FARESTON
Active material: Toremifene
When ATH: L02BA02
CCF: Anti-estrogen drug with antitumor activity
ICD-10 codes (testimony): C50
When CSF: 15.13.01
Manufacturer: ORION CORPORATION (Finland)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Pills white, round, flat, with a beveled edge, with code “Up to20” on one side.
| 1 tab. | |
| Toremifen (in the citrate form) | 20 mg |
Excipients: corn starch, lactose, povidone, sodium starch glycolate (Type A), magnesium stearate, microcrystalline cellulose, silica colloidal anhydrous.
10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (10) – packs cardboard.
30 PC. – plastic bottles (1) – packs cardboard.
60 PC. – plastic bottles (1) – packs cardboard.
100 PC. – plastic bottles (1) – packs cardboard.
Pills white, round, flat, with a beveled edge, with code “To60” on one side.
| 1 tab. | |
| Toremifen (in the citrate form) | 60 mg |
Excipients: corn starch, lactose, povidone, sodium starch glycolate (Type A), magnesium stearate, microcrystalline cellulose, silica colloidal anhydrous.
10 PC. – packings Valium planimetric (3) – packs cardboard.
30 PC. – plastic bottles (1) – packs cardboard.
60 PC. – plastic bottles (1) – packs cardboard.
100 PC. – plastic bottles (1) – packs cardboard.
Pharmacological action
Antitumor anti -estrogenic non -nested drug, Derivative of triphenylelene.
Toremifen is specifically associated with estrogenic receptors, competing with estradiol, inhibits the synthesis of DNA and cell replication caused by estrogens. In high doses, Toremifen can have an antitumor effect, estrogen -dependent action.
In patients with breast cancer, the antitumor effect of tremihifen is mainly associated with its anti -estrogenic activity, although other mechanisms cannot be excluded (Regulation of oncogen expression, The secretion of growth factor, apoptosis, influence on the kinetics of the cell cycle).
Pharmacokinetics
Absorption
After taking Toremifen is completely absorbed. Cmax plasma levels achieved after 3 no (2-5 no). Eating does not affect the completeness of absorption, but can increase the time of achievement Cmax on 1.5-2 no. These changes have no clinical value.
Distribution
Plasma protein binding (mainly with Albumin) – 99.5%. Css In blood plasma is installed during 3-4 weeks (at a dose 60 mg / day).
Metabolism and excretion
For a fast distribution phase with average t1/2 about 4 no (2-12 no) the phase of slow excretion with the average t comes1/2 about 5 d (2-10 d).
Toremifen is metabolized in the liver by hydroxylation and demethylilation with the participation of the CyP3A4 isoenzyme with the formation of an active metabolite – N-Demetiltoremifena. Average T1/2 N-Demetiltoremifena – 11 d (4-20 d). In the blood serum, more 3 metabolite: Deaminohydroxitoremiafen, 4-hydroxytoremiafen and n,N-Didemetiltoremifen. Total clearance – 5 l /.
Displayed through the intestine, mainly as metabolites; about 10% – kidney.
Testimony
- estrogen -dependent breast cancer in women in the postmenopaudal period.
Dosage regimen
Assign inside. The batch is individually.
As a standard dose for the first line of hormone therapy, it is recommended to receive at the dose 60 MG daily for a long time.
When prescribing a pharystone as a second hormonal treatment line, the dose of the drug can be increased to 240 mg / day (by 120 mg 2 times / day).
If signs of disease progression the drug overturned.
Side effect
Effects, due to anti -estrogenic effects: common – hot flashes (tides), increased sweating, vaginal bleeding or secretion, fatigue, nausea, rash, itching in the genital area, fluid retention, dizziness, depression. These effects are usually expressed in a mild degree.
On the part of the endocrine system: rarely – weight gain.
From the digestive system: rarely – anorexia, vomiting, constipation.
CNS: rarely – headache, insomnia, transaminase elevation; in some cases – severe liver (jaundice).
On the part of the organ of vision: rarely – blurred vision, including changes in the cornea, cataracts.
Cardio-vascular system: rarely – deep vein thrombosis, pulmonary embolism.
Dermatological reactions: rarely – skin rash, alopecia.
Other: rarely – breathlessness.
In patients with metastases in the bone, cases of development of hypercalcemia were observed at the very beginning of treatment.
The risk of endometrial changes increases, such as hyperplasia, polyps and cancer. This can be caused by the main pharmacological property of the drug – estrogenic stimulation.
Contraindications
- Endometrial hyperplasia (incl. history);
- Severe hepatic impairment (incl. history);
- Thromboembolism (incl. history);
- Pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug.
FROM caution prescribe the drug for leukopenia, thrombocytopenia, hypercalcemia (incl. With metastases into bone tissue).
Pregnancy and lactation
Freston is contraindicated in use during pregnancy and during lactation (breast-feeding).
Cautions
Before starting treatment, the patient should undergo an examination by a gynecologist. Particular attention should be paid to the state of the endometrium mucosa. Then gynecological examinations must be repeated at least 1 per year.
Patients, suffering from diseases such as arterial hypertension, diabetes, having a high level of body weight index (>30) or a long -term zgt, are at risk on the occurrence of endometrial cancer and therefore need careful monitoring.
Toremifen is not recommended to be used in patients, who had a history of cases of severe thromboembolic disease.
Patients with decompensated heart failure or severe angina pectoris need careful monitoring.
Since patients with bone metastases at the beginning of treatment with the drug can develop hypercalcemia, These patients need careful monitoring.
Overdose
Symptoms: with a daily dose of Feston 680 MG was observed dizziness, headache, nausea and / or vomiting. Theoretically, an overdose can manifest itself by increasing anti -estrogenic effects (tides) or estrogen effects (vaginal bleeding).
Treatment: symptomatic therapy.
Drug Interactions
Preparations, Reducing renal expression of calcium (incl. thiazide diuretics), can increase the risk of hypercalcemia.
Inductors of microsomal oxidation (eg, phenobarbital, phenytoin or carbamazepine), can accelerate the metabolism of Toremifen, reducing its concentration in serum. In such cases, the daily dose should be doubled.
The interaction between anti -estrogen and warfarin can lead to a pronounced increase in bleeding time (the simultaneous use of tremiafen and drugs of this group should be avoided).
Theoretically, the metabolism of Toremifen can slow down under the influence of drugs, inhibitors CYP3A4, with the participation of which the metabolism of Tremifen is carried out. Such drugs include ketoconazole and other similar antifungal drugs, as well as erythromycin, oleandomiцin.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored in a dry place inaccessible to children at a temperature of 15 ° to 25 ° C. Shelf life – 5 years.
