Index of drugs

Oral hormonal contraception. The decision to prescribe the preparation should be made on the basis of an individual assessment of risk factors in women, in particular the risk of venous thromboembolism and the risk of venous thromboembolism associated with the use of the drug in relation to other combined hormonal contraceptives.

1 tabl contains: 0.15 mg dezogestrel and 0.03 mg ethinyl estradiol (and <80 mg lactose).

A complex oral contraceptive. The contraceptive effect results from the interaction of various factors, among which the most important is the inhibition of ovulation and changes in the consistency of cervical mucus. Following oral administration, desogestrel is rapidly and completely absorbed and metabolized to etonogestrel. C_max in serum, it occurs about 1.5 hours after administration. Bioavailability is 62-81%. Etonogestrel binds to blood albumin and sex hormone binding globulin (SHBG). Only 2-4% of the drug concentration in the blood is unbound, 40-70% specifically binds to SHBG. Ethinyloestradiol-induced increases in SHBG change distribution within plasma proteins, resulting in increased SHBG-related fraction and a decrease in albumin-related fractions. Etonogestrel is completely metabolised as a result of metabolism characteristic of steroid compounds. The plasma concentration of etonogestrel decreases in two phases. The final drug distribution phase is determined by T_0,5 approximately 30 hours. Dezogestrel and its metabolites are excreted in urine and bile at a ratio of 6: 4. After oral administration, ethinyl estradiol is completely and rapidly absorbed. C_max in plasma, is achieved in 1-2 h after administration. The total bioavailability resulting from the pre-system coupling and the first pass effect is around 60%. Ethinyl estradiol binds extensively to plasma albumin with non-specific binding (approximately 98.5%) and increases SHBG in plasma. Ethinylestradiol undergoes pre-systemic coupling in the small intestine and in the liver. It is metabolized mainly by aromatic hydroxylation, resulting in the formation of numerous hydroxyl and methyl derivatives, occurring in free form and bound to glucoronides and sulphates. Plasma ethinyl estradiol concentration decreases in two phases and in the final phase T_0,5 is about 24 h. Ethinyl estradiol that is unchanged is not excreted and its metabolites are excreted in urine and bile at a ratio of 4: 6. T_0,5 ethinyl estradiol metabolites excretion is about 1 day.

Hypersensitivity to the active substances or to any of the excipients. Occurrence or risk of venous thromboembolism (VTE): venous thromboembolism - active (treated with anticoagulants) or history of venous thromboembolism, e.g. deep vein thrombosis (DVT), pulmonary embolism (PE); known hereditary or acquired predisposition for venous thromboembolic disease, eg resistance to activated C protein (APC) (including Leiden V factor), antithrombin III deficiency, protein C deficiency, protein S deficiency; extensive surgery associated with long-term immobilization; high risk of venous thromboembolism due to multiple risk factors. Occurrence or risk of arterial thromboembolism (ATE): arterial thromboembolic events - active (eg myocardial infarction) or prodromal symptoms (eg angina pectoris): cerebrovascular disease - active stroke, previous stroke or prodromal symptoms (e.g., transient ischemic attack - TIA); confirmed hereditary or acquired tendency to occur in arterial thromboembolic disorders, eg hyperhomocysteinemia and the presence of anti-phospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant); migraine with focal neurological symptoms in an interview; high risk of arterial thromboembolic events due to the presence of multiple risk factors or the presence of one of the major risk factors, such as: diabetes with vascular complications, severe hypertension, severe dyslipoproteinaemia.Pancreatitis now or in the past if associated with severe hypertriglyceridaemia. The presence of severe liver disease in the past or in the past, as long as the biochemical parameters of liver function do not return to normal. Occurring or past history of a benign or malignant liver cancer. Presence or suspicion of genital or breast malignant tumors dependent on sex hormones. Endometrial hyperplasia. Bleeding from the vagina of unknown etiology. Pregnancy or its suspicion.

The use of any combined hormonal contraceptives is associated with an increased risk of venous thromboembolism. The use of preparations containing levonorgestrel, norgestimate or norethisterone is associated with the lowest risk of venous thromboembolism. The use of other drugs such as Marvelon may be associated with a 2-fold greater risk. The decision to use the preparation from outside the lowest risk of venous thromboembolism should only be made after talking to the patient to ensure that she understands the risk of venous thromboembolism associated with the preparation, how current risk factors affect this risk and that the risk of venous thromboembolism is the highest in the first year of use. There is also some evidence that the risk is increased when combined hormonal contraceptives are taken again after an interruption of 4 weeks or more. In patients using combined hormonal contraceptives, cases of thrombosis in other blood vessels, such as the hepatic, mesenteric, renal, or retinal veins and arteries, have been reported very rarely. The risk of venous thromboembolic complications in patients using a combined hormonal contraceptive may increase significantly if additional risk factors occur, especially if there are several risk factors at the same time. The use of the preparation is contraindicated if the patient has several risk factors at the same time, increasing the risk of venous thrombosis. If a woman has more than one risk factor, it is possible that the risk increase is greater than the sum of the single factors - in this case, the overall risk of venous thromboembolism should be assessed. If the benefit-risk assessment is negative, no complex hormonal contraceptives should be prescribed. Risk factors for venous thromboembolism: obesity (BMI body mass index over 30 kg / m²) - the risk increases significantly with the increase in BMI, this is especially important for women who also have other risk factors; long-term immobilization, extensive surgery, any surgical operation in the lower limbs or pelvis, neurosurgical surgery or serious trauma - it is recommended to stop using the tablets for at least 4 weeks before the planned surgery and not to resume use within 2 weeks from the time of return for motor function (another method of contraception should be used), anticoagulant therapy should be considered if the preparation has not been discontinued early (temporary immobilization, including air travel> 4 h, may also be a risk factor for venous thromboembolism, especially in women with co-existing other risk factors); positive family history (occurrence of venous thromboembolism in siblings or parents, especially at a relatively young age, e.g. before 50) - if genetic predisposition is suspected, a woman should be referred for a decision to use a combined hormonal contraceptive consultation with a specialist; other diseases associated with venous thromboembolism (cancer, systemic lupus erythematosus, haemolytic-uremic syndrome, chronic inflammatory bowel diseases (eg Crohn's disease or ulcerative colitis) and sickle-cell anemia); age - especially at the age of over 35 years. Consensus was not reached as to the possible role of varicose veins and thrombophlebitis of surface veins on the occurrence or progression of venous thromboembolism. The increased risk of thromboembolism during pregnancy and in particular in the 6th week should be considered. postpartum period.Epidemiological studies have shown a connection between the use of hormonal contraceptives and an increased risk of arterial thromboembolism (myocardial infarction) or cerebrovascular events (eg, transient ischemic attack, stroke). Cases of arterial thromboembolic events can be fatal. The risk of arterial thromboembolism or cerebrovascular accidents in patients using combined hormonal contraceptives is increased in women who have risk factors. The use of the preparation is contraindicated if the patient has one serious or several risk factors for arterial thromboembolic events that place the patient at high risk of arterial thrombosis. If a woman has more than one risk factor, it is possible that the risk increase is greater than the sum of individual factors - in this case, the total risk should be assessed. If the benefit-risk assessment is negative, no complex hormonal contraceptives should be prescribed. Risk factors for arterial thromboembolic events: age - especially those over 35 years of age; smoking - women should be carefully instructed not to smoke if they intend to use a combined hormonal contraceptive, women over the age of 35 who have not stopped smoking should be carefully instructed to use a different method of contraception; hypertension; obesity (body mass index BMI over 30 kg / m²) - the risk increases significantly with the increase in BMI, this is especially important for women who also have other risk factors; positive family history (occurrence of arterial thromboembolism in siblings or parents, especially at a relatively young age, eg before 50) - if genetic predisposition is suspected, before a decision to use a combined hormonal contraceptive is made, the woman should be referred for consultation with a specialist; migraine - an increase in the frequency or severity of migraine during use of combined hormonal contraceptives (which may indicate the occurrence of a cerebrovascular event) may be a reason to discontinue use immediately; other conditions associated with adverse events within the vessels (diabetes, hyperhomocysteinemia, valvular heart disease, atrial fibrillation, dyslipoproteinemia and systemic lupus erythematosus). Epidemiological studies have reported an increased risk of cervical cancer in women on long-term use of combined oral contraceptives. However, the question remains to what extent the impact on the magnitude of this risk is exerted, for example, by sexual behavior including the use of mechanical contraceptives. In women taking oral contraceptives, the relative risk of breast cancer slightly increases. Increased risk gradually decreases within 10 years after discontinuation of tablets. In rare cases, mild liver cancer has been found among women using oral complex contraception, and even more rarely malignant liver tumors. In individual cases, these tumors have resulted in life-threatening bleeding into the abdominal cavity. The possibility of developing liver cancer in differential diagnosis should be considered if there is severe pain in the upper abdomen, enlargement of the liver or symptoms of intra-abdominal haemorrhage in women using contraceptive pill. The risk of developing pancreatitis may be greater in women using contraceptive pill if they or hypertriglyceridemia are diagnosed with members of the immediate family. If hypertension develops clinically relevant when using the tablets, it is recommended to discontinue the use of tablets and initiate hypertension treatment. When the blood pressure value is restored to normal, the tablets can be used again. Some diseases have been observed or exacerbated both during pregnancy or the use of combined birth control pills, but no conclusive evidence confirms the effect of birth control pills on their course: jaundice and / or pruritus associated with cholestasis, formation of gallstones, porphyria, systemic lupus erythematosus , haemolytic-uremic syndrome, Sydenham chorea, herpes of pregnant women, hearing loss due to otosclerosis, (hereditary) angioneurotic edema. acute or chronic liver problems may require discontinuation of contraceptive pills until liver function parameters return to normal. Recurrence of cholestatic jaundice, which occurred for the first time during pregnancy or during earlier use of sex hormones, is an indication for interruption of oral contraception.The use of oral contraceptives may have an effect on peripheral insulin resistance and Glucose tolerance - there is no evidence to suggest a need to change the way diabetes is treated. However, patients with diabetes who use contraceptive pills should be carefully monitored. Crohn's disease and ulcerative colitis may be associated with the use of combined hormonal contraceptives. Chloasma may occur occasionally, especially in women who have had pregnancy in the past. Women prone to chloasma should avoid solar radiation or ultraviolet radiation when using contraceptive pills. The preparation contains lactose (<80 mg) - patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type), glucose-galactose malabsorption or using a diet lacking lacotosis should take into account the dose of lactose included in the preparation. The efficacy of combined contraceptive pills can be reduced if the tablet is omitted, gastrointestinal disorders and concomitant use of other medicines. The preparation containing St. John's wort should not be used during treatment because of the risk of decreased clinical efficacy. During the use of oral contraceptives, especially during the first months, irregular bleeding (spotting, intermenstrual bleeding) may occur. Therefore, the assessment of irregular bleeding is possible only after an adaptation period of approx. 3 months. Non-hormonal causes of abnormal bleeding should be considered if persist or occur after previous regular cycles and perform appropriate diagnostic tests (with curettage of the uterine cavity, if necessary) to rule out cancer or pregnancy. In some patients, withdrawal bleeding may not take place in the intermission of tablets.

The preparation is contraindicated during pregnancy. If pregnancy occurs during use, stop taking it immediately. Most epidemiological studies do not confirm the increased risk of having a defective child if the woman used a combined hormonal contraceptive before pregnancy or the teratogenic effects of combined hormonal contraceptives on the fetus in case of inadvertent use in early pregnancy.
The risk of venous thromboembolism in women in the postpartum period should be taken into account when deciding whether to restart the treatment. The use of combined hormonal contraceptives may have an effect on breastfeeding, because these foods can reduce the amount of food and change its composition. Therefore, it is usually not recommended to use combined hormonal contraceptives during breastfeeding. Small amounts of sex hormones and / or their metabolites may be secreted with breast milk, however, no adverse effects on the health of the child were found.

Common: depressed mood, mood changes, headache, nausea, abdominal pain, pain, breast tenderness, weight gain. Uncommon: fluid retention, decreased sex drive, migraine, vomiting, diarrhea, rash, urticaria, breast enlargement. Rare: hypersensitivity, increased sexual desire, contact lens intolerance, venous thromboembolism, arterial thromboembolism, erythema nodosum, erythema multiforme, discharge, discharge from the breast, weight loss. In women using combined hormonal contraceptives, there is an increased risk of venous and arterial thrombosis and thromboembolic events, including myocardial infarction, stroke, transient ischemic attack, venous thrombosis and pulmonary embolism. In women taking oral COCs, a number of side effects have been observed: hypertension, hormone-dependent tumors (eg liver cancer, breast cancer), chloasma, Crohn's disease, ulcerative colitis, porphyria, systemic lupus erythematosus, Sydenhama chorea, haemolytic syndrome -leasuria, impaired liver function, jaundice associated with cholestasis, hearing loss due to otosclerosis, cervical cancer, hypertriglyceridaemia, (hereditary) angioneurotic edema.

Orally.The tablets should be taken in the direction of the arrows on the packaging, at the same time each day, with a little water if necessary. Taking tablets should continue for 21 days. Taking the tablets from the Next pack should begin after a 7-day break. During this interval, withdrawal bleeding usually occurs, usually 2-3 days after taking the last tablet. Bleeding may continue despite the start of taking the tablets from the next pack.Beginning of the first preparation pack. If in the previous month the patient did not use hormonal contraception (for the last month): start taking the first tablet of the preparation on the first day of the cycle, i.e. the first day of menstruation. Taking tablets can also be started between the 2nd and 5th day of the cycle, but in this case an additional method of contraception (mechanical) should be used for the first 7 days of taking the tablets in the first cycle.If the patient previously took another composite contraceptive (pill, contraceptive vaginal rings, contraceptive plasters): taking the tablets of the preparation should begin the day after the last tablet with the active substance of the previous preparation. However, no later than on the 1st day after the discontinuance or after taking the last placebo tablet the preparation was taken beforehand. If using a vaginal or transdermal system, start taking the tablets on the day the system is removed, but no later than the date when the next intravaginal or transdermal patch system would be required. If a woman has used the previous method consistently and appropriately and if she is sure she is not pregnant, then she can stop taking a complex hormone and go to another drug on any day of the cycle. The break in taking hormones in the previous method should never take longer than recommended.If the patient previously used a contraceptive containing only progestogen (mini-tablet, injections, implant, progestin-releasing intrauterine therapy): you can stop taking a mini-tablet any day (for the implant or system on the day of its removal, for the injection on the day when the next injection should be made) and the next start taking the tablets of the preparation. In all these cases, an additional method of contraception (barrier method) should be used for the first 7 days of taking tablets.After a miscarriage in the first trimester of pregnancy: taking tablets can be started immediately after a miscarriage and no additional contraception is needed.After delivery, about time or miscarriage in the second trimester of pregnancy: tablets should be started between the 21st and 28th day after the physiological birth or after a second-trimester pregnancy. In case of later start of tablets, an additional method of contraception (mechanical method) should be used for the first 7 days of taking tablets. After the intercourse, pregnancy should be ruled out before taking the tablets or wait for the first menstrual period.Proceeding in case of skipping tablets. If the delay in taking tablets is less than 12 hours, the contraceptive effectiveness is preserved, the forgotten tablet should be taken as soon as possible, and the rest as usual. If the delay is more than 12 hours, the contraceptive effectiveness of the tablet may be reduced. The procedure in the case when the patient forgot to take the tablets should comply with two basic principles: 1. The interval in taking tablets should not be longer than 7 days. 2. Take the tablets continuously for 7 days to achieve sufficient inhibition of the hypothalamus-pituitary-ovary secretion axis.Skipping tabl. in the first week of use: take the forgotten tablet as soon as possible, even if it means taking 2 tablets at the same time, and the next one as usual. For the next 7 days, use an additional method of contraception, eg a condom. It is possible to become pregnant if you have sexual intercourse during the week preceding the forgotten tablet. The risk of getting pregnant is the higher the higher the number of tablets you forget and the closer you are to a regular break in taking the tablets.Skipping tabl. in the second week of use: take the tablet as soon as possible, even if it means taking 2 tablets at the same time, and the next tablets should be taken as usual. If during the 7 days preceding forgetting, the tablets were taken correctly, no additional contraceptive methods are required. If the above condition was not met or the patient forgot to take more than one tablet, an additional method of contraception should be recommended for the next 7 days.Skipping tabl. in the third week of use: due to the closeness of the interruption in taking tablets, the risk of decreasing the contraceptive effectiveness increases sharply. However, reduced contraceptive efficacy can be prevented by adjusting the pattern of tablets. There are two options for taking the tablets without the need for an additional method of contraception, provided that within 7 days before forgetting the tablet, the patient took the tablets correctly. In another case, the patient should use the first of the two options listed below and at the same time use an additional contraceptive method for 7 days. 1. Take the forgotten tablet as soon as possible, even if it means taking 2 tablets at the same time and the next as usual. After taking the last tablet from the pack, the next day you should start taking the tablets from the new package, ie without taking a break. The withdrawal bleeding may only occur after you have finished taking the tablets from the second pack. However, staining or minor breakthrough bleeding may occur during the administration of tablets. 2. You can also advise stopping taking the remaining tablets from the packaging. Then take a 7-day or shorter break in taking the tablets, including the days you have forgotten to take your tablets and start taking the tablets from the new packaging. If you forget to take your tablet and you do not have the expected withdrawal bleeding in the first tablet-free break, you should consider the possibility of pregnancy.Proceedings in the case of gastrointestinal disorders. In the case of severe gastrointestinal disturbances, the absorption may have been impaired, then an additional method of contraception should be used. If vomiting occurs within 3 to 4 hours after taking the tablet, the absorption may have been impaired. It is a situation similar to forgetting a tablet, so you should act as if you forget it. If the patient does not want to change the pattern of taking tablets should take an additional tablet of the preparation from a different package.Proceedings in the event of a change in the starting day or delay of the date of bleeding. The preparation is not indicated for delaying the start of the bleeding. However, if in exceptional situations, there is a need to delay the day of bleeding, the tablets should be started from the next pack of the preparation, without taking a 7 day break. You can take the tablets from this package until it is depleted. Staining or minor breakthrough bleeding may occur during this time. To return to regular tablets, a 7-day break should be done before starting a new pack. In order to change the day of withdrawal bleeding, the patient should be advised to shorten the interval in taking tablets for as many days as needed. Shortening the break carries a greater risk that bleeding will not occur at all, and intermenstrual bleeding or spotting during intake of tablets from the next packet may occur (as in the case of delaying the time of bleeding).