Tegonat 20 — Tegafur, Gimeracil & Oteracil Capsules, 42 Caps · Tegafur / Gimeracil / Oteracil

Tegonat 20 is supplied as hard gelatin capsules.

Qualitative and Quantitative Composition per Capsule:

• Active Ingredients:
  • — Tegafur — 20 mg.
  • — Gimeracil — 5.8 mg.
  • — Oteracil potassium — 19.6 mg.
• Excipients: Lactose monohydrate, magnesium stearate, talc, capsule shell components (gelatin, titanium dioxide, colorants).

Packaging and Presentation: Hard gelatin capsules containing powder or granules. 7 capsules per blister strip. 6 blister strips (total 42 capsules) are packaged in an outer carton displaying Tegonat 20 (Tegafur, Gimeracil and Oteracil Capsules) along with Natco Pharma corporate graphics and official prescribing information.

Pharmacodynamics:
Tegonat combines three active agents. Tegafur is converted into 5-fluorouracil (5-FU), inhibiting DNA synthesis and cell division via thymidylate synthase blockade. Gimeracil prevents hepatic DPD degradation of 5-FU, maintaining therapeutic exposure. Oteracil potassium reduces GI phosphorylation of 5-FU, lessening gastrointestinal toxicity without impairing antitumor efficacy.

Pharmacokinetics:

• Absorption: All three components are rapidly and almost completely absorbed from the GI tract. Peak plasma concentration ($C_{max}$) is reached within 1–2 hours.
• Distribution: Plasma protein binding of tegafur is minimal (~4–7%); gimeracil and oteracil binding is similarly low. Volume of distribution is adequate for tissue penetration.
• Metabolism: Tegafur is metabolized in the liver to 5-FU primarily via CYP2A6 cytochrome P450 isoenzymes. Gimeracil and oteracil are excreted mostly unchanged.
• Elimination: Excreted predominantly renally via urine. Terminal elimination half-life ($T_{1/2}$) of tegafur is approximately 7–10 hours.

Tegonat 20 is indicated in adult patients for:

• Gastric Cancer: Treatment of unresectable or recurrent/metastatic gastric cancer (as monotherapy or combination regimens).
• Colorectal Cancer: Adjuvant treatment of colon cancer following radical surgery, as well as metastatic colorectal cancer.
• Head and Neck Cancer: Treatment of squamous cell carcinoma of the head and neck.
• Breast and Non-Small Cell Lung Cancer: Utilized per oncology protocols in combination regimens.

Tegonat 20 is administered orally twice daily (morning and evening), approximately 30 minutes after a meal.

Dosing Regimen:
Dosage is calculated individually by the attending oncologist based on the patient's body surface area (BSA) (based on the tegafur content):

• BSA < 1.25 m²: 40 mg (tegafur equivalent) twice daily.
• BSA 1.25 to < 1.5 m²: 50 mg twice daily.
• BSA ≥ 1.5 m²: 60 mg twice daily.

Standard Schedule: Administered daily for 28 consecutive days followed by a 14-day rest period (42-day cycle). This cycle is repeated as prescribed.

Administration of Tegonat 20 is contraindicated in:

• Hypersensitivity: Known hypersensitivity to tegafur, gimeracil, oteracil potassium, or any excipient.
• Severe Bone Marrow Suppression: Severe leukopenia, neutropenia, or thrombocytopenia.
• Severe Renal Impairment: Creatinine clearance < 30 ml/min.
• Severe Hepatic Impairment: Pronounced hepatic dysfunction.
• Concurrent Medications: Co-administration with other fluoropyrimidines or sorivudine/brivudine (severe life-threatening drug interaction).
• Pregnancy and Lactation: Contraindicated in pregnant or breastfeeding women.

Evaluated drug interactions include:

• Other Fluoropyrimidines (capecitabine, 5-fluorouracil): Strict contraindication due to severely amplified toxicity.
• Antiviral Agents (sorivudine, brivudine): Inhibit DPD enzymes, leading to massive accumulation of 5-FU and potentially fatal toxicity. Tegegonat must not be initiated within 4 weeks of sorivudine or brivudine cessation.
• Phenytoin: Tegafur may increase plasma phenytoin concentrations, elevating toxicity risks. Monitoring is required.

Pregnancy:
Tegonat 20 is contraindicated during pregnancy due to teratogenic and embryo-fetal toxicity risks. Women of childbearing potential must use effective contraception during treatment and post-therapy.

Lactation:
Excretion into breast milk is unstudied. Breastfeeding must be discontinued during treatment.

The most frequent and clinically significant adverse reactions include:

• Gastrointestinal Tract: Stomatitis, diarrhea, nausea, vomiting, anorexia, abdominal pain (GI toxicity is mitigated by oteracil but remains notable).
• Hematologic Toxicity: Leukopenia, neutropenia, anemia, thrombocytopenia. Regular complete blood counts are mandatory.
• Hepatic & Renal Parameters: Elevations in transaminases (ALT, AST), bilirubin, and serum creatinine.
• Skin & Appendages: Skin hyperpigmentation, alopecia, hand-foot syndrome (palmar-plantar erythrodysesthesia).
• General Disorders: Fatigue, asthenia, pyrexia.

Symptoms:
Overdose manifests as exaggerated adverse reactions: severe myelosuppression (profound leukopenia, thrombocytopenia), severe stomatitis, diarrhea, nausea, vomiting, and mucosal ulceration.

Treatment:
No specific antidote exists. Supportive and symptomatic care should be initiated, including hospitalization, hematologic monitoring, blood component transfusions, and colony-stimulating factors if indicated.

Storage Requirements for Tegonat 20:

• 🌡️ Temperature Range: Store in a dry, light-protected place at temperatures not exceeding 25–30 °C.
• 💧 Moisture Protection: Keep in original blister packaging to protect capsules from moisture.
• 👶 Safety Precautions: Keep strictly out of reach of children.
• ⏳ Shelf Life: Stated on carton and blisters. Do not use past expiration date. Prescription-only hospital medicine.

To verify authenticity of genuine Tegonat 20 manufactured by Natco Pharma, inspect the following features:

• ✅ Corporate Logo: Distinctive blue-green Natco Pharma corporate logo printed on the outer carton and blister foil.
• ✅ Packaging Markings: Clear factory printing displaying Batch No., Mfg. Date, Exp. Date, and product designation Tegonat 20 (Tegafur, Gimeracil and Oteracil Capsules).
• ✅ Blister Quantity: Standard box contains exactly 6 blister strips of 7 capsules each (total 42 capsules).
• ✅ Print Quality: High-grade packaging artwork without color fading or typography errors.