If you drink jess. Jess drug, instructions for use, contraindications and side effects. Use in the elderly

Jess is a monophasic oral contraceptive drug with antiandrogenic properties.

Release form and composition

Jess dosage form - film-coated tablets: biconvex, round, the core is at a break from almost white to white: active - light pink, on one side there is an engraving in the correct hexagon in the form of the letters "DS"; placebo - white, on one side engraved in the correct hexagon in the form of the letters "DP" (28 pcs., including 24 active and 4 placebos, in blisters, in a folding book 1 or 3 blisters; 30 pcs. (active tablets) in blister packs, 1 blister pack in flex-cartridges, in a carton box 1 or 3 flex-cartridges, possibly complete with a Clyk dispenser).

Active ingredients in 1 active tablet:

• ethinylestradiol (in the form of betadex clathrate) - 0.02 mg;
• drospirenone - 3 mg.

Auxiliary components in 1 tablet (active / placebo):

• core: lactose monohydrate - 48.18 / 23.205 mg, microcrystalline cellulose - 0 / 54.21 mg, corn starch - 28 / 0 mg, magnesium stearate - 0.8 / 0.585 mg;
• shell: talc - 0.3036 / 0.2024 mg, hypromellose - 1.5168 / 1.0112 mg, titanium dioxide - 1.1748 / 0.7864 mg, red dye iron oxide - 0.0048 / 0 mg.

Pharmacological properties

Pharmacodynamics

Jess is one of the combined hormonal contraceptives that have antimineralocorticoid and antiandrogenic effects.

The contraceptive effect is based on the interaction of various factors, the most important of which are changes in the properties of cervical secretion and suppression of ovulation.

The Pearl Index, when used correctly, is less than 1 (may increase if the recommended regimen is not followed).

During therapy, the menstrual cycle becomes more regular, painful periods develop less frequently, the intensity of bleeding decreases, which reduces the likelihood of anemia. In addition, according to the results of epidemiological studies, the use of combined oral contraceptives helps to reduce the likelihood of developing ovarian and endometrial cancer.

One of the active components of Jess - drospirenone - has an antimineralocorticoid effect. Prevents weight gain and edema associated with estrogen-induced fluid retention, resulting in a well tolerated drug. Drospirenone has a positive effect on premenstrual syndrome (PMS).

Also, drospirenone has antiandrogenic activity and helps to reduce acne, oily hair and skin. This effect is similar to the action of natural progesterone, which is produced by the body.

Drospirenone does not have estrogenic, androgenic, antiglucocorticoid and glucocorticoid activity. All this, combined with antiandrogenic and antimineralocorticoid action, provides drospirenone with a pharmacological and biochemical profile similar to natural progesterone.

Drospirenone, when used with ethinyl estradiol, has a beneficial effect on the lipid profile, characterized by an increase in HDL.

Jess can be taken in the usual ("24 + 4") or "flexible" (extended) mode, which consists in the continuous intake of active tablets for 120 days. Thus, a continuous period of taking can be from 24 to 120 days, and the break in taking the tablets should not be longer than 4 days. This mode of therapy is possible only with the Clyk dispenser and flex cartridges. It allows you to achieve the maximum duration of periods without bleeding (up to 120 days) and reduce the total number of days of menstruation per year to 41 days.

Pharmacokinetics

Drospirenone

Absorption: the substance is rapidly and almost completely absorbed; bioavailability - 76-85% (food intake has no effect); C max (maximum concentration of the substance) in serum is reached after approximately 1-2 hours and is about 38 ng / ml.

Distribution: after oral administration, a two-phase decrease in serum drospirenone levels is observed with a T 1/2 (half-life) of 1.6 ± 0.7 h and 27 ± 7.5 hours, respectively. Does not bind to globulin, binding occurs with serum albumin. C ss max (equilibrium concentration during cyclic administration) of the substance in serum is reached between the 7th and 14th day of therapy and is approximately 70 ng / ml.

Metabolism: The substance is extensively metabolized. Metabolites in plasma are mainly represented by acidic forms of drospirenone. Also, drospirenone is a substrate for oxidative metabolism, which is catalyzed by the cytochrome P 450 isoenzyme CYP3A4.

Excretion: The rate of metabolic clearance of the substance in serum is 1.5 ± 0.2 ml / min / kg. T 1/2 - approximately 40 hours. Excreted unchanged only in trace amounts. Excretion of metabolites occurs by the kidneys and through the intestines in a ratio of approximately 1.4: 1.2.

Ethinylestradiol

Absorption: completely and quickly absorbed; after a single oral administration, Cmax is reached after 1-2 hours and is approximately 88-100 pg / ml. Absolute bioavailability during the "first pass" through the liver is about 60%. The bioavailability of ethinylestradiol may be reduced by concomitant food intake.

Distribution: serum concentration of ethinylestradiol decreases biphasically, T 1/2 of the terminal phase is 24 hours. The apparent V d is about 5 l/kg. The substance is strongly, but not specifically, bound to serum albumin (approximately 98.5%) and causes an increase in serum SHBG concentrations.

Metabolism: The substance undergoes significant primary metabolism in the liver and intestines. The rate of metabolic clearance is approximately 5 ml / min / kg.

Withdrawal: in unchanged form is practically not displayed. Metabolites of ethinylestradiol are excreted through the intestines and by the kidneys in a ratio of 6: 4. T 1/2 metabolites - 24 hours.

Indications for use

Jess is prescribed for contraception, including for the concomitant treatment of moderate acne (acne vulgaris) and severe premenstrual syndrome.

Contraindications

Absolute:

• the presence of an increased risk of arterial / venous thrombosis;
• thrombosis (arterial and venous) and thromboembolism (including pulmonary embolism, deep vein thrombosis, myocardial infarction), including a burdened history of these diseases, cerebrovascular disorders;
• the presence of a predisposition (hereditary or acquired) to arterial / venous thrombosis (including resistance to activated protein C, deficiency of antithrombin III, protein C and S), hyperhomocysteinemia, antibodies to phospholipids;
• adrenal insufficiency;
• malignant / benign tumors of the liver, including a aggravated anamnesis;
• hormone-dependent malignant diseases, including those of the mammary glands or genital organs, including those diagnosed or suspected;
• severe / acute renal failure;
• bleeding from the vagina, having an unclear etiology;
• angina pectoris, transient ischemic attacks and other conditions preceding thrombosis, including a aggravated anamnesis;
• migraine accompanied by focal neurological symptoms, including a aggravated anamnesis;
• diabetes mellitus with vascular complications;
• glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
• pregnancy (confirmed or suspected) and the period of breastfeeding;
• individual intolerance to the components of the drug.

Relative (diseases / conditions in the presence of which the appointment of Jess requires an assessment of the benefit-risk ratio):

• presence of risk factors for thrombosis and thromboembolism, including smoking, thrombosis, family history at a young age of myocardial infarction or cerebrovascular accident, migraine, major trauma, major surgery, valvular heart disease, cardiac arrhythmias, prolonged immobilization, dyslipoproteinemia, obesity , arterial hypertension;
• hereditary angioedema;
• other diseases in which peripheral circulatory disorders may occur, including diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, superficial vein phlebitis, sickle cell anemia, ulcerative colitis and Crohn's disease;
• liver disease;
• hypertriglyceridemia;
• postpartum period;
• diseases that first arose or worsened during pregnancy or against the background of previous use of sex hormones, for example, cholestasis, jaundice, porphyria, cholelithiasis, otosclerosis with hearing loss, herpes pregnant, Sydenham's chorea.

Instructions for use Jess: method and dosage

Reception mode "24 + 4"

Jess tablets must be taken daily (without interruption), at about the same time, 1 pc. a day with a small amount of water. After 28 days (after the end of the tablets from the previous package), the reception is continued from the new package. As a rule, withdrawal bleeding begins 2-3 days after the start of the placebo tablets (inactive, white) and may continue until the start of the next pack.

"Flexible" reception mode

Tablets must be taken daily, at about the same time, 1 pc. a day with a small amount of water. This mode can only be used with flex cartridges and a Clyk dispenser. Jess is taken continuously for at least 24 days. At the discretion of the patient, a break of 4 days (maximum) can be made between 25 and 120 days of therapy. The interval in therapy should be done no later than 120 days of continuous tablet intake. Taking pills after each break should have a minimum duration of 24 days, a maximum of 120 days. Withdrawal bleeding usually develops during a break in taking the drug. If spotting/bleeding from the vagina occurs for 3 consecutive days from day 25 to day 120, it is recommended to take a break of 4 days, which will reduce the total number of days of bleeding.

Starting the drug

• not taking any hormonal contraceptives in the previous month: therapy is started on the 1st day of the menstrual cycle (i.e., on the 1st day of menstrual bleeding), additional contraceptive measures are not required. If the reception is started on the 2-5th day, it is recommended to use barrier methods of contraception for the first 7 days;
• switching from other combined oral contraceptives, vaginal ring or contraceptive patch: it is preferable to start therapy the next day after taking the last active tablet, but no later than the next day after the usual seven-day break (21 tablets in a package) or taking the last inactive tablet (28 tablets in a package) ); vaginal ring or patch - therapy begins on the day of removal, but no later than the day when a new patch should be pasted or a new ring inserted;
• switching from contraceptives containing only gestagens, or from a progestogen-releasing intrauterine contraceptive (the first 7 days it is recommended to use barrier methods of contraception): switching from "mini-pili" - you can start therapy on any day (without interruption); transition from an implant or intrauterine contraceptive with a progestogen - therapy begins on the day of their removal; switching from an injectable contraceptive - therapy is started on the day when the next injection should be made;
• use after an abortion (spontaneous / medical) and childbirth: abortion in the first trimester of pregnancy - you can start taking Jess immediately after an abortion without additional protection measures; abortion in the II trimester and childbirth (in cases of lack of breastfeeding) - therapy can be started after 21-28 days (if therapy starts later, additional barrier methods of contraception are required for 7 days). In cases where sexual intercourse has already taken place, you need to wait for the first menstruation or first exclude pregnancy.

Termination of therapy

You can refuse to take Jess at any time. In cases of pregnancy planning, it is recommended to wait for natural menstrual bleeding after the end of therapy.

Taking missed pills

If a placebo tablet was missed during the 24 + 4 regimen, it is recommended that they be discarded so that the period of taking them is not accidentally extended. Additional measures are not required.

If the delay is less than 24 hours, the Jess effect is not reduced. The missed single dose should be taken as soon as possible without changing the dosing regimen in the future.

With a longer skip, contraceptive protection may decrease. The more pills missed and the closer the break is to the inactive pill phase (24+4 mode) or pill-free period (flex mode), the higher the chance of pregnancy. In such cases, the following recommendations should be followed:

• the break in taking Jess should not be more than 7 days (for the "flexible" regimen and the "24 + 4" regimen, the recommended interval for taking active tablets is 4 days);
• adequate suppression of the hypothalamic-pituitary-ovarian system is achieved after 7 days of continuous therapy.

Using the Clyk dispenser, you can control the intake of tablets. The dispenser also warns the woman in cases of the need to use an additional method of contraception (the exclamation mark symbol on the display when a pill is missed or if pills are taken irregularly for more than 7 days in a row). In cases where more than one tablet is missed, it is recommended to consult a doctor.

If information from the Clyk dispenser is not available or if there is doubt about its reliability, the following recommendations should be followed.

Days 1-7 on any regimen: Take the missed pill as soon as possible, even if it means taking 2 pills at once. For the next 7 days, the woman should use additional protective measures. If sexual contact has taken place within 7 days before the date of the pass, the likelihood of pregnancy should be taken into account.

Days 8-14 with 24+4 and Days 8-24 with Flex: Take the missed pill as soon as possible, even if it means taking 2 pills at once. Further adjustment of the dosing regimen should not be made. If in the previous period the Jess regimen was not violated, additional protective methods should not be used. Otherwise, and if ≥ 2 tablets are missed within 7 days, the recommendations for additional protective measures should be followed.

Days 15–24 with the “24 + 4” regimen and 25–120 days with the “flexible” regimen: during this period there is a possibility of a decrease in the effectiveness of the drug. One of the following two rules must be strictly observed. Moreover, if during the 7 days preceding the first missed tablet, the regimen of the drug was not violated, there is no need to use additional protective measures. Otherwise, you should use the first of the following schemes and use a barrier method of contraception for an additional 7 days.

1. You need to take the missed dose as soon as possible, even if you have to take 2 tablets at once. 24 + 4 mode - subsequent tablets are taken at the usual time until the active tablets in the package run out, after which you need to start taking the active tablets from the new package, skipping the placebo. Until the new pack is finished, withdrawal bleeding is unlikely, but spotting/breakthrough bleeding may occur. "Flexible" regimen - tablets should be taken daily for at least 7 days.
2. Mode "24 + 4" - taking active tablets can be interrupted, and after 4 days of a break, start taking from a new package according to the usual scheme. In cases where withdrawal bleeding does not occur while taking the placebo, the absence of pregnancy must be confirmed. "Flexible" mode - it is permissible to take a four-day break (including the day of the pass), and then start a new cycle. If withdrawal bleeding does not occur during the next interval period, pregnancy can be assumed.

Against the background of severe gastrointestinal disorders, the absorption of Jess may be incomplete, and therefore additional protective measures must be taken.

If there was diarrhea or vomiting within 3-4 hours after taking the active tablet, it is necessary to follow the recommendations for skipping tablets, or take an additional single dose.

To delay the onset of withdrawal bleeding, inactive tablets should be skipped. Thus, this period can be extended for any period until the end of the tablets from the package. You can stop taking active tablets at any time you wish, taking a break of 4 days.

Side effects

Possible adverse reactions with two regimens (> 10% - very often; > 1% and< 10% – часто; >0.1% and< 1% – нечасто; >0.01% and< 0,1% – редко; < 0,01% – очень редко; с неустановленной частотой – в случаях, когда по имеющейся информации определить частоту появления нарушения не представляется возможным):

It is also possible to develop disorders characterized by a very rare development, or with delayed symptoms (presumably there is a connection with taking Jess):

• pancreatitis on the background of hypertriglyceridemia;
• liver tumors (benign and malignant);
• tumors;
• erythema nodosum, erythema multiforme (only when using a "flexible" regimen);
• chloasma;
• the appearance / aggravation of symptoms of hereditary angioedema;
• increased blood pressure;
• conditions appearing/worsening during therapy (no relationship proven), including jaundice and/or pruritus associated with cholestasis, porphyria, cholelithiasis, systemic lupus erythematosus, Sydenham's chorea, hemolytic uremic syndrome, herpes during pregnancy, otosclerosis-associated reduction hearing;
• effects on insulin resistance/changes in glucose tolerance;
• impaired hepatic function;
• Crohn's disease, ulcerative colitis;
• hypersensitivity reactions (including rash, urticaria).

It must be taken into account that when used in combination with other drugs (enzyme inducers), breakthrough bleeding / reduced contraceptive effectiveness may develop.

Overdose

Main symptoms: vomiting, nausea, metrorrhagia, spotting; there are no data on cases of serious overdose.

Therapy: symptomatic; there is no specific antidote.

special instructions

When prescribing / conducting therapy, it is necessary to take into account the presence of conditions / risk factors (in cases of appearance / aggravation of symptoms, Jess is canceled):

• diseases of the cardiovascular system: with a combination of several risk factors or a high severity of one of them, the likelihood of mutual reinforcement should be taken into account; the risk of thrombosis and thromboembolism increases with smoking, obesity, aggravated family history, prolonged immobilization, extensive injuries and major surgical interventions, against the background of migraine (in cases of increased severity / frequency of migraine, the drug is canceled), atrial fibrillation, dyslipoproteinemia, diseases of the heart valves, arterial hypertension, as well as with age;
• tumors: among the most significant risk factors for cervical cancer is persistent human papillomavirus infection; the development of benign tumors during the period of therapy is observed only in rare cases, in extremely rare cases, the occurrence of malignant liver tumors is noted; when conducting a differential diagnosis for severe pain in the abdomen, signs of intra-abdominal bleeding or liver enlargement, these factors should be taken into account;
• hyperkalemia against the background of an increased risk of its development: the first cycle of therapy should be carried out under the control of serum potassium concentration;
• pancreatitis against the background of hypertriglyceridemia or a burdened family history of this disease;
• clinically significant, persistent increase in blood pressure: Jess should be canceled, therapy can be continued after reaching normal blood pressure values ​​with antihypertensive therapy;
• angioedema: onset/worsening of symptoms.

Before prescribing Jess tablets, a medical examination and a personal / family history should be carried out. It is also necessary to exclude pregnancy. The volume of additional studies and the frequency of follow-up examinations are determined individually. Control examinations, as a rule, are carried out at least once every 6 months.

From HIV infection (AIDS) and other sexually transmitted diseases, Jess does not protect.

A decrease in the effectiveness of the drug can be observed when you skip taking active tablets, in cases of vomiting and diarrhea, and also due to drug interactions.

Evaluation of any irregular bleeding should only be done after an adaptation period of approximately 3 cycles (or 3 months for flexible dosing). In cases where irregular bleeding recurs or develops after previous regular cycles, a thorough diagnostic examination should be carried out in order to exclude pregnancy or malignant neoplasms.

It must be taken into account that Jess can promote the growth of certain tumors and hormone-dependent tissues.

Use during pregnancy and lactation

According to the instructions, Jess is contraindicated for use during pregnancy and lactation.

When planning pregnancy, the drug can be interrupted at any time.

When pregnancy is diagnosed, therapy is immediately canceled; there is no information on the effect of therapy on the health of the mother and fetus.

Taking Jess during lactation can lead to a decrease in the amount of breast milk and a change in its composition.

Application in childhood

Jess can be appointed only after the onset of menarche. There is no need for dose adjustment.

For impaired renal function

Acute / severe renal failure is a contraindication to taking Jess.

For impaired liver function

The use of the drug is contraindicated in the following cases:

• liver failure and severe liver disease (before normalization of indicators);
• malignant / benign liver tumors, including a aggravated anamnesis.

Use in the elderly

Women after the onset of menopause, Jess is not prescribed.

drug interaction

Possible interactions:

• drugs that induce microsomal enzymes: an increase in the clearance of sex hormones, as a result of which there may be a decrease in the contraceptive effect / the appearance of breakthrough uterine bleeding (it is recommended to choose a different non-hormonal method of contraception or use a barrier method of contraception, including a period of 28 days after the withdrawal of such drugs);
• barbiturates, phenytoin, carbamazepine, primidone, rifampicin and, probably, felbamate, oxcarbazepine, griseofulvin, topiramate, as well as preparations containing St. John's wort: an increase in the clearance of Jess and a decrease in its effects;

Terms and conditions of storage

Store at temperatures up to 30 °C. Keep away from children.

Best before date:

• flex-cartridge of 30 tablets - 3 years;
• blister of 28 tablets - 5 years.