Absolute bioavailability of reboxetine enantiomers and effect of gender on pharmacokinetics

Fleishaker, Joseph C.; Mucci, Massimiliano; Pellizzoni, C.; Poggesi, Italo

doi:10.1002/(sici)1099-081x(199901)20:1<53::aid-bdd157>3.0.co;2-p

Cited by 42 publications

(31 citation statements)

References 7 publications

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“…Reboxetine is well absorbed and undergoes little firstpass metabolism (9), so that the increase in plasma level of reboxetine is due to reduced capacity for elimination of the drug. This is manifested in the low apparent clearance of reboxetine in this population (0.56 l/h) and in the increase in terminal half-life in elderly subjects (24 ± 6 h vs. 12 ± 3 h in non-elderly volunteers [4]).…”

Section: Resultsmentioning

confidence: 84%

Pharmacokinetics of reboxetine in healthy, elderly volunteers

Bergmann

Laneury²,

Duchêne³

et al. 2000

Eur. J. Drug Metab. Pharacokinet.

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The pharmacokinetic characteristics of reboxetine, a unique selective noradrenaline reuptake inhibitor (selective NRI) for the treatment of depression, were studied in 12 healthy, elderly volunteers (mean age 81 years +/- 9 years). All subjects received a single 4-mg dose of reboxetine, and plasma reboxetine concentrations were measured by HPLC. Reboxetine was well tolerated by all subjects. Exposure to reboxetine was higher in this group of very elderly subjects, compared with data obtained in a similar study of young, healthy volunteers. Cmax in the elderly was 271 +/- 86 ng/ml, compared with 111 +/- 28 ng/ml in the young subjects after a single 4-mg dose, although in both groups Cmax was observed after 2 h. The AUC infinity was nearly four times that in the younger subjects (8345 +/- 3107 ng.h/ml vs. 2106 +/- 881 ng.h/ml) and the t1/2 was twice as long (24 +/- 6 h vs. 12 +/- 3 h). Renal clearance was also reduced. Reboxetine 8-10 mg/day has been effective and well tolerated in clinical trials in non-elderly depressed patients. The increased exposure to reboxetine observed in our very elderly subjects supports a reduction of the starting dose to 4 mg/day (in two divided doses) in the elderly.

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Section: Resultsmentioning

confidence: 84%

Pharmacokinetics of reboxetine in healthy, elderly volunteers

Bergmann

Laneury²,

Duchêne³

et al. 2000

Eur. J. Drug Metab. Pharacokinet.

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“…4) were selected according to literature data [36][37][38][39] and confirmed as the actually desired transporters using the SEA search tool. 40) The three-dimensional structures of these compounds were obtained from the ZINC database (codes ZINC01530638, ZINC00002284 and ZINC00020228, respectively).…”

Section: Methodsmentioning

confidence: 92%

Molecular Docking and Panicolytic Effect of 8-Prenylnaringenin in the Elevated T-Maze

et al. 2014

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“…181 Reboxetine is absorbed rapidly and almost completely after oral administration. 182,183 Food delays but does not influence the extent of absorption (see Table 2). 184 Reboxetine is extensively bound to plasma proteins and has a moderate distribution volume compared with other antidepressants.…”

Section: Reboxetinementioning

confidence: 99%

“…175 Nausea, diarrhea, constipation, dry mouth, insomnia, decreased appetite, hyperhidrosis and dizziness ($10%) 175 ; less common: nervousness, tremor, and increased blood pressure (2%). 45,183 Withdrawal rates due to adverse events 4%-8%. Response and remission rates: 58% and 48%, respecitvely, after 8 weeks.…”

mentioning

confidence: 99%

Getting the balance right: Established and emerging therapies for major depressive disorders

Perović

Jovanović²,

Miljković³

et al. 2010

NDT

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Major depressive disorder (MDD) is a common and serious illness of our times, associated with monoamine deficiency in the brain. Moreover, increased levels of cortisol, possibly caused by stress, may be related to depression. In the treatment of MDD, the use of older antidepressants such as monoamine oxidase inhibitors and tricyclic antidepressants is decreasing rapidly, mainly due to their adverse effect profiles. In contrast, the use of serotonin reuptake inhibitors and newer antidepressants, which have dual modes of action such as inhibition of the serotonin and noradrenaline or dopamine reuptake, is increasing. Novel antidepressants have additive modes of action such as agomelatine, a potent agonist of melatonin receptors. Drugs in development for treatment of MDD include triple reuptake inhibitors, dual-acting serotonin reuptake inhibitors and histamine antagonists, and many more. Newer antidepressants have similar efficacy and in general good tolerability profiles. Nevertheless, compliance with treatment for MDD is poor and may contribute to treatment failure. Despite the broad spectrum of available antidepressants, there are still at least 30% of depressive patients who do not benefit from treatment. Therefore, new approaches in drug development are necessary and, according to current research developments, the future of antidepressant treatment may be promising.

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Absolute bioavailability of reboxetine enantiomers and effect of gender on pharmacokinetics

Cited by 42 publications

References 7 publications

Pharmacokinetics of reboxetine in healthy, elderly volunteers

Pharmacokinetics of reboxetine in healthy, elderly volunteers

Molecular Docking and Panicolytic Effect of 8-Prenylnaringenin in the Elevated T-Maze

Getting the balance right: Established and emerging therapies for major depressive disorders

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