Company: Nordic Pharma Ireland.
Legal category: Prescription. High Tech. Sport permitted.
Active ingredients: Tegafur/gimeracil/oteracil 15/4.35/11.8mg, 20/5.8/15.8mg.
Description: Hard capsule with white body/brown cap or white body/white cap marked TC448 or TC442 respectively.
Presentation: 15mg-126, €382.50; 20mg-84, €340.00.
Indication: Treatment of advanced gastric cancer in combination with cisplatin.
Pharmacology: Following oral administration, tegafur is gradually converted into the anti-cancer substance 5-fluorouracil (5-FU), mainly by CYP2A6 enzyme activity in the liver. Gimeracil is a dihydropyrimidine dehydrogenase (DPD) inhibitor and prevents degradation of 5-FU by the body. Oteracil, an orotate phosphoribosyltransferase inhibitor, decreases the activity of 5-FU in normal gastrointestinal (GI) mucosa. The combination of tegafur, gimeracil and oteracil maintains 5-FU exposure and anti-tumour activity while reducing toxicity associated with 5-FU alone.
Dosage: Adult: Dose based on body surface area (BSA). Take at least 1 hour before or after food. Usually 25mg/m2 (expressed as tegafur content) twice daily for 21 consecutive days followed by 7 days rest (1 treatment cycle); repeat cycle every 4 weeks. With this regimen, administer 75mg/m2 cisplatin intravenously once every 4 weeks (discontinue cisplatin after 6 cycles). Modify dose based on BSA or toxicity, see SPC. Elderly: As per adults. Children: Under 18 years, safety and efficacy not established.
Contraindications: Hypersensitivity to any of the active substances or excipients. History of severe and unexpected reactions to fluoropyrimidine therapy. Known DPD deficiency. Severe bone marrow suppression. End stage renal disease patients requiring dialysis. Pregnancy, lactation.
Special precautions: Monitor closely and perform lab tests including haematology, liver function, renal function and serum electrolytes frequently. Discontinue if progressive disease or intolerable toxicity observed. Not recommended: Severe renal impairment. Treatment-related bone marrow suppression (including neutropaenia, leukopaenia, thrombocytopaenia, anaemia, pancytopaenia) reported. Monitor: For renal or ocular toxicity; patients with low white blood cell counts. Avoid dehydration. Diarrhoea or dehydration (≥Grade 2); suspend/adjust dose if occurs. Use adequate contraception (males and females) during and up to 6 months after discontinuation. Driving/using machines. Contains lactose.
Drug interactions: Contra: DPD inhibitors including sorivudine or brivudine (within 4 weeks), other fluoropyrimidines (minimum 7 days). Caution: Coumarin anticoagulants, folinic acid, nitromidazoles, methotrexate, clozapine, cimetidine, phenytoin. Avoid: CYP2A6 inhibitors, allopurinol.
Adverse drug reactions: Neutropenia, leukopenia, anaemia, thrombocytopenia, peripheral neuropathy, diarrhoea, vomiting, nausea, constipation, GI haemorrhage or inflammation, stomatitis, flatulence, abdominal pain or discomfort, dysphagia, dyspepsia, dry mouth, fatigue, febrile neutropenia, lymphopenia, anorexia, dehydration and electrolyte disorders, insomnia, dizziness, headache, dysgeusia, vision/lacrimal/corneal disorders, conjunctivitis, hearing impairment, hypotension, hypertension, deep vein thrombosis, dyspnoea, epistaxis, hiccups, cough, hyperbilirubinaemia, increased alanine aminotransferase or aspartate aminotransferase, Palmar-Plantar erythrodysesthesia, rash, skin hyperpigmentation, dry skin, pruritus, alopecia, musculoskeletal pain, renal failure, increased blood creatinine or urea, decreased glomerular filtration rate, mucosal inflammation, pyrexia, decreased weight, peripheral oedema, chills.
Full prescribing information and references available from Nordic Pharma Ireland. Telephone: (01) 4688997. Email: info@nordicpharma.ie