Ginipral: instructions for use. Ginipral instructions for use, contraindications, side effects, reviews European name of the analogue ginipral

Selective beta2-adrenomimetic, reduces the tone and contractile activity of the myometrium.
Drug: GINIPRAL®

Active substance of the drug: hexoprenaline
ATX coding: R03CC05
KFG: A drug that reduces the tone and contractile activity of the myometrium
Registration number: P No. 015664/03
Registration date: 09/07/07
Owner reg. credential: NYCOMED AUSTRIA GmbH (Austria)

Ginipral release form, drug packaging and composition.

The tablets are white, round, biconvex. 1 tab. hexoprenaline sulfate 500 mcg
Excipients: corn starch, lactose hydrate (80 mg), copovidone, disodium edetate dihydrate, talc, magnesium stearate, glycerol palmitate stearate.
10 pieces. - blisters (2) - cardboard boxes.
The solution for intravenous administration is transparent, colorless. 1 ml 1 amp. hexoprenaline sulfate 5 mcg 10 mcg
Excipients: sodium pyrosulfite, disodium edetate dihydrate, sodium chloride, sulfuric acid 2N (to maintain pH level), water for injection.
2 ml - ampoules (5) - plastic trays (1) - cardboard boxes.
2 ml - ampoules (5) - plastic trays (5) - cardboard boxes.
The concentrate for the preparation of solution for infusion is transparent, colorless. 1 ml 1 amp. hexoprenaline sulfate 5 mcg 25 mcg
5 ml - ampoules (5) - plastic trays (1) - cardboard boxes.

The description of the drug is based on the officially approved instructions for use.

Pharmacological action Ginipral

Selective beta2-adrenomimetic, reduces the tone and contractile activity of the myometrium. Reduces the frequency and intensity of uterine contractions, suppresses spontaneous and oxytocin-induced labor contractions. During childbirth, it normalizes excessively strong or irregular contractions.
Under the influence of the drug, premature contractions in most cases stop, which allows you to prolong pregnancy until the normal due date.
Due to its 2-selectivity, the drug has little effect on the cardiac activity and blood flow of the pregnant woman and the fetus.

Pharmacokinetics of the drug.

Suction
Hexoprenaline is well absorbed after oral administration.
Metabolism
The drug consists of two catecholamine groups, which are methylated by catecholamine-O-methyltransferase. Hexoprenaline becomes biologically inactive only if both catecholamine groups are methylated. This property, as well as the drug’s high ability to adhere to surfaces, are considered the reasons for its long-lasting effect.
Removal
It is excreted mainly in the urine unchanged and in the form of metabolites. During the first 4 hours after administration of the drug, 80% of the administered dose is excreted in the urine in the form of free hexoprenaline and monomethyl metabolite. Then the excretion of dimethyl metabolite and conjugated compounds (glucuronide and sulfate) increases. A small part is excreted in the bile in the form of complex metabolites.

Indications for use:

For solution
Acute tocolysis
- inhibition of labor contractions during childbirth with acute intrauterine asphyxia, with immobilization of the uterus before cesarean section, before turning the fetus from a transverse position, with umbilical cord prolapse, with complicated labor;
- an emergency measure in case of premature birth before delivering the pregnant woman to the hospital.
Massive tocolysis
- inhibition of premature labor contractions in the presence of a smoothed cervix and/or dilatation of the uterine pharynx.
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.
For tablets
- threat of premature birth (primarily as a continuation of infusion therapy).

Dosage and method of administration of the drug.

For solution
The contents of the ampoule must be administered intravenously slowly over 5-10 minutes using automatically dosing infusion pumps or using conventional infusion systems - after diluting with isotonic sodium chloride solution to 10 ml. The dose of the drug should be selected individually.
For acute tocolysis, the drug is prescribed in a dose of 10 mcg (1 amp. 2 ml). In the future, if necessary, treatment can be continued with infusions.
In case of massive tocolysis, administration of the drug begins with 10 mcg (1 amp. 2 ml), followed by infusion of Ginipral at a rate of 0.3 mcg/min. As an alternative treatment, it is possible to use only infusions of the drug at a rate of 0.3 mcg/min without prior bolus administration of the drug.
For long-term tocolysis, the drug is prescribed as a long-term drip infusion at a rate of 0.075 mcg/min.
If contractions do not resume within 48 hours, treatment with Ginipral 500 mcg tablets should be continued.
For tablets
The tablets should be taken with a small amount of water.
If there is a threat of premature birth, the drug is prescribed in a dose of 500 mcg (1 tablet) 1-2 hours before the end of the Ginipral infusion.
The drug should be taken 1 tablet first. every 3 hours, and then every 4-6 hours. The daily dose is 2-4 mg (4-8 tablets).

Side effects of Ginipral:

From the central nervous system and peripheral nervous system: headache, dizziness, anxiety, mild tremor of the fingers.
From the cardiovascular system: tachycardia in the mother (heart rate in the fetus in most cases remains unchanged), arterial hypotension (mainly diastolic); rarely - rhythm disturbances (ventricular extrasystole), cardialgia (quickly disappear after discontinuation of the drug).
From the digestive system: rarely - nausea, vomiting, inhibition of intestinal motility, intestinal obstruction (it is recommended to monitor bowel regularity), temporary increase in transaminase levels.
Allergic reactions: difficulty breathing, bronchospasm, impaired consciousness up to coma, anaphylactic shock (in patients with bronchial asthma or patients with hypersensitivity to sulfites).
Laboratory indicators: hypokalemia, hypocalcemia at the beginning of therapy, increased plasma glucose levels.
Other: increased sweating, oliguria, edema (especially in patients with kidney disease).
Side effects in newborns: hypoglycemia, acidosis.

Contraindications to the drug:

Thyrotoxicosis;
- tachyarrhythmias;
- myocarditis;
- mitral valve disease and aortic stenosis;
- IHD;
- arterial hypertension;
- severe liver and kidney diseases;
- angle-closure glaucoma;
- uterine bleeding, premature placental abruption;
- intrauterine infections;
- pregnancy first trimester;
- lactation (breastfeeding);
- hypersensitivity to the components of the drug (especially in patients with bronchial asthma and a history of hypersensitivity to sulfites).

Use during pregnancy and lactation.

The drug is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding). In the second and third trimesters of pregnancy, the drug is used according to indications.

Special instructions for the use of Ginipral.

During the period of use of Ginipral, it is recommended to carefully monitor the functions of the cardiovascular system (heart rate, blood pressure) of the mother and fetus. It is recommended to record an ECG before and during treatment.
Patients with hypersensitivity to sympathomimetics should be prescribed Ginipral in small doses, selected individually, under constant medical supervision.
If there is a significant increase in the mother's heart rate (more than 130 beats/min) and/or with a significant decrease in blood pressure, the dose of the drug should be reduced.
If difficulty breathing, pain in the heart, or signs of heart failure occur, the use of Ginipral should be stopped immediately.
The use of Ginipral may cause an increase in glucose in the blood plasma (especially during the initial period of treatment), so carbohydrate metabolism should be monitored in mothers with diabetes. If childbirth occurs immediately after a course of treatment with Ginipral, it is necessary to consider the possibility of hypoglycemia and acidosis in newborns due to transplacental penetration of lactic and ketone acids.
When using Ginipral, diuresis decreases, so you should carefully monitor symptoms associated with fluid retention in the body.
In some cases, simultaneous use of GCS during Ginipral infusions may cause pulmonary edema. Therefore, during infusion therapy, constant careful clinical monitoring of patients is necessary. This is especially important in the combined treatment of GCS in patients with kidney disease. Strict limitation of excess fluid intake is necessary. The risk of possible development of pulmonary edema requires limiting the volume of infusions as much as possible, as well as using dilution solutions that do not contain electrolytes. You should limit your salt intake from food.
It is recommended to monitor the regularity of bowel movements during the period of use of the drug.
Before starting tocolytic therapy, it is necessary to take potassium supplements, because with hypokalemia, the effect of sympathomimetics on the myocardium is enhanced.
The simultaneous use of general anesthesia (halothane) and sympathomimetics can lead to cardiac arrhythmias. Ginipral should be discontinued before using halothane.
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 therapy with the use of beta-agonists, the symptoms of concomitant dystrophic myotonia may intensify. In such cases, the use of diphenylhydantoin (phenytoin) drugs is recommended.
When using the drug in the form of tablets with tea or coffee, the side effects of Ginipral may increase.

Drug overdose:

Symptoms: severe tachycardia in the mother, arrhythmia, finger tremor, headaches, increased sweating, anxiety, cardialgia, decreased blood pressure, shortness of breath.
Treatment: use of Ginipral antagonists - non-selective beta-blockers that completely neutralize the effect of the drug.

Interaction of Ginipral with other drugs.

When used together with beta-blockers, the effect of Ginipral is weakened or neutralized.
When used together with methylxanthines (including theophylline), the effectiveness of Ginipral is enhanced.
When Ginipral is used together with GCS, the intensity of glycogen accumulation in the liver decreases.
When used together, Ginipral weakens the effect of oral hypoglycemic drugs.
When Ginipral is used together with other drugs with sympathomimetic activity (cardiovascular and bronchodilator drugs), the effect of the drugs on the cardiovascular system may be enhanced and symptoms of overdose may appear.
When used together with ftorotan and beta-agonists, the side effects of Ginipral on the cardiovascular system increase.
Ginipral is incompatible with ergot alkaloids, MAO inhibitors, tricyclic antidepressants, as well as with drugs containing calcium and vitamin D, dihydrotachysterol and mineralocorticoids.
Sulfite is a highly active component, so you should refrain from mixing Ginipral with solutions other than isotonic sodium chloride solution and 5% dextrose (glucose) solution.

Terms of sale in pharmacies.

The drug is available with a prescription.

Terms of storage conditions for the drug Ginipral.

List B. The drug should be stored in a place protected from light, out of reach of children at a temperature of 18° to 25°C. The shelf life of the solution for intravenous administration is 3 years. The shelf life of the tablets is 5 years.

Instructions for use of the drug for specialists

Ginipral®

Tradename

Ginipral®

International nonproprietary name

Hexoprenoline

Dosage form

Tablets 0.5 mg

Solution for intravenous administration 10 mcg/2.0 ml

Concentrate for solution for infusion 25 mcg/5.0 ml

One tablet contains

active substance - hexoprenaline sulfate 0.5 mg,

excipients: corn starch, lactose hydrate, copovidone, disodium edetate dihydrate, talc, magnesium stearate, glycerol palmitostearate.

1 ml of solution for intravenous administration contains

1 ml of concentrate for preparing the solution contains

active substance - hexaprenaline sulfate 5 mcg,

excipients: sodium pyrosulfite, sodium chloride, disodium edetate dihydrate, sulfuric acid to optimize pH, water for injection

Description

The tablets are white, round, biconvex.

Solution for intravenous administration and concentrate for preparation of solution for infusion - a clear, colorless solution.

Pharmacotherapeutic group

Other drugs for the treatment of gynecological diseases. Tocolytic drugs-sympathomimetics.

PBX code G02CA

Pharmacological properties

Pharmacokinetics

Ginipral® consists of two catecholamine groups, which in the human body undergo a methylation process through catecholamine-O-methyltransferase. While the effect of isoprenaline is almost completely stopped with 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.

After oral administration, hexoprenaline is well absorbed from the gastrointestinal tract.

After intravenous administration, 80% of unchanged hexoprenaline and its monomethyl derivative are excreted in the urine within 4 hours. Excretion of dimethyl derivative and conjugated compounds (glucuronide and sulfate) occurs in a smaller volume and somewhat later. A small part is excreted in the bile in the form of complex metabolites. After oral administration, part of the dose is excreted in the urine as a dimethylated metabolite.

Pharmacodynamics

Ginipral® is a b 2-sympathomimetic agent 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 allows you to maintain pregnancy until the normal due date. Due to its b 2-selectivity, Ginipral® has a slight effect on cardiac activity and blood flow in both the pregnant woman and the fetus.

Indications for use

For intravenous injections and infusions:

acute tocolysis: inhibition of labor contractions during childbirth with acute intrauterine asphyxia (fetal distress), immobilization of the uterus before cesarean section, before turning the fetus from a transverse position, with umbilical cord prolapse, with complicated labor

emergency measures for premature birth outside the hospital, before delivering the pregnant woman to the hospital

massive tocolysis: inhibition of premature labor contractions in the presence of a smoothed cervix and/or dilatation of the uterine pharynx

long-term tocolysis: prevention of premature labor due to intensified or frequent contractions without contraction or dilatation of the uterine os

immobilization of the uterus before, during and after Cerclage surgery

For oral administration:

threat of premature birth (primarily as a continuation of infusion therapy).

Directions for use and doses

Ginipral® 0.5 mg tablets should be taken with a small amount of water. In the absence of other recommendations, the indicated dosage should be strictly followed.

If there is a threat of premature birth: 1-2 hours before the end of the Ginipral® infusion, start taking Ginipral® tablets. Take 1 tablet every 3 hours first, and then every 4-6 hours.

Solution for intravenous administration and concentrate for the preparation of solution for infusion Ginipral®.

The contents of the 10 mcg ampoule must be administered slowly (over 5-10 minutes), either using a mechanical injector, or, if this is not possible, after dilution with an isotonic sodium chloride solution or 5% glucose solution.

Acute tocolysis

10 mcg of Ginipral®, diluted in 10 ml of sodium chloride solution or 5% glucose solution, is administered slowly intravenously over 5-10 minutes. If necessary, continue administration by intravenous infusion at a rate of 0.3 mcg/min (see massive tocolysis).

Massive tocolysis

Initially, 10 mcg slowly intravenously, followed by intravenous infusion at a rate of 0.3 mcg/min. The drug can be administered at a rate of 0.3 mcg/min without prior intravenous injection.

The dose calculation of 0.3 mcg/min corresponds to:

When using automatically dosing infusion pumps (syringe dispensers for infusion therapy), 75 mcg of concentrate for infusion (3 ampoules) is diluted with an isotonic solution of sodium chloride or 5% glucose solution to 50 ml; infusion rate 0.3 mcg/min.

The maximum daily dose is 430 mcg/day (exceeding the dose is possible only in exceptional cases).

Rules for preparing the infusion solution: the infusion concentrate is diluted with 500 ml of isotonic sodium chloride solution or 5% glucose solution. The prepared solution is administered intravenously, 20 drops = 1 ml.

The dose calculation of 0.075 mcg/ml corresponds to:

When using automatically dosing infusion pumps (syringe dispensers for infusion therapy), 75 mcg of concentrate for infusion (3 ampoules) is diluted with an isotonic solution of sodium chloride or 5% glucose solution to 50 ml; infusion rate 0.075 mcg/min.

If contractions do not resume within 48 hours, Ginipral® can be administered orally in tablet form, a single dose of 0.5 mg.

Side effects

dizziness, anxiety, slight tremor of fingers, sweating, headache

nausea, vomiting, decreased intensity of intestinal motility, intestinal atony

tachycardia, decreased blood pressure, especially diastolic, cardiac arrhythmias, pain in the heart area

difficulty breathing

increased blood sugar levels, especially in diabetes, increases due to the glycogenolytic effect of the drug, decreased potassium concentration in the blood

decreased diuresis, especially in the initial stage of treatment

bronchospasm, anaphylactic shock

Contraindications

hypersensitivity to one of the components of the drug

hyperthyroidism

heart rhythm disturbances, myocarditis, mitral stenosis/insufficiency

valve, aortic stenosis

severe liver and kidney diseases

angle-closure glaucoma

uterine bleeding (premature placental abruption)

intrauterine infections

I trimester of pregnancy

lactation period

Drug interactions

Non-selective β-blockers weaken the effect of Ginipral® or neutralize it.

With simultaneous use of methylxanthines, including theophylline, the effect of Ginipral® is enhanced.

Excessive accumulation of glycogen in the liver, caused by the use of glucocorticoids, is reduced by the action of Ginipral®.

Ginipral® weakens the insulin effect of antidiabetic drugs. The simultaneous use of Ginipral® with sympathomimetics used to treat bronchial asthma (Berotec, Salbutamol, Beclazone and others) or sympathomimetics for systemic use (Ephedrine, Isoprenaline and others) should be avoided, as this may cause increased cardiac activity and lead to overdose.

With the simultaneous use of sympathomimetics and halothane, the development of heart rhythm disturbances is possible.

special instructions

When using Ginipral®, you should monitor the blood pressure and pulse of the mother, as well as the fetal heartbeat. ECG monitoring before and during treatment is recommended.

Patients with diabetes need to regularly monitor their blood sugar levels.

Patients with hypersensitivity to sympathomimetics should take Ginipral® in small doses determined individually.

If there is a significant increase in the mother's heart rate (more than 130 beats/min) and a significant decrease in blood pressure, the dose should be reduced.

If there are complaints of difficulty breathing, pain in the heart and signs of heart failure, the use of Ginipral® should be stopped immediately.

Pregnant women suffering from diabetes mellitus should monitor carbohydrate metabolism, because the use of Ginipral®, especially in the initial stages of treatment, may cause an increase in blood sugar levels.

In some cases, the use of corticosteroids during infusions of Ginipral® may cause pulmonary edema. Therefore, during infusion therapy, careful continuous clinical monitoring of the patient is necessary. This is especially important in combined treatment with corticosteroids and Ginipral® in the presence of concomitant diseases accompanied by fluid retention in the body (kidney disease, gestosis). Excessive fluid intake should be avoided, not exceeding the daily infusion volume of 1500 ml. Limit salt intake in food.

Before starting tocolytic therapy, it is necessary to take potassium supplements because with hypokalemia, the effect of sympathomimetics on the myocardium is enhanced.

Taking Ginipral® must be stopped before anesthesia using halothane.

With prolonged tocolytic therapy, it is necessary to ensure that there is no placental abruption. Clinical symptoms of premature placental abruption can be smoothed out with tocolytic therapy. When the fetal bladder ruptures and when the cervix is ​​dilated by more than 2-3 cm, the effectiveness of tocolytic therapy is low.

When conducting tocolytic therapy with the use of β-adrenergic agonists, it is possible to increase the symptoms of concomitant dystrophic myotonia. In such cases, the use of diphenylhydantoin (phenytoin) is recommended.

Pregnancy and lactation

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 transplacental penetration of acidic metabolic products (lactic and ketonic acids).

Overdose

Symptoms: marked increase in maternal heart rate, tremors, headache, increased sweating.

Treatment: reducing the dose of the drug; to eliminate severe manifestations of drug overdose, it is necessary to use Ginipral® antagonists - non-selective beta-adrenolytic drugs that completely neutralize the effect of Ginipral®.

Release form

Pills

Primary packaging - 10 tablets in blister pack No. 2

Solution for intravenous administration

Primary packaging - ampoules of 2 ml No. 5

Secondary packaging - cardboard box

Concentrate for the preparation of solution for infusion

Primary packaging - ampoules of 5 ml No. 5

Secondary packaging - cardboard box.

Storage conditions

Store at a temperature of +18ºС - + 25ºС, in a place protected from direct sunlight.

Keep out of the reach of children!

Best before date

Tablets - 5 years

Solution for intravenous administration and concentrate for infusion - 3 years

Do not use after expiration date

Conditions for dispensing from pharmacies

On prescription

Manufacturer

Nycomed Austria GmbH, Austria

Representative office in the Republic of Kazakhstan "NycomedOsteuropa Marketing Service GmbH",

Begalina136 A, tel. 2444 004, fax 2444 005

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Dosage form:  solution for intravenous administration 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 beta2-adrenergic agonist ATX:  

R.03.C.C.05 Hexoprenaline

Pharmacodynamics:

Selectively stimulates beta 2 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 (Ca 2+) 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 beta2-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 muscle, 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 (T 1/2) 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 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:

Tocolytic therapy (drug relaxation of the uterine muscles) from the 20th week of pregnancy.

- Acute tocolysis- rapid suppression of contractions during childbirth in case of acute intrauterine asphyxia (fetal distress), in case of umbilical cord prolapse; in preparation for a caesarean section (to relieve uterine hypertonicity before transferring the pregnant woman to the operating room); complicated labor (hypertensive, uncoordinated or prolonged uterine contractions, difficult labor due to abnormal position or presentation of the fetus); when performing external rotation of the fetus when its position is incorrect. As an emergency measure in case of premature birth before delivering the pregnant woman to the hospital.

- Massive tocolysis- inhibition of premature contractions in the presence of a smoothed cervix and/or dilatation of the cervix.

- Long-term tocolysis- prevention of premature birth with intensified or frequent contractions without cervical effacement or cervical dilatation; relaxation of the uterus before, during and after cerclage application.

Contraindications:

Hypersensitivity to the components of the drug. Since the drug contains sulfite, Ginipral® solution for intravenous administration should not be used to treat patients with sulfite bronchial asthma;

Thyrotoxicosis;

Heart disease (including a history);

Arterial hypertension;

Severe liver and kidney diseases;

Angle-closure glaucoma;

Bleeding from the vagina of any etiology;

Intrauterine infections.

Carefully:Hypersensitivity to adrenomimetics, arterial hypotension, diabetes mellitus, dystrophic myotonia, intestinal atony, simultaneous treatment with glucocorticosteroids, concomitant diseases accompanied by edema, bronchial asthma. Pregnancy and lactation:

The drug Ginipral® is not prescribed until the 20th week of pregnancy and during lactation (breastfeeding) (see section "Indications for use").

From the 20th week of pregnancy, the drug is used according to indications.

Directions for use and dosage:Instructions for using ampoules with a breaking point:

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.

1. Acute tocolysis

10 mcg (1 ampoule of 2 ml). The contents of the ampoule are administered intravenously slowly (over 5-10 minutes) using an automatically dosing infusion pump or intravenously in a slow stream, diluting the drug to 10 ml with an isotonic sodium chloride solution.

In the future, if necessary, treatment can be continued with an infusion at a rate of 0.3 mcg/min (see paragraph 2 “Massive tocolysis”).

2. Massive tocolysis

At the beginning, treatment begins with a slow bolus injection of 10 mcg (1 ampoule of 2 ml), followed by an infusion of Ginipral® at a rate of 0.3 mcg/min.

As an alternative treatment, it is possible to use only an infusion of the drug Ginipral® at a rate of 0.3 mcg/min, without prior bolus administration of the drug.

Dose calculation.

0.3 µg/min corresponds to:

2 (20 mcg) 150 drops/min

3 (30 mcg) 100 drops/min

5 (50 mcg) 60 drops/min

6 (60 mcg) 50 drops/min

10 (100 mcg) 30 drops/min

For administration using automatically dosing infusion pumps, the drug is diluted with 0.9% sodium chloride solution or 5% glucose (dextrose) solution to 50 ml.

The daily dose of 430 mcg may only be exceeded in exceptional cases.

3. Long-term tocolysis

When administered using standard infusion systems (20 drops = 1 ml), the drug is dissolved in 500 ml of 0.9% sodium chloride solution or 5% glucose solution (dextrose).

Dosage calculation.

0.075 µg/min corresponds to:

Number of ampoules Rate of intravenous administration

3 (30 mcg) 25 drops/min

5 (50 mcg) 15 drops/min

When administered using automatically dosing infusion pumps, the drug is diluted with 0.9% sodium chloride solution or 5% glucose (dextrose) solution to 50 ml.

If contractions do not resume within 48 hours, treatment can be continued with Ginipral® 0.5 mg tablets (see appropriate instructions for use).

The indicated dose can only be used as a guide; during tocolysis it must be adjusted individually.

A solution of the drug Ginipral® in 0.9% sodium chloride solution or 5% glucose (dextrose) solution is prepared immediately before using infusion therapy.

During the period of tocolytic therapy, the volume of fluid entering the body (including oral administration) should not exceed 1500 ml per day. In this regard, it is preferable to administer the drug using automatically dosing infusion pumps.

Side effects:

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).

Endocrine system disorders

Frequency unknown: hyperglycemia, lipolysis, temporary increase in the activity of “liver” transaminases in the blood serum.

Metabolic and nutritional disorders

Frequency unknown: hypokalemia at the beginning of therapy (later the potassium level normalizes).

Nervous system disorders

Very common: muscle tremors.

Frequency unknown: headache, anxiety, dizziness.

Heart disorders

Rarely: ventricular extrasystole, paroxysmal atrial tachycardia.

Frequency unknown: tachycardia, palpitations, increased cardiac output, decreased peripheral vascular resistance, increased systolic pressure and decreased diastolic pressure leading to increased pulse pressure, cardialgia; angina pectoris, myocardial ischemia.

Respiratory, thoracic and mediastinal disorders

Frequency unknown: pulmonary edema.

Gastrointestinal disorders

Rarely: nausea.

Frequency unknown: vomiting, intestinal atony.

Skin and subcutaneous tissue disorders

Common: increased sweating.

Frequency unknown: redness of the skin.

Immune system disorders

Frequency unknown: hypersensitivity to sulfite.

Renal and urinary tract disorders

Frequency unknown: decreased diuresis (especially in the initial phase of treatment).

Fetal disorders

Frequency unknown: slight changes in heart rate. Disorders in newborns

Frequency unknown: hypoglycemia, acidosis, anaphylactic shock, bronchospasm.

Overdose:

Symptoms: tachycardia, tremor, anxiety, dizziness, increased sweating, arrhythmia, headaches, cardialgia, decreased blood pressure (BP), shortness of breath.

Treatment: symptomatic therapy. Non-selective beta-blockers are recommended as antidotes, which completely neutralize the effect of the drug Ginipral®, however, it is necessary to take into account the possibility of developing bronchospasm in patients with bronchial asthma.

Interaction:

Non-selective beta-blockers weaken or neutralize the effect of Ginipral®.

Ginipral® weakens the effect of oral hypoglycemic drugs. Some non-selective adrenergic agonists (including) and betag-adrenergic agonists, halogen-containing drugs for general anesthesia (for example,) increase the side effects of the drug Ginipral® on the cardiovascular system.

Concomitant use with non-potassium-sparing diuretics may cause hypokalemia and arrhythmia.

Ginipral® should not be used together with monoamine oxidase inhibitors, tricyclic antidepressants, with drugs containing calcium and vitamin D. Combined use with dihydrotahysterol, ergot alkaloids or mineralocorticoids may increase the hemodynamic effect of hexoprenaline.

Sodium disulfite 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.

Special instructions:

Patients with hypersensitivity to adrenomimetics should use Ginipral® in reduced doses prescribed individually, under constant medical supervision.

Before starting treatment with Ginipral®, it is necessary to conduct an ECG monitoring.

During treatment with Ginipral®, regular monitoring of ECG, respiratory rate, pulse and blood pressure in the mother, and fetal heart rate is necessary.

If the mother's heart rate increases (more than 130 beats/min) or if there are significant fluctuations in blood pressure, the dose of the drug should be reduced.

If signs of myocardial ischemia appear (pain in the heart, changes in the ECG), Ginipral® is immediately discontinued.

Initial hypokalemia should be corrected with potassium supplements before initiating tocolytic therapy.

If birth occurs immediately after treatment with Ginipral®, newborns should be examined for hypoglycemia and acidosis (blood pH).

In patients with diabetes mellitus, during treatment with Ginipral® it is necessary to regularly monitor the concentration of glucose in the blood plasma.

Clinical signs of premature placental abruption during tocolytic therapy with Ginipral® may be less pronounced.

With long-term tocolytic therapy, it is necessary to check the state of the fetoplacental system using standard research methods.

In the case of premature rupture of membranes when the cervix is ​​dilated more than 2-3 cm, prolongation of pregnancy with tocolytic therapy is unlikely.

During treatment with Ginipral®, it is necessary to avoid excessive fluid intake, since diuresis decreases under the influence of the drug. Symptoms reflecting fluid retention in the body (swelling of the legs, difficulty breathing) should be closely monitored, especially during concomitant treatment with glucocorticosteroids and with concomitant diseases that contribute to fluid retention (kidney disease, gestosis, proteinuria and hypertension). Given the risk of developing pulmonary edema, only solutions that do not contain electrolytes should be used, and the volume of infusion solutions administered should also be limited.

Ginipral contains hexoprenaline as the main active ingredient. This compound belongs to the pharmaceutical group of selective β-2-adrenergic agonists. It is produced in two forms: tablets and solution for parenteral use.

Ginipral tablets contain 500 mcg of hexoprenaline. Ginipral solution is produced in ampoules of 2 ml. They contain 10 mcg of hexoprenaline.

pharmachologic effect

Ginipral stimulates type 2 adrenaline beta receptors. A large number of them are located in the uterus. When they are activated, a tocolytic effect is realized. The contractility of the uterus decreases due to relaxation of the smooth muscles of the myometrium.

When using Ginipral:

• the number and strength of contractions decreases;
• labor ceases;
• the blood vessels of the uterus dilate;
• blood supply to the placenta improves.

The drug blocks both natural and oxytocin-induced contractions. It makes it possible to prolong pregnancy so that childbirth takes place at the physiological time.

Indications

Ginipral is used for acute, massive or long-term tocolysis. This term refers to a decrease in uterine contractility.

Acute tocolysis involves inhibition of contractions in the following cases:

• loss of umbilical cord loops;
• immobilization of the uterus before surgical delivery;
• rotation of the fetus from transverse presentation;
• acute intrauterine asphyxia;
• complications of childbirth.

Acute tocolysis is also needed if it is necessary to control a woman’s contractions for some time. For example, in the case of premature birth, while the patient is being taken to the maternity hospital.

Massive tocolysis is carried out to relieve contractions with an open uterine pharynx and a smoothed cervix.

Long-term tocolysis is necessary in order to carry a child to the physiological term of pregnancy. Prescribed mainly for ICN. Combined with other methods of preventing excessively early birth. Long-term tocolysis begins during and after cervical suturing surgery. Also, long-term tocolysis is prescribed to block premature labor in the event of frequent contractions, if there is no smoothing of the cervix and opening of the uterine pharynx.

Contraindications for use

Ginipral affects the function of the respiratory, cardiovascular and digestive systems, and not just the reproductive organs. Therefore, the drug has many contraindications. These include:

Thyrotoxicosis. In this condition, the pulse and blood pressure increase, and cardiac arrhythmias appear. Ginipral can aggravate all these disorders.

Tachyarrhythmia. This is an increase in heart rate. Ginipral also increases the heart rate, so it is not used in the presence of tachycardia.

Myocarditis. This is an inflammatory disease of the heart muscle. Since Ginipral affects myocardial contractility, in case of myocarditis its administration is dangerous for the health and life of the patient.

For the same reason, Ginipral is not used for other cardiovascular diseases:

• any mitral defects;
• aortic valve stenosis;
• arterial hypertension;
• cardiac ischemia.

Glaucoma. Ginipral is not used for angle-closure glaucoma because it increases intraocular pressure, which can lead to optic nerve atrophy.

The drug is not contraindicated in some gynecological diseases:

• intrauterine infectious pathologies;
• premature placental abruption;
• uterine bleeding.

Ginipral dilates the vessels of the uterus and increases uteroplacental blood flow. Therefore, it may make bleeding worse.

The drug is not used for insufficiency of liver and kidney function. Because in this case it becomes difficult to remove it from the body. As a result, the effect of the drug can be excessively strong and prolonged.

Ginipral is not used in the 1st trimester of gestation, but is used exclusively in the 2nd or 3rd trimester. It is also prohibited for use during lactation because it passes into breast milk and then into the baby’s body.

Mode of application

Ginipral is available in tablets and solution for parenteral administration. Therapy is usually started with parenteral forms. The contents of the ampoule are administered intravenously. This is required to ensure the gradual achievement of the required concentration of the active substance in the blood. Ginipral is usually diluted in an isotonic sodium chloride solution. In the future, treatment can be continued with tablets. They are taken orally with water.

Dosage

Acute tocolysis. Ginipral is prescribed intravenously at a dose of 10 mcg. This corresponds to 1 ampoule. The drug is injected into the vein in a stream, slowly, over 5 minutes or more. Then an infusion of Ginipral may be prescribed if appropriate indications are present.

Massive tocolysis. Ginipral is administered intravenously by drip at a rate of 0.3 mcg per minute. Before this, one injection of 10 mcg of Ginipral is usually prescribed intravenously. Although in some cases it is not necessary, and treatment begins immediately with infusions.

Long-term tocolysis. Ginipral is infused into a vein as a dropper. Infusions are carried out at a rate of 0.075 mcg per minute. If contractions do not resume within 2 days, the drug is further prescribed in tablets. The first tablet is taken 2 hours before stopping the last infusion. Initially, the drug is taken 1 tablet every 3 hours. Next, take Ginipral 1 tablet every 6 hours. If necessary, the daily dose can be increased. It is allowed to take the drug 1 tablet every 4 hours. The maximum daily dose is 8 tablets.

Side effects

β-2-adrenergic receptors are located not only in the uterus, but also in many other organs. Accordingly, Ginipral also affects their function. This means that the drug can cause a large number of side effects. They are all reversible. And in case of excessive severity, the effect of Ginipral can be interrupted by antagonists of this drug - beta-2 adrenergic receptor blockers.

Side effects from the central nervous system:

• anxiety;
• trembling fingers;
• headache;
• dizziness.

Ginipral affects the cardiovascular system. The mother's pulse may increase, diastolic and sometimes systolic blood pressure decreases. Heart pain and rhythm disturbances may appear, the most likely of which are ventricular extrasystoles. At the same time, the fetal pulse remains within normal limits.

Side effects from the digestive system are rare. Among them:

• nausea and vomiting;
• intestinal atony;
• constipation and functional intestinal obstruction.

The regularity of stool depends on the tone of the smooth muscles of the intestinal wall. When it decreases, peristaltic contractions are weakened. Therefore, when using Ginipral, it is necessary to monitor whether the pregnant woman has stool.

When using Ginipral in patients with kidney diseases, their function may be impaired. Then the following side effects develop:

• decrease in daily diuresis;
• swelling.

Some women note increased sweating while using Ginipral. They also experience some changes in the composition of their blood:

• calcium and potassium levels decrease - occurs only at the beginning of therapy;
• increase in glucose levels.

Laboratory changes can also be observed in newborns. They may have a shift in blood pH to the acidic side. In addition, a decrease in plasma glucose levels is often observed.

Like any other drugs, Ginipral can cause allergic reactions if there is individual sensitivity to its components. Possible manifestations:

• difficulty breathing due to bronchospasm;
• disturbance of consciousness;
• in patients with bronchial asthma, anaphylactic shock may develop.

Overdose

If a dose of Ginipral is prescribed too high, as well as if it is used against the background of renal or liver failure, an overdose is possible. Its main symptoms are anxiety, heart pain, low blood pressure, increased sweating, and trembling fingers. In case of overdose, the use of Ginipral antagonists is required. These are any beta-2 adrenergic receptor blockers. When they are prescribed, the effect of Ginipral on the body completely stops.

special instructions

Before starting treatment, it is advisable to conduct electrocardiography. This is required to determine possible contraindications from the cardiovascular system. After using Ginipral, cardiac activity is monitored in both the mother and the fetus. If the mother's pulse rises to 130 beats per minute or more, the dose of the drug should be reduced. Dosage reduction is also required if blood pressure drops excessively.

The reasons for stopping the use of Ginipral are:

• the appearance of pain in the heart;
• difficulty breathing;
• signs of heart failure.

Some patients are too sensitive to sympathomimetic drugs. For them, even small doses of Ginipral will cause too pronounced effects and a large number of side effects. In this case, individual dosage selection is required under the supervision of a doctor.

In women with diabetes, under the influence of Ginipral, blood glucose levels may increase. These changes are especially pronounced during the initial period of therapy. In this regard, carbohydrate metabolism indicators must be carefully monitored. And if childbirth occurred immediately after a course of treatment with Ginipral, it must be taken into account that a large amount of ketone acids and lactic acid could enter the child’s blood through the placenta. Therefore, the newborn may develop acidosis. He may also have low blood glucose levels.

The use of Ginipral reduces blood pressure. Therefore, diuresis may decrease. As a result, some mothers experience fluid retention. Swelling appears. Ginipral is often administered along with infusion therapy. That is, a large amount of fluid enters a woman’s body, which cannot be quickly eliminated due to reduced diuresis. As a result, there is a risk of pulmonary edema. To avoid such consequences, you must:

• promptly pay attention to symptoms of fluid retention in the body;
• assess renal function before starting therapy to assess the risk of complications;
• limit fluid intake during treatment, as well as salty foods;
• limit the volume of infusions;
• If possible, use infusion solutions that do not contain electrolytes.

The condition of patients who receive glucocorticoids for chronic kidney diseases (for example, glomerulonephritis) is monitored especially carefully.

During treatment, monitoring of intestinal function is necessary. The use of Ginipral can cause functional intestinal obstruction due to a significant decrease in smooth muscle tone. Therefore, you need to pay attention to how regular the patient’s stool is.

It should be borne in mind that too low a level of potassium in the blood increases the effect of Ginipral on the myocardium. Accordingly, the risk of cardiac side effects increases. Therefore, treatment should be carried out after monitoring the level of potassium in the blood or prophylactic administration of potassium supplements to prevent its possible deficiency.

Sometimes delivery is performed by caesarean section. This operation is performed under general anesthesia. Some anesthesia drugs, if used together with Ginipral, can disrupt the heart rhythm. The anesthesiologist should take this into account.

During treatment with Ginipral tablets, it is not advisable to drink tea or coffee. Because methylxanthines enhance the effect of the drug. This also applies to theophylline, theobromine, and caffeine. In this case, the risk of side effects from hexoprenaline increases.

During long-term treatment with Ginipral, it should be taken into account that:

• drug therapy can weaken the symptoms of premature placental abruption, which will complicate timely diagnosis;
• The effectiveness of Ginipral decreases when the cervix is ​​dilated by more than 2 cm, as well as in the case of rupture of the membranes of the fetal bladder.

Drug-drug interactions

Ginipral cannot be used in conjunction with beta-2 adrenergic receptor blockers. Because they completely neutralize the effect of hexoprenaline.

The action of Ginipral is potentiated (enhanced) by any methylxanthines, including caffeine and theophylline.

When treating patients with diabetes, it should be taken into account that Ginipral increases blood glucose levels. It also reduces the effect of using glucose-lowering drugs. And the combined use of Ginipral with glucocorticoids reduces the intensity of glycogen deposition in the liver.

The drug should not be taken together with drugs that have sympathomimetic activity. These are bronchodilators and cardiovascular drugs. Otherwise, the effect of Ginipral is enhanced and symptoms of overdose may appear.

The drug should not be used in conjunction with the following medications:

• ergot alkaloids;
• tricyclic antidepressants;
• monoamine oxidase inhibitors;
• mineralocorticoids;
• calcium and vitamin D.

When Ginipral is prescribed together with other beta-adrenergic receptor stimulants, as well as ftorotan, the frequency and severity of side effects from the heart and blood vessels may increase.

Terms and conditions of storage

Ginipral belongs to list B. This means that it can cause harm to the body if used uncontrolled. When stored in a pharmacy, they are locked at night. Storage temperature – from 18 to 25 degrees. The shelf life of the solution for parenteral administration is 3 years, and the tablets are 5 years.

Average price per drug

Ginipral in solution for intravenous administration costs 250 rubles for 5 ampoules. Ginipral for oral administration has a price of 170 rubles for 20 tablets.

Analogs

Ipradol is an analogue of Ginipral in terms of the active substance. It also contains hexoprenaline. But it is used in another area - in pulmonology for the treatment of bronchial asthma and emphysema.

Ginipral- a drug that helps reduce the contractile activity of the uterus, relieve its tone, and relax the smooth muscles of the bronchi. 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 β2-selectivity, Ginipral has a slight effect on cardiac activity and blood flow in the pregnant woman and fetus.

Indications for use:
Ginipral used as a tocolytic agent in case of threat of premature birth (in the third trimester of pregnancy), in case of acute intrauterine asphyxia of the fetus (impaired blood supply to the fetus), during childbirth (in case of discoordinated labor - abnormal contractions of the uterus during childbirth), to suppress uterine contractions before surgery intervention (cervical dissection, caesarean section).

Mode of application

Apply Ginipral intravenously and orally (in tablets). A “shock” dose is administered intravenously (in acute cases) slowly - 5-10 mcg of ginipral in 10-20 ml of isotonic sodium chloride solution. For infusions (for long-term treatment), dilute 50 mcg (the contents of 2 ampoules of 25 mcg - “concentrate” of ginipral) in 500 ml of 5% glucose solution. Administer at a rate of 25 drops per minute (about 0.125 mcg per minute). If necessary, increase the dose by 5 drops every 5 minutes. The minimum injection rate is 10 drops per minute, the maximum injection rate is 60 drops per minute.
Tablets should be taken 2-3 hours before the end of parenteral (intravenous) administration. Prescribe 1 tablet first, then after 3 hours, 1 tablet every 4-6 hours; only 4-8 tablets per day.

Side effects

Of the side effects from Ginipral Possible headache, anxiety, tremor (trembling limbs), sweating, dizziness. Rarely - nausea, vomiting. There are isolated reports of atony (loss of tone) of the intestines; increased levels of serum transaminases (enzymes). There may be an increase in the mother's heart rate and a decrease in blood pressure, especially diastolic (“lower” blood pressure). In several cases, ventricular extrasystoles (heart rhythm disturbances) and complaints of pain in the heart area were observed. These symptoms disappear after stopping treatment. The fetal heart rate in most cases does not change or changes little. Increased concentration of glucose (sugar) in the blood. This effect is more pronounced in patients with diabetes. Decreased diuresis (urination), especially in the initial phase of treatment. During the first few days of treatment, a decrease in the concentration of calcium in the blood plasma is possible; During further treatment, the calcium concentration normalizes.

Contraindications

:
Contraindications to the use of the drug Ginipral are: thyrotoxicosis (thyroid disease); cardiovascular diseases, especially tachyarrhythmia (heart rhythm disturbance), myocarditis (inflammation of the heart muscles), mitral valve lesions, idiopathic hypertrophic subaortic stenosis (non-inflammatory disease of the muscle tissue of the left ventricle of the heart, characterized by a sharp narrowing of its cavity); severe kidney and liver diseases; angle-closure glaucoma (increased intraocular pressure); heavy uterine bleeding; premature placental abruption; infectious lesions of the endometrium (inner lining of the uterus); hypersensitivity to the drug, especially in patients with bronchial asthma.

Pregnancy

:
Ginipral helps to reduce the intensity of uterine contractions, reduce the frequency of uterine contractions, and helps normalize irregular, too strong grips during childbirth. The use of Ginipral allows you to avoid premature contractions, which eliminates the possibility of having a baby earlier than expected. According to reviews of Ginipral, the drug can cause increased heart rate in the mother and fetus, improved blood circulation, lowered blood pressure, and relaxation of blood vessels.

Interaction with other drugs

A number of drugs that lower blood pressure (for example, beta-blockers) weaken the effect Ginipral or neutralize it.
Methylxanthines (for example, theophylline) enhance the effect Ginipral.
Effect of oral hypoglycemic agents during therapy Ginipral weakens.
Some sympathomimetics (cardiovascular and antiasthmatic drugs) increase side effects Ginipral(tachycardia).
General anesthesia (fluorotane) and adrenergic stimulants increase side effects on the cardiovascular system.
Ginipral incompatible with ergot alkaloids, MAO inhibitor drugs, tricyclic antidepressants, as well as with drugs containing calcium and vitamin D, as well as with dihydrotahysterol and mineralocorticoids.

Overdose

:
Overdose symptoms Ginipral: anxiety, tremor, increased sweating, severe tachycardia, arrhythmia, headaches, cardialgia, decreased blood pressure (BP), shortness of breath.
Treatment: use of antagonists Ginipral- non-selective beta-blockers that completely neutralize the effect Ginipral.

Storage conditions

List B. In a place protected from light.

Release form

In ampoules containing 0.025 mg or 0.01 mg; tablets 0.5 mg.

Compound

:
1 tablet Ginipral contains: hexoprenaline sulfate - 0.50 mg, corn starch - 27.8 mg, lactose hydrate - 80.0 mg, copovidone - 8.0 mg, disodium edetate dihydrate - 0.5 mg, talc - 0.8 mg, magnesium stearate - 0.8 mg, glycerol palmitostearate - 1.6 mg.

Main settings

Name:	GINIPRAL
ATX code:	G02CA05 -