Ginipral dropper instructions for use. Ginipral - description of the drug, instructions for use, reviews

Photo of the drug

Latin name:  Gynipral

ATX Code: G02CA05

Active substance:  Hexoprenaline (Hexoprenaline)

Producer: MbH GLOBOPHARM Pharmazeutische Produktions- und Handelsgesellschaft (Austria), Takeda (Germany), GmbH Nycomed Austria (Austria)

Description relevant to: 05.12.17

Ginipral is a selective beta2-blocker used in obstetric practice.

Active substance

Hexoprenaline (Hexoprenaline).

Release form and composition

Available in two dosage forms.

• Tablets are white, round, biconvex. Packed in blisters for 10 jokes.
• The solution for intravenous administration is a clear, colorless liquid. Packed in 2 ml ampoules.

Indications for use

The threat of premature birth (continued infusion therapy).

The solution for intravenous administration is used in the following situations:

• acute tocolysis (inhibition of labor pain in complicated births, immobilization of the uterus before cesarean section, acute intrauterine asphyxia, umbilical cord prolapse, before the child turns from the transverse position);
• emergency measure before delivery of a woman to the hospital during premature birth;
• massive tocolysis (inhibition of premature contractions during the opening of the uterus or the presence of a smoothed cervix);
• prolonged tocolysis (uterine immobilization before, during, and also after cervical cerclage);
• prevention of preterm labor with rapid or intense contractions without opening the pharynx or smoothing the cervix.

Contraindications

• myocarditis;
• tachyarrhythmias;
• cardiac ischemia;
• arterial hypertension;
• aortic stenosis and mitral valve disease;
• thyrotoxicosis;
• angle-closure glaucoma;
• uterine bleeding;
• premature detachment of the placenta;
• intrauterine infections;
• severe liver and kidney disease;
• hypersensitivity to the components of the drug.

Contraindicated in the first trimester of pregnancy and during lactation.

Instructions for use Ginipral (method and dosage)

The tablets are taken orally with a little water.

If there is a threat of premature birth: 500 mcg (1 tab.) 1 - 2 hours before the end of the infusion.

The drug should be taken first at 1 tab. every 3 hours and then every 4 to 6 hours

Daily dose: 2 to 4 mg (4 to 8 tablets).

The solution is administered intravenously, slowly over a period of 5 to 10 minutes, using automatically dosing infusion pumps or using conventional infusion systems. The contents of the ampoule are diluted with isotonic sodium chloride solution to 10 ml. The dose of the drug is selected individually.

• In acute tocolysis: 10 mcg (1 amp. In 2 ml). If necessary, treatment can be continued with infusion.
• With massive tocolysis: 10 mcg (1 amp., 2 ml), followed by infusion at a rate of 0.3 mcg per minute.
• Alternative: only infusion with a drug at a rate of 0.3 mcg per minute without prior bolus administration.
• With prolonged tocolysis: continuous drip infusion at a rate of 0.075 mcg per minute.

In the absence of contractions within 48 hours, 500 mcg tablets should be connected.

Side effects

The use of ginipral may cause the following side effects:

• Cardiovascular system: maternal arterial hypotension, tachycardia, cardialgia, cardiac arrhythmias (ventricular extrasystole).
• Central and peripheral nervous system: dizziness, headache, slight tremor of fingers, anxiety.
• Gastrointestinal tract: inhibition of intestinal motility, nausea, vomiting, intestinal obstruction, a temporary increase in the concentration of transaminases.
• Laboratory indicators: hypocalcemia (at the beginning of treatment), hypokalemia, increased concentration of glucose in the blood.
• Allergic reactions: bronchospasm, shortness of breath, anaphylactic shock, impaired consciousness (sometimes up to a coma).
• Other: edema, oliguria, increased sweating.

Side effects in newborns are acidosis and hypoglycemia.

Overdose

An overdose of ginipral is accompanied by the following symptoms:

• arrhythmia in the mother;
• severe tachycardia;
• lowering blood pressure;
• cardialgia;
• headaches;
• anxiety;
• increased sweating.

Overdose treatment consists in the use of drugs antagonists, which include non-selective beta-blockers that completely neutralize the effect of the drug.

Analogs

Analogs by ATX code: Ipradol.

Do not make the decision to replace the drug yourself, consult your doctor.

pharmachologic effect

• Ginipral is a selective beta 2 -adrenomimetic that reduces the tone and contractile activity of the myometrium. The active substance - hexoprenaline, reduces the frequency and intensity of uterine contractions, inhibits spontaneous, as well as labor pains caused by oxytocin. During childbirth, normalizes excessively strong or irregular contractions.
• The action of the drug is aimed at stopping premature contractions, which allows you to extend the pregnancy to the normal term of delivery.
• It is able to have a slight effect on the cardiac activity and blood flow of a pregnant woman and the fetus. This phenomenon is associated with beta 2 selectivity of the active substance.
• It is excreted mainly in urine unchanged and in the form of metabolites. A small part is excreted with bile in the form of complex metabolites.

special instructions

• Patients with hypersensitivity to sympathomimetics, the drug must be prescribed in minimum doses, selected individually. Hexoprenaline in this situation is used under constant medical supervision.
• During the treatment period, careful monitoring of the functions of the cardiovascular system (blood pressure, heart rate) should be carried out for both the mother and the child. Before and during therapy, it is recommended to record an electrocardiogram. With a marked decrease in blood pressure or a significant increase in heart rate, the dose should be reduced.
• If cardialgia, shortness of breath, or symptoms of heart failure occur, Ginipral treatment should be stopped immediately.
• The use of the drug helps to reduce diuresis, so the patient should carefully monitor signs indicating fluid retention in the body.
• During therapy, regular monitoring of intestinal activity is necessary.
• The use of hexoprenaline can lead to an increase in the concentration of glucose in the blood, therefore, mothers with diabetes require control of carbohydrate metabolism. Combining the drug with glucocorticosteroids can lead to pulmonary edema (especially when it comes to patients suffering from kidney disease).
• During treatment, strict restriction of fluid intake is necessary. Also, salt intake should be limited.
• Before starting tocolytic treatment, potassium preparations should be taken, since the effect of sympathomimetics on the heart muscle with hypokalemia is enhanced. With prolonged tocolytic treatment, it is necessary to monitor the condition of the fetoplacental complex, and also make sure that there is no detachment of the placenta.
• The simultaneous use of sympathomimetics and drugs for anesthesia can provoke heart rhythm disturbances.
• Before using halothane, the use of drugs should be discontinued.
• Tocolytic therapy in combination with beta-adrenergic agonists causes an increase in the symptoms of concomitant dystrophic myotonia. In this situation, it is recommended to resort to diphenylhydantoin preparations.
• The use of tablets with coffee or tea leads to an increase in side effects of the drug.

During pregnancy and breastfeeding

Contraindicated in the first trimester of pregnancy and with breastfeeding.

In the II and III trimesters of pregnancy, it is used according to indications.

In childhood

Information is absent.

In old age

Information is absent.

With impaired renal function

Contraindicated in severe kidney disease.

With impaired liver function

Contraindicated in severe liver diseases.

Drug interaction

• Joint administration with beta-blockers weakens or neutralizes the effect of drugs.
• Joint administration with methylxanthines (including theophylline) enhances the effectiveness of the drug.
• The simultaneous use of corticosteroids reduces the intensity of glycogen accumulation in the liver.
• Concomitant use with preroral hypoglycemic drugs weakens the effect of the latter.
• Joint administration with other drugs with sympathomimetic activity (cardiovascular and bronchodilator drugs) can enhance the effect on the cardiovascular system and cause overdose symptoms.
• The combined use with fluorotan and beta-adrenostimulants enhances side effects from the cardiovascular system.
• Incompatible with ergot alkaloids, MAO inhibitors, tricyclic antidepressants, as well as with preparations containing calcium and vitamin D, dihydrotachysterol and mineralocorticoids.
• During therapy, the drug should refrain from mixing with other solutions, except for isotonic sodium chloride solution and 5% dextrose (glucose) solution.

As part of one tablets  located 500 mcg hexoprenaline sulfate   + lactose hydrate, edetate disodium dihydrate, talc, palmitate glycerol stearate, corn starch, copovidone, magnesium stearate.

IN solution for intravenous administration  active substance per 1 ml - 5 μg + disodium edetate dihydrate, diluted sulfuric acid, sodium pyrosulfite, sodium chloride, water for injection.

Release form

The medicine is released in pills, in blisters of 10 pieces each, in a cardboard box 2 blisters. The tablets are white, round, convex.

Also, the product is released in the form of injection solution  in 2 ml ampoules, in contour plastic packs of 5 pieces each, in cardboard packs of 1 or 5 packs.

pharmachologic effect

Tocolitic.

Pharmacodynamics and pharmacokinetics

Hexoprenaline   - selective beta-2-sympathomimetic, consisting of two catecholamine groups. The active substance has the ability to block specific uterine receptors and relax its muscles. The frequency and intensity of contractions is significantly reduced. The medicine blocks labor pains (spontaneous or arising under the influence of the hormone).

During childbirth, Ginipral can normalize the strength and regularity of uterine contractions and inhibit premature contractions. The medicine, in those who took during pregnancy, allowed the fetus to be brought to normal. The drug has the ability to slightly affect   STS   pregnant woman and fetus.

Immediately after intravenous administration of the drug, inhibition of contractions begins, the action of the drug lasts about 20 minutes.

After ingestion, the active substance is exposed methylation through catecholamine-o-methyltransferase . It is noteworthy that the process methylation   only one of catecholamine groups otherwise hexoprenaline   will become biologically inactive. Therefore, the tool for quite a long time affects the body.

In the first 4 hours after taking the drug, about 80% of the active components of the drug are excreted in the urine. A small amount of the drug is excreted in the form of bile.

Indications for use

Tablets are prescribed for the existing threat of premature birth, including as part of a comprehensive treatment.

The use of injections and droppers is shown:

• before the fetal revolution (if necessary, a revolution);
• with an obvious or hidden loss of the umbilical cord or its entanglement;
• for uterine immobilization   before ;
• as an emergency measure, if premature birth occurs, before delivering the woman to honey. institution;
• when braking contractions during childbirth (with acute intrauterine );
• for inhibition of premature contractions, if the uterus is opened or the cervix is \u200b\u200bsmoothed;
• for the prevention of premature contractions;
• during cervical cerclage   to immobilize the uterus.

Contraindications

The drug is not prescribed:

• with heart and high blood pressure;
• women suffering from severe kidney and liver diseases;
• at;
• at;
• in the first trimester of pregnancy;
• with heart rhythm disturbance, myocarditis ;
• persons with mitral valve disease   or aortic stenosis ;
• at;
• when on the components of the product (especially on sulfites );
• during the period ;
• with intrauterine infections and premature bleeding placental abruption .

Side effects

As a rule, there are no problems with this drug.

During the reception, anxiety, nausea, may develop.

Instructions on Ginipral (Method and dosage)

Depending on the task and the condition of the pregnant woman, various dosage forms in various dosages are used.

Instructions for use Ginipral tablets

The tablet is swallowed whole, while drinking water.

As a rule, the medicine is prescribed one tablet every 3 hours, then the interval between doses is reduced to 4-6 hours. The average daily dosage is from 2 to 4 mg of the drug (up to 8 tablets).

If there is a threat of premature birth, then the medicine is taken in a dosage of 500 mcg 60-120 minutes before the end of the infusion hexoprenaline .

Ginipral infusion during pregnancy

Dosage is selected individually, after consultation with a doctor.

The contents of one capsule are usually diluted in an isotonic solution.   sodium chloride . Enter slowly, gradually, in 5-10 minutes.

• at acute toxolysis   make an intravenous injection of 10 μg of the drug, then go on an infusion;
• during massive toxolysis   use one ampoule (2 ml), the average injection rate is 0.3 micrograms per minute;
• at prolonged toxolysis   the doctor selects the dosage, the rate of administration is 0.075 mcg per minute.

If after 2 days the contractions did not resume, then they switch to the tablet form.

Overdose

With an overdose, severe tachycardia , dizziness , headache   and may decrease, develop anxiety   and.

Interaction

Do not mix Ginipral and other solutions in one syringe (dropper) except isotonic solution   and glucose .

Beta blockers   neutralize or significantly weaken the effect of the drug.

The medicine weakens the effect   hypoglycemic   preparations.

Methylxanthines , in particular Theophylline   able to enhance the effectiveness of the drug.

It is not recommended to combine the drug with sympathomimetics , beta adrenostimulants   and fluorotane   due to increased load on cardiovascular system .

Combination glucocorticosteroids —Ginipral   able to reduce the intensity of the processes of accumulation in the liver glycogen .

Ginipral during pregnancy

Acceptance of funds in the first 12 weeks is prohibited.

The use of droppers during pregnancy is indicated in the 2nd and 3rd trimesters. Injections should be carried out under the supervision of a physician.

Often prescribed tablets during pregnancy in the later stages, to reduce the likelihood of premature birth with uterine hypertonicity .

Taking medication during lactation is highly not recommended.

Judging by the reviews, side effects from the drug sometimes appear, so you can drink it only after consulting a doctor.

Instructions on how to take Ginipral tablets during pregnancy are described above.

It should be added that often doctors prescribe Ginipral during pregnancy (in the complex). Thus, it is possible to avoid the manifestation of side effects from both drugs.

INSTRUCTION

for medical use of the drug

Ginipral
(GYNIPRAL)

Composition:
active substance: hexoprenaline;
1 tablet contains 0.5 mg of hexoprenaline sulfate;
Excipients: lactose, corn starch, pre-Latinized starch, copovidone, Trilon B (Trilon B), talc, glycerol distearate, magnesium stearate.

Dosage form.  Tablets.

Pharmacotherapeutic group.

Means for use in gynecology. Sympathomimetics that suppress uterine contractility. ATS code G02C A 05.

Indications.

The threat of premature birth (primarily - as a continuation of other fusion therapy).

Contraindications

Hyper sensitivity to the components of the drug, hypersensitivity to sulfites; thyrotoxicosis; cardiovascular diseases, coronary heart disease, arterial hypertension, cardiac arrhythmias occurring with tachycardia, myocarditis, mineral valve defect and idiopathic hypertrophic subaortic stenosis; severe liver and kidney disease; closed angle glaucoma; uterine bleeding, premature exfoliation of the placenta; internally uterine infections.

Dosage and administration

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

Adverse reactions

Ginipral is generally well tolerated by patients.
While taking Ginipral, headache, anxiety, slight finger tremors, sweating, palpitation, tachycardia, dizziness may develop, in rare cases, nausea, vomiting.
Sometimes redness of the skin may be observed.
Perhaps a slight increase in heart rate (HR), a decrease in blood pressure, especially diastolic.
Isolated cases of cardiac arrhythmias (ventricular extrasystole) and complaints of pain behind the sternum were recorded. These symptoms quickly disappear after discontinuation of the drug.
Blood sugar levels, especially in diabetes, increase due to the glycogen-lytic effect of the drug.
Diuresis is reduced, 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 serum.
During treatment with Ginipral, intestinal motility may decrease. In rare cases, intestinal atony was observed (it is necessary to control vata stool regularity).
In newborns, hypoglycemia and acidosis, bronchospasm, anaphylactic shock can occur.

Overdose.

Symptoms: severe tachycardia, tremor, headache, dizziness, increased sweating, arrhythmia, anxiety, cardialgia, decreased blood pressure, shortness of breath.
Treatment. Usually, to reduce side effects, a reduction in the dosage of the drug is sufficient. To eliminate severe symptoms, the use of non-selective beta-blockers that completely neutralize the action of Ginipral is recommended.

Use during pregnancy or lactation.

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

Children.The drug is not used in children.

Features of the application.During treatment, vata should be constantly monitored for blood pressure, pulse, heart activity, as well as fetal heartbeat.
  Patients with hypersensitivity to sympathomimetics should use Ginipral in small doses, individually prescribed, under the constant supervision of a doctor.
  With a significant increase in the heart rate in the mother (more than 130 beats / min) or / and a significant decrease in blood pressure, the dose should be reduced, if there are complaints of shortness of breath, pain in the heart, and with signs of heart failure, the drug should be discontinued.
  When treating patients with diabetes, it is necessary to monitor the metabolism of carbohydrates, 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 consider the possibility of hypoglycemia and acidosis in newborns due to the penetration of acidic metabolic products (milk and ketone compounds).
  With the use of the drug, diuresis is reduced, so it is necessary to control the cotton wool for symptoms associated with fluid retention in the body.
In some cases, the simultaneous use of corticosteroids during infusion of the drug can cause pulmonary edema. This is especially important for combined treatment with corticosteroids in patients with concomitant diseases that lead to fluid retention (kidney disease, early pregnancy toxicosis).
  Before starting tocolytic therapy, it is necessary to take potassium preparations, since with hypokalemia, the effect of sympathomimetics on the myocardium is enhanced.
  The simultaneous use of certain drugs (for example, halothane) and sympathomimetics can lead to heart rhythm disturbances; it is necessary to prevent co-administration with these drugs.
  With prolonged tocolytic therapy, it is necessary to monitor the state of the fetoplacental complex in cotton and make sure that there is no detachment of the placenta. Clinical symptoms of premature placental abruption can be alleviated against the background of tocolytic therapy.
  With rupture of the fetal bladder and with the opening of the cervix by more than 2-3 cm, the effectiveness of tocolytic therapy is small.
  During tocolytic treatment using beta-adrenergic agonists, the symptoms of concomitant dystrophic myotonia may intensify. In such cases, the use of diphenylhydantoin (phenytoin) preparations is recommended.
  Patients who have rare hereditary galactose intolerance, lactase deficiency or malabsorption of glucose-galactose should not use the drug.
  In the process of tocolytic treatment, it is necessary to control the release of intestines.
  Coffee and tea can enhance the side effects of ginipral.

The ability to influence the reaction rate when driving a car or other mechanisms.

  Some adverse reactions from the central nervous system in individual cases may affect the ability to drive vehicles or work with mechanisms.

Interaction with other drugs and other types of interactions.

Non-selective beta-blockers weaken or neutralize the effect of Ginipral.
Methylxanthin (e.g., theophylline) enhances the action of ginipral.
The intensity of glycogen accumulation in the liver, caused by the use of corticosteroids, decreases under the influence of Ginipral.
The effect of oral hypoglycemic agents during treatment with Ginipral is weakened.
Co-treatment with some sympathomimetic tics (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 preparations containing ergot alkaloids, as well as with preparations containing calcium, vitamin D, dihydrotachysterol and mineralcorticoids, as well as with MAO inhibitors, tricyclic antidepressants.
  Means for general anesthesia (fluorotan) and adrenostimulants enhance side effects from the cardiovascular system.

Pharmacological properties.

Pharmacological

Ginipral is a selective beta-2-sympathomimetic, relaxes the muscles of the uterus. Under the influence of Ginipral, the frequency and intensity of uterine contractions decreases. The drug suppresses spontaneous labor, as well as due to oxytocin labor. During childbirth, it normalizes very strong or irregular contractions. Under the action of Ginipral, premature contractions in most cases stop, which allows you to extend the pregnancy to the normal term of delivery. Inhibition of labor pain is observed immediately after intravenous administration of the drug and lasts about 20 minutes. The effect of the drug lengthens after a subsequent drip of the drug. Due to its beta-2 selectivity, Ginipral has an insignificant effect on the cardiac activity and blood flow of the pregnant woman and the fetus.

Pharmacokinetics

The drug consists of two catecholamine groups, which undergo methylation in the human body due to catecholamine-O-methyltransfer basics. If the action of isoprenaline almost completely ceases with the introduction of one methyl group, hexoprenaline becomes biologically inactive only in the case of methylation of both of its catecholamine groups. This property, as well as the high ability of Ginipral, adhesives on the surface are considered to be the reason for its long long-term action.
When using hexoprenaline, during the first 4 hours, 80% of the active substances are excreted unchanged in the urine, 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 with bile in the form of complex metabolites.

Pharmaceutical characteristics.

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

Shelf life.  5 years.

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

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

Pregnancy is a special condition of the female body that requires a careful and careful attitude to your health. Quite often, at various stages of gestation, various unfavorable conditions appear, one of which is elevated, capable of provoking premature birth. To prevent undesirable consequences, a number of substances are prescribed to relax the myometrium. Many obstetricians prescribe the drug "Ginipral" (tablets) as such a means.

Its analogs are also used quite often, because drugs affect individual organisms individually - those who help well may not give the desired effect in others. In addition, this drug, despite its high effectiveness in the prevention of preterm labor, has a fairly large number of contraindications and side effects, which causes some patients to fear and unwillingness to take it. In any case, opt for this medicine or decide how to replace Ginipral, it is recommended only by the attending physician.

Description of the drug

The drug “Ginipral” is produced in the form of white biconvex round tablets containing in each 500 μg of hexoprenaline sulfate, in the form of an intravenous solution with a dosage of 5 μg per 1 ml of liquid (10 μg of active substance per 1 ampoule). A concentrate is also produced for the preparation of a solution for infusion (25 μg of hexoprenaline sulfate in one ampoule).

Mechanism of action

The drug “Ginipral”, whose effect is due to the properties of hexoprenaline sulfate, which is classified as selective beta2-adrenergic agonist, refers to substances that reduce the tone and contractile activity of the uterus muscles (myometrium), that is, it helps to prevent premature labor.

With the introduction, especially intravenous, it quickly causes a decrease in the increased tone of the uterus, which helps to reduce the frequency and intensity of contraction of the muscles of the uterus, inhibition of spontaneous contractions or provoked by the appointment of oxytocin contractions. When used during labor, it helps to normalize too strong or irregular contractions. Termination of premature contractile activity of the uterus allows a woman to convey pregnancy to the optimal time for the appearance of the baby.

In addition to a specific effect, the drug has some effect on the state of cardiac activity and blood flow of both the mother and the fetus, which must be taken into account when prescribing.

Indications

Since this drug causes relaxation of the uterine muscles, a decrease in the frequency and intensity of their contractions, interfering with the opening of the cervix, the use of Ginipral is due to this particular action.

The drug in solution is prescribed in case of emergency to quickly suppress contractions:

• when acute intrauterine asphyxiation of the fetus occurs during childbirth;
• before carrying out a manual rotation of the child from a transverse position;
• when the umbilical cord falls out;
• with complicated labor;
• to relax the uterus before cesarean section;
• during preterm birth to inhibit contractions before sending the pregnant woman to the hospital.

Ginipral is also used intravenously:

• with the risk of premature labor pain;
• to relax the muscles of the uterus during the suturing procedures on her neck to prevent its untimely opening;
• for inhibition of contractions during an insufficient period of pregnancy or with rapid and increased contractions against the background of an unprepared neck.

The use of Ginipral for such indications may require taking a whole course of the drug, which can last for several months.

Tablets are prescribed for the risk of premature birth, mainly as a continuation of infusion treatment.

Contraindications

The use of the drug is associated with a number of serious side effects, therefore, it is used only as prescribed by the doctor, taking into account all the available contraindications, sometimes canceling the Ginipral drug, the analogues of which may be more suitable in a particular situation.

You can not take the drug for a number of diseases:

• thyrotoxicosis;
• tachyarrhythmias;
• defects and aortic stenosis;
• myocarditis;
• arterial hypertension;
• severe diseases of the kidneys and liver;
• angle-closure glaucoma;
• uterine bleeding of various etiologies, premature placental abruption;
• the development of intrauterine infections;
• in the first trimester of pregnancy;
• lactation (breastfeeding);
• hypersensitivity to the components of the drug (especially with bronchial asthma or a history of sulfite sensitivity).

The presence of a whole list of contraindications makes it necessary in some cases to look for a replacement for Ginipral, an analogue of which can be very difficult to choose, since it has a specific effect on the myometrium, and not on the entire smooth muscle as a whole.

Application chart

As already mentioned, taking Ginipral requires strict indications and accurate adherence to dosage. Intravenous administration is preferably carried out in a hospital using automatic dosing infusomats or droppers, since treatment with the drug involves its slow delivery for 5-10 minutes.

In case of emergency, in order to quickly stop the contractions, the solution is used in a dose of 10 μg (one ampoule containing 2 ml of the drug), followed by infusion of the Ginipral preparation. A dropper is prescribed with a very slow introduction at a rate of 0.3 mcg / min. If a gradual decrease in uterine activity is expected, the solution is administered for a longer time (0.075 μg / min).

With a positive effect of such treatment, further therapy can be carried out using tablets in a dose of 500 μg, which are recommended to be washed down with a sufficient amount of water, but not tea or coffee, which can enhance the negative effect of the substance. The daily dose of tablets is 4-8 pieces when taking them one tablet at first after 3 hours, then - after 4-6 hours.

special instructions

The presence of a large number of side effects requires monitoring the health of both the patient and the fetus, in particular, it is necessary to monitor the function of the cardiovascular system. It is advisable to measure the ECG before and during treatment.

If the patient has an increased sensitivity to such drugs, he is prescribed in small doses, selected strictly individually, with constant monitoring by the attending physician.

If severe tachycardia or a decrease in blood pressure is observed, the dose of the drug is reduced. The manifestation of signs such as shortness of breath, pain in the heart, symptoms of cardiac ischemia, suggests the immediate withdrawal of this drug. In order to reduce, “Verapamil” is prescribed in addition to the Ginipral preparation, which is aimed at neutralizing the negative effect on the cardiovascular system.

With an increase in blood sugar caused by the use of this drug, you need to carefully monitor the carbohydrate metabolism in women with diabetes.

The drug "Ginipral" helps to reduce urine output, therefore, it is necessary to note all the changes that may be associated with the retention of fluid in the body. Sometimes co-administration with glucocorticosteroids can lead to pulmonary edema, therefore it is necessary to constantly monitor during the infusion period, as well as the volume of the injected solution.

Side effects

When using a drug that can affect the entire body in a complex manner, such as the Ginipral drug, side effects can occur on the part of any body system:

• a negative effect on the central and peripheral nervous systems is characterized by headache, dizziness, anxiety, slight trembling in the fingers;
• the effect on the cardiovascular system can cause tachycardia, arterial hypotension (most often diastolic) in a pregnant woman, rhythm disturbance or cardialgia, which quickly disappear after drug withdrawal, can occur much less often;
• rare disorders of the digestive tract can manifest as nausea, vomiting, inhibition of intestinal motility up to complete stagnation of the food coma;
• in the presence of sensitivity to the components of the drug, allergic reactions can occur in the form of shortness of breath, bronchospasm, impaired consciousness, which can go into a coma, in patients with bronchial asthma or hypersensitivity to sulfites - up to anaphylactic shock.

In addition, sweating may intensify, oliguria and edema may occur. In newborns, hypoglycemia and acidosis are often observed.

Overdose

In an emergency situation of preterm birth or in the case of persistent uterine hypertonicity, it is necessary to prescribe this drug in significant quantities, which can cause an excess of the maximum allowed daily dose and the associated negative consequences.

Symptoms of an overdose include: severe tachycardia in a pregnant woman (the fetus is extremely rare), arrhythmia, trembling fingers, headache of different localization, increased sweating, anxiety, cardialgia, decreased blood pressure and shortness of breath. The occurrence of such symptoms is the basis for the cancellation of the drug "Ginipral", an analogue of which may not give such a clinical picture.

With the manifestation of such symptoms, antagonist substances are prescribed, which are non-selective beta-blockers that are able to completely neutralize the effect of the drug.

Interaction with other medicinal substances

The presence of a disease in a pregnant woman may require the mandatory intake of medicines that are not always compatible with this muscle relaxant, so the question may arise: "How to replace Ginipral if withdrawal of the main drug is not possible?"

Substances exhibiting an atypical effect when co-administered with Ginipral solution or tablets include:

• beta-blockers that can weaken or completely neutralize the effect of the drug "Ginipral";
• methylxanthines (including the substance "Theophylline"), enhancing its effectiveness;
• glucocorticosteroids, the combined action of which can lead to a decrease in the rate of glycogen accumulation by the liver;
• oral hypoglycemic substances when used together with this drug are less effective in showing their therapeutic effect;
• the interaction of this medication with cardiovascular and bronchodilators may lead to an increase in their influence and the appearance of signs of overdose;
• fluorotan and beta-adrenostimulants increase the incidence of side effects in relation to the heart and other elements of the circulatory system;
• ergot alkaloids, MAO inhibitors, and agents containing calcium and vitamin D, as well as dihydrotachysterol and mineralocorticoids, are completely incompatible with the Ginipral preparation, the cancellation of which in this case is absolutely necessary.

Since the active substance (hexoprenaline sulfate) has a high activity, it is allowed to breed it exclusively with sodium chloride and 5% dextrose (glucose).

The drug "Ginipral": analogues and synonyms

Relating to the group of beta-adrenergic agonists, this remedy has a number of drugs similar in action and indications:

• "Partusisten" - is available as a sterile solution for intravenous administration and in the form of tablets, is prescribed to prevent premature birth only in a hospital setting.
• "Ritodrin" - is mainly used for bronchial asthma and other obstructive conditions, but it is also able to relax the uterine muscle.
• “Fenoterol” - has a similar effect, it is used only under medical supervision in hospitals.
• "Salbupart" - is prescribed in case of danger of premature birth, is administered very slowly intravenously for 6-12 hours.

A similar effect in reducing uterine tone is possessed by the substance magnesia, which, by blocking calcium channels, quite effectively relaxes the myometrium, while exhibiting much fewer side effects.

Another medicine that can replace the Ginipral preparation is the Indomethacin analogue, which refers to prostaglandin inhibitors. It can well reduce the increased uterine tone, but when used after a gestational age of 32 weeks, it causes a significant amount of serious undesirable effects: it helps to slow the maturation of the fetal lung tissue, and can cause jaundice and enterocolitis.

Some obstetricians prescribe the drug "Nifedipine" to reduce uterine tone. It is not a specific tool that is used in gynecology, its scope mainly concerns the treatment of cardiovascular pathologies, but since this tool helps to relax smooth muscles, it can also be used to relieve tension in the uterus muscles. It should be noted that the drug causes a decrease in blood pressure, which prevents the appointment of patients with hypotension.

The drug that reduces the tone and contractile activity of the myometrium

Active substance

Hexoprenaline Sulfate (hexoprenaline)

Release form, composition and packaging

IV solution   transparent, colorless.

Excipients: sodium pyrosulfite, disodium edetate dihydrate, sulfuric acid 2N (to maintain pH), water d / i.

2 ml - ampoules (5) - plastic pallets (1) - cardboard boxes.

pharmachologic effect

Selective beta 2 -adrenomimetic reduces the tone and contractile activity of the myometrium. Reduces the frequency and intensity of uterine contractions, inhibits spontaneous, as well as labor pains caused by oxytocin. During childbirth, normalizes excessively strong or irregular contractions.

Under the action of the drug, premature contractions in most cases cease, which allows you to extend the pregnancy to the normal term of delivery.

Due to its beta 2 selectivity, the drug has little effect on the activity and blood flow of the pregnant woman and the fetus.

Pharmacokinetics

Metabolism

The drug consists of two catecholamine groups, which are methylated by COMT. Hexoprenaline becomes biologically inactive only in the case of methylation of both catecholamine groups. This property, as well as the high ability of the drug to adhere to the surface, are considered to be the reasons for its prolonged action.

Breeding

It is excreted mainly in urine unchanged and in the form of metabolites. During the first 4 hours after using 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 with bile in the form of complex metabolites.

Indications

Acute tocolysis

- inhibition of labor contractions during childbirth during acute intrauterine asphyxiation, during immobilization of the uterus before cesarean section, before the fetus rotates from a transverse position, with umbilical cord prolapse, with complicated labor;

- An emergency measure for premature birth before delivery of the pregnant woman to the hospital.

Massive tocolysis

- inhibition of premature labor pain in the presence of a smoothed cervix and / or opening of the uterus.

Long Tocolysis

- Prevention of preterm birth in reinforced or rapid contractions without smoothing the cervix or opening the uterus;

- Uterine immobilization before, during and after cervical cerclage.

Contraindications

- thyrotoxicosis;

- tachyarrhythmias;

- myocarditis;

- Mitral valve disease and aortic stenosis;

- arterial hypertension;

- severe liver and kidney disease;

- angle-closure glaucoma;

- uterine bleeding, premature detachment of the placenta;

- intrauterine infections;

- I trimester of pregnancy;

- lactation (breastfeeding);

- Hypersensitivity to the components of the drug (especially in patients with bronchial asthma and a history of hypersensitivity to sulfites).

Dosage

The contents of the ampoule must be administered intravenously slowly for 5-10 minutes using automatically dosing infusomats or using conventional infusion systems - after diluting with isotonic sodium chloride solution to 10 ml. The dose of the drug should be selected individually.

At acute tocolysis  the drug is prescribed in a dose of 10 μg (1 amp. in 2 ml). In the future, if necessary, treatment can be continued with the help of infusions.

At massive tocolysis  administration of the drug begins with 10 μg (1 amp. in 2 ml), followed by infusion of Ginipral at a rate of 0.3 μg / min. As an alternative treatment, it is possible to use only infusions of the drug at a rate of 0.3 μg / min without prior bolus administration of the drug.

At long tocolysis  the drug is prescribed as a long drip infusion at a rate of 0.075 mcg / min.

If resumption of contractions does not occur within 48 hours, continue treatment with 500 mcg Ginipral tablets.

Side effects

From the nervous system:  headache, dizziness, anxiety, slight 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, oppression of intestinal motility, intestinal obstruction (it is recommended to monitor the regularity of stool), a temporary increase in transaminases.

Allergic reactions: difficulty breathing, bronchospasm, impaired consciousness up to coma, anaphylactic shock (in patients with bronchial asthma or patients with hypersensitivity to sulfites).

From the laboratory indicators:  hypokalemia, hypocalcemia at the beginning of therapy, increased plasma levels.

Other:  increased sweating, oliguria, edema (especially in patients with kidney disease).

Side effects in newborns:  hypoglycemia, acidosis.

Overdose

Symptomssevere maternal tachycardia, arrhythmia, finger tremors, headaches, sweating, anxiety, cardialgia, decreased blood pressure, shortness of breath.

Treatment:the use of Ginipral antagonists - non-selective, which completely neutralize the effect of the drug.

Drug interaction

When combined with beta-blockers, the effect of Ginipral is weakened or neutralized.

When combined with methylxanthines (including c), the effectiveness of Ginipral is enhanced.

With the combined use of Ginipral with GCS, the intensity of glycogen accumulation in the liver decreases.

When combined, Ginipral weakens the effect of oral hypoglycemic drugs.

With the combined use of Ginipral with other drugs with sympathomimetic activity (cardiovascular and bronchodilator drugs), the effect of the drugs on the cardiovascular system and the appearance of overdose symptoms are possible.

When combined with fluorotane and beta-adrenostimulants, the side effects of Ginipral from the cardiovascular system are enhanced.

Incompatible with ergot alkaloids, MAO inhibitors, tricyclic antidepressants, as well as with preparations containing calcium and vitamin D, dihydrotachysterol and mineralocorticoids.

Sulfite is a highly active component, so you should refrain from mixing Ginipral with other solutions, except for isotonic sodium chloride solution and 5% dextrose (glucose) solution.

special instructions

Patients with hypersensitivity to sympathomimetics should be prescribed Ginipral in small doses, individually selected, under the constant supervision of a doctor.

With a significant increase in heart rate in the mother (more than 130 beats / min) or / and with a marked decrease in blood pressure, the dose of the drug should be reduced.

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

The use of Ginipral can cause an increase in blood glucose (especially in the initial period of treatment), therefore, carbohydrate metabolism in mothers with diabetes should be monitored. 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 transplacental penetration of lactic and ketonic acids.

With the use of Ginipral, diuresis is reduced, so you should carefully monitor the symptoms associated with fluid retention in the body.

In some cases, the simultaneous use of GCS during Ginipral infusions can cause pulmonary edema. Therefore, with infusion therapy, constant careful clinical monitoring of patients is necessary. This is especially important in the combined treatment of corticosteroids in patients with kidney disease. Strict restriction of excess fluid intake is necessary. The risk of possible development of pulmonary edema requires limiting the amount of infusion as much as possible, as well as the use of dilution solutions that do not contain electrolytes. Limit salt intake with food.

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

The simultaneous use of funds for general anesthesia (halothane) and sympathomimetics can lead to heart rhythm disturbances. Ginipral should be discontinued before using halotane.

With prolonged tocolytic therapy, it is necessary to monitor the condition of the fetoplacental complex, to make sure that there is no detachment of the placenta. Clinical symptoms of premature placental abruption can be alleviated against the background of tocolytic therapy. With rupture of the fetal bladder and with the opening of the cervix by more than 2-3 cm, the effectiveness of tocolytic therapy is small.

During tocolytic therapy using beta-adrenergic agonists, the symptoms of concomitant dystrophic myotonia may intensify. In such cases, the use of diphenylhydantoin (phenytoin) preparations is recommended.

Pregnancy and lactation

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