Chloe

Chloe is a medicine for antiandrogen.

Indications of the chloe

It is used to eliminate androgen pathologies in women:

• acne, especially pronounced nature, and also accompanied by the development of inflammatory processes or seborrhea, as well as the formation of nodules (papulyzno-pustular acne or nodular-cystic acne);
• androgenic alopecia;
• hirsutism to an easy degree.

It can also be used as a contraceptive (but the drug is not used solely as a contraceptive, it is prescribed only for therapy with androgen states in women).

Release form

Release in tablets, according to 21 or 7 pieces (placebo tablets) on the blister. Inside the package - 1 or 3 blister plates.

[1]

Pharmacodynamics

The acetate of cyproterone is an active component of the drug. It slows down the action of androgens produced by the female body. The medicine allows you to treat pathologies, provoked by the binding of androgens or disease due to hypersensitivity to these hormones.

During the period of Chloe's use, the intense activity of the sebaceous glands slows down, which are important factors in the development of seborrhea and acne. Thanks to the medicine, existing rashes disappear within 3-4 months of the course. Increased fat content of hair with skin decreases more quickly. Usually it decreases or hair loss occurs, which is often observed in seborrhea.

Therapy is prescribed for women who are in reproductive age, who have a moderate degree of hirsutism (in particular, this applies to slightly strengthened facial hair). However, the result becomes noticeable after a minimum of several months of therapy.

In addition to anti-androgenic effects, the active component has pronounced gestagenic properties. It is this circumstance that can trigger a cycle disturbance. You can avoid this by combining the substance with ethinyl estradiol (just such a combination is observed in Chloe). This combination is quite effective, provided the cyclic use of drugs with full compliance with the instructions.

The contraceptive effect of drugs results from the combined action of various factors, the most important of which is the inhibition of the ovulation process, as well as changes in cervical excretion. In addition to preventing pregnancy, the combination of estrogen / progestogen relative to antiandrogen has additional advantages that can help in the process of deciding whether or not to use this method of contraception. The medication helps to make the cycle more regular, weakens soreness in menstruation and reduces bleeding. This makes it possible to reduce the incidence of anemia of iron deficiency.

There is information that the use of combined oral contraception in large doses (0.05 mg of ethinyl estradiol) caused a decrease in the likelihood of ovarian cysts, as well as inflammations in the pelvic organs, ectopic pregnancy and benign neoplasms in the thoracic glands. A similar effect from the use of lower dosages of drugs should be confirmed.

[2], [3], [4], [5],

Pharmacokinetics

Acetate of cyproterone.

With the internal use of the substance, its rapid and complete absorption occurs. Inside the serum, the peak level is observed approximately 1.6 hours after application and is equal to 15 ng / ml. Bioavailability indicators are 88%.

The substance is almost completely synthesized only with plasma albumin. About 3.5-4% of the total serum component of the component has a free form. Ethinyl estradiol causes an increase in the indices of globulin, it is synthesized with sex hormones, but it does not affect the protein bond of cyproterone acetate in any way. The distribution volume of the component is 986 ± 437 liters.

Ciproterone acetate is almost completely metabolized. The main plasma degradation product is 15β-OH-CPA, which is formed with the participation of the CYP3A4 enzyme of the hemoprotein P450. The serum clearance of the substance is 3.6 ml / minute / kg.

Serum index of cyproterone acetate decreases in 2 elimination periods in which the half-life of the substance is 0.8 hours, and also 2.3-3.3 days. Partly the substance is outputted unchanged. Decay products are excreted with bile and urine in a ratio of 2k1. The half-life of the decay products is approximately 1.8 days.

The pharmacokinetic properties of cyproterone acetate do not change under the influence of globulin, which synthesizes the sex hormone. With an everyday intake of drugs, its rate rises by approximately 2.5 times, and at the second stage of the treatment cycle it reaches stability.

Ethinyl estradiol.

With oral use of ethinyl estradiol, it is absorbed completely and quickly. The peak level inside the serum is observed after 1.6 hours and is about 71 pg / ml. During the absorption and during the first hepatic passage the substance undergoes a metabolism, as a result of which the average total bioavailability is about 45% with a significant individual variability (within 20-65%).

Ethinyl estradiol is quite active, but at the same time it is very specific synthesized with serum albumin (by 98%), and also stimulates an increase in the serum levels of globulin, which synthesizes the sex hormone. The distribution volume is approximately 2.8-8.6 l / kg.

The substance undergoes a general conjugation inside the walls of the small intestine, as well as inside the liver. Metabolism occurs mainly through the aromatic hydroxylation process, but a large number of different methylated and hydroxylated degradation products are bound, which have a free form or are conjugated to sulfuric and glucuronic acid. The indicator of the metabolic cleansing factor is 2.3-7 ml / minute / kg.

The indicator of ethinyl estradiol decreases in 2 segments of half-lives, which are approximately 10-20 hours. Excretion of unchanged substance does not occur, and the decay products are excreted with bile, and urine in the proportion of 6k4. The half-life of the decay products is approximately 1 day.

Stable values can be achieved at the 2nd stage of the treatment cycle. Serum values are 60% higher than the individual dosage.

[6], [7], [8],

Dosing and administration

The medication is required to be taken regularly to achieve the desired result and to provide contraceptive effect. At the time of treatment, it is necessary to cancel the intake of other hormonal drugs.

The Chloe regimen is similar to that for most oral contraceptives combined. You need to take tablets at least during 3-4 menstrual cycles after the manifestations of the disease disappear. With the re-development of symptoms, it is allowed to repeat the therapeutic course several weeks or months after the completion of the first. With irregular use of drugs, there may be bleeding in the period between menstruation, and weakening of its contraceptive and medicinal properties.

Tablets are taken every day, always at about the same time. If necessary, you can drink them with water. The dose is 1 tablet per day, and the duration of the course is 28 days. To start a new pack of pills is necessary after 7 days of the use of the placebo tablets, during which the bleeding that develops due to the cancellation begins approximately 2-3 days after the extreme use of the active drug. After the start of a new pack, the patient's bleeding may continue.

The length of the course depends on the severity of the pathology. Usually it lasts for several months.

It is recommended to stop the use of drugs after 3-4 cycles after the signs of the disease completely disappear.

Despite the fact that Chloe has a contraceptive effect, you can not continue to use tablets only for contraception.

[14], [15]

Use of the chloe during pregnancy

Pregnant to take Chloe is prohibited. At the onset of pregnancy during the course of treatment, it is necessary to immediately cancel the medicine.

Do not use tablets and when breastfeeding. The acetate of cyproterone penetrates into the mother's milk, and through it is transmitted to the baby (about 0.2% of the dosage taken by the mother - about 1 μg / kg). During the lactation period, about 0.02% of the daily dosage of the substance ethinylestradiol taken by the mother can be transmitted through milk to the baby.

Contraindications

The main contraindications:

• intolerance of the active components of the drug or its auxiliary elements;
• the presence of an anamnesis of arterial or venous thrombotic / thromboembolic pathologies (such as DVT, myocardial infarction, and pulmonary embolism) or stroke;
• history of prodromal signs of thrombosis (eg, angina or transitory circulatory disorder in the brain);
• the presence in the anamnesis of migraine attacks accompanied by neurological manifestations of the focal type;
• diabetes mellitus, in which vascular damage is observed;
• presence of multiple or severe factors of the possibility of developing thrombosis of the arterial or venous type;
• a history of pancreatitis that develops against a background of hypertriglyceridemia in severe form;
• presence in the anamnesis of functional hepatic disorders in a severe degree (until the moment when the liver is normalized);
• present in the history of liver tumors (malignant or benign type);
• the presumed presence of malignant neoplasms (for example, in the region of the mammary glands or genitals), depending on the sex hormones;
• having an unknown origin of bleeding from the vagina;
• the medicine is not assigned to men.

[9], [10], [11], [12],

Side effects of the chloe

Use of the medicine can cause the appearance of such side effects:

• testimony of studies: a change in the weight index;
• manifestations from the NA: often there are headaches, occasionally - migraine attacks;
• visual organs: occasionally there may be a hypersensitivity to contact lenses;
• Gastrointestinal disorders: often there are abdominal pains and nausea; rarely there may be diarrhea and vomiting. Other disorders of the digestive process are also possible;
• subcutaneous layers and skin: there may be a variety of skin reactions (such as nodular or polyiform erythema, as well as rashes);
• disorders of metabolic processes: occasionally fluid retention;
• immune manifestations: hypersensitivity is occasionally observed;
• mammary glands and reproductive organs: often there are pains in the area of mammary glands, as well as their tension; less likely to increase them; very rarely appear discharge from the breast or vagina;
• mental disorders: often there are changes in mood, as well as a depressed mood; occasionally there may be a breakdown of sexual desire.

In patients with hereditary form of Quinck edema, external estrogens can enhance the manifestations of the disease or cause its appearance.

[13]

Overdose

There is no information about the development of negative manifestations due to an overdose of the medicine. Signs are vomiting with nausea; young girls have a weak bleeding from the vagina.

Antidotes have no medication, symptomatic therapy.

Interactions with other drugs

Interaction of drugs containing estrogen / progestogen, with other medicines may cause a decrease in contraceptive effectiveness or the occurrence of breakthrough bleeding. The basics of interactions are outlined below.

Metabolic processes in the liver: it is possible to develop interaction with induction drugs of microsomal enzymes, which increase the level of the coefficient of purification of sex hormones. Among them are barbiturates and rifampicin with primidone, phenytoin and carbamazepine, and in addition, possibly topiramate with griseofulvin, as well as oxcarbazepine with felbamate and the means containing St. John's wort.

In addition, there is information that drugs slowing HIV protease (such as ritonavir), and with it NRTI (for example, nevirapine), or a combination of these drugs, can affect liver metabolism.

Portal-biliary circulation. According to the results of individual clinical tests, it can be noted that the process of portal-biliary circulation of estrogens can decrease due to the use of certain antibiotics (those that can reduce the performance of ethinylestradiol: tetracyclines and penicillins).

If you use any of the above drugs, a woman should use a barrier method of contraception (or any other) in addition to Chloe during the treatment period. During the application of inducers of microsomal enzymes, it is required to use the barrier method throughout the entire treatment period with the corresponding drug, and then for another 28 days after its withdrawal. In the case of using an antibiotic (except griseofulvin and rifampicin), the barrier method should be applied during the first week after the drug is withdrawn. In a situation where barrier contraception is still used, and a pack of Chloe tablets has already ended, you can start taking medication from a new package without the usual interval.

Oral contraception can affect the metabolism of other medicines. At the same time plasma and tissue parameters of active components of drugs may increase (in cyclosporine) or decrease (in lamotrigine).

Impact on laboratory test data. The use of Chloe and similar drugs may affect the data of some laboratory tests. Among such are the biochemical characteristics of the hepatic function, as well as the work of the adrenal glands with kidneys and thyroid glands. In addition, the plasma level of the protein (carrier) - a corticosteroid-synthesizing globulin. Together with this lipid / lipoprotein fractions, the characteristics of fibrinolysis with coagulation, as well as the metabolism of carbohydrates. Often, such changes do not go beyond the permissible norm.

Storage conditions

Tablets should be kept in a place inaccessible to young children. The temperature maximum is 25 ° C.

Shelf life

Chloe is suitable for use within 3 years from the date of release of the medicinal product.