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Brand Name :
Tolectin
(United States) [Available]Synonyms :
tolmetin
Class :
Nonsteroidal anti-inflammatory drugs (NSAIDs)
Dosage Forms & Strengths
Capsule
400 mg
Tablet
200 mg
600 mg
Not more than 1800 mg each day
200 to 600 mg orally every eight hours
Not more than 1800 mg each day
200 to 600 mg orally every eight hours
Administration
Take with 8-to-12-ounce water to ignore gastro-intestinal effects
Dosage Forms & Strengths
Capsule
400 mg
Tablet
200 mg
600 mg
For more than 2 Years:
Initial dose of 20 to 30 mg/kg/day given orally divided into every 6 to 8 hours
Maintenance dose of 15-30 mg/kg/day divided into every 6 to 8 hours
For less than 2 years:
Safety and efficacy not determined
20-28 mg/kg/day orally divided every 6 hours
Administration
Take with 8-to-12-ounce water to ignore gastro-intestinal effects
Refer to adult dosing
the excretion rate of oxybenzone may be decreased by tolmetin, leading to increased serum levels of oxybenzone
interaction with NSAIDs may lead to increased toxicity such as myelosuppression, renal toxicity, and GI toxicity
interaction with NSAIDs may lead to increased toxicity such as myelosuppression, renal toxicity, and GI toxicity
When tolmetin is used together with bufexamac, this leads to enhanced risk or seriousness of adverse outcomes
May enhance the toxic effects of the other by pharmacodynamic synergism
May enhance the toxic effects of the other by pharmacodynamic synergism
May enhance the toxic effects of the other by pharmacodynamic synergism
May enhance the toxic effects of the other by pharmacodynamic synergism
May enhance the toxic effects of the other by pharmacodynamic synergism
may enhance the toxicity of the other through anti coagulation
may enhance the risk or severity of hypertension when combined
may have a decrease in excretion when combined with tolmetin
Actions and Spectrum:
tolmetin is a non-steroidal anti-inflammatory medicine (NSAID) that is used to treat pain and inflammation in several illnesses, including menstrual cramps, arthritis, and gout. It functions by preventing the body from producing prostaglandins, which are chemicals that induce pain and inflammation.
tolmetin has both analgesic (pain-relieving) and anti-inflammatory properties. It belongs to the same family of NSAIDs as ibuprofen and naproxen and works similarly to other medications in this group called propionic acids.
When used orally, the medication is quickly absorbed and reaches peak plasma concentrations in 1-2 hours. It is broken down in the liver and eliminated through the urine. Its activity lasts for around 6 to 8 hours.
Frequency Defined
<1%
Stevens-Johnson syndrome
Toxic epidermal necrolysis
Gastrointestinal hemorrhage
Thrombotic tendency observations
Erythema multiforme
Scaling eczema
Gastrointestinal perforation
Inflammatory disorder of digestive tract
Neutropenia
Thrombocytopenia
Jaundice
Agranulocytosis
Anemia
Liver failure
Hematuria
Proteinuria
Bronchospasm
Anaphylactoid reaction
Cerebrovascular accident
Acute renal failure
>10%
liver function test increased (up to 15%)
1-10%
Edema
Weight gain, Weight loss
Abdominal pain
Diarrhea
Nausea (10%)
Hypertension (3-9%)
Myocardial infarction (<2%)
Asthenia
Dizziness
Headache
Flatulence
Indigestion
Nausea, Vomiting
Black Box Warning
The elevated risk of potentially deadly cardiovascular events, including heart attack and stroke, is highlighted in the black box warning for tolmetin. Those who take tolmetin at greater dosages or for longer periods of time than advised, as well as those who have pre-existing cardiovascular disease or risk factors for it, may be at higher risk.
tolmetin is among the NSAIDs that the warning indicates can result in gastrointestinal bleeding, perforation and ulceration all of which can be deadly. Those having a history of gastrointestinal bleeding or ulcers and elderly people are at increased risk for these side effects.
Contraindication/Caution:
Contraindication:
Caution:
Pregnancy warnings:
Pregnancy category: C
Lactation: Excreted into human milk and safety in infants not known.
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
tolmetin is a non-steroidal anti-inflammatory medication (NSAID) with analgesic, antipyretic, and anti-inflammatory effects that can help with pain and inflammation. It functions by preventing the prostaglandin-producing enzyme cyclooxygenase (COX) from producing any new prostaglandins. Chemical mediators called prostaglandins encourage heat, discomfort, and inflammation.
Ibuprofen, naproxen, and tolmetin are all NSAIDs that belong to the propionic acid class. When administered orally, it is quickly absorbed and reaches peak plasma concentrations in one to two hours. The medication undergoes substantial liver metabolization and is eliminated in the urine.
Pharmacodynamics:
tolmetin inhibits both COX-1 and COX-2 enzymes since it is a non-selective COX inhibitor. A constitutive enzyme called COX-1 is involved in the synthesis of prostaglandins, which support the maintenance of regular physiological processes including maintaining the stomach lining and controlling blood flow to the kidneys.
Chemical mediators called prostaglandins have a role in the development of fever, discomfort, and inflammation. It further relieves pain, fever, and inflammation by inhibiting COX and lowering prostaglandin synthesis.
Pharmacokinetics:
Absorption
Peak plasma concentrations of tolmetin are obtained within 1-2 hours of oral treatment and are quickly absorbed. The medication has a high absolute bioavailability, with a 95% absorption from the gastrointestinal system.
Distribution
tolmetin has a very narrow volume of distribution and is well bound to plasma proteins, particularly albumin. The medication is absorbed into many tissues, including the synovial fluid, where it may build up to larger amounts than in the plasma.
Metabolism
tolmetin undergoes substantial oxidative and glucuronidation metabolization in the liver. Tolmetin’s principal metabolite, 5-hydroxytolmetin, is a potent COX inhibitor.
Elimination and excretion
tolmetin and its metabolites are largely excreted in the urine, and after 24 hours of dosing, 80–90% of the medication has been removed. Tolmetin has a relatively short elimination half-life of 2-3 hours, meaning that it leaves the body relatively fast.
Administration:
To lower the risk of gastrointestinal upset, tolmetin is normally taken orally with meals and is available as tablets. Depending on the patient’s reaction to the medication and the seriousness of the disease being treated, the dose may need to be changed.
Patient information leaflet
Generic Name: tolmetin
Why do we use tolmetin?
tolmetin is a non-steroidal anti-inflammatory medicine (NSAID) that is primarily used to treat the pain, swelling, and fever brought on by a number of illnesses, such as osteoarthritis, rheumatoid arthritis, dysmenorrhea, acute gout, ankylosing spondylitis