Drospirenone - Ethinyl Estradiol

Drospirenone - Ethinyl Estradiol:

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Drospirenone + Estradiol: instructions and application
Russian title
Drospirenone + Estradiol
Latin name for substances Drospirenone + Estradiol
Drospirenone + Estradiol
Pharmacotherapeutic group substances Drospirenone + Estradiol
Estrogens, progestins, and their homologues and their antagonists in combination
Typical clinical and pharmacological article

Farmdeystvie. Combined estrogen-progestin medication. Estradiol in the human body turns into a natural 17 beta-estradiol. Drospirenone - a derivative of spironolactone, which has progestin, antigonadotropnym and antiandrogenic and antimineralokortikoidnym action. Estradiol restores estrogen deficiency in the body after menopause, and provides effective treatment for psycho-emotional and vegetative menopausal symptoms (such as hot flashes, sweating, sleep disturbance, increased nervous excitability, irritability, palpitations, false angina, dizziness, headache, decreased libido, myalgia , arthralgia), involution of the skin and mucous membranes, especially the mucous membranes of the genitourinary system (urinary incontinence, dryness and irritation of the mucous membrane of the vagina, dyspareunia). Warns bone loss caused by estrogen deficiency, which is mainly due to the suppression of the function of osteoclasts and the shift in the process of bone remodeling toward bone formation. Proved that the prolonged use of HRT reduces the risk of peripheral bone fractures in women after menopause. With the abolition of HRT the rate of decline in bone mass are comparable with those typical for the period immediately after menopause. Has not been proved that using HRT, you can achieve the restoration of bone mass to premenopausal levels. HRT also has a positive effect on collagen content in skin, skin density, slows the formation of wrinkles. Thanks to the antiandrogenic properties of drospirenone, the drug has a therapeutic effect on androgen-dependent diseases such as acne, seborrhea, androgenic alopecia. Drospirenone has antimineralokortikoidnoy activity, increases the excretion of Na + and water, which may prevent increased blood pressure, body weight, edema, breast tenderness and other symptoms associated with fluid retention. After 12 weeks of use of the drug noted a slight decrease in blood pressure (systolic - an average of 2-4 mm Hg diastolic - by 1-3 mm Hg). Effect on blood pressure is more pronounced in women with borderline hypertension. After 12 months of preparation the average body weight remained unchanged or decreased to 1,1-1,2 kg. Drospirenone is deprived of androgen, estrogen and glucocorticosteroid антиглюкокортикостероидной activity has no effect on glucose tolerance and insulin resistance, which in combination with antimineralokortikoidnym and antiandrogenic effects, drospirenone provides biochemical and pharmacological profile similar to natural progesterone. The drug leads to a decrease in total cholesterol and LDL, as well as the slight increase in triglycerides. Drospirenone attenuates increase in the concentration of triglycerides, vyzyvamy estradiol. Adding drospirenone prevents the development of hyperplasia and endometrial cancer. Observational studies suggest that among postmenopausal women using HRT reduces the incidence of colon cancer. The mechanism of action so far unclear.

Pharmacokinetics. Estradiol: after oral administration is rapidly and completely absorbed. In the course of absorption and "primary transmission" through the liver, estradiol is largely exposed to the metabolism (including estrone, estriol and estrone sulfate). Bioavailability - about 5%. Food intake did not affect the bioavailability of estradiol. Cmax - 22 pg / ml, TSmax - 6-8 pm Css estradiol after multiple doses is approximately 2 times higher than after a single dose. The average concentration of estradiol in serum is in the range 20-43 pg / ml. After discontinuation of the drug concentrations of estradiol and estrone returned to baseline values within 5 days. Estradiol binds to albumin and globulin, sex hormone binding (SHBG). Free fraction of estradiol in serum is approximately 1.12% and the fraction of matter associated SHBG - 40-45%. The apparent volume of distribution - about 1 liter / kg. Metabolized primarily in the liver and partially in the intestine, kidney, skeletal muscle and the target organs with the formation of estrone, estriol, kateholestrogenov, as well as sulfate and glyukuronidnyh conjugates of these compounds with a substantially lower estrogenic activity or pharmacologically inactive. Clearance of estradiol - about 30 ml / min / kg. Estradiol metabolites excreted in urine and bile with T1 / 2 - 24 hours Drospirenone: after oral administration is rapidly and completely absorbed. Bioavailability - 76-85%. Food intake did not affect the bioavailability. Cmax - 22 ng / ml, TSmax - 1 h after single and multiple receiving 2 mg drospirenone. After that, there is a two-phase reduction of serum concentration with the end of T1 / 2 approximately 35-39 hours Css achieved after approximately 10 days of daily dosing. Due to the long T1 / 2 drospirenone Css 2-3 times higher than the concentration after a single dose. Drospirenone binds to serum albumin and is not associated with SHBG and corticoid-binding globulin. About 3-5% of drospirenone is not associated with proteins. The main metabolites are the acid form of drospirenone and 4,5-digidrodrospirenon-W-sulfate, which are formed without the participation of cytochrome P450. Clearance of drospirenone - 1,2-1,5 ml / min / kg. Write mainly in the form of metabolites in urine and feces at a ratio of 1,2:1,4, with T1 / 2 approximately 40 h, a fraction excreted unchanged in.

Testimony. HRT for menopausal disorders in postmenopausal women with non-removed uterus. Prevention of postmenopausal osteoporosis.

Contraindications. Hypersensitivity, unexplained vaginal bleeding, or suspected breast cancer or suspected hormone-dependent precancerous or hormone-dependent cancers, benign or malignant liver tumors (including history), severe liver disease, severe kidney disease, in m . h. history (up to normalization of renal function), acute arterial thrombosis or thromboembolism (including myocardial infarction, stroke), deep vein thrombosis in the art. acute venous thromboembolism (including history), marked hypertriglyceridemia, pregnancy, lactation.

With caution. Hypertension, congenital hyperbilirubinemia (Gilbert's syndrome, Dubin-Johnson and Rotor), cholestatic jaundice or cholestatic pruritus during pregnancy, endometriosis, uterine fibroids, diabetes.

Dosing. Oral, 1 tablet daily. Swallow the tablet whole, squeezed a small amount of liquid. If a woman does not take estrogens or transferred to other combined hormonal preparation for continuous reception, she may begin treatment at any time. Patients who switch from a combined preparation for cyclical HRT should begin taking the drug after the bleeding, "cancel".

After discontinuation of 28 tablets from the current package, the next day, start a new pack, taking the first pill on the same day of the week as the first pill from the previous package.

Time of day when a woman takes the drug, it does not matter, but if she started to take the pills at any particular time, it must adhere to this time and beyond. Forgotten tablet should drink as soon as possible. If, however, after the usual time of reception has been more than 24 hours, an additional tablet should not be accepted. You missed a few pills may develop vaginal bleeding.

Side effects. From the reproductive system: "breakthrough" uterine bleeding and spotting (usually stop during therapy), changes in the character of vaginal discharge, increasing the size of the fibroids, a condition similar to premenstrual syndrome, pain, stress and / or breast enlargement, benign breast glands.

From the digestive system: dyspepsia, flatulence, nausea, vomiting, abdominal pain, recurrent cholestatic jaundice.

For the skin: skin rashes, itchy skin, chloasma, erythema nodosum, erythema multiforme.

CNS: headache, migraine, dizziness, emotional lability, anxiety, increased nervous irritability, fatigue, insomnia.

Other: rarely - heart palpitations, edema, increased blood pressure, varicose veins, superficial thrombophlebitis, venous thrombosis and thromboembolism, muscle cramps, weight change, changes in libido, visual disturbances, intolerance to contact lenses, and allergic reactions.

Overdose. Acute toxicity studies showed no risk of severe side effects if accidentally taking the drug in an amount many times greater than the daily therapeutic dose.

Symptoms (estimated): nausea, vomiting, vaginal bleeding.

Treatment: symptomatic, there is no specific antidote.

Interaction. Prolonged treatment with drugs which induce liver enzymes (including derivatives of hydantoin, barbiturates, primidone, carbamazepine, rifampicin, oxcarbazepine, topiramate, felbamate, griseofulvin) could increase the clearance of sex hormones and reduce their clinical efficacy. Maximal enzyme induction is usually observed 2-3 weeks after starting treatment and may persist for 4 weeks after stopping treatment.

In rare cases, against the background of the accompanying admission of certain antibiotics (including penicillin and tetracycline groups) there was a decrease of concentration of estradiol.

Drugs are largely exposed to the conjugation (including paracetamol) may increase the bioavailability of estradiol by competitive inhibition of conjugation in the process of absorption.

Ethanol can increase the concentration of circulating estradiol.

Special instructions. Does not apply to contraception. If you need contraception, you should use non-hormonal methods (with the exception of calendar and temperature methods). If you suspect a pregnancy, you should stop taking the drug for as long as the pregnancy will not be excluded.

A number of controlled, randomized and epidemiological studies found an increased relative risk of venous thromboembolism (including deep vein thrombosis or pulmonary embolism) during HRT. Therefore, the appointment of HRT for women with risk factors for venous thromboembolism is necessary to correlate the risks and benefits and to discuss with the patient.

Risk factors for venous thromboembolism include personal and family history (presence of venous thromboembolism in the immediate family in the relatively young age may indicate genetic predisposition), and obese. The risk of venous thromboembolism also increases with age. The possible role of varicose veins in the development of venous thromboembolism remains controversial.

The risk of venous thromboembolism may temporarily increase during prolonged immobilization, extensive planning, operations, trauma, or massive trauma. Depending on the cause or duration of immobilization should decide whether a temporary cessation of HRT.

Should immediately discontinue treatment if symptoms of thrombotic disorders or suspected their appearance.

In the randomized controlled trials with prolonged use of combined conjugated estrogens and medroxyprogesterone was not obtained evidence of positive impact on the CAS. Was also found increased risk of stroke. So far, not been long-term randomized controlled trials with other drugs for HRT to detect a positive effect on morbidity and mortality related to CAS. Therefore unknown whether the increased risk in HRT preparations containing other types of estrogen and progestogen.

During prolonged estrogen alone increases the risk of endometrial hyperplasia or carcinoma. Studies have confirmed that the combination with progestin reduces the risk of hyperplasia and cancer endometriya.Po clinical trials and the results of observational studies have found increased risk of developing breast cancer among women using HRT for several years. This may be due to earlier diagnosis, biological effects of HRT, or a combination of both factors. The relative risk increases with duration of treatment (at 2.3% over 1 year of use). This compares with an increased risk of breast cancer in women each year delay in natural menopause (at 2.8% for 1 year delay). The increased risk gradually decreases to normal levels during the first 5 years after cessation of HRT. Breast cancer detected in women taking HRT, usually more localized than in women, it did not take.

HRT increases mammographic breast density, which in some cases may have a negative impact on the radiological detection of breast cancer.

Therapy with sex hormones in rare cases benign, and even more rarely - malignant liver tumors, in some cases life-threatening intraabdominal bleeding. When a pain in the upper abdomen, liver enlargement or signs of intraabdominal haemorrhage in the differential diagnosis should consider the probability of having liver tumors.

Established that estrogen increases the bile lithogenicity that increases the risk of cholelithiasis in predisposed patients.

Should immediately discontinue treatment, the appearance of the first migraine or frequent and unusually severe headaches, as well as the appearance of other symptoms - possible precursors of thrombotic stroke in the brain.

The relationship between HRT and the development of clinically significant hypertension has not been established. In women taking HRT, described a slight increase in blood pressure, clinically significant improvement is noted rarely. However, in some cases, the development while taking HRT persistent clinically significant hypertension should consider the abolition of HRT.

In renal failure may decrease the ability of removing K +. Receiving drospirenone has no effect on the concentration of K + in serum in patients with mild to moderate renal insufficiency. The risk of developing hyperkalemia is theoretically impossible to exclude a group of patients in whom the concentration of K + in serum before treatment was determined at the upper limit of normal, and that further take potassium-sparing drugs.

For non-severe hepatic dysfunction, including various forms of hyperbilirubinemia (Dubin-Johnson syndrome, Rotor), requires medical supervision and periodic liver function tests. With deteriorating liver function tests HRT should be discontinued.

At relapse of cholestatic jaundice or cholestatic pruritus observed for the first time during pregnancy or previous treatment of sex hormones, you should immediately discontinue HRT.

Need special surveillance of women with moderate hypertriglyceridemia. In such cases, the use of HRT may cause a further increase in concentration of triglycerides in the blood, which increases the risk of acute pancreatitis.

Although HRT may influence the peripheral insulin resistance and glucose tolerance, need to change the treatment regimen of patients with diabetes mellitus during HRT, does not normally arise. Nevertheless, women with diabetes during HRT should be monitored.

Some patients under the influence of HRT may develop undesirable manifestations of estrogen stimulation, including abnormal uterine bleeding. Frequent or persistent abnormal uterine bleeding during treatment are an indication for the study of the endometrium.

If the treatment of irregular menstrual cycles, no results, you should conduct a survey to exclude organic disease character.

Under the influence of estrogen uterine fibroids may increase in size. In this case, treatment should be discontinued.

It is recommended to discontinue treatment with relapse of endometriosis on the background of HRT.

If you suspect the presence of prolactinoma before treatment should eliminate the disease.