Description overdue on 10/12/2014
- Latin name: Progesterone
- ATC code: G03DA04
- Active substance: Progesterone (Progesterone)
- Manufacturer: JSC "Dalkhimpharm", Russia JSC "Farmak", Ukraine PJSC "Biopharma", Ukraine
- Composition
- Product form
- Pharmacological action
- Pharmacodynamics and pharmacokinetics
- Indications
- Contraindications
- Side effects
- Instructions on Progesterone
- Overdose
- Cooperation
- Terms of sale
- Storage conditions
- Shelf life
- Cautions
- Analogs
- During pregnancy (and lactation)
- Reviews
- Price, where to buy
Composition
Progesterone 1 ml 1% injectable solution containing 0, 01 grams of the active ingredient, as well as benzyl benzoate (Benzylii benzoas) and refined olive / peach oil (Oleum Olivarum / Oleum Persicorum).
The structure of one milliliter injection Progesterone 2, 5% included 0, 025 grams of active ingredient, benzyl benzoate (Benzylii benzoas) and refined olive / peach oil (Oleum Olivarum / Oleum Persicorum).
Progesterone 1 and 2%, 5% is produced in 1 ml ampoules, pre-packaged in packs of 5 or 10 pieces.
The composition of the gel and capsules varies depending on whether the pharmaceutical company produces these dosage forms.
Product form
To date, sold in pharmacies:
- Progesterone tablets for oral administration in capsules for intravaginal use;
- Progesterone ampoules in the form of injection solution in the peach or olive oil;
- Gel Progesterone is for external use only.
Pharmacological action
Progestogens . The active ingredient of the drug related to Clinico-pharmacological group "Gestagens" and participates in the functioning of the system "hypothalamus-pituitary-ovaries."
Pharmacodynamics and pharmacokinetics
Progestogen - this steroid hormone Which is produced in the body ovarian corpus luteum .
Mechanism of action of progesterone is associated with their ability to interact with specific progestin receptors which are located on the surface of target cells.
Contacting them, the substance enters the cell nucleus and activates deoxyribonucleic acid and ribonucleic acid stimulates synthesis.
Effect on the woman's body is that the drug:
- stimulates transition endometrium (the mucous layer of the inner mucosa that lines the uterine body) of the proliferative phase, which coincides with a follicular and ovulatory phases of the ovarian cycle, secretion;
- creates optimal conditions for implantation embryo It reduces sensitivity uterus and the fallopian tubes to the action of oxytocin and has a tocolytic effect;
- stimulates lipoprotein lipase ;
- increases the fat reserves of the organism;
- enhances the level of basal and stimulated (background) insulin It stimulates intracellular recycling Glucose ;
- enhances cumulation glycogen liver;
- It stimulates the synthesis of adrenal cortex hormone mineralokortikosteroidnogo aldosterone ;
- provokes gipoazotemiyu ;
- It increases the urinary excretion of nitrogen-containing metabolic products;
- It inhibits the production of a number of hypothalamic releasing factor lyuteotropina (LH) and follicle stimulating hormone (FSH) and thus biosynthesis pituitary gonadotropins ;
- reduces the permeability of the capillary walls in the tissues of the breast;
- reduces puffiness dependent the phase of the menstrual cycle connective framework;
- suppresses proliferative and mitotic activity ductal epithelial tissue (in the case when applied in the form of progesterone gel).
When taken orally, intravaginal application of the drug capsules, administered by injection into the muscle and the skin, the substance is rapidly absorbed. If application to the skin in gel form almost not absorbed and does not enter the systemic circulation.
The maximum plasma concentration when taking pills inside observed after 1-3 hours, with intravaginal application of this rate is reached in 2-6 hours.
Progesterone is characterized by the ability to bind to proteins at 96-99% (mainly albumin (about 50-54%) and 43-48% of the kortikosteroidsvyazyvayuschim globulin ).
AT liver biotransformed to inactive substance metabolites (mainly pregnandiol and pregnanolon ).
From 50 to 60% of the material is eliminated kidney More than 10% - with bile ; excreted from bile products metabolization progesterone derived from the content bowel and may be enterohepatic recycling .
Indications
Progesterone: what it is in the form of capsules for oral administration?
Admission capsules is indicated for premenstrual syndrome and if a woman diagnosed fibrosing adenosis (fibrocystic disease).
As progestin component the drug is prescribed for HRT ( hormone replacement therapy ) In the period preceding Menopause Directly at menopause (including, if Premature menopause ), As well as postmenopausal .
Capsules for intravaginal: indications for use
Capsules for intravaginal application shows:
- if necessary, the appointment of women in the case of HRT ovarian dysfunction Accompanied by a lack of progesterone ( oocyte donation );
- for supporting luteal phase in preparation for IVF ;
- for supporting luteal phase in induced or spontaneous menstrual cycle .
As a preventive measure the drug is prescribed for the prevention and the usual threatening spontaneous abortion Due progestin insufficiency ; at endocrine infertility ; to prevent development fibroids and Endometriosis .
Indications of oil solution
Because progesterone is monthly (in case of delay due to a deficiency of this hormone), he was appointed to various kinds of adjustments menstrual disorders .
Thus, the appointment of an oily solution is useful when amenorrhea (absence of menstrual bleeding over several cycles) oligomenoree (ie, delayed menstrual bleeding for more than 40 days).
In addition, injections are prescribed for:
- related impairment of sexual glands algomenoree (painful menstruation);
- anovulatory metrorrhagia (not related to ovulation uterine bleeding);
- endocrine infertility (including those caused by failure of the corpus luteum);
- threat miscarriage ;
- diagnostic procedures, which aim to determine the level of secretion estrogenovё + .
Progesterone at a delay menstruation can be used both in tablet form and in the injections. However, more often still designate an injection, since the effect is noticeable after much faster than after administration of the tablets.
Indications gel
Applications using progesterone gel form prescribed for mastalgia and mastitis .
Intravaginal application of the gel are shown for the treatment of progesterone deficiency secondary amenorrhea As well as reproductive programs if a woman is required to remedy the lack of progesterone in the oocyte donation .
Contraindications
All formulations are contraindicated Progesterone:
- at hypersensitivity to the drug;
- the presence of serious renal dysfunction and / or hepatic function ;
- if the patient is diagnosed hepatitis ;
- at acute inflammation of the venous wall And when occurring in acute thromboembolic disorders ;
- patients who have elevated risk of blood clots ;
- vaginal (vaginal) bleeding of unclear origin ;
- frustrated miscarriage ;
- incomplete abortion ;
- porphyrin disease .
Additional contraindications to the appointment of an oily solution include:
- availability cancer of the breast or genital (for breast carcinoma Exceptions are cases when progesterone is administered as part of combination therapy);
- pregnancy (from 14 weeks).
Side effects
Treatment of progesterone can cause allergic reactions.
Action on the woman's body in a capsule form of the drug, in some cases accompanied by:
- hypersomnia;
- arising after 1-3 hours after taking the pill coming dizziness;
- various kinds menstrual irregularities (eg, reduction of its duration or the appearance of intermediate bleeding).
The most frequent side effects of injections:
- acute blockage of the lumen of blood vessels clot ;
- thrombophlebitis (thrombosis, accompanied by inflammation of the venous wall);
- thrombosis, retinal blood vessels ;
- improving performance Blood Pressure ;
- appearance edema ;
- chronic cholecystitis Characterized by the formation of stones in the gallbladder (calculous cholecystitis);
- increased drowsiness ;
- headache ;
- apathy ;
- blurred vision;
- hair loss ( alopecia );
- reduction libido ;
- hirsutism (hair growth in women by male pattern);
- nausea and vomiting;
- poor appetite and consequently weight reduction;
- menstrual irregularities ;
- cholestatic hepatitis ;
- depression ;
- dysphoria (gender identity disorder);
- is not associated with breast-feeding the milk from the mammary glands ( galactorrhea );
- increase tenderness and tension of the mammary glands;
- local reactions (redness of the skin and tenderness at the injection site).
Instructions on Progesterone
Injections of Progesterone: instructions for use
Injections of Progesterone makes the muscle or under the skin.
With dysfunctional uterine bleeding It shows daily administration for 6-8 days 0, 5-1, 5 ml of a solution of one percent. If the patient undergoing the procedure curettage of the uterus, a course of injections started after 18-20 days.
If it is impossible to carry out curettage, administration of the drug is allowed even during bleeding. When using progesterone during the last bleeding may temporarily amplified (usually 3-5 days).
For this reason, patients with moderate to severe forms anemia It recommended to pour 0, 2-0, 25 liters of blood. When stopped bleeding should not interrupt the treatment before 6 days. If the bleeding has not stopped after 6-8 days of treatment, continue the introduction of the solution is considered inappropriate.
With algodismenoree (painful menstruation), treatment is initiated 6-8 days before menstruation. Patients shown daily administration for 6-8 days 0, 5 to 1 ml of a one percent solution. The treatment is allowed to be repeated several times.
As a preventive measure for prevent miscarriage daily or every other day is administered 0, 5 to 2, 5 ml of a one percent solution. Injections continue to do until the complete disappearance threatening symptoms. When habitual miscarriage drug should be administered through IV month of pregnancy.
And the maximum single daily dose to adult patients with progesterone into the muscle at 0, 025 g
Progesterone for monthly call: how to chop at a delay menstruation
With hypogonadism, amenorrhea And for inducing menses in the event of a delay, treatment is initiated with prescribing estrogenic effect. The goal of therapy is to achieve sufficient proliferation of endometrial cells . Upon completion of the course with the action of estrogen drugs prescribed to patients injections of progesterone.
Treatment involves daily administration of 0, 5, or every other day for 1 ml of oil solution of one percent (and in some cases may be assigned Progesterone 2, 5% for monthly call). Usually, it takes 5 to 10 injections.
Instructions for Progesterone in tablets and in the form of a gel
The tablets are taken orally (not tied to meal times), or intravaginal use, the gel is used as a local agent. The dosage regimen, the optimal dosage form and duration of treatment is determined depending on the evidence and the characteristics of the disease.
Generally, a daily dose is from 200 to 400 mg progesterone. To maintain luteal phase in IVF patient indicates the dosage of 600 mg progesterone multiplicity application 3 times a day (200 mg every 8 hours).
For one application requires 2 5 grams of gel (equivalent to 25 mg of progesterone). The gel is applied by means of a special applicator metering breast skin daily once or twice a day (before complete absorption) or in the second phase of the menstrual cycle (from the 16th to the 25th day). Treatment is usually carried out for three cycles.
Repeated course is possible if indicated.
Overdose
With an overdose of progesterone increases the risk of the above side effects and their severity thus enhanced. When the unwanted symptoms of use of the drug is stopped. After the disappearance of the side effects of treatment continues, but with smaller doses.
Overdosing preparation in gel form is considered unlikely because of the fact that its systemic absorption is extremely small.
Cooperation
Reduces the intensity of the action Anabolic steroids . oksitoksicheskih drugs (ie means of stimulating uterine activity ) Synthesized in the anterior pituitary gonadotropins .
Reduces lactogenic effect Oxytocin .
Together with the application diuretics . bromocriptine ; drugs to lower high blood pressure ; systemic coagulants . immunosuppressive Progesterone enhances the action of these drugs.
Before the drug in combination with barbiturates marked decrease its pharmacological activity.
Progesterone reduces the effectiveness of anticoagulants.
Terms of sale
Prescription.
Storage conditions
Store in a dry, dark place at a temperature between 15 and 25 degrees Celsius. Keep away from children.
Shelf life
The product is fit for use for 5 years from the date of issue.
Cautions
With caution and under constant control used in diseases of the heart and blood vessels . epilepsy , Mild to moderate renal impairment For treating diabetic patients suffering from asthma and migraine .
Also Progesterone is prescribed with caution and patients with a history mental disorders . If you experience the first signs of depression treatment should be stopped. You should also pay attention to the early signs of thromboembolism . Their appearance is a cause for discontinuation.
Patients with diabetes between progesterone treatment should be continuously monitored indicators blood glucose .
Since steroid hormones are metabolized in the liver, progesterone is not indicated in patients with impaired liver function .
Treatment of progesterone may be accompanied by a weakening of concentration, so caution should be exercised in the management of vehicles and busy with other activities that require a high rate of psychomotor reactions or are a potential threat to life and limb.
Prolonged use of high doses of progesterone can cause cessation of menstruation.
Preparation in the form of gel is applied, without rubbing it into the skin of the breast and massaging them. After applying the cream should not be exposed to direct sunlight.
Analogs
Depo-Provera
Prozhestozhel
Utrozhestan
The progesterone-containing drugs - it Utrozhestan . Iprozhin . Kraynon . Pradzhisan . Prozhestozhel . Ehndometrin . The multi-component analog of the drug - vaginal capsules Triozhinal .
Progesterone during pregnancy
Tablets and injections during pregnancy are shown only in cases when it is necessary to warn spontaneous miscarriage. Reliable data on the safety of the drug during pregnancy in the form of a gel is not.
During the period of lactation should refrain from the use of tablets and injections of progesterone. The gel is prescribed when no alternative therapies, and the potential benefit to the mother outweighs the risk to the child.
It argued that the drug helps to get rid of an unwanted pregnancy, and therefore often have questions, "How to rip early pregnancy using Progesterone? ".
However, this is impossible because contrary progesterone promotes pregnancy (for this reason, the drug is prescribed for women who are diagnosed with "infertility", as well as women who have to IVF). But a deficiency of this hormone just might lead to a miscarriage.
Reviews of progesterone
The largest number of reviews on the drug can be found on a special forum devoted to the problem of female infertility.
Most women who have had difficulty conceiving and carrying a child, say the effectiveness of progesterone, even in cases where the patient suffered several miscarriages before the course of application of this means upon the occurrence of another pregnancy. That is, in some cases, Progesterone - this is the only chance to save the pregnancy.
However, there are negative comments about the drug. They are connected with a sufficiently large number of side-effects and contraindications to its application. In addition, some of the women receiving treatment progesterone, did not notice any effect of the prescribed therapy.
Whatever it was, as in the case with other drugs, self-progesterone unacceptable. To begin the application rate is possible only after a thorough examination and on the basis of these analyzes.
Price Progesterone
Price injections in Russia - from 105 rubles per pack of ampoules with a one percent solution and from 360 rubles for packaging vials of oily solution of 2, 5%. Buy pills can be an average of 180 rubles (the price depends on the place of purchase, the manufacturer of the drug, the concentration of active ingredient in a single tablet and the number of tablets in the package).
In the Ukrainian pharmacies price Progesterone tablets averaged 45 UAH. The cost of vials with a solution of 1% - from 12 UAH, ampoules 2, 5% are an average of 32 USD.
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