Drospirenon

Дроспиренон Constitutional formula

The description is actual on 08.02.2016

  • Latin name: Drospirenonum
  • ATH code: G03FA17, G03AA12
  • Chemical formula: C24H30O3
  • CAS code: 67392-87-4

Chemical name

1,2 dihydrospirorenonum, (6R,7R,8R,9S,10R,13S,14S,15S,16S,17S)-1,3,4,6,6a,7,8,9,10,11,12,13,14,15,15a,16-гексадекагидро-10,13-диметилспиро-[17H-ditsiklopropa-6,7:15,16] of a tsiklopent [a] fenantrin-17,2 ′ (5H) - furan]-3,5 ′ (2H) - Dion))

Chemical properties

Drospirenon, what is it? This substance treats group of peroral contraceptive means. Most often it is applied in a combination with other hormones. Medicine is capable to have therapeutic effect on androgenzavisimy diseases.

Drospirenon, what hormone is? Drospirenon is a synthetic hormone, on the properties is close to natural progesterone, derivative Spironolactonum. The molecular mass of a chemical compound = 366,5 grams on mol. Substance density = 1,26 grams on cm3, temperature of melting makes about 200 degrees Celsius.

Drospirenon in Wikipedia is mentioned in articles about hormonal contraception and influence of medicines on sexual function of the person.

Pharmacological action

Gestagenny, anti-gonadotropic, antimineralokortikoidny, anti-androgenic.

Pharmacodynamics and pharmacokinetics

Thanks to the fact that this substance possesses pronounced anti-androgenic properties it favorably influences the course of androgenzavisimy diseases, such as an acne, an alopecia and seborrhea. Drospirenon stimulates removal of ions of sodium and other liquids from an organism owing to what arterial pressure is normalized, puffiness and morbidity in mammary glands falls down, body weight decreases.

Clinical trials showed that after 4 months of use of medicine systolic pressure decreases on average by 2-4 mm of a mercury column, and diastolic — by 1-3 mm of mercury., weight is lost on 1-2 kg. At women during a menopause the probability of developing of a colon cancer, hyperplasia and cancer of an endometria considerably decreases.

Synthetic hormone does not possess oestrogenic, androgenic and glucocorticosteroid activity, does not change an insulinorezistentnost and reaction of an organism to glucose. In the course of treatment by drug at the patient cholesterol level in blood and LPNP decreases, concentration of triglycerides slightly increases.

After reception of the tablets containing Drospirenon, active agent is quickly and almost completely acquired by an organism. Biological availability of substance makes about 75-85%. Parallel meal does not exert impact on drug pharmacokinetics. Concentration of medicine in a blood plasma decreases dvukhfazno, the elimination half-life makes 35-40 hours. At systematic, daily reception equilibrium concentration of means is observed in 10 days.

At means big extent of linkng with proteins of plasma (seralbumin) – about 95-97%. The main metabolites of hormone are formed, without mentioning system of P450 cytochrome. Drug in the form of metabolites with a stake and urine is removed, the insignificant part is excreted in not changed look.

Indications to use

Means is appointed:

  • as a part of complex therapy for prevention of postmenopauzny osteoporosis;
  • in need of carrying out hormonal contraception at women with deficit of folates or a delay of liquid in an organism;
  • as replaceable hormonal treatment at climacteric frustration for elimination of inflow, perspiration and other vasculomotor symptoms;
  • at involutional changes of an urinogenital path at women with an unextracted uterus;
  • in combination with other synthetic hormones for contraception;
  • for contraception at heavy PMS;
  • at a severe and moderate form of eels for contraception.

Contraindications

Medicine is contraindicated:

  • to patients with an allergy to Drospirenon;
  • at a porphyria;
  • to persons with tendency to formation of blood clots;
  • at a heavy liver failure;
  • during a lactation;
  • at a thrombembolia or thrombophlebitis in a severe form;
  • if at the patient vaginal bleedings of an unknown origin are observed;
  • at a breast cancer or other generative organs;
  • to pregnant women.

Side effects

During treatment by drug can develop:

  • allergic reactions of varying severity, dizziness;
  • thromboembolism of a pulmonary artery or vessels of a brain;
  • thrombophlebitis, blood clots in retina veins;
  • arterial hypertension, puffiness, headaches;
  • calculous cholecystitis;
  • drowsiness, apathy, depressions;
  • decrease in visual acuity, vomiting, growth or weight reduction;
  • galactorrhoea, nausea, hirsutism;
  • alopecia, painful feelings and swelling of mammary glands;
  • bloody or unusual consistence vaginal allocations;
  • decrease in a sexual inclination, hloazm;
  • sleeplessness, decrease in a convulsive threshold, varicosity.

Drospirenon, application instruction (Way and dosage)

Depending on in what combination this hormone is in a tablet, it is appointed according to various schemes of treatment. According to the instruction for Drospirenon in tablets, he is accepted once a day, at the same time.

Therapy is begun after cancellation of the previous hormonal means, according to recommendations of the doctor. Treatment duration is also established in an individual order and often depends on efficiency of carrying out therapy.

Overdose

At overdose there can be nausea, vaginal bleeding, vomiting. Because medicine has no specific antidote, treatment – symptomatic.

Interaction

At prolonged treatment by drugs which is induced by liver enzymes (barbiturates, carbamazepine, oskarbazepiny, hydantoin derivatives, Primidonum, rifampicin, topiramaty, griseofulvin, felbamaty) increases clearance of this substance and reduces their efficiency. As a rule this effect is shown in 2-3 weeks, after the beginning of carrying out therapy and remains within a month after the termination of administration of drugs.

Medicine reduces efficiency of the drugs stimulating smooth muscles of a uterus and anabolic steroids.

Terms of sale

The recipe is necessary.

Special instructions

When carrying out a number of uncontrollable randomized researches the increased risk of development of a venous thromboembolism was revealed during treatment by means. It is necessary to appoint with extra care drug to women who have a predisposition to developing of a venous thrombembolia (heredity, obesity, age). It is necessary to correlate attentively indicators "risk – advantage".

Seldom against treatment arose high-quality, and is even more rare — malignant tumors of a liver. If the patient has any symptoms of this disease, pain in the area under edges, increase in body and intra belly bleeding, then treatment needs to be interrupted.

At patients with moderate and easy degree of a renal failure reception of this synthetic hormone can affect concentration of potassium ions in blood serum. There is a small risk of development of a hyperpotassemia, especially, if the patient in addition takes kaliysberegayushchy medicine.

Before an initiation of treatment means recommends to pass gynecologic and all-medical examination, it is recommended to pay special attention to cytologic research of tserkvialny slime and mammary glands, system of a blood coagulation, to exclude pregnancy. During therapy periodically these researches should be repeated.

With antibiotics

It is probable that some antibiotics can affect a drug metabolism.

Drugs in which contains (Analogues)

Coincidence on the ATH code of the 4th level:

Hormone Drospirenon in contraceptives: Angélique, Angélique Micro (with oestradiol); Yarina, Dailla, Midiana, Dimia, Jes, Vidora, Modell Pro, Simitsia, Modell Trend (+ ethinylestradiol); Yarina Plus, Jes Plus (+ ethinylestradiol + calcium levomefolinat).

Gestoden or Drospirenon, what is better?

Both synthetic hormones belong to drugs of the last generation. They are rather effective and possess the minimum quantity of side effects. The medicines containing Gestoden more often are appointed at a dysmenorrhea and for installation of a regular menstrual cycle. Drospirenon it is reasonable to use for contraception to reduce expressiveness of PMS, to get rid of an acne, to bring excess liquid out of an organism. It is necessary to remember the increased risk of development of a thromboembolism and hyperpotassemia during treatment by Drospirenon.

Dezogestrel or Drospirenon, what is better?

Dezogestrel, as well as Drospirenon belongs to hormonal contraceptives of the last generation. By analogy with Gestoden, substance is applied to elimination of a dysmenorrhea. Also it should be noted that during clinical trials was established that the risk of a set of weight is higher during treatment by Drospirenon. Anyway, the attending physician has to accept the decision on what of the listed above substances should be chosen.

Responses

About drug generally positive. Especially well doctors write about medicine, noting its high performance against low probability of development of side effects.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance use Drospirenon surely consult with the attending physician.