Regulon

Regulon is a complex monophasic contraceptive drug for oral administration. It has contraceptive and estrogen-progestogenic effects.

Indications Regulon

It is used as a means of contraception.

However, various tests confirm that the drug has therapeutic properties (in addition to contraceptive properties). For example, its use would be advisable if a woman has dysfunctional uterine bleeding, as well as PMS, dysmenorrhea, etc.

The medication effectively eliminates periodic pain in the lower abdominal region, reduces the abundance and painfulness of menstruation and dyspareunia, and also eliminates weak, dark-colored vaginal discharge during the perimenstrual period and pain in the mammary glands.

Regulon is often prescribed to increase the effectiveness of endometriosis treatment. During uterine fibroids, it is used to stop the growth of the tumor (this makes sense if its diameter is no more than 2 cm). At the same time, the drug helps to resolve retention cysts that occur in the ovaries.

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Release form

The drug is released in tablet form, in the amount of 21 pieces inside blister plates. The box contains 1 or 3 such plates.

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Pharmacodynamics

The medicinal effect is provided by the ability of its active elements to suppress the pituitary binding of gonadotropins (among them lutropin and FSH). As a result, the ovulation process is complicated and the density of cervical mucus increases, which prevents the passage of spermatozoa into the uterine cavity.

Ethinyl estradiol is an artificial analogue of the substance estradiol (it begins to be produced by the female body from the moment of the first menstruation).

Desogestrel has a strong antiestrogenic and gestagenic effect, similar to the effect of internal progesterone. The component has low androgenic and anabolic activity.

During the use of the drug, a woman (if initial menorrhagia is observed) experiences a significant reduction in blood loss during menstruation, and the condition of the epidermis also improves (especially if the patient has acne).

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Pharmacokinetics

Desogestrel together with ethinyl estradiol are almost completely and rapidly absorbed from the gastrointestinal tract. Desogestrel is immediately metabolized, during which a bioactive breakdown product, 3-keto-desogestrel, is formed.

Cmax values are observed after 1.5 hours from the moment of administration and are 2 ng/ml (for desogestrel), and also after 1-2 hours and are 80 pg/ml (for ethinyl estradiol).

The bioavailability of desogestrel is within 62-81%, and ethinyl estradiol is about 60% (due to presystemic conjugation processes and the first hepatic passage of the element).

The half-life of 3-keto-desogestrel is 30 hours (metabolites are excreted from the body with urine and feces in a ratio of 4 to 6), and that of ethinyl estradiol is 24 hours (about 40% of the element along with its decay products is excreted in the urine, and the remainder (about 60%) is excreted in the feces).

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Dosing and administration

Scheme of drug use.

You should start taking the drug from the 1st day of the menstrual cycle - in the amount of 1 piece daily (at the same time of day), for a period of 21 days. Then, after taking the last tablet, you need to take a 7-day break, during which period bleeding similar to menstruation should occur.

Later, on the 8th day after taking the last medicinal tablet (4 weeks after the start of taking the drug, on the same day of the week), even if bleeding continues, the use of the drug is resumed - from a new blister pack.

Permissible duration of use of the drug.

Subject to the above instructions, the drug can be taken at any time during which a woman requires contraception. When taking the tablets in accordance with all the rules and recommendations, the contraceptive effect of the drug is maintained during the 7-day period.

Initial dose: 1 tablet.

Regulon should be started on the 1st day of the cycle. No additional contraception is required. When starting to take the drug between the 2nd and 5th days of the cycle, it is necessary to additionally use barrier contraception during the first week of its use.

If more than 5 days have passed since the onset of menstruation, it is recommended to postpone the start of taking the medication until the next menstrual cycle.

Scheme of drug use after childbirth.

Women who have stopped breastfeeding are allowed to start taking the medicine after 3 weeks from the day of delivery (it is necessary to consult a gynecologist before this). In this case, there is no need for additional use of contraceptives.

If sexual intercourse took place shortly after childbirth, the start of taking the medication should be postponed until the start of a new cycle.

If you start using Regulon later than 21 days after giving birth, you will need to use additional contraceptives during the first week of the initial cycle of use.

Taking medication after an abortion procedure.

In the absence of any contraindications, the drug can be used from the 1st day after the abortion procedure. In this case, additional contraceptives do not need to be used.

Quite often, the medicine is prescribed after curettage procedures.

The advisability of taking medications after a curettage procedure or abortion (for example, in case of a frozen pregnancy) is associated with the need to restore healthy ovarian function and the need to prevent the development of inflammatory complications - according to statistics, they are observed in approximately every 3rd woman who has had a repeated abortion.

Thanks to the use of drugs, it is possible to compensate for the progesterone deficiency associated with abortion, as well as the development of proliferative processes caused by it within the reproductive system (including fibroids, hyperplasia in the theca tissue area, Stein-Leventhal syndrome, internal endometriosis, mastopathy, endometriosis, endometrial hyperplasia, Frankel syndrome, etc.).

The process of transition from other hormonal agents.

When switching from another contraceptive, you must take the first tablet on the day following the end of the pack, designed for 28 days (21 days of use + 7 days of interval). No additional contraception is required.

In case of switching from the mini-pill, the first Regulon tablet is taken on the first day of the new cycle. There is no need to use additional contraceptives.

If there is no menstruation while using the mini-pill, you can start taking the medicine on any day of the cycle, but only after the absence of pregnancy has been diagnosed.

During the first 7 days of the initial cycle of use, additional methods of contraception (such as a cap containing spermicide, a condom, or abstinence from sexual intercourse) must be used. The calendar method of contraception will be ineffective in this case.

Use to delay the onset of menstruation.

To delay menstrual bleeding, the drug is continued without a 7-day break. In case of delay of menstruation, breakthrough bleeding or spotting may develop, but they do not weaken the contraceptive properties of the drug.

The regular regimen of drug use is resumed after a 7-day break.

Scheme for taking the drug in case of missing one tablet.

In cases where up to 12 hours have passed since the missed dose, the tablet should be taken as soon as it is remembered. Then the use continues as usual.

In cases where more than 12 hours have passed since the missed dose, the medicine loses 100% contraceptive reliability for the period of the given cycle. In this regard, additional contraception must be used before the start of a new cycle.

If you missed taking the medication during the first 2 weeks of your cycle, you need to take 2 tablets at once the next day and then continue taking it according to the standard regimen (while you need to use additional contraceptives until the end of this cycle).

If you miss a dose between days 14 and 21, you should continue regular use of the medicine, taking the previously forgotten tablet, and not taking a 1-week break.

Missing a pill increases the likelihood of ovulation or the occurrence of bloody vaginal discharge. This is due to the fact that the drug contains a small portion of estrogen. Therefore, in such cases, it is necessary to additionally use barrier contraception.

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Use Regulon during pregnancy

Taking Regulon during pregnancy is strictly prohibited. During breastfeeding, you should either stop taking the drug or not breastfeed. This is necessary because tablets taken in the postpartum stage reduce the volume of milk secreted, worsen the lactation process and negatively affect the development of the child.

The onset of pregnancy after a period of use of the drug.

The contraceptive effect of the drug develops due to the ability of its components (artificial analogues of estradiol with progestogens) to prevent the release of a mature egg from the follicle.

As a contraceptive, it can be used for several years, and in this regard, many women are concerned about whether the drug will have a negative impact on the functioning of the reproductive system, as well as on the course of pregnancy in the future.

If the medication is taken correctly (use according to the scheme specified in the drug instructions and compliance with all indications prescribed by the gynecologist), conception can be planned after its use is finished without any obstacles. Often, after the cancellation of Regulon, pregnancy occurs approximately six months after regular sexual activity.

At the planning stage, it is recommended to stop taking the medication at least 3 months before the possible date of conception.

Contraindications

Main contraindications:

• the presence of hypersensitivity to the elements of the therapeutic agent;
• severe forms of liver disease;
• functional hyperbilirubinemia, which has a benign form (this includes rare pigment-type hepatoses, which are hereditary in nature);
• history of jaundice during pregnancy;
• familial hyperlipidemia;
• history of liver tumors;
• elevated blood pressure to a moderate or severe degree;
• migraine;
• a history of thromboembolism or thrombosis and existing strong or multiple factors that increase the likelihood of their occurrence, as well as the presence in the history of information that the patient has had precursors to thrombosis;
• herpes type 2;
• the presence of vaginal bleeding of unknown etiology;
• diagnosed estrogen-dependent neoplasms or suspicion of their presence;
• diabetes mellitus in a severe stage (accompanied by angiopathy);
• gestational diabetes mellitus;
• disorders of hemocoagulation activity;
• severe itching and otosclerosis (or progression of these disorders) caused by a previous pregnancy or the use of GCS.

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Side effects Regulon

Among the most serious adverse reactions to the use of the drug (if they occur, you should stop taking the drug):

• increased blood pressure;
• thromboembolism in the area of arteries or veins (this includes the formation of blood clots in the area of deep veins, myocardial infarction with stroke, etc.);
• thromboembolism in the area of the hepatic/renal veins or arteries, and in addition thromboembolism in the area of the mesenteric or retial veins or arteries (single);
• otosclerosis-induced hearing loss;
• GUS;
• porphyria;
• exacerbation of the process of the reactive form of SLE (rarely);
• Sydenham's chorea, which resolves after discontinuation of the drug (single).

Among the side effects that are less dangerous to health:

• acyclic form of bleeding that is not related to menstruation, and in addition, the occurrence of bloody discharge from the vagina;
• amenorrhea that develops after stopping taking the drug;
• galactorrhea;
• changes in the condition of cervical mucus;
• soreness and tension in the mammary glands, as well as their enlargement;
• the appearance of inflammation inside the vagina;
• vaginal candidiasis;
• vomiting along with nausea;
• the appearance or worsening of jaundice or itching caused by cholestasis;
• chloasma;
• transmural ileitis;
• cholelithiasis;
• erythema, which has an exudative or nodular form;
• the appearance of a rash on the epidermis;
• migraine, as well as headaches;
• mood lability and depression;
• increased sensitivity of the cornea;
• decreased carbohydrate tolerance;
• weight gain;
• accumulation of fluid inside the body;
• allergy symptoms.

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Overdose

Poisoning with Regulon can lead to nausea, symptoms of dyspepsia, severe headaches, vomiting, as well as cramps in the calf muscles and bloody vaginal discharge that is not related to menstruation.

The drug has no antidote, so symptomatic measures should be taken to eliminate signs of intoxication. As a first aid when using a large dose of the drug, a gastric lavage procedure is used (it must be carried out during the first 2-3 hours from the moment of using the substance).

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Interactions with other drugs

The medicinal efficacy of oral contraceptives is reduced when combined with liver enzyme inducers (including carbamazepine, oxcarbazepine, primidone with rifampicin and topiramate, as well as hydantoin, felbamate and barbiturates, griseovulfin and St. John's wort). However, when these substances are combined, the risk of breakthrough bleeding increases.

Maximum induction rates are observed after at least 2-3 weeks, but can persist for up to 1 month after stopping taking the drug.

Disruption of the cycle and weakening of the contraceptive properties of the drug may be observed in case of combination with such drugs as barbiturates, laxatives, antibiotics (especially ampicillin or tetracycline), certain antispasmodics and antidepressants.

In situations where it is necessary to use the above medications, barrier contraception should be used (during the entire period of therapy, and also during the additional 7-28 days - taking into account which particular drug was used).

If anticoagulants are required during the use of Regulon, the PT values should be additionally monitored. Sometimes it may also be necessary to change the dosage regimen of the anticoagulant used.

Due to the increased risk of complications, it is prohibited to combine the drug with hepatotoxic medications.

The use of oral contraceptives may reduce the body's tolerance to carbohydrates and also increase the need for insulin and oral hypoglycemic agents.

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Storage conditions

Regulon should be kept in a place closed to small children. Temperature values are within the range of 15-30°C.

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Shelf life

Regulon can be used within 36 months from the date of manufacture of the therapeutic agent.

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Analogues

The analogs of the drug are Novinet, Mercilon and Marvelon with Tri-Merci.

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Reviews

Regulon is considered one of the most popular contraceptives - this fact is confirmed by numerous reviews.

Most women who have used this drug note a small number of side effects of the drug, high reliability and reasonable cost, and in addition, the fact that after the end of the use of Regulon, conception occurs without significant difficulties.

But there are also negative opinions about the drug - they usually talk about the negative effects of the drug (such as acyclic bleeding of varying severity, nausea, itching in the genital area and noticeable weight gain).

In the reviews of specialists, this is explained by the fact that often such symptoms are associated with hypersensitivity of the patient's body to some elements of the drug, or with the fact that the medication is simply not suitable for this particular woman. To reduce the risk of negative reactions to a minimum, it is necessary to strictly follow the drug instructions.

If there is no improvement, in this case, it is necessary to consider the option of discontinuing the drug and selecting another contraceptive medication (it is necessary to undergo all required examinations first).