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Analgesic
Proprietary names. Amuno; Artracin; Confortid; Flexin Continus; Imbrilon; Indochron;
Indocid; Indocin; Indoflex; Indolar; Indomax; Indotard; Maximet SR; Mobilan; Pardelprin;
Rheumacin; Rimacid; Slo-Indo.
1-(4-Chlorobenzoyl)-5methoxy2methyl1H-indole3acetic acid
C19H16ClNO4=357.8
CAS53861
Dissociation Constant.
pKa4.5.
Partition Coefficient.
Log P(octanol/pH 7.4), 1.0.
Colour Tests.
Liebermann's Testblack; Mandelin's Testgrey; Marquis Testorange; Sulfuric Acid
orange
Thinlayer Chromatography.
System TARf 94; system TDRf 16; system TERf 05; system TFRf 13; system TG
Rf 20; system TADRf 38; system TAERf 83; system TAFRf 63; system TAJRf
46; system TAKRf 90; system TALRf 90. (Chromic acid solution, greybrown; acidified
potassium permanganate solution, positive.)
Gas Chromatography.
Ultraviolet Spectrum.
Methanolic acid318 nm (A11=180a); aqueous alkali230, 279 nm (A11=213a). (See below)
Infrared Spectrum.
Principal peaks at wavenumbers 1681, 1228, 1218, 1706, 1299, 1065 cm1 (KBr disk).
Mass Spectrum.
Principal ions at m/z 139, 141, 357, 111, 359, 140, 113, 75; M (OH-)-Me2 239, 298, 135, 191,
107, 103.
Quantification
Gas chromatography.
In plasma or urine: indometacin and desmethylindometacin, limit of detection 10 g/L, ECD
P. Guissou et al.,J. Chromatogr.,1983, 277(28) B Biomed. Appl., 368373.
Gas chromatographymass spectrometry.
In plasma or synovial fluid, limit of detection <0.1 g/LM. Dawson et al.,Biomed.
Environ. Mass Spectrom.,1990, 19, 453458. In plasma or urine: indometacin and other
NSAIDsA. K. Singh et al.,J. Chromatogr.,1991, 568, 351361.
High performance liquid chromatography.
After a single oral dose of 50 mg given to 20 subjects, peak plasma concentrations of 1.0 to
3.0 mg/L (mean 1.9) were attained in 1 to 4. [K. C. Kwan et al.,J. Pharmacokinet.
Biopharm.,1976, 4, 255280.]
Steadystate plasma concentrations of 0.31 to 0.63 mg/L (mean 0.49) were attained in about
6 days after oral doses of 25 mg three times a day to 5 subjects. [G. Alvn et al.,Clin.
Pharmaol. Ther.,1975, 18, 364373.]
Toxicity.
Toxic effects may be produced by plasma concentrations greater than 5 mg/L.
Halflife.
Plasma halflife, 3 to 15 h.
Volume of distribution.
About 1 L/kg.
Clearance.
Plasma clearance, 1 to 2 mL/min/kg.
Distribution in blood.
Plasma:whole blood ratio, 1.9.
Protein binding.
In plasma, 90 to 99%.
Note.
For a review of the pharmacokinetics of indometacin see L. Helleberg,Clin.
Pharmacokinet.,1981, 6, 245258.
Dose.
50 to 200 mg daily.