JESS
Active material: Drospirenone, Ethinylestradiol
When ATH: G03AA12
CCF: Monophasic oral contraceptive with anti-androgenic properties
ICD-10 codes (testimony): L70, N94.3, Z30.0
When CSF: 15.11.04.01
Manufacturer: BAYER SCHERING PHARMA AG (Germany)
Pharmaceutical form, composition and packaging
Pills, Film-coated (active) light pink, round, lenticular, engraved in letters “DS” the right on one side of the hexagon; of presentations – core from white to almost white and light pink envelope (24 PC. in blister).
| 1 tab. | |
| ethinylestradiol (in the form of clathrate betadeks) | 20 g |
| Drospirenone | 3 mg |
Excipients: lactose monohydrate, corn starch, magnesium stearate.
The composition of the shell: gipromelloza, talc, Titanium dioxide, iron oxide red dye.
Pills, Film-coated (inactive) white, round, lenticular, engraved in letters “DP” the right on one side of the hexagon; of presentations – core from white to almost white and a white jacket (4 PC. in blister).
Excipients: lactose monohydrate, corn starch, povidone, magnesium stearate.
The composition of the shell: gipromelloza, talc, Titanium dioxide.
28 PC. – blisters (1) – Laptop-clamshell (1) complete with a self-adhesive admission calendar – film.
28 PC. – blisters (1) – Laptop-clamshell (3) complete with a self-adhesive admission calendar – film.
Pharmacological action
Monophasic oral contraceptive with anti-androgenic properties and antimineralocorticoid.
The contraceptive effect of COCs is based on the interaction of various factors, the most important of which are inhibition of ovulation and changes in the properties of cervical secretions, with the result that it becomes tight for spermatozoa.
When used properly, Pearl Index (number of pregnancies 100 women per year) is less than 1. When skipping pills or incorrect use Pearl Index may rise.
Women, taking combined oral contraceptives, the menstrual cycle becomes more regular, rarely observed painful menstruation, It decreases the amount of bleeding, which reduces the risk of anemia. Besides, According to epidemiological studies, with combined oral contraceptives reduce the risk of endometrial cancer and ovarian cancer.
Drospirenone, contained in the product Jess, It has antimineralokortikoidnym action. Prevents weight gain and edema, associated with fluid retention caused by estrogen, which provides a very good tolerability. Drospirenone has a positive effect on premenstrual syndrome (PMS). Jess demonstrated clinical efficacy in alleviating the symptoms of severe PMS, such as the expression of psycho-emotional disorders, breast engorgement, headache, pain in muscles and joints, weight gain and other symptoms, associated with the menstrual cycle.
Drospirenone is also possesses antiandrogenic activity and reduces acne, oily skin and hair. This action is similar to that of drospirenone natural progesterone, produced by the body.
Drospirenone has no androgenic, estrogenic, glucocorticoid and antiglucocorticoid activity. All this combined with anti-androgen action and antimineralokortikoidnym drospirenone provides biochemical and pharmacological profile, similar to natural progesterone.
In drospirenone combined with ethinylestradiol demonstrated a beneficial effect on the lipid profile, characterized by an increase in HDL.
Pharmacokinetics
Drospirenone
Absorption
When administered drospirenone is rapidly and almost completely absorbed. After a single oral administration of Cmax drospirenone in serum is reached after about 1-2 and h is about 35 ng / ml. Bioavailability – 76-85%. As compared with the reception substance fasting, food intake does not affect the bioavailability of drospirenone.
Distribution
Drospirenone binds to serum albumin and globulin binds, binding sex steroids (GTN), or corticosteroid-svyazыvayushtim globulinom (KSG). Only 3-5% the total concentration of the substance present in serum as free steroid. Ethinylestradiol-induced increase in SHBG does not affect the binding of serum proteins drospirenone. Average apparent Vd is 3.7 ± 1.2 L / kg.
During the cycle of treatment Cssmax drospirenone in serum obtained between 7 and 14 day treatment and is about 60 ng / ml. Elevated concentrations of drospirenone in serum of about 2-3 times (by cumulation), that was conditioned by the relation T1/2 in the terminal phase and the dosing interval. Further increases in serum concentrations of drospirenone notes between 1 and 6 reception cycle, after which the increase in concentration is not observed.
Metabolism
After oral administration drospirenone is extensively metabolized. Most metabolites in plasma are presented acid form of drospirenone.
Deduction
After ingestion observed biphasic reduction in serum drospirenone, with T1/2, respectively, 1.6± 0.7 h and 27 ± 7.5 h. Metabolic clearance rate of drospirenone in serum is 1.5 ± 0.2 ml / min / kg. In unaltered drospirenone appears only in trace amounts. The metabolites of drospirenone are excreted in the feces and urine at a ratio of about 1.2:1.4. T1/2 – 40 no.
Pharmacokinetics in special clinical situations
Css drospirenone in serum of women with renal insufficiency mild (CC 50-80 ml / min) They were comparable with those of women with normal renal function (CC > 80 ml / min). In women with renal insufficiency moderately (CC 30-50 ml / min) serum drospirenone was an average of 37% higher, than women with normal function nochek. Drospirenone Treatment was well tolerated in all groups. Receiving drospirenone no clinically significant effect on the concentration of potassium in the serum. Pharmacokinetics in renal failure, severe has not been studied.
Drospirenone is well tolerated by patients with mild or moderate hepatic insufficiency (Class B for Child-Pugh). Pharmacokinetics in severe hepatic impairment has not been studied.
Ethinylestradiol
Absorption
After oral ethinyl estradiol rapidly and completely absorbed. Cmax after a single oral administration is achieved through 1-2 and h is about 88-100 pg / ml. Absolute bioavailability as a result of first-pass metabolism and conjugation “first pass” through the liver is about 60%. Concomitant food intake reduces the bioavailability of ethinylestradiol in about 25% examined, whereas in other subjects such changes were noted.
Distribution
Ethinylestradiol largely, but not specifically, associated with serum albumin (about 98.5%) and causes an increase in serum concentrations of SHBG in. In Кажущийсяd is about 5 l / kg. Css achieved during the second half of the treatment cycle,, and serum levels of ethinyl estradiol increased by approximately 1.4-2.1 times.
Metabolism
Ethinylestradiol is subject to first-pass kongirovaniyu in the mucosa of the small intestine and the liver. Ethinylestradiol is primarily metabolized by aromatic hydroxylation, This produces various hydroxylated and methylated metabolites, presented in the form of free metabolites, and as conjugates with glucuronic and sulfuric acids. Ethinylestradiol completely metabolized. The rate of metabolic clearance of ethinyl estradiol is about 5 ml / min / kg.
Deduction
The concentration of ethinyl estradiol in the serum is reduced dwuhfazno, T1/2 terminal phase – 24 no. Ethinylestradiol virtually no output unchanged. Ethinylestradiol metabolites are excreted in the urine and bile in the ratio 4:6. T1/2 metabolites – 24 no.
Testimony
- Contraception;
- Treatment of moderate forms of acne (acne vulgaris);
- Treatment of a severe form of premenstrual syndrome.
Dosage regimen
Tablets should be taken in order, indicated on the packaging, every day at about the same time, with a little water. Tablets are taken without interruption in the reception. It should take 1 pi. / day successively for 28 days. Each subsequent pack should be started the day after the last tablet of the previous package.
Withdrawal bleeding, usually, It begins 2-3 days after you start taking the inactive pills and could not yet be completed before the next package.
If you do not receive any hormonal contraceptive use in the previous month
The drug begin in the 1 st day of the menstrual cycle (ie. in the 1 st day of menstrual bleeding). Shall start receiving 2-5 th day of the menstrual cycle, but in this case it is recommended to additionally use a barrier method of contraception during the first 7 days of receiving the tablets of the first package.
When switching from other combined oral contraceptive, vaginal ring or contraceptive patch
Preferably start taking the drug the next day after taking the last active tablet of the previous package, but, in any case no later than one day after the usual 7 day break (for products, containing 21 tablet) or after the last inactive tablet (for products, containing 28 tablets packaged). Jess The drug should be started on the day of removal of the vaginal ring or patch, but not later than the day, must be entered when a new ring or pasted a new patch.
When switching from contraceptives, containing only progestin (“minipill”, injectable form, implant), or a progestogen-releasing intrauterine device (Mirena)
A woman can go to the reception “minipill” Jess on any day (nonstop), with contraceptive implant or vnutrimatochnogo with gestagenom – on the day of its removal, with injectable contraceptive – in a day, when it should be done next injection. In all cases, you must use an additional barrier method of contraception during the first 7 days of tablet.
After an abortion in the I trimester of pregnancy
The woman may start taking the drug immediately. Under this condition the woman does not need any additional contraceptive measures.
After delivery or abortion in the II trimester of pregnancy
It is recommended to start taking the drug at 21-28 days after delivery or abortion in the II trimester of pregnancy. If the reception is started later, you must use an additional barrier method of contraception during the first 7 days of tablet. But, if a woman has been sexually active, before you start taking Jess pregnancy it must be excluded or must wait for the first menstruation.
Admission missed tablets
Skipping inactive pills can be ignored. Nonetheless, they should be discarded, not to accidentally extend the period of receiving the inactive pills. The following guidelines apply only to missing active pills.
If the delay in taking the drug was less 12 no, contraceptive protection is not reduced. The woman should take the missed pill as soon as possible, and should be taken at the usual time.
If the delay in pill made more 12 no, contraceptive protection may be reduced. The more missed tablets and the closer to the phase of the tablets pass reception inactive pills, the higher the probability of pregnancy.
This can be guided by the following two basic rules:
- Taking the drug should never be interrupted for more than 4 day;
- To achieve adequate suppression of the hypothalamic-pituitary-ovarian system required 7 continuous days of taking the pills.
Respectively, the delay in taking active pills was more than 12 no (the interval from the receipt of the last active pill More 36 no), we can recommend the following:
From the 1st to the 7th day
The woman should take the last missed tablet immediately, as soon as remember it, even if this means taking two tablets at the same time. Next, she continues to take tablets at the usual time. Besides, during subsequent 7 days necessary to additionally use a barrier method of contraception (eg, condom). If intercourse took place during the 7 days before skipping tablet, should take into account the possibility of pregnancy.
From the 8th to 14th day
The woman should take the last missed tablet immediately, as soon as remember it, even if this means taking two tablets at the same time. Next, she continues to take tablets at the usual time.
Given that, that women on the pill right for 7 days, preceding the first missed tablet, no need for additional measures of contraception. Otherwise, as well as the passage of two or more pills must also use a barrier method of contraception (eg, condom) during 7 days.
From the 15th to the 24th day
The risk of reduced reliability is imminent because of the approaching phase receiving inactive pills. A woman should strictly adhere to one of the two following options:. Wherein, if during 7 days, preceding the first missed tablet, all the pills are taken correctly, there is no need to use additional contraceptive methods. Otherwise, you must use the first of the following schemes and additionally use a barrier method of contraception (eg, condom) during 7 days.
1. The woman should take the last missed tablet as soon as possible, once remember (even, if it is, taking two tablets at the same time). Next take the pills at the usual time, there are no more active pills in a pack. Four inactive tablets should be discarded and immediately start taking pills of the next pack. Withdrawal bleeding is unlikely, there are no more active tablets in the second pack, but may experience spotting and breakthrough bleeding while taking the pill.
2. A woman can also interrupt taking the tablets from the current package. Then, it must take a break of not more than 4 days, including the days pass pills, and then start receiving the drug from a new package.
If the woman missed active pills, and while taking the inactive pill withdrawal bleeding has not come, Pregnancy must be excluded.
Recommendations for gastro-intestinal disorders
Severe gastrointestinal disorders may be incomplete absorption, therefore it is necessary to take additional contraceptive measures.
If during the 4 hours after receiving an active tablet will occur vomiting, should be guided by the recommendations by skipping pills. If a woman does not want to change their usual regimen and move the start of menstruation to another day of the week, additional active pill should be taken from a different package.
How to change the menstrual cycles or delay the onset of menstruation
That delay the onset of menstruation, She should continue taking pills from the next pack Jess, skipping the inactive pills from the current package. Thus, cycle can be extended, optional, at any time, there are no more active tablets in the second package. Against the background of the drug from the second package, women may experience spotting or breakthrough uterine bleeding. Regular intake Jess then resumes after the end of the reception phase inactive pills.
That postpone the start of menstruation The next day of the week, the woman should be reduced next phase of receiving the inactive tablets to the desired number of days. The shorter the interval, the higher the risk, that it will not have withdrawal bleeding, will continue to spotting and breakthrough bleeding while receiving a second package.
Side effect
When receiving combined oral contraceptives may experience irregular bleeding (spotting or breakthrough bleeding), especially during the first months of use.
While taking combined oral contraceptive in women were observed, and other undesirable effects, whose connection with the drug administration has not been confirmed, nor disproved.
The incidence of adverse events was classified as follows:: often (≥ 1/100), infrequently (≥1/1000, <1/100), rarely (<1/1000).
From the digestive system: often – nausea, abdominal pain; infrequently – vomiting, diarrhea.
CNS: often – asthenic syndrome, headache, depressed mood, mood swings, nervousness; infrequently – migraine, decreased libido; rarely – increase libido.
On the part of the organ of vision: rarely – intolerance to contact lenses (discomfort when wearing).
On the part of the reproductive system: often – breast pain, breast engorgement, menstrual disorders, vaginal candidiasis, uterine bleeding; infrequently – hypertrophy breast; rarely – vaginal discharge, discharge from the breast.
On the part of the skin and its appendages: often – acne; infrequently – rash, hives; rarely – uzlovataya эritema, erythema multiforme.
Other: often – weight gain; infrequently – fluid retention; rarely – weight loss, hypersensitivity reactions.
How and when taking other combined oral contraceptives, in rare cases may develop thrombosis and thromboembolism.
In women with hereditary angioedema estrogen may cause or aggravate the symptoms.
Contraindications
Jess drug should not be used in the presence of any of the states, listed below. If any of these conditions develop for the first time in patients receiving, the drug should be immediately abolished.
- Thrombosis (venous and arterial) and thromboembolism present or in history (incl. deep vein thrombosis, pulmonary embolism, myocardial infarction), cerebrovascular disorders;
- State, predshestvuyuschye thrombosis (incl. transient ischemic attacks, angina) in the present or past;
- Migraine with focal neurological symptoms in the present or in history;
- Diabetes with vascular complications;
- Multiple or severe risk factors for venous or arterial thrombosis (incl. complicated valvular lesions; Atrial fibrillation; cerebrovascular disease, or coronary artery; uncontrolled hypertension; major surgery with prolonged immobilization; smoking at the age of 35 years);
- Pancreatitis with severe hypertriglyceridemia now or in history;
- Hepatic failure and severe liver disease (until, liver function tests have not yet normalized);
- Liver tumors (benign or malignant) in the present or past;
- Severe renal insufficiency, acute renal failure;
- Adrenal insufficiency;
- Identification of hormone-dependent cancers (incl. genital or breast) or suspicion of them;
- Vaginal bleeding of unknown origin;
- Pregnancy or suspected it;
- Lactation;
- Hypersensitivity to any component of the drug Jess.
The use with caution
If any of the conditions / risk factors, the following, currently available, you should carefully weigh the potential risks and expected benefits of the use of combined oral contraceptive in each individual case:
- Risk factors for thrombosis and embolism (smoking; thrombosis, myocardial infarction or cerebrovascular accident at a young age in any of the next of kin; obesity; dyslipoproteinemia; arterial hypertension; migraine; valvular heart disease; irregular heartbeat; prolonged immobilization; major surgery; extensive trauma);
- Other diseases, which may occur when peripheral circulatory disorders (diabetes; systemic lupus erythematosus; hemolytic uremic syndrome; Crohn's disease and ulcerative colitis; drepanocytemia; phlebitis of superficial veins);
- Hereditary angioedema;
- Hypertriglyceridemia;
- Liver disease;
- Diseases, for the first time created or aggravated during pregnancy or previous use of the background of sex hormones (eg, jaundice, cholestasis, cholelithiasis, otosclerosis with hearing impairment, porphyria, Herpes pregnant, Huntington Sidenhema);
- Postpartum.
Pregnancy and lactation
Jess is not indicated during pregnancy and lactation.
If pregnancy is detected during treatment Jess, the drug should be immediately canceled. However, extensive epidemiological studies have revealed no increased risk of developmental defects in children, born to women, treated with sex steroids (incl. Combined oral contraceptives) before pregnancy, or teratogenicity, when sex steroids taken inadvertently in early pregnancy.
Existing data on the results of the drug during pregnancy Jess limited, that does not allow any conclusions about the impact of the drug on pregnancy, the health of the fetus and newborn. Any significant epidemiological data on drug Jess currently available.
Acceptance of combined oral contraceptives may decrease the amount of breast milk and change its composition, so, their use is not recommended until weaning. A small amount of sex steroids and / or their metabolites may be derived from human milk, but there is no confirmation of their negative impact on the health of newborn.
Cautions
If any of the conditions / risk factors, the following, currently available, you should carefully weigh the potential risks and expected benefits of the use of combined oral contraceptive in each individual case and discuss it with the woman before, she decides to start taking the drug. This weighting, first amplifying or display any of these conditions or risk factors, the woman should consult with their physician, who can decide whether to cancel the drug.
Diseases of the cardiovascular system
Available epidemiological data on the increase in the incidence of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke) while taking combined oral contraceptive. These diseases are rare. The risk of venous thromboembolism (VTЭ) is maximum in the first year of use of these drugs. The approximate incidence of VTE in women, taking low-dose oral contraceptives (< 50 mcg ethinyl estradiol), up to 4 on 10 000 person-years as compared with 0.5-3 on 10 000 person-years among women, do not use oral contraceptives. The incidence of VTE in the background of pregnancy 6 on 10 000 person-years.
The risk of thrombosis (venous and / or arterial) and thromboembolism is increased:
- With age;
- Smokers (with the number of cigarettes or increasing age the risk further increases, especially in older women 35 years). Women, receiving combined oral contraceptives, it is strongly recommended to quit smoking;
- If there is a family history (eg, venous or arterial thromboembolism ever in close relatives or parents at a relatively young age). In the case of hereditary or acquired predisposition, a woman should be assessed appropriately skilled to address the issue of the possibility of using combined oral contraceptives;
- Obesity (BMI than 30 kg / m2);
- When dislipoproteinemia;
- In hypertension;
- In migraine;
- In diseases of the heart valves;
- Atrial fibrillation;
- During prolonged immobilization, major surgery, any surgery on the legs or major trauma. In these situations it is desirable to discontinue the use of combined oral contraceptive (in the case of the planned operation, at least, four weeks before her) and not to renew the appointment within two weeks after immobilization.
The question of the possible role of varicose veins and superficial thrombophlebitis in venous thromboembolism remains controversial.
It should take into account the increased risk of thromboembolism during the postpartum period.
Peripheral circulatory disorders also may occur in diabetes, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia.
Increased frequency and severity of migraine during use of COCs (that may precede cerebrovascular disorders) It may be grounds for the immediate cessation of these drugs.
In assessing the risks and benefits should be considered, that adequate treatment of the disease may reduce the associated risk. Also note, the risk of thrombosis and thromboembolism in pregnancy higher, than when low-dose oral contraceptives (< 50 mcg ethinyl estradiol).
Tumors
The most important risk factor for cervical cancer, It is persistent human papilloma virus infection. There are reports of some increase in the risk of cervical cancer in long-term use of combined oral contraceptives. Communication with the reception combined oral contraceptives has not been proven. Reserved controversy regarding, the extent to which these findings are associated with screening for cervical pathology, or with the sexual behavior (less frequent use of barrier methods of contraception).
Meta-analysis 54 Epidemiological studies have shown, that there is a slightly increased relative risk of developing breast cancer, diagnosed in women, receiving combined oral contraceptives currently (relative risk 1.24). The increased risk gradually disappears during the 10 years after stopping these drugs. Because, that breast cancer is rare in women under 40 years, increase in the number of breast cancer diagnoses in women, taking combined oral contraceptives are currently taking or have recently, is small relative to the total risk of the disease. The observed increase in risk may be due to an earlier diagnosis of breast cancer in women, applying the combined oral contraceptives, biological effects of oral contraceptives, or a combination of both factors. Women, use the combined oral contraceptives, revealed a less pronounced clinical breast cancer, than in women, never let them to apply.
In rare cases, against the background of the use of combined oral contraceptives to observe the development of benign, and very rare – malignant liver tumors, which in some cases led to life-threatening intra-abdominal haemorrhage. In case of severe pain in the abdomen, liver enlargement or signs of intra-abdominal bleeding it should be considered in the differential diagnosis.
Other conditions
Clinical studies have shown no effect of drospirenone concentration of potassium in the serum of patients with mild to moderate renal insufficiency. There is a theoretical risk of hyperkalemia in patients with impaired renal function at the initial concentration of potassium in the ULN, at the same time taking medicines, resulting in a delay of potassium in the body. Nonetheless, in women with an increased risk of hyperkalemia it is recommended to determine the concentration of potassium in the plasma during the first cycle of the drug Jess.
In women with hypertriglyceridaemia (or the presence of this condition in the family history) may increase the risk of developing pancreatitis while taking combined oral contraceptives.
Although a slight increase in blood pressure have been reported in many women, taking combined oral contraceptives, clinically significant increase occurred rarely. Nonetheless, If while taking combined oral contraceptives develops persistent, a clinically significant increase in blood pressure, these drugs should be discontinued and treat hypertension. Acceptance of combined oral contraceptives may be continued, if using antihypertensive treatment achieved normal blood pressure values.
The following states, as reported, develop or worsen both during pregnancy, and when receiving combined oral contraceptives, but their relationship with the intake of combined oral contraceptives has not been proven: Jaundice and / or itching, associated with cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Huntington Sidenhema; Herpes pregnant; hearing loss, otosclerosis-related. Also described cases of Crohn's disease and ulcerative colitis in the background of the use of combined oral contraceptives.
In women with hereditary forms of angioedema exogenous estrogens may induce or worsen symptoms of angioedema.
Acute or chronic disturbances of liver function may require the cancellation of combined oral contraceptives until, until liver function tests have not returned to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous use of sex hormones, It requires discontinuation of combined oral contraceptives.
Although combined oral contraceptives may influence insulin resistance and glucose tolerance, no need to change the therapeutic regimen in patients with diabetes, using low-dose combined oral contraceptives (<50 mcg ethinyl estradiol). Nonetheless, Women with diabetes should be carefully observed while taking combined oral contraceptives. Sometimes it can develop chloasma, especially in women with a history of chloasma pregnant. Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to sunlight and ultraviolet radiation.
Laboratory Tests
Acceptance of combined oral contraceptives can affect the results of certain lab tests, including liver function tests, kidney, Thyroid, adrenal, level in the plasma transport proteins, carbohydrate metabolism, parameters of coagulation and fibrinolysis. Changes do not usually go beyond the normal range.
Drospirenone increases plasma renin activity and aldosterone, because of its effect antimineralokortikoidnym.
Medical examinations
Before the start or resumption of the drug Jess should be familiar with the life history, family history of women, conduct a thorough general medical (including measurement of blood pressure, Heart Rate, body mass index) and gynecological examination (including the study of mammary glands and cytological examination of cervical mucus), exclude pregnancy. The amount of additional research and the frequency of control examinations determined individually. Typically, control examinations should be carried out not less 1 per year.
It should warn the woman, that combined oral contraceptives do not protect against HIV infection (AIDS) and other diseases, sexually transmitted.
Decline in efficiency
The effectiveness of combined oral contraceptive pills can be reduced by skipping pills, with vomiting and diarrhea, or resulting from drug interactions.
Inadequate control of the menstrual cycle
While taking combined oral contraceptives may experience irregular bleeding (spotting or breakthrough bleeding), especially during the first months of use. Therefore, the evaluation of any irregular bleeding should be done only after a period of adaptation, of approximately three cycles.
If irregular bleeding or develop after repeated previous regular cycles, should conduct a thorough examination to exclude malignancy or pregnancy.
Some women during the tablet-free interval may not develop withdrawal bleeding. If combined oral contraceptives are taken according to the directions, unlikely, that a woman is pregnant. Nonetheless, Before that combined oral contraceptives taken regularly or, if there are no two consecutive withdrawal bleeding, to continue taking the drug should be excluded pregnancy.
Preclinical safety data
Preclinical data, obtained in the standard tests to identify multiple dose toxicity at doses, and genotoxicity, carcinogenic potential and toxicity to the reproductive system, It does not indicate a special risk for humans. Nonetheless, it should be remembered, that sex steroids can promote the growth of certain hormone-dependent tissues and tumors.
Effects on ability to drive vehicles and management mechanisms
Not found.
Overdose
Serious violations have been reported in overdose. In preclinical studies also observed serious adverse effects as a result of an overdose.
Symptoms, which may occur with overdose: nausea, vomiting, spotting from the vagina or metrorrhagia.
Treatment: No specific antidote, symptomatic treatment should be carried out.
Drug Interactions
The interaction of oral contraceptives with other drugs may lead to breakthrough bleeding and / or reduce the contraceptive reliability.
Effect PA hepatic metabolism
Use of drugs, inducing hepatic microsomal enzymes, can lead to increased clearance of sex hormones. These drugs include phenytoin, barbiturates, prymydon, Carbamazepine, rifampicin; also have assumptions about oxcarbazepine, topiramate, felbamate, griseofulvin and preparations, containing St. John's wort.
Inhibitors of HIV Protease (eg, ritonavir) and non-nucleoside reverse transcriptase inhibitors (eg, Nevirapine) and combinations thereof may also potentially affect hepatic metabolism.
Effect on the enterohepatic circulation.
According to separate studies, certain antibiotics (eg, penitsillinы and tetracycline) may reduce the enterohepatic circulation of estrogens, thereby, lowering the concentration of ethinyl estradiol.
During supplementation, influencing microsomal enzymes, and for 28 days after their cancellation should additionally use a barrier method of contraception.
While antibiotics (such as ampicillin and tetracycline) and for 7 days after their cancellation should additionally use a barrier method of contraception. If the period of use of barrier methods ends later, than Bean in a package, you need to go to the next package Jess without the usual tablet-free interval.
The main metabolites of drospirenone are formed in the plasma without the participation of cytochrome P450. It is therefore unlikely effect of inhibitors of cytochrome P450 metabolism drospirenone.
Combination oral contraceptives may affect the metabolism of other drugs, which leads to increased (eg, cyclosporine) or reduction (eg, lamotrigine) their concentration in the plasma and tissues.
Based on in vitro studies of the interaction, as well as in vivo study in female volunteers, prinimayushtih omeprazole, simvastatin and midazolam as markers, we can conclude, that the effect of drospirenone in a dose of 3 mg of the metabolism of other medicinal substances likely.
There is a theoretical possibility of increasing serum potassium levels in women, Jess treated concomitantly with other drugs, that may increase serum potassium levels. These medications include ACE inhibitors, angiotensin II receptor antagonists, Some anti-inflammatory drugs, potassium-sparing diuretics and aldosterone antagonists. However, studies, evaluating the interaction of drospirenone with ACE inhibitors or indomethacin, There were no significant differences between serum potassium compared with placebo. Nonetheless, female, taking medications, that may increase serum potassium levels, It is recommended to determine the concentration of serum potassium during the first cycle of receiving the drug Jess.
To identify possible interactions should read the instructions for use of the medication.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored in a dry, inaccessible to children at temperature not exceeding 30 ° C. Shelf life – 5 years.
