Release form and composition
Ginipral is available in the following dosage forms:
- Tablets: white, biconvex, round (10 pieces in blisters, 2 blisters in a cardboard box);
- Solution for intravenous administration: colorless, transparent (in ampoules of 2 ml, 5 ampoules in plastic trays, 1 or 5 trays in a cardboard box).
1 tablet contains:
- Active substance: hexoprenaline sulfate – 0.5 mg;
- Auxiliary components: talc, corn starch, copovidone, lactose hydrate, disodium edetate dihydrate, magnesium stearate, glycerol palmitate stearate.
1 ml contains:
- Active substance: hexoprenaline sulfate – 0.005 mg;
- Auxiliary components: disodium edetate dihydrate, 2N sulfuric acid (to maintain pH level), sodium pyrosulfite, sodium chloride, water for injection.
Pharmacological properties
Pharmacodynamics
The action of the drug is based on the mechanisms of selective stimulation of β2-adrenergic receptors and activation of adenylate cyclase with a subsequent increase in the production of cyclic adenosine monophosphate, which stimulates the calcium pump, which redistributes calcium ions (Ca2+) in myocytes and reduces its concentration in myofibrils. Dilates blood vessels, bronchi, reduces the tone and contractile activity of the myometrium, resulting in improved uteroplacental blood flow. Stimulates glycogenolysis.
Due to β2-selectivity, Ginipral has a slight effect on the blood flow and cardiac activity of the pregnant woman and fetus. When taken, the tone decreases, the intensity and frequency of uterine contractions decreases, including their complete cessation, which allows you to prolong pregnancy until the onset of timely labor.
When administered intravenously, hexoprenaline suppresses oxytocin-induced and spontaneous labor contractions, and during childbirth normalizes irregular and excessively strong contractions.
When administered intravenously, the tocolytic effect of the drug begins immediately after injection and lasts about 20 minutes. The effect of the drug is maintained by subsequent long-term intravenous infusion.
Pharmacokinetics
- absorption: after oral administration, 5 to 11% of hexoprenaline is absorbed from the gastrointestinal tract. The time to reach maximum concentration is approximately 2 hours;
- distribution: there are no data on the distribution of the active substance in the human body. In animal studies, in the case of intravenous administration, significant concentrations of hexoprenaline were found in skeletal muscles, kidneys, liver, and to a lesser extent in the myocardium and brain;
- metabolism: hexoprenaline is metabolized by catechol-O-methyltransferase to mono-3-O-methyl-hexoprenaline and to di-3-O-methyl-hexoprenaline;
- Elimination: When taken orally, the half-life is approximately 50 minutes. Up to 90% of the drug is excreted through the intestines, up to 5% by the kidneys in the form of glucuronides. When administered intravenously, the half-life is approximately 25 minutes. Over the course of 1 day, approximately 44% of the dose of hexoprenaline is excreted by the kidneys, and about 5% is excreted through the intestines. Over the next 8 days, these figures are 54% and 15.5%, respectively. At the initial stage, both free hexoprenaline and methylated metabolites, sulfates and conjugates of both metabolites with glucuronic acid are excreted by the kidneys. After 2 days, only di-3-O-methyl-hexoprenaline is detected in the urine. Approximately 10% of the dose is excreted in bile, mainly conjugates of O-methylated metabolites. Some reabsorption occurs in the intestines because less of the substance is excreted in the stool than is found in the bile.
Indications for use
According to the instructions, Ginipral in the form of an injection solution is prescribed in the following cases:
- Massive tocolysis: to inhibit premature labor contractions when the uterus is dilated and/or the cervix is effaced;
- Acute tocolysis: as an emergency measure for premature birth before taking the pregnant woman to the hospital; to inhibit labor contractions during childbirth when the uterus is immobilized before cesarean section, acute intrauterine asphyxia, complicated labor, umbilical cord prolapse, and also before turning the fetus from a transverse position;
- Long-term tocolysis: for the prevention of premature birth with frequent or intensified contractions without dilation of the uterus or cervical effacement; when immobilizing the uterus before, during and after cervical cerclage.
Ginipral in tablet form is used when there is a threat of premature birth (most often as a continuation of infusion therapy).
How is childbirth after taking Ginipral?
Women taking the drug usually gave birth on the date indicated by the ultrasound specialist, after waiting for natural contractions. But the process itself occurs individually for everyone. It is possible to give birth calmly and without problems to that category of women in labor who were treated with Ginepral with very strong uterine tone. Labor began on time - most often, 3 weeks after discontinuation of the course of treatment.
The second half of pregnant women carry the child until 42 weeks and are admitted to the hospital, since natural contractions did not occur. To stimulate contractions, they are given a drug, most often oxytocin. If it is not suitable, other methods are selected.
If the cervix is fully dilated, but there are no contractions, the patient is prepared for surgery. In this case, a caesarean section is urgently required.
Often, this substance is the only way to carry and safely give birth to a child, so it is recommended to listen to the opinion of specialists.
Contraindications
- Tachyarrhythmias;
- Thyrotoxicosis;
- Aortic stenosis and mitral valve disease;
- Myocarditis;
- Severe kidney and liver diseases;
- Arterial hypertension;
- Cardiac ischemia;
- Premature placental abruption, uterine bleeding;
- Intrauterine infections;
- Angle-closure glaucoma;
- Lactation period (breastfeeding);
- Hypersensitivity to the components of the drug (especially in patients with bronchial asthma and a history of hypersensitivity to sulfites).
During pregnancy, Ginipral is contraindicated for use in the first trimester.
Ginipral during pregnancy - reviews
There are much more positive comments about the use of Ginipral than negative ones. Patients highlight the immediate effect, which helped many to maintain a normal pregnancy, carry and give birth to a healthy child.
Prevention of premature birth is a very important advantage of the drug. If you take pills or give an injection in the required dosage, the drug instantly relieves even the strongest contractions of the uterus.
Of course, like any medicine, Ginipral also has a number of negative aspects, which should also be taken into account before taking it. Many pregnant women experience severe discomfort for some time immediately after taking the pills internally, the first 40 to 45 minutes.
After this period of time, the unpleasant sensations passed without a trace. However, these disadvantages seem insignificant against the background of the enormous advantages. We can conclude that Ginipral during pregnancy is an effective and fast-acting medicine that allows you to carry your baby to term.
Instructions for use of Ginipral: method and dosage
The solution is administered intravenously slowly over 5-10 minutes. The doctor selects the dose individually. A Ginipral dropper is placed after dilution to 10 ml with isotonic sodium chloride solution, using automatic dosing infusion pumps or conventional infusion systems.
The regimen for using Ginipral droppers is determined by the indications:
- Massive tocolysis: administration of Ginipral begins with 0.01 mg (1 ampoule of 2 ml) followed by infusion at a rate of 0.0003 mg per minute. Infusion use of the drug without prior bolus administration is also possible;
- Acute tocolysis: the drug is used in a dose of 0.01 mg. If necessary, therapy can be continued with infusions;
- Long-term tocolysis: Ginipral is prescribed as a long-term drip infusion at a rate of 0.000075 mg per minute.
If contractions do not resume within 48 hours, treatment is continued with Ginipral tablets.
Ginipral tablets are taken orally with a small amount of water.
If there is a threat of premature birth, Ginipral is prescribed at a dose of 0.5 mg (1 tablet) 1-2 hours before the end of the infusion.
First take 1 tablet every 3 hours, then every 4-6 hours. Daily dose – from 4 to 8 tablets (2-4 mg).
Prevention of uterine hypertonicity
If the doctor has diagnosed increased tension in the smooth muscles and uterine walls, the pregnant woman is prescribed a calm environment, minimal stress, no worries or stress.
The main thing is to take the prescribed medicine on time and as prescribed. During the course of treatment it is strictly forbidden to have sexual intercourse. To reduce tension on the abdominal walls, it is best to lie down a lot and keep a bolster or rolled blanket under your knees.
Shoes during short permitted walks should be as comfortable as possible - without a hint of heels or high platforms. If a woman has chronic diseases, then it is necessary to treat them as quickly as possible.
Calmness and a healthy lifestyle are the best prevention for a pregnant woman
During the course of treatment, it is recommended to visit less crowded places. If we talk about food and menus at the time of treatment, then a pregnant woman needs to eat a lot of foods high in magnesium. You can take vitamins, a complex or one microelement. Magnesium will help reduce hypertension, reducing the excitability of the nervous system.
Where this element is found: buckwheat, oatmeal, bran, greens and legumes.
It is important to take a responsible approach to conceiving and carrying a future baby: take more walks, eat right, listen to the opinions of doctors, and follow a daily routine.
Side effects
- Central and peripheral nervous system: dizziness, headache, slight tremor of fingers, anxiety;
- Digestive system: rarely - vomiting, nausea, suppression of intestinal motility, temporary increase in transaminase levels, intestinal obstruction (it is recommended to monitor bowel regularity);
- Cardiovascular system: maternal tachycardia (in most cases, the fetal heart rate remains unchanged), arterial hypotension (usually diastolic); rarely - cardialgia (usually disappears quickly after discontinuation of the drug), rhythm disturbances (ventricular extrasystole);
- Laboratory indicators: hypocalcemia at the beginning of treatment, hypokalemia, increased plasma glucose levels;
- Allergic reactions: bronchospasm, difficulty breathing, impaired consciousness up to coma, anaphylactic shock (in patients with bronchial asthma or hypersensitivity to sulfites);
- Other: oliguria, increased sweating, edema (especially in patients with kidney disease).
In newborns, side effects may include acidosis and hypoglycemia.
Side effects of the drug Ginipral
Dizziness, anxiety, slight tremor of the fingers, increased sweating, tachycardia, headache, and increased activity of the liver may appear. There may be a decrease in blood pressure, especially diastolic. In some cases, nausea and vomiting appear. Isolated cases of heart rhythm disturbances (ventricular extrasystole), cardialgia, and difficulty breathing were recorded. These symptoms disappear very quickly after stopping use of the drug. Blood sugar levels, especially in diabetes, increase due to the glycogenolytic effect of the drug. Diuresis decreases, especially in the initial stage of treatment. In patients with a tendency to retain fluid in the tissues, this can lead to edema. During treatment with GINIPRAL®, the intensity of intestinal motility may decrease (pay attention to the regularity of stool). In newborns - hypoglycemia and acidosis, bronchospasm, anaphylactic shock.
special instructions
When using Ginipral, it is recommended to carefully monitor the function of the cardiovascular system (blood pressure, heart rate) of the fetus and mother. An ECG should also be recorded before and during treatment.
Patients with hypersensitivity to sympathomimetics are recommended to be prescribed small doses of Ginipral, which the doctor selects individually. Also, such patients require constant medical supervision.
If there is a significant increase in the mother's heart rate (more than 130 beats per minute) and/or with a significant decrease in blood pressure, the dose of the drug should be reduced.
If signs of heart failure, pain in the heart and difficulty breathing occur, the use of Ginipral should be stopped immediately.
During therapy, especially in the initial period, an increase in glucose in the blood plasma is possible, and therefore in mothers with diabetes mellitus it is necessary to monitor indicators of carbohydrate metabolism. If birth occurs immediately after a course of treatment, the possibility of developing acidosis and hypoglycemia in the newborn, which is associated with transplacental penetration of ketone and lactic acids, should be taken into account.
When using Ginipral, diuresis decreases, so you need to carefully monitor signs of fluid retention in the body.
Sometimes the simultaneous use of glucocorticosteroids during Ginipral infusions can lead to pulmonary edema. Therefore, during infusion therapy, constant monitoring of the patient’s condition is necessary. This is especially important in combined treatment with glucocorticosteroids in patients with kidney disease. It is necessary to strictly limit excess fluid intake. Due to the risk of possible development of pulmonary edema, the volume of infusions should be limited as much as possible. It is also recommended to limit salt intake in your diet.
During the period of use of the drug, you need to monitor the regularity of intestinal activity.
Before starting tocolytic treatment, you need to take potassium supplements, since the effect of sympathomimetics on the myocardium is enhanced by hypokalemia.
The simultaneous use of sympathomimetics and general anesthesia (halothane) can cause cardiac arrhythmias. Therefore, before using halothane, therapy with Ginipral should be discontinued.
With long-term tocolytic therapy, it is necessary to monitor the state of the fetoplacental complex. It is also necessary to ensure that there is no placental abruption, the clinical symptoms of which can be smoothed out against the background of tocolytic therapy. When the cervix is dilated by more than 2-3 cm and the amniotic sac is ruptured, the use of Ginipral is ineffective.
When carrying out tocolytic treatment with the use of beta-agonists, the symptoms of concomitant dystrophic myotonia may increase. In these cases, the use of diphenylhydantoin (phenytoin) drugs is recommended.
It is possible that the side effects of Ginipral may increase when taken in the form of tablets with coffee or tea.
Overdose of the drug Ginipral, symptoms and treatment
An overdose of GINIPRAL can be determined by a strong increase in the mother's heart rate, the occurrence of tremor, palpitations, headache, and sweating. These manifestations can usually be removed by 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.
List of pharmacies where you can buy Ginipral:
- Moscow
- Saint Petersburg
Drug interactions
When using Ginipral simultaneously with certain medications, undesirable effects may occur:
- Beta-blockers: weakening or neutralizing the action of Ginipral;
- Oral hypoglycemic drugs: weakening of their effect;
- Methylxanthines (including theophylline): enhancing the effectiveness of Ginipral;
- Glucocorticosteroids: reducing the intensity of glycogen accumulation in the liver;
- Other drugs with sympathomimetic activity (bronchodilators and cardiovascular drugs): the appearance of overdose symptoms and increased effects of these drugs on the cardiovascular system;
- Ftorotan and beta-agonists: increased side effects of Ginipral on the cardiovascular system.
Ginipral is incompatible with tricyclic antidepressants, monoamine oxidase inhibitors (MAOIs), ergot alkaloids, as well as medications containing vitamin D and calcium, mineralocorticoids and dihydrotachysterol.
Sulfite is a highly active component, so you should not mix Ginipral with any other solutions other than 5% glucose solution (dextrose) and isotonic sodium chloride solution.
