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  • Acyl-amino-alcyl benzoic acid derivative  (1)
  • drug concentration  (1)
  • 1
    ISSN: 1432-0428
    Keywords: Acyl-amino-alcyl benzoic acid derivative ; hypoglycaemic agent ; insulin release ; pancreatic polypeptide ; glucagon ; somatostatin ; tolbutamide ; unanaesthetized dogs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The effects of HB 699, a non-sulphonyl urea acyl-amino-alcyl benzoic acid derivative, were studied in unanaesthetized dogs. Changes in blood glucose and plasma insulin, glucagon, pancreatic polypeptide and somatostatin were measured after a single intravenous injection. HB 699 caused hypoglycaemia and stimulated insulin secretion in a dosedependent manner. The effects of HB 699 (40 mg/ kg) on pancreatic hormone secretion were compared to those of tolbutamide given at a dose (12 mg/kg) which induced a similar maximal hypoglycaemia. Both drugs caused a similar increase in insulin release (180±32% for tolbutamide and 240±41% for HB 699) lasting for approximately 1 hour. Despite hypoglycaemia, plasma glucagon concentrations were unaltered by either substance. HB 699 caused a marked increase in the secretion of pancreatic polypeptide (220±60% at 30 min) for up to 2 hours, whereas tolbutamide caused no significant change in plasma pancreatic polypeptide levels. In contrast, while tolbutamide caused a significant (45±12%) but short-lived increase in plasma somatostatin concentrations, HB 699 had no significant effect.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: Carbamazepine ; Saliva ; Mania ; Carbamazepine epoxide ; drug concentration ; Concentration-response relationship ; therapeutic monitoring
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The study was designed to investigate the antimanic profile of carbamazepine as a first-line drug in affective or schizoaffective disorders, to correlate the clinical efficacy with the plasma level of carbamazepine and its 10,11-epoxide metabolite, and to test the potential value of monitoring the salivary level. It was administered alone for 3 weeks to 21 acute manic inpatients. During the first week, the dosage was rapidly increased to 800 mg/day in order to produce steady-state plasma levels of carbamazepine on Day 7. The individual dose was then adjusted to maintain the therapeutic range of 8–12 mg/l. Plasma and saliva levels of the drug and its metabolite, as well as clinical status were assessed weekly. Overall, there was 62% globally improved patients and 77% in affective disorders. The improvement of manic symptoms was significantly lower in schizoaffective than in affective disorders, whereas the dropout rate and the need for antipsychotic medication was higher in the former group. The antimanic response was significantly correlated with the plasma levels both of carbamazepine and its epoxide metabolite, with a time-lag consistent with a delayed drug effect. Drug and metabolite concentrations in saliva were close to their plasma free fraction and were strongly correlated with their plasma levels, suggesting the potential value of salivary drug monitoring.
    Type of Medium: Electronic Resource
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