Producer: Gedeon Richter (Gedeon Richter) Hungary
ATC code: G03AB03
Farm group:
Release form: Solid dosage forms. Pills.
General characteristics. Compound:
Active ingredients: Tablets I: contain 0.03 mg ethinylestradiol and 0.05 mg levonorgestrel,
Tablets II: contain 0.04 mg ethinylestradiol and 0.075 mg levonorgestrel,
Tablets III: contain 0.03 mg ethinylestradiol and 0.125 mg levonorgestrel.
Excipients Tablets I.
Shell: sucrose, talc, calcium carbonate, titanium dioxide (E171), copovidone, macrogol 6000, colloidal silicon dioxide, povidone, carmellose sodium, iron oxide red (E172).
Tablets II.
Core: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg).
Shell: sucrose, talc, calcium carbonate, titanium dioxide (E171), copovidone, macrogol 6000, colloidal silicon dioxide, povidone, carmellose sodium.
Tablets III.
Core: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg).
Shell: sucrose, talc, calcium carbonate, titanium dioxide (E171), copovidone, macrogol 6000, colloidal silicon dioxide, povidone, carmellose sodium, yellow iron oxide (E172).
Pharmacological properties:
Pharmacodynamics. Combined (three-phase) oral contraceptive estrogen-progestogen drug. When taken, it inhibits the pituitary secretion of gonadotropic hormones.
Sequential administration of film-coated tablets, a drug containing different amounts of progestogen (levonorgestrel) and estrogen (ethinyl estradiol) provides blood concentrations of these hormones close to their concentrations during normal menstrual cycle, and contributes to the secretory transformation of the endometrium. The contraceptive effect is associated with several mechanisms. Under the influence of levonorgestrel, a blockade of the release of releasing factors (luteinizing and follicle-stimulating hormones) of the hypothalamus occurs, inhibition of the secretion of gonadotropic hormones by the pituitary gland, which leads to inhibition of the maturation and release of an egg ready for fertilization (ovulation). Ethinylestradiol maintains a high viscosity of cervical mucus (makes it difficult for spermatozoa to enter the uterine cavity). Along with the contraceptive effect, the menstrual cycle is normalized due to the replenishment of the level of endogenous hormones with the hormonal components of Tri-Regol® tablets. In seven-day periods, when the next break in taking the drug follows, comes.
Pharmacokinetics. Levonorgestrel is rapidly absorbed (less than 4 hours). Levonorgestrel does not have a "first pass" effect through the liver. The half-life is 8-30 hours (average 16 hours). Most of the levonorgestrel in the blood binds to albumin and sex hormone-binding globulin.
Ethinylestradiol is rapidly and almost completely absorbed from gastrointestinal tract. The maximum plasma concentration is reached in the range of 1-1.5 hours. The half-life is 26 ± 6.8 hours. Ethinylestradiol has a “first pass” effect through the liver (the so-called “first pass” effect). Metabolism is carried out in the liver and intestines.
When administered orally, ethinylestradiol is excreted from the blood plasma within 12 hours.
Metabolites of ethinylestradiol: water-soluble derivatives of sulfate or glucuronide conjugation, enter the intestine with bile, where they are disintegrated by intestinal bacteria. 60% of levonorgestrel is excreted by the kidneys, 40% - through the intestines, 40% of ethinylestradiol is excreted by the kidneys and 60% - through the intestines.
Indications for use:
Dosage and administration:
Using the drug for the first time:
Take orally, at the same time of the day, if possible in the evening, without chewing and drinking a small amount of liquid.
For the purpose of contraception in the first cycle, Tri-Regol® is prescribed 1 tablet daily. for 21 days, starting from day 1 of the menstrual cycle, then a 7-day break is taken, during which typical menstrual bleeding occurs. The next package containing 21 film-coated tablets should be taken on the 8th day after a 7-day break.
The drug is taken as long as there is a need for contraception.
When switching from another oral contraceptive to taking Tri-Regol®, a similar scheme is used.
After an abortion, it is recommended to start taking the drug on the same or the next day after the operation.
After childbirth, the drug is recommended only for women who are not breastfeeding.
Reception should begin no earlier than the first day of menstruation, cycle.
During lactation, the use of the drug is contraindicated.
If a woman has not taken Tri-Regol® within the prescribed period, the missed pill should be taken within the next 12 hours. If 36 hours have passed after taking the pill, contraception cannot be considered reliable. However, in order to avoid intermenstrual bleeding, it is necessary to continue taking the drug from the already started package, minus the missed tablet(s). At this time, it is recommended to additionally use another, non-hormonal method of contraception (for example, barrier).
Application Features:
Before starting the use of the drug, it is necessary to exclude pregnancy, conduct a general medical and gynecological examination (examination of the mammary glands, cytological analysis of the smear).
While taking the drug, regular gynecological examinations are required every 6 months.
The use of oral contraceptives is allowed no earlier than 6 months after the viral infection and subject to the normalization of hepatic functions.
When there is a sharp pain in upper divisions abdomen, hepatomegaly, or signs of intra-abdominal hemorrhage may be suspected. In this case, the drug should be discontinued.
With the appearance of acyclic spotting, it is possible to continue taking the drug Tri-Regol® after the exclusion of organic pathology by the attending physician.
If detected during the use of the drug, the question of the advisability of continuing to take Tri-Regol® should be decided.
In case of or taking the drug should be continued, while it is recommended to additionally use another, non-hormonal method of contraception.
At least 3 months before the planned pregnancy, the drug should be stopped.
Under the influence of oral contraceptives (due to the estrogen component), some laboratory parameters may change (functional parameters of the liver, kidneys, adrenal glands, thyroid gland, indicators of blood coagulation and fibrinolytic factors, levels of lipoproteins and transport proteins).
The drug should be stopped immediately the following cases:
- with a first-time or intensified migraine-like or unusually strong, with an acute deterioration in visual acuity, with a suspicion of a heart attack;
- at sharp rise blood pressure, the appearance of jaundice or hepatitis without jaundice, the occurrence of generalized itching or increased epileptic seizures;
- at the onset of pregnancy;
- 6 weeks before the planned operation, with prolonged immobilization (for example, after injuries).
The effect of the drug on the ability to drive a car and other mechanisms
Taking the drug does not affect the ability to drive a car and work with other mechanisms.
Side effects:
Side effects observed during the use of the drug, classified into categories depending on the frequency of their occurrence: very often ≥1 / 10; often >1/100, ≤1/10, sometimes ≥1/1000, ≤1/100; rarely ≥1/10000, ≤1/1000; very rarely ≤1/10000 including individual messages.
Nausea, vomiting, headache, engorgement of the mammary glands, weight gain, decreased libido, depressed mood, intermenstrual, in some cases - swelling of the eyelids, blurred vision, discomfort when wearing contact lenses(these phenomena are temporary and disappear after discontinuation without prescribing any therapy). Rarely, an increase in the concentration of triglycerides, blood glucose, a decrease in glucose tolerance, an increase in blood pressure, jaundice, hepatitis, liver adenoma, gallbladder diseases (for example, cholelithiasis,) thrombosis and venous, hair loss, increased vaginal discharge, vaginal candidiasis, increased fatigue, diarrhea. At long-term use very rarely, generalized itching, calf muscles, an increase in the frequency of epileptic seizures, and coarsening of the voice may occur.
Interaction with other drugs:
The drug should be used with caution while taking:
Ampicillin, rifampicin, chloramphenicol, neomycin, polymycin B, sulfonamides, tetracyclines, dihydroergotamine, tranquilizers, phenylbutazone, since these drugs can weaken the contraceptive effect, it is recommended to additionally use a different, non-hormonal contraceptive method;
- anticoagulants, coumarin or indandione derivatives (it may be necessary to determine the prothrombin index and change the dose of the anticoagulant);
- tricyclic antidepressants, maprotiline, beta-blockers (may increase bioavailability and therefore toxicity);
- oral hypoglycemic drugs, insulin (it may be necessary to change their doses);
-bromocriptine (decreased effectiveness);
-drugs with possible hepatotoxic effects, especially dantrolene (risk of increased hepatotoxicity, especially in women over 35 years of age).
Contraindications:
Hypersensitivity to any component of the drug.
Pregnancy, lactation period, severe, liver tumors, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), cholelithiasis, cholecystitis,; the presence or indication of a history of severe cardiovascular (including decompensated) and cerebrovascular changes, thromboembolism and a predisposition to them, deep veins lower extremities, hormone-dependent malignant neoplasms genital organs and mammary glands (including suspicion of them), family forms
Tri-Regol is an estrogen-progestin contraceptive for oral use.
Release form and composition of Tri-Regol
The drug is available in the form of coated tablets of three types: pink; white and yellow.
The main active ingredients of the tablets are levonorgestrel and ethinylestradiol.
As excipients they use: magnesium stearate, colloidal silicon dioxide, lactose monohydrate, talc, corn starch.
Tablets differ in the number of main active ingredients.
Pharmacological action of Tri-Regol
Tri-Regol is a three-phase oral contraceptive drug based on estrogens and gestagens. Taking Tri-Regol contributes to the inhibition of pituitary secretion of gonadotropic hormones.
This drug contains various amounts of estrogen and progestogen, supports these hormones in female body at a level close to the normal menstrual cycle.
The contraceptive effect of Tri-Regol is based on the action of several mechanisms. Under the action of levonorgestrel, the release of releasing factors of the hypothalamus is blocked and the secretion of gonadotropic hormones is inhibited. As a result, the maturation of the egg and its release are inhibited. Ethinylestradiol maintains a significant viscosity of the cervical mucus, which leads to difficulty in the movement of spermatozoa to the uterine cavity.
Indications for use Tri-Regol
According to the instructions, Tri-Regol is used for oral contraception.
Contraindications
According to the instructions, Tri-Regol is not prescribed for:
- cholecystitis;
- severe liver disease;
- chronic colitis;
- liver tumors;
- cholelithiasis;
- congenital syndromes of Rotor, Dubin-Johnson, Gilbert;
- phlebitis of the deep veins of the legs;
- severe cardiovascular, cerebrovascular changes, thromboembolism in history and at present, as well as with a predisposition to them;
- malignant neoplasms of the mammary glands and genital organs (hormone-dependent);
- prolonged immobilization;
- family forms of hyperlipidemia;
- extensive injuries;
- arterial hypertension;
- chronic hemolytic anemia;
- availability surgical interventions and at surgical operations on foot;
- pancreatitis in history and at present;
- sickle cell anemia;
- jaundice due to the use of drugs containing steroids;
- severe forms of diabetes;
- cystic skid;
- vaginal bleeding of unknown cause;
- migraine;
- glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
- otosclerosis with worsening during pregnancy;
- idiopathic jaundice of pregnant women, herpes of pregnant women, severe skin itching of pregnant women;
- hypersensitivity to the components included in the drug;
- pregnancy and lactation;
- smoking over the age of 35;
and over 40 years of age.
Tri-Regol is carefully prescribed for:
- compensated diabetes mellitus without vascular complications;
- varicose disease;
- arterial hypertension with blood pressure less than 160/100;
- epilepsy;
- multiple sclerosis;
- porphyria;
- small chorea;
- tetany;
- bronchial asthma;
- depression;
- mastopathy;
- uterine myoma;
- tuberculosis;
as well as in adolescence, when a regular ovulatory cycle has not yet been established.
How to use Tri-Regol and dosage
The drug is intended for oral administration.
Tri-Regol tablets are taken at the same time, mostly in the evening. They should be swallowed whole with a few sips of water.
In the first cycle, the drug is taken every day, 1 tablet from the first day of the cycle for 21 days, then there is a break (7 days) when menstrual bleeding occurs. After a break, the next package of the drug, designed for 21 days, begins.
Reception of Tri-Regol should be carried out as long as there is a need for contraception.
If the next dose of the drug is missed, then you need to drink a pill in the next 12 hours. But if more than 36 hours have passed after taking Tri-Regol, then contraception with this drug is not reliable. Therefore, an additional non-hormonal method of contraception is required.
Side effects of Tri-Regol
According to reviews, Tri-Regol can cause side effects.
Reproductive system: decreased libido, breast engorgement, intermenstrual bleeding.
Nervous system: depressed mood, headache.
Digestive system: nausea, vomiting.
Sense organs: swelling of the eyelids, blurred vision, conjunctivitis.
Metabolism: weight gain.
Skin: chloasma.
Overdose
According to reviews of Tri-Regol, an overdose of the drug is manifested by nausea and uterine bleeding.
If these symptoms occur in the first 2-3 hours, it is necessary to perform a gastric lavage and apply symptomatic treatment measures.
Interaction with other drugs
When taking Tri-Regol simultaneously with:
- rifampicin, ampicillin, neomycin, chloramphenicol, polymyxin B, tetracyclines, sulfonamides, dihydroergotamines, tranquilizers, phenylbutazone - the contraceptive effect of the drug is weakened;
- derivatives of indandione or coumarin, anticoagulants - it may be necessary to unscheduledly determine the prothrombin index and adjust the dose of the anticoagulant;
- maprotiline, tricyclic antidepressants, beta-blockers - the toxicity of these drugs may increase;
- oral hypoglycemic drugs and insulin - their doses may need to be adjusted;
- drugs with a possible hepatotoxic effect - the risk of increased hepatotoxicity increases.
special instructions
If hepatomegaly, sharp pain in the upper abdomen or signs of intra-abdominal hemorrhage occur, Tri Regol must be canceled.
In the presence of acyclic spotting after the exclusion of organic pathologies, you can continue to take the drug.
If a woman is planning a pregnancy, then Tri-Regol should be canceled three months before the planned pregnancy.
With vomiting or diarrhea, you should continue to take the drug, but you need to use an additional non-hormonal method of contraception.
Cancellation of Tri-Regol occurs in the following cases:
- at the onset of pregnancy;
- 6 weeks before the planned surgery;
- with a sharp increase in blood pressure, an increase in epileptic seizures, the occurrence of hepatitis or jaundice, generalized itching;
- with unusually severe headache, acute visual impairment, suspected heart attack or thrombosis.
Storage conditions Tri Regola
Tri-Regol is stored in a place protected from children at a temperature of 15-30ºС.
Combined oral contraceptives.
Composition Tri-regol
Ethinylestradiol + Levonorgestrel.
Manufacturers
Gedeon Richter A.O. (Hungary)
pharmachologic effect
Combined hormonal contraceptive for oral administration.
Suppresses ovulation by blocking the release of FSH and LH in the pituitary gland, promotes the secretory transformation of the endometrium.
Increases the viscosity of cervical mucus, which prevents the penetration of spermatozoa.
Consistent administration of tablets of the drug containing different amounts of progestogen (levonorgestrel) and estrogen (ethinyl estradiol) allows you to replenish and ensure the concentration of these hormones in the blood, close to physiological, with the subsequent normalization of the menstrual cycle.
When taken orally, the active substances are quickly and completely absorbed from the gastrointestinal tract.
Excreted by the kidneys and intestines.
Side effects Tri-regol
Dyspepsia, mastalgia, weight gain or loss, decreased glucose tolerance, changes in libido, vaginal bleeding, headaches, mood lability, fatigue, convulsions in calf muscles, skin rashes.
Indications for use
Contraception; Menstrual disorders.
Contraindications Tri-regol
Pregnancy; - lactation period breastfeeding); - severe liver disease; - hereditary hyperbilirubinemia (Gilbert's syndrome, Dubin-Johnson syndrome, Rotor's syndrome); - cholecystitis; - chronic colitis; - heavy cardiovascular diseases(including history); - cerebrovascular diseases (including history); - thromboembolism and predisposition to them; - tumor of the liver; - breast or endometrial cancer; - family forms of hyperlipidemia; - heavy arterial hypertension; - heavy diabetes; - sickle cell anemia; - chronic hemolytic anemia; - bleeding from the vagina unclear etiology; - migraine; - otosclerosis (aggravated during previous pregnancies); - severe idiopathic jaundice during pregnancy in history; - heavy pruritus with a history of pregnancy; - herpetic infection with a history of pregnancy; - hypersensitivity to the components of the drug.
Method of application and dosage
For the purpose of contraception:
- inside,
- 1 tab. from the 1st-5th day of menstruation,
- preferably before bed.
Start with taking ocher-yellow tablets (6 days), then take apricot-pink tablets (5 days) and then for 10 days - tablets white color.
After a week break (at this time menstrual-like bleeding occurs), the next 21-day course is started.
For medicinal purposes:
- the dosing regimen is determined individually.
Overdose
No information.
Interaction
The effect is reduced by inducers of microsomal oxidation (rifampicin, barbiturates, phenytoin), antibiotics a wide range(tetracyclines), sulfonamides, pyrazolone derivatives.
special instructions
Drugs should be used as prescribed by a doctor.
Before starting the use of the drug, it is necessary to exclude the presence of pregnancy, to conduct a general medical and gynecological examination (measuring blood pressure, determining the level of glucose in the urine, examining liver function, examining the mammary glands, cytological analysis of a smear).
Women over 35 years of age who take a hormonal contraceptive are advised to completely stop smoking, because. smoking while taking hormonal contraceptive increases the risk of developing diseases of the cardiovascular system, in particular thrombosis and thromboembolism.
If pregnancy is planned, the intake should be stopped 3 months before its expected onset and a non-hormonal method of contraception should be used.
Active ingredients:
I. One pink film-coated tablet contains ethinylestradiol 0.03 mg and levonorgestrel 0.05 mg
II. One white film-coated tablet contains 0.04 mg ethinylestradiol and 0.075 mg levonorgestrel
III. One dark yellow film-coated tablet contains 0.03 mg ethinylestradiol and 0.125 mg levonorgestrel.
Excipients:
Tablets I.
Sheath: Carmellose sodium, povidone, iron oxide red (E172), anhydrous colloidal silicon dioxide, macrogol 6000, copovidone, titanium dioxide (E171), calcium carbonate, talc, sucrose.
Tablets II.
Core: Silica colloidal anhydrous, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg). ^ ^
Sheath: Carmellose sodium, povidone, anhydrous colloidal silicon dioxide, macrogol 6000, copovidone, titanium dioxide (E171), calcium carbonate, talc, sucrose. Tablets III.
Core: Silica colloidal anhydrous, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg).
Sheath: Sodium carmellose, iron oxide yellow (E172), povidone, colloidal anhydrous silicon dioxide, macrogol 6000, copovidone, titanium dioxide (E171), calcium carbonate, talc, sucrose.
Description
Tablets I.
Pink, round biconvex film-coated tablets with glossy
surface
Tablets II.
White, round, biconvex film-coated tablets with glossy
surface
Tablets III.
Dark yellow, round, biconvex film-coated tablets with a glossy surface.
Indications for use
Tri-Regol is a hormonal contraceptive. Combined contraceptives act by inhibiting the action of gonadotropins. Although the primary mechanism of action of the drugs is to inhibit ovulation, they also cause other changes, including changes in the consistency of cervical mucus, which makes it difficult for sperm to pass into the uterine cavity, as well as changes in the endometrium, which reduces the likelihood of implantation The drug should be taken only as directed and under regular medical supervision .
Contraindications
In the presence of pregnancy, severe liver disease, impaired fat metabolism, severe hypertension, severe diabetes mellitus and vaginal bleeding of unknown cause. The drug should also not be taken with previously transferred jaundice or herpes during pregnancy and with the following previously transferred or present conditions:
- diseases with the formation of blood clots (formation of a blood clot in the vessels) and with a predisposition to these diseases^,
- Liver tumor -
- a malignant tumor of the mammary glands or uterus.
Among women using hormonal contraceptives, the risk of certain diseases (eg, thromboembolic diseases, myocardial infarction, cerebral stroke) may increase. The risk of developing these diseases increases with age (over 35), especially among smokers. Therefore, women over 35 years of age are advised to completely stop smoking.
Pregnancy and lactation
If pregnancy is detected, the drug should be stopped immediately, because according to some studies, taking oral hormonal contraceptives in early period pregnancies slightly increase the risk of fetal malformations.
Breast-feeding: Hormonal contraceptives can reduce lactation and change the composition of milk, and also pass into breast milk in small amounts, so the use of the drug during breast-feeding is not indicated.
Dosage and administration
The drug should be taken at the dose and for the time determined by the doctor. Taking the drug for the first time:
Use one film-coated tablet per day, preferably at the same time of day.
The drug should be started on the first day of the menstrual cycle and continued for 21 days. After this, it is necessary to take a seven-day break, during which menstrual-like bleeding occurs. The beginning and the correct sequence of taking the drug (first 6 pink, then 5 white and then 10 dark yellow tablets) are indicated by numbers and an arrow on the blister.
The next 21-day cycle of taking the drug should be started after a 7-day break. So each cycle starts on the same day of the week.
Switching to Tri-Regol after taking ANOTHER combination drug for 21 days:
The drug Tri-Regol should be taken according to the above scheme. The first Tri-Regol tablet should be taken on the first day after a seven-day break. If the previous contraceptive contained 22 tablets, the first tablet Tri-Regol must be taken on the first day after a six-day break. If the previous contraceptive contained 28 tablets, the first tablet of Tri-Regol should be taken without interruption. §*”
v S *
Switching to taking the drug Tri-Regol after taking the drug "mini", which contains a progestogen
The first Tri-Regol tablet should be taken on the first day of menstruation, even if the mini tablet has already been taken. In this case, there is no need to use an additional method of contraception.
In the presence of vomiting or diarrhea, it is necessary to additionally use another (non-hormonal) method of contraception.
With the appearance of intermenstrual bleeding, you should continue taking the drug, since bleeding usually stops spontaneously. If the bleeding does not stop or recurs, you should consult a doctor.
If no bleeding occurs during the 7-day break, pregnancy should be excluded.
After childbirth or after an abortion, the course of administration can be started as directed by the doctor, but not earlier than the first day of the second menstruation.
If, for medical reasons, an earlier start of contraception is justified, then the drug should be started on the first day of the first menstruation, but in the first two weeks it must be combined with another (non-hormonal) method of contraception.
Side effect
Triregol, like all medicines, can cause side effects.
While taking the drug, nausea, vomiting, headache, tension of the mammary glands, changes in body weight and libido, depressed mood, chloasma (pigment spots), discomfort when wearing contact lenses, intermenstrual bleeding, increased blood pressure, increased blood glucose , skin rash, the appearance of a condition with the formation of blood clots (thrombosis), diseases of the liver and gallbladder, fatigue, diarrhea.
Inform your doctor about the appearance of the above complaints or symptoms.
Overdose
If you have taken more than the prescribed dose of the drug, contact your doctor immediately.
Children who have accidentally taken large doses of oral contraceptives do not have severe abnormalities, so there is no need for drug treatment with an overdose. If an overdose of the drug is detected within 2-3 hours, a gastric lavage should be performed. There is no specific antidote, treatment is symptomatic.
Interaction with other drugs
Be sure to tell your doctor or pharmacist if you are taking or have recently taken any medicines, including medicines sold without a doctor's prescription.
The drug should be used with caution simultaneously with:
- ampicillin, rifampicin, chloramphenicol, neomycin, penicillin B, sulfonamides, tetracyclines, dihydroergotamine, tranquilizers, phenylbutazone (the contraceptive effect may decrease, therefore it is necessary to use another, non-hormonal contraceptive method),
- anticoagulants, coumarin or indandione derivatives (it is necessary to re-determine the prothrombin time and, if necessary, change the dose of the anticoagulant),
- tricyclic antidepressants, maprotiline, beta-blockers (their bioavailability and toxicity may increase),
- oral antidiabetic agents, insulin (it may be necessary to change the dose of these agents),
- bromocriptine (decreased effectiveness),
- hepatotoxic drugs, especially with dantrolene (the risk of hepatotoxicity increases, especially in women over 35 years of age).
Tri-Regol- a three-phase oral hormonal contraceptive that has an inhibitory effect on ovulation. Contains levonorgestrel and ethinylestradiol.
Combined oral contraceptives block the action of gonadotropins. The primary action of these drugs is aimed at inhibiting ovulation. The drug causes a change in the cervical mucus, which makes it difficult for sperm to pass into the uterine cavity and affects the endometrium, thereby reducing the possibility of implantation of a fertilized egg. All this contributes to the prevention of pregnancy.
Pharmacokinetics.
Levonorgestrel.
Absorption: when taken, levonorgestrel is rapidly and completely absorbed from the gastrointestinal tract. Bioavailability - almost 100% due to the lack of primary metabolism.
Distribution most of Levonorgestrel binds to plasma proteins, mainly to albumin and sex hormone-binding globulin.
Metabolism: Basically, it consists in the elimination of the Δ 4-3-oxo group and hydroxylation at positions 2 α, 1b and 16b, after which conjugation occurs. Most of the metabolites that circulate in the blood are 3α,5b-tetrahydro-levonorgestrel sulfates. Excretion of the drug occurs mainly in the form of glucuronides. Some primary levonorgestrel also circulates as 17b-sulfate. Metabolic clearance is marked by individual variability, which may partly explain the significant differences in levonorgestrel concentrations that are observed in patients.
Conclusion: The half-life of levonorgestrel shows individual variability and is approximately 36 hours at steady state. Levonorgestrel is excreted in the urine
(40-68%) and feces (16-48%) in the form of metabolites (sulfate and conjugates with glucuronic acid).
Ethinylestradiol.
Absorption: ethinylestradiol is absorbed rapidly and almost completely, the maximum concentration in blood serum is reached after 1.5 hours. After presystemic conjugation and metabolism, the absolute bioavailability is 60%. The area under the curve and Cmax may increase slightly over time.
Distribution Ethinylestradiol is 98% bound to plasma proteins, mainly to albumin.
Metabolism Ethinylestradiol is cleaved by presystemic conjugation. 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-ethinylestradiol and 2-methoxy-ethinylestradiol. Both ethinylestradiol and the metabolites of the first phase are excreted as conjugates (sulfates and glucuronides) into the bile and enter the hepato-intestinal circulation.
Conclusion: ethinylestradiol is excreted from blood plasma with an elimination half-life, which averages 29 hours (26-33 hours); plasma clearance varies in the range of 10-30 l / h. Withdrawal of conjugates of ethinylestradiol and its metabolites with urine and feces in a ratio of 1: 1.
Indications for use:
A drug Tri-Regol intended for oral contraception.
Mode of application:
Inside, in the order indicated on the package, at about the same time, one tablet a day, with a small amount of liquid.
Using the drug for the first time
Tri-Regol apply from the 1st day of menstruation, 1 tablet per day for 21 days. Starting on days 2-7 is also possible, but during the first cycle it is recommended to additionally use a non-hormonal method of contraception (such as condoms or spermicides) during the first seven days of taking the pills.
Since the composition of the tablets different color is different, in the first 6 days you should take pink tablets, over the next 5 days - white tablets, after which you should take dark yellow tablets for 10 days. The sequence of taking tablets of different colors is indicated by numbers and arrows on the package.
After the end of 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 contraception is necessary, a 21-day course of Triregol should be started again. With regular intake of Tri-REGOL, the contraceptive effect is maintained even during a 7-day break.
According to the indicated scheme, Tri-Regol should be taken as long as prevention of pregnancy is desired.
Switching to Tri-Regol from another oral contraceptive: The first Tri-Regol tablet should be started the day after you took the last active (hormone-infused) tablet from the blister pack of the previous contraceptive - no later than 1 day after the usual break in use previous combined hormonal contraceptive (or after taking the last placebo pill from the previous package).
Switching to the drug Tri-Regol from a progestogen-only product (low-dose oral contraceptive, injection, implant or intrauterine device): switching from a low-dose oral contraceptive can be done on any day of the menstrual cycle (from the implant and intrauterine device the day after they are removed from the injection - in the day the next injection is due). In this case, it is recommended to additionally use a 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 drug should be started immediately on the same day after the operation. Additional methods of contraception are not required.
After childbirth or abortion in the second trimester of pregnancy, the drug should be started in a woman who is not breastfeeding, 21-28 days after childbirth or abortion in the second trimester of pregnancy. If the start of oral contraception using the drug Tri-Regol occurs later, then it is necessary to additionally use a barrier method of contraception during the first 7 days of taking the tablets.
If sexual intercourse has already taken place, pregnancy should be excluded before taking the pills, or taking the pills should be postponed until the first menstrual bleeding.
Breast-feeding: For information on use while breast-feeding, see the Use During Pregnancy or Lactation section.
Missed pills: If a woman does not take a pill in time for any reason, she should take it within 12:00. In this case, there is no need to use additional methods contraception. Other tablets should be taken at the usual time.
If more than 12:00 has passed, you must take the last missed tablet as soon as you remember it, even if you have to take two tablets on the same day. Then continue taking the drug as usual. In this case, additional non-hormonal methods of contraception (barrier methods, spermicides) must be used for the next 7 days.
If there are less than 7 tablets left in the current package, you should start taking the tablets from the next package immediately after taking the last tablet from the current package; this means that there should be no pause between packs. In this case, withdrawal bleeding is not expected until the end of the second pack; however, spotting and breakthrough bleeding may occur.
If withdrawal bleeding does not occur after completion of the second pack, pregnancy should be excluded until the tablets from the next pack are resumed.
Gastrointestinal diseases: in the presence of vomiting or diarrhea, the effectiveness of the drug decreases due to incomplete absorption active ingredients. Use additional non-hormonal methods of contraception (barrier methods, spermicides) while symptoms are present and for the next 7 days to prevent premature bleeding.
With vomiting or acute diarrhea that developed within 3-4 hours after taking the pill, see the tips described in the Missed pills section.
How to stop menstrual bleeding.
To delay menstrual bleeding, taking Tri-Regol tablets from a new package should be started with dark yellow tablets (last phase) the day after the end of the current package, without a pause between them.
The duration of the delay in menstrual bleeding depends on the number of dark yellow tablets consumed from the second package. During given period breakthrough bleeding or spotting may occur. Regular intake of Tri-Regol can be restored after the usual 7-day break.
There have been reports of the following serious adverse reactions in women using COCs, detailed information about which is presented in the section "Peculiarities of use": venous and arterial thromboembolic complications; arterial hypertension; liver tumors; diseases that may develop or worsen with the use of COCs, although the evidence for this fact is inconclusive, include: Crohn's disease, ulcerative colitis, epilepsy, migraine, endometriosis, uterine myoma, porphyria, systemic lupus erythematosus, herpes of pregnancy, chorea; hearing loss associated with otosclerosis; hemolytic-uremic syndrome, cholestatic jaundice; chloasma; acute and chronic hepatic disorders can lead to interruption of COC intake to normalize liver function.
The frequency of breast cancer diagnosis is slightly higher among PDA users. Since breast cancer is rarely diagnosed in women under 40 years of age, the overdiagnosis of breast cancer in women taking or recently taking COCs is small compared to the overall risk of developing breast cancer. A causal relationship with CPC has not been elucidated. More detailed information is indicated in the sections "Contraindications" and "Peculiarities of use".
In women with hereditary angioedema, the use of estrogens may induce or exacerbate the symptoms of angioedema.
Contraindications:
Combined oral contraceptives (COCs) are not recommended to be taken in the presence of diseases and pathological conditions below.
With the development of such diseases with the use of COCs, the drug should be stopped immediately:
- pregnancy or suspected pregnancy, breastfeeding period
- hypersensitivity to the components of the drug
- the presence or reference to a history of arterial or venous thromboembolic diseases (for example, deep vein thrombophlebitis, thromboembolism pulmonary artery) in combination with risk factors or without them (see section "Peculiarities of application");
- 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 attack of ischemia, angina pectoris);
- the presence or indication of a history of cerebrovascular accident
Severe or multiple risk factors for venous or arterial thrombosis may currently be considered a contraindication (see section 4.4).
section "Peculiarities of application");
- cardiovascular diseases (heart disease, heart rhythm disturbances, heart valve pathology)
- severe course of hypertension;
- diabetes mellitus with vascular disorders;
- ophthalmic disorders of vascular origin;
- a history of severe liver disease until liver function returns to normal;
- the presence or indication of a history of liver tumors (benign or malignant)
- migraine in history with focal neurological symptoms;
- diagnosed or suspected malignant tumors that are caused by sex steroids (eg, genital or mammary glands);
- vaginal bleeding of unknown etiology.
Pregnancy:
When pregnancy is established, taking the drug Tri-Regol should be stopped immediately.
If a woman becomes pregnant while taking the pills, further use should be stopped immediately.
The results of a large number of epidemiological studies have not found any increased risk of birth defects in children, born of women who used COCs before pregnancy, nor teratogenic effects in case of inadvertent use of birth control pills in early pregnancy.
Breastfeeding. Hormonal contraceptives can reduce excretion and change the composition of milk, and also penetrate in small amounts into breast milk Therefore, taking these drugs during breastfeeding is contraindicated.
Interaction with other drugs:
Interactions between the CCP and others medicines may lead to deterioration in the effectiveness of the contraceptive and / or breakthrough bleeding and / or ineffectiveness of this method of contraception.
Women who are taking any of these drugs are advised to temporarily use a barrier or other method of contraception in addition to COCs. When taking drugs that induce liver enzymes, the barrier method is required for use during the entire course of treatment with such drugs and for 28 days after its completion.
For women who are taking antibiotics (with the exception of rifampicin and griseofulvin), it is recommended to use the barrier method during the period of antibiotic treatment and for 7 days after its completion.
If concomitant drug therapy continues after the end of the tablets from the PDA pack, the next PDA pack should be started without the usual break.
Hepatic metabolism: Interactions may occur with drugs that induce microsomal enzymes, increasing the clearance of sex hormones (eg, phenytoin, barbiturates, primidone, carbamazepine, rifampicin, and possibly also oxcarbazepine, topiramate, felbamate, griseofulvin, and drugs containing St. John's wort (Hypericum perforatum).
In addition, there have been reports that HIV protease inhibitors (eg, ritonavir) and non-nucleoside reverse transcriptase inhibitors (eg, nevirapine) and combinations thereof may increase hepatic metabolism.
Hepatic recirculation: There is information that hepatic estrogen recirculation may increase when certain antibiotics (eg, penicillin, tetracycline) are prescribed as concomitant medicinal products, which may lead to a decrease in serum ethinyl estradiol concentrations.
Troleandomycin may increase the risk of intrahepatic cholestasis when administered concomitantly with COCs.
The mechanism of their action, 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 may persist for at least 4 weeks after their withdrawal. Cases of contraceptive failure have also been reported with concomitant use of antibiotics such as ampicillin and tetracycline, but the mechanism of action remains unknown.
In the case of short-term use of any of these drugs that cause an increase in liver enzymes, it is recommended to use additional barrier methods of contraception from the moment the use of these drugs is started, during the entire period of treatment and within 4 weeks after their withdrawal. Women who receive these antibiotics in a short course should temporarily use barrier methods of contraception simultaneously with contraceptive pills, that is, during the period of concomitant use. medicinal product and within 7 days after its cancellation. If the next package of Tri-Regol tablets ends earlier than the period of time that requires the use of additional contraceptives, you should start the tablets from a new package without interrupting the drug. In this case, "withdrawal bleeding" should not be expected until the pills from the second package run out. If the patient does not experience "withdrawal bleeding" after finishing taking the pills from the second pack, she should consult a doctor to rule out pregnancy. In the case of long-term use of these drugs, patients are advised to use other contraceptives.
St. John's wort (Hypericum perforatum) herbal preparations are not recommended to be administered simultaneously with these drugs, as this leads to a potential decrease in the contraceptive effect of Tri-Regol tablets. There have been reports of breakthrough bleeding and unintended pregnancy. The decrease in the contraceptive effect persists for at least 2 weeks after stopping treatment with St. John's wort.
There have been reports of elevated plasma concentrations of cyclosporine with concomitant use of COCs. PDAs were found to be able to induce the metabolism of lamotrigine resulting in sub-therapeutic plasma levels of lamotrigine.
Laboratory research. The use of steroidal contraceptives may affect the results of certain laboratory research, including biochemical parameters of liver, thyroid, adrenal and kidney function at the level of plasma proteins, for example, GCS-binding globulin and lipid / lipoprotein fraction; indicators of carbohydrate metabolism and indicators of blood coagulation and fibrinolysis. Changes usually do not exceed the laboratory limits of the norm.
Overdose:
Symptoms of an accidental drug overdose Tri-Regol: severe headache, dyspeptic disorders (nausea, vomiting). Vaginal bleeding due to drug withdrawal.
Treatment: the drug is canceled, treatment is symptomatic. There is no specific antidote.
If an overdose is detected within 2-3 hours and it is significant, then it is possible to perform a gastric lavage.
Storage conditions:
Store at a temperature not exceeding 25 0 С.
Keep out of the reach of children!
Release form:
Tri-Regol - coated tablets.
Packing: combi-packing: 21 tablets in a blister (6 pink tablets, 5 white tablets, 10 dark yellow tablets), 1 or 3 blisters together with a cardboard case for storing a blister in a pack.
Compound:
1 tablet Tri-Regol pink contains ethinylestradiol 0.03 mg, levonorgestrel 0.05 mg
1 tablet Tri-Regol white contains ethinylestradiol 0.04 mg, levonorgestrel 0.075 mg
1 tablet Tri-Regol dark yellow contains ethinylestradiol 0.03 mg, levonorgestrel 0.125 mg
Excipients: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose, carmellose sodium, povidone, polyethylene glycol (macrogol 6000), iron oxide red (E172), iron oxide yellow (E172), copolyvidone, titanium dioxide (E 171) , calcium carbonate, sucrose.
