Abstract | OBJECTIVE: To test the effect of SR 49059, an orally active, nonpeptide, selective and specific antagonist of the vasopressin V1a receptors in humans. DESIGN: A placebo-controlled, double-blind, cross-over trial. SETTING: The Department of Obstetrics and Gynaecology, Lund University Hospital, Sweden. PARTICIPANTS: Twelve healthy women, who had previously been sterilised by tubal ligation. INTERVENTIONS: MAIN OUTCOME MEASURE: The area between the recording curve and zero level of pressure. Vital signs, safety parameters and drug plasma concentrations were also measured. RESULTS: The spontaneous uterine activity as well as the response to lysine vasopressin injections before administration of the test drugs were almost identical at the two experiments. Following intake of SR 49059 the area under the recording curve (0-10 min) after the second, third, and fourth injection of lysine vasopressin were reduced by 57, 42, and 66%, respectively, compared with placebo. Trough plasma concentrations of lysine vasopressin were markedly higher and systolic blood pressure slightly lower after antagonist administration than after placebo, whereas no significant difference between treatments was observed in diastolic pressure, heart rate or plasma osmolality. CONCLUSIONS:
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Authors | T Bossmar, R Brouard, A Döberl, M Akerlund |
Journal | British journal of obstetrics and gynaecology
(Br J Obstet Gynaecol)
Vol. 104
Issue 4
Pg. 471-7
(Apr 1997)
ISSN: 0306-5456 [Print] England |
PMID | 9141585
(Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antidiuretic Hormone Receptor Antagonists
- Indoles
- Pyrrolidines
- Receptors, Vasopressin
- Lypressin
- relcovaptan
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Topics |
- Administration, Oral
- Adult
- Antidiuretic Hormone Receptor Antagonists
- Blood Pressure
(drug effects)
- Cross-Over Studies
- Double-Blind Method
- Female
- Heart Rate
(drug effects)
- Humans
- Indoles
(pharmacology)
- Lypressin
(blood)
- Pyrrolidines
(pharmacology)
- Receptors, Vasopressin
(metabolism, physiology)
- Time Factors
- Uterine Contraction
(drug effects)
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