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  • pharmacokinetics  (4)
  • Blunt abdominal trauma  (2)
  • 1
    ISSN: 1432-1041
    Keywords: ketoprofen ; pharmacokinetics ; relative bioavailability ; single doses ; repeated doses ; prediction of kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of ketoprofen was studied in the same healthy subjects after single oral, intramuscular and rectal doses, and after repeated oral administration. No significant difference in the mean t1/2 (1.13–1.27 h) was observed after the different modes of administration. The mean [AUC] 0 ∞ after rectal administration of a suppository showed the minimum significant difference (p〈0.05) from that after oral administration of the capsule. The apparent volume of distribution (Vd/F) was approximately 10–15% of body weight. The renal contribution (mean, 0.10–0.15 ml/min/kg) to the plasma clearance of free ketoprofen was assumed to be, at most, 8.3–12.9%. The projected cumulative excretion of total (free plus conjugated) ketoprofen via urine exceeded 63–75% of the dose, of which approximately 90% was ketoprofen glucuronide. A mean of 71–96% and 73–93% of the oral capsule was estimated to be systemically available after administration of the intramuscular preparation and rectal suppository, respectively. In four of seven subjects, CPK concentration was elevated after the intramuscular injection. The mean steady-state concentration of ketoprofen in plasma ranged from 0.43 to 5.62 µg/ml after the final dose of a 50 mg q.i.d. regimen. The disposition data and plasma levels observed at steady-state were in agreement with those predicted from the single oral dose study. The accumulation ratio was 1.08±0.08. The results suggest that the rectal suppository can be recommended as an extravascular mode of administration of this drug.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: theophylline ; smoking habit ; absolute bioavailability ; pharmacokinetics ; sustained release preparation ; plain tablet preparation ; antipyrine pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability and pharmacokinetics of theophylline from a plain uncoated and 2 newly designed, sustained-release tablet formulations, as compared to intravenous aminophylline, were studied in 12 healthy adult male volunteers. The subjects were divided into two groups (n=6) with respect to smoking habit and on 4 separate occasions each received, on a randomized cross-over basis, a single dose of 400 mg equivalent of theophylline from every dosage form. The intravenous aminophylline study showed that habitual smoking had a significant (p〈0.05) effect on plasma theophylline clearance (0.051±0.006 vs 0.035±0.004 l/kg/h). Smoking significantly reduced the raw AUC from the 4 dosage forms (p〈0.05), but did not change the characteristics of absorption of each formulation. There was a non-significant trend towards reduced absolute bioavailability of theophylline from sustained-release formulations in smokers (percentage mean difference — 16% for one formulation and 13% for another). The trend was not observed for the plain uncoated tablet, which was rapidly absorbed (p〈0.01 to 0.05 in Ka, tmax and Cmax compared to sustained-release tablets). Similarity of the in vitro dissolution profiles of the two sustained-release formulations did not imply similarity of the in vivo absorption characteristics. Plasma clearances of theophylline and antipyrine were significantly correlated (p〈0.05,r=0.693,n=10). Thus, smoking enhanced the elimination of theophylline regardless of the dosage form administered. However, the extent to which habitual smoking may affect the hepatic first-pass effect on theophylline from sustained-release formulations requires further study. The results also suggest that theophylline and antipyrine may share a similar or common and presumably polycyclic hydrocarbon-inducible form(s) of microsomal drugmetabolizing enzyme.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1041
    Keywords: carteolol ; pharmacokinetics ; beta-adrenoreceptor blocking drug ; absolute bioavailability ; plasma levels ; urinary excretion ; renal handling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and absolute bioavailability of a new nonselective β-adrenoreceptor blocking agent, carteolol, were investigated after administration of single intravenous and oral doses to eight normal volunteers. Plasma and urine drug concentrations were measured by an HPLC method. The pharmacokinetic parameters after intravenous dosing were obtained by a two-compartment analysis: elimination or β-phase t1/2 4.7±0.3 h; Vc, 0.74±0.101/kg; Vd, 4.05±0.48 l/kg; Cl, 10.13±0.94 ml/min/kg; ClR, 6.56±0.58 ml/min/kg; and ClNR, 3.57±0.40 ml/min/kg. The absolute bioavailability obtained from plasma data was 83.7±8.0%, which was consistent with that derived from analysis of urine of 82.7±4.2%. The amounts excreted unchanged in urine up to 48 h after the intravenous and oral doses were 65.0±1.5% and 53.8±3.2% of the administered doses, respectively. The t1/2 for removal of the drug derived from plasma and urine findings after intravenous and oral dosing were similar, which indicates that the main route of elimination of carteolol is via the kidneys. As the ClR of carteolol exceeded the Cl of creatinine there may be renal tubular secretion of the drug.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-1041
    Keywords: SUN 1165 ; renal failure ; antiarrhythmic agent ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of a new Class I antiarrhythmic agent, SUN 1165, has been studied in 32 patients with varying degrees of renal impairment following a single oral dose of 50 mg. The apparent volume of distribution at steady state was 1.48 1 · kg−1, the absorption rate constant was 2.2 h−1, and plasma protein binding was 26.8% in subjects with normal renal function. These variables were not altered with renal impairment. More than 60% of SUN 1165 given orally was excreted unchanged via the kidney, both by tubular secretion and glomerular filtration. The elimination rate constant, the apparent total body clearance and the apparent renal clearance were linearly correlated with the endogenous creatinine clearance. The half-time of elimination was 3.4 h in normal subjects and it was prolonged to 23.7 h in severe renal failure (creatinine clearance below 20 ml · min−1 · 1.48 m−2). Dosage adjustment of SUN 1165 is necessary in renal failure.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Pediatric surgery international 12 (1997), S. 132-136 
    ISSN: 1437-9813
    Keywords: Key words Laparoscopy ; Blunt abdominal trauma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  This study evaluates the safety and role of laparoscopy in the diagnosis of blunt abdominal trauma in children. Laparoscopy was performed in five patients aged 3 to 13 years because of persistent abdominal pain after blunt trauma. A laparotomy was not indicated from the physical examination, laboratory data, or radiologic findings. With the patient under general anesthesia, a 10-mm trocar was inserted through the umbilical fossa and the intra-abdominal organs were observed for 10 – 60 min under an insufflation pressure of 10 – 12 mmHg. The patients remained hemodynamically stable without pneumothorax development. Three patients underwent laparatomies: one, who had blood in the omental sac, had a duodenal injury with hemorrhagic necrosis and underwent a resection; one with ascites and high amylase levels had an injury of the main pancreatic duct and underwent resection of the pancreatic tail; and one who had fresh blood in the upper abdomen and Douglas’ pouch had a splenic hemorrhage and underwent hemostasis. The other two had serous or serosanguinous ascites and recovered without surgery. In patient 1, the same amount of information might have been obtained from a barium study. In patient 2, the pancreatic transection might have been diagnosed from ascites shown on serial computed tomograms. Patient 3 might also have been treated successfully non-surgically. It hus appears that laparoscopy may be a safe diagnostic method for blunt abdominal trauma in children, however, this small series has yielded insufficient information to assess its usefulness in making the diagnosis and the decision for laparotomy. Further studies are required to ascertain whether it will make any significant difference in the form of management.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Pediatric surgery international 12 (1997), S. 132-136 
    ISSN: 1437-9813
    Keywords: Laparoscopy ; Blunt abdominal trauma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This study evaluates the safety and role of laparoscopy in the diagnosis of blunt abdominal trauma in children. Laparoscopy was performed in five patients aged 3 to 13 years because of persistent abdominal pain after blunt trauma. A laparotomy was not indicated from the physical examination, laboratory data, or radiologic findings. With the patient under general anesthesia, a 10-mm trocar was inserted through the umbilical fossa and the intra-abdominal organs were observed for 10–60 min under an insufflation pressure of 10–12 mmHg. The patients remained hemodynamically stable without pneumothorax development. Three patients underwent laparatomies: one, who had blood in the omental sac, had a duodenal injury with hemorrhagic necrosis and underwent a resection; one with ascites and high amylase levels had an injury of the main pancreatic duct and underwent resection of the pancreatic tail; and one who had fresh blood in the upper abdomen and Douglas' pouch had a splenic hemorrhage and underwent hemostasis. The other two had serous or serosanguinous ascites and recovered without surgery. In patient 1, the same amount of information might have been obtained from a barium study. In patient 2, the pancreatic transection might have been diagnosed from ascites shown on serial computed tomograms. Patient 3 might also have been treated successfully non-surgically. It hus appears that laparoscopy may be a safe diagnostic method for blunt abdominal trauma in children, however, this small series has yielded insufficient information to assess its usefulness in making the diagnosis and the decision for laparotomy. Further studies are required to ascertain whether it will make any significant difference in the form of management.
    Type of Medium: Electronic Resource
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