Instructions Desaminooxytocin tablets 50 IU blister No. 10
Composition
active ingredient: demoxytocin;
1 tablet contains 50 IU of demoxytocin;
excipients: sucrose; lactose monohydrate; methylcellulose; calcium stearate; potato starch.
Dosage form
Pills.
Main physicochemical properties: round, flat-cylindrical tablets of white color with a bevel and a score.
Pharmacotherapeutic group
Pituitary and hypothalamic hormones and analogues. Posterior pituitary hormones. Oxytocin and its derivatives. ATC code H01B B01.
Pharmacological properties
Pharmacodynamics
In terms of chemical structure, demoxytocin is close to oxytocin, a 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, thus increasing its contraction. The drug stimulates the contraction of the smooth muscles of the uterus, and also, by stimulating the contraction of myoepithelial cells of the mammary gland, enhances milk secretion.
When applied transbuccally, demoxytocin, unlike oxytocin, is not broken down by salivary enzymes and easily penetrates through the oral mucosa into the systemic circulation. Uterine contractions begin 20–40 minutes (maximum 50–60 minutes) after transbuccal application of demoxytocin. The effect depends on the dose and lasts up to 180 minutes. The uterotonic activity of demoxytocin is 2 times higher than that of oxytocin. In the postpartum period, demoxytocin accelerates uterine involution and shortens the time of postpartum hemorrhage.
The lactogenic effect of demoxytocin begins earlier, is more pronounced and lasts longer than that of oxytocin, which is explained by its resistance to enzymatic inactivation. Demoxytocin stimulates the formation and secretion of milk, normalizes the lactation process, preventing breast engorgement and the formation of mastitis.
Demoxytocin does not have pronounced vasopressor and antidiuretic activity, so it can be used in women with arterial hypertension, late toxicosis of pregnancy, and impaired renal function.
Pharmacokinetics
Deoxytocin is rapidly and completely absorbed through the oral mucosa and enters the bloodstream. When administered transbuccally, 1 tablet of 50 IU deoxytocin is absorbed within 15–30 minutes. Enzymes in saliva do not destroy the drug, as it is resistant to oxytocinases; elimination of deoxytocin occurs within 30–60 minutes.
Indication
To stimulate and enhance labor activity in case of primary and secondary weakness.
To stimulate lactation in the postpartum period.
Contraindication
Hypersensitivity to demoxytocin and/or to any of the excipients of the medicinal product. Hypertonic uterine contractions, mechanical damage to the reproductive tract, fetal hypoxia, intrauterine fetal death.
Disproportion between the size of the pelvis and the fetus, transverse or oblique position of the fetus, placenta previa or umbilical vessels, premature detachment of the placenta, umbilical cord prolapse, threatened uterine rupture due to multiple pregnancies, uterine distension (multiple pregnancy, polyhydramnios), invasive cervical carcinoma, polyhydramnios, multiple pregnancies, and the presence of scars on the uterine wall after surgeries, including cesarean section.
The drug should not be used for a long time in severe preeclampsia and severe heart and vascular diseases, as well as in the case of an inert uterus (resistance to deoxytocin/oxytocin).
Interaction with other medicinal products and other types of interactions
Inhalation of drugs used for anesthesia (cyclopropane, halothane) may reduce the effect of demoxytocin (increases the hypotensive effect and the risk of arrhythmia). In caudal anesthesia, demoxytocin may increase the sympathomimetic vasoconstrictor pressor effect.
Due to the fact that prostaglandins increase the uterotonic effect of demoxytocin, the latter should not be used within 6 hours after vaginal application of prostaglandins.
Demoxytocin is incompatible with other drugs that have an oxytocin effect.
Beta-adrenergic agonists reduce the effectiveness of demoxytocin.
Application features
Demoxytocin can be used only for medical indications, under the supervision of medical personnel in a maternity hospital. During drug stimulation of labor, careful supervision of the woman in labor is necessary (monitoring the intensity of uterine contractions, cervical dilation, fetal movement through the birth canal, fetal heart rate and position, individual patient response to demoxytocin, dose adjustment if necessary). In case of excessively strong labor activity, the drug should be discontinued.
if there is a risk of fetal and pelvic size discrepancy (demoxytocin should not be used if the risk is significant); if there is secondary uterine inertia; in case of pregnancy-induced hypertension, heart disease; in case of use of the drug by pregnant women over 35 years of age; if the patient has a history of cesarean section in the lower uterine segment; if intrauterine fetal death has been confirmed or the amniotic fluid contains meconium (amniotic fluid embolism may occur).
The effect of demoxytocin is enhanced by the simultaneous use of prostaglandins (very careful supervision is required), as well as during caudal anesthesia (the hypertensive effect of sympathomimetic vasopressor drugs may be enhanced) (see section "Interaction with other medicinal products and other types of interactions").
There is evidence that the use of the deoxytocin analogue, oxytocin, to induce labour increases the risk of a rare postpartum disseminated intravascular coagulation (DIC). This risk is more pronounced in women aged 35 years and older, as well as in women with pregnancy complications or gestational age greater than 40 weeks. In such cases, oxytocin and its analogues should be used with caution, and the physician should be alert for signs of DIC.
Desaminooxytocin tablets contain sucrose and lactose, monohydrate. This medicinal product is not recommended for patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency, as well as patients with rare hereditary problems of galactose intolerance or the Lapp lactase deficiency.
Ability to influence reaction speed when driving vehicles or other mechanisms
No studies have been conducted to assess the effect on the ability to drive or use machines. The drug should be used in a hospital setting.
Use during pregnancy or breastfeeding
During pregnancy, demoxytocin should be used with caution only under strict indications due to the increased risk of complications for the mother and fetus.
Small amounts of demoxytocin may pass into breast milk. Complications are unknown. The drug is destroyed in the baby's gastrointestinal tract.
Method of administration and doses
The tablet should be applied transbuccally, placing it behind the cheek alternately on the right and left and holding it in the mouth until completely dissolved and absorbed. To excite and stimulate labor, 50 IU (1 tablet) is usually used every 30 minutes; the required amount of the drug should be determined individually. If regular strong contractions occur, the following single doses should be halved (use ½ tablet) or the interval between doses should be increased (up to 1 hour). The maximum dose is usually 500 IU (10 tablets), rarely 900 IU or more. In the absence of effect, the drug can be taken again after 24 hours, if this is permissible.
To stimulate lactation, demoxytocin should be administered from the 2nd to the 6th postpartum day at a dose of 25–50 IU (½–1 tablet) 5 minutes before feeding the child 2–4 times a day.
Children
Do not prescribe to children.
Overdose
There are no data on overdose cases yet. When taken orally, demoxytocin is rapidly inactivated in the digestive tract.
Symptoms: severe side effects are possible with transbuccal administration of large doses (see section "Adverse reactions").
Treatment: the drug should be discontinued immediately. Treatment is symptomatic. There is no specific antidote.
Adverse reactions
Deoxytocin in therapeutic doses does not cause clinically significant side effects. Large doses of deoxytocin and increased sensitivity of the uterus may cause the following side effects:
in the mother: uterine spasms (also when using low doses), uterine hypertonicity, tetanic contractions, uterine hyperactivity with ruptures of the uterus and vaginal tissues; nausea, vomiting, hypersalivation, increased blood pressure, tachycardia, arrhythmia; possible fatal outcome.
In case of complications of pregnancy and childbirth, life-threatening afibrinogenemia, postpartum hemorrhage, anaphylactic shock may occur. There is a risk of disseminated intravascular coagulation;
in the fetus: bradycardia, arrhythmia, asphyxia, acute fetal hypoxia, meconium staining of the amniotic fluid; possible fatal outcome; in newborns: jaundice, retinal hemorrhage.
The following adverse reactions are listed below, ranked by MedDRA system organ class and frequency: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency unknown (cannot be estimated from the available data).
On the part of the immune system
Rare: hypersensitivity reactions, including anaphylactic reactions (with difficulty breathing, hypotension or shock).
From the nervous system
Common: headache.
From the heart
Common: tachycardia, bradycardia.
Uncommon: arrhythmias.
Gastrointestinal tract
Common: nausea, vomiting.
Skin and subcutaneous tissue disorders
Rare: rash.
Expiration date
5 years.
Do not use after the expiration date.
Storage conditions
Keep out of reach of children.
Packaging
10 tablets in a blister, 1 blister in a cardboard pack.
Vacation category
According to the recipe.
Producer
JSC "Grindex".
Location of the manufacturer and its business address
Krustpils Street, 53, Riga, LV-1057, Latvia.
