Instruction for use: Hydroxyprogesterone caproate (Hydroxyprogesteroni caproas)

Pharmacological group

Estrogens, gestagens; Their homologues and antagonists

Antineoplastic hormonal agents and hormone antagonists

Characteristic

Virtually nerastvorim in water, soluble in ethanol, fatty oils.

Pharmacotherapy

Analog of the hormone of the yellow body (progesterone). Chemically different from progesterone in that in position 17 contains the residue of caproic acid. Being a hydroxyprogesterone ester, it is metabolized more slowly than progesterone (it has a longer action). After a single intravenous injection of an oily solution, its effect lasts from 7 to 14 days. On biological properties similar to progesterone. Binding to receptors on the surface of cells of target organs 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 hormone, and after fertilization creates the necessary conditions for the implantation and development of a fertilized egg. Reduces the excitability and contractility of the muscles of the uterus and fallopian tubes, stimulates the development of the end elements of the breast.

Pharmacokinetics

Quickly and almost completely absorbed after sc and in / m introduction. Metabolized in the liver with the formation of conjugates with glucuronic and sulfuric acids. T1 / 2 - a few minutes. It is excreted by the kidneys - 50-60%, with bile - more than 10%. The amount of metabolites excreted by the kidneys varies depending on the phase of the yellow body.

Indication

Conditions associated with deficiency of the yellow body: threatening and started miscarriage (prevention and treatment), amenorrhea (primary and secondary), dysfunctional uterine bleeding.

Contraindications

Hepatitis, hepatic insufficiency, breast and genital cancers, propensity to thrombosis.

Carefully

Carefully. Diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes, asthma, epilepsy, migraine, depression; Hyperlipoproteinemia, ectopic pregnancy, lactation period.

Dosing

In / m (intramuscularly). To prevent and treat a threatening and started miscarriage, enter 0.125-0.25 g (1-2 ml of 12.5% solution) once a week. Applied only in the first half of pregnancy.

In amenorrhea (primary, secondary) is appointed immediately after the termination of the use of estrogenic drugs by 0.25 g, once, or in 2 injections.

For the treatment of dysfunctional uterine bleeding, the drug is less convenient than progesterone, tk. Its effect is slow, but it can be used to normalize the cycle: 0,0625-0,125 g (0,5-1 ml of 12,5% solution) on the 20-22 day of the cycle.

Side effect

From the nervous system: drowsiness, headache, depression, apathy, dysphoria.

On the part of the digestive system: cholestatic hepatitis, nausea, vomiting, decreased appetite, calculous cholecystitis.

From the genitourinary system: a decrease in libido, a reduction in the menstrual cycle, intermediate bleeding.

From the senses: a violation of vision.

From the SSS (cardiovascular system): increased blood pressure (arterial pressure), edema, thromboembolism (including pulmonary arteries and cerebral vessels), thrombophlebitis, retinal vein thrombosis.

On the part of the endocrine system: galactorrhea, alopecia, weight gain, increase, pain and tension of the mammary glands; Hirsutism.

Allergic reactions.

Local reactions: soreness in the injection site.