Universal reference book for medicines
Product name: FARESTON (FARESTON)

Active substance: toremifene

Type: Antiestrogenic drug with antitumor effect

Manufacturer: ORION CORPORATION (Finland)
Composition, form of production and packaging
Tablets are
white, round, flat, with bevelled edge, with code "TO20" on one side.

1 tab.

toremifene (in the form of citrate) 20 mg

Auxiliary substances: corn starch, lactose, povidone, sodium starch glycolate (type A), magnesium stearate, microcrystalline cellulose, colloidal silicon anhydrous.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (10) - packs cardboard.
30 pcs.
- polyethylene bottles (1) - cardboard packs.
60 pcs.
- polyethylene bottles (1) - cardboard packs.
100 pieces.
- polyethylene bottles (1) - cardboard packs.
Tablets are white, round, flat, with bevelled edge, with the code "TO60" on one side.

1 tab.

toremifene (in the form of citrate) 60 mg

Auxiliary substances: corn starch, lactose, povidone, sodium starch glycolate (type A), magnesium stearate, microcrystalline cellulose, colloidal silicon anhydrous.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
30 pcs.
- polyethylene bottles (1) - cardboard packs.
60 pcs.
- polyethylene bottles (1) - cardboard packs.
100 pieces.
- polyethylene bottles (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Antineoplastic anti-estrogenic non-steroidal drug, a derivative of 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, not associated with estrogen-dependent effects.
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, effect on the kinetics of the cell cycle) can not be ruled out.

PHARMACOKINETICS

Suction

After oral administration, toremifene is completely absorbed.
C max in blood plasma is achieved after 3 hours (2-5 hours). Eating does not affect the completeness of absorption, but can increase the time to reach Cmax by 1.5-2 hours. These changes have no clinical significance.
Distribution

Binding to plasma proteins (mainly with albumin) is 99.5%.
C ss in the blood plasma is established within 3-4 weeks (at a dose of 60 mg / day).
Metabolism and excretion

After the rapid phase of distribution with an average T 1/2 of about 4 hours (2-12 hours), a slow elimination phase begins with an average T 1/2 of about 5 days (2-10 days).

Toremifene is metabolized in the liver by hydroxylation and demethylation with the participation of the CYP3A4 isoenzyme with the formation of an active metabolite - N-demethyltoremifene.
The mean T 1/2 of N-demethyltoremifene is 11 days (4-20 days). In the blood serum, there were found three more metabolites: deaminohydroxytorrhoefen, 4-hydroxytorhomiphene and N, N -di-demethyltoremiphene. The total ground clearance is 5 l / h.
It is excreted through the intestines, mainly in the form of metabolites;
about 10% - by the kidneys.
INDICATIONS

- Estrogen-dependent breast cancer in women in the postmenopausal period.

DOSING MODE

Assign inside.
The dosage regimen is set individually.
As a standard dose for the first line of hormone therapy, taking a dose of 60 mg daily for a long time is recommended.

With the appointment of Fareston as the second line of hormonal treatment, the dose of the drug can be increased to 240 mg / day (120 mg 2 times / day).

When there are signs of progression of the disease, taking the drug is canceled.

SIDE EFFECT

The most common side effects are hot flashes (hot flushes), sweating, uterine bleeding or vaginal discharge (whites), fatigue, nausea, rash, itching in the genital area, fluid retention, dizziness and depression.
These side effects are usually mild and are caused by the antiestrogenic action of toremifene.
The frequency of unwanted reactions is classified as follows: very often (> 1/10), often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1 / 10,000, <1/1000), very rarely (<1/10 000), the frequency is unknown (it can not be estimated from available data).

Possible adverse events are presented according to organ systems and are distributed according to the frequency of development.

Benign, malignant and unspecified neoplasms (including cysts and polyps): very rarely - endometrial cancer.

On the part of the hematopoiesis system: the frequency is unknown - thrombocytopenia, anemia and leukopenia.

Mental disorders: often - depression;
infrequently - insomnia.
From the nervous system: often - dizziness;
infrequently - a headache.
From the side of the organ of vision: very rarely - the opacity of the cornea.

From the side of the hearing organ and labyrinthine disturbances: rarely - vertigo.

From the cardiovascular system: very often - tides;
infrequently - thromboembolic conditions.
On the part of the respiratory system: infrequently - shortness of breath.

From the digestive tract: often - nausea, vomiting;
infrequent loss of appetite, constipation.
From the liver and biliary tract: rarely - increased activity of hepatic transaminases;
very rarely - jaundice.
From the skin and subcutaneous tissues: very often - sweating;
often - a rash, itching; very rarely - alopecia.
On the part of the reproductive system and mammary glands: often - uterine bleeding or leucorrhoea;
infrequently - endometrial hypertrophy; rarely - endometrial polyps; very rarely - endometrial hyperplasia.
Other: often - fatigue, swelling;
infrequently - an increase in body weight.
Thromboembolic complications include deep venous thrombosis, thrombophlebitis and pulmonary embolism.

Therapy with toremifene is accompanied by changes in the activity of hepatic enzymes (increased activity of transaminases) and in very rare cases with more severe impairment of liver function (jaundice).

In some cases, patients with bone metastases at the beginning of treatment with toremifene noted hypercalcismia.

Hypertrophy of the endometrium may develop during treatment due to the partial estrogenic effect of toremifene.
There is a risk of increased changes in the endometrium such as hyperplasia, polyposis and cancer. This can be caused by the main pharmacological property of toremifene - estrogen stimulation.
Toremifene dose-dependently increases the QT interval.

CONTRAINDICATIONS

- hyperplasia of the endometrium (including in the anamnesis);

- severe hepatic insufficiency (including in the anamnesis);

- thromboembolism (including in the anamnesis);

- congenital or acquired documented elongation of the QT interval;

- clinically significant bradycardia;

- Clinically significant heart failure with a reduced fraction of the left ventricular ejection;

- violation of electrolyte balance, especially with unadjusted hypokalemia;

- symptomatic arrhythmia in the anamnesis;

- simultaneous use of drugs that extend the QT interval;

- Pregnancy;

- lactation (breastfeeding);

- hypersensitivity to toremifene and / or any other component of the drug.

With caution, prescribe the drug for leukopenia, thrombocytopenia, hypercalcemia (including metastases in bone tissue), decompensated heart failure, severe angina, proaritmogenic conditions (acute myocardial ischemia, prolongation of the QT interval), lactase deficiency, lactose intolerance, glucose syndrome -galactose malabsorption, elderly patients.

PREGNANCY AND LACTATION

Torimifen is recommended to patients in the postmenopausal period.

The drug is contraindicated for use in pregnancy and lactation.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe hepatic insufficiency (including in the anamnesis).

APPLICATION IN ELDERLY PATIENTS

Caution is prescribed to elderly patients.

SPECIAL INSTRUCTIONS

Before starting treatment, the patient must undergo a checkup with a gynecologist.
Particular attention should be paid to the condition of the endometrium. Then gynecological examinations should be repeated at least once a year.
Patients suffering from diseases such as hypertension, diabetes mellitus having a high BMI (> 30) or receiving prolonged HRT, are at risk for endometrial cancer and therefore need careful monitoring.

Toremifene is not recommended for use in patients who have a history of severe thromboembolic complications.

Patients with decompensated heart failure or severe angina pendant need careful monitoring.

Since in patients with metastases in the bone at the beginning of treatment with the drug may develop hypercalcemia, these patients need careful monitoring.

On the ECG of some patients, when taking toremifene, a dose-dependent prolongation of the QT interval was observed.

Toremifene should be used with caution in patients with pro-arrhythmogenic conditions (especially in elderly patients), such as acute myocardial ischemia or prolonged QT interval, as this may lead to an increased risk of ventricular arrhythmia (including ventricular pirouette arrhythmia) and cardiac arrest .

If during treatment with toremifene symptoms or signs that may indicate an arrhythmia are present, therapy should be discarded and an ECG should be done.

If the interval QT> 500 msec, do not take toremifene.

Tablets of Fareston contain lactose.

Anemia, leukopenia and thrombocytopenia were noted.
When taking toremifene, the number of erythrocytes, leukocytes or platelets should be monitored.
Impact on the ability to drive vehicles and manage mechanisms

Toremifene does not affect the ability to drive a car and other mechanisms.

OVERDOSE

Symptoms: with a daily dose of 680 mg, there were vertigo, headaches, nausea and / or vomiting.
Theoretically, an overdose may be manifested by increased anti-estrogenic effects (hot flashes) or estrogenic effects (vaginal bleeding). The possibility of a dose-dependent prolongation of the QT interval should be taken into account.
Treatment: symptomatic therapy.

DRUG INTERACTION

Drugs that reduce renal calcium excretion (including thiazide diuretics) may increase the risk of hypercalcemia.

Inducers of microsomal oxidation (eg, phenobarbital, phenytoin or carbamazepine) can accelerate the metabolism of toremifene, reducing its concentration in the serum.
In such cases, the daily dose should be doubled.
The 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).

Inhibitors of cytochrome isoenzymes CYP3A (erythromycin, oleandomycin, ketoconazole and other antifungal drugs) reduce the rate of metabolism of toremifene (caution should be exercised while using these medicines with toremifene).

The additive effect on the prolongation of the QT interval between toremifene and the following drugs can not be ruled out, which can lead to an increased risk of ventricular arrhythmias, including ventricular pirouette-type arrhythmias:

- Class I antiarrhythmics (eg, quinidine, hydroquinidine, disopyramide);

- Class III antiarrhythmic drugs (for example, amiodarone, sotalol, dofetilide, ibutilide);

- Neuroleptics (eg, phenothiazine, pimozide, sertindole, haloperidol, sultopride);

- certain antimicrobial agents (moxifloxacin, erythromycin, pentamidine, antimalarials, in

features of halofantrine);

- certain antihistamines (terfenadine, astemizole, misolastine);

- Other (cisapride, winkamine IV, beprideil, difemanyl).

The simultaneous administration of toremifene with these drugs is contraindicated.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a dry place inaccessible to children at a temperature of 15 ° to 25 ° C.
Shelf life - 5 years.
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