Chemical: Drug
propofol

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for propofol

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2B6 *4 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *5 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *6 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *7 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *9 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *2 N/A N/A N/A
No VIP available CA VA
rs3745274 NC_000019.10:g.41006936G>T, NC_000019.9:g.41512841G>T, NG_007929.1:g.20638G>T, NM_000767.4:c.516G>T, NP_000758.1:p.Gln172His, XM_005258569.1:c.516G>T, XM_005258569.3:c.516G>T, XM_005258570.1:c.516G>T, XM_005258571.1:c.364+2490G>T, XM_006723050.2:c.516G>T, XM_011526546.1:c.516G>T, XM_011526547.1:c.516G>T, XM_011526548.1:c.484+2490G>T, XM_011526549.1:c.-75-1G>T, XM_011526550.1:c.364+2490G>T, XP_005258626.1:p.Gln172His, XP_005258627.1:p.Gln172His, XP_006723113.1:p.Gln172His, XP_011524848.1:p.Gln172His, XP_011524849.1:p.Gln172His, rs56308434, rs57685583
G > T
SNP
Q172H
No VIP available CA VA
rs58597806 NC_000002.11:g.234581346G>A, NC_000002.12:g.233672700G>A, NG_002601.2:g.87957G>A, NM_019075.2:c.855+35323G>A, NM_019076.4:c.855+54138G>A, NM_021027.2:c.766G>A, NP_066307.1:p.Asp256Asn, XR_241241.1:n.852G>A
G > A
SNP
D256N
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • 2,6-Diisopropylphenol
  • Diisopropylphenol
  • propofol
Trade Names
  • Diprivan
  • Disoprivan
  • Disoprofol
  • Rapinovet
Brand Mixture Names

PharmGKB Accession Id

PA451141

Type(s):

Drug

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. 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.

Source: Drug Bank

Indication

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

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

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.

Source: Drug Bank

Pharmacology

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 circulation).

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.

Source: Drug Bank

Protein Binding

95 to 99%, primarily to serum albumin and hemoglobin

Source: Drug Bank

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.

Source: Drug Bank

Half-Life

Initial distribution phase t 1/2alpha=1.8-9.5 minutes. Second redistirubtion phase t 1/2beta=21-70 minutes. Terminal elimination phase t 1/2gamma=1.5-31 hours.

Source: Drug Bank

Toxicity

Overdosage may increase pharmacologic and adverse effects or cause death.
<p>IV LD 50=53 mg/kg (mice), 42 mg/kg (rats). Oral LD 50 (as a solution in soybean oil)=1230 mg/kg (mice), 600 mg/kg (rats)</p>

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

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

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C12H18O

Source: Drug Bank

Isomeric SMILES

CC(C)c1cccc(c1O)C(C)C

Source: OpenEye

Canonical SMILES

CC(C)C1=CC=CC(C(C)C)=C1O

Source: Drug Bank

Average Molecular Weight

178.2707

Source: Drug Bank

Monoisotopic Molecular Weight

178.135765198

Source: Drug Bank

SMILES

CC(C)C1=CC=CC(C(C)C)=C1O

Source: Drug Bank

InChI String

InChI=1S/C12H18O/c1-8(2)10-6-5-7-11(9(3)4)12(10)13/h5-9,13H,1-4H3

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ALB (source: Drug Bank)
FAAH (source: Drug Bank)
GABRA1 (source: Drug Bank)
GABRB2 (source: Drug Bank)
GABRB3 (source: Drug Bank)
SCN4A (source: Drug Bank)

Drug Interactions

Interaction Description
tacrine - propofol The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Propofol, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Propofol is initiated, discontinued or if the dose is changed. (source: Drug Bank)
tizanidine - propofol Propofol may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Induces
Contraindicated With

Publications related to propofol: 19

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of the Cytochrome P450 2B6 (CYP2B6) Gene Polymorphism c.516G>T (rs3745274) on Propofol Dose Variability. European journal of drug metabolism and pharmacokinetics. 2015. Mourão Artemísia L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Neurotoxicity of generic anesthesia agents in infants and children: an orphan research question in search of a sponsor. JAMA. 2015. Psaty Bruce M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Pharmacogenetics, Plasma Concentrations, Clinical Signs and EEG during Propofol Treatment. Basic & clinical pharmacology & toxicology. 2014. Khan Muhammad Suleman, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cytochrome P450-mediated drug metabolism in the brain. Journal of psychiatry & neuroscience : JPN. 2012. Miksys Sharon, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of efavirenz on UDP-glucuronosyltransferase 1A1, 1A4, 1A6, and 1A9 activities in human liver microsomes. Molecules (Basel, Switzerland). 2012. Ji Hye Young, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Influence of sex on propofol metabolism, a pilot study: implications for propofol anesthesia. European journal of clinical pharmacology. 2011. Loryan Irena, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug Metabolism within the Brain Changes Drug Response: Selective Manipulation of Brain CYP2B Alters Propofol Effects. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2011. Khokhar Jibran Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Absorption, distribution, metabolism and excretion pharmacogenomics of drugs of abuse. Pharmacogenomics. 2011. Meyer Markus R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP2B6. Pharmacogenetics and genomics. 2010. Thorn Caroline F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Structure, function, regulation and polymorphism of human cytochrome P450 2A6. Current drug metabolism. 2009. Di Yuan Ming, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Substrate specificity, regulation, and polymorphism of human cytochrome P450 2B6. Current drug metabolism. 2009. Mo Sui-Lin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphic drug metabolism in anaesthesia. Current drug metabolism. 2009. Restrepo Juan G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CYP2B6: new insights into a historically overlooked cytochrome P450 isozyme. Current drug metabolism. 2008. Wang Hongbing, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effect of D256N and Y483D on propofol glucuronidation by human uridine 5'-diphosphate glucuronosyltransferase (UGT1A9). Basic & clinical pharmacology & toxicology. 2008. Takahashi Hiroko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance. Pharmacogenomics. 2007. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Identification of common polymorphisms in the promoter of the UGT1A9 gene: evidence that UGT1A9 protein and activity levels are strongly genetically controlled in the liver. Pharmacogenetics. 2004. Girard Hugo, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The effect of valproic acid on drug and steroid glucuronidation by expressed human UDP-glucuronosyltransferases. Biochemical pharmacology. 2003. Ethell Brian T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Involvement of human liver cytochrome P4502B6 in the metabolism of propofol. British journal of clinical pharmacology. 2001. Oda Y, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0409-4699-30
DrugBank:
DB00818
PDB:
PFL
ChEBI:
8495
KEGG Compound:
C07523
KEGG Drug:
D00549
PubChem Compound:
4943
PubChem Substance:
46504991
9726
Drugs Product Database (DPD):
2242973
ChemSpider:
4774
HET:
PFL
Therapeutic Targets Database:
DAP000662
FDA Drug Label at DailyMed:
28d7ba00-f824-4e55-139a-03f509c099db

Clinical Trials

These are trials that mention propofol and are related to either pharmacogenetics or pharmacogenomics.

No trials found.

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Sources for PharmGKB drug information: DrugBank, PubChem.