Climara transdermal therapeutic system is 3.9 mg/12.

CLIMAR – estrogenic.

pharmacokinetics

Estradiol released from the patch (50 g daily) and transdermally enters the bloodstream at a constant speed, maintaining a predetermined level of the hormone in plasma.

Active substance:
Estradiol

Manufacturer

Bayer Pharma AG, Germany

Prescribing

Adults are prescribed by a doctor, for post-menopausal women, for women in menopause

Composition

1 patch comprises:

The active ingredient is:

estradiol hemihydrate;

Excipients:

ethyl oleate – 19.25 mg

isopropyl – 9.65 mg,

glyceryl monolaurate – 4.8 mg,

acrylate copolymer – 99 mg.

Indications

At menopause, osteoporosis

Hormone replacement therapy for disorders caused by natural or surgical menopause (only in the case of non-cancer diseases): vasomotor symptoms (hot flushes, sweating), sleep disorders, atrophic processes.

Prevention of postmenopausal osteoporosis.

Contraindications

Hypersensitivity, breast cancer, endometriosis, tumor liver, tumor, depending on sex steroid hormones, vaginal bleeding of unknown etiology, thromboembolic processes (thrombophlebitis, thrombosis), pregnancy, breast-feeding.

Side effects

Local Reactions: The most commonly – skin irritation at the site of application.

On the part of the reproductive system: breakthrough bleeding and spotting from the vagina, increasing the size of uterine fibroids, changes in vaginal secretion, pain and breast enlargement.

From the digestive system: nausea, vomiting, stomach pain, epigastric pain, bloating, cholestatic jaundice.

Dermatologic reactions: chloasma, melasma, which may be persistent.

Allergic reactions: in some cases – allergic contact dematit, itching, generalized rash.

CNS: headache, migraine, dizziness, and depression.

Other: changes in body weight, current worsening of porphyria, edema, changes in libido, muscle cramps

How to accept, acceptance rate and dosage

When HRT to reduce the symptoms of estrogen deficiency due to natural menopause or the surgical removal yaichnikovprimenyayut TTS containing the lowest dose of estradiol. If necessary, can be employed TTC higher dose of estradiol. Subsequently CLIMAR be applied with the lowest effective dose of the active substance.

With a view to the prevention of osteoporosis, treatment should begin immediately after the onset of menopause. Recommended long-term treatment, which established the scheme individually.

Treatment should be carried out either continuously or in cyclic operation.

Estrogen therapy is only used if a woman has had a hysterectomy. In all other cases, prescribe appropriate doses of progestogen therapy for 10-14 days each month.

TTC must be secured every week continuously. Each used patch should be removed after 7 days, after that a new patch is attached to a different location.

It may also be recommended CLIMAR use in a cyclic mode. In this case, the TTC is attached weekly for 3 consecutive weeks, followed by a 7-day intervals without attaching the patch to the next treatment.

Menstrualnopodobnoe bleeding normally occurs 2-3 days after discontinuation of the progestogen.

Dosing TTC

After removing the protective film transdermal (patch) is attached on the adhesive side of the clean, dry intact skin (no signs of irritation) along the spine or on the buttocks. TTS is not attached to the breast or near them. The site chosen for fixing the plaster must not be in bold; to avoid attachment to the waist region, as by friction tight clothing patch he may come off.

The patch should be inserted immediately after opening the package and remove the protective film. The patch should be firmly pressed to place his palm fixation for about 10 seconds. It must be ensured that there is good contact with the skin, especially around the edges.

Place of application should be changed at intervals of 1 week.

If the patch is attached correctly, it is possible to take a bath and shower as usual. It will be appreciated that the patch may come off from the skin under the influence of very hot water or sauna.

If the patch has come unstuck, you should stick a new patch on the remaining days of the 7-day interval.

Storage conditions

The drug should be kept out of reach of children at a temperature not higher than 30 ° C.

Active substance

Estradiol

Interaction

Prolonged simultaneous application CLIMAR preparation with inducers of microsomal liver enzymes (e.g., derivatives of hydantoin, barbiturates, primidone, carbamazepine, rifampicin, but also, apparently, to oxcarbamazapine, topiramate, felbamate and griseofulvin) may increase the clearance of hormones and decreased clinical efficacy . Maximal enzyme induction is generally not seen for 2-3 weeks but may then persist for at least 4 weeks after the cessation of drug therapy.

Significant use of alcohol during use of HRT may lead to increased levels of circulating estradiol.

Special conditions

Before treatment, the process or re-appointment of HRT woman should undergo a thorough general medical and gynecological examination, including pelvic examination (with cytological examination of cervical mucus), abdominal cavity, mammary glands, blood pressure control, the study of the coagulation system and lipid profile. In patients with diabetes need to control glucose in the blood (at least 1 time per year).

Hormonal contraception must be discontinued at the beginning of HRT, the patient should be encouraged to non-hormonal contraception if necessary.

If any of the conditions / risk factors mentioned below are available before the start of therapy, or progress, in each case should consider the potential risks and benefits of therapy CLIMAR before commencing or continuing HRT.

Diseases of the cardiovascular system. A number of epidemiological studies have revealed a slight increase in the incidence of venous thromboembolism (VTE), such as deep vein thrombosis or pulmonary embolism in women taking HRT. If HRT is recommended for women with risk factors for VTE should carefully weigh the risk / benefit ratio of the therapy.

risk factors for VTE include a personal and family history (VTE development with close relatives at a relatively young age may indicate genetic predisposition) and severe obesity. The risk of VTE also increases with age. No single point of view on the possible role of varicose veins in VTE development.

VTE risk increases with prolonged immobilization, major surgery or major trauma. Depending on the etiology of the disease and the duration of immobilization should be considered temporary cessation of HRT.

Treatment should be discontinued immediately in the presence of thromboembolic symptoms or suspicion on them.

Endometrial cancer. With long-term exposure to estrogen increases the risk of endometrial hyperplasia or carcinoma. Studies have confirmed that the additional appointment of progestogens reduces the risk of endometrial hyperplasia and / or endometrial cancer.

Mammary cancer. A meta-analysis of 51 epidemiological studies showed that there is a slightly increased risk of breast cancer diagnosed in women who received HRT for 5 years. The observed increase in risk may be due to early diagnosis of breast cancer, the biological effects of HRT, or a combination of both factors. The relative risk increases as the duration of treatment. This compares with an increased risk of breast cancer observed in women with delay of natural menopause every year. The increased risk gradually disappears after treatment within the first 5 years after discontinuation of HRT. breast cancer diagnosed in women receiving hormone replacement therapy, compared to those who did not use HRT, rarely metastasizes.

Liver tumors. In extremely rare instances, even less benign or malignant liver tumor were observed after administration of hormonal drugs such CLIMAR. In rare cases, these tumors led to life-threatening intra-abdominal bleeding. The main symptoms of liver tumors are epigastric pain, enlargement of the liver and / or symptoms intraabdominal bleeding.

Gallbladder disease. Estrogens increase the lithogenic bile. In some cases, increased predisposition to diseases of the gallbladder on the background of estrogen therapy.

Other conditions. Treatment should be discontinued immediately if the first time develop migraine or unusually severe headaches or experience other symptoms that are possible precursors of cerebral blood flow.

If in spite of the changes in application space, according to the recommendations, there is a recurring, persistent irritation of the skin (eg, persistent erythema, or itching at the site of application) the application of the TTC should be discontinued.

The general relationship between HRT and the development of clinical hypertension has not been established. Despite the fact that a small increase in blood pressure described in women taking HRT, clinically significant increase in blood pressure observed with such treatment is extremely rare. However, if in individual cases during HRT develops persistent, clinically significant hypertension should consider discontinuing HRT.

Sex steroids may be poorly metabolized in patients with reduced liver function. When HRT via transdermal active agent is not metabolized in the liver during the “first pass” through the liver, in such cases the HRT should be used with caution.

Recurrence of cholestatic jaundice or cholestatic pruritus which developed earlier in pregnancy or during previous use of sex steroids, demands the immediate cessation of HRT.

Some patients receiving HRT may develop undesirable manifestations of estrogen stimulation such as abnormal uterine bleeding. Frequent or persistent abnormal uterine bleeding during treatment is an indication for the study of the endometrium.

Uterine fibroids may increase in size under the influence of estrogen. If this occurs, then treatment should be discontinued.

If endometriosis is exacerbated during treatment, it is recommended the termination of therapy.

If you suspect a prolactinoma diagnosis should be excluded prior to initiating therapy.

Sometimes it can develop chloasma, especially in women with a history of instructions chloasma during pregnancy. Women with a tendency to rise to chloasma should avoid prolonged exposure to sunlight and UV-radiation during HRT.

The following states arise or worsen during HRT: epilepsy, benign breast disease, asthma, migraine, porphyria, otosclerosis, SLE, chorea. Although their relationship with HRT is not finally established, in such cases, women receiving hormone replacement therapy should be monitored carefully.

Laboratory tests. for HRT formulations may influence the results of some laboratory tests including liver function tests, the parameters of the thyroid gland, adrenal gland, and kidney, levels of transport proteins in plasma, e.g., corticosteroid-binding globulin, and fractions of lipids and lipoproteins, parameters of carbohydrate metabolism, coagulation parameters and fibrinolysis.

Effects on ability to drive vehicles and management mechanisms

Any effect was not observed.

Overdose

When applications CLIMAR overdose is unlikely.

Symptoms: nausea, vomiting; in some cases – withdrawal bleeding.

Treatment: removal of the patch, symptomatic therapy. A specific antidote is not known.