Registration Dossier
Registration Dossier
Data platform availability banner - registered substances factsheets
Please be aware that this old REACH registration data factsheet is no longer maintained; it remains frozen as of 19th May 2023.
The new ECHA CHEM database has been released by ECHA, and it now contains all REACH registration data. There are more details on the transition of ECHA's published data to ECHA CHEM here.
Diss Factsheets
Use of this information is subject to copyright laws and may require the permission of the owner of the information, as described in the ECHA Legal Notice.
EC number: 245-826-4 | CAS number: 23694-14-6
- Life Cycle description
- Uses advised against
- Endpoint summary
- Appearance / physical state / colour
- Melting point / freezing point
- Boiling point
- Density
- Particle size distribution (Granulometry)
- Vapour pressure
- Partition coefficient
- Water solubility
- Solubility in organic solvents / fat solubility
- Surface tension
- Flash point
- Auto flammability
- Flammability
- Explosiveness
- Oxidising properties
- Oxidation reduction potential
- Stability in organic solvents and identity of relevant degradation products
- Storage stability and reactivity towards container material
- Stability: thermal, sunlight, metals
- pH
- Dissociation constant
- Viscosity
- Additional physico-chemical information
- Additional physico-chemical properties of nanomaterials
- Nanomaterial agglomeration / aggregation
- Nanomaterial crystalline phase
- Nanomaterial crystallite and grain size
- Nanomaterial aspect ratio / shape
- Nanomaterial specific surface area
- Nanomaterial Zeta potential
- Nanomaterial surface chemistry
- Nanomaterial dustiness
- Nanomaterial porosity
- Nanomaterial pour density
- Nanomaterial photocatalytic activity
- Nanomaterial radical formation potential
- Nanomaterial catalytic activity
- Endpoint summary
- Stability
- Biodegradation
- Bioaccumulation
- Transport and distribution
- Environmental data
- Additional information on environmental fate and behaviour
- Ecotoxicological Summary
- Aquatic toxicity
- Endpoint summary
- Short-term toxicity to fish
- Long-term toxicity to fish
- Short-term toxicity to aquatic invertebrates
- Long-term toxicity to aquatic invertebrates
- Toxicity to aquatic algae and cyanobacteria
- Toxicity to aquatic plants other than algae
- Toxicity to microorganisms
- Endocrine disrupter testing in aquatic vertebrates – in vivo
- Toxicity to other aquatic organisms
- Sediment toxicity
- Terrestrial toxicity
- Biological effects monitoring
- Biotransformation and kinetics
- Additional ecotoxological information
- Toxicological Summary
- Toxicokinetics, metabolism and distribution
- Acute Toxicity
- Irritation / corrosion
- Sensitisation
- Repeated dose toxicity
- Genetic toxicity
- Carcinogenicity
- Toxicity to reproduction
- Specific investigations
- Exposure related observations in humans
- Toxic effects on livestock and pets
- Additional toxicological data
Basic toxicokinetics
Administrative data
- Endpoint:
- basic toxicokinetics in vivo
- Type of information:
- experimental study
- Adequacy of study:
- key study
- Reliability:
- 4 (not assignable)
- Rationale for reliability incl. deficiencies:
- secondary literature
Data source
Reference
- Reference Type:
- review article or handbook
- Title:
- Pharmacotoxicological aspects of levosulpiride.
- Author:
- Rossi F
- Year:
- 1 995
- Bibliographic source:
- Pharmacol Res. 1995 Feb;31(2):81-94.
Materials and methods
Test material
- Reference substance name:
- Sulpiride
- EC Number:
- 239-753-7
- EC Name:
- Sulpiride
- Cas Number:
- 15676-16-1
- Molecular formula:
- C15H23N3O4S
- IUPAC Name:
- N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
Constituent 1
Results and discussion
Any other information on results incl. tables
In rats treated with sulpiride 200 mg/kg by oral route the pharmacokinetic parameters were the following: Cmax 6.8µg/ml; tmax 3 h; t1/2 1.4 h; bioavailability 15%. The low bioavailability of sulpiride following oral administration (about 15%) is due not to the metabolism in the liver, but to a reduced absorption by the gastrointestinal tract. Many metabolites were obtained from rats and dogs orally treated with sulpiride. Particularly, in rats, metabolites represented 56% of the administered drug (60 mg/kg) and 38% of them were conjugates. In the dog, the metabolites represented 15% of the administered sulpiride (50 mg/kg), of which 4% were conjugates. However, none of the metabolites documented in these species was found in human urine. In the Rhesus monkeys treated with sulpiride at 10 mg/kg by oral or intravenous route, in both the urine and the bile were documented the following fractions of the administered dose: 60-80% sulpiride, 10-30% 5-oxopyrrolidine sulpiride and 3-8% unidentified metabolite. After intramuscular administration (50 mg) to healthy volunteers, the bioavailability of L-sulpiride is practically complete (about 99%), whereas the oral bioavailability of the same dosage is about 30%. The half-lives are 6.2, 8.3 and 9.7 h respectively, for the intravenous, intramuscular and oral administration (50 mg), with a total clearance of about 260 ml/min. Sulpiride is not bound to plasma proteins to any large extent. In dog plasma 16% of the sulpiride is bound over a concentration range of 1 to 50µg/ml. In human plasma 14% is bound over the same concentration range. Thus, the protein binding is constant and independent of sulpiride concentrations in dog plasma and human plasma. The results of a comparative pharmacokinetic study after single oral administration of D-, L- and racemic sulpiride demonstrated that the pharmacokinetic profiles are largely identical. Also, the urinary excretion is similar for racemic and L-sulpiride and accounts for about 65-70% of the dose after intravenous administration, totally as unchanged drug. The mean renal clearance is in the range 260-310 ml/min after intravenous administration of the two drugs (L- and racemic-sulpiride) and suggests a tubular secretion of sulpiride since clearance exceeded glomerular filtration rate. This conclusion is also supported by data on metabolism of sulpiride.
Applicant's summary and conclusion
- Executive summary:
In rats treated with sulpiride 200 mg/kg by oral route the pharmacokinetic parameters were the following: Cmax 6.8 µg/ml; tmax 3 h; t1/2 1.4 h; bioavailability 15%. The low bioavailability of sulpiride following oral administration (about 15%) is due not to the metabolism in the liver, but to a reduced absorption by the gastrointestinal tract. Many metabolites were obtained from rats and dogs orally treated with sulpiride. Particularly, in rats, metabolites represented 56% of the administered drug (60 mg/kg) and 38% of them were conjugates. In the dog, the metabolites represented 15% of the administered sulpiride (50 mg/kg), of which 4% were conjugates. However, none of the metabolites documented in these species was found in human urine. In the Rhesus monkeys treated with sulpiride at 10 mg/kg by oral or intravenous route, in both the urine and the bile were documented the following fractions of the administered dose: 60-80% sulpiride, 10-30% 5-oxopyrrolidine sulpiride and 3-8% unidentified metabolite. After intramuscular administration (50 mg) to healthy volunteers, the bioavailability of L-sulpiride is practically complete (about 99%), whereas the oral bioavailability of the same dosage is about 30%. The half-lives are 6.2, 8.3 and 9.7 h respectively, for the intravenous, intramuscular and oral administration (50 mg), with a total clearance of about 260 ml/min. Sulpiride is not bound to plasma proteins to any large extent. In dog plasma 16% of the sulpiride is bound over a concentration range of 1 to 50 µg/ml. In human plasma 14% is bound over the same concentration range. Thus, the protein binding is constant and independent of sulpiride concentrations in dog plasma and human plasma. The results of a comparative pharmacokinetic study after single oral administration of D-, L- and racemic sulpiride demonstrated that the pharmacokinetic profiles are largely identical. Also, the urinary excretion is similar for racemic and L-sulpiride and accounts for about 65-70% of the dose after intravenous administration, totally as unchanged drug. The mean renal clearance is in the range 260-310 ml/min after intravenous administration of the two drugs (L- and racemic-sulpiride) and suggests a tubular secretion of sulpiride since clearance exceeded glomerular filtration rate. This conclusion is also supported by data on metabolism of sulpiride.
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice.
Reproduction or further distribution of this information may be subject to copyright protection. Use of the information without obtaining the permission from the owner(s) of the respective information might violate the rights of the owner.