Ginipral® (Gynipral®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceHexoprenalineHexoprenaline
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  • Ginipral®
    pills inwards 
    BIOTEK MFPDK, CJSC     Russia
  • Ginipral®
    solution in / in 
    Nycomed Austria GmbH     Austria
    • Dosage form: & nbspsolution for intravenous administration
    Composition:
    Each 2 ml ampoule contains:
    Active substance: hexoprenaline sulfate 0.01 mg.
    Excipients: sodium metabisulphite (sodium disulphite) 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:A clear, colorless solution.
    Pharmacotherapeutic group:Tocolytic agent - beta2-adrenomimetic selective
    ATX: & nbsp

    R.03.C.C.05   Hexoprenaline

    Pharmacodynamics:
    Selectively stimulates beta2-adrenoceptors, activates adenylate cyclase with subsequent increase in the formation of cyclic adenosine monophosphate (cAMP), which stimulates the work of the calcium pump, redistributing calcium ions (Ca2+) in myocytes, resulting in a decrease in the concentration of the latter in myofibrils. Expands bronchi, blood vessels, reduces contractile activity and tone of myometrium, thereby contributing to the improvement of uteroplacental blood flow. Stimulates glycogenolysis.
    Due to its beta2-selectivity, Ginipral® has a negligible effect on cardiac activity and the blood flow of the pregnant and fetus.
    Under the influence of the drug Ginipral®, the tone of the uterus decreases, the frequency and intensity of uterine contractions decreases, until their complete cessation, which allows prolonging the pregnancy, incl. before the onset of timely (urgent) birth.
    Ginipral® with intravenous injection depresses spontaneous as well as birth-related labor caused by oxytocin; during childbirth normalizes excessively strong or irregular contractions.
    The toxic effect of the drug Ginipral® begins immediately after intravenous injection and lasts approximately 20 minutes. The action of the drug is supported by a subsequent long-term intravenous infusion.
    Pharmacokinetics:
    Distribution
    There is no data on the distribution of hexoprenaline in the human body. In studies on animals with intravenous administration, a significant concentration of hexoprenaline was observed in the liver, kidneys and skeletal muscles, 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.
    Excretion
    When administered intravenously, the half-life (T1/2) - about 25 minutes.Within 24 hours, about 44% of the dose of hexoprenaline is excreted by the kidneys and through the intestine 5%, within 8 days 54% and 15.5%, respectively. In the initial stage, the kidneys display a free hexoprenaline and both methylated metabolite, as well as their corresponding sulfates and conjugates with glucuronic acid. After 48 hours in urine, only di-3-O-methyl-hexoprenaline is detected. About 10% of the dose is excreted with bile, mainly in the form of conjugates of O-methylated metabolites. In the intestine there is some reabsorption, t. with feces less substance is output, than it is found out in bile.
    Indications:
    Tokolitichesky therapy (medicamental relaxation of the muscles of the uterus) from the 20th week of pregnancy.
    - Acute tocolysis - rapid suppression of labor during labor in the case of acute intrauterine asphyxia (distress of the fetus), with the prolapse of the umbilical cord; in preparation for cesarean section (to remove hypertension of the uterus before transferring the pregnant woman to the operating room); complicated labor activity (hypertensive, uncoordinated or prolonged uterine contractions, obstructed labor due to improper position or presentation of the fetus); when performing an external turn of the fetusif its position is wrong. As an emergency measure for premature delivery before delivery of the pregnant woman to the hospital.
    - Massive tocolysis - inhibition of premature contractions in the presence of a smoothed cervix of the uterus and / or opening of the cervix.
    - Prolonged tocolysis - prevention of preterm labor with intensified or accelerated bouts without smoothing the cervix or opening the cervix; relaxation of the uterus before, during and after the application of the cerclage.
    In the case of premature rupture of membranes with the opening of the cervix more than 2-3 cm prolongation of pregnancy by tocolytic therapy is unlikely.
    Contraindications:
    - Hypersensitivity to the components of the drug. Since the preparation contains sulfite, Ginipral® IV solution should not be used to treat patients with sulfitic bronchial asthma;
    - Thyrotoxicosis;
    - Diseases of the heart (including in history);
    - Arterial hypertension;
    - Severe liver and kidney disease;
    - Closed-angle 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 the indications.
    Dosing and Administration:Instructions for the use of ampoules with a break point:
    Place the tip of the ampoule point to the top!
    Gently tapping your finger and shaking the ampoule, letting the solution from the tip of the ampoule drain down.
    Place the tip of the ampoule point to the top!
    Break the tip down, as shown in the picture.
    1. Acute tocolysis
    10 mcg (1 ampoule of 2 ml each). The contents of the ampoule are administered intravenously slowly (for 5-10 minutes) with the help of an automatic metering infuzomata or intravenously slowly by jetting, diluting the drug to 10 ml with isotonic sodium chloride solution.
    In the future, if necessary, the treatment can be continued with infusion at a rate of 0.3 μg / min (see clause 2 "Massive tocolysis").
    2. Massive tocolysis
    At the beginning, the treatment starts with a slow bolus injection of 10 μg (1 ampoule of 2 ml), followed by infusion of the drug Ginipral ® at a rate of 0.3 μg / min.
    As an alternative treatment, it is possible to use only infusion of the drug Ginipral® at a rate of 0.3 μg / min, without the preliminary bolus administration of the drug.
    When administered with 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).
    Calculation of the dose.
    0.3 μg / min corresponds to:
    Ampoules Amount of intravenous administration
    2 (20 μg) 150 drops / min
    3 (30 μg) 100 drops / min
    5 (50 μg) 60 drops / min
    6 (60 μg) 50 drops / min
    10 (100 μg) 30 drops / min
    For administration using automatically dosing infusomats, the drug is diluted with 0.9% sodium chloride solution or 5% glucose solution (dextrose) to 50 ml.
    The daily dose of 430 μg can be exceeded only in exceptional cases.
    3. Prolonged tocolysis
    The recommended dose is 0.075 μg / min.
    When administered with 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).
    Calculation of dosage.
    0.075 μg / min corresponds to:
    Ampoules Amount of intravenous administration
    3 (30 μg) 25 drops / min
    5 (50 μg) 15 drops / min
    When administered using automatically dosing infusomats, the drug is diluted with 0.9% sodium chloride solution or 5% glucose solution (dextrose) to 50 ml.
    If there is no resumption of contractions within 48 hours, the treatment can be continued with Ginipral® 0.5 mg tablets (see the appropriate instructions for use).
    This dose can only be used as an indicative dose, in the course of tocolysis it must be regulated individually.
    A solution of the drug Ginipral® in a 0.9% solution of sodium chloride or 5% glucose solution (dextrose) is prepared immediately before the use of infusion therapy.
    During tocolytic therapy, the volume of fluid entering the body (including ingestion) should not exceed 1500 ml per day. In this regard, it is preferable to administer the drug with the aid of automatically dosing infusomats.
    Side effects:
    Classification of adverse adverse reactions (NDR) by frequency of development:
    Very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000); frequency is unknown (can not be estimated from available data).
    Disorders from the endocrine system
    The frequency is unknown: hyperglycemia, lipolysis, a temporary increase in the activity of "hepatic" transaminases in the serum.
    Disorders from the metabolism and nutrition
    The frequency is unknown: hypokalemia at the beginning of therapy (further the content of potassium is normalized).
    Disturbances from the nervous system
    Very often: muscle tremor.
    The frequency is unknown: headache, anxiety, dizziness.
    Heart Disease
    Rarely: ventricular extrasystole, paroxysmal atrial tachycardia.
    The frequency is unknown: tachycardia, palpitations, increased cardiac output, decreased peripheral vascular resistance, increased systolic pressure and decreased diastolic pressure, leading to an increase in pulse pressure, cardialgia; stenocardia, myocardial ischemia.
    Disturbances from the respiratory system, chest and mediastinal organs
    The frequency is unknown: pulmonary edema.
    Disorders from the gastrointestinal tract
    Rarely: nausea.
    The frequency is unknown: vomiting, intestinal atony.
    Disturbances from the skin and subcutaneous tissues
    Often: increased sweating.
    Frequency unknown: redness of the skin.
    Immune system disorders
    Frequency unknown: hypersensitivity to sulfite.
    Disorders from the kidneys and urinary tract
    Frequency unknown: decreased diuresis (especially in the initial phase of treatment).
    Fetal disorders
    Frequency unknown: slight changes in heart rate. Infringements at newborns
    The frequency is unknown: hypoglycemia, acidosis, anaphylactic shock, bronchospasm.
    Overdose:
    Symptoms: tachycardia, tremor, anxiety, dizziness, increased sweating, arrhythmia, headaches, cardialgia, lowering of blood pressure (BP), dyspnea.
    Treatment: symptomatic therapy. As antidotes are recommended non-selective beta-blockers, which completely neutralize the effect of the drug Ginipral®, but it is necessary to consider the possibility of developing bronchospasm in patients with bronchial asthma.
    Interaction:
    Non-selective beta-blockers weaken or neutralize the effect of the drug Ginipral®.
    Methylxanthines (for example, theophylline) increase the effect of the drug Ginipral®.
    Ginipral® weakens the effect of oral hypoglycemic drugs. Some non-selective adrenomimetics (incl. epinephrine) and betag-adrenomimetics, halogen-containing drugs for general anesthesia (for example, halothane) increase the side effects of the drug Ginipral® from the side of the cardiovascular system.
    Joint application with kaliynesberegayuschimi diuretics can cause hypokalemia and arrhythmia.
    Ginipral® not be used together with monoamine oxidase inhibitors, tricyclic antidepressants, to preparations containing calcium and vitamin D. The combined use of dihydrotachysterol, ergot alkaloids or mineralocorticoid may increase the hemodynamic effect hexoprenaline.
    Glucocorticosteroids (for example prednisolone, hydrocortisone, dexamethasone, betamethasone, triamcinolone) And increase the hyperglycemic effect bronhodilyatiruyuschy hexoprenaline, the combined use may cause hypokalemia and arrhythmia.
    Caffeinated beverages (including tea and coffee) can increase the side effects Ginipral® preparation.
    Sodium disulfite is a highly active component, therefore it is not recommended to mix Ginipral® with other solutions, except for 0.9% sodium chloride solution or 5% glucose solution (dextrose).
    Special instructions:
    Patients with hypersensitivity to adrenomimetics should use Ginipral® in reduced doses prescribed individually, under the constant supervision of a physician.
    Before starting treatment with Ginipral ®, ECG monitoring is necessary.
    During the period of treatment with Ginipral ®, regular monitoring of the ECG, respiration rate, pulse and blood pressure in the mother, and the heart rate of the fetus are necessary.
    When the mother's heart rate rises (more than 130 beats per minute) or with significant fluctuations in blood pressure, the dose of the drug should be reduced.
    When there are signs of myocardial ischemia (pain in the heart, changes on the ECG), Ginipral® is immediately withdrawn.
    The initial hypokalemia should be eliminated by potassium preparations before tocolytic therapy begins.
    If the birth occurred immediately after treatment with Ginipral®, newborns should be examined for hypoglycemia and acidosis (blood pH).
    In patients with diabetes mellitus during the treatment with the drug Ginipral®, regular monitoring of the glucose concentration in the blood plasma is necessary.
    Clinical signs of premature placental abruption on the background of tocolytic therapy with Ginipral® may be less pronounced.
    With prolonged tocolytic therapy, it is necessary to check the condition of the fetoplacental system using standard methods of investigation.
    In the case of premature rupture of membranes with the opening of the cervix more than 2-3 cm prolongation of pregnancy by tocolytic therapy is unlikely.
    During the period of treatment with the drug Ginipral®, excessive fluid intake should be avoided, as the drug reduces diuresis. It should be carefully observed for signs, reflective fluid retention (edema of the legs, labored breathing), particularly while glucocorticosteroids and the treatment of diseases associated with promoting fluid retention (kidney disease, preeclampsia, proteinuria, and hypertension). Given the risk of developing pulmonary edema, you should use only solutions that do not contain electrolytes,and it is also necessary to limit the amount of infusion solutions administered.
    It is necessary to reduce salt intake. Daily fluid intake should not exceed 1.5 liters. If there are signs of fluid retention and symptoms of pulmonary edema (cough, shortness of breath), the drug should be discarded.
    During tocolytic therapy with Ginipral®, the regularity of the stool should be controlled, the drug suppresses the intestinal peristalsis.
    If halothane anesthesia is planned, therapy with Ginipral® should be discontinued. If an operative intervention is necessary, the anesthetist should be informed of the therapy with Ginipral®.
    Tokoliticheskaya therapy with beta-adrenomimetics can strengthen the symptoms of the present dystrophic myotonia.
    In rare cases, the solution contained in the preparation Ginipral® for intravenous administration, sodium disulfite can cause severe allergic reaction and bronchospasm.
    It is necessary to take into account the intake of any other drugs in case of prescribing Ginipral®.
    If there are side effects or conditions related to contraindications, it is necessary to inform the doctor.
    Effect on the ability to drive transp. cf. and fur:During the treatment period, care should be taken when driving vehicles and during classes with potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:The solution for intravenous administration is 5 μg / ml.
    Packaging:
    2 ml per ampoule of colorless glass with a break point, one ring gray and one ring of turquoise.
    By 5 ampoules in a plastic outline uncoated packaging.
    For 1 or 5 contour mesh packages together with the instruction for use are placed in a cardboard box.
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiration date.
    The prepared infusion solution should be used immediately!
    Terms of leave from pharmacies:On prescription
    Registration number:P N 015664/02
    Date of registration:24.03.2009 / 30.08.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Nycomed Austria GmbHNycomed Austria GmbH Austria
    Manufacturer: & nbsp
    Representation: & nbspNycomed Distribution Ltd.Nycomed Distribution Ltd.
    Information update date: & nbsp16.04.2017
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