Atosiban

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Atosiban
Systematic (IUPAC) name
1-(3-mercaptopropanoic acid)-
2-(O-ethyl-D-tyrosine)-4-L-threonine-
8-L-ornithine-oxytocin
Identifiers
CAS number 90779-69-4
ATC code G02CX01
PubChem 68613
Chemical data
Formula C43H67N11O12S2 
Mol. mass 994.199
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes intravenous

Atosiban (Tractocile or Antocin, RWJ 22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication to halt premature labor. Although initial studies suggested it could be used as a nasal spray and hence would not require hospital admission, it is not used in that form. It was developed by Ferring Pharmaceuticals in Sweden and first reported in the literature in 1985.[1]

Chemically, it is a modified form of oxytocin that inhibits the action of this hormone on the uterus, leading to a cessation of contractions. It is therefore a tocolytic.

A 2005 systematic review by the Cochrane Collaboration showed that while atosiban had less side-effects than alternative drugs (such as ritodrine), it was no better than placebo in the major outcomes, and in one study showed worse neonatal outcomes. The reviewers suggest nifedipine may be more promising.[2]

[edit] References

  1. ^ Akerlund M, Carlsson AM, Melin P, Trojnar J (1985). "The effect on the human uterus of two newly developed competitive inhibitors of oxytocin and vasopressin". Acta Obstet Gynecol Scand. 64 (6): 499–504. PMID 4061066. 
  2. ^ Papatsonis D, Flenady V, Cole S, Liley H (2005). "Oxytocin receptor antagonists for inhibiting preterm labour". Cochrane database of systematic reviews (Online) (3): CD004452. doi:10.1002/14651858.CD004452.pub2. PMID 16034931.