Tamoxifen
Salyutas Pharma GmbH
1570 Items
2019-09-19
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Clinical Pharmacology
Tamoxifen is a non-steroidal anti-estrogen agent, which also has weak estrogenic properties. Its action is based on the ability to block estrogen receptors. Tamoxifen, as well as some of its metabolites, compete with estradiol for binding sites to the cytoplasmic estrogen receptors in the tissues of the breast, uterus, vagina, the anterior pituitary gland and tumors with a high content of estrogen receptors. In contrast to the estrogen receptor complex, the tamoxifen receptor complex does not stimulate DNA synthesis in the nucleus, but inhibits cell division, which leads to regression of tumor cells and their death.
Pharmacokinetics
Suction and distribution
After oral administration, tamoxifen is well absorbed. Cmax in serum is achieved within 4 to 7 hours after taking a single dose.
The equilibrium concentration of tamoxifen in serum is usually achieved after 3-4 weeks of intake. Communication with plasma proteins - 99%.
Metabolism and excretion
Metabolized in the liver to form several metabolites.
Removal of tamoxifen from the body is biphasic in nature with initial T1/2 from 7 to 14 h and with the subsequent slow terminal T1/2 within 7 days. It is excreted mainly in the form of conjugates, mainly with feces and only small amounts are excreted in the urine.
Indications
The drug can be used to treat:
- ovarian cancer:
- endometrial cancer;
- kidney cancer;
- melanomas;
- soft tissue sarcoma with estrogen receptors present in the tumor;
- prostate cancer with resistance to other drugs.
Composition
1 tablet contains:
Active substances: tamoxifen citrate 30.4 mg, which corresponds to the content of tamoxifen 20 mg.
Excipients: lactose monohydrate - 142.6 mg, sodium starch glycolate - 20 mg, povidone - 5 mg, microcrystalline cellulose - 49.6 mg, magnesium stearate - 2.4 mg.
Shell composition: White opadry dye - 5 mg (lactose - 1.8 mg, titanium dioxide - 1.3 mg, hypromellose - 1.4 mg, polyethylene glycol 4000 - 0.5 mg).
Tamoxifen is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Tamoxifen | Salyutas Pharma GmbH | Germany | pills |
| Tamoxifen | Ozon | Russia | pills |
| Tamoxifen | Orion Corporation/Pharmacor | Finland | pills |
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Dosage and Administration
The dosage regimen is set individually, depending on the evidence, the patient's condition and the antitumor therapy regimen used.
Adverse reactions
On the part of the digestive system: nausea, vomiting, increased activity of hepatic transaminases; in some cases - fatty liver, cholestasis, hepatitis.
From the side of the central nervous system: rarely - depression, dizziness, headache, retrobulbar neuritis.
On the part of the organ of vision: rarely - retinopathy, keratopathy, cataracts.
From the hematopoietic system: rarely - thrombocytopenia, leukopenia.
On the part of the endocrine system: in women - endometrial hyperplasia, vaginal bleeding, hot flashes, weight gain; in men, impotence, decreased libido.
Since the cardiovascular system: edema, thromboembolism, phlebitis.
Dermatological reactions: alopecia, rash, pruritus.
Other: pain in the bones and lesions, fever.
Contraindications
- Thrombophlebitis;
- pregnancy;
- hypersensitivity to tamoxifen.
Drug interactions
When applied simultaneously with anticoagulants coumarin derivatives increases the risk of increased anticoagulant action; with cytostatics, the risk of thrombosis may increase.
With simultaneous use with allopurinol may hepatotoxic effect; with aminoglutethimide, a decrease in plasma tamoxifen concentration, apparently due to an increase in its metabolism.
In patients receiving tamoxifen, prolonged neuromuscular blockade caused by atracuria is possible.
With the 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: prolongation of prothrombin time, hematuria, hematoma are possible.
When applied simultaneously with mitomycin, the risk of hemolytic-uremic syndrome increases.
Perhaps a decrease in the concentration of tamoxifen in the blood plasma, which, apparently, is due to the induction of CYP3A4 isoenzyme under the action of rifampicin.
Estrogens may reduce the therapeutic effect of tamoxifen.
Pregnancy and Lactation
Tamoxifen is contraindicated for use during pregnancy. If necessary, use during lactation should stop breastfeeding.
In experimental studies, the teratogenic effect of tamoxifen has been established.
Special instructions
With caution used for leukopenia, thrombocytopenia, hypercalcemia, in patients with cataracts, hyperlipidemia.
In the course of treatment, the pattern of peripheral blood should be regularly monitored (especially the platelet count); the level of calcium and glucose in the blood; long-term use shows observation of the oculist (every 3 months).
It should not be combined with drugs containing hormones, especially estrogen.
With simultaneous use with drugs that affect the blood coagulation system, dose adjustment of tamoxifen is necessary.
In experimental studies, the carcinogenic effect of tamoxifen has been established.
Overdosage
Acute overdose of tamoxifen was not observed in humans.
Symptoms: It should be expected that an overdose may cause an increase in the above described adverse reactions.
Treatment: there are no specific antidotes, treatment should be symptomatic.
- Brand name: Tamoxifen
- Active ingredient: Tamoxifen
- Dosage form: pills, coated.
- Manufacturer: Salyutas Pharma GmbH
- Country of Origin: Germany
Studies and clinical trials of Tamoxifen (Click to expand)
- Another view of the tamoxifen trial
- Neonatal treatment with tamoxifen causes immediate alterations of the sexually dimorphic nucleus of the preoptic area and medial preoptic area in male rats
- Effects of tamoxifen, an antiestrogen, on rat prostate carcinogenesis by 3,2′-dimethyl-4-aminobiphenyl and testosterone do not support an estrogen role in testosterone promotion
- Prostate cancer cell growth inhibition by tamoxifen is associated with inhibition of protein kinase C and induction of p21waf1/cip1
- Induction of apoptosis by mifepristone and tamoxifen in human LNCaP prostate cancer cells in culture
- Prognostic factors in elderly women with metastatic breast cancer treated with tamoxifen: An analysis of patients entered on four prospective clinical trials
- Chronic oral etoposide and tamoxifen in the treatment of far-advanced hepatocellular carcinoma
- Endometrial carcinoma associated with breast carcinoma: Low incidence with tamoxifen use
- Phase II trial of tamoxifen, etoposide, mitoxantrone, and cisplatin in patients with metastatic breast carcinoma
- A Phase I and pharmacokinetic study of high dose tamoxifen and weekly cisplatin in patients with metastatic melanoma
- Tamoxifen-associated venous thrombosis and activated protein C resistance due to factor V leiden
- The effects of postradiation treatment with tamoxifen on local control and cosmetic outcome in the conservatively treated breast
- The incidence of subsequent endometrial carcinoma with tamoxifen use in patients with primary breast carcinoma
- Tamoxifen and breast conservation : Do we still need radiotherapy?
- A randomized trial of tamoxifen alone or combined with octreotide in the treatment of women with metastatic breast carcinoma
- Effects of tamoxifen on telomerase activity in breast carcinoma cell lines
- A phase III randomized trial of dacarbazine and carboplatin with and without tamoxifen in the treatment of patients with metastatic melanoma
- High dose tamoxifen plus cisplatin and etoposide in the treatment of patients with advanced, inoperable nonsmall cell lung carcinoma
- Paclitaxel and tamoxifen : An active regimen for patients with metastatic melanoma
- A clinical trial of intravenous vinorelbine tartrate plus tamoxifen in the treatment of patients with advanced malignant melanoma
- Combined modality treatment of locally advanced breast carcinoma in elderly patients or patients with severe comorbid conditions using tamoxifen as the primary therapy
- Estrogen receptor (ER) and its messenger ribonucleic acid expression in the genital tract of female mice exposed neonatally to tamoxifen and diethylstilbestrol
- Effect of neonatal exposure to diethylstilbestrol and tamoxifen on pelvis and femur in male mice
- Modulation of lymphokine-activated killer cell-mediated cytotoxicity by estradiol and tamoxifen
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