Medroxyprogesterone-LENS - instructions for use, dose, side effects, contraindications

Excipients: macrogol 4000 (polyethylene oxide 4000, polyethylene glycol 4000), polysorbate 80 (Tween 80), sodium chloride, methyl parahydroxybenzoate (nipagin), propyl parahydroxybenzoate (nipazole), water for injection.

Description:White or white with a yellowish hue of color suspension. When standing, a white precipitate forms and a colorless or slightly yellowish supernatant that turns into a suspension after shaking.

Pharmacotherapeutic group:Progestogen

ATX: & nbsp

L.02.A.B.02 Medroxyprogesterone

L.02.A.B Progestogens

Pharmacodynamics:

Medroxyprogesterone acetate (MPA) does not possess estrogenic activity, its androgenic activity is minimal.In small doses, it inhibits the secretion of gonadotropic hormones of the pituitary gland (especially luteinizing hormone), so that women of childbearing age are prevented from maturing follicles and prolonged anovulation is observed. Reduces vasomotor symptoms in menopause, inhibits secretory changes in the endometrium, increases the viscosity of cervical mucus.

When parenteral administration in high doses has antitumor effect in hormone-dependent malignant neoplasms. The antitumor effect is apparently due to influence on the hypothalamic-pituitary-gonadal system, the receptors of progestins and estrogens, and the metabolism of steroids at the cellular level. In high doses (500 mg / day or more), glucocorticosteroid activity may manifest.

Pharmacokinetics:After intramuscular administration, absorption is slow, which ensures the creation of low, but constant concentrations of medroxyprogesterone in the blood plasma. The connection with plasma proteins is 90-95%. Penetrates through the blood-brain barrier, excreted in breast milk. Metabolised in the liver. Half-life is 6 weeks.It is excreted with bile, as well as kidneys in the form of metabolites and unchanged.

Indications:Additional and palliative treatment of recurrent and metastatic endometrial cancer, kidney cancer; palliative treatment in hormone-dependent forms of recurrent breast cancer in postmenopausal women.

Contraindications:

Hypersensitivity to medroxyprogesterone or to any other substance in the formulation;
vaginal bleeding of unclear etiology;
severe liver dysfunction;
pregnancy and the period of breastfeeding;

Carefully:Thrombophlebitis, thromboembolism or stroke (increased risk of developing or in anamnesis), renal, hepatic or heart failure, hypercalcemia, epilepsy, migraine, bronchial asthma, diabetes, depressive states.

Pregnancy and lactation:Contraindicated in pregnancy and lactation.

Dosing and Administration:

It is administered intramuscularly.

The dose of Medroxyprogesterone-LENS® is determined individually and depends on the indications. With endometrial cancer and kidney cancer: the initial dose is 500 mg - 1000 mg once a week.If within a few weeks or months in a patient's condition there has come an improvement and stabilization of the process is achieved, then a maintenance therapy is prescribed at a dose of 500 mg per month.

In breast cancer: the initial dose is 500 mg / day for 28 days. Then apply maintenance doses - 500 mg twice a week. The treatment is continued until a positive effect of the drug is observed. The results of therapy for breast cancer may appear delayed - even after 8-10 weeks from the beginning of treatment with the drug.

Immediately before use, the vial should be shaken well to allow the drug to form a homogeneous suspension.

Side effects:

From the genitourinary system: dysfunctional uterine bleeding (irregular, abundant, lean), amenorrhea, changes in cervical secretion, erosion of the cervix, prolonged anovulation, changes in libido.

From the nervous system: confusion, depression, dizziness, euphoria, fatigue, headache, insomnia, decreased ability to concentrate, increased nervous excitability, drowsiness, visual disturbances.

From the side of the digestive system: constipation, diarrhea, dry mouth, abnormal liver function, jaundice, nausea, vomiting, changes in appetite

From the endocrine system: galactorrhea, mastodynia, tenderness of the breast or mammary glands, effects characteristic of corticosteroids (such as Cushing's syndrome), decreased glucose tolerance, diabetic cataracts, exacerbation of diabetes mellitus, glucosuria.

From the side of the cardiovascular system: stroke, myocardial infarction, chronic heart failure, increased blood pressure, a feeling of strong palpitations, pulmonary embolism, retinal vascular thrombosis, tachycardia, thromboembolic disorders, thrombophlebitis.

On the part of the hematopoiesis system: an increase in the number of leukocytes and platelets in the blood.

From the skin and skin appendages: acne, alopecia, hirsutism, itching, rash, urticaria. From the immune system: hypersensitivity reactions (anaphylaxis and anaphylactoid reactions, angioedema).

Local Reactions: pain, residual compaction, discoloration of the skin at the injection site.

Other: swelling / fluid retention in the body, hypercalcemia, hyperthermia, weight change, adrenergic effects (such as hand tremor, sweating, muscle cramps at night), decreased bone density (PCT).

Overdose:

The use of very high doses of the drug can cause a number of symptoms, including an increase in body weight (with some fluid retention), increased fatigue, and also in some cases the effects inherent in corticosteroids.

In cases of overdose, discontinue use of the drug. Specific treatment is not required.

Interaction:Aminoglutethimide reduces the plasma concentration of medroxyprogesterone acetate, which can lead to a decrease in its effectiveness.

Special instructions:

The drug is used strictly according to prescription and under the supervision of a doctor.

With dysfunctional uterine bleeding, it is necessary to exclude uterine cancer and other organic lesions.

Care should be taken in the treatment of patients whose condition may be adversely affected by fluid retention in the body.

When treating the drug, you should carefully monitor the condition of patients who were previously treated for depression.

When treating patients with diabetes mellitus, the ability of MPA to reduce glucose tolerance should be considered.

If the cytological or histological examination of the endometrium or cervix is performed against the background of the treatment, the pathologist should be warned about the therapy.

With sudden partial or complete loss of vision, or with sudden development of exophthalmos, double vision, migraine attacks, the drug should be stopped immediately. If there is a lesion of the blood vessels of the fiber or edema of the nipple of the optic nerve, the treatment of MPA should be canceled.

Although there has been no causal relationship between the use of MPA and the development of thromboembolic disorders in patients with these abnormalities in the history or when they occur against the background of treatment, the possible risk and benefit should be carefully assessed when initiating or deciding whether to continue treatment. The use of MPA as a contraceptive intramuscularly at 150 mg once in 3 months in adult women of childbearing age and in adolescent girls leads to a decrease in PCT of the lumbar bones for 5 years on average by 5.4% and 4.2%, respectively,while during the first 2 years after the discontinuation of the drug, bone tissue is partially restored. The greatest decrease in PCT is observed in the first 2 years of application of the drug.

All patients who use MPA are recommended to take calcium and vitamin D preparations, and in some cases with prolonged use - periodically measure PBC.

In some patients receiving MPA, suppression of the function of the adrenal cortex (decrease in the concentration of adrenocorticotropic hormone (ACTH) and hydrocortisone in the blood) is revealed.

When conducting laboratory studies, it should be noted that the use of MPA can reduce the levels of the following endocrine biomarkers: steroids in blood plasma and urine (cortisol, estrogens, pregnanediol, progesterone, testosterone); gonadotropins in blood plasma and in urine (LH and FSH); specific globulin that binds sex hormones.

When conducting the metapyrone test, it should be borne in mind that high doses of MPA used in oncology can cause partial adrenal insufficiency (a decrease in the response of the pituitary-adrenal system), so before the introduction of the metapyron, it is necessary to check the ability of the adrenal cortex to respond to ACTH.

Form release / dosage:Suspension for intramuscular injection of 500 mg / 3.3 ml and 1000 mg / 6.7 ml (150 mg / ml).

Packaging:

In vials of colorless or light-protective glass.

1 bottle with instructions for use in a cardboard pack.

For the hospital: 35, 50, 85 bottles in a box of cardboard with application instructions for use, based on one instruction for 10 bottles.

Storage conditions:In a place protected from light and inaccessible to children at a temperature not exceeding 30 ° C.

Shelf life:

3 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000457 / 01

Date of registration:13.08.2007 / 29.07.2016

Expiration Date:Unlimited

The owner of the registration certificate:LENS-PHARM, LLC LENS-PHARM, LLC Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp26.04.2018

Illustrated instructions

Instructions

Medroxyprogesterone-LENS (Medroxyprogesteron-LANS)