Iprozhin - instructions for use, doses, side effects, contraindications

Active substanceProgesteroneProgesterone

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Dosage form: & nbspcapsules

Composition:

COMPOSITION per one capsule:

Active substance: progesterone micronized - 100 mg / 200 mg.

Excipients: peanut oil - 149.0 mg / 298.0 mg; soy lecithin 1.0 mg / 2.0 mg;

Capsule shell *: gelatin - 77.0 mg / 158.60 mg; glycerol - 32.12 mg / 64.10 mg; titanium dioxide - 0.88 mg / 2.17 mg.

* - in terms of a dry capsule shell.

Description:

Soft capsules are ovoid in shape, white or almost white in color.

The contents of capsules are a thin suspension of white or white with a hint of color.

Pharmacotherapeutic group:Gestagen

ATX: & nbsp

G.03.D.A Derivative derivatives

G.03.D.A.04 Progesterone

Pharmacodynamics:

The active substance of Iprozyn is progesterone - The hormone of the yellow body. Linking to receptors on the surface of cells target organs, progesterone penetrates into the nucleus where, by activating DNA, stimulates the synthesis of RNA. Promotes the transition of the mucous membrane of the uterus from the phase of proliferation caused by the follicular hormone to the secretory phase, and after fertilization - to the condition necessary for the development of a fertilized egg. Reduces excitability and contractility of the musculature of the uterus and fallopian tubes. Promotes the development of normal endometrium. Stimulates the development of the end elements of the breast and induces lactation. 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 aldosterone; in small doses increases, and in large - suppresses the production of gonadotropic hormones of the pituitary gland; reduces azotemia, increases excretion of nitrogen by the kidneys.

Pharmacokinetics:

Absorption and distribution

After oral intake is well absorbed in the gastrointestinal tract (GIT). Time to reach the maximum concentration (TCmAfter 1-3 hours, the concentration of progesterone in the blood plasma increases from 0.13 ng / ml to 4.25 ng / ml after 1 h and is 11.75 ng / ml after 2 hours. 8.37 ng / ml after 3 hours, 2 ng / ml - after 6 hours. 1.64 ng / ml - after 8 hours.

When intravaginal application is rapidly absorbed, a high concentration of progesterone in the blood plasma is observed after 1 h. TCmah - 2-6 hours. With the introduction of 100 mg twice a day, the average concentration in the blood plasma is 9.7 mg / ml for 24 hours. With the addition of more than 200 mg, the progesterone concentration corresponds to the 1 trimester of pregnancy. The connection with plasma proteins is 90%.

Metabolism and excretion

Metabolized in the liver with the enzyme system CYP2C19. The main metabolites are 20-alpha-hydroxy-delta-4-alpha-pregnanolone and 5-alpha-dihydroprogesterone. It is excreted by the kidneys - 50-60%.

Indications:

Progesterone deficiency in women: For oral administration:

- infertility due to luteal insufficiency:

- premenstrual syndrome; fibrocystic mastopathy:

- disorders of the menstrual cycle due to a violation of ovulation or anovulation:

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

For intravaginal application:

- support of the luteal phase in the programs of assisted reproductive technologies:

- support of the luteal phase in the spontaneous or induced menstrual cycle infertility due to luteal insufficiency;

- threatening abortion or prevention of habitual abortion due to progesterone deficiency:

- prevention (prevention) of preterm delivery in women at risk (with shortening of the cervix and / or the presence of anamnestic data of premature birth and / or premature rupture of the membranes);

- premature menopause;

- HRT in combination with estrogen-containing drugs:

- HRT in case of progesterone deficiency with non-functioning (absent) ovaries (egg donation).

Contraindications:

- Hypersensitivity to progesterone or any of the excipients of the drug;

- deep vein thrombosis. thrombophlebitis;

- thromboembolic disorders (thromboembolism pulmonary artery, myocardial infarction, stroke), intracranial hemorrhage or the presence of these conditions / diseases in the anamnesis;

- severe violations of liver function; severe liver disease (including cholestatic jaundice, hepatitis, Dubin-Johnson syndrome, rotor, malignant liver tumors) at present or in the anamnesis;

- bleeding from the vagina of unknown origin;

- incomplete abortion;

- porphyria;

- established or suspected malignant neoplasms of the mammary glands or genitals;

- children under 18 years of age (efficacy and safety not established);

- the period of breastfeeding.

Carefully:Diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine. depression, hyperlipoproteinemia. violations of liver function of light and moderate severity, photosensitivity. The drug should be used with caution in the II and III trimesters of pregnancy.

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 use of the drug is contraindicated during breastfeeding.

Dosing and Administration:

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

Oral:

The drug is recommended to be taken orally in the evening before going to bed (it is not recommended to take before, after or during meals).

With premenstrual syndrome, fibrocystic mastopathy, violation of the menstrual cycle due to a violation of ovulation or anovulation, premenopause - 200 or 400 mg / day for 10 days (from 17 to 26 day of the cycle).

With HRT in perimenopause against the background of taking estrogen-containing drugs - 200 mg / day for 12 days.

With HRT in postmenopausal women in a continuous mode against the background of taking estrogens Iprogine is used in a dose of 100-200 mg from the first day of taking estrogen-containing drugs. The dose is selected individually.

Intravaginal:

Support of the luteal phase during the in vitro fertilization: it is recommended to use from 200 to 600 mg per day, starting from the day of injection of chorionic gonadotropin during the first and second trimester of pregnancy.

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

In cases of threatening abortion or in order to prevent habitual abortion, Progesterone deficiency: 200-400 mg per day in 2 divided doses every day in the first and second trimesters of pregnancy.

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

Complete absence of progesterone the women with non-functioning (absent) ovaries (donation of eggs): on the background of estrogen therapy on 100 mg per day on the 13th and 14th days of the cycle, then 100 mg twice a day from the 15th to the 25th day of the cycle, from the 26th day, and in In case of pregnancy, the dose increases by 100 mg per day every week, reaching a maximum of 600 mg per day, divided into 3 doses. This dose can be applied for 60 days.

Side effects:

The undesirable reactions 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:> 1/10000, <1/1000; very rarely: <1/10000.

System of organs	Adverse events
System of organs	often	infrequently	rarely	rarely
Violations of the genitals and mammary gland	Menstrual irregularities Amenorrhea Acyclic bleeding	Mammalgia
Disorders from the psyche				Depression
Disturbances from the nervous system	Headache	Drowsiness Transient dizziness
Disorders from the gastrointestinal tract	Bloating	Vomiting Diarrhea Constipation	Nausea
Disturbances from the liver and bile ducts		Cholestatic jaundice
Immune system disorders				Hives
Disturbances from the skin and subcutaneous tissues		Itching Acne		Chloasma

Drowsiness, transient dizziness are possible, as a rule, 1-3 hours after taking the drug. These undesirable reactions can be reduced by lowering the dose, applying the drug before bed or switching to the vaginal route of administration.

These undesirable reactions 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 course of treatment begins 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 gestagens.

Postmarketing application

In the postmarketing application, the following adverse events were noted with the oral administration of progesterone: insomnia: premenstrual syndrome; tension in the mammary glands; vaginal discharge; pain in the joints; hyperthermia: increased sweating at night: fluid retention: change in body weight: acute pancreatitis: alopecia, hirsutism; changes in libido; thrombosis and thromboembolic complications (with HRT in combination with estrogen-containing drugs): increase blood pressure.

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

With vaginal application

Individual cases of development of local intolerance reactions of the drug components (in particular, soy lecithin) have been reported as 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), ns were noted.

Overdose:Symptoms: drowsiness dizziness, euphoria, shortening 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 too low concentrations of estradiol.

Treatment:

in case of occurrence of drowsiness or dizziness it is necessary to reduce the daily dose or to prescribe the drug before going to sleep 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 perimenopause and with HRT in postmenopause it is necessary to make sure that the concentration of estradiol is optimal.

In case of an overdose, if necessary, symptomatic treatment is performed.

Interaction:

When administered orally

Strengthens the action of diuretics, hypotensive drugs. immunosuppressants, anticoagulants. Reduces the lactogenic effect of oxytocin.

Simultaneous use with induction drugs of microsomal liver enzymes CYP3A4, such as barbiturates, antiepileptic drugs (phenytoin), rifampicin, phenylbutazone, spironolactone, griseofulvin, is accompanied by an acceleration of the metabolism of progesterone in the liver.

Simultaneous intake of progesterone with certain antibiotics (penicillins, tetracyclines) can lead to a decrease in its effectiveness due to the violation of intestinal hepatic recirculation of sex hormones due to changes in the intestinal microflora.

The degree of expression of these interactions can vary in different patients, so the prognosis of clinical effects of these interactions is difficult.

Ketoconazole may increase the bioavailability of progesterone.

Progesterone can increase the concentration of ketoconazole and cyclosporine.

Progesterone may decrease the effectiveness of bromocriptine.

Progesterone can cause a decrease in glucose tolerance,as a result - increase the need for insulin or other hypoglycemic drugs in patients with diabetes mellitus.

Bioavailability of progesterone can be reduced in smoking patients and with excessive consumption of alcohol.

With intravaginal application

The interaction of progesterone with other drugs for intravaginal application was not evaluated. It should avoid the simultaneous use of other drugs used intravaginally, to prevent disruption of the release and absorption of progesterone.

Special instructions:The drug Iprozhin can not be used for the purpose of contraception.

The drug should not be taken with the poor, since eating increases the bioavailability of progesterone.

The use of Iprozhin after the first trimester of pregnancy can cause the development of cholestasis. Take the drug with caution in patients with diseases and conditions that are may be aggravated by fluid retention (arterial hypertension, cardiovascular diseases, chronic renal failure, epilepsy, migraine, bronchial asthma); the patients with diabetes mellitus; violations of liver function of mild and moderate severity; photosensitivity.

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

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.

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

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 Do not use the drug until the cause is determined, including a histological examination of the endometrium.

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. The use of Iprozhin in these cases can only lead to a delay in the rejection and evacuation of a non-viable fetal egg. The use of Iprozhin in order to prevent habitual abortion is justified only in cases of progesterone insufficiency.

When carrying out HRT with estrogen-containing drugs during the period of perimenopause, the use of Iprozhin is recommended for at least 12 days of the menstrual cycle.

In the continuous mode of HRT in postmenopause, the use of the drug is recommended from the first day of taking estrogen-containing drugs.

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

Because of the risk of developing thromboembolic complications, the drug should be discontinued in case of: visual disorders such as loss of vision, exophthalmos, double vision, vascular lesions of the retina: migraines; venous thromboembolism or thrombotic complications, regardless of their location.

If there is a history of thrombophlebitis, the patient should be carefully monitored. When using Iprozhin with estrogen containing preparations, it is necessary to refer to instructions for their use regarding the risks of venous thromboembolism. Clinical trial results Women Health Initiative Study (WHI) indicate a slight increase in the risk of breast cancer for a long, more than 5 years. the joint use of estrogen-containing drugs with gestagens. With regard to the use of estrogen-containing drugs in combination with progesterone in HRT, there is no evidence of an increased risk of breast cancer.

Results of the study WHI 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 behavior. If there is a clinical indication, a breast examination and gynecological examination should be performed.

If there is a history of chloasma or a tendency to develop it, patients are advised to avoid UV irradiation.

The use of progesterone may affect the results of some laboratory tests, including indicators of liver function, thyroid function; coagulation parameters; concentration of pregnanediol.

Effect on the ability to drive transp. cf. and fur:When taking orally, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Capsules, 100 mg, 200 mg.

Packaging:

Dosage of 100 mg:

For 15 capsules in a blister (PVC / PVDC / Alum.) For 2 or 6 blisters together with the instructions for use are placed in a cardboard box.

Dosage of 200 mg:

15 capsules per blister (PVC / PVDC / Alum.) For 1 or 3 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000284

Date of registration:17.02.2011 / 18.05.2016

Expiration Date:Unlimited

The owner of the registration certificate:Italfarmaco SpAItalfarmaco SpA Italy

Manufacturer: & nbsp

CATALENT FRANCE BEINHEIM, S.A. France

Representation: & nbspITF, LLCITF, LLCRussia

Information update date: & nbsp28.11.2017

Illustrated instructions

Instructions

Ipergine (Iprozhin)