Dydrogesterone in its molecular structure, chemical and pharmacological properties very similar to natural progesterone. Due to the fact that not a dydrogesterone derivative of testosterone, it has no side effects typical of most synthetic progestogens, androgen so called progestogen.
Dydrogesterone has no estrogenic, androgenic, anabolic, glucocorticoid and thermogenic activity. As progestagenic component of hormone replacement therapy (HRT) in menopause, dydrogesterone contributes to maintaining the favorable action of estrogen on blood lipid profile. However, unlike estrogen, which is usually a negative effect on the blood clotting system, dydrogesterone has no effect on coagulation parameters. No adverse effects on carbohydrate metabolism and liver function.
Dydrogesterone with oral selectively acts on the endometrium, thereby preventing an increased risk of endometrial hyperplasia and / or carcinogenesis with an excess of estrogen. It is indicated in all cases of endogenous progesterone deficiency.
The drug has no contraceptive effect.
When treating dydrogesterone therapeutic effect is achieved without suppressing ovulation or menstrual dysfunction. Didrogesteron allows conception and continuation of the pregnancy during treatment.
After oral administration, dydrogesterone is rapidly absorbed from the gastrointestinal tract. Cmax in plasma attained at 2 hours after ingestion.
Plasma protein binding is 97%.
Dydrogesterone is metabolized in the liver by hydroxylation of the ketone groups of the 20th carbon atom. Along with this, also observed hydroxylating methyl groups 21st carbon atom and a very minor amount of 16-α carbon atom.
Excreted in the urine of 56 to 79% preferably in the form of glucuronic acid conjugates. The presence of unchanged substance was found. After 24 h, displayed approximately 85% at 72 hours removal process is almost ended.
Pharmacokinetics in special clinical situations
Information about the delay in the body or enhance the action of progesterone in patients with impaired renal function have been reported.
10 mg dydrogesterone.
of lactose monohydrate – 111.1 mg,
Valium – 2.8 mg,
corn starch – 14 mg,
Colloidal silicon dioxide – 1.4 mg,
magnesium stearate – 700 micrograms.
Opadry White Y-1-7000 (hypromellose, polyethylene glycol 400, titanium dioxide (E171)) – 4 mg.
At menopause, from menstrual disorders, from a threatening miscarriage
Condition characterized by a deficiency of progesterone:
- infertility due to luteal insufficiency;
- threatening or habitual miscarriage (with progesterone deficiency);
- premenstrual syndrome;
- dysmenorrhea, irregular menstruation;
- secondary amenorrhea (in combined therapy with estrogens);
- dysfunctional uterine bleeding.
Hormone Replacement Therapy
- to neutralize the proliferative effect of estrogens on the endometrium as part of hormone replacement therapy in women with disorders due to natural or surgical menopause with an intact uterus.
- Hypersensitivity to dydrogesterone or other ingredients.
Be wary: should be prescribed when specifying a history of itching during a previous pregnancy.
From hemopoiesis system: in rare cases – hemolytic anemia.
Immune system: very rarely – hypersensitivity reactions.
CNS: headache, migraine.
On the part of the hepatobiliary system: rarely – a slight dysfunction of the liver, sometimes accompanied by weakness or malaise, jaundice, or pain in the abdomen.
On the part of the reproductive system: in rare cases – breakthrough uterine bleeding (which can be prevented by increasing the dose); increased sensitivity of the mammary glands.
Skin and subcutaneous tissue: allergic reactions such as skin rash, itching, hives; very rarely – angioedema.
Other: rarely – peripheral edema.
How to accept, acceptance rate and dosage
The drug is taken orally.
In endometriosis appoint 10 mg 2-3 times / day with a 5-to 25-day cycle or continuously.
Infertility (due to luteal insufficiency) – 10 mg / day from the 14th to the 25th day of the cycle. Treatment should be carried out continuously for at least 6 consecutive cycles. The treatment is recommended to continue in the first months of pregnancy, as recommended in habitual abortion.
When the threatened abortion administered 40 mg once, then – 10 mg every 8 hours until disappearance of symptoms.
When habitual abortion drug is prescribed 10 mg of 2 times / day to 20 weeks of gestation with subsequent tapering.
Premenstrual syndrome – 10 mg 2 times / day from the 11th to the 25th day of the cycle.
Dysmenorrhea – 10 mg of 2 times / day with a 5-to 25-day cycle.
At irregular menstruation – 10 mg 2 times / day from the 11th to the 25th day of the cycle.
When administered estrogens amenorrhea 1 time / day from the 1st to the 25th day of the cycle, together with djufaston – 10 mg of 2 times / day from the 11th to 25th day of the cycle.
To stop dysfunctional uterine bleeding Dyufaston® administered 10 mg of 2 times / day for 5-7 days.
For the prevention of dysfunctional uterine bleeding Dyufaston® administered 10 mg of 2 times / day from the 11th to 25th day of the cycle.
In hormone replacement therapy in combination with continuous estrogen therapy Dyufaston® appoint 10 mg 1 time / day for 14 days within 28-day cycle. When the cyclic regimen Dyufaston® estrogens is administered in a dose of 10 mg 1 time / day for the last 12-14 days of estrogen.
If ultrasound or biopsy evidence of inadequate response to progestogen drug, the daily dose should be increased to 20 mg.
In a dry place at a temperature not higher than 30 ° C, in the original package
In an application with djufaston inducers of hepatic microsomal enzymes (such as phenobarbital, rifampin) may accelerate metabolism of progesterone and reduce the effectiveness of the drug.
Cases of incompatibility with other drugs known.
Some patients may experience breakthrough bleeding, which can be prevented by increasing the dose of the drug.
In the case of destination Dydrogesterone in combination with estrogens (e.g. HRT) should consider the contraindications and warnings associated with the use of estrogen.
Before starting HRT should compile a complete medical history. During treatment, it is recommended to periodically control the individual tolerability of HRT. The patient should be informed about any changes in her breasts should be reported to your doctor. Studies, including mammography, should be carried out in accordance with generally accepted screening patients.
When HRT accurate assessment of the risks and benefits determined in due course.
Sometime during the first months of treatment, you may experience breakthrough uterine bleeding. If breakthrough bleeding occurs after a period of drug administration or continue after the course of treatment, should examine the cause, make endometrial biopsy to exclude endometrial malignancy.
It requires careful clinical examination when specifying a history of a progesterone-dependent tumors (e.g., meningioma), and in the case of progression of pregnancy or during the preceding hormonal therapy.
Should not be administered to patients with Dyufaston® genetically determined galactose intolerance, lactase deficiency or malabsorption syndrome.
Effects on ability to drive vehicles and other machines that require high concentration of attention
The drug does not affect the ability to drive vehicles and management mechanisms.
Pregnancy and lactation
Can be used during pregnancy duphaston indicated.
Dydrogesterone is excreted in breast milk. Breastfeeding during treatment is not recommended.
So far, cases of drug overdose Dyufaston® were reported.
Treatment: the random receiving a dose considerably exceeding the therapeutic one, recommended gastric lavage; if necessary symptomatic treatment.
No specific antidote.