European journal of clinical pharmacology
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Eur. J. Clin. Pharmacol. · Aug 2007
Randomized Controlled Trial Multicenter Study Comparative StudyComparison of intravenous dexketoprofen and dipyrone in acute renal colic.
The aim of this study was to assess the efficacy and safety of a single intravenous (i.v.) bolus of dexketoprofen trometamol compared with an i.v. infusion of dipyrone in patients with moderate to severe pain due to renal colic. ⋯ Dexketoprofen 50 mg administered as a single i.v. bolus was effective for the relief of moderate to severe pain in patients with renal colic, with a good safety profile and efficacy similar to i.v. dipyrone 2 g. Dexketoprofen produced analgesia that was faster in onset.
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Eur. J. Clin. Pharmacol. · Aug 2007
Randomized Controlled TrialPharmacokinetics of morphine-6-glucuronide following oral administration in healthy volunteers.
After oral administration, morphine-6-glucuronide (M6G) displays an atypical absorption profile with two peak plasma concentrations. A proposed explanation is that M6G is hydrolysed to morphine in the colon, which is then absorbed and subsequently undergoes metabolism in the liver to morphine-3-glucuronide (M3G) and M6G. The aims of this study were to confirm and elucidate the biphasic absorption profile as well as clarify the conversion of M6G to morphine after a single oral administration of M6G in healthy volunteers. ⋯ The pharmacokinetic profile of M6G after oral administration was confirmed and with the presence of M3G and morphine in plasma after oral administration of M6G, proof seems to be found of the constant and prolonged absorption of M6G. The K(M6G_abs)/K(M6G_M6G) ratio of 10 indicates that the second absorption peak of M6G consists of approximately 10 times more absorbed M6G than reglucuronidated M6G. However, further studies are required to determine the precise kinetics of the second absorption peak.
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Eur. J. Clin. Pharmacol. · Apr 2007
Randomized Controlled TrialEarly-phase pharmacokinetics of enteral and parenteral nimodipine in patients with acute subarachnoid haemorrhage - a pilot study.
The pharmacokinetics of nimodipine following enteral administration in the early phase after subarachnoid haemorrhage (SAH) has not been described. If a sufficient absorption could be achieved with enterally administered nimodipine, this would be more feasible dosage form and result in a significant reduction in pharmaceutical costs given that the parenteral formulation of nimodipine currently used is tenfold more expensive than the enteral formulation. ⋯ This pilot study indicates that the rate and extent of nimodipine absorption following enteral administration in some acute SAH patients could be negligible, and this may particularly be the case in patients with a decreased level of consciousness.
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Eur. J. Clin. Pharmacol. · Apr 2006
Randomized Controlled TrialInvestigation of sarizotan's impact on the pharmacokinetics of probe drugs for major cytochrome P450 isoenzymes: a combined cocktail trial.
The 5HT(1A) receptor agonist sarizotan is in clinical development for the treatment of dyskinesia, a potentially disabling complication in Parkinson's disease. We investigated the effect of sarizotan on the clinical pharmacokinetics of probe drugs for cytochrome P450 (CYP) to evaluate the risk of CYP-related drug-drug interactions. ⋯ At a dose higher than that intended for clinical use (1 mg b.i.d.), sarizotan had no effect on the metabolism and pharmacokinetics of specific probe drugs for CYP isoenzymes 1A2, 2C19, 2C9, 2D6 and 3A4. Pharmacokinetic interactions with co-administered drugs metabolised by these CYP isoforms are not expected, and dose adjustment of co-administered CYP substrates is not necessary.
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Eur. J. Clin. Pharmacol. · Jun 2005
Randomized Controlled Trial Comparative StudyThe effects of tramadol on static and dynamic pupillometry in healthy subjects--the relationship between pharmacodynamics, pharmacokinetics and CYP2D6 metaboliser status.
The main objective of the present study was to provide information on whether static and dynamic pupillometry can be used for pharmacodynamic profiling, particularly when investigating opioid-like drugs, such as tramadol. ⋯ The EMs and PMs of CYP2D6 treated with tramadol behaved differently in static and dynamic pupillometry. The reason for this could largely be explained with the aid of the metaboliser status and the pharmacokinetic properties of tramadol. In EMs, the pupillometric response was mainly driven by the (+)-M1, which comprises the mu action component of tramadol; whereas, in PMs, the non-mu component appears to play an important role. Thus, pupillometry was found to be useful in pharmacodynamic profiling and provides a good correlation with the pharmacokinetics.