Arimidex

Lab Test Result

Composition

In 1 tablet of Arimidex, there is 1 mg of Anastrozole as active substance.

Lactose monohydrate, sodium carboxymethyl starch, povidone, magnesium stearate, water as auxiliary components.

Package

Tablets in sachet.

Pharmacological Effect

Antineoplastic.

Pharmacodynamics and Pharmacokinetics

Pharmacodynamics
Highly selective aromatase inhibitor - an enzyme, with which, in post-menopause, androstenedione in tissues is converted to estradiol. Reducing its level has a therapeutic effect in breast cancer. It was found that a dose of 1 mg reduces its level by 80%.

Does not possess an androgenic, progestogen and estrogenic effect. Even in doses up to 10 mg does not affect the secretion of cortisol and aldosterone, therefore, substitution treatment with corticosteroids is not carried out.

It causes changes in bone tissue, which are prevented by the appointment of bisphosphonates, especially patients with an average and high risk of osteoporosis and fractures.

This drug does not cause changes in lipid levels in the blood.

Pharmacokinetics
Absorption occurs quickly and maximum concentration is determined 2 hours after taking the pill. Eating does not reduce the degree of absorption, so it does not affect the concentration of the drug in plasma. After a week of administration, 90-95% of the equilibrium concentration is reached. 40% bounds to blood proteins. Output is slow, T1/2 is 40-50 hours. Within 72 hours, about 10% of the dose is excreted in the urine. The clearance of Anastrozole does not change with liver cirrhosis and renal dysfunction. The main metabolite, triazole, does not inhibit aromatase.

Indications for Use

• Supportive treatment of early breast cancer in postmenopausal women;
• Supportive treatment of early breast cancer after treatment with Tamoxifen;
• Common postmenopausal breast cancer.

Contraindications

• Hypersensitivity;
• Premenopausal cancer;
• Pregnancy and the period of breastfeeding;
• Marked hepatic and renal insufficiency;
• Use of Tamoxifen or estrogen-containing drugs;
• Childhood age.

It is used with caution in osteoporosis, ischemic heart disease, hypercholesterolemia, impaired liver function, glucose-galactose malabsorption, lactase deficiency.

Side Effects

Common side effects:

• tides;
• arthralgia and joint stiffness;
• pain in bones;
• headache;
• drowsiness;
• light or moderately severe asthenia;
• nausea, vomiting;
• diarrhea;
• anorexia;
• dryness of the vaginal mucosa;
• uterine bleeding (after drug withdrawal);
• skin rash;
• thinning hair;
• allergic reactions;
• carpal tunnel syndrome (if there are risk factors for this disease);
• increased activity of liver enzymes;
• decreased bone mineral density and the risk of osteoporosis.

Less common side reactions:

• trigger finger;
• hives;
• erythema, vasculitis;
• Stevens-Johnson syndrome;
• angioedema;
• hepatitis.

Arimidex, Instructions for Use (Method and Dosage)

Tablets are taken internally at one and the same time. Dose - 1 mg once a day, treatment is long. With adjuvant therapy - 5 years. With mild and moderately severe renal dysfunction in patients, dose adjustment is not performed. Also, it is not required for mild effects on liver function.

Instructions for Arimidex use contains a warning that in the presence of uterine bleeding when taking this drug, is necessary to consult a gynecologist. When the disease progresses, the drug is stopped.

Asthenia and drowsiness, as adverse reactions, can adversely affect the performance of works that require concentration of attention and reaction speed, as well as the ability to drive vehicles.

Overdose

There is no single dose, which can lead to life-threatening conditions. Since there is no specific antidote, symptomatic treatment and control of the function of vital organs is carried out.

Interaction

The use of Phenazone and Cimetidine does not lead to clinically significant drug interactions. Also there is no information on the interaction with other antitumor drugs.

It is known that estrogen-containing drugs reduce the effect of the active substance.

Tamoxifen also weakens the pharmacological action of Anastrozole.

Storage Conditions

Storage temperature up to 30° C.

Shelf Life

5 years.

Arimidex Analogues

Analogues related to one group: Femara, Letroxyl, Letrozole, Aromasin, Aromadex, Aromaxyl, Exedrol.