Levonorgestrel + Estradiol (Levonorgoestrelum + Oestradiolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

"Estrogens, gestagens, their homologues and antagonists"

Included in the formulation
АТХ:

G.03.F.B   Progestogens in combination with estrogens (combinations for sequential administration)

G.03.F.B.09   Levonorgestrel and estrogen

Pharmacodynamics:

Combined estrogen-progestational drug. In the first 9 days of taking the drug, the tablets contain estrogen, then for 12 days - in combination with gestagen, which prevents endometrial hyperplasia. The seven-day break in taking the drug simulates a physiological hormonal cycle. In women with an unrefined uterus, the menstrual cycle is normalized.

Estradiol replenishes the deficiency of estrogen during menopause, providing treatment for climacteric disorders: hot flashes, hyperhidrosis, emotional lability, tachycardia, cardialgia, urinary incontinence due to weakening of the sphincter of the bladder.

Relieves the soreness of sexual intercourse due to the dryness of the vaginal mucosa, prevents the involution of the skin by increasing the formation of collagen fibers.

With regular use, the levels of total cholesterol, low density lipoproteins decrease, the content of triglycerides and high-density lipoproteins increases, which prevents the development and progression of atherosclerosis.

Estradiol suppresses the activity of osteoclasts, preventing the development of postmenopausal osteoporosis.

Levonorgestrel provides maturation of endometrial cells, stopping the stimulation of their growth by estradiol.

Pharmacokinetics:

Estradiol

After oral administration, it is quickly and completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 2-3 hours. Metabolism in the liver.

The elimination half-life is 24 hours. Elimination by the kidneys.

Levonorgestrel

After oral intake absorbed quickly and completely (bioavailability 100%). The maximum concentration in the blood plasma is reached after 1-1.5 hours. It binds to plasma proteins by 97.5%. Metabolised in the liver.

The elimination half-life is 24.4 hours. Elimination by the kidneys.

Indications:

It is used as a means for hormone replacement therapy in women in the period of natural or artificial (after surgical treatment) menopause.

ICD-10

XIII.M80-M85.M81.0   Postmenopausal osteoporosis

XIII.M80-M85.M81.1   Osteoporosis after removal of ovaries

XIV.N80-N98.N95.3   Conditions associated with artificially induced menopause

XIV.N80-N98.N95.1   Menopause and menopause in women

XIV.N80-N98.N95   Menopause disorders and other disorders in the perimenopausal period

Contraindications:

Tumors of the mammary glands, endometrial and ovarian cancer, acute diseases and liver tumors, intracranial hypertension (including history), thrombophlebitis and thromboembolism in history, undiagnosed bleeding from genital organs and urinary tract, diabetes mellitus complicated by angiopathy, ischemic heart disease.

Individual intolerance
Carefully:

Diseases of the liver and bile ducts, Crohn's disease, jaundice, including history, multiple sclerosis, hypertension, epilepsy, tuberculosis, varicose veins, mastopathy.

Pregnancy and lactation:Recommendations for FDA - category X. During pregnancy and during lactation it is contraindicated.
Dosing and Administration:

Inside. 1 tablet once a day, regardless of the time of food intake for 21 days with a break of 7 days. With the remaining menstrual cycle, the drug begins with 4 days. In the absence of menstruation - from any day. If you miss a drug, take the next pill for 12 hours, or two on the next day. The course of treatment before the disappearance of symptoms of menopause, with a view to preventing osteoporosis - up to 10 years.

The highest daily dose: 1 dragee.

The highest single dose: 2 dragees (if you miss a drug).

Side effects:

Central and peripheral nervous system: intracranial hypertension, bulbospinal paralysis, headache, emotional lability, fast fatigue.

The cardiovascular system: thrombophilia.

Digestive system: nausea, vomiting, flatulence.

Reproductive system: metrorrhagia, stress and enlargement of the mammary glands, a change in the libido.

Sense organs: intolerance to contact lenses.

Dermatological manifestations: Chloasma, erythema nodosum.

Allergic reactions.

Overdose:

Symptoms: nausea, vomiting.

Treatment: symptomatic.

Interaction:

Decrease in the effectiveness of estrogens is observed with simultaneous administration with antibiotics of the penicillin series, tetracyclines, ritonavir.

Ascorbic acid, paracetamol, atorvastatin increase the concentration of estrogens.

Reduces the effectiveness of glucocorticoids, clofibrate.

Enhances the effect of hepatotoxic drugs due to the activation of hepatic blood flow by estrogens.

When used simultaneously with cyclosporine, the risk of toxicity increases.

Levonorgestrel affects the effectiveness of anticoagulants and hypoglycemic drugs.

Special instructions:

Smoking of tobacco reduces the concentration of estrogen, increasing the risk of cardiovascular disease.

The drug does not have a contraceptive effect. In the absence of a menstrual-like reaction in response to the withdrawal of the drug, it is recommended to exclude pregnancy. If the result is positive, cancel the drug. At random reception of a preparation in the beginning of pregnancy of the data on disturbance of an embryogenesis it is not revealed.

Instructions
Up