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toremifene citrate - refers to anti-estrogen drugs. It is produced in the form of tablets. In bodybuilding, it is used by people as a drug for PKT. Its action is to block the process of aromatization, which can cause gynecomastia when taking steroid drugs. The structure of the drug is similar to Tamoxifen, but unlike the latter, it does not have as many side effects.
The pharmacological action is anti-estrogenic, antitumor.
It penetrates into tumor cells, competitively binds with estrogen receptors and prevents formation of estrogenreceptor (17-beta-estradiol+receptor) complex, inhibits estrogen-stimulated DNA synthesis and suppresses replication. Induces transformation of growth factor inhibiting oncogenesis, affects oncogenic regulation leading to apoptosis of cancer cells. In high doses it is effective with insufficient action of hormonal and cytostatic drugs. Thus, in patients resistant to tamoxifen, using high doses of toremifene reduces tumor size.
Effect on Cardiac Electrophysiology. The effect of 20, 80, and 300 mg (about 5 times the recommended dose of 60 mg) of toremifene on the QT interval was evaluated in a double-blind, randomized study in healthy men aged 18 to 45 years. The QT interval was measured at toremifene equilibrium (on day 5 of dosing) for 24 hours. A dose- and concentration-dependent increase in the QT interval and an ECG T-wave change was observed, presumably caused by toremifene and N-demethyltremifene. Toremifene had no effect on HR, PR and QRS interval duration.
When administered orally it is rapidly absorbed, Tmax is 3 hours. It is biotransformed in liver by hydroxylation and demethylation with CYP3A4 with N-demethyltoremifene formation, which shows weak antitumor activity in vivo. Excretion is biexponential: T1/2 in the distribution phase is 4 hours, the final T1/2 is about 5 days. It is excreted as metabolites, mainly in the faeces, about 10% - in the urine within 1 week.
Toremifene citrate helps achieve these effects:
- Block excess estradiol, which has arisen due to aromatization, after taking androgenic steroids, and to prevent estrogen-related side effects of gynecomastia;
- Restore the natural level of endogenous testosterone in the blood;
- stimulate the production of gonadotropic hormones, which include follicle-stimulating and luteinizing hormone, which helps reduce the phenomenon of rebound.
The drug can cause side effects if the dosage is exceeded. These include dizziness, nausea, increased sweating, and allergies. It is possible to avoid "side effects" if the drug is taken correctly.
The nervous system and sensory organs: dizziness, cataracts, increased IOP.
Cardiovascular system and blood (hematopoiesis, hemostasis): myocardial infarction, pulmonary embolism, thrombocytopenia.
Gastrointestinal tract: nausea, dyspeptic symptoms, hepatotoxicity.
Other: allergic reactions, hypercalcemia, endometrial hyperplasia, thrombophlebitis, thrombosis, fever, increased sweating.
Hypersensitivity, prolonged QT interval (congenital/acquired), unadjusted hypokalemia and hypomagnesemia, thromboembolism (including anamnesis).
2.Which manufacturers of drugs of category Toremifene citrate are represented on the greatanabolicsteroids.com website?
Self-medication can be dangerous for your health. Information about the active substance is provided solely to familiarize themselves, so before use, refer to your doctor.
Do not engage in self-medication! It may be dangerous for your health!