title: Plasma concentration and acute clinical effects of docarpamine, orally active dopamine prodrug, in infants.
abstract: Currently, there are no data available on the optimal doses and efficacy of docarpamine in infants. In the present study, three doses of docarpamine, 15.0-20.4 (19.0 +/- 1.9; mean +/- SD) mg/kg per dose every 8 h to 10 infants suffering heart failure. Age and bodyweight were from 1 to 4 (1.4 +/- 1) months and 2960-5160 (3350 +/- 872) g, respectively. In all infants, plasma concentrations of free dopamine were measured 1, 2 and 3 h after the first administration. Heart rate and systolic blood pressure were examined before and at the same time as the first administration. In seven infants, the 24 h urinary output and urinary excretion of electrolytes and creatinine before and during docarpamine were measured. Peak plasma concentration of free dopamine (ng/mL) was achieved after 1 or 2 h of administration, 0-163.1 (37.9 +/- 47.2) and 0-105.0 (37.8 +/- 39.3), respectively. The concentration had decreased rapidly by 3 h to 0-34.2 (12.4 +/- 11.0). Both heart rate (b.p.m.) and blood pressure (mmHg) tended to increase from 120-154 (140 +/- 15) and 56-90 (76 +/- 11) to a peak of 124-162 (148 +/- 14) and 70-92 (79 +/- 8), respectively (P = 0.197, P = 0.289). There were no significant changes in urinary output or excreta. Oral docarpamine of 15-20 mg/kg per dose can achieve plasma free concentrations of dopamine that increase heart rate and systolic blood pressure.
authors.affiliation: Department of Pediatrics, School of Medicine, Sapporo Medical University, Hokkaido, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Tomita
authors.forename: S
authors.initials: S
authors.lastname: Fuse
authors.forename: S
authors.initials: S
authors.lastname: Chiba
mesh_terms: D000284:Administration, Oral; D000367:Age Factors; D004298:Dopamine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D018491:Dopamine Agonists / Q000008:administration & dosage* / Q000378:metabolism / Q000494:pharmacology; D016903:Drug Monitoring; D006333:Heart Failure / Q000188:drug therapy* / Q000378:metabolism; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D007223:Infant; D007231:Infant, Newborn; D011355:Prodrugs / Q000008:administration & dosage* / Q000378:metabolism / Q000494:pharmacology; D013997:Time Factors
chemical_list: D018491:Dopamine Agonists; D011355:Prodrugs; C052143:docarpamine; D004298:Dopamine