Indications
Estrogen-dependent breast cancer in postmenopausal women.
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Estrogen-dependent breast cancer in postmenopausal women.
With caution: prescribe the drug for leukopenia, thrombocytopenia, hypercalcemia (including bone metastases).
1 tablet contains:
Active ingredients:
toremifene (in citrate form) 60 mg.
Excipients:
corn starch,
lactose, povidone,
sodium starch glycolate (type A),
magnesium stearate,
microcrystalline cellulose,
colloidal anhydrous silicon.
In a contour cell pack of 10 tablets.
There are 3 contour cell packages in a cardboard box.
The bottle contains 60 tablets.
In a cardboard box 1 bottle.
1 tablet contains:
Active ingredients:
toremifene (in citrate form) 60 mg.
Auxiliary substances:
corn starch,
lactose, povidone,
sodium starch glycolate (type A),
magnesium stearate,
microcrystalline cellulose,
colloidal anhydrous silicon.
In a contour cell pack of 10 tablets.
There are 3 contour cell packages in a cardboard box.
The bottle contains 60 tablets.
In a cardboard box 1 bottle.
Pharmacodynamics
Antitumor anti-estrogenic nonsteroidal drug derived from triphenylethylene.
Toremifene specifically binds to estrogen receptors, competing with estradiol, inhibits estrogen-induced DNA synthesis and cell replication. In high doses, toremifene may have an antitumor effect that is not associated with estrogen-dependent action.
In patients with breast cancer, the antitumor effect of toremifene is mainly associated with its anti-estrogenic activity, although other mechanisms (regulation of oncogene expression, growth factor secretion, induction of apoptosis, influence on cell cycle kinetics) cannot be excluded.
Pharmacokinetics
Suction
After oral use, toremifene is completely absorbed. Cmax in blood plasma is reached after 3 h (2-5 h). Food intake does not affect the completeness of absorption, but can increase the time to reach Cmax by 1.5-2 hours. These changes are not clinically relevant.
Distribution
Binding to plasma proteins (mainly albumin) is 99.5%. Css in blood plasma is established within 3-4 weeks (at a dose of 60 mg / day).
Metabolism and elimination
A fast phase of distribution with an average T1/2 of about 4 hours (2-12 hours) is followed by a slow phase of elimination with an average T1 / 2 of about 5 days (2-10 days).
Toremifene is metabolized in the liver by hydroxylation and demethylation with the participation of the CYP3A4 isoenzyme to form the active metabolite-N-demethyltoremifene. The average T1 / 2 of N-demethyltoremiphene was 11 days (4-20 days).3 more metabolites were detected in the blood serum: deaminohydroxytoremiphene,4-hydroxytoremiphene and N, N-didemethyltoremiphene. Total ground clearance – 5 l / h.
It is excreted through the intestines, mainly in the form of metabolites; about 10% – by the kidneys.
Estrogen-dependent breast cancer in postmenopausal women.
Fareston is contraindicated for use during pregnancy and lactation (breastfeeding).
With caution: prescribe the drug for leukopenia, thrombocytopenia, hypercalcemia (including bone metastases).
Effects due to anti-estrogenic effects: most often – paroxysmal sensations of heat (hot flashes), increased sweating, vaginal bleeding or discharge, increased fatigue, nausea, rash, itching in the genital area, fluid retention, dizziness, depression. These effects are usually mild.
Endocrine system disorders: rarely-weight gain.
From the digestive system: rarely – anorexia, vomiting, constipation.
From the central nervous system: rarely-headache, insomnia, increased transaminase levels; in some cases-severe liver function disorders (jaundice).
From the side of the organ of vision: rarely-visual impairment, including corneal changes, cataracts.
From the cardiovascular system: rarely-deep vein thrombosis, pulmonary embolism.
Dermatological reactions: rarely – skin rash, alopecia.
Other: rarely-shortness of breath.
Patients with bone metastases have experienced cases of hypercalcemia at the very beginning of treatment.
This increases the risk of endometrial changes, such as hyperplasia, polyposis, and cancer. This may be caused by the main pharmacological property of the drug – estrogenic stimulation.
Medications that reduce renal calcium excretion (including thiazide diuretics) may increase the risk of hypercalcemia.
Inducers of microsomal oxidation (for example, phenobarbital, phenytoin, or carbamazepine) can accelerate the metabolism of toremifene, reducing its concentration in serum. In such cases, the daily dose should be doubled.
Interaction between antiestrogens and warfarin can lead to a marked increase in bleeding time (simultaneous use of toremifene and drugs of this group should be avoided).
Theoretically, the metabolism of toremifene can be slowed down under the influence of drugs that inhibit the CYP3A4 isoenzyme, with the participation of which toremifene is metabolized. These medications include ketoconazole and other similar antifungal medications, as well as erythromycin and oleandomycin.
Assign inside. The dosage regimen is set individually.
As a standard dose for first-line hormone therapy, it is recommended to take a dose of 60 mg daily for a long time.
When prescribing Fareston as a second-line hormonal treatment, the dose of the drug can be increased to 240 mg / day (120 mg 2 times / day).
If signs of disease progression appear, the drug is discontinued.
Symptoms: dizziness, headaches, nausea, and/or vomiting were observed with a daily dose of Fareston 680 mg. Theoretically, an overdose can be manifested by increased anti-estrogenic effects (hot flashes) or estrogenic effects (vaginal bleeding).
Treatment: performing symptomatic therapy.
Before starting treatment, the patient should be examined by a gynecologist. Special attention should be paid to the condition of the endometrial mucosa. Then gynecological examinations should be repeated at least once a year.
Patients suffering from diseases such as hypertension, diabetes mellitus, having a high body mass index (>30) or receiving long-term HRT are at risk for endometrial cancer and therefore need to be carefully monitored.
Toremifen is not recommended for use in patients with a history of severe thromboembolic disease.
Patients with decompensated heart failure or severe angina should be closely monitored.
Since patients with bone metastases may develop hypercalcemia at the beginning of treatment with the drug, these patients need careful monitoring.
Tablets
Store in a dry place out of the reach of children at a temperature of 15° to 25°C.
life is 5 years.
Toremifen
By prescription
Tablets
For adults as directed by your doctor
Breast Cancer, Cancer
Out of stock
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