Arimidex. 1 mg. 28 tablets

Arimidex. 1 mg. 28 tablets
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Arimidex is used for the treatment of advanced breast cancer in postmenopausal women. Effectiveness has not been demonstrated in estrogen-negative patients if they had a previous positive clinical response to tamoxifen.

Arimidex. 1 mg. 28 tablets

 
 
COMPOSITION

Each tablet contains 1 mg anastrozole .

ANNEX

  Treatment of advanced breast cancer in postmenopausal women . Efficiency was not usanovena in estrogen - negative patients if they had a previous positive clinical response to tamoxifen
 

  DOSAGE

  Adults (including the elderly ): One tablet of 1 mg taken orally once daily.

  Children: Not recommended for use in children.

  Renal impairment: No dose adjustment recommended in mild or moderate renal impairment.

  Hepatic impairment: No dose adjustment recommended in mild hepatic impairment.

 

CONTRAINDICATIONS

  Arimidex is contraindicated in :

 * Premenopausal women

 * Pregnant and lactating

 * Patients with severe renal impairment ( creatinine clearance below 20 ml / min )

 * Patients with moderate and severe hepatic impairment

  * Patients with a history of hypersensitivity to anastrazole or any of the other excipients on the packaging

  Estrogen - containing preparations should be administered simultaneously with Arimidex as they antagonize the pharmacological action .

 

special warnings

  Arimidex is not recommended for use in children as safety and efficacy have not been established in this group of patients.

  Menopause should be biochemically demonstrated in any patient suspected about the hormonal status.

  No evidence of safe use of Arimidex in patients with moderate and severe hepatic impairment or severe disorder in renal function ( creatinine clearance below 20 ml / min ) .

 

Interaction with other medicinal

  Clinical interaction study with cimetidine and antipyrine indicate that it is unlikely that co-administration of Arimidex with other drugs will result in clinically significant drug interactions mediated by cytochrome P450 .

  When reviewing the database of clinical trials related safety showed no evidence of clinically significant interaction in patients treated with Arimidex , which also received other commonly prescribed drugs.

  Until now there are no clinical data on the use of Arimidex in combination with other antitumor agents.

  Estrogen - containing preparations should be administered simultaneously with Arimidex as they antagonize the pharmacological action .

 

Pregnancy and lactation

  Arimidex is contraindicated for pregnant and lactating women.

 

DRIVE AND USE MACHINES

  Arimidex is unlikely to impair the ability to drive and use machines. When using Arimidex however reports of somnolence and asthenia and while these symptoms persist, care should be taken when driving or operating machinery.

 

POSSIBLE SIDE EFFECTS

  Arimidex is generally well tolerated . Adverse events were mild to moderate, with only a few cases of discontinuation for this reason.

  Pharmacological effects of Arimidex can cause some expected effects. These include hot flushes, vaginal dryness and thinning hair . The Arimidex may be associated with gastrointestinal disorders (anorexia , nausea , vomiting and diarrhea) , asthenia , somnolence , headache, or rash.

  In rare cases vaginal bleeding, the most frequently in patients in the first week of therapy after switching from preceding hormonal therapy to treatment with Arimidex . If bleeding continues it is necessary to conduct further research to clarify .

  Not identified from sledsvena causal link between the use of anastrazole and thromboembolic events . In clinical trials , the incidence of thromboembolic complications in the administration of 1 mg of anastrazole and megestrol acetate did not differ statistically significantly , although at this frequency of 10 mg is lower .

  Reported liver changes (increases in gamma -GT or less of the alkaline phosphatase ) in patients with advanced breast cancer , many of which had metastasized to the liver and / or bone. Causation of these changes has not been established . In clinical trials with Arimidex observed a slight increase in total cholesterol .

 

OVERDOSE

  There is no clinical experience of accidental overdose. In animal studies, anastrozole demonstrated low acute toxicity. Clinical trials were conducted with different doses of Arimidex 60 mg single dose given to healthy volunteers - men and up to 10 mg daily given to postmenopausal women with advanced breast cancer ; these dosages were well tolerated . There was no single dose of Arimidex that cause life-threatening symptoms.

  There is no specific antidote to overdosage and treatment must be symptomatic. In the treatment of overdose should be considered the possibility of adopting multiple drugs. If the patient is conscious, can cause vomiting . Dialysis may be helpful because Arimidex is not highly bound to plasma proteins. Below are general supportive care, including frequent monitoring of vital signs and close observation of the patient .

 

Pharmacological Properties

Pharmacodynamic properties

  Arimidex is a potent and highly selective non-steroidal aromatase inhibitor . In postmenopausal women, estradiol is produced primarily by the conversion of androstenedione to estrone by the enzyme complex aromatase in peripheral tissues. Estrone is subsequently converted to estradiol . It has been shown that the reduction in circulating levels of estradiol has beneficial effects in women with breast carcinoma . In postmenopausal women, a daily dose of 1 mg Arimidex resulted in suppression of estradiol over 80 %, which is evidenced by a high sensitive assay .

  Arimidex does not have gestagenic , androgenic or estrogenic activity.

  To 10 mg daily dose of Arimidex is not povliiyala secretion of cortisol or aldosterone , measured before and after the usual stimulation of ACTH. It is therefore not necessary to add a corticosteroid .

  pharmacokinetics

  Absorption of anastrozole is rapid and maximum plasma concentrations typically occur within 2 hours after (fasting ) . Anastrozole is eliminated slowly with a plasma half - life of elimination of 40 to 50 hours. Food slightly reduces the rate but not the extent of absorption . Not expected slight decrease in absorption lead to clinically significant effect on the equilibrium concentrations when taking Arimidex tablets once daily. Approximately 90 to 95% of plasma concentrations of anastrozole equilibrium is reached after 7 days. No evidence of dependency of the pharmacokinetics of anastrozole time or dose .

  The pharmacokinetics of anastrozole is not dependent on the age of the women in the menopause .

  Anastazol pharmacokinetics in children have not been studied.

  Anastrozole is bound to plasma proteins, only 40 %.

  Anastrozole is extensively metabolised in postmenopausal women , and less than 10 % excreted unchanged in urine within 72 hours after admission . Metabolism of anastrozole is done by N- dealkylation , hydroxylation and glucuronidation . The metabolites are excreted primarily in the urine. Triazole, the major metabolite in plasma and urine did not inhibit aromatase .

  The apparent oral clearance of anastrozole in volunteers with stable hepatic cirrhosis or renal impairment was in the range observed in healthy volunteers.

 

   Preclinical safety data of relevance to the prescriber

  acute toxicity

  In acute toxicity studies in rodents , the median lethal dose of anastrozole was greater than in the oral administration 100mg/kg/24h and greater than 50mg/kg/24h by the intraperitoneal route . In an acute toxicity study in dogs , the median lethal dose for dogs was higher than 45mg/kg/24h .

  chronic toxicity

  Studies of repeated dose toxicity were conducted in rats and dogs. When toxic tests have been established threshold ineffective dose , but the effects seen at lower doses ( 1 mg / kg daily ) and mid doses (dogs - 3 mg / kg per day, rats - 5 mg / kg per day ) were associated or pharmacological properties of anastrozole or the induction of enzyme activity and were not accompanied by toxic or degenerative changes .

  mutagenicity

  Genetic toxicology studies of anastrozole showed that he was not mutagenic or clastogenic activity.

  reproductive toxicity

  Oral administration of anastrozole to pregnant rats and rabbits did not cause teratogenic effects at doses up to 1.0 and 0.2 mg / kg per day , respectively . Effects that have been observed ( placental enlargement in rats and pregnancy failure in rabbits ) were related to the pharmacological properties of the compound .

  Survival of the offspring of rats treated with anastrozole at doses at or above ~ 0.02mg kg / day ( 17 days of gestation to 22 days after birth ) was compromised. These effects were related to the pharmacological effects of the substance on delivery. There were no adverse effects on behavior or reproduction of the first generation , which can be associated with the treatment of the mother by anastrozole .

  Carcinogenesis

  The results of the two-year oncogenicity study in rats showed an increase in the incidence of hepatic neoplasms and polyps of the body of the uterus in females and thyroid adenoma in males at the high dose ( 25mg/kg/den ) . These changes occurred in a dose which is 100 times higher than that which is accepted as a therapeutic in humans , and it is believed that the changes are not clinically relevant for patients receiving anastrozole .

  The results of the two-year oncogenicity study in mice showed induction of benign ovarian tumors and abnormal incidence of lymphoreticular neoplasms (fewer histiocytic sarcomas in females and more deaths as a result of lymphomas ) . These changes are considered as specific effects in mice when treated with aromatase inhibitors and are not of clinical significance in the treatment of patients with anastrozole .

 

PHARMACEUTICAL PARTICULARS

 

       List of excipients

  Lactose Ph. Eur.

  Polyvidone Ph.Eur.

  Sodium starch glycolate B.P.

  Magnesium Stearate Ph. Eur.

  Methylhydroxypropyl cellulose Ph. Eur.

  Macrogol 300 BP

  Titanium dioxide Ph. Eur. (E171) .

 

    Incompatibilities

  Not known

 

SHELF LIFE

  3 years when stored at temperatures below 30 ° C.

 

 STORAGE

  No special precautions.
 
 
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