Regulon from the Hungarian pharmaceutical company GEDEON RICHTER is a monophasic tablet contraceptive. When the first contraceptives were synthesized in the fifties of the last century, hardly anyone could have imagined that their therapeutic effect on the female body would be valued almost more than the contraceptive effect. Long-term clinical studies have shown that patients taking combined tablet contraceptives were much less likely to encounter not only gynecological, but also general somatic problems. In the course of improving the quantitative and qualitative composition of these drugs, an effective regimen was found, called prolonged, when the drug is taken continuously, without the traditional weekly interval. At the same time, it is possible to achieve not only the prevention of unplanned pregnancy, but also reduce the risk of developing many diseases. One of the drugs suitable for use in this regimen is Regulon, a combination of ethinyl estradiol and desogestrel (III generation progestogen). Even a relatively small amount of desogestrel is more than enough to suppress ovulation (60 mcg of the substance per day suppresses ovulation by 100%). Back in the late 90s of the last century, it was noted that etonogestrel, an active metabolite of desogestrel, has extremely high affinity for progesterone receptors, has high progestogenic activity and exhibits a powerful antigonadotropic effect.
One Regulon tablet includes 150 mcg of desogestrel, i.e. 2.5 times the amount required to completely suppress ovulation. Another component of the contraceptive effect of the drug is its ability to inhibit the formation of gonadotropins. In addition to this, due to changes in the rheological properties of mucus, the movement of sperm along the cervical canal slows down, and changes in the thickness and structure of the endometrium do not allow a fertilized egg to implant on its mucosa. The second component of the drug, ethinyl estradiol, is an artificial analogue of the female sex hormone estradiol produced in the body. Regulon improves the lipid profile, which is manifested in an increase in the concentration of high-density lipoproteins (“good” cholesterol) while maintaining a constant content of low-density lipoproteins (“bad” cholesterol). Taking the drug can significantly reduce blood loss during menstruation (with existing menorrhagia), improve the condition of the skin, and prevent the occurrence of acne. Before using Regulon, you must undergo an in-depth medical examination (history collection, blood pressure measurement, laboratory tests, gynecological examination). Such medical monitoring should be carried out every six months during the period of use of the drug.
Pharmacology
Monophasic oral contraceptive. The main contraceptive effect is to inhibit the synthesis of gonadotropins and suppress ovulation. In addition, by increasing the viscosity of cervical mucus, the movement of sperm through the cervical canal slows down, and changes in the condition of the endometrium prevent the implantation of a fertilized egg.
Ethinyl estradiol is a synthetic analogue of endogenous estradiol.
Desogestrel has a pronounced gestagenic and antiestrogenic effect, similar to endogenous progesterone, and weak androgenic and anabolic activity.
Regulon has a beneficial effect on lipid metabolism: it increases the concentration of HDL in the blood plasma without affecting the content of LDL.
When taking the drug, the loss of menstrual blood is significantly reduced (in case of initial menorrhagia), the menstrual cycle is normalized, and a beneficial effect on the skin is noted, especially in the presence of acne vulgaris.
Pharmacokinetics
Desogestrel
Suction
Desogestrel is quickly and almost completely absorbed from the gastrointestinal tract and is immediately metabolized into 3-keto-desogestrel, which is a biologically active metabolite of desogestrel.
Cmax is reached after 1.5 hours and is 2 ng/ml. Bioavailability - 62-81%.
Distribution
3-keto-desogestrel binds to plasma proteins, mainly albumin and sex hormone binding globulin (SHBG). V d is 1.5 l/kg. C ss is established by the second half of the menstrual cycle. The level of 3-keto-desogestrel increases 2-3 times.
Metabolism
In addition to 3-keto-desogestrel (which is formed in the liver and in the intestinal wall), other metabolites are formed: 3α-OH-desogestrel, 3β-OH-desogestrel, 3α-OH-5α-H-desogestrel (first phase metabolites). These metabolites do not have pharmacological activity and are partially converted, through conjugation (the second phase of metabolism), into polar metabolites - sulfates and glucuronates. Clearance from blood plasma is about 2 ml/min/kg body weight.
Removal
T1/2 of 3-keto-desogestrel is 30 hours. Metabolites are excreted in the urine and feces (in a ratio of 4:6).
Ethinyl estradiol
Suction
Ethinyl estradiol is quickly and completely absorbed from the gastrointestinal tract. Cmax is achieved 1-2 hours after taking the drug and is 80 pg/ml. The bioavailability of the drug due to presystemic conjugation and the “first pass” effect through the liver is about 60%.
Distribution
Ethinyl estradiol is completely bound to plasma proteins, mainly albumin. Vd is 5 l/kg. C ss is established by the 3-4th day of administration, while the level of ethinyl estradiol in the serum is 30-40% higher than after a single dose of the drug.
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 excreted into bile and enter the enterohepatic circulation. Clearance from blood plasma is about 5 ml/min/kg body weight.
Removal
T1/2 of ethinyl estradiol averages about 24 hours. About 40% is excreted in the urine and about 60% in feces.
Release form
White or almost white, film-coated tablets, round, biconvex, marked “P8” on one side and “RG” on the other.
Excipients: α-tocopherol, magnesium stearate, colloidal silicon dioxide, stearic acid, povidone, potato starch, lactose monohydrate.
Film shell composition: propylene glycol, macrogol 6000, hypromellose.
21 pcs. - blisters (1) - cardboard packs.
21 pcs. - blisters (3) - cardboard packs.
Dosage
The drug is prescribed orally.
Taking pills starts on the 1st day of the menstrual cycle. Prescribe 1 tablet/day for 21 days, if possible at the same time of day. After taking the last tablet from the package, take a 7-day break, during which menstrual-like bleeding occurs due to drug withdrawal. The next day after a 7-day break (4 weeks after taking the first tablet, on the same day of the week), resume taking the drug from the next package, also containing 21 tablets, even if the bleeding has not stopped. This pill regimen is followed as long as there is a need for contraception. If you follow the rules of administration, the contraceptive effect remains during the 7-day break.
First dose of the drug
The first tablet should be taken on the first day of the menstrual cycle. In this case, it is not necessary to use additional methods of contraception. You can start taking pills from the 2-5th day of menstruation, but in this case, in the first cycle of using the drug, you must use additional methods of contraception in the first 7 days of taking the pills.
If more than 5 days have passed since the start of menstruation, you should delay starting the drug until your next menstruation.
Taking the drug after childbirth
Women who are not breastfeeding can start taking the pill no earlier than 21 days after giving birth, after consulting with their doctor. In this case, there is no need to use other methods of contraception. If there has already been sexual contact after childbirth, then taking the pills should be postponed until the first menstruation. If a decision is made to take the drug later than 21 days after birth, then additional methods of contraception must be used in the first 7 days.
Taking the drug after an abortion
After an abortion, in the absence of contraindications, you should start taking pills from the first day after surgery, and in this case there is no need to use additional methods of contraception.
Switching from another oral contraceptive
When switching from another oral drug (21- or 28-day): it is recommended to take the first Regulon tablet the day after completing the course of the 28-day package of the drug. After completing the 21-day course, you must take the usual 7-day break and then start taking Regulon. There is no need to use additional methods of contraception.
Switching to Regulon after using oral hormonal drugs containing only progestogen ("mini-pills")
The first Regulon tablet should be taken on the 1st day of the cycle. There is no need to use additional methods of contraception.
If menstruation does not occur while taking the mini-pill, then after excluding pregnancy, you can start taking Regulon on any day of the cycle, but in this case, in the first 7 days it is necessary to use additional methods of contraception (using a cervical cap with spermicidal gel, a condom, or abstinence from sexual intercourse). The use of the calendar method in these cases is not recommended.
Delay of the menstrual cycle
If there is a need to delay menstruation, you must continue taking the tablets from the new package, without a 7-day break, according to the usual regimen. When menstruation is delayed, breakthrough or spotting bleeding may occur, but this does not reduce the contraceptive effect of the drug. Regular use of Regulon can be resumed after the usual 7-day break.
Missed pills
If a woman forgot to take a pill on time, and no more than 12 hours have passed since the omission, she needs 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 a missed 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 in the first or second week of the cycle, you need to take 2 tablets. the next day and then continue regular use using additional methods of contraception until the end of the cycle.
If you miss a pill in the third week of the cycle, you should take the forgotten pill, continue taking it regularly and 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 miss a pill and therefore the use of additional methods of contraception is recommended.
Vomiting/diarrhea
If vomiting or diarrhea occurs after taking the drug, then absorption of the drug may be inadequate. If the symptoms stop within 12 hours, then you need to take one more tablet. After this, you should continue taking the tablets as usual. If vomiting or diarrhea continues for more than 12 hours, then it is necessary to use additional methods of contraception during vomiting or diarrhea and for the next 7 days.
Overdose
Symptoms: nausea, vomiting, in girls - bleeding from the vagina.
Treatment: in the first 2-3 hours after taking the drug in a high dose, gastric lavage is recommended. There is no specific antidote, treatment is symptomatic.
Interaction
Medicines 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 achieved 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 Regulon (the mechanism of interaction has not been established). If co-administration 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 - within 28 days) after discontinuation of the drug.
Oral contraceptives may decrease carbohydrate tolerance and increase the need for insulin or oral antidiabetic agents.
Side effects
Side effects requiring 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.
From the senses: hearing loss caused by otosclerosis.
Other: hemolytic-uremic syndrome, porphyria; rarely - exacerbation of reactive systemic lupus erythematosus; very rarely - Sydenham's chorea (passing after discontinuation of the drug).
Other side effects that are more common but less severe. The advisability of continuing to use the drug is decided individually after consultation with a doctor, based on the benefit/risk ratio.
From the reproductive system: acyclic bleeding/bloody discharge from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, the development of inflammatory processes in the vagina, candidiasis, tension, pain, enlarged mammary glands, galactorrhea.
From the digestive system: nausea, vomiting, Crohn's disease, ulcerative colitis, the 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.
On the part of the organ of vision: increased sensitivity of the cornea (when wearing contact lenses).
Metabolism: fluid retention in the body, change (increase) in body weight, decreased tolerance to carbohydrates.
Other: allergic reactions.
Indications
Contraception.
Contraindications
- the presence of severe and/or multiple risk factors for venous or arterial thrombosis (including severe or moderate arterial hypertension with blood pressure ≥ 160/100 mm Hg);
- presence or indication in history of precursors of thrombosis (including transient ischemic attack, angina pectoris);
- migraine with focal neurological symptoms, incl. in the anamnesis;
- venous or arterial thrombosis/thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the leg, pulmonary embolism) currently or in history;
- a history of venous thromboembolism;
- diabetes mellitus (with angiopathy);
- pancreatitis (including a history), accompanied by severe hypertriglyceridemia;
- dyslipidemia;
- severe liver diseases, cholestatic jaundice (including during pregnancy), hepatitis, incl. history (before normalization of functional and laboratory parameters and within 3 months after their normalization);
- jaundice when taking GCS;
- gallstone disease currently or in history;
- Gilbert's syndrome, Dubin-Johnson syndrome, Rotor syndrome;
- liver tumors (including history);
- severe itching, otosclerosis or its progression during a previous pregnancy or taking corticosteroids;
- hormone-dependent malignant neoplasms of the genital organs and mammary glands (including if they are suspected);
- vaginal bleeding of unknown etiology;
- smoking over the age of 35 (more than 15 cigarettes per day);
- pregnancy or suspicion of it;
- lactation period;
- hypersensitivity to the components of the drug.
The drug should be prescribed with caution in conditions that increase the risk of developing venous or arterial thrombosis/thromboembolism: age over 35 years, smoking, family history, obesity (body mass index more than 30 kg/m2), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular heart defects, atrial fibrillation, prolonged immobilization, extensive surgery, surgery on the lower extremities, severe trauma, varicose veins and superficial thrombophlebitis, the postpartum period, the presence of severe depression (including a history), changes in biochemical parameters ( activated protein C resistance, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, including lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease , ulcerative colitis, sickle cell anemia, hypertriglyceridemia (incl. family history), acute and chronic liver diseases.
Features of application
Use during pregnancy and breastfeeding
The use of the drug during pregnancy and breastfeeding is contraindicated.
During breastfeeding, it is necessary to resolve the issue of either discontinuing the drug or stopping breastfeeding.
Use for liver dysfunction
Contraindicated in liver failure.
The drug should be prescribed with caution for acute and chronic liver diseases.
Use for renal impairment
With caution and only after a thorough assessment of the benefits and risks of use, the drug should be prescribed for renal failure (including a history).special instructions
Before starting to use the drug, it is necessary to conduct a general medical examination (detailed family and personal history, blood pressure measurement, laboratory tests) and gynecological examination (including examination of the mammary glands, pelvic organs, cytological analysis of a cervical smear). Such examinations during the period of taking the drug are carried out regularly, every 6 months.
The drug is a reliable contraceptive: the Pearl index (an indicator of the number of pregnancies occurring during the use of a contraceptive method in 100 women over 1 year) when used correctly is about 0.05.
In each case, before prescribing hormonal contraceptives, the benefits or possible negative effects of their use are individually assessed. This issue must be discussed with the patient, who, after receiving the necessary information, will make the final decision on the preference for hormonal or any other method of contraception.
The woman's health condition must be carefully monitored. If any of the following conditions/diseases appear or worsen while taking the drug, you must 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 and renal failure;
- epilepsy;
- migraine;
- the 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 B 6 can be used for correction);
- sickle cell anemia, because in some cases (for example, infections, hypoxia), estrogen-containing drugs for this pathology can provoke thromboembolism;
- the appearance of abnormalities in laboratory tests assessing liver function.
Thromboembolic diseases
Epidemiological studies have shown that there is a connection between taking oral hormonal contraceptives and an increased risk of developing 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).
Some researchers suggest that the likelihood of venous thromboembolic disease is greater with drugs containing desogestrel and gestodene (third generation drugs) than with drugs containing levonorgestrel (second generation drugs).
The incidence of spontaneous occurrence of new cases of venous thromboembolic disease in healthy non-pregnant women not taking oral contraceptives is about 5 cases per 100 thousand women per year. When using second generation drugs - 15 cases per 100 thousand women per year, and when using third generation drugs - 25 cases per 100 thousand women per year.
When using oral contraceptives, arterial or venous thromboembolism of the hepatic, mesenteric, renal or retinal vessels is very rarely observed.
The risk of arterial or venous thromboembolic disease increases:
- with age;
- when smoking (heavy smoking and age over 35 years are 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;
- for obesity (body mass index more than 30 kg/m2);
- with dislipoproteinemia;
- with arterial hypertension;
- for diseases of the heart valves complicated by hemodynamic disorders;
- with atrial fibrillation;
- with diabetes mellitus complicated by vascular lesions;
- with prolonged immobilization, after major surgery, after surgery on the lower extremities, after severe trauma.
In these cases, it is assumed to temporarily stop using the drug (no later than 4 weeks before surgery, and resume no earlier than 2 weeks after remobilization).
Women after childbirth have an increased risk of venous thromboembolic disease.
It should be taken into account that diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia increase the risk of developing venous thromboembolic diseases.
It should be taken into account that resistance to activated protein C, hyperhomocysteinemia, protein C and S deficiency, antithrombin III deficiency, and the presence of antiphospholipid antibodies increase the risk of developing arterial or venous thromboembolic diseases.
When assessing the benefit/risk ratio of taking the drug, it should be taken into account that targeted treatment of this condition reduces the risk of thromboembolism. Symptoms of thromboembolism are:
- sudden chest pain that radiates to the left arm;
- sudden shortness of breath;
- any unusually severe headache that continues 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 severe numbness of half the body, movement disorders, severe unilateral pain in the calf muscle, acute abdomen.
Tumor diseases
Some studies have reported an increased incidence of cervical cancer in women who took hormonal contraceptives for a long time, but the results of the studies are inconsistent. Sexual behavior, infection with the human papillomavirus 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 the risk of breast cancer among women taking oral hormonal contraceptives, but the higher detection rate of breast cancer may have been associated with more regular medical screening. Breast cancer is rare among women under 40, whether they are taking hormonal birth control or not, and increases with age. Taking pills can be considered one of many risk factors. However, the 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 benign or malignant liver tumors in women taking hormonal contraceptives for a long time. This should be kept in mind when differentially assessing abdominal pain, which may be associated with an increase in liver size or intraperitoneal bleeding.
Chloasma can develop in women with a history of this disease during pregnancy. Those women who are at risk of developing chloasma should avoid contact with sunlight or ultraviolet radiation while taking Regulon.
Efficiency
The effectiveness of the drug may be reduced 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 concomitantly taking another drug that 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, spotting or breakthrough bleeding appears, in such cases it is advisable to continue taking the tablets until they run out in the next package. If at the end of the second cycle menstrual-like bleeding does not begin or acyclic bleeding does not stop, stop taking the pills and resume it only after pregnancy has been ruled out.
Changes in laboratory parameters
Under the influence of oral contraceptive pills - due to the estrogen component - the level of some laboratory parameters (functional indicators of the liver, kidneys, adrenal glands, thyroid gland, hemostasis indicators, levels of lipoproteins and transport proteins) may change.
Additional Information
After acute viral hepatitis, the drug should be taken after normalization of liver function (no earlier than 6 months).
With diarrhea or intestinal disorders, vomiting, the contraceptive effect may be reduced. While continuing to take 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 in women over 35 years of age) and on the number of cigarettes smoked.
The woman should be warned that the drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive a car or operate machinery.
Regulon is a contraceptive containing estrogen and gestagen. The drug has a contraceptive, estrogen-progestogenic effect.
It is characterized by the ability to inhibit the production of gonadotropin, preventing the onset of ovulation and the penetration of active sperm into the uterine cavity.
Regulon is considered an effective oral contraceptive and is used as a means of preventing unwanted pregnancy. The drug is also used to normalize the menstrual cycle and treat dysfunctional uterine bleeding.
Clinical and pharmacological group
Monophasic oral contraceptive.
Terms of sale from pharmacies
Can be purchased with a doctor's prescription.
Price
How much does Regulon cost in pharmacies? The average price is 500 rubles.
Composition and release form
The dosage form of Regulon is film-coated tablets: almost white or white, biconvex, round, marked “P8” on one side, “RG” on the other (21 pcs. in blisters, 1 or 3 blisters in a cardboard pack ).
Active ingredients in 1 tablet:
- Desogestrel – 0.15 mg;
- Ethinyl estradiol – 0.03 mg.
Additional components: magnesium stearate, α-tocopherol, lactose monohydrate, stearic acid, colloidal silicon dioxide, potato starch, povidone.
Film coating: propylene glycol, hypromellose, macrogol 6000.
pharmachologic effect
Regulon tablets, due to the active ingredients included in their composition (ethinyl estradiol is an analogue of estrogen, and desogestrel is an analogue of progesterone), have a contraceptive effect. They suppress the synthesis of gonadotropin hormones and the process of ovulation (the release of a mature egg). In addition, the active substances make it difficult for sperm to move in the cervical canal due to thickening of the cervical mucus and change the endometrial epithelium (the inner layer of the uterine wall), which interferes with the process of implantation (attachment of a fertilized egg).
The drug also has a beneficial effect on the lipid (fat) metabolism of a woman’s body, increasing the concentration of high-density lipoproteins, normalizing the menstrual cycle, and reducing the intensity of menstrual bleeding.
Indications for use
Regulon is used to prevent unwanted pregnancy.
Contraindications
Absolute:
- Dyslipidemia;
- Gallstone disease currently or in history;
- Pregnancy (including suspected);
- Breastfeeding period;
- Smoking over 35 years of age (more than 15 cigarettes per day);
- Thrombosis (arterial or venous) or thromboembolism currently or in history, including deep vein thrombosis of the leg, stroke, myocardial infarction, pulmonary embolism;
- Severe liver damage, hepatitis (including history), cholestatic jaundice, including that developed during a previous pregnancy (before normalization of laboratory and functional parameters and for three months after their return to normal);
- Jaundice caused by taking glucocorticoids (medicines containing steroid hormones);
- Liver tumors (including history);
- Dubin-Johnson, Gilbert, Rotor syndromes;
- Malignant hormone-dependent neoplasms of the mammary glands and genital organs (diagnosed or suspected);
- Severe itching, otosclerosis or its aggravation when taking glucocorticosteroids or during a previous pregnancy;
- Vaginal bleeding of unknown origin;
- Clearly expressed and/or multiple risk factors for thrombosis of veins or arteries (including moderate or severe arterial hypertension with blood pressure readings ≥ 160/100 mm Hg);
- Precursors of thrombosis (including angina pectoris, transient ischemic attack), including data in the anamnesis;
- Venous thromboembolism in relatives;
- Migraine accompanied by focal neurological symptoms (including indications in the anamnesis);
- Pancreatitis occurring with severe hypertriglyceridemia (including a history);
- Diabetes mellitus complicated by angiopathy;
- Hypersensitivity to the components of the product.
Relative (must be used with extreme caution due to the high risk of arterial or venous thrombosis/thromboembolism):
- Epilepsy;
- Migraine;
- Obesity (body mass index more than 30 kg/m²);
- Age over 35 years;
- Arterial hypertension;
- Family history;
- Dyslipoproteinemia;
- Valvular heart defects, atrial fibrillation;
- Postpartum period;
- Ulcerative colitis, Crohn's disease;
- Sickle cell anemia;
- Liver diseases in acute and chronic form;
- Hypertriglyceridemia (including indications in family history);
- Extensive surgery, surgery on the lower extremities;
- Prolonged immobilization;
- Severe injury;
- Varicose veins and superficial thrombophlebitis;
- Severe depression (including history);
- Diabetes mellitus without vascular disorders;
- Changes in biochemical parameters (protein C or S deficiency, activated protein C resistance, antithrombin III deficiency, hyperhomocysteinemia, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant);
- Systemic lupus erythematosus (SLE).
Prescription during pregnancy and lactation
Pregnancy is an absolute contraindication to the use of Regulon. During lactation, you should stop taking the drug or stop breastfeeding.
This is due to the fact that taking pills in the postpartum period provokes a decrease in the amount of milk, impairs lactation and negatively affects the growth of the child.
Pregnancy after Regulon birth control pills
The contraceptive effect of Regulon tablets is associated with the ability of the synthetic analogues of the endogenous hormones estradiol and progestogens included in its composition to prevent the release of a mature egg from the follicle.
The drug can be used as a means of contraception for several years. However, many women are concerned about whether this will somehow affect reproductive function and subsequent pregnancy.
Gynecologists answer such questions as follows: if you take the pills correctly (that is, take them according to the regimen described in the instructions and in compliance with all the recommendations of your doctor), then after taking them you can plan a pregnancy. Typically, pregnancy after Regulon occurs after about 6 months of active sexual activity.
For a woman who is planning a child, doctors recommend stopping taking the drug at least three months before conception.
Dosage and method of administration
As indicated in the instructions for use, Regulon is prescribed orally.
Taking pills starts on the 1st day of the menstrual cycle. Prescribe 1 tablet/day for 21 days, if possible at the same time of day. After taking the last tablet from the package, take a 7-day break, during which menstrual-like bleeding occurs due to drug withdrawal. The next day after a 7-day break (4 weeks after taking the first tablet, on the same day of the week), resume taking the drug from the next package, also containing 21 tablets, even if the bleeding has not stopped. This pill regimen is followed as long as there is a need for contraception. If you follow the rules of administration, the contraceptive effect remains during the 7-day break.
First dose of the drug:
- The first tablet should be taken on the first day of the menstrual cycle. In this case, it is not necessary to use additional methods of contraception. You can start taking pills from the 2-5th day of menstruation, but in this case, in the first cycle of using the drug, you must use additional methods of contraception in the first 7 days of taking the pills. If more than 5 days have passed since the start of menstruation, you should delay starting the drug until your next menstruation.
Taking the drug after an abortion:
- After an abortion, in the absence of contraindications, you should start taking pills from the first day after surgery, and in this case there is no need to use additional methods of contraception.
Taking the drug after childbirth:
- Women who are not breastfeeding can start taking the pill no earlier than 21 days after giving birth, after consulting with their doctor. In this case, there is no need to use other methods of contraception. If there has already been sexual contact after childbirth, then taking the pills should be postponed until the first menstruation. If a decision is made to take the drug later than 21 days after birth, then additional methods of contraception must be used in the first 7 days.
Switching from another oral contraceptive:
- When switching from another oral drug (21- or 28-day): it is recommended to take the first Regulon tablet the day after completing the course of the 28-day package of the drug. After completing the 21-day course, you must take the usual 7-day break and then start taking Regulon. There is no need to use additional methods of contraception.
Switching to Regulon after using oral hormonal drugs containing only progestogen (“mini-pills”):
- The first Regulon tablet should be taken on the 1st day of the cycle. There is no need to use additional methods of contraception. If menstruation does not occur while taking the “mini-pill”, then after excluding pregnancy, you can start taking Regulon on any day of the cycle, but in this case, in the first 7 days it is necessary to use additional methods of contraception (using a cervical cap with spermicidal gel, a condom, or abstinence from sexual intercourse). The use of the calendar method in these cases is not recommended.
Delay of the menstrual cycle:
- If there is a need to delay menstruation, you must continue taking the tablets from the new package, without a 7-day break, according to the usual regimen. When menstruation is delayed, breakthrough or spotting bleeding may occur, but this does not reduce the contraceptive effect of the drug. Regular use of Regulon can be resumed after the usual 7-day break.
Vomiting/diarrhea:
- If vomiting or diarrhea occurs after taking the drug, then absorption of the drug may be inadequate. If the symptoms stop within 12 hours, then you need to take one more tablet. After this, you should continue taking the tablets as usual. If vomiting or diarrhea continues for more than 12 hours, then it is necessary to use additional methods of contraception during vomiting or diarrhea and for the next 7 days.
Missed pills
If a woman forgot to take a pill on time, and no more than 12 hours have passed since the omission, she needs 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 a missed 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 in the first or second week of the cycle, you need to take 2 tablets. the next day and then continue regular use using additional methods of contraception until the end of the cycle.
If you miss a pill in the third week of the cycle, you should take the forgotten pill, continue taking it regularly and 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 miss a pill and therefore the use of additional methods of contraception is recommended.
Side effect
Regulon may cause the following side effects:
- From the senses: partial hearing loss associated with otosclerosis.
- Other: Sydenham's chorea, hemolytic-uremic syndrome, porphyria.
- From the cardiovascular system: arterial or venous thromboembolism, arterial hypertension.
Less common side effects:
- From the central nervous system: headaches, frequent mood swings, depression.
- Dermatological reactions: rash, nodular or exudative erythema.
- From the organs of vision: sensitivity of the cornea when wearing contact lenses.
- From the metabolic side: fluid stagnation in the body, weight gain or decreased tolerance to carbohydrates.
- From the digestive system: nausea, ulcerative colitis, vomiting, Crohn's disease, cholestasis, the occurrence or exacerbation of jaundice.
- From the reproductive system: inflammatory processes of the vagina, enlargement of the mammary glands or painful sensations in them, acyclic bleeding from the vagina, galactorrhea, candidiasis.
- Other: allergic reactions.
Overdose
If the recommended therapeutic dose of Regulon tablets is exceeded, nausea, vomiting may develop, and young women may experience bleeding from the vagina. Treatment consists of washing the stomach, if no more than 3 hours have passed since the overdose, washing the intestines, taking sorbents (activated carbon), and carrying out symptomatic therapy in a medical hospital.
special instructions
It is not recommended to start taking the drug without consulting a gynecologist, since Regulon can only be used as prescribed by a doctor based on the results of a preliminary general medical and gynecological examination. The doctor must study in detail both the general condition of the woman (family and personal history, laboratory tests, blood pressure), and the results of an examination of the pelvic organs, mammary glands, and cytological analysis of a cervical smear. The decision to use hormonal oral contraceptive therapy should be weighed, taking into account all the benefits and negative effects.
The woman must be warned about the need for regular (once every 6 months) preventive examination while taking the pills. When diseases of the hemostatic system appear or worsen, abnormalities in laboratory parameters of liver function, signs of renal and/or cardiovascular failure, migraine, epilepsy, diabetes mellitus not complicated by vascular disorders, severe depression, estrogen-dependent tumors or gynecological diseases, sickle cell anemia The drug should be stopped and non-hormonal methods of contraception should be used.
The risk of developing thromboembolic diseases while taking hormonal contraceptives exists, but it is no higher than during pregnancy. In rare cases, arterial or venous thromboembolism of retinal vessels or renal, hepatic, and mesenteric vessels may occur. Their likelihood increases in women with heavy smoking, age over 35 years, obesity, arterial hypertension, heart valve pathologies complicated by hemodynamic disorders, atrial fibrillation, dyslipoproteinemia, prolonged immobilization, diabetes mellitus complicated by vascular lesions, as well as in the presence of thromboembolic diseases in the family history ( parents, sister, brother).
Before elective surgery on the lower extremities or major surgery, the drug should be temporarily stopped and resumed after remobilization after 2 weeks.
Symptoms of thromboembolism include sudden chest pain radiating to the left arm, shortness of breath, severe headache, accompanied by diplopia, partial or complete sudden loss of vision, dizziness, aphasia, collapse, weakness, severe numbness of half the body, focal epilepsy, acute abdomen, impaired motor skills. functions, expressed by unilateral pain in the calf muscle.
Women predisposed to chloasma should avoid exposure to direct sunlight and ultraviolet radiation.
The effectiveness of the drug may be impaired by concomitant therapy with other drugs, in which case the use of additional barrier methods of contraception is required.
If there is acyclic bleeding or absence of menstrual-like bleeding after regular use of tablets from two blisters, the tablets should be stopped and an examination should be performed to exclude pregnancy.
The estrogenic components of oral contraceptives may affect the level of laboratory parameters of the functional parameters of the thyroid gland, kidneys, adrenal glands, hemostasis, liver, transport proteins and lipoproteins.
The use of Regulon in women with menorrhagia significantly reduces menstrual blood loss, normalizes the menstrual cycle, and has a beneficial effect on the condition of the skin, especially with acne vulgaris.
In case of severe liver pathologies, hepatitis, cholestatic jaundice, the drug can be prescribed only 3 months after recovery and preservation of normal laboratory and functional parameters.
The drug does not protect against sexually transmitted diseases, including HIV infection (AIDS).
Taking pills does not affect a woman’s ability to drive a car or use other machinery.
Interaction with other drugs
Medicines 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 achieved 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 Regulon (the mechanism of interaction has not been established). If co-administration is necessary, it is recommended to use an additional barrier method of contraception throughout the course of treatment and for 7 days (for rifampicin - within 28 days) after discontinuation of the drug.
Oral contraceptives may decrease carbohydrate tolerance and increase the need for insulin or oral antidiabetic agents.
Regulon contains 30 mcg and 150 mcg , as well as auxiliary components: magnesium stearate (Magnesium stearate), α-tocopherol (Alpha-tocopheryl acetate), colloidal silicon dioxide (Silicon dioxide colloidal), stearic acid (Stearic acid), povidone (Povidone), potato starch (Solani amylum) , lactose monohydrate.
The film shell is made using macrogol 6000 (Macrogol 6000), propylene glycol (Propylene glycol), hypromellose (Hypromellose).
Release form
Regulon is supplied to pharmacies in the form of film-coated tablets. The tablets are packaged in 21 pieces in blisters, 1 or 3 blisters in one cardboard package.
pharmachologic effect
The drug belongs to the group combined monophasic oral . Pharmacological action of Regulon - contraceptive , estrogen-progestogen .
Pharmacodynamics and pharmacokinetics
According to the annotation, the mechanism of action of the drug is based on the ability of its active substances suppress the synthesis of gonadotropins by the pituitary gland (in particular, luteinizing And follicle-stimulating hormones ).
It makes it difficult ovulation , helps increase the density of cervical mucus and, as a result, prevents penetration spermatozoa in internal space of the uterine body .
Ethinyl estradiol is a synthetic analogue that begins to be produced in a woman’s body, starting from the first menstruation.
Desogestrel has a pronounced progestational And antiestrogenic effect , similar to the one that has endogenous . The substance is characterized by weak anabolic and androgenic activity .
During the period of taking Regulon tablets in a woman (in the case of initial menorrhagia ) significantly reduces blood loss during menstruation and improves the condition of the skin (especially if there is acne vulgaris ).
AND desogestrel , And ethinylestradiol and are quickly and almost completely absorbed from the digestive tract. Desogestrel At once metabolized with education in biology active - 3-keto-desogestrel .
Plasma concentration reaches its maximum:
- after 1.5 hours - for desogestrel (plasma concentration indicator - 2 ng in 1 ml);
- after 1-2 hours - for ethinyl estradiol (plasma concentration indicator - 80 pg in 1 ml).
Bioavailability indicator:
- For desogestrel — from 62 to 81%;
- For ethinyl estradiol - about 60% (this is due to presystemic conjugation and the effect of the first passage of the substance through the liver barrier).
Half-life:
- For 3-keto-desogestrel — 30 hours ( products excreted in urine and intestinal contents in a ratio of 4:6);
- For ethinyl estradiol - 24% (approximately 40% of the substance and its metabolites are excreted in the urine, the remaining approximately 60% in the intestinal contents).
Indications for use
The annotation for Regulon states that the main purpose of the drug is to protect against unwanted symptoms.
However, research confirms that in addition to contraceptive effect , Regulon is also characterized by the presence of a therapeutic effect. So, to the question “tablets - what are they for?” the instructions for the drug indicate that the use of Regulon is advisable when dysfunctional uterine bleeding , premenstrual syndrome , dysmenorrhea etc..
The drug effectively relieves periodic aching pain in the lower abdomen, helps reduce the pain and profuseness of menstrual bleeding, dyspaurenia , eliminates minor dark-colored discharge from the genital tract during the perimenstrual period, as well as soreness of the mammary glands.
It is often prescribed to increase the effectiveness of prescribed therapy. When the drug is prescribed to stop growth (this is advisable if the diameter of the latter does not exceed 2 cm). In addition, Regulon promotes resorption ovarian retention cysts .
After 40 years, when a woman, as a rule, has already decided on family planning and having the required number of children, Regulon allows you to prevent abortion and its adverse consequences (according to statistics, most pregnancies at this age end in induced abortion).
Contraindications
Contraindications to the use of Regulon are:
- intolerance to any component of the drug;
- serious liver disease ;
- functional (benign) hyperbilirubinemia (including rare hereditary pigmentary hepatoses);
- indicated in the anamnesis jaundice in pregnancy ;
- family forms hyperlipidemia ;
- indicated in the anamnesis liver tumors ;
- moderate or severe arterial hypertension ;
- indicated in the anamnesis or, the presence of pronounced and/or multiple risk factors for their development, as well as the presence in the anamnesis of information that the woman had harbingers of thrombosis ;
- Type II ;
- vaginal bleeding of unknown origin ;
- discovered estrogen-dependent tumors or suspicion of them;
- severe forms (with angiopathy );
- pregnancy diabetes ;
- disruption of the hemocoagulation system ;
- strong , otospongiosis (or their progression) associated with a previous pregnancy or use glucocorticosteroids .
Side effects of Regulon
The most dangerous side effects of Regulon, which require discontinuation of the drug, include:
- arterial hypertension ;
- thromboembolism of veins and arteries (including formation of blood clots in deep veins , etc.);
- thromboembolism of veins and arteries of the liver and kidneys , and thromboembolism of retial and/or mesenteric veins and arteries (very rarely);
- hearing loss caused by otospongiosis ;
- porphyrin disease ;
- hemolytic-uremic syndrome ;
- exacerbation of the course reactive systemic lupus erythematosus (in rare cases);
- disappearing after discontinuation of the drug rheumatic chorea (in extremely rare cases).
Less serious side effects of the drug include:
- not related to menstruation acyclic bleeding , as well as the appearance bloody vaginal discharge ;
- observed after discontinuation of the drug;
- changes in the condition of cervical (vaginal) mucus;
- increase, tension and breast tenderness ;
- emergence inflammatory processes in the vagina ;
- galactorrhea ;
- nausea;
- vomit;
- development or exacerbation of pruritus and/or jaundice associated with cholestasis ;
- Crohn's disease (granulomatous enteritis);
- cholelithiasis ;
- erythema nodosum or exudative ;
- the appearance of skin rashes;
- chloasma ;
- mood swings;
- depression ;
- increased sensitivity of the cornea of the eye ;
- decreased tolerance (tolerance) to carbohydrates;
- weight gain;
- accumulation of fluid in the body;
Regulon birth control pills: instructions for use
How to take Regulon correctly?
Start taking pills from day 1 menstrual cycle , one per day, at the same time of day, for 3 weeks (21 days). After the last tablet is taken, it is necessary to maintain a seven-day interval, during which bleeding similar to menstrual bleeding should occur.
On the 8th day after the last tablet was taken (4 weeks after starting the drug, on the same day of the week), even if the bleeding has not stopped, taking the tablets is resumed from the next blister.
According to the scheme described above, the tablets are taken as long as the need for. If a woman takes pills, following all the rules and recommendations specified in the instructions for Regulon, contraceptive effect also persists during the seven-day interval.
First pill intake
The first tablet of the drug is taken on day 1 of the cycle. In this case, there is no need to use additional methods of contraception. If you start taking it between 2 and 5 days of the cycle, then during the first 7 days of the first cycle of using Regulon you should resort to using barrier contraceptives .
If after the start menstrual bleeding more than 5 days have passed, it is advisable to start taking the drug in the next cycle.
How to drink Regulon after childbirth?
If a woman is not breastfeeding, she can start taking pills 21 days after birth (after prior consultation with her gynecologist). In such a situation, there is no need to use additional contraception.
If sexual intercourse took place after childbirth, it is recommended to postpone the start of taking Regulon until the next cycle.
If the drug is started later than 3 weeks after birth, additional methods of contraception should be used in the first 7 days of the first cycle of use.
Taking pills after an abortion
If there are no contraindications, tablets can be taken from 1 day after, without supplementing them with other contraceptives.
Regulon is also often prescribed after curettage.
The advisability of prescribing pills after abortion/curettage (in particular, after frozen pregnancy ) due to the need restore normal ovarian function and prevent the development of inflammatory complications, which, according to statistics, are observed in approximately every third woman who has had a repeat abortion.
The optimal means are considered to be drugs that include highly active gestagenic substance , which has no side effects, and, in particular, Regulon tablets produced by Gedeon Richter.
Taking the drug allows you to compensate for the caused deficiency progesterone and the development of related proliferative processes in the reproductive system (including tec tissue hyperplasia , fibroids , hyperplasia , hyperthecosis , etc.).
Switching to Regulon from other hormonal drugs
When switching to the drug from another contraceptive, the first tablet should be taken the next day after completing the 28-day package (21 days of use + 7 days of break). There is no need to use additional contraception.
When switching to Regulon s, the first tablet is taken on day 1 of the cycle, without supplementing the intake with other methods of contraception.
If no menstrual bleeding occurs during the period of taking the mini-pill, you can start taking Regulon on any day of the cycle, but only after pregnancy has been ruled out.
In the first 7 days of the first cycle of administration, there is a need for additional protective measures, for which they usually use a condom, a cap with spermicidal gel, or abstain from sexual intercourse. The calendar method of contraception in this case is ineffective.
Delay of menstruation
When to defer menstruation , continue to take the pills without taking a break for 7 days. When deferred menstrual bleeding Breakthrough bleeding or spotting may occur, which, however, does not reduce the contraceptive effect of the drug.
Regular intake of tablets is restored after a 7-day interval.
How to take Regulon if you miss a pill?
If no more than 12 hours have passed since missing a pill, the forgotten pill is taken immediately after being remembered. Further reception continues according to the usual scheme.
If the interval between doses is more than 12 hours, the reliability of the drug in a given cycle cannot be considered one hundred percent. Therefore, you should use additional contraception until your next cycle.
If you miss 1 tablet in the first 7-14 days of the cycle, you should take 2 tablets at once the next day, after which the reception is continued according to the usual regimen using additional contraceptives until the end of the cycle.
If a tablet was missed between 14 and 21 days, regular use is continued by taking the forgotten tablet and without taking a 7-day break.
Missing a dose increases your risk ovulation and/or the appearance of bloody vaginal discharge . This is due to the fact that the drug contains a minimum dose and requires the use of additional contraceptives.
Overdose
Symptoms of an overdose of Regulon are:
- nausea;
- vomit;
- pronounced headache ;
- convulsions calf muscles;
- Vaginal bleeding not associated with menstruation.
Since the drug does not have a specific effect, symptomatic therapy is used to relieve the symptoms of an overdose. First aid after taking a high dose of Regulon is gastric lavage (it is recommended to do this in the first two to three hours after taking the pills).
Interaction
The effectiveness of oral contraceptives is reduced in combination with drugs that induce liver: hydantoin, , barbiturates , oxcarbazepine , felbamate , primidone , preparations of St. John's wort , griseowulfine .
In addition, when used in combination with Regulon, these drugs increase the likelihood of breakthrough bleeding.
The level of induction reaches its maximum no earlier than 2-3 weeks later, but can persist up to 4 weeks after discontinuation of the drug.
Menstrual irregularities and a decrease in the contraceptive effect may be observed when used simultaneously with:
- antibiotics (especially with and);
- barbiturates ;
- some antispasmodics ;
- laxatives ;
- antidepressants .
In cases where taking the above medications is necessary, it is recommended to protect yourself using barrier contraceptives (during the entire treatment period, as well as for an additional 7-28 days, depending on which medicine was prescribed).
If necessary, use anticoagulants During the period of taking Regulon, it is necessary to carry out additional prothrombin time monitoring . In some situations, adjustment of the dosage regimen may be necessary. anticoagulant .
Due to the increased likelihood of complications, Regulon should not be combined with hepatotoxic agents .
While taking oral contraceptives, you may:
- decreased tolerance to carbohydrates;
- increasing need for oral antidiabetic drugs and .
Terms of sale
On prescription.
Storage conditions
The optimal temperature for storing Regulon is from 15 to 30 degrees Celsius. Keep away from children.
Best before date
36 months.
special instructions
If taking Regulon is accompanied by a deterioration in liver test results, it is recommended to immediately stop taking the pills.
In the first few months of taking the drug, there may be acyclic intermenstrual bleeding , which are not grounds for stopping the pills. However, if they continue for three months or more, it is necessary to undergo a detailed examination.
Since in women who smoke, taking Regulon is accompanied by an increased risk thromboembolic complications , they are encouraged to decide on quitting smoking.
If menstruation after Regulon does not occur in the second cycle, the possibility of pregnancy should be excluded.
The teratogenic effect of Regulon has not been proven. For this reason, if pregnancy occurs while taking the pills, there is no need to interrupt it.
How long can you take Regulon?
During the period of taking Regulon tablets, changes occur in a woman’s body that are characteristic of the first weeks pregnancy . A woman who already has children experiences the same processes in her reproductive system that would occur if she gave birth and nursed several children.
It is well known that having a large number of children is the most effective method of protection against oncological diseases of the reproductive system and mammary glands .
Thus, long-term use of Regulon enhances the therapeutic effect of the drug. Taking pills is allowed until the woman is faced with the question of planning a child.
Regulon and menstruation
Usually, menstrual bleeding when taking Regulon it becomes more scarce. However, it also happens that a woman may develop an addiction to the drug, which most often manifests itself in the form of spotting.
Stopping taking pills is usually accompanied by increased work ovaries . Therefore, one of the consequences of canceling Regulon may be very heavy menstrual bleeding .
If there are no periods after discontinuation, this may also be due to failure of ovarian function . As a rule, she and therefore menstrual cycle , are restored a month after stopping Regulon. To determine the level in the body, gynecologists recommend taking the necessary tests a month after stopping the drug.
Regulon and weight: do hormonal pills make you fat?
It is generally accepted that reception hormonal contraceptives can provoke weight gain. However, doctors claim that if you follow all the rules for taking Regulon, as well as your daily routine and nutrition, the pills do not have any effect on a woman’s weight.
Typically, weight gain while taking birth control pills may be due to the fact that they contain desogestrel characterized by the ability to retain fluid in the body (for example, progesterone is the cause of edema during pregnancy).
Is it possible to get pregnant while taking the drug?
When taking Regulon correctly, the likelihood of pregnancy is negligible. The effectiveness of the drug is very close to 100%.
The risk of becoming pregnant is highest during the period of changing the contraceptive, in cases where there were missed pills, violations of the dosing schedule (the pills were taken at different times each time) and also if the effect of the pill was neutralized (for example, by an absorbent).
Silest , Egestrenol , Oralcon , Bonade .Which is better - Regulon or Novinet?
Regulon and Novinet These are generic drugs. They have the same composition, indications for use and contraindications, but are produced by different companies.
Regulon or Janine - which is better?
Both Regulon and Janine - This low-dose monophasic contraceptives . They have a similar mechanism of action, but differ in composition. Regulon is a combination ethinyl estradiol And desogestrel , and as part of Janine ethinylestradiol supplemented (at the same time the dose progestogenic The component in the Janine dragee is slightly higher than in Regulon).
The most significant difference between the drugs is their price - Regulon is much cheaper than its analogue.
Regulon and alcohol
Alcohol has no effect on changing the pharmacological profile of the drug, however, in a number of diseases it can provoke a worsening of their course: for example, when alcohol is combined with Regulon, it can cause a seizure.
Regulon and pregnancy
It is an absolute contraindication to the use of Regulon. During lactation, you should stop taking the drug or stop breastfeeding.
This is due to the fact that taking pills in the postpartum period provokes a decrease in the amount of milk, impairs lactation and negatively affects the growth of the child.
Pregnancy after Regulon birth control pills
Contraceptive effect Regulon tablets are associated with the ability of the synthetic analogues included in its composition endogenous hormones estradiol And progestogens prevent the release of a mature egg from the follicle .
As contraception The drug can be used for several years. However, many women are concerned about whether this will somehow affect reproductive function and subsequent pregnancy.
Gynecologists answer such questions as follows: if you take the pills correctly (that is, take them according to the regimen described in the instructions and in compliance with all the recommendations of your doctor), then after taking them you can plan a pregnancy. Typically, pregnancy after Regulon occurs after about 6 months of active sexual activity.
For a woman who is planning a child, doctors recommend stopping taking the drug at least three months before conception.
Monophasic oral contraceptive
Active ingredients
Ethinylestradiol
- desogestrel (desogestrel)
Release form, composition and packaging
Film-coated tablets white or almost white, round, biconvex, marked "P8" on one side and "RG" on the other.
Excipients: α-tocopherol, magnesium stearate, colloidal silicon dioxide, stearic acid, potato starch, lactose monohydrate.
Film shell composition: propylene glycol, macrogol 6000, hypromellose.
21 pcs. - PVC/PVDC/Aluminium blisters (1) - cardboard packs.
21 pcs. - PVC/PVDC/Aluminium blisters (3) - cardboard packs.
pharmachologic effect
Monophasic oral contraceptive. The main contraceptive effect is to inhibit the synthesis of gonadotropins and suppress ovulation. In addition, by increasing the viscosity of cervical mucus, the movement of sperm through the cervical canal slows down, and changes in the condition of the endometrium prevent the implantation of a fertilized egg.
Ethinyl estradiol is a synthetic analogue of endogenous estradiol.
Desogestrel has a pronounced gestagenic and antiestrogenic effect, similar to endogenous, weak androgenic and anabolic activity.
Regulon has a beneficial effect on lipid metabolism: it increases the concentration of HDL in the blood plasma without affecting the content of LDL.
With the use of the drug, the loss of menstrual blood is significantly reduced (in case of initial menorrhagia), the menstrual cycle is normalized, and a beneficial effect on the skin is noted, especially in the presence of acne vulgaris.
Pharmacokinetics
Desogestrel
Suction
Desogestrel is quickly and almost completely absorbed from the gastrointestinal tract and is immediately metabolized into 3-keto-desogestrel, which is a biologically active metabolite of desogestrel.
Cmax is reached after 1.5 hours and is 2 ng/ml. Bioavailability - 62-81%.
Distribution
3-keto-desogestrel binds to blood proteins, mainly albumin and sex hormone binding globulin (SHBG). V d is 1.5 l/kg. C ss is established by the second half of the menstrual cycle. The level of 3-keto-desogestrel increases 2-3 times.
Metabolism
In addition to 3-keto-desogestrel (which is formed in the liver and in the intestinal wall), other metabolites are formed: 3α-OH-desogestrel, 3β-OH-desogestrel, 3α-OH-5α-H-desogestrel (first phase metabolites). These metabolites do not have pharmacological activity and are partially converted, through conjugation (the second phase of metabolism), into polar metabolites - sulfates and glucuronates. Clearance from blood plasma is about 2 ml/min/kg body weight.
Removal
T1/2 of 3-keto-desogestrel is 30 hours. Metabolites are excreted in the urine and feces (in a ratio of 4:6).
Ethinyl estradiol
Suction
Ethinyl estradiol is quickly and completely absorbed from the gastrointestinal tract. Cmax is achieved 1-2 hours after taking the drug and is 80 pg/ml. The bioavailability of the drug due to presystemic conjugation and the “first pass” effect through the liver is about 60%.
Distribution
Ethinyl estradiol is completely bound to plasma proteins, mainly to. Vd is 5 l/kg. C ss is established by the 3-4th day of administration, while the level of ethinyl estradiol in the serum is 30-40% higher than after a single dose.
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 excreted into bile and enter the enterohepatic circulation. Clearance from blood plasma is about 5 ml/min/kg body weight.
Removal
T1/2 of ethinyl estradiol averages about 24 hours. About 40% is excreted by the kidneys and about 60% through the intestines.
Indications
- contraception.
Contraindications
- the presence of severe and/or multiple risk factors for venous or arterial thrombosis (including severe or moderate arterial hypertension with blood pressure ≥ 160/100 mm Hg);
- precursors of thrombosis (including transient ischemic attack, angina) currently or in history;
- migraine with focal neurological symptoms, incl. in the anamnesis;
- venous or arterial thrombosis/thromboembolism (including deep vein thrombosis of the leg, pulmonary embolism, myocardial infarction, stroke) currently or in history;
- history of venous thromboembolism;
— diabetes mellitus (with angiopathy);
- pancreatitis (including a history), accompanied by severe hypertriglyceridemia;
- dyslipidemia;
- severe liver diseases, cholestatic jaundice (including during pregnancy), hepatitis, incl. history (before normalization of functional and laboratory parameters and within 3 months after their normalization);
- jaundice due to taking corticosteroids;
- gallstone disease currently or in history;
- Gilbert's syndrome, Dubin-Johnson syndrome, Rotor syndrome;
- liver tumors (including in history);
- severe itching, otosclerosis or its progression during a previous pregnancy or taking corticosteroids;
— hormone-dependent malignant neoplasms of the genital organs and mammary glands (including if they are suspected);
- vaginal bleeding of unknown etiology;
- smoking over the age of 35 (more than 15 cigarettes per day);
— pregnancy or suspicion of it;
- lactation period;
- hypersensitivity to the components of the drug.
Carefully the drug should be prescribed for conditions that increase the risk of developing venous or arterial thrombosis/thromboembolism: age over 35 years, smoking, family history, obesity (body mass index more than 30 kg/m2), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular defects heart, atrial fibrillation, prolonged immobilization, extensive surgery, surgery on the lower extremities, severe trauma, varicose veins and superficial thrombophlebitis, the postpartum period, the presence of severe depression (including a history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, including lupus), diabetes mellitus not complicated by vascular disorders, systemic lupus erythematosus (SLE), Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (incl. family history), acute and chronic liver diseases.
Dosage
The drug is prescribed orally.
Taking tablets starts on the 1st day of the menstrual cycle and takes 1 tablet/day for 21 days, if possible at the same time of day. After taking the last tablet from the package, take a 7-day break, during which menstrual-like bleeding occurs due to drug withdrawal. The next day after a 7-day break (4 weeks after taking the first tablet, on the same day of the week), resume taking the drug from the next package, also containing 21 tablets, even if the bleeding has not stopped. This pill regimen is followed as long as there is a need for contraception. If you follow the rules of administration, the contraceptive effect remains during the 7-day break.
First dose of the drug
The first tablet should be taken on the first day of the menstrual cycle. In this case, it is not necessary to use additional methods of contraception. You can start taking pills from the 2-5th day of menstruation, but in this case, in the first cycle of using the drug, you must use additional methods of contraception in the first 7 days of taking the pills.
If more than 5 days have passed since the start of menstruation, you should delay starting the drug until your next menstruation.
Taking the drug after childbirth
Women who are not breastfeeding can start taking the pill no earlier than 21 days after giving birth, after consulting with their doctor. In this case, there is no need to use other methods of contraception. If there has already been sexual contact after childbirth, then taking the pills should be postponed until the first menstruation. If a decision is made to take the drug later than 21 days after birth, then additional methods of contraception must be used in the first 7 days.
Taking the drug after an abortion
After an abortion, in the absence of contraindications, you should start taking pills from the first day after surgery, and in this case there is no need to use additional methods of contraception.
Switching from another oral contraceptive
When switching from another oral drug (21- or 28-day): it is recommended to take the first tablet of Regulon the next day after completing the course of the 28-day package of the drug. After completing the 21-day course, you must take the usual 7-day break and then start taking Regulon. There is no need to use additional methods of contraception.
Switching to taking Regulon after using oral hormonal drugs containing only progestogen ("mini-pills")
The first Regulon tablet should be taken on the 1st day of the cycle. There is no need to use additional methods of contraception.
If menstruation does not occur while taking the mini-pill, then after excluding pregnancy, you can start taking Regulon on any day of the cycle, but in this case, in the first 7 days it is necessary to use additional methods of contraception (using a cervical cap with spermicidal gel, a condom, or abstinence from sexual intercourse). The use of the calendar method in these cases is not recommended.
Delay of the menstrual cycle
If there is a need to delay menstruation, you must continue taking the tablets from the new package, without a 7-day break, according to the usual regimen. When menstruation is delayed, breakthrough or spotting bleeding may occur, but this does not reduce the contraceptive effect of the drug. Regular intake of Regulon tablets can be resumed after the usual 7-day break.
Missed pills
If a woman forgot to take the pill on time, and after missing it, no more than 12 hours, You need to take the forgotten pill, and then continue taking it at the usual time. If there is a gap between taking pills more than 12 hours - This is considered a missed pill; contraceptive reliability in this cycle is not guaranteed and the use of additional methods of contraception is recommended.
If you miss one tablet per first or second week of the cycle, you need to take 2 tablets. the next day and then continue regular use using additional methods of contraception until the end of the cycle.
If you miss a pill third week of the cycle you need to take the forgotten pill, continue taking it regularly and 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 miss a pill and therefore the use of additional methods of contraception is recommended.
Vomiting or diarrhea
If vomiting or diarrhea occurs after taking the drug, then absorption of the drug may be inadequate. If the symptoms stop within 12 hours, then you need to take one more tablet. After this, you should continue taking the tablets as usual. If vomiting or diarrhea continues for more than 12 hours, then it is necessary to use additional methods of contraception during vomiting or diarrhea and for the next 7 days.
Side effects
Side effects that require immediate discontinuation of the drug:
Arterial hypertension;
Hemolytic-uremic syndrome;
Porphyria;
Hearing loss due to otosclerosis.
Rarely: arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism); exacerbation of reactive systemic lupus erythematosus.
Very rarely: arterial or venous thromboembolism of the hepatic, mesenteric, renal, retinal arteries and veins; Sydenham's chorea (passing after discontinuation of the drug).
Other side effects that are less severe but more common are listed below. The advisability of continuing to use the drug is decided individually after consultation with a doctor, based on the benefit/risk ratio.
From the reproductive system: acyclic bleeding/bloody discharge from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, development of inflammatory processes in the vagina, candidiasis.
From the mammary glands: tension, pain, breast enlargement, galactorrhea.
From the digestive system: nausea, vomiting, diarrhea, epigastric pain, Crohn's disease, ulcerative colitis, hepatitis, the occurrence or exacerbation of jaundice and/or itching associated with cholestasis, cholelithiasis.
From the skin: Erythema nodosum, exudative erythema, rash, chloasma.
From the side of the central nervous system: headache, migraine, mood changes, depression.
From the senses: increased sensitivity of the cornea (when wearing contact lenses).
From the side of metabolism: fluid retention in the body, change (increase) in body weight, decreased tolerance to carbohydrates.
Others: allergic reactions.
Overdose
Symptoms: nausea, vomiting, and in girls - bleeding from the vagina.
Treatment: In the first 2-3 hours after taking the drug in a high dose, gastric lavage is recommended. There is no specific antidote, treatment is symptomatic.
Drug interactions
Medicines that induce liver enzymes, such as hydantoin, barbiturates, primidone, 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 achieved 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 Regulon (the mechanism of interaction has not been established). If co-administration 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 - within 28 days) after discontinuation of the drug.
Oral contraceptives may decrease carbohydrate tolerance and increase the need for insulin or oral antidiabetic agents.
special instructions
Before starting to use the drug, it is necessary to conduct a general medical examination (detailed family and personal history, blood pressure measurement, laboratory tests) and gynecological examination (including examination of the mammary glands, pelvic organs, cytological analysis of a cervical smear). Such examinations during the period of taking the drug are carried out regularly, every 6 months (due to the need for timely identification of risk factors and contraindications that have arisen).
The drug is a reliable contraceptive: the Pearl index (an indicator of the number of pregnancies occurring during the use of a contraceptive method in 100 women over 1 year) when used correctly is about 0.05.
In each case, before prescribing hormonal contraceptives, the benefits or possible negative effects of their use are individually assessed. This issue must be discussed with the patient, who, after receiving the necessary information, will make the final decision on the preference for hormonal or any other method of contraception.
The woman's health condition must be carefully monitored. If any of the following conditions/diseases appear or worsen while taking the drug, you must stop taking the drug and switch to another, non-hormonal method of contraception:
— diseases of the hemostasis system;
— conditions/diseases predisposing to the development of cardiovascular and renal failure;
- epilepsy;
- migraine;
- the 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 impaired tryptophan metabolism, then vitamin B 6 can be used for correction);
- sickle cell anemia, because in some cases (for example, infections, hypoxia), estrogen-containing drugs for this pathology can provoke thromboembolism;
- the appearance of abnormalities in laboratory tests assessing liver function.
Thromboembolic diseases
Epidemiological studies have shown that there is a connection between taking oral hormonal contraceptives and an increased risk of developing 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).
Some researchers suggest that the likelihood of venous thromboembolic disease is greater with drugs containing desogestrel and gestodene (third generation drugs) than with drugs containing levonorgestrel (second generation drugs).
The incidence of spontaneous occurrence of new cases of venous thromboembolic disease in healthy non-pregnant women not taking oral contraceptives is about 5 cases per 100 thousand women per year. When using second generation drugs - 15 cases per 100 thousand women per year, and when using third generation drugs - 25 cases per 100 thousand women per year.
When using oral contraceptives, arterial or venous thromboembolism of the hepatic, mesenteric, renal or retinal vessels is very rarely observed.
The risk of arterial or venous thromboembolic disease increases:
- with age;
- when smoking (heavy smoking and age over 35 years are risk factors);
- if there is a family history of thromboembolic diseases (for example, in parents, brother or sister). If a genetic predisposition is suspected, it is necessary to consult a specialist before using the drug;
- for obesity (body mass index more than 30 kg/m2);
- for dislipoproteinemia;
- for arterial hypertension;
— for diseases of the heart valves complicated by hemodynamic disorders;
- with atrial fibrillation;
- with diabetes mellitus complicated by vascular lesions;
- with prolonged immobilization, after major surgery, after surgery on the lower extremities, after severe trauma.
In these cases, it is assumed to temporarily stop using the drug (no later than 4 weeks before surgery, and resume no earlier than 2 weeks after remobilization).
Women after childbirth have an increased risk of venous thromboembolic disease.
It should be taken into account that diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia increase the risk of developing venous thromboembolic diseases.
It should be taken into account that resistance to activated protein C, hyperhomocysteinemia, protein C and S deficiency, antithrombin III deficiency, and the presence of antiphospholipid antibodies increase the risk of developing arterial or venous thromboembolic diseases.
When assessing the benefit/risk ratio of taking the drug, it should be taken into account that targeted treatment of this condition reduces the risk of thromboembolism. Symptoms of thromboembolism are:
- sudden chest pain that radiates to the left arm;
- sudden shortness of breath;
- any unusually severe headache that continues 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 severe numbness of half the body, movement disorders, severe unilateral pain in the calf muscle, symptom complex "acute" abdomen.
Tumor diseases
Some studies have reported an increased incidence of cervical cancer in women who took hormonal contraceptives for a long time, but the results of the studies are inconsistent. Sexual behavior, infection with the human papillomavirus 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 the risk of breast cancer among women taking oral hormonal contraceptives, but the higher detection rate of breast cancer may have been associated with more regular medical screening. Breast cancer is rare among women under 40, whether they are taking hormonal birth control or not, and increases with age. Taking oral contraceptives may be considered one of many risk factors. However, the 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 benign or malignant liver tumors in women taking hormonal contraceptives for a long time. This should be kept in mind when differentially assessing abdominal pain, which may be associated with an increase in liver size or intraperitoneal bleeding.
Chloasma
Chloasma can develop in women with a history of this disease during pregnancy. Those women who are at risk of developing chloasma should avoid contact with sunlight or ultraviolet radiation while taking Regulon.
Efficiency
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 oral contraceptives.
If the patient is concomitantly taking another drug that 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, spotting or breakthrough bleeding appears, in such cases it is advisable to continue taking the tablets until they run out in the next package. If at the end of the second cycle menstrual-like bleeding does not begin or acyclic bleeding does not stop, stop taking the pills and resume it only after pregnancy has been ruled out.
Changes in laboratory parameters
Under the influence of an oral cotraceptive drug - due to the estrogen component - the level of some laboratory parameters (functional indicators of the liver, kidneys, adrenal glands, thyroid gland, hemostasis indicators, levels of lipoproteins and transport proteins) may change.
Additional Information
After acute viral hepatitis, the drug should be taken after normalization of liver function (no earlier than 6 months).
With diarrhea or intestinal disorders, vomiting, the contraceptive effect may be reduced. While continuing to take 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 in women over 35 years of age) and on the number of cigarettes smoked.
The woman should be warned that the drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
Impact on the ability to drive vehicles and machinery
The drug does not affect the ability to drive a car or operate machinery.
Pregnancy and lactation
The use of the drug during pregnancy and breastfeeding is contraindicated.
During breastfeeding, it is necessary to resolve the issue of either discontinuing the drug or stopping breastfeeding.
For impaired renal function
WITH caution and only after a thorough assessment of the benefits and risks of use the drug should be prescribed for renal failure (including a history of it).
