Tolmetin

Tolmetin
Skeletal formula
Space-filling model
Names
Pronunciation/ˈtɒlmətɪn/
Trade namesTolectin
IUPAC name
  • [1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetic acid
Clinical data
Drug classNonsteroidal anti-inflammatory drug (NSAID)[1]
Main usesInflammation[1]
Side effectsAbdominal pain, diarrhea, swelling, dizziness, increased blood pressure[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use		By mouth
Typical dose400 mg TID[2]
External links
AHFS/Drugs.comMonograph
MedlinePlusa681033
Legal
Legal status
  • AU: S4 (Prescription only)
Pharmacokinetics
Elimination half-life1-2 hours, next phase up to 5 hours
Chemical and physical data
FormulaC15H15NO3
Molar mass257.289 g·mol−1
3D model (JSmol)
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) checkY
  • Key:UPSPUYADGBWSHF-UHFFFAOYSA-N checkY

Tolmetin, sold under the brand name Tolectin among others, is a medication used to treat inflammation in conditions such as osteoarthritis and rheumatoid arthritis.[1] It is taken by mouth.[1] Benefits are generally seen within a week.[2]

Common side effects include abdominal pain, diarrhea, swelling, dizziness, and increased blood pressure.[1] Other side effects can include kidney problems, liver problems, heart disease, Stevens-Johnson syndrome, and anaphylaxis.[1] Use in the last part of pregnancy may harm the baby, while use when breastfeeding is safe.[1][2] It is a nonsteroidal anti-inflammatory drug (NSAID) and inhibits both COX-1 and COX-2.[1]

Tolmetin was approved for medical use in the United States in 1976.[1] It is available as a generic medication.[3] In the United States 60 tablets of 600 mg costs about 96 USD as of 2021.[3] It is not available in the United Kingdom.[4]

Medical uses

Tolmetin is applicable in the treatment of rheumatoid arthritis,[5][6] osteoarthrosis,[7][8] pain,[9] and ankylosing spondylitis.[10]

Dosage

The typical dose is 400 mg three times per day.[2]

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.[11] 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.[11] Overdose can result in drowsiness, nausea, epigastric pain, and vomiting.

In October 2020, the U.S. Food and Drug Administration (FDA) required the drug label to be updated for all nonsteroidal anti-inflammatory medications to describe the risk of kidney problems in unborn babies that result from low amniotic fluid.[12][13] They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy.[12][13]

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.[14]

References

  1. 1 2 3 4 5 6 7 8 9 10 "Tolmetin Monograph for Professionals". Drugs.com. Archived from the original on 22 April 2021. Retrieved 6 October 2021.
  2. 1 2 3 4 Thompson, Andrew E. (7 October 2009). Tarascon Pocket Rheumatologica. Jones & Bartlett Publishers. p. 223. ISBN 978-1-4496-7187-7. Archived from the original on 9 October 2021. Retrieved 6 October 2021.
  3. 1 2 "Tolectin Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 6 October 2021.
  4. ↑ Watts, Richard (2009). Oxford Desk Reference: Rheumatology. Oxford University Press. p. 355. ISBN 978-0-19-922999-4. Archived from the original on 2021-10-09. Retrieved 2021-10-06.
  5. ↑ Cordrey LJ (October 1976). "Tolmetin sodium, a new anti-arthritis drug: double-blind and long-term studies". Journal of the American Geriatrics Society. 24 (10): 440–6. doi:10.1111/j.1532-5415.1976.tb03256.x. PMID 61224. S2CID 26040280.
  6. ↑ Cardoe N, Steele CE (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): 688–94. doi:10.1185/03007997609112003. PMID 800970.
  7. ↑ Liyanage SP, Steele CE (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.
  8. ↑ 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.
  9. ↑ Stacher G, Bauer P, Ehn I, Schreiber E (June 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.
  10. ↑ Calin A (July 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. S2CID 33879936.
  11. 1 2 "Tolmetin". MedlinePlus. Archived from the original on 2007-06-10. Retrieved 2007-07-02.
  12. 1 2 "FDA Warns that Using a Type of Pain and Fever Medication in Second Half of Pregnancy Could Lead to Complications". U.S. Food and Drug Administration (FDA) (Press release). 15 October 2020. Archived from the original on 16 October 2020. Retrieved 15 October 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  13. 1 2 "NSAIDs may cause rare kidney problems in unborn babies". U.S. Food and Drug Administration. 21 July 2017. Archived from the original on 17 October 2020. Retrieved 15 October 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  14. ↑ "Tolmetin". DrugBank. Archived from the original on 2021-08-29. Retrieved 2007-07-02.
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