Aromasin tab n / 25mg about 30 pc

Description

Composition
Active substance:
Exemestane 25 mg.
Excipients:
Mannitol 26.0 mg hypromellose 1.50 mg, polysorbate – 80 0.125 mg, 2.125 mg of crospovidone, colloidal silicon dioxide 0.125 mg Microcrystalline cellulose 4.625 mg, 2.375 mg sodium carboxymethyl starch, magnesium stearate 0.625 mg.
Composition sugar shell: 1.81 mg of Hypromellose, simetikonovaya emulsion 0.009 mg macrogol – 6,000 0,181 mg, 1,157 mg magnesium carbonate, titanium dioxide 3.453 mg Methyl parahydroxybenzoate 0.003 mg, 0.697 mg polyvinyl alcohol, sucrose 30.19 mg; (Components for imparting gloss: tsetilefirny Wax 0.0175 mg, 0.01 mg talc, carnauba wax, 0.0225 mg).
Composition of Ink: shellac, ethanol, isobutanol, dye iron oxide (E 172), titanium dioxide (E 171).
Description:
Round, biconvex tablets with a white or grayish white color shade, sugar-coated tablets, labeled “7663” on one side formed with black paint.
Product form:
Film-coated tablets 25 mg.
15 tablets in blister PVDC / PVC – PVDC aluminum foil; 1, 2 or 6 blisters together with instructions for use placed in a cardboard box.
Contraindications
Hypersensitivity to eksemestanu or to any other component of the preparation
Premenopazualny endocrine status
Pregnancy and lactation
Carefully
Dysfunction of the liver or kidney.
Indications
Common breast cancer in women with natural or induced postmenopausal women, including those with the progression of the disease on the background of anti-estrogen therapy, as well as the progression of the disease after repeated application of different types of hormonal therapy.
Adjuvant treatment of early breast cancer in women posmenopauze with estrogen-receptor-positive or unknown receptor status, after completion of 2-3 years of initial adjuvant tamoxifen therapy in order to reduce the risk of recurrence (distant or regional), as well as contralateral breast cancer.
Interaction with other drugs
Preparations containing estrogens, completely negate the pharmacological effect of exemestane.
The drug is metabolized by cytochrome P450 (CYP) 3A4 and aldoketoreduktaz and does not inhibit any of the major CYP-isozymes. Specific inhibition of isozyme CYP3A4 ketoconazole had no significant effect on the pharmacokinetics of exemestane. Despite the established pharmacokinetic interaction eksemestana with rifampicin, a potent inducer of CYP3A4 isoenzyme, Aromazina® pharmacological activity (inhibition of estrogen) remains unchanged, so the dose adjustment is required.
Overdose
A single dose of the drug, which might cause a life-threatening symptoms has not been established. Use of exemestane in a single dose up to 800 mg in healthy women and at a daily dose of 600 mg in postmenopausal women breast well tolerated with advanced cancer. No specific antidote.
Treatment – symptomatic under regular monitoring of vital signs and careful observation.
pharmachologic effect
Pharmacological group:
The antitumor agent, an inhibitor of estrogen synthesis.
Pharmacodynamics:
Exemestane – irreversible steroidal aromatase inhibitor is similar in structure to the natural substance androstenedione.
In postmenopausal women, estrogens are produced primarily by conversion of androgens to estrogens by the enzyme aromatase in peripheral tissues. Blocking the formation of estrogens by aromatase inhibition is an effective and selective method of breast cancer in postmenopausal women, treatment of hormone-dependent cancers. The mechanism of action of the drug Aromazin® due to the fact that it binds irreversibly to the active fragment of an enzyme causing its inactivation. In postmenopausal women Aromazin® significantly reduces the concentration of serum estrogens from the dose is 5 mg, the maximum reduction (> 90%) is achieved at doses of 10-25 mg. In postmenopausal women with breast cancer who received 25 mg of the drug daily, the overall level of the enzyme aromatase in the body was reduced by 98%.
Exemestane has no progestogenic and estrogenic activity. Revealed only slight androgenic activity, mainly with high doses. Aromazin® no effect on the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of drug action. In this regard, there is no need for replacement therapy with glucocorticoids and mineralocorticoids.
In applying the drug even at low doses, there is a slight increase in the levels of luteinizing hormone (LH) and follicle stimulating hormone (FSH) in serum, that is characteristic of drugs of this pharmacologic group and probably develops as a feedback on the pituitary level: reducing the concentration of estrogen It stimulates the secretion of gonadotropins in the pituitary gland and also in postmenopausal women.
Pharmacokinetics:
After oral administration, exemestane is absorbed rapidly, mainly from the gastrointestinal tract. The absolute bioavailability of the drug has not been established. It is believed that it is limited to extensive first pass effect through the liver. In single dose 25 mg dose maximum plasma concentration equal to 17 ng / ml, is reached after 2 h. Simultaneous food intake increases the bioavailability by 40%.
Pharmacokinetic parameters are linear. Terminal half-life is approximately 24 hours. Communication with plasma proteins – about 90%. Exemestane and its metabolites do not bind to red blood cells. If readmission unpredictable cumulation exemestane was observed.
Exemestane biotransformation process is carried out by oxidation of the methylene group in the 6 position under the action of the isoenzyme CYP3A4 and / or recovery 17-keto group under the action aldoketoreduktazy followed by conjugation. The metabolic products eksemestana either inactive or less active in the inhibition of aromatase than the parent compound.
Approximately equal amounts of exemestane (about 40%) excreted in the urine and feces within a week. From 0.1 to 1% is excreted in the urine unchanged.
Pronounced relationship between systemic exposure to the drug and age is not established.
In patients with severe renal insufficiency (creatinine clearance (CC)
Patients with moderate to severe hepatic insufficiency systemic exposure eksemestana 2 – 3 times higher, but the dose adjustment is required.
Pregnancy and breast-feeding
The use exemestane during pregnancy is prohibited because of the potential risk to the fetus. The drug also should not be given during breastfeeding.
Conditions of supply of pharmacies
On prescription.
side effects
In general, good tolerability Aromazina®; undesirable effects when using the drug at a dose of 25 mg / day, mainly small or moderately expressed.
Listed below are undesirable reactions distributed by body system and frequency: very often (> 10%), frequent (> 1%,
special instructions
Aromazin® should not be administered to women with premenopausal endocrine status, therefore, in cases where it is clinically justified, postmenopausal status should be confirmed determination of the level of LH, FSH and estradiol.
Aromazin® should not be administered simultaneously with preparations containing estrogens.
Due to the action of a powerful estrogenponizhayuschim exemestane may decrease in bone mineral density. Before the start of adjuvant therapy is recommended to perform eksemestanom densitometry to assess bone mineral density in postmenopausal women with osteoporosis or at risk of osteoporosis. During treatment, you must eksemestanom special surveillance of women with osteoporosis with matching destination therapy.
Patients should be warned of the possibility of occurrence during treatment Aromazinom® somnolence, asthenia and dizziness. If you experience these symptoms, patients are advised to refrain from driving and other activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
Storage conditions
At a temperature of not higher than 30 ° C.
Keep out of the reach of children.
Dosing and Administration
Adults and elderly patients
The recommended dose is 25 mg 1 time per day, preferably after meal.
Patients patients with early breast cancer drug treatment is recommended to continue so long as the total duration of successive adjuvant hormonal therapy did not reach 5 years. Treatment of patients with advanced breast cancer – a long period. If signs of tumor progression of the disease or the appearance of contralateral breast cancer Aromazinom® treatment should cease.
Hepatic or renal failure
correction dose is not required.
Children
Not recommended for use in children.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist