Novinet, 63 pcs.

Pharmacodynamics

Novinet® is a combined oral contraceptive drug, the main contraceptive effect of which is inhibition of gonadotropin synthesis and suppression of ovulation. In addition, by increasing the viscosity of cervical mucus, the movement of sperm through the cervical canal is slowed, and changes in the condition of the endometrium prevent the implantation of a fertilized egg.

Ethinylestradiol is a synthetic analogue of endogenous estradiol, desogestrel has pronounced gestagenic and anti-estrogenic effects similar to endogenous progesterone, weak androgenic and anabolic activity.

Novinet ® has beneficial effects on lipid metabolism: increases the concentration of high-density lipoproteins (HDL) in the blood plasma, while not affecting the low-density lipoproteins (LDL).

When using the drug it is registered a significant decrease of amount of lost blood each month (at initial menorrhagia), menstrual cycle is normalized, and favorable effect on skin is noted (especially at the presence of acne vulgaris).

Pharmacokinetics

Desogestrel

Intake

Intake

. When taken orally, desogestrel is absorbed from the gastrointestinal (GI) tract quickly and almost completely. It is metabolized to 3-keto-desogestrel, which is the biologically active metabolite of desogestrel. The average maximum serum concentration (Cmax) is 2 ng/ml, reached 1.5 hours later (Tmax) after taking the tablet. Bioavailability of the drug is 62-81%. Distribution in the body 3-keto-desogestrel binds to plasma proteins, mainly to albumin and to globulin binding sex hormones (GSSH). 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: Zα-ON-desogestrel, Zβ-ON-desogestrel, Zα-ON-5α-N-desogestrel (first phase metabolites). They have no pharmacological activity, and partially, by conjugation (second phase metabolism), are converted to polar metabolites (sulfates and glucuronates). Clearance from blood plasma is about 2 ml/min per 1 kg of body weight.

Exhaustion

The average half-life of 3-keto-desogestrel is 30 hours. Metabolites are excreted by the kidneys and through the intestine (in a ratio of 4:6).
Stable concentrations are established by the second half of the cycle. At this time, ketogestrel levels increase 2-3 times.
Ethinylestradiol

Ethinylestradiol absorption

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

Distribution in the body

Ethinylestradiol is completely bound to plasma proteins, mainly to albumin. The volume of distribution is 5 l/kg.

Metabolism

The presystemic conjugation of ethinylestradiol is significant. Passing the intestinal wall (first phase of metabolism) it undergoes conjugation in the liver (second phase of metabolism). Ethinylestradiol and its conjugates of the first phase of metabolism (sulfates and glucuronides) are excreted in bile and enter enter enterohepatic circulation.

The blood plasma clearance is about 5 ml/min per 1 kg body weight.

Extraction from the body

The average half-life of ethinylestradiol is about 24 hours. About 40% is excreted by the kidneys and about 60% through the intestine.
Stable concentration is established by 3-4 days, with blood serum levels of ethinylestradiol 30-40% higher than after a single dose

Indications

Active ingredient

Composition

Active substances:

Ethinylestradiol – 0.020 mg,

desogestrel – 0.150 mg;

Associates:

quinoline yellow dye E 104,

α-tocopherol,

magnesium stearate,

colloidal silicon dioxide,

stearic acid,

povidone,

Potato starch,

Lactose monohydrate;

Film coating:

propylene glycol,

macrogol 6000,

hypromellose.

How to take, the dosage

Ingestion. The tablets are taken from the 1st day of the menstrual cycle and are taken 1 tablet a day for 21 days, if possible at the same time of the day. After taking the last tablet of the pack there is a 7-day break, during which menstrual bleeding occurs due to withdrawal of the drug.

The day after the 7-day break (4 weeks after taking the 1st tablet, on the same day of the week) we resume taking the drug from the next package, also containing 21 tablets, even if bleeding has not stopped. Such scheme of reception of tablets is adhered to as long as there is a need for contraception. The contraceptive effect is maintained even during a 7-day break if the rules for taking the pills are followed.

The 1st dose of the drug

The 1st tablet should be taken from the 1st day of the menstrual cycle. In this case it is not necessary to use additional methods of contraception. It is possible to start taking the pills from the 2nd to 5th day of a menstrual cycle, but in this case additional contraceptive methods should be used during the first 7 days of taking the pills in the 1st cycle. If more than 5 days have passed after the beginning of menstruation, it is necessary to postpone the beginning of taking the drug until the next menstruation.

Taking the drug after childbirth

Non-breastfeeding women may not start taking the pills until 21 days after childbirth, with prior consultation with their doctor. In this case there is no need to use other contraceptive methods. If you have already had sexual intercourse after childbirth, then you should wait with taking the pills until your first menstrual period. If it is decided to take the drug later than 21 days after childbirth, then additional contraceptive methods should be used for the first 7 days.

Taking the drug after an abortion

After an abortion, if there are no contraindications, the pills should be started from day 1, and in this case no additional contraceptive methods are needed.

Transitioning from another oral contraceptive

Taking Novinet® after the contraceptive pill (with 30 mcg ethinylestradiol) containing 21 tablets

The 1st tablet of Novinet® is recommended to be taken the day after completion of the previous pill. It is not required to take a 7-day break or to wait for the beginning of menstruation. There is no need to use additional contraceptive methods.

To take Novinet® after the contraceptive pill containing 28 tablets, a new Novinet® package should be started the day after the pills in the package run out.

To take Novinet® after using a progestagen-only contraceptive (mini-pills). The first tablet of Novinet® should be taken on the first day of the cycle. It is not necessary to use additional contraceptive methods.

If menstruation does not occur while taking the mini-pill, Novinet® may be started on any day of the cycle after ruling out pregnancy, but in this case additional contraceptive methods are required in the first 7 days.

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

Postponing your menstrual cycle

If you need to delay your period, you should continue taking your pills from a new pill pack without a 7-day break, taking the usual regimen. Intermittent menstruation may cause breakthrough or smeary bleeding, but this does not reduce the contraceptive effect of the drug. Regular use of Novinet® can be restored after a regular 7-day break.

Missed pills

If a woman forgets to take her pill on time and it has not been more than 12 hours since she missed it, simply take the forgotten pill and continue at your usual time. If more than 12 hours have passed between taking the pill, it is considered a missed pill; reliable contraception is not guaranteed in this cycle and the use of additional contraceptive methods is recommended.

If you miss one pill in the 1st or 2nd week of your cycle, you should take two pills the next day and then continue regular use, using additional contraception until the end of the cycle. If you miss a pill in the 3rd week of your cycle, 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 there is an increased risk of ovulation and/or bleeding if the pill is missed, and therefore the use of additional contraceptive methods is recommended.

The order of administration in case of vomiting or diarrhea

If vomiting or diarrhea occurs after taking the drug, then absorption of the drug may be incomplete. If the symptoms stop within 12 hours, one more tablet should be taken. After this you should continue taking the tablets in the usual manner. If symptoms persist beyond 12 hours, additional contraception should be used during vomiting or diarrhea and the following 7 days.

Interaction

Drugs that induce hepatic enzymes, such as guidantoin, barbiturates, primidone, carbamazepine, rifampicin, oxcarbazepine, topiramate, felbamate, griseofulvin, preparations of St John’s wort reduce the effectiveness of oral contraceptives and increase the risk of breakthrough bleeding. Maximum induction is usually not reached before 2-3 weeks, but may continue for up to 4 weeks after drug withdrawal.

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

The oral contraceptives may decrease carbohydrate tolerance and increase the need for insulin or oral antidiabetic agents.

Special Instructions

Before starting the drug and every 6 months thereafter, it is recommended to take a detailed family and personal history and undergo general medical and gynecological examinations (gynecological examination, cytological smear, breast and liver function tests, control of blood pressure (BP), blood cholesterol concentration, urine tests).

These tests should be repeated periodically, due to the need for timely identification of risk factors or emerging contraindications.

The product is a reliable contraceptive: the Perl Index (the number of pregnancies that occurred in 100 women in a 1-year period while using the method) is about 0.05 when used correctly.

In each case, the benefits or possible negative effects of hormonal contraceptives are individually evaluated before they are prescribed. This must be discussed with the patient, who makes the final decision about whether she prefers hormonal or any other method of contraception after receiving the appropriate information.

The woman’s state of health should be carefully monitored. If any of the following conditions/diseases occur or worsen while taking this medication, you should stop taking the medication and switch to a different, non-hormonal contraceptive method:

– diseases of the hemostasis system.
– conditions/diseases predisposing to the development of cardiovascular, renal failure.
– epilepsy
– migraine
– risk of estrogen-dependent tumor or estrogen-dependent gynecological diseases;
– diabetes, not complicated by vascular disorders;
– severe depression (if depression is associated with a tryptophan metabolism disorder, vitamin B6 may be used for correction);
– sickle cell anemia, as in some cases (e.g., infections, hypoxia) estrogen-containing drugs in this pathology may provoke thromboembolic phenomena.
– appearance of abnormalities in laboratory tests to assess liver function.
– Thromboembolic diseases

Epidemiological studies have proven that there is an association between the intake of oral hormonal contraceptives and an increased risk of arterial and venous thromboembolic diseases (including myocardial infarction and myocardial infarction).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 lower than in pregnancy (60 cases per 100 thousand pregnancies).

In the use of oral contraceptives, arterial or venous thromboembolism of hepatic, mesenteric, renal or retinal vessels is very rare.

The risk of arterial or venous thromboembolic disease increases:
– with age;
– with smoking (heavy smoking and age over 35 years are risk factors);
– with a family history of thromboembolic disease (for example, parents, brother or sister). If genetic predisposition is suspected, it is necessary to consult with a specialist before using the drug.
– in obesity (body mass index over 30 kg/m2);
– in dislipoproteinemia;
– in arterial hypertension;
– in diseases of the heart valves, complicated by hemodynamic disorders,
– in atrial fibrillation;
– In diabetes mellitus complicated by vascular lesions;
– In prolonged immobilization, after major surgical intervention, after surgical intervention on the lower extremities, after severe trauma.

In these cases, temporary discontinuation of the drug is expected: preferably to stop at least 4 weeks before surgical intervention, and to resume at least 2 weeks after remobilization.

The risk of venous thromboembolic disease in women after childbirth is increased.

Diseases such as diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn’s disease, nonspecific ulcerative colitis, and sickle cell anemia increase the risk of venous thromboembolic disease.

Biochemical abnormalities such as activated protein C resistance, hyperchromocysteinemia, protein C, S deficiency, antithrombin III deficiency, and the presence of antiphospholipid antibodies increase the risk of arterial or venous thromboembolic disease.

When evaluating the benefit/risk ratio of taking the drug, it should be kept in mind that targeted treatment of this condition reduces the risk of thromboembolism. Signs of thromboembolism are:
– sudden chest pain that irradiates to the left arm,
– sudden shortness of breath,
– any unusually severe headache lasting a long time or occurring for the first time, especially when combined with sudden total or partial loss of vision or diplopia, aphasia, dizziness, collapse, focal epilepsy), weakness or marked numbness of half the body, motor disturbances, severe unilateral pain in the calf muscle, acute abdominal pain).

Tumor diseases

Some studies have reported an increased incidence of cervical cancer in women who have taken hormonal contraceptives for a long time, but results are inconsistent. 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 found that there was a relative increase in breast cancer risk among women taking oral hormonal contraceptives, but that higher detection of breast cancer could be related to more regular health screenings.

Breast cancer is rare among women under age 40, whether or not they take hormonal birth control, and increases with age. Taking the pill can be considered one of many risk factors. Nevertheless, a woman should be made aware of the possibility of developing breast cancer based on a benefit-risk assessment (protection against ovarian and endometrial cancer).

There are few reports of benign or malignant liver tumors in women taking hormonal contraceptives for a long time. This should be kept in mind in the differential diagnostic evaluation of abdominal pain, which may be associated with increased liver size or intra-abdominal bleeding.

The 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 be reduced by the following conditions: missed pills, vomiting and diarrhea, concomitant use of other drugs that reduce the effectiveness of birth control pills.

If a patient is taking another medication at the same time that may decrease the effectiveness of the birth control pills, additional contraceptive methods should be used.

The pills may be less effective if irregular, heavy, or intermittent bleeding occurs after a few months of use, in which case it is helpful to continue taking the pills until the next pill pack ends. If menstrual bleeding does not begin at the end of the second cycle, or if acyclic bleeding persists, stop taking the pills and resume only after ruling out pregnancy.

Chloasms

Chloasms may occasionally occur in women who have a history of them during pregnancy. Those women who are at risk for chloasma should avoid contact with sunlight or ultraviolet light while taking the pill.

Contraindications

With caution
Conditions that increase the risk of venous or arterial thrombosis/thromboembolism: age over 35 years, smoking, family history, obesity (body mass index over 30 kg/sq.m), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular heart disease, atrial fibrillation, prolonged immobilization, extensive surgery, lower extremity surgery, severe trauma, varicose veins and superficial thrombophlebitis, postpartum period, presence of severe depression, including In anamnesis, changes of 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 disease.

Side effects

Side effects requiring drug withdrawal:

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

Sensory organs: hearing loss associated with otosclerosis.

Others: hemolytic-uremic syndrome, porphyria; rarely – exacerbation of reactive systemic lupus erythematosus; very rare – Sydenham’s chorea (which resolves after discontinuation of the drug).

Other side effects (more frequent, but less severe). The appropriateness of continuing the drug is decided on an individual basis after consultation with a physician, based on the benefit/risk ratio.

In the sexual system: acyclic bleeding/bloody vaginal discharge, amenorrhea after drug withdrawal, changes in vaginal mucus, development of vaginal inflammation, candidiasis, tension, pain, increased mammary glands, galactorrhea.

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

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

CNS disorders: headache, migraine, mood swings, depression.

A visual organ: increased sensitivity of the cornea (when wearing contact lenses).

Metabolic disorders: fluid retention in the body, change (increase) in body weight, decreased carbohydrate tolerance.

Others: allergic reactions.

Overdose

Possible nausea, vomiting, in girls – bloody vaginal discharge.

The drug has no specific antidote, treatment is symptomatic.

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

Pregnancy use

Novinet is contraindicated during pregnancy.

Novinet is contraindicated during lactation (breastfeeding) because it suppresses lactation and affects the quality of milk. In addition, the active substances are excreted with breast milk.

Taking Novinet should be stopped 3 months before the planned pregnancy. If the pregnancy occurs the drug should be discontinued.

If there is no menstrual bleeding the continuation of the drug is allowed only after the exclusion of pregnancy.

Similarities