Utrogestan capsules 200 mg 14 pcs
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Active ingredients
Release form
Composition
Pharmacological effect
Progestin drug. Progesterone, the active ingredient of the drug Utrozestan, is a hormone of the corpus luteum. By binding to receptors on the surface of target organ cells, it penetrates the nucleus, where by activating DNA, it stimulates RNA synthesis.
It promotes the transition of the uterine mucosa from the proliferative phase caused by follicular hormone to the secretory phase. After fertilization promotes the transition to the state necessary for the development of a fertilized egg. Reduces the excitability and contractility of the muscles of the uterus and fallopian tubes, stimulates the development of the terminal elements of the mammary gland.
Stimulating protein lipase, increases fat reserves, increases glucose utilization. Increasing the concentration of basal and stimulated insulin, contributes to the accumulation of glycogen in the liver, increases the production of pituitary gonadotropic hormones, reduces azotemia, increases the excretion of nitrogen in the urine.
It activates the growth of the secretory section of the mammary glands acini, induces lactation.
Promotes the formation of normal endometrium.
Pharmacokinetics
When taken orally
Absorption Micronized progesterone is absorbed from the gastrointestinal tract. The concentration of progesterone in the blood plasma gradually increases during the first hour, Cmax is noted 1-3 h after administration. The concentration of progesterone in the blood plasma increases from 0.13 ng / ml to 4.25 ng / ml after 1 h, to 11.75 ng / ml - after 2 h and amounts to 8.37 ng / ml after 3 hours, 2 ng / ml after 6 hours and 1.64 ng / ml after 8 hours after administration. Metabolism The main metabolites that are determined in blood plasma are 20-alpha-hydroxy-delta-4 alpha pregnanolone and 5 alpha dihydroprogesterone.
Removal
Excreted in the urine as metabolites, 95% of them are glucuron-conjugated metabolites, mainly 3-alpha, 5-beta-pregnanediol (pregnandion). These metabolites, which are determined in plasma and in urine, are similar to substances formed during physiological secretion of yellow of the body. When administered intravaginally
Suction
Absorption occurs quickly, progesterone accumulates in the uterus.A high level of progesterone is observed after 1 h after administration. Cmax of progesterone in plasma is reached 2-6 hours after administration. With the introduction of the drug in 100 mg 2 times / day, the average concentration remains at 9.7 ng / ml for 24 hours. When given in doses of more than 200 mg / day, the concentration of progesterone corresponds to the first trimester of pregnancy.
Metabolism
Metabolized to form predominantly 3-alpha, 5-beta-pregnanediol. Plasma 5-beta pregnanol level is not increased.
Removal
Excreted in the urine as metabolites, the main part is 3-alpha, 5-beta-pregnanediol (pregnandion). This is confirmed by a constant increase in its concentration (Cmax 142 ng / ml after 6 h).
Indications
Contraindications
Precautionary measures
Use during pregnancy and lactation
In pregnancy, the drug can only be used intravaginally.
The drug should be used with caution in the II and III trimesters of pregnancy due to the risk of cholestasis.
Progesterone penetrates into breast milk, so the use of the drug is contraindicated during breastfeeding.
Dosage and administration
Side effects
Drowsiness or rapid dizziness, appearing 1 to 3 hours after taking the drug.
Shortening of the menstrual cycle and intermenstrual bloody discharge. These side effects were observed only when taking the drug inside.
Overdose
Symptoms: drowsiness, transient dizziness, euphoria, shortening of the menstrual cycle, dysmenorrhea.
In some patients, the average therapeutic dose may be excessive due to the present or unstable endogenous progesterone secretion, particular sensitivity to the drug, or too low an estradiol concentration.
Treatment: - in case of drowsiness or dizziness, it is necessary to reduce the daily dose or prescribe the drug at bedtime for 10 days of the menstrual cycle, - in case of shortening of the menstrual cycle or bloody discharge, it is recommended to transfer the treatment to a later day of the cycle (for example, 19). th instead of the 17th), - in perimenopause and in postmenopausal HRT, it is necessary to ensure that the concentration of estradiol is optimal.
In case of overdose, symptomatic treatment is carried out if necessary.
Interaction with other drugs
When administered orally, Progesterone enhances the action of diuretics, antihypertensive drugs, immunosuppressants, anticoagulants. Reduces the lactogenic effect of oxytocin.
The simultaneous use of CYP3A4 liver microsomal enzymes with inducer drugs, such as barbiturates, antiepileptic drugs (phenytoin), rifampicin, phenylbutazone, spironolactone, griseofulvin, is accompanied by an acceleration of progesterone metabolism in the liver.
Simultaneous administration of progesterone with certain antibiotics (penicillins, tetracyclines) can lead to a decrease in its effectiveness due to a violation of the enterohepatic recirculation of sex hormones due to changes in the intestinal microflora.
The severity of these interactions may vary in different patients, so the prognosis of the clinical effects of these interactions is difficult. Ketoconazole may increase the bioavailability of progesterone. Progesterone may increase the concentration of ketoconazole and cyclosporine.
Progesterone may decrease the effectiveness of bromocriptine.
Progesterone can cause a decrease in glucose tolerance, as a result of which - to increase the need for insulin or other hypoglycemic drugs in patients with diabetes mellitus.
Bioavailability of progesterone can be reduced in patients who smoke and with excessive use of alcohol. With intravaginal use
The interaction of progesterone with other drugs with intravaginal use was not evaluated. The simultaneous use of other drugs used intravaginally should be avoided to avoid impairing the release and absorption of progesterone.
special instructions
The drug Utrozhestan can not be used for contraception.
The drug can not be taken with food, because food intake increases the bioavailability of progesterone.
Patients with a history of depression should be monitored, and if severe depression develops, the drug should be discontinued.
Patients with concomitant cardiovascular diseases or their history should also be observed periodically by a doctor.
The use of the drug Utrogestan after the first trimester of pregnancy may cause the development of cholestasis.
With prolonged treatment with progesterone, it is necessary to regularly conduct medical examinations (including the study of liver function), treatment should be canceled in case of deviations from normal indicators of functional liver tests or cholestatic jaundice.
When using progesterone, a decrease in glucose tolerance and an increase in the need for insulin and other hypoglycemic drugs in patients with diabetes mellitus is possible.
In the case of amenorrhea in the treatment process, it is necessary to exclude the presence of pregnancy.
If the treatment starts too early at the beginning of the menstrual cycle, especially before the 15th day of the cycle, a shortening of the cycle and / or acyclic bleeding is possible. In the case of acyclic bleeding should not use the drug to determine their causes, including the conduct of histological examination of the endometrium.
With a history of chloasma or a tendency to its development, patients are advised to avoid UV exposure. More than 50% of cases of spontaneous abortions in early pregnancy are due to genetic disorders. In addition, the cause of spontaneous abortions in early pregnancy can be infectious processes and mechanical damage. The use of the drug Utrogestan in these cases can only lead to a delay in rejection and evacuation of the non-viable ovum.
The use of the drug Utrozhestan to prevent threatened abortion is justified only in cases of progesterone deficiency.
The drug Utrozhestan includes soy lecithin, which can cause hypersensitivity reactions (urticaria and anaphylactic shock).
When conducting hormone replacement therapy with estrogens during the period of perimenopause, the use of the drug Utrogestan is recommended for at least 12 days of the menstrual cycle.
In continuous mode of post-menopausal hormone therapy, the use of the drug is recommended from the first day of estrogen administration.
When conducting HRT increases the risk of venous thromboembolism (deep vein thrombosis or pulmonary artery thromboembolism), the risk of ischemic stroke, IBS. , double vision, vascular lesions of the retina, migraines, - venous thromboembolism or thrombotic complications, regardless of their location.
If there is a history of thrombophlebitis, the patient should be closely monitored.
When using the drug Utrozhestan with estrogen-containing drugs, refer to the instructions for their use on the risks of venous thromboembolism. progestin. It is not known whether there is an increase in the risk of breast cancer in postmenopausal women during HRT with estrogen-containing drugs in combination with progesterone. a woman should be examined to identify contraindications to her. In the presence of clinical indications, an examination of the mammary glands and a gynecological examination should be carried out.
The use of progesterone can affect the results of some laboratory tests, including indicators of liver function, thyroid gland, coagulation parameters, the concentration of pregnandiol.
Influence on ability to drive motor transport and control mechanisms
When using the drug orally, care must be taken when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.