Modell Pure, 2 mg+0.035 mg 21 pcs

Pharmgroup:

The sexual hormones and modulators of the sexual system.

Pharmic action:

MODELL PURE is a combined low-dose monophasic oral contraceptive with antiandrogenic activity. The mechanism of action is caused by its constituent antiandrogenic component of the steroid structure – cyproterone acetate and oral estrogen – ethinyl estradiol.

Ciproterone acetate has the ability to competitively bind to natural androgen receptors (testosterone, dihydroepiandrosterone, androstenedione, etc.) formed in small quantities in women, mainly in the adrenal glands, ovaries and skin. By blocking androgen receptors in target organs it reduces phenomena of androgenization in women (due to disruption of processes mediated by hormone-receptor complexes at the level of main intracellular mechanisms).

Hereby the treatment of diseases caused by increased formation of androgens or specific sensitivity to these hormones becomes possible.

Modelle Pure reduces sebaceous gland activity, which plays an important role in the development of acne and seborrhea. After 3-4 months of therapy this usually leads to the disappearance of the existing rash. Excessive greasiness of the hair and skin disappears even earlier. Hair loss, which often accompanies seborrhea, is also reduced.

Therapy with Modell Pure in women of reproductive age reduces the clinical manifestations of mild forms of hirsutism; however, the effect of treatment should be expected only after several months of use.

In addition to its antiandrogenic properties, cyproterone acetate has gestagenic activity, which mimics that of corpus luteum hormone. Like other drugs with gestagenic activity, it inhibits pituitary gonadotropic hormone secretion and inhibits ovulation, which accounts for its contraceptive effect.

Ethinylestradiol enhances central and peripheral effects of cyproterone acetate on ovulation, preserves high viscosity of cervical mucus that makes it difficult for sperm to enter the uterine cavity and helps ensure reliable contraceptive effect.

With taking the drug the cycle becomes more regular, painful menstrual periods are less frequent, the intensity of bleeding decreases, and as a result the risk of iron deficiency anemia decreases.

Pharmacokinetics:

Cyproterone acetate.

Cyproterone acetate is completely absorbed from the gastrointestinal (GI) tract after administration. After oral administration of one tablet maximum plasma concentration (Cmax) is reached after 1.6 hours and is 15 ng/ml. Bioavailability is 88%.

Cyproterone acetate is almost completely bound to plasma albumin, approximately 3.5-4% is free. Because binding to proteins is nonspecific, changes in sex steroid-binding globulin (SBSG) levels do not affect the pharmacokinetics of cyproterone acetate.

The pharmacokinetics of cyproterone acetate are biphasic with a half-life (T1/2) of 0.8 hours and 2.3 days for the first and second phases, respectively. Total plasma clearance is 3.6 ml/min/kg. It is biotransformed by hydroxylation and conjugation, the main metabolite being the 15b-hydroxyl derivative. It is excreted mainly as metabolites by the kidneys and through the intestine at a ratio of 1:2, a small portion is excreted unchanged through the intestine. T1/2 for metabolites of cyproterone acetate is 1.8 days.

Ethinylestradiol.

Ethinylestradiol is quickly and completely absorbed from the gastrointestinal tract after administration. During absorption and “first passage” through the liver, ethinylestradiol undergoes intensive metabolism, which accounts for the bioavailability of approximately 45%, and its significant individual variability.

The binding to plasma proteins (albumin) is high (2% are free in plasma). Ethinylestradiol increases hepatic synthesis of hGPS and corticosteroid-binding globulin (CRBG) during continuous administration. Against the background of treatment, the serum HSPC concentration increases from approximately 100 nmol/L to 300 nmol/L, the serum concentration of CRC increases from approximately 50 µg/ml to 95 µg/ml.

The pharmacokinetics of ethinylestradiol are biphasic, with a T1/2 of 1-2 h and approximately 20 h, respectively. Plasma clearance is about 5 ml/min/kg. Ethinylestradiol is excreted from the body as metabolites; about 40% is excreted by the kidneys, 60% – through the intestine.

Indications

– treatment of women with severe androgenism (acne, especially common forms and forms accompanied by seborrhea, inflammation or formation of nodules (papule-pustular acne, nodular-cystic acne), androgenetic alopecia and mild forms of hirsutism) when other treatments of these symptoms are not effective.

Active ingredient

Composition

1 tablet:

– ciproterone acetate micronized 2 mg

– ethinyl estradiol micronized 0.035 mg

auxiliary substances:

Lactose monohydrate,

Corn starch,

povidone K25,

talc,

magnesium stearate,

coating composition:

saccharose, calcium carbonate, talc, E171 titanium dioxide, povidone K 90, polyethylene glycol 6000, glycerol 85%, iron oxide pigment, mountain glycol wax

How to take, the dosage

The drug is only prescribed for the treatment of adrogenia, but because it has contraceptive properties, no other hormonal contraceptive drugs should be taken during treatment.

Modelle Pure is taken orally, 1 tablet a day. The tablet is taken without chewing and with a small amount of liquid. The timing of the medication is not important, but subsequent dosing should be done at the same chosen hour, preferably after breakfast or dinner.

The administration of Modell Pure begins on the 1st day of the cycle, using the tablet of the corresponding day of the week from the calendar pack.
The daily administration of the drug is carried out using tablets from the calendar pack in the direction of the arrow printed on the foil, until all the tablets are taken. After the end of taking all 21 tablets of yellow-orange color from the calendar pack, the remaining white tablets should be taken during the next 7 days. Menstruation should occur during the last 7 days of your cycle (28 days). Menstruation usually begins 2-3 days after the 21st day of the cycle of treatment with Modell Pure. The next pack should be started the day after taking the pills from the previous pack is completely finished, whether bleeding continues or not.

When switching from combined oral contraceptives, Modell Pure should be started the day after taking the last tablet with the active ingredients of the previous drug, but in no case later than the day after the usual 7-day break in intake (for products containing 21 pills). Then according to the scheme described above. If the patient has taken the previous contraceptive daily for 28 days, Modell Pure should be started after taking the last inactive pill.

When switching from contraceptives containing only gestagens (“mini-pills”), Modell Pure can be started without a break. When using injectable forms of contraceptives, Modell Pure can be started on the day the next injection is due. If you change from an implant, on the day it is removed. In all cases, it is necessary to use an additional barrier method of contraception during the first seven days of taking the drug.

After an abortion in the first trimester of pregnancy a woman can start taking the drug immediately. In this case the woman does not need any additional contraceptive methods.

After childbirth or a second trimester abortion, the drug should be started on days 21-28. If intake is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the drug. If a woman was sexually active between childbirth or abortion and the start of Modell Pure, pregnancy should be ruled out first or the first menstruation should be waited.

A woman should take a missed pill as soon as possible, the next pill is taken at the usual time. A delay of less than 12 hours does not reduce the reliability of contraception. If the delay in taking the pill is more than 12 hours, the reliability of contraception may be reduced.

If pills are taken more than 12 hours late (the interval from taking the last pill is more than 36 hours) during the first and second weeks of the drug, the woman should take the last missed pill as soon as she can remember (even if this means taking two pills at once). The next pill is taken at the usual time. Additionally, a barrier method of contraception should be used for the next 7 days.

If the delay in taking the pill was more than 12 hours (the interval from taking the last pill is more than 36 hours) during the third week of taking the drug, the woman should take the last missed pill as soon as she remembers (even if this means taking two pills at the same time) as soon as possible. The next pill is taken at the usual time. In addition, taking a pill from a new pack should be started as soon as the current pack is finished, i.e., without interruption.

It is likely that the woman will not have a bleeding withdrawal until the end of the second pack, but she may have a masticated bloody discharge or breakthrough uterine bleeding on the days she takes the pills. If the woman had vomiting within 3 to 4 h of taking the drug, absorption of the active ingredients may be incomplete.

In this case, it is necessary to focus on the recommendations for skipping the pill. In order to delay the onset of menstruation, the woman should continue taking the pills from the new package of the drug immediately after taking all pills from the previous package, without interruption. The pills from this new package may be taken as long as the woman wishes (until the package ends). While taking the pills from the second package, the woman may experience menses or breakthrough uterine bleeding. The pills in the next package should be started after all 28 pills have been taken.

In order to postpone the day her period starts to another day of the week, a woman should shorten the nearest interval between pills by as many days as she wants. The shorter the interval, the higher the risk that she won’t have a bleeding withdrawal and, subsequently, will have spotting and breakthrough bleeding while taking her second pack (just like when she would like to delay the start of her period).

In the treatment of hyperandrogenic conditions, the duration of intake is determined by the severity of the disease. After the disappearance of symptoms it is recommended to take the drug for at least another 3-4 months. If there is a relapse in a few weeks or months after completion of the course, Modell Pure may be retreated.

Interaction

Substances affecting the effectiveness of Modell Pure (liver enzyme inducers and antibiotics).

The drugs that reduce the contraceptive effectiveness of the drug include drugs inducing liver enzymes and antibiotics. During their use and for 7 days after their withdrawal, an additional barrier method of contraception should be used.

Hepatic enzyme induction (increased hepatic metabolism): The use of drugs that induce hepatic microsomal enzymes may lead to increased clearance of sex hormones. These medications include phenytoin, barbiturates, primidone, carbamazepine, and rifampicin; there is also speculation about oxcarbazepine, topiramate, felbamate, ritonavir, and griseofulvin and medications containing St John’s wort.

In addition, HIV proteases (e.g., ritonavir) and non-nucleoside reverse transcriptase inhibitors (e.g., nevirapine), and combinations thereof can potentially increase hepatic metabolism.

The effect on intestinal-hepatic circulation.

According to some clinical studies, certain antibiotics (e.g., penicillins and tetracyclines), may decrease intrahepatic circulation of estrogen, thereby lowering the concentration of ethinylestradiol.

The effect of estrogen/progestagen combinations on other drugs.

The estrogen/progestagen combinations, like Modell Pure, can affect the metabolism of some other drugs, resulting in an increase (e.g., cyclosporine) or decrease (e.g., lamotrigine) in their plasma and tissue concentrations.

Laboratory tests.

The administration of drugs like Modell Pure may affect the results of some laboratory tests, including indicators of liver, kidney, thyroid, adrenal function, plasma levels of transport proteins, carbohydrate metabolism parameters, coagulation and fibrinolysis parameters. The changes usually do not go beyond normal values.

Special Instructions

The drug should not be used for contraceptive purposes. The drug is prescribed only for the treatment of adrogenia, but since it has contraceptive properties, no other hormonal contraceptive drugs should be taken during treatment.
If there are risk factors, the potential risk and expected benefits of therapy should be carefully evaluated and discussed with the woman before she decides to start taking the drug. If any of the following conditions or risk factors increase or first appear, the decision should be made to discontinue the drug.

Cardiovascular disease.

There is an association between use of combined oral contraceptives and an increased risk of venous and arterial thrombosis and thromboembolic events, such as myocardial infarction, deep vein thrombosis, pulmonary embolism, and cerebrovascular events. These diseases are rare.

The risk of venous thromboembolism (VTE) is highest in the first year of oral contraceptive use. The risk of thrombosis and thromboembolism in pregnancy is higher than with low-dose combined oral contraceptives (less than 0.05 mg ethinylestradiol).

Venous thromboembolism can be fatal (1-2% of cases). Venous thromboembolism, manifested as deep vein thrombosis and/or pulmonary embolism, can occur with any combined oral contraceptive.

In women taking combined oral contraceptives, extremely rare cases of thrombosis of other blood vessels, such as hepatic, mesenteric, renal, cerebral arteries and veins, as well as retinal vessels, have been described. There is no consensus on the association between these events and taking combined oral contraceptives.
Symptoms of deep vein thrombosis include: unilateral swelling in the leg or along a vein in the leg, pain or discomfort in the leg only when upright or walking, localized temperature rise in the affected extremity, redness or discoloration of the skin on the leg.

The symptoms of pulmonary artery thromboembolism are: sudden onset of unexplained shortness of breath or rapid breathing, sudden attack of cough that may be accompanied by hemoptysis, sharp pain in the chest that may increase with deep breathing, anxiety, severe dizziness; rapid or irregular heartbeat. Some of these symptoms (e.g., “shortness of breath” and “cough”) are nonspecific and, as such, may be misinterpreted as signs of more frequent and less severe disorders (e.g., respiratory infections).

Arterial thromboembolism may include cerebrovascular disorders, vascular occlusion, or myocardial infarction.
Symptoms of cerebrovascular disorders may include sudden weakness or numbness of the face, upper and lower extremities, especially on one side of the body, sudden confusion, impaired speech or difficulty seeing; sudden visual impairment in one or both eyes, sudden gait disturbance, dizziness, loss of balance or coordination of movements, sudden severe or prolonged headache for no apparent reason, loss of consciousness or fainting with or without a seizure. Other signs of vascular occlusion may also include sudden pain, swelling or mild lividity of the extremities, and “acute abdominal” symptoms.

The symptoms of myocardial infarction include: pain, discomfort, pressure, heaviness, feeling of tightness or distention in the chest, in the arm or behind the sternum, feeling of discomfort with irradiation to the back, cheekbones, throat, arm, stomach, feeling of fullness or distention in the stomach, feeling of choking, cold sweats, nausea, vomiting or dizziness, severe weakness, feeling of anxiety, shortness of breath, rapid or irregular heartbeat.

Arterial thromboembolism can be fatal.

The risk of thrombosis (venous and/or arterial), thromboembolic or cerebrovascular disorders increases:
– with age
– in smokers (with more cigarettes or increased age, the risk further increases, especially in women over 35);
– with a family history (ie.i.e. venous or arterial thromboembolism ever in close relatives or parents at a relatively young age). If a hereditary predisposition is known or suspected, a woman should consult a physician to decide on the possibility of taking combined oral contraceptives
– in obesity (body mass index more than 30 kg/m2)
– in dyslipoproteinemia
– in arterial hypertension
– in migraine
– in heart valve disease
– in atrial fibrillation
– prolonged immobilization, serious surgery, any leg surgery or extensive trauma. In these situations, it is advisable to stop using combined oral contraceptives (in the case of planned surgery, at least four weeks before) and not resume for two weeks after the end of immobilization.

The possible role of varicose veins and superficial thrombophlebitis in the development of venous thromboembolisms remains controversial. An increased risk of thromboembolism in the postpartum period should be considered.

Circulatory disorders may also be seen in diabetes mellitus, polycystic ovarian syndrome, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn’s disease or nonspecific ulcerative colitis) and sickle cell anemia.

An increase in the frequency and severity of migraine during the use of combined oral contraceptives (which may precede cerebrovascular disorders) may be grounds for immediate discontinuation of these drugs.
Biochemical parameters that may be indicators of hereditary or acquired predisposition to venous or arterial thrombosis include activated protein C resistance, hyperhomocysteinemia, antithrombin-III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).

Tumors.

There is a slightly increased relative risk of breast cancer diagnosed in women who were using combined oral contraceptives at the time of the study, which is associated with earlier breast cancer diagnosis in these women, the biological effects of combined oral contraceptives, or a combination of both factors.

In rare cases, development of benign liver tumors and in even rarer cases development of malignant liver tumors have been observed against the background of combined oral contraceptives. In some cases, liver tumors can lead to life-threatening intra-abdominal bleeding. If severe upper abdominal pain, liver enlargement, or signs of intra-abdominal bleeding occur, consider a liver tumor in the differential diagnosis.

Other conditions.

In women with hypertriglyceridemia (or a family history of this condition), there may be an increased risk of pancreatitis while taking combined oral contraceptives.

While small increases in blood pressure have been described in many women taking combined oral contraceptives, clinically significant increases have rarely been reported. However, if a persistent, clinically significant increase in blood pressure develops while taking combined oral contraceptives, the medications should be discontinued and treatment for hypertension should be initiated. The combined oral contraceptives may be continued if normal blood pressure values are achieved with hypotensive therapy.

The following conditions observed in pregnancy may also appear or worsen while taking combined oral contraceptives: jaundice and/or pruritus associated with cholestasis; gallstone formation; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Sydingham chorea; herpes of pregnancy; hearing loss associated with otosclerosis. However, the relationship between the development of these conditions and the use of combined oral contraceptives has not been proven.

In women with hereditary angioedema, exogenous estrogens may provoke or exacerbate symptoms of the disease.

In women with acute or chronic liver function abnormalities, discontinuation of combined oral contraceptives should be considered until liver function returns to normal. If recurrent cholestatic jaundice develops for the first time during pregnancy or previous use of sex hormones, the combined oral contraceptives should be discontinued.

While combined oral contraceptives may affect insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetic patients using low-dose combined oral contraceptives (< 0.05 mg ethinylestradiol). However, women with diabetes mellitus should be carefully monitored while taking combined oral contraceptives.

In the background of using combined oral contraceptives, manifestations of Crohn’s disease and nonspecific ulcerative colitis have been observed.

Women with a tendency to chloasma should avoid prolonged sun exposure and exposure to ultraviolet radiation while taking combined oral contraceptives.

If women with hirsutism develop symptoms recently or significantly worsen, other causes such as androgen-producing tumor or congenital adrenal cortex dysfunction should be considered in making a differential diagnosis.

Medical exams.

Women should undergo a thorough general and gynecological examination (including measurement of blood pressure, breast, abdominal and pelvic examination, including cytological examination of cervical mucus) before starting Modell Pure and periodically during the use of the drug; pregnancy should be excluded. In addition, clotting disorders should be excluded. Periodic medical monitoring is important because contraindications, such as transient ischemic attacks and others, or risk factors such as hereditary predisposition to venous or arterial thrombosis may become apparent during use of Modell Pure.

A woman should be warned that preparations like Modell Pure do not protect against HIV infection (AIDS) or other sexually transmitted diseases!

Decreased efficacy.

The effectiveness of combined oral contraceptive medications may be reduced if pills are missed, if vomiting and diarrhea occur, or as a result of drug interactions.

The effect on the menstrual cycle.

In combination oral contraceptives, irregular bleeding (spotting or breakthrough bleeding) may occur, especially during the first months of use. Therefore, any irregular bleeding should be evaluated only after an adjustment period of about three cycles.

If irregular bleeding recurs or develops after previous regular cycles, a thorough evaluation should be performed, including a diagnostic curettage to rule out malignancy or pregnancy.

Some women may not develop withdrawal bleeding during a break in the drags. If the combined oral contraceptives have been taken as directed, it is unlikely that the woman is pregnant. However, if the combined oral contraceptives have been taken irregularly before, or if there are no two consecutive bleeding withdrawals, pregnancy must be ruled out before continuing the drug.

Dermal allergy tests and decreases in luteinizing hormone (LH) and follicle stimulating hormone (FSH) concentrations may change during treatment.

The treatment should be stopped immediately 3 months before the planned pregnancy and approximately 6 weeks before the planned surgical intervention, or prolonged immobilization.

Particular effects of the drug on the ability to drive or use potentially dangerous machinery.

No effect

Contraindications

Medications containing the estrogen/gestagen combination should not be used in the presence of any of the conditions listed below.
– Hypersensitivity to any of the components of the drug MODELL PURE
– Thrombosis/thromboembolism (venous and arterial) currently or in the history (e.g., deep vein thrombosis, pulmonary thromboembolism, myocardial infarction, cerebrovascular disorders)
– Conditions preceding thrombosis (e.g., transient ischemic attacks, angina pectoris), current or past history
– Presence of expressed or multiple risk factors for venous or arterial thrombosis
– Migraine with focal neurological symptoms in past history
– Diabetes mellitus with vascular complications
– severe liver disease until liver function indicators return to normal
– liver tumors (benign or malignant) at present or in the past
– suspected or known hormone-dependent malignancies (e.g., genital or mammary)
– vaginal bleeding of unclear genesis
– pregnancy or suspectedbr> – pregnancy or suspected pregnancy
– lactation
– arterial hypertension
– uterine bleeding of unclear etiology
– pancreatitis (including those of unknown etiology).ч. history) if accompanied by severe hypertriglyceridemia
– congenital hyperbilirubinemia (Gilbert, Dabin-Johnson and Rotor syndromes)
– sickle cell anemia
– idiopathic jaundice or itching in a previous pregnancy
– otosclerosis with worsening during pregnancy – hyperprolactinemia
With caution – epilepsy, depression, ulcerative colitis, liver and gallbladder disease, uterine myoma, mastopathy, chorea, tetany, porphyria, multiple sclerosis, varicose veins, tuberculosis, kidney disease, adolescence (without regular ovulatory cycles).

Side effects

Often:
– headache, depressed mood, mood changes
– nausea, abdominal pain
– weight gain
– soreness and tightness of the breasts
Infrequent:
– migraine
– vomiting, diarrhea
– fluid retention in the body
– breast enlargement
– rash, urticaria
– decreased libido
Rarely:
– hypersensitivity reactions
– poor tolerance of contact lenses
– weight loss
– increased libido
– vaginal discharge, mammary gland discharge
– rash, erythema nodosum, erythema multiforme, pigmented spots on the face (chloasma)
The following serious side effects have been reported in women using combined oral contraceptives:
– venous thromboembolic disorders
– arterial thromboembolic disorders
– cerebrovascular disorders
– arterial hypertension
– hypertriglyceridemia
– glucose tolerance disorders or effects of peripheral insulin resistance
– liver tumors (benign and malignant) – liver function abnormalities
– chloasma
– in women with hereditary angioedema provoking or worsening of disease symptoms under the influence of exogenous estrogens
– appearance or worsening of the following conditions, the connection of which with taking combined oral contraceptives is not proved jaundice and/or pruritus associated with cholestasis; gallstone formation; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Sydingham’s chorea; herpes of pregnancy; hearing loss associated with otosclerosis, Crohn’s disease and nonspecific ulcerative colitis, cervical cancer.

Overdose

Symptoms: nausea, vomiting, slight vaginal bleeding.

Treatment: symptomatic. There is no specific antidote.

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