TAMOXIFEN HEXAL® instructions

P N011849/01 [П N011849/01]

Tamoxifen

Tamoxifen

Film-coated tablets

Active Ingredient: Tamoxifen citrate 15.2 mg, 30.4 mg, 45.6 mg, or 60.8 mg, equivalent to 10 mg, 20 mg, 30 mg, or 40 mg of tamoxifen, respectively.

Excipients: Lactose monohydrate: 71.3 mg, 142.6 mg, 213.9 mg, or 285.2 mg., Sodium starch glycolate: 10.0 mg, 20.0 mg, 30.0 mg, or 40.0 mg., Povidone: 2.5 mg, 5.0 mg, 7.5 mg, or 10.0 mg., Microcrystalline cellulose: 24.8 mg, 49.6 mg, 74.4 mg, or 99.2 mg., Magnesium stearate: 1.2 mg, 2.4 mg, 3.6 mg, or 4.8 mg.

Coating: White opadry coating: 2.5 mg, 5.0 mg, 7.5 mg, or 10.0 mg, consisting of: Lactose: 0.9 mg, 1.8 mg, 2.7 mg, or 3.6 mg, Titanium dioxide: 0.65 mg, 1.3 mg, 1.95 mg, or 2.6 mg., Hypromellose: 0.7 mg, 1.4 mg, 2.1 mg, or 2.8 mg., PEG 4000: 0.25 mg, 0.5 mg, 0.75 mg, or 1.0 mg

10 mg Tablets: Round, white or slightly yellowish, biconvex, film-coated tablets with a smooth surface.

20 mg Tablets: Round, white or slightly yellowish, biconvex, film-coated tablets with a score line on one side and a smooth surface.

30 mg Tablets: Round, white or slightly yellowish, biconvex, film-coated tablets with a smooth surface.

40 mg Tablets: Round, white or slightly yellowish, biconvex, film-coated tablets with a score line on one side and a smooth surface.

Antineoplastic agent – antiestrogen

L02BA01

Tamoxifen is a non-steroidal triphenylethylene derivative with both estrogen antagonist and agonist properties in different tissues. In breast cancer patients, tamoxifen primarily acts as an antiestrogen by blocking estrogen receptors in tumor cells.

Tamoxifen and its metabolites compete with estradiol for binding to cytoplasmic estrogen receptors in tissues such as the breast, uterus, vagina, pituitary gland, and estrogen receptor-positive tumors. Unlike the estrogen-receptor complex, the tamoxifen-receptor complex inhibits DNA synthesis, reducing tumor cell proliferation and inducing cell death.

For estrogen receptor-positive breast cancer, tamoxifen adjuvant therapy significantly reduces recurrence and improves survival, particularly with 5-year treatment compared to shorter durations.

Approximately 10-20% of postmenopausal women experience reduced total cholesterol and LDL levels. Tamoxifen may also preserve bone mineral density in postmenopausal women.

Tamoxifen is well absorbed orally, with maximum serum levels reached 4-7 hours post-administration. Steady-state serum concentrations occur after 3-4 weeks of daily doses (20-40 mg/day). Plasma protein binding is approximately 98%.

Metabolized in the liver, tamoxifen forms several metabolites, including N-desmethyltamoxifen, which retains antiestrogenic activity. The drug and its metabolites accumulate in the liver, lungs, brain, pancreas, skin, and bones. The primary metabolite is further processed by CYP2D6 to endoxifen, a potent metabolite.

Excretion follows a biphasic pattern: an initial half-life of 7-14 hours and a terminal phase of approximately 7 days. Elimination occurs primarily via the feces, with minor renal excretion.

  • Adjuvant therapy for early-stage estrogen receptor-positive breast cancer
  • Treatment of locally advanced or metastatic estrogen receptor-positive breast cancer
  • Breast cancer in men (including post-castration cases)
  • Other solid tumors with estrogen receptor overexpression resistant to standard therapies
  • Hypersensitivity to tamoxifen or any components of the formulation
  • Pregnancy and breastfeeding
  • Pediatric use (under 18 years)

Renal impairment, diabetes, eye disorders (e.g., cataracts), deep vein thrombosis, thromboembolic disease, hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia, concurrent use of anticoagulants, and hereditary lactose intolerance.

Tamoxifen is contraindicated during pregnancy due to the risk of fetal harm, spontaneous abortion, or congenital anomalies. Breastfeeding is not recommended, as tamoxifen inhibits lactation, and its excretion in milk is unknown.

Adults: 20 mg daily (standard dose), with a maximum dose of 40 mg daily. Tablets should be swallowed whole with water. Treatment is typically long-term, lasting up to 5 years as adjuvant therapy.

Very Common (≥1/10): Hot flashes, vaginal bleeding, menstrual irregularities

Common (≥1/100 to <1/10): Headache, dizziness, visual disturbances, nausea, fluid retention. Increased cholesterol, triglycerides. Endometrial changes (hyperplasia, polyps)

Uncommon (≥1/1,000 to <1/100): Stroke, thromboembolic events

Rare (<1/1,000): Neutropenia, severe liver damage

Symptoms may include exaggerated side effects such as QT interval prolongation. Treatment involves symptomatic care, as no specific antidote exists.

Increased thromboembolic risk with cytotoxic drugs

Decreased tamoxifen efficacy with CYP2D6 inhibitors (e.g., fluoxetine)

Enhanced anticoagulant effect of warfarin

Regular gynecological exams are advised. Monitor calcium levels in metastatic bone disease and blood clotting parameters in those on anticoagulants.

Film-coated tablets: 10 mg, 20 mg, 30 mg, 40 mg. Packaged in blisters of 10 tablets, with 3 or 10 blisters per carton.

Store below 25°C. Keep out of reach of children.

5 years. Do not use after the expiration date.

Prescription only.

Hexal AG, Industriestrasse 25, 83607 Holzkirchen, Germany. https://www.hexal.de/

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