicine and Biosciences in Kansas City, MO. He completed residency training in Emergency Medicine at Newark Beth Israel Medical Center in Newark, New Jersey.

Brand Name: Diprivan

Generic Name: propofol

Drug Class: General Anesthetics, Systemic

What Is Propofol and How Does It Work?

Propofol is an intravenous (IV) sedative-hypnotic agent that can be used for initiation and maintenance of Monitored Anesthesia Care (MAC) sedation, combined sedation and regional anesthesia, induction of general anesthesia, maintenance of general anesthesia, and intensive care unit (ICU) sedation of intubated, mechanically ventilated patients.

Propofol is available under the following different brand names: Diprivan.

Dosages of Propofol:

Adult and Pediatric Dosage Forms and Strengths

Injectable solution

  • 10 mg/mL

Dosage Considerations – Should be Given as Follows:

There are reports of the abuse of propofol for recreational and other improper purposes, which have resulted in fatalities and other injuries. Instances of self-administration of propofol by health care professionals have also been reported, which have resulted in fatalities and other injuries. Inventories of propofol should be stored and managed to prevent the risk of diversion, including restriction of access and accounting procedures as appropriate to the clinical setting.

Anesthesia

Induction, Adult

  • Adults under 55 years ASA I/II: 40 mg intravenously (IV) every 10 seconds until onset (2-2.5 mg/kg IV when not pre-medicated with oral benzodiazepines or intramuscular opioids)
  • Adults over 55 years or debilitated or ASA III/IV: 20 mg IV every 10 seconds until onset (1-1.5 mg/kg); do not use rapid bolus because as it will increase likelihood of undesirable cardiorespiratory depression, including hypotension, apnea, airway obstruction, and/or oxygen desaturation

Induction, Pediatric

  • Children under 3 years: Not recommended
  • 3-16 years ASA I/II: 2.5-3.5 mg/kg intravenously (IV) over 20-30 sec when not pre-medicated or when lightly pre-medicated with oral benzodiazepines or intramuscular opioids; younger patients may required higher induction doses than older children; lower dosage recommended for children ASA III/IV

Maintenance, Adult

  • Adults under 55 years ASA I/II: 0.1-0.2 mg/kg/minute intravenously (IV); administered in a variable rate infusion with nitrous oxide 60% to 70% and oxygen provides anesthesia for patients undergoing general surgery; maintenance infusion should immediately follow induction dose to provide satisfactory or continuous anesthesia during induction phase
  • Intermittent bolus: Increments of 25-50 mg (2.5-5 mL) may be administered with nitrous oxide in adults undergoing general surgery; administer incremental boluses when changes in vital signs indicate response to surgical stimulation or light anesthesia
  • Adults over 55 years or debilitated or ASA III/IV: 0.05-0.1 mg/kg/minute intravenously (IV)

Maintenance, Pediatric

  • Children 2 months-16 years ASA I/II: 0.125-0.3 mg/kg/minute intravenously (IV); after 30 minutes, if clinical signs of light anesthesia are absent, decrease infusion rate; children 5 years or younger may require larger infusion rates compared to older children

MAC Sedation

Initiation

  • 0.1-0.15 mg/kg/minute intravenously (IV) for 3-5 minutes; titrate to desired clinical effect; monitor respiratory function; administered as slow infusion or slow injection while monitoring cardiorespiratory function
  • Slow injection: 0.5 mg/kg administered over 3-5 minutes; titrate to clinical response
  • Elderly: Do not use rapid bolus dose administration; administer over 3-5 minutes; reduce dose to approximately 80% of usual adult dose according to their condition, response, and changes in vital signs

Maintenance

  • Variable rate of infusion method preferable over intermittent bolus dose method
  • Variable rate infusion method: 0.025-0.075 mg/kg/minute intravenously (IV) during first 10-15 min sedation maintenance; subsequently decrease infusion rates over time to 25 to 50 mcg/kg/minute and adjust clinical response; allow approximately 2 min for onset of peak drug effect to titrate to clinical response; titrate downward in absence of clinical signs of light sedation until mild response to stimulation obtained to avoid sedative administration at rates higher than clinically necessary
  • Intermittent bolus method: Administer 10-20 mg increments and titrate to desired level of sedation
  • Elderly: 0.02-0.06 mg/kg/minute IV; do not use rapid bolus dose administration; reduce rate of administration to 80% of usual adult dose according to their condition, response, and changes in vital signs

Postoperative Nausea/Vomiting

  • 20 mg intravenously (IV); may repeat

ICU Patient

  • Initiation: 0.005 mg/kg/minute intravenously (IV) for at least 5 minutes; titrate to desired clinical effect; increase by 5-10 mcg/kg/minute over 5-10 minute intervals until desired sedation level achieved; allow a minimum of 5 minutes between adjustments for onset of peak effect
  • For medical ICU patients or patients who recovered from effect of general anesthesia or deep sedation, rate of administration of 50 mcg/kg/min or more may be required to achieve adequate sedation
  • Maintenance: 0.005-0.05 mg/kg/minute intravenous (IV) individualized and titrated to clinical response; (0.005 mg/kg/minute increment increase every 5 minutes)
  • Discontinuation: Avoid discontinuation prior to weaning or for daily evaluation of sedation levels; may result in rapid awakening with associated anxiety, agitation, and resistance to mechanical ventilation

SLIDESHOW

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What Are Side Effects Associated with Using Propofol?

Common side effects of Propofol include:

Less common side effects of propofol include:

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

What Other Drugs Interact with Propofol?

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe Interactions of propofol include:

  • None

Serious Interactions of propofol include:

  • ceritinib
  • doxapram
  • epinephrine
  • epinephrine racemic
  • fentanyl
  • fentanyl intranasal
  • fentanyl iontophoretic transdermal system
  • fentanyl transdermal
  • fentanyl transmucosal
  • isocarboxazid
  • norepinephrine
  • phenelzine
  • phenylephrine
  • phenylephrine PO
  • pirfenidone
  • rasagiline
  • selegiline
  • sodium oxybate
  • tranylcypromine

Propofol has moderate interactions with at least 178 different drugs.

Mild Interactions of propofol include:

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

QUESTION

Medically speaking, the term "myalgia" refers to what type of pain? See Answer

What Are Warnings and Precautions for Propofol?

Warnings

This medication contains propofol. Do not take Diprivan if you are allergic to propofol or any ingredients contained in this drug

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

  • Documented hypersensitivity, egg allergy, soybean/soy allergy

Effects of Drug Abuse

  • There are reports of the abuse of propofol for recreational and other improper purposes, which have resulted in fatalities and other injuries. Instances of self-administration of propofol by health care professionals have also been reported, which have resulted in fatalities and other injuries. Inventories of propofol should be stored and managed to prevent the risk of diversion, including restriction of access and accounting procedures as appropriate to the clinical setting
  • Anxiety, agitation, and resistance to mechanical ventilation may occur with abrupt withdrawal

Short-Term Effects

  • See "What Are Side Effects Associated with Using Propofol?"

Long-Term Effects

  • Propofol infusion syndrome may occur; this is characterized by severe metabolic acidosis, hyperkalemia, lipemia, rhabdomyolysis, hepatomegaly, and cardiac and renal failure (especially with prolonged, high-dose infusions greater than 5 mg/kg/hours for greater than 48 hours)
  • Prolonged or repeated exposure may result in negative effects on fetal or young children's brain development
  • See "What Are Side Effects Associated with Using Propofol?"

Cautions

  • Use caution in asthma (bronchial), bleeding disorders, cardiac disease, hepatic impairment, hypertension, and renal impairment
  • May not be sufficiently activated in patients with hepatic dysfunction; use with caution
  • Long-term administration of nonsteroidal anti-inflammatory drugs (NSAIDs) may result in renal papillary necrosis and other renal injury; patients at greatest risk include elderly individuals, those with impaired renal function, hypovolemia, heart failure, liver dysfunction, or salt depletion, and those taking diuretics, angiotensin-converting enzyme inhibitors, or angiotensin-receptor blockers
  • Risk of serious gastrointestinal (GI) toxicity, including bleeding, ulcers, and perforation
  • May cause drowsiness, dizziness, blurred vision, and other neurologic effects
  • May decrease platelet adhesion and aggregation, prolonging bleeding time; monitor closely patients with history of coagulation disorders
  • May increase risk of hyperkalemia
  • May cause photosensitivity reactions
  • Severe skin reactions may occur; discontinue use at first sign of rash
  • Heart Failure (HF) risk
    • Nonsteroidal anti-inflammatory drugs (NSAIDs) have the potential to trigger heart failure by prostaglandin inhibition that leads to sodium and water retention, increased systemic vascular resistance, and blunted response to diuretics
    • NSAIDs should be avoided or withdrawn whenever possible
    • AHA/ACC Heart Failure Guidelines; Circulation. 2016; 134

Pregnancy and Lactation

  • Use propofol with caution during pregnancy if benefits outweigh risks
  • Animal studies show risk and human studies are not available or neither animal nor human studies were done
  • There is positive evidence of human fetal risk if propofol is used for prolonged periods or near term (premature closure of ductus arteriosus)
  • Quebec Pregnancy Registry identified 4705 women who had spontaneous abortions by 20 weeks' gestation; each case was matched to 10 control subjects (n=47,050) who had not had spontaneous abortions; exposure to non-aspirin NSAIDs
  • during pregnancy was documented in approximately 7.5% of cases of spontaneous abortions and approximately 2.6% of controls
  • It is unknown whether propofol is excreted in breast milk; its effect on infants is unknown
  • Do not give propofol to nursing mothers


SOURCE:
Medscape. Propofol.
https://reference.medscape.com/drug/diprivan-propofol-343100
DailyMed. Propofol.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6f8bebf9-d87b-469a-911a-21135ba841ae

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