Tocolytics in obstetrics. Tocolytic (conservation) therapy

In the past, obstetricians have tried several dozen relief drugs. premature birth and maintaining pregnancy in the second and third trimester. Majority remedies not accepted for use due to serious side effects such drugs and possible harm for the fetus. It is hard to believe that alcohol was used to stop preterm labor in the last century, but now it is a historical fact.
Modern medicine has about sixty serious clinical studies on tocolytic therapy, not to mention a huge number (several hundred) small studies... The use of tocolytics is actual topic, since for many years doctors have been looking for a "panacea" so that they can get the desired result with the least negative impact on the mother and fetus. But such a panacea was not found. Moreover, having examined those drugs that were used in obstetrics with or without caution, doctors realized with considerable concern that most drugs could not be used. It turned out that it is not so easy to prevent or stop premature birth, and if this is possible, then it is possible to prolong the pregnancy only by 2-7 days, and very rarely until the calendar date.
Magnesium sulfate (magnesia), indomethacin and nifedipine remained in the arsenal of modern obstetrics.

The oldest and most common drug is magnesium sulfate solution - magnesia... Unlike other drugs, magnesium is more toxic to the mother and safer for the fetus. Most often, it causes nausea, hot flashes, headache, dizziness, blurred vision, in worst cases, impaired respiratory and cardiac functions. The most dangerous complication is pulmonary edema. Magnesium sulfate crosses the placenta and can cause respiratory impairment in newborns if this drug was used to stop labor, but unsuccessfully.
It is very unpleasant that magnesium is given intravenously to almost every pregnant woman (worst of all - on early dates pregnancy), and day hospitals where such women go, have become the cry of the latest "obstetric fashion", a kind of cultivator of all kinds of rumors, myths, prejudices and fears. This drug does not act on the uterus and does not suppress its contractile function in the early stages of pregnancy, so it should not be prescribed to everyone who has been diagnosed with uterine hypertonicity by ultrasound or who has something sore in the lower abdomen somewhere. The development of side effects is much more dangerous than the nonexistent benefits from the use of magnesia.
The specificity of magnesium sulfate is that the non-contracting uterus is not sensitive to this drug, so if there are no contractions, then the drug should not be prescribed. Foreign doctors, most of them, use this very principle, and besides, they do not use magnesium for more than two days, and in rare cases for more than 4 days.
The use of magnesium sulfate requires constant monitoring of laboratory parameters of electrolyte (salt) metabolism in the mother and her general condition, which, alas, is not practiced by many doctors.
Since no tocolytic drug has any advantages in prolonging pregnancy, after stopping the administration of magnesium, other tocolytics are not prescribed, including for the purpose of "prophylaxis".

If magnesia is preferred in the third trimester, then indomethacin more effective in the second trimester, mainly before 30 weeks of pregnancy. This drug belongs to the group of inhibitors of prostaglandin synthesis, or in other words, this drug inhibits the production of substances (prostaglandins) that play a role in the contraction of the muscles of the uterus. It is popular with non-pregnant women for treatment premenstrual syndrome and painful periods.
Indomethacin is also effective for polyhydramnios. However, this drug has negative influence on the fetus, especially if it is used in the third trimester, so it is usually not prescribed after 32 weeks. In women, it can cause gastrointestinal bleeding, allergic reaction and blood clotting disorders. Headache and dizziness are also common. From the same group of drugs, naproxen, aspirin and a number of other drugs were occasionally used, but there is little information about their benefits in preventing premature birth.

Hormonal drug - progesterone, in its various forms, which is abused in early pregnancy, used certain period the time in pregnant women is between 24-32 weeks of gestation, but the results have been inconsistent. Most doctors do not use progesterone or its analogues during the second half of pregnancy.

TO nifedipine, which belongs to the group of calcium channel blockers and which is often used to treat hypertension and cardiovascular diseases, is treated with great caution, since it is a new drug in obstetrics. It also has many side effects, however, with correct appointment, very effective in the short-term prolongation of pregnancy.

One of the new drugs that began to be used in obstetrics not so long ago is nitroglycerine... Nitroglycerin is known to many older people suffering from cardiovascular diseases, in particular angina pectoris or angina pectoris. The drug exists in different forms and for the prevention of preterm birth after invasive procedures (amniocentesis, cordocentesis, laser relief of placental vessels, etc.), as well as for the relief of preterm labor, it is used in the form of percutaneous patches, intravenous infusions or droppers, nasal sprays, tablets under the tongue. The effectiveness of nitroglycerin is still being studied in a number of countries by conducting large clinical trials. Like all tocolytics, nitroglycerin is prescribed only at 24-32 weeks, not earlier or later.
The indication for the appointment of nitroglycerin is the presence of at least 4 contractions within 20 minutes and the shortening of the cervix, that is, the criteria for setting preterm labor are taken into account. Also, this drug is not prescribed if another tocolytic drug has been prescribed to the woman before.

Preparations from the group of beta-sympathomimetics, which include terbutaline, ritodrin, and very well-known in the territory former countries Union Ginipral - not used in many countries due to serious side effects. The use of this group of drugs causes abnormalities in the mother's heart, and can also lead to cardiac arrhythmias, cardiac ischemia (pre-infarction and infarction) and pulmonary edema.
As numerous clinical researches, beta-sympathomimetics do not reduce the incidence of preterm birth, do not improve the outcome of pregnancy, do not reduce the incidence of newborns, do not improve the weight of newborns, and therefore should not be used by pregnant women, especially for the prevention of preterm birth. Many of these drugs have never been tested on pregnant women, although they are prescribed for the purpose of prolonging pregnancy, and the studies that have already been carried out are not enough to talk about the safety of beta-sympathomimetics for pregnant women and their offspring. For example, clinical studies of Ginipral regarding the prevention and management of preterm labor were carried out in the 1980s, and more recent publications are devoted to cases with serious side effects of hexoprenaline.
All beta mimetics affect carbohydrate metabolism, increasing blood sugar levels by almost 40%, which means increasing insulin production. In women with diabetes, blood sugar levels can rise even higher and lead to a loss of glucose control.
Very often, pregnant women are prescribed Ginipral with or without additional drugs ostensibly for the prevention of premature birth, if, God forbid, the doctor does not like the "hypertonicity of the uterus." Unfortunately, few pregnant women read the instructions for use of the drugs they are taking.
If beta-mimetics, which include ginipral, do not improve the outcome of pregnancy and do not lower the rate of preterm birth, is it worth prescribing this drug, which also has many side effects? The answer logically suggests itself: of course, in this case - not worth it. And why is it prescribed to almost all pregnant women in a row? Primarily because of reinsurance.

Pregnant women, long before pregnancy, are tuned in by doctors to pregnancy complications and "terrible" threats of pregnancy loss. Thus, the woman is in constant fear loss of pregnancy. First, she takes progesterone, then switches to ginipral - not a single day of pregnancy without a pill (I think that such a slogan can be hung during the course of most antenatal clinics). If, for some reason, a woman does not take the prescribed drugs, then in the event of an interruption and loss of pregnancy, she will reproach herself or she will be reproached for having lost her pregnancy due to her refusal to take medications.
Many women do not know and do not understand that the prescribed medications are often not related to the maintenance of pregnancy, or, conversely, can lead to termination of pregnancy if they are abused. Doctors also reinsure themselves so that later no one could reproach them that they did not do "everything possible" to preserve the pregnancy. The fact that the concept of "everything possible" has acquired big sizes in the number of dangerous and harmful drugs and procedures, no one analyzes, refutes or criticizes, since most work according to the principle "the more, the better, because what the hell is not kidding ..."
There is no need to be afraid of premature birth, although they are fraught with many negative consequences... But the mother's positive attitude, the absence of fear and panic act much more salutary than combinations of often unnecessary medications, on which a woman becomes psychologically dependent.

Substances that reduce the tone and contractile activity of the myometrium are used to stop premature labor, as well as in case of excessively violent labor.

Substances used to stop premature labor are denoted by the term " tocolytic agents"(Tokos - childbirth; lysis - termination).

Currently, β2-adrenomimetic agents are most often used as tocolytic agents, in particular, the drug fenoterol partusisten, salbutamol. Partusisten is administered by intravenous drip and, after the effect is achieved, continue to be administered orally in tablets. Side effects of partusisten: tachycardia a slight decrease blood pressure increasing blood sugar. Salbutamol is administered orally.

The tocolytic effect is exerted by magnesium sulfate when administered intravenously or intramuscularly, as well as ethyl alcohol.

With excessively violent labor, ether anesthesia is used.

Fenoterol

Pharmacology

pharmachologic effect - beta-adrenomimetic, bronchodilatory, tocolytic.

It excites beta 2 -adrenergic receptors, activates adenylate cyclase and causes the accumulation of cAMP. Relaxes the smooth muscles of the bronchi, stabilizes the membranes of mast cells and basophils (the release of biologically active substances decreases), improves mucociliary clearance. Increases heart rate and strength. Has a tocolytic effect. As a tocolytic agent, it is used orally and intravenously. Along with a decrease in the tone and contractile activity of the myometrium, it improves the uteroplacental blood flow, which leads to an increase in the oxygen concentration in the fetal blood.

Application of the substance Fenoterol

Broncho-obstructive syndrome: bronchospasm during exercise, spastic bronchitis in children, bronchial asthma, chronic obstructive bronchitis, pulmonary emphysema; bronchopulmonary diseases (silicosis, bronchiectasis, tuberculosis). As a bronchodilator drug before inhalation of other drugs (antibiotics, mucolytic drugs, glucocorticoids). For carrying out bronchodilator tests in the study of the function of external respiration.

In obstetrics: the threat of premature birth, the threat of spontaneous miscarriage after 16 weeks of pregnancy, after the application of a purse-string suture in case of cervical insufficiency, complicated labor during the period of cervical opening and fetal expulsion, intrauterine fetal hypoxia, urgent obstetric conditions (prolapse of the umbilical cord, threatening rupture of the uterus); cesarean section (the need to relax the uterus).

Side effects of the substance Fenoterol

hand tremors, dizziness, headache, nervousness, weakness, change in taste.

tachycardia, palpitations; when using high doses - a decrease in DBP and an increase in SBP, arrhythmia, angina pectoris; an increase in fetal heart rate.

On the part of the respiratory system: cough, paradoxical bronchospasm, dryness or irritation in the mouth or throat.

By organsGastrointestinal tract: nausea, vomiting.

Others: sweating, myalgia and muscle spasm, decreased motility upper divisions urinary tract, hypokalemia, allergic reactions.

Salbutamol

Pharmacology

pharmachologic effect - bronchodilator, tocolytic.

Highly selectively stimulates beta 2 -adrenergic receptors, activates intracellular adenylate cyclase. The bronchodilator effect is due to the relaxation of the smooth muscles of the bronchi. It is not destroyed by pulmonary catechol-O-methyltransferase and therefore has a long-term effect. Relaxes the uterus, inhibits the contractile activity of the myometrium, prevents premature birth.

When inhaled, 10–20% reaches the small bronchi and is gradually absorbed, part of the dose after swallowing is absorbed from the gastrointestinal tract. When using prolonged-release tablets, it is well absorbed. C max is 30 ng / ml. The duration of circulation in the blood at the therapeutic level is 3-9 hours, then the concentration gradually decreases. Plasma protein binding - 10%. Passes through the placenta, enters breast milk. Undergoes biotransformation in the liver. T 1/2 - 3.8 hours. It is excreted regardless of the route of administration with urine and bile, mainly unchanged (90%) or in the form of glucuronide.

The maximum speed of action (removal of bronchospasm) is achieved with the inhalation route of administration. Bronchodilation occurs as early as the 4-5th minute, increases by the 20th minute and reaches a maximum in 40-60 minutes; the duration of the effect is 4–5 hours. The most pronounced result is obtained after inhalation of 2 doses, a further increase in the dose does not lead to an increase in bronchial patency, but increases the likelihood of side effects (tremor, headache, dizziness). It has a positive effect on mucociliary clearance (in chronic bronchitis it increases it by 36%), stimulates mucus secretion, and activates the functions of the ciliated epithelium. It inhibits the release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced release of histamine, eliminates antigen-dependent suppression of mucociliary transport and the release of neutrophil chemotaxis factor. Prevents the development of allergen-induced bronchospasm. May cause desensitization and reduction in the number of beta-adrenergic receptors, incl. on lymphocytes. It has a number of metabolic effects - it reduces the content of potassium in the plasma, affects glycogenolysis and insulin secretion, and has hyperglycemic effects (especially in patients with bronchial asthma) and lipolytic effect, increases the risk of acidosis.

Application of the substance Salbutamol

Prevention and relief of bronchospasm in bronchial asthma, symptomatic treatment of broncho-obstructive syndrome (incl. Chronical bronchitis, chronic obstructive pulmonary disease, emphysema), nocturnal asthma (prolonged tablet forms); the threat of premature birth (at gestational periods from 16 to 38 weeks).

Side effects of the substance Salbutamol

From the side nervous system and sense organs: tremors (usually of the hands), anxiety, tension, increased excitability, dizziness, headache, sleep disturbances, short-term convulsions.

From the side of cardio-vascular system and blood (hematopoiesis, hemostasis): palpitations, tachycardia (during pregnancy - in the mother and fetus), arrhythmia, enlargement peripheral vessels, decrease in DBP or increase in SBP, myocardial ischemia, heart failure, cardiopathy.

By organsGastrointestinal tract: nausea, vomiting, dry or irritated mouth or throat, loss of appetite.

Others: bronchospasm (paradoxical or caused by hypersensitivity to salbutamol), pharyngitis, difficulty urinating, sweating, increased blood glucose, free fatty acids, hypokalemia (dose-dependent), allergic reactions in the form of erythema, facial edema, shortness of breath, the development of physical and mental drug dependence ...

Authors: Berezovskaya E.P.
In the past, obstetricians have tried several dozen drugs for stopping premature birth and maintaining pregnancy in the second and third trimester. Most medications are not accepted for use because of the serious side effects of such medications and possible harm to the fetus. It is hard to believe that alcohol was used to stop preterm labor in the last century, but now it is a historical fact.
Modern medicine has about sixty serious clinical studies on tocolytic therapy, not to mention a huge number (several hundred) of small studies. The use of tocolytics is a hot topic, since for many years doctors have been looking for a "panacea" so that they can get the desired result with the least negative impact on the mother and fetus. But such a panacea was not found. Moreover, having examined those drugs that were used in obstetrics with or without caution, doctors realized with considerable concern that most drugs could not be used. It turned out that it is not so easy to prevent or stop premature birth, and if this is possible, then it is possible to prolong the pregnancy only by 2-7 days, and very rarely until the calendar date.
Magnesium sulfate (magnesia), indomethacin and nifedipine remained in the arsenal of modern obstetrics.

The oldest and most common drug is a solution of magnesium sulfate - magnesia. Unlike other drugs, magnesium is more toxic to the mother and safer for the fetus. Most often, it causes nausea, hot flashes, headache, dizziness, blurred vision, in worst cases, impaired respiratory and cardiac functions. The most dangerous complication is pulmonary edema. Magnesium sulfate crosses the placenta and can cause respiratory impairment in newborns if this drug was used to stop labor, but unsuccessfully.
It is very unpleasant that magnesium is administered intravenously to almost every pregnant woman (worst of all - in the early stages of pregnancy), and day hospitals, where such women are sent, have become the cry of the latest "obstetric fashion", a kind of cultivator of all kinds of rumors, myths, prejudices and fears. This drug does not act on the uterus and does not suppress its contractile function in the early stages of pregnancy, so it should not be prescribed to everyone who has been diagnosed with uterine hypertonicity by ultrasound or who has something sore in the lower abdomen somewhere. The development of side effects is much more dangerous than the nonexistent benefits from the use of magnesia.
The specificity of magnesium sulfate is that the non-contracting uterus is not sensitive to this drug, so if there are no contractions, then the drug should not be prescribed. Foreign doctors, most of them, use this very principle, and besides, they do not use magnesium for more than two days, and in rare cases for more than 4 days.
The use of magnesium sulfate requires constant monitoring of laboratory parameters of electrolyte (salt) metabolism in the mother and her general condition, which, alas, is not practiced by many doctors.
Since no tocolytic drug has any advantages in prolonging pregnancy, after stopping the administration of magnesium, other tocolytics are not prescribed, including for the purpose of "prophylaxis".

If magnesia is preferred in the third trimester, then indomethacin is more effective in the second trimester, mainly up to 30 weeks of gestation. This drug belongs to the group of inhibitors of prostaglandin synthesis, or in other words, this drug inhibits the production of substances (prostaglandins) that play a role in the contraction of the muscles of the uterus. It is popular with non-pregnant women for the treatment of premenstrual syndrome and painful periods.
Indomethacin is also effective for polyhydramnios. However, this drug has a negative effect on the fetus, especially if it is used in the third trimester, so it is usually not prescribed after 32 weeks. In women, it can cause gastrointestinal bleeding, allergic reactions and bleeding disorders. Headache and dizziness are also common. From the same group of drugs, naproxen, aspirin and a number of other drugs were occasionally used, but there is little information about their benefits in preventing premature birth.

The hormonal drug, progesterone, in its various forms, which is abused in early pregnancy, has been used for a period of time in pregnant women between 24-32 weeks of gestation, but the results have been inconsistent. Most doctors do not use progesterone or its analogues during the second half of pregnancy.

Nifedipine, which belongs to the group of calcium channel blockers and is often used to treat hypertension and cardiovascular diseases, is treated with great caution, as it is a new drug in obstetrics. It also has many side effects, however, when used correctly, it is very effective in short term prolongation of pregnancy.

One of the new drugs that began to be used in obstetrics not so long ago is nitroglycerin. Nitroglycerin is known to many older people suffering from cardiovascular diseases, in particular angina pectoris or angina pectoris. The drug exists in various forms and for the prevention of preterm birth after invasive procedures (amniocentesis, cordocentesis, laser arresting of placental vessels, etc.), as well as for stopping preterm labor, it is used in the form of percutaneous patches, intravenous infusions or droppers, nasal sprays, tablets under the tongue. The effectiveness of nitroglycerin is still being studied in a number of countries by conducting large clinical trials. Like all tocolytics, nitroglycerin is prescribed only at 24-32 weeks, not earlier or later.
The indication for the appointment of nitroglycerin is the presence of at least 4 contractions within 20 minutes and the shortening of the cervix, that is, the criteria for setting preterm labor are taken into account. Also, this drug is not prescribed if another tocolytic drug has been prescribed to the woman before.

Preparations from the group of beta-sympathomimetics, which include terbutaline, ritodrin, and genipral, which is very well-known in the former Soviet Union, are not used in many countries due to serious side effects. The use of this group of drugs causes abnormalities in the mother's heart, and can also lead to cardiac arrhythmias, cardiac ischemia (pre-infarction and infarction) and pulmonary edema.
Numerous clinical studies have shown that beta-sympathomimetics do not reduce the incidence of preterm birth, do not improve the outcome of pregnancy, do not reduce the incidence of newborns, do not improve the weight of newborns, and therefore should not be used by pregnant women, especially for the prevention of preterm birth. Many of these drugs have never been tested on pregnant women, although they are prescribed for the purpose of prolonging pregnancy, and the studies that have already been carried out are not enough to talk about the safety of beta-sympathomimetics for pregnant women and their offspring. For example, clinical studies of genipral regarding the prevention and management of preterm labor were carried out in the 1980s, and more recent publications are devoted to cases with serious side effects of hexoprenaline.
All beta mimetics affect carbohydrate metabolism, increasing blood sugar levels by almost 40%, which means increasing insulin production. In women with diabetes, blood sugar levels can rise even higher and lead to a loss of glucose control.
Very often, pregnant women are prescribed genipral with or without additional medications, ostensibly for the prevention of premature birth, if, God forbid, the doctor does not like the "uterine hypertonicity". Unfortunately, few pregnant women read the instructions for use of the drugs they are taking.
If beta-mimetics, which include genipral, do not improve the outcome of pregnancy and do not lower the rate of preterm birth, is it worth prescribing this drug, which also has many side effects? The answer logically suggests itself: of course, in this case - not worth it. And why is it prescribed to almost all pregnant women in a row? Primarily because of reinsurance.

Pregnant women, long before pregnancy, are tuned in by doctors to pregnancy complications and "terrible" threats of pregnancy loss. Thus, the woman is in constant fear of losing her pregnancy. First, she takes progesterone, then she switches to genipral - not a single day of pregnancy without a pill (I think that such a slogan can be hung during the course of most antenatal clinics). If, for some reason, a woman does not take the prescribed drugs, then in the event of an interruption and loss of pregnancy, she will reproach herself or she will be reproached for having lost her pregnancy due to her refusal to take medications.
Many women do not know and do not understand that the prescribed medications are often not related to the maintenance of pregnancy, or, conversely, can lead to termination of pregnancy if they are abused. Doctors also reinsure themselves so that later no one could reproach them that they did not do "everything possible" to preserve the pregnancy. The fact that the concept of "everything possible" has acquired large dimensions in the number of dangerous and harmful drugs and procedures, no one analyzes, refutes or criticizes, since most work according to the principle "the more, the better, because why the devil is not joking ... "
There is no need to be afraid of premature birth, although they are fraught with many negative consequences. But the mother's positive attitude, the absence of fear and panic act much more salutary than combinations of often unnecessary medications, on which a woman becomes psychologically dependent.

Gynipral

Synonyms: Hexoprenaline.

Pharmachologic effect. In connection with the influence on the 6a2-adrenergic receptors of the uterus, it has a tocolytic (relaxing the muscles of the uterus) effect. Corresponds to the drug hexoprenaline.

Indication for use. It is used as a tocolytic agent with the threat of premature birth (in the third trimester of pregnancy), with acute intrauterine fetal asphyxia (impaired blood supply to the fetus), during childbirth (with discoordinated labor - improper contractions of the uterus during childbirth), to suppress uterine contractions before surgical intervention(incision of the cervix, cesarean section).

Method of administration and dosage. Ginipral is used intravenously and inside (in tablets). A "shock" dose (in acute cases) is injected intravenously slowly - 5-10 μg of ginipral in 10-20 ml of isotonic sodium chloride solution. For infusions (with long-term treatment), dilute 50 μg (contents of 2 ampoules of 25 μg each - "concentrate" of ginipral) in 500 ml of 5% glucose solution. Injected at a rate of 25 drops per minute (about 0.125 μg per minute). If necessary, the dose is increased by 5 drops every 5 minutes. The minimum injection rate is 10 drops per minute, maximum speed introduction - 60 drops per minute.

The tablets begin to be taken 2-3 hours before the end of the parenteral (intravenous) administration. First, 1 tablet is prescribed, then after 3 hours, 1 tablet every 4-6 hours; only 4-8 tablets per day.

Side effect. Headache, anxiety, tremors (tremors of the limbs), sweating, dizziness are possible. Rarely - nausea, vomiting. There are isolated reports of intestinal atony (loss of tone); an increase in the content of serum transaminases (enzymes). An increase in the mother's heart rate, a decrease in blood pressure, especially diastolic ("lower" blood pressure), is possible. In several cases, ventricular extrasystoles(cardiac arrhythmias) and complaints of pain in the region of the heart. These symptoms disappear after stopping treatment. The fetal heart rate in most cases does not change or changes little. An increase in the concentration of glucose (sugar) in the blood. This effect is more pronounced in patients with diabetes mellitus. Decreased urine output (urination), especially in initial phase treatment. During the first few days of treatment, a decrease in the concentration of calcium in the blood plasma is possible; in progress further treatment the calcium concentration is normalized.

Contraindications Thyrotoxicosis (disease thyroid gland); cardiovascular diseases especially tachyarrhythmia (heart rhythm disturbance), myocarditis (inflammation of the muscles of the heart), lesions mitral valve, idiopathic hypertrophic subaortic stenosis (non-inflammatory disease muscle tissue the left ventricle of the heart, characterized by a sharp narrowing of its cavity); serious illnesses kidney and liver; angle-closure glaucoma (increased intraocular pressure); heavy uterine bleeding; premature detachment of the placenta; infectious lesions endometrium (inner lining of the uterus); hypersensitivity to the drug, especially in patients with bronchial asthma.

Release form. In ampoules containing 0.025 mg or 0.01 mg each; tablets of 0.5 mg.

Storage conditions.

Isoxuprine (Isoxsuprine )

Synonyms: Duvadilan.

Pharmachologic effect. It has a tocolytic (relaxing the muscles of the uterus) effect by stimulating beta-adrenergic receptors. Reduces the tone of smooth muscles blood vessels skeletal muscles, eliminates spasm (sharp narrowing of the lumen) of blood vessels, increases blood supply to tissues

Indication for use. Threat of premature birth, obliterating endarteritis (inflammation of the inner lining of the arteries of the extremities with a decrease in their lumen), Raynaud's disease (narrowing of the lumen of the vessels of the extremities), spasm of peripheral vessels.

Method of administration and dosage. With the threat of premature birth, intravenous drip infusion is prescribed (100 mg of the drug per 500 ml of 5% glucose solution) at a rate of 1-1.5 ml / min; the rate of administration is gradually increased to 2.5 ml / min. When the condition improves (cessation of contractions), they switch to intramuscular injection drug: within 24 hours - 10 mg every 3 hours. In the next 48 hours, 10 mg every 4-6 hours. After that, within 2 days, isoxsuprine is prescribed orally, 20 mg 4 times a day. In diseases of peripheral vessels, it is prescribed orally at 20 mg 4 times a day. In more severe cases, intravenous drip administration is prescribed (20 mg of the drug per 100 ml of 5% glucose solution) at a rate of 1.5 ml / min 2 times a day. Intramuscular administration of the drug, 10 mg 3-4 times a day, is also possible.

Side effect. Tachycardia (increased heart rate), hypotension (lower blood pressure), dizziness, flushing of the upper half of the body, to the face with parenteral administration(intravenously and intramuscularly); nausea, vomiting, rash.

Contraindications Recent bleeding, hypotension (low blood pressure), angina pectoris.

Release form. Tablets of 0.02 g of isoxsuprine hydrochloride in a package of 50 pieces; solution for injection (in 1 ml 5 mg of isoxsuprine hydrochloride) in 2 ml ampoules in a package of 6 pieces.

Storage conditions. List B. In a cool place.

PARTUSISTEN (Partusisten)

Synonyms: Fenoterol.

Pharmachologic effect. It has a tocolytic (relaxing the muscles of the uterus) effect. Belongs to the group of beta2-adrenostimulants. Corresponds to the drug fenoterol.

Indication for use. The experience of using partusisten shows that it is effective remedy to eliminate the threat of premature birth and does not adversely affect the fetus and newborn.

Method of administration and dosage. Assign intravenously (drip) and inside in the form of tablets. Shortly after the start intravenous administration usually there is a significant decrease in pain, the tension of the uterus is relieved, then the pain and contractions of the uterus completely stop.

Inside take 5 mg every 2-3 hours; daily dose- up to 40 mg. With increased sensitivity (the appearance of tachycardia / increased heart rate /, muscle weakness, etc.), a single dose is reduced to 2.5 mg, and the daily dose is reduced to 30 mg. The duration of the course of treatment is 1-3 weeks. Intravenous drip (0.5 mg in 250-500 ml of 5% glucose solution) is injected at 15-20 drops per minute until the contraction of the uterus is inhibited.

Partusisten is used in specialized hospitals under close medical supervision.

Side effect. The drug can cause tachycardia, tremors (tremors) of the hands, muscle weakness, decreased blood pressure, sweating, nausea, and vomiting. It is noted that side effects decrease under the influence of verapamil - 30 mg intravenously.

Contraindications Heart defects, disorders heart rate, thyrotoxicosis (thyroid disease), glaucoma (increased intraocular pressure).

Release form. Ampoules of 0.025 mg; tablets of 0.5 mg.

Storage conditions. List B. In the dark place.

RITODRIN (Ritodrinum)

Synonyms: Prempar, Pre-Par, Utopar.

Pharmachologic effect. The action is close to fenoterol, salbupart and other beta2-adrenergic agonists.

Indication for use. It is used as a tocolytic (relaxing the muscles of the uterus) means with the threat of premature termination of pregnancy.

Method of administration and dosage. Inside appoint 5-10 mg 4-6 times a day. Usually, at these doses, uterine contractions stop and the possibility of maintaining pregnancy increases. The duration of the drug is 1-4 weeks. With the onset of preterm labor, oral (through the mouth) use is not effective enough and the drug is administered intravenously; To do this, dilute 50 mg of the drug in 500 ml of isotonic sodium chloride solution and inject it drip, starting at 10 drops per minute, then gradually increase the rate of administration (15 drops) until the uterus is completely relaxed. To continue the effect, the drug is administered intramuscularly at 10 mg every 4-6 hours, after which it is administered orally at 10 mg 4-6 times a day with a gradual dose reduction.

Ritodrin, as well as partusisten, is used in specialized medical institutions.

Side effects and contraindications. Possible side effects and precautions are the same as with Partusisten.

Release form. 5 mg tablets; ampoules of 10 mg.

Storage conditions. List B. In the dark place.

SALBUPART

Synonyms: Salbutamol, Ventolin, Ekovent, etc.

Pharmachologic effect. By its action on the contractile activity of the uterus, salbupart is close to partusisten. Refers to beta2-adrenostimulants. Corresponds to the drug salbutamol.

Indication for use. It is used as a tocolytic (relaxing the muscles of the uterus) means to eliminate the threat of premature birth, as well as after operations on the pregnant uterus.

Method of administration and dosage. Introduced intravenously. The contents of one ampoule (5 mg) are diluted in 400-500 ml of isotonic sodium chloride solution or 5% glucose solution. Enter at a rate of 15-20 drops (starting with 5 drops) per minute. The rate of administration depends on the intensity of uterine contractions and tolerance (monitor heart rate and other hemodynamic parameters). Duration of administration is 6-12 hours.

Side effects and contraindications are the same as for partusisten.

Release form. 0.1% solution in capsules of 5 ml (5 mg).

Storage conditions. List B. In the dark place.

TERBUTALIN (Terbutalin)

Synonyms: Brikanil, Arubendol, Betasmak, Brika-lin, Brikan, Brikar, Drakanil, Spiranil, Terbutol, Tergil, etc.

Pharmachologic effect. By pharmacological properties close to salbutamol. It has a tocolytic (relaxing the muscles of the uterus) effect.

Indication for use. Used as a tocolytic (relaxing the muscles of the uterus) means to eliminate the threat of premature birth.

Method of administration and dosage. As a tocolytic agent (in obstetric practice) is used in the form of drip intravenous infusion (10-25 μg per minute in isotonic solution glucose or sodium chloride) with a further transition to subcutaneous injections (250 μg = 1/2 ampoule) 4 times a day for 3 days. At the same time, 5 mg is administered orally 3 times a day.

Side effects and contraindications are the same as for partusisten (see page 378).

Release form. Tablets of 0.0025 g (2.5 mg) in a package of 20 pieces; 0.05% solution (0.5 mg) of terbutaline sulfate in ampoules containing 1 ml each, in a package of 10 ampoules.

Storage conditions. List B. In the dark place.

TROPACIN (Tropacinum)

Synonyms: Diphenyltropine hydrochloride, Tropazin.

Pharmachologic effect. In terms of pharmacological properties, tropacin is close to atropine (see page 92). In obstetric practice, it is used as an antispasmodic (relieving spasms) agent that inhibits contractile activity uterus.

Indication for use. As a tocolytic (relaxing the muscles of the uterus) a remedy for the threat of premature birth and abortion.

Method of administration and dosage. As a tocolytic agent inside 0.02 g 2 times a day.

Side effects and contraindications

Release form. Tablets 0.001; 0; 003; 0.005; 0.01; 0.015 g in a package of 10 pieces.

Storage conditions. List A. In a well-closed container, protected from light.

Tocolytics are drugs that have a tocolytic effect, which consists in reducing the tone of the uterus and stopping or decreasing its contractions. These drugs are usually used during pregnancy. The purpose of their use is to prevent premature birth and improve blood supply to the placenta, if a woman has later dates toxicosis develops.

Tocolytics - what is it?

Tocolytics are a group of drugs with beta-adrenomimetic activity. Their action is aimed at two purposes: reducing the tone uterine muscles and expansion of the lumen of the vessels of the placenta.

When using tocoliths for treatment, smooth muscles relax, the frequency and strength of its rhythmic contractions (contractions) decrease, and labor activity stops. Also, drugs belonging to this group are able to dilate blood vessels, improving blood flow in the uterus and placenta, which increases the flow of oxygen and essential substances to the fetus. In addition, tocolytics dilate the bronchi, which improves the flow of oxygen into the body and activates metabolism.

Classification of tocolytics

Tocolytics have a rather complex classification, since this group medications combines drugs with different mechanisms of action.

The most commonly used drugs in this group are adrenergic agonists related to beta-2-adrenergic receptor stimulants. Their representatives are drugs such as izadrin, partusisten, fenoterol and others. The action of these medicines based on the fact that when they are taken, the beta-2-adrenergic receptors of the uterus are activated, which improves the blood supply to this organ. At the same time, relaxation of the muscles of the uterus is observed. In addition, when using these drugs, there is a weakening of intestinal motility, mild tachycardia, and other side effects are possible.

Another group of tocolytics are preparations based on magnesia, or magnesium sulfate. They reduce the activity of the uterus and inhibit labor.

Also have a mild tocolytic effect acetylsalicylic acid and indomethacin, which suppress the production of prostaglandins. The use of papaverine as tocolytics, no-shpy and other antispasmodics is ineffective.

Tocolytics during pregnancy: use

Indications for the use of tocolytics during pregnancy are the following factors:

• an increased likelihood of a miscarriage in a woman for more than 16 weeks;
• fetal asphyxia;
• too active generic activity with insufficient preparation birth canal, for example, with a small dilatation of the cervix;
• the threat of premature birth;
• contractions with unambiguous indicators for the use of a cesarean section;
• the possibility of uterine rupture;
• rupture of the bladder, accompanied by the loss of umbilical cord elements;
• severe pain during childbirth.

Conditions for the use of tocolytics

Most often, tocolytics are prescribed when the likelihood of premature birth or the threat of miscarriage after 15 weeks of pregnancy. They can also be prescribed to regulate uterine contractions during the period of cervical dilatation and childbirth in pathologies such as hypertonicity, too strong uncoordinated muscle contractions, tetanus and other conditions. The conditions for the use of tocolytics are considered to be a living fetus and a whole fetal bladder, as well as an insignificant release of water. It is possible to prescribe these drugs when the uterus is dilated up to 4 cm.

Tocolytics in obstetrics: contraindications

Contraindications for the use of tocolytics are:

• multiple pregnancy;
• individual hypersensitivity to drug components;
• death of the fetus before the onset of labor;
• detachment or placenta previa;
• lactation period;
• diseases of the cardiovascular system, such as high blood pressure, heart failure, heart attack, severe bleeding, tachycardia, blood clotting disorders, heart defects;
• common diseases: diabetes, glaucoma, auditory pathology or vestibular apparatus, ulcer, colitis and others;
• kidney problems, manifested by severe swelling of the legs;
• intrauterine infections.

From side effects of this group of drugs, the following are most often found:

• deterioration of visual function;
• increased excitability and nervousness;
• weakness and dizziness;
• hearing loss;
• possible nosebleeds;
• deterioration in the perception of taste, the appearance of a feeling of bitterness and dry mouth;
• tachycardia;
• shortness of breath resulting from spasm of small bronchi;
• pain in the abdomen, muscles and migraines and more.

Tocolytic drugs: list

The list of drugs related to tocolytics includes:

1. Fenoterol and similar agents - fenoterol hydrobromide and Berotek.
2. Partusisten and its analogues: Salgim and Ginipral.
3. Indomethacin and preparations based on it: Indovis, Indobene and others.
4. Terbutaline.