Letrozole is a selective aromatase inhibitor primarily used in the treatment of hormone receptor-positive breast cancer. This medication works by inhibiting the activity of aromatase, thereby reducing estrogen levels in the body and suppressing tumor growth. It is widely used as adjuvant therapy in postmenopausal women with early breast cancer and for the treatment of advanced or metastatic breast cancer.
Letrozole’s pharmacological mechanism differs from other aromatase inhibitors; it is a non-steroidal compound that modulates estrogen metabolism pathways. Clinical trials have confirmed its significant efficacy in reducing the risk of cancer recurrence, making it a first-line hormonal therapy option.
The generic name is "Letrozole," with the main brand being "Femara." Different countries may have other brand names, but the generic name Letrozole is universally recognized. The medication is supplied in tablet form, typically as a 2.5 mg dose.
Letrozole belongs to the subclass of "Aromatase Inhibitors" within non-steroidal drugs, similar to anastrozole and exemestane. Its chemical structure and mechanism of action differ from anti-estrogen drugs like tamoxifen, focusing specifically on inhibiting estrogen synthesis pathways.
Main indications include:
This medication is also used for hormone receptor-positive tumors, with regular imaging and blood tests for monitoring. In certain cases, it may be combined with chemotherapy or targeted therapy.
Mild side effects include:
Severe side effects require immediate medical attention:
Contraindications: Absolute contraindication in pregnant women or women who may become pregnant, as it may cause fetal abnormalities. Patients with severe hepatic or renal impairment should have dosage adjustments, and breastfeeding women should avoid use.
Black box warnings include the risk of decreased bone mineral density; bone density should be checked before and after treatment. If unexplained bone pain or fractures occur during therapy, medication should be discontinued and medical advice sought. Patients over 65 require special monitoring of bone metabolism indices.
Use with CYP2C19 enzyme inducers (e.g., carbamazepine) may reduce efficacy, requiring dose adjustments. Combining with bisphosphonates can reduce bone loss; inform your healthcare provider if you are on osteoporosis treatment. Avoid concurrent use with gastric acid suppressants like omeprazole, as absorption may be affected. Vitamin D and calcium supplements should be used under medical supervision to mitigate osteoporosis risk.
The standard dose is 2.5 mg orally once daily, taken with or without food. Take at the same time each day to maintain stable drug levels. The typical treatment cycle lasts for 5 years, and adherence to the full course as prescribed by the physician is essential.
Dosage adjustments: Patients with severe hepatic impairment should have reduced doses; caution is advised in patients with a creatinine clearance below 30 ml/min. Do not alter the dose without medical consultation; adjustments should be made by an oncologist.
If a dose is missed and remembered within 12 hours of the scheduled time, take it as soon as possible. If it is close to the next dose, skip the missed dose and resume the regular schedule. Do not double doses to compensate for missed ones.
Acute overdose may cause severe bone pain, arrhythmias, or liver dysfunction. If overdose is suspected, seek immediate medical attention and bring the medication container. Treatment is supportive, possibly including dialysis or symptomatic management.
It is recommended to avoid excessive intake of high-fat or greasy foods, as they may affect drug absorption. Coffee, tea, and other caffeinated beverages can be consumed normally, but if gastrointestinal discomfort occurs, it is advisable to take the medication separately from these drinks. Adequate intake of vitamin D and calcium is recommended to help mitigate bone density loss.
How can joint pain or bone discomfort caused by Letrozole be alleviated?Low-impact exercises such as swimming and walking can improve joint stiffness. Avoid high-impact activities. Your doctor may suggest short-term use of NSAIDs like ibuprofen, but check for drug interactions first. Physical therapy or warm compresses can also help relieve localized discomfort.
What precautions should be taken when combining Letrozole with other medications?If used with hepatic enzyme inducers like carbamazepine, efficacy may decrease; inform your doctor of all medications, including herbal supplements. When combined with anticoagulants such as warfarin, regular blood coagulation monitoring is necessary. Do not adjust doses without medical guidance.
How should bone density be monitored during treatment?Bone density scans (DEXA) should be performed every 6 to 12 months, especially if treatment exceeds 2 years. Report any unexplained back pain, height loss, or fractures immediately. Regular weight-bearing exercises and calcium supplementation can reduce osteoporosis risk, but follow your doctor’s instructions.
What should be done if a dose of Letrozole is missed?If missed and remembered on the same day, take it immediately. If close to the next scheduled dose, skip the missed dose and continue with the regular schedule. Do not double doses. Frequent missed doses may affect treatment efficacy; consider setting reminders or using a medication organizer, and communicate regularly with your healthcare team.
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