Gestoden, Ethinyl estradiol | Logest tablets coated about. 75 mcg + 20 mcg 21 pcs.

Release form

Coated tablets

packaging

21 pcs

Pharmacological action

LOGEST prevents ovulation by suppressing the pituitary hormones and developing follicles. The thickening of cervical mucus prevents the penetration of sperm into the uterus. The drug normalizes the menstrual cycle, reducing pain and bleeding.

Pharmacokinetics of

gestoden. After oral administration, it is rapidly and completely absorbed (bioavailability of approximately 99%). Serum Cmax (3.5 ng / ml) is reached after approximately 1 hour. Gestoden binds to serum albumin and sex hormone binding globulin (SHBG, 69%). Only about 1.3% of the total serum levels of gestodene are in free form. The relative distribution of fractions (free gestoden associated with albumin and associated with SHBG) depends on the concentration of SHBG in serum. Following the induction of SHBG, the fraction associated with SHBG increases to 80%, the free and albumin-bound fraction decreases. Gestoden is almost completely metabolized. The metabolic clearance rate is 0.8 ml / min / kg. A two-phase decrease in serum concentration is observed, T1 / 2 in the terminal phase is about 12 hours. In an unchanged form gestodene is not excreted, but only in the form of metabolites (T1 / 2 - approximately 24 hours), which are excreted in urine and bile in a ratio of about 6 :4.

Ethinyl estradiol. After oral administration, it is rapidly and completely absorbed from the digestive tract. The absolute bioavailability is on average 45% due to the effect of the "first passage" through the liver. Serum Cmax (65 pg / ml) is reached after 1.7 hours. It binds non-specifically to serum albumin (approximately 98%), about 2% is in plasma in free form. The apparent volume of distribution is 2.8–8.6 l / kg. It is subjected to presystemic conjugation both in the mucosa of the small intestine and in the liver. The main metabolic pathway is aromatic hydroxylation. The metabolic clearance rate from blood plasma is 2.3–7 ml / min / kg. A two-phase decrease in serum levels is observed: T1 / 2 - about 1 hour and 10–20 hours, respectively. Unchanged from the body is not excreted. Excreted in the form of metabolites with urine and bile in a ratio of 4: 6 with T1 / 2 for about 24 hours.

Based on T1 / 2 of the final phase and daily dose, the equilibrium concentration is reached after 5-6 days of taking the drug.

Indications

Contraception.

Contraindications

LogestВ® should not be used if any of the conditions listed below is present. If any of these conditions develops for the first time during administration, the drug should be immediately discontinued.

Thrombosis (venous and arterial) and thromboembolism currently or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders).

States, preceding thrombosis (including transient ischemic attacks, angina pectoris), currently or in history.

Migraine with focal neurological symptoms in history.

Diabetes mellitus with vascular complications.

Multiple or severe risk factors for venous or arterial thrombosis, including damage to the valvular apparatus of the heart, cardiac arrhythmias, diseases of the vessels of the brain or coronary arteries of the heart uncontrolled arterial hypertension.

Pancreatitis with severe hypertriglyceridemia at present or in history.

Liver failure and severe liver disease (until the liver tests return to normal).

Tumors of the liver (benign or malignant) are currently or in history.

Identified or suspected hormone-dependent malignant diseases (including genitals or mammary glands).

Vaginal bleeding of unknown origin.

Pregnancy or suspicion of it.

Breastfeeding period.

Hypersensitivity to any of the components of LogestВ®.

Prolonged immobilization, serious surgery, leg surgery, extensive injuries.

CAUTION

Severe impaired fat metabolism (obesity, hyperlipidemia) thrombophlebitis of superficial veins otosclerosis with impaired hearing, idiopathic jaundice or pruritus during previous pregnancy, migraine headache, congenital hyperbilirubinemia (Gilbert syndromes, Dubin-Johnson and Rotor) diabetes mellitus systemic lupus erythematosus hemolytic uremic syndrome Crohn's disease sickle cell anemia arterial hypertension.

Use during pregnancy and lactation

Logest® is not prescribed during pregnancy and during lactation. If pregnancy is detected while taking Logest®, the drug is immediately canceled. However, extensive epidemiological studies did not reveal any increased risk of developmental defects in children born to women who received sex hormones before pregnancy, or teratogenicity when sex hormones were taken by negligence in the early stages of pregnancy.

Taking combined oral contraceptives can reduce the amount of breast milk and change its composition, so their use is contraindicated in lactation. A small amount of sex steroids and / or their metabolites may be excreted in milk, however, there is no evidence of their negative effects on the health of the newborn.

Special instructions

In case of a planned operation, it is recommended to stop taking the drug, at least 4 weeks before it and do not resume taking it within 2 weeks after the end of the immobilization.

During the administration of drugs that affect microsomal enzymes, and within 28 days after their withdrawal, the barrier method of contraception should be additionally used.

While taking antibiotics such as ampicillins and tetracyclines and within 7 days after they are canceled, you should additionally use the barrier method of contraception.

If the period of use of the barrier method of protection ends later than the dragee in the package, proceed to the next LogestВ® package without the usual interruption in the reception of dragees.

If any of the conditions / risk factors listed below are currently available, you should carefully weigh the potential risk and the expected benefits of LogestВ® treatment in each individual case and discuss it with the woman before she decides to start taking the drug. In the event of a worsening, worsening or first manifestation of any of these conditions or risk factors, a woman should consult with her doctor, who can decide whether to discontinue the drug.

Diseases of the cardiovascular system

There is evidence of an increase in the incidence of venous and arterial thrombosis and thromboembolism when taking combined oral contraceptives.

However, the frequency of venous thromboembolism that develops when taking combined oral contraceptives is less than the frequency associated with pregnancy (6 per 10,000 pregnant women per year).

In women, taking combined oral contraceptives, extremely rare cases of thrombosis of other blood vessels, such as the hepatic, mesenteric, renal arteries and veins, the central retinal vein and its branches, are described. The connection with the use of combined oral contraceptives has not been proven.

A woman needs to stop taking the drug and consult a doctor if symptoms of venous or arterial thrombosis or cerebrovascular disorders develop, which may include: unilateral leg pain and / or swelling sudden severe chest pain with or without radiation in the left arm sudden shortness of breath sudden attack of cough any unusual, strong, prolonged headache, sudden partial or complete loss of vision, diplopia, slurred speech, or aphasia, dizziness, loss of consciousness with or without a convulsive seizure, weakness or very significant loss of sensation, which suddenly appeared on one side or in one part of the body of the motor symptoms of "acute abdomen".

The risk of thrombosis (venous and / or arterial) and thromboembolism increases: - with age

- in smokers (with an increase in the number of cigarettes or an increase in age, the risk further increases, especially in women over 35 years old)

in the presence of: - a family history (t i.e., venous or arterial thromboembolism ever in close relatives or parents at a relatively young age) in the case of a hereditary predisposition, a woman should be examined by an appropriate specialist to decide on the possibility of taking combined oral contraceptives

- obesity (body mass index more than 30 kg / m2)

- dyslipoproteinemia

- arterial hypertension

- migraine

- heart valve disease

c - fibrillation prolonged immobilization, serious surgery, any leg surgery or extensive injury.

In these situations, it is advisable to stop the use of combined oral contraceptives (in the case of the planned operation, at least 4 weeks before it) and not to resume taking within 2 weeks after the end of the immobilization.

The increased risk of postpartum thromboembolism should be considered.

Circulatory disorders can also occur in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia.

An increase in the frequency and severity of migraines during the use of combined oral contraceptives (which may be preceded by cerebrovascular disorders) may be grounds for immediate discontinuation of these drugs.

Biochemical parameters that may be indicative of a hereditary or acquired predisposition to venous or arterial thrombosis include resistance to activated protein C, hyperhomocysteinemia, antithrombin-III deficiency, protein C deficiency, protein S deficiency, the presence of antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).

Tumors

There is an increased risk of developing cervical cancer with persistent papillomavirus infection. Its connection with the use of combined oral contraceptives has not been proven. Contradictions remain regarding the extent to which these findings relate to the characteristics of sexual behavior and the use of barrier contraception.

It has also been found that there is a slightly increased relative risk of developing breast cancer diagnosed in women who have used combined oral contraceptives. Its connection with the use of combined oral contraceptives has not been proven. The observed increased risk may be due to an earlier diagnosis of breast cancer in women, using combined oral contraceptives.

In rare cases, against the background of the use of combined oral contraceptives, the development of liver tumors was observed. The appearance of severe pain in the abdomen or signs of intra-abdominal bleeding, an increase in the liver should be considered when making a differential diagnosis.

Other conditions

Women with hypertriglyceridemia (or having a family history of this condition) may increase the risk of developing pancreatitis while taking combined oral contraceptives.

Although a slight increase in blood pressure has been described in many women taking combined oral contraceptives, clinically significant increases were rare. However, if during the administration of combined oral contraceptives persistent develops, a clinically significant increase in blood pressure, these drugs should be discontinued and treatment of arterial hypertension should be started. Taking combined oral contraceptives can be continued if normal blood pressure values ​​are achieved with antihypertensive therapy.

The following conditions have been reported to develop or worsen both during pregnancy and when taking combined oral contraceptives, but their relationship with taking combined oral contraceptives has not been proven: jaundice and / or itching associated with cholestasis, the formation of gallbladder stones in porphyria systemic lupus erythematosus hemolytic uremic syndrome of Sydenham herpes chorea of ​​pregnant women hearing loss associated with otosclerosis. Cases of Crohn’s disease and ulcerative colitis with the use of combined oral contraceptives have also been described.

Acute or chronic impaired liver function may require cessation of the use of combined oral contraceptives until liver function returns to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or the previous intake of sex hormones, requires discontinuation of combined oral contraceptives.

Although combined oral contraceptives may affect insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in patients with diabetes mellitus, using low-dose combined oral contraceptives (

) Women who are prone to chloasma while taking combined oral contraceptives should avoid prolonged exposure to the sun and exposure to ultraviolet radiation.

Laboratory tests

Taking combined oral contraceptives may affect the results of some laboratory tests, including liver function tests kidneys, thyroid gland, adrenal glands, plasma transport protein level, carbohydrate indicators sharing parameters coagulation and fibrinolysis. The changes do not usually go beyond the normal range.

Effects on the menstrual cycle

In patients receiving combined oral contraceptives may experience irregular bleeding (spotting or breakthrough bleeding) especially during the first months of use. Therefore, any irregular bleeding should be evaluated only after an adaptation period of approximately 3 cycles.

If irregular bleeding recurs or develops after previous regular cycles, a thorough examination should be performed to rule out malignant neoplasms or pregnancy.

Some women may not develop withdrawal bleeding during a break in taking dragees. If combined oral contraceptives were taken as directed, it is unlikely that the woman is pregnant. However, if before that combined oral contraceptives were taken irregularly, or if 2 withdrawal bleeds were absent in a row, pregnancy should be excluded before continuing with the drug.

Medical examinations

Before using LogestВ®, a woman is advised to undergo a thorough general medical and gynecological examination (including mammary gland examination and cytological examination of cervical mucus), to exclude pregnancy. In addition, violations of the blood coagulation system should be excluded.

In case of prolonged use, it is necessary to conduct control examinations, the frequency of which depends on the individual characteristics of the woman.

A woman should be warned that drugs like LogestВ® do not protect against HIV infection (AIDS) and other sexually transmitted diseases!

No effect on ability to drive a vehicle and machinery has been identified.

Composition

1 tablet contains: active ingredients: gestoden 0.075 mg, ethinyl estradiol 0.02 mg,

excipients: lactose monohydrate - 37.155 mg corn starch - 15.5 mg povidone 25000 - 1.7 mg of magnesium stearate - 0.55 mg,

shell: sucrose - 19.66 mg povidone 700000 - 0.171 mg macrogol 6000 - 2.18 mg calcium carbonate - 8.697 mg talc - 4.242 mg mountain glycolic wax - 0.05 mg

Dosage and administration

Inside, with a small amount of water, daily at about the same time of day, in the order indicated on the package. Take 1 table. per day, continuously for 21 days. Reception of the next package begins after a 7-day break in taking the tablets, during which withdrawal bleeding usually occurs. Bleeding, as a rule, begins 2-3 days after taking the last pill and may not end before taking a new package.

Logest® intake begins:

- in the absence of any hormonal contraceptives in the previous month. Reception of Logest® begins on the first day of the menstrual cycle (i.e. on the first day of menstrual bleeding). It is allowed to start taking on the 2nd – 5th day of the menstrual cycle, but in this case it is recommended to additionally use the barrier method of contraception during the first 7 days of taking the tablets from the first

package - when switching from other combined oral contraceptives, a vaginal ring or a contraceptive patch. It is preferable to start taking Logest® the day after taking the last hormone-containing tablet from the previous package, but in no case later than the next day after the usual 7-day break (for drugs containing 21 tablets) or after taking the last inactive tablet (for drugs containing 28 tablets in a package). Logest® should be started on the day the vaginal ring or patch is removed, but no later than the day when a new ring is to be inserted or a new

patch is applied - when switching from contraceptives containing only gestagens (mini-pill, injection, implant) or gestagen-releasing intrauterine contraceptive device (Mirena). A woman can switch from a mini-drink to Logest® any day (without a break), from an implant or an intrauterine contraceptive with gestagen - on the day of its removal, from the injection form - from the day the next injection should have been made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking

tablets - after an abortion in the first trimester of pregnancy. A woman can start taking the drug immediately. Subject to this condition, a woman does not need additional contraceptive protection

- after childbirth or abortion in the second trimester of pregnancy. It is recommended to start taking the drug on the 21–28th day after childbirth (if the woman does not breast-feed) or abortion in the second trimester of pregnancy. If administration is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the tablets. If a woman has already had a sex life, pregnancy should be ruled out before the start of Logest® or it is necessary to wait for the first menstruation.

Taking missed tablets. If the delay in taking the drug was less than 12 hours, contraceptive protection does not decrease. A woman should take the pill as soon as possible, the next one is taken at the usual time.

If the delay in taking the pills was more than 12 hours, contraceptive protection may be reduced. In this case, one can be guided by the following two basic rules:

- the drug should never be interrupted for more than 7 days

- it takes 7 days of continuous pill administration to achieve adequate suppression of hypothalamic-pituitary-ovarian regulation.

If the delay in taking the pills was more than 12 hours (the interval since taking the last pill was more than 36 hours), the following tips can be given.

First week of taking

A woman should take the last missed tablet as soon as possible (even if it means taking two tablets at the same time). The next tablet is taken at the usual time. Additionally, a barrier method of contraception (such as a condom) should be used over the next 7 days. If sexual intercourse took place during the week before skipping a pill, you must consider the likelihood of pregnancy.

Second week of taking

A woman should take the last missed tablet as soon as possible (even if it means taking two tablets at the same time). The next tablet is taken at the usual time. Provided that the woman took the pill correctly for the 7 days preceding the first missed pill, there is no need to use additional contraceptive measures. Otherwise, as well as when skipping taking two or more tablets, it is necessary to additionally use barrier methods of contraception (such as a condom) for 7 days.

Third week of taking

The risk of a decrease in reliability is inevitable due to the upcoming break in pills. A woman should strictly adhere to one of the following two options (if in the 7 days preceding the first missed pill all tablets were taken correctly, there is no need to use additional contraceptive methods):

1. A woman should take the last missed pill as soon as possible (even if it means taking two tablets at the same time). The next tablet is taken at the usual time until the tablets from the current package run out. The next packaging should be started immediately. Withdrawal bleeding is unlikely until the second pack is over, but spotting and breakthrough bleeding may occur while taking the tablets.

2. A woman may also stop taking pills from the current package. Then she should take a break for 7 days, including the day the pill was skipped, and then start taking a new package.

If a woman missed taking the pill, and then during the break in taking the pill she does not have withdrawal bleeding, pregnancy must be excluded.

Recommendations for vomiting and diarrhea

If a woman has vomited or diarrhea within 4 hours after taking active tablets, absorption may not be complete and additional contraceptive measures should be taken. In these cases, you should be guided by the recommendations when skipping pills.

Change the day onset of menstrual bleeding

In order to delay the onset of menstruation, a woman should continue taking pills from the new Logest® pack immediately after taking all the pills from the previous one, without interruption in intake. Tablets from this new package can be taken as long as the woman wants (until the package is finished). Against the background of taking the drug from the second package, a woman may have spotting or breakthrough uterine bleeding. You should resume taking Logesta® from a new pack after the usual 7-day break.

In order to postpone the day the menstrual bleeding begins on another day of the week, a woman should be advised to shorten the next break in taking the pills for as many days as she wants. The shorter the interval, the higher the risk, that she will not have withdrawal bleeding and there will be spotting and breakthrough bleeding in the future when taking the second pack (the same as when she would like to delay the onset of menstruation).

Additional information for selected patient groups

Elderly patients. Not applicable. Logest® is not indicated after menopause.

Patients with impaired liver function. The drug Logest® is contraindicated in women with severe liver diseases until liver function indicators return to normal.

Patients with impaired renal function. Logest® has not been specifically studied in patients with impaired renal function. Available data do not suggest correction of the dosage regimen in such patients.

Side effects of

In rare cases, there may be soreness and tension of the mammary glands, enlargement of the mammary glands, discharge from the mammary glands, spotting spotting and breakthrough uterine bleeding, headache, migraine, changes decreased / mood changes, poor tolerance of contact lenses, visual impairment, nausea, vomiting, abdominal pain, changes in vaginal secretion, skin rash, erythema nodosum, erythema multiforme, generalization itching, cholestatic jaundice, fluid retention, weight loss, allergic reactions rarely - increased fatigue, diarrhea sometimes - chloasma, especially in women with a history of pregnant chloasma.

As with other combined oral contraceptives, rare cases of thrombosis and thromboembolism are possible.

Drug interactions

Sulfanilamides, pyrazolone derivatives can enhance the metabolism of the steroid hormones that make up the drug.

Long-term drug treatment, inducing liver enzymes, which increases the clearance of sex hormones, can lead to breakthrough bleeding and / or a decrease in the contraceptive effectiveness of Logest®. Such drugs include phenytoin, barbiturates, primidone, carbamazepine and rifampicin. There are also suggestions regarding oxcarbazepine, topiramate, felbamate, ritonavir and griseofulvin and preparations containing St. John's wort.

Contraceptive protection is reduced when taking antibiotics such as ampicillins and tetracyclines, because, according to some reports, they can reduce the intrahepatic circulation of estrogens, thereby lowering the concentration of ethinyl estradiol.

Oral combined contraceptives can affect the metabolism of other drugs (including cyclosporine), which leads to a change in their concentration in plasma and tissues.

When taking estrogen-progestogen drugs, you may need to adjust the dosage regimen of hypoglycemic drugs and indirect anticoagulants.

Overdose

Symptoms: nausea, vomiting, spotting or metrorrhagia.

Treatment: symptomatic. There is no specific antidote.

Storage Conditions

In a dark place at a temperature not exceeding 25 РC.

Shelf life

3 years.

Conditions prescription from pharmacies

Prescription

dosage form

tablets

Prescribing

Prescribing

For women of childbearing age, Adults as prescribed by a doctor

Bayer Pharma AG, Germany1920twitter.com/wp-content/uploads/2008/08/picture-picture-picture.html