Progesterone
Progesterone: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Progesterone
ATX code: G03DA04
Active ingredient: progesterone (progesterone)
Producer: JSC Dalkhimpharm (Russia), ANHUI CHENGSHI MANUFACTURE MEDICINE, Co. Ltd. (China), PJSC "Biopharma" (Ukraine)
Description and photo update: 2018-26-10
Prices in pharmacies: from 365 rubles.
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Progesterone is a drug that has a gestagenic effect.
Release form and composition
Progesterone is produced in the form of a solution for intramuscular administration (oily): a clear oily liquid, colorless or pale yellow or golden yellow (1 ml in a colorless glass ampoule; 10 ampoules in a blister, 1 blister in a cardboard box; 5 ampoules in a contour cell packaging, 2 packs or 10 ampoules in a cardboard box).
Composition of 1 ml solution:
- active substance: progesterone - 10 or 25 mg;
- additional components: olive oil and medical benzyl benzoate or soy oil and benzyl alcohol (depending on the manufacturer).
Pharmacological properties
Pharmacodynamics
Progesterone is a hormone of the corpus luteum and exhibits a gestagenic effect. By communicating with receptors located on the surface of cells of target organs, the agent penetrates into the nucleus, in which it activates deoxyribonucleic acid, which leads to increased synthesis of ribonucleic acid. The drug promotes the transformation of the proliferation phase of the uterine mucosa caused by follicular hormone into the secretory phase, and after fertilization of the egg, it provides the necessary conditions for its normal implantation and further development. Progesterone helps to reduce the excitability and contractility of the muscles of the uterus and fallopian tubes. The agent stimulates the growth of the secretory acini of the mammary glands and induces lactation, ensures the development of a normal endometrium.
By enhancing the action of protein lipase, progesterone leads to an increase in fat stores and improved glucose utilization, increasing basal and stimulated insulin secretion, creates optimal conditions for the accumulation of glycogen in the liver, and also increases aldosterone production. In small doses, the agent activates, and in large doses, it suppresses the production of gonadotropic hormones of the pituitary gland. Reduces azotemia, enhances the excretion of nitrogen by the kidneys.
Pharmacokinetics
After intramuscular (i / m) administration, the drug is rapidly and almost completely absorbed. The maximum concentration in blood plasma with intramuscular administration of 10 mg of progesterone is observed approximately 8 hours after the injection and remains above the basal level for 24 hours.
The agent is characterized by high binding to blood plasma proteins, primarily albumin - by 50–54% and corticosteroid-binding globulin - by 43–48%.
The biotransformation of progesterone occurs in the liver, with the formation of metabolites - pregnanolone and pregnandiol, which are conjugated with sulfuric and glucuronic acids. The isoenzyme CYP2C19 is involved in the metabolic process.
The half-life is several minutes, 50-60% of the substance is eliminated by the kidneys, over 10% through the intestines. The number of metabolites that are excreted by the kidneys varies depending on the phase of the corpus luteum.
Indications for use
- endocrine infertility (including with insufficient function of the corpus luteum);
- anovulatory metrorrhagia;
- amenorrhea;
- the threat of termination of pregnancy;
- algomenorrhea, oligomenorrhea (associated with hypogenitalism);
- diagnostics of the formation of endogenous estrogens.
Contraindications
Absolute:
- diagnosed or suspected neoplasms of the mammary gland and genitals (as a monotherapy drug);
- intracranial hemorrhage, thromboembolic disorders (stroke, myocardial infarction, pulmonary embolism) or a history of indications of these conditions / diseases;
- thrombophlebitis (including a history), deep vein thrombosis, retinal vascular thrombosis, the presence of risk factors for blood clots;
- severe liver disease or severe functional liver disorders (including malignant liver tumors, including a history);
- idiopathic jaundice, herpes, or itching during a previous pregnancy;
- porphyria;
- incomplete abortion or miscarriage;
- vaginal bleeding of unknown origin;
- II – III trimesters of pregnancy;
- lactation period;
- age up to 18 years;
- hypersensitivity to any of the constituents of the drug.
Relative (use Progesterone with extreme caution):
- chronic renal failure;
- arterial hypertension;
- diseases of the cardiovascular system (CVS);
- bronchial asthma;
- diabetes;
- hyperlipoproteinemia;
- migraine;
- epilepsy;
- depression;
- functional disorders of the liver of mild and moderate severity;
- I trimester of pregnancy (use is allowed only to prevent spontaneous miscarriage);
- photosensitivity.
Instructions for the use of Progesterone: method and dosage
Progesterone is administered by intramuscular injection.
Recommended dosing regimen depending on the indication:
- algodismenorrhea: the course begins 6-8 days before the onset of menstruation; the drug is administered daily at 5 or 10 mg for 6–8 days;
- algodismenorrhea due to underdevelopment of the uterus: combined with drugs of estrogenic action at the rate of 10,000 IU every other day for 2-3 weeks, in the next 6 days, use Progesterone;
- hypogenitalism and amenorrhea: use after the use of estrogenic drugs daily at 5 mg or every other day at 10 mg for 6-8 days;
- bleeding associated with ovarian dysfunction: appoint 5-15 mg daily for 6-8 days; in the case of preliminary curettage of the mucous membrane of the uterine cavity, the introduction of the drug begins after 18–20 days, if it is impossible to perform curettage, the solution is administered during bleeding; during therapy, a temporary increase in bleeding is possible (for 3-5 days), as a result of which, against the background of moderate and severe anemia, it is recommended to preliminarily carry out blood transfusion (200–250 ml); after stopping the bleeding within 6 days, the administration of Progesterone should be continued; if after 6-8 days of therapy the bleeding does not stop, further use of the drug is inappropriate;
- insufficiency of the corpus luteum: 12.5 mg per day is administered for 2 weeks from the moment of ovulation, if necessary, treatment is continued until 11 weeks of pregnancy;
- prevention / treatment of threatening and incipient miscarriage caused by insufficiency of the function of the corpus luteum: daily or every other day, 10-25 mg until the symptoms of the threat of miscarriage are completely removed; with a habitual abortion, a solution is injected until the fourth month of pregnancy;
- diagnostics of the formation of endogenous estrogens: once 100 mg.
Side effects
- nervous system: dizziness, headache, drowsiness / insomnia, optic neuritis, mood lability, asthenia, apathy, depression, dysphoria;
- digestive system: decreased appetite, bloating, vomiting, diarrhea, nausea, constipation, abdominal pain, cholecystitis, cholestatic hepatitis, cholestatic jaundice;
- endocrine system: hirsutism;
- immune system: urticaria, rash, pruritus, anaphylactoid reactions;
- metabolism: increase / decrease in body weight, edema;
- CVS: increased blood pressure, thrombophlebitis, thromboembolism (including vessels of the brain and pulmonary artery), retinal vein thrombosis, hemorrhagic rash;
- organ of vision: visual impairment;
- skin and subcutaneous tissues: alopecia, acne, erythema nodosum, erythema multiforme;
- musculoskeletal and connective tissue: back pain;
- urinary system: cystitis;
- mammary gland and genitals: changes in libido, shortening of the menstrual cycle, premenstrual syndrome, spotting spotting or breakthrough bleeding, amenorrhea, discomfort and itching in the vagina, vaginal discharge, changes in the viscosity of cervical secretions, spasm of uterine muscles, cervical erosion, ovarian hyperstimulation syndrome, vulvovaginitis, enlargement of the mammary glands, galactorrhea, pain and tension in the mammary glands, malignant neoplasms in the mammary gland;
- general disorders and local reactions: general malaise, hyperthermia, hot flashes, fatigue, hyperemia, irritation, soreness, hematoma, edema, induration and itching at the injection site.
Overdose
Overdose symptoms may include: dysmenorrhea, shortening of the menstrual cycle, transient dizziness, drowsiness, euphoria.
In some cases, the average therapeutic dose may be excessively high due to a particular sensitivity to the agent, too low a level of estradiol, unstable existing or emerging endogenous secretion of progesterone. With the development of gestagen-dependent side reactions, Progesterone therapy should be interrupted, and after removing these violations, resume at a lower dosage. If necessary, symptomatic treatment is possible.
special instructions
Before starting therapy, a medical examination should be carried out, including an examination of the pelvic organs and mammary glands, and a Pap test.
In view of the possible threat of thromboembolic complications, it is required to abandon the use of Progesterone when the following disorders appear: vascular lesions of the retina, double vision, loss of vision, thrombophlebitis, venous or arterial thromboembolism, thrombosis, regardless of localization.
With a history of indications of thrombophlebitis, as well as with diseases of the CVS, at present or in history, it is necessary to carefully monitor the patient's condition.
Progesterone should be used with extreme caution in patients with a history of depression; if a severe form of this disease appears, drug therapy should be discontinued.
With a long course of treatment, it is recommended to carry out regular medical examinations, including a study of liver activity, and in the event of cholestatic jaundice or deviations from the normal values of liver function tests, cancel the administration of Progesterone.
During the period of therapy, there may be a violation of glucose tolerance and an increase in the need for insulin and other hypoglycemic drugs in the presence of diabetes mellitus, and therefore it is necessary to carefully monitor the concentration of glucose in the blood.
If amenorrhea occurs during treatment, it is necessary to exclude a possible pregnancy, and with the development of acyclic bleeding, the solution should not be injected until their cause is identified (including before the histological examination of the endometrium).
The use of Progesterone can affect the results of such laboratory tests as coagulation parameters, indicators of the thyroid gland and liver function, the concentration of pregnandiol.
When observing the precipitation of crystals in the solution, the ampoule with the drug can be heated in a boiling water bath, shaking until the crystals dissolve. If, upon cooling to 36–38 ° C, the crystals do not fall out again and the solution is clear, it is usable.
Influence on the ability to drive vehicles and complex mechanisms
Since the use of Progesterone can provoke the appearance of visual impairment and dizziness, during the period of treatment, patients who drive vehicles or other complex mechanisms need to be careful.
Application during pregnancy and lactation
According to the instructions, Progesterone is contraindicated in the II – III trimesters of pregnancy. In the first trimester of pregnancy, the drug is allowed to be used exclusively to prevent spontaneous miscarriage.
During breastfeeding, it is contraindicated to inject the drug, since it penetrates into breast milk.
Pediatric use
The safety profile of Progesterone in patients under 18 years of age has not been studied. The drug is not prescribed for children and adolescents.
With impaired renal function
In the presence of chronic renal failure, the drug must be used with extreme caution.
For violations of liver function
It is contraindicated to use the drug in patients with severe hepatic impairment. For mild to moderate hepatic impairment, use Progesterone with caution.
Use in the elderly
There are no data confirming the safety and efficacy of using the drug in patients over 65 years of age. There are no indications for the administration of the drug in old age.
Drug interactions
- oxytocin - its lactogenic effect decreases;
- barbiturates - the effect of progesterone is weakened;
- drugs that stimulate the smooth muscles of the uterus, anabolic steroids, gonadotropic hormones of the anterior pituitary gland - the intensity of the action of these drugs decreases;
- antihypertensive drugs, diuretics, immunosuppressants, anticoagulants - their effect is enhanced;
- antiepileptic drugs (phenytoin), griseofulvin, spironolactone, phenylbutazone, rifampicin - progesterone metabolism in the liver is accelerated;
- bromocriptine - the effectiveness of this drug decreases;
- ketoconazole - an increase in the concentration of ketoconazole and an increase in the bioavailability of progesterone is possible;
- cyclosporine - the level of its content increases;
- ethanol (in large doses) - the bioavailability of progesterone decreases.
In different patients, the severity of these interactions can differ significantly, so the clinical effects of the latter are difficult to predict.
Analogs
Progesterone analogs are: Iprozhin, VANEL, Krainon, Progestozhel, Prajisan, Utrozhestan.
Terms and conditions of storage
Store in a place protected from light and out of reach of children at a temperature of 5-25 ° C.
The shelf life is 3 years or 5 years (depending on the manufacturer).
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Progesterone
Reviews of Progesterone are mostly positive. Patients who used the drug note its effectiveness in the treatment of metrorrhagia and other menstrual irregularities, as well as with the threat of termination of pregnancy. In many cases, according to reviews, the drug has demonstrated effectiveness when problems arise with conceiving and bearing a child.
The disadvantages of the patient's drug include a large number of contraindications and possible side effects, as well as a sharp pain in the / m injections of Progesterone and the appearance of seals, hematomas and edema at the injection site. To prevent the development of undesirable local reactions and reduce the pain from the injection, the patients are recommended to heat the ampoule in the palms of their hands or in hot water before administering the drug.
There are also reviews that indicate the lack of effect from therapy.
The price of Progesterone in pharmacies
The price of Progesterone for a package containing 10 ampoules of 1 ml can be approximately: 10 mg / ml - 270–390 rubles; 25 mg / ml - 540-760 rubles.
Progesterone: prices in online pharmacies
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Drug name Price Pharmacy |
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Progesterone 10 mg / ml solution for intramuscular administration (oily) 1 ml 10 pcs. 365 RUB Buy |
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Progesterone solution for in. oil 1% 1ml 10 pcs. 409 r Buy |
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Progesterone 25 mg / ml solution for intramuscular administration (oily) 1 ml 10 pcs. 797 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
