Atosiban


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Premature labour
Adult: For the treatment of cases with regular uterine contractions (>30 seconds at a rate of ≥4 contractions per 30 minutes), cervical dilation of 1-3 cm (0-3 cm for nulliparas) and effacement of ≥50%, gestational age of 24-33 completed weeks, and normal fetal heart rate: Initially, 6.75 mg as a bolus inj of a solution containing 6.75 mg/0.9 mL of atosiban over 1 minute, immediately followed by a continuous infusion of a solution containing 0.75 mg/mL of atosiban at a rate of 0.3 mg/min over 3 hours, then reduce the rate to 0.1 mg/min over 45 hours. Max dose: 330.75 mg. Max treatment duration: 48 hours. If re-treatment is needed, the full 48-hour treatment regimen, including the initial bolus inj may be done (refer to specific product guidelines).
Hướng dẫn pha thuốc
Further dilute 10 mL (two 5 mL vials) of atosiban 37.5 mg/5 mL concentrate for solution for infusion with NaCl 0.9%, lactated Ringer's solution, or dextrose 5% in water to obtain a final concentration of 75 mg/100 mL.
Chống chỉ định
Gestational age <24 or >33 completed weeks, premature rupture of membranes >30 weeks of gestation, antepartum uterine haemorrhage requiring immediate delivery, eclampsia and severe pre-eclampsia requiring delivery, suspected intra-uterine infection, placenta praevia, abruptio placenta, abnormal fetal heart rate, intra-uterine fetal death.
Thận trọng
Patient with intra-uterine growth retardation, multiple pregnancies. Patient under the gestational age of 24-27 weeks. Consider the benefits and potential risks of delaying delivery in patients whom premature rupture of membranes cannot be excluded. Hepatic impairment. Lactation.
Tác dụng không mong muốn
Significant: Chorioamnionitis, postpartum haemorrhage. Rarely, severe noncardiogenic pulmonary oedema.
Cardiac disorders: Tachycardia.
Gastrointestinal disorders: Nausea, vomiting.
General disorders and administration site conditions: Inj site reaction, pyrexia.
Immune system disorders: Rarely, allergic reaction.
Metabolism and nutrition disorders: Hyperglycaemia.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Insomnia.
Reproductive system and breast disorders: Rarely, uterine atony.
Skin and subcutaneous tissue disorders: Pruritus, rash.
Vascular disorders: Hypotension, hot flushes.
Chỉ số theo dõi
Monitor uterine contractions, fetal heart rate, and blood loss after delivery.
Tương tác
Increased risk of pulmonary oedema with other drugs that have tocolytic activity (e.g. Ca channel blockers, β2-agonists).
Tác dụng
Description:
Mechanism of Action: Atosiban is an oxytocin peptide analogue. It competitively inhibits oxytocin receptors thereby causing a reduction in oxytocin-mediated release of inositol triphosphate (IP3) from myometrial cell membranes, which consequently causes decreased Ca release and extracellular Ca influx, ultimately causing a reduced frequency of uterine contractions.
Onset: Approx 10 minutes.
Pharmacokinetics:
Distribution: Crosses the placenta and enters breast milk. Volume of distribution: 18 ± 7 L. Plasma protein binding: 46-48%.
Metabolism: Partially metabolised.
Excretion: Via urine (small amount as unchanged drug). Terminal elimination half-life: 1.7 hours.
Đặc tính

Chemical Structure Image
Atosiban

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5311010, Atosiban. https://pubchem.ncbi.nlm.nih.gov/compound/Atosiban. Accessed Dec. 20, 2023.

Bảo quản
Store between 2-8°C. Protect from light.
Phân loại MIMS
Thuốc tác dụng lên tử cung
Phân loại ATC
G02CX01 - atosiban ; Belongs to the class of other gynecologicals. Used to inhibit uncomplicated premature labour between 24 and 33 weeks of gestation.
Tài liệu tham khảo
Anon. Atosiban. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 31/03/2023.

Atosiban Accord 37.5 mg/5 mL Concentrate for Solution for Infusion (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 31/03/2023.

Atosiban Accord 6.75 mg Solution for Injection in Pre-filled Syringe (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 31/03/2023.

Buckingham R (ed). Atosiban. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/03/2023.

Joint Formulary Committee. Atosiban. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/03/2023.

Tractocile 37.5 mg/5 mL Concentrate for Solution for Infusion (Ferring Pharmaceuticals Ltd). MHRA. https://products.mhra.gov.uk. Accessed 31/03/2023.

Tractocile 7.5 mg/mL Solution for Injection, 7.5 mg/mL Concentrate for Solution for Infusion (Ferring GmbH). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 31/03/2023.

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