Delsia tablets p / o, No. 21
Russian Pharmacy name:
Делсия таблетки п/о, №21
Contraception.
It is taken orally 1 time / day according to a special scheme.
Active ingredients:
Drospirenone - 3 mg
Ethinylestradiol - 30 mcg
Excipients: lactose monohydrate - 60 mg, corn starch - 12.77 mg, colloidal silicon dioxide - 0.8 mg, hypromellose 2910 - 1.6 mg, talc - 1.2 mg, magnesium stearate - 0.6 mg.
The composition of the film shell: opadry II yellow 31F82689 - 2.4 mg (hypromellose 2910 - 33%, lactose monohydrate - 28%, titanium dioxide (E171) - 22.5%, macrogol 6000 - 10%, talc - 5%, iron dye yellow oxide (E172 ) - 1.5%).
Thrombosis (venous and arterial) currently or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders);
conditions preceding thrombosis (including transient ischemic attacks, atrial fibrillation, angina pectoris) at present or in history;
the presence of multiple or pronounced risk factors for venous or arterial thrombosis, incl. complicated lesions of the valve apparatus of the heart, atrial fibrillation, diseases of the vessels of the brain or coronary arteries;
uncontrolled arterial hypertension, prolonged immobilization, volumetric surgery, surgery on the lower extremities, major injuries, smoking over the age of 35, obesity with a BMI of more than 30 kg / m2;
hereditary or acquired predisposition to venous or arterial thrombosis, such as resistance to activated protein C (APC), antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia, and the presence of antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant);
migraine with focal neurological symptoms at present or in history;
diabetes mellitus with diabetic angiopathy;
liver failure and severe liver disease (before the normalization of the indicators of liver function tests and within 3 months after the return of these indicators to normal);
liver tumors (benign or malignant), current or history;
severe or acute renal failure;
identified hormone-dependent malignant diseases (including genitals or mammary glands) or suspicion of them;
vaginal bleeding of unknown origin;
pregnancy or suspicion of it;
lactation period (breastfeeding);
pancreatitis with severe hypertriglyceridemia at present or in history;
hypersensitivity to the components of the combination.
If any of the above diseases or conditions develop for the first time against the background of the use of a drug containing this combination, then it should be immediately canceled.
Carefully
Risk factors for the development of thrombosis and thromboembolism: smoking, obesity with a BMI less than 30 kg / m2, dyslipoproteinemia, controlled arterial hypertension, migraine without focal neurological symptoms, uncomplicated valvular heart disease, the presence of thrombosis and thromboembolism in the family history, or cerebral circulation at a young age in one of the closest relatives); age over 35 in non-smoking women.
Diseases in which peripheral circulation disorders may occur: diabetes mellitus without vascular disorders, SLE, hemolytic uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia, phlebitis of superficial veins.
Hereditary angioedema.
Hypertriglyceridemia;
Liver disease of mild to moderate severity.
Diseases that first appeared or worsened during pregnancy or against the background of previous use of sex hormones (including jaundice and / or itching associated with cholestasis, cholelithiasis, otosclerosis with hearing impairment, porphyria, herpes during pregnancy in history, Sindenhem's chorea , chloasma, postpartum period).
Description:
Film-coated tablets, yellow, round, biconvex, engraved with '647' on one side and smooth on the other; in cross section: the core is from white to almost white and the film coat is yellow.
Composition for 1 tab.
Active ingredients:
Drospirenone - 3 mg
Ethinylestradiol - 30 mcg
Excipients: lactose monohydrate - 60 mg, corn starch - 12.77 mg, colloidal silicon dioxide - 0.8 mg, hypromellose 2910 - 1.6 mg, talc - 1.2 mg, magnesium stearate - 0.6 mg.
The composition of the film shell: opadry II yellow 31F82689 - 2.4 mg (hypromellose 2910 - 33%, lactose monohydrate - 28%, titanium dioxide (E171) - 22.5%, macrogol 6000 - 10%, talc - 5%, iron dye yellow oxide (E172 ) - 1.5%).
Clinical and pharmacological group: Combined hormonal contraceptive with antimineralcorticoid and antiandrogenic action
Pharmaco-therapeutic group: Combined contraceptive (estrogen + gestagen)
pharmachologic effect
Combined monophasic hormonal contraceptive. The contraceptive effect is based on the interaction of various factors, the most important of which are inhibition of ovulation, an increase in the viscosity of the cervical secretion, as a result of which it becomes impermeable to sperm.
If used correctly, the Pearl index (an indicator reflecting the number of pregnancies in 100 women who use a contraceptive drug during the year) is less than 1. If you miss a dose or use it incorrectly, the Pearl index may increase.
In a therapeutic dose, drospirenone also has antiandrogenic and weak antimineralocorticoid properties. Deprived of estrogenic, glucocorticoid and antiglucocorticoid activity, drospirenone has a pharmacological profile similar to that of natural progesterone. Possessing antiandrogenic activity, it helps to reduce the production of secretion of the sebaceous glands and improve the clinical course in women with acne (acne vulgaris). This should be taken into account when choosing a contraceptive drug, especially for women with hormone-dependent fluid retention, as well as for women with acne and seborrhea. In combination with ethinyl estradiol, it improves the lipid profile and increases the concentration of HDL.
The use of this combination regulates menstrual bleeding, helping to reduce the severity of pain and the volume of menstrual bleeding, reducing one of the risk factors for the development of iron deficiency anemia.
Pharmacokinetics
When taken orally, drospirenone is rapidly and almost completely absorbed. After a single oral administration, Cmax in blood plasma is about 35 ng / ml, Tmax in plasma is 1-2 hours. Bioavailability is 76-85%. Food intake does not affect the bioavailability of drospirenone. It binds to plasma albumin and does not bind to sex hormone binding globulin (SHBG) or corticosteroid binding globulin (CSG). The concentration of free drospirenone does not exceed 3-5% of the dose received. An estradiol-induced increase in SHBG does not affect the binding of drospirenone to plasma proteins. Average apparent Vd - 3.7 ± 1.2 l / kg. Css of drospirenone in blood plasma is reached between 7 and 14 days of treatment and is approximately 60 ng / ml. A further increase in concentration is observed between approximately 1 and 6 cycles of administration,no further increase in concentration is observed. It is metabolized in the liver with little or no involvement of the cytochrome P450 system. Plasma metabolites are mainly represented by acid forms of drospirenone, formed as a result of rupture of the lactone ring, and 4,5-dihydro-drospirenone-3-sulfate. It is metabolized almost completely. The metabolic clearance rate is 1.5 ± 0.2 ml / min / kg. Metabolites are excreted through the intestines and kidneys in a ratio of 1.2: 1.4. T1 / 2 of metabolites is about 40 hours.2 ml / min / kg. Metabolites are excreted through the intestines and kidneys in a ratio of 1.2: 1.4. T1 / 2 of metabolites is about 40 hours.2 ml / min / kg. Metabolites are excreted through the intestines and kidneys in a ratio of 1.2: 1.4. T1 / 2 of metabolites is about 40 hours.
When taken orally, ethinyl estradiol is rapidly and almost completely absorbed. After a single oral administration, Cmax is 88-100 ng / ml, Tmax 1-2 hours. It is metabolized during absorption and during the 'first pass' through the liver. Absolute oral bioavailability is 60%. Concomitant food intake decreases bioavailability in about 25% of volunteers. Plasma protein binding is about 98.5%. Ethinylestradiol induces the synthesis of SHBG in the liver. The apparent Vd of ethinyl estradiol is about 5 L / kg. The css is reached during the second half of the ingest cycle. Ethinylestradiol passes into breast milk in small amounts (0.02% of the dose taken). About 50-60% of ethinyl estradiol undergoes presystemic conjugation in the mucous membrane of the small intestine and liver ('first pass' effect).The main metabolic pathway is aromatic hydroxylation, resulting in the formation of hydroxylated and methylated metabolites, both free and in the form of conjugates with glucuronic and / or sulfuric acids. Part of ethinyl estradiol conjugated with glucuronic acid, after excretion in the bile, is reabsorbed in the intestine (enterohepatic recirculation). It is completely metabolized (practically not excreted unchanged). The metabolic clearance rate from blood plasma is 5 ml / min / kg. Ethinyl estradiol metabolites are excreted by the kidneys and through the intestines in a ratio of 4: 6, T1 / 2 is about 24 hours.conjugated with glucuronic acid, after excretion in the bile, it is reabsorbed in the intestine (intestinal-hepatic recirculation). It is completely metabolized (practically not excreted unchanged). The metabolic clearance rate from blood plasma is 5 ml / min / kg. Ethinyl estradiol metabolites are excreted by the kidneys and through the intestines in a ratio of 4: 6, T1 / 2 is about 24 hours.conjugated with glucuronic acid, after excretion in the bile, it is reabsorbed in the intestine (intestinal-hepatic recirculation). It is completely metabolized (practically not excreted unchanged). The metabolic clearance rate from blood plasma is 5 ml / min / kg. Ethinyl estradiol metabolites are excreted by the kidneys and through the intestines in a ratio of 4: 6, T1 / 2 is about 24 hours.
Indications
Contraception.
Side effect
From the immune system: rarely - bronchial asthma, hypersensitivity reactions.
From the nervous system: often - headache.
Mental disorders: often - a depressive state; infrequently - a change in libido.
From the side of the organ of hearing: rarely - hearing loss.
From the side of the cardiovascular system: often - migraine; infrequently - an increase in blood pressure, a decrease in blood pressure; rarely - thromboembolism.
From the digestive system: often - nausea; infrequently - vomiting, diarrhea.
On the part of the skin and subcutaneous tissues: infrequently - acne, eczema, itching; rarely - erythema nodosum, erythema multiforme.
On the part of the reproductive system and the mammary gland: often - menstrual irregularities, acyclic bleeding, breast tenderness, hypersensitivity of the mammary gland, leucorrhoea, vulvovaginal candidiasis; infrequently - breast enlargement, vaginitis; rarely - discharge from the mammary glands.
Others: infrequently - fluid retention, changes in body weight.
Contraindications for use
Thrombosis (venous and arterial) currently or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders); conditions preceding thrombosis (including transient ischemic attacks, atrial fibrillation, angina pectoris) at present or in history; the presence of multiple or pronounced risk factors for venous or arterial thrombosis, incl. complicated lesions of the valve apparatus of the heart, atrial fibrillation, diseases of the vessels of the brain or coronary arteries; uncontrolled arterial hypertension, prolonged immobilization, volumetric surgery, surgery on the lower extremities, major injuries, smoking over the age of 35, obesity with a BMI of more than 30 kg / m2;hereditary or acquired predisposition to venous or arterial thrombosis, such as resistance to activated protein C (APC), antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia, and the presence of antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant); migraine with focal neurological symptoms at present or in anamnesis; diabetes mellitus with diabetic angiopathy; liver failure and severe liver disease (before the normalization of the indicators of liver function tests and within 3 months after the return of these indicators to normal); liver tumors (benign or malignant), current or history; severe or acute renal failure; identified hormone-dependent malignant diseases (incl.genitals or mammary glands) or suspicion of them; vaginal bleeding of unknown origin; pregnancy or suspicion of it; lactation period (breastfeeding); pancreatitis with severe hypertriglyceridemia at present or in history; hypersensitivity to the components of the combination.
If any of the above diseases or conditions develop for the first time against the background of the use of a drug containing this combination, then it should be immediately canceled.
Carefully
Risk factors for the development of thrombosis and thromboembolism: smoking, obesity with a BMI less than 30 kg / m2, dyslipoproteinemia, controlled arterial hypertension, migraine without focal neurological symptoms, uncomplicated valvular heart disease, the presence of thrombosis and thromboembolism in the family history, or cerebral circulation at a young age in one of the closest relatives); age over 35 in non-smoking women.
Diseases in which peripheral circulation disorders may occur: diabetes mellitus without vascular disorders, SLE, hemolytic uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia, phlebitis of superficial veins.
Hereditary angioedema.
Hypertriglyceridemia;
Liver disease of mild to moderate severity.
Diseases that first appeared or worsened during pregnancy or against the background of previous use of sex hormones (including jaundice and / or itching associated with cholestasis, cholelithiasis, otosclerosis with hearing impairment, porphyria, herpes during pregnancy in history, Sindenhem's chorea , chloasma, postpartum period).
Application during pregnancy and lactation
Use during pregnancy and lactation (breastfeeding) is contraindicated.
Application for violations of liver function
Contraindicated in women with severe liver disease until the liver function tests return to normal; liver tumors (benign or malignant), currently or in history.
Application for impaired renal function
Contraindicated in severe or acute renal failure.
Application in children
The drug is indicated only after the onset of menarche.
Use in elderly patients
The drug is not indicated after menopause.
special instructions
Before starting the use of drugs containing this combination, pregnancy should be excluded and it is recommended to undergo a thorough general medical and gynecological examination, including an examination of the mammary glands and cytological examination of the cervix. In addition, a violation of the blood coagulation system should be excluded. In case of long-term use, preventive control examinations must be carried out at least once every 6 months.
A number of epidemiological studies have revealed an increase in the incidence of venous and arterial thrombosis and thromboembolism when taking COCs. The greatest risk of developing these complications exists in the first year of taking the drug (especially in the first 3 months) or resuming the drug after a 4-week break. The use of any COC can be complicated by the development of venous thromboembolism (VTE), manifested as deep vein thrombosis and pulmonary embolism. The estimated incidence of VTE in women taking oral contraceptives with a low dose of estrogen (less than 50 mcg ethinylestradiol) is up to 4 per 10,000 women per year, compared with 0.5-3 per 10,000 women who do not use oral contraceptives.
The risk of thrombosis (venous and / or arterial) and thromboembolism increases: with age, in smokers (with an increase in the number of cigarettes smoked or with increasing age, the risk further increases, especially in women over 35 years old), in the presence of a family history (i.e. venous or arterial thromboembolism ever in close relatives or parents at a relatively young age), obesity (BMI more than 30 kg / m2); dyslipoproteinemia, arterial hypertension, heart valve disease, atrial fibrillation; prolonged immobilization; temporary immobilization, including air travel for more than 4 hours; serious surgical intervention; any surgery on the lower extremities or major trauma - in these situations, it is necessary to stop taking the drug;in the case of a planned surgical intervention - 4 weeks before it and do not resume taking it within 2 weeks after the end of immobilization.
Peripheral circulatory disorders can also occur in diabetes mellitus, SLE, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis), and sickle cell anemia.
An increase in the frequency and severity of migraines during COC use (which may precede cerebrovascular disorders) may warrant immediate discontinuation of these drugs.
In rare cases, against the background of the use of COCs, the development of liver tumors was observed. In the event of severe abdominal pain, enlarged liver, or signs of intra-abdominal bleeding, this should be taken into account when making a differential diagnosis.
Recurrent cholestatic jaundice, which develops for the first time during pregnancy or during the previous intake of sex hormones, requires discontinuation of COCs.
Women with hypertriglyceridemia or a family history have an increased risk of developing pancreatitis while taking COCs.
Although a small increase in blood pressure has been described in many women taking COCs, clinically significant increases have rarely been observed. The relationship between COC intake and a clinically significant increase in blood pressure has not been established. However, if a persistent, clinically significant increase in blood pressure develops while taking COCs, discontinuation of the drug and treatment of arterial hypertension is necessary. Taking COCs can be continued after consulting a doctor if blood pressure has returned to normal with the help of antihypertensive therapy.
Although COCs can affect insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetic patients using COCs. However, women with diabetes should be closely monitored while taking COCs.
Women with a tendency to chloasma while taking COCs should avoid prolonged exposure to the sun and exposure to UV radiation.
Due to the anti-mineralocorticoid activity, drospirenone increases the concentration of renin and aldosterone in blood plasma.
Taking COCs may worsen the course of endogenous depression and epilepsy.
Ќа фоне приема ќ могут отмечатьс¤ нерегул¤рные кровотечени¤ (мажущие кров¤нистые выделени¤ или кровотечение 'прорыва'), особенно в течение первых мес¤цев применени¤. ѕоэтому оценка любых нерегул¤рных кровотечений ¤вл¤етс¤ значимой только после 3-4 мес¤цев контрацепции.
?сли нерегул¤рные кровотечени¤ повтор¤ютс¤ или развиваютс¤ после предшествующих регул¤рных циклов, следует провести тщательное обследование дл¤ исключени¤ злокачественных новообразований или беременности.
” некоторых женщин во врем¤ перерыва в приеме таблеток может не развитьс¤ кровотечение 'отмены'. ?сли прием ќ проводилс¤ в соответствии с указани¤ми, то беременность маловеро¤тна. “ем не менее, если до этого прием ќ проводилс¤ нерегул¤рно, или если отсутствуют подр¤д два кровотечени¤ 'отмены', то до продолжени¤ приема препарата необходимо исключить беременность.
Ћекарственное взаимодействие
?лительное лечение препаратами-индукторами микросомальных ферментов печени, в результате которого повышаетс¤ клиренс половых гормонов, может вести к снижению контрацептивной эффективности. таким препаратам относ¤тс¤: фенитоин, барбитураты, примидон, карбамазепин, окскарбазепин, рифампицин, рифабутин, топирамат, фелбамат, гризеофульвин и препараты, содержащие зверобой продыр¤вленный.
»нгибиторы ¬»„-протеазы (ритонавир), ненуклеозидные ингибиторы обратной транскриптазы (невирапин) и их комбинации, также потенциально могут вли¤ть на печеночный метаболизм. ћаксимальна¤ индукци¤ ферментов обычно достигаетс¤ примерно через 10 дней после начала приема этих лекарственных средств, но может сохран¤тьс¤, по крайней мере, в течение 4 недель после их отмены. ѕри одновременном приеме препаратов, вли¤ющих на индукцию микросомальных ферментов печени и в течение 28 дней после их отмены, необходимо временно использовать барьерный метод контрацепции.
онтрацептивна¤ защита снижаетс¤ на фоне приема антибиотиков пенициллинового и тетрациклинового р¤дов из-за уменьшени¤ ими внутрипеченочной циркул¤ции эстрогенов, и как следствие, понижени¤ концентрации этинилэстрадиола. ¬о врем¤ приема этих антибиотиков и в течение 7 дней после их отмены необходимо дополнительно использовать барьерный метод контрацепции.
“.к. основные метаболиты дроспиренона в плазме человека образуютс¤ без участи¤ системы цитохрома –450, ингибиторы данной ферментной системы не вли¤ют на метаболизм дроспиренона.
ѕероральные комбинированные эстроген-гестагенные контрацептивы могут вли¤ть на метаболизм других препаратов, что приводит к повышению (циклоспорин), или снижению (ламотриджин) их концентрации в плазме и ткан¤х.
‘орма выпуска/дозировка:
“аблетки, покрытые пленочной оболочкой, 3 мг+0,03 мг.
”паковка:
21 tablets in a PVC / aluminum foil blister.
1 blister, together with a pocket for carrying a blister and instructions for use, are placed in a cardboard box.
Storage conditions:
At a temperature not higher than 25 ? C.
Keep out of the reach of children.