Composition, form of production and packaging
Solution for the / m introduction of oily light yellow or golden yellow, transparent.
1 ml
hydroxyprogesterone caproate 125 mg
Excipients: benzyl benzoate medical - 300 Ојl, olive oil - up to 1 ml.
1 ml - ampoules glass (5) - packings cellular planimetric (2) - packs cardboard.
1 ml - ampoules (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Synthetic analogue 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 intramuscular injection of an oily solution, its effect lasts from 7 to 14 days. On biological properties similar to progesterone. By binding to receptors on the surface of the cells of target organs, it penetrates into the nucleus, where, by controlling the transcription of DNA, it affects the synthesis of RNA. Promotes the transition of the mucous membrane of the uterus from the phase of proliferation caused by follicle-stimulating hormone into the secretory hormone, and after fertilization creates the necessary conditions for the implantation and development of a fertilized egg. Reduces excitability and contractility of the musculature of the uterus and fallopian tubes, stimulates the development of alveoli (milk forming regions) of the mammary glands
PHARMACOKINETICS
Quickly and almost completely absorbed after intramuscular injection.
Metabolized in the liver with the formation of conjugates with glucuronic and sulfuric acids.
T 1/2 is 5 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
INDICATIONS
Conditions associated with malnutrition of the yellow body:
- amenorrhea (primary and secondary);
- dysfunctional uterine bleeding.
DOSING MODE
Method of administration: intramuscularly. Before administration, the preparation should be heated to 30-40 В° C. In amenorrhea (primary, secondary) is appointed immediately after the termination of the use of estrogenic medicines of 250 mg once or in two administrations.
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 62.5-125 mg (0.5-1 ml) 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: decreased libido, menstrual cycle disorders.
From the senses: a blurred vision.
From the cardiovascular system: increased blood pressure, peripheral edema, thromboembolism (including pulmonary arteries and cerebral vessels), thrombophlebitis, retinal vein thrombosis.
On the part of the endocrine system: galactorrhea, alopecia, .increase in body weight, increase, pain and tension of the mammary glands, hirsutism.
Allergic reactions .
Local reactions: soreness in the injection site.
CONTRAINDICATIONS
- Hepatitis;
- liver failure;
- cancer of the breast and genital organs;
- propensity to thrombosis;
- children's age till 15 years,
- second half of pregnancy;
hypersensitivity to the components of the drug.
With caution: with 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.
PREGNANCY AND LACTATION
The drug is not used during pregnancy. In the case of pregnancy on the background of the drug should be immediately interrupted treatment; there is no data on the necessity of abortion. The drug is contraindicated in the second half of pregnancy and during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution in chronic renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in hepatic insufficiency and hepatitis.
APPLICATION FOR CHILDREN
Contraindicated for children under 15 years.
SPECIAL INSTRUCTIONS
In the case of crystal precipitation 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 upon cooling to 36-38 В° C the crystals do not fall again, the solution is suitable for use.
The administration of the drug should be performed only by the attending physician, under his supervision after an accurate diagnosis.
In the treatment of amenorrhea in children, verification of the diagnosis of amenorrhea is primarily necessary.
Treatment before the pubertal period should be aimed at stimulating growth. After 15-17 years, it is possible to carry out substitution therapy with estrogens and gestagens, which causes cyclic uterine bleeding!
Influence on ability to drive vehicles, mechanisms
Care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, since the drug can 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, with subsequent administration of smaller doses. If necessary, perform symptomatic treatment.
DRUG INTERACTION
Weaken the effect of drugs that stimulate the reduction of myometrium (oxytocin), anabolic steroids (nandrolone), gonadotropic hormones of the pituitary gland.
Strengthens the action of diuretics, hypotensive drugs, immunosuppressants, bromocriptine.
Reduces the effectiveness of anticoagulants.
The gestagenic activity of the drug is reduced by inducers of microsomal oxidation (barbiturates, hydantoins, rifshpicin, etc.).
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dark place at a temperature of 5 to 25 В° C. Keep out of the reach of children. Shelf life - 5 years.
