💊 Buy Arimidex Online Without Prescription

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Antineoplastic drug. Aromatase inhibitor

Pharmachologic effect

Highly selective non-steroidal aromatase inhibitor. Aromatase is an enzyme by which, in postmenopausal women, androstenedione in peripheral tissues is converted into estrone and then into estradiol. Reducing circulating estradiol levels has a therapeutic effect in breast cancer patients. In postmenopausal women, the drug in a daily dose of 1 mg causes a decrease in estradiol levels by 80%.

Arimidex does not possess progestogenic, androgenic and estrogenic activity.

Arimidex in a daily dose of up to 10 mg has no effect on the secretion of cortisol and aldosterone (therefore, the use of the drug does not require replacement of corticosteroids).

Pharmacokinetics

Suction

After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours (on an empty stomach). Food decreases the rate of absorption somewhat, but not the degree of absorption. Small changes in the rate of absorption do not lead to a clinically significant effect on the Css of the drug in plasma with a daily intake of 1 tab. Arimidexa.

Distribution

Anastrozole binds to plasma proteins by 40%. Approximately 90-95% of Css is achieved after 7 days of taking the drug. There is no information about the cumulation of the drug and the dependence of the pharmacokinetic parameters of anastrozole on time and dose.

Metabolism

Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronidation. Triazole, the major plasma metabolite, does not inhibit aromatase.

Withdrawal

Anastrozole is excreted slowly, T1 / 2 - 40-50 hours.

Anastrozole and its metabolites are excreted mainly in the urine (less than 10% of the excreted dose - unchanged), within 72 hours after taking the drug.

Pharmacokinetics in special clinical situations

The determined clearance of anastrozole after oral administration in volunteers with stabilized liver cirrhosis or impaired renal function does not differ from the clearance determined in healthy volunteers.

The pharmacokinetics of anastrozole does not depend on age in postmenopausal women.

Indications

adjuvant therapy for early hormone-positive breast cancer in postmenopausal women;
treatment of advanced breast cancer in postmenopausal women;
adjuvant therapy for early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.

Contraindications

severe renal failure (creatinine clearance less than 20 ml / min);
hepatic impairment of moderate and severe degree (safety and efficacy have not been established);
concomitant therapy with tamoxifen;
childhood (safety and effectiveness have not been established);
pregnancy;
lactation (breastfeeding);
hypersensitivity to anastrozole and other components of the drug.

The drug is not prescribed for premenopausal women.

Dosage

For adults, including elderly patients, the drug is prescribed 1 mg orally 1 time / day, for a long time. If signs of disease progression appear, the drug should be discontinued. As an adjuvant therapy, the recommended duration of treatment is 5 years.

Patients with mild to moderate renal impairment do not require dose adjustment.

Patients with mild hepatic impairment do not require dose adjustment.

The tablet should be swallowed whole and washed down with water. It is recommended to take the drug at the same time of the day.

Side effects

Determination of the frequency of adverse reactions: very often (> 10%); often (1-10%); rarely (0.1-1%); very rare (<0.1%).
From the side of the cardiovascular system: very often - hot flashes.
From the musculoskeletal system: often - arthralgia.
Reproductive system disorders: often - vaginal dryness; rarely - vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormone therapy to Arimidex).
From the digestive system: often - nausea, diarrhea; rarely - anorexia, vomiting, increased activity of GGT and alkaline phosphatase.
From the nervous system: often - headache, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease); rarely, drowsiness.
From the side of metabolism: rarely - hypercholesterolemia. Taking the drug can cause a decrease in bone mineral density due to a decrease in the level of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures.
Dermatological reactions: often - thinning hair, skin rash; very rarely - erythema multiforme (Stevens-Johnson syndrome).
Allergic reactions: very rarely - angioedema, urticaria, anaphylactic shock.
Others: often - asthenia.

Overdose

Single clinical cases of drug overdose are described. A single dose of Arimidex, at which life-threatening symptoms develop, has not been established.

Treatment: there is no specific antidote. If necessary, symptomatic therapy is carried out: induction of vomiting (if the patient is conscious), general supportive therapy, monitoring the patient and monitoring the function of vital organs and systems. Dialysis is possible.

Drug interactions

Clinical studies on drug interactions with antipyrine and cimetidine indicate that co-administration of Arimidex with other drugs is unlikely to lead to clinically significant interactions due to cytochrome P450.

There is no clinically significant drug interaction when taking Arimidex at the same time as other commonly prescribed drugs.

At the moment, there is no information on the use of Arimidex in combination with other antineoplastic drugs.

Preparations containing estrogens should not be administered concurrently with Arimidex, because they reduce the pharmacological action of the latter.

Tamoxifen should not be administered concurrently with Arimidex, as it can weaken the pharmacological effect of the latter.

Special instructions

In women with a receptor-negative tumor to estrogen, the effectiveness of Arimidex has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.

In case of doubt about the hormonal status of the patient, menopause should be confirmed by the determination of sex hormones in the blood serum.

There is no data on the safety of the use of Arimidex in patients with severe hepatic impairment or in patients with severe renal failure (CC less than 20 ml / min).

In case of persisting uterine bleeding while taking Arimidex, consultation and supervision of a gynecologist is necessary.

Preparations containing estrogens should not be administered concurrently with Arimidex.

By decreasing the level of circulating estradiol, Arimidex can cause a decrease in bone mineral density.

In patients with osteoporosis or at risk of developing osteoporosis, bone mineral density should be assessed using densiometry (for example, DEXA scanning) at the beginning of treatment and over time. If necessary, treatment or prevention of osteoporosis should be initiated under close medical supervision.

There is no data on the simultaneous use of anastrozole and preparations of GnRH analogs.

It is not known whether anastrozole improves treatment outcomes when used with chemotherapy.

Safety data for long-term treatment with anastrozole have not yet been obtained.

With the use of Arimidex, ischemic diseases were observed more often than with tamoxifen therapy, however, no statistical significance was noted.

Caution

The efficacy and safety of Arimidex and tamoxifen when used simultaneously, regardless of the status of hormonal receptors, are comparable to those when using tamoxifen alone. The exact mechanism of this phenomenon is not yet known.

Use in pediatrics

The safety and efficacy of the drug in children have not been established.

Influence on the ability to drive vehicles and mechanisms

Some of the side effects of Arimidex, such as asthenia and drowsiness, can adversely affect the ability to perform work that requires increased concentration and psychomotor speed. In this regard, it is recommended that when these symptoms appear, be careful when driving or moving machinery.

Pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Childhood use

The drug is contraindicated for use in children (safety and effectiveness have not been established).

With impaired renal function