NCT01676246|CompletedPhase 1
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Sponsor study identifier
interventional
36
1 country
1
Study Start
May 2008
Date type not reportedThis date has not been verified as actual or estimated.
Primary Completion
May 2009
Actual (reported)Study Completion
June 2009
Actual (reported)Flupirtine is metabolized in-vitro via carbamate cleavage and N acetylation to glucuronides and mercapturic acid derivatives. The formation of reactive, toxic intermediate products may be influenced by genetic polymorphisms of the involved conjugative metabolic pathways. So the purpose of this study is to measure pharmacokinetics, metabolism and analgesic effects of flupirtine in dependence on the function of NAT2, UGT1A1 and GSTP1.
Registry-reported information. Elapsed time and enrollment totals alone do not measure study progress or recruitment pace.
June 2009
Actual (reported)Click on a node to explore related trials.
Dates and qualifiers reported by the registry. Estimated dates do not confirm that a milestone has occurred.
May 2008
Date type not reportedThis date has not been verified as actual or estimated.
May 2009
Actual (reported)June 2009
Actual (reported)August 28, 2012
Actual (reported)August 30, 2012
Actual (reported)bioavailability (F)
ratio of the area under the concentration time curve after oral to intravenous administration of study medication
before and 0.5,1,1.5,2,2.5,3,3.5,4,5,6,8,10,12,16,24,48,72,96,120 h after administration of study medication
delayed onset of muscle soreness (DOMS)
For pain measurements, muscle pain is stimulated by standing on tiptoes of one leg for 30 s, which requires a constriction of the affected calf muscles. The other leg is lifted and the subjects are allowed to hold on to a table to keep their balance. The pain intensity during this stimulation is then rated by means of a 10 cm visual analogue scale (VAS). The VAS is extended from "no pain" to "intolerable pain" with a precision of 1 mm.
before and 2, 4, 6, 8 h after study medication
electric pain threshold
A painful 5 Hz sine waves electrical stimuli (increase of intensity 0.2 mA/s, from 0 to 20 mA), will be applied via two gold electrodes placed on the medial and lateral side of the distal phalangeal joint (middle finger of the left hand as default-testing site). During testing, subjects keep a button continuously pressed until they find the pain intolerably and interrupt the current by releasing the button. The electrical current at which this occurred is defined as pain tolerance, the target parameter of this pain model. Each value of pain tolerance is the median of five subsequent measurements obtained at an interval of 1 min.
before and 2, 4, 6, 8 h (and 10, 12 h on study day 8) after study medication and on study days 1,2,3,4,5,6,7
amount of excretion (Ae) in urine
in 24 h intervals for 3 days
amount of excretion (Ae) of feces
5 day sampling period
100 mg flupirtine per os, pharmacokinetics of flupirtine, induce delayed onset of muscle soreness (DOMS), electric pain measurement
100 mg flupirtine intravenous, pharmacokinetics of flupirtine, induce delayed onset of muscle soreness (DOMS), electric pain measurement
Administration of 100 mg flupirtine intravenous (3 mg solution intravenously, 1 vial Kadadolon® inject)
Administration of 100 mg flupirtine per os (1 capsule Kadadolon®)
Department of Clinical Pharmacology, Ernst-Moritz-Arndt-University Greifswald
Greifswald, Mecklenburg-Vorpommern, 17487, Germany
36 participants (actual enrollment reported by the registry).
First Submitted
August 28, 2012
First Posted
August 30, 2012
Study Start
May 2008
Date type not reportedThis date has not been verified as actual or estimated.
400 mg flupirtine per os, pharmacokinetics of flupirtine, electric pain measurement
Administration of 400 mg flupirtine (1 Kadadolon® S long retard tablet)
The DOMS exercise protocol consists of two sets of 50 concentric/eccentric contractions of the calf muscles of one leg with a rest of 5 min in-between. The exercise is performed 22-26 h prior to medication. For pain measurements, muscle pain is stimulated by standing on tiptoes of one leg for 30 s, which requires a constriction of the affected calf muscles. The other leg is lifted and the subjects are allowed to hold on to a table to keep their balance. The pain intensity during this stimulation is then rated by means of a 10 cm visual analogue scale (VAS). The VAS is extended from "no pain" to "intolerable pain" with a precision of 1 mm. The stimulation is repeated with the other leg. The sequence of the legs is chosen randomly.
The method has been described to be sensitive to quantify analgesic opioid effects. Painful 5 Hz sine waves electrical stimuli (increase of intensity 0.2 mA/s, from 0 to 20 mA), which predominantly activate C-fibres, will be applied via two gold electrodes placed on the medial and lateral side of the distal phalangeal joint (middle finger of the left hand as default-testing site). During testing, subjects keep a button continuously pressed until they find the pain intolerably and interrupt the current by releasing the button. The electrical current at which this occurred is defined as pain tolerance, the target parameter of this pain model. Each value of pain tolerance is the median of five subsequent measurements obtained at an interval of 1 min.
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Primary Completion
May 2009
Actual (reported)Study Completion
June 2009
Actual (reported)Last Updated
August 30, 2012
Record last verified: 2012-08
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