Gynipral® [Hexoprenaline]
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Pharmacological properties
Gynipral is a selective β2-sympathomimetic that relaxes the muscles of the uterus. under the influence of Gynipral, the frequency and intensity of uterine contractions decreases. the drug suppresses spontaneous, as well as labor pains caused by oxytocin. during childbirth normalizes very strong or irregular contractions. under the action of Gynipral, premature contractions in most cases stop, which allows you to extend the pregnancy to the normal term of delivery. suppression of labor pain is observed immediately after iv administration of the drug and lasts about 20 minutes. the effect of the drug increases after a subsequent drip of the drug. due to its β2-selectivity, Gynipral has an insignificant effect on the cardiac activity and blood circulation of the pregnant woman and the fetus.
Pharmacokinetics The drug consists of two catecholamine groups that undergo methylation in the human body due to catecholamine-O-methyltransferase. 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 Gynipral to adhere to the surface, is considered to be the reason for its prolonged action.
When using hexoprenaline for 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.
Indications
- Acute tocolysis. inhibition of labor contractions during childbirth in acute intrauterine asphyxiation, immobilization of the uterus before cesarean section, before the fetus rotates from a transverse position, with umbilical cord prolapse, with complicated labor. as 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 labor in reinforced or accelerated contractions without smoothing the cervix or opening the uterus. uterine immobilization before, during, and after the church operation.
Application
After dilution for iv injection or infusion.
- Acute tocolysis. For 10 μg Gynipral (1 ampoule of 2 ml), diluted in 10 ml of 0.9% sodium chloride solution or 5% glucose solution, slowly injected intravenously for 5-10 minutes. If necessary, continue the introduction by intravenous infusion at a rate of 0.3 μg / min.
- Massive tocolysis. At the beginning of treatment, they begin with the introduction of 10 μg (1 ampoule of 2 ml) iv slowly, then intravenously infuse Gynipral at a rate of 0.3 μg / min. You can enter the drug at a rate of 0.3 μg / min and without prior iv injection. Intravenously drip (20 drops = 1 ml).
Dissolve the concentrate for infusion in 500 ml of 0.9% sodium chloride solution or 5% glucose solution.
Dosage calculation: 0.3 mcg / min corresponds to
The number of ampoules, n (mcg) | I / O rate, drops / min |
---|---|
1 (25) | 120 |
2 (50) | 60 |
3 (75) | 40 |
4 (100) | 30 |
When using automatically dispensing infusomats, 75 μg (3 ampoules of concentrate for infusion of 25 μg Gynipral) are diluted with 0.9% sodium chloride solution or 5% glucose solution up to 50 ml, the infusion rate is 5 = 0.3 μg / min. The daily dose of 430 mcg is exceeded only in exceptional cases.
- Long-term tocolysis. The recommended dose is 0.075 mcg / min.
When using automatically dispensing infusomats, 75 μg (3 ampoules of concentrate for infusion of 25 μg Gynipral) are diluted with 0.9% solution of sodium chloride or 5% solution of glucose to 50 ml, infusion rate 3 = 0.075 μg / min.
Enter as an infusion (20 drops = 1 ml). Dissolve the concentrate for infusion in 500 ml of 0.9% sodium chloride solution or 5% glucose solution.
Dosage calculation: 0.075 mcg / min corresponds to
The number of ampoules, n (mcg) | I / O rate, drops / min |
---|---|
1 (25) | 30 |
2 (50) | 15 |
Use the prepared solution within 24 hours. If the contractions do not resume within 48 hours, treatment can be continued with Gynipral in the form of 0.5 mg tablets. The indicated dosing can only be used as an approximation, with tocolysis it is necessary to adjust it individually.
Incompatibility. Sulfite is a highly active component, so you should refrain from mixing Gynipral with other solutions, except for 0.9% sodium chloride solution and 5% glucose solution.
Contraindications
Hyper