Toremifen
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Clinical Pharmacology
Antineoplastic antiestrogenic nonsteroidal preparation, triphenylethylene derivative.
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 anti-tumor effect of toremifene is mainly related to its anti-estrogenic activity, although other mechanisms cannot be ruled out (regulation of oncogene expression, secretion of growth factor, induction of apoptosis, effect on the kinetics of the cell cycle).
Pharmacokinetics
Suction
After oral administration, toremifene is completely absorbed. Cmax in blood plasma is reached after 3 hours (2-5 hours). Meal does not affect the complete absorption, but may increase the time to reach Cmax at 1.5-2 hours. These changes have no clinical significance.
Distribution
Plasma protein binding (mainly albumin) - 99.5%. Css in blood plasma is established within 3-4 weeks (at a dose of 60 mg / day).
Metabolism and excretion
Beyond the fast distribution phase with medium T1/2 about 4 h (2-12 h) the slow elimination phase begins with an average T1/2 about 5 days (2-10 days).
Toremifene is metabolized in the liver by hydroxylation and demethylation with the participation of the CYP3A4 isoenzyme with the formation of an active metabolite, N-demethyltremifene. Average t1/2 N-demethyltoremifene - 11 days (4-20 days). Three more metabolites were detected in the blood serum: deaminogidroksitoremifene, 4-hydroxy toremifene and N, N-didemethyltremifene. Overall clearance - 5 l / h.
Excreted through the intestines, mainly in the form of metabolites; about 10% by the kidneys.
Indications
Estrogen-dependent breast cancer in postmenopausal women.
Composition
1 tablet contains:
Active substances: toremifene (in the form of citrate) 60 mg.
Excipients: corn starch, lactose, povidone, sodium starch glycolate (type A), magnesium stearate, microcrystalline cellulose, anhydrous colloidal silicon.
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Dosage and Administration
Assign inside. The dosing regimen is set individually.
As a standard dose for the first line of hormone therapy, it is recommended to take a dose of 60 mg daily for a long time.
When prescribing Phareston as a second line of hormonal treatment, the dose of the drug can be increased up to 240 mg / day (120 mg 2 times / day).
If there are signs of disease progression, taking the drug is canceled.
Adverse reactions
Effects due to anti-estrogenic effects: most frequently, hot flashes (flushing), excessive sweating, vaginal bleeding or discharge, fatigue, nausea, rash, itching in the genital area, fluid retention, dizziness, depression. These effects are usually mild.
On the part of the endocrine system: rarely an increase in body weight.
From the digestive system: rarely - anorexia, vomiting, constipation.
From the side of the central nervous system: rarely - headache, insomnia, increased transaminase levels; in some cases - severe violations of the liver (jaundice).
On the part of the organ of vision: rarely - visual impairment, including changes in the cornea, cataract.
Since the cardiovascular system: rarely - deep vein thrombosis, pulmonary embolism.
Dermatological reactions: rarely - skin rash, alopecia.
Other: rarely - shortness of breath.
In patients with bone metastases, cases of hypercalcemia were observed at the very beginning of treatment.
The risk of endometrial changes such as hyperplasia, polyposis and cancer increases. This may be caused by the main pharmacological property of the drug - estrogen stimulation.
Carefully: prescribe medication for leukopenia, thrombocytopenia, hypercalcemia (including with bone metastases).
Drug interactions
Drugs that reduce renal excretion of calcium (including thiazide diuretics) may increase the risk of hypercalcemia.
Inductors 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.
The interaction between antiestrogens and warfarin can lead to a pronounced increase in bleeding time (the simultaneous use of toremifene and drugs of this group should be avoided).
Theoretically, toremifene metabolism can be slowed down under the influence of drugs inhibiting the isoenzyme CYP3A4, with the participation of which the metabolism of toremifene is carried out. These drugs include ketoconazole and other similar antifungal drugs, as well as erythromycin, oleandomycin.
Pregnancy and Lactation
Fareston is contraindicated for use during pregnancy and lactation (breastfeeding).
Special instructions
Before treatment, the patient should be examined by a gynecologist. Particular attention should be paid to the condition of the endometrial mucosa. Then gynecological examinations should be repeated at least 1 time per year.
Patients suffering from such diseases as arterial hypertension, diabetes mellitus, having a high body mass index (> 30) or having received long-term HRT are at risk of developing endometrial cancer and therefore need careful monitoring.
Toremifen is not recommended for use in patients who had a history of severe thromboembolic disease.
Patients with decompensated heart failure or severe angina pectoris need careful monitoring.
Since patients with bone metastases may develop hypercalcemia at the beginning of drug treatment, these patients need to be carefully monitored.
Overdosage
Symptoms: with a daily dose of 680 mg of Fauston, dizziness, headaches, nausea and / or vomiting were observed. Theoretically, an overdose can be manifested by increased anti-estrogenic effects (hot flashes) or estrogenic effects (vaginal bleeding).
Treatment: conducting symptomatic therapy.
- Brand name: Fareston
- Active ingredient: Toremifen
- Dosage form: Pills.
- Manufacturer: Orion Corporation
- Country of Origin: Finland