Logest, 75 mcg+20 mcg 21 pcs

LOGEST is contraceptive.

Pharmacokinetics

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

After HSPH induction, the HSPH-bound fraction increases to 80%, the free and albumin-bound fraction decreases. Gestoden is almost completely metabolized. Metabolic clearance rate is 0.8 ml/min/kg. There is a biphasic decrease in serum concentration, T1/2 in the terminal phase is about 12 hours. In unchanged form gestoden is not excreted, but only as metabolites (T1/2 – approximately 24 hours), which are excreted with urine and bile at a ratio of approximately 6:4.

Ethinylestradiol.

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. Absolute bioavailability averages 45% due to the “first pass” effect through the liver. Cmax in blood serum (65 pg/ml) is reached after 1.7 h. Non-specific binding to serum albumin (approximately 98%), about 2% is free in plasma. Apparent volume of distribution is 2.8-8.6 l/kg. It is subjected to presystemic conjugation both in small intestine mucosa and in liver. The main way of metabolism is aromatic hydroxylation.

The metabolic clearance rate from blood plasma is 2.3-7 ml/min/kg. There is a biphasic decrease in serum levels: T1/2 is about 1 h and 10-20 h respectively. It is not excreted from the body unchanged. It is excreted as metabolites in the urine and bile at a ratio of 4:6 with a T1/2 of about 24 hours.

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

Indications

Active ingredient

Composition

Active substances:

Hestoden 0.075 mg,

ethinylestradiol 0.02 mg,

Associates:

Lactose monohydrate, 37.155 mg;

Corn starch, 15.5 mg;

Povidone 25000 – 1.7 mg;

Magnesium stearate – 0.55 mg,

Shell:

saccharose, 19.66 mg; povidone 700000, 0.171 mg; macrogol 6000, 2.18 mg; calcium carbonate – 8.697 mg; talcum powder – 4.242 mg; mountain glycol wax – 0.05 mg

How to take, the dosage

To be taken by mouth, with a small amount of water, daily at approximately the same time of the day, in the order indicated on the package. Take 1 tablet a day, continuously for 21 days. Taking the next package begins after a 7-day break in the intake of pills, during which there is usually a bleeding withdrawal. Bleeding usually begins 2 to 3 days after taking the last pill and may not end until the start of the new pack.

Logest® is started:

If you have not taken any hormonal contraceptives in the previous month. Taking Logest® starts on the first day of the menstrual cycle (i.e. the first day of menstrual bleeding). It is allowed to start taking Logest® on day 2-5 of menstrual cycle, but in this case it is recommended to use an additional barrier method of contraception during the first 7 days of taking the pills from the first package;

– when changing from other combined oral contraceptives, vaginal ring or contraceptive patch. It is preferable to start Logesta® the day after taking the last hormone-containing pill from the previous package, but in no case later than the day after the usual 7-day break (for products containing 21 tablets) or after taking the last inactive pill (for products containing 28 tablets in the package). The use of Logest® should be started on the day of removal of the vaginal ring or patch, but not later than the day on which a new ring or a new patch is to be inserted;

– when changing from contraceptives containing only gestagens (mini-pills, injectable forms, implant) or from a gestagen-releasing intrauterine contraceptive (Mirena). A woman may change from a mini-pill to Logest® on any day (without a break), from an implant or intrauterine contraceptive with gestagen – 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 the 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 that the drug be started on day 21-28 after childbirth (if the woman is not breastfeeding) or in the second trimester of pregnancy. If you start taking the drug later, you should additionally use a barrier method of contraception during the first 7 days of taking the pills. If a woman has already been sexually active, pregnancy must be excluded before taking Logest® or her first menstrual period must be awaited.

Taking missed pills. If the delay in taking the drug is less than 12 hours, 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 pills are taken more than 12 hours late, contraceptive protection may be reduced. The following two basic rules can guide you in this process:

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

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

If the delay in taking the pills is more than 12 hours (the interval since the last pill was taken is more than 36 hours), the following advice may be given.

The first week of taking the medication

The woman should take the last missed pill as soon as possible (even if that means taking two pills at once). The next pill is taken at the usual time. In addition, a barrier method of contraception (such as a condom) must be used for the next 7 days. If sexual intercourse took place during the week before skipping the pill, it is necessary to consider the possibility of pregnancy.

The second week of taking the drug

The woman should take the last missed pill as soon as possible (even if that means taking two pills at once). The next pill is taken at the usual time. Provided the woman has taken the pills correctly in the 7 days preceding the first missed pill, no additional contraceptive measures are necessary. Otherwise, and if two or more pills are missed, additional barrier methods of contraception (e.g., a condom) should be used for 7 days.

The third week of taking the drug

The risk of decreased reliability is inevitable because of the impending interruption of the pills. A woman should strictly stick to one of the following two options (if all pills were taken correctly in the 7 days preceding the first missed pill, no additional contraceptive methods are necessary):

1. The woman should take the last missed pill as soon as possible (even if this means taking two pills at once). The next pill is taken at the usual time until the pills from the current package are finished. The next package should be started immediately. Bleeding cancellation is unlikely until the second package is finished, but there may be a bleeding disorder or breakthrough bleeding while taking the pills.

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

If a woman misses taking the pill and then has no bleeding cancellation during the break in taking the pill, pregnancy must be ruled out.

Recommendations for vomiting and diarrhea

If a woman has had vomiting or diarrhea within 4 h of taking the active pills, absorption may be incomplete and additional contraceptive measures must be taken. In these cases, the recommendations for skipping the pills should be followed.

Changing the day menstrual bleeding starts

In order to delay the onset of menstruation, a woman should continue taking pills from a new package of Logesta® immediately after taking all pills from the previous package, without interruption. The pills from this new package may be taken as long as the woman wishes (until the package ends). While taking the pills from the second package, a woman may experience menses or breakthrough uterine bleeding. Logesta® from a new pack should be resumed after the usual 7-day break.

In order to move the start day of menstrual bleeding to another day of the week, a woman should be advised to shorten her immediate break from taking the pills by as many days as she wants. The shorter the interval, the greater the risk that she won’t have a bleeding withdrawal and will subsequently have masticatory discharge and breakthrough bleeding while taking her second pack (just as she would if she wanted to delay the start of her period).

Further information for specific groups of patients

Patients who are elderly. Not applicable. Logest® is not indicated after the onset of menopause.

Patients with liver dysfunction. 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 a dosing regimen adjustment in these patients.

Interaction

Sulfonamides and pyrazolone derivatives can increase the metabolism of the steroid hormones in the drug.

Long-term treatment with drugs that induce liver enzymes, as a result of which the clearance of sex hormones increases, may lead to breakthrough bleeding and/or decrease the contraceptive effectiveness of the drug 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 some evidence suggests they may reduce intrahepatic circulation of estrogen, thereby lowering ethinyl estradiol concentrations.

The oral combination contraceptives can affect the metabolism of other drugs (including cyclosporine), resulting in changes in their plasma and tissue concentrations.

The dosing regimen of hypoglycemic drugs and indirect anticoagulants may need to be adjusted when taking estrogen-gestagen drugs.

Special Instructions

If surgery is planned, it is recommended to discontinue the drug at least 4 weeks prior to surgery and not to resume for 2 weeks after the end of immobilization.

When taking drugs that affect microsomal enzymes and for 28 days after their withdrawal, an additional barrier method of contraception should be used.

When taking antibiotics such as ampicillins and tetracyclines and for 7 days after their withdrawal, an additional barrier method of contraception should be used.

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

If any of the conditions/risk factors listed below are present, the potential risks and expected benefits of Logesta® treatment should be carefully weighed on a case-by-case basis and discussed with the woman before she decides to start the drug. If any of these conditions or risk factors worsen, intensify, or first appear, the woman should consult her physician, who may decide if the drug should be discontinued.

Cardiovascular disease

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

However, the incidence of venous thromboembolism developing while taking combined oral contraceptives is lower than the incidence 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 hepatic, mesenteric, renal arteries and veins, central retinal vein and its branches, have been described. An association with the intake of combined oral contraceptives has not been proven.

The woman should stop taking the drug and consult a physician if she develops symptoms of venous or arterial thrombosis or cerebrovascular disorders, which may include: unilateral leg pain and/or swelling; sudden severe chest pain with or without irrigation to the left arm; sudden shortness of breath; sudden cough attack; any unusual, severe, prolonged headache; sudden partial or complete loss of vision; diplopia unintelligible speech or aphasia; dizziness; loss of consciousness with or without a seizure; weakness or very significant loss of sensation, suddenly on one side or in one part of the body; motor disturbances; “acute abdominal symptoms.

The risk of thrombosis (venous and/or arterial) and thromboembolism increases:
– with age;
– in smokers (with more cigarettes or increased age the risk further increases, especially in women over 35);
if there is:
– a family history (ie.е. venous or arterial thromboembolism ever in close relatives or parents at a relatively young age); in case of hereditary predisposition, the woman should be examined by an appropriate specialist to decide on the possibility of taking combined oral contraceptives;
– obesity (body mass index over 30 kg/m2);
– dyslipoproteinemia;
– arterial hypertension;
– migraine;
– 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 (if surgery is planned, at least 4 weeks before it) and not to resume taking them for 2 weeks after the end of immobilization.

The increased risk of thromboembolism in the postpartum period should be considered.

Circulatory disorders may also be noted in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn’s disease or nonspecific ulcerative colitis) and sickle cell anemia.

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

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

Tumors

There have been reports of an increased risk of cervical cancer with persistent papillomavirus infection. Its association with taking combined oral contraceptives has not been proven. There remains controversy about the extent to which these findings relate to patterns of sexual behavior and use of barrier contraception.

It has also been found that there is a slightly increased relative risk of breast cancer diagnosed in women who have used combined oral contraceptives. Its connection with the use of combined oral contraceptives has not been proved. The observed increase in risk may be a consequence of earlier diagnosis of breast cancer in women who used combined oral contraceptives.

In rare cases, the development of liver tumors has been observed during the use of combined oral contraceptives. Severe abdominal pain or signs of intra-abdominal bleeding or enlargement of the liver should be considered in making a differential diagnosis.

Other conditions

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

While small increases in BP have been described in many women taking combined oral contraceptives, clinically significant increases have rarely been reported. However, if a persistent, clinically significant increase in BP develops while taking combined oral contraceptives, the medications should be stopped and treatment for arterial hypertension should be initiated. The combined oral contraceptives may be continued if normal BP is achieved with hypotensive therapy.

The following conditions have been reported to develop or worsen both during pregnancy and while taking combined oral contraceptives, but their association with taking 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. Cases of Crohn’s disease and nonspecific ulcerative colitis have also been described with combined oral contraceptives.

Acute or chronic liver dysfunction may require discontinuation of combined oral contraceptives until liver function returns 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.

While combined oral contraceptives may affect insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetic patients using low-dose combined oral contraceptives (/p>

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

Laboratory tests

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

The effect on the menstrual cycle

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

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

Some women may not develop withdrawal bleeding during a break in the drags. If the combined oral contraceptives have been taken as directed, it is unlikely that the woman is pregnant. However, if the combined oral contraceptives have been taken irregularly before, or if there are no consecutive 2 bleeding withdrawals, pregnancy must be ruled out before continuing the medication.

Medical examinations

Before starting Logest® therapy, a woman is recommended to undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), to rule out pregnancy. In addition, disorders of the blood clotting system should be excluded.

In case of long-term use, follow-up examinations should be carried out, the frequency of which depends on the individual characteristics of the woman.

Warn women that Logest® products do not protect against HIV infection (AIDS) or other sexually transmitted diseases!

The effect on the ability to drive or operate machinery has not been identified.

Contraindications

Side effects

In rare cases, there may be breast soreness and tightness, breast enlargement, mammary discharge, oozing and breakthrough uterine bleeding, headache, migraine, change in libido, decrease/change in mood, poor tolerance of contact lenses, visual disturbances, nausea, vomiting, abdominal pain, changes in vaginal secretion, skin rash, erythema nodosa, erythema multiforme, generalized pruritus, cholestatic jaundice, fluid retention, weight changes, allergic reactions; rarely – increased fatigue, diarrhea; sometimes – chloasma, especially in women with a history of pregnancy chloasma.

As with other combined oral contraceptives in rare cases, the development of thrombosis and thromboembolism is possible.

Overdose

Symptoms: nausea, vomiting, oozing or metrorrhagia.

Treatment: symptomatic. There is no specific antidote.

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