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Atosiban is a synthetic peptide oxytocin receptor antagonist, used to prevent premature birth. It works by competitively binding to oxytocin receptors on the uterine smooth muscle, thereby reducing the frequency and intensity of contractions. Its structure is similar to oxytocin, but has been modified to enhance receptor affinity and stability.
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Atosiban COA
Clinical application:
Premature birth treatment: Delaying delivery to allow more time for fetal maturation or for administering glucocorticoids to promote lung maturation.
Administration method: Intravenous injection (initial loading dose + continuous infusion), with rapid onset and a half-life of approximately 12 minutes.
Advantages:
High selectivity: Compared to traditional β₂ agonists (such as ritodrine), it has fewer cardiovascular side effects.
Safety: It has a good tolerance for both mothers and infants, and there are no significant long-term adverse reactions.
Limitations:
The cost is high and the medication response needs to be closely monitored. This represents an important advancement in the treatment of premature birth, and is particularly suitable for pregnant women who are intolerant to traditional medications.
The use of delaying premature birth
Premature delivery refers to those who give birth between 28 weeks and less than 37 weeks of pregnancy. The newborn born at this time is called a premature baby, weighing 1000-2499g. Premature birth is one of the important causes of perinatal death and disease. Premature babies are prone to various complications such as respiratory distress syndrome, intracranial hemorrhage, and infection due to immature organ systems, which seriously affect their quality of life and prognosis.Therefore, taking effective measures to delay premature birth and gain more intrauterine development time for the fetus has important clinical significance.Atosiban is an analogue of oxytocin, which can competitively bind to oxytocin and vasopressin V1A receptors, thereby blocking the pathways of action of oxytocin and vasopressin.
Oxytocin plays an important regulatory role during childbirth, as it can stimulate uterine smooth muscle contraction and promote delivery.Atoxiban inhibits the interaction between oxytocin and its receptors by binding to them, reducing the excitability of uterine smooth muscle and decreasing the frequency and intensity of uterine contractions, thus achieving the goal of delaying premature birth.Specifically, it can bind to the oxytocin receptor on the muscle membrane, preventing the increased production of inositol triphosphate stimulated by oxytocin, thereby preventing the release of stored calcium from the sarcoplasmic reticulum, and subsequently opening voltage-gated calcium channels.
Atosiban is still the only uterine specific uterine contraction inhibitor approved by the European EMA for premature birth.In relevant guidelines and expert consensus both domestically and internationally, this is also recommended for the treatment of pregnant women with signs of premature birth.Generally speaking, when pregnant women experience regular uterine contractions lasting at least 30 seconds each time, with 4 or more contractions within 30 minutes, cervical dilation of 1-3cm (in primiparous women, it reaches 0-3cm), cervical softening of over 50%, age of 18 years or older, and normal fetal heart rate.This can be considered to delay premature delivery,this is mainly used for pregnant women with regular uterine contractions between 24 and 33 weeks of gestation, normal fetal heart rate, and diagnosed as premature delivery.
Delaying premature birth during 24-27 weeks of pregnancy is of great significance in improving fetal survival and reducing the incidence of complications, as the fetus is not yet fully developed at this time. However, the efficacy of atosiban in this gestational week has not been fully determined, and doctors need to conduct a comprehensive evaluation based on the specific situation of the pregnant woman.At 28-33 weeks of pregnancy, the fetal organs develop relatively well, but there is still a certain risk of premature birth. The use of it can effectively inhibit uterine contractions, prolong gestational weeks, and buy time for further fetal development.
Usage in protecting the fetus
The goal of protecting the fetus is to maintain pregnancy and ensure normal fetal development in the uterus until full-term delivery. This creates a stable intrauterine environment for the fetus by inhibiting uterine contractions and reducing their adverse effects on the fetus. It can reduce the excitability of uterine smooth muscle, prevent the contraction of uterine muscles, thereby reducing the frequency and intensity of contractions, avoiding problems such as fetal hypoxia and distress caused by premature contractions, and improving the quality of life and prognosis of fetuses. At present, commonly used fetal protection drugs in clinical practice also include β 2-receptor agonists (such as Rituojun and Terbutaline), magnesium sulfate, and prostaglandin synthase inhibitors (such as indomethacin).
Compared to these drugs, this has unique advantages. Although β 2-receptor agonists can also inhibit uterine contractions, they can cause cardiovascular adverse reactions such as increased heart rate, elevated blood sugar, and decreased blood potassium, which can impose a certain burden on pregnant women's bodies. Magnesium sulfate requires close monitoring of blood magnesium concentration during use, as excessive use may lead to serious adverse reactions such as respiratory depression and decreased muscle tone. However, the side effects of it are relatively minor, with minimal impact on the cardiovascular system of pregnant women and higher safety.
In practical clinical applications, there are many successful cases of using this to preserve pregnancy. For example, a 28 year old pregnant woman experiences regular uterine contractions at 28 weeks of pregnancy, lasting about 40 seconds each time, with 4-5 contractions every 30 minutes, cervical dilation of 1.5cm, and cervical softening reaching 60%. The doctor diagnosed it as a sign of premature birth and immediately administered this treatment. The initial dose is 6.75mg, administered by injection of 7.5mg/ml solution.
Subsequently, a high dose of 7.5mg/ml concentration (300 μ g per minute) was administered for 3 hours; Then, a low dose of 7.5mg/ml concentrated solution (100 μ g per minute) was administered for up to 45 hours, with continuous treatment not exceeding 48 hours. After treatment, the uterine contractions of pregnant women were significantly reduced, and the frequency of contractions decreased from 4-5 times every 30 minutes before treatment to 1-2 times every 2-3 hours, and cervical dilation stopped. In the end, the pregnant woman successfully extended her gestational age to 37 weeks, gave birth smoothly, and the newborn's health condition was good.
Detailed steps and chemical equations for synthesizing
1. Synthesis of Fmoc Pro Orn Gly NH2 Tripeptide
(1) Fmoc Pro Orn (Boc) Gly NH2 was obtained by acylation of Fmoc Pro OH, Orn (Boc) OH, and Gly NH2, respectively.
Dissolve the product obtained in step 1 in an appropriate amount of DMF, add condensation agents EDC and HOBt, and mix Fmoc Pro Orn (Boc) Gly NH2 with the condensation agent evenly.(2) Under nitrogen protection, stir the mixture obtained in step 2 for a certain period of time to complete the condensation reaction.
(3) Detect the reaction solution and monitor the reaction process using thin-layer chromatography (TLC) or high-performance liquid chromatography (HPLC). When the reaction is approaching the endpoint, add an appropriate amount of hydrochloric acid to free the tripeptide.(4) Dialyze, concentrate, and dry the mixture obtained in step 4 to obtain the target tripeptide.
Chemical equation:
Fmoc Pro Orn (Boc)-Gly-NH2 + C2H4Cl2 + C6H5N3O → Fmoc Pro Orn (Boc)-Gly-NH2
Fmoc Pro Orn (Boc)-Gly-NH2 + HCl → Fmoc Pro Orn (Boc)-GlyNH2
2. Synthesis of Fmoc Pro Orn (Triphenylmethyl Resin) Gly NH2
(1) Dissolve the trimethyl resin in an appropriate amount of DMF and stir evenly.(2) Mix the resin solution obtained in step 1 with the Fmoc Pro Orn (Boc) Gly NH2 tripeptide solution obtained in step 5 evenly.
(3) Under nitrogen protection, stir the mixture obtained in step 2 for a certain period of time to fully couple the resin with the tripeptide.(4) Filter the reaction solution to remove unreacted resin and obtain the target resin.
Fmoc Pro Orn (Boc) - Gly-NH2 + Triphenylmethyl resin → Fmoc Pro Orn (Triphenylmethyl resin) -Gly-NH2
(1) Acylation of each amino acid or fragment in the product sequence yields a series of acylated amino acids or fragments.
(2) Dissolve the resin obtained in step 3 in an appropriate amount of DMF, add an appropriate amount of condensation agent, and then add acylated amino acids or fragments one by one. After each addition, stir for a certain time to fully couple the amino acids or fragments with the resin.
(3) By monitoring the reaction process through TLC or HPLC, when all amino acids or fragments have been coupled, the reaction solution is filtered to remove unreacted amino acids or fragments, and the target linear peptide resin is obtained.
Fmoc Pro Orn (triphenylmethyl resin)-Gly-NH2 + acylated amino acids or fragments → Atoxiban linear peptide resin
(1) Crack the linear peptide resin obtained in step 4, remove the triphenylmethyl protective group, and obtain the linear peptide.
(2) Dissolve the linear peptide obtained in step 1 in an appropriate amount of water, add an appropriate amount of oxidant (such as H2O2, NaOH, etc.), and conduct the oxidation reaction at a certain temperature.
(3) After a certain reaction time, the reaction solution is dialyzed, concentrated, and dried to obtain the target atoxicillin.
product linear peptide resin+cleaver → linear peptide+triphenylmethyl derivative
Linear peptide + oxidant → C43H67N11O12S2 + H2O
The discovery history of Atosiban can be traced back to the 1990s. At that time, scientists realized the role of oxytocin in premature birth and began searching for compounds that could antagonize oxytocin. After extensive screening and research, it was discovered. It was initially developed by Ferrer Grupo from Spain and later approved for market launch.It as an artificially synthesized peptide compound, has a chemical structure similar to oxytocin. Its mechanism of action is to competitively bind to oxytocin receptors on uterine smooth muscle and decidua, preventing oxytocin mediated release of inositol triphosphate, thereby inhibiting uterine contractions.
It has a high degree of uterine specificity and a strong and long-lasting effect on inhibiting uterine contractions, and its effect on cardiovascular smooth muscle is weak, without affecting the heart rate and blood pressure of the mother and fetus.
In clinical studies, atoxiban has been proven to be effective in preventing preterm birth and reducing the risk of preterm birth. Compared with other uterine contraction inhibitors, atoxiban has better efficacy and fewer adverse reactions. Therefore, atoxicillin is widely used in clinical practice and has become one of the important drugs for preventing premature birth.
The discovery of product has undergone extensive screening and research, and its pharmacological properties are unique. It has a high degree of uterine specificity and a strong and long-lasting effect on inhibiting uterine contractions. In clinical studies, atoxiban has been proven to be effective in preventing preterm birth, reducing the risk of preterm birth, and becoming one of the important drugs for preventing preterm birth.
Frequently Asked Questions
What are the benefits of this?
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Atosiban binds to oxytocin receptors, decreasing both the frequency and intensity of uterine contractions, thereby suppressing uterine contractile activity and inducing uterine quiescence. hours. Both oxytocin and vasopressin play roles in the induction and maintenance of uterine contractions during labour.
What are the side effects of this?
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Reported side effects for atosiban include nausea, vomiting, chest pain and dyspnoea. Importantly, atosiban is not contraindicated in cardiac disease or diabetes. There has been no direct comparison of atosiban and nifedipine in clinical trials.
What is the role of it in IVF?
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Since Atosiban is a combined oxytocin/vasopressin V1A antagonist, it works mainly by blocking oxytocin and vasopressin V1a receptors to decrease the frequency and amplitude of uterine contractions, which may enhance implantation and pregnancy rates.
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