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  • 1
    ISSN: 1432-1041
    Keywords: Glipizide ; Insulin secretion ; Diabetes mellitus ; NIDDM ; sulphonylurea treatment ; hypocaloric diet weight control
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Of 23 patients with non-insulin-dependent diabetes mellitus (NIDDM), whose fasting blood glucose had not reached ≤6.0 mmol·l−1 after 10 weeks of dietary regulation, 15, who had had a weight reduction of −2.8 kg by dietary control, did achieve a fasting blood glucose ≤6.0 mmol·l−1 after addition of ≤20 mg glipizide daily. They had a sustained (≥2 years) increase in meal-induced insulin secretion (32% increase in postprandial C-peptide AUC), and a sustained reduction in postprandial hyperglycaemia (34% reduction in AUC). Ten of the patients took a mean daily dose 〈5mg (4.8 mg) and had a sustained increase in insulin secretion rate (increased C-peptide slope). The 15 patients had no elevation of basal insulin secretion and no impairment of weight reduction. The remaining 8 subjects, who showed little or no weight reduction on dietary control, had little or no reduction in fasting blood glucose despite long-term treatment with 20 mg glipizide daily, a less sustained increase in meal-induced insulin secretion, a smaller reduction of postprandial hyperglycaemia, and an increase in body weight. On diagnosis the 8 subjects did not differ from the other 15 subjects in age, body weight, blood glucose, HbA1c, C-peptide or insulin, nor in their glucose and insulin responses to a test dose of glipizide; the main reason for the apparent drug failure appeared to be deficient compliance with dietary regulation rather than a primary inability to respond to sulphonylurea treatment. The findings indicate that glipizide is able to promote and maintain increased meal-induced insulin secretion and near-normal fasting and non-fasting blood glucose levels without continuous B cell stimulation. However, these improvements prevail mainly in subjects who persist with hypocaloric dietary regulation.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 20 (1981), S. 123-125 
    ISSN: 1432-1041
    Keywords: paracetamol ; breast milk ; plasma ; drug excretion in breast milk ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Breast milk and plasma levels of paracetamol were monitored in 3 lactating women after ingestion of a single 500 mg dose of paracetamol. The paracetamol concentrations were consistently lower in milk, with a mean milk/plasma AUC ratio of 0.76. This value was in close agreement with the milk/plasma partition ratio of 0.81 foundin vitro, and could be related to quantitative binding differences between the two fluids. The half-lives of paracetamol in plasma and breast milk were almost identical, with an overall mean of 2.7 h. As less than 0.1% of the maternal dose would be present in 100 ml milk, breast feeding need not be discontinued due to paracetamol treatment in conventional dosage.
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  • 3
    ISSN: 1432-1041
    Keywords: glipizide ; diabetes mellitus ; NIDDM ; insulin release ; glucose disposal
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An early defect in subjects with non-insulin-dependent diabetes mellitus (NIDDM) and the preceding phase of impaired glucose tolerance (IGT) is a reduction in early insulin release and hence a prolonged elevation of postprandial blood glucose. We therefore assessed whether a rapidly acting sulphonylurea (glipizide 5 mg 0.5 h before a test meal) could correct these disturbances in 38 IGT/NIDDM subjects, whose early insulin release and postprandial blood glucose elevations remained unimproved after 10 weeks of dietary regulation. We also assessed whether the efficacy of glipizide was dependent upon the ambient blood glucose concentration, and if early systemic availability of the drug was important for the blood glucose lowering effect. A single dose of glipizide normalized early insulin release and hence reduced the postprandial blood glucose increase that was not lowered by dietary regulation. The efficacy of glipizide was dependent upon the early systemic availability of the drug, but early systemic availability and efficacy were independent of the extent of blood glucose elevation, at least within a range of 6–12 mmol·l−1 of fasting blood glucose.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 20 (1981), S. 229-231 
    ISSN: 1432-1041
    Keywords: atenolol ; metoprolol ; beta blockers ; excretion in milk ; accumulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Passage of the cardioselective beta adrenoceptor antagonists atenolol and metoprolol from serum to breast milk was assessed in 7 lactating women treated with atenolol due to hypertension developing during pregnancy, and in 3 healthy women who agreed to take metoprolol at cessation of lactation. For both drugs, the concentration in breast milk was higher than that in serum at every time studied, and the resulting AUC values were 1.5–6.8 times (atenolol) and 2.6–3.7 times (metoprolol) greater in milk than in serum. Assuming ingestion of 75 ml milk per meal, and as the maximum milk concentrations recorded were 6.35 µmol/l (atenolol) and 2.58 µmol/l (metoprolol), the data indicate that the dose following a meal at the time of maximum maternal drug concentration would not exceed 0.13 mg atenolol and 0.05 mg metoprolol, and would be considerably less after the other meals. In the only infant from whom serum samples could be obtained, the plasma atenolol concentration ranged between 0 and 0.26 µmol/l. None of the atenolol-exposed infants had any sign of an effect of the beta blocker. It would seem likely that, unless renal (atenolol) or hepatic (metoprolol) function in the infant were pronouncedly impaired, breast feeding need not be interrupted due to maternal medication with ordinary doses of either of these drugs. However, the infants should be observed for signs of beta blockade.
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