2012
DOI: 10.1124/dmd.112.045120
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Excretion and Metabolism of Milnacipran in Humans after Oral Administration of Milnacipran Hydrochloride

Abstract: ABSTRACT:The pharmacokinetics, excretion, and metabolism of milnacipran were evaluated after oral administration of a 100-mg dose of [ 14 C]milnacipran hydrochloride to healthy male subjects. The peak plasma concentration of unchanged milnacipran (ϳ240 ng/ml) was attained at 3.5 h and was lower than the peak plasma concentration of radioactivity (ϳ679 ng Eq of milnacipran/ml) observed at 4.3 h, indicating substantial metabolism of milnacipran upon oral administration. Milnacipran has two chiral centers and is … Show more

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Cited by 10 publications
(5 citation statements)
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“…Plasma clearance was ∼2 times greater for F2696 than for levomilnacipran. The pharmacokinetic results are consistent with those of a milnacipran human mass balance study, in which the elimination rate for F2696 was higher than for levomilnacipran 9. Given the favorable characteristics of this enantiomer, levomilnacipran was selected for development as an antidepressant.…”
supporting
confidence: 76%
See 1 more Smart Citation
“…Plasma clearance was ∼2 times greater for F2696 than for levomilnacipran. The pharmacokinetic results are consistent with those of a milnacipran human mass balance study, in which the elimination rate for F2696 was higher than for levomilnacipran 9. Given the favorable characteristics of this enantiomer, levomilnacipran was selected for development as an antidepressant.…”
supporting
confidence: 76%
“…Milnacipran is a racemic mixture of levomilnacipran (1 S , 2 R -milnacipran) and F2696 (1 R , 2 S -milnacipran); the 2 enantiomers are not interconvertible 9. Regulatory guidelines in the United States and Europe recommend development of enantiomers over racemic drugs where appropriate,10 for a variety of reasons 11.…”
mentioning
confidence: 99%
“…[20][21][22][23] The plasma concentrations (in µM) after the administration of the SNRIs duloxetine and milnacipran have been reported to be 0.0704±0.0422 and 0.847±0.117, respectively. 24,25) In the present study, the order of cytotoxicity in HepG2 cells was sertraline, paroxetine, and duloxetine, with IC 50 values (in µM) of 1.24, 7.34, and 8.95, respectively. The plasma concentration of sertraline was about one-half that of paroxetine, and nearly equal to that of duloxetine.…”
Section: Discussionmentioning
confidence: 52%
“… 13 , 14 The metabolism and excretion of milnacipran in humans have been reported previously. 13 As already described for the racemic drug, milnacipran, 15 , 16 the primary route of metabolism of levomilnacipran is N -desethylation. Direct conjugation of levomilnacipran is a minor route of metabolism.…”
Section: Discussionmentioning
confidence: 91%