Zoleta 2.5 mg

Description

Indications

• Adjuvant treatment for postmenopausal women with hormone receptor-positive early breast cancer.
• Extended adjuvant therapy for postmenopausal women with early breast cancer (positive or unknown estrogen or progesterone receptor status) after 5 years of adjuvant tamoxifen therapy.
• First-line treatment for postmenopausal women with hormone-dependent advanced breast cancer.
• Treatment of advanced breast cancer in women with postmenopausal status (natural or artificially induced) who have previously been treated with antioestrogens.
• Pre-operative therapy for localized hormone receptor-positive breast cancer in postmenopausal women, allowing subsequent breast-conserving surgery for women initially not considered candidates. Treatment after surgery should follow standard care protocols.
  Use as per the guidance of a registered physician.

Pharmacology
Mechanism of Action:
Letrozole is a potent, nonsteroidal aromatase inhibitor that competitively binds to the cytochrome P450 enzyme’s haem, inhibiting estrogen biosynthesis in all tissues. By suppressing estrogen levels, it deprives estrogen-dependent breast cancer cells of growth stimuli. In postmenopausal women, estrogens are mainly produced by aromatase, which converts adrenal androgens (androstenedione and testosterone) into estrone (E1) and estradiol (E2). Letrozole blocks this process, reducing estrogen levels in both peripheral and malignant tissues.

Letrozole has been shown to reduce serum estrone and estradiol by up to 78% in healthy postmenopausal women. In patients with advanced breast cancer, doses of 0.1 to 5 mg have reduced plasma estrogen concentrations by up to 95%. The drug does not accumulate androgenic precursors, as it does not affect plasma androgen concentrations.

Pharmacokinetics:
Letrozole is rapidly and completely absorbed with an absolute bioavailability of 99.9%. Food slightly delays absorption but does not affect the overall extent. Plasma protein binding is around 60%, mostly to albumin. Letrozole is metabolized primarily to an inactive carbinol metabolite. The apparent half-life is approximately 2 days, and steady-state levels are reached within 2 to 6 weeks after daily administration of 2.5 mg.

Dosage & Administration

• Adults and Elderly: The recommended dose is 2.5 mg once daily. In adjuvant and extended adjuvant settings, treatment should continue for 5 years or until tumor relapse. For metastatic disease, continue treatment until tumor progression. No dosage adjustment is necessary for elderly patients.
• Patients with Hepatic and/or Renal Impairment: No adjustment is required for mild to moderate hepatic or renal impairment. However, patients with severe hepatic impairment (Child-Pugh score C) should be closely monitored.

Drug Interactions
Co-administration with cimetidine and warfarin has shown no clinically significant interactions.

Contraindications

• Known hypersensitivity to letrozole, other aromatase inhibitors, or any of the ingredients.
• Pregnancy, lactation, and premenopausal women.
• Severe hepatic dysfunction.

Side Effects

• Common: Hot flashes, hypercholesterolemia, fatigue, increased sweating, bone and joint pain (arthralgia), skin rash, headache, dizziness, malaise, gastrointestinal disturbances (nausea, vomiting, constipation, diarrhea), loss or increase in appetite, muscle pain, osteoporosis, bone fractures, edema, depression, weight gain, hair loss, hypertension, abdominal pain, dry skin, vaginal bleeding, palpitations, joint stiffness, chest pain.
• Rare: Anxiety, nervousness, irritability, memory issues, somnolence, insomnia, carpal tunnel syndrome, eye disorders (blurred vision, irritation), urticaria, vaginal discharge or dryness, urinary tract infections, elevated liver enzymes, jaundice.

Pregnancy & Lactation

• Zoleta is contraindicated during pregnancy, as it has shown teratogenic effects in animal studies. It is not known if letrozole is excreted in human milk, so it should not be used in nursing women.

Precautions & Warnings

• Exercise caution in patients with moderate hepatic dysfunction.
• Renal impairment does not require dosage adjustments, but the potential for removal by dialysis should be considered.
• Fatigue and dizziness may impair the ability to operate machinery or drive.

Overdose Effects
There is no clinical experience with overdose. Zoleta is not highly protein-bound, so dialysis may be beneficial. Inducing emesis is recommended if the patient is alert. Supportive care and monitoring are key.

Therapeutic Class
Hormonal Chemotherapy

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

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