Geksoprenalin (When ATH R03CC05)

When ATH:
R03CC06

Pharmacological action.

Means, reducing tone and contractile activity of the myometrium, beta2-sympathomimetic. It reduces the frequency and intensity of uterine contractions. It inhibits spontaneous, and oxytocin induced labor pains. During labor normalises excessively strong or irregular contractions.

Under the influence of hexoprenaline premature contractions in most cases terminated, allowing you to extend the normal period of pregnancy to birth. Due to the selectivity of β2-adrenoceptor hexoprenaline has little effect on the heart and bloodstream of the fetus and the pregnant woman.

Pharmacokinetics

Hexoprenaline well absorbed after oral administration. The molecule of the active substance consists of two groups of catecholamine, who undergo methylation by the COMT. Hexoprenaline becomes biologically inactive only if methylation of both groups catecholamine.

Report mostly in the urine unchanged and as metabolites. For the first 4 h after application 80% of the administered dose excreted in urine as free and hexoprenaline monometilmetabolita. Then increases excretion dimetilmetabolita and related compounds (glucuronide and sulfate). A small portion is excreted in the bile in the form of complex metabolites.

Testimony

For parenteral administration,: Acute tocolysis – inhibition of labor pains during childbirth in acute intrauterine asphyxia, immobilisation of the uterus before the cesarean section, before the turn of the lateral position of the fetus, prolapse of the umbilical cord, in complicated labor, as an emergency measure in preterm labor before delivery of the pregnant to the hospital; massive tocolysis – inhibition of preterm labor contractions in the presence of a smoothed cervical and / or disclosure of cervix; long tocolysis – prevention of preterm labor with reinforced or shortness of battles without smoothing the cervix or opening cervix, immobilisation of the uterus to, during and after surgery Cerclage-.

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

Dosage regimen

Parenterally administered into / in the form of injections and infusions.

Dosages for parenteral administration set individually, depending on the clinical situation.

For oral single dose of 500 g, Frequency and duration of use as defined clinical situation.

Side effect

CNS: headache, anxiety, tremor, dizziness.

Cardio-vascular system: slight tachycardia, decrease in blood pressure (especially diastolic); rarely – PVCs, precordialgia (These symptoms quickly disappear after canceling hexoprenaline).

From the digestive system: inhibition of intestinal motility, a temporary increase in the activity of serum transaminase; rarely – nausea, vomiting, bowel atony.

Other: decrease in urine output (especially at the beginning of treatment), an increase in blood glucose (in diabetes, this effect is stronger), increased sweating; in the first days of treatment – lowering the potassium concentration in the blood (during further treatment – normalization).

Fetal heart rate, in most cases, remains unchanged or slightly changed.

Contraindications

Hyperthyroidism, cardiovascular diseases (heart rhythm disturbances, proceeding with tachycardia, miokardit, mitral valve, aortalnыy stenosis), severe liver disease, severe kidney disease, zakrыtougolynaya glaucoma, uterine bleeding (premature detachment of the placenta), intrauterine infection, lactation (breast-feeding), Hypersensitivity to hexoprenaline.

Cautions

When using hexoprenaline should monitor heart rate and blood pressure of mother, as well as the fetal heartbeat. ECG monitoring is recommended before and during treatment.

In patients with hypersensitivity to sympathomimetics hexoprenaline should be used in low doses, Customised, under the constant supervision of a doctor.

With a significant increase in heart rate in the mother (more 130 u. / min) and / or a marked decrease in blood pressure should reduce the dose; if complaints of shortness of breath, pain in the heart and signs of heart failure, the use should be discontinued immediately hexoprenaline.

Before the start of tocolytic therapy should appoint drugs potassium, tk. if hypokalemia sympathomimetic effect on the myocardium intensifies.

Against the background of hexoprenaline should limit salt intake from food.

When conducting tocolytic therapy should monitor the regularity of the chair.

Pregnant women with diabetes should monitor the concentration of glucose in the blood, tk. use hexoprenaline, especially at the beginning of treatment, can cause elevation of blood glucose levels.

If the birth occurs immediately after the treatment hexoprenaline, It must take into account the possibility of hypoglycemia in infants and acidosis due to transplacental penetration of acid metabolic products (dairy acid and ketone).

In some cases, the use of corticosteroids during the introduction hexoprenaline may develop pulmonary edema. Therefore, infusion therapy must be continued careful clinical monitoring of patients. This is especially important when the need for combination therapy with corticosteroids and hexoprenaline in patients with concomitant diseases, accompanied by fluid retention (incl. kidney diseases).

Since the introduction of hexoprenaline there is a risk of pulmonary edema, It should be possible to limit the amount of fluid, administered at infusion, Besides, dilution of the drug is preferred to use solutions, not containing electrolytes.

When prolonged tocolytic therapy, make sure no abruption. Clinical symptoms of premature detachment of the placenta can be smoothed out against the backdrop of tocolytic therapy. When rupture of membranes and cervical dilatation of more than 2-3 see the effectiveness of tocolytic therapy is low.

Drug Interactions

When conducting tocolytic therapy with beta-agonists may increase symptoms related dystrophic myotonia. In such cases the use of derivatives of diphenylhydantoin (phenytoin).

Hexoprenaline not recommended for use in conjunction with ergot alkaloids, as well as drugs, containing calcium and vitamin D, digidrotahisterol or mineralocorticoid.

The intensity of the accumulation of glycogen in the liver, caused by the use of GCS, decreases under the influence of hexoprenaline.

With simultaneous use of nonselective beta-blockers weaken or neutralize the effects of his hexoprenaline.

With simultaneous use of methylxanthines, incl. theophylline, enhance the effect hexoprenaline.

In an application hexoprenaline reduces hypoglycemic effect of hypoglycemic agents.

At simultaneous application with other sympathomimetic hexoprenaline (means for normalizing the blood circulation, antiasthmatics) may increase the stimulating effect on the cardiovascular system and the emergence of symptoms of overdose (combinations should be avoided).

With simultaneous application of sympathomimetics and halothane may develop cardiac arrhythmias.

Before using halothane hexoprenaline should be abolished.