Desaminooxytocin® [Demoxytocin]

Pharmacological properties

in chemical structure, demoxytocin is close to oxytocin - the hormone of the posterior pituitary gland. it can be considered as a synthetic analogue of oxytocin. the mechanism of action and pharmacological properties of demoxytocin and oxytocin are similar. demoxytocin affects the permeability of the cell membrane, increasing the content of calcium ions in smooth muscle cells, thereby increasing its contraction. the drug stimulates the contraction of smooth muscles of the uterus, as well as stimulating the contraction of myoepithelial cells of the mammary gland, enhances the secretion of milk.

With buccal administration, demoxytocin, unlike oxytocin, is not cleaved by saliva enzymes, and easily penetrates the oral mucosa into the systemic circulation. Uterine contractions begin 20–40 min (max. 50–60 min) after buccal administration of demoxytocin. The effect is dose dependent and lasts up to 180 minutes. The uterotonic activity of demoxytocin is 2 times higher than the activity of oxytocin. In the postpartum period, demoxytocin accelerates uterine involution and shortens postpartum hemorrhage.

The lactogenic effect of demoxytocin begins earlier, is more pronounced and lasts longer compared to oxytocin due to resistance to enzymatic inactivation. Demoxytocin stimulates the formation and excretion of milk, normalizes the process of lactation, preventing hardening of the breast and the formation of mastitis.

Demoxitocin does not have a pronounced vasopressor and antidiuretic activity, so it can be used by women with hypertension, late pregnancy toxicosis and impaired renal function.

Pharmacokinetics Demoxytocin is rapidly and completely absorbed through the mucous membrane of the oral cavity and enters the bloodstream. With buccal administration of 1 tablet of 50 IU, demoxytocin is absorbed within 15-30 minutes. Saliva enzymes do not destroy the drug because it is resistant to oxytocinase; elimination of demoxytocin is carried out within 30-60 minutes.

Indications

To excite and strengthen labor activity with its primary and secondary weakness; to stimulate lactation in the postpartum period.

Application

The tablet is applied buccally, laying on the cheek alternately to the right and left, holding in the mouth until complete disintegration and absorption. to excite and stimulate labor, usually 50 IU (1 tablet) is used every 30 minutes; the required amount of the drug is determined individually. with the appearance of regular, strong contractions, the following single doses should be reduced by 2 times (apply ½ tablet) or increase the interval between doses (up to 1 hour). the maximum dose is usually 500 IU (10 tablets), rarely ≥900 IU. in the absence of effect, the drug can be taken again after 24 hours, if permissible.

To stimulate lactation, demoxytocin should be administered from the 2nd to the 6th postpartum day, 25–50 IU (½ – 1 tablet) 5 minutes before the baby is fed 2–4 times a day.

Children. Do not prescribe to children.

Contraindications

Hypersensitivity to demoxytocin and / or any of the excipients of the drug. hypertensive contractions of the uterus, mechanical damage to the reproductive tract, fetal hypoxia, fetal death.

Inconsistency in the size of the pelvis and fetus, transverse or oblique position of the fetus, placenta or umbilical cord vessels, premature detachment of the placenta, omission of the umbilical cord, threatening uterine rupture due to a large number of pregnancies, uterine distension (multiple pregnancy, polyhydramnios), invasive carcinoma , a large number of pregnancies and the presence of scars on the wall of the uterus after surgery, including cesarean section.

The drug can not be used for a long time with severe preeclampsic toxicosis and severe diseases of the heart and blood vessels, as well as in the case of an inert uterus (resistance to demoxytocin / oxytocin).

Side effects

In therapeutic doses, demoxitocin does not cause clinically significant side effects. the use of demoxytocin in high doses and increased sensitivity of the uterus can lead to the following side effects:

in the mother: uterine cramps (also when used in low doses), uterine hypertonicity, tetanic contractions, uterine hyperactivity with uterine and vaginal tissue ruptures; nausea, vomiting, hypersalivation, increased blood pressure, tachycardia, arrhythmia; death is possible. In case of complications of pregnancy and childbirth, life-threatening afibrinogenemia, postpartum hemorrhage, and anaphylactic shock can occur. There is a risk of disseminated intravascular coagulation (DVK);

in the fetus: bradycardia, arrhythmia, asphyxia, acute fetal hypoxia, staining of amniotic fluid with meconium; death is possible;

in newborns: there may be jaundice, retinal hemorrhage.

The following side effects are ordered according to the classification of organ system groups and the frequency of MedDRA: very often (≥1 / 10), often (≥1 / 100 to 1/10), infrequently (≥1 / 1000 to 1/100), rarely ( ≥1 / 10,000 to 1/1000), very rarely (1/10 000), unknown (cannot be determined from the available data).

On the part of the immune system: rarely - hypersensitivity reactions, including anaphylactic reactions (with difficulty breathing, hypotension, or shock).

From the nervous system: often - headache.

From the side of the heart: often - tachycardia, bradycardia; infrequently - arrhythmia.

From the digestive tract: often - nausea, vomiting.

On the part of the skin and subcutaneous tissues: rarely - rashes.

special instructions

The use of demoxytocin can be carried out only for medical reasons, under the supervision of medical personnel in a maternity hospital. during drug-induced stimulation of labor, careful monitoring of the woman in labor is required (control of the intensity of uterine contractions, opening of the cervix, fetal advancement through the birth canal, heart rate and position of the fetus, individual patient response to demoxitocin, dose selection if necessary). with excessively strong labor, the use of the drug should be discontinued.

Particular care should be taken:

• if there is a risk of mismatch in the size of the fetus and pelvis (do not use demoxytocin if the risk is significant);
• in the presence of secondary inertness of the uterus;
• Hypertension due to pregnancy, heart disease;
• pregnant women over the age of 35;
• if there is a history of cesarean section in the lower segment of the uterus;
• if fetal death or amniotic fluid containing meconium has been ascertained (amniotic fluid embolism may occur).

The effect of demoxytocin is enhanced with the simultaneous use of prostaglandins (very careful observation is necessary), as well as with caudal anesthesia (the hypertensive effect of sympathomimetic vasopressor drugs may be enhanced) (see INTERACTIONS).

There is evidence that the use of an analogue of demoxytocin, oxytocin, to initiate labor, increases the risk of postpartum DVK, which is rarely observed. This risk is more pronounced in women over the age of 35, as well as in women with pregnancy complications or a pregnancy duration of 40 weeks. In such cases, oxytocin and its analogues should be used with caution, and the doctor should be careful about the manifestations of DVK.

Desaminoxytocin tablets contain sucrose and lactose monohydrate. This drug is not recommended for patients with rare congenital fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency, as well as for persons with rare congenital galactose intolerance or Lapp-lactase deficiency.

Use during pregnancy and lactation. During pregnancy, demoxytocin should be used with caution only for strict indications in connection with an increased risk of complications for the woman in labor and the fetus.

The penetration of demoxytocin in small amounts into breast milk is possible.Complications are unknown. The drug is destroyed in the digestive tract of the child.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Studies to assess the impact on the ability to drive vehicles or operate machinery have not been conducted. The drug is used in a hospital.

Interactions

Inhalation of drugs used for anesthesia (cyclopropane, halothane), possibly reduces the effect of demoxytocin (enhances the hypotensive effect and the risk of arrhythmia). with caudal anesthesia, demoxytocin can increase the severity of sympathomimetic vasoconstrictor pressor action.

Due to the fact that prostaglandins increase the uterotonic effect of demoxytocin, the latter is not used within 6 hours after vaginal administration of prostaglandins.

Demoxytocin is incompatible with other drugs with the effect of oxytocin.

β-adrenergic agonists reduce the effectiveness of demoxytocin.

Overdose

There are currently no data on overdose cases. when administered, demoxytocin is rapidly inactivated in the digestive tract.

Symptoms: with buccal administration in high doses, severe side effects are possible (see ADVERSE EFFECTS).

Treatment: discontinue use of the drug immediately. The treatment is symptomatic. There is no specific antidote.

Storage conditions

In the original packaging to protect from the effects of light and moisture at a temperature not exceeding 25 ° c.