Novynette, pills, 21pcs

Composition

Active ingredients:

ethinyl estradiol-0.020 mg,

desogestrel-0.150 mg;

Auxiliary substances:

quinoline yellow dye E 104,

alpha-tocopherol,

magnesium stearate,

colloidal silicon dioxide,

stearic acid,

povidone, potato starch,

lactose monohydrate;

Film shell:

propylene glycol,

macrogol 6000,

hypromellose.

Pharmacological action

Pharmacodynamics

Novynette® is a combined oral contraceptive drug, the main contraceptive effect of which is to inhibit the synthesis of gonadotropins and suppress ovulation. In addition, by increasing the viscosity of the cervical mucus, the movement of spermatozoa through the cervical canal slows down, and a change in the state of the endometrium prevents the implantation of a fertilized egg.

Ethinyl Estradiol is a synthetic analog of endogenous estradiol, desogestrel has a pronounced progestogenic and anti-estrogenic effect, similar to endogenous progesterone, weak androgenic and anabolic activity. Novynette® has a beneficial effect on lipid metabolism: it increases the concentration of high-density lipoproteins (HDL) in blood plasma, without affecting the content of low-density lipoproteins (LDL).

Against the background of the use of the drug, there is a significant decrease in the amount of blood lost monthly (with initial menorrhagia), the menstrual cycle normalizes, and a favorable effect on the skin is noted (especially in the presence of vulgar acne).

Pharmacokinetics

Desogestrel

Suction

When taken orally, desogestrel is absorbed from the gastrointestinal tract (GI) quickly and almost completely. It is metabolized to 3-keto-desogestrel, which is a biologically active metabolite of desogestrel. The average maximum serum concentration (Cmax) of 2 ng / ml is reached 1.5 hours (Tmax) after taking the tablet. The bioavailability of the drug is 62-81%. Distribution in the body,3-keto-desogestrel binds to plasma proteins, mainly albumins and sex hormone binding globulin (SHBG). The volume of distribution is 1.5 l/kg.

Metabolism

In addition to 3-keto-desogestrel, which is formed in the liver and in the intestinal wall, other metabolites are formed: Z-OH-desogestrel, Zb-OH-desogestrel, Z-OH-5α-N-desogestrel (phase I metabolites). They have no pharmacological activity, and partially, by conjugation (the second phase of metabolism), are converted to polar metabolites (sulfates and glucuronates). Plasma clearance is about 2 ml / min per 1 kg of body weight.

Elimination from the body

The average elimination half-life of 3-keto-desogestrel is 30 hours. Metabolites are excreted by the kidneys and through the intestines (in a ratio of 4: 6). A stable concentration is established by the second half of the cycle. At this time, the level of ketogestrel increases 2-3 times. Ethinyl Estradiol

Suction

Ethinyl Estradiol is absorbed quickly and completely from the gastrointestinal tract. The average maximum serum concentration (Cmax) is 80 pg / ml-1-2 hours (Tmax) after taking the tablet. Bioavailability due to presystemic conjugation and the first pass effect is about 60%.

Distribution in the body

Ethinyl estradiol binds completely to plasma proteins, mainly albumins. The volume of distribution is 5 l / kg.

Metabolism

Presystemic conjugation of ethinyl estradiol is significant. Bypassing the intestinal wall (first phase of metabolism), it undergoes conjugation in the liver (second phase of metabolism). Ethinyl estradiol and its conjugates of the first phase of metabolism (sulfates and glucuronides) are released into the bile and enter the enterohepatic circulation.

Plasma clearance is about 5 ml / min per 1 kg of body weight.

Excretion from the body

The average elimination half-life of ethinyl estradiol is about 24 hours. About 40% is excreted by the kidneys and about 60% through the intestines. A stable concentration is established by 3-4 days, while the level of ethinyl estradiol in the blood serum is 30-40% higher than after a single dose.

Indications

Contraception.

Use during pregnancy and lactation

Novynette is contraindicated for use during pregnancy. Novynette is contraindicated for use during lactation (breastfeeding), as it suppresses lactation and affects the quality of milk. In addition, active substances are excreted in breast milk. Novynette should be discontinued 3 months before the planned pregnancy. In case of pregnancy, the drug should be discontinued. In the absence of menstrual-like bleeding, continuation of the intake is allowed only after the exclusion of pregnancy.

Contraindications

• pregnancy or suspicion of it;
• lactation;
• the presence of severe and/or multiple risk factors for venous or arterial thrombosis (including hypertension moderate or severe AD 160/100 mm Hg. St and more);
• the harbingers of thrombosis (including transient ischemic attack, angina), including in the anamnesis;
• migraine with focal neurological symptoms, including in the anamnesis;
• venous or arterial thrombosis/thromboembolism (including deep vein thrombosis of the leg, pulmonary embolism, myocardial infarction, stroke) in real time or history,
• the presence of venous thromboembolism in relatives;
• diabetes mellitus (with the presence of angiopathy);
• pancreatitis (including in history), accompanied by severe hypertriglyceridemia;
• dyslipidemia;
• severe liver disease, cholestatic jaundice (including during pregnancy), hepatitis, including history (up to the normalization of functional and laboratory parameters and within three months after the return of these parameters to normal);
• jaundice as a result of taking drugs that contain steroids;
• cholelithiasis in real time or history;
• Gilbert syndrome, Dubin-Johnson, Rotor;
• liver tumors (including in the anamnesis);
• severe itching, otosclerosis or progression of otosclerosis during a previous pregnancy or when taking steroids;
• hormone-dependent malignancies of the genital organs and mammary glands (including suspicion of them);
• vaginal bleeding of unknown etiology;
• the Smoking age 35 years (more than 15 cigarettes a day);
• individual hypersensitivity to the drug or its components.

With caution

Conditions that increase the risk of venous or arterial thrombosis/thromboembolism: age over 35 years, smoking, family history, obesity (body mass index greater than 30 kg/sq. m), dyslipoproteinemia, hypertension, migraine, epilepsy, valvular heart disease, atrial fibrillation, prolonged immobilization, extensive surgery, lower limb surgery, severe trauma, varicose veins, etc. superficial thrombophlebitis, postpartum period, presence of severe depression, including in the anamnesis, changes in biochemical parameters (activated protein C resistance, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant).

Diabetes mellitus not complicated by vascular disorders, systemic lupus erythematosus (SLE), Crohn’s disease, ulcerative colitis, sickle cell anemia; hypertriglyceridemia (including family history), acute and chronic liver diseases.

Side effects

Side effects that require discontinuation of the drug:

From the cardiovascular system: arterial hypertension; rarely-arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism); very rarely-arterial or venous thromboembolism of the hepatic, mesenteric, renal, retinal arteries and veins.

Sensory disorders: hearing loss due to otosclerosis.

Others: hemolytic-uremic syndrome, porphyria; rarely-exacerbation of reactive systemic lupus erythematosus; very rarely-Sydenham’s chorea (passing after drug withdrawal).

Other side effects (more common, but less severe). The expediency of continuing to use the drug is decided individually after consultation with a doctor, based on the benefit/risk ratio.

From the genital system: acyclic bleeding/spotting from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, development of inflammatory processes of the vagina, candidiasis, tension, pain, breast enlargement, galactorrhea.

From the digestive system: nausea, vomiting, Crohn’s disease, ulcerative colitis, occurrence or exacerbation of jaundice and / or itching associated with cholestasis, cholelithiasis.

Dermatological reactions: erythema nodosum, exudative erythema, rash, chloasma.

From the central nervous system: headache, migraine, mood lability, depression.

From the side of the organ of vision: increased sensitivity of the cornea (when wearing contact lenses).

From the side of metabolism: fluid retention in the body, changes (increase) in body weight, decreased tolerance to carbohydrates.

Other: allergic reactions.

Interaction

Drugs that induce liver enzymes, such as hydantoin, barbiturates, primidone, carbamazepine, rifampicin, oxcarbazepine, topiramate, felbamate, griseofulvin, St. John’s wort preparations reduce the effectiveness of oral contraceptives and increase the risk of breakthrough bleeding. The maximum level of induction is usually reached no earlier than 2-3 weeks, but can last up to 4 weeks after discontinuation of the drug.

Ampicillin and tetracycline reduce the effectiveness of Novynette (the mechanism of interaction has not been established). If co-use is necessary, it is recommended to use an additional barrier method of contraception throughout the entire course of treatment and for 7 days (for rifampicin – for 28 days) after discontinuation of the drug.

Oral contraceptives may reduce carbohydrate tolerance, increase the need for insulin, or increase the need for oral antidiabetic medications.

How to take, course of use and dosage

Inside. Taking tablets begins on the 1st day of the menstrual cycle and takes 1 tablet. per day for 21 days, if possible at the same time of day. After taking the last tablet from the package, a 7-day break is taken, during which menstrual-like bleeding occurs due to drug withdrawal. The next day after a 7-day break (4 weeks after taking the 1st tablet, on the same day of the week), the drug is resumed from the next package, also containing 21 tablets, even if the bleeding has not stopped. This scheme of taking pills is followed as long as there is a need for contraception. If the rules of reception are observed, the contraceptive effect remains even during the 7-day break.

1st drug intake

Reception of the 1st table should be started from the 1st day of the menstrual cycle. In this case, you do not need to use additional methods of contraception. Taking pills can be started from the 2nd-5th day of menstruation, but in this case, in the 1st cycle of using the drug, additional methods of contraception should be used in the first 7 days of taking pills. If more than 5 days have passed since the start of menstruation, you should postpone the start of taking the drug until the next menstruation.

Taking the drug after childbirth

Non-breast-feeding women can start taking pills no earlier than the 21st day after giving birth, after consulting their doctor first. In this case, there is no need to use other methods of contraception. If you have already had sexual contact after giving birth, then you should wait until the first menstruation to take the pills. If a decision is made to take the drug later than 21 days after delivery, then additional methods of contraception should be used in the first 7 days.

Taking the drug after an abortion

After an abortion, if there are no contraindications, you should start taking pills from the 1st day, and in this case there is no need to use additional methods of contraception.

Switching from another oral contraceptive

Taking Novynette® after a contraceptive (with 30 mcg of ethinyl estradiol) containing 21 tablets. The 1st table of Novynette® is recommended to be taken the next day after completing the course of the previous drug. You don’t need to take a 7-day break or wait for your period to start. There is no need to use additional methods of contraception.

Taking Novynette® after a contraceptive containing 28 tablets. The next day after the end of the tablets in the package, you should start a new package of Novynette®.

Taking Novynette® after using a progestogen-only contraceptive (mini-pili). The 1st tablet of Novynette® should be taken on the 1st day of the cycle. There is no need to use additional methods of contraception.

If there is no menstruation when taking mini-pili, then after excluding pregnancy, you can start taking Novynette® on any day of the cycle, but in this case, additional methods of contraception should be used in the first 7 days.

In the above cases, the following non-hormonal methods are recommended as additional methods of contraception: the use of a cervical cap with spermicidal gel, a condom, or abstinence from sexual contact. The calendar method is not recommended in these cases.

Postponing the menstrual cycle

If there is a need to delay menstruation, it is necessary to continue taking tablets from the new package without a 7-day break, according to the usual scheme. If menstruation is delayed, breakthrough or spotting bleeding may appear, but this does not reduce the contraceptive effect of the drug. Regular use of Novynette® can be restored after the usual 7-day break.

Missed pills

If a woman forgot to take a pill in a timely manner, and no more than 12 hours have passed since the skip, you just need to take the forgotten pill, and then continue taking it at the usual time. If more than 12 hours have passed between taking pills — this is considered skipping the pill, the reliability of contraception in this cycle is not guaranteed and the use of additional methods of contraception is recommended.

If you miss one tablet at the 1st or 2nd week of the cycle, you should take 2 tablets the next day and then continue taking it regularly, using additional methods of contraception until the end of the cycle. If you miss a pill for the 3rd week of the cycle, you should take the forgotten pill, continue taking it regularly and do not take a 7-day break. It is important to remember that due to the minimum dose of estrogen, the risk of ovulation and/or spotting increases if you skip taking the pill, and therefore the use of additional methods of contraception is recommended.

How to use it for vomiting or diarrhea

If vomiting or diarrhea occurs after taking the drug, then the absorption of the drug may be defective. If the symptoms stopped within 12 hours, then you need to take another 1 tablet. additionally. After that, you should continue taking the pills in the usual way. If symptoms continue for more than 12 hours, then additional methods of contraception should be used during vomiting or diarrhea and for the next 7 days.

Overdose

Possible nausea, vomiting, in girls-spotting from the vagina.

The drug does not have a specific antidote, and the treatment is symptomatic.

If symptoms of overdose occur in the first 2-3 hours after taking the drug, gastric lavage is possible.

Special instructions

Before starting to use the drug and every 6 months thereafter, it is recommended to collect a detailed family and personal history and undergo a general medical and gynecological examination (examination by a gynecologist, taking a cytological smear, examination of mammary glands and liver function, monitoring of blood pressure (BP), cholesterol concentration in the blood, urinalysis).

These studies should be repeated periodically, due to the need for timely identification of risk factors or contraindications that have occurred. The drug is a reliable contraceptive drug: the Pearl index (an indicator of the number of pregnancies that occurred during the use of the method of contraception in 100 women within 1 year) when used correctly is about 0.05.

In each case, before prescribing hormonal contraceptives, the benefits or possible negative effects of taking them are individually evaluated. This issue should be discussed with the patient, who, after receiving the necessary information, will make a final decision on the preference for hormonal or any other method of contraception.

A woman’s health status should be carefully monitored. If any of the following conditions/diseases appear or worsen while taking the drug, you should stop taking the drug and switch to another, non-hormonal method of contraception:

– diseases of the hemostatic system. – conditions / diseases predisposing to the development of cardiovascular or renal failure. – epilepsy-migraine – risk of developing an estrogen-dependent tumor or estrogen-dependent gynecological diseases; – diabetes mellitus, not complicated by vascular disorders;- severe depression (if depression is associated with a violation of tryptophan metabolism, then vitamin B6 can be used for correction);- sickle cell anemia, since in some cases (for example, infections, hypoxia) estrogen-containing drugs can provoke thromboembolism in this pathology. – the appearance of abnormalities in laboratory tests of liver function assessment. – Thromboembolic diseases

Epidemiological studies have shown that there is a link between taking oral hormonal contraceptives and an increased risk of arterial and venous thromboembolic diseases (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism). An increased risk of venous thromboembolic diseases has been proven, but it is significantly less than during pregnancy (60 cases per 100 thousand pregnancies). Arterial or venous thromboembolism of the hepatic, mesenteric, renal or retinal vessels is very rarely observed when using oral contraceptives. The risk of arterial or venous thromboembolic diseases increases:- with age;- when smoking (heavy smoking and age over 35 years are considered risk factors);- if there is a family history of thromboembolic diseases (for example, parents, brother or sister). If a genetic predisposition is suspected, it is necessary to consult a specialist before using the drug. – with obesity (body mass index above 30 kg / m2); – with dyslipoproteinemia;- with arterial hypertension;- for diseases of the heart valves complicated by hemodynamic disorders, – for atrial fibrillation;- with diabetes mellitus complicated by vascular lesions;- during prolonged immobilization, after major surgery, after surgery on the lower extremities, after a serious injury.

In these cases, temporary discontinuation of the drug is expected: it is advisable to stop no later than 4 weeks before surgery, and resume – no earlier than 2 weeks after remobilization.

Increased risk of venous thromboembolic diseases in women after childbirth.Diseases such as diabetes mellitus, systemic lupus erythematosus, hemolytic – uremic syndrome, Crohn’s disease, ulcerative colitis, and sickle cell anemia increase the risk of venous thromboembolic diseases.

Such biochemical abnormalities as resistance to activated protein C, hyperchromocysteinemia, protein C and S deficiency, antithrombin III deficiency, and the presence of antiphospholipid antibodies increase the risk of arterial or venous thromboembolic diseases. When assessing the benefit / risk ratio of taking the drug, it should be borne in mind that targeted treatment of this condition reduces the risk of thromboembolism. Signs of thromboembolism are:- sudden chest pain that radiates to the left arm, – sudden shortness of breath, – any unusually severe headache that lasts for a long time or appears for the first time, especially when combined with sudden complete or partial loss of vision or diplopia, aphasia, dizziness, collapse, focal epilepsy), weakness or pronounced numbness in half of the body, motor disorders, severe unilateral pain in the calf muscle, acute abdomen).

Tumor diseases

Some studies have reported an increase in the incidence of cervical cancer in women who have taken hormonal contraceptives for a long time, but the results of studies are contradictory. Sexual behavior, human papillomavirus infection, and other factors play a significant role in the development of cervical cancer.

A meta-analysis of 54 epidemiological studies showed that there is a relative increase in the risk of breast cancer among women taking oral hormonal contraceptives, but the higher detection of breast cancer could be associated with more regular medical examinations. Breast cancer is rare among women younger than 40, whether or not they are taking hormonal birth control pills, and increases with age. Taking pills can be considered one of many risk factors. However, a woman should be made aware of the possible risk of developing breast cancer, based on an assessment of the benefit-risk ratio (protection against ovarian and endometrial cancer).

There are few reports of the development of a benign or malignant liver tumor in women who take hormonal contraceptives for a long time. This should be taken into account in the differential diagnostic assessment of abdominal pain, which may be associated with an increase in liver size or intra-abdominal bleeding. A woman should be warned that the drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases.

The effectiveness of the drug may decrease in the following cases: missed pills, vomiting and diarrhea, simultaneous use of other drugs that reduce the effectiveness of birth control pills.

If the patient is taking another medication at the same time, which may reduce the effectiveness of birth control pills, additional methods of contraception should be used.

The effectiveness of the drug may decrease if after several months of their use irregular, smearing or breakthrough bleeding appears, in such cases it is advisable to continue taking tablets until they end in the next package. If at the end of the second cycle, menstrual-like bleeding does not begin or acyclic spotting does not stop, stop taking the pills and resume it only after excluding pregnancy.

Chloasma

Chloasma can sometimes occur in women who have a history of chloasma during pregnancy. Those women who are at risk of developing chloasma should avoid contact with sunlight or ultraviolet light while taking the pills.

Changes in laboratory parameters

Under the influence of oral birth control pills-due to the estrogenic component-the level of certain laboratory parameters may change (functional parameters of the liver, kidneys, adrenal glands, thyroid gland, hemostasis indicators, lipoprotein and transport protein levels).

After acute viral hepatitis, it should be taken after normalization of liver function (no earlier than 6 months). With diarrhea or intestinal disorders, vomiting, the contraceptive effect may decrease (without stopping taking the drug, it is necessary to use additional non-hormonal methods of contraception). Women who smoke have an increased risk of developing vascular diseases with serious consequences (myocardial infarction, stroke). The risk depends on age (especially for women over 35) and the number of cigarettes they smoke. During lactation, the excretion of milk may decrease, in small amounts, the drug is excreted in breast milk.

EFFECT OF THE DRUG ON THE ABILITY TO DRIVE A CAR AND WORK MECHANISMS

Studies on the possible effect of the drug on the ability to drive a car or other mechanisms have not been conducted.

Form of production

Film-coated tablets

Storage conditions

At a temperature of 15-30 °C

Shelf life

3 years

Active ingredient

Desogestrel, Ethinyl Estradiol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

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

Indications

Contraception