Novinet

General characteristics. Structure:

Active agents: ethinylestradiol - 0.020 mg, dezogestret - 0,150 mg.

Excipients: dye quinolinic yellow E 104, α-tocopherol, magnesium stearate, silicon dioxide colloid, stearic acid, povidone, potato starch, lactoses monohydrate;
Film cover: propylene glycol, macrogoal 6000, gipromelloza.

Pharmacological properties:

Pharmacodynamics. Новинет® is the combined peroral contraceptive drug which main contraceptive effect consists in inhibition of synthesis of gonadotrophins and suppression of an ovulation. Besides, due to increase in viscosity of cervical slime the movement of spermatozoa via the cervical channel is slowed down, and change of a condition of an endometria interferes with implantation of an oospore. Ethinylestradiol is a synthetic analog of endogenous oestradiol, dezogestret possesses the expressed gestagenny and anti-oestrogenic action, similar to endogenous progesterone, weak androgenic and anabolic activity. Новинет® makes favorable impact on lipidic exchange: increases concentration of lipoproteins of the high density (LPVP) in a blood plasma, without influencing at the same time the maintenance of lipoproteins of the low density (LPNP). Against the background of use of drug considerable reduction of amount of monthly lost blood (is noted at an initial menorrhagia), the menstrual cycle is normalized, favorable impact on skin is noted (especially in the presence of vulgar eels).

Pharmacokinetics. Dezogestrel. Absorption.
At oral administration dezogestret it is soaked up from the digestive tract (DT) quickly and almost completely. It is metabolized in 3-keto-dezogestrel which is biologically active metabolite of a dezogestrel. Average maximum concentration in blood serum (Cmax) of 2 ng/ml, is reached in 1,5 hours (Tmax) after reception of a tablet. Bioavailability of drug makes 62-81%. Distribution in an organism 3-keto-dezogestrel contacts proteins of a blood plasma, generally albumine and the globulin, connecting sex hormones (G,CSH). The volume of distribution makes 1,5 l/kg.

Metabolism. Except 3-keto-dezogestrela which is formed in a liver and in an intestines wall other metabolites are formed: Зα-ОН-дезогестрел, Зβ-ОН-дезогестрел, Зα-ОН-5α-Н-дезогестрел (metabolites of the first phase). They have no pharmacological activity, and partially, by conjugation (the second phase of a metabolization), turn into polar metabolites (sulfates and glyukuronata). Clearance from a blood plasma about 2 ml/min. on 1 kg of body weight.

Removal from an organism. The average time of semi-removal 3-keto-dezogestrela makes 30 hours. Metabolites are removed by kidneys and through intestines (in the ratio 4:6).
Stable concentration is established to the second half of a cycle. At this time the level of a ketogestrel increases by 2-3 times.

Этинилэстрадиол.Всасывание.Этинилэстрадиол it is soaked up from a GIT quickly and completely. Average maximum concentration in blood serum (Cmax) makes 80 pg/ml - in 1-2 hours (Tmax) after reception of a tablet. Bioavailability because of presistemny conjugation and effect of the first passing - about 60%.
Distribution in an organism
Ethinylestradiol completely contacts proteins of a blood plasma, generally albumine. The volume of distribution makes 5 l/kg.

Metabolism. Presistemny conjugation of ethinylestradiol is considerable. Passing an intestines wall, (the first phase of metabolism) it is exposed to conjugation in a liver (the second phase of metabolism). Ethinylestradiol and its conjugates of the first phase of metabolism (sulfates and glucuronides) are emitted in bile and enter enterogepatichesky circulation.
Clearance from a blood plasma about 5 ml/min. on 1 kg of body weight.
Allocation from an organism
The average time of semi-removal of ethinylestradiol makes about 24 hours. About 40% are removed by kidneys and about 60% through intestines.
Stable concentration is established by 3-4 day, at the same time ethinylestradiol level in blood serum is 30-40% higher, than after a single dose.

Indications to use:

Contraception.

Route of administration and doses:

Inside. Reception of tablets is begun from the first day of a menstrual cycle and accepted on 1 tablet a day within 21 days, whenever possible at the same time days.
After reception of the last tablet do a 7-day break during which there is menstrualnopodobny bleeding owing to drug withdrawal of packaging.
Next day after a 7-day break (in four weeks after reception of the first tablet, on the same day weeks) resume administration of drug from the following packaging which is also containing 21 tablets even if bleeding did not stop. Adhere to such scheme of reception of tablets until there is a need for contraception. At observance of Regulations of Admission, the contraceptive effect remains also for the period of a 7-day break.

First administration of drug
Reception of the first tablet should be begun from the first day of a menstrual cycle. In this case it is not required to use additional methods of contraception.
Reception of tablets it is possible to begin and from 2-5 in the afternoon periods, but in this case in the first cycle of use of drug it is necessary to apply additional methods of contraception in the first 7 days of reception of tablets.
If there passed more than 5 days after the beginning of periods, it is necessary to postpone the beginning of administration of drug until the following periods.

Administration of drug after the delivery
Not nursing women can begin reception of tablets not earlier than 21 days after the delivery, previously having consulted with the doctor. In this case there is no need for use of other methods of contraception.
If after the delivery there was already a sexual contact, then with reception of tablets it is necessary to wait to the first periods.
If the decision on administration of drug later, than in 21 days after the delivery is made, then in the first 7 days it is necessary to use additional methods of contraception.

Administration of drug after abortion
After abortion, in the absence of contraindications, it is necessary to begin reception of tablets from the first day, and in this case there is no need for use of additional methods of contraception.

Transition from other oral contraceptive
Administration of drug of Novinet® after use of other hormonal oral contraceptive of the ethinylestradiol containing 30 mkg, according to 21 day schemes:
The first pill Novinet® is recommended to be taken next day after end of a rate of the previous drug. It is not required to maintain a 7-day break or began to wait for periods. There is no need for use of additional methods of contraception.
Upon transition to Novinet® from the drug containing 28 tablets follows next day after tablets in packaging ended to begin new packaging of Novinet®.

Transition to Novinet® after use of the peroral hormonal drugs containing only progestogen (so-called "mini-pileas"):
The first pill Novinet® should be taken in the first day of a cycle. There is no need for use of additional methods of contraception.
If at reception mini-saw there are no periods, then after an exception of pregnancy it is possible to begin reception of Novinet® in any day of a cycle, but in this case in the first 7 days it is necessary to apply additional methods of contraception.
In the above cases as additional methods of contraception use of the following non-hormonal methods is recommended: use of a cervical cap with spermicidal gel, condom, or abstention from sexual contacts. Use of a calendar method in these cases is not recommended.

Delay of a menstrual cycle
If there is a need for a periods delay, it is necessary to continue reception of tablets from new packaging, without 7-day break, according to the usual scheme. At a delay of periods there can be breakthrough or smearing bleedings, but it does not reduce contraceptive effect of drug. Regular reception of Novinet® can be recovered after a usual 7-day break.

The passed tablets
If the woman forgot to take a pill timely, and after the admission there passed no more than 12 hours, it is necessary just to take the forgotten pill, and further to continue inclusion in usual time. If between reception of tablets there passed more than 12 hours - it is considered the admission of a tablet, reliability of contraception in this cycle is not guaranteed and recommended use of additional methods of contraception.
At the admission of one tablet on the first or second week of a cycle, it is necessary to take 2 pill in the next day and then to continue regular reception, using additional methods of contraception until the end of a cycle.
At the admission of a tablet on the third week of a cycle it is necessary to take the forgotten pill, to continue regular reception and not to do a 7-day break. It is important to remember that in connection with the minimum dose of estrogen the risk of an ovulation and/or bloody allocations at the admission of reception of a tablet increases and therefore use of additional methods of contraception is recommended.

What to do at vomiting or diarrhea?
If after administration of drug vomiting or diarrhea develops, then absorption of drug can be defective. If symptoms stopped within 12 hours, then it is necessary to take one more pill in addition. After that it is necessary to continue reception of tablets normally. If symptoms proceed more than 12 hours, then it is necessary to use additional methods of contraception during vomiting or diarrhea and in the next 7 days.

Features of use:

Before use of drug and in the subsequent the detailed family and personal anamnesis is recommended to collect each 6 months and to undergo all-medical and gynecologic examination (survey by the gynecologist, capture of a cytologic smear, a research of mammary glands and function of a liver, control of the arterial pressure (AP), concentration of cholesterol in blood, the analysis of urine). These researches need to be repeated periodically, due to the need of early detection of risk factors or the arisen contraindications.
Drug is well-tried contraceptive medicine: Perl's index (an indicator of number of the pregnancies which occurred during use of a method of contraception for 100 women during 1 year) at the correct use makes about 0:05.
In each case before purpose of hormonal contraceptives advantages or possible negative effects of their reception are individually estimated. This question needs to be discussed with the patient who after obtaining the necessary information will make the final decision on preference of hormonal or any other method of contraception. The state of health of the woman needs to be controlled carefully. If during administration of drug any of below the listed states/diseases appears or worsens, it is necessary to stop administration of drug and to pass to other, non-hormonal method of contraception:
- diseases of system of a hemostasis.
- the states / diseases contributing to development of a cardiovascular, renal failure.
- epilepsy
- migraine
- the risk of development is oestrogenic - a dependent tumor or is oestrogenic - dependent gynecologic diseases;
- the diabetes mellitus which is not complicated by vascular disorders;
- a heavy depression (if the depression is connected with tryptophane exchange disturbance, then for the purpose of correction it is possible to apply B6 vitamin);
- drepanocytic anemia as in some cases (for example, infections, a hypoxia) it is oestrogenic - the containing drugs at this pathology can provoke the thromboembolism phenomena.
- emergence of deviations in laboratory tests of assessment of function of a liver.

- Thromboembolic diseases
Epidemiological researches proved that there is a communication between reception of peroral hormonal contraceptives and increase in risk of arterial and venous thromboembolic diseases (including a myocardial infarction, a stroke, a deep vein thrombosis of the lower extremities, a thromboembolism of a pulmonary artery). The increased risk of venous thromboembolic diseases is proved, but it is much less, than at pregnancy (60 cases on 100 thousand pregnancies).
At use of peroral contraceptive drugs the arterial or venous thromboembolism of hepatic, mezenterialny, renal vessels or vessels of a retina is very seldom observed.
The risk of emergence of arterial or venous thromboembolic diseases increases:
- with age;
- when smoking (intensive smoking and age are more senior than 35 years treat risk factors);
- in the presence in the family anamnesis of thromboembolic diseases (for example, at parents, the brother or the sister). At suspicion on genetic predisposition, it is necessary to consult before use of drug with the specialist.
- at obesity (the index of body weight is higher than 30 kg/sq.m);
- at dislipoproteinemiya;
- at arterial hypertension;
- at diseases of the valves of heart complicated by hemodynamic disturbances
- at fibrillation of auricles;
- at the diabetes mellitus complicated by vascular defeats;
- at a long immobilization, after a big operative measure, after an operative measure on the lower extremities, after a severe injury.
In these cases temporary phase-out of drug is supposed: it is desirable to stop not later, than in 4 weeks prior to an operative measure, and to renew - not early, than in 2 weeks after a remobilization.
The risk of developing of venous thromboembolic diseases at women after the delivery increases.
Such diseases as diabetes mellitus, system lupus erythematosus, gemolitiko-an uraemic syndrome, a disease the Krone, nonspecific ulcer colitis, drepanocytic anemia, increase risk of development of venous thromboembolic diseases.
Such biochemical aberrations as resistance to the activated protein With, the giperkhromotsisteinemiya, deficit of proteins of C, S, deficit of antithrombin III, existence of anti-phospholipidic antibodies, increase risk of formation of arterial or venous thromboembolic diseases.
At ratio assessment the advantage / risk of administration of drug should be meant that purposeful treatment of this state reduces risk of formation of a thromboembolism. Signs of developing of a thrombembolia are:
- a sudden stethalgia which irradiates in the left hand,
- sudden asthma,
- any unusually severe headache proceeding long time or developing for the first time, especially at a combination to sudden total or partial loss of sight or a diplopia, aphasia, dizziness, a collapse, focal epilepsy), weakness or the expressed numbness of a half of a body, motive disturbances, severe unilateral pain in a gastrocnemius muscle, an acute abdomen).

Tumoral diseases
In some researches reported about increase of developing of cancer of neck of uterus at those women who long time accepted hormonal contraceptives, but results of researches are contradictory. In development of cancer of neck of uterus the sexual behavior, infection with a virus of papilloma of the person and other factors play a significant role.
The metaanalysis of 54 epidemiological researches showed that there is a relative increase in danger of cancer of mammary glands among the women accepting peroral hormonal contraceptives, however higher detectability of cancer of mammary glands could be connected with more regular medical examination. Cancer of mammary glands occurs seldom among women more young than 40 years irrespective of, they accept hormonal contraceptives or not, and increases with age. Reception of tablets can be regarded as one of many risk factors. Nevertheless, the woman has to be informed of a possibility of risk of development of cancer of mammary glands, proceeding from assessment of a ratio of advantage and risk (protection against cancer of an ovary and an endometria).
There are not numerous messages on development of a benign or malignant tumor of a liver in women, is long accepting hormonal contraceptives. It should be meant at differential diagnostic assessment of abdominal pains which can be connected with increase in the size of a liver or intra belly bleeding.
It is necessary to warn the woman that drug does not protect from HIV infection (AIDS) and other diseases, sexually transmitted.
Efficiency of drug can decrease at the following cases: the passed tablets, vomiting and diarrhea, simultaneous use of other drugs reducing efficiency of contraceptive tablets.
If the patient at the same time accepts other drug which can reduce efficiency of contraceptive tablets, it is necessary to apply additional methods of contraception.

Efficiency of drug can decrease if after several months of their use there are irregular, smearing or breakthrough bleedings, in such cases it is reasonable to continue reception of tablets before their termination in the following packaging. If at the end of the second cycle menstrualnopodobny bleeding does not begin or acyclic bloody allocations do not stop, to stop reception of tablets and to renew only it after a pregnancy exception.

Hloazma. Hloazma from time to time can occur at those women at whom they took place in the anamnesis during pregnancy. Those women who have a risk of emergence хлоазм should avoid contact with sunshine or ultraviolet during reception of tablets.

Changes of laboratory indicators
Under the influence of peroral contraceptive tablets - in connection with an oestrogenic component - the level of some laboratory parameters (functional indicators of a liver, kidneys, adrenal glands, a thyroid gland, hemostasis indicators, levels of lipoproteins and transport proteins) can change.
After an acute viral hepatitis it is necessary to accept after normalization of function of a liver (not earlier than in 6 months). At diarrhea or intestinal frustration, vomiting the contraceptive effect can decrease (without stopping administration of drug, it is necessary to use additional non-hormonal methods of contraception). The smoking women have the increased risk of development of vascular diseases with serious effects (a myocardial infarction, a stroke). The risk depends on age (especially at women 35 years are more senior) and on quantity of the smoked cigarettes. In the period of a lactation release of milk can decrease, in insignificant quantities components drug is emitted with breast milk.

INFLUENCE OF DRUG ON ABILITY TO DRIVE THE CAR AND WORKING MECHANISMS
Researches on studying of possible influence of drug on ability to drive the car or other mechanisms were not conducted.

Side effects:

Side effects at which emergence the immediate termination of administration of drug is necessary:
- arterial hypertension;
- gemolitiko-uraemic syndrome;
- porphyria;
- the hearing loss caused by an otosclerosis.
Seldom meeting: arterial and venous thromboembolisms (в.т.ч. myocardial infarction, stroke, deep vein thrombosis of the lower extremities, thromboembolism of a pulmonary artery); aggravation of a reactive system lupus erythematosus.
Very seldom meeting: arterial or venous thromboembolism of hepatic, mezenterialny, renal, retinal arteries and veins; the chorea of Sidenkhem (passing after drug withdrawal).

Other side effects, less heavy, but more often meeting. Expediency of continuation of use of drug is solved individually after consultation with the doctor, proceeding from a ratio advantage/risk.
- Reproductive system: acyclic bleedings / bloody allocations from a vagina, an amenorrhea after drug withdrawal, change of a condition of vulval slime, development of inflammatory processes of a vagina (e.g.: candidiasis).
- Mammary glands: tension, pain, increase in mammary glands, galactorrhoea.
- Digestive tract and gepato-biliary system: nausea, vomiting, a disease Krone, ulcer colitis, emergence or an exacerbation of jaundice and/or the itch connected with a cholestasia, a cholelithiasis.
- Skin: nodal / exudative erythema, rash, hloazma.
- Central nervous system: headache, migraine, changes of mood, depressions.
- Metabolic disturbances: a liquid delay in an organism, change (increase) of body weight, decrease in tolerance to carbohydrates.
- Eyes: increase in sensitivity of a cornea when carrying contact lenses.
- Other: allergic reactions.

Interaction with other medicines:

The medicines inducing liver enzymes, such as hydantoin, barbiturates, Primidonum, carbamazepine, rifampicin, окскарбазепин, топирамат, фелбамат the griseofulvin, HP containing a St. John's Wort ordinary reduce efficiency of oral contraceptives and increase risk of developing of bleedings of "break". The maximum level of induction is usually reached not earlier than 2-3 weeks, but can proceed to 4 weeks after drug withdrawal.
Ampicillin, tetracycline - reduce efficiency (the mechanism of interaction is not installed).
In need of joint reception, it is recommended to use an additional barrier method of contraception throughout all course of treatment and within 7 days (for rifampicin - within 28 days) after drug withdrawal.
Peroral contraceptives can reduce tolerance to carbohydrates, increase the need for insulin or peroral antidiabetic means.

Contraindications:

- pregnancy or suspicion on it;
- lactation;
- existence of heavy and/or multiple factors of risk of venous or arterial thrombosis (including arterial hypertension of average or heavy degree with the ABP 160/100 мм.рт.ст and more);
- thrombosis harbingers (including the tranzitorny ischemic attack, stenocardia), including in the anamnesis;
- migraine with focal neurologic symptomatology, including in the anamnesis;
- venous or arterial thrombosis / thromboembolism (including shin deep vein thrombosis, embolism of a pulmonary artery, myocardial infarction, stroke) now or anamnesis,
existence of a venous thromboembolism at relatives;
- a diabetes mellitus (with existence of an angiopatiya);
- the pancreatitis (including in the anamnesis) which is followed by the expressed gipertriglitseridemiya;
- dislipidemiya;
- a serious illness of a liver, cholestatic jaundice (including during pregnancy), hepatitis, including in the anamnesis (before normalization of functional and laboratory parameters and within three months after return of these indicators to norm);
- jaundice owing to reception of the HP containing steroids;
- zhelchekamenny disease now or anamnesis;
- Gilbert's syndrome, Cudgel Johnson, Rotor;
- liver tumors (including in the anamnesis);
- a severe itch, an otosclerosis or progressing of an otosclerosis during the previous pregnancy or at reception of glucocorticosteroids;
- hormonedependent malignant new growths of generative organs and mammary glands (including suspicion on them);
- vaginal bleeding of not clear etiology;
- smoking is aged more senior than 35 years (more than 15 cigarettes a day);
- individual hypersensitivity to drug or its components.

With care
The states increasing risk of development of venous or arterial thrombosis / thromboembolism: the age is more senior than 35 years, smoking, the family anamnesis, obesity (an index of body weight more than 30 kg / кв.м), a dislipoproteinemiya, arterial hypertension, migraine, epilepsy, valve heart diseases, fibrillation of an auricle, a long immobilization, extensive surgical intervention, surgical intervention on the lower extremities, a severe injury, a varicosity and superficial thrombophlebitis, the puerperal period, existence of a heavy depression, including in the anamnesis, changes of biochemical indicators (resistance of the activated protein With, a gipergomotsisteinemiya, deficit of antithrombin III, deficit of a protein of C or S, anti-phospholipidic antibodies, including antibodies to cardiolipin, lupoid anticoagulant).
The diabetes mellitus which is not complicated by vascular disorders, the system lupus erythematosus (SLE), a disease Krone, ulcer colitis, a sickemia; a gipertriglitseridemiya (including in the family anamnesis), acute and chronic diseases of a liver.

Pregnancy and period of a lactation
Use of drug during pregnancy and during feeding by a breast contraindicated.

Overdose:

Nausea, vomiting are possible, girls have bloody allocations from a vagina.
Drug has no specific antidote, a symptomatic treatment.
If symptoms of overdose arise in the first 2-3 hours after administration of drug, the gastric lavage is possible.

Storage conditions:

At a temperature of 15-30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated. 21 tablets in the blister (Al/PVH/PVDH). 1 or 3 blisters in a cardboard pack with the application instruction.