Logest pills 75mcg+20mcg, 21pcs

Composition

Active ingredients:

gestoden 0.075 mg,

ethinyl estradiol 0.02 mg,

Auxiliary substances:

lactose monohydrate-37.155 mg;

corn starch-15.5 mg;

povidone 25000-1.7 mg;

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

Pharmacological action

LOGEST-contraceptive.

Pharmacokinetics

Gestoden. After oral use, it is rapidly and completely absorbed (bioavailability is approximately 99%). Serum cmax (3.5 ng/ml) is reached after approximately 1 h. Gestoden binds to serum albumin and sex hormone-binding globulin (SHBG,69%). Only about 1.3% of total serum levels of gestodene are in free form. The relative distribution of fractions (free gestodene, albumin-bound and SHBG-bound) depends on the serum SHBG concentration.

Following SHBG induction, the SHBG-bound fraction increases to 80%, while the free and albumin-bound fractions decrease. Gestodene is almost completely metabolized. The metabolic clearance rate is 0.8 ml / min / kg. There is a two-phase decrease in serum concentration, T 1/2 in the terminal phase is about 12 hours. In unchanged form, gestoden is not excreted, but only in the form of metabolites (T 1/2-approximately 24 hours), which are excreted in the urine and bile in a ratio of approximately 6: 4.

Ethinyl Estradiol.

After oral use, it is rapidly and completely absorbed from the gastrointestinal tract. Absolute bioavailability is on average 45% due to the “first pass” effect through the liver. Cmax in blood serum (65 pg / ml) is reached after 1.7 hours. Non-specifically binds to serum albumins (approximately 98%), about 2% is found in plasma in free form. The apparent volume of distribution is 2.8-8.6 l / kg. It undergoes presystemic conjugation both in the mucosa of the small intestine and in the liver. The main pathway of metabolism is aromatic hydroxylation.

The rate of metabolic clearance from blood plasma is 2.3-7 ml / min / kg. There is a biphasic decrease in serum levels:  T 1/2 — about 1 hour and 10-20 hours, respectively. It is not excreted unchanged from the body. It is excreted as metabolites in the urine and bile in a ratio of 4: 6 with a T 1/2 of about 24 hours.

Based on T 1/2 of the final phase and the daily dose, the equilibrium concentration is reached after 5-6 days of taking the drug.

Indications

Contraception.

Contraindications

• tumors of the mammary glands and genitals
• spotting from the genital tract of unknown origin
• thrombophlebitis
• impaired kidney and liver function
• severe diabetes mellitus
• atherosclerosis
• migraine.

Side effects

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

As with other combined oral contraceptives, thrombosis and thromboembolism may occur in rare cases.

Interaction

Sulfonamides, pyrazolone derivatives can enhance the metabolism of the steroid hormones included in the preparation.

Long-term treatment with drugs that induce liver enzymes, which increases the clearance of sex hormones, may lead to breakthrough bleeding and / or a decrease in the contraceptive effectiveness of Logest®. These drugs include: phenytoin, barbiturates, primidone, carbamazepine and rifampicin; there are also suggestions for 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 changes in their concentration in plasma and tissues.

When taking estrogen-progestogenic drugs, it may be necessary to adjust the dosage regimen of hypoglycemic drugs and indirect anticoagulants.

How to take, course of use and dosage

Inside, with a small amount of water, daily at approximately the same time of day, in the order indicated on the package. Take 1 table each. per day, continuously for 21 days. Taking the next pack begins after a 7-day break from taking the pills, during which withdrawal bleeding usually occurs. Bleeding usually begins 2-3 days after taking the last pill and may not end until you start taking a new package.

Taking Logest® begins:

– in the absence of taking any hormonal contraceptives in the previous month. 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 a barrier method of contraception during the first 7 days of taking 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 the package). Logest® should be started on the day of removal of the vaginal ring or patch, but not later than the day when a new ring or patch should be inserted;

– when switching from progestogen-only contraceptives (mini-pills, injectable forms, implants) or from a progestogen-releasing intrauterine contraceptive (Mirena). A woman can switch from a mini-pill to Logest® on any day (without a break), from an implant or intrauterine contraceptive with a progestogen-on the day of its removal, from an injectable form-from the day when 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 pills;

– after an abortion in the first trimester of pregnancy. A woman can start taking the drug immediately. If this condition is met, the 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 21st-28th day after giving birth (if the woman is not breastfeeding) or having an abortion in the second trimester of pregnancy. If the reception is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the tablets. If the woman has already had sexual activity, pregnancy should be excluded before taking Logest® or it is necessary to wait for the first menstruation.

Taking missed pills. If the delay in taking the drug is less than 12 hours, the contraceptive protection is not reduced. The woman should take the pill as soon as possible, and the next one is taken at the usual time.

If the delay in taking pills is more than 12 hours, the contraceptive protection may be reduced. In this case, you can follow the following two basic rules: :

– the drug should never be interrupted for more than 7 days;

– 7 days of continuous tablet use are required to achieve adequate suppression of hypothalamic-pituitary-ovarian regulation.

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

First week of taking the drug

A woman should take the last missed pill as soon as possible (even if it means taking two pills 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 for the next 7 days. If sexual intercourse took place during the week before skipping the pill, the likelihood of pregnancy should be taken into account.

The second week of taking the drug

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

Third week of taking the drug

The risk of reduced reliability is inevitable due to the upcoming break in taking pills.A woman should strictly adhere to one of the following two options (if all pills were taken correctly in the 7 days preceding the first missed pill, 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 pills at the same time). The next tablet is taken at the usual time, until the tablets from the current package run out. The next package should be started immediately. Withdrawal bleeding is unlikely until the second pack is finished, but there may be spotting and breakthrough bleeding while taking the pills.

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

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

Recommendations for vomiting and diarrhea

If a woman has had vomiting or diarrhea for up to 4 hours after taking the active tablets, absorption may be incomplete and additional contraceptive measures should be taken. In these cases, you should follow the recommendations when skipping pills.

Changing the day of onset of menstrual-like bleeding

In order to delay the onset of menstruation, a woman should continue taking tablets from the new Logest ® package immediately after taking all the tablets from the previous one, without interruption in taking them. Tablets from this new package can be taken for as long as the woman wishes (until the package runs out). Against the background of taking the drug from the second package, a woman may experience spotting or breakthrough uterine bleeding. Resume taking Logest® from a new pack after the usual 7-day break.

In order to move the day of the onset of menstrual-like bleeding to another day of the week, a woman should be advised to shorten the next break in taking pills for as many days as she wants. The shorter the interval, the higher the risk that she will not have withdrawal bleeding and will continue to have spotting and breakthrough bleeding while taking the second package (just as in the case when she would like to delay the onset of menstruation).

Additional information for individual patient groups

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

Patients with impaired liver function. Logest® is contraindicated in women with severe liver disease until liver function returns to normal.

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

Overdose

Symptoms: nausea, vomiting, spotting or metrorrhagia.

Treatment: symptomatic. There is no specific antidote.

Special instructions

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

When taking medications that affect microsomal enzymes, and for 28 days after their withdrawal, you should additionally use a barrier method of contraception.

When taking antibiotics such as ampicillins and tetracyclines and for 7 days after their withdrawal, you should additionally use a barrier method of contraception.

If the period of using the barrier method of protection ends later than the pills in the package, you need to move on to the next package of Logesta® without the usual break in taking pills.

If any of the conditions / risk factors listed below are currently present, the potential risk and expected benefit of Logest® treatment should be carefully weighed on a case-by-case basis and discussed with the woman before she decides to start taking the drug. If any of these conditions or risk factors become more severe, worsen, or first appear, a woman should consult with her doctor, who may decide whether to discontinue the medication.

Diseases of the cardiovascular system

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

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

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, have been reported in women taking combined oral contraceptives. The association with the use of combined oral contraceptives has not been proven.

Women need to stop taking the drug and consult a doctor if you develop symptoms of venous or arterial thrombosis or cerebrovascular disorders, which can include: unilateral leg pain and/or swelling; sudden severe pain in the chest with or without radiating to the left arm; sudden breathlessness; sudden attack of coughing; any unusual, severe, prolonged headache; sudden partial or complete loss of vision; diplopia; slurred speech or aphasia; vertigo; loss of consciousness with or without convulsive seizure; weakness or very significant loss of sensitivity suddenly appeared on one side or in one part of the body; movement disorders; 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 increases further, especially in women over 35 years of age); in the presence of:- family history (i. e. venous or arterial thromboembolism ever in close relatives or parents at a relatively young age); in the case of hereditary predisposition, the woman should be examined by an appropriate specialist to decide whether to take combined oral contraceptives;- obesity (body mass index more than 30 kg / m2); – dyslipoproteinemia; – arterial hypertension; – migraines; – heart valve diseases; – atrial fibrillation;- prolonged immobilization, major surgery, any leg surgery, or extensive trauma.

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

An 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 diseases (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 precede cerebrovascular disorders) may be a reason for immediate discontinuation of these medications.

Biochemical parameters that can be indicators of 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, and the presence of antiphospholipid antibodies (cardiolipin antibodies, lupus anticoagulant).

Tumors

There are reports of an increased risk of developing cervical cancer with persistent papillomavirus infection. Its association with the use of combined oral contraceptives has not been proven. Controversy persists as to the extent to which these findings relate to the characteristics of sexual behavior and the use of barrier contraception.

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

In rare cases, the development of liver tumors was observed against the background of the use of combined oral contraceptives. The appearance of severe abdominal pain or signs of intra-abdominal bleeding, liver enlargement should be taken into account when making a differential diagnosis.

Other states

Women with hypertriglyceridemia (or a family history of this condition) may have an increased risk of developing pancreatitis while taking combined oral contraceptives.

Although a small increase in blood pressure has been reported in many women taking combined oral contraceptives, clinically significant increases have rarely been observed. However, if a persistent, clinically significant increase in blood pressure develops while taking combined oral contraceptives, these drugs should be discontinued and treatment for arterial hypertension should be initiated. The use of combined oral contraceptives can be continued if normal blood pressure values are achieved with the help of antihypertensive therapy.

The following conditions have been reported to develop or worsen both during pregnancy and with combined oral contraceptives, but their association with combined oral contraceptives has not been proven: jaundice and/or pruritus associated with cholestasis; gallstone formation; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Sydenham’s chorea; herpes of pregnancy; hearing loss associated with otosclerosis. There are also cases of Crohn’s disease and ulcerative colitis associated with the use of combined oral contraceptives.

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

Although combined oral contraceptives may have an effect on insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetic patients using low-dose combined oral contraceptives (

Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to the sun and exposure to ultraviolet radiation.

Laboratory tests

The use of combined oral contraceptives may affect the results of certain laboratory tests, including liver, kidney, thyroid, and adrenal function, plasma transport protein levels, carbohydrate metabolism, and coagulation and fibrinolysis parameters. Changes usually do not exceed the limits of normal values.

Effects on the menstrual cycle

While taking combined oral contraceptives, irregular bleeding (spotting spotting or breakthrough bleeding) may occur, especially during the first months of use. Therefore, any irregular bleeding should only be evaluated after an adjustment period of approximately 3 cycles.

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

Some women may not develop withdrawal bleeding during a break from taking pills. If combined oral contraceptives were taken as directed, it is unlikely that the woman is pregnant. However, if previously combined oral contraceptives were taken on an irregular basis, or if there are no consecutive withdrawal bleeds, pregnancy should be excluded before continuing the drug.

Medical examinations

Before starting the use of Logest®, a woman is recommended to undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), to exclude pregnancy. In addition, violations of the blood coagulation system should be excluded.

In the case of long-term 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 such as Logest® do not protect against HIV infection (AIDS) and other sexually transmitted diseases!

The effect on the ability to drive a car and equipment was not revealed.

Form of production

Tablets

Storage conditions

In a dark place, at a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Gestodene, Ethinyl Estradiol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For women of childbearing age

Indications

Contraception