Health Anti-Estrogen Steroids pormone Tamoxifen for Increase Muscle Mass Keep Active
What is Tamoxifen?
Tamoxifen is a nonsteroidal antiestrogen drug. Its structure is similar to estrogen, the existing Z-type and O-isomers. Physical and chemical properties are different from each other, physiological activities are different. E type has weak estrogenic activity, Z type has anti-estrogen effect. If estrogen receptor (ER) is present in breast cancer cells, estrogen enters tumor cells and binds to ER, promotes tumor cell mRNA and DNA synthesis, and stimulates tumor cell growth. However, the tamoxifen Z-isomer enters the cell, competes with ER to form a receptor complex that inhibits estrogen action and inhibits breast cancer cell proliferation. Clinically used in breast cancer patients with high levels of estrogen, and its androgen and other anti-cancer drugs (such as doxorubicin, etc.) to improve the efficacy of advanced breast cancer patients after menopause and show good results oral: a 10 Times ~ 20mg, 2 times a day, the common side effects for the rinse, genital itching, occasionally vaginal bleeding, a few may be headache, liquid retention, long time may have retinal disease, vision loss, the other can have bone marrow suppression and gastrointestinal reactions.
Tamoxifen for the treatment of breast cancer can reduce the mortality and recurrence rates of estrogen - dependent breast cancer patients, with good prospects. Another endocrine therapy for aromatase inhibitors can inhibit the effects of aromatase, to prevent adrenal secretion of rhodoxicin in peripheral tissues (fat, skin, muscle) into estrogen, further reducing postmenopausal women's estrogen levels. The current treatment of postmenopausal estrogen and progesterone receptor-positive breast cancer is one of the important means.
Application of Timoxifen
Interested non-steroidal estrogen antagonists in the treatment of certain forms of breast cancer. Tamoxifen is a protein kinase C inhibitor that induces apoptosis in human malignant glioma cell lines
Use tamoxifen is a selective estrogen responsive regulator (SERM), a protein kinase C inhibitor and an anti-angiogenic factor. Tamoxifen is a prodrug that metabolizes 4-hydroxy tamoxifen (4-OHT) and endothelin through cytochrome P450 isoforms CYP2D6 and CYP3A4. In breast cancer, the activity of tamoxifen on ERBB2 is dependent on PAX2. Blocking estrogen - stimulated VEGF production in breast tumor cells. Protein kinase C inhibitors. Induced apoptosis of human glioma cells. Tamoxifen and its metabolite 4-hydroxy tamoxifen is a selective estrogenic response inhibitor (SERM) as an estrogen antagonist in the mammary gland. Blocking estrogen - stimulated VEGF production in breast tumor cells.
Product use
Products to anti-estrogen inducer, dysfunctional uterine bleeding, polycystic ovary, menstrual disorders and drug amenorrhea and other gynecological diseases; it is used as a line of breast cancer line. Nolvadex or tamoxifen citrate, a non-steroidal antiestrogen used for oral administration, usually by athletes as post-circulation therapy to reduce or prevent excessive estrogen formation, which can lead to oily skin , Acne, liquid retention and men's femininity development.
1. Treatment of women with metastatic breast cancer recurrence.
2. For the treatment of breast cancer after the transfer of adjuvant therapy, and relapse prevention.
3. For the treatment of ovarian cancer, endometrial cancer and endometriosis.
The original of Tamoxifen
For the preliminary study of estrogen drugs, scientists found that anti-estrogen drugs can prevent rat endometrial hyperplasia and embryo implantation, and has a contraceptive effect, hoping to be used as a contraceptive in the human British reproductive endocrinologist Walpole The study of tamoxifen was first reported in 196. When studying the antiestrogens - benzoylphenols, they found that their two derivatives had different physiological effects. The vaginal epithelium keratosis index and uterine weight gain index were used as evaluation indexes. The results showed that homeopathic structures (ICI47,699) had estrogenic effects on uterine and vaginal epithelial cells in rats and mice; the trans-structure (ICI46,747) had very weak estrogenic effects on rat vaginal epithelial cells , The uterus with anti-estrogen effect, can terminate early pregnancy and inhibit ovulation, but also on the uterus and vagina with anti-estrogen effect on mouse epithelial cells. Now is the ICI46,747 trans structure of tamoxifen, and scientists expect ICI46,747 to be a new contraceptive for humans. However, in clinical trials, they found that the drug did not show the same effect on rats, but the drug could stimulate endometrial hyperplasia and promote ovulation. Therefore, the clinical tamoxifen first used for ovulation infertility patients ovulation drugs, is still in use. For the ovarian hyperstimulation program assisted reproductive technology treatment field, the ovulation effect is also better. Thus, tamoxifen has estrogen-like and anti-estrogen effects, and has different effects on different species and tissues.
Pharmacokinetics of Tamoxifen
This product is easy to absorb oral, generally taking drugs 3 hours after the peak plasma concentration; due to intestinal circulation, the product concentration in the body more durable; in the liver metabolism, the product mainly excreted in the stool, bile (58% ~ 100 (Only 2% to 21%); after the isotope labeled the animal of the product, it was found that radioactivity was highest in the animal's ovary. For postmenopausal women, the concentration in the endometrium is twice that of plasma.
Contraindications of Tamoxifen
1. Allergy to this product is taboo.
2. taboo eye disease patients.
3. Patients with deep venous thrombosis and pulmonary embolism or patients receiving anticoagulation.
4. Pregnant and lactating mothers taboo.
Precautions of Tamoxifen
1. Carefully use liver dysfunction. If the bone is transferred, patients are required to regularly check serum calcium in early treatment.
2. The safety of the drug classified by the FDA class D.
Drug interactions of Timoxifen
1. Drugs combined with fluorouracil, cyclophosphamide, methotrexate, vincristine and doxorubicin, etc., can improve its effect.
The drug can increase the dopaminergic effect of bromocriptine mesylate.
Data show that drugs can extend the neuromuscular block of atracurium.
4. Drugs can enhance the role of anticoagulants, not with anticoagulants (such as warfarin, two coumarin anticoagulants) in combination.
5. Antacids and cimetidine fumotidine can change the pH value of the stomach, so that the decomposition of enteric-coated tablets, the stomach has a stimulating effect, so when used in combination, these drugs interval 1 ~ 2 hours.
Estrogen can affect the treatment of drugs, should not be used in combination.
7. In vitro test results show that the drug may inhibit the metabolism of tacrolimus.
8. In combination with mitomycin, the risk of hemolytic syndrome and hematuria increases.
9. Drugs combined with triptolide can promote the growth of mouse tumors, so the combination should be cautious.
With allopurinol, the drug may increase liver toxicity.
Drugs combine with other cytotoxic drugs to increase the risk of thromboembolism.
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MGF
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2mg
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PEG MGF
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CJC-1295 with DAC
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CJC-1295 without DAC
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PT-141
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MT-1(Melanotan-1)
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MT-2(Melanotan-2)
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GHRP-2
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Tesamorelin
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DSIP
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Selank
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Epitalon
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ACE 031
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GDF-8
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Follistatin 315
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1mg(-20ºC)
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Follistatin 344
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Adipotide
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79561-22-1
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Angiotensin Acetate
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58-49-1
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Argpressin Acetate
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113-79-1
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Aviptadil Acetate
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40077-57-4
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Bivalirudin Trifluoroacetate
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128270-60-0
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Deslorelin Acetate
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57773-65-6
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Desmopressin Acetate
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16679-58-6
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Eledoisin Acetate
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69-25-0
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Eptifibatide Acetate
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148031-34-9
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Felypressin Acetate
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56-59-7
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GLP-1 (7-37) Acetate
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106612-94-6
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Taspoglutide
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275371-94-3
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Glucagon Hydrochloride
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16941-32-5
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Lixisenatide
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320367-13-3
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Gonadorelin Acetate
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34973-08-5
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Leuprorelin Acetate
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53714-56-0
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Lysipressin Acetate
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50-57-7
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Nafarelin Acetate
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76932-56-4
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Octreotide
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79517-01-4
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Ornipressin Acetate
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3397-23-7
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Secretin Acetate
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108135-74-8
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Somatostatin Acetate
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38916-34-6
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Splenopentin Acetate
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105184-37-0
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Terlipressin Acetate
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14636-12-5
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Teriparatide Acetate
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52232-67-4
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Triptorelin Acetate
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57773-63-4
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Vasopressin Acetate
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9034-50-8
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Bate-Amyloid(1-42)human
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107761-42-2
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Abarelix Acetate
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183552-38-7
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Endothelin-1 Acetate
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117399-94-7
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CRF (human, rat) Acetate
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86784-80-7
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CRF (ovine) Trifluoroacetate
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79804-71-0
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Dynorphin A (1-13) Acetate
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72957-38-1
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Enfuvirtide Acetate (T-20)
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159519-65-0
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Fertirelin Acetate
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38234-21-8
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GRF (human) Acetate
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83930-13-6
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Liraglutide
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204656-20-2
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Dalmarelin Acetate
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61012-19-9
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Nesiritide Acetate (BNP-32)
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114471-18-0
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Pramlintide Acetate
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196078-30-5
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Salmon Calcitonin Acetate
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47931-85-1
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tesamorelin
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106612-94-6
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Tetracosactide Acetate (ACTH 1-24)
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16960-16-0
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Thymosin α1 Acetate
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14636-12-5
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Thymosin β4 Acetate
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77591-33-4
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Atosiban Acetate
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90779-69-4
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Cetrorelix Acetate
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130143-01-0
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Exenatide Acetate
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141732-76-5
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Histrelin Acetate
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76712-82-8
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Taltirelin Acetate
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103300-74-9
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Vapreotide Acetate
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116430-60-5
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Gonaderelin
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33515-09-2
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Cecropin B
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80451-05-4
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Oxytocin Acetate
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50-56-6
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Sincalide
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25126-32-3
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Protirelin
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24305-27-9
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Ganirelix acetate
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123246-29-7
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