瑞宁得（Arimidex）

[Functions and Indications]
Arimidex (Arimidex) is suitable for the treatment of advanced breast cancer in postmenopausal women.

[Model and specifications]
Tablets: 1mg 28 tablets.

【Usage and Dosage】
Take 1 mg orally daily.

【Clinical research】

Single-dose test: A single dose of Anatozole (0.1-60 mg) is rapidly absorbed. The tmax is 2 hours when taken on an empty stomach. The plasma concentration is proportional to the dose. Elimination is slow, plasma t1/2 is about 40 to 50 hours. Anatozole pharmacokinetics are linear between 1 and 20 mg. Cl/F is 18.8ml.min-1. Anatozole pharmacokinetic parameters are less variable.

Multi-dose test: After multiple doses of 0.5 mg and 1 mg, the accumulated concentration of anatozole in plasma is about 3 to 4 times. After 7 days, the steady-state plasma concentration reaches 90% to 95%. Pharmacokinetic parameters showed no obvious time-dose dependence. The Cl/F of this product for patients with advanced breast cancer is 12 to 15ml.min-1, and for healthy postmenopausal women is 11 to 30ml.min-1.

Bioavailability, metabolism, and excretion: Food can directly reduce its absorption rate, but the AUC remains unchanged. Once-daily administration of anatozole slightly alters the absorption rate without causing significant changes in steady-state plasma concentrations. The relative bioavailability of oral tablets is 100% compared to anatozole injection. Anatozole absorption rate is >70%, and its metabolism is extensive. At 24 hours after administration, the main radioactive component in anatozole plasma was anatozole. After 72 hours, the radioactive substance concentration increased to be equal to the anatozole concentration. Within 72 hours, less than 10% of the prototype drug was excreted in urine. Metabolic processes include N-dealkylation, hydroxylation and glucuronidation. Its metabolites are mainly excreted through urine and very little through feces. The main metabolite has no aromatase inhibitory effect.

Anatozole dose adjustment is not recommended in patients with mild hepatic or mild or moderate renal impairment. To date, no interactions between anatozole and other drugs have been identified. It has no inhibitory or induction effects on hepatic enzyme systems involved in the metabolism of antipyrine. Age has no significant effect on the pharmacokinetics of this product.

【Precautions】
This product is not suitable for pregnant women, lactating women, pre-menopausal women and children. Patients with severe liver and kidney damage should use with caution. Because weakness and drowsiness can occur with this product, caution should be exercised in patients who drive or operate machinery.

[Adverse reactions and contraindications]
30% of patients developed gastrointestinal disturbance symptoms such as nausea, vomiting and diarrhea after taking anatozole. 10% to 15% of patients experience weakness, headache, flushing, and back bone pain. In addition, dyspnea, peripheral tissue edema, vaginal bleeding, sweating, high blood pressure, and weight gain may also occur, but the incidence is less than MA. Even when taken in large doses, this product does not produce imperceptible inhibitory effects on mineralocorticoids or glucocorticoids. Changes in liver function (increased γ-GT or decreased alkaline phosphatase) have been reported in patients with advanced breast cancer with liver and/or gastric metastasis. A slight increase in total cholesterol levels was observed in clinical trials.

【Storage】
Store at room temperature away from light.

【Manufacturer】
Alisca Pharmaceuticals.