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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 233-240 
    ISSN: 1432-1041
    Keywords: Atropine ; methylatropine ; heart rate ; saliva secretion ; arrhythmia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Intravenous atropine sulphate (0.25, 0.40, 0.75 and 1.50 mg), atropine methylnitrate (0.08, 0.13 and 0.25 mg) and saline were given to 72 healthy medical students. The effects on heart rate and rhythm, systolic and diastolic blood pressure and salivary secretion were studied. Salivation was inhibited by all the doses of the two drugs. There was a clear dose-response relationship and methylatropine was about 3 times as potent as atropine. Heart rate was accelerated by 0.75 and 1.50 mg atropine, and 0.25 mg methylatropine, whereas 0.25 mg atropine and 0.08 and 0.13 mg methylatropine induced bradycardia, which was considered to be due to a peripheral action. It is suggested that the drugs act as partial agonists at muscarinic receptors. No clear effect on blood pressure was seen, except for the highest dose of atropine, after which the diastolic pressure was increased. 20 out of 59 subjects who received anticholinergics developed supra-ventricular arrhythmias; with both drugs periods of nodal rhythm were most common. They appeared shortly after the injection and usually lasted for a few minutes.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: theophylline ; caffeine ; apnoea ; aminophylline ; infant ; plasma level ; plasma clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma concentrations of caffeine and theophylline were simultaneously determined in 17 preterm infants after oral administration of aminophylline for treatment of apnoea. The ratio of caffeine/theophylline concentration in plasma increased during the first 2 weeks of treatment, owing to the longer time required for caffeine than for theophylline to reach steady state. The caffeine/theophylline ratio at steady state was 0.57±0.03 (mean±SE). Thus, caffeine contributed significantly to the total methylxanthine load in the infants. The plasma clearance of theophylline was calculated from the plasma steady state concentrations. In 3 preterm infants treated with oral aminophylline, repeated sampling showed an approximately linear increase in clearance with time from 16.8±0.4 (mean±SE) at a postnatal age of 6–11 days to 30.9±2.5 ml/kg/h at 64–69 days. In 1 full-term infant treated with oral theophylline from 3.5 to 11.5 months of age, the plasma clearance of theophylline increased in a roughly linear manner, reaching a plateau of about 100 ml/kg/h at 6–7 months of age. This corresponds to the clearance found in 1–4 year old infants.
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  • 3
    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.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 29 (1986), S. 619-623 
    ISSN: 1432-1041
    Keywords: terbutaline ; pregnancy ; pharmacokinetics ; preterm labour ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Terbutaline in plasma was determined in three groups of women by gas chromatography-mass spectrometry. Eight women received a single i.v. dose of 0.25 mg terbutaline sulphate during pregnancy and 3–6 months after delivery. Mean plasma clearance was 29% higher during pregnancy than after delivery. There was a subsequent decrease in mean terminal half-life from 5.3 to 3.7 h and in mean residence time from 5.3 to 3.4 h. There was no change in volume of distribution. A second group of pregnant women in premature labour (n=8) received oral terbutaline 5 mg t.d.s. The dosing was repeated after delivery. The mean steady state plasma concentration of terbutaline was about 30% lower during pregnancy than after delivery. A third group of women in preterm labour (n=8) was treated with an i.v. infusion of terbutaline. The concentrations of terbutaline found on cessation of uterine contractions ranged between 12.8 and 31.5 ng/ml. At present there is no basis for formulation of a “therapeutic plasma level” of terbutaline for the treatment of preterm labour.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Histochemistry and cell biology 78 (1983), S. 195-209 
    ISSN: 1432-119X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary The distribution of carbonic anhydrase in the kidney of the cynomolgus monkey was studied by the histochemical method of Hansson. Glomeruli and Bowman's capsule were inactive. Convoluted proximal tubules showed high enzyme activity at the brush border and the basolateral membranes and in the cytoplasm. Straight proximal tubules were less intensely stained. In nephrons with long loops of Henle, the descending thin limb contained weak enzyme activity, whereas the ascending thin limb was inactive. The thick limb of Henle's loop displayed most enzyme activity at the luminal cell border. In distal convoluted tubules enzyme activity was restricted to the basal part of the cells. In the late distal tubule, intercalated cells appeared among the “ordinary” distal cells and contained abundant cytoplasmic enzyme. Many intensely stained intercalated cells were also found in the cortical and outer medullary segments of the collecting duct, intermingled with more weakly stained chief cells. In the inner medullary segment of the collecting duct, enzyme activity gradually disappeared. Many capillaries were clearly stained for enzyme activity. The capillary staining apparently varied with that of the kidney tubules; virtually all capillaries in the cortex, but very few in the inner medulla, were stained. The distribution of carbonic anhydrase in the kidney tubules of the monkey is very similar to that in man and in the rat, but the primate kidney differs from the rat kidney by the presence of capillary enzyme activity. The functional importance of this difference is not clear at present.
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