PHARMACOLOGICAL ACTION: TOLECTIN* 200 is an orally administered, non-steroidal anti-inflammatory agent with analgesic and antipyretic activity. TOLECTIN* 200 relieves pain and reduces swelling, tenderness and stiffness. In those patients responding to TOLECTIN* 200 therapy, subjective clinical improvement usually begins within one to two days after starting treatment. Objective improvement can normally be seen within two weeks.
The exact mode of action of TOLECTIN* 200 is not known but no effect on pituitary or adrenal function has been demonstrated either in animal or in human studies. The results of various animal tests suggest that TOLECTIN* 200 acts directly at the site of inflammation and not by reflex action or by release of a mediator substance. TOLECTIN* 200 is well absorbed and rapidly excreted; more than 80% of orally administered drug is excreted in the urine within 24 hours, while peak plasma levels are found 30-60 minutes after ingestion of the medicine.
TOLECTIN* 200 reduces the symptoms of specific inflammatory conditions, but does not alter the progressive course of the underlying disease.
CONTRA-INDICATIONS: TOLECTIN* 200 should not be used in patients in whom salicylates or other non-steroidal anti-inflammatory medicines produce hypersensitivity reactions. Patients who exhibit hypersensitivity to TOLECTIN* 200 should be withdrawn from therapy.
The safe use of TOLECTIN* 200 during pregnancy or lactation has not been established and is not recommended.
No teratogenic effects have been found in animals.
Because the safety and effectiveness have not been established in infants under 2 years of age, use of TOLECTIN* 200 is not recommended.
DOSAGE AND DIRECTIONS FOR USE:
Usual adult dosage The recommended starting dose of TOLECTIN* 200 is 1 200 mg daily in divided doses. Control is usually achieved at doses of 6001 800 mg/day in divided doses.
Doses larger than 2 000 mg/day have not been studied and are not recommended.
Usual children's dosage (2 years and older) The recommended starting dose is 20 mg/kg/day in divided doses three or four times per day. When control has been achieved, the usual dose ranges from 1530 mg/kg/day. Doses higher than 30 mg/kg/day have not been studied and therefore are not recommended.
Daily salicylate requirements can usually be reduced and often stopped once clinical response to TOLECTIN* 200 has been obtained.
TOLECTIN* 200 may be administered together with gold salts or corticosteroids in rheumatoid arthritis. Gastro-intestinal side-effects may be reduced by giving TOLECTIN* 200 with food or immediately after meals.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS: Headache, skin rash, dizziness, elevated blood pressure and oedema of the ankles have been reported. If headache persists despite dosage reduction, cessation of TOLECTIN* 200 therapy may be required. No sedation or euphoria has been observed during treatment with TOLECTIN* 200.
Anaphylactoid reactions may occur and should be treated with adrenalin, corticosteroids, aminophyllin and antihistamines.
Heartburn, epigastric discomfort, diarrhoea, nausea and vomiting as well as a positive stool guaiac test have been encountered.
Comparative studies in animals have shown that TOLECTIN* 200 should be given with extreme caution to patients with active gastric or duodenal ulcers, weighing the possible beneficial anti-inflammatory effects against possible aggravation of the peptic ulcer. TOLECTIN* 200 should be used with caution in patients with a history of upper gastro-intestinal tract disease.
Peptic ulceration and gastro-intestinal bleeding have been reported in patients receiving TOLECTIN* 200 therapy.
While no renal or hepatic toxicity has been observed during treatment with TOLECTIN* 200, patients with marked impairment of liver or kidney function should, on general principles, be closely monitored if TOLECTIN* 200 is administered and lower doses used.
TOLECTIN* 200 inhibits platelet function and prolongs bleeding time; therefore, patients who have pre-existing coagulation disorders should be carefully observed when TOLECTIN* 200 is administered.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT: Symptoms will probably be an aggravation of the adverse effects listed above. Treatment should be along conventional lines and such supportive therapy as indicated should be administered.
IDENTIFICATION: Off-white, round tablet 11,1 mm (7/16") in diameter, bevelled and scored on one face, hex-bevelled and engraved "McNEIL" on second face.
PRESENTATION: TOLECTIN* 200 is supplied as 200 mg tablets in 30's, 100's and 500's.
STORAGE INSTRUCTIONS: Keep out of reach of children. Store below 25°C.
REGISTRATION NUMBER: G/3.1/131
NAME AND BUSINESS ADDRESS OF APPLICANT: Janssen Pharmaceutica (Pty) Ltd
(Reg. No. 80/11122/07)