Atosiban PSK (Solution, Concentrate) Instructions for Use
ATC Code
G02CX01 (Atosiban)
Active Substance
Atosiban (Rec.INN registered by WHO)
Clinical-Pharmacological Group
Oxytocin antagonist. A drug that reduces the tone and contractile activity of the myometrium
Pharmacotherapeutic Group
Other agents used in gynecology
Pharmacological Action
A labor suppressant, an oxytocin receptor blocker. Atosiban is a synthetic peptide that is a competitive antagonist of human oxytocin at the receptor level. By binding to oxytocin receptors, Atosiban reduces the frequency of uterine contractions and myometrial tone, leading to suppression of uterine contractility. Atosiban also binds to vasopressin receptors, inhibiting the effect of vasopressin, but does not affect the cardiovascular system.
In the case of preterm labor in a woman, Atosiban in recommended doses suppresses uterine contractions and provides functional rest for the uterus. Uterine relaxation begins immediately after the administration of atosiban; within 10 minutes, the contractile activity of the myometrium is significantly reduced, maintaining stable functional rest of the uterus (≤ 4 contractions per hour) for 12 hours.
Pharmacokinetics
Pharmacokinetic parameters (Vd, clearance and T1/2) are dose-independent. After IV infusion (300 mcg/min for 6-12 hours), the Cmax of atosiban in plasma is reached within 1 hour after the start of the infusion (on average 442 ± 73 ng/ml, in the range from 298 to 533 ng/ml). Plasma protein binding is 46-48%. Atosiban crosses the placental barrier. After administration of atosiban at a rate of 300 mcg/min, the ratio of atosiban concentration in the fetus to atosiban concentration in the mother is 0.12. The mean Vd is 18.3 ± 6.8 L.
Two metabolites have been identified in plasma and urine. The ratio of the concentration of the main metabolite M1 to the concentration of atosiban in plasma was 1.4 and 2.8 at the second hour of infusion and after its cessation, respectively. Metabolite M1 has pharmacological activity equivalent to atosiban and is excreted in breast milk.
Inhibition of cytochrome P450 isoenzymes by atosiban is unlikely.
After the infusion is stopped, the plasma concentration of the drug decreases rapidly with T1/2α-phase and T1/2β-phase values of 0.21 ± 0.01 and 1.7 ± 0.3 hours, respectively. The mean clearance value is 41.8 ± 8.2 L/h.
Atosiban is detected in urine in very small amounts; its concentration in urine is 50 times lower than the concentration of M1. The amount of atosiban excreted in feces was not determined.
Indications
For the threat of preterm labor in pregnant women: regular uterine contractions lasting at least 30 seconds and with a frequency of 4 or more times within 30 minutes; cervical dilation from 1 to 3 cm (0-3 cm for nulliparous women) and cervical effacement of more than 50%; gestational age from 24 to 33 full weeks; normal fetal heart rate.
ICD codes
| ICD-10 code | Indication |
| O60 | Preterm labor and delivery |
| ICD-11 code | Indication |
| JB00.Z | Preterm labor or delivery, unspecified |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Solution, Concentrate
It is administered intravenously immediately after the diagnosis of “preterm labor” is made in three stages: 1) first, an initial dose of 6.75 mg is administered over 1 minute; 2) immediately after this, an infusion is carried out at a dose of 300 mcg/min (administration rate 24 ml/h, atosiban dose 18 mg/h) for 3 hours; 3) after this, a prolonged (up to 45 hours) infusion of atosiban is carried out at a dose of 100 mcg/min (administration rate 8 ml/h, atosiban dose 6 mg/h).
The total duration of treatment should not exceed 48 hours. The maximum dose of atosiban for the entire course is 330 mg.
If it is necessary to re-administer atosiban, one should also start with stage 1, followed by infusion administration (stages 2 and 3). Re-administration can be started at any time after the first administration of the drug and can be repeated up to 3 cycles. If uterine contractile activity persists after 3 cycles of atosiban therapy, the use of another drug should be considered.
Adverse Reactions
From the digestive system: very common (>1/10) – nausea, less often – vomiting.
From metabolism common (>1/100, <1/10) – hyperglycemia.
From the nervous system common (>1/100, <1/10) – headache, dizziness; rare (>1/1000, <1/100) – insomnia.
From the cardiovascular system common (>1/100, <1/10) – tachycardia, arterial hypotension, hot flashes.
From the skin rare (>1/1000, <1/100) – itching, skin rash.
From the reproductive system very rare (>1/10,000, <1/1000) – uterine bleeding, uterine atony.
Other very rare (>1/10,000, <1/1000) – allergic reactions.
Contraindications
Gestational age less than 24 or more than 33 full weeks; premature rupture of membranes at a gestational age of more than 30 weeks; abnormal fetal heart rate; uterine bleeding requiring immediate delivery; eclampsia and severe preeclampsia requiring immediate delivery; intrauterine fetal death; suspected intrauterine infection; placenta previa; placental abruption; any conditions of the mother and fetus in which prolongation of pregnancy is dangerous; breastfeeding period; age under 18 years; hypersensitivity to atosiban.
Use in Pregnancy and Lactation
Atosiban should be used only in cases of diagnosed preterm labor from 24 to 33 full weeks of gestation.
Atosiban is contraindicated during lactation (breastfeeding).
Use in Hepatic Impairment
There is no experience with the use of atosiban in patients with impaired liver and kidney function.
Use in Renal Impairment
There is no experience with the use of atosiban in patients with impaired liver and kidney function.
Pediatric Use
The drug is contraindicated for use in children and adolescents under 18 years of age.
Geriatric Use
Not applicable.
Special Precautions
In case of suspected premature rupture of membranes, the benefit of using Atosiban to prolong labor should be weighed against the potential risk of developing chorioamnionitis.
Use Atosiban with caution in multiple pregnancies, as well as at 24-27 weeks of gestation (due to lack of sufficient clinical experience).
In case of persistent uterine contractions during the administration of Atosiban, uterine contractions should be monitored and fetal heart rate should be monitored. The possibility of using other drugs should also be considered.
There is no experience with the use of atosiban in patients with impaired liver and kidney function.
Atosiban is not used in cases of abnormal placental attachment.
In case of intrauterine fetal growth retardation, the decision to continue or re-administer atosiban depends on the assessment of fetal maturity.
As an oxytocin antagonist, Atosiban may theoretically promote uterine relaxation and provoke postpartum uterine bleeding, so the degree of blood loss after delivery should be constantly assessed.
Drug Interactions
Concomitant use of atosiban with ergot alkaloids is not advisable due to opposite pharmacological actions and indications for use.
Storage Conditions
Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.
Dispensing Status
Rx Only
Important Safety Information
This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Concentrate for solution for infusion 7.5 mg/1 ml: fl. 5 ml
Solution for intravenous administration 7.5 mg/1 ml: vial 0.9 ml
Marketing Authorization Holder
OHFK, JSC (Russia)
Manufactured By
Pharmidea, LLC (Latvia)
Packaging and Quality Control Release
Pharmidea, LLC (Latvia)
Or
OHFK, JSC (Russia)
Dosage Forms
 |
Atosiban | Concentrate for solution for infusion 7.5 mg/1 ml: fl. 5 ml |
| Solution for intravenous administration 7.5 mg/1 ml: vial 0.9 ml |
Dosage Form, Packaging, and Composition
Concentrate for solution for infusion clear, colorless.
| 1 ml | |
| Atosiban (as atosiban acetate) | 7.5 mg |
Excipients : mannitol – 50 mg, 1M hydrochloric acid solution – to pH 4.5, water for injections – to 1 ml.
5 ml – vials of colorless glass (1) – cardboard packs.
Solution for intravenous administration clear, colorless.
| 1 ml | |
| Atosiban (as atosiban acetate) | 7.5 mg |
Excipients : mannitol – 50 mg, 1M hydrochloric acid solution – to pH 4.5, water for injections – to 1 ml.
0.9 ml – vials of colorless glass (1) – cardboard packs.
Concentrate for solution for infusion 7.5 mg/1 ml: fl. 5 ml
Solution for intravenous administration 7.5 mg/1 ml: vial 0.9 ml
Marketing Authorization Holder
Promomed Rus LLC (Russia)
Manufactured By
Biokhimik, JSC (Russia)
Dosage Forms
|
Atosiban | Concentrate for solution for infusion 7.5 mg/1 ml: fl. 5 ml |
| Solution for intravenous administration 7.5 mg/1 ml: vial 0.9 ml |
Dosage Form, Packaging, and Composition
Concentrate for solution for infusion as a colorless, clear solution.
| 1 ml | |
| Atosiban (as acetate) | 7.5 mg |
Excipients : mannitol, hydrochloric acid (for pH adjustment), water for injections.
5 ml – glass vials with a capacity of 10 ml (1) – cardboard packs.
Solution for intravenous administration colorless, clear.
| 1 ml | |
| Atosiban (as acetate) | 7.5 mg |
Excipients : mannitol, hydrochloric acid (for pH adjustment), water for injections.
0.9 ml – glass vials with a capacity of 2 ml (1) – cardboard packs.
Concentrate for solution for infusion 7.5 mg/1 ml: vial 5 ml 1 pc.
Marketing Authorization Holder
PSK Pharma, LLC (Russia)
Dosage Form
|
Atosiban PSK | Concentrate for solution for infusion 7.5 mg/1 ml: vial 5 ml 1 pc. |
Dosage Form, Packaging, and Composition
Concentrate for solution for infusion as a clear, colorless solution.
| 1 ml | |
| Atosiban (as acetate) | 7.5 mg |
Excipients : mannitol, 1M hydrochloric acid solution (for pH adjustment), water for injections.
5 ml – vials of colorless glass with a capacity of 10 ml (1) – cardboard packs×.
× a first-opening control label may be applied.
Solution for intravenous administration 6.75 mg/0.9 mL: fl. 1 pcs.
Marketing Authorization Holder
PSK Pharma, LLC (Russia)
Dosage Form
|
Atosiban PSK | Solution for intravenous administration 6.75 mg/0.9 mL: fl. 1 pcs. |
Dosage Form, Packaging, and Composition
Solution for intravenous administration as a clear, colorless solution.
| 1 ml | 1 vial | |
| Atosiban (as acetate) | 7.5 mg | 6.75 mg |
Excipients : mannitol, 1M hydrochloric acid solution (for pH adjustment), water for injections.
0.9 ml – vials of colorless glass with a capacity of 4 ml (1) – cardboard packs×.
× a first-opening control label may be applied.
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