Letrozol 2.5mg Tablet | Letrozol | 10pcs
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Home Medicines Hormonal Therapy Letrozol 2.5mg Tablet 5pcs

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Letrozol 2.5mg Tablet 5pcs

Generic: Letrozole

Type: Tablet

Pack Size: 5 Pcs

Letrozole is a potent, nonsteroidal aromatase inhibitor that reduces estrogen biosynthesis by competitively inhibiting the aromatase enzyme. This deprives estrogen-dependent breast cancer cells of their growth stimulus.

  • In Postmenopausal Women: Estrogens are synthesized by aromatase converting adrenal androgens (androstenedione, testosterone) to estrone (E1) and estradiol (E2). Letrozole effectively suppresses estrogen levels without affecting androgen levels.
  • Suppression Rates: Single doses (0.1–2.5 mg) suppress serum estrone and estradiol by 75–78%, achieving maximum suppression within 48–78 hours.

Pharmacokinetics:

  • Absorption: Rapid, complete absorption (bioavailability ~99.9%). Food delays absorption slightly without affecting clinical relevance.
  • Protein Binding: ~60% (primarily to albumin).
  • Metabolism: Converted to an inactive carbinol metabolite primarily by CYP3A4 and CYP2A6.
  • Half-Life: ~2 days.
  • Steady State: Achieved within 2–6 weeks of daily 2.5 mg administration.

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✅ Description:

Pack Image of Pack Image: Letrozol 2.5 mg Tablet (2 x 14)
Adjuvant Treatment: Postmenopausal women with hormone receptor-positive early breast cancer. Extended Adjuvant Therapy: Postmenopausal women with early breast cancer (positive or unknown estrogen/progesterone receptor status) after completing 5 years of adjuvant tamoxifen therapy. First-Line Therapy: Hormone-dependent advanced breast cancer in postmenopausal women. Advanced Breast Cancer: Treatment for postmenopausal women with natural or induced menopausal status who have previously been treated with antiestrogens. Pre-Operative Therapy: Localized hormone receptor-positive breast cancer in postmenopausal women to enable breast-conserving surgery for non-candidates initially. Post-surgery treatment should follow standard care protocols.
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✔️ Side Effects of Letrozol 2.5

Common:

  • Hot flashes, hypercholesterolemia, fatigue, sweating, arthralgia, rash, headache, dizziness, malaise.
  • Gastrointestinal disturbances: nausea, vomiting, constipation, diarrhea, abdominal pain.
  • Musculoskeletal issues: osteoporosis, joint pain/stiffness, fractures.
  • Edema, depression, weight gain, hypertension, vaginal bleeding.

Rare:

  • Anxiety, insomnia, memory issues, somnolence, blurred vision, skin irritation, carpal tunnel syndrome, urinary tract infections, and increased liver enzymes.
✔️ Dosage & Administration of Letrozol 2.5

Adults and Elderly:

  • Standard Dose: 2.5 mg once daily.
  • Adjuvant/Extended Therapy: Continue for 5 years or until tumor relapse.
  • Metastatic Disease: Continue until tumor progression.

Hepatic/Renal Impairment:

  • No dosage adjustment is required for moderate hepatic or renal impairment (creatinine clearance ≥10 mL/min).
  • Patients with severe hepatic impairment (Child-Pugh score C) require close monitoring.

Children: Not applicable.

✔️ Interaction
  • Co-administration with cimetidine or warfarin does not result in clinically significant interactions.
  • Letrozole is metabolized by CYP3A4 and CYP2A6, but inhibitors of these enzymes have not shown significant interactions.
✔️ Contraindications
  • Hypersensitivity to Letrozole or other aromatase inhibitors.
  • Pregnancy, lactation, and premenopausal women.
  • Severe hepatic dysfunction.
✔️ Overdose Effects of Letrozol 2.5
  • Clinical Experience: Limited data on overdosage.
  • Management: Supportive care, monitoring of vital signs, and emesis induction if alert. Dialysis may be considered due to low protein binding.
✔️ Pregnancy & Lactation
  • Pregnancy: Category X. Studies in animals indicate teratogenic effects and fetal toxicity. Use in pregnant women is contraindicated.
  • Lactation: It is unknown if letrozole is excreted in breast milk. Due to potential adverse effects on the infant, nursing is contraindicated during therapy.
✔️ Precautions & Warnings
  • Hepatic Impairment: Exercise caution in patients with moderate hepatic dysfunction.
  • Renal Impairment: No dose adjustment is needed for creatinine clearance ≥10 mL/min.
  • Driving/Operating Machinery: Fatigue and dizziness may impair abilities; patients should be warned.
✔️ Storage Conditions

Store below 30°C, away from light and moisture. Keep out of reach of children.

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