WordNet

a silvery soft waxy metallic element of the alkali metal group; occurs abundantly in natural compounds (especially in salt water); burns with a yellow flame and reacts violently in water; occurs in sea water and in the mineral halite (rock salt) (同)Na, atomic number 11

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ソジウム,ナトリウム(金属元素;化学記号はNa)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/01/21 23:27:09」(JST)

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Tolmetin /ˈtɒlmətɨn/ is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. It is used primarily to reduce hormones that cause pain, swelling, tenderness, and stiffness in conditions such as osteoarthritis and rheumatoid arthritis, including juvenile rheumatoid arthritis. In the United States it is marketed as Tolectin and comes as a tablet or capsule.

Clinical trials

Tolmetin is applicable in the treatment of rheumatoid arthritis,^[1]^[2] osteoarthrosis,^[3]^[4] pain,^[5] and ankylosing spondylitis.^[6]

Mechanism of action

Although the mechanism of action of tolmetin is unknown, research involving humans and animals has shown that tolmetin does not achieve anti-inflammatory response by stimulation of the adrenal or pituitary gland, but it has shown tolmetin restrains prostaglandin synthetase in vitro and reduces plasma levels of prostaglandin E, possibly causing the anti-inflammatory response.

When tested in rats tolmetin prevented experimentally stimulated polyarthritis and reduced inflammation. In patients with rheumatoid arthritis or osteoarthritis tolmetin restrained disease activity as efficiently as aspirin and indometacin, although the occurrence of mild gastrointestinal adverse effects and tinnitus was lower in patients treated with tolmetin than it was with aspirin-treated patients and the occurrence of adverse effects of the central nervous system was lower with tolmetin than it was with indometacin.^[7]

Side effects

Tolmetin can increase the risk of heart or circulatory conditions such as heart attacks and strokes. It should not be taken shortly before or after coronary artery bypass surgery.^[8] Tolmetin can also increase the risk of gastrointestinal conditions such as perforation or bleeding, which is fatal. Antacids can be taken with tolmetin to relieve stomachaches that often occur.^[8] Overdose can result in drowsiness, nausea, epigastric pain, and vomiting.

Chemical synthesis

Tolmetin can be synthesized by the following route:^[9]

J. Carson, U.S. Pat. 3.752.826 (1973).
J.R. Carson, Fr. Pat. 1.574.570 (1969)

References

^ Cordrey L J (1976). "Tolmetin sodium, a new anti-arthritis drug: double-blind and long-term studies". Journal of the American Geriatrics Society 24 (10): 440–446. PMID 61224.
^ Cardoe N; Steele C E (1976–1977). "A double-blind crossover comparison of tolmetin sodium and phenylbutazone in the treatment of rheumatoid arthritis". Current medical research and opinion 4 (10): 688–694. doi:10.1185/03007997609112003. PMID 800970.
^ Liyanage S P; Steele C E (1977–1978). "Tolmetin in osteoarthrosis of the hip and knee: double-blind crossover trials". Current medical research and opinion 5 (4): 299–305. doi:10.1185/03007997709110184. PMID 343992.
^ Davies, J; Dixon, AS; Steele, CE (1980). "Tolmetin sodium and indomethacin in the treatment of osteoarthrosis of the hip: a double-blind crossover study". Current medical research and opinion 7 (2): 115–20. doi:10.1185/03007998009112037. PMID 7002480.
^ Stacher, G; Bauer, P; Ehn, I; Schreiber, E (1979). "Effects of tolmetin, paracetamol, and of two combinations of tolmetin and paracetamol as compared to placebo on experimentally induced pain. A double blind study". International journal of clinical pharmacology and biopharmacy 17 (6): 250–5. PMID 381221.
^ Calin, A (1983). "Clinical use of tolmetin sodium in patients with ankylosing spondylitis: a review". Journal of clinical pharmacology 23 (7): 301–8. doi:10.1002/j.1552-4604.1983.tb02740.x. PMID 6350376.
^ "Tolmetin". DrugBank. Retrieved 2007-07-02.
^ ^a ^b "Tolmetin". MedlinePlus. Archived from the original on 2007-06-10. Retrieved 2007-07-02.
^ Carson, John R.; McKinstry, Doris N.; Wong, Stewart (1971). "5-Benzoyl-1-methylpyrrole-2-acetic acids as antiinflammatory agents". Journal of Medicinal Chemistry 14 (7): 646. doi:10.1021/jm00289a026.

UpToDate Contents

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English Journal

Spectroscopic investigation of tolmetin interaction with human serum albumin.

Neamtu S, Tosa N, Bogdan M.SourceDepartment of Molecular and Biomolecular Physics, National Institute of Isotopic and Molecular Technology, 400293 Cluj-Napoca, Romania. Electronic address: silvia.neamtu@itim-cj.ro.
Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2013 Nov;85:277-82. doi: 10.1016/j.jpba.2013.07.032. Epub 2013 Aug 5.
The interaction of tolmetin (TOL) with human serum albumin (HSA) in physiological buffer solution (pH 7.4) was studied by fluorescence and UV-vis absorption spectroscopy at different temperatures, combined with time-resolved fluorescence measurements. The experimental results showed that there was a
PMID 23973633

A simple method to evaluate reactivity of acylglucuronides optimized for early stage drug discovery.

Jinno N, Ohashi S, Tagashira M, Kohira T, Yamada S.SourceLaboratory for Safety Assessment and ADME, Pharmaceuticals Research Center, Asahi Kasei Pharma Corporation.
Biological & pharmaceutical bulletin.Biol Pharm Bull.2013 Sep 1;36(9):1509-13. Epub 2013 Jul 5.
Drugs containing the carboxylic functional group can be metabolized to form acylglucuronides believed to cause idiosyncratic drug toxicity when the acylglucuronide is unstable. Recent studies have shown that the half-life of an acylglucuronide in phosphate buffer is the best means for classifying ac
PMID 23832447

The effect of inorganic salt type and concentration on hydrophilic drug loading into microspheres using the emulsion/solvent diffusion method.

Yağ G, Calış S, Arıca-Yegin B.SourceDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University , Sıhhiye-Ankara , Turkey.
Drug development and industrial pharmacy.Drug Dev Ind Pharm.2013 Apr 19. [Epub ahead of print]
Abstract Aim: In order to avoid gastric irritation caused by tolmetin sodium (TS), gastro resistant Eudragit® S 100 microsphere formulations were prepared with the emulsion/solvent diffusion method. Materials: Considering the high water solubility of the TS molecule, the effects of the presence of
PMID 23600654

Japanese Journal

Development of non-steroidal anti-inflammatory drug intolerance over a 3 year period

SHIRAI Toshihiro,MATSUI Takashi,UTO Tomohiro,CHIDA Kingo,NAKAMURA Hirotoshi
Allergology international : official journal of the Japanese Society of Allergology 53(2), 191-192, 2004-06-01
NAID 10014079655

Efficacy of tolmetin sodium for adhesion prevention in rabbit and rat models

LEGRAND EK
J Surg Res 56, 67-71, 1994
NAID 30018858235

EFFECTS OF SOME ANTI-INFLAMMATORY DRUGS ON BIOCHEMICAL VALUES AND ON HEPATIC PEROXISOMAL ENZYMES OF RAT

WATANABE TAKAFUMI,SUGA TETSUYA
Journal of pharmacobio-dynamics 8(12), 1060-1067, 1985-12
… Effects of tolmetin, diclofenac Na, fenbufen, alclofenac, aminopyrine, mepirizole, thiaramide and aspirin as a positive control, which are widely used in this country as anti-inflammatory drugs, and on body and liver weights, triglyceride and cholesterol level and hepatic peroxisomal enzymes of normolipemic rats were examined. … Tolmetin (100 mg/kg) and fenbufen (50 mg/kg) increased carnitine acetyltransferase (CAT) and fatty acyl-coenzyme A oxidizing system (FAOS) activities, which participate in hepatic lipid metabolism. …
NAID 110003637884

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リンク元

「トルメチン」

Tolmetin
Systematic (IUPAC) name
	[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetic acid
Clinical data
Trade names	Tolectin
AHFS/Drugs.com	monograph
MedlinePlus	a681033
Legal status	AU: Prescription Only (S4);
Routes	oral
Pharmacokinetic data
Half-life	1-2 hours, next phase up to 5 hours
Identifiers
CAS number	26171-23-3
ATC code	M01AB03 M02AA21
PubChem	CID 5509
DrugBank	DB00500
ChemSpider	5308
UNII	D8K2JPN18B
KEGG	D02355
ChEBI	CHEBI:71941
ChEMBL	CHEMBL1020
Chemical data
Formula	C15H15NO3
Molecular mass	257.285 g/mol
	SMILES O=C(c1ccc(n1C)CC(=O)O)c2ccc(cc2)C;
	InChI InChI=1S/C15H15NO3/c1-10-3-5-11(6-4-10)15(19)13-8-7-12(16(13)2)9-14(17)18/h3-8H,9H2,1-2H3,(H,17,18) ; Key:UPSPUYADGBWSHF-UHFFFAOYSA-N ;
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英: tolmetin
化: トルメチンナトリウム tolmetin sodium
商: トレクチン

酸性非ステロイド性抗炎症薬

[1] Cordrey L J (1976). "Tolmetin sodium, a new anti-arthritis drug: double-blind and long-term studies". Journal of the American Geriatrics Society 24 (10): 440–446. PMID 61224.

[2] Cardoe N; Steele C E (1976–1977). "A double-blind crossover comparison of tolmetin sodium and phenylbutazone in the treatment of rheumatoid arthritis". Current medical research and opinion 4 (10): 688–694. doi:10.1185/03007997609112003. PMID 800970.

[3] Liyanage S P; Steele C E (1977–1978). "Tolmetin in osteoarthrosis of the hip and knee: double-blind crossover trials". Current medical research and opinion 5 (4): 299–305. doi:10.1185/03007997709110184. PMID 343992.

[4] Davies, J; Dixon, AS; Steele, CE (1980). "Tolmetin sodium and indomethacin in the treatment of osteoarthrosis of the hip: a double-blind crossover study". Current medical research and opinion 7 (2): 115–20. doi:10.1185/03007998009112037. PMID 7002480.

[5] Stacher, G; Bauer, P; Ehn, I; Schreiber, E (1979). "Effects of tolmetin, paracetamol, and of two combinations of tolmetin and paracetamol as compared to placebo on experimentally induced pain. A double blind study". International journal of clinical pharmacology and biopharmacy 17 (6): 250–5. PMID 381221.

[6] Calin, A (1983). "Clinical use of tolmetin sodium in patients with ankylosing spondylitis: a review". Journal of clinical pharmacology 23 (7): 301–8. doi:10.1002/j.1552-4604.1983.tb02740.x. PMID 6350376.

[DrugBank-7] "Tolmetin". DrugBank. Retrieved 2007-07-02.

[MedlinePlus-8] "Tolmetin". MedlinePlus. Archived from the original on 2007-06-10. Retrieved 2007-07-02.

[9] Carson, John R.; McKinstry, Doris N.; Wong, Stewart (1971). "5-Benzoyl-1-methylpyrrole-2-acetic acids as antiinflammatory agents". Journal of Medicinal Chemistry 14 (7): 646. doi:10.1021/jm00289a026.

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tolmetin sodium