Femara, 2,5mg 30 pcs.

How to take, the dosage

For adults, the recommended dose of Femara® is 2.5 mg once daily, daily long-term.

As an extended adjuvant therapy, treatment should be continued for 5 years (no longer than 5 years).

Femara should be discontinued if there are signs of disease progression.

In elderly patients, there is no need to adjust the dose of Femara.

In patients with hepatic and/or renal impairment (CKR ≥ 10 ml/min) no dose adjustment is required. However, patients with severe hepatic impairment (class C on the Child-Pugh scale) should be under constant monitoring.

The tablets are taken orally, regardless of meals.

Interaction

In concomitant administration of letrozole with cimetidine and warfarin no clinically significant interaction is observed.

There is currently no clinical experience with the use of letrozole in combination with other anticancer agents.

According to the results of in vitro studies letrozole inhibits the activity of cytochrome Р450 isoenzymes – 2A6 and 2C19 (the latter moderately). When deciding on the significance of these data for the clinic it should be taken into account that CYP2A6 isoenzyme does not play a significant role in drug metabolism.

In in vitro experiments it has been shown that letrozole used in concentrations 100 times greater than the equilibrium values in plasma has no ability to significantly inhibit the metabolism of diazepam (substrate for CYP2C19).

Thus, clinically significant interactions with CYP2C19 isoenzyme are unlikely. However, caution should be exercised when co-administering letrozole and drugs metabolized predominantly with the participation of the above mentioned isoenzymes and with a narrow therapeutic index.

Special Instructions

Patients with severe hepatic impairment should be under constant monitoring.

Impact on the ability to drive and operate vehicles and other mechanisms requiring high concentration

Some side effects of the drug, such as general weakness and dizziness, may affect the ability to perform potentially dangerous activities requiring concentration and quick reactions.

In this regard, caution should be exercised when driving vehicles and operating machinery.

Contraindications

• Endocrine status, typical for the reproductive period;
• pregnancy;
• lactation (breast-feeding) period;
• children and adolescents under 18 years of age;
• high sensitivity to letrozole or any other component of the drug.
• There are no data on the use of Femara® in patients with a creatinine clearance of less than 10 ml/min. Before prescribing Femara in these patients, the balance between the potential risk and the expected effect of treatment should be carefully weighed.
  

Side effects

The incidence of side effects is estimated as follows:

• occurring very frequently (≥10%);
• often (≥1, < 10%);
• sometimes (≥0.1%, < 1%);
• frequently (≥0.01, < 0.1%);
• very rarely ( < 0.01%, including individual reports).

As a rule, adverse reactions were mild to moderate and mostly related to suppression of estrogen synthesis.

Gastrointestinal system disorders: frequently – nausea, vomiting, dyspepsia, constipation, diarrhea; sometimes – abdominal pain, stomatitis, dry mouth, increased liver enzyme activity.

CNS and peripheral nervous system disorders: frequently – headache, dizziness, depression; sometimes – anxiety, nervousness, irritability, somnolence, insomnia, memory impairment, dysesthesia, paraesthesia, hypoesthesia, sensory perception disorders, episodes of cerebral circulation disorders.

Hematopoietic system: sometimes – leukopenia.

The cardiovascular system: sometimes – palpitations, tachycardia, thrombophlebitis of superficial and deep veins, increased BP, CHD (angina, myocardial infarction, heart failure), thromboembolism; rarely – pulmonary embolism, arterial thrombosis, stroke.

Respiratory system disorders: sometimes – dyspnea, cough.

Dermatological reactions: frequently – alopecia, increased sweating, skin rash (including erythematous, maculopapular, vesicular rash, psoriasis-like rash); sometimes – skin itching, dry skin, urticaria; very rarely – angioedema, anaphylactic reactions.

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

Senses: sometimes – cataracts, eye irritation, blurred vision, impaired sense of taste.

The urinary system: sometimes – frequent urination, urinary tract infections.

Reproductive system disorders: sometimes – vaginal bleeding, vaginal discharge, vaginal dryness, pain in the breasts.

Others: very often – hot flashes (hot flashes); often – increased fatigue, asthenia, malaise, peripheral edema, weight gain, hypercholesterolemia, anorexia, increased appetite; sometimes – weight loss, thirst, hyperthermia (pyrexia), dry mucous membranes, generalized edema, pain in tumor foci.

Overdose

There have been isolated reports of Femara® overdose.

Treatment: No specific treatment of overdose is known.

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

Pregnancy use

Femara® is contraindicated in pregnancy and lactation.

Women in the perimenopausal and early postmenopausal periods should use reliable contraception until stable postmenopausal hormone levels are established during therapy with Femara, given the potential for pregnancy.

Similarities

Letrozol, Estrolet, Letrozol, Loreta, Lestrodex