Lestrodex, 2,5mg 30 pcs.

Letrozole has anti-estrogenic effect, it selectively inhibits aromatase (enzyme of estrogen synthesis) by a highly specific competitive binding to the subunit of this enzyme – cytochrome P450 heme. It blocks estrogen synthesis both in peripheral and tumor tissues.

Indications

– early stages of breast cancer whose cells have hormone receptors in postmenopausal women as adjuvant therapy;

– early stages of breast cancer in postmenopausal women after completion of standard adjuvant tamoxifen therapy as extended adjuvant therapy;

– common hormone-dependent breast cancer in postmenopausal women (first-line therapy);

– common breast cancer in postmenopausal women (natural or induced) who received prior anti-estrogen therapy.

Active ingredient

Composition

How to take, the dosage

Orally, regardless of meals.

The recommended dose of Lestrodex is 2.5 mg once daily.

For extended adjuvant therapy, treatment should be continued for 5 years or until signs of disease progression.

In patients with advanced or metastatic cancer, treatment with Lestrodex should be continued until clear progression of the tumor.

Dose adjustment is not required for older patients.

Patients with impaired hepatic and/or renal function: No dose adjustment is required for hepatic or renal impairment (CK greater than 10 ml/min).

There is insufficient data when using the drug in patients with CKD less than 10 ml/min or in patients with severe liver dysfunction (grade C on the Child-Pugh scale). Continuous monitoring of this group of patients is required during therapy with Lestrodex.

Interaction

Clinical experience on the use of letrozole in combination with other anticancer agents is currently not available.

According to the results of in vitro studies letrozole inhibits the activity of cytochrome Р450 isoenzymes CYP2A6 and to a moderate extent – CYP2C19.

Cautious use of letrozole with drugs that are metabolized primarily with the participation of the above mentioned isoenzymes and have a narrow therapeutic index should be observed.

Special Instructions

In patients whose postmenopausal status is unclear, determination of luteinizing hormone, follicle-stimulating hormone, and/or estradiol concentrations is recommended before initiating treatment to confirm menopausal status.

Renal dysfunction

There are insufficient data on the use of letrozole in patients with a CK of less than 10 ml/min. The ratio of potential risk to expected benefit should be assessed in patients with a CKG of less than 10 mL/min.

Hepatic impairment

Lestrodex should be used with caution, only after careful assessment of the ratio of potential benefit to possible risk in patients with severe hepatic impairment (Child-Pugh class C).

The effect on bone tissue

Letrozole has a strong effect on reducing estrogen concentrations. In patients with a history of osteoporosis and/or fractures or with an increased risk of osteoporosis, bone mineral density should be evaluated by lensitometry at the beginning of treatment and regularly during treatment. If necessary, osteoporosis treatment or prophylaxis should be prescribed and the patient’s condition should be closely monitored.

Other precautions

Because each film-coated tablet of Lestrodex contains 58.4 mg of lactose in the form of lactose monohydrate, it is not recommended for use in patients with rare hereditary galactose intolerance, severe lactase deficiency, or glucose-galactose malabsorption.

Impact on driving and operating machinery

While therapy with Lestrodex may cause fatigue and dizziness as well as drowsiness, care should be taken when performing work requiring increased attention and rapid motor and mental reactions (including driving or operating machinery).

Contraindications

– endocrine status characteristic of the reproductive period;

– pregnancy;

– lactation period;

– children under 18 years of age (efficacy and safety in children have not been established);

– hypersensitivity to the active substance or any of the excipients of the drug.

With caution: significant hepatic (class C according to the Child-Pugh scale) and renal insufficiency (creatinine clearance (CK) less than 10 ml/min), lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Side effects

In general, adverse reactions were mild to moderate and mostly related to suppression of estrogen synthesis (e.g., flushing of the face, alopecia, and vaginal bleeding).

The frequency of adverse reactions is distributed as follows:

Very common (> 1/10), common (> 1/100, < 1/10), occasional (> 1/1000, < 1/100), rare (> 1/10 000 < 1/1000), very rare (< 1/10 000), frequency not known.

Infectious and parasitic diseases: sometimes urinary tract infections.

Denign, malignant and unspecified neoplasms (including cysts and polyps): sometimes pain in tumor foci (not applicable with adjuvant and long-term adjuvant treatment).

Hematopoietic system disorders: sometimes – leukopenia.

Metabolism and nutrition: frequently – anorexia, appetite increase, hypercholesterolemia; sometimes – generalized edema.

Psychiatric disorders: often – depression; sometimes – anxiety, including nervousness and irritability.

CNS: often – headache, dizziness: sometimes – drowsiness, insomnia, memory impairment; sensory disorders (dysesthesia), including paresthesia; hypoesthesia, impaired sense of taste, episodes of cerebral circulatory disorders.

Visually: sometimes – cataracts, eye irritation, blurred vision.

Cardiovascular system disorders: sometimes – palpitations, tachycardia, thrombophlebitis, including thrombophlebitis of superficial and deep veins, arterial hypertension, coronary heart disease; rarely – pulmonary embolism, arterial thrombosis, stroke.

Respiratory system disorders: sometimes – dyspnea, cough.

The digestive system: often – nausea, vomiting, dyspepsia, constipation, diarrhea; sometimes – abdominal pain, stomatitis, dry mouth.

Hepatic and biliary tract disorders: sometimes – increased liver enzymes activity.

Skin disorders: very common – increased sweating; common – apopecia; rash, including erythematous. maculopapular. vesicular rash; psoriasis-like rash; sometimes – itching, dry skin, urticaria; frequency not known – angioedema, anaphylactic reactions.

Muscular system disorders: very common – arthralgia: often – myalgia, bone pain, osteoporosis, bone fractures; sometimes – arthritis.

The urinary system: sometimes – frequent urination.

The genital system: sometimes – vaginal bleeding, vaginal discharge, vaginal dryness, pain in the breasts.

General disorders and disorders at the site of administration: very often – hot flashes, fatigue, including asthenia; often – malaise, peripheral edema; sometimes – hyperthermia, dry mucous membranes, thirst.

Impact on the results of laboratory and instrumental studies: often – weight gain; sometimes – weight loss.

Overdose

There have been isolated reports of cases of letrozole overdose.

Treatment: No specific methods of treatment of overdose are known.

Symptomatic and supportive therapy is indicated. Letrozole is excreted from the plasma by hemodialysis.

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