Universal reference book for medicines
Product name: UTROZHESTAN ® (UTROGESTAN ® )

Active substance: progesterone

Type: Gestagen

Manufacturer: BESINS HEALTHCARE (Belgium) manufactured by CYNDEA PHARMA (Spain) by order of BESINS HEALTHCARE (Belgium)
Composition, form of production and packaging
Capsules
soft gelatinous, round, shiny, yellowish color;
the contents of the capsules are an oily whitish homogeneous suspension without visible phase separation.
1 caps.

progesterone natural micronized 100 mg

Excipients: sunflower oil - 149 mg, soy lecithin - 1 mg.

The composition of the capsule shell: gelatin - 76.88 mg, glycerol - 31.45 mg, titanium dioxide - 1.67 mg.

14 pcs.
- blisters (2) - packs of cardboard.
Capsules soft gelatinous, oval, shiny, yellowish color;
the contents of the capsules are an oily whitish homogeneous suspension without visible phase separation.
1 caps.

progesterone natural micronized 200 mg

Excipients: sunflower oil - 298 mg, soy lecithin - 2 mg.

The composition of the capsule shell: gelatin - 153.76 mg, glycerol - 62.9 mg, titanium dioxide - 3.34 mg.

7 pcs.
- blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Gestagenic preparation.
Progesterone, the active substance of the drug Utrozestan ® , is a hormone of the yellow body. Binding to receptors on the surface of cells of target organs penetrates into the nucleus, where activating DNA stimulates RNA synthesis.
Promotes the transition of the mucous membrane of the uterus from the proliferation phase, caused by the follicular hormone, into the secretory phase.
After fertilization promotes transition to a condition necessary for the development of a fertilized egg. Reduces excitability and contractility of the muscles of the uterus and fallopian tubes, stimulates the development of the end elements of the breast.
Stimulating proteinolipase, increases fat stores, increases the utilization of glucose.
Increasing the concentration of basal and stimulated insulin, promotes the accumulation of glycogen in the liver, increases the production of gonadotropic hormones of the pituitary gland; reduces azotemia, increases the excretion of nitrogen in the urine.
Activates the growth of the secretory department of the mammary glands, induces lactation.

Promotes the formation of normal endometrium.

PHARMACOKINETICS

Ingestion

Suction

Micronized progesterone is absorbed from the digestive tract.
The concentration of progesterone in the blood plasma gradually rises during the first hour, C max is observed 1-3 hours after administration.
The concentration of progesterone in the blood plasma increases from 0.13 ng / ml to 4.25 ng / ml after 1 h, to 11.75 ng / ml after 2 hours and is 8.37 ng / ml after 3 h, 2 ng / ml after 6 h and 1.64 ng / ml - 8 hours after admission.

Metabolism

The main metabolites that are determined in the blood plasma are 20-alpha-hydroxy-delta-4-alpha-pregnanolone and 5-alpha-dihydroprogesterone.

Excretion

It is excreted in the urine in the form of metabolites, 95% of them are glucuron-conjugated metabolites, mainly 3-alpha, 5-beta-pregnanediol (pregnannione).

These metabolites, which are determined in the blood plasma and in urine, are similar to substances formed during the physiological secretion of the yellow body.

With intravaginal injection

Suction

Absorption occurs quickly, progesterone accumulates in the uterus.
A high level of progesterone is observed 1 h after administration. C max of progesterone in the blood plasma is achieved 2-6 hours after administration. When the drug is administered 100 mg twice a day, the average concentration remains at the level of 9.7 ng / ml for 24 hours.
When administered at doses of more than 200 mg / day, the progesterone concentration corresponds to the I trimester of pregnancy.

Metabolism

Metabolized with the formation of predominantly 3-alpha, 5-beta-pregnanediol.
The level of 5-beta-pregnanolone in plasma does not increase.
Excretion

It is excreted in the urine in the form of metabolites, the main part is 3-alpha, 5-beta-pregnanediol (pregnannione).
This is confirmed by a constant increase in its concentration (C max 142 ng / ml after 6 h).
INDICATIONS

Progesterone deficiency in women:

oral route of administration:

- infertility due to luteal insufficiency;

- Premenstrual tension syndrome;

- violations of the menstrual cycle due to a violation of ovulation or anovulation;

- fibrocystic mastopathy;

- pre-menopause;

- hormone replacement therapy (HRT) in peri- and postmenopausal (in combination with estrogen-containing drugs).

vaginal route of administration:

- Threatening abortion or prevention of habitual abortion due to insufficient progesterone;

- Prevention (prevention) of preterm delivery in women at risk (with cervical shortening and / or

presence of anamnestic data of preterm labor and / or

premature rupture of membranes);

- support of the luteal phase during preparation for in vitro fertilization;

- support of the luteal phase in the spontaneous or induced menstrual cycle;

premature menopause;

- HRT (in combination with estrogen-containing drugs);

- infertility due to luteal insufficiency;

- HRT with a deficiency of progesterone with non-functioning (absent) ovaries (donation of oocytes).

DOSING MODE

The duration of treatment is determined by the nature and characteristics of the disease.

Oral route of administration

The drug should be taken orally, washed down with water.
In most cases, when progesterone is inadequate, the daily dose of Utrozestan ® is 200-300 mg divided into 2 divided doses (morning and evening).
If the luteal phase is insufficient (premenstrual tension syndrome, fibrocystic mastopathy, dysmenorrhea, premenopause), the daily dose of the drug is 200 or 400 mg for 10 days (usually from the 17th to the 26th day of the cycle).

With HRT in perimenopause with the use of estrogens, the drug Utrozestan ® is used at 200 mg / day for 12 days.

With HRT in postmenopause in a continuous mode, the drug Utrozestan ® is used in a dose of 100-200 mg from the first day of taking estrogens.
The dose is selected individually.
Vaginal route of administration

Capsules are injected deep into the vagina.

Prevention (prevention) of preterm delivery in women at risk (with cervical shortening and / or the presence of anamnestic data of premature birth and / or premature rupture of membranes): the usual dose is 200 mg at bedtime, from 22nd to 34th weeks pregnancy.

Complete absence of progesterone in women with non-functioning (absent) ovaries (egg donation): against estrogen therapy 200 mg / day on the 13th and 14th days of the cycle, then 100 mg 2 times / day from the 15th to The 25th day of the cycle, from the 26th day and in the case of pregnancy determination, the dose increases by 100 mg / day every week, reaching a maximum of 600 mg / day, divided into 3 doses.
This dose is usually applied for 60 days.
Support of the luteal phase during the in vitro fertilization cycle: it is recommended to use 200 to 600 mg / day, starting from the day of injection of the chorionic gonadotropin during the I and II trimesters of pregnancy.

Support of the luteal phase in the spontaneous or induced menstrual cycle, infertility associated with a violation of the function of the yellow body: it is recommended to apply 200-300 mg / day, starting from the 17th day of the cycle for 10 days, in the case of delay in menstruation and pregnancy diagnosis treatment should be continued.

In cases of threatening abortion or in order to prevent habitual abortion that occur against the background of progesterone deficiency: 200-400 mg / day in 2 divided doses every day in the first and second trimesters of pregnancy.

SIDE EFFECT

The undesirable phenomena listed below, indicated by the oral route of application , are distributed according to the frequency of occurrence according to the following gradation: often (> 1/100, <1/10);
infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000).
System of organs Adverse effects

often infrequently rarely very rarely

On the part of the genitals and mammary glands Disorders of the menstrual cycle Amenorrhea Acyclic bleeding Mastodynia

From the side of the psyche Depression

From the side of the nervous system Headache Drowsiness Transient dizziness

From the gastrointestinal tract bloating Vomiting Diarrhea Constipation Nausea

From the side of the liver and bile ducts Cholestatic jaundice

From the immune system Hives

From the skin and subcutaneous tissues of the itch of Acne Chloasma

Drowsiness, transient dizziness are possible, as a rule, 1-3 hours after taking the drug.
These side effects can be reduced by lowering the dose, applying the drug at bedtime or switching to a vaginal route of administration.
These undesirable effects are usually the first signs of an overdose.

Drowsiness and / or transient dizziness are observed, in particular, in the case of concomitant hypoestrogenia.

Reducing the dose or restoring a higher estrogenation immediately eliminates these phenomena without reducing the therapeutic effect of progesterone.

If the treatment starts too early (in the first half of the menstrual cycle, especially before the 15th day), there may be a shortening of the menstrual cycle or acyclic bleeding.

Recorded changes in the menstrual cycle, amenorrhea, or acyclic bleeding are common to all progestogens.

Application in clinical practice

In the post-marketing application, the following adverse events with oral administration of progesterone were noted: insomnia, premenstrual syndrome, mammary tension, vaginal discharge, joint pain, hyperthermia, increased sweating at night, fluid retention, weight change,

acute pancreatitis, alopecia, hirsutism, changes in libido, thrombosis and thromboembolic complications (with HRT in combination with estrogen-containing drugs), increased blood pressure.

The composition of the drug includes soy lecithin, which can cause hypersensitivity reactions (hives and anaphylactic shock).

With vaginal application

Some cases of development of local intolerance reactions of the drug components have been reported (in particular,

soy lecithin) in the form of hyperemia of the vaginal mucosa, burning, itching, oily discharge.

Systemic side effects with intravaginal application of the drug at recommended doses, in particular,

drowsiness or dizziness (observed with oral administration of the drug) were not noted.

CONTRAINDICATIONS

- hypersensitivity to the components of the drug;

- deep vein thrombosis, thrombophlebitis, thromboembolic disorders (pulmonary embolism, myocardial infarction, stroke), intracranial hemorrhage or the presence of these conditions / diseases in the anamnesis;

bleeding from the vagina of unknown origin;

- incomplete abortion;

- porphyria;

- established or suspected malignant neoplasms of the mammary glands and genitals.

For oral use:

- severe liver disease (including cholestatic jaundice, hepatitis, Dubin-Johnson syndromes, rotor, malignant liver tumors) at present or in the anamnesis.

With caution should apply the drug for diseases of the cardiovascular system, arterial hypertension, chronic kidney failure, diabetes, bronchial asthma, epilepsy, migraine, depression, hyperlipoproteinemia.

PREGNANCY AND LACTATION

At pregnancy the preparation can be applied only intravaginally.

The drug should be used with caution in the II and III trimesters of pregnancy because of the risk of developing cholestasis.

Progesterone penetrates into breast milk, so the use of the drug is contraindicated during breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution apply the drug for chronic kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated use of the drug in porphyria;
when administered orally with severe liver disease (including cholestatic jaundice, hepatitis, Dubin-Johnson syndromes, rotor, malignant liver tumors) currently or in the anamnesis.
SPECIAL INSTRUCTIONS

The drug Utrozestan ® can not be used for the purpose of contraception.

The drug should not be taken with food;
eating increases the bioavailability of progesterone.
The drug Utrozestan ® should be taken with caution in patients with diseases and conditions that can worsen with fluid retention (arterial hypertension, cardiovascular disease, chronic renal failure, epilepsy, migraine, bronchial asthma);
in patients with diabetes mellitus; violations of liver function of mild and moderate severity;photosensitivity.
It is necessary to observe patients with depression in the anamnesis, and in case of development of depression of a serious degree, it is necessary to cancel the drug.

Patients with concomitant cardiovascular diseases or their presence in anamnesis should also be observed periodically by a physician.

Use of the drug Utrozestan ® after the first trimester of pregnancy can cause the development of cholestasis.

Prolonged treatment with progesterone requires regular physical examinations (including liver function tests);
treatment should be canceled in case of deviations from normal indicators of functional liver or cholestatic jaundice.
When using progesterone, it is possible to reduce glucose tolerance and increase the need for insulin and other hypoglycemic drugs in patients with diabetes mellitus.

In the case of amenorrhea in the process of treatment, it is necessary to exclude the presence of pregnancy.

If the treatment starts too early at the beginning of the menstrual cycle, especially before the 15th day of the cycle, a cycle shortening and / or acyclic bleeding may occur.
In the case of acyclic bleeding, the drug should not be used until the cause is determined, including the histological examination of the endometrium.
If there is a history of chloasma or a tendency to develop it, patients are advised to avoid UV irradiation.

More than 50% of cases of spontaneous abortions in the early stages of pregnancy are due to genetic disorders.
In addition, the cause of spontaneous abortions in the early stages of pregnancy can be infectious processes and mechanical damage. Use of the drug Utrozestan ® in these cases can only lead to a delay in the rejection and evacuation of a non-viable fetal egg.
The use of the drug Utrozestan ® in order to prevent threatening abortion is justified only in cases of progesterone insufficiency.

The composition of the drug Utrozestan ® includes soy lecithin, which can cause hypersensitivity reactions (hives and anaphylactic shock).

When carrying out HRT with estrogens during the period of perimenopause, the use of the drug Utrozestan ® is recommended for no less than 12 days of the menstrual cycle.

With the continuous mode of HRT in postmenopause, the use of the drug is recommended from the first day of taking estrogens.

When HRT is increased, the risk of developing venous thromboembolism (deep vein thrombosis or pulmonary embolism), the risk of ischemic stroke, IHD.

Because of the risk of developing thromboembolic complications, the drug should be discontinued if:

- visual disturbances such as loss of vision, exophthalmos, double vision, vascular lesions of the retina;
migraine;
- venous thromboembolism or thrombotic complications, regardless of their location.

If there is a history of thrombophlebitis, the patient should be carefully monitored.

When using the drug Utrozestan ® with estrogen-containing drugs, you should refer to the instructions for their use regarding the risks of venous thromboembolism.

The results of the Clinical Study of the Women's Health Initiative Study (WHI) indicate a slight increase in the risk of breast cancer in the long-term, more than 5 years, combined use of estrogen-containing drugs with synthetic gestagens.
It is not known whether there is an increased risk of breast cancer in postmenopausal women with HRT using estrogen-containing drugs in combination with progesterone.
The results of the WHI study also revealed an increased risk of developing dementia at the onset of HRT at the age of over 65 years.

Before the onset of HRT and regularly during the course of HRT, a woman should be examined for contraindications to her.
If there is a clinical indication, a breast examination and gynecological examination should be performed.
The use of progesterone may affect the results of some laboratory tests, including indicators of liver function, thyroid function;
coagulation parameters; concentration of pregnanediol.
Impact on the ability to drive vehicles and manage mechanisms

When using the drug orally, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: drowsiness, transient dizziness, euphoria, shortening of the menstrual cycle, dysmenorrhea.

In some patients, the average therapeutic dose may be excessive because of the available or occurring unstable endogenous secretion of progesterone, a particular sensitivity to the drug, or a too low concentration of estradiol.

Treatment:

- in case of occurrence of drowsiness or dizziness, it is necessary to reduce the daily dose or prescribe the drug before bedtime for 10 days of the menstrual cycle;

- in the case of a shortening of the menstrual cycle or "smearing" bloody discharge, it is recommended that the treatment be started on a later day of the cycle (for example, on the 19th day instead of the 17th);

- in perimenopausal and make sure that the estradiol concentration is optimal for hormone replacement therapy in postmenopausal women.
In overdose symptomatic treatment if necessary.
DRUG INTERACTION

For oral application
progesterone enhances the action of diuretics, antihypertensive drugs, immunosuppressants, anticoagulants.
Reduces the lactogenic effect of oxytocin.
The simultaneous use of drugs, CYP3A4 inducers microsomal enzymes of the liver, such as barbiturates, antiepileptics (phenytoin), rifampicin, phenylbutazone, spironolactone, griseofulvine, accompanied by acceleration of progesterone metabolism in the liver.
Simultaneous administration of progesterone with some antibiotics (penicillins, tetracyclines) may reduce its effectiveness due to violation of enterohepatic recirculation of sex hormones due to changes in the intestinal microflora.
The severity of these interactions can be varied in different patients, and the prognosis of clinical effects of these interactions is complicated.
Ketoconazole may increase the bioavailability of progesterone.
Progesterone can increase the concentration of ketoconazole and cyclosporin.
Progesterone can reduce the effectiveness of bromocriptine.
Progesterone may cause impaired glucose tolerance, whereby - the need to increase the insulin or other hypoglycemic agents in patients with diabetes.
The bioavailability of progesterone can be reduced in smokers and patients with excessive alcohol consumption.
When intravaginal application
progesterone interaction with other drugs in intravaginal application was not evaluated. It should avoid the simultaneous use of other drugs used intravaginally, to avoid disturbing the release and absorption of progesterone.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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