Description

Simple

A medication used as an anesthetic in surgery.

Clinical

A medication used in general anesthesia and for sedation.

Overview

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. Recovery from propofol-induced anaesthesia is generally rapid and associated with less frequent side effects (e.g. drowsiness, nausea, vomiting) than with thiopental, methohexital, and etomidate. Propofol may be used prior to diagnostic procedures requiring anaesthesia, in the management of refractory status epilepticus, and for induction and/or maintenance of anaesthesia prior to and during surgeries.

Pharmacology

Indication

Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.

Pharmacodynamic

Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain ci... Read more

Mechanism of action

The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.

Absorption

Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.

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 t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.

Route of elimination

It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.

Toxicity

Overdosage may increase pharmacologic and adverse effects or cause death.
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)

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

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
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Propofol.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Propofol.
1-benzylimidazole
The risk or severity of hypertension can be increased when Propofol is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of hypertension can be increased when Propofol is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Propofol is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Propofol is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Propofol.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Propofol is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Propofol is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Propofol.
7-Nitroindazole
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
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Propofol.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Propofol.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Propofol.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Propofol.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Propofol.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Propofol.
Abacavir
The metabolism of Abacavir can be decreased when combined with Propofol.
Abatacept
The metabolism of Propofol can be increased when combined with Abatacept.
Abediterol
The risk or severity of hypertension can be increased when Propofol is combined with Abediterol.
3 References
  1. 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. 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. 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