Anastrozole
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2019-09-19
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Clinical Pharmacology
Antitumor agent. It is a selective non-steroidal aromatase inhibitor. In postmenopausal estradiol is mainly formed from estrone, which is produced in peripheral tissues by transformation from androstenedione (with the participation of the aromatase enzyme). Reducing circulating estradiol has a therapeutic effect in women with breast cancer. In postmenopausal anastrozole in a daily dose of 1 mg causes a decrease in estradiol levels by 80%. Anastrozole does not possess progestogenic, androgenic and estrogenic activity; in therapeutic doses does not affect the secretion of cortisol and aldosterone.
Pharmacokinetics
After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours (on an empty stomach). Food somewhat reduces the rate, but not the degree of absorption. Plasma protein binding is 40%. No cumulation reported.
Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronization. Triazole, the main metabolite that is detected in plasma and urine, does not inhibit aromatase.
Anastrozole and its metabolites are excreted mainly with urine (less than 10% - unchanged), within 72 hours after a single dose. T1 / 2 from plasma - 40-50 h.
Anastrozole clearance after oral administration in volunteers with stabilized liver cirrhosis or renal dysfunction does not differ from clearance determined in healthy volunteers.
The pharmacokinetics of anastrozole in postmenopausal women does not change.
Indications
Postmenopausal breast cancer.
Composition
pills, film coated white, round, biconvex, with engraving "ANA 1" on one side of the tablet; on a break - white or almost white.
| 1 tab. | |
| anastrozole | 1 mg |
Excipients: lactose monohydrate, povidone, sodium carboxymethyl starch, magnesium stearate.
Film coating: white opadry (macrogol 400, hypromellose, titanium dioxide).
Anastrozole is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Anazales | pills | ||
| Selana | Nativa | Russia | pills |
| Anastrozole | Ozon | Russia | pills |
| Arimidex | AstraZeneca | UK | pills |
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Dosage and Administration
For oral use. - 1 mg 1 time / day.
Adverse reactions
On the part of the endocrine system: "hot flashes", vaginal dryness and thinning hair.
On the part of the digestive system: anorexia, nausea, vomiting, diarrhea. In patients with advanced breast cancer in most cases with metastases to the liver, there was an increase in the level of GGT, more rarely - ALP.
From the side of the central nervous system: asthenia, drowsiness, headache.
On the part of metabolism: a slight increase in total cholesterol.
Allergic reactions: skin rash.
Contraindications
The period of premenopause, severe renal failure (CC less than 20 ml / min), moderate and severe liver failure, pregnancy, lactation, childhood, hypersensitivity to anastrozole.
Drug interactions
Anastrozole reduces the effectiveness of estrogen.
Clinical studies have shown that with simultaneous use of anastrozole with antipyrine and cimetidine, drug interactions due to induction of microsomal liver enzymes are unlikely.
Special instructions
In case of uncertainty of the patient's hormonal status, the condition of the menopause must be confirmed by additional biochemical studies.
The safety of using anastrozole in patients with moderately impaired liver function has not been established.
Anastrozole should not be used simultaneously with estrogen.
Influence on ability to drive motor transport and control mechanisms
During the period of treatment should not perform work that requires a high concentration of attention and quick psychomotor reactions.
- Brand name: Anazales
- Active ingredient: Anastrozole
- Manufacturer: Synthesis AKOMP
Studies and clinical trials of Anastrozole (Click to expand)
- A Phase III trial comparing anastrozole (1 and 10 milligrams), a potent and selective aromatase inhibitor, with megestrol acetate in postmenopausal women with advanced breast carcinoma
- Use of the aromatase inhibitor anastrozole in the treatment of patients with advanced prostate carcinoma
- Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor positive advanced breast carcinoma : Results of two randomized trials designed for combined analysis
- An ultraperformance liquid chromatography–tandem mass spectrometry method for determination of anastrozole in human plasma and its application to a pharmacokinetic study
- Hydrophilic interaction chromatography–electrospray ionization tandem mass spectrometric analysis of anastrozole in human plasma and its application to a pharmacokinetic study
- Rapid determination of anastrozole in plasma by gas chromatography with electron capture detection and its application to an oral pharmacokinetic study in healthy volunteers
- An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane
- Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor–positive advanced breast carcinoma
- Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma in postmenopausal women : A prospective combined analysis of two multicenter trials
- Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early-stage breast cancer : Results of the ATAC (Arimidex, Tamoxifen Alone or in Combination) trial efficacy and safety update analyses
- Benefit and projected cost-effectiveness of anastrozole versus tamoxifen as initial adjuvant therapy for patients with early-stage estrogen receptor–positive breast cancer
- Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma : A prospectively planned combined survival analysis of two multicenter trials
- Comparison of anastrozole versus tamoxifen as preoperative therapy in postmenopausal women with hormone receptor-positive breast cancer : The pre-operative “Arimidex” compared to Tamoxifen (PROACT) trial
- Impact of chemotherapy regimens prior to endocrine therapy : Results from the ATAC (Anastrozole and Tamoxifen, Alone or in Combination) trial
- Erratum: Buzdar AU, Guastalla J-P, Nabholtz J-M, et al. Impact of chemotherapy regimens prior to endocrine therapy: results from the ATAC (Anastrozole and Tamoxifen, Alone or in Combination) trial. Cancer. 2006; 107(3):472–80.
- Exemestane versus anastrozole as front-line endocrine therapy in postmenopausal patients with hormone receptor-positive, advanced breast cancer : Final results from the Spanish Breast Cancer Group 2001-03 phase 2 randomized trial
- Effects of morphine on testosterone levels in rat C6 glioma cells: Modulation by anastrozole
- Giving patients a choice improves quality of life: a multi-centre, investigator-blind, randomised, crossover study comparing letrozole with anastrozole
- Transdermal patches for site-specific delivery of anastrozole: In vitro and local tissue disposition evaluation
- Lumpectomy Plus Tamoxifen or Anastrozole With or Without Whole Breast Irradiation in Women With Favorable Early Breast Cancer
- Efficacy of Anastrozole on Local Recurrence in Patients With Favorable Early Breast Cancer
- Anastrozole quantification in human plasma by high-performance liquid chromatography coupled to photospray tandem mass spectrometry applied to pharmacokinetic studies
- LC and LC–MS/MS study of forced decomposition behavior of anastrozole and establishment of validated stability-indicating analytical method for impurities estimation in low dose anastrozole tablets
- Validated assay for the quantification of anastrozole in human plasma by capillary gas chromatography-63Ni electron capture detection
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