Tolectin

Tolectin - General Information

A non-steroidal anti-inflammatory agent (anti-inflammatory agents, NON-steroidal) similar in mode of action to indomethacin. [PubChem]

Pharmacology of Tolectin

Tolectin is a nonsteroidal anti-inflammatory agent. Studies in animals have shown tolmetin to possess anti-inflammatory, analgesic and antipyretic activity. In the rat, tolmetin prevents the development of experimentally induced polyarthritis and also decreases established inflammation. In patients with either rheumatoid arthritis or osteaoarthritis, tolmetin is as effective as aspirin and indomethacin in controlling disease activity, but the frequency of the milder gastrointestinal adverse effects and tinnitus was less than in aspirin-treated patients, and the incidence of central nervous system adverse effects was less than in indomethacin-treated patients. In patients with juvenile rheumatoid arthritis, tolmetin is as effective as aspirin in controlling disease activity, with a similar incidence of adverse reactions. tolmetin has produced additional therapeutic benefit when added to a regimen of gold salts and, to a lesser extent, with corticosteroids. Tolectin should not be used in conjunction with salicylates since greater benefit from the combination is not likely, but the potential for adverse reactions is increased.

Tolectin for patients

TOLECTIN, like other drugs of its class, is not free of side effects. The side effects of these drugs can cause discomfort and, rarely, there are more serious side effects, such as gastrointestinal bleeding, which may result in hospitalization and even fatal outcomes.

NSAID's (Nonsteroidal Anti-Inflammatory Drugs) are often essential agents in the management of arthritis, but they also may be commonly employed for conditions which are less serious.

Physicians may wish to discuss with their patients the potential risks and likely benefits of NSAID treatment, particularly when the drugs are used for less serious conditions where treatment without NSAID's may represent an acceptable alternative to both the patient and physician.

Tolectin Interactions

The in vitro binding of warfarin to human plasma proteins is unaffected by tolmetin, and tolmetin does not alter the prothrombin time of normal volunteers. However, increased prothrombin time and bleeding have been reported in patients on concomitant TOLECTIN and warfarin therapy. Therefore, caution should be exercised when administering TOLECTIN to patients on anticoagulants.

In adult diabetic patients under treatment with either sulfonylureas or insulin there is no change in the clinical effects of either TOLECTIN or the hypoglycemic agents.

Caution should be used if TOLECTIN is administered concomitantly with methotrexate. TOLECTIN and other nonsteroidal anti-inflammatory drugs have been reported to reduce the tubular secretion of methotrexate in an animal model, possibly enhancing the toxicity of methotrexate.

Laboratory Tests

Because serious GI tract ulceration and bleeding can occur without warning symptoms, physicians should follow chronically treated patients for the signs and symptoms of ulceration and bleeding and should inform them of the importance of this follow-up.

Tolectin Contraindications

Anaphylactoid reactions have been reported with TOLECTIN as with other nonsteroidal anti-inflammatory drugs. Because of the possibility of cross-sensitivity to other nonsteroidal anti-inflammatory drugs, particularly zomepirac sodium, anaphylactoid reactions may be more likely to occur in patients who have exhibited allergic reactions to these compounds. For this reason, TOLECTIN should not be given to patients in whom aspirin and other nonsteroidal anti-inflammatory drugs induce symptoms of asthma, rhinitis, urticaria and other symptoms of allergic or anaphylactoid reactions. Patients experiencing anaphylactoid reactions on TOLECTIN should be treated with conventional therapy, such as epinephrine, antihistamines and/or steroids.

Additional information about Tolectin

Tolectin Indication: For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis, including the treatment of acute flares long-term management. Also for treatment of juvenile rheumatoid arthritis.
Mechanism Of Action: The mode of action of tolmetin is not known. However, studies in laboratory animals and man have demonstrated that the anti-inflammatory action of tolmetin is not due to pituitary-adrenal stimulation. Tolectin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action. Tolectin does not appear to alter the course of the underlying disease in man.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Tolmetin
Synonyms: Tolmetine [INN-French]; Tolmetino [INN-Spanish]; Tolmetinum [INN-Latin]; Tolmetina [DCIT]; Tolmetin Sodium
Drug Category: Anti-Inflammatory Agents, Non-Steroidal; Cyclooxygenase Inhibitors
Drug Type: Small Molecule; Approved

Other Brand Names containing Tolmetin: Tolectin; Tolectin DS;
Absorption: Rapidly and almost completely absorbed with peak plasma levels being reached within 30-60 minutes after an oral therapeutic dose.
Toxicity (Overdose): Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain.
Protein Binding: Not Available
Biotransformation: Essentially all of the administered dose is recovered in the urine in 24 hours either as an inactive oxidative metabolite or as conjugates of tolmetin.
Half Life: Biphasic elimination from the plasma consisting of a rapid phase with a half-life of one to 2 hours followed by a slower phase with a half-life of about 5 hours.
Dosage Forms of Tolectin: Capsule Oral
Tablet Oral
Chemical IUPAC Name: 2-[1-methyl-5-(4-methylbenzoyl)pyrrol-2-yl]acetic acid
Chemical Formula: C15H15NO3
Tolmetin on Wikipedia: https://en.wikipedia.org/wiki/Tolmetin
Organisms Affected: Humans and other mammals