Lexel

2.5 mg

Generic

Letrozole

Indications

Letrozole is used to treat advanced/metastatic breast cancer in postmenopausal women who have hormone receptor positive or unclear receptor status.

Dosage & Administration

The recommended dose of letrozole is 2.5 mg once a day. As long as a tumor response is observed, letrozole treatment should continue. If the tumor stops responding based on tumor progression, the drug should be discontinued. For elderly patients, there is no need to modify the normal adult dosing regimen. Patients with mild to moderate hepatic or renal insufficiency do not need to adjust the dose.

Interaction

Even though cimetidine is a known inhibitor of one of the cytochrome P450 isoenzymes capable of metabolizing letrozole in vitro, clinical interaction investigations with these medicines revealed that co-administration of letrozole with these treatments did not result in clinically significant drug responses.

Contraindications

Letrozole is contraindicated in patients known or suspected to be allergic to letrozole, other aromatase inhibitors, or any of their ingredients. It is contraindicated for pregnant, lactating and premenopausal women. It is also contraindicated for severe liver dysfunction.

Side Effects

Letrozole side effects are usually mild to moderate, and very rarely severe enough to need discontinuation. Many can be attributable to the underlying condition or the normal pharmacological effect of oestrogen deficiency (hot flushes, hair thinning). Musculoskeletal discomfort, arthralgia, headache, fatigue, nausea, dyspnoea, peripheral oedema, coughing, constipation, vomiting, chest pain, viral infection, diarrhoea, rash, stomach pain, dyspepsia, and anorexia are the most commonly reported adverse effects. Dizziness, weight gain, and pruritus are all less common symptoms.

Pregnancy & Lactation

At 0.03 mg/kg, oral treatment of letrozole to pregnant rats caused teratogenicity and maternal toxicity. At doses greater than 0.003 mg/kg, embryotoxicity and foetotoxicity were observed, as well as an increase in the incidence of foetal deformity in the animals treated. However, because there are no good and well-controlled studies of letrozole in pregnant women, it is not advised for usage in these individuals. Letrozole is not known to be excreted in human milk. Letrozole should not be given to a nursing mother because many medications are excreted in human milk.

Precautions & Warnings

There is no need to alter the dose for breast cancer patients with moderate hepatic impairment, although it is advised to proceed with caution because letrozole elimination is primarily based on internal metabolic clearance. At dosages of 2.5 mg and 5 mg, renal impairment (calculated creatinine clearance: 20 to 50 ml / min) has no effect on the steady-state plasma levels of letrozole. As a result, there is no need to change the dose for this form of kidney failure. Because of its poor binding to plasma proteins, letrozole is predicted to be eliminated from the blood by dialysis. The potential dangers and benefits for these patients should be carefully examined before taking letrozole.

Therapeutic Class

Hormonal Chemotherapy

Storage Conditions

Keep the temperature below 30°C and away from light and moisture. Keep out of children's reach.