Gross formula
C 26 H 29 NOPharmacological group of the substance Tamoxifen
Nosological classification (ICD-10)
CAS Code
10540-29-1Characteristics of the substance Tamoxifen
Antitumor agent (anti-estrogen). Tamoxifen citrate is a white, odorless, crystalline powder. Very slightly soluble in water (1:5000), easily soluble in hot water (1:2), soluble in ethanol, methanol, acetone. Hygroscopic at high humidity, sensitive to ultraviolet radiation. Molecular weight 563.65.
Pharmacology
pharmachologic effect- antitumor, antiestrogenic.Competitively binds to estrogen receptors in target organs, like estrogens, translocates along with the receptor into the tumor cell nucleus and thus blocks the effect of estrogens.
Well absorbed from the gastrointestinal tract, T max - 4-7 hours, time to reach C ss - 3-4 weeks. Plasma protein binding - 99%. Metabolized in the liver by hydroxylation and demethylation. The main metabolite, N-desmethyl tamoxifen, has activity similar to that of tamoxifen. Elimination is biphasic with an initial T1/2 of 7-14 hours followed by a slow terminal T1/2 of 7 days. It is excreted primarily through the intestines, mainly in the form of metabolites, and a small amount by the kidneys.
Use of the substance Tamoxifen
Breast cancer: especially in menopausal women, in men after castration, carcinoma in situ mammary duct; adjuvant therapy for breast cancer. Estrogen-sensitive tumors; endometrial cancer.
Contraindications
Hypersensitivity, pregnancy, breastfeeding.
Restrictions on use
History of deep vein thrombosis and pulmonary embolism during treatment with indirect coumarin anticoagulants, thrombocytopenia, leukopenia, hypercalcemia, hyperlipidemia, cataracts or visual impairment.
Use during pregnancy and breastfeeding
Contraindicated during pregnancy (pregnancy should be excluded before starting treatment).
Breastfeeding should be discontinued during treatment (it is not known whether tamoxifen passes into breast milk).
Side effects of Tamoxifen
From the nervous system and sensory organs: headache, dizziness, fatigue, depression, confusion, blurred vision, corneal changes, cataracts and retinopathy.
From the cardiovascular system and blood (hematopoiesis, hemostasis): thrombophlebitis, thromboembolism, transient leukopenia, thrombocytopenia.
From the gastrointestinal tract: abdominal pain, nausea, vomiting, loss of appetite, constipation, increased levels of liver enzymes, severe liver dysfunction (cholestasis, hepatitis).
From the genitourinary system: bleeding or vaginal discharge, amenorrhea or irregular menstruation in premenopausal patients, the occurrence of reversible cystic ovarian tumor, fluid retention, itching in the genital area.
Allergic reactions: skin rash.
Others: alopecia, pain in the area of the lesion and/or in the bones, an increase in the size of soft tissue formations (accompanied by severe erythema of the affected areas and adjacent areas), hypercalcemia, paroxysmal sensation of heat, increased body temperature; with long-term use - cases of endometrial changes, including hyperplasia, polyps, intrauterine fibroids and in isolated cases - endometrial cancer.
Interaction
When combined with cytostatics, the risk of thrombosis increases. Estrogens may reduce the therapeutic effect of tamoxifen. Can be used in combination with progestins. Potentiates the effect of indirect anticoagulants.
Routes of administration
Inside.
Precautions for the substance Tamoxifen
Before starting treatment, women should undergo a thorough gynecological examination. Tamoxifen causes ovulation, which increases the risk of pregnancy, so women of reproductive age should use reliable methods of contraception (non-hormonal) during treatment and for 3 months after the end of treatment.
The drug should be stopped if bloody discharge from the vagina or vaginal bleeding appears, signs of thrombosis of the veins of the lower extremities (pain in the legs or swelling), or thromboembolism of the branches of the pulmonary artery (shortness of breath).
During treatment, it is necessary to monitor blood clotting indicators, blood patterns (leukocytes, platelets), and liver function indicators. An ophthalmological examination is recommended before and periodically during treatment.
In patients with bone metastases, serum calcium concentrations should be determined periodically during the initial treatment period (in case of severe hypercalcemia, tamoxifen should be temporarily discontinued). In patients with hyperlipidemia, during treatment it is necessary to monitor the concentration of cholesterol and TG in the blood serum.
Ineffective in treating patients with metastases (especially to the liver).
Interactions with other active ingredients
Trade names
| Name | The value of the Vyshkowski Index ® |
| 0.0087 | |
When malignant tumors are detected in the mammary glands and genital organs of men and women, doctors prescribe the drug Tamoxifen. It includes non-steroidal substances that have an anti-estrogenic effect, which suppresses the growth of pathological cells and normalizes hormonal levels. Read the instructions for use of the drug to use it correctly. Only a doctor prescribes treatment; do not take medication without his permission, it is dangerous.
Instructions for use of Tamoxifen
According to the accepted medical classification, the drug Tamoxifen is included in the group of hormone antagonists and similar drugs and has an anti-estrogenic effect. This effect of the drug is achieved due to the content of the active substance tamoxifen citrate, which binds estrogens in certain areas of the body and slows down the progress of tumor growth.
Composition and release form
Tamoxifen is available only in tablet format; there are no other drugs under this name. Composition and description:
Pharmacodynamics and pharmacokinetics
Tamoxifen is a non-steroidal substance and has an anti-estrogenic effect. This effect occurs due to the binding of estrogens in specific areas. Autogenous hormone receptors are suppressed, and the progress of tumor growth, which is stimulated by estrogens, slows down. After entering the stomach and intestines, the substance is quickly absorbed.
The maximum concentration of the component is observed 4-7 hours after administration, the state of equilibrium occurs after 4-6 weeks. Almost 99% of the drug is bound to plasma proteins (albumin). Metabolism of the drug occurs in the liver, the drug is excreted in bile and urine. Excretion is biphasic, elimination lasts 14-28 hours for the first phase and 14 days for the second.
Indications for use
The instructions for use included inside each pack of tablets contain information about the indications for use of the drug. These include diseases and conditions:
- adjuvant therapy for breast cancer in women;
- treatment of breast cancer with affected lymph nodes and metastases in men and women;
- breast cancer in premenopausal women;
- breast cancer in men after castration;
- kidney, ovarian, prostate cancer;
- melanoma, carcinoma containing estrogen receptors.
How to take Tamoxifen
In addition to treating breast and endometrial cancer, the drug can be taken by bodybuilders to increase endurance and muscle efficiency. Depending on the purpose of Tamoxifen, the dosage, mode of use, and duration of therapy differ. The tablets are taken orally, washed down with water. The dosage regimen is determined individually by the doctor, based on the patient’s position, the severity of the disease, and the stage of progress.
For breast cancer and endometrial cancer
For breast cancer, the daily dose of the drug is 20 mg; for the common form of the disease, the dosage will be 30-40 mg/day, and the maximum is 40 mg. Doctors note an objective response to therapy 4-10 weeks after the start of treatment; with metastases in bone tissue, the effect may appear several months after the accumulation of the active substance.
The tablets are not chewed, washed down with liquid, when more than 2 tablets are prescribed. can be divided into several steps. The course of treatment lasts until remission is achieved and is determined by the doctor. If necessary, therapy is supplemented with cytostatic agents and radiation treatments. If a single dose of tablets is indicated, the dose is taken in the morning.
Application in bodybuilding
Due to the fact that Tamoxifen increases testosterone levels in the body, it is used in sports and bodybuilding. Taking the drug 20 mg in a ten-day course increases the level of male hormones in the blood by 42%, and after a month and a half the effect will be 83%. The goals of using the medication are also to increase muscle mass, definition, increase overall body weight or reduce fat concentration, prevent gynecomastia, fluid accumulation, and fat deposits.
Tamoxifen prevents the development of iron deficiency anemia, jaundice, liver dysfunction, hepatonecrosis, hypocoagulation, and masculinization in women. The drug is used in post-course therapy. The dose is selected individually (10-40 mg/day); taking less than 30 mg/day is not accompanied by side effects. The full course is seven packs of 30 tablets.
How to take Tamoxifen after a course
The drug is taken after a course of steroids - in the second week of the steroid cycle. This feature is associated with an increase in estrogen levels by the end of the first week of the cycle. The end of the course occurs 2-4 weeks after completion of steroid use. The daily dose of the drug is 20-60 mg 2-3 times/day. To calculate the dosage after a course of androgens, luteotropins and anabolic steroids (AAS), the following rules are used:
- total dose of AAS less than 0.5 g/week - dose of Tamoxifen 20 mg/day;
- 0.5-1 g/week – 40 mg/day;
- more than 1 g/week – 60 mg/day.
When comparing Tamoxifen with other drugs aimed at reducing the side effects caused by anabolic steroids and improving athletic performance, the drug in question wins or vice versa. Compared to Proviron, less product is required, but Proviron is an estrogen antagonist and suppresses the formation of hormones, preventing aromatization of steroids and atherosclerosis. Men are advised to choose Proviron, it acts on the cause, and does not just mask and eliminate the symptoms of the problem.
If an athlete takes anabolic steroids that are not subject to aromatization, there is no need to use aromatase inhibitors; Tamoxifen is included in the intake at the final stage of the cycle. Compared to Clomid, it is preferable. Tamoxifen has less effect on the pituitary gland, but restores the level of endogenous testosterone equally well, does not increase the level of testosterone-binding globulin, and is cheaper.
special instructions
The use of the drug is associated with a number of rules, which are described in the special instructions paragraph of the instructions. Excerpts from there:
- the medication is used with caution in the treatment of patients with kidney pathologies, diabetes mellitus, ophthalmological diseases, a history of thromboembolic lesions, leukopenia, thrombocytopenia, hypercalcemia;
- long-term use of the medication requires constant monitoring of the level of calcium, leukocytes, coagulation parameters and platelets in the blood, observation by an ophthalmologist for studies of intracranial and ocular pressure;
- It is unlikely that the drug reduces the speed and concentration of attention, clarity of vision, therefore the drug is approved for use while driving vehicles and driving dangerous mechanisms.
During pregnancy
Before starting therapy, patients undergo a thorough examination; pregnancy should be excluded. Women of childbearing age are required to reliably protect themselves during the entire course of treatment and for another three months after completion, replace oral contraceptive pills with barrier contraceptives. The use of Tamoxifen during pregnancy and breastfeeding is prohibited; this risks disrupting hormonal levels and development with the growth of the fetus or newborn child.
Alcohol compatibility
According to doctors, it is strictly forbidden to combine the drug with alcohol, alcohol-containing drinks and medications. This leads to increased load on the liver, risk of poisoning and reduced effectiveness of the medication.
Drug interactions
During therapy with Tamoxifen, caution should be exercised when prescribing other medications. Combinations and risks:
- combination with other hormonal drugs, especially those containing estrogens, is prohibited;
- coumarin drugs that affect blood coagulation require Tamoxifen dose adjustment;
- cytostatics, diuretics increase the risk of thrombosis;
- Bromocriptine increases the concentration of the active substance and metabolites in the blood plasma, its dopaminergic effect is enhanced;
- Allopurinol enhances the hepatotoxic effect, aminoglutethimide reduces the concentration of the substance in plasma;
- the drug prolongs the neuromuscular blockade caused by Atracurium;
- increases prothrombin time, causes hematuria and hematomas in combination with Warfarin;
- Rifampicin reduces the concentration of the active component in the blood plasma;
- Antacids and antihistamines provoke a premature loss of the effect of the pill, so 1-2 hours should pass between taking medications.
Side effects
The instructions for use indicate the side effects of Tamoxifen in women and men. These include:
- leukopenia, thrombocytopenia, neutropenia, pancytopenia;
- hot flashes, vaginal, uterine bleeding, menstrual irregularities, vaginal discharge, itching of the genitals, vulva;
- endometrial hyperplasia, polyps, endometriosis, endometrial cancer;
- cessation of menstruation, reversible cystic edema of the ovaries and the development of cysts;
- impotence, loss of libido, myasthenia gravis;
- nausea, vomiting, anorexia, loss of taste, constipation, diarrhea, increased acidity of gastric juice;
- decreased visual acuity, corneal opacities, cataracts, retinopathy;
- pancreatitis, hypertriglyceridemia, fatty liver infiltration, hypertrophy;
- cholestasis, hepatitis, alopecia (baldness), erythema multiforme;
- hypersensitivity, angioedema;
- bullous pemphigoid;
- thrombosis, pulmonary embolism.
Overdose
According to doctors, there were no acute cases of Tamoxifen overdose. Manifestations of drug poisoning include increased side effects. To eliminate them, you must urgently consult a doctor for treatment. There are no specific antidotes to the substance, hemodialysis is not effective, symptomatic therapy and drug withdrawal are prescribed.
Contraindications
From the instructions for use of the drug you know about its contraindications. These include:
- hypersensitivity to the components of the composition;
- pregnancy, lactation (breastfeeding);
- children and adolescents up to 18 years of age;
- severe thrombocytopenia, leukopenia;
- hypercalcemia;
- pulmonary embolism, deep vein thrombosis;
- cataracts, liver dysfunction;
- severe thrombophlebitis;
- hyperlipidemia.
Terms of sale and storage
The drug can only be purchased with a prescription; it is stored at temperatures up to 25 degrees, away from children, in a dry, dark place for three years.
What can replace Tamoxifen?
Tamoxifen analogue in the treatment of breast cancer can be either direct or indirect. The first group includes drugs with the same composition, the second - with the same therapeutic effect, but different components. Analogs of the drug are:
- Zitazonium, Vero-Tamoxifen - direct analogues, synonyms with the same substance;
- Fareston, Faslodex - drugs contain toremifene and have antitumor and antiestrogenic effects. Tamoxifen. What it is. Watch the video
Tamoxifen is prescribed worldwide for the treatment and prevention of estrogen-dependent malignancies in both men and women. But the drug has become most widespread as an effective remedy in the fight against breast cancer in the fair sex.
It is often used in sports pharmacology in conjunction with anabolic steroids. However, doctors warn that this substance is classified as prohibited, and its detection in the results of doping tests leads to disqualification.
The drug is not intended for parenteral administration and is available in tablet form. Each pill contains tamoxifen citrate in a single dose (10, 20, 30 or 40 mg). Of the auxiliary components, manufacturers use “standard” lactose, cellulose, starch, magnesium and silicon compounds.
In accordance with the pharmacological classification, the drug belongs to the group of antitumor drugs. According to the principle of action of tamoxifen citrate, it is a selective estrogen receptor modulator. In structure, each receptor is a protein that is modified under the influence of other proteins of a strictly defined type. They can be located both on the surface of the cell membrane and inside the cell itself. But in any case, receptors provide a response to the influence of a particular substance (hormone, neurotransmitter, etc.).
In fact, Tamoxifen is not a hormone-like drug, since it does not have estrogenic activity and does not affect testosterone synthesis. The active ingredient of the drug is similar to estrogen only in structure, and not in its effect on the body. And due to this tamoxifen citrate interacts with specific cellular receptors, roughly speaking, blocks them and makes them immune to estrogen.
Moreover, it affects all receptors of this type, regardless of their location:
- cells of the mammary and mammary glands in women and men;
- prostate tissue;
- uterus, vagina;
- anterior pituitary gland;
- soft fabrics, etc.
During malignant transformation of cells, the estrogen-receptor connection leads to pathological division of cellular structures. However, the tamoxifen citrate-receptor complex in no way affects DNA synthesis in the nucleus, but rather, on the contrary, inhibits malignant tissue proliferation. It is thanks to this property that this drug has found wide use in oncology.
The unique properties of this drug (despite quite numerous side effects) served as an impetus for the study of its additional properties and effects on the human body. Thus, experts have found that Tamoxifen can be successfully used for severe damage to the central nervous system.
Clinical trials conducted with volunteers demonstrated its effectiveness in:
- spinal cord injuries;
- Alzheimer's disease;
- Parkinson's disease;
- multiple sclerosis (this disease is extremely difficult to treat. The innovative medicine Cladribine or drugs based on teriflunomide are successfully used for treatment);
- severe cognitive disorders of other origins.
The mechanism of the neuroprotective action of Tamoxifen is associated with its effect on dopamine receptors. But the possibility of using the drug in neurology is currently being studied in clinical trials.
When taken orally, tamoxifen citrate is rapidly absorbed from the digestive tract and is almost completely bound to plasma proteins. The time to reach maximum concentration is individual for each patient and on average ranges from 4 to 7 hours.
Further transformation of the drug occurs in the liver with the formation of therapeutically active metabolites. The drug is released primarily through the intestines in two stages: 7 - 8 hours after administration, and then a week later. Equilibrium therapeutic concentrations of the drug in the blood are achieved on the 7th - 10th day of therapy.
Tamoxifen: instructions for use, use in bodybuilding, adverse reactions and contraindications
As a rule, the drug is prescribed only when malignant neoplasms that are sensitive to the influence of hormones from the estrogen group are detected.
Tamoxifen is prescribed for:
- breast cancer in women (in this case, the doctor may prescribe the drug Kisqali, Halaven, Kadcyla, a drug based on pertuzumab or pablociclib);
- oncological lesions of the mammary glands in representatives of the stronger sex;
- malignant prostatic hyperplasia (in the absence of effect from other methods of conservative therapy);
- adnexal cancer in women;
- malignant lesions of the endometrium, lining the inner surface of the uterine walls;
- prolactinoma (benign adenoma) of the pituitary gland;
- some types of melanomas;
- sarcomas formed in soft tissues;
- kidney cancer.
But in the vast majority of cases, Tamoxifen is prescribed for the treatment of breast cancer in men and women. According to experts, the growing number of favorable outcomes of this disease over the past 10 years is due to the use of this drug.
Sometimes the drug is prescribed when there is a decrease or complete absence of active sperm in the seminal fluid. The medicine is also prescribed after surgery on the male genital organs (testicles, prostate gland, etc.) to prevent severe hormonal disorders.
If the doctor prescribes Tamoxifen, the instructions for use do not give clear instructions regarding the dosage of this drug. This is due to the fact that the required amount of the drug should be determined only by the doctor based on the patient’s condition, the patient’s well-being and the presence of concomitant pathologies.
Take the medicine either once a day (in the morning), or divide the prescribed dosage in half and drink twice a day (morning and evening). In this case, Tamoxifen should be taken strictly at the same time, avoiding omissions or delays. The duration of treatment is also determined individually, but the course of use is rarely less than several months.
Features of the use of Tamoxifen in bodybuilding
It is no secret that professional sports is closely related to pharmacology. Many men prefer to improve their training results by using a variety of drugs that are far from harmless.
One of the most commonly used drugs in bodybuilding and bodybuilding are anabolic steroids. They help quickly build muscle mass and increase endurance during intense physical activity. However, long-term use of such medications, especially in high doses, is fraught with serious side effects.
The fact is that steroids, as a result of metabolic transformations in the male body, are converted into estrogens. The most striking external manifestation of this process is gynecomastia, that is, an increase in the size of the mammary glands. To prevent this effect, it is necessary to take Tamoxifen, although the instructions for use do not describe this method of achieving sports results.
There is an opinion among bodybuilders that the drug has the following effect:
- helps “dry out” fat deposits;
- increases physical endurance;
- helps build muscle mass;
- prevents lipid metabolism disorders;
- has a hepatoprotective effect.
A number of these effects have not been clinically confirmed, however, Tamoxifen is included in most pharmacological correction regimens for athletes. It is taken only in combination with steroid drugs.
Tamoxifen administration begins at 2 - 3 weeks of using steroid medications at a dosage of 0.01 - 0.02 g per day. The use of the medicine is continued for another 14 - 21 days after the end of steroid therapy.
Restrictions on taking Tamoxifen
All contraindications to the use of the drug given in the instructions can be divided into two groups: absolute, in which the use of the drug is strictly prohibited, and relative, when the course of treatment must be completed only under the supervision of a doctor, and Tamoxifen should be taken in the minimum possible dosage.
Absolute contraindications include:
- individual allergic reaction to the components of the drug;
- period of childbearing and breastfeeding;
- age under 18 years due to lack of clinical and practical experience in use.
In women, taking Tamoxifen can stimulate ovulation, especially during menopause. In animal experiments, it was found that the drug causes severe damage to the musculoskeletal, genitourinary, digestive and nervous systems of the fetus, intrauterine death at different stages of pregnancy, and miscarriages. Therefore, while taking Tamoxifen, women are recommended to use reliable, but not hormonal, contraceptives. Take a pregnancy test or hCG test every four weeks so that you can have an early abortion relatively safely.
Relative contraindications to the use of Tamoxifen are:
- violation of the rheological properties of blood;
- thrombophlebitis and varicose veins of the extremities or pelvic organs due to the risk of exacerbations;
- severe liver pathologies, possible stagnation of bile and hepatitis;
- damage to the organs of vision;
- blood lipid profile disorders;
- increased calcium concentration;
- disturbances in the absorption and metabolism of lactose.
In such cases, Tamoxifen is started in a medical facility with a minimum dose. Then, if the patient feels well and is well tolerated, the dosage is gradually increased to a therapeutically justified dose. If any complications occur, treatment with Tamoxifen is stopped immediately.
Adverse reactions
All side effects caused by the drug are due to blocking the influence of estrogen interaction with cellular receptors. Therefore, unwanted reactions occur quite often.
Note:
- hot flashes and increased sweating;
- bloody vaginal discharge not associated with the menstrual cycle;
- increased hair loss;
- irritation and discomfort in the external genital area;
- the emergence of a problem of excess body weight;
- swelling;
- lack of appetite;
- nausea, vomiting, epigastric pain;
- bowel disorders;
- drowsiness, feeling of constant fatigue, depression;
- headache and dizziness;
- fever;
- convulsions and paresthesia;
- visual disturbances;
- amenorrhea in women, decreased libido and erectile dysfunction in men.
When treating malignant soft tissue lesions during the first 10 to 14 days of treatment, a reversible increase in their size, pain and redness of the skin in the area of their localization is possible. This condition requires mandatory and constant monitoring by a doctor. If the situation does not improve, the drug is discontinued.
If you are predisposed to vascular diseases, the development of varicose veins and thrombophlebitis is possible. In women over 45 years of age, benign ovarian cysts sometimes form, which resolve after stopping Tamoxifen therapy without medication or surgery. There is also a risk of endometrial growth with subsequent development of endometriosis and fibroids.
To date, there is no information about cases of Tamoxifen overdose either in the description of the drug or in scientific publications. But doctors suggest that the severity of adverse reactions and neurological disorders may increase. Due to the connection with blood proteins, the introduction of antidotes is impractical. Therefore, overdose treatment is carried out depending on the patient’s symptoms and complaints.
Tamoxifen for men: interactions with other medications, cost, analogues, reviews
The drug can not be used simultaneously with all medications. Thus, attention must be paid to the following aspects:
- When treating with antacids, using medications for the treatment of gastritis, peptic ulcers and reducing high acidity, it is necessary to observe at least a two-hour interval between taking Tamoxifen and these medications. Otherwise, its effect may be reduced.
- When used simultaneously with a number of diuretics and other medications that retain calcium in the body, a critical increase in the level of this mineral is possible.
- Combination with cytostatics significantly increases the likelihood of blood clots.
- Tamoxifen and hormonal contraceptives mutually reduce the therapeutic effect.
Patients often ask their doctor about the compatibility of the drug with alcohol. The fact is that Tamoxifen tablets for women and men are metabolized in the liver (like alcohol) and affect the nervous system. Therefore, simultaneous intake of alcoholic beverages reduces the effect of therapy on the one hand and increases the likelihood of complications on the other.
The cost of Tamoxifen largely depends on the manufacturing company, the number of tablets in the package and their dosage. The price of an imported drug ranges from 180 to 200 rubles (30 tablets of 0.02 g), while for a domestic drug you will have to pay about 140 rubles.
Tamoxifen is also offered in pharmacies under other trade names:
- Nolvadex;
- Novofen;
- Tamoplex;
- Bilen.
Other antiestrogenic antitumor drugs have a similar effect:
- Fareston;
- Faslodex (intended for injection).
Currently, Iscador is also used, a drug based on natural ingredients. Torisel or Nolvadex are often prescribed to treat kidney cancer.
Zharkov Igor Konstantinovich, oncologist, doctor of the highest category, Ph.D.“Tamoxifen is primarily attractive due to the combination of effect and cost. Unlike other drugs for the treatment of breast cancer, this drug is relatively inexpensive, but at the same time it stops the spread and growth of malignant tumors. “I know about the use of Tamoxifen to improve athletic performance, but as a doctor, it is recommended to take it only under strict indications and as prescribed by a doctor.”
Igor, 24 years old. “I’ve been working out in the gym for about 5 years and have always been focused on visible results. Simple workouts to strengthen muscles did not interest me. Together with the trainer, we created a training program with the parallel use of steroids and Tamoxifen. I took medications according to the schedule. Endurance has noticeably improved, the fat layer has disappeared, and the muscles have acquired the desired relief. I haven’t noticed any complications yet, however, I advise you to weigh everything carefully before repeating my experience.”
Tamoxifen for men is a potent drug that should not be taken without first consulting a doctor. There are a number of strict indications for its use. The medicine often causes unwanted reactions; it should be taken only under the supervision of a doctor and laboratory blood test results.
Tamoxifen – Tamoxifen citrate is a non-steroidal anti-estrogen drug that is widely used in clinical medicine. It is classified as a selective regulator of estrogen receptor activity, with agonistic and antagonistic properties. Chemical formula (Z)2--N,N-dimethylethanamine-2-hydroxy-1,2,3-propanetricarboxylate.
Historical reference
Tamoxifen was first synthesized in 1962 by ICI. Used in the USA to treat some forms of infertility in women. Since 1971, it began to be used in the treatment of breast cancer. Since 1977, the drug has been on the market in many countries under various names and is beginning to enjoy popularity.
Pharmacological action (according to the manufacturer)
Tamoxifen is classified as a non-steroidal antiestrogenic drug, despite this, it has weak estrogenic properties. The action of the drug is based on the ability to block estrogen receptors. Tamoxifen and some of its metabolites compete with estradiol for binding sites for cytoplasmic estrogen receptors in breast, uterine, vaginal, anterior pituitary and estrogen receptor-rich tumors. Unlike the estrogen receptor complex, the tamoxifen receptor complex does not have a stimulating effect on DNA synthesis in the nucleus; it suppresses cell division, and this leads to regression of tumor cells, and subsequently death.
Properties of tamoxifen
This is a substance of non-steroidal origin, a derivative of triphenylethylene, which has a mixed agonist/antagonist effect. Tamoxifen is used in medical practice as a means of influencing breast cancer caused by excessive estrogenic activity. It works by blocking endogenous estrogen from exerting its biological properties.
Male athletes use it to combat the side effects of AAS aromatization (except for the fight against prolactin gynecomastia from nandrolones). One of the problems in the sports world is gynecomastia, that is, the development of breast tissue in men. Initially, it may appear as swelling or a small lump in the nipple area. Later, this can turn into denser and more voluminous tissue, up to the need for surgical intervention. Estrogen leads to water retention and an increase in the amount of subcutaneous fat. In addition, the drug stops the negative feedback of estrogen along the hypothalamic-pituitary-testicular axis, affecting the increase in the production of gonadotropins (LH and FSH). In this action it resembles Clomid and cyclophenyl. More LH means more testosterone. This effect is most appreciated after the “course”, as part of a comprehensive PCT program.
Do not forget that all triphenylethylene compounds (tamoxifen citrate, clomiphene citrate, toremifene citrate) most often have an estrogen-like effect in the liver. What this means is that they can block estrogen in some areas of the body, while still working as estrogen in other areas. An important role here is the ability to regulate the level of synthesis of good and bad cholesterol. People who use steroids are likely to develop cardiovascular risk factors that are exacerbated by the use of aromatase inhibitors. The use of tamoxifen can lead to the disappearance of gynecomastia and at the same time maintain the necessary balance of good and bad cholesterol.
Use of tamoxifen
Reception (for men):
When taking the drug to suppress estrogenic side effects, the dose is 10-30 mg per day. To suppress already developed signs of gynecomastia, 40 mg per day (20 mg in the morning and 20 mg in the evening). For PCT (post-cycle therapy, it usually lasts 3 weeks), as a rule, 40 mg per day is sufficient (20 mg in the morning and 20 mg in the evening), if the course of steroids was short or weak (a course with oxandrolone), then you can get by with 20 mg per day (10 mg in the morning and 10 mg in the evening).
Reception (for women):
Tamoxifen is used by women only in one case - in the fight against breast cancer.
Side effects of tamoxifen
- From the digestive system: nausea, vomiting, increased activity of liver transaminases; in some cases - fatty liver infiltration, cholestasis, hepatitis.
- From the central nervous system: rarely - depression, dizziness, headache, retrobulbar neuritis.
- On the part of the organ of vision: uncommon – retinopathy, keratopathy, cataract.
- From the hematopoietic system: uncommon – thrombocytopenia, leukopenia. (in this regard, people with thrombophlebitis, thrombocytopenia, and leukopenia are not advised to use this drug!)
- From the endocrine system: in women – endometrial hyperplasia, vaginal bleeding, hot flashes, weight gain; in men - impotence, decreased libido.
- From the cardiovascular system: edema, thromboembolism, phlebitis.
- Dermatological reactions: alopecia, rash, itching.
- Other: pain in bones and lesions, increased body temperature.
It should be said that the side effects of tamoxifen appear in cases of long-term use in doses of 40 mg per day and above. It turns out that PCT for 3-4 weeks or the use of tamoxifen at a dose of 10 mg per day during a course of steroids will almost never cause any of the described side effects.
Indications for medicinal use
Breast cancer in menopausal women, breast cancer in men after castration, kidney cancer, melanoma (containing estrogen receptors), ovarian cancer; prostate cancer with resistance to other drugs.
Contraindications for medical use
Thrombophlebitis, pregnancy, hypersensitivity to tamoxifen.
medicine
Tamoxifen
Tradename
Tamoxifen
International nonproprietary name
Tamoxifen
Dosage form
Tablets 10 mg, 20 mg
Compound
One tablet contains
active substance - tamoxifen citrate 15.2 mg and 30.4 mg
(equivalent to tamoxifen 10 mg and 20 mg),
Excipients: lactose monohydrate, microcrystalline cellulose, magnesium or calcium stearate, colloidal anhydrous silica
Description
White, flat-cylindrical tablets with an engraving of the letter “G” on one side (for a dosage of 10 mg) and an engraving of the letter “G” on one side and a cross-shaped mark on the other side (for a dosage of 20 mg)
Pharmacotherapeutic group
Antitumor hormonal drugs. Hormone antagonists and their analogues. Antiestrogens. Tamoxifen.
ATX code L02BA01
Pharmacological properties
Pharmacokinetics
Tamoxifen is rapidly absorbed when taken orally. The maximum concentration in blood plasma is 4-7 hours after administration. Equilibrium plasma concentrations are achieved after 4 weeks of therapy. The half-life is about 7 days. Tamoxifen is metabolized by hydroxylation and demethylation in the liver, undergoes enterohepatic recirculation, and is excreted in the bile in the form of metabolites.
Pharmacodynamics
Tamoxifen has an antitumor effect, the mechanism of which is due to the ability to competitively inhibit estrogen receptors in target organs and tumors originating from these organs. As a result, a complex appears that translocates together with the receptor into the tumor cell nucleus and inhibits the hypertrophy of cells dependent on estrogen regulation. It has antioxidant properties and is able to suppress the synthesis of prostaglandins in tumor tissue.
Indications for use
Estrogen-dependent breast cancer in women (especially in menopause) and breast cancer in men.
- kidney cancer
- estrogen receptor-containing melanoma
- ovarian cancer
- prostate cancer with resistance to other drugs
Endometrial cancer
Soft tissue sarcoma in the presence of estrogen receptors in the tumor
Directions for use and doses
The dosage regimen is set individually, depending on the indications, the patient’s condition and the antitumor therapy regimen used. The average dose is 20-40 mg per day.
The tablets should be taken without chewing, with a small amount of liquid, in one dose in the morning, or dividing the required dose into two doses - morning and evening.
The maximum single dose is 40 mg. The maximum daily dose is 40 mg. The duration of treatment is determined individually depending on the indications.
Side effects
When treating with tamoxifen, the most common adverse reactions are those associated with its antiestrogenic effect.
Often:
- paroxysmal sensations of heat (hot flashes)
- vaginal bleeding or discharge, itching in the genital area
- alopecia
- pain in the affected area
- ossalgia
- weight gain
Rarely:
- fluid retention, peripheral edema
- anorexia, nausea, vomiting, constipation or diarrhea
- increased fatigue, depression, confusion, headache
pain, dizziness, drowsiness, myasthenia gravis
- increase in body temperature
- skin rash, dry skin
- visual impairment including corneal changes, cataracts, retinopathy and retrobulbar neuritis
At the beginning of treatment, an exacerbation of the disease is possible:
- an increase in the size of soft tissue formations, sometimes accompanied by severe erythema of the affected areas and surrounding areas, which usually resolves within 2 weeks
- the likelihood of thrombosis, thrombophlebitis and thromboembolism may increase
- Transient leukopenia and thrombocytopenia may sometimes occur, as well as an increase in liver enzymes, very rarely accompanied by more severe liver dysfunction (such as fatty liver, cholestasis and hepatitis)
- Some patients with bone metastases experienced hypercalcemia at the start of treatment
- tamoxifen causes metrorrhagia, amenorrhea or irregular menstruation in women in the premenopausal period, as well as the reversible development of cystic ovarian tumors, vaginal discharge; with long-term treatment with tamoxifen, changes in the endometrium can be observed (including hyperplasia, polyps and in isolated cases endometrial cancer, as well as the development of fibroids uterus)
- in men there may be a decrease in potency and/or libido.
Contraindications
- thrombophlebitis
Hypersensitivity to tamoxifen or any other component of the drug
- children and teenagers up to 18 years of age
- pregnancy and lactation
- hereditary fructose intolerance, Lapp lactase enzyme deficiency, glucose-galactose malabsorption
Carefully
- renal failure
- diabetes
- eye diseases (including cataracts)
- deep vein thrombosis and thromboembolic disease (including history)
- hyperlipidemia
- severe leukopenia and thrombocytopenia
- hypercalcemia
Drug interactions
When used simultaneously with anticoagulants, coumarin derivatives, the risk of increased anticoagulant action increases; with cytostatics - there may be an increased risk of thrombosis.
When used simultaneously with allopurinol, increased toxic effects on the liver are possible; with aminoglutethimide - a decrease in the concentration of tamoxifen in plasma (apparently due to an increase in its metabolism).
In patients receiving tamoxifen, the neuromuscular blockade caused by atracurium may be prolonged.
With simultaneous use of bromocriptine, the dopaminergic effect of bromocriptine may be enhanced.
In patients receiving tamoxifen, when using warfarin, there is a risk of developing a threatening clinical situation - a possible prolongation of prothrombin time, hematuria, and the development of hematomas.
When used simultaneously with mitomycin, the risk of developing hemolytic-uremic syndrome increases.
When used simultaneously with rifampicin, a decrease in the concentration of tamoxifen in the blood plasma is possible, which is due to the induction of the cytochrome P 450 isoenzyme CYP3A4 under the influence of rifampicin.
Estrogens may reduce the therapeutic effect of tamoxifen.
Antacids, H2-histamine receptor blockers and other drugs of similar action, increasing the pH value in the stomach, can cause premature dissolution and loss of the protective effect of the enteric coating of the tablet. The interval between taking tamoxifen and these drugs should be 1-2 hours.
Drugs that reduce calcium excretion (for example, thiazide diuretics) may increase the risk of developing hypercalcemia.
special instructions
Use with caution for leukopenia, thrombocytopenia, hypercalcemia, in patients with cataracts, hyperlipidemia. During treatment, the peripheral blood picture (especially the platelet count), calcium and glucose levels in the blood should be regularly monitored. With long-term use, observation by an ophthalmologist is indicated (every 3 months).
Women receiving tamoxifen should undergo regular gynecological examinations. If bloody vaginal discharge or vaginal bleeding occurs, you should stop taking the drug and undergo a thorough medical examination.
In patients with bone metastases, serum calcium concentrations should be periodically determined during the initial treatment period, especially when thiazide diuretics are used concomitantly. In case of severe disturbances, tamoxifen should be temporarily discontinued.
When treated with the drug, the likelihood of thrombosis and thromboembolism may increase. Women at increased risk of thromboembolism should be carefully evaluated. If signs of thrombosis of the lower extremities appear (pain in the legs or swelling), pulmonary embolism (shortness of breath), the drug should be discontinued.
At the beginning of treatment, an exacerbation of the disease is possible - pain and an increase in the size of soft tissue formations, sometimes accompanied by severe erythema of the affected areas and adjacent areas - which usually resolves within 2 weeks.
Tamoxifen causes amenorrhea or irregular menstrual periods in premenopausal women. The development of reversible cystic changes in the ovaries may occur.
In patients with hyperlipidemia, during treatment it is necessary to monitor the concentration of cholesterol and triglycerides in the blood serum.
Before starting treatment with the drug, you should undergo a thorough ophthalmological examination. If visual disturbances appear during treatment, an urgent ophthalmological examination is necessary, since some disturbances may disappear after cessation of treatment if detected in the early stages.
Pregnancy and lactation
Before starting treatment with Tamoxifen, pregnancy should be excluded. Tamoxifen may cause ovulation, which increases the risk of pregnancy; therefore, effective non-hormonal contraception should be provided during treatment and for 2 months after completion of treatment with tamoxifen.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
Given the side effects, caution should be exercised when driving vehicles or potentially dangerous machinery.
Overdose
Symptoms: allergic reactions, itching, skin hyperemia, skin rash, tachycardia, increased levels of uric acid in the blood.
Treatment: symptomatic.
Release form and packaging
10 tablets each in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil. 3 blisters each along with instructions for medical use in the state and Russian languages in a cardboard pack.
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 o C.
Keep out of the reach of children!
Shelf life
Do not use the drug after the expiration date.
Conditions for dispensing from pharmacies
On prescription
Manufacturer
tel. +7 727 309 74 07,
fax +7 727 309 74 14
Registration Certificate Holder
Abdi Ibrahim Global Pharm LLP, Kazakhstan
Almaty, st. Dzhandosova 184 "g",
Address of the organization that accepts claims from consumers regarding the quality of products (products) on the territory of the Republic of Kazakhstan
Abdi Ibrahim Global Pharm LLP, Kazakhstan
Almaty, st. Dzhandosova 184 "g",
Phone number +7 727 309 74 07
Fax number +7 727 309 74 14
E-mail address [email protected]
