Progesterone

Pharmacological properties

progesterone is a corpus luteum hormone. the drug causes the transformation of the proliferation phase of the uterine mucosa into the secretory phase, which is necessary for the normal implantation of a fertilized egg, and after fertilization it contributes to its development. progesterone also reduces the excitability and contractility of the muscles of the uterus and fallopian tubes, ensures the preservation of pregnancy; stimulates the development of mammary glands. in low doses it stimulates, and in high - inhibits the secretion of gonadotropic hormones. inhibits the effect of aldosterone, which leads to increased secretion of sodium and chlorine in the urine. has a catabolic and immunosuppressive effect.

Pharmacokinetics After i / m or s / c injection, it is rapidly and well absorbed at the injection site. Progesterone metabolism occurs in the liver, a small part of it accumulates in the subcutaneous fat. The main product of the conversion of progesterone is biologically active pregnanediol. Pregnandiol after conjugation with glucuronic acid enters the bloodstream from the liver, and then into the urine. A smaller portion of progesterone is converted to pregnanolol and pregnandion. All metabolites of progesterone excreted in the urine are inactive.

Indications

Amenorrhea, dysfunctional (anovulatory) uterine bleeding; endocrine infertility, including due to insufficiency of the corpus luteum; miscarriage, oligomenorrhea, algomenorrhea (against the background of hypogonadism).

Application

The drug is administered in / m or s / c. for dysfunctional uterine bleeding, 5–15 mg daily is prescribed for 6–8 days. if curettage of the uterine mucosa was previously cured, injections begin after 18–20 days. if curettage is not possible, inject it even during bleeding. when ingesta is used during bleeding, its temporary (3-5 days) increase may occur, which is why patients with moderate to severe anemia are recommended to conduct a blood transfusion (200–250 ml). when stopping bleeding, do not interrupt treatment earlier than 6 days. if the bleeding did not stop after 6-8 days of treatment, further administration of the drug ingest is impractical.

With hypogonadism and amenorrhea, treatment begins with the use of estrogen drugs in order to achieve sufficient proliferation of the endometrium. Immediately after the end of estrogen administration, Ingest is prescribed 5 mg daily or 10 mg every other day for 6–8 days.

With algodismenorrhea, treatment with the drug Ingest begins 6-8 days before menstruation. The drug is administered daily at 5-10 mg for 6-8 days. The course of treatment can be repeated several times.

To prevent and eliminate the threat of miscarriage, 10–25 mg of Ingesta is administered daily or every other day until the symptoms of the threat of miscarriage disappear completely. With the usual miscarriage, the drug is administered until the 4th month of pregnancy.

The highest single and daily dose for i / m administration is 25 mg (2.5 ml of 1% solution or 1 ml of 2.5% solution).

Contraindications

Liver diseases, impaired liver function, hepatitis, liver and kidney failure, cholestatic jaundice during pregnancy (history), benign hyperbilirubinemia, neoplasms of the mammary gland and genital organs, tachycardia, tendency to thrombosis, active venous or arterial thromboembolism, severe or severe a history of these conditions; nervous disorders with symptoms of depression; porphyria; pregnancy after the 36th week; an ectopic pregnancy or a history of missed pregnancy; vaginal bleeding of unknown origin, condition after abortion; hypersensitivity to the components of the drug.

Side effects

The drug is usually well tolerated, in isolated cases, the manifestations of such adverse reactions are possible:

from the cardiovascular system: tachycardia, circulatory disorders, increased blood pressure, venous thromboembolism;

from the nervous system: headache, dizziness, drowsiness, insomnia, depression;

from the reproductive system and mammary glands: engorgement, increased sensitivity and pain of the mammary glands, disorders of the external genitalia, such as burning, dryness, genital itching, changes in vaginal discharge, bleeding, vaginal mycosis, premenstrual syndrome, menstrual irregularities, acyclic spotting, amenorrhea, oligomenorrhea, hirsutism, decreased libido, uterine cramps;

from the digestive tract: bloating, abdominal pain, nausea, vomiting, constipation, diarrhea;

endocrine disorders: impaired glucose tolerance;

from the respiratory system: shortness of breath;

from the hepatobiliary system: impaired liver function and changes in functional liver samples, cholestatic jaundice;

metabolic and alimentary disorders: increase or decrease in body weight, edema, albuminuria;

on the part of the skin and soft tissues: allergic manifestations on the skin, erythema multiforme, pruritus, urticaria, rash, acne, chloasma, alopecia, hirsutism;

general disorders and condition at the injection site: increased fatigue, fever, hypersensitivity reactions, including anaphylactic reactions, pain and swelling at the injection site;

laboratory parameters: changes in the lipid profile of blood plasma;

effect on the fetus: excess progesterone can lead to virilization of the female fetus (to the uncertainty of gender).

special instructions

Caution should be used in diseases of the cardiovascular system, ar, chronic renal failure, diabetes mellitus, BA, epilepsy, migraine, depression, hyperlipoproteinemia.

Ingest should also be used with caution in patients with a history of mental disorders, the drug must be discontinued when the first signs of depression appear.

In patients with diabetes, it is necessary to carefully monitor the level of glucose in the blood.

When using Ingesta, it is necessary to be attentive to the early signs and symptoms of thromboembolism, and if they occur, drug therapy should be discontinued.

Since steroid hormone metabolism is carried out in the liver, Ingest should not be used in patients with impaired liver function.

With prolonged use of Injesta in high doses, a cessation of menstruation is possible.

The drug should not be used for bleeding from the genital tract, the cause of which has not been established, and in patients with a history of peripheral arterial disease. During treatment, regular examinations are recommended, the frequency and volume of which are determined individually.

In the presence of any progesterone-dependent tumor, such as meningioma, in the history and / or its progression during pregnancy or previous hormonal therapy, patients should be closely monitored by a doctor.

Use during pregnancy or lactation. During pregnancy, the drug is used only for the prevention and treatment of the threat of miscarriage. After the 36th week of pregnancy, the use of the drug is contraindicated. Do not use the drug in women planning a pregnancy in the near future. The risk of congenital anomalies, including sexual abnormalities in children of both sexes, associated with the action of exogenous progesterone during pregnancy, has not been fully established. Ingesta passes into breast milk, therefore, the drug should not be used during lactation.

Children. The drug is not used in pediatric practice.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. The drug may cause dizziness and drowsiness. During the treatment period, it is necessary to refrain from driving vehicles, from potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Interactions

Ingesta weakens the effect of drugs that stimulate the reduction of myometrium (oxytocin, pituitrin), anabolic steroids (nandrolone, methandienone), gonadotropic hormones of the pituitary gland. when interacting with oxytocin, the severity of the lactogenic effect decreases. enhances the action of diuretics, antihypertensive drugs, immunosuppressants, bromocriptine and systemic coagulants. reduces the effectiveness of anticoagulants. the effect of ingesta is reduced with the combined use of barbiturates. changes the effects of hypoglycemic agents. with simultaneous use with inducers of liver enzymes, an increase or decrease in the concentration of ingesta in the blood plasma is possible.

Overdose

When exceeding the recommended doses of the drug, side effects are more likely to occur, described in the corresponding section. if side effects occur, treatment with the drug should be discontinued, and after their disappearance, resume at low doses. if necessary, carry out symptomatic treatment.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° c.