Gestodene is almost completely metabolized. Serum clearance of approximately 0.8 ml / min / kg. The content of gestodene in serum is subjected to a two-phase reduction. The half-life (T1 / 2) in anadrol results the terminal phase is about 12 h unmodified form gestodene is not displayed, but only in the form of metabolites (T1 / 2 – about 24 hours.) Which are excreted in the urine and bile in a ratio of about 6: 4. .
The equilibrium concentration. On the pharmacokinetics of gestodene influence SHBG levels in serum. As a result, the level of daily dosing substance in serum increased about four times during the second half of a treatment cycle.
Absorption. After oral administration, ethinylestradiol is rapidly and completely absorbed. Maximum serum concentration equal to approximately 65 pg / ml, achieved after 1.7 hours. During the suction and the first passage through the liver is metabolized ethinylestradiol, whereby its oral bioavailability averages about 45%.
Distribution. Ethinyl estradiol is almost full (about 98%), while non-specifically binds to albumin. Ethinyl estradiol induces the synthesis of SHBG. The apparent volume of distribution of ethinylestradiol is 2.8 -8.6 l / kg.
Metabolism. Ethinylestradiol undergoes conjugation presistemna as mucosa of the small intestine and in the liver. The main route of metabolism of aromatics hydroxylation. The rate of plasma clearance of 2.3 – 7 ml / min / kg.
. Withdrawal A decrease in serum concentrations of ethinyl estradiol is biphasic; The first phase is characterized by a half-life of about 1 hour, the second – 10-20 hours. In an unmodified form of the organism is not displayed. Ethinylestradiol metabolites are excreted in the urine and bile in a ratio of 4: 6 with a half-life of about 24 hours.
The equilibrium concentration. The equilibrium concentration is achieved in about one week.
Contraindications Logest should not be applied if any of the conditions listed below. If any of these conditions develop for the first time in patients receiving the drug should be immediately repealed.
- Thrombosis (venous and arterial) and thromboembolism present or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular accident).
- Conditions prior thrombosis (including transient ischemic attack, angina pectoris) now or in history.
- Migraine with focal neurological symptoms (including history).
- Diabetes mellitus with vascular complications.
- Multiple or severe venous or arterial thrombosis risk factors, including valvular lesions, heart rhythm disturbances, cerebrovascular disease, or coronary arteries; uncontrolled hypertension.
- Pancreatitis with severe hypertriglyceridemia now or in history.
- Liver failure and severe liver disease (as long as liver function tests have not come back to normal).
- Liver tumors (benign or malignant) now or in history.
- Identified hormone malignancies (including genital or mammary glands) or are suspected.
- Vaginal bleeding of unknown origin.
- Pregnancy or suspected it.
- The period of lactation.
- Hypersensitivity to any component of the drug Logest
- Prolonged immobilisation, major surgery, surgery on the legs, extensive trauma.
Application with caution:
– The expressed disturbances of lipid metabolism (obesity, hyperlipidemia); – superficial vein thrombophlebitis, – otosclerosis with hearing impairment during the previous pregnancy – idiopathic jaundice or pruritus during a previous pregnancy; – migraine with aura; – congenital hyperbilirubinemia (Gilbert syndrome, Dubina- Johnson and Rotor); – diabetes; – systemic lupus erythematosus – hemolytic uremic syndrome – Crohn’s disease; – sickle-cell anemia; – hypertension.
Pregnancy and lactation Logest not appointed during pregnancy and lactation.
If pregnancy is detected during the reception Logest the drug, the drug is immediately canceled. However, extensive epidemiological studies have revealed no increased risk of defects in children born to women treated with hormones prior to pregnancy or teratogenic effects when sex hormones were taken inadvertently in early pregnancy.
Admission combined oral contraceptives can reduce the amount of breast milk and change its composition, so their use is contraindicated during lactation. Small amounts of sex steroids and / or their metabolites may be excreted in milk, but there is no confirmation of their negative impact on the health of the newborn.
Dosing and Administration Drops should be taken orally in the order indicated on the package, every day at about the same time, with a little water. Take one tablet a day continuously for 21 days. Receiving the next pack is started after a 7-day break in taking pills, during which usually occurs withdrawal bleeding. Bleeding usually begins 2-3 days after the last pellet and can not end before receiving a new package.
How to start taking Logest
- Without taking any hormonal contraceptive use in the preceding month.
Admission Logest begins on the first day of the menstrual cycle (ie the first day of menstrual bleeding). Shall start receiving 2-5 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 tablet-taking from the first package.
- When switching from other combined oral contraceptives.
Preferably begin receiving Logest the next day after the last active pellets from the previous package, but in any case no later than the next day after the usual 7 day interval (for formulations comprising 21 pills) or after the last inactive pills (for preparations containing 28 pills in the package).
- When switching from contraceptives containing only progestin ( “mini-pill”, an injectable form, implant) or from a progestogen-releasing intrauterine device (Mirena).
A woman can go to the mini-pill Logest on any day (without a break), with the implant or intrauterine device with progestin – the date of its removal from the injection mold – the day when the next injection should have to be made. In all cases, you must use an additional barrier method of contraception during the first 7 days of tablet-taking.
- After an abortion in the first trimester of pregnancy.
The woman may start taking the drug immediately. Subject to this condition the woman does not need additional contraceptive protection.
- After delivery or abortion in the second trimester of pregnancy.
It is recommended to start taking the drug on day 21-28 after delivery or abortion in the second trimester of pregnancy. If the reception is started later, you must use an additional barrier method of contraception during the first 7 days of tablet-taking. However, if a woman has been sexually active, before you start taking Logest pregnancy should be excluded or must wait for the first menstrual period.
Receiving Missed Pills If the delay in receiving the drug was less than 12 hours, contraceptive protection is not reduced. The woman should take pills as soon as possible, should be taken at the usual time.
If the delay in taking pills made more than 12 hours, contraceptive protection may be reduced. It is possible to be guided by the following two basic rules:
- The drug should never be interrupted for more than 7 days.
- 7 days continuous administration of pills required to achieve adequate suppression of the hypothalamic-pituitary-ovarian regulation.
Accordingly, these tips may be given if the delay in receiving a dragee was 12 hours (the interval since last receiving pellets over 36 hours):
- The first week of taking the drug
The woman should take the last missed pills as soon as possible, as soon as you remember (even if this means taking two pills at once). Next take the pills at the usual time. Additionally, it should be used a barrier method of contraception (such as a condom) for the next 7 days. If intercourse took place during the week before skipping pills, you need to take into account the chance of pregnancy.
The more pills missed and the closer they are to a break in the reception of active substances, the greater the likelihood of pregnancy.
- The second week of taking the drug
The woman should take the last missed pills as soon as possible, as soon as you remember (even if this means taking two pills at once). Next take the pills at the usual time.
Provided that the woman has taken pills correctly in the 7 days preceding the first missed pills, there is no need to use additional contraceptive measures. Otherwise, as well as skipping anadrol results of two or more must be added dragees barrier methods (such as condoms) for 7 days.
- The third week of taking the drugThe risk of reduced reliability is imminent because of the forthcoming break in taking pills.
A woman should strictly adhere to one of the two following options. While in the 7 days preceding the first missed pills, all the pills are taken correctly, there is no need to use additional contraceptive methods.
1. The woman should take the last missed pills as soon as possible, as soon as you remember (even if this means taking two pills at once). Next take the pills at the usual time until the end of the current package of pills. The next pack should be started immediately. Withdrawal bleeding is unlikely until the end of the second pack, but may experience spotting and breakthrough bleeding during the tablet-taking. 2. A woman can also interrupt the reception of pills from the current package. Then she should take a break for 7 days, including the day of skipping pills, and then start taking a new package.
If a woman misses pills, and then during a break in taking pills she had no withdrawal bleeding, pregnancy must be excluded.
Recommendations in case of vomiting and diarrhea If a woman has had vomiting or diarrhea within 4 hours after taking the active pills, absorption may not be complete and should be additional contraceptive measures are taken. In these cases, you should be guided by the recommendations by skipping pills.
Changing the date of the beginning of the menstrual cycle In order to delay the onset of menstruation, the woman should continue taking pills from a new package Logest immediately after taking all the pills from the previous one, without a break in the reception.Drops of this new packaging may be taken for as long as the woman wants (as long as the packaging is not finished). Against the background of the drug from the second package, women may experience spotting or breakthrough uterine bleeding. Resume Logest reception from a new package follows the usual 7-day break.
In order to move the first day of menstruation to another day of the week, the woman should be advised to shorten the next break in taking pills for as many days, as much as she wants. The shorter the interval, the higher the risk that she will not have withdrawal bleeding, and in the future, will be spotting and breakthrough bleeding while taking second pack (just as when she wanted to delay the onset of menstruation.
Side effects: Soreness and tension of the mammary glands, breast enlargement, discharge from the breast; spotting and breakthrough uterine bleeding; headache; migraine; changes in libido; reduction / mood changes;poor tolerance of contact lenses; blurred vision; nausea; vomiting; stomach ache; changes in vaginal secretion; skin rash; erythema nodosum; erythema multiforme; generalized itching; cholestatic jaundice;fluid retention; change in body weight; allergic reactions. Rarely – increased fatigue, diarrhea.
Sometimes it can develop chloasma, especially in women with a history of chloasma during pregnancy.
As when taking other combined oral contraceptives in rare cases may develop thrombosis and thromboembolism.
Overdose Symptoms that may occur in overdose:. Nausea, vomiting, spotting or metrorrhagia no specific antidote, symptomatic treatment should be conducted.
The interaction with other drugs Sulfonamide derivatives, pyrazolone can enhance metabolism included in the preparation of steroid hormones.
Long-term treatment with drugs that induce liver enzymes, resulting in increased clearance of sex hormones can lead to breakthrough bleeding and / or reduce the contraceptive efficacy of the drug Logest.
These medicines include: phenytoin, barbiturates, primidone, carbamazepine and rifampicin; also there are suggestions with regard to oxcarbazepine, topiramate, felbamate, ritonavir and griseofulvin and products containing St. John’s wort.
The contraceptive protection is reduced when taking antibiotics (such as ampicillin and tetracycline), since, according to some sources, some antibiotics may reduce intrahepatic circulating estrogen, thereby reducing the concentration of ethinyl estradiol.
Combination oral contraceptives may affect the metabolism of other drugs (including Cyclosporine), which leads to a change in their concentration in the plasma and tissues.
When receiving estrogen-progestin drugs may require correction dosing regimen hypoglycemic agents and anticoagulants.
Specific guidance in the case of the planned operation should stop taking the drug for at least 4 weeks before it and not to renew the appointment within 2 weeks after the immobilization.
During reception drugs affecting microsomal enzymes and for 28 days after their removal should additionally use a barrier method of contraception.
During reception of antibiotics (such as ampicillin and tetracycline) and for 7 days after their removal should additionally use a barrier method of contraception.
If the period of use of barrier methods of protection ends later than Bean in a package, you need to go to the next package Logest without the usual break in receiving pills.
If any of the conditions / risk factors mentioned below are currently available, you should carefully weigh the potential risks and expected benefits of treatment Logest in each individual case and discussed with the woman before she decides to start taking the drug. In the case of aggravation, or amplification of the first manifestations of any of these conditions or risk factors, the woman should consult with your doctor, who can decide whether to cancel the drug.
- Diseases of the cardiovascular system
There is evidence of increasing incidence of venous and arterial thrombosis and thromboembolism while taking combined oral contraceptives.
However, the incidence of venous thromboembolism (VTE), developing while taking combined oral contraceptives, is less than the rate associated with pregnancy (6 per 10 000 pregnant women per year).
In women taking combined oral contraceptives are described in extremely rare cases, thrombosis of other blood vessels, eg, hepatic, mesenteric, renal arteries and veins, central retinal vein and its branches.Communication with the reception of combined oral contraceptives has not been proved.
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 irradiation in the left arm; sudden shortness of breath; sudden attack of coughing; any unusual, severe, prolonged headache; sudden partial or complete loss of vision; diplopia; slurred speech or aphasia; dizziness; loss of consciousness and / or without convulsive seizure; weakness or very marked numbness suddenly appeared on one side or in one part of the body; motor disturbances; symptoms of “acute abdomen”. The risk of thrombosis (venous and / or arterial) and thromboembolism is increased: -c age y smoking (with the number of cigarettes or increasing age the risk further increases, especially in women over 35 years old);
in the presence of:
– Family history (ie 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 assessed and the appropriate specialist to solve the question of the possibility of COC; – obesity (body mass index over 30 kg / m 2 ); – dislipoproteinemia; – hypertension; – migraine, – disease of the heart valves; – atrial fibrillation; – prolonged immobilization, major surgery, any surgery to the legs, or major trauma. In these situations, it is desirable to discontinue the use of combined oral contraceptive (in case the intended operation of at least four weeks prior to it) and not to resume reception within two weeks after the immobilization.
It is necessary to take into account the increased risk of thromboembolism during the postpartum period. Circulatory disorders also may occur in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn’s disease or ulcerative colitis) and sickle cell anemia.
Increased frequency and severity of migraine during use of combined oral contraceptives (which may be preceded by a cerebrovascular accident) may be a reason for immediate discontinuation of these drugs.
Biochemical parameters which can be indicative of hereditary or acquired predisposition to venous or arterial thrombosis include resistance to activated protein C, hyperhomocysteinemia, deficiency of antithrombin-III, deficiency of protein C, protein deficit S, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).
There have been reports of an increased risk of cervical cancer in long-term use of combined oral contraceptives. His connection with the intake of combined oral contraceptives has not been proved.Contradictions persist as to the extent to which these findings relate to the characteristics of sexual behavior and other factors such as human papilloma virus (HPV).
It was also found that there is a slightly increased relative risk of developing breast cancer diagnosed in women who used combined oral contraceptives. His connection with the intake of combined oral contraceptives has not been proved. The observed increase in 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 was observed the development of liver tumors. In case of severe pain in the abdomen, liver enlargement or signs of intra-abdominal bleeding it should be considered in the differential diagnosis.
- other conditions
Women with hypertriglyceridemia (or in the presence of the state in family history) may increase the risk of developing pancreatitis while taking oxymetholone 50 combined oral contraceptives.
Although a slight increase in blood pressure have been reported in many women taking COCs, clinically relevant increases were rare. However, if while taking combined oral contraceptives develops persistent, clinically significant increase in blood pressure, should be discontinued these drugs and begin treatment of hypertension. Receiving COCs can be continued, if using antihypertensive anadrol results therapy achieved normal blood pressure values.
The following conditions have been reported to develop or worsen both during pregnancy and when taking combined oral contraceptives, but their relationship with the intake of combined oral contraceptives has not been proven: jaundice and / or pruritus related to cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; chorea; herpes gestationis; hearing loss associated with otosclerosis. cases of Crohn’s disease are also described and ulcerative colitis background on the use of combined oral contraceptives.
Acute or chronic disturbances of liver function may require the elimination of the use of combined oral contraceptives, as long as liver function tests have not returned to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous use of sex hormones, requires discontinuation of COCs.
Although COCs may have an effect on insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetics using low-dose COCs (<0.05 mg ethinylestradiol). However, women with diabetes should be carefully monitored during the reception of combined oral contraceptives.
Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to sunlight and ultraviolet radiation.
Laboratory tests using combined oral contraceptives can affect the results of certain lab tests, including liver function, kidney, thyroid, adrenal, levels of transport proteins in the plasma, carbohydrate metabolism, coagulation and fibrinolysis parameters. Changes do not usually go beyond the normal range.
The effect on the menstrual cycle While taking combined oral contraceptives may experience irregular bleeding (spotting or breakthrough bleeding), especially during the first months of use. Therefore, the evaluation of any irregular bleeding should be done only after a period of adaptation of approximately three cycles.
If irregular bleeding recur or develop after previous regular cycles, you should conduct a thorough examination to exclude malignancy or pregnancy.
In some women, during a break in taking pills may not develop withdrawal bleeding. If combined oral contraceptives are taken according to directions, it is unlikely that the woman is pregnant. Nevertheless, if before that combined oral contraceptives are taken irregularly or if there are no two consecutive withdrawal bleeding, to continue receiving the drug should be excluded pregnancy.
Medical examinations recommended to undergo a thorough general medical and gynecological examination before the beginning of the use of the drug Logest woman (including the study of mammary glands and cytological examination of cervical mucus), exclude pregnancy. In addition, to exclude blood coagulation disorders.
In the case of long-term use of the drug must be at least 1 times a year to conduct follow-up examinations.
It should warn the woman that type Logest medications do not protect against HIV infection (AIDS) and other sexually transmitted diseases through!