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Tocainide

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Tocainide
File:Tocainide.svg
Systematic (IUPAC) name
N-(2,6-dimethylphenyl)alaninamide
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
MedlinePlus a601248
Pharmacokinetic data
Bioavailability 0.9-1 (oral)
Protein binding 10-20%
Metabolism glucuronidation (primary)
Half-life 9-14 R, 13-20 S
Excretion 30-50% urine (unchanged)
Identifiers
41708-72-9 7pxY
C01BB03
PubChem CID 38945
DrugBank DB01056 7pxY
ChemSpider 35632 7pxY
UNII 27DXO59SAN 7pxY
KEGG D06172 7pxY
ChEBI CHEBI:9611 7pxY
ChEMBL CHEMBL1762 7pxY
Chemical data
Formula C11H16N2O
192.258 g/mol
 14pxY (what is this?)  (verify)

Tocainide (Tonocard) is a class Ib antiarrhythmic agent. It is no longer sold in the United States.

Pharmacokinetics

Tocainide 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 bioavailability 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. (Not verbatim)

Synthesis

References

  1. ^ R.N. Boyes, E.W. Byrnes, DE 2235745  (1972).
  2. ^ Astra Pharmaceutical Products Inc., GB 1461602  (1974).
  3. ^ R.N. Boyes, B.R. Duce, E.M. Smith, E.W. Byrnes, 2400540  (1974).
  4. ^ Byrnes, Eugene W. (1979). "New antiarrhythmic agents. 1. Primary .alpha.-amino anilides". Journal of Medicinal Chemistry 22 (10): 1171–1176. doi:10.1021/jm00196a005.  edit

External links

Burton ME. Applied Pharmacokinetics & Pharmacodynamics: Principles of Therapeutic Drug Monitoring. 4th ed. Philadelphia: Lippincott Williams & Wilkins; 2006.


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