Taiy Chemical
Atosiban Acetate
Synonym Tractocile
Species Human
Protein Accession P96525
Purity Greater than 98%
Endotoxin Level Less than 1 EU/µg
Biological Activity Potent oxytocin receptor antagonist
Expression System E. coli
Fusion Tag None
Predicted Molecular Mass 9943 Da
Formulation Lyophilized from a 0.2 µm filtered solution of 20mM PB,150mM NaCl, pH 7.2
Reconstitution Centrifuge vial before opening. Reconstitute in sterile PBS, pH 7.4 to a concentration of 50 µg/ml
Storage & Stability Store at -20°C. Aliquot and store at -80°C for long term storage. Avoid repeated freeze-thaw cycles.
FAQ
What is Atosiban Acetate, and how does it function in medical practice?

Atosiban Acetate is a medication used primarily in obstetrics to delay premature birth. It serves as a tocolytic agent, which means it is specifically designed to suppress preterm labor. Atosiban works by antagonizing the hormones oxytocin and vasopressin. Oxytocin is a natural hormone in the body that plays a critical role in inducing uterine contractions. By blocking oxytocin, Atosiban effectively reduces the contractions of the uterus and helps in managing preterm labor by delaying delivery to allow additional time for fetal development. It's particularly valuable in cases where early labor poses significant risks to the mother or the fetus, as postponing birth can give the newborn a better chance for healthy outcomes through further growth and maturity in the womb. Additionally, Atosiban is known for having a favorable side effect profile compared to other tocolytics like beta-sympathomimetic agents. Such agents can often cause cardiovascular side effects including tachycardia and hypertension, whereas Atosiban tends to be more well-tolerated. The drug is administered intravenously, typically beginning with a bolus dose followed by a continuous infusion over a period that can last up to 48 hours. A significant benefit of Atosiban is its ability to rapidly decrease uterine contraction frequency, often within minutes of the initial dose, which is crucial for emergency obstetric management. It also poses fewer risks of adverse effects that may compromise either the maternal or fetal well-being, thus providing a safer management plan during critical periods of pregnancy. Its use, however, is usually restricted to settings where premature labor is diagnosed and monitored by healthcare professionals, ensuring that both the mother and fetus receive comprehensive care during the treatment process.

What are the scientific studies backing the effectiveness of Atosiban Acetate?

Several clinical studies have been conducted to evaluate the efficacy and safety of Atosiban Acetate. One of the most notable is the "Worldwide Atosiban Versus Beta-mimetics Study Group" trial, which was a large-scale, randomized, double-blind study comparing Atosiban to beta-mimetics, a different category of tocolytics. This trial demonstrated that Atosiban was as effective as these drugs in postponing preterm labor, but with significantly fewer side effects. The trial focused on women experiencing preterm labor between 24 and 33 weeks' gestational age and showed that Atosiban successfully delayed delivery for at least 48 hours or longer, which was considerable enough to administer steroids to enhance fetal lung maturity. Another meta-analysis reviewed data from multiple randomized controlled trials and emphasized that Atosiban is not only effective but offers an improved safety profile compared to other tocolytics. Women treated with Atosiban reported fewer cardiac and pulmonary adverse effects than those treated with alternatives like ritodrine, a common beta-mimetic. Beyond its primary function of delaying delivery, some research has pointed to potential benefits of Atosiban in reducing neonatal morbidity associated with prematurity, such as respiratory distress syndrome and neonatal intensive care unit admissions. Investigations have also looked into the pharmacokinetics and pharmacodynamics of Atosiban, determining its efficacy is partly due to its highly specific action as an oxytocin receptor antagonist with negligible off-target effects, ensuring reduced adverse outcomes. These findings collectively underpin the use of Atosiban in clinical practice as a reliable and safe intervention in managing preterm labor, contributing significantly to its adoption across numerous medical centers around the world.

Are there any known contraindications or precautions associated with Atosiban Acetate use?

Atosiban Acetate, like any medication, comes with certain contraindications and precautions that healthcare providers must consider to ensure patient safety. Primarily, Atosiban is contraindicated in cases where prolonging pregnancy is either not beneficial or poses risks greater than preterm birth itself. Such situations include, but aren't limited to, hemorrhage, eclampsia and severe preeclampsia, chorioretinitis, or any chronic hepatopathy or renal impairment. Another critical contraindication is hypersensitivity to Atosiban or any of its excipients, as allergic reactions could complicate a patient's condition. Additionally, Atosiban is not recommended for use in pregnant women less than 24 weeks or beyond 33 weeks gestation due to limited research in these groups, and its benefits do not outweigh potential risks outside this timeframe. When administering Atosiban, healthcare providers must assess the risk of infection, particularly if there is suspected or confirmed intrauterine infection since prolonging labor in infected settings could lead to adverse maternal outcomes. Another important precaution is the potential for decreased fetal heart rate due to decreased uterine perfusion. Therefore, continuous fetal monitoring is essential during administration to immediately address any complications. Physicians should also be wary of cases with potential for uterine rupture, especially in women with previous cesarean sections or uterine surgeries. It is critical that Atosiban administration is done in a hospital setting equipped to handle obstetric emergencies. Moreover, its use should be accompanied by compliance with existing protocols to assess fetal status appropriately, such as ultrasonography, to determine amniotic fluid levels and placental blood flow. Thus, while Atosiban Acetate is indeed beneficial for delaying preterm birth, its administration requires an array of considerations and meticulous evaluation to ensure a safe outcome for both mother and child. The detailed analysis of individual patient conditions and coordinated care in specialized settings is crucial in optimizing treatment efficacy while minimizing potential risks.

How does Atosiban Acetate compare to alternative treatments for preterm labor?

Atosiban Acetate holds a unique position among treatments for preterm labor due to its specific action as an oxytocin receptor antagonist, leading to a distinctive safety and efficacy profile. Comparing Atosiban with beta-sympathomimetic agents, which are globally recognized for managing preterm labor, underscores several critical differences. Beta-mimetics like terbutaline and ritodrine have been commonly used but are associated with an array of cardiovascular side effects including maternal tachycardia, hypotension, and pulmonary edema under certain conditions. In contrast, Atosiban's mode of action typically circumvents these cardiovascular issues, offering a more tolerable experience for most users. Additionally, calcium channel blockers like nifedipine also serve as tocolytic agents, and while they have proven effective, they too carry risks like hypotension and occasional elevations of hepatic enzymes, which require careful monitoring. These profiles underscore why Atosiban is often favored due to its targeted approach and minimal systemic side effects. Moreover, magnesium sulfate has been used as a tocolytic but predominantly in the United States partially due to its neuroprotective benefits for the neonatal brain. However, it entails strict monitoring due to potential toxicity, especially concerning respiratory and renal functions, hence the treatment burden is potentially higher compared to Atosiban. Furthermore, the onset of action of Atosiban Acetate is particularly rapid, with studies indicating decreased uterine contractions almost immediately following administration. This aspect makes Atosiban appealing in acute scenarios where time is critical. Despite these benefits, cost considerations and availability also influence the choice of treatment. Not all healthcare systems might have ready access to Atosiban or the infrastructure to administer it. Yet, in settings where it is feasible, Atosiban often ranks as a preferred choice due to its efficacy in stabilizing uterine activity with fewer adverse maternal effects, enhancing both maternal and fetal safety during the sensitive period of preterm labor.

What is the typical administration protocol for Atosiban Acetate in a clinical setting?

The administration of Atosiban Acetate follows a structured protocol designed to optimize its tocolytic effects while ensuring patient safety. It is typically administered intravenously, beginning with an initial bolus dose followed by a continuous infusion. The treatment protocol is split into three phases. Initially, a bolus dose of 6.75 mg is administered intravenously over one minute. This rapid administration is crucial as it quickly introduces the drug into the system to target and block the oxytocin receptors, effectively quelling uterine contractions right at the onset of treatment. Following the bolus, the second phase involves a high-dose continuous infusion over three hours. During this period, Atosiban is infused at a rate of 18 mg/hour, allowing sustained delivery of the medication to maintain uterine relaxation. The final phase of administration consists of a subsequent infusion of 6 mg/hour, which can last for a maximum of 45 hours, subject to clinical judgment based on contraction patterns and maternal-fetal well-being. The total duration of treatment must not exceed 48 hours, which is deemed sufficient to allow other treatments, such as antenatal glucocorticoids for fetal lung maturation, to take effect or arrange for safe delivery if required. Throughout this process, patients are closely monitored for any signs of adverse reactions, changes in labor patterns, and fetal responses to garner a comprehensive understanding of the therapeutic progress. These measures extend to periodic assessments of uterine contractions and fetal heart rate to promptly assess any need for adjustments to the treatment plan. The discrete phases of Atosiban administration outline its capacity to provide not just immediate relief from preterm labor symptoms, but also to maintain optimal conditions for maternal and fetal health across a twenty-four to forty-eight-hour management window. It underscores the drug's adaptability within critical obstetric care, optimizing outcomes during the fraught period of impending preterm birth.

What are the potential side effects of using Atosiban Acetate?

While Atosiban Acetate is generally well-tolerated, it is not without possible side effects that must be monitored during its administration. The side effects are typically mild to moderate in intensity and do not necessitate discontinuation of therapy in most cases. The most common adverse effects reported include injection site reactions, which might manifest as mild erythema or swelling in the localized area where the intravenous infusion is applied. Some women may also experience nausea, a fairly general side effect that does not impede the drug's therapeutic action but may require supportive care such as dietary modifications or antiemetic treatments if persistent. Dizziness and headaches have also been observed, generally occurring as transient responses that dissipate as the patient acclimatizes to the medication. Rarely, more significant side effects like tachycardia may occur, necessitating close monitoring of maternal heart rate when therapy is ongoing. Interestingly, since Atosiban specifically targets oxytocin receptors, it does not typically interfere with other physiological functions, reducing the incidence of multisystemic side effects, a frequent concern with other tocolytic drugs like beta-mimetics. It's also noteworthy that the majority of adverse effects tend to resolve upon cessation of treatment, which is encouraging in maintaining therapy adherence. Importantly, continuous fetal monitoring is prioritized during Atosiban administration, as any potential side effects perceived from uterine contractions ceasing suddenly can be challenging to differentiate from genuine fetal distress without comprehensive assessments. Overall, Atosiban maintains a favorable side effect profile. However, maintaining diligent observation and established protocols are paramount in timely identification and management of any complications, ensuring that the benefits of its use in controlling preterm labor outweigh the risks with sustained maternal-fetal health as the primary focus throughout treatment.
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