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| Clinical data | |
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| Trade names | Tolectin |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a681033 |
| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Eliminationhalf-life | 1-2 hours, next phase up to 5 hours |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.043.164 |
| Chemical and physical data | |
| Formula | C15H15NO3 |
| Molar mass | 257.289 g·mol−1 |
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Tolmetin (/ˈtɒlmətɪn/) is anonsteroidal anti-inflammatory drug (NSAID) of the heterocyclicacetic acid derivative class.
Tolmetin was originally approved by the US FDA in 1976. It is available internationally.[1]
It is used primarily to reduce hormones that cause pain, swelling, tenderness, and stiffness in conditions such asosteoarthritis andrheumatoid arthritis, includingjuvenile rheumatoid arthritis. In theUnited States it was marketed asTolectin and comes as a tablet or capsule.
Tolmetin is applicable in the treatment ofrheumatoid arthritis,[2][3]osteoarthrosis,[4][5] pain,[6] andankylosing spondylitis.[7]
Although themechanism of action of tolmetin is unknown, research involving humans and animals has shown that tolmetin does not achieve anti-inflammatory response by stimulation of theadrenal orpituitary gland, but it has shown tolmetin restrainsprostaglandin synthetasein vitro and reduces plasma levels ofprostaglandin E, possibly causing the anti-inflammatory response.
When tested in rats, tolmetin prevented experimentally stimulatedpolyarthritis and reduced inflammation. In patients with rheumatoid arthritis orosteoarthritis tolmetin was as effective asaspirin andindometacin, although the occurrence of mild gastrointestinaladverse effects andtinnitus was lower in patients treated with tolmetin than it was with aspirin-treated patients and the occurrence of adverse effects of thecentral nervous system was lower with tolmetin than it was with indomethacin.[8]
Tolmetin can increase the risk of heart or circulatory conditions such asheart attacks andstrokes. It should not be taken shortly before or aftercoronary artery bypass surgery.[9] 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 relievestomachaches that often occur.[9] Overdose can result in drowsiness,nausea, epigastric pain, and vomiting.
In October 2020, the U.S.Food and Drug Administration (FDA) required thedrug label to be updated for all nonsteroidalanti-inflammatory medications to describe the risk of kidney problems in unborn babies that result from low amniotic fluid.[10][11] They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy.[10][11]
This article incorporates text from this source, which is in thepublic domain. This article incorporates text from this source, which is in thepublic domain.| pyrazolones / pyrazolidines | |
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| salicylates | |
| acetic acid derivatives and related substances | |
| oxicams | |
| propionic acid derivatives (profens) |
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| n-arylanthranilic acids (fenamates) | |
| COX-2 inhibitors (coxibs) | |
| other | |
| NSAID combinations | |
Key:underline indicates initially developed first-in-class compound of specific group;#WHO-Essential Medicines;†withdrawn drugs;‡veterinary use. | |
