Chloe

Chloe is an antiandrogen drug.

Indications Chloe

It is used to eliminate androgen pathologies in women:

• acne, especially of a pronounced nature, as well as those accompanied by the development of inflammatory processes or seborrhea, as well as the formation of nodules (papular-pustular or nodular-cystic acne);
• androgenic alopecia;
• mild hirsutism.

It can also be used as a contraceptive (but the drug is prohibited for use solely as a contraceptive; it is prescribed only for the treatment of androgen states in women).

Release form

Released in tablets, 21 or 7 pieces (placebo tablets) per blister. Inside the package - 1 or 3 blister plates.

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Pharmacodynamics

Cyproterone acetate is the active component of the drug. It slows down the action of androgens produced by the female body. The drug allows you to treat pathologies caused by the binding of androgens or diseases due to hypersensitivity to these hormones.

During the period of using Chloe, the increased activity of the sebaceous glands, which are important factors in the development of seborrhea and acne, slows down. Thanks to the drug, existing rashes disappear within 3-4 months of the course. Increased oiliness of hair and skin decreases more quickly. Hair loss, which is often observed with seborrhea, usually decreases or disappears.

The therapy is prescribed to women of reproductive age who have hirsutism to a moderate degree (especially slightly increased facial hair). However, the result becomes noticeable after at least several months of therapy.

In addition to the antiandrogenic effect, the active component has pronounced gestagenic properties. This circumstance can provoke cycle disorders. This can be avoided by combining the substance with ethinyl estradiol (this is the combination observed in Chloe). This combination is quite effective, provided that the drug is used cyclically with full compliance with the instructions.

The contraceptive effect of the drug occurs as a result of the combined action of various factors, the most important of which is the suppression of the ovulation process, as well as changes in cervical excretion. In addition to preventing pregnancy, the combination of estrogen/gestagen relative to the antiandrogen has additional advantages that can help in the decision process whether or not to use this method of contraception. The drug helps to make the cycle more regular, reduces pain during menstruation and reduces bleeding. This also helps to reduce the incidence of iron deficiency anemia.

There is information that the use of combined oral contraception in high doses (0.05 mg of ethinyl estradiol) caused a decrease in the likelihood of ovarian cysts, as well as inflammation in the pelvic organs, ectopic pregnancy and benign neoplasms in the mammary glands. A similar effect from the use of lower doses of the drug still needs to be confirmed.

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Pharmacokinetics

Cyproterone acetate.

When taken internally, the substance is rapidly and completely absorbed. In serum, the peak level is observed approximately 1.6 hours after administration 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 is in free form. Ethinyl estradiol causes an increase in globulin levels, is synthesized with sex hormones, but does not affect the protein bond of cyproterone acetate. The distribution volume of the component is 986±437 l.

Cyproterone 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 hemoprotein P450. Serum clearance of the substance is 3.6 ml/minute/kg.

Serum cyproterone acetate decreases in 2 elimination periods, in which the half-life segments of the substance are noted - 0.8 hours, and 2.3-3.3 days. The substance is partially excreted unchanged. The decay products are excreted with bile and urine in a ratio of 2:1. 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 the sex hormone-synthesizing globulin indices. With daily administration of the drug, its index increases approximately 2.5 times, and at the 2nd stage of the treatment cycle it reaches stability.

Ethinyl estradiol.

When taken orally, ethinyl estradiol is absorbed completely and rapidly. Peak serum levels are observed after 1.6 hours and are approximately 71 pg/ml. During absorption and first liver passage, the substance undergoes metabolism, resulting in an average overall bioavailability of approximately 45% with significant individual variability (within 20-65%).

Ethinyl estradiol is synthesized quite actively, but also very specifically with serum albumin (98%), and also stimulates an increase in serum levels of sex hormone-synthesizing globulin. The distribution volume is approximately 2.8-8.6 l/kg.

The substance undergoes general conjugation within the small intestinal wall and also within the liver. Metabolism occurs mainly by aromatic hydroxylation, but a large number of different methylated and hydroxylated breakdown products are bound, which are free or conjugated with sulfuric and glucuronic acid. The metabolic clearance coefficient is 2.3-7 ml/min/kg.

The ethinyl estradiol level decreases in 2 half-life periods of approximately 10-20 hours. There is no excretion of unchanged substance, and the decay products are excreted in the bile and urine in a ratio of 6:4. The half-life of the decay products is approximately 1 day.

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

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Dosing and administration

The medicine must be taken regularly to achieve the desired result and provide contraceptive effect. During treatment, it is necessary to stop taking other hormonal drugs.

The regimen for taking Chloe is similar to the regimen for using most combined oral contraceptives. The tablets should be taken at least during 3-4 menstrual cycles after the symptoms of the disease have disappeared. If symptoms recur, the therapeutic course can be repeated several weeks or months after the first one has been completed. If the drug is used irregularly, bleeding may occur between periods, as well as its contraceptive and medicinal properties may be weakened.

The tablets are taken every day, always at about the same time. If necessary, they can be washed down with water. The dose is 1 tablet per day, and the course duration is 28 days. It is necessary to start a new pack of tablets after a 7-day interval of taking placebo tablets, during which bleeding due to drug withdrawal begins approximately 2-3 days after the last use of the active drug. After starting a new pack, the patient may continue to bleed.

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

It is recommended to stop using the drug after 3-4 cycles after the signs of the disease have completely disappeared.

Even though Chloe also has a contraceptive effect, you cannot continue to use the pills for contraception alone.

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Use Chloe during pregnancy

Pregnant women are prohibited from taking Chloe. If pregnancy occurs during the course of treatment, the drug must be discontinued immediately.

The tablets should not be used during breastfeeding. Cyproterone acetate penetrates into breast milk and is transferred to the infant through it (about 0.2% of the dose taken by the mother - approximately 1 mcg / kg). During lactation, about 0.02% of the daily dose of ethinyl estradiol taken by the mother can be transferred to the child through milk.

Contraindications

Main contraindications:

• intolerance to the active components of the drug or its auxiliary elements;
• history of arterial or venous thrombotic/thromboembolic pathologies (such as DVT, myocardial infarction, and pulmonary embolism) or stroke;
• history of prodromal signs of thrombosis (for example, angina pectoris or transient cerebrovascular accident);
• history of migraine attacks accompanied by focal neurological manifestations;
• diabetes mellitus, in which vascular damage is observed;
• the presence of multiple or severe factors that may lead to the development of arterial or venous thrombosis;
• a history of pancreatitis that develops against the background of severe hypertriglyceridemia;
• history of severe functional liver disorders (until liver function returns to normal);
• history of liver tumors (malignant or benign);
• suspected presence of malignant neoplasms (for example, in the mammary glands or genitals) that depend on sex hormones;
• vaginal bleeding of unknown origin;
• The medicine is not prescribed to men.

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Side effects Chloe

Using the medicine may cause the following side effects:

• research indications: change in body weight index;
• manifestations from the nervous system: headaches often occur, and migraine attacks occasionally occur;
• visual organs: hypersensitivity to contact lenses may occasionally occur;
• Gastrointestinal disorders: abdominal pain and nausea often occur; diarrhea and vomiting may be observed rarely. Other digestive disorders are also possible;
• subcutaneous layers and integument: various skin reactions may occur (such as erythema nodosum or erythema multiforme, as well as rashes);
• metabolic disorders: fluid retention is occasionally possible;
• immune manifestations: hypersensitivity is rarely observed;
• mammary glands and reproductive organs: pain in the mammary glands often appears, as well as their tension; less often, their enlargement is possible; discharge from the breast or vagina appears very rarely;
• Mental disorders: mood swings and depressive moods are common; sexual desire disorder may occasionally occur.

In patients with a hereditary form of Quincke's edema, external estrogens can increase the manifestations of the disease or cause its occurrence.

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Overdose

There is no information about the development of negative manifestations due to drug overdose. Signs include vomiting with nausea; in young girls, slight bleeding from the vagina occurs.

The medicine has no antidotes; therapy is symptomatic.

Interactions with other drugs

Interactions of drugs containing estrogen/progestogen with other drugs may result in decreased contraceptive effectiveness or breakthrough bleeding. Key information regarding interactions is provided below.

Metabolic processes in the liver: possible interaction with drugs-inducers 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 products containing St. John's wort.

In addition, there is information that drugs that inhibit HIV protease (such as ritonavir), and along with them NRTIs (for example, nevirapine), or combinations 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 indicators of ethinyl estradiol: tetracyclines and penicillins).

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

Oral contraception may affect the metabolism of other drugs. In this case, plasma and tissue indices of active drug components may increase (for cyclosporine) or decrease (for lamotrigetine).

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

Storage conditions

The tablets must be kept out of the reach of small children. Maximum temperature is 25°C.

Shelf life

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