Letrozole

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Generic Name of Letrozole - Learn More

Letrozole

Letrozole Precaution - What You Need to Know

Before starting Letrozole, it is essential for patients to consult their healthcare provider due to the following precautions:

- Hormone-sensitive cancers: Letrozole is used to treat hormone receptor-positive breast cancer, but it should be avoided in patients with hormone receptor-negative breast cancer, as it will not be effective in those cases.
- Osteoporosis and Bone Health: Letrozole may lead to a decrease in bone mineral density, increasing the risk of osteoporosis and bone fractures. Patients at risk for bone issues should be monitored regularly, and prophylactic measures, like calcium and vitamin D supplementation, should be considered.
- Liver Disease: Since Letrozole is metabolized in the liver, it should be used with caution in patients with liver impairment. Liver function tests should be conducted before starting treatment and periodically thereafter.
- Cardiovascular Disease: Caution is advised in patients with pre-existing cardiovascular conditions because the use of Letrozole may exacerbate certain heart conditions.
- Pregnancy and Breastfeeding: Letrozole is contraindicated in pregnancy due to its potential to harm a developing fetus. It should not be used during breastfeeding either, as it may pass into breast milk and affect the infant.
- Use in Pre-menopausal Women: Letrozole is generally not recommended for pre-menopausal women unless they have had a surgical menopause (i.e., removal of ovaries) or are undergoing ovarian suppression therapy.

Letrozole Indication - Uses and Benefits

Letrozole is primarily used to treat certain types of hormone receptor-positive breast cancer, including:

- Breast Cancer: Letrozole is used as a first-line treatment for early-stage hormone receptor-positive breast cancer in postmenopausal women. It is also used for advanced breast cancer and in cases where other treatments (such as tamoxifen) have failed.
- Adjuvant Therapy: After primary treatment such as surgery, Letrozole can be prescribed to reduce the risk of recurrence in postmenopausal women with early-stage, hormone receptor-positive breast cancer.
- Metastatic Breast Cancer: In cases of advanced breast cancer, especially in postmenopausal women, Letrozole helps slow the progression of the disease.
- Fertility Issues: In some cases, Letrozole is used off-label to treat infertility in women by stimulating ovarian function, especially in women with conditions like polycystic ovary syndrome (PCOS).

Letrozole Contraindications - Important Warnings

Letrozole is contraindicated in the following situations:

- Pregnancy: Letrozole is contraindicated during pregnancy due to the risk of birth defects and harm to the fetus. Women should avoid becoming pregnant during treatment with Letrozole, and it should be discontinued immediately if pregnancy occurs.
- Breastfeeding: It is contraindicated in breastfeeding women, as it may harm the infant. Letrozole passes into breast milk, and its effects on a breastfeeding child are unknown.
- Pre-menopausal Women: It should not be used in pre-menopausal women unless they are undergoing ovarian suppression. In these women, ovarian estrogen production is still significant, and Letrozole would be ineffective.
- Hypersensitivity: Patients who have known hypersensitivity to Letrozole or any of its components should avoid its use.
- Severe Liver Impairment: It is contraindicated in patients with severe hepatic impairment (i.e., cirrhosis or active liver disease), as the metabolism of Letrozole may be significantly affected.

Letrozole Side Effects - What to Expect

Letrozole may cause both common and serious side effects:

- Common Side Effects:
- Hot flashes and flushing are the most frequently reported side effects, due to the reduction in estrogen levels.
- Joint pain and muscle pain may occur, which can interfere with daily activities and mobility.
- Fatigue and tiredness are also commonly experienced.
- Nausea and vomiting are occasionally seen in patients taking Letrozole.
- Headaches and dizziness may occur in some patients.
- Weight gain and swelling in the hands or feet can also be side effects.
- Bone thinning (osteoporosis) and fractures are long-term risks due to the reduction in estrogen levels.

- Severe Side Effects:
- Liver toxicity: Elevated liver enzymes have been reported, indicating liver dysfunction. Liver function should be monitored.
- Bone fractures: As Letrozole reduces estrogen levels, bone mineral density may decrease, leading to an increased risk of fractures, especially in postmenopausal women.
- Severe allergic reactions: These may include swelling of the face or throat, difficulty breathing, and hives.
- Vaginal bleeding or spotting may occur, especially in women who have been on hormone therapy for a long time.
- Osteoporosis-related fractures due to the loss of bone density should be monitored, and calcium and vitamin D supplementation may be required.

Letrozole Pregnancy Category ID - Safety Information

5

Letrozole Mode of Action - How It Works

Letrozole is an aromatase inhibitor that works by blocking the enzyme aromatase, which converts androgens (male hormones) into estrogen in peripheral tissues (such as fat). Estrogen plays a crucial role in the growth and spread of many types of breast cancer that are estrogen receptor-positive (ER-positive). By inhibiting aromatase, Letrozole reduces the amount of estrogen available to these cancer cells, thereby slowing or stopping their growth. This action is particularly effective in postmenopausal women, where ovarian estrogen production is minimal, and the peripheral conversion of androgens to estrogen becomes a primary source.

Letrozole Drug Interactions - What to Avoid

Letrozole may interact with other medications, potentially affecting its efficacy or causing harmful effects:

- Estrogen-containing Medications: Since Letrozole works by blocking the production of estrogen, any drugs containing estrogen (e.g., hormonal contraceptives, hormone replacement therapy) may reduce its effectiveness. Women on Letrozole should avoid estrogen supplements.
- CYP3A4 Inhibitors: Medications that inhibit the CYP3A4 enzyme (e.g., ketoconazole, clarithromycin) may increase Letrozole levels in the blood, potentially leading to increased side effects. Dose adjustments may be necessary when using these drugs together.
- CYP3A4 Inducers: On the flip side, drugs that induce CYP3A4 (e.g., rifampicin, phenytoin) may lower Letrozole levels, reducing its effectiveness.
- Warfarin: Warfarin and other anticoagulants should be monitored closely if used in combination with Letrozole, as there may be an increased risk of bleeding or altered clotting.

Letrozole Adult Dose - Recommended Dosage

The usual adult dose of Letrozole for breast cancer treatment is:

- For Early-Stage Breast Cancer: 2.5 mg once daily as adjuvant therapy for postmenopausal women.
- For Advanced or Metastatic Breast Cancer: 2.5 mg once daily. The treatment is typically continued until disease progression or unacceptable side effects.
- For Fertility Induction (off-label): 2.5 to 5 mg once daily, taken for 5 days starting on day 3 to 5 of the menstrual cycle.

Letrozole Child Dose - Dosage for Children

Letrozole is not approved for use in children, and its safety and efficacy have not been established in pediatric populations.

As always, patients should consult with their healthcare provider before starting Letrozole to ensure proper dosing and monitoring throughout treatment.

Letrozole Renal Dose - Dosage for Kidney Conditions

No dosage adjustment of Letrozole is necessary for patients with mild to moderate renal impairment (creatinine clearance >10 mL/min). However, Letrozole has not been studied in patients with severe renal impairment (creatinine clearance <10 mL/min), so caution is recommended in these patients.