Julia is used to treat or relieve symptoms of the following diseases: Dysfunctional Uterine Bleeding, Osteoporotic Fractures, Premenstrual Dysphoric Disorder, Menstrual Irregularities, Vulvovaginal Atrophy, Estrogen Deficiency, Vasomotor Symptoms, Hirsutism, Dysmenorrhea, Endometriosis,
Drospirenone is a progestin-only birth control pill that is used to prevent pregnancy.
Julia is a drug made in Malta. You need a doctor's prescription to buy it. But its analogues can be bought online anywhere in the world without going to a specialist.
Drospirenone is a complete analogue of Julia. It has the same composition, dosage and methods of use. Also Drospirenone has a lower cost compared to Julia.
To buy Julia, click on the "buy now" button and then in our online store select the medicine and the desired dosage. Follow the instructions below.
Free delivery is valid for purchases from $200. We deliver medicines around the world and provide the best prices.
You can also use a coupon giving a 5% discount.
Get emergency medical help if you have even mild symptoms: stomach cramps, breast tenderness; problems with contact lenses, a change in the pattern or severity of migraine headaches; or missed/irregular periods, nipple discharge, nausea, vomiting; loss of scalp hair,
Tell your doctor if you have ever had:
Tell your doctor if you are pregnant or breastfeeding. Stop taking drospirenone if you become pregnant.
Heparin: May enhance the hyperkalemic effect of Drospirenone. Monitor therapy
Artemether: May decrease the serum concentration of Progestins (Contraceptive). Management: Consider the use of an alternative (i.e., non-hormonal) means of contraception in all women of childbearing potential who are using artemether. Consider therapy modification
Eslicarbazepine: May decrease the serum concentration of Progestins (Contraceptive). Management: Alternative, non-hormonal means of birth control should be considered for women of child-bearing potential. Consider therapy modification
Food reduces the rate of absorption, but not the extent of absorption.
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One of the most important extragenital effects of endogenous progesterone is its antimineralcorticoid effect as a natural aldosterone antagonist. Aldosterone, supporting the active absorption of sodium and excretion of potassium and hydrogen ions with urine in the distal renal tubules, performs the biological function of a regulator of extracellular metabolism and water metabolism. In the luteal phase of the menstrual cycle, against the background of increased secretion of progesterone, an increase in natriuresis occurs .
Estradiol and synthetic estrogens have the opposite sodium progesterone-saving effect, which is mainly due to an increase in the synthesis of angiotensinogen in the liver and, accordingly, an increase in the level of angiotensin, the main stimulant for the production of aldosterone. Synthetic progestogens, derivatives of 17a-hydroxyprogesterone and 19-nortestosterone, have no antimineralcorticoid effect and do not counteract the stimulating effect of estrogen on the renin – angiotensin – aldosterone system (RAAS). The result of sodium and fluid retention in women taking estrogen-containing drugs for contraception and hormone replacement therapy (HRT) can be an increase in body weight due to fluid retention, swelling and increased blood pressure in predisposed women.
Drospirenone is a new progestogen, a derivative of 17a – spironolactone, the spectrum of effects of which is progestogen, antimineralocorticoid and antiandrogen characteristic of natural progesterone. The antimineralocorticoid activity of drospirenone is 8 times higher than that of spironolactone (a diuretic with antimineralcorticoid activity) [5,6].
The results of this property of the drug is a decrease in body weight and a decrease in systolic and diastolic blood pressure. The loss of sodium in the body caused by drospirenone does not lead to a clinically significant increase in potassium concentration, which allows it to be used even in women with impaired renal function .
In a study by Oelkers et al. a significant increase in cumulative sodium excretion was found in the group of healthy women who received 2 mg of drospirenone compared with the placebo group . It should also be noted an increase in the level of aldosterone in plasma and its excretion in the urine, which, according to the authors, characterizes the compensatory activation of RAAS in response to a change in the electrolyte composition of the blood.
As part of the same study, it was shown that drospirenone significantly increases plasma renin activity, and this effect does not depend on the dose of the drug. In addition, a slight decrease in body weight was found in patients taking a drug containing 30 μg of ethinyl estradiol and 3 mg of drospirenone (Yarina) [8,9], in contrast to women taking a contraceptive containing 30 μg of ethinyl estradiol in combination with 150 μg of desogestrel, in which, on the contrary, there was a slight increase in body weight [10,11].
These data indicate that drospirenone in the composition of COCs is able to effectively counteract estrogen-dependent sodium and fluid retention.
Drospirenone is also an antagonist of androgen receptors. Antiandrogenic activity of drospirenone is 5–10 times stronger than progesterone, but lower than cyproterone acetate [12-14].
Combined oral contraceptives (COCs), by inhibiting the secretion of androgens by the before begin, have a positive effect on acne and seborrhea. In addition, ethinyl estradiol (EE) causes an increase in the concentration of sex steroid binding globulin (SHGS), which reduces the free fraction of androgens in blood plasma. The severity of the androgenic effect of the progestogen, which is part of the combined preparations, significantly affects the effects of EE, such as an increase in SHG and antiatherogenic changes in the spectrum of lipoproteins. Drospirenone does not lower the level of SHGS  and has an antiatherogenic effect on lipid metabolism .
The use of combined estrogen – progestogen preparations containing drospirenone for contraception and hormone replacement therapy provides additional benefits related to the pharmacological and clinical features of this progestogen.
Modern hormonal contraceptives provide a real opportunity to control the timing of pregnancy and thus reduce the risk of maternal mortality associated with abortion. However, this does not limit their effect on reproductive health. Estrogen-progestogen contraceptives have numerous non-contraceptive prophylactic and therapeutic effects: they reduce the profusion, duration and pain of menstrual blood loss, positively affect the skin condition, reduce the risk of anemia, ectopic pregnancy, inflammatory diseases of the pelvic organs, benign and malignant neoplasms of the ovaries, endometrial cancer.
Currently, according to WHO (2001), about 100 million women use hormonal methods of contraception. There is no doubt that the relevance of hormonal contraception will increase in the future.
The new progestogen drospirenone is part of the combined low-dose monophasic contraceptive Yarin (Schering AG, Germany), containing 30 μg EE and 3 mg drospirenone.
As you know, the effectiveness of contraceptive methods is determined by the number of pregnancies that occur in 100 women in the first 12 months of contraceptive use (Pearl Index). For Yarina, this figure is 0.07, which meets the criteria for a highly effective contraceptive .
Studies of the julia of COC use have shown that about 30% of women stop using drugs during the first year . The main reason for the withdrawal of COCs are side effects . Side effects such as weight gain, engorgement and tenderness of the mammary glands, increased blood pressure are associated with the effect of EE on RAAS.
Due to the antimineralcorticoid activity, drospirenone prevents the retention of sodium and fluid in the body, which maintains stability of body weight, blood pressure and prevents breast engorgement when taking Yarina. During the first month of admission, headache, tension of the mammary glands, decreased libido, depression are found in 3.1–4.6%; nausea - in 4.6–6.2% of cases. By the sixth month of treatment, all of the above symptoms are mostly resolved .
The healing properties of COC
Drospirenone, which has an effect similar to spironolactone on RAAS, opens up new therapeutic possibilities for using COCs.
This primarily relates to the treatment of premenstrual syndrome (PMS). Not less than 95% of women of reproductive age, to one degree or another, have symptoms such as irritability (93.8%), engorgement and tenderness of the mammary glands (87.5%), flatulence (75%), to one degree or another several days before menstruation. headache (56.3%), mood changes with a tendency to depression (56.3%), swelling (50%) .
The use of COCs is the most common therapeutic tactic for PMS. However, the severity of the symptoms of PMS is not always reduced, and may even worsen, due to a deficiency of natural progesterone.
Numerous clinical studies have shown the positive effect of the drug Yarin on the somatic and psycho-emotional symptoms of PMS.
In an open, uncontrolled study by Apter D. et al. [twenty]. The effectiveness of the drug was evaluated in 336 women aged 18 to 42 years using the The Psychological General Well-Being Index (PGWBI) health questionnaire, which includes indicators such as anxiety, decreased mood, general well-being, ability to control their emotions, and overall health activity. After three cycles of treatment, there was a tendency to improve, and after six cycles, for example statistically significant increase in overall well-being was revealed. In addition, an assessment was made of the severity of somatic symptoms. The reduction of symptoms of bloating and engorgement of the mammary glands occurred by the 6th cycle of taking the drug, respectively, in 77.3 and 69% of women. In addition, in 52% of cases, patients noted a decrease in swelling of the limbs. Body weight remained stable or even decreased slightly. Despite the fact that the placebo group was not provided in this study, this drawback was offset by the duration of treatment (12 months), as it is known that after 3 to 6 months the placebo effect is leveled .
In another study conducted in the USA in 2002, Borenstein J. et al. assessed the effect of the drug on premenstrual symptoms and quality of life in more than a thousand women with PMS. Premenstrual symptoms and quality of life were evaluated before treatment and after two cycles of therapy. The use of Yarina has led to an improvement in the physical and psycho-emotional symptoms of PMS, as well as general well-being and quality of life .
Boschitsch E. et al. studied the effectiveness of the use of Yarina and a drug containing 30 μg of EE and 150 μg of desogestrel in the treatment of PMS. In the group of women receiving Yarina, a significant decrease in body weight was noted. In addition, there was a statistically significant decrease in the severity of premenstrual symptoms, such as depressed mood, fluid retention, and increased appetite. The drug had a positive effect on skin manifestations. The number of acne elements decreased by 62.5%, seborrhea decreased by 25.1%. After the study, 75.6% of women expressed a desire to continue taking the drug .
In a study by Brown C. et al. 326 women aged 18 to 35 completed the 23-component Women’s Health Assessment Questionnaire at the beginning of the follow-up and after the completion of the 6th cycle of Yarina's intake. At the end of the 6th cycle, improvement was noted on scales characterizing fluid retention and emotional status. It should be emphasized that the results were similar in groups of patients who had not previously used oral contraceptives and who used OCs that did not contain drospirenone .
In a randomized, placebo-controlled study, Freeman E.W. et al. The effectiveness of the drug Yarina was studied for 3 menstrual cycles in 82 women with severe Remember that, the so-called premenstrual dysphoric syndrome. Patients who received treatment with a drug containing EE and drospirenone showed a significantly more pronounced improvement in the indicators of the COPE questionnaire (the Calendar of Premenstrual Experiences) for all 22 points. A significant difference between the groups was obtained by factor 3 - constant increased appetite, acne [25,26].
In all of the studies described above, the standard regimen for taking the drug was used: taking the 21st tablet, followed by a seven-day break. It is known that it is during this period of time that women taking oral contraceptives often experience symptoms of PMS .
The use of the extended COC regimen, when the patient receives the drug daily for 9-12 weeks and only then takes a break, increases the effectiveness of PMS therapy. In this case, a decrease in symptoms was noted by 74% of women . In the case of using such a regimen, bleeding breakthroughs are quite rare, a menstrual-like reaction occurs when tablets are canceled .
Given these data, a study was conducted on the use of Yarina in extended mode . It was attended by 1,433 women, 175 of whom received the drug continuously for 42–126 days. It was shown that swelling of the extremities decreased by 49% in patients taking the drug in extended mode compared with 34% in patients using the standard 21-day regimen. The soreness of the mammary glands decreased by 50 and 40%, respectively, the feeling of bloating by 37 and 29%. Also, an extended intake regimen for women with acne is also more effective. The breakthrough bleeding rate was 15% at the beginning of therapy and tended to decrease with continued use of the drug. No increase in the incidence of other side effects has been observed.
Thus, the extended regimen can be used to increase the therapeutic effectiveness of Yarina.
The antiandrogenic properties of COCs with drospirenone are due to several mechanisms: the suppression of ovulation, the ability of drospirenone to block androgen receptors and the absence of a decrease in the concentration of sex steroid-binding globulin .
The use of the drug Yarina is pathogenetically substantiated in women with overweight or high blood pressure when taking combined contraceptives, as well as requiring treatment in connection with premenstrual syndrome, acne, mild arterial hypertension or "idiopathic edema".
Hormone replacement therapy with drospirenone
Discontinuation of the estrogen-producing function of the ovaries, leading to the development of vasomotor symptoms, sleep disturbance, decreased resistance to psychological and emotional stress, urogenital and sexual disorders, changes in appearance, osteoporosis, back pain and fractures, significantly reduces the quality of life of older women. Correction of all these manifestations is the goal of hormone replacement therapy in peri- and postmenopausal women.
Drospirenone is part of a combination preparation for continuous HRT in postmenopausal women Angelique (Schering AG, Germany), containing 17b-estradiol and 2 mg of drospirenone.
The use of drospirenone in a combination preparation for HRT, similar to Yarina, reduces the frequency of side effects (such as mastodynia, swelling, weight gain due to fluid retention) and improves tolerance to therapy. Increasing the acceptability of therapy (“compliance”) is an essential condition for its maximum effectiveness, since prophylactic effects are achieved only with a sufficient duration of estrogen therapy. In addition, the anti-aldosterone effect of drospirenone is especially important for women in older age groups who have a higher incidence of hypertension and coronary heart disease.
It is known that check renin – angiotensin – aldosterone system has a multicomponent effect on the function of the cardiovascular system. Angiotensin II has a strong direct vasoconstrictor effect on the arteries and a less strong vasoconstrictor effect on the veins. In addition, angiotensin II serves as the main stimulant for the production of aldosterone, the main regulator of water-electrolyte balance, acting through mineralocorticoid receptors in the distal tubules of the kidneys.
At the same time, it has been relatively recently discovered that aldosterone receptors are also located in other organs, including the brain, blood vessels, and heart . This indicates the role of aldosterone in the physiology and pathology of the cardiovascular system. Excessive synthesis of aldosterone, which always accompanies the course of heart failure, leads to stimulation of fibroblasts, which, in turn, causes an increase in collagen synthesis, development of interstitial fibrosis, impaired functional activity of the myocardium with the development of diastolic dysfunction of the left ventricle. In addition, excessive synthesis of aldosterone contributes to an increase in sodium reabsorption, loss of potassium, and water retention in the renal tubules, which, in turn, leads to an increase in circulating blood volume and, as a result, to overload of the left ventricle of the heart with volume and pressure, which also leads to progression heart failure.
The effect of aldosterone on the development of cardiovascular pathology includes effects on cardiac and vascular fibrosis, hypertension, endothelial dysfunction, suppression of fibrinolysis, and heart rhythm disturbance. It has been shown that the use of the aldosterone receptor blocker spironolactone reduces blood pressure, improves endothelial function, reduces left ventricular hypertrophy, reduces the incidence of fatal arrhythmias and, as a result, leads to a 30% reduction in mortality among patients with severe cardiac pathology .
In large cohorts of patients, it was shown that the circulatory level of norepinephrine, renin, angiotensin II, aldosterone, endothelin-1 and adrenomedulin correlates with both the severity and prognosis of chronic heart failure. In particular, there is a complex relationship between the activity of the renin – angiotensin – aldosterone system and the overproduction of endothelin – 1. As the Framingham Offspring Study (Framingham, Massachusetts) showed, even in normotensive individuals, a single measurement in the morning hours of aldosterone made it possible to predict the likelihood of high blood pressure several years later.
In a multicenter study, serum potassium and blood pressure were studied in postmenopausal women 45–70 years old who did not have diabetes and received the drug Angelik and angiotensin converting enzyme inhibitors or angiotensin II receptor blockers . In the examined women, the hypotensive effect of HRT was noted. In addition, hyperkalemia was not detected in any of the observed groups.
The antihypertensive effect was also confirmed by the results of a 12-week, multicenter, randomized, double-blind, placebo-controlled study of the effect of the drug Angelic on blood pressure in 212 postmenopausal women with moderate hypertension (blood pressure within 140 / 90–159 / 99 mm Hg). Compared with the placebo group in women who used Angelique, there was a significant decrease in blood pressure and the absence of significant changes in serum potassium content .
The presented research results indicate the new julias of combined estrogen – progestogen preparations containing drospirenone as a progestogen component. Due to the antimineral corticoid and antiandrogenic effect of drospirenone, the contraceptive drug Yarina has good tolerance associated with maintaining a stable weight, no increase in blood pressure, improving skin condition, and effectiveness in relieving premenstrual symptoms. In addition, data have been obtained indicating the potential of HRT with drospirenone to reduce the risk of cardiovascular disease in postmenopausal women.
1. Andreeva E.N. et al. New possibilities of progestogens: drospirenone - a progestogen with antimineralcorticoid properties. Russian Bulletin of the Obstetrician-Gynecologist. 2004; 6.
2. Pasman N.M. Yarina is the first experience of using oral contraceptive with medicinal properties in Novosibirsk. Russian Bulletin of the Obstetrician-Gynecologist. 2005; 1.
3. Megevitinova EA, Prilepskaya VN Premenstrual syndrome. Gynecology 2002; application: 3–8.
4. Oelkers W. Drospirenone, a progestogen with antimineralocorticoid properties: a short review. Mol Cell Endocrinol. 2004 Mar 31; 217 (1–2): 255–61.
5. Losert W, Casals – Stenzel J, Buse M. Progestogens with antimineralcorticoid activity. Arzneimittelforschung 1985; 35: 459–71.
6. Muhn P, Fuhrmann U, Fritzemeier KH, et al. Drospirenone: a novel progestogen with antimineralcorticoid and antiandrogenic activity. Ann N Y Acad Sci 1995; 761: 311–35.
7. Oelkers W, Berger V, Bolik A, et al. Dihydrospirorenone, a new progestogen with antimineralcorticoid activity: effects on ovulation, electrolyte excretion, and the rennin – aldosterone system in normal women. J Clin Endocrinol Metab 1991; 73: 837–42.
8. Oelkers W, Helmerhorst FM, Wuttke W, et al. Effect of an oral contraceptive containing drospirenone on the rennin – angiotensin – aldosterone system in healthy female volunteers. Gynecol Endocrinol 2000; 14: 204–13.
9. Oelkers W, Foidart JM, Dombrovicz, et al. Effects of a new oral contraceptive containing an antimineralcorticoid progestogen, drospirenone, on the rennin – aldosterone system, body weight, blood pressure, glucose tolerance, and lipid metabolism. J Clin Endorinol Metab 1995; 80: 1816–21.
10. Huber J, Foidart JM, Wuttke W, Efficacy and tolerability of a monophasic oral contraceptive containing ethynilestradiol and drospirenone. Eur J Contracept reprod Health Care 2000; 5: 25–34.
11. Foidart JM, Wuttke W, Bouw GM, et al. A comparative investigation of contraceptive reliability, cycle control and tolerance of two monophasic oral contraceptives containing either drospirenone or desogestrel. Eur J Contracept Reprod Health Care 2000; 5: 124–34.
12. Huber J, Foidart JM, Wuttke W, Efficacy and tolerability of a monophasic oral contraceptive containing ethynilestradiol and drospirenone. Eur J Contracept reprod Health Care 2000; 5: 25–34.
13. Oelkers W, Berger V, Bolik A, et al. Dihydrospirorenone, a new progestogen with antimineralcorticoid activity: effects on ovulation, electrolyte excretion, and the rennin – aldosterone system in normal women. J Clin Endocrinol Metab 1991; 73: 837–42.
14. Fuhrmann U, Krattenmacher R, Slater EP, et al. The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception 1996; 54: 243–51.
15. van Vloten WA, van Haselen CW, van Zuuren EJ, Gerlinger C, Heithecker R. The effect of 2 combined oral Contraceptives containing either drospirenone or cyproterone acetate on acne and seborrhea. Cutis 2002 Apr; 69 (4 Suppl): 2–15.
16. Gaspard U, Endrikat J, Desager JP, Buicu C, Gerlinger C, Heithecker R. A randomized study on the influence of oral contraceptives containing ethinylestradiol combined with drospirenone or desogestrel on lipid and lipoprotein metabolism over a period of 13 cycles. Contraception 2004 Apr; 69 (4): 271–8.
17. Huber J, Foidart JM, Wuttke W, Efficacy and tolerability of a monophasic oral contraceptive containing ethynilestradiol and drospirenone. Eur J Contracept reprod Health Care 2000; 5: 25–34
18. Pinter B. Continuation and compliance of contraceptive use. Eur J Contracept Reprod Health Care. 2002 Sep; 7 (3): 178–83. Review PMID: 12428939.
19. Aubeny E. et al. Oral contraception: patterns of non – compliance. The Coraliance study. Eur J Contracept Reprod Health Care. 2002 Sep; 7 (3): 155–61.
20. Apter D, Borsos A, Baumgartner W, Melis GB, Vexiau – Robert D, Colligs – Hakert A, Palmer M, Kelly S. Effect of an oral contraceptive containing drospirenone and ethinylestradiol on general well – being and fluid – related symptoms. Eur J Contracept Reprod Health Care. 2003 Mar; 8 (1): 37-51.
21. Wiklund I, Dimenas E, Wahl M. Factors of importance when evaluating quality of life in clinical trials. Control Clin Trials 1990; 11: 169–79.
22. Borenstein J, Yu HT, Wade S, Chiou CF, Rapkin A. Effect of an oral contraceptive containing ethinyl estradiol and drospirenone on premenstrual symptomatology and health – related quality of life. J Reprod Med. 2003 Feb; 48 (2): 79–85.
23. Boschitch E, Skarabis H, Wuttke W et al. The acceptability of a novel oral contraceptive containing drospirenone and its effect on well – being. The Eur J of Contracept and Reprod Health Care 2000; 5 (suppl 3): 34–40.
24. Brown C, Ling F, Wan J. A new monophasic oral contraceptive containing drospirenone. Effect on premenstrual symptoms. J Reprod Med. 2002 Jan; 47 (1): 14–22.
25. Freeman EW, Kroll R, Rapkin A, Pearlstein T, Brown C, Parsey K, Zhang P, Patel H, Foegh M; PMS / PMDD Research Group. Evaluation of a unique oral contraceptive in the treatment of premenstrual dysphoric disorder. J Womens Health Gend Based Med. 2001 Jul – Aug; 10 (6): 561–9.
26. Freeman EW. Evaluation of a unique oral contraceptive (Yasmin) in the management of premenstrual dysphoric disorder. Eur J Contracept Reprod Health Care. 2002 Dec; 7 Suppl 3: 27–34; discussion 42–3.
27. Sulak P, Scow RD, Preece C, et al. Hormone withdrawal symptoms in oral contraceptive users. Obstet Gynecol 2000; 95: 261–6.
28. Sulak PJ, Cressman BE, Waldrop E, et al. Extending the duration of active oral contraceptive pills to manage hormone withdrawal symptoms. Obstet Gynecol 1997; 89: 179–83
29. Clarke AK, Miller SJ. The debate regarding continuous use of oral contraceptives. Ann Pharmacother 2001; 35: 1480–4.
30. Sillem M, Schneidereit R, Heithecker R, et al. Use of an oral contraceptive containing drospirenone in an extended regimen. Eur J Contracept Reprod Health Care 2003; 8: 162–169.
31. Mansour D Experiences with Yasmin: the acceptability of a novel oral contraceptive and its effect on well – being. Eur J Contracept reprod Health Care. 2002 Dec; 7 Suppl 3: 35–41.
32. Stier TC, Koenig S, Lee DY, Chawla M, Frishman W. Aldosterone and aldosterone antagonism in cardiovascular disease: focus on eplerenone (Inspra) Heart Dis 2003; 5: 102–118.
33. Preston RA, White WB, Pitt B, Norris PM, Foegh M, Hanes V. Drospirenone / estradiol effect on serum potassium of postmenopausal women at risk for hyperkalemia. Obstet Gynecol 2004; 103: 4; 26S – 27S.
34. White WB, Pitt B, Foegh M, Hanes V. Drospirenone with estradiol lowers blood pressure in postmenopausal women with systolic hypertension. Obstet Gynecol 2004; 4, suppl., 26S.
Gestagen. In a therapeutic dose, drospirenone also has antiandrogenic and weak antimineralocorticoid activity. Drospirenone alternative devoid of any estrogenic, glucocorticoid and antiglucocorticoid activity, which provides a pharmacological profile very close to the profile of the natural hormone progesterone.
In clinical studies, evidence has been obtained indicating that weak antimineralocorticoid properties result in a slight antimineralocorticoid effect.
Due to its small antimineralocorticoid activity, drospirenone increases the activity of renin and aldosterone in blood plasma.
After oral administration, drospirenone is absorbed rapidly and almost completely. C max of the active substance in blood serum is 38 ng / ml and is achieved 1-2 hours after a single dose. Bioavailability is 76-85%. Concomitant food intake does not affect the bioavailability of drospirenone.
Drospirenone binds to serum albumin and does not bind to sex hormone binding globulin (SHBG) or corticoid binding globulin (HSC). Only 3-5% of the total serum concentration of drospirenone exists as free steroids. The increase in SHBG induced by ethinyl estradiol does not affect the binding of drospirenone to serum proteins. The apparent average V d of drospirenone is 3.7 ± 1.2 L / kg.
During one treatment cycle, C ss max of drospirenone in blood plasma is about 70 ng / ml, achieved after 8 days of treatment. Serum drospirenone concentrations increase by approximately 3 times due to the ratio of the final T 1/2 and the dosage interval.
After oral administration, drospirenone undergoes an intensive metabolism. The main metabolites in the blood plasma are the acid form of drospirenone, formed during the opening of the lactone ring, and 4,5-dihydro-drospirenone-3-sulfate, both formed without the participation of the P450 system. Drospirenone is slightly metabolized by CYP3A4 and is able to inhibit this enzyme, as well as in vitro CYP1A1, CYP2C9 and CYP2C19.
T 1/2 of drospirenone with a corresponding decrease in its concentration in blood serum after oral administration is 31 hours. The renal clearance of metabolites of drospirenone in blood serum is 1.5 ± 0.2 ml / min / kg. Drospirenone is excreted only in trace amounts unchanged. Drospirenone metabolites are excreted through the intestines and kidneys in a ratio of about 1.2: 1.4. T 1/2 metabolites by the kidneys and through the intestines is about 40 hours.
C ss of drospirenone in blood plasma in women with mild renal insufficiency (CC 50-80 ml / min) was comparable with the corresponding parameters in women with normal renal for treating. In women with moderate renal failure (CC 30-50 ml / min), the concentration of drospirenone in blood plasma was on average 37% higher than in women with normal renal function. Drospirenone therapy was well tolerated in women with mild to moderate renal failure. Drospirenone did not have a clinically significant effect on serum potassium.
In a single-use study, oral clearance in volunteers with moderate liver failure was reduced by about 50% compared with individuals with normal liver function. The marked decrease in the clearance of drospirenone in volunteers with moderate liver failure does not lead to any significant differences in the content of potassium in the blood serum. Even with diabetes mellitus and the concomitant use of spironolactone (two factors that can provoke hyperkalemia in a patient), there was no increase in serum potassium above VGN. It can be concluded that drospirenone is well tolerated by patients with mild to moderate hepatic insufficiency (class B on the Child-Pugh scale).
Take orally as part of fixed combinations with ethinyl estradiol according to a special scheme.
A single dose of drospirenone when taken as part of fixed combinations with ethinyl estradiol is 3 μg.
Adverse reactions have been reported with the use of drospirenone / ethinyl estradiol in the combination.
Infectious and parasitic diseases: rarely - candidiasis.
From the hemopoietic system: rarely - anemia, thrombocytosis.
From the immune system: rarely - allergic reactions; frequency unknown - hypersensitivity reactions.
From the endocrine system: rarely - endocrine disorders.
From the side of metabolism: rarely - hyperkalemia, hyponatremia.
Mental disorders: often - emotional lability; infrequently - depression, nervousness, decreased libido, drowsiness; rarely - anorgasmia, insomnia.