Tamoxifen (Nolvadex another name, Tamoksimed) – a drug belonging to the group of sex hormones. Available in the form of tablets taken orally. Initially the drug intended for the treatment and prevention of breast cancer in women. Recently, however, I gained a lot of popularity among men bodybuilders. The reason is that most of the steroids taken by athletes, provoke the growth of estrogen, the female sex hormones, which adversely affects the man’s body in the form of so-called feminization. It is manifested in excessive water retention in the body, increasing body fat or even the growth of the breast, do not need any sane man. Tamoxifen is a nonsteroidal anti-estrogenic agents, i.e. it blocks estrogen receptors, so there is no connection “hormone receptor”. This normalizes blood estrogen and testosterone increases. Therefore, bodybuilders and bodybuilders take Tamoxifen to reduce weight while dieting and stimulate muscle growth, as well as for the prevention of adverse events during the course of steroids.

 

Dosing

During the course of tamoxifen steroids used primarily as a prophylactic measure to prevent gynecomastia (breast enlargement), and hormonal disorders. For this purpose, sufficient to take a dosage of 10 mg per day. Dose daily reception will vary in the amount of 10-30mg per day. In rare cases, the dose may be increased to 40mg. More than 40 mg is not recommended to take in order to avoid increased side effects.

In general, a single scheme of reception does not exist. Instructions supplied with the drug, can be thrown away immediately. It is designed for the reception of the funds for other purposes entirely. Individual reception algorithm must be developed specialist. But more often than Tamoxifen is introduced into the course, starting from the second week of reception anaboliticheskih steroids, because the level of estrogen in the blood increases it by the end of the first week of the course.

 

Note that Tamoxifen does not stop completely aromatization steroids, but only blocks the estrogen receptors. Therefore, a sharp increase in blood estrogen may occur after discontinuation of the drug. To avoid this, anti-estrogen drugs are taken in combination with aromatase inhibitors. Read more

The best effect has, in combination with Proviron. Tamoxifen deactivates estrogen receptors and Proviron prevents aromatization of steroids, what “tamoks” does not always cope alone. This is a time-tested and

many professional athletes complex, struggling with an excess of estrogen, which gives the best results.

How to take the course after Tamoxifen?

Why do you need post-cycle therapy (PCT):

• Restore your own testosterone
• Save to gain muscle mass
• Prevent feminization

Avoid testicular atrophy (chorionic gonadotropin is introduced for this purpose in FCT)

To reduce side effects from the course

Post-cycle therapy is necessary no matter how heavy or light the course was. During this period, continue to take Tamoxifen at a dose of 10-20mg per day in combination with Proviron for two – three weeks.

FCT also recommends a course with tamoxifen after 3-4 weeks after a course of steroids anaboliticheskih.

Tamoxifen, however, in no case can not be used after a course of steroids, which included trenbolone or nandrolone.

 

Of the side effects of Tamoxifen are sometimes observed:

 

• Fervescence
• dizziness
• nausea
• Reduced potency
• Partial baldness
• Rashes on the body (acne)
• Increased fatigue

 

 

 

 

 

However, it is worth noting that the correct approach to the reception of the drug and dosage to 30mg. day side effects are very rare.

 

 

 

Contraindications

 

Before using Tamoxifen is best to check their health, passing a comprehensive examination and consult with a specialist, because there are a number of contraindications.

 

Among them:

 

• Individual intolerance
• kidney disease
• Increased blood clotting
• diabetes
• Hormonal disorders
• liver disease

Considering the contraindications, do not assign themselves this drug alone. Health more awards at competitions and steep shapes of the body.

Also, do not get involved in this drug to women – athletes. It is fraught with hot flashes, excessive body weight, bone pain, irregular menstruation, endometriosis and even infertility.

 

tamoxifen woman

 

Admission results

 

In addition to prevention of estrogen growth and prevent the feminization of, use of the drug reaches several purposes:

 

1. Power indicators are improving.
2. Increased relief and muscle hardness.
3. The reduction of body fat.
4. The risk of developing atherosclerosis is significantly reduced, as the risk of cardiovascular diseases.
5. Improves liver function.

Conclusion

Apart from the main effect – blocking estrogen receptors, for which athletes take Tamoxifen, the drug is still a number of properties, beneficial effect on the body. In particular, it increases the level of “good cholesterol” in the blood. This high density cholesterol, which reduces the risk of atherosclerosis and other diseases of the heart and blood vessels. What is especially important for athletes who have a predisposition to such diseases. Besides “tamoks” – a mild drug and it does not load the liver. On the contrary, he helps her, because it has greater activity for blocking estrogen in this organ.

Tamoxifen also stimulates the release into the blood of a large number of gonadotropins, that contributes to the development of your testosterone, which is certainly a plus for the athlete.

Clinico-pharmacological group

Antiestrogen drug with antitumor activity

Pharmachologic effect

Tamoxifen is a nonsteroidal anti-estrogen agent having also weak estrogenic properties. Its action is based on the ability to block estrogen receptors. Tamoxifen, as well as some of its metabolites, estradiol compete for binding sites with cytoplasmic estrogen receptors in breast tissue, uterus, vagina, pituitary gland tumor and with a high content of estrogen receptors. In contrast to estrogen receptor complex receptor complex tamoxifen does not stimulate DNA synthesis in the nucleus and inhibits cell division that leads to tumor regression and cell death.

After oral administration, tamoxifen is well absorbed. Serum Cmax achieved in the range of 4 to 7 h after administration of a single dose. Tamoxifen equilibrium concentration in serum is usually achieved after 3-4 weeks of administration. Relationship to plasma proteins – 99%.

It is metabolized in the liver with the formation of metabolites.

Tamoxifen excretion from the body has a biphasic pattern with an initial T1 / 2 of 7 to 14 hours followed by a slow and a terminal T1 / 2 for 7 days. It provided mainly as conjugates, mainly with faeces and only a small amount excreted in urine. Read more

Dosage

The dosage regimen is generally determined individually depending on the evidence. The daily dose is 20-40 mg. As a standard dose is recommended to take 20 mg of tamoxifen daily for a long time inside. If signs of progression of the disease reception cancel preparation.

Tablets should be taken with liquid, squeezed small amounts of liquid, at once in the morning, or by separating the required dose into two doses, morning and evening.

Overdose

Acute overdose of tamoxifen in humans has not been observed. It is expected that an overdose can cause amplification of the above adverse reactions. There is no specific antidote, treatment should be symptomatic.

Drug interactions

When concomitant administration of tamoxifen and cytotoxic drugs increases the risk of thrombosis.

Antacids, histamine H2-blockers of receptors and other drugs of similar action by raising pH in the stomach can cause premature dissolution and loss of protective effect of enteric tablets. The interval between tamoxifen and these drugs should be 1-2 hours.

There are reports on the strengthening of the anticoagulant effect of drugs tamoxifen coumarin (eg warfarin).

Drugs that reduce the excretion of calcium (eg, thiazide diuretics number) may increase the risk of hypercalcemia.

The combined use of tamoxifen and tegafur can contribute to the development of chronic active hepatitis and cirrhosis.

Concomitant use of tamoxifen with other hormonal drugs (especially estrogensoderjath contraceptives) leads to a weakening of the specific actions of both drugs.

Pregnancy and lactation

Contraindicated.

Tamoxifen can cause ovulation, which increases the risk of pregnancy, in connection with which women who are sexually active, during (and for about 3 months after) treatment with tamoxifen is recommended to use a mechanical or non-hormonal contraceptive.

Side effects

When tamoxifen most common adverse reactions associated with its anti-estrogenic activity, manifested in the form of hot flashes (hot flushes), vaginal bleeding or discharge, itching in the genital area, alopecia, pain in the area of ??the lesion, ossalgia, weight gain.

Less frequently or infrequently observed the following side effects: water retention, anorexia, nausea, vomiting, constipation, fatigue, depression, confusion, headache, dizziness, drowsiness, fever, skin rash, visual disturbances, including corneal changes, cataracts , retinopathy and optic neuritis.

At the beginning of the treatment capacity of local worsening of the disease – an increase in the size of soft tissue structures, sometimes accompanied by severe erythema lesions and surrounding areas – which usually resolves within 2 weeks. It may increase the risk of thrombophlebitis and thromboembolism. Sometimes there may be transient leukopenia and thrombocytopenia, as well as an increase in liver enzymes, rarely accompanied by a severely impaired liver function, such as fatty liver, cholestasis and hepatitis.

In some patients with bone metastases at the beginning of the treatment of hypercalcemia observed.

Tamoxifen causes amenorrhea or irregular menstruation in women in pre-menopausal, as well as the development of reversible cystic ovarian tumors.

With long-term treatment with tamoxifen may experience endometrial changes including hyperplasia, polyps, and in rare cases – endometrial cancer, and the development of uterine fibroids.

Terms and Conditions of storage

List B. In a dry place at temperatures no higher than 25 ° C. Shelf life – 3 years.

testimony

– Estrogen-dependent breast cancer in women (especially in menopause) and male breasts.

The drug can be used to treat ovarian cancer, endometrial cancer, kidney cancer, melanoma, soft tissue sarcomas in the presence of estrogen receptor in the tumor, as well as for the treatment of prostate cancer with resistance to other drugs.

Contraindications

– Pregnancy;

– Lactation;

– Hypersensitivity to tamoxifen and / or any other ingredients of the formulation.

Precautions: renal failure, diabetes, eye diseases (including cataracts), deep vein thrombosis and thromboembolic disease (including history), hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia, concomitant therapy with indirect anticoagulants.

special instructions

Women taking tamoxifen should undergo regular gynecological examination. When bleeding from the vagina, or vaginal bleeding should stop taking the drug.

In patients with bone metastases periodically during the initial period of treatment should be determined the concentration of calcium in blood serum. In case of apparent violations of tamoxifen should be suspended.

If signs of thrombosis of the lower extremities (leg pain or swelling), pulmonary embolism (shortness of breath), the drug should be discontinued.

During therapy should be periodically monitored blood coagulation indices, blood calcium, blood count (leukocytes and platelets), liver function, blood pressure, inspect an ophthalmologist.

Patients with hyperlipidemia in the treatment necessary to control the concentration of cholesterol and triglycerides in the blood serum.

Effects on ability to drive vehicles and management mechanisms

In the period of treatment should refrain from activities potenialno hazardous activities that require high concentration and psychomotor speed reactions.