

Oxyprogesterone is an analogue of the hormone of the corpus luteum (progesterone). Chemically different from progesterone in that in position 17 contains a residue of caproic acid. Being an ester of hydroxyprogesterone, is slower progesterone is metabolized (has a longer effect). After a single intramuscular injection of the oil solution, its action lasts from 7 to 14 days. Biological properties similar to progesterone. By binding to receptors on the surface of target organ cells, it penetrates into the nucleus, where, by activating DNA, it stimulates RNA synthesis. It promotes the transition of the uterine mucosa from the proliferation phase caused by follicular hormone to the secretory one, 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 end elements of the mammary gland.
Pharmacokinetics
Quickly and almost completely absorbed after intramuscular administration.
Metabolized in the liver to form conjugates with glucuronic and sulfuric acids.
T1 / 2 is 5 min. Excreted by the kidneys - 50-60%, with bile - more than 10%. The number of metabolites excreted by the kidneys varies depending on the phase of the corpus luteum
Conditions associated with insufficiency of the corpus luteum: threatening and begun miscarriage (prevention and treatment), amenorrhea (primary and secondary), dysfunctional uterine bleeding.
1 ml of solution contains:
Active ingredient: hydroxyprogesterone capronate;
Excipients: medical benzyl benzoate - 300 μl, olive oil - up to 1 ml.
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Intramuscularly.
For the purpose of prevention and treatment of threatened and begun miscarriage injected at 0.125-0.25 g (1-2 ml of a 12.5% solution) once a week. Apply only in the first half of pregnancy.
With amenorrhea (primary, secondary) is prescribed immediately after discontinuation of the use of estrogen drugs of 0.25 g, once, or in 2 administrations.
For the treatment of dysfunctional uterine bleedingthe drug is less convenient than progesterone, because its effect comes slowly, but it can be used to normalize the cycle: 0.0625-0.125 g (0.5-1 ml of 12.5% solution) on days 20-22 of the cycle.
From the nervous system: drowsiness, headache, depression, apathy, dysphoria.
From the digestive system: cholestatic hepatitis, nausea, vomiting, loss of appetite, calculous cholecystitis.
From the genitourinary system: decreased libido, reduced menstrual cycle, intermediate bleeding.
From the senses: visual impairment.
From the CCC: increased blood pressure, edema, thromboembolism (including the pulmonary artery and brain vessels), thrombophlebitis, retinal vein thrombosis.
On the part of the endocrine system: galactorrhea, alopecia, weight gain, increase, pain and exertion of the mammary glands; hirsutism. Allergic reactions.
Local reactions: soreness at the injection site.
Carefully: in diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression; hyperlipoproteinemia.
Treatment is often combined with the appointment of estrogen drugs or carried out directly after estrogen therapy.
Weakens the effect of drugs that stimulate the reduction of myometrium (oxytocin), anabolic steroids (nandrolone), pituitary gonadotropic hormones.
Enhances the action of diuretics, antihypertensive drugs, immunosuppressants, bromocriptine.
Reduces the effectiveness of anticoagulants.
The progestogenic activity of the drug is reduced by inductors of microsomal oxidation (barbiturates, hydantoins, riffshitsin, etc.).
The drug is not used during pregnancy. In the event of pregnancy on the background of the drug should immediately discontinue treatment; data on the need for abortion is not. The drug is contraindicated in the second half of pregnancy and during breastfeeding.
In case of precipitation of crystals or crystallization of the entire contents of the ampoule, the ampoule should be heated in a boiling water bath with shaking. If the crystals disappear and the solution becomes transparent, and when cooled to 36-38 ° C, the crystals will not fall out again, the solution is suitable for use.
The purpose of the drug should be made only by the attending physician, under his control after an accurate diagnosis.
When treating amenorrhea in children, verification of the diagnosis of amenorrhea is primarily necessary.
Treatment before puberty should be aimed at stimulating growth. After 15-17 years old, estrogen and gestagen replacement therapy can be performed, which causes cyclic uterine bleeding!
Influence on ability to steer vehicles, mechanisms
Care should be taken when driving and other potentially hazardous activities that require increased concentration and psychomotor reactions, as the drug can cause side effects that can affect these abilities.
Symptoms: depression of the central nervous system, drowsiness, tachycardia; high blood pressure, weakness, sweating.
Treatment: discontinuation of therapy until symptoms disappear, followed by the administration of lower doses. If necessary, carry out symptomatic treatment.
Studies and clinical trials of Hydroxyprogesterone Caproate (Click to expand)