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.