Universal reference book for medicines
Product name: ORALCON (ORALCON)

Active substance: ethinylestradiol, levonorgestrel

Type: Monophasic oral contraceptive

Manufacturer: FAMY CARE (India)

Composition, form of production and packaging
The tablets covered with a cover
(sugar) of white color, round, biconcave;
view on the transverse - the core is white or almost white.
1 tab.

ethinylestradiol 30 μg

levonorgestrel 150 μg

Auxiliary substances: lactose granulated (lactose - 81.5%, sucrose - 9.58%, corn starch - 8.92%, disodium edetate - 0.023%, methylparahydroxybenzoate - 0.134%) - 58.319 mg, polacrilin potassium - 1 mg, magnesium stearate - 0.5 mg.

The composition of the 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, microcrystalline cellulose 0.22 mg, titanium dioxide 0.28 mg, macrogol 6000 (polyethylene glycol 6000) - 0.268 mg.

21 pcs.
- blisters (1) - packs of cardboard.
21 pcs.
- blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Oralcon is a low-dose monophasic oral combined estrogen-progestational drug.
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

Suction

After oral administration, levonorgestrel is rapidly and completely absorbed, its C max in 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 with blood plasma albumin and with globulin binding sex hormones (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 V d of levonorgestrel is about 184 liters after a single dose.
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 equilibrium concentration, the clearance rate is reduced to about 0.7 ml / min / kg.
Metabolism

Levonorgestrel is almost completely metabolized.
The clearance rate from 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 T 1/2 is about 20-23 hours. In unchanged 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.
Ethinylestradiol

Suction

After ingestion, ethinylestradiol is rapidly and completely absorbed.
C max in blood plasma, equal to about 95 pg / ml, is achieved in 1-2 hours. During the absorption and "first passage" through the liver, ethinyl estradiol is metabolized, resulting in an average bioavailability of about 45% (individual differences within 20-65%).
Distribution

Ethinyl estradiol is almost completely (approximately 98%), although non-specific, binds to albumin.
Ethinylestradiol induces synthesis of SHBG. The apparent V d ofethinylestradiol is 2.8-8.6 l / kg.
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.
Considering the variable final T 1/2 and daily oral intake, the equilibrium concentration is achieved in about one week.
Metabolism

Ethinyl estradiol undergoes 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 the blood plasma is 2.3-7 ml / min / kg.
Excretion

Reduction in the concentration of ethinyl estradiol in blood plasma is biphasic;
the first phase is characterized by T 1/2 about 1 h, the second - 10-20 h. 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 T 1/2 about 24 hours.
INDICATIONS

- Prevention of unwanted pregnancy (contraception);

- hormone-dependent functional disorders of the menstrual cycle.

DOSING MODE

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 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 break.

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:
- taking the drug should never be interrupted 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 must 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 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 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:
1) 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 spotting and bleeding "breakthrough" during the taking of tablets;
2) 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, there may be spotting 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 the woman not having a bleeding "cancellation", and further, smearing and bleeding "breakthrough" during the reception of the second package of Oralcon (as well as in the case of a delay in the onset 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 EFFECT

Possible: nausea, vomiting, headache, engorgement of the mammary glands, weight gain, decreased libido and mood, coarsening of the voice, the appearance of intermenstrual bleeding, in some cases - eyelid edema, conjunctivitis, visual impairment, discomfort when wearing contact lenses (these phenomena are temporary and disappear after withdrawal 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.

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 on the background of admission, the drug should be immediately withdrawn:
- Thrombosis (venous and arterial) and thromboembolism at present or in the anamnesis (including deep vein thrombosis, pulmonary embolism, myocardial infarction), cerebrovascular disorders;

- conditions preceding thrombosis (including transient ischemic attacks, angina pectoris) at present or in the anamnesis;

- multiple or expressed risk factors for venous or arterial thrombosis;

- migraine with focal neurologic symptoms at present or in anamnesis;

- diabetes mellitus with vascular complications;

- pancreatitis with severe hypertriglyceridemia at present or in the anamnesis;

- liver failure and severe liver disease (before the normalization of liver function tests);

- Liver tumors (benign or malignant) at present or in the anamnesis;

- identified hormone-dependent malignant diseases (including genitals or mammary glands) or suspicion of them;

bleeding from the vagina of unknown origin;

- Pregnancy or suspicion of it;

- the period of lactation (breastfeeding);

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

- Hypersensitivity to the components of the drug.

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 in each case should be correlated:

- risk factors for thrombosis and thromboembolism (smoking, thrombosis, myocardial infarction or cerebrovascular accident at a young age in any of the next of kin, obesity, dyslipoproteinemia, arterial hypertension, migraine without focal neurological symptoms, heart valve disease, heart rhythm disturbances, prolonged immobilization, extensive surgical interventions, extensive trauma);

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

- liver disease of mild and moderate severity, with normal liver function tests;

- diseases that first appeared or worsened during pregnancy or on the background of previous reception of sex hormones (for example, jaundice, cholestasis, gallbladder disease, otosclerosis with hearing impairment, porphyria, herpes pregnant, 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 in pregnancy and during breastfeeding.
If the pregnancy is detected during the oral medication, then it should be immediately same cancel.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 in the period of breastfeeding.
A small amount of sex hormones and / or their metabolites can be excreted in breast milk.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Is contraindicated in liver failure and severe liver disease (before normalization of liver function tests), liver tumors (benign or malignant) currently or history.
Precautions for liver mild and moderate severity (with normal values in liver function tests).
SPECIAL INSTRUCTIONS

If any of the conditions / diseases / risk factors mentioned below are currently available, it is necessary to carefully correlate the potential risks and expected benefits of the use of combined oral contraceptives, in each individual case and discuss it with the woman before she decides to start taking the drug. In the event of aggravation, the gain or the first manifestation of any of these conditions or risk factors, the woman should consult with your doctor, who can decide whether to cancel the drug.
Diseases of the cardiovascular system
Epidemiological studies indicate a relationship between the use of combined oral contraceptives and increased incidence of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disturbances) when receiving combined oral contraceptives. These diseases are rare. The risk of developing venous thromboembolism (VTE) is greatest in the first year of taking these drugs. The increased risk is present after initial use of combined oral contraceptives or resume reception of the same or different combined oral contraceptives (after the interval between doses of the drug in 4 weeks or more).Data from a large prospective study involving 3 groups of female volunteers suggest that this increased risk is present mainly in the first 3 months.
The overall risk of VTE in women taking low-dose combined oral contraceptives (<50 micrograms ethinyl estradiol) are 2-3 times higher than in non-pregnant women who are not taking contraceptives combined, however, this risk is lower than the risk of VTE at pregnancy and childbirth. VTE may be fatal (1 - 2% of cases). VTE, manifested as deep vein thrombosis or pulmonary embolism may occur when using any combined oral contraceptives.
Very rarely using COCs thrombosis occurs in other blood vessels, for example, hepatic, mesenteric, renal, and cerebral arteries veins or the retinal vessels. Consensus about the connection between the occurrence of these events and the use of combined oral contraceptives available.
The risk of thrombosis (venous and / or arterial) and thromboembolism is increased:
- age;
- smokers with increasing number of cigarettes or increasing age the risk increases, especially in women over 35 years old);
- if there is a family history (eg venous or arterial thromboembolism ever in close relatives or parents at a relatively young age). In the case of hereditary or acquired predisposition, the woman should be assessed and the appropriate specialist to address the issue of the possibility of using combined oral contraceptives;
- obesity (BMI over 30 kg / m);
- when dislipoproteinemia;
- arterial hypertension;
- migraine;
- in diseases of the heart valves;
- atrial fibrillation;
- with prolonged immobilization, major surgery, any surgery to the legs, or major trauma. In these situations it is desirable to stop taking combined oral contraceptives (in the case of planned operation, at least 4 weeks prior to it) and not to resume reception at 2 weeks after the immobilization.
The possible role of varicose veins and superficial thrombophlebitis in venous thromboembolism is controversial. It should take into account the increased risk of thromboembolism during the postpartum period. Peripheral circulatory disorders also may occur in diabetes, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel diseases (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 risks and benefits should be taken into account that adequate treatment of the relevant condition may reduce the associated risk of thrombosis. It should also be borne in mind that the risk of thrombosis and thromboembolism in pregnancy is higher than when taking low-dose oral contraceptives (<0.05 mg etnnilestradiola).
Tumors

The most significant risk factor for cervical cancer is persistent papilloma virus infection. There are reports of some increase in the risk of cervical cancer in long-term use of combined oral contraceptives. Communication with the reception of combined oral contraceptives has not been proved.
Reserved controversy as to what extent these findings associated with screening for cervical abnormalities or features with sexual behavior (less frequent use of barrier methods of contraception). A meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of breast cancer diagnosed in women taking combined oral contraceptives currently (relative risk 1.24), increased risk disappears gradually within 10 years after discontinuation of drugs.
Due to the fact that breast cancer is rare in women under 40 years, the increase in diagnosed breast cancer in women taking combined oral contraceptives are currently taking or have recently, is insignificant in relation to the total risk of the disease. His connection with the reception of combined oral contraceptives has not been proved. The observed increase in risk may also be the result of earlier detection of breast cancer in women who use a combined oral contraceptives. In women, ever use a combined oral contraceptives, the cancer is detected at an earlier stage than in women, never let them apply. In rare cases, against the background of the use of combined oral contraceptives saw the development of benign,and in extremely rare - malignant tumors of the liver, which in some cases lead to life-threatening intraabdominal bleeding. In case of occurrence of severe abdominal pain, signs of liver enlargement or intraabdominal hemorrhage this should be considered in the differential diagnosis.
Other states

Women with hypertriglyceridemia (or the presence of this condition have a family history) may increase the risk of developing pancreatitis while taking combined oral contraceptives.
Although a slight increase in blood pressure have been reported in many women taking COCs, clinically relevant increases were rare. However, if while taking combined oral contraceptives develops persistent, clinically significant increase in blood pressure, should be discontinued these drugs and begin treatment of hypertension.
Receiving COCs can be continued, if using antihypertensive therapy achieved normal values of arterial pressure.
The following conditions have been reported to develop or worsen both during pregnancy and when taking combined oral contraceptives, but their connection with the reception of combined oral contraceptives has not been proven: jaundice and / or pruritus related to cholestasis; the formation of gallstones;
porphyria; systemic lupus erythematosus; hemolytic-uremic syndrome; Sydenham's chorea; herpes gestationis; hearing loss associated with otosclerosis. Cases of Crohn's disease and ulcerative colitis against application of combined oral contraceptives are also described.
In women with hereditary forms of angioedema exogenous estrogens may induce or worsen symptoms of angioedema.
Acute or chronic disturbances of liver function may require the cancellation of combined oral contraceptives as long as liver function tests have not returned to normal. Recurrent cholestatic jaundice that develops for the first time during pregnancy or previous use of sex hormones, requires
discontinuation of COCs.
Although combined oral contraceptives may influence insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetics using low-dose combined oral contraceptives (<50 micrograms ethinyl estradiol). However, women with diabetes should be carefully observed while taking combined oral contraceptives.
Sometimes it can develop chloasma, especially in women with a history of chloasma during pregnancy. Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to sunlight and ultraviolet radiation.
Effect on bleeding patterns
In patients receiving combined oral contraceptives may experience irregular bleeding (spotting or breakthrough bleeding), especially during the first few months of use. Therefore, evaluation of any irregular bleeding should be performed only after a period of adaptation of approximately 3 cycles. If irregular bleeding recur or develop after previous regular cycles, you should conduct a thorough examination to exclude malignancy or pregnancy. Some women during the tablet-free interval may not develop bleeding "cancel". If combined oral contraceptives are taken according to the directions, it is unlikely that the woman is pregnant. Nevertheless,if before COCs were taken regularly or if no two consecutive withdrawal bleeding to continue taking the drug should be excluded pregnancy.
Impact on the ability to drive vehicles and manage mechanisms

Does not affect.
OVERDOSE

No cases of overdose have been reported.
Possible signs of overdose include nausea, vomiting, spotting from the vagina or metrorrhagia.
Treatment: No specific antidote, treatment - symptomatic.
DRUG INTERACTION

Some drugs may decrease the effectiveness of the drug: antiepileptic drugs (including primidone, phenytoin, barbiturates, carbamazepine, oxcarbazepine, topiramate, felbamate), antituberculosis agents (including rifampin, rifabutin), drugs to treat HIV infection (including ritonavir, nevirapine); medicaments based on a Hypericum perforatum.
Reduced contraceptive efficacy can be observed, and while the use of certain antimicrobial drugs (ampicillin, rifampicin, chloramphenicol, neomycin, polymyxin B, sulfonamides, tetracyclines), which is associated with a change in the microflora in the intestine.
When receiving a progestogen-estrogen drugs may require correction dosing regimen hypoglycemic drugs and anticoagulants.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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