Atosiban

G02CX01

Solid fuel

Tocolytics

Oxytocin antagonist

In water ≤ 100 mg / mL at 20 ° C

Template: Infobox chemical / molecular formula search available

Atosiban (trade name Tractocile ®; Manufacturer Ferring ) is a drug from the group of tocolytics, which is used for the suppression of uterine contractions ( tocolysis ). It is therefore an alternative to fenoterol and nifedipine.

• 2.1 Mechanism of action ( pharmacodynamics )

Clinical information

Areas of application (indications )

The active ingredient atosiban is indicated to delay preterm birth in pregnant women if the following criteria are met:

• Regular uterine contractions with a minimum duration of 30 seconds and a frequency of ≥ 4 per 30 minutes.
• Opening of the cervix to a length of 1-3 cm (0-3 in first-time mothers ) and effacement of ≥ 50%.
• Age ≥ 18 years.
• Pregnancy in the 24th - 33rd completed weeks of gestation.
• Normal fetal heart rate.

Contraindications ( contraindications)

The drug should not be used in people who may be hypersensitive (allergic) to atosiban. In women before 24 or after 33 weeks of pregnancy or women with premature rupture of membranes, bleeding from the uterus, eclampsia ( a dangerous condition at the end of pregnancy, which is caused by toxins in the blood), preeclampsia ( disease that lead to eclampsia can ) or problems with the placenta atosiban should not be used as well.

Pharmacological properties

Mechanism of action ( pharmacodynamics )

Atosiban is a competitive antagonist at the oxytocin receptor. The potency of atosiban on human oxytocin receptor is lower than that of oxytocin, and it is not selective. After binding, the contraction frequency and the tone of the uterine musculature is reduced, resulting in a suppression of uterine contractions resulting. Atosiban binds with greater affinity to the human vasopressin V1a receptor, at which it inhibits the action of vasopressin. Atosiban is acting against the labor and ensures a uterine quiescence. In comparative studies with β -agonists, atosiban showed similar effect, whereby cardiovascular effects were not observed. With the recommended dosage immobilization for up to 12 hours can be achieved.

Chemical and pharmaceutical information

Atosiban is the International Nonproprietary Name (INN ) for 1 - (3- mercaptopropionyl ) -2 - ( d-4 - ethoxyphenylalanyl )-4- l -threonine -8 - l -ornithine - oxytocin, a synthetic structural analogue of the endogenous neuropeptide oxytocin, and is parenterally administered as atosiban acetate.