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Pharmacological properties

combined oral contraceptives block the effect of gonadotropins. the primary effect of these drugs is aimed at inhibiting ovulation. the drug causes a change in cervical mucus, which complicates the passage of sperm into the uterine cavity and affects the endometrium, thereby reducing the possibility of implantation of a fertilized egg. all this helps prevent pregnancy.

Pharmacokinetics Levonorgestrel. Absorption: when administered, levonorgestrel is absorbed quickly and completely in the digestive tract. Bioavailability is almost 100% due to the lack of primary metabolism.

Distribution: most of levonorgestrel binds to plasma proteins, mainly with albumin and globulin, which binds sex hormones.

Metabolism: mainly consists in cleavage of the Δ4-3-oxo group and hydroxylation at positions 2α, 1β and 16β, after which conjugation occurs. Most of the metabolites that circulate in the blood are 3α, 5-tetrahydro-levonorgestrel sulfates. Excretion of the drug occurs mainly in the form of glucuronides. A certain amount of primary levonorgestrel also circulates in the form of 17β-sulfate. Metabolic clearance is characterized by individual variability, which may partially explain the significant differences in the concentration of levonorgestrel observed in patients.

Excretion: T½ levonorgestrel shows individual variability and is approximately 36 hours in steady state. Levonorgestrel is excreted in urine (40–68%) and feces (16–48%) in the form of metabolites (sulfate and conjugates with glucuronic acid).

Ethinyl estradiol. Absorption: ethinyl estradiol is absorbed rapidly and almost completely, Cmax in blood plasma is reached after 1.5 hours. After presystemic conjugation and metabolism, the absolute bioavailability is 60%. AUC and Cmax may increase slightly over time.

Distribution: ethinyl estradiol is 98% bound to plasma proteins, mainly to albumin.

Metabolism: ethinyl estradiol is broken down by presystemic conjugation. It passes through the intestinal wall (first phase of metabolism) and enters the liver, where conjugation occurs (second phase of metabolism). The most important metabolites of the first phase of metabolism are 2-OH-ethinyl estradiol and 2-methoxy-ethinyl estradiol. Both ethinyl estradiol and the metabolites of the first phase are excreted in the form of conjugates (sulfates and glucuronides) in the bile and enter the hepatic intestinal circulation.

Excretion: ethinyl estradiol is excreted from blood plasma with T½ , which averages 29 hours (26–33 hours); clearance of blood plasma varies in the range of 10-30 l / h. Excretion of conjugates of ethinyl estradiol and its metabolites occurs with urine and feces in a ratio of 1: 1.

Indications

Oral contraception.

Application

Mode of application. inside, in the order indicated on the package, at about the same time, 1 tablet per day, with a small amount of liquid.

The use of the drug for the first time. Tri-Regol is used from the 1st day of menstruation, 1 tablet per day for the 21st day. Starting on days 2–7 is also possible, but during the first cycle it is recommended to additionally use non-hormonal methods of contraception (such as condoms or sperm-destroying drugs) during the first 7 days of taking the tablets.

Since the composition of the tablets of different colors is different, pink tablets should be taken in the first 6 days, white tablets in the next 5 days, after which dark yellow tablets should be taken for 10 days. The order of taking tablets of different colors is indicated by numbers and arrows on the package.

After the 21-day course of taking the drug, a 7-day break follows, during which menstrual bleeding usually occurs (usually on the 2nd or 3rd day). Regardless of whether bleeding has occurred or not, and regardless of its duration, on the first day after a 7-day break, if further protection is necessary, a 21-day course of taking Tri-Regol should be started again. With regular administration of Tri-Regol, the contraceptive effect persists during a 7-day break.

According to the indicated scheme, Tri-Regol should be taken while a pregnancy warning is desirable.

Switching to Tri-Regol from another oral contraceptive: taking the first Tri-Regol tablet should be started the day after the last active (hormone-containing) tablet is taken from the blister of the previous contraceptive - no later than 1 day after the usual break when using the previous combined hormonal birth control (or after taking the last placebo pill from the previous package).

Switching to taking Tri-Regol from a progestogen-only drug (low-dose oral contraceptive, injection, implant or intrauterine contraceptive): Switching from a low-dose oral contraceptive can be done any day of the menstrual cycle (from the implant and intrauterine contraceptive the next day after their removal; with the injection - on the day when the next injection should be prescribed). In this case, it is recommended to additionally use the barrier method of contraception during the first 7 days of taking the tablets.

After an abortion or after a miscarriage in the first trimester of pregnancy, the use of the drug should begin immediately on the same day after surgery. Additional methods of contraception are not required.

After childbirth or abortion in the II trimester of pregnancy, the drug should be started for a woman who does not breast-feed, 21–28 days after childbirth or abortion in the II trimester of pregnancy. If the start of oral contraception with the use of the Tri-Regol drug occurs later, it is necessary to additionally apply the barrier method of contraception during the first 7 days of taking the tablets.

If sexual intercourse has already taken place, pregnancy should be ruled out before taking pills or taking pills should be postponed until the first menstrual bleeding.

Breastfeeding: information on the use during breastfeeding is presented in the section "Use during pregnancy and lactation."

Missed pills: if a woman did not take the pill in a timely manner for any reason, she should take it within 12 hours. In this case, there is no need to use additional methods of contraception. The remaining tablets are taken at the usual time.

If more than 12 hours have passed, you must take the last missed pill as soon as you remember, even if you have to drink two tablets on the same day. Then continue to take the drug as usual. In this case, in the next 7 days it is necessary to apply additional non-hormonal methods of contraception (barrier methods, spermicides).

If less than 7 tablets remain in the current package, you should start taking tablets from the next package immediately after taking the last tablet from the current package; this means that there should be no pause between packages. In this case, withdrawal bleeding is not expected until the end of the second package; however, spotting and breakthrough bleeding may occur.

If withdrawal bleeding did not occur after completion of the second package, pregnancy should be excluded before resuming taking the tablets from the next package.

Gastrointestinal diseases: in the presence of vomiting or diarrhea, the effectiveness of the drug decreases due to incomplete absorption of the active substances. It is necessary to apply additional non-hormonal methods of contraception (barrier methods, spermicides) while symptoms are present, and over the next 7 days to prevent premature bleeding.

For vomiting or acute diarrhea that develops within 3-4 hours after taking the pill, use the recommendations described in the “Missed Pills” section.

How to delay menstrual bleeding.To delay menstrual bleeding, taking Tri-Regol tablets from a new package should start with dark yellow tablets (last phase) the day after the current package ends, without a pause between them. The duration of the delay in menstrual bleeding depends on the number of dark yellow tablets taken from the second package. Breakthrough bleeding or spotting may occur during this period. Regular administration of Tri-Regol may be resumed after a typical 7-day break.

Contraindications

Combined oral contraceptives (PDA) are not recommended in the presence of the following diseases and pathological conditions. with the development of such diseases when using PDA, the drug should be stopped immediately: pregnancy or suspected pregnancy, lactation; hypersensitivity to the components of the drug; history or references to arterial or venous thromboembolic diseases (e.g. deep vein thrombophlebitis, pulmonary thromboembolism) in combination with or without risk factors (see specific instructions); the presence of a risk of arterial or venous thromboembolism (blood clotting disorder, heart disease, atrial fibrillation, cerebrovascular disorders, myocardial infarction); a history of prodromal symptoms of thrombosis (transient bouts of ischemia, angina pectoris); the presence or history of a disorder of cerebral circulation; a severe degree or the presence of multiple risk factors for venous or arterial thrombosis can now be considered a contraindication (see special instructions); cardiovascular diseases (heart disease, cardiac arrhythmias, pathology of heart valves); severe course of ag; diabetes mellitus with vascular disorders; ophthalmic disorders of vascular origin; severe liver disease, history, until liver function indicators are normalized; the presence or history of liver tumors (benign or malignant); a history of migraine with focal neurological symptoms; diagnosed or suspected malignant tumors that are caused by sex steroids (e.g. genitals or mammary glands); vaginal bleeding of unknown etiology.

Side effects

By organ systems and frequency of occurrence (very often ≥1 / 10, often ≥1 / 100–1 / 10; infrequently ≥1 / 1000–1 / 100, rarely ≥1 / 10 000–1 / 1000; very rarely 1 / 10,000) side effects may be as follows.

Infections and parasitic diseases: often - vaginitis, candidiasis.

Benign, malignant and unspecified neoplasms (including cysts and polyps): infrequently - breast cancer; very rarely - hepatocellular carcinoma, liver adenoma.

On the part of the immune system: rarely - anaphylactic reactions, urticaria, angioedema, hypersensitivity reactions; very rarely - exacerbation of systemic lupus erythematosus.

From the side of metabolism: often - fluid retention; infrequently - increase or decrease in appetite; rarely - decrease in glucose tolerance, hyperlipidemia, hypertriglyceridemia; very rarely - exacerbation of porphyria.

Mental disorders: often - mood changes, depression, depressive mood; infrequently - a decrease or increase in libido, nervousness.

From the nervous system: very often - headache, migraine; often - increased irritability, dizziness; very rarely - exacerbation of chorea, acute violation of cerebral circulation.

From the side of the organ of vision: rarely - intolerance to contact lenses; very rarely - optic neuritis *, retinal artery thrombosis, visual impairment.

On the part of the hearing organ: rarely - otosclerosis.

From the vessels: infrequently - AH; rarely - thrombosis, embolism; very rarely - worsening of varicose veins, myocardial infarction.

From the digestive system: often - nausea, vomiting, pain in the stomach; infrequently - colic in the stomach, flatulence, diarrhea; very rarely - pancreatitis.

From the liver and biliary tract: rarely - cholestatic jaundice; very rarely - disorders of the gallbladder, gallstone disease **.

On the part of the skin and subcutaneous tissue: often - acne; infrequently - skin rash, urticaria, chloasma (melasma), hirsutism, alopecia; seldom - erythema nodosum, exudative erythema multiforme.

From the kidneys and urinary tract: very rarely - hemolytic uremic syndrome.

From the reproductive system and mammary glands: very often - breakthrough bleeding, spotting between menstruation; often - chest pain, pain in the area of ​​the mammary glands, engorgement of the mammary glands, the appearance of a secret from the mammary glands, dysmenorrhea, menstrual changes, changes in erosion and secretion from the cervix, amenorrhea; rarely - vaginal discharge.

Research: often - a change in secretion from the cervix, a decrease or increase in body weight; rarely - decrease in folate ***.

* Optic neuritis can lead to partial or complete loss of vision.

** The use of CPC can lead to a worsening of the current disease of the gallbladder and accelerate the development of this disease in women who have not previously had symptoms.

*** The use of CPC can lead to a decrease in the level of folate in blood plasma.

The following adverse reactions (without indication of frequency) are described by women who used birth control pills:

From the side of metabolism: hypercholesterolemia.

Mental disorders: irritability.

From the nervous system: cerebrovascular disorders.

From the vessels: phlebitis.

On the part of the skin and subcutaneous tissue: hypertrichosis, seborrhea.

From the skeletal muscles and connective tissue: a feeling of heaviness.

From the reproductive system and mammary glands: anovulatory cycles, oligomenorrhea, metrorrhagia, disorders of the mammary glands.

The following serious adverse reactions have been reported in women using CPC, detailed information on which is presented in the SPECIAL INSTRUCTIONS section: venous and arterial thromboembolic complications; Hypertension; tumors of the liver; diseases that can develop or worsen when taking CCP, although the evidence of this fact is inconclusive, include Crohns disease, ulcerative colitis, epilepsy, migraine, endometriosis, uterine fibroids, porphyria, systemic lupus erythematosus, herpes pregnant, small chorea; hearing loss associated with otosclerosis; hemolytic uremic syndrome, cholestatic jaundice; chloasma; acute and chronic hepatic impairment can lead to interruption of CPC intake until normal liver function.

The diagnosis of breast cancer is slightly higher among women taking CCPs. Because breast cancer is rarely diagnosed in women under the age of 40, an excess of breast cancer diagnoses in women taking or recently taking CPC is not significant compared to the overall risk of developing breast cancer. The causal relationship with the CCP has not been clarified. For more information, see the CONTRAINDICATIONS and SPECIAL INSTRUCTIONS sections.

In women with hereditary angioedema, the use of estrogens can induce or exacerbate the symptoms of angioedema.

special instructions

Medical examination / consultation. Before starting the use of the drug or re-prescribing the drug, it is necessary to collect a detailed family history and conduct a general medical and gynecological examination (primarily measuring hell, determining the level of glucose in the blood and urine, examining the function of the liver, examining the mammary glands, cytological analysis of the smear) to exclude risk of disease and pregnancy. the frequency and nature of the examinations should be based on established clinical guidelines, considering each case separately.

A woman must be warned that the drug does not protect her from sexually transmitted infections, including AIDS.

Special warnings. Smoking increases the risk of serious adverse reactions from the cardiovascular system while using CCP. This risk increases with age, depends on the number of cigarettes smoked, and is especially high in women aged 35 and over. All women using CCPs should be strongly advised to quit smoking. Smoking women over the age of 35 need to consider prescribing other methods of contraception.

If you have any diseases / risk factors listed below, you should evaluate the beneficial effects of CPC and the possible risks of their use in a particular woman and discuss with her the appropriate benefits and risks before she decides to use such drugs. In the event of the first manifestation, worsening, or aggravation of any of these diseases or risk factors, consult your doctor. Then the doctor must decide to interrupt taking the CCP.

Impaired blood circulation. Epidemiological studies have shown that the incidence of venous thromboembolism in women using low estrogen oral contraceptives (50 μg ethinyl estradiol) is 20–40 cases out of 100,000 women per year, but this risk varies depending on the amount of progestogen. This amounts to 5–10 cases out of 100,000 women per year for women who do not use the CCP. The use of any combined contraceptive increases the risk of venous thromboembolic diseases compared with these indicators in women who do not use CPC.

The risk of these diseases reaches a maximum in the first year of drug use. This increased risk is lower than the risk of venous thromboembolic diseases detected during pregnancy is 60 cases per 100,000 pregnancies (1–2% of these cases end fatally).

In general, the likelihood of thromboembolic diseases with oral contraceptives containing levonorgestrel and 30 μg of ethinyl estradiol is 20 cases out of 100,000 women per year.

Epidemiological studies have also been associated with the use of CPC with an increased risk of developing myocardial infarction, a transient attack of ischemia and stroke.

Very rarely there have been reports of thrombosis of other blood vessels, for example, liver, mesenteric, renal veins, retinal veins and arteries in women taking birth control pills. The connection between the development of these phenomena with the use of hormonal contraceptives has not been proven.

The risk of thromboembolism (arterial and / or venous) and cerebral circulation increases with age; when smoking (excessive smoking and age, especially over 35 years old, are additional risk factors); with a burdened family history (for example, diseases of a father or brother, sister at a young age). If there is a congenital predisposition to thromboembolic diseases, it is necessary to consult a specialist before using the drug; for obesity (body mass index 30 kg / m2); with impaired fat metabolism (dyslipoproteinemia); with hypertension; with migraine; with diseases of the heart valves; with atrial fibrillation; with prolonged immobilization, heavy operations, operations on the lower extremities, severe injuries. Due to the fact that the risk of thromboembolic diseases increases in the postoperative period, it is proposed to stop taking the drug 4 weeks before surgery and start taking it 2 weeks after remobilization of the patient; there is no consensus on the possible role of varicose veins and superficial thrombophlebitis in the development or progression of venous thrombosis.

Symptoms of venous or arterial thrombotic / thromboembolic diseases or symptoms of a cerebrovascular disorder may include unusual unilateral pain and / or swelling of the legs; sudden sharp chest pain, regardless of whether it spreads to the left arm; sudden respiratory failure; sudden cough for no apparent reason; any unusual, acute or prolonged headache; sudden partial or complete loss of vision; diplopia; slurred speech or aphasia; vertigo; collapse with or without focal epileptic seizure; weakness or very pronounced numbness that suddenly affects one side or one part of the body; movement disorders; sharp belly.

CCP intake has generally been associated with an increased risk of developing acute myocardial infarction or apoplexy stroke. The mechanisms of the effect of Tri-Regol on the risk of developing acute myocardial infarction have not been studied.

In the postpartum period, the increased risk of venous thromboembolism should be considered (see Use during pregnancy and lactation).

Other diseases that are associated with unwanted side effects from the circulatory system include diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohns disease or ulcerative colitis), and sickle cell anemia.

If the frequency or severity of migraine increases with the use of oral contraceptives (which may be a precursor or cerebrovascular event), the drug should be discontinued immediately.

Biochemical factors that may indicate a congenital or acquired predisposition to venous or arterial thrombosis include resistance to activated protein C, Leiden mutation of factor V, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies, anticardi lupus anticoagulant) and dyslipoproteinemia.

Tumors Some studies have reported an increase in the incidence of cervical cancer in women who have been taking combined oral contraceptives for a long time, but the results are mixed. In the formation of cervical cancer, sexual behavior and other factors, such as the human papillomavirus, occur, so the relationship between cervical cancer and the use of combined oral contraceptives is ambiguous.

An analysis of epidemiological studies has shown that women who use CPC have a slightly increased relative risk of developing breast cancer. This increased risk is gradually reduced within 10 years after cessation of the use of CPC. Since breast cancer is rarely seen in women under 40 years of age, the increase in the number of diagnosed cases of breast cancer in women who use CCPs now or in the past is not significant compared to the risk of developing breast cancer throughout their life.

Evidence for a causal relationship is not presented in these studies. The increased risk may be due to the early diagnosis of breast cancer in women who use CPC, the biological effects of CPC, or a combination of both of these factors.

In women using oral contraceptives, breast cancer is diagnosed at a slightly earlier stage compared to women who have not used CPC.

With prolonged use of sex hormones, benign, very rarely malignant tumors of the liver were occasionally noted, which in some cases can lead to life-threatening bleeding in the abdominal cavity.With the appearance of severe acute pain in the upper abdomen, an enlarged liver, or with signs of intraperitoneal bleeding, a liver tumor may be suspected. This must be taken into account when establishing a differentiated diagnosis.

Other diseases Women with hypertriglyceridemia or a family history of the disease are at an increased risk of pancreatitis with CPC. Women with hyperlipidemia, if they decide to use CPC, need careful medical supervision.

A slight increase in blood pressure was reported in many women who took CPC, but clinically significant increases were rare. Only in these rare cases, an immediate cessation of PDA was justified. If the use of CPC with existing hypertension constantly increases blood pressure or a significant increase in blood pressure does not correspond to antihypertensive treatment, the intake of CPC should be discontinued. In some cases, the use of CPC can be resumed if normal blood pressure values ​​can be achieved using antihypertensive therapy.

Although evidence of association with the use of CPC is inconclusive, there have been reports of the development or exacerbation of such diseases during pregnancy and when taking CPC: jaundice and / or itching associated with cholestasis; the formation of calculi in the gallbladder; porphyria; systemic lupus erythematosus, hemolytic uremic syndrome; chorea; herpes pregnant; hearing loss associated with otosclerosis.

In women with hereditary angioedema, estrogen administration can induce or exacerbate symptoms of angioedema.

Acute or chronic liver dysfunction may require discontinuation of CPC until liver function levels return to normal. Relapse of cholestatic jaundice and / or itching that occurred during pregnancy or the previous use of sex steroid hormones requires discontinuation of CPC.

Although CPCs may affect peripheral insulin resistance and glucose tolerance, there is no evidence of a need to change the dosing regimen for patients with diabetes and taking CPC. Nevertheless, while taking a CCP, careful monitoring of women with diabetes should be carried out.

With the use of CPC, the development of Crohns disease and ulcerative colitis is associated.

In rare cases, chloasma may develop, especially in women with a history of pregnant spots. Women with a tendency to chloasma should avoid direct sunlight or UV radiation when using PDAs.

Women who develop severe depression during the period of taking CPC should stop using these drugs and use alternative methods of contraception until the causal relationship between the symptoms of depression and the use of CPC is assessed. Women with a large history of depressive episodes require careful monitoring, and when you resume symptoms of depression, you should stop taking CPC.

Decreased efficiency. The effectiveness of CPC may be reduced if you miss a pill, vomiting, or diarrhea (see APPLICATION) or because of concomitant medications (see INTERACTIONS).

Decrease in cycle control. As with all PDAs, irregular bleeding (spotting or breakthrough bleeding) may develop, especially during the first months of use. Therefore, the assessment of any irregular bleeding makes sense only after the completion of the adaptation period of about three cycles.

If irregular bleeding persists or develops after previous regular cycles, the use of non-hormonal methods and appropriate diagnostic measures to exclude malignant neoplasms or pregnancy are recommended.These measures may include curettage.

In some women, after a break in intake, withdrawal bleeding may not occur. If CPC was used in accordance with the APPLICATION section, then pregnancy is unlikely. However, if the indications of the APPLICATION section before the first absence of withdrawal bleeding were not met, or if two withdrawal bleeds are absent in a row, pregnancy should be excluded before continuing with CPC.

This medicine contains lactose and sucrose, so it can not be used for hereditary intolerance to galactose, lactose, glucose-galactose malabsorption or sucrose-isomaltase deficiency and for fructose intolerance.

Use during pregnancy and lactation. When pregnancy is established, the drug should be stopped immediately.

If a woman becomes pregnant while taking the pills, then further administration should be stopped immediately.

According to the results of a large number of epidemiological studies, neither an increased risk of developing birth defects in children born to women who used CPC before pregnancy, nor teratogenic effects with the unintended use of birth control pills in early pregnancy were revealed.

Lactation. Hormonal birth control can reduce the secretion and change the composition of milk, as well as a small amount penetrate into breast milk, so taking these drugs during breastfeeding is contraindicated.

Children. The drug is not intended for use in children.

The ability to influence the reaction rate when driving vehicles or other mechanisms. The drug does not affect the ability necessary to drive vehicles or other mechanisms.

Interactions

Interactions between PDA and other drugs can lead to a deterioration in the effectiveness of the contraceptive and / or breakthrough bleeding and / or inefficiency of this method of contraception.

Women taking any of these drugs are advised to temporarily use a barrier or other method of contraception in addition to CPC. When taking drugs that induce liver enzymes, the barrier method is necessary for use during the entire course of treatment with such drugs and within 28 days after its completion.

Women taking antibiotics (with the exception of rifampicin and griseofulvin) are advised to use the barrier method for the period of antibiotic treatment and for 7 days after its completion.

If concomitant drug therapy continues after taking pills from a pack of CPC, the next pack of CPC should be started without a usual break.

Hepatic metabolism: interactions can occur with drugs that induce microsomal enzymes, increasing the clearance of sex hormones (e.g. phenytoin, barbiturates, primidone, carbamazepine, rifampicin, and possibly also oxcarbazepine, topiramate, felbamate, griseofulvin and drugs ( Hypericum perforatum)).

In addition, there have been reports that HIV protease inhibitors (e.g. ritonavir) and non-nucleoside reverse transcriptase inhibitors (e.g. nevirapine), as well as combinations thereof, can increase hepatic metabolism.

Hepatic-intestinal recirculation: There is information that hepatic-intestinal recirculation of estrogens may increase when certain antibiotics are prescribed (e.g. penicillin, tetracycline) as concomitant drugs, which can lead to a decrease in the concentration of ethinyl estradiol in blood plasma.

Troleandomycin may increase the risk of developing intrahepatic cholestasis while being used with CPC.

The mechanism of their action is based on the ability of these substances to increase the activity of liver enzymes. The maximum induction of enzymes, as a rule, is observed no earlier than 2-3 weeks after the start of the use of these drugs, but can persist for at least 4 weeks after their withdrawal. Cases of contraceptive failure have also been identified with the simultaneous use of antibiotics such as ampicillin and tetracycline, but the mechanism of action remains unknown.