Ingesta

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT INJESTA® (INJESTA®)

Composition:

Active ingredient: progesterone;

1 ml of solution contains 10 mg or 25 mg of progesterone calculated as 100 % substance;

Excipients: 2.5 % solution – benzyl benzoate, ethyloleate; 1 % solution – ethyloleate.

Pharmaceutical form. Injection solution.

Main physicochemical properties: oily liquid of light green or light yellow color with a specific odor.

Pharmacotherapeutic group.

Progestogens. ATC code G03D A04.

Pharmacological Properties.

Pharmacodynamics.

Progesterone is a hormone of the corpus luteum. The drug induces transformation of the proliferative phase of the endometrium into the secretory phase, which is necessary for normal implantation of a fertilized ovum; after fertilization, it supports its development. Progesterone also reduces excitability and contractility of the uterine and fallopian tube musculature, thereby maintaining pregnancy, and stimulates mammary gland development. In small doses it stimulates, while in large doses it suppresses, gonadotropic hormone secretion. It inhibits the action of aldosterone, resulting in enhanced urinary excretion of sodium and chloride. It exerts catabolic and immunosuppressive effects.

Pharmacokinetics.

After intramuscular or subcutaneous injection, it is rapidly and well absorbed from the site of administration. Progesterone metabolism occurs in the liver, with a minor portion accumulating in subcutaneous adipose tissue. The main metabolic product is biologically active pregnandiol. Pregnanediol, after conjugation with glucuronic acid, leaves the liver into the blood and is subsequently excreted in the urine. A smaller portion of progesterone is converted into pregnanolone and pregnandione. All urinary metabolites of progesterone are inactive.

Clinical characteristics.

Indications.

Amenorrhea, dysfunctional (anovulatory) uterine bleeding; endocrine infertility, including that caused by luteal insufficiency; habitual abortion, oligomenorrhea, algodysmenorrhea (in the context of hypogonadism).

Contraindications.

Liver diseases, impaired liver function, hepatitis, hepatic and renal insufficiency, cholestatic jaundice during pregnancy (in medical history), benign hyperbilirubinemia; neoplasms of the breast and genital organs; tachycardia, predisposition to thrombosis, active venous or arterial thromboembolism, severe thrombophlebitis or these conditions in medical history; neuropsychiatric disorders with depressive symptoms; porphyria; pregnancy after 36 weeks; ectopic pregnancy or missed abortion in medical history; vaginal bleeding of unknown origin, condition after abortion; hypersensitivity to the components of the drug.

Interaction with other medicinal products and other forms of interactions.

Inzhesta® reduces the effect of drugs stimulating myometrial contractions (oxytocin, pituitrin), anabolic steroids (retabolil, nerobol), and pituitary gonadotropic hormones. When combined with oxytocin, the lactogenic effect is diminished. It enhances the action of diuretics, antihypertensive agents, immunosuppressants, bromocriptine, and systemic coagulants. It reduces the effectiveness of anticoagulants. The effect of Inzhesta® is decreased when used concomitantly with barbiturates. It alters the effects of hypoglycemic agents. When used simultaneously with hepatic enzyme inducers, plasma concentrations of Inzhesta® may either increase or decrease.

Special precautions for use.

The drug should be used with caution in patients with cardiovascular disorders, arterial hypertension, chronic renal insufficiency, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression, and hyperlipoproteinemia.

Injesta® should also be used with caution in patients with a history of psychiatric disorders. The drug must be discontinued at the first signs of depression.

In patients with diabetes mellitus, blood glucose levels should be carefully monitored.

When using Injesta®, attention should be paid to early signs and symptoms of thromboembolism. If such symptoms occur, treatment with the drug must be discontinued.

Since metabolism of steroid hormones occurs in the liver, Injesta® should not be administered to patients with impaired liver function.

Prolonged use of high doses of Injesta® may lead to cessation of menstruation.

The drug should not be used in patients with undiagnosed vaginal bleeding or in those with a history of peripheral arterial disease. During treatment, regular check-ups are recommended; their frequency and extent are determined individually.

Patients with a history of any progesterone-dependent tumor, such as meningioma, and/or its progression during pregnancy or previous hormonal therapy should remain under close medical supervision.

Use during pregnancy or breastfeeding.

The drug should be used during pregnancy only for the prevention and treatment of threatened miscarriage. Use of the drug after the 36th week of pregnancy is contraindicated. The drug should not be used in women who intend to become pregnant in the near future. The risk of congenital anomalies, including genital anomalies in children of both sexes, associated with the action of exogenous progesterone during pregnancy, has not been fully established. Injesta® passes into breast milk; therefore, the drug should not be used during breastfeeding.

Ability to affect reaction speed when driving vehicles or operating machinery.

The drug may cause dizziness and drowsiness. During treatment, patients should refrain from driving vehicles and from engaging in potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Administration and Dosage.

The drug should be administered intramuscularly or subcutaneously.
For dysfunctional uterine bleeding, the drug should be used at a dose of 5–15 mg daily for 6–8 days. If curettage of the endometrium has been previously performed, injections should be started 18–20 days after the procedure. If curettage cannot be performed, administer Inzhesta® even during bleeding. When Inzhesta® is used during bleeding, a temporary increase in bleeding (for 3–5 days) may occur; therefore, patients with moderate or severe anemia should receive a blood transfusion (200–250 ml) prior to treatment. Even if bleeding has stopped, treatment should not be discontinued earlier than after 6 days. If bleeding does not cease after 6–8 days of treatment, further administration of Inzhesta® is not advisable.

For hypogonadism and amenorrhea, treatment should begin with the use of estrogenic agents to achieve sufficient endometrial proliferation. Immediately after completing estrogen therapy, administer Inzhesta® at 5 mg daily or 10 mg every other day for 6–8 days.

For algomenorrhea, treatment with Inzhesta® should begin 6–8 days before menstruation. The drug should be administered daily at 5–10 mg for 6–8 days. The treatment course may be repeated several times.

For prevention and management of threatened miscarriage, administer 10–25 mg of Inzhesta® daily or every other day until symptoms of threatened miscarriage have completely disappeared. In cases of habitual miscarriage, continue administration until the fourth month of pregnancy.

The maximum single and daily dose for adults by intramuscular injection is 25 mg (2.5 ml of a 1% solution or 1 ml of a 2.5% solution).

Children.

The drug is not indicated for use in pediatric practice.

Overdose.

When higher doses are used, adverse effects described in the relevant section occur more frequently. If adverse effects occur, treatment with the drug should be discontinued; after their disappearance, therapy may be resumed at lower doses. Symptomatic treatment should be administered if necessary.

Adverse reactions.

Progesterone is usually well tolerated. In isolated cases, the following adverse reactions may occur:

Cardiovascular system: tachycardia, circulatory disturbances, increased blood pressure, venous thromboembolism;

Nervous system: headache, dizziness, drowsiness, insomnia, depression;

Reproductive system and mammary glands: breast swelling, increased sensitivity and breast pain, disorders of the external genital organs such as burning, dryness, genital pruritus, changes in vaginal discharge, bleeding, vaginal fungal infection, premenstrual syndrome, menstrual cycle disturbances, acyclic bloody discharge, amenorrhea, oligomenorrhea, hirsutism, decreased libido, uterine spasms;

Gastrointestinal tract: abdominal distension, abdominal pain, nausea, vomiting, constipation, diarrhea, flatulence;

Endocrine disorders: impaired glucose tolerance;

Respiratory system: dyspnea;

Hepatobiliary system: liver function disorders and changes in liver function tests, cholestatic jaundice;

Metabolic and nutritional disorders: appetite changes, weight gain or weight loss, edema, albuminuria;

Skin and subcutaneous tissues: skin allergic reactions, erythema multiforme, pruritus, urticaria, skin rash, acne, chloasma, alopecia, hirsutism;

General disorders and injection site reactions: increased fatigue, weakness, fever, hypersensitivity reactions including anaphylactic reactions; fluid retention, paresthesia; injection site changes including pain and swelling;

Laboratory parameters: changes in plasma lipid profile;

Effect on the fetus: excessive amounts of progesterone may cause virilization of the female fetus (up to ambiguity of sex).

Shelf life.

For 2.5% injection solution – 3 years.

For 1% injection solution – 2 years.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

1 ml in an ampoule. 5 or 10 ampoules per pack. 5 ampoules in a blister. 1 or 2 blisters per pack.

Prescription category.

By prescription only.

Manufacturer.

JSC "Farmak".

Manufacturer's address and place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.