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| CAS No.: | 41708-72-9 |
|---|---|
| Name: | TOCAINIDE |
| Article Data: | 5 |
| Molecular Structure: | |
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| Formula: | C11H16 N2 O |
| Molecular Weight: | 192.261 |
| Synonyms: | (RS)-Tocainide;(?à)-Tocainide;2-Amino-2',6'-propionoxylidide; Astra W 36095; DL-Tocainide; Racemic tocainide;Tocainide; W 36095 |
| EINECS: | 255-505-0 |
| Density: | 1.0529 (rough estimate) |
| Melting Point: | 246-266 °C |
| Boiling Point: | 328.25°C (rough estimate) |
| Hazard Symbols: |
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| Risk Codes: | R22 |
| Safety: | Human and experimental poison by ingestion. Human systemic effects by ingestion: mental disturbances, coma, cardiac damage, nausea or vomiting, and aplastic anemia. When heated to decomposition it emits toxic fumes of NOx. |
| PSA: | 55.12000 |
| LogP: | 2.36240 |
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Chemistry
Product Name: Tocainide (CAS NO.41708-72-9)
Molecular Formula: C11H16N2O
Molecular Weight: 192.26g/mol
Mol File: 41708-72-9.mol
Einecs: 5-505-0
Boiling point: 330.1 °C at 760 mmHg
Flash Point: 153.5 °C
Density: 1.094 g/cm3
Surface Tension: 44 dyne/cm
Enthalpy of Vaporization: 57.27 kJ/mol
Vapour Pressure: 0.00017 mmHg at 25°C
XLogP3: 0.8
H-Bond Donor: 2
H-Bond Acceptor: 2
Product Categories: Active Pharmaceutical Ingredients
Uses
Tocainide (CAS NO.41708-72-9) is a class Ib antiarrhythmic agent.
Toxicity Data With Reference
| 1. | orl-hmn TDLo:5714 µg/kg:CNS,GIT | DRFUD4 Drugs of the Future. 2 (1977),141. | ||
| 2. | orl-man TDLo:2606 mg/kg/11W-I:BLD | NEJMAG New England Journal of Medicine. 314 (1986),583. | ||
| 3. | orl-man LDLo:229 mg/kg:CNS,CVS | BMJOAE British Medical Journal. 288 (1984),760. | ||
| 4. | orl-mus LD50:529 mg/kg | DRFUD4 Drugs of the Future. 2 (1977),141. | ||
| 5. | orl-mus LD50:94 mg/kg | JMCMAR Journal of Medicinal Chemistry. 24 (1981),1059. |
Safety Profile
Human and experimental poison by ingestion. Human systemic effects by ingestion: mental disturbances, coma, cardiac damage, nausea or vomiting, and aplastic anemia. When heated to decomposition it emits toxic fumes of NOx.
Safety Information of Tocainide (CAS NO.41708-72-9):
Hazard Codes: Xn.gif){kind=small}
Risk Statements: 22
22: Harmful if swallowed
Specification
Tocainide ,its CAS NO. is 41708-72-9. is a lidocaine analog, that does not have significant 1st pass metabolism. It is found in two enantiomers. The R isomer is 4x as potent as the S. Oral bioavaliability is 0.9-1.0. In the blood tocainide is 10-20% protein bound. The Volume of distribution is 2.5-3.5 L/kg. 30-50% is excreted unchanged in the urine. The more active R-isomer is cleared faster in anephric patients or those with severe renal dysfunction. The main metabolite is the glucuronidated tocainide carbamic acid. The glucuronosyl transferase is apparently induced by rifampin. Weak inhibition of Cyp1A2 leads to a mild theophylline interaction.
The synonyms of Tocainide is 2-Amino-2',6'-propionoxylidide ; 2-Amino-n-(2,6-dimethylphenyl)-propanamid ; 6'-Propionoxylidide, 2-amino-2 ; Alanyl-2,6-xylidide ; Astra W-36095 ; W-36095 .