Tamoxifen HEXAL
Tamoxifen HEXAL: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Tamoxifen HEXAL
ATX code: L02BA01
Active ingredient: tamoxifen (Tamoxifen)
Producer: Salutas Pharma, GmbH (Germany)
Description and photo update: 2019-09-07
Prices in pharmacies: from 130 rubles.
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Tamoxifen HEXAL is an antineoplastic antiestrogen drug.
Release form and composition
The drug is available in the form of coated tablets: white or yellowish, round, biconvex, with a smooth uniform surface, in doses of 20 and 40 mg, a dividing line is applied on one of the sides (10 pcs. In blisters, in a cardboard box 3 or 10 packages and instructions for the use of Tamoxifen HEXAL).
1 tablet contains:
- active substance: tamoxifen citrate - 15.2; 30.4; 45.6 or 60.8 mg, which is equivalent to 10, 20, 30 or 40 mg of tamoxifen, respectively;
- auxiliary components: sodium starch glycolate, lactose 1H 2 O, povidone, magnesium stearate, microcrystalline cellulose;
- shell composition: white opadry dye (lactose, polyethylene glycol 4000, titanium dioxide, hypromellose).
Pharmacological properties
Pharmacodynamics
Tamoxifen HEXAL is an antineoplastic hormonal drug. Its active ingredient, tamoxifen, is a non-steroidal agent of the triphenylethylene group, which has antiestrogenic and weak estrogenic properties. The combined pharmacological action of tamoxifen extends to various tissues. In breast cancer, it interferes with the binding of estrogens to estrogen receptors in neoplastic cells, exhibiting mainly an antiestrogenic effect. In tumors with a high content of estrogen receptors, tissues of the uterus, vagina, breast and anterior pituitary gland, tamoxifen and its metabolites compete with estradiol for binding sites with cytoplasmic estrogen receptors. The tamoxifen receptor complex, unlike the estrogen receptor complex, does not stimulate the synthesis of DNA (deoxyribonucleic acid) in the nucleus. It suppresses the process of cell division, causing regression of tumor cells and their death.
Adjuvant therapy with tamoxifen for estrogen-positive or nonspecified breast tumors significantly reduces the number of relapses of the disease and increases life expectancy up to 10 years. Treatment with the drug for five years allows you to achieve a more pronounced effect than with a course of therapy lasting one or two years. Age, menopause, dose of tamoxifen or adjuvant chemotherapy do not affect clinical efficacy.
The use of tamoxifen in the postmenopausal period leads to a decrease in the concentration of total cholesterol and low density lipoproteins in the blood plasma in about 10–20% of women, and helps to preserve bone mineral density.
The inconsistency of the clinical response to tamoxifen therapy may be due to polymorphism of the CYP2D6 isoenzyme. It should be borne in mind that at a low metabolic rate of tamoxifen, the therapeutic response can be significantly reduced. There are no specific recommendations for the treatment of patients with a slow metabolism of the CYP2D6 isoenzyme.
Pharmacokinetics
After oral administration, tamoxifen is absorbed quite well. Its maximum concentration in serum after a single dose is reached within 4-7 hours. Against the background of regular use of tamoxifen in a daily dose of 20–40 mg for 21–28 days, an equilibrium concentration of tamoxifen in the blood serum is achieved.
Plasma protein binding - 98%.
Tamoxifen metabolism occurs in the liver with the help of the CYP3A4 isoenzyme with the formation of the main serum metabolite of N-desmethyltamoxifen, which, with the participation of the CYP2D6 isoenzyme, is metabolized to another active metabolite, endoxifen, and several subsequent metabolites with antiestrogenic properties identical to the parent substance. Compared to patients with normal CYP2D6 activity, in patients with CYP2D6 enzyme deficiency, the concentration of endoxifen is approximately 75% lower. To the same extent, the level of decrease in the concentration of endoxifen in the blood is affected by the simultaneous use of strong inhibitors of the isoenzyme CYP2D6.
The accumulation of tamoxifen and its metabolites occurs in the liver, pancreas, lungs, skin, brain and bones.
Tamoxifen is characterized by two phases of the half-life (T 1/2). The initial T 1/2 is 7-14 hours, the subsequent terminal T 1/2 lasts up to 7 days.
The drug is excreted in the form of conjugates mainly through the intestines, the rest through the kidneys.
Indications for use
- early breast cancer with estrogen-positive receptors as adjuvant therapy;
- mammary cancer;
- locally advanced or metastatic breast cancer with estrogen-positive receptors;
- breast cancer in men after castration;
- solid neoplasms with overexpression of estrogen receptors, resistant to standard therapy.
Contraindications
Absolute:
- period of pregnancy;
- lactation;
- age up to 18 years;
- hypersensitivity to the components of the drug.
It is recommended to use Tamoxifen HEXAL tablets with caution in case of renal failure, cataracts and other eye diseases, diabetes mellitus, deep vein thrombosis and thromboembolic disease (including history), leukopenia, thrombocytopenia, hyperlipidemia, hypercalcemia, concomitant therapy of indirect anticoagulants in patients with lactose-tolerance,, lactase deficiency or glucose-galactose malabsorption syndrome.
Tamoxifen HEXAL, instructions for use: method and dosage
Tamoxifen HEXAL tablets are taken orally, swallowing whole (without violating the integrity of the film shell) and drinking a small amount of liquid.
The doctor sets the dosage regimen and duration of treatment individually, taking into account clinical indications.
The prescribed dose of tamoxifen is taken in the morning or divided into two doses - morning and evening.
Recommended dosage: The standard dose is 20 mg per day. The maximum daily dose is 40 mg.
Long-term therapy is usually required. So, with adjuvant therapy for breast cancer, it is recommended to continue treatment with tamoxifen for 5 years.
Tamoxifen HEXAL should be discontinued if signs of disease progression appear.
Side effects
Unwanted disorders are classified as follows: very common - ≥ 1/10; often - ≥ 1/100 and <1/10; infrequently - ≥ 1/1000 and <1/100; rarely - ≥ 1/10 000 and <1/1000; very rarely - <1/10 000; frequency not established - based on the available data, it is not possible to establish the frequency of occurrence of side effects:
- from the lymphatic system and blood: often - anemia; infrequently - thrombocytopenia, leukopenia; rarely - neutropenia, agranulocytosis; very rarely - pancytopenia;
- from the nervous system: often - dizziness, headache; frequency not established - drowsiness, confusion, depression, photophobia;
- from the endocrine system: often - hypercalcemia (more often with bone metastases at the beginning of treatment);
- from the immune system: hypersensitivity reactions;
- on the part of metabolism and nutrition: very often - fluid retention in the body; often - an increase in plasma triglyceride levels; very rarely - a significant increase in the concentration of triglycerides in plasma, including in combination with pancreatitis; frequency not established - weight gain, anorexia;
- on the part of the organ of vision: often - visual impairment (including cataracts, corneal changes, retinopathy, sometimes reversible); rarely - optic neuritis (including with the development of blindness), neuropathy of the optic nerve;
- on the part of the vessels: often - transient ischemic attacks, thromboembolism (including thromboembolism of the pulmonary arteries), deep vein thrombosis and cramps of the lower extremities; infrequently - stroke;
- on the part of the hepatobiliary system: often - fatty degeneration of the liver, increased activity of hepatic transaminases; infrequently - cirrhosis of the liver; very rarely - hepatitis, jaundice, cholestasis, liver failure (up to death), liver cell necrosis;
- from the gastrointestinal tract: very often - nausea; often - diarrhea, constipation, vomiting;
- dermatological reactions: very often - rash; often - alopecia, hypersensitivity reactions, angioedema, urticaria; rarely - vasculitis; very rarely - polymorphic erythema, systemic lupus erythematosus, bullous pemphigoid, Stevens-Johnson syndrome;
- from the genitals and mammary glands: very often - vaginal discharge, vaginal bleeding, menstrual irregularities, in women in the premenopausal period - amenorrhea; often - an itching sensation in the genital area, proliferative changes in the endometrium (polyps, hyperplasia, neoplasia, less often endometriosis), an increase in uterine fibroids; infrequently - endometrial cancer; rarely - vaginal polyposis, uterine sarcoma (often malignant mixed tumor of Müller), polycystic ovary, in men - impotence, decreased libido;
- from the respiratory system, chest and mediastinal organs: infrequently - interstitial pneumonitis;
- from the musculoskeletal system: often - myalgia; very rarely - bone pain;
- others: very often - hot flashes (paroxysmal appearance of a feeling of heat); rarely - pain in the area of the affected tissues (especially at the beginning of therapy); very rarely - late cutaneous porphyria; frequency has not been established - increased fatigue, increased body temperature.
In addition, taking Tamoxifen HEXAL can potentiate the exacerbation of the disease, manifested by an increase in the size of soft tissue formations, pronounced erythema of the affected and adjacent areas. It usually goes away within two weeks after starting therapy.
Overdose
Symptoms of an acute overdose of tamoxifen have not been established. Possible increased side effects of the drug, prolongation of the QT interval.
Treatment: the appointment of symptomatic therapy. There is no specific antidote.
special instructions
The use of Tamoxifen HEXAL must be accompanied by regular monitoring of the blood picture, indicators of leukocytes, platelets and blood coagulation, the level of calcium in the blood, liver function, blood pressure, state of vision.
During the treatment period, women are advised to undergo regular gynecological examinations to determine endometrial cancer or uterine sarcoma (including Muller's malignant mixed tumor). This is due to an increase in the incidence of these pathologies against the background of the use of Tamoxifen HEXAL. A comprehensive examination is also required when vaginal bleeding or bleeding occurs with the simultaneous discontinuation of pills.
It should be borne in mind that concomitant therapy with other cytotoxic agents increases the risk of thromboembolic complications in patients.
After treatment of breast cancer with tamoxifen, patients may develop additional foci of primary tumor that are not localized in the endometrium or in the breast opposite the affected one. The causal relationship of these neoplasms has not been established.
At the beginning of the use of Tamoxifen HEXAL in patients with bone metastases, the level of calcium concentration in the blood serum should be monitored. If there is a pronounced deviation of these indicators from the initial parameters, taking the tablets should be temporarily stopped.
Pain or swelling in the legs during therapy with Tamoxifen HEXAL indicates the development of venous thrombosis of the lower extremities, shortness of breath - pulmonary embolism, therefore, if they appear, immediate discontinuation of the drug is required.
In patients with severe leukopenia, thrombocytopenia or hypercalcemia, Tamoxifen HEXAL should be prescribed after a careful assessment of the potential risk and the expected therapeutic effect of therapy.
With hyperlipidemia, it is necessary to carefully monitor the level of concentration in blood serum of cholesterol and triglycerides.
The patient should undergo an ophthalmic examination before starting treatment with tamoxifen. If visual impairment occurs during the treatment period, you must immediately contact an ophthalmologist, diagnosing an early stage of cataract or retinopathy allows you to eliminate the resulting disorders by canceling Tamoxifen HEXAL.
Influence on the ability to drive vehicles and complex mechanisms
There is a risk of undesirable phenomena that have a negative effect on concentration and the speed of psychomotor reactions, therefore, during the period of taking Tamoxifen HEXAL, care must be taken, and if dizziness, visual impairment or drowsiness occurs, refrain from driving and performing other potentially hazardous activities.
Application during pregnancy and lactation
The appointment of Tamoxifen HEXAL is contraindicated in the period of gestation and breastfeeding.
The use of the drug during pregnancy can cause spontaneous abortion, congenital malformations and fetal death.
Since tamoxifen inhibits lactation, breastfeeding during drug therapy is not possible. Milk production does not start for several months after the cessation of its use due to the persistence of the therapeutic effect of the drug. If it is necessary to prescribe Tamoxifen HEXAL during lactation, breastfeeding should be discontinued.
Due to the fact that the drug potentiates ovulation and increases the risk of unwanted conception, it is recommended to use barrier or non-hormonal contraception for women of childbearing age during the entire period of treatment and approximately three months after discontinuation of Tamoxifen HEXAL.
Pediatric use
The appointment of Tamoxifen HEXAL for the treatment of patients under 18 years of age is contraindicated.
With impaired renal function
Tamoxifen HEXAL should be taken with caution in patients with renal insufficiency.
Drug interactions
- bupropion, paroxetine, fluoxetine, antidepressants of the selective serotonin reuptake inhibitors group, quinidine, cinacalcet and other potent inhibitors of the CYP2D6 isoenzyme: a decrease in the plasma concentration of tamoxifen and its clinical effect is possible (joint use should be avoided);
- cytostatics: the risk of thrombus formation increases;
- warfarin and other drugs of the coumarin series: their anticoagulant effect is enhanced (careful monitoring is required to correct the dose of these drugs in a timely manner);
- thiazide diuretics: while taking drugs that slow down the excretion of calcium, the risk of developing hypercalcemia increases;
- tegafur: the risk of active chronic hepatitis, liver cirrhosis increases;
- hormonal agents: when combined with tamoxifen, they mutually weaken each other's action;
- rifampicin and other drugs metabolized by the isoenzyme CYP3A4: can reduce the concentration of tamoxifen in blood plasma;
- bromocriptine: the level of plasma concentration of tamoxifen and its main metabolite increases;
- anastrozole: its pharmacokinetic effect is weakened.
Analogs
Tamoxifen HEXAL analogs are: Tamoxifen, Vero-Tamoxifen, Tamoxifen Lahema, Tamoxifen-Ebeve, Tamoxifen-Ferein, Fazlodeks, Fareston, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tamoxifen HEXAL
Reviews about Tamoxifen HEXAL are positive. Comparing with similar drugs, patients indicate a less pronounced manifestation of adverse events and give preference to this drug.
Price for Tamoxifen HEXAL in pharmacies
The price of Tamoxifen HEXAL for a package containing 30 tablets at a dose of 20 mg can be 155–194 rubles.
Tamoxifen HEXAL: prices in online pharmacies
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Drug name Price Pharmacy |
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Tamoxifen Hexal 20 mg film-coated tablets 30 pcs. 130 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
