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

Active substanceProgesteroneProgesterone

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Dosage form: & nbspcapsules

Composition:

1 capsule contains:

Active substance:

Progesterone micronized with 100 mg or 200 mg

Excipients:

Peanut butter - 149.0 mg / 298.0 mg, soy lecithin - 1 mg / 2 mg,

capsule: gelatin - 77.7 mg / 158.9 mg, glycerol - 31.5 mg / 64.30 mg, titanium dioxide - 0.90 mg / 1.80 mg.

Description:

Soft gelatin capsules egg-shaped, white with a yellowish-brownish hue of color, containing a thick suspension of almost white.

Pharmacotherapeutic group:Gestagen

ATX: & nbsp

G.03.D.A Derivative derivatives

G.03.D.A.04 Progesterone

Pharmacodynamics:

The drug VANEL as an active substance contains gestagen progesterone, similar to natural progesterone, the hormone of the yellow body.By binding to receptors on the surface of the cells of target organs, it penetrates into the nucleus, where, by activating DNA, it 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.

Activates the growth of the secretory department of the mammary glands and induces lactation. Promotes the formation of normal endometrium.

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 in the pituitary gland; reduces azotemia, increases the release of nitrogen in the urine.

Pharmacokinetics:

Ingestion

Suction

Micronized progesterone is absorbed from the gastrointestinal tract. The concentration of progesterone in the blood plasma gradually increases during the first hour, the maximum concentration in the blood plasma (Cmah) is noted 1-3 hours after admission.The concentration of progesterone in the blood plasma increases from 0.13 ng / ml to 4.25 ng / ml after 1 hour, to 11.75 / ml after 2 hours and is 8.37 ng / ml after 3 hours, 2 ng / ml through 6 h and 1.64 ng / ml 8 hours after administration.

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 by the kidneys in the form of metabolites, 95% of them are glucuron-conjugated metabolites, mainly 3-alpha, 5-beta-pregnanediol (pregnagnion). These metabolites, which are determined in the blood plasma and in the urine are similar to substances formed during the physiological secretion of the yellow body.

With vaginal administration

Suction

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

Metabolism

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

Excretion

It is excreted by the kidneys in the form of metabolites, the main part is 3-alpha, 5-beta-preggnadiol (pregnagnion). The ego is confirmed by a constant increase in its concentration (Cmah 142 ng / ml after 6 hours).

Indications:

Progesterone deficiency in women:

For oral administration:

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

- infertility due to luteal insufficiency;

- premenstrual syndrome;

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

- fibrocystic mastopathy;

- period of menopausal transition;

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

For intravaginal application:

- MGT in case of progesterone deficiency with non-functioning (absent) ovaries (donation of eggs);

- 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);

- 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;

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

- infertility due to luteal insufficiency;

- threatening abortion or prevention of habitual abortion due to insufficient progesterone.

Contraindications:

Hypersensitivity to progesterone or any of the excipients of the drug; deep vein thrombosis; thrombophlebitis; thromboembolic disorders (thromboembolism of the pulmonary artery, myocardial infarction, stroke); intracranial hemorrhage or the presence of these conditions / diseases in the anamnesis; congenital or acquired predisposition to arterial or venous thrombosis; bleeding from the genital tract of unknown origin; incomplete abortion; porphyria; established or suspected malignant neoplasms of the mammary gland and genital organs; severe liver disease (including cholestatic jaundice, hepatitis, Dubin-Johnson syndrome, Rotor,malignant liver tumors) at present or in the anamnesis; children under 18 years of age (effectiveness 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 mild and moderate severity; photosensitivity.

The drug should be used with caution in II and III trimesters of pregnancy.

Pregnancy and lactation:

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

Progesterone penetrates into breast milk, so the 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.

Orally

The drug is taken orally after meals in the evening, washed down with water. In most cases, with progesterone deficiency, the daily dose of the drug VANEL is 200-300 mg, divided into 2 doses (200 mg in the evening and 100 mg in the morning, if necessary).

-For threatening abortion or to prevent habitual abortion due to progesterone deficiency: 200-600 mg daily in the I and II trimesters of pregnancy. Further use of the drug VANEL is possible on the prescription of the attending physician based on the evaluation of the clinical data of the pregnant woman.

-If the luteal phase is inadequate (premenstrual syndrome, fibro-cystic mastopathy, dysmenorrhea, menopausal transition period) the daily dose of the drug VANEL is 200 or 400 mg, taken within 10 days (usually from the 17th to the 26th day of the cycle).

-When MGT in perimenopause against the background of taking estrogen, the drug VANEL is used at 200 mg per day for 12 days.

-In post-menopausal MGT in continuous mode, the drug VANEL is used in a dose of 100-200 mg from the first day of taking estrogen-containing drugs. The dose is selected individually.

Intravaginally

Capsules are injected deep into the vagina.

-Warning (prevention) of premature birth in women at risk (with shortening of the cervix 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 the 22nd to the 34th week of pregnancy.

Complete absence of progesterone in women with non-functioning ovaries (ovaries not present) (donation of oocytes): against the background of estrogen therapy at 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 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.

-Support of the luteal phase during the in vitro fertilization cycle: it is recommended to take 200 to 600 mg per day, starting from the day of injection of the chorionic gonadotropin during the first and second trimester of pregnancy. -Support luteal phase in spontaneous or induced menstrual cycle, infertility, associated with a violation 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 pregnancy diagnosis treatment should be continued.

- Threatening abortion or prevention of habitual abortion due to lack of progesterone: 200-400 mg per day in 2 divided doses daily in the first and second trimesters of pregnancy.

Side effects:

The following undesirable phenomena noted with the oral administration of the drug are distributed according to the frequency of occurrence according to the following classification: often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely ≥1 / 10000, <1/1000), very rarely (<1/10000).

Violations of the genitals and breast:

Often: disorders of the menstrual cycle, amenorrhea, acyclic bleeding;

Not often: mastodonia.

Disorders from the psyche:

Very rarely: depression.

Impaired nervous system:

Often: headache;

Infrequent: drowsiness, transient dizziness.

Disorders from the gastrointestinal tract:

Often: bloating;

Infrequent: vomiting, diarrhea, constipation;

Rarely: nausea.

Disorders from the liver and biliary tract:

Infrequent: cholestatic jaundice.

Immune system disorders:

Very rarely: urticaria.

Disturbances from the skin of the subcutaneous tissues:

Infrequently: acne, itching;

Very rarely: chloasma.

Drowsiness, transient dizziness is possible, as a rule, 1-3 h after oral administration of 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 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 gestagens.

Application in clinical practice

When used in clinical practice, the following undesirable effects were noted when administered orally progesterone: insomnia, premenstrual syndrome, tension in the mammary gland, vaginal discharge, joint pain, hyperthermia, increased sweating at night, fluid retention, weight change, acute pancreatitis, alopecia, hirsutism, changes in libido, thrombosis and thromboembolic complications when conducting MGT in combination estrogen-containing drugs), increasing blood pressure.

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

With vaginal application reported on individual cases of development of reactions at the site of administration associated with intolerance to the components of the drug (in particular, soy lecithin), in the form of hyperemia of the vaginal mucosa, burning, itching, oily discharge. Systemic side effects with intravaginal administration of the drug at recommended doses, in particular, drowsiness or dizziness (observed with oral administration of the drug), were not noted.

Overdose:

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

In some patients, the average therapeutic dose may be excessive because of 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 - reduction of a daily dose or reception of a preparation before a dream within 10 days of a menstrual cycle;

- In case of a shortening of the menstrual cycle or "smearing" bloody discharge - to postpone the beginning of treatment on a later day of the cycle (for example, on the 19th day instead of the 17th);

- in perimenopause and with MGT 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

Progesterone enhances 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, carbamazepine), rifampicin, phenylbutazone, spironolactone, griseofulvin, causes 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 may vary in different patients, therefore the prognosis of the clinical effects of these interactions is difficult.

Ketoconazole may increase the bioavailability of progesterone.

Progesterone can increase the concentration of ketoconazole and cyclosporine in the blood; Progesterone may reduce the effectiveness of bromocriptine.

Progesterone can cause a decrease in glucose tolerance and an increase in the need for insulin and 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 is necessary to avoid simultaneous the use of other drugs used intravaginally, to prevent disruption of the release and absorption of progesterone.

Special instructions:

The drug VANEL can not be used for contraception.

The drug VANEL should not be taken with food, as eating increases the bioavailability of progesterone.

The drug VANEL should be taken with caution in patients with conditions and diseases that can worsen with fluid retention on the background of taking progesterone (arterial hypertension, cardiovascular disease, chronic renal failure, epilepsy, migraine, bronchial asthma); in patients with diabetes mellitus, with violations of liver function of mild and moderate severity, with increased photosensitivity.

It is necessary to observe patients with depression in the anamnesis, and in case of development of severe depression, the drug should be withdrawn.

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

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

The use of the drug WANEL 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 treatment process, pregnancy should be excluded.

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 be possible. In the case of acyclic bleeding, the drug should not be used until the cause is determined, including the histological examination of the endometrium.

It is recommended to avoid UV irradiation in the presence of chloasma in the anamnesis or a tendency to develop it.

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 the drug VANEL in these cases can only lead to a delay in the rejection and evacuation of the non-viable fetal egg. The use of the drug VANEL in order to prevent threatening abortion is justified only in the case of a deficiency of progesterone.

When carrying out MGT with estrogen during the period of perimenopause, the use of the drug VANEL during no less than 12 days of the menstrual cycle is recommended.

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

When carrying out MGT, the risk of developing venous thromboembolism (deep vein thrombosis or pulmonary embolism) increases; the risk of developing ischemic stroke, ischemic heart disease. Because of the risk of developing thromboembolic complications, you should stop taking the medication in case of visual disturbances such as loss of vision, exophthalmos, double vision, vascular lesions of the retina; venous thromboembolism or thrombotic complications, regardless of their location.

In the presence of thrombophlebitis in an anamnesis, the patient should be carefully monitored.

When using the drug VANEL with estrogen-containing drugs, you need to refer to instructions for their medical 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 in long-term, more than 5 years, the 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 when estrogen-containing drugs are administered with MGT in combination with progesterone.

Results of the study WMI also revealed an increased risk of developing dementia at the onset of MGT over the age of 65 years.

Before the beginning of the MGT and regularly during its conduct, a woman should be examined to identify contraindications to its conduct. 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.

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 requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Capsules of 100 mg and 200 mg.

Packaging:

15 capsules per blister of PVC / PVDC / Aluminum foil; for 1, 2 or 6 blisters together with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004425

Date of registration:22.08.2017

Expiration Date:22.08.2022

The owner of the registration certificate:Exeltys Khelskea S.L.Exeltys Khelskea S.L. Spain

Manufacturer: & nbsp

Laboratorios LEON FARMA, S.A. Spain

Representation: & nbspExeltys Khelskea S.L.Exeltys Khelskea S.L.Spain

Information update date: & nbsp12.09.2017

Illustrated instructions

Instructions

WANEL (Vanel)