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 belongs to the non-steroidal compound class, capable of regulating 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 commercial names, but the generic name Letrozole is universally recognized. The medication is supplied in tablet form, typically as a 2.5 mg dose.
Letrozole is classified as a non-steroidal aromatase inhibitor within the subclass of aromatase inhibitors, alongside anastrozole and exemestane. Its chemical structure and mechanism of action differ from anti-estrogen drugs like tamoxifen, specifically targeting estrogen synthesis pathways.
Main indications include:
This medication is also used for hormone receptor-positive tumors, but requires 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, due to the risk of fetal abnormalities. Patients with severe hepatic or renal impairment should have dose adjustments. Breastfeeding women should also avoid use.
Black box warning includes 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 markers.
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 co-administration with gastric acid suppressants like omeprazole, as they may affect absorption. 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 duration is 5 years, and adherence to the prescribed course is essential.
Dosage adjustments: Patients with severe hepatic impairment should have reduced doses; caution is advised in patients with 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, take it as soon as possible. If it is close to the next scheduled 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, consider taking medication separately from these drinks. Adequate intake of vitamin D and calcium is advised to reduce the risk of bone density loss.
How can I relieve joint pain or bone discomfort caused by Letrozole?Low-impact exercises such as swimming or walking can help improve joint stiffness. Avoid high-impact activities. Your doctor may recommend short-term use of NSAIDs like ibuprofen, but check for interactions first. Physical therapy or warm compresses can also help alleviate localized discomfort.
What precautions should be taken when combining Letrozole with other medications?If taken with liver enzyme inducers like carbamazepine, efficacy may decrease; inform your doctor of all medications, including herbal supplements. When combined with anticoagulants like warfarin, regular blood clotting monitoring is necessary. Do not adjust doses without medical advice.
How should I monitor changes in bone density during treatment?Bone density scans (DEXA) are recommended every 6 to 12 months, especially if treatment exceeds 2 years. Report any unexplained back pain, height loss, or fractures immediately. Regular weight-bearing exercise and calcium supplementation can help reduce osteoporosis risk, under medical guidance.
What should I do if I miss a dose of Letrozole?If you remember within the same day, take the missed dose immediately. If it is close to the next dose, skip the missed dose and continue with your regular schedule. Do not double doses. Frequent missed doses can affect treatment efficacy; consider setting reminders or using a medication organizer and communicate with your healthcare team regularly.
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