Oralcon - instructions for use, doses, side effects, contraindications

Lactose granulated * 58.319 mg, polucriline potassium 1.0 mg, magnesium stearate 0.5 mg. Sugar shell: Ethyl cellulose 0.325 mg, talc purified 10.53 mg, acacia gum 1.77 mg, disodium edetate 0.00585 mg, sucrose 15.61 mg, cellulose microcrystalline 0.22 mg, titanium dioxide 0.28 mg, macrogol 6000 (polyethylene glycol 6000) 0.268 mg.

* consists of lactose 81.5%, sucrose 9.58%, corn starch 8.92%, disodium edetate 0.023%, methylparahydroxybenzoate 0.134%.

Description:White round biconvex tablets, covered with sugar shell. A cross-sectional view is the core of a white or almost white color.

Pharmacotherapeutic group:Contraceptive agent combined (estrogen + progestogen)

ATX: & nbsp

G.03.A.B Progestogens and estrogens (combinations for sequential administration)

G.03.A.B.03 Levonorgestrel and ethinyl estradiol

Pharmacodynamics:Oralcon is a low-dose monophasic oral combined estrogen-gestagenic contraceptive. The contraceptive effect of Oralcon is carried out by means of complementary mechanisms, the most important of which are suppression of ovulation and a change in the viscosity of the secretion of the cervix, as a result of which it becomes impenetrable for spermatozoa. In women taking combined oral contraceptives, the menstrual cycle becomes more regular, the pain and intensity of menstrual bleeding decreases, and one of the risk factors for the development of iron deficiency anemia is reduced.In addition, there is evidence that the risk of developing endometrial cancer and ovarian cancer is reduced. When properly applied, the Perl index (an indicator that reflects the frequency of pregnancy in 100 women during the year of use of the contraceptive) is less than 1. When missing tablets or improperly used, the Pearl index may increase.

Pharmacokinetics:

Levonorgestrel

Absorption. After oral ingestion levonorgestrel quickly and completely absorbed, its maximum concentration in blood plasma, equal to 3-4 ng / ml, is reached after about 1 hour. Bioavailability of levonorgestrel with oral administration is almost complete.

Distribution. Levonorgestrel binds to blood plasma albumin and to sex hormone binding globulin (SHBG). In a free form there is only about 1.3% of the total concentration in the blood plasma; about 64% are specifically associated with SHBG and about 34% are not specifically associated with albumin. Induction with ethinylestradiol synthesis of SHBG affects the binding of levonorgestrel to plasma proteins, causing an increase in the fraction associated with SHBG and a decrease in the fraction associated with albumin.The apparent volume of distribution of levonorgestrel is about 184 liters after a single dose.

Metabolism. Levonorgestrel almost completely metabolized. The clearance rate from the blood plasma is approximately 1.3-1.6 ml / min / kg.

Excretion. The concentration of levonorgestrel in the blood plasma undergoes a two-phase reduction. The final half-life is about 20-23 hours. In unmodified form levonorgestrel is not excreted, but only in the form of metabolites, which are excreted by the kidneys and through the intestine in a ratio of approximately 1: 1.

Equilibrium concentration. With a daily intake of the drug, the concentration of levonorgestrel in the blood plasma increases approximately 3-4 times, reaching the equilibrium concentration in the second half of the course of admission. The pharmacokinetics of levonorgestrel is affected by the concentration of SHBG, which when levonorgestrel is used together with ethinyl estradiol grows about 1.7 times. At an equilibrium concentration, the clearance rate is reduced to about 0.7 ml / min / kg.

Ethinylestradiol

Absorption. After oral administration ethinyl estradiol quickly and completely absorbed. The maximum concentration in the blood plasma, equal to about 95 pg / ml, is achieved in 1-2 hours. During the intake and primary passage through the liver ethinyl estradiol is metabolized, as a result of which its bioavailability when ingested is an average of about 45% (individual differences within 20-65%).

Distribution. Ethinylestradiol almost completely (approximately 98%), although non-specific, binds to albumin. Ethinylestradiol induces synthesis of SHBG. The apparent volume of distribution of ethinylestradiol is 2.8-8.6 l / kg.

Metabolism. Ethinylestradiol is subjected to presystemic conjugation, both in the mucosa of the small intestine and in the liver. The main pathway of metabolism is aromatic hydroxylation. The clearance rate from plasma is 2.3-7 ml / min / kg.

Excretion. Reduction in the concentration of ethinyl estradiol in blood plasma is biphasic; the first the phase is characterized by a half-life period of about 1 hour, the second - 10-20 hours. Unchanged from the body is not excreted. Metabolites of ethinyl estradiol are excreted by the kidneys and through the intestine in a ratio of 4: 6 with a half-life of about 24 hours.

Equilibrium concentration. With daily oral administration of Oralcon, the concentration of ethinylestradiol in the blood plasma increases slightly, reaching a maximum value of 114 pg / ml at the end of the course.Given the volatile end-point of half-life and the daily oral intake, equilibrium concentration is achieved in about one week.

Indications:

- Pprevention of unwanted pregnancy (contraception);

- hormone-dependent functional disorders of the menstrual cycle.

Contraindications:

The drug should not be used in the presence of any of the conditions / diseases listed below. If any of these conditions / diseases develop for the first time against the background of the medication, the drug should be immediately withdrawn.

- Thrombosis (venous and arterial) and thromboembolism now or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction), cerebrovascular disorders.

- Conditions preceding thrombosis (including, transient ischemic attacks, angina pectoris) are currently or in history.

- The presence of severe or multiple risk factors for venous or arterial thrombosis may also be a contraindication (see section "Special instructions").

- Migraine with focal neurologic symptoms at present or in the anamnesis.

- Diabetes mellitus with vascular complications.

- Pancreatitis with severe hypertriglyceridemia at present or in the anamnesis.

- Hepatic insufficiency and severe liver disease (before the normalization of liver function tests).

- Liver tumors (benign or malignant) are currently or in the anamnesis.

- Revealed hormone-dependent malignant diseases (including genital organs or mammary glands) or suspected of them.

- Bleeding from the vagina of unknown origin.

- Pregnancy or suspicion of it.

- Lactation period.

- Hypersensitivity to any of the components of the drug;

- Lactose / fructose intolerance, lactase / sucrose / isomaltase deficiency, glucose-galactose malabsorption (due to the presence of lactose and sucrose in the composition).

Carefully:If any of the conditions / diseases / risk factors listed below are currently available, the potential risk and the expected benefit of using combined oral contraceptives should be carefully correlated in each individual case:

- Risk factors for thrombosis and thromboembolism: smoking, thrombosis,myocardial infarction or cerebrovascular accident at a young age in someone of the next of kin; obesity; dyslipoproteinemia, arterial hypertension; migraine without focal neurological symptoms; heart valve diseases; heart rhythm disturbance, prolonged immobilization, extensive surgical interventions, extensive trauma.

- Other diseases in which there may be violations of peripheral circulation: diabetes mellitus without vascular complications; systemic lupus erythematosus; hemolytic-uremic syndrome; Crohn's disease and ulcerative colitis; sickle-cell anemia; and phlebitis of superficial veins.

- Hypertriglyceridemia.

- Liver diseases of mild and moderate severity, with normal liver function tests.

- The disease first appeared or worsen during pregnancy, or on the background of the previous use of sex hormones (eg, jaundice, cholestasis, gallbladder disease, otosclerosis with hearing impairment, porphyria, herpes during pregnancy, Sydenham's chorea).

In women with hereditary forms of angioedema, exogenous estrogens can cause or worsen symptoms of angioedema.

Pregnancy and lactation:Oralcon is contraindicated during pregnancy and during lactation. If pregnancy is detected during oral medication, the drug should be immediately discontinued. However, numerous epidemiological studies have not revealed any increased risk of developmental defects in children born to women who received sex hormones before pregnancy or teratogenicity, when sex hormones were negligently taken early in pregnancy.

Taking combined oral contraceptives can reduce the amount of breast milk and change its composition, so, as a rule, their use is contraindicated during breastfeeding. A small amount of sex hormones and / or their metabolites can be excreted with milk.

Dosing and Administration:

Use inside with a little water. 1 tablet approximately at the same time, from the first day of the cycle and further "along the arrow", as indicated on the package. Take continuously for 21 days. Acceptance of the next package begins after a 7-day break in taking the tablets, during which bleeding "cancellation" usually develops.Bleeding, as a rule, begins on day 2-3 after taking the last pill and can continue until the start of the new package.

In the absence of taking any other hormonal contraceptives in the previous month

The drug is taken on the 1st day of the menstrual cycle (ie, on the 1st day of menstrual bleeding). Possible reception on day 2-5 of the menstrual cycle, however, in this case it is recommended to additionally use the barrier method of contraception during the first 7 days of taking Oralcon tablets from the 1 st package.

Transition from other combined oral contraceptives, vaginal ring or plaster

It is recommended to start taking Oralcon on the next day after taking the last active tablet from the previous package of another contraceptive, but not later than the next day after the 7-day ticking.

In the case of a previous use of a vaginal ring or patch, Oralcon's administration begins on the day of removal of the vaginal ring or patch, but not later than the day when a new ring is to be inserted or a new patch is stuck.

Transition from contraceptives containing only gestagens ("mini-pili", injectable forms, implants) or from an intrauterine contraceptive releasing gestagen

With the "mini-drank" you can go any day (without interruption), from the implant or intrauterine contraceptive - on the day of its removal, from the injection form - the day the next injection is to be made. In all cases it is necessary to use barrier methods of contraception during the first 7 days of Oralcon.

Application of Oralcon after abortion in the first trimester of pregnancy

You can start taking the drug immediately. If this rule is followed, the woman does not need additional contraceptive protection.

Application Oralcon after childbirth or abortion in the II trimester of pregnancy

Reception of the drug is recommended to begin on the 21-28th day after childbirth or abortion in the II trimester of pregnancy. If the drug is started later, it is necessary to use the barrier method of contraception during the first 7 days of taking Oralcon. However, if a woman has had sexual intercourse before starting Oralcon, first pregnancy should be excluded or it is necessary to wait for the first menstruation.

Passing Oralcon

If the delay in taking the drug is less than 12 hours, the contraceptive effect does not decrease.It is necessary to take the pill as soon as possible, the next tablet is taken at the usual time.

If the delay in taking the drug was more than 12 hours, the contraceptive effect is reduced. The more pills are missed, and the closer the pass to the 7-day break, the higher the probability of pregnancy.

In this case it is necessary to remember:

- The drug should never be discontinued for more than 7 days;

- 7 days of continuous reception is required for adequate suppression of the hypothalamic-pituitary-ovarian system

If you miss a drug that is more than 12 hours (that is, the interval from the time you take the last pill for more than 36 hours), you should follow the following rules:

- If the pass occurred at week 1, you need to take the last missed tablet as soon as possible (as soon as the woman remembers), even if it means taking 2 tablets at a time. The next tablet is taken at the usual time. Additionally, the barrier method of contraception can be used for the next 7 days. If the sexual intercourse took place during the week preceding the admission of pills, it is necessary to take into account the probability of pregnancy.

- If the pass occurred at week 2, you must take the last missed tablet as soon as possible (as soon as the woman remembers), even if it means taking 2 tablets

- at the same time. The next tablet is taken at the usual time. If the tablets were taken correctly during the 7 days preceding the first missed pill, there is no need for additional methods of barrier contraception. Otherwise, or if two or more tablets are missed, the barrier method of contraception must be used additionally within 7 days.

If the pass occurred at the 3rd week of taking the drug, the risk of reducing the contraceptive effect is unavoidable. If the tablets were taken correctly during the 7 days preceding the first missed pill, there is no need for additional methods of barrier contraception. You can use two rules:

- it is necessary to take the last missed tablet as soon as possible (as soon as the woman remembers), even if it means taking 2 tablets at a time. The following tablets are taken at the usual time, until they end in this package.Receipt of tablets from the following packaging must be started immediately. Bleeding "cancellation" is unlikely until the end of the second package, while there may be "smearing" discharge and bleeding "breakthrough" during the taking of tablets;

- You can interrupt the taking of tablets from the current package and take a break for 7 days, including the day of skipping the tablets and then start taking the tablets from the new package.

If a woman missed taking pills and during the break she does not have a bleeding "withdrawal", it is necessary to exclude pregnancy.

Change in the day of menstrual bleeding

If there is a need to delay the onset of menstrual bleeding, you should start taking Oralcon tablets from the new package, immediately after the end of the pills in the previous package (without taking a break). Tablets from this package should be taken for as long as a woman plans to push the onset of menstrual bleeding or until the end of the tablets in the second package. Against the background of taking the drug from the second package, it is possible "smearing" discharge or "breakthrough" uterine bleeding.Oralcon should be resumed after the usual 7-day break from the new package. In order to shift the day of the onset of menstrual bleeding to another day of the week, the shortest interval in taking the tablets for the required number of days should be shortened. However, it must be remembered that the shorter the interval between tablets, the higher the likelihood of a woman having a bleeding "cancellation", and further, "smearing" secretions and bleeding "breakthrough" during the second package of Oralcon (as well as in the case of delay the beginning of menstrual bleeding).

Recommendations for taking the drug in case of vomiting or diarrhea

If vomiting or diarrhea occurred within 4 hours after taking the drug, then its absorption might be incomplete, so additional barrier methods of contraception should be used in this case. It is necessary to adhere to the rules, as well as when missing pills.

With hormone-dependent functional disorders of the menstrual cycle, the dose and course of treatment are selected by the doctor individually in each specific case.

Side effects:

Nausea, vomiting, headache, breast engorgement, weight gain, decreased libido and mood, coarsening of the voice, the appearance of intermenstrual bloody discharge, in some cases - eyelid edema, conjunctivitis, visual impairment, discomfort when wearing contact lenses (these phenomena are temporary character and disappear after cancellation without prescribing any therapy).

With prolonged admission, chloasma, hearing loss, generalized pruritus, jaundice, calf muscle cramps, and increased frequency of epileptic seizures can very rarely occur.

Rarely there is hypertriglyceridemia, hyperglycemia, decreased glucose tolerance, increased blood pressure, thrombosis and venous thromboembolism, skin rashes, a change in the nature of vaginal secretion, vaginal candidiasis, increased fatigue, diarrhea.

Overdose:

No cases of overdose have been reported. Possible symptoms of an overdose: nausea, vomiting, "smearing" spotting from the vagina or metrorrhagia.

There is no specific antidote, treatment is symptomatic.

Interaction:Some medicines may reduce the effectiveness ofdrug: antiepileptic drugs (including, primidon, phenytoin, barbiturates, carbamazepine, oxcarbazepine, topiramate, felbamate), anti-tuberculosis drugs (including, rifampicin, rifabutin), gynecological examinations for the detection of cervical disease or with features of sexual behavior (a more rare use of barrier methods of contraception).

When diarrhea, vomiting contraceptive effect is reduced (without stopping the drug, it is necessary to use additional non-hormonal methods of contraception).

Treatment should be stopped immediately after pregnancy, the development of migraine headaches (if they were not previously), with the emergence of early signs of phlebitis or phlebotrombosis (unusual pain or bloating of the veins on the legs), jaundice, visual impairment, cerebrovascular disorders, stitching pains of unclear etiology when breathing or coughing, pain and feelings of tightness in the chest, with increased blood pressure, as well as 3 months before the planned pregnancy and approximately 6 weeks before the planned chi urgicheskogo intervention during prolonged immobilization.

Moderate bloody discharge during taking the drug does not require discontinuation.

Special instructions:

If any of the conditions / diseases / risk factors listed below are currently available, the potential risk and the expected benefit of using combined oral contraceptives should be closely related, in each individual case, and discussed with the woman before she decides to start taking the drug. In case of weighting, strengthening or the first manifestation of any of these conditions or risk factors, a woman should consult a doctor who can decide whether to cancel the drug:

Diseases of the cardiovascular system

The results of epidemiological studies indicate the existence of a relationship between the use of contraceptives. It is necessary to stop the use of the drug (in the case of a planned operation, at least 4 weeks before it) and not to resume taking it within 2 weeks after the end of immobilization. The relationship between the administration of combined oral contraceptives and the increased incidence of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, myocardial infarction,cerebrovascular disorders) when taking combined oral contraceptives. These diseases are rare. The risk of developing venous thromboembolism (VTE) is maximal in the first year of taking such drugs. An increased risk is present after the initial use of combined oral contraceptives or the resumption of the use of the same or different combined oral contraceptives (after a break between doses of 4 weeks or more). Data from a large prospective study involving 3 groups of female volunteers show that this increased risk is present mainly during the first 3 months.

The overall risk of VTE in women taking low-dose combined oral contraceptives (<50 mcg ethinyl estradiol) is two to three times higher than in non-pregnant women who do not take combined contraceptives, however, this risk remains lower compared to the risk of VTE when pregnancy and childbirth. VTE can lead to death (in 1-2% of cases). VTE, manifested as deep vein thrombosis, or pulmonary embolism, can occur when using any combination oral contraceptives.

Very rarely, when combined oral contraceptives are used, thrombosis of other blood vessels arises, for example, liver, mesenteric, renal, cerebral veins and arteries or retinal vessels. There is no consensus on the relationship between the onset of these events and the use of combined oral contraceptives.

The risk of developing thrombosis (venous and / or arterial) and thromboembolism increases:

- with age;

- smokers with an increase in the number of cigarettes or an increase in the age of the risk increases, especially in women over 35 years of age);

In the presence of:

- family history (for example, venous or arterial thromboembolism ever at close relatives or parents at a relatively young age). In the case of a hereditary or acquired predisposition, a woman should be examined by an appropriate specialist to decide on the possibility of taking combined oral contraceptives;

- Obesity (body mass index more than 30 kg / m²);

- dyslipoproteinemia;

- arterial hypertension;

- migraine;

- heart valve diseases;

- Atrial fibrillation;

- prolonged immobilization, extensive surgical intervention, any operation on the lower limbs or extensive trauma. In these situations, it is advisable to stop using combined oral contraceptives (in the case of a planned operation at least four weeks before) and not to resume admission within two weeks after the end of immobilization.

The question of the possible role of varicose veins and superficial thrombophlebitis in the development of venous thromboembolism remains controversial. You should consider the increased risk of thromboembolism in the postpartum period. Violations of peripheral circulation can also occur in diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. The increase in frequency and severity of migraine during use of combined oral contraceptives (which may be preceded by cerebrovascular disorders) can be grounds for immediate discontinuation of these drugs.When assessing the status of the risk and benefit, it should be borne in mind that adequate treatment of the relevant condition can reduce the associated risk of thrombosis. It should also be taken into account that the risk of thrombosis and thromboembolism in pregnancy is higher than when taking low-dose oral contraceptives (<0.05 mg of ethinyl estradiol).

- Tumors

The most significant risk factor for developing cervical cancer is a persistent papillomavirus infection. There are reports of a slight increase in the risk of developing cervical cancer with long-term use of combined oral contraceptives. The connection with the use of combined oral contraceptives has not been proven. There are contradictions as to the extent to which these findings are associated with screening for cervical pathology or with peculiarities of sexual behavior (more rare use of barrier methods of contraception). A meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of developing breast cancer diagnosed in women taking combined oral contraceptives at present (relativerisk 1, 24). The increased risk gradually disappears within 10 years after discontinuation of these medications. Due to the fact that breast cancer is rarely seen in women under 40 years of age, the increase in diagnosed breast cancer in women taking combined oral contraceptives now or recently has been insignificant in relation to the overall risk of this disease. His association with the use of combined oral contraceptives has not been proven. The observed increase in risk may also be the result of an earlier diagnosis of breast cancer in women using combined oral contraceptives. In women who have ever used combined oral contraceptives, cancer is detected at earlier stages than in women who never used them. In rare cases, combined with oral contraceptives, the development of benign, and extremely rare

- malignant liver tumors, which in some cases led to life-threatening intra-abdominal hemorrhage. In case of severe pain in the abdomen,increase in the liver or signs of intra-abdominal bleeding, this should be taken into account when making a differential diagnosis.

- Other states

Women with hypertriglyceridemia (or having this condition in a family history) may have an increased risk of developing pancreatitis while taking combined oral contraceptives. Although a small increase in blood pressure was described in many women taking combined oral contraceptives, clinically significant increases were rarely noted. Nevertheless, if a persistent, clinically significant increase in blood pressure develops during the intake of combined oral contraceptives, these drugs should be discontinued and the treatment of hypertension should begin. Reception of combined oral contraceptives can be continued if normal blood pressure values are achieved with the help of antihypertensive therapy.

The following conditions have been reported to develop or worsen, both during pregnancy and when taking combined oral contraceptives, but their association with combined oral contraceptives has not been proven: jaundice and / or pruritus,associated with cholestasis; formation of stones in the gallbladder; porphyria; systemic lupus erythematosus; hemolytic-uremic syndrome; chorea; herpes pregnant; hearing loss associated with otosclerosis. Cases of Crohn's disease and ulcerative colitis are also described against combined use of oral contraceptives. In women with hereditary forms of angioedema, exogenous estrogens can cause or worsen symptoms of angioedema. Acute or chronic liver dysfunction may require the cancellation of combined oral contraceptives until the liver function returns to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous reception of sex hormones, requires discontinuation of combined oral of contraceptives. Although 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 (<0.05 mg ethinyl estradiol).Nevertheless, women with diabetes should be carefully observed during the intake of combined oral contraceptives. Sometimes chloasma can develop, especially in women with a history of pregnancy chloasma. Women with a tendency to chloasma when taking combined oral contraceptives should avoid prolonged exposure to the sun and exposure to ultraviolet radiation.

Effect on the nature of bleeding

On the background of taking combined oral contraceptives, there may be irregular bleeding (spotting spotting or "breakthrough" bleeding), especially during the first months of use. Therefore, any irregular bleeding should be assessed only after an adaptation period of approximately three cycles. If irregular bleeding recurs or develops after previous regular cycles, a thorough examination should be conducted to exclude malignant neoplasms or pregnancy. Some women during the break in the reception of tablets may not develop bleeding "cancellation."If combined oral contraceptives are taken as directed, it is unlikely that a woman is pregnant. However, if previously combined oral contraceptives were taken irregularly or if there are no consecutive two bleeding cancellations, the continuation of the drug should be excluded pregnancy.

Effect on the ability to drive transp. cf. and fur:Does not affect.

Form release / dosage:

The coated tablets are 150 μg + 30 μg.

Packaging:

For 21 tablets in a blister of PVC / aluminum foil. 1 or 3 blisters with instructions for use in a cardboard pack.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date indicated by the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003705/10

Date of registration:04.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:Fami Ker LimitedFami Ker Limited India

Manufacturer: & nbsp

FAMY CARE, Limited India

Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.

Information update date: & nbsp10.06.2017

Illustrated instructions

Instructions

Oralcon (Oralcon)