Progesterone - instructions for use, dose, side effects, contraindications

Progesterone - the hormone of the yellow body, has a gestagenic effect. By binding to receptors on the surface of cells of target organs, it penetrates into the nucleus, where, by activating deoxyribonucleic acid, it stimulates the synthesis of ribonucleic acid. Promotes the transition of the mucous membrane of the uterus from the proliferation phase, caused by the follicular hormone, into the secretory,and after fertilization creates the necessary conditions for the implantation and development of a fertilized egg. Reduces excitability and contractility of the musculature of the uterus and fallopian tubes. Stimulates the development of the end elements of the breast and induces lactation. Promotes the development of normal endometrium.

Stimulating proteinolipase, increases fat stores, increases the utilization of glucose, increases the concentration of basal and stimulated insulin, promotes the accumulation of glycogen in the liver, increases the production of aldosterone; in small doses accelerates, and in large - suppresses the production of gonadotropic hormones of the pituitary gland; reduces azotemia, increases excretion of nitrogen by the kidneys.

Pharmacokinetics:

Absorption

Quickly and almost completely absorbed after intramuscular injection (in / m). The maximum concentration in the blood plasma after the / m administration of 10 mg of progesterone is reached for approximately 8 hours and remains above the basal level for about 24 hours.

Distribution

Progesterone actively binds to blood plasma proteins, mainly with albumin (50-54%) and corticosteroid-binding globulin (43-48%).

Metabolism

Metabolised in the liver with the formation of metabolites - pregnanodiol and pregnanolone, which are conjugated with glucuronic and sulfuric acids. Isozyme participates in metabolism CYP2C19.

Excretion

Metabolites of progesterone are excreted by the kidneys - 50-60%, through the intestine - more than 10%. The amount of metabolites excreted by the kidneys varies depending on the phase of the yellow body. Half-life is a few minutes.

Indications:

Infertility due to deficiency of the yellow body.

Contraindications:

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

- known or suspected neoplasms of the mammary gland or genitals;

- severe impairment of liver function or severe liver disease, including malignant liver tumors, currently or in history;

- pregnancy (possible only intravaginal application of progesterone);

- the period of breastfeeding;

- idiopathic jaundice, pruritus or herpes during an earlier pregnancy;

- thromboembolic disorders (pulmonary embolism, myocardial infarction, stroke), intracranial hemorrhage or the presence of datastates / diseases in the history;

- deep vein thrombosis, retinal vascular thrombosis; thrombophlebitis now or in history;

- bleeding from the vagina of unknown origin;

- incomplete abortion or miscarriage;

- porphyria;

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

Carefully:

Diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression, hyperlipoproteinemia, impaired hepatic and mild liver function; photosensitivity.

Pregnancy and lactation:

In pregnancy progesterone can be used only intravaginally. In this dosage form, the use of the drug during pregnancy is contraindicated. Progesterone penetrates into breast milk, so the use of the drug is contraindicated in the period of breastfeeding.

Dosing and Administration:

The drug is administered intramuscularly.

Infertility due to deficiency of the yellow body - 12.5 mg / day for 2 weeks from the moment of ovulation.

Use in special clinical cases

Elderly age

Efficacy and safety in elderly patients (over 65 years) is not established. There are no indications for the use of the drug in the elderly.

Children

Efficacy and safety in children under the age of 18 years is not established.

Indications for use of the drug in children and adolescents are absent.

Impaired liver function

The use of the drug in patients with severe impairment of liver function is contraindicated. In patients with impaired liver function of mild and moderate severity, the drug is used with caution.

Impaired renal function

In patients with impaired renal function, the drug is used with caution.

Side effects:

Immune system disorders: skin itching, rash, hives, anaphylactoid reactions.

Disorders from the endocrine system: hirsutism.

Disorders from the metabolism and nutrition: swelling, increased or decreased body weight, decreased appetite.

Disorders from the psyche: apathy, dysphoria, depression, mood lability.

Disturbances from the nervous system: headache, dizziness, drowsiness, insomnia, asthenia, optic neuritis.

Disturbances on the part of the organ of sight: impaired vision.

Vascular disorders: increased blood pressure, thromboembolism (including pulmonary arteries), thrombosis of cerebral vessels or veins of the retina, thrombophlebitis, hemorrhagic rash.

Disorders from the gastrointestinal tract: nausea, vomiting, bloating, constipation, diarrhea, abdominal pain.

Disturbances from the liver and bile ducts: cholecystitis, cholestatic jaundice, cholestatic hepatitis.

Violations of the genitals and mammary gland: a change in the libido; "breakthrough" bleeding; "smearing" spotting; amenorrhea; shortening of the menstrual cycle; cervical erosion; spasm of the muscles of the uterus, vaginal discharge, itching and discomfort in the vagina, vulvovaginitis, ovarian hyperstimulation syndrome, "hot flashes", malignant diseases of the breast; change in the viscosity of the secretion of the cervix; premenstrual syndrome; galactorrhea; increase, pain and tension of the mammary glands.

Disturbances from musculoskeletal and connective tissue: backache.

Disturbances from the skin and subcutaneous tissues: acne, alopecia, erythema multiforme, nodal erythema.

Disorders from the kidneys and urinary tract: cystitis.

General disorders and disorders at the site of administration: hyperthermia; hyperemia, irritation and / or pain at the injection site, hematoma, compaction, edema and itching at the injection site, general malaise, fatigue.

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: These overdose manifestations can be reduced by reducing the dose, restoring high estrogenation, or switching to the vaginal route of administration. If necessary, perform symptomatic treatment.

Interaction:

Progesterone enhances the action of diuretics, hypotensive drugs, immunosuppressants, anticoagulants; reduces the lactogenic effect of oxytocin.

Simultaneous application 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.

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 can 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, thereby increasing 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.

Special instructions:

Prior to the use of the drug Progesterone It is necessary to conduct a medical examination, including a survey of the mammary glands and pelvic organs and a Pap smear test.

Because of the risk of developing thromboembolic complications, the drug should be discontinued in the event of: visual disturbances such as loss of vision, double vision,vascular lesions of the retina; migraine; arterial or venous thromboembolism, thrombophlebitis, thrombosis, regardless of localization.

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

A drug Progesterone apply with caution in patients with diseases and conditions that can worsen with fluid retention (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.

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.

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

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

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

The crystals fall out. In the case of crystals falling out, the ampoule should be heated in a boiling water bath with shaking until the crystals dissolve completely. If the solution becomes clear, and when cooled to 36-38 ° C, the crystals do not fall again, the drug is usable.

Effect on the ability to drive transp. cf. and fur:

During treatment, care must be taken when managing vehicles, mechanisms or engaging in activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intramuscular administration [oily], 25 mg / ml.

Packaging:

1 ml per ampoule of colorless neutral glass (type I) with a colored break point. For each ampoule a label is applied or labeled with a quick-fixing paint.

10 ampoules per blister of PVC, 1 blister each, along with instructions for use in a pack of cardboard.

Storage conditions:

In the dark 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-003749

Date of registration:26.07.2016

Expiration Date:26.07.2021

The owner of the registration certificate:ALVILS, LTD. ALVILS, LTD. Russia

Manufacturer: & nbsp

ANHUI CHENGSHI MANUFACTURE MEDICINE, Co. Ltd. China

Representation: & nbspAlvils, OOOAlvils, OOO

Information update date: & nbsp21.08.2016

Illustrated instructions

Instructions

Progesterone (Progesterone)