Beta-adrenomimetics

Isadrin (isoprenaline, isoproterenol, Novorrinum). In connection with the characteristic stimulating effect on beta-adrenergic receptors, isadrine causes a strong bronchodilator effect, increased and intensified contractions of the heart, increases cardiac output. At the same time, it reduces the overall peripheral resistance of blood vessels due to arterial vasoplegia, lowers arterial pressure, reduces the filling of the ventricles of the heart. The drug increases the demand for myocardium in oxygen. Isadrin is not contraindicated in pregnancy. No damaging effect of the drug on the fetus or the mother's body was found.

The experimental and clinical substantiation of the use of beta-adrenomimetics, in particular of isadrin, in the complex therapy of miscarriage is carried out. Pregnant women were prescribed either only Isadrin or Isadrin in combination with spasmolytic or with no-shp. Iazrin was given in the form of tablets 0.5-0.25 mg 4 times a day. The effectiveness of preserving therapy was greatest if pregnant women received isadrin in combination with spasmolithine at a dose of 0.1 mg 3 times a day or in a dose of 0.4 mg 2-3 times a day [90 and 85%]. A smaller effect was noted in pregnant women who received only isadrine (75%). With a mildly expressed threat of termination of pregnancy, a combination of isadrin with anticholinergic spasmolytic or a combination of isadrin and no-shpy can be used. The enhancement of tocolytic effect is explained by the effect of synergy with a combination of two different drugs.

Reduction of side effects caused by izadrin when combined with a no-shpa can be explained by the fact that no-shpa selectively acts on the beta-adrenoreceptors of the heart, as a result of which tachycardia decreases. Spasmolitin also reduces the side effect of isadrin, as it causes bradycardia and hypokalemia and soothes tachycardia and hyperkalemia caused by isadrin.

Form release: 0.5% and 1% solutions in vials of 25 and 100 ml (for inhalation) and tablets or powders containing 0.5 mg of the drug.

Orciprenadia sulfate (alupent, asthmopent). The chemical structure and pharmacological properties of the drug is close to the isadrin, but in comparison with it does not cause severe tachycardia and lower blood pressure.

Orciprenaline sulfate is not contraindicated in pregnancy. The most widely used in the treatment of threatening premature birth and hypertension of the uterus in childbirth. It passes through the placental barrier and can cause tachycardia in the fetus when the dose is exceeded 10 μg / min. At the mother in therapeutic doses does not cause significant side effects, on the contrary, it improves placental perfusion. Positive results were noted when it was used in childbirth in the treatment of distress (suffering) of the fetus, especially due to abnormalities of labor or compression of the umbilical cord. The drug has no teratogenic effect.

If there is a pronounced threat of termination of pregnancy, orciprenaline sulfate (alupent) is first intravenously dripped in a dose of 2-4 ml of a 0.05% solution in a 5% glucose solution at a rate of 20 drops per minute. After the tocolytic effect is achieved, maintenance therapy is administered by injecting 1 ml 4 times a day intramuscularly.

A separate group consists of pregnant women who receive alupent according to the above scheme in combination with a 25% solution of magnesium sulfate 10-20 ml intramuscularly 2-3 times a day. This combination is the most effective in 75% of pregnant women.

An assessment was made of the state of central hemodynamics in various ways of introducing alupent during labor in the treatment of non-coordinated labor. The administration of alupent in a dose of 0.5 mg intramuscularly with the method of microperfusion at a dose of 0.06 mg / h was compared. When intramuscular injection of the drug in the labor, sharp changes in hemodynamics were observed, and the use of microperfusion of alupent gave less pronounced changes in the main indices of central hemodynamics, resulting in normalization of the contractile activity of the uterus, reducing its basic tone by a factor of 2.

Prolonged use of the drug during pregnancy is possible with the appointment of tablets of 0.02 g 3-4 times a day. The effect in this case usually occurs after 1 hour and lasts 4-6 hours.

Form release: aerosol inhalers, containing 400 single doses (for 0.75 mg) of the drug; ampoules of 1 ml of a 0.05% solution (0.5 mg); tablets of 0.02 g.

Terbutaline (terbutaline sulfate, bricanil). It also refers to the number of adrenomimetics with a selective effect on beta-adrenergic receptors. Its effect on the contractions and tone of the uterus has been studied in detail, and it has been found that it is advisable to use the drug in case of severe symptoms of the threat of abortion and even if there is an opening of the uterine throat or the beginning of premature birth.

According to detailed toxicological studies, bricanil is slightly toxic. In the experiment, it was shown that in doses of 0.02-0.4 μg / ml it reduces the frequency and amplitude, and in many cases completely stops the uterine contractions. Based on the inhibitory effect of briquanil on the contractile activity of the uterus, it was suggested that it affects the prostaglandin level, which is confirmed experimentally.

At physiological birth intravenous injection of bricanil at a dose of 10-20 mcg / min for 20-45 min effectively blocks spontaneous or oxytocin-induced generic activity. The intensity of labor in these cases is reduced to a greater extent than their frequency.

In menacing or early premature births, the drug is usually injected into a vein, dissolving 5 mg of bricanil, respectively, in 1000 ml of isotonic sodium chloride or glucose solution. It should be taken into account that 20 drops of the solution contain 5 μg of briquanyl and then the dosage of the preparation is individually adjusted taking into account the severity of its effect and the tolerance of the organism.

It is usually recommended to start the injection at a rate of 40 cap / min, i.e. 10 μg / min, then every 10 minutes the rate of administration is increased by 20 drops, reaching 100 drops, i.e. 25 μg / min. This dosage is maintained for 1 hour, and then every 30 minutes reduced by 20 drops, establishing a minimum effective maintenance dose. Usually already on the 2nd-4th day the drug is administered at a dose of 250 mcg 4 times a day.

In accordance with our research, another method of administering the drug is also effective when threatening premature birth, when 0.5 mg of bricanil contained in 1 ml of an aqueous solution is diluted in 500 ml of 5% glucose solution and injected slowly intravenously at doses of 1.5 up to 5 μg / min. Further therapy is carried out by prescribing briikanil tablets at a dose of 2.5 mg 4-6 times a day. In addition, as the symptoms of threatening premature birth diminish, it is advisable to prescribe briquanyl by 1 ml intramuscularly and then applying it in the form of tablets. The duration of action of briikanil, administered parenterally, lasts 6-8 hours.

Simultaneous use of briikanil and MAO inhibitors is not permissible (!), Since it can cause hypertensive crisis. It is not recommended to use it simultaneously with inhalation anesthetics from the fluorine-containing group (phorotan, etc.), as well as with beta-adrenoreceptor blockers, since the substances neutralize each other's action.

Form release: tablet briikanil contains 2.5 mg terbutaline sulphate, in the package - 20 tablets; ampoules briikanil for 0.5 mg terbutaline sulphate, in the package - 10 ampoules.

Ritodrin (yotopar). The drug has no contraindications for use during pregnancy. By the duration of its action, it is most effective and has the least severe side effects from the cardiovascular system.

Ritodrin effectively inhibits uterine contractions and is successfully used in the treatment of a threatening abortion, hypertension of the uterus during childbirth, as well as in acidosis in the fetus. After its introduction, the intensity, frequency and basal tone of the uterus decrease. In addition, the preparation improves the fetal condition, judging by the average value of the fetal heart rate and the pH value. Intravenous administration of ritodrin at a dose of 100-600 μg / min does not adversely affect the fetus in the treatment of threatening premature births. It is also not inherently teratogenic.

Ritodrin is recommended to be used in doses of 5 to 10 mg 4-6 times a day in the treatment of threatening premature births. The efficacy of ritodrin in late toxicosis has been shown to regulate labor activity.

The use of the drug at a dose of 1.5-3 μg / min has a pronounced therapeutic effect in this contingent of parturients, especially if there are excessively intense or frequent contractions, as well as an increased basal tone of the uterus and in the case of non-coordinated labor.

In the treatment of preterm labor, intravenous administration of the drug with an initial dose of 0.05 mg / min is used, and gradually every 10 minutes the dose of the drug is increased by 0.05 mg / min. A clinically effective dose is usually in the range of 0.15 and 0.3 mg / min. The administration of the drug continues from 12 to 48 hours after the termination of uterine contractions.

When administered intramuscularly, the initial dose is 10 mg, and if the effect of 10 mg of ritodrine does not occur, then 10 mg is repeated during the first hour and 10-20 mg of the drug every 2 to 6 hours afterwards if there is a threat of termination of pregnancy for 12-48 h. The dose is increased or decreased depending on the clinical effect of ritodrine and possible side complications.

The taking of ritodrin tablets inside to fix the therapeutic effect is usually performed immediately after parenteral administration of the drug at 10 mg every 2 to 6 hours, the dose may also increase or decrease depending on the effect and side effects.

In the case of severe impairment of the fetus due to uterine hyperactivity, the drug is administered starting at a dose of 0.05 mg / min, gradually increasing it every 15 minutes until the uterine activity decreases. The effective dose is usually between 0.15 and 0.3 mg / kg body weight. If the fetus has a pronounced acidosis (with a pH of less than 7.10), the use of ritodrine is not recommended.

Contraindications to the use of the drug are massive bleeding during labor, diseases in the mother or fetus that require abortion, as well as cardiovascular diseases in the mother. Side effects of taking ritodrin in appropriate doses are insignificant. There are no unpleasant subjective sensations when the drug is administered very slowly and in the position of the woman on its side. Sometimes there is only a progressive increase in the pulse rate and in some cases, facial hyperemia, sweating and tremor, as well as nausea and vomiting.

Form release: tablets of 10 mg, 20 tablets per package; ampoules, 10 mg / ml or 50 mg / ml, with 6 ampoules per package.

Partusisten (fenoterol). The drug has a pronounced relaxing effect on the uterus. It has a particularly successful ratio of its high antispasmodic activity and a relatively limited effect on the cardiovascular system. It is used in the form of intravenous infusions, as well as inside with the purpose of further consolidating the therapeutic effect of parenteral injections. Tablets are also used for intermittent treatment according to appropriate indications. In a number of modern studies, continuous administration of subcutaneous beta-adrenomimetics is used, or intravaginal administration is severe in severe intolerance.

Indications for the use of partusisten are threatening premature births, threatened miscarriage after a 16-week gestation period, and increased uterine tone after Shirokkar surgery and other surgical procedures performed on the uterus during pregnancy.

In childbirth the drug is most often used for abnormalities of labor, especially with uterine hyperactivity, increased basal tone, in preparation for surgical delivery (caesarean section, obstetric forceps), with symptoms of asphyxia of the fetus.

The drug is contraindicated in thyrotoxicosis, various heart diseases, especially heart rhythm disorders, tachycardia, aortic stenosis, intrauterine infection.

As a rule, tocolytic treatment is carried out by intravenous long-term drop infusion. In most cases, the optimal parenteral dose of partusisten is 1-3 μg / min. In some cases, however, there is a need to lower the dose to 0.5 or increase to 4 μg / min, respectively.

For the preparation of intravenous infusion, 1 ampoule (10 ml) of partuscene is diluted in 250 ml of sterile isotonic sodium chloride solution or 5% glucose solution or lavulose.

In the treatment of threatening premature births or a threatening late miscarriage at the end of the infusion therapy, oral administration of the drug is recommended in order to prevent subsequent uterine contractions.

In those cases where only one oral treatment is prescribed, it is recommended to use Pargusysten 1 tablet (5 mg) every 3-4 hours, i.e. 6-8 tablets daily.

During the use of partusisten, the pulse rate and arterial pressure, as well as the heart rate of the fetus should be monitored regularly.

Pregnant women with diabetes should carefully and continuously monitor carbohydrate metabolism, as the use of the drug can lead to a significant increase in blood sugar levels. In such cases, during the use of partusisten, it is necessary to increase the dosage of antidiabetic agents preventing such complications. Indication for the use of partusisten is also fetoplacental insufficiency, since the parusisis improves utero-placental circulation. Pargusisten even in small doses has a pronounced antispasmodic effect and regardless of the dose leads to a decrease in labor activity and a decrease in basal tone, first of all the amplitude of uterine contraction decreases, and later their duration and frequency.

With intravenous administration of partusisten, the effect occurs after 10 minutes, with oral administration after 30 minutes and stops after 3-4 hours after administration.

In the presence of side effects from the cardiovascular system, it is possible to additionally assign isoptin, which reduces or prevents these side effects, and also is a synergistic action on the uterus of partusisten. Isoptin, together with partusistenom can be administered intravenously in a dose of 30-150 mg / min or applied inwards at a dose of 40-120 mg.

Form release: the ampoule (10 ml) contains 0.5 mg partusisten, 1 tablet - 5 mg (packaged 100 tablets, and ampoules are packed in 5 and 25 pieces).

[1], [2], [3], [4], [5], [6]