Ginipral action. Medicinal reference book geotar

Ginipral is a drug used to treat diseases of the urogenital organs.

Release form and composition

Ginipral is produced in the form of biconvex white round tablets, in blisters of 10 pcs. One tablet contains 500 mcg of hexoprenaline sulfate and excipients - magnesium stearate, lactose hydrate, copovidone, corn starch, glycerol palmitate stearate, disodium edetate dihydrate and talc.

Ginipral is also produced in the form of a colorless, transparent solution, in ampoules of 2 ml. Each of them contains 10 mcg of hexoprenaline sulfate and excipients such as:

• Disodium edetate dihydrate;
• Sodium pyrosulfite;
• Sulfuric acid 2N;
• Sodium chloride;
• Water for injections.

Indications for use

Ginipral solution, according to the instructions, is used for acute, massive and long-term tocolysis.

The drug in tablet form is prescribed in cases of threatened premature birth.

Contraindications

The use of Ginipral is contraindicated in case of myocarditis, thyrotoxicosis, arterial hypertension, angle-closure glaucoma, tachyarrhythmia, intrauterine infections, premature placental abruption, as well as in cases of hypersensitivity to the components that make up the drug.

The drug is also contraindicated for coronary heart disease, mitral valve disease, aortic stenosis, uterine bleeding, severe liver and kidney diseases.

Ginipral is not prescribed in the first trimester of pregnancy, or during breastfeeding.

Directions for use and dosage

The drug in the form of a solution is administered intravenously slowly over 5-10 minutes using conventional infusion systems or automatically dosing infusion pumps. Before use, the product is diluted in an isotonic sodium chloride solution to 10 ml. The dosage of Ginipral for acute and massive tocolysis is 1 ampoule.

If contractions do not resume within 2 days, therapy is continued with Ginipral tablets, which are taken orally with a small amount of water. In cases of threatened preterm birth, patients take 1 tablet 1-2 hours before stopping the Ginipral infusion.

Side effects

The instructions for Ginipral indicate that the drug may cause side effects from certain body systems, namely:

• Intestinal obstruction, nausea, vomiting and temporary increase in transaminase levels (digestive system);
• Dizziness, slight tremor of fingers, headache and anxiety (central and peripheral nervous system);
• Maternal tachycardia, rhythm disturbance and cardialgia (cardiovascular system).

Ginipral can cause oliguria, increased sweating, edema, increased plasma glucose levels, hypocalcemia and hypokalemia at the beginning of therapy, as well as allergic reactions - bronchospasm, anaphylactic shock, difficulty breathing and impaired consciousness up to coma.

In newborns, the drug causes acidosis and hypoglycemia.

Symptoms of an overdose of Ginipral are headaches, severe tachycardia in the mother, increased sweating, arrhythmia, shortness of breath, anxiety, finger tremor, decreased blood pressure and cardialgia. In such cases, the prescription of non-selective beta-blockers is required.

special instructions

During drug therapy, it is important to carefully monitor the functions of the cardiovascular system of the mother and fetus. It is recommended to record an ECG before and during treatment. The dose of Ginipral should be reduced if there is a marked decrease in blood pressure or a significant increase in heart rate in the mother.

If it is necessary to use Ginipral in patients with hypersensitivity to sympathomimetics, the dose of the drug should be minimal and selected individually, and therapy should be carried out under the supervision of a physician.

Drug therapy should be stopped immediately if the patient experiences pain in the heart area, difficulty breathing, or signs of heart failure.

In mothers with diabetes mellitus, at the beginning of treatment it is necessary to monitor carbohydrate metabolism, since the use of Ginipral in most cases causes an increase in glucose in the blood plasma.

In cases where labor occurs after a course of treatment with the drug, it should be taken into account that the newborn may experience acidosis and hypoglycemia associated with the transplacental penetration of ketone and lactic acids.

It should be borne in mind that during the use of Ginipral, diuresis may decrease, and therefore it is recommended to pay special attention to the appearance of symptoms indicating fluid retention in the body.

Analogs

There are no synonyms for the drug. An analogue of Ginipral is the drug Partusisten.

Terms and conditions of storage

Ginipral, according to the instructions, should be stored in a well-ventilated, dry place, out of reach of children and protected from light, at a temperature varying between 18-25 °C.

The drug is dispensed from pharmacies according to a doctor's prescription. The shelf life of the solution is three years, tablets – five years. After the expiration date, Ginipral must be disposed of.

Tradename: GINIPRAL ®

International nonproprietary name:

Chemical rational name:
C 22 H 34 N 2 O 10 S
N,N"-bis-hexamethylenediamine sulfate.

Dosage form:

Compound:

Description
Transparent colorless solution.

Pharmacotherapeutic group:

ATX code: R03CC05.

Pharmacological properties

Pharmacodynamics
GINIPRAL ® is a selective β 2 - sympathomimetic that relaxes the muscles of the uterus. Under the influence of GINIPRAL ® the frequency and intensity of uterine contractions decreases. The drug inhibits spontaneous and oxytocin-induced labor contractions; During childbirth, it normalizes excessively strong or irregular contractions.
Under the influence of GINIPRAL ®, premature contractions stop in most cases, which makes it possible to prolong pregnancy until the normal due date. Due to its β 2 - selectivity, GINIPRAL ® has little effect on cardiac activity and blood flow in a pregnant woman and fetus.

Pharmacokinetics
GINIPRAL ® consists of two catecholamine groups, which in the human body undergo methylation via catecholamine-O-methyltransferase. While the effect of isoprenaline is almost completely abolished by the introduction of one methyl group, hexoprenaline becomes biologically inactive only if both of its catecholamine groups are methylated. This property, as well as the high ability of GINIPRAL ® to adhere to surfaces, are considered the reasons for its long-lasting action. Studies with 3H-labeled substances conducted on rats showed that the urinary excretion of biologically active substances continues longer after intravenous injection than after administration of isoprenaline; after 2 hours, only 0.6% of isoprenaline was excreted unchanged. In comparison, when using hexoprenaline during the first 4 hours, 80% of the biologically active substances were excreted in the urine unchanged, that is, in the form of free hexoprenaline and monomethyl derivative. Subsequently, the excretion of dimethyl derivative and conjugated compounds (glucuronide and sulfate) increases. A small part is excreted in the bile in the form of complex metabolites. In addition, when administered intrabronchially, labeled 3 H-hexoprenaline is excreted in the urine in the form of a biologically active substance for a relatively long time. Part of the injected substance remains active at the injection site for quite a long time. After intramuscular administration, the active metabolite was also well excreted in the urine. The effect of the drug is observed at the injection site for quite a long time. Hexoprenaline is well absorbed when taken orally, and part of it is excreted in the urine as a dimethylated metabolite.

Indications for use
1. Acute tocolysis
Inhibition of labor contractions during childbirth with acute intrauterine asphyxia, immobilization of the uterus before cesarean section, before turning the fetus from a transverse position, with umbilical cord prolapse, with complicated labor. As an emergency measure in case of premature birth before taking the pregnant woman to the hospital.
2. Massive tocolysis
Inhibition of premature labor contractions in the presence of a smoothed cervix and/or dilatation of the uterine pharynx.
3. Long-term tocolysis
Prevention of premature birth during intensified or frequent contractions without cervical effacement or dilatation of the uterus. Immobilization of the uterus before, during and after cervical cerclage.

Contraindications

Compound

Each 2 ml ampoule contains:

Active substance: hexoprenaline sulfate 0.01 mg.

Excipients: sodium metabisulfite (sodium disulfite) 0.04 mg, disodium edetate dihydrate 0.05 mg, sodium chloride 18.00 mg, sulfuric acid 1 M solution as needed to bring to pH 3.0, water for injection up to 2.00 ml Description: Transparent colorless solution.

Pharmacotherapeutic group: tocolytic agent - selective betag-adrenergic agonist.

ATX code: G02 C.A.

Pharmacological properties

Pharmacodynamics

Selectively stimulates betag-adrenergic receptors, activates adenylate cyclase with a subsequent increase in the formation of cyclic adenosine monophosphate (cAMP), which stimulates the calcium pump, which redistributes calcium ions (Ca2+) in myocytes, resulting in a decrease in the concentration of the latter in myofibrils. Expands the bronchi, blood vessels, reduces contractile activity and myometrial tone, thereby helping to improve uteroplacental blood flow. Stimulates glycogenolysis. Due to its betag selectivity, Ginipral® has a slight effect on cardiac activity and blood flow in the pregnant woman and fetus.

Under the influence of the drug Ginipral®, the tone of the uterus decreases, the frequency and intensity of uterine contractions decreases, until they completely stop, which allows you to prolong pregnancy, incl. before the onset of timely (urgent) labor. Ginipral®, when administered intravenously, inhibits spontaneous and oxytocin-induced labor contractions; During childbirth, it normalizes excessively strong or irregular contractions.

The tocolytic effect of Ginipral® begins immediately after intravenous injection and lasts approximately 20 minutes. The effect of the drug is maintained by subsequent long-term intravenous infusion.

Pharmacokinetics

Distribution

There is no data on the distribution of hexoprenaline in the human body. In animal studies, when administered intravenously, significant concentrations of hexoprenaline were observed in the liver, kidneys and skeletal muscles, and to a lesser extent in the brain and myocardium. Metabolism

Hexoprenaline is metabolized by catechol-O-methyl-transferase to mono-3-O-methyl-hexoprenaline and di-3-O-methyl-hexoprenaline.

Removal

When administered intravenously, the half-life (T1/2) is about 25 minutes. Within 24 hours, about 44% of the dose of hexoprenaline is excreted by the kidneys and 5% through the intestines, within 8 days 54% and 15.5%, respectively. In the initial stage, free hexoprenaline and both methylated metabolites, as well as their corresponding sulfates and conjugates with glucuronic acid, are excreted by the kidneys. After 48 hours, only di-3-O-methyl-hexoprenaline is detected in the urine. About 10% of the dose is excreted in bile, mainly in the form of conjugates of O-methylated metabolites. Some reabsorption occurs in the intestines, because Less substance is excreted in feces than is found in bile.

Indications for use

For short-term treatment of uncomplicated preterm birth:

Stopping labor between 22 and 37 weeks of pregnancy in patients without medical or gynecological contraindications to tocolytic therapy.

External rotation (of the fetus) onto the head. Use in emergency situations with premature uterine contractions outside the hospital setting before transport to the hospital.

Directions for use and doses

Instructions for using ampoules with a breaking point:

Place the tip of the ampoule pointing up! Gently tapping with your finger and shaking the ampoule, allow the solution to flow down from the tip of the ampoule.

Place the tip of the ampoule pointing up! Break off the tip downwards, as shown in the picture.

Treatment with hexoprenaline should only be carried out by obstetricians/physicians experienced in the use of tocolytic drugs. It should be carried out in institutions adequately equipped to conduct continuous monitoring of the health of the mother and fetus.

Hexoprenaline should be prescribed immediately after diagnosis of preterm labor and examination of the patient to determine the presence of contraindications to the use of hexoprenaline.

This procedure should include an adequate assessment of the patient's cardiovascular system, with monitoring of cardiorespiratory function, checked using an electrocardiogram (ECG) throughout the entire treatment period.

Dosage

Initial dose: Begin with a bolus of hexoprenaline 10 mcg intravenously over 5 to 10 minutes. A bolus can be prepared by adding the contents of 1 ampoule (10 mcg of hexoprenaline) to isotonic saline or glucose solution to a total volume of 10 ml. The initial dose should be followed by a continuous infusion of 0.3 mcg hexoprenaline per minute (see below). In addition, infusion therapy can be started without an initial bolus dose.

Continuous dose: Begins with an infusion of 0.3 mcg of hexoprenaline per minute. The infusion rate should be doubled every 10 minutes until any signs of uterine contractions have subsided for at least 24 hours or until the mother's pulse rate reaches 120 beats per minute.

Calculation of drip infusion rate at a dosage of 0.3 mcg/min: 20 drops = 1 ml. Long-term treatment solution can be prepared by adding the contents of 1 or more ampoules (25 mcg hexoprenaline) to isotonic saline or glucose solution to a total volume of 500 mL.

The daily dose of 430 mcg of hexoprenaline was exceeded only in isolated cases.

The recommended maintenance dose is 0.075 mcg hexoprenaline per minute. Calculation of drip infusion rate at a dosage of 0.075 mcg/min: 20 drops = 1 ml. Long-term treatment solution can be prepared by adding the contents of 1 or more ampoules (25 mcg hexoprenaline) to isotonic saline or glucose solution to a total volume of 500 mL.

Amount of hexoprenaline Total volume of drops/min. ml/min.

25 mcg (1 ampoule) 500 ml 30 drops/min. 1.5 ml/min.

50 mcg (2 ampoules) 500 ml 15 drops/min. 1.5 ml/min.

The initial dose is a bolus of 10 mcg of hexoprenaline intravenously over 5 to 10 minutes. A bolus can be prepared by adding the contents of 1 ampoule (10 mcg of hexoprenaline) to isotonic saline or glucose solution to a total volume of 10 ml. If necessary, start a long-term dose with an infusion of 0.3 mcg of hexoprenaline per minute (see dosage for short-term treatment of premature contractions during contraction and/or dilatation of the cervix).

The infusion should be increased by 0.05 mcg/min. every 10 minutes and titrated against uterine activity and maternal pulse to achieve satisfactory tocolysis and maintain maternal heart rate less than 120 beats/min.

Duration of treatment

According to data, should not exceed 48 hours, since the main effect of tocolytic therapy is to delay labor up to 48 hours; no statistically significant effect on perinatal mortality or morbidity was observed in randomized controlled trials. This short-term delay can be used to implement other interventions designed to improve perinatal health.

Special precautions forinfusion

The dose should be adjusted on an individual basis, taking into account suppression of contractions, increased heart rate and changes in blood pressure, which are limiting factors. During treatment, these parameters must be carefully checked. The mother's maximum heart rate should not exceed 120 beats per minute. Careful monitoring of hydration levels is important to avoid the risk of maternal pulmonary edema. The volume of liquid in which the drug is prescribed should be kept to a minimum. Also need to use

infusion control device, preferably a syringe pump:

Contraindications

Hexoprenaline is contraindicated in the following cases:

Hypersensitivity to hexoprenaline or any of the excipients any condition at less than 22 weeks' gestation as a tocolytic agent for patients with pre-existing coronary artery disease or for patients with significant risk factors for developing it

coronary heart disease.

Threatened miscarriage during the 1st and 2nd trimester any condition of the mother or fetus in which prolongation of pregnancy is dangerous, for example, severe toxicosis, intrauterine infection, vaginal bleeding due to placenta previa, eclampsia or severe preeclampsia, placental abruption or umbilical cord compression intrauterine fetal death, a known fatal congenital or chromosomal abnormality leading to death, severe liver and kidney disease, glaucoma.

Hexoprenaline is contraindicated in any pre-existing medical conditions for which a beta mimetic would have an adverse effect, such as pulmonary hypertension and heart disease, such as hypertrophic obstructive cardiomyopathy, or any other type of left ventricular outflow tract obstruction, such as aortic stenosis .

Special instructions and special precautions for use

Treatment should be carried out in institutions adequately equipped to provide ongoing monitoring of the health of the mother and fetus.

If the membranes are ruptured or the cervix is ​​more than 4 cm dilated, tocolysis with beta-agonists is not recommended. In the case of tocolysis, hexoprenaline should be used with caution, and cardiorespiratory function and ECG monitoring should be monitored throughout treatment.

The following control measures should be taken at all times for the mother and, where possible/appropriate, for the fetus:

Blood pressure and heart rate - ECG Electrolyte and fluid balance - to monitor pulmonary edema Glucose and lactate levels - with special attention to those with diabetes Potassium levels - beta-agonists associated with decreased serum potassium, which increases the risk of arrhythmias ( see section 4.5).

Treatment should be discontinued if signs of myocardial ischemia (such as chest pain or ECG changes) develop.

Hexoprenaline should not be used as a tocolytic in patients with significant risk factors or suspected pre-existing heart disease (eg, tachyarrhythmia, heart failure, or valvular heart disease). For preterm labor in patients with known or suspected heart disease, the cardiologist should evaluate the use of hexoprenaline before intravenous infusion.

Pulmonary edema

Since pulmonary edema and myocardial ischemia have been reported during or after treatment of preterm labor with beta-agonists, fluid balance and cardiorespiratory function require special attention. Patients with predisposing factors, including multiple pregnancies, fluid retention, infection, and maternal preeclampsia, may be at increased risk of developing pulmonary edema.

Administration using a syringe pump, as opposed to intravenous infusion, will limit the risk of excess fluid. If signs of pulmonary edema or myocardial ischemia develop, discontinuation of treatment should be considered. It's special

concerns combination therapy with the use of corticosteroids and in the presence of concomitant diseases (renal diseases, edema, proteinuria, hypertension-preeclampsia).

Blood pressure and frequency heartbeat

Infusion of beta-agonists is usually accompanied by an increase in cardiac output. rhythm mothers approximately 20 to 50 beats per minute. The mother's pulse should be monitored, and the need to control such increases by dose reduction or discontinuation of the drug should be assessed on a case-by-case basis. In general, the mother's pulse should not exceed a steady rate of 120 beats per minute.

The patient's blood pressure may decrease slightly during the infusion; it will affect diastolic pressure more than systolic. The decrease in diastolic pressure occurs, as a rule, in the range from 10 to 20 mmHg. Art. The effect of the infusion on fetal heart rate is less noticeable, but an increase of up to 20 beats per minute may also occur. To minimize the risk of hypotension associated with tocolytic therapy, take particular care to avoid vein compression during the infusion process by keeping the patient in the right or left lateral decubitus position.

Beta-agonists have been associated with increased blood glucose levels. Therefore, in mothers with diabetes, blood glucose and lactate levels should be monitored and diabetes treatment adjusted accordingly to meet the needs of the diabetic mother during tocolysis.

If delivery occurs soon after treatment with hexoprenaline, the newborn baby should be monitored for signs of hypoglycemia, as hexoprenaline may lead to increases in maternal blood glucose and insulin, and for possible hyperacidity due to the potential passage of acidic metabolites across the placenta (lactate). , ketone acids).

Hyperthyroidism

Hexoprenaline should be prescribed with extreme caution to patients suffering from thyrotoxicosis, and only after a careful assessment of the benefits and risks of treatment.

Hypersensitivity to sympathomimetics

During tocolytic therapy with beta-adrenergic agents, the intensity of signs of already existing dystrophic myotonia may increase.

In selected patients with hypersensitivity to sympathomimetics, hexoprenaline should only be used in low, individually selected doses, and with particularly careful medical supervision.

Pyrosulfite contained in hexoprenaline injection solution or its concentrate for infusion solution rarely causes serious hypersensitivity reactions or bronchospasms.

Interaction with other drugs and other forms of interactions

Halogenated anesthetics

Due to the additive antihypertensive effect, sluggish uterine contractions may lead to bleeding; In addition, serious disturbances in ventricular rhythm due to increased cardiac reactivity have been reported during interactions with halogenated anesthetics.

If possible, treatment should be discontinued 6 hours before any planned anesthesia with halogenated anesthetics.

Corticosteroids

Systemic corticosteroids are often given during preterm labor to promote fetal lung development. Cases of pulmonary edema have occurred in women taking beta-agonists and corticosteroids concomitantly.

Corticosteroids are known to increase blood glucose and may decrease serum potassium and coadministration should be used cautiously and the patient should be monitored closely due to the increased risk of hypoglycemia and hypokalemia.

Antidiabetic drugs

Beta-agonists have been associated with increases in blood glucose levels, which may; be interpreted as a weakening of antidiabetic therapy, but this may require adjustment of individual antidiabetic therapy.

Potassium removal agents

Because of the hypokalemic effects of beta-agonists, it is known that coadministration of potassium-sparing agents increases the risk of hypokalemia, and agents such as diuretics, digoxin, methylxanthines, and corticosteroids should only be used after a careful assessment of benefits and risks, taking into account the increased risk of cardiac arrhythmias resulting from hypokalemia.

Other forms of interaction

Non-selective P-blockers reduce the effectiveness or completely neutralize the beta2 agonist effect of hexoprenaline.

Sodium lisulfite is a highly active component, therefore it is not recommended to mix Ginipral® with solutions other than 0.9% sodium chloride solution or 5% glucose (dextrose) solution.

Use during pregnancy and breastfeeding

The drug Ginipral® is not prescribed before the 20th week and after the 37th week of pregnancy, as well as during lactation (breastfeeding). Within the specified time frame, the drug is used according to indications (see section “Indications for use”).

Impact on the ability to drive vehicles and operate machinery

During the treatment period, care should be taken when driving vehicles and while engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Side effect

Classification of adverse adverse reactions (ADRs) by frequency of development:

Very common (>1/10); often (>1/100,<1/10); нечасто (>1/1000, <1/100); редко (>1/10000, <1/1000); очень редко (<1/10000); частота неизвестна (невозможно оценить на основе имеющихся данных).

The most common side effects of hexoprenaline are related to the pharmacological activity of the beta mimetics and may be limited or avoided by careful monitoring of hemodynamic parameters such as blood pressure and heart rate, and necessary dose adjustments. As a rule, they disappear after stopping therapy.

Endocrine system disorders

Frequency unknown: lipolysis;

Metabolic and nutritional disorders

Frequency unknown: * hypokalemia ; ,

Rarely: *hyperglycemia.

Nervous system disorders

Very common: muscle tremors;

Heart disorders

Very often: *tachycardia;

Often: * increased heart rate, * decreased diastolic blood pressure;

Rarely: *heart rhythm disturbances, for example, atrial fibrillation, myocardial ischemia; Frequency unknown: increased cardiac output, increased systolic pressure, slight changes in fetal heart rate, complaints of angina pectoris.

From the outside cardiovascular systems

Common: *hypotension

Rarely: *peripheral vasodilation.

Respiratory, thoracic and mediastinal disorders Frequency unknown: *pulmonary edema.

Gastrointestinal disorders

Rarely: nausea.

Skin and subcutaneous tissue disorders

Common: sweating;

Frequency unknown: redness of the skin.

Ginipral is a drug that reduces contractile activity and muscle tone of the uterus.

Release form and composition

Ginipral tablets are made containing the active substance - hexoprenaline sulfate - 500 mcg, as well as excipients: lactose hydrate, corn starch, disodium edetate dihydrate, copovidone, magnesium stearate, glycerol palmitate stearate, talc. Blisters contain 10 pieces.

Ginipral is prepared as a solution for intravenous administration, containing 10 mcg of hexoprenaline sulfate in 1 ampoule, as well as additional substances: water for injection, sodium chloride, sodium pyrosulfite, disodium edetate dihydrate, 2N sulfuric acid. In ampoules of 2 ml, 5 pieces per box.

Ginipral concentrate is prepared for the preparation of a solution for infusion, containing 25 mcg of hexoprenaline sulfate in 1 ml, as well as auxiliary components: deionized water, sodium chloride, sodium pyrosulfate, sulfuric acid, disodium edetate dihydrate. In packs of 5 ampoules.

Indications for use

According to the instructions, Ginipral solution and concentrate for preparing the solution are indicated for use in the following cases:

• Acute tocolysis: slowing of labor contractions during childbirth due to acute intrauterine asphyxia, umbilical cord prolapse, before turning the fetus from a transverse position, before cesarean section, complication of labor;
• Premature birth (as an emergency measure before taking the patient to the hospital);
• Massive tocolysis: suspension of premature labor if the woman in labor has a smoothed cervix and dilation of the uterine pharynx;
• Long-term tocolysis: frequent and intensified contractions without opening the uterine throat and smoothing the cervix (to prevent premature birth), immobilization of the uterus before, during and after cervical cerclage;

Ginipral tablets are prescribed when there is a threat of premature birth (mainly as a continuation of infusion treatment).

Contraindications

According to the instructions, Ginipral should not be taken in the following cases:

• Cardiac ischemia;
• Myocarditis;
• Thyrotoxicosis;
• Aortic stenosis, mitral valve disease;
• Tachyarrhythmias;
• Premature placental abruption, uterine bleeding;
• First trimester of pregnancy;
• Severe renal and/or liver dysfunction;
• High blood pressure;
• Angle-closure glaucoma;
• Breastfeeding period;
• Intrauterine infections;
• Hypersensitivity to the active or auxiliary components of the drug.

Directions for use and dosage

The dose of Ginpral solution is selected individually. The contents of the ampoule should be administered slowly intravenously over 5-10 minutes - after dilution with an isotonic NaCl solution.

For acute tocolysis, 1 ampoule (2 ml) of the drug is prescribed. If necessary, treatment is continued with infusions;

For massive tocolysis, treatment with the solution is prescribed in the amount of 1 ampoule, followed by infusion of Ginipral at a rate of 0.3 mcg per minute.

For long-term tocolysis, the drug is prescribed as a continuous drip infusion at a rate of 0.075 mcg per minute.

If the resumption of contractions does not occur within two days, the patient is transferred to taking Ginipral tablets.

Before use, the concentrate for preparing Ginipral solution should be diluted in 5 ml of distilled water so that the total concentration of the active substance is 5 mcg in 1 ml of solution.

The prepared solution is used parenterally, in the form of intravenous injections and infusions. The dosage of parenteral administration of Ginipral is determined individually, depending on the clinical symptoms.

Ginipral tablets are taken orally with a sufficient amount of liquid.

If there is a threat of premature birth, 1 tablet of Ginipral is prescribed 1-2 hours before the end of the infusion.

The medicine is taken 1 tablet every three hours, then 1 tablet every 4-6 hours. The daily dose of Ginipral should not exceed 4-8 tablets.

Side effects

The use of Ginipral may cause the following side effects:

• Cardiovascular system: decreased blood pressure, maternal tachycardia, cardiac arrhythmias, cardialgia;
• Central and peripheral nervous systems: anxiety, dizziness, finger tremor, headache;
• Digestive system: intestinal obstruction, nausea and vomiting, deterioration of intestinal motility, temporary increase in liver transaminases;
• Laboratory indicators: hypocalcemia, hypokalemia, increased plasma glucose levels;
• Allergies: bronchospasm, difficulty breathing, impaired consciousness, anaphylactic shock;
• Side effects of Ginipral in newborns: acidosis, hypoglycemia.

special instructions

During treatment with Ginipral, patients should monitor the functions of the cardiovascular system of the mother and fetus.

In case of hypersensitivity to sympathomimetics, it is recommended to prescribe Ginipral in small doses and under constant medical supervision.

If the mother experiences a pronounced increase in heart rate (more than 130 beats per minute) or a significant decrease in blood pressure, the dose of Ginipral should be reduced.

If signs of heart failure, pain in the heart area, or difficulty breathing appear, the use of Ginipral should be stopped immediately.

In women with diabetes mellitus, carbohydrate metabolism should be monitored during therapy with Ginipral, since the use of the drug may cause an increase in plasma glucose levels.

In some cases, the simultaneous use of Ginipral and glucocorticosteroids can cause pulmonary edema, especially in cases of impaired renal function. Therefore, the patient must be under regular medical supervision during treatment.

Analogs

Structural analogues of Ginipral are Ipradol and Hexoprenaline.

Drugs that have a similar pharmacological effect are: Partusisten, Salbutamol, Fenoterol, Magnesia.

Terms and conditions of storage

According to the instructions, Ginipral is stored in a dark, dry place out of reach of children. The shelf life of the solution and concentrate is 3 years, tablets – 5 years.

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INSTRUCTIONS

on medical use of the drug

Ginipral
(GYNIPRAL)

Compound:
active ingredient: hexoprenaline;
1 tablet contains 0.5 mg of hexoprenaline sulfate;
Excipients: lactose, corn starch, previously latinized starch, copovidone, Trilon B (trilon B), talc, glycerol distearate, magnesium stearate.

Dosage form. Pills.

Pharmacotherapeutic group.

Products for use in gynecology. Sympathomimetics that suppress uterine contractility. ATC code G02С A 05.

Indications.

Threat of premature birth (primarily as a continuation of other fusion therapies).

Contraindications.

Hypersensitivity to the components of the drug, increased sensitivity to sulfites; thyrotoxicosis; cardiovascular diseases, coronary heart disease, arterial hypertension, cardiac arrhythmias occurring with tachycardia, myocarditis, mitral valve disease and idiopathic hypertrophic subaortic stenosis; severe liver and kidney diseases; closed angle glaucoma; uterine bleeding, premature placental abruption; internal uterine infections.

Directions for use and doses

Use orally. The tablets are swallowed whole with water.
1-2 hours before stopping the Ginipral infusion, start taking tablets.
Take 1 tablet every 3 hours first, then every 4-6 hours
(From 4 to 8 Ginipral tablets per day).

Adverse reactions

Ginipral is usually well tolerated by patients.
While taking Ginipral, headache, anxiety, slight tremor of the fingers, sweating, palpitation, tachycardia, dizziness, and in rare cases, nausea and vomiting may develop.
Sometimes there may be redness of the skin.
There may be a slight increase in heart rate (HR), a decrease in blood pressure, especially diastolic.
Isolated cases of heart rhythm disturbances (ventricular extrasystole) and complaints of chest pain were recorded. These symptoms disappear quickly after stopping the drug.
Blood sugar levels, especially in diabetes, increase due to the glycogen-lytic effect of the drug.
Diuresis decreases, especially at the beginning of treatment. Sometimes there was a temporary decrease in potassium levels (at the beginning of treatment) and an increase in the concentration of transaminases in the blood serum.
During treatment with Ginipral, the intensity of intestinal motility may decrease. In rare cases, intestinal atony was observed (control of stool regularity is necessary).
In newborns, hypoglycemia and acidosis, bronchospasm, and anaphylactic shock may occur.

Overdose.

Symptoms: severe tachycardia, tremor, headache, dizziness, increased sweating, arrhythmia, anxiety, cardialgia, decreased blood pressure, shortness of breath.
Treatments. Usually, reducing the dosage of the drug is sufficient to eliminate side effects. To eliminate severe symptoms, it is recommended to use non-selective beta-blockers, which completely neutralize the effect of Ginipral.

Use during pregnancy or breastfeeding.

Ginipral is prescribed for use during pregnancy (see section "Indications").
The drug is not prescribed for use during breastfeeding.

Children. The drug is not used for children.

Features of application. During treatment, blood pressure, pulse, cardiac activity, and fetal heartbeat should be constantly monitored.
Patients with hypersensitivity to sympathomimetics should use Ginipral in small doses prescribed individually, under constant medical supervision.
If there is a significant increase in the mother's heart rate (more than 130 beats/min) and/or a significant decrease in blood pressure, the dose should be reduced; if there are complaints of difficulty breathing, pain in the heart and if signs of heart failure appear, the use of the drug should be discontinued.
When treating patients with diabetes, it is necessary to monitor carbohydrate metabolism, since the use of Ginipral, especially at the initial stage of treatment, can cause an increase in blood sugar.
If childbirth occurs immediately after a course of treatment with Ginipral, it is necessary to take into account the possibility of hypoglycemia and acidosis in newborns due to the penetration of acidic metabolic products (lactic and ketone compounds).
When using the drug, diuresis decreases, so it is necessary to control vata for symptoms associated with fluid retention in the body.
In some cases, simultaneous use of corticosteroids during drug infusions can cause pulmonary edema. This is especially important in combined treatment with corticosteroids in patients with concomitant diseases that lead to fluid retention (kidney disease, early toxicosis of pregnancy).
Before starting tocolytic therapy, it is necessary to take potassium supplements, since with hypokalemia the effect of sympathomimetics on the myocardium is enhanced.
The simultaneous use of certain narcotic drugs (for example, halothane) and sympathomimetics can lead to cardiac arrhythmias; co-administration with these drugs should be prevented.
With prolonged tocolytic therapy, it is necessary to monitor the condition of the fetoplacental complex and ensure that there is no placental abruption. Clinical symptoms of premature placental abruption can be smoothed out with tocolytic therapy.
When the membranes rupture and when the cervix is ​​dilated by more than 2-3 cm, the effectiveness of tocolytic therapy is low.
During tocolytic treatment with beta-agonists, the symptoms of concomitant dystrophic myotonia may increase. In such cases, the use of diphenylhydantoin (phenytoin) drugs is recommended.
Patients with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not use the drug.
During tocolytic treatment, it is necessary to control the release of the intestines.
Coffee and tea may increase the side effects of Ginipral.

The ability to influence the reaction speed when driving vehicles or other mechanisms.

Some adverse reactions from the central nervous system in individual cases may affect the ability to drive vehicles or operate machinery.

Interaction with other drugs and other types of interactions.

Non-selective beta-blockers weaken or neutralize the effect of Ginipral.
Methylxanthine (for example, theophylline) enhances the effect of Ginipral.
The intensity of glycogen accumulation in the liver caused by the use of GCS is reduced under the influence of Ginipral.
The effect of oral hypoglycemic agents during therapy with Ginipral is weakened.
Concomitant treatment with certain sympathomimetic drugs (cardiovascular and anti-asthmatic drugs) should not be carried out, since the effect of the drugs on the cardiovascular system is enhanced and the risk of adverse reactions due to overdose increases.
Ginipral should not be used in conjunction with drugs containing ergot alkaloids, as well as with drugs containing calcium, vitamin D, dihydrotachysterol and mineralcorticoids, as well as with MAO inhibitors, tricyclic antidepressants.
General anesthesia (fluorotane) and adrenergic stimulants increase side effects on the cardiovascular system.

Pharmacological properties.

Pharmacological

Ginipral is a selective beta-2 sympathomimetic that relaxes the uterine muscles. Under the influence of Ginipral, the frequency and intensity of uterine contractions decreases. The drug suppresses spontaneous and oxytocin-induced labor contractions. During childbirth, it normalizes very strong or irregular contractions. Under the influence of Ginipral, premature contractions stop in most cases, which makes it possible to prolong pregnancy until the normal due date. Suppression of labor contractions is observed immediately after intravenous administration of the drug and lasts approximately 20 minutes. The effect of the drug is prolonged after subsequent drip administration of the drug. Due to its beta-2 selectivity, Ginipral has a slight effect on cardiac activity and blood flow in the pregnant woman and fetus.

Pharmacokinetics

The drug consists of two catecholamine groups, which in the human body undergo a methylation process due to catecholamine-O-methyltransferase. While the action of isoprenaline is almost completely abolished by the introduction of one methyl group, hexoprenaline becomes biologically inactive only if both of its catecholamine groups are methylated. This property, as well as the high ability of Ginipral to adhesive on the surface, is considered the reason for its long-lasting action.
When using hexoprenaline, during the first 4 hours, 80% of the active substances are excreted in the urine unchanged, that is, in the form of free hexoprenaline and monomethyl derivative. After this, the excretion of dimethyl derivative and related compounds (glucuronide and sulfate) increases. A small part is excreted in the bile in the form of complex metabolites.

Pharmaceutical characteristics.

Basic physical and chemical properties: white, round, biconvex.

Best before date. 5 years.

Storage conditions. Store at a temperature not exceeding 25 º C in a place protected from light and out of reach of children.

Package. 10 tablets in a blister. 2 blisters in a cardboard box.