2010/06/06

TRIAKLIM

Pharmacological action

The combined three-phase preparation for hormone replacement therapy in peri-and postmenopausal women. Estradiol eliminates symptoms caused by lack of endogenous estrogen. Norethisterone prevents over-stimulation of the endometrium due to the action of estrogen.

Estradiol is identical to the endogenous estradiol, produced ovaries. It reduces or eliminates the early symptoms of estrogen deficiency causes a moderate proliferation of the endometrium and enhances trophism urinary organs. Plays an important role in the development of the bone tissue, prevents or reduces the decrease of bone mineral component, prevents the development of osteoporosis. Influencing the hypothalamic-pituitary system, eliminates the vegetative-vascular and psycho-emotional disorders.

The synthetic progestin - norethisterone, like progesterone serves to reduce the increased stimulation and proliferation of the endometrium, arising under the influence of estrogen.

While receiving a pink tablets or the end of the reception of white tablets of the drug occurs menstrualnopodobnoe bleeding due to cancellation of gestagen component.

The drug is not Triaklim contraceptives.


Pharmacokinetics

Estradiol

Absorption and distribution

Once inside quickly and completely absorbed. Estradiol is almost entirely associated with plasma proteins, mainly binding globulin sex hormone, and to a lesser extent to albumin.

Metabolism and excretion

Under the "first passage" through the liver biotransformiruetsya to less active metabolites: estrone and estriol. Estrone and estriol are allocated bile in the lumen of the small intestine, where the re-absorbed. Total loss of activity occurs as a result of oxidation in the liver.

Write mainly in the urine in the form of biotransformation products (sulfate and glucuronide) and partly in an unchanged form.

Norethisterone

Absorption and distribution

Rapidly and almost completely absorbed from the gastrointestinal tract. C max in plasma is achieved in the range 1-3 h.

Metabolism and excretion

Biotransformiruetsya in the liver. T 1 / 2 varies between 5-12 h, on average 7.6 h. Approximately 60% of the dose released in the form of metabolites in the urine and a small amount - with the feces.


Statement

-Hormone replacement therapy in menopause to reduce symptoms associated with estrogen deficiency (vasomotor lability, atrophy of urogenital organs);

Prophylaxis postmenopauznogo osteoporosis at an increased risk of its development.


Dosage regimen

Assign 1 pi. / day every day.

In the final cessation of menses or rare and sporadic menses (2-4 monthly intervals) treatment can be started any day.

When a saved menstrual cycles of the first pills start with 5 days of menstrual cycle.

Acceptance of the drug should start with light gray tablets, then go to the reception of white tablets, then - to receive the pink tablets. Therapy is carried out without interruption. Typically, during the reception pink tablets containing a low dose of estrogen, cyclic come menstrualnopodobnye bleeding. Occasionally they may appear earlier in the last days of submission of white tablets.

For the prevention of osteoporosis treatment should be started after the onset of menopause as early as possible in the first 2-3 years.

Tablets should be taken by mouth, without chewing and drinking a small amount of liquid.

The drug is not prescribed for children and men.


Side effect

On the part of the urogenital system: in the first months of treatment - mazhuschie or intermenstrual breakthrough bleeding, change in the nature of menstruation, dysmenorrhea, symptoms such as premenstrual syndrome, enlargement of uterine fibroids, the change of cervical erosion and the degree of cervical secretion after 3 months of treatment - amenorrhea, changes in libido.

On the part of the endocrine system: in the first months of treatment - the voltage and / or an increase in mammary glands release secretions from the mammary glands.

On the part of the digestive system: in the first months of treatment - nausea, vomiting, abdominal cramping, bloating, cholestatic jaundice.

Dermatological reactions: chloasma or melazma, erythema multiforme, nodular erythema, hemorrhagic rash, hirsutism, and after 3 months of treatment - alopecia, skin rash, itching.

From the central nervous system: in the first months of treatment - headaches, migraines, dizziness, depression, chorea.

On the part of the organ of vision: after 3 months of treatment - in vision.

Since the cardiovascular system: in the first months of treatment - swelling, after 3 months of treatment - thrombosis, thromboembolism, increased blood pressure.

Miscellaneous: Increase or decrease in body weight, decrease glucose tolerance, worsening trends porphyria, cramping calf muscles.


Contraindications

, Pregnancy (including estimated);

-Lactation (breastfeeding);

-Acute and chronic liver disease, liver disease, or transferred, after which the indices of liver function is not normalized, hepatic impairment;

-Hepatic tumors (hemangioma, liver cancer);

-Thromboembolic disease (including history);

Disturbances of cerebral blood flow (ischemic or hemorrhagic stroke);

-Retinopathy, angiopathy;

-Malignant tumor of the breast or endometrium (including the assumed or history);

-Estrogenozavisimaya swelling (including swelling of the genitals), or suspicion thereof;

, Fibroadenoma of the breast;

-Endometriosis;

-Idiopathic jaundice or itching during a previous pregnancy;

-Genital herpes (including history);

-Bleeding from the genital tract of unknown origin;

-Severe disease (CHD, atherosclerosis, heart disease, myocarditis);

-Severe kidney disease;

-Hypersensitivity to any component of the drug.


Application of pregnancy and breastfeeding

Use of the drug is contraindicated in pregnancy or suspected it, and during lactation.


Application for violations of liver function

Contraindicated in acute and chronic liver disease or illness the liver, after which the indicators of liver function is not normalized, as well as in liver failure.


Application for violations of renal function

With extreme caution should be prescribed the drug for kidney.


Cautions

With extreme caution should be prescribed the drug for asthma, diabetes, migraine, heart failure, liver and gall bladder, epilepsy, hypertension, depression, ulcerative colitis, uterine cancer, fibrocystic mastopathy, varicose veins, kidney disease, tuberculosis , porphyria.

Before using the product should have a general medical examination (blood pressure, the state of the mammary glands, abdominal and pelvic), and gynecological examination to exclude endometrial hyperplasia. With long-term treatment should be carried out gynecological examination every 6 months (analysis of Pap smear of the cervix and the study of mammary glands), in addition, patients should be trained in self-breast examination. If necessary, conduct regular mammograms.

Requires regular monitoring of liver function, blood pressure, urine tests, blood lipid levels.

Acceptance of the drug should be stopped immediately if symptoms phlebitis, deep vein thrombosis, thromboembolic disease, with a significant increase in blood pressure, with the appearance of jaundice, when detecting liver tumors, with the appearance migrenepodobnyh headaches for the first time, the sudden visual impairment, with prolonged immobilization, with the increase of attacks epilepsy in pregnancy.

Prolonged monotherapy with oestrogens (over 1 year) increases the risk of hyperplasia and endometrial cancer. The combination of estrogen with gestagens reduces this risk. When during the reception Triaklima irregular bleeding from the genital tract should be carried out histological examination of endometrial smear. If intermenstrual bleeding lasts longer than 3 months or appeared for the first time after several months of drug treatment, should be diagnostic curettage to exclude malignant tumors of the uterus.

Long-term estrogen therapy is associated with some increased risk of breast cancer to women in menopause. If the duration of treatment of about 5 years or more should consider carefully the risk to the expected beneficial effect. Precautions should be prescribed the drug to women with knotted or fibrocystic mastopathy, including history. The state of the mammary glands in this case is subject to strict controls, including regular mammograms.

In the course of hormone replacement therapy for some diseases may deteriorate. Therefore, patients with otosclerosis, multiple sclerosis, systemic lupus erythematosus, porphyria, melanoma, epilepsy, migraine or asthma should regularly and thoroughly examination. In addition, under the influence of estrogen therapy may increase in the size of the available uterine fibroids with a subsequent worsening of symptoms of endometriosis.

Should closely monitor the status of patients with cardiovascular disease or renal dysfunction, because the drug contributes to water retention and sodium in the body. Patients with hypertension should routinely monitor blood pressure.

In the initial period of taking the medication a patient with diabetes requires careful monitoring because of possible reduction in glucose tolerance.

When you receive Triaklima increases the risk of gallbladder disease.

During the course of Triaklima may be distorted by the results of some laboratory parameters: the function of the liver, kidney, adrenal gland, thyroid gland.

Acceptance of the drug should be discontinued for 6 weeks before the planned surgery to prevent thrombosis.


Overdose

Symptoms: nausea, vomiting, breast tenderness or excessive formation of cervical mucus.

Treatment: No specific antidote, if necessary, carry symptomatically.


Drug Interactions

Effectiveness Triaklima decreases with simultaneous application with inducers of microsomal liver enzymes (hydantoin, fenilbutazon), with barbiturates, antiepileptic drugs (phenytoin, carbamazepine) due to increased metabolism of components of the product, with antibiotics (ampicillin, rifampin), with drugs for general anesthesia, opioid analgesics, anxiolytics, ethanol, some antihypertensive drugs.

With simultaneous application of Triaklima with hypoglycemic agents may require adjustment of doses of the latter.

Mineral oil may decrease the absorption Triaklima from the intestine.