Tamoxifen - Instructions For Use, Reviews, Side Effects, Price

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Tamoxifen

Tamoxifen: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. Drug interactions
12. 12. Analogs
13. 13. Terms and conditions of storage
14. 14. Terms of dispensing from pharmacies
15. 15. Reviews
16. 16. Price in pharmacies

Latin name: Tamoxifenum

ATX code: L02BA01

Active ingredient: Tamoxifen citrate (Tamoxifen citrate)

Producer: Shreya Life Science Pvt. Ltd (India), Severnaya Zvezda CJSC, Obolenskoye Pharmaceutical Enterprise CJSC, OZON Pharmaceutical Company (Russia), Orion Corporation (Finland)

Description and photo update: 2019-12-08

Prices in pharmacies: from 30 rubles.

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Tamoxifen is a non-steroidal anti-estrogen drug with an antitumor effect.

Release form and composition

The dosage form of Tamoxifen is tablets: from white to white with a creamy or grayish tint, flat-cylindrical; 10 mg each - with a chamfer; 20 mg each - with a line and a chamfer (30, 50, 100 pcs. in bottles, 1 bottle in a cardboard box; 10 or 30 pcs. in blisters, 1–6 or 10 packages in a cardboard box; 10, 20, 30, 40, 50 or 100 pieces in polymer containers, 1 container in a cardboard box).

Composition of 1 tablet:

• active substance: tamoxifen - 10 or 20 mg (tamoxifen citrate - 15.2 mg or 30.4 mg);
• auxiliary components (10/20 mg, respectively): magnesium stearate - 1.8 / 3.6 mg; lactose monohydrate - 117.2 / 234.4 mg; povidone - 6.1 / 12.2 mg; potato starch - 39.7 / 79.4 mg.

Pharmacological properties

Pharmacodynamics

Tamoxifen is a non-steroidal antiestrogenic drug that also has weak estrogenic activity. Its mechanism of action is due to its ability to block estrogen receptors. The metabolites of the drug and tamoxifen itself are competitors for estradiol, binding to the cytoplasmic estrogen receptors located in the tissues of the anterior pituitary gland, uterus, vagina, breast, as well as in tumor tissues. The tamoxifen receptor complex, unlike the estrogen receptor complex, does not stimulate the formation of DNA in the nucleus. It suppresses cell division, causing tumor cells to die.

Pharmacokinetics

Tamoxifen is well absorbed when taken orally. Its maximum serum concentration is reached within 4-7 hours after taking a single dose. Equilibrium drug concentrations are observed in serum after about 3-4 weeks of treatment. Tamoxifen is 99% bound to plasma proteins.

The drug is metabolized in the liver with the participation of the isoenzyme CYP2C9. As a result, several metabolites are formed.

Tamoxifen is excreted in two phases: the initial elimination half-life is 7-14 hours, and the terminal half-life is 7 days. The drug is excreted mainly in the form of metabolites and mainly through the intestines. Only a small part of tamoxifen is excreted by the kidneys.

Indications for use

• early breast cancer with estrogen-positive receptors (adjuvant therapy);
• locally advanced or metastatic breast cancer with estrogen-positive receptors (treatment);
• breast cancer, including in male patients after castration.

In the presence of overexpression of estrogen receptors, Tamoxifen can also be used to treat other solid tumors that are resistant to standard therapies.

Contraindications

Absolute:

• age up to 18 years (for this category of patients, the safety profile has not been studied);
• pregnancy and lactation;
• hypersensitivity to the components of the drug.

Relative (Tamoxifen is prescribed with caution in the presence of the following diseases / conditions):

• eye diseases, including cataracts;
• hyperlipidemia;
• hypercalcemia;
• thrombocytopenia;
• severe thrombophlebitis;
• liver disease;
• thromboembolic disease, including the presence of anamnestic data;
• leukopenia;
• hereditary lactose intolerance, lactase deficiency or malabsorption of galactose / glucose (lactose is part of Tamoxifen).

Instructions for the use of Tamoxifen: method and dosage

Tamoxifen is taken by mouth with a small amount of liquid. Do not chew the tablets.

The daily dose is taken 1 time per day (in the morning) or divided into 2 doses (in the morning and evening).

Usually the doctor determines the dosage regimen individually.

The daily dose can vary from 20 to 40 mg.

As a standard dose, a daily intake of 20 mg for a long time is recommended.

If symptoms of disease progression appear, Tamoxifen is discontinued.

Side effects

The most common side effects of Tamoxifen are associated with its antiestrogenic effect, they manifest themselves as hot flashes (hot flashes), vaginal bleeding or discharge, itching in the genital area, alopecia, pain in the area of the lesion, ossalgia, weight gain.

Less commonly, the development of the following disorders is observed: allergic reactions (including angioedema), fever, anorexia, fluid retention, nausea, constipation, vomiting, confusion, depression, fatigue, headache, drowsiness, dizziness, skin rash (including isolated cases erythema multiforme, Stevens-Johnson syndrome and bullous pemphigoid), visual impairment (including retinopathy, cataracts, corneal changes), retrobulbar neuritis, decreased libido in men, impotence.

In very rare cases, during the use of Tamoxifen, the development of interstitial pneumonitis is noted.

At the beginning of the course, there may be a local exacerbation of the disease (in the form of an increase in the size of soft tissue formations), in some cases it is accompanied by pronounced erythema of the affected areas and adjacent areas. As a rule, these violations are of a transient nature and disappear within 14 days.

Other possible disorders: often - leg cramps; infrequently - transient thrombocytopenia / leukopenia, an increase in the activity of hepatic enzymes (in very rare cases, it is accompanied by more severe functional disorders of the liver - fatty liver infiltration, hepatitis, cholestasis); rarely - an increase in the concentration of serum triglycerides (sometimes occurs in combination with pancreatitis).

Some patients with bone metastases developed hypercalcemia at the beginning of the course. During the period of Tamoxifen use, the likelihood of thromboembolism and thrombophlebitis may increase.

Possible side effects of Tamoxifen in women: amenorrhea or irregular menstruation (in the premenopausal period), reversible ovarian cystic tumors; with prolonged use of the drug - changes in the endometrium, including uterine fibroids, polyps, hyperplasia, in isolated cases - uterine sarcoma and endometrial cancer.

Overdose

Cases of acute overdose have not been registered. When taking ultra-high doses of the drug, the development of symptoms of neurotoxicity is possible: dizziness, hyperreflexia, tremor, unsteadiness of gait.

There is no specific antidote for Tamoxifen. In case of overdose, symptomatic treatment is prescribed.

special instructions

Women during the period of taking Tamoxifen are shown to carry out regular (1 time in 3 months) gynecological examinations. In cases of vaginal bleeding or vaginal bleeding, therapy is canceled.

Tamoxifen can cause ovulation, which increases the chance of pregnancy. During the period of use of the drug and for 3 months after the end of the course, women of reproductive age are recommended to use reliable non-hormonal methods of contraception.

In the presence of bone metastases, periodically during the initial period of therapy, it is necessary to determine the serum calcium concentration in the blood. In case of severe disorders (hypercalcemia), Tamoxifen is temporarily stopped.

Against the background of hyperlipidemia, it is necessary to control the serum concentration of cholesterol and triglycerides in the blood.

In cases of signs of vein thrombosis of the lower extremities (in the form of pain in the legs or their swelling), pulmonary embolism (in the form of shortness of breath), therapy is canceled.

During treatment, the following indicators should be periodically monitored: blood coagulation, liver function, calcium content in the blood, blood picture (leukocytes, platelets). It is also necessary to monitor blood pressure and have an eye exam every 3 months.

During the period of Tamoxifen use, it is recommended to be careful when driving vehicles and performing potentially hazardous work, which require increased concentration of attention and speed of psychomotor reactions.

Application during pregnancy and lactation

According to the instructions, Tamoxifen is prohibited for use during pregnancy. If there is a need to take the drug during breastfeeding, breastfeeding should be discontinued.

In experimental studies, it was found that tamoxifen has a teratogenic effect on the fetus.

Pediatric use

The drug is prohibited for use in children and adolescents under 18 years of age, since there is no data on the safety and effectiveness of Tamoxifen administration to children.

Drug interactions

With the combined use of Tamoxifen with certain drugs / substances, the following effects may develop:

• indirect anticoagulants - coumarin derivatives (for example, warfarin): increased anticoagulant effect;
• cytostatics: an increase in the likelihood of thrombus formation;
• tegafur: increased likelihood of developing liver cirrhosis and active chronic hepatitis;
• medicines that reduce calcium excretion (for example, thiazide diuretics): an increase in the likelihood of hypercalcemia;
• bromocriptine: an increase in the plasma concentration of tamoxifen and N-desmethyltamoxifen in the blood;
• other hormonal drugs (especially estrogen-containing contraceptives): weakening the effect of both drugs.

Analogs

Tamoxifen analogs are: Tamoxifen Hexal, Tamoxifen-Ferein, Vero-Tamoxifen, Tamoxifen Lahema, Tamoxifen-Ebeve, Fareston, Fazlodeks.

Terms and conditions of storage

Store in a dark place at temperatures up to 25 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Tamoxifen

The drug is used to treat serious diseases, including hormonal disorders and cancer. Reviews of Tamoxifen are generally positive, since the drug is a really effective remedy. However, the assessment of Tamoxifen based only on reviews is not entirely correct due to the individual effect of the drug on each patient.

The main disadvantage of the drug is the occurrence of side effects and the appearance of other, no less serious pathologies, for example, endometrial cancer, during treatment. However, this disease develops only with prolonged (more than 10 years) therapy and the frequency of its occurrence does not exceed 3% (in women who have taken Tamoxifen for 5 years - no more than 1.6%).

The results of the studies have shown that with long-term therapy with Tamoxifen, the survival rates in women with breast cancer increase by an order of magnitude, therefore, the question of the effectiveness of the drug and the expediency of its appointment is decided exclusively by the attending physician, regardless of the presence of positive or negative reviews of the drug.

Price for Tamoxifen in pharmacies

Tamoxifen prices depend on dosage, packaging and country of origin. So, tablets in a dosage of 10 mg Russian-made (30 pcs. In a package) can be bought at a price of 40-50 rubles, Finnish-made - 100-125 rubles. Tamoxifen tablets 20 mg (30 pcs. Per package), produced in Russia, costs 50-135 rubles, and produced in Finland - 130-215 rubles. Finnish-made tablets in a dosage of 20 mg (100 pieces per pack) are sold in pharmacies at a price of 600-700 rubles.

Tamoxifen: prices in online pharmacies

Drug name Price Pharmacy

Tamoxifen 10 mg tablets 30 pcs. RUB 30 Buy

Tamoxifen 20 mg tablets 30 pcs. RUB 49 Buy

Tamoxifen tablets 10mg No. 30 Ozone RUB 50 Buy

Tamoxifen 20 mg tablets 30 pcs. RUB 80 Buy

Tamoxifen 10 mg tablets 30 pcs. RUB 95 Buy

Tamoxifen tablets 20mg 30 pcs. Ozone 118 RUB Buy

Tamoxifen 10mg tablets 30 pcs. 118 RUB Buy

Tamoxifen Hexal 20 mg film-coated tablets 30 pcs. 130 RUB Buy

Tamoxifen tablets p.p. 20mg 30 pcs. RUB 180 Buy

Tamoxifen tablets 20mg 30 pcs. 209 RUB Buy

Tamoxifen 20 mg tablets 100 pcs. 399 RUB Buy

Tamoxifen tablets 20mg 100 pcs. 555 RUB Buy

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, 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!