- Overview
- Properties
- Genetics
- Related Genes
- Related Drugs
- Related Diseases
- Datasets
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Overview
| Generic Names: | 2,6-Diisopropylphenol; Diisopropylphenol; propofol |
|---|---|
| Trade Names: | Diprivan; Disoprivan; Disoprofol; Rapinovet |
| PharmGKB Accession Id: | PA451141 |
Description
An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206) (source: Drug Bank)
Indication
Used for both induction and/or maintenance of anesthesia. (source: Drug Bank)
ATC Therapeutic Category
- N01AX:Other general anesthetics
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 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
Hepatic (source: Drug Bank)
Protein Binding
95 to 99% (source: Drug Bank)
Isomeric SMILES Code:
CC(C)c1cccc(c1O)C(C)C (source: Drug Bank)
Curated Annotations (
)
-
rs58597806
at chr2:234246085
in
UGT1A10,
UGT1A7,
UGT1A8,
UGT1A9
A study in 100 healthy Japanese volunteers showed that carriers of D256N may be at risk of suffering adverse effects of propofol and other substrates that are primarily metabolized by UGT1A9. In in vitro analyses the K(m) of wild-type and D256N for propofol glucuronidation were 111.2 and 43.6 microM, respectively. The V(max) of D256N was 8.1% and the efficiencies (V(max)/K(m)) was 19.1% of the wild-type. The V(max) value of D256N variant for mycophenolic acid was only 9.5% of the wild-type.- Variant Name:
- UGT1A9: D256N
- Related Drugs:
- propofol, xenobiotics
- Evidence:
-
PMID:18816295
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
CYP2A6 |
|
Publications |
|
CYP2B6 |
|
Publications |
|
|
NQO1 |
|
Publications |
|
|
SULT1A1 |
|
Publications |
|
|
UGT1A10 |
|
Variants |
|
|
UGT1A7 |
|
Variants |
|
|
UGT1A8 |
|
Variants |
|
|
UGT1A9 |
|
Publications, Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ALB |
|
(source: Drug Bank) |
| FAAH |
|
(source: Drug Bank) |
| GABRA1 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
- mRNA expression levels of PXR splice variants in livers
- FA
Submitted by Erin G. Schuetz, PhD involving CYP3A4, NR1I2, , amiodarone, cimetidine, dopamine, erythromycin, ethanol, glucocorticoids, hmg coa reductase inhibitors, midazolam, nicotine, phenobarbital, phenytoin, propofol, thyroid preparations and vasopressin
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
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LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.