Oxyprogesterone Capronate (Solution) Instructions for Use

Marketing Authorization Holder

Dalkhimpharm, JSC (Russia)

ATC Code

G03DA03 (Hydroxyprogesterone)

Active Substance

Hydroxyprogesterone caproate (Rec.INN registered by WHO)

Dosage Form

Oxyprogesterone Capronate

Oil-based solution for intramuscular injection 125 mg/1 ml: amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Oil-based solution for intramuscular injection light yellow or golden yellow in color, transparent.

Excipients: medical benzyl benzoate – 300 µl, olive oil – up to 1 ml.

1 ml – glass ampoules (5) – contour cell packs (2) – cardboard boxes.
1 ml – ampoules (10) – cardboard boxes.

Clinical-Pharmacological Group

Gestagen

Pharmacotherapeutic Group

Progestogen

Pharmacological Action

Synthetic analogue of the corpus luteum hormone (progesterone). It differs chemically from progesterone by containing a caproic acid residue at position 17. Being an ester of hydroxyprogesterone, it is metabolized more slowly than progesterone (exerts a more prolonged action). After a single intramuscular injection of an oil solution, its action lasts from 7 to 14 days. In its biological properties, it is similar to progesterone.

By binding to receptors on the surface of target organ cells, it penetrates the nucleus where, by regulating DNA transcription, it affects RNA synthesis. It promotes the transition of the uterine mucosa from the proliferation phase, induced by follicle-stimulating hormone, into the secretory phase, and after fertilization, creates the necessary conditions for the implantation and development of the fertilized egg.

It reduces the excitability and contractility of the uterine and fallopian tube muscles, and stimulates the development of alveoli (milk-forming sections) of the mammary glands.

Pharmacokinetics

Rapidly and almost completely absorbed after intramuscular injection.

Metabolized in the liver to form conjugates with glucuronic and sulfuric acids.

T_1/2 is 5 min. Excreted by the kidneys – 50-60%, with bile – more than 10%. The amount of metabolites excreted by the kidneys varies depending on the corpus luteum phase.

Indications

Conditions associated with corpus luteum insufficiency:

• Amenorrhea (primary and secondary);
• Dysfunctional uterine bleeding.

ICD codes

Dosage Regimen

Route of administration: intramuscularly. Before administration, the drug must be warmed to 30-40°C (86-104°F). For amenorrhea (primary, secondary), it is prescribed immediately after discontinuation of estrogenic medications, 250 mg once or in two injections.

For the treatment of dysfunctional uterine bleeding, the drug is less convenient than progesterone, because its effect is slow to onset; however, it can be used to normalize the cycle: 62.5-125 mg (0.5-1 ml) on days 20-22 of the cycle.

Adverse Reactions

Nervous system disorders: drowsiness, headache, depression, apathy, dysphoria.

Digestive system disorders: cholestatic hepatitis, nausea, vomiting, decreased appetite, calculous cholecystitis.

Genitourinary system disorders: decreased libido, menstrual cycle disorders.

Sense organ disorders: visual impairment.

Cardiovascular system disorders: increased blood pressure, peripheral edema, thromboembolism (including pulmonary artery and cerebral vessels), thrombophlebitis, retinal vein thrombosis.

Endocrine system disorders: galactorrhea, alopecia, weight gain, enlargement, pain and tension in the mammary glands, hirsutism.

Allergic reactions.

Local reactions: pain at the injection site.

Contraindications

• Hepatitis;
• Hepatic insufficiency;
• Breast cancer and genital organ cancer;
• Tendency to thrombosis;
• Children under 15 years of age,
• Second half of pregnancy;
• Hypersensitivity to the drug components.

With caution in cardiovascular diseases, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression; hyperlipoproteinemia.

Treatment is often combined with the prescription of estrogenic drugs or carried out directly after estrogen therapy.

Use in Pregnancy and Lactation

The drug is not used during pregnancy. If pregnancy occurs during the use of the drug, treatment must be discontinued immediately; there are no data on the need to terminate the pregnancy. The drug is contraindicated in the second half of pregnancy and during breastfeeding.

Use in Hepatic Impairment

Contraindicated in hepatic insufficiency and hepatitis.

Use in Renal Impairment

With caution in chronic renal failure.

Pediatric Use

Contraindicated in children under 15 years of age.

Special Precautions

If crystals precipitate or the entire contents of the ampoule crystallize, the ampoule should be heated in a boiling water bath with shaking. If the crystals disappear and the solution becomes transparent, and upon cooling to 36-38°C (96.8-100.4°F) the crystals do not precipitate again, the solution is suitable for use.

Prescription of the drug should only be done by the attending physician, under their supervision after an accurate diagnosis has been established.

When treating amenorrhea in children, verification of the amenorrhea diagnosis is necessary first and foremost.

Treatment before puberty should be aimed at stimulating growth. After 15-17 years, replacement therapy with estrogens and gestagens can be carried out, which causes cyclic uterine bleeding!

Effect on the ability to drive vehicles, machinery

Caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, as the drug may cause side effects that can affect these abilities.

Overdose

Symptoms: depression of the central nervous system, drowsiness, tachycardia; increased blood pressure, weakness, sweating.

Treatment: discontinuation of therapy until symptoms disappear, followed by the prescription of lower doses. If necessary, symptomatic treatment is carried out.

Drug Interactions

Weakens the effect of drugs that stimulate myometrial contraction (oxytocin), anabolic steroids (nandrolone), pituitary gonadotropic hormones.

Enhances the effect of diuretics, antihypertensive drugs, immunosuppressants, bromocriptine.

Reduces the effectiveness of anticoagulants.

The gestagenic activity of the drug is reduced by inducers of microsomal oxidation (barbiturates, hydantoins, rifampicin, etc.).

Storage Conditions

Store in a light-protected place at a temperature between 5°C and 25°C (41°F to 77°F). Keep out of reach of children.

Shelf Life

Shelf life – 5 years.

Dispensing Status

By prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.