title: The effect of relcovaptan (SR 49059), an orally active vasopressin V1a receptor antagonist, on uterine contractions in preterm labor.
abstract: Relcovaptan (SR 49059) is a non-peptide, orally active vasopressin V1a receptor inhibitor. The effect on uterine contractions in 18 women with preterm labor in pregnancy weeks 32-36 was assessed in a double-blind investigation. The inclusion criterion was at least four regular uterine contractions over 30 min as measured by external tocodynamometry. Twelve patients received at random a single oral dose of 400 mg relcovaptan and six received placebo, and contractions were monitored up to 6 h thereafter. Rescue medication (beta-adrenoceptor-stimulating drug) was allowed after 2 h. Before drug administration a mean (+/- SE) of 8.2 +/- 1.4 and 9.7 +/- 1.6 contractions/30 min were recorded in the relcovaptan- and placebo-treated groups, respectively. In the former group, the frequency of uterine contractions started to decrease within the first half hour, and 1.5-2 h after dosing it was steady at 3.2 +/- 0.9 contractions/30 min. Correspondingly, after placebo, 7.8 +/- 2.2 contractions/30 min were recorded, a statistically significant difference (p = 0.017). The activity in the relcovaptan-treated women remained low, whereas in the placebo group inhibited uterine contractions were observed only in women receiving 'rescue' tocolytic treatment. It is concluded that relcovaptan inhibits preterm labor.
authors.affiliation: Department of Obstetrics and Gynecology, University Hospital, Lund, Sweden.
authors.forename: Margareta
authors.initials: M
authors.lastname: Steinwall
authors.forename: Thomas
authors.initials: T
authors.lastname: Bossmar
authors.forename: Rémi
authors.initials: R
authors.lastname: Brouard
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Laudanski
authors.forename: Per
authors.initials: P
authors.lastname: Olofsson
authors.forename: Remigiusz
authors.initials: R
authors.lastname: Urban
authors.forename: Kerstin
authors.initials: K
authors.lastname: Wolff
authors.forename: Gérard
authors.initials: G
authors.lastname: Le-Fur
authors.forename: Mats
authors.initials: M
authors.lastname: Akerlund
mesh_terms: D000284:Administration, Oral; D000328:Adult; D065092:Antidiuretic Hormone Receptor Antagonists; D015148:Cardiotocography; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D007211:Indoles / Q000008:administration & dosage*; D007752:Obstetric Labor, Premature / Q000188:drug therapy*; D011247:Pregnancy; D011263:Pregnancy Trimester, Third; D011759:Pyrrolidines / Q000008:administration & dosage*; D015149:Tocolytic Agents / Q000008:administration & dosage*; D016896:Treatment Outcome; D014590:Uterine Contraction / Q000187:drug effects
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D007211:Indoles; D011759:Pyrrolidines; D015149:Tocolytic Agents; C082134:relcovaptan