Last updated
Tolmetin Structural Formulae.png
Clinical data
Trade names Tolectin
AHFS/ Monograph
MedlinePlus a681033
Routes of
By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
Pharmacokinetic data
Elimination half-life 1-2 hours, next phase up to 5 hours
  • [1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetic acid
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard 100.043.164 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C15H15NO3
Molar mass 257.289 g·mol−1
3D model (JSmol)
  • O=C(c1ccc(n1C)CC(=O)O)c2ccc(cc2)C
  • 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) Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Tolmetin /ˈtɒlmətɪn/ is a nonsteroidal anti-inflammatory drug (NSAID) of the heterocyclic acetic acid derivative class. 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 can be fatal. Antacids can be taken with tolmetin to relieve stomachaches that often occur. [8] 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. [9] [10] They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy. [9] [10]

Related Research Articles

<span class="mw-page-title-main">Nonsteroidal anti-inflammatory drug</span> Class of therapeutic drug for relieving pain and inflammation

Non-steroidal anti-inflammatory drugs (NSAID) are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of use, but largely include an increased risk of gastrointestinal ulcers and bleeds, heart attack, and kidney disease.

<span class="mw-page-title-main">Ibuprofen</span> Medication used for treating pain, fever, and inflammation

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that is used for treating pain, fever, and inflammation. This includes painful menstrual periods, migraines, and rheumatoid arthritis. It may also be used to close a patent ductus arteriosus in a premature baby. It can be used by mouth or intravenously. It typically begins working within an hour.

<span class="mw-page-title-main">Diclofenac</span> Nonsteroidal anti-inflammatory drug

Diclofenac, sold under the brand name Voltaren, among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammatory diseases such as gout. It is taken by mouth or rectally in a suppository, used by injection, or applied to the skin. Improvements in pain last for as much as eight hours. It is also available in combination with misoprostol in an effort to decrease stomach problems.

<span class="mw-page-title-main">Naproxen</span> Nonsteroidal anti-inflammatory drug (NSAID) used to treat pain

Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain, menstrual cramps, inflammatory diseases such as rheumatoid arthritis, gout and fever. It is taken orally. It is available in immediate and delayed release formulations. Onset of effects is within an hour and lasts for up to twelve hours.

<span class="mw-page-title-main">Celecoxib</span> Nonsteroidal anti-inflammatory drug

Celecoxib, sold under the brand name Celebrex among others, is a COX-2 inhibitor and nonsteroidal anti-inflammatory drug (NSAID). It is used to treat the pain and inflammation in osteoarthritis, acute pain in adults, rheumatoid arthritis, ankylosing spondylitis, painful menstruation, and juvenile rheumatoid arthritis. It may also be used to decrease the risk of colorectal adenomas in people with familial adenomatous polyposis. It is taken by mouth. Benefits are typically seen within an hour.

COX-2 inhibitors are a type of nonsteroidal anti-inflammatory drug (NSAID) that directly targets cyclooxygenase-2, COX-2, an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and is the main feature of celecoxib, rofecoxib, and other members of this drug class.

<span class="mw-page-title-main">Indometacin</span> Anti-inflammatory drug

Indometacin, also known as indomethacin, is a nonsteroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling from inflammation. It works by inhibiting the production of prostaglandins, endogenous signaling molecules known to cause these symptoms. It does this by inhibiting cyclooxygenase, an enzyme that catalyzes the production of prostaglandins.

<span class="mw-page-title-main">Etoricoxib</span> Selective COX-2 Inhibitor

Etoricoxib, sold under the trade name Arcoxia, is a selective COX-2 inhibitor from McOLSON Research Laboratories. Currently it is approved in more than 80 countries worldwide but not in the US, where the Food and Drug Administration (FDA) has required additional safety and efficacy data for etoricoxib before it will issue approval.

<span class="mw-page-title-main">Oxaprozin</span> Chemical compound

Oxaprozin, also known as oxaprozinum, is a nonsteroidal anti-inflammatory drug (NSAID), used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis. Chemically, it is a propionic acid derivative. Safety and efficacy has been established in children over 6 years with juvenile rheumatoid arthritis only, and there is an increased risk of adverse reactions in the elderly population.

<span class="mw-page-title-main">Etodolac</span> Nonsteroidal Anti-Inflammatory Drug

Etodolac is a nonsteroidal anti-inflammatory drug (NSAID).

<span class="mw-page-title-main">Diflunisal</span> Nonsteroidal anti-inflammatory (NSAID), Used as an analgesic & anti inflammatory

Diflunisal is a salicylic acid derivative with analgesic and anti-inflammatory activity. It was developed by Merck Sharp & Dohme in 1971, as MK647, after showing promise in a research project studying more potent chemical analogs of aspirin. It was first sold under the brand name Dolobid, marketed by Merck & Co., but generic versions are now widely available. It is classed as a nonsteroidal anti-inflammatory drug (NSAID) and is available in 250 mg and 500 mg tablets.

<span class="mw-page-title-main">Zomepirac</span>

Zomepirac is an orally effective nonsteroidal anti-inflammatory drug (NSAID) that has antipyretic actions. It was developed by McNeil Pharmaceutical, approved by the FDA in 1980, and sold as the sodium salt zomepirac sodium, under the brand name Zomax. Due to its clinical effectiveness, it was preferred by doctors in many situations and obtained a large share of the analgesics market; however, it was subsequently withdrawn in March 1983 due to its tendency to cause serious anaphylaxis in a small, but unpredictable, subset of the patient population.

<span class="mw-page-title-main">Amtolmetin guacil</span> Chemical compound

Amtolmetin guacil is a non-steroidal anti-inflammatory drug (NSAID). It is a prodrug of tolmetin sodium.

<span class="mw-page-title-main">Meclofenamic acid</span> Chemical compound

Meclofenamic acid is a drug used for joint, muscular pain, arthritis and dysmenorrhea. It is a member of the anthranilic acid derivatives class of nonsteroidal anti-inflammatory drugs (NSAIDs) and was approved by the US FDA in 1980. Like other members of the class, it is a cyclooxygenase (COX) inhibitor, preventing the formation of prostaglandins.

<span class="mw-page-title-main">Fenoprofen</span> Chemical compound

Fenoprofen is a nonsteroidal anti-inflammatory drug (NSAID). Fenoprofen calcium is used for symptomatic relief for rheumatoid arthritis, osteoarthritis, and mild to moderate pain. It has also been used to treat postoperative pain. Fenoprofen is marketed in the US as Nalfon. It is available as a generic medication.

<span class="mw-page-title-main">Tenoxicam</span> Chemical compound

Tenoxicam, sold under the brand name Mobiflex among others, is a nonsteroidal anti-inflammatory drug (NSAID). It is used to relieve inflammation, swelling, stiffness, and pain associated with rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, tendinitis, bursitis, and periarthritis of the shoulders or hips.

<span class="mw-page-title-main">Acemetacin</span> Chemical compound

Acemetacin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis, rheumatoid arthritis, lower back pain, and relieving post-operative pain. It is manufactured by Merck KGaA under the tradename Emflex, and is available in the UK and other countries as a prescription-only drug.

<span class="mw-page-title-main">Axial spondyloarthritis</span> Medical condition

Axial spondyloarthritis is a chronic, autoinflammatory disease predominantly affecting the axial skeleton. The best-known member of the axial spondyloarthritis disease family is ankylosing spondylitis. Axial spondyloarthritis is an umbrella term that was introduced in 2009 to characterize a diverse disease family that share clinical and genetic features, such as the involvement of the axial skeleton. The expression was introduced in order to unify (1) less severe forms of spondylitis, (2) the early phase of ankylosing spondylitis as well as (3) ankylosing spondylitis itself into one term.

<span class="mw-page-title-main">Antiarthritics</span>

An antiarthritic is any member of the group of drugs used to relieve or prevent arthritic symptoms, such as joint pain and joint stiffness. Depending on the antiarthritic drug class, it can be responsible for managing pain, reducing inflammation and/or acting as an immunosuppressant. These drugs are typically given orally, topically or through administration by injection. The choice of antiarthritic medication is often determined by the type/nature of arthritis, the severity of symptoms as well as other factors, such as the tolerability of side effects.

<span class="mw-page-title-main">Glucametacin</span>

Glucametacin is a non-steroidal anti-inflammatory drug used for the treatment of mild or moderate pain associated with rheumatoid arthritis, osteoarthritis, and other rheumatological disorders. It has analgesic and anti-inflammatory effects.


  1. 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.
  2. 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.
  3. 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.
  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 (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.
  6. 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.
  7. "Tolmetin". DrugBank. Retrieved 2007-07-02.
  8. 1 2 "Tolmetin". MedlinePlus. Archived from the original on 2007-06-10. Retrieved 2007-07-02.
  9. 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. Retrieved 15 October 2020.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  10. 1 2 "NSAIDs may cause rare kidney problems in unborn babies". U.S. Food and Drug Administration. 21 July 2017. Retrieved 15 October 2020.PD-icon.svg This article incorporates text from this source, which is in the public domain .