Propofol


Description

Propofol is an intravenous anaesthetic agent used for induction and maintenance of general anaesthesia. IV administration of propfol is used to induce unconsciousness after which anaesthesia may be maintained using a combination of medications. Recov...

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Pharmacology

Indication

Used for induction and/or maintenance of anaesthesia and for management of refractory status epilept... Read more

Pharmacodynamic

Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or seda... Read more

Mechanism of action

The action of propofol involves a positive modulation of the inhibitory function of the neurotransmi... Read more

Absorption

Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to... Read more

Protein binding

95 to 99%, primarily to serum albumin and hemoglobin

Volume of distribution

60 L/kg [healthy adults]

Clearance

23 - 50 mL/kg/min1.6 - 3.4 L/min [70 Kg adults]

Half life

Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t Read more

Route of elimination

It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the ki... Read more

Toxicity

Overdosage may increase pharmacologic and adverse effects or cause death.
IV LD50=53...

IV LD50=53 mg/kg (mice), 42 mg/kg (rats). Oral LD50 (as a solution in soybean oil)=1230 mg/kg (mice), 600 mg/kg (rats)

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Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Hypotension US
  • adult
  • Kind: experimental
    • Percent: 26%
  • Clinical Trial
    Stinging US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Burning US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Pain US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Stinging US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Pain US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Burning US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Movement US
    • pediatric
  • Kind: experimental
    • Percent: 17%
  • Clinical Trial
    Movement US
    • pediatric
  • Kind: experimental
    • Percent: 17%
  • Clinical Trial
    Hypotension US
    • pediatric
  • Kind: experimental
    • Percent: 17%
  • Clinical Trial
    Hypotension US
    • pediatric
  • Kind: experimental
    • Percent: 17%
  • Clinical Trial
    Burning US
    • pediatric
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Pain US
    • pediatric
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Burning US
    • pediatric
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Stinging US
    • pediatric
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Stinging US
    • pediatric
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Pain US
    • pediatric
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Hypotension US
    • adult
  • Kind: experimental
    • Percent: 3-10%
  • Clinical Trial
    Movement US
    • adult
  • Kind: experimental
    • Percent: 3-10%
  • Clinical Trial
    Hypotension US
    • adult
  • Kind: experimental
    • Percent: 3-10%
  • Clinical Trial
    Movement US
    • adult
  • Kind: experimental
    • Percent: 3-10%
  • Clinical Trial
    Hyperlipemia US
    • adult
  • Kind: experimental
    • Percent: 3-10%
  • Clinical Trial
    Respiratory acidosis during weaning US
    • adult
  • Kind: experimental
    • Percent: 3-10%
  • Clinical Trial
    Hypertension US
    • pediatric
  • Kind: experimental
    • Percent: 8%
  • Clinical Trial
    Hypertension US
    • pediatric
  • Kind: experimental
    • Percent: 8%
  • Clinical Trial
    Rash US
    • pediatric
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Rash US
    • pediatric
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Bradycardia US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Bradycardia US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Arrhythmia US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Arrhythmia US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Tachycardia nodal US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Tachycardia nodal US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Hypertension US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Hypertension US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Apnea US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Apnea US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Pruritus US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Pruritus US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Decreased cardiac output US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Bradycardia US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Tachycardia nodal US
    • pediatric
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Pruritus US
    • pediatric
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Tachycardia nodal US
    • pediatric
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Pruritus US
    • pediatric
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Arrhythmia US
    • pediatric
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Arrhythmia US
    • pediatric
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Premature Ventricular Contractions US
    • adult
    • pediatric
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Allergies to eggs, egg products, soybeans, soy products
        • Drugbank Id: DBCOND0108027

    Food Interactions

      Information currently not available.

    Interactions

    Type in a drug name to check for interaction with Propofol

    The serum concentration of (R)-warfarin can be increased when it is combined with Propofol.
    The serum concentration of (S)-Warfarin can be increased when it is combined with Propofol.
    The risk or severity of hypertension can be increased when Propofol is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Propofol is combined with 1-benzylimidazole.
    The risk or severity of hypertension can be increased when Propofol is combined with 2,5-Dimethoxy-4-ethylamphetamine.
    The risk or severity of adverse effects can be increased when Propofol is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Propofol.
    The risk or severity of adverse effects can be increased when Propofol is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Propofol.
    The risk or severity of adverse effects can be increased when Propofol is combined with 4-Methoxyamphetamine.
    The metabolism of 5-androstenedione can be decreased when combined with Propofol.
    The risk or severity of adverse effects can be increased when Propofol is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Propofol.
    The metabolism of 7-ethyl-10-hydroxycamptothecin can be decreased when combined with Propofol.
    The risk or severity of adverse effects can be increased when Propofol is combined with 7-Nitroindazole.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Propofol.
    The metabolism of 8-azaguanine can be decreased when combined with Propofol.
    The metabolism of 8-chlorotheophylline can be decreased when combined with Propofol.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Propofol.
    The metabolism of 9-Deazaguanine can be decreased when combined with Propofol.

    References

    • 1 . Vasile B, Rasulo F, Candiani A, Latronico N: The pathophysiology of propofol infusion syndrome: a simple name for a complex syndrome. Intensive Care Med. 2003 Sep;29(9):1417-25. Epub 2003 Aug 6. [PubMed: 12904852]
    • 2 . Ke JJ, Zhan J, Feng XB, Wu Y, Rao Y, Wang YL: A comparison of the effect of total intravenous anaesthesia with propofol and remifentanil and inhalational anaesthesia with isoflurane on the release of pro- and anti-inflammatory cytokines in patients undergoing open cholecystectomy. Anaesth Intensive Care. 2008 Jan;36(1):74-8. [PubMed: 18326136]
    • 3 . Hong JY, Kang YS, Kil HK: Anaesthesia for day case excisional breast biopsy: propofol-remifentanil compared with sevoflurane-nitrous oxide. Eur J Anaesthesiol. 2008 Jun;25(6):460-7. doi: 10.1017/S026502150800375X. Epub 2008 Feb 26. [PubMed: 18298873]

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