Composition, form of production and packaging
The solution for intravenous and / or injection is colorless, transparent.
1 ml
oxytocin 5 IU
Excipients: glacial acetic acid - 2.5 mg, chlorobutanol hemihydrate - 3 mg, ethanol 96% - 40 mg, water d / and - up to 1 ml.
1 ml - glass ampoules (5) - contour plastic packaging (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
Synthetic hormone preparation. On pharmacological and clinical properties is similar to endogenous oxytocin of the posterior lobe of the pituitary gland. Interacts with oxytocin-specific receptors of uterine myometrium, belonging to the superfamily of G-proteins. The number of receptors and the reaction to the action of oxytocin increase with the progression of pregnancy and reach a maximum toward its end. Stimulates the genital activity of the uterus by increasing the permeability of cellular membranes for calcium and increasing its intracellular concentration, also by further reducing the resting potential of the membrane and increasing its excitability.Causes contractions, like normal spontaneous labor, temporarily worsening the blood supply of the uterus. With an increase in the amplitude and duration of muscle contractions, the uterine pharynx extends and smooths. In appropriate quantities it is able to strengthen the contractile capacity of the uterus from moderate in strength and frequency, characteristic of spontaneous motor activity, to the level of prolonged tetanic contractions.
Causes the reduction of myoepithelial cells adjacent to the alveoli of the breast, improving the excretion of breast milk.
Influencing the smooth muscles of the vessels, causes vasodilation and increases blood flow in the kidneys, coronary vessels and vessels of the brain. Typically, blood pressure remains unchanged, however, with IV injection in high doses or a concentrated solution of oxytocin, blood pressure may temporarily decrease with the development of reflex tachycardia and a reflex increase in cardiac output. Following the initial decline in blood pressure should be a long, although a slight increase.
In contrast to vasopressin, oxytocin has minimal antidiuretic effect, however, hyperhydration is possible with the administration of oxytocin with large quantities of electrolyte solutions and / or with too rapid administration. Does not cause contraction of the muscles of the bladder and intestines.
PHARMACOKINETICS
With iv introduction, the action of oxytocin on the uterus appears almost instantaneously and lasts for 1 hour. With the / m introduction, the myotonic action occurs in the first 3-7 minutes and lasts for 2-3 hours.
Like vasopressin, oxytocin is distributed throughout the extracellular space. Small amounts of oxytocin, apparently, fall into the fetal circulation system. T 1/2 is 1-6 minutes and becomes shorter in late pregnancy and lactation. Most of the drug is rapidly metabolized in the liver and kidneys. In the process of enzymatic hydrolysis, it is inactivated, first of all, under the influence of tissue oxytokinase (oxytokinase is also in the placenta and plasma). Only a small amount of oxytocin is excreted in the urine unchanged.
INDICATIONS
- for induction and stimulation of labor: primary and secondary weakness of labor; the need for early delivery in connection with gestosis, Rh-conflict, intrauterine fetal death; a premature pregnancy; premature discharge of amniotic fluid;
- management of births in the pelvic presentation;
- for prophylaxis and treatment of hypotonic bleeding after abortion (including for long periods of pregnancy);
- in the early postpartum period to accelerate postpartum involution of the uterus;
- for contraction of the uterus in cesarean section (after removal of the afterbirth).
DOSING MODE
In / in or / m.
In order to induce and strengthen labor activity, oxytocin is used exclusively in / in, in a hospital setting, under appropriate medical supervision. The simultaneous use of the drug in / in and / m is contraindicated. The dose is selected taking into account the individual sensitivity of the pregnant and fetus.
For rodovozbuzhdeniya and stimulation of labor, oxytocin is used exclusively as an intravenous drip infusion. Strict monitoring of the prescribed rate of infusion is mandatory. For the safe use of oxytocin during stimulation and strengthening of labor, it is necessary to use an infusion pump or other similar device, as well as monitoring the force of uterine contractions and cardiac activity of the fetus. In case of excessive strengthening of the contractile activity of the uterus, the infusion should be stopped immediately, as a result, the excess muscular activity of the uterus rapidly decreases.
1. Before starting the drug, you should start to enter a physiological solution that does not contain oxytocin.
2. To prepare a standard infusion of oxytocin in 1000 ml of non-hydrating fluid, dissolve 1 ml (5 IU) of oxytocin and mix thoroughly by rotating the vial. In 1 ml of the infusion so prepared, 5 DM of oxytocin are contained. For an accurate dosing of the infusion solution, an infusion pump or other similar device should be used.
3. The rate of administration of the initial dose should not exceed 0.5-4 mJ / min, which corresponds to 2-16 cap / min. 1 drop of infusion contains 0.25 MED oxytocin). Every 20-40 minutes it can be increased by 1-2 mU / min, until the desired degree of contractile activity of the uterus is achieved. After reaching the desired frequency of uterine contractions corresponding to spontaneous labor, and with the opening of the uterine pharynx to 4-6 cm in the absence of signs of fetal distress, it is possible to gradually reduce the infusion rate at a rate similar to its acceleration.
In later pregnancy, infusion with greater speed requires caution, only in rare cases, a speed exceeding 8-9 mU / min may be required. In the case of preterm labor, a high rate may be required, which in some cases may exceed 20 mU / min (80 cap / min).
1. It is necessary to control the heartbeat of the fetus, the tone of the uterus at rest, the frequency, duration and force of its contractions.
2. In case of uterine hyperactivity or fetal distress, oxytocin should be discontinued immediately and oxygen therapy should be provided to the mother. The condition of the mother and fetus must be checked again by a specialist doctor.
Prevention and treatment of hypotonic bleeding in the puerperium
1. In / in drip infusion: in 1000 ml of non-hydrating fluid dissolve 10-40 IU of oxytocin; for the prevention of uterine atony usually requires 20-40 pm / min oxytocin.
2. Intramuscular injection: 5 IU / ml oxytocin after placental separation.
Incomplete or abortive abortion
10 IU / ml of oxytocin is added to 500 ml of saline or a mixture of 5% glucose and physiological saline. The rate of intravenous infusion is 20-40 cap / min.
SIDE EFFECT
At parturient women
On the part of the reproductive system: with high doses or hypersensitivity - hypertension of the uterus, spasm, tetany, rupture of the uterus; increased bleeding in the postpartum period as a result of oxytocin induced thrombocytopenia, afibrinogenemii and gipoprotrombinemii, sometimes hemorrhages in the pelvic organs. With careful medical supervision of childbirth, the risk of bleeding in the postpartum period is reduced.
From the cardiovascular system : when used in high doses - arrhythmia, ventricular extrasystole, severe arterial hypertension (in the case of vasopressor drugs), arterial hypotension (with simultaneous application with anesthetic cyclopropane), reflex tachycardia, shock, with too rapid introduction - bradycardia, subarachnoid hemorrhage.
From the digestive system : nausea, vomiting.
From the side of water-electrolyte metabolism : severe hyperhydration with prolonged intravenous administration (usually at a speed of 40-50 pm / min) with a large amount of fluid (antidiuretic effect of oxytocin), can occur with a 24-hour slow infusion of oxytocin, accompanied by convulsions and coma; rare - lethal outcome.
Allergic reactions: anaphylaxis and other allergic reactions, with too rapid introduction of bronchospasm; rare - lethal outcome.
In a fetus or newborn
As a consequence of the administration of oxytocin to the mother, a low Apgar score at the 1st and 5th minutes, hyperbilirubinemia of newborns, with too rapid introduction, a decrease in the level of fibrinogen in the blood, bleeding in the retina of the eye; as a consequence of the contractile activity of the uterus - sinus bradycardia, tachycardia, ventricular extrasystole and other arrhythmias, changes in the CNS, fetal death as a result of asphyxiation.
CONTRAINDICATIONS
- the presence of contraindications for vaginal delivery (eg, presentation or prolapse of the umbilical cord, full or partial placenta previa);
- a narrow basin (anatomical and clinical);
- transverse or oblique position of the fetus;
- facial presentation of the fetus;
- premature birth;
- threatening rupture of the uterus;
- the uterus after multiple births;
- partial presentation of the placenta;
- uterine septicemia;
- invasive cervical carcinoma;
- Hypertension of the uterus (which did not occur during childbirth);
- compression of the fetus;
- arterial hypertension;
- chronic renal failure;
- Hypersensitivity to the components of the drug.
PREGNANCY AND LACTATION
In the first trimester of pregnancy oxytocin is used only for spontaneous or induced abortions. Numerous data on the use of oxytocin, its chemical structure and pharmacological properties indicate that, if the recommendations are adhered to, the likelihood of the effect of oxytocin on increasing the frequency of formation of malformations of the fetus is low.
In small amounts excreted in breast milk.
When using the drug to stop uterine bleeding for breast-feeding, you can proceed only after the course of treatment with oxytocin.
APPLICATION FOR FUNCTIONS OF THE LIVER
In the presence of contraindications for vaginal delivery (including with a violation of kidney function) the drug is prohibited.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Data on the use of the drug in patients with violations of the liver are not provided.
APPLICATION IN ELDERLY PATIENTS
Not applicable.
SPECIAL INSTRUCTIONS
Before the insertion of the fetal head into the pelvic inlet, oxytocin can not be used to stimulate labor.
Before you start using oxytocin, you should compare the expected benefits of therapy with the possibility, albeit small, of the development of hypertension and tetany of the uterus.
Each patient receiving oxytocin IV, should be in hospital under the constant supervision of experienced specialists who have experience in using the drug and recognizing complications. If necessary, immediate assistance from a specialist doctor should be provided. To avoid complications during the use of the drug should be constantly monitored uterine contractions, cardiac activity of the woman in labor and fetus, blood pressure. If signs of hyperactivity in the uterus should immediately stop the introduction of oxytocin, resulting in uterine contractions caused by the drug, usually soon subsided.
With adequate use, oxytocin causes uterine contractions similar to spontaneous labor. Excessive stimulation of the uterus with improper application of the drug is dangerous for the woman in labor, and for the fetus. Even with adequate application of the drug and appropriate observation, hypertensive contractions of the uterus occur with increased sensitivity of the uterus to oxytocin.
It is necessary to consider the risk of development of afibrinogenemia and increased blood loss.
There are cases of maternity death as a result of hypersensitivity reactions, subarachnoid hemorrhage, uterine rupture and fetal death for various reasons associated with parenteral administration of the drug for the induction of labor and stimulation of labor in the first and second birth periods.
As a result of the antidiuretic effect of oxytocin, the development of hyperhydration is possible, especially with the use of a constant infusion of oxytocin and the consumption of fluid inside.
The drug can be diluted in solutions of sodium lactate, sodium chloride and glucose. The finished solution should be used within the first 8 hours after its preparation.Compatibility studies were performed with infusions of 500 ml.
The effect of the drug on the ability to drive a car and mechanisms, work on which is associated with an increased risk of injury
Oxytocin does not affect the ability to drive a car and mechanisms that are associated with an increased risk of injury.
OVERDOSE
Symptoms mainly depend on the degree of uterine hyperactivity, regardless of the presence of hypersensitivity to the drug. Hyperstimulation with hypertonic and tetanic contractions or with a basal tone? 15-20 mm aq. Art. between two contractions leads to discoordination of labor, tearing of the body or cervix, vagina, bleeding in the postpartum period, utero-placental insufficiency, fetal bradycardia, its hypoxia, hypercapnia, compression, birth trauma or death. Hyperhydration with seizures as a result of the antidiuretic effect of oxytocin is a serious complication and develops with prolonged administration of the drug in high doses (40-50 ml / min).
Treatment of hyperhydration: elimination of oxytocin, restriction of fluid intake, use of diuretics to force diuresis, IV injection of hypertonic saline, correction of electrolyte imbalance, arresting seizures with appropriate doses of barbiturates and ensuring careful care of the patient in a coma.
DRUG INTERACTION
With the introduction of oxytocin 3-4 h after the application of vasoconstrictors together with caudal anesthesia, severe arterial hypertension is possible.
With anesthesia with cyclopropane, halothane, cardiovascular action of oxytocin may change, with unforeseen development of arterial hypotension, sinus bradycardia, and AV rhythm in the parturient woman during anesthesia.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of 2 В° to 15 В° C. Shelf life - 3 years.
