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reboxetine

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Description

Reboxetine: A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID127151
CHEMBL ID383921
CHEBI ID135342
SCHEMBL ID34533
MeSH IDM0201546

Synonyms (45)

Synonym
71620-89-8
reboxetine
DB00234
reboxetine [inn]
CHEBI:135342
(r)-2-((r)-(2-ethoxyphenoxy)(phenyl)methyl)morpholine
98769-81-4
edronax (tn)
D08472
reboxetine (inn)
(2r)-2-[(r)-(2-ethoxyphenoxy)-phenylmethyl]morpholine
A837261
reboxetine [inn:ban]
unii-947s0yz36i
947s0yz36i ,
hsdb 7701
morpholine, 2-((r)-(2-ethoxyphenoxy)phenylmethyl)-, (2r)-rel-
AKOS015966368
CHEMBL383921
SCHEMBL34533
reboxetine [hsdb]
reboxitine
reboxetine [vandf]
(+/-)-(2r*)-2-((.alpha.r*)-.alpha.-(o-ethoxyphenoxy)benzyl)morpholine
reboxetine [mi]
reboxetine [who-dd]
DTXSID1048257
morpholine, 2-[(r)-(2-ethoxyphenoxy)phenylmethyl]-, (2r)-rel-
morpholine, 2-[(2-ethoxyphenoxy)phenylmethyl]-, (r*,r*)-
AB00920697_06
41X ,
(2r)-2-[(r)-(2-ethoxyphenoxy)(phenyl)methyl]morpholine
us9944618, compound id no. 178
bdbm388642
reboxe- tine
r,r-reboxetine
BCP12060
D95753
AS-56251
(r,r)-(-)-reboxetine
DTXSID401315414
105017-38-7
EN300-19659906
HY-14560
CS-0003444

Research Excerpts

Overview

Reboxetine is a norepinephrine reuptake inhibitor that may be useful in treating pediatric depression as well as attention-deficit/hyperactivity disorder (ADHD) Reboxetine seems to be an alternative in the treatment of enuretic children who have not responded to standard treatment.

ExcerptReferenceRelevance
"Reboxetine is a potent and selective norepinephrine reuptake inhibitor that was effective in combination with citalopram for resistant obsessive-compulsive disorder (OCD). "( Reboxetine Combination Therapy With Fluoxetine in Moderate to Severe Obsessive-Compulsive Disorder: A Placebo-Controlled, Double-Blind, Randomized Trial.
Akhondzadeh, S; Boroon, M; Hasanzadeh, A; Moghaddam, HS; Shalbafan, M; Shamabadi, A; Tilaki, EH,
)
3.02
"Reboxetine is a norepinephrine reuptake inhibitor that may be useful in treating pediatric depression as well as attention-deficit/hyperactivity disorder (ADHD). "( Reboxetine treatment for autistic spectrum disorder of pediatric patients with depressive and inattentive/hyperactive symptoms: an open-label trial.
Golubchik, P; Sever, J; Weizman, A,
)
3.02
"Reboxetine seems to be an alternative in the treatment of enuretic children who have not responded to standard treatment."( Reboxetine in therapy-resistant enuresis: A randomized placebo-controlled study.
Hägglöf, B; Lundmark, E; Nevéus, T; Stenberg, A, 2016
)
3.32
"Reboxetine is a clinically used antidepressant and is a racemic mixture of two enantiomers, SS- and RR-reboxetine. "( Estimation of binding rate constants using a simultaneous mixed-effects method: application to monoamine transporter reuptake inhibitor reboxetine.
Benson, N; Birdsall, NJ; Butt, RP; Napier, C; Ploeger, B; Sale, H; Snelder, N; van der Graaf, PH, 2010
)
2.01
"Reboxetine is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of a new antidepressant class. "( Reboxetine in clinical practice: a review.
Corbo, M; Fiori, F; Martinotti, G; Sepede, G, 2012
)
3.26
"Reboxetine is a chiral compound, and is marketed as a racemic mixture of (R,R)- and (S,S)-reboxetine; however, the pharmacokinetic and toxicological profiles of the two enantiomers are rather different."( Separation of reboxetine enantiomers by means of capillary electrophoresis.
Cannazza, G; Fanali, S; Mandrioli, R; Parenti, C; Raggi, MA; Sabbioni, C, 2002
)
1.4
"Reboxetine is a selective norepinephrine (NE) reuptake inhibitor and shows only low affinity for adrenergic and muscarinic receptors."( Effects of reboxetine, a selective norepinephrine reuptake inhibitor, on sympathetic and parasympathetic outflow to the heart: preliminary data.
Agelink, MW; Baumann, B; Majewski, T; Strum, S; Ullrich, H, 2002
)
1.43
"Reboxetine is a selective norepinephrine (NE) reuptake inhibitor that exerts significant antidepressant action. "( Norepinephrine-gamma-aminobutyric acid (GABA) interaction in limbic stress circuits: effects of reboxetine on GABAergic neurons.
Bodie, B; Herman, JP; Renda, A, 2003
)
1.98
"Reboxetine is a noradrenergic antidepressant that is not metabolized by CYP450 and may offer a valuable option in the treatment of MDD in HIV-seropositive patients."( An open trial of reboxetine in HIV-seropositive outpatients with major depressive disorder.
Carvalhal, AS; Correa, J; de Abreu, PB; Kapczinski, F; Spode, A, 2003
)
1.38
"Reboxetine (REB) is a member of a new class of antidepressant drugs, which selectively inhibit the neuronal reuptake of noradrenaline. "( Effect of repeated treatment with reboxetine on the central alpha 1-adrenergic and dopaminergic receptors.
Dziedzicka-Wasylewska, M; Kuśmider, M; Margas, W; Rogóz, Z; Skuza, G; Solich, J,
)
1.85
"Reboxetine is a novel antidepressant with a selective action on noradrenaline. "( Reboxetine promotes social bonding in healthy volunteers.
Bond, AJ; Tse, WS, 2003
)
3.2
"Reboxetine is a specific norepinephrine transporter (NET) inhibitor and has been marketed in several countries as a racemic mixture of the (R,R) and (S,S) enantiomers for the treatment of depression. "( Evaluation of a new norepinephrine transporter PET ligand in baboons, both in brain and peripheral organs.
Alexoff, D; Carter, P; Ding, YS; Garza, V; King, P; Lin, KS; Logan, J; Shea, C; Xu, Y, 2003
)
1.76
"Reboxetine is a selective noradrenaline reuptake inhibitor, whereas mirtazapine acts as an antagonist at noradrenergic alpha(2), serotonin (5-HT(2)), 5-HT(3) and histamine H(1) receptors. "( Mirtazapine decreases stimulatory effects of reboxetine on cortisol, adrenocorticotropin and prolactin secretion in healthy male subjects.
Baghai, T; Laakmann, G; Schüle, C, 2004
)
2.03
"Reboxetine is a novel selective noradrenaline reuptake inhibitor. "( Reboxetine induces similar sleep-EEG changes like SSRI's in patients with depression.
Held, K; Kuenzel, HE; Murck, H; Steiger, A; Ziegenbein, M, 2004
)
3.21
"Reboxetine is a novel antidepressant, which inhibits the reuptake of norepinephrine."( Adjunctive use of reboxetine in schizophrenia.
Arlt, J; Jahn, H; Kiefer, F; Naber, D; Raedler, TJ; Schick, M; Wiedemann, K, 2004
)
1.38
"Reboxetine is a selective norepinephrine reuptake inhibitor."( A possible antienuretic effect of reboxetine in children and adolescents with attention deficit/hyperactivity disorder: case series.
Laor, N; Lerer-Amisar, D; Ratner, S; Toren, P; Weizman, A, 2005
)
2.05
"Reboxetine is a novel antidepressant that has been shown to be effective in the treatment of major depressive disorders. "( The effects of reboxetine and amitriptyline, with and without alcohol on cognitive function and psychomotor performance.
Hindmarch, I; Kerr, JS; Powell, J, 1996
)
2.09
"Reboxetine is an effective antidepressant in the forced swim test and open field test in bulbectomised rats."( Noradrenaline in basic models of depression.
Leonard, BE, 1997
)
1.02
"Reboxetine is a new selective noradrenaline reuptake inhibitor that has been shown to be effective in both the short-(4-8 weeks) and long-term (up to 12 months) treatment of depression. "( Reboxetine: additional benefits to the depressed patient.
Montgomery, SA, 1997
)
3.18
"Reboxetine is a unique selective norepinephrine reuptake inhibitor (NRI) with proven antidepressant efficacy in pharmacologic and biochemical tests predictive of antidepressant properties. "( Antidepressant efficacy and tolerability of the selective norepinephrine reuptake inhibitor reboxetine: a review.
Burrows, GD; Maguire, KP; Norman, TR, 1998
)
1.96
"Reboxetine is a racemic mixture of FCE 22071 and FCE 21684 enantiomers. "( Dose proportionality of reboxetine enantiomers in healthy male volunteers.
d'Athis, P; Dostert, P; Jannuzzo, MG; Olive, G; Poggesi, I; Rey, E, 1999
)
2.05
"Reboxetine is a new antidepressant acting by selective inhibition of noradrenaline reuptake (NARI) at the synaptic cleft. "( [Reboxetine (Edronax)].
Souery, D; Sternon, J, 1999
)
2.66
"Reboxetine is a new selective norepinephrine reuptake inhibitor (selective NRI) for the short- and long-term treatment of depression that is effective and well tolerated at a dose of 8 to 10 mg/day. "( Pharmacokinetics of single-dose reboxetine in volunteers with renal insufficiency.
Coulomb, F; Duchêne, P; Ducret, F; Fiorentini, F; Fleishaker, JC; Houin, G; Jannuzzo, MG; Laneury, JP; Poggesi, I, 2000
)
2.03
"Reboxetine is a potent antidepressant, with efficacy comparable to that of imipramine, desipramine, and fluoxetine, and has improved side-effect profile. "( Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor.
Amara, SG; Bonsignori, A; Carfagna, N; Franklin, S; Hoffmann, WP; Hyslop, DK; McArthur, RA; Piercey, MF; Porsolt, RD; Sonders, MS; Tinholt, PM; Wong, EH, 2000
)
3.19
"Reboxetine is a potent, selective, and specific norepinephrine reuptake inhibitor (selective NRI) as determined by both in vitro and in vivo measurements. "( Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor.
Amara, SG; Bonsignori, A; Carfagna, N; Franklin, S; Hoffmann, WP; Hyslop, DK; McArthur, RA; Piercey, MF; Porsolt, RD; Sonders, MS; Tinholt, PM; Wong, EH, 2000
)
3.19
"Reboxetine is a potent, selective, and specific noradrenergic reuptake inhibitor. "( Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor.
Amara, SG; Bonsignori, A; Carfagna, N; Franklin, S; Hoffmann, WP; Hyslop, DK; McArthur, RA; Piercey, MF; Porsolt, RD; Sonders, MS; Tinholt, PM; Wong, EH, 2000
)
3.19
"Reboxetine is a selective noradrenaline reuptake inhibitor--the first in its class to be marketed."( The need for new and better antidepressants: reboxetine a new option.
Dencker, SJ, 2000
)
1.29
"Reboxetine is a selective noradrenaline reuptake inhibitor (selective NRI) which is effective and well tolerated in the treatment of depressed adult patients."( Reboxetine in the maintenance therapy of depressive disorder in the elderly: a long-term open study.
Aguglia, E, 2000
)
2.47
"Reboxetine is a selective norepinephrine reuptake inhibitor shown to be an effective agent in the treatment of major depressive illness. "( Reboxetine: a selective norepinephrine reuptake inhibitor for the treatment of depression.
Doraiswamy, PM; Scates, AC, 2000
)
3.19
"Reboxetine seems to be an option for the treatment of bulimia nervosa."( Reboxetine in the treatment of bulimia nervosa: a report of seven cases.
Bailer, U; de Zwaan, M; El-Giamal, N; Kasper, S; Lennkh, C; Schüssler, P; Strnad, A, 2000
)
2.47
"Reboxetine is a novel selective norepinephrine inhibitor that has been evaluated in the treatment of patients with depression. "( Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression.
Fleishaker, JC, 2000
)
2.04
"Reboxetine is a new antidepressant drug acting as a potent and selective noradrenaline reuptake inhibitor on the noradrenergic neuronal system. "( Bioanalysis of racemic reboxetine and its desethylated metabolite in a therapeutic drug monitoring setting using solid phase extraction and HPLC.
Bengtsson, F; Norlander, B; Ohman, D; Peterson, C, 2001
)
2.06
"Reboxetine is a non-tricyclic antidepressant with selective noradrenergic (NA) reuptake-blocking effects. "( Effect of the selective noradrenergic reuptake inhibitor reboxetine on the firing activity of noradrenaline and serotonin neurons.
Blier, P; Szabo, ST, 2001
)
2
"Reboxetine is an antidepressant whose major mechanism of action is as a noradrenergic reuptake inhibitor."( Reboxetine add on therapy to haloperidol in the treatment of schizophrenia: a preliminary double-blind randomized placebo-controlled study.
Berk, M; Schutz, G, 2001
)
2.47
"Reboxetine is a selective noradrenaline reuptake inhibitor (NARI). "( [Analgesic effect of the selective noradrenaline reuptake inhibitor reboxetine].
Chevts, V; Schaffler, K; Schüler, P; Seibel, K, 2002
)
1.99
"Reboxetine is a new norepinephrine reuptake inhibitor (NRI) drug recently introduced in the therapy for depressed patients. "( Determination of reboxetine, a recent antidepressant drug, in human plasma by means of two high-performance liquid chromatography methods.
Casamenti, G; Mandrioli, R; Pinzauti, S; Ragg, MA; Volterra, V, 2002
)
2.1
"Reboxetine is a selective noradrenergic reuptake inhibitor that displays an antidepressant profile in both animal tests and in clinical trials. "( Effects of acute and chronic reboxetine treatment on stress-induced monoamine efflux in the rat frontal cortex.
Lucki, I; Page, ME, 2002
)
2.05

Effects

Reboxetine has potent antidepressant activity, low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals. Reboxetine 8-10 mg/day has been effective and well tolerated in clinical trials in non-elderly depressed patients.

ExcerptReferenceRelevance
"Reboxetine has been approved for the treatment of Major Depression in many European countries, but the application for approval was rejected in the United States."( Reboxetine in clinical practice: a review.
Corbo, M; Fiori, F; Martinotti, G; Sepede, G, 2012
)
2.54
"reboxetine) has provided potentially important avenues of treatment for the disorder."( Reboxetine and citalopram in panic disorder: a single-blind, cross-over, flexible-dose pilot study.
Mohr, N; Muller, JE; Seedat, S; Stein, DJ; van Rheede van Oudtshoorn, E, 2003
)
2.48
"Reboxetine has potent antidepressant activity, low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals."( Review of the pharmacokinetics and metabolism of reboxetine, a selective noradrenaline reuptake inhibitor.
Benedetti, MS; Dostert, P; Poggesi, I, 1997
)
1.27
"Reboxetine has received two letters of approval from the Food and Drug Administration for the treatment of major depression in adults. "( Reboxetine: a selective norepinephrine reuptake inhibitor for the treatment of depression.
Doraiswamy, PM; Scates, AC, 2000
)
3.19
"Reboxetine has been shown to be an effective first-line treatment for patients with all grades of depression, to be effective in the prevention of relapse and recurrence and to offer significant benefits in terms of relieving the impaired social functioning associated with depressive disorders."( Reboxetine: the first selective noradrenaline re-uptake inhibitor.
el Giamal, N; Hilger, E; Kasper, S, 2000
)
2.47
"Reboxetine 8-10 mg/day has been effective and well tolerated in clinical trials in non-elderly depressed patients."( Pharmacokinetics of reboxetine in healthy, elderly volunteers.
Bergmann, JF; Duchene, P; Fleishaker, JC; Houin, G; Laneury, JP; Ségrestaa, JM,
)
1.18

Treatment

Reboxetine treatment was associated with a significant decrease in absolute and relative low-frequency power as well as in mean arterial pressure. 25 (56%) patients were considered "very much improved" or "much improved"; 8 (18%) patientswere "minimally improved"; 7 (16%) received ratings that reflected "no change" or minimal worsening. 5 (11%) were rated as "much worse" or 'very much worse'

ExcerptReferenceRelevance
"Reboxetine treatment may reduce, modestly but significantly, depressive and ADHD symptoms in adolescents with ASD. "( Reboxetine treatment for autistic spectrum disorder of pediatric patients with depressive and inattentive/hyperactive symptoms: an open-label trial.
Golubchik, P; Sever, J; Weizman, A,
)
3.02
"Reboxetine treatment was associated with 1) a significant decrease in absolute and relative low-frequency power as well as in mean arterial pressure on day 2, and 2) a significant decrease in the average low- to high-frequency ratio on days 2 and 10. "( Effects of reboxetine, a selective norepinephrine reuptake inhibitor, on sympathetic and parasympathetic outflow to the heart: preliminary data.
Agelink, MW; Baumann, B; Majewski, T; Strum, S; Ullrich, H, 2002
)
2.15
"With reboxetine treatment, 25 (56%) patients were considered "very much improved" or "much improved"; 8 (18%) patients were "minimally improved"; 7 (16%) received ratings that reflected "no change" or minimal worsening, and 5 (11%) were rated as "much worse" or "very much worse.""( Reboxetine: a preliminary report on its use through the Special Access Program.
Chue, P; Cohen, NL; Craigen, G; Kennedy, SH; Lam, RW; McIntyre, RS; Rosenbluth, M; Sokolov, ST, 2002
)
2.21
"Reboxetine treatment led to a rapid (evident at 2 days) enhancement in BDNF transcription in several hippocampal regions."( Hippocampal brain-derived neurotrophic factor expression following treatment with reboxetine, citalopram, and physical exercise.
Alejandre, H; Chen, MJ; Garcia, C; Ivy, AS; Russo-Neustadt, AA, 2004
)
1.27
"Reboxetine treatment (surprisingly) led to an even more enhanced serotonin transporter density (Bmax = 1322 +/- 46), while noradrenaline transporter density seemed to be unaffected."( Very early treatment with fluoxetine and reboxetine causing long-lasting change of the serotonin but not the noradrenaline transporter in the frontal cortex of rats.
Banaschewski, T; Bock, N; Hüther, G; Moll, GH; Quentin, DJ; Rothenberger, A, 2005
)
1.32
"Reboxetine-treated patients were more likely to experience constipation, difficulty urinating, and insomnia."( A meta-analysis of clinical trials comparing reboxetine, a norepinephrine reuptake inhibitor, with selective serotonin reuptake inhibitors for the treatment of major depressive disorder.
Kasper, S; Möller, HJ; Nelson, JC; Papakostas, GI, 2008
)
1.33
"Reboxetine treatment over 1 year is more effective than placebo in the prevention of relapse in patients with recurrent depression. "( Reboxetine, a unique selective NRI, prevents relapse and recurrence in long-term treatment of major depressive disorder.
Arnaud-Castiglioni, R; Gaszner, P; Mehilane, L; Versiani, M, 1999
)
3.19
"Reboxetine treatment (10 and 30 mg/kg) significantly decreased immobility and defaecation in the forced swim test in dose dependent manner."( Reboxetine attenuates forced swim test-induced behavioural and neurochemical alterations in the rat.
Connor, TJ; Harkin, A; Kelliher, P; Kelly, JP; Leonard, BE, 1999
)
2.47
"Reboxetine-treated patients were less likely to develop hypotension and related symptoms (7% vs."( Reboxetine versus imipramine in the treatment of elderly patients with depressive disorders: a double-blind randomised trial.
Bercoff, E; Chiu, E; Katona, C; Tack, P; Versiani, M; Woelk, H, 1999
)
2.47
"Treatment with reboxetine conferred no advantage over citalopram in those with physical symptoms, and it is less well tolerated."( Are multiple physical symptoms a poor prognostic factor or just a marker of depression severity? Secondary analysis of the GenPod trial.
Button, KS; Crawford, A; Green, A; Lewis, G; Nutt, D; Peters, TJ; Wiles, N, 2014
)
0.74
"Treatment with reboxetine in a schedule commonly used in the FST resulted in a potentiated noradrenergic response to the swim challenge concomitant with behavioral alterations consistent with antidepressant-like activity."( Simultaneous analyses of the neurochemical and behavioral effects of the norepinephrine reuptake inhibitor reboxetine in a rat model of antidepressant action.
Brown, K; Lucki, I; Page, ME, 2003
)
0.89

Toxicity

The study suggests that reboxetine use by lactating women is safe for the breastfed infant. The rate of discontinuation due to adverse effects was not significantly different from that observed with placebo in short-term studies. Only one patient dropped out due to a side effect (constipation)

ExcerptReferenceRelevance
" The rate of discontinuation due to adverse effects with reboxetine was not significantly different from that observed with placebo in short-term studies."( Reboxetine: tolerability and safety profile in patients with major depression.
Tanum, L, 2000
)
1.99
" Safety was evaluated by recording spontaneously reported adverse events."( Switching to reboxetine: an efficacy and safety study in patients with major depressive disorder unresponsive to fluoxetine.
Fava, M; McGrath, PJ; Sheu, WP, 2003
)
0.69
" No toxic effects in RCSN-3 cells were observed when the cells were incubated with 100 microm FeCl3 alone or complexed with dopamine."( Monoamine transporter inhibitors and norepinephrine reduce dopamine-dependent iron toxicity in cells derived from the substantia nigra.
Cardenas, S; Caviedes, P; Graumann, R; Martinez-Alvarado, P; Olea-Azar, C; Paris, I; Perez-Pastene, C; Raisman-Vozari, R; Segura-Aguilar, J; Vieira, MN, 2005
)
0.33
" Only one patient, in the reboxetine group, dropped out due to a side effect (constipation)."( [Comparison of reboxetine and sertraline in terms of efficacy and safety in major depressive disorder].
Akgöz, S; Akkaya, C; Eker, SS; Kirli, S; Sarandöl, A, 2005
)
0.98
"To investigate the transfer of reboxetine into milk, the absolute and relative infant doses via milk and to assess plasma concentrations and adverse unwanted effects in the breastfed infant."( Transfer of reboxetine into breastmilk, its plasma concentrations and lack of adverse effects in the breastfed infant.
Hackett, LP; Ilett, KF; Kohan, R; Kristensen, JH; Rampono, J, 2006
)
1
" Three of the infants met normal developmental milestones and no adverse effects were seen in any infant."( Transfer of reboxetine into breastmilk, its plasma concentrations and lack of adverse effects in the breastfed infant.
Hackett, LP; Ilett, KF; Kohan, R; Kristensen, JH; Rampono, J, 2006
)
0.71
"The study suggests that reboxetine use by lactating women is safe for the breastfed infant."( Transfer of reboxetine into breastmilk, its plasma concentrations and lack of adverse effects in the breastfed infant.
Hackett, LP; Ilett, KF; Kohan, R; Kristensen, JH; Rampono, J, 2006
)
1.02
" In 9% of patients, RLS was recorded as a side effect related to the administration of AD."( Restless legs syndrome as side effect of second generation antidepressants.
Gallwitz, T; Kirch, MH; Messer, T; Rottach, KG; Schaner, BM; Teufel, LM; Zivotofsky, AZ, 2008
)
0.35
" Where drugs have numerous actions the adverse effects of noradrenaline reuptake may be difficult to isolate, although in this respect the adverse effects of reboxetine, a specific noradrenaline re-uptake inhibitor, are illuminating."( A review of the adverse effects and safety of noradrenergic antidepressants.
Taylor, D; Whiskey, E, 2013
)
0.59
" Adverse effects are common, occur early on in treatment and are reported to be one of the main reasons for discontinuation of antidepressant treatment."( Adverse effects from antidepressant treatment: randomised controlled trial of 601 depressed individuals.
Cowen, P; Crawford, AA; Lewis, G; Lewis, S; Nutt, D; O'Donovan, MC; Peters, TJ; Wiles, N, 2014
)
0.4
"To investigate the association between adverse effects occurring in the first 2 weeks of antidepressant treatment and discontinuation by 6 weeks as the outcome."( Adverse effects from antidepressant treatment: randomised controlled trial of 601 depressed individuals.
Cowen, P; Crawford, AA; Lewis, G; Lewis, S; Nutt, D; O'Donovan, MC; Peters, TJ; Wiles, N, 2014
)
0.4
"Individuals randomised to reboxetine reported a greater number of adverse effects and were more likely to stop treatment than individuals receiving citalopram."( Adverse effects from antidepressant treatment: randomised controlled trial of 601 depressed individuals.
Cowen, P; Crawford, AA; Lewis, G; Lewis, S; Nutt, D; O'Donovan, MC; Peters, TJ; Wiles, N, 2014
)
0.7
"The majority of adverse effects were not individually associated with discontinuation from antidepressant treatment."( Adverse effects from antidepressant treatment: randomised controlled trial of 601 depressed individuals.
Cowen, P; Crawford, AA; Lewis, G; Lewis, S; Nutt, D; O'Donovan, MC; Peters, TJ; Wiles, N, 2014
)
0.4

Pharmacokinetics

The pharmacokinetics of reboxetine are linear across the dosage range of 2-8 mg/day in elderly depressed patients. Cmax and AUCtau values are higher (and more variable) than in young adults.

ExcerptReferenceRelevance
" Reboxetine pharmacokinetic parameters, calculated after the single dose using non-compartmental analysis, were in good agreement with those obtained in previous studies."( Pharmacokinetics of reboxetine in healthy volunteers. Single against repeated oral doses and lack of enzymatic alterations.
Edwards, DM; Jørgensen, NP; Paus, E; Pellizzoni, C; Poggesi, I; Strolin Benedetti, M, 1996
)
1.53
" It is a mixture of (R,R) and (S,S) enantiomer, the latter being more potent but no qualitative differences in pharmacodynamic properties are observed between the two."( Review of the pharmacokinetics and metabolism of reboxetine, a selective noradrenaline reuptake inhibitor.
Benedetti, MS; Dostert, P; Poggesi, I, 1997
)
0.55
" After reboxetine administration mean tmax was about 1 h for both enantiomers."( Pharmacokinetics of reboxetine enantiomers in the dog.
Benecchi, A; Brianceschi, G; Dostert, P; Frigerio, E; Pellizzoni, C; Poggesi, I; Strolin Benedetti, M, 1997
)
1.08
" Mean terminal half-life after administration of ketoconazole (21."( Ketoconazole inhibits the clearance of the enantiomers of the antidepressant reboxetine in humans.
Brown, MT; Fleishaker, JC; Herman, BD, 1999
)
0.53
" tmax and t1/2 were not significantly different between groups."( Pharmacokinetics of single-dose reboxetine in volunteers with renal insufficiency.
Coulomb, F; Duchêne, P; Ducret, F; Fiorentini, F; Fleishaker, JC; Houin, G; Jannuzzo, MG; Laneury, JP; Poggesi, I, 2000
)
0.59
"To examine the pharmacokinetic characteristics of the selective norepinephrine reuptake inhibitor, reboxetine, in elderly patients with depression."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.85
" Pharmacokinetic evaluations were carried out at two dosage levels in each group: at the end of weeks 1 and 3 in group A (2 and 6 mg/day), and at the end of weeks 2 and 4 in group B (4 and 8 mg/day)."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.63
" The mean area under the plasma concentration-time curve (AUCtau) and the maximum plasma drug concentration (Cmax) showed considerable variation between patients; at a dosage of 4 mg/day, AUCtau was 1,466-6,866 ngxh/ml and Cmax ranged from 169 to 663 ng/ml."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.63
"The pharmacokinetics of reboxetine are linear across the dosage range of 2-8 mg/day in elderly depressed patients, although Cmax and AUCtau values are higher (and more variable) than in young adults."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.94
" The plasma concentration-time profile following oral administration is best described by a 1-compartment model, and the mean half-life (approximately 12 hours) is consistent with the recommendation to administer the drug twice daily."( Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression.
Fleishaker, JC, 2000
)
0.6
" Ethnic group effects on pharmacokinetic parameters were assessed by ANOVA."( Pharmacokinetics of reboxetine in healthy volunteers with different ethnic descents.
Fleishaker, JC; Hendershot, PE; Lin, KM; Nuccio, ID; Poland, RE, 2001
)
0.63
"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)."( Pharmacokinetics of reboxetine in healthy, elderly volunteers.
Bergmann, JF; Duchene, P; Fleishaker, JC; Houin, G; Laneury, JP; Ségrestaa, JM,
)
0.72

Bioavailability

The absolute bioavailability of reboxetine enantiomers was assessed in six male and six female volunteers. Reboxetine is well absorbed after oral administration.

ExcerptReferenceRelevance
" These results provide evidence for the higher bioavailability and/or lower clearance of both enantiomers in mice than in rats, and for a higher penetration of both enantiomers into mouse brain compared to rat brain."( Stereoselective and species-dependent kinetics of reboxetine in mouse and rat.
Brianceschi, G; Castelli, MG; Dostert, P; Frigerio, E; Pellizzoni, C; Strolin Benedetti, M; Tocchetti, P, 1995
)
0.54
"The absolute bioavailability of reboxetine enantiomers was assessed in six male and six female volunteers."( Absolute bioavailability of reboxetine enantiomers and effect of gender on pharmacokinetics.
Fleishaker, JC; Mucci, M; Pellizzoni, C; Poggesi, I, 1999
)
0.88
" Reboxetine is well absorbed after oral administration."( Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression.
Fleishaker, JC, 2000
)
1.51

Dosage Studied

The pharmacokinetics of reboxetine are linear across the dosage range of 2-8 mg/day in elderly depressed patients, although Cmax and AUCtau values are higher (and more variable) than in young adults. The results obtained evidenced that reboxETine at a dosage of 4 mg/d mildly reduced only depressive symptoms.

ExcerptRelevanceReference
" The dosing regimen was well tolerated by all subjects."( Pharmacokinetics of reboxetine in healthy volunteers. Single against repeated oral doses and lack of enzymatic alterations.
Edwards, DM; Jørgensen, NP; Paus, E; Pellizzoni, C; Poggesi, I; Strolin Benedetti, M, 1996
)
0.62
" Pharmacokinetic evaluations were carried out at two dosage levels in each group: at the end of weeks 1 and 3 in group A (2 and 6 mg/day), and at the end of weeks 2 and 4 in group B (4 and 8 mg/day)."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.63
" The mean area under the plasma concentration-time curve (AUCtau) and the maximum plasma drug concentration (Cmax) showed considerable variation between patients; at a dosage of 4 mg/day, AUCtau was 1,466-6,866 ngxh/ml and Cmax ranged from 169 to 663 ng/ml."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.63
"The pharmacokinetics of reboxetine are linear across the dosage range of 2-8 mg/day in elderly depressed patients, although Cmax and AUCtau values are higher (and more variable) than in young adults."( Pharmacokinetics of reboxetine in elderly patients with depressive disorders.
Fleishaker, JC; Pellizzoni, C; Poggesi, I, 2000
)
0.94
" Dosage adjustments may be appropriate in elderly patients and those with renal and hepatic impairment."( Reboxetine: a selective norepinephrine reuptake inhibitor for the treatment of depression.
Doraiswamy, PM; Scates, AC, 2000
)
1.75
" The pharmacokinetics of reboxetine are linear following both single and multiple oral doses up to a dosage of 12 mg/day."( Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression.
Fleishaker, JC, 2000
)
0.9
" These samples were drawn as trough levels in steady state with a dosage range of 2-16 mg/day."( Bioanalysis of racemic reboxetine and its desethylated metabolite in a therapeutic drug monitoring setting using solid phase extraction and HPLC.
Bengtsson, F; Norlander, B; Ohman, D; Peterson, C, 2001
)
0.62
" No dosage adjustment is necessary for Asians or blacks."( Pharmacokinetics of reboxetine in healthy volunteers with different ethnic descents.
Fleishaker, JC; Hendershot, PE; Lin, KM; Nuccio, ID; Poland, RE, 2001
)
0.63
"25-5 mg/kg) did not affect the cocaine dose-response curve or its ED50 values."( Does combined treatment with novel antidepressants and a dopamine D3 receptor agonist reproduce cocaine discrimination in rats?
Filip, M; Papla, I,
)
0.13
" There were no significant changes in parkinsonian motor symptoms or dosage of levodopa."( Effect of reboxetine on depression in Parkinson's disease patients.
Lemke, MR, 2002
)
0.72
" Methodological limitations included variability in definitions of treatment-resistant depression and response to treatment, dosing of medications, and reporting of adverse events."( Combining antidepressants for treatment-resistant depression: a review.
Cohen, NL; Kennedy, SH; Lam, RW; Wan, DD, 2002
)
0.31
"Failure to respond may be defined as a < 25% decrease on an accepted symptom rating scale such as the Montgomery-Asberg Depression Rating Scale (MADRS) or the Hamilton Rating Scale for Depression (HAM-D) in a patient who has received an adequate dosage for 4 weeks."( Partial response and nonresponse to antidepressant therapy: current approaches and treatment options.
Aguglia, E; Amore, M; Delgado, PL; Gastpar, M; Hawley, C; Hirschfeld, RM; Kasper, S; Linden, M; Massana, J; Mendlewicz, J; Möller, HJ; Montgomery, SA; Nemeroff, CB; Saiz, J; Such, P; Torta, R; Versiani, M, 2002
)
0.31
" A lower and flexible reboxetine dosing schedule will be recommended for future research to improve its tolerability in PTSD patients."( Reboxetine versus fluvoxamine in the treatment of motor vehicle accident-related posttraumatic stress disorder: a double-blind, fixed-dosage, controlled trial.
Kotler, M; Shabash, E; Shaked, G; Spivak, B; Strous, RD; Weizman, A, 2006
)
2.09
" In the present study, we performed a full dose-response study of the effect of systemic reboxetine and desipramine on DA and NA in dialysates from the parietal and occipital cortices."( Differential alpha-mediated inhibition of dopamine and noradrenaline release in the parietal and occipital cortex following noradrenaline transporter blockade.
Cacciapaglia, F; Di Chiara, G; Frau, R; Valentini, V, 2006
)
0.56
"Under dual challenge conditions, we observed a linear dose-response relationship in the magnitude and duration of emotion-induced retrograde amnesia."( Emotion-induced retrograde amnesia varies as a function of noradrenergic-glucocorticoid activity.
Dolan, RJ; Hawellek, B; Hurlemann, R; Klingmuller, D; Kolsch, H; Maier, W; Matusch, A, 2007
)
0.34
" However, in combination studies, pretreatment with either disulfiram or nepicastat produced leftward shifts in the cocaine dose-response function and also conferred cocaine-like stimulus effects to the selective NE transporter inhibitor, reboxetine (0."( Dopamine β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats.
DePoy, LM; Manvich, DF; Weinshenker, D, 2013
)
0.57
" Rats had a lumbar intrathecal catheter implanted at the time of nerve injury for administration of reboxetine (10 μg) in both acute and chronic dosing experiments."( Intrathecal reboxetine suppresses evoked and ongoing neuropathic pain behaviours by restoring spinal noradrenergic inhibitory tone.
Donaldson, LF; Hickey, L; Hughes, S; Lumb, BM; Pickering, AE, 2015
)
1.01
" On the basis of these data, novel dosing strategies were developed for five antidepressants to mimic the pharmacological profile of the antidepressant with the longest half-life, fluoxetine."( The role of 5-HT1A receptors in mediating acute negative effects of antidepressants: implications in pediatric depression.
Cao, YJ; Hendrix, CW; Kaplin, AI; Rahn, KA, 2015
)
0.42
" The fact that few patients achieved complete dryness may be due to the low dosage used."( Reboxetine in therapy-resistant enuresis: A randomized placebo-controlled study.
Hägglöf, B; Lundmark, E; Nevéus, T; Stenberg, A, 2016
)
1.88
"Although recent investigations combining noradrenergic and antimuscarinic drugs have shown promising short-term results to treat obstructive sleep apnea (OSA), the mid-term effect and optimal dosage remain uncertain."( Effect of oxybutynin and reboxetine on obstructive sleep apnea: a randomized, placebo-controlled, double-blind, crossover trial.
Bayon, V; Berger, M; Bradley, B; Dussez, R; Haba-Rubio, J; Heiniger, G; Heinzer, R; Lecciso, G; Marchi, NA; Siclari, F; Solelhac, G; Van Den Broecke, S, 2023
)
1.21
" Mianserin and mirtazapine (separately) induced dose-dependent antinociception, each one yielding a biphasic dose-response curve, and they were antagonized by naloxone."( Treatment-Resistant Depression (TRD): Is the Opioid System Involved?
Keidan, L; Pick, CG; Schreiber, S, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)0.00180.00081.541620.0000AID1709035
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.03900.00031.465610.0000AID1709034
Voltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)Ki10.00000.01900.01900.0190AID1709032
Voltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)Ki10.00000.09900.09900.0990AID1709033
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (31)

Processvia Protein(s)Taxonomy
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
calcium ion transportVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of calcium ion transportVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
calcium ion transport into cytosolVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
membrane depolarization during bundle of His cell action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of membrane repolarization during action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
positive regulation of high voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
cellular response to amyloid-betaVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
neuromuscular junction developmentVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
organ growthVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
regulation of multicellular organism growthVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
positive regulation of organ growthVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
muscle cell developmentVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
rhythmic synaptic transmissionVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel activity involved in bundle of His cell action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
metal ion bindingVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
metal ion bindingVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
sarcoplasmic reticulumVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
extracellular exosomeVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
neuronal dense core vesicleVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
plasma membraneVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1709033Displacement of [3H]-gabapentin from human Cav alpha2delta2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.
AID1709035Inhibition of human NET expressed in HEK293 cells assessed as reduction in ASP+ uptake incubated for 20 mins before ASP+ addition and measured after 90 mins by scintillation counting method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.
AID1709032Displacement of [3H]-gabapentin from human Cav alpha2delta1 expressed in CHO-K1 cell membranes incubated for 60 mins by scintillation counting method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.
AID1709034Displacement of [3H]-nisoxetine from human NET expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (598)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's47 (7.86)18.2507
2000's333 (55.69)29.6817
2010's187 (31.27)24.3611
2020's31 (5.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.94

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index67.94 (24.57)
Research Supply Index6.71 (2.92)
Research Growth Index4.90 (4.65)
Search Engine Demand Index117.93 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (67.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials193 (30.83%)5.53%
Reviews59 (9.42%)6.00%
Case Studies48 (7.67%)4.05%
Observational0 (0.00%)0.25%
Other326 (52.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (36)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multi-center, Long-term, Open-label Study of [S,S]-Reboxetine (PNU-165442G) Administered Once Daily in Patients With Fibromyalgia [NCT00607256]Phase 3500 participants (Actual)Interventional2007-10-20Terminated
Noradrenaline, Acetylcholine and Dynamic Learning in Healthy Humans [NCT03957174]107 participants (Actual)Interventional2019-06-01Completed
Double-blind Clinical Trial Controlled With Placebo of the Efficacy of Reboxetine and Citalopram as an Adjunct Treatment to Second Generation Antipsychotics in the Treatment of Negative Symptoms of Schizophrenia [NCT01300364]Phase 4249 participants (Anticipated)Interventional2008-11-30Recruiting
International Committee of Medical Journal Editors [NCT02179268]Phase 3203 participants (Actual)Interventional2012-03-31Completed
A Multi-center, Long-term, Open-label Extension Study of [S,S]-Reboxetine (PNU-165442G) Administered Once Daily in Patients With Fibromyalgia [NCT00754221]Phase 3390 participants (Actual)Interventional2008-05-31Terminated(stopped due to This study has been terminated early as the esreboxetine development program is being discontinued. There are no safety or efficacy concerns.)
A Randomized, Double-Blind Placebo Controlled Trial Of [S,S]-Reboxetine In Patients With Chronic Painful Diabetic Peripheral Neuropathy. [NCT00625833]Phase 2330 participants (Actual)Interventional2007-12-31Terminated(stopped due to Study was terminated for futility following the planned interim analysis.)
A Multi-center, Randomized, Double-blind, Placebo-controlled, 3-Week Crossover Study to Assess the Efficacy and Safety of AXS-12 in Subjects With Cataplexy and Excessive Daytime Sleepiness in Narcolepsy [NCT03881852]Phase 221 participants (Actual)Interventional2019-01-30Completed
A 14-week, Randomized, Double-blind, Placebo-controlled, Multi-center Study of [S,S]-Reboxetine (PNU-165442G) Administered Once Daily (O.D.) in Patients With Fibromyalgia [NCT00612170]Phase 31,129 participants (Actual)Interventional2007-12-31Completed
Studying the Role of Brain Molecules for Decision Making [NCT04384562]160 participants (Anticipated)Interventional2020-12-17Recruiting
Reboxetine for Obstructive Sleep Apnoea After Upper Airway Surgery: a Randomised, Double-blind, Placebo-controlled Study [NCT05978505]Phase 220 participants (Anticipated)Interventional2023-08-15Not yet recruiting
Cognitive Flexibility and Its Correlation to Sleep and Neuroplasticity In The Course Of Depression During Different Treatments [NCT00993876]45 participants (Actual)Interventional2005-08-31Completed
Sertraline/[S,S]-Reboxetine Combination Versus Sertraline And [S,S]-Reboxetine Monotherapy In Major Depressive Disorder (MDD) In A Double-Blind, Placebo-Controlled, Eight Week Study. [NCT00636246]Phase 2510 participants (Actual)Interventional2004-06-30Completed
Investigating Fundamental Mechanisms of Mental and Physical Fatigue Using Neurotransmitter Reuptake Inhibitors and Electroencephalography: a Randomized Counterbalanced Crossover Trial [NCT05880342]Phase 362 participants (Anticipated)Interventional2023-05-03Recruiting
A Study to Assess the Long-term Efficacy and Safety of AXS-12 in the Treatment of Cataplexy and Excessive Daytime Sleepiness in Subjects With Narcolepsy [NCT05113745]Phase 390 participants (Anticipated)Interventional2021-10-20Enrolling by invitation
A Phase 2B Long-Term, Randomized, Open-Label, Safety And Tolerability Trial Comparing [S,S]-Reboxetine (PNU-165442g) With Routine Care In Patients With Postherpetic Neuralgia (PHN). [NCT00354094]Phase 2600 participants Interventional2006-11-30Terminated(stopped due to The study was stopped due to business/operational issues.)
Effects of Single Dose Citalopram and Reboxetine on Urethral and Anal Closure Function on Healthy Female Subjects [NCT04097288]Phase 124 participants (Actual)Interventional2019-09-17Completed
Phase 1 Study of Reboxetine Adjuvant Therapy and Cognitive and Behavioral Measures [NCT00409201]Phase 130 participants Interventional2006-03-31Recruiting
A Randomized, Double-Blind, Placebo-Controlled, Multi- Center Study to Assess the Efficacy and Safety of AXS-12 in the Treatment of Cataplexy and Excessive Daytime Sleepiness in Subjects With Narcolepsy [NCT05059223]Phase 390 participants (Anticipated)Interventional2021-09-15Recruiting
The Relation Between Attentional, Sensory and Emotional Dysregulation in Adults With Posttraumatic Stress Disorder: a Double-blind, Placebo-controlled Randomized Controlled Trial of the Combined Treatment With Reboxetine and Methylphenidate [NCT05133804]Phase 253 participants (Anticipated)Interventional2022-06-01Recruiting
Entwicklung Neuronaler Repräsentationen Nach Schlaganfall: Verbesserung Motorischer Leistungen Durch Transkranielle Gleichstromstimulation Und Noradrenerge Co-Stimulation [NCT00853866]Phase 412 participants (Actual)Interventional2009-01-31Completed
Effect of Escitalopram vs. Reboxetine on Somatic and Visceral Sensitivity of Patients With Major Depressive Disorder: a Randomized, Double Blind Clinical Trial [NCT00209807]Phase 442 participants (Anticipated)Interventional2005-09-30Recruiting
A 5-Week, Randomized, Double-Blind, Placebo-Controlled Multi-Center Study Of [S,S]-Reboxetine In Patients With Postherpetic Neuralgia (PHN), Who Are Gabapentin Treatment Failures. [NCT00143442]Phase 2184 participants Interventional2003-12-31Completed
Phase 2, Randomized, Double-Blind, Parallel-Group, Four Week, Efficacy And Safety Trial Of [S,S]-Reboxetine (PNU-165442g) And Atomoxetine In Adults With Attention Deficit Hyperactivity Disorder. [NCT00562055]Phase 20 participants (Actual)Interventional2007-11-30Withdrawn(stopped due to This study was withdrawn due to business reasons.)
An Open-Label Extension Trial Assessing The Safety And Tolerability Of [S,S]-Reboxetine In Patients With Postherpetic Neuralgia (PHN). [NCT00353808]Phase 2112 participants (Actual)Interventional2006-07-31Terminated(stopped due to This study has been terminated early as the esreboxetine development program is being discontinued. There are no safety or efficacy concerns.)
A Phase 2b Long-Term, Randomized, Open-Label, Safety And Tolerability Trial Comparing [S,S]-Reboxetine (PNU-165442g) With Routine Care In Patients With Chronic Painful Diabetic Peripheral Neuropathy (DPN). [NCT00348894]Phase 2136 participants (Actual)Interventional2006-07-31Terminated(stopped due to - Study was terminated due to insufficient clinical efficacy observed in previous studies conducted in postherpetic neuralgia.)
[S,S]-Reboxetine Add-On Trial: A Randomized, Double-Blind, Placebo-Controlled, Multi-Center Trial Of [S,S]-Reboxetine In Patients With Postherpetic Neuralgia (PHN) Concomitantly Treated With Pregabalin. [NCT00334685]Phase 2136 participants (Actual)Interventional2006-08-22Terminated(stopped due to The Data Monitoring Committee terminated the study on the basis of futility (insufficient clinical response).)
Pharmacological Interaction Between Reboxetine and 3,4-Methylenedioxymethamphetamine (MDMA, Ecstasy): Pharmacological Effects and Pharmacokinetics [NCT00886886]Phase 116 participants (Actual)Interventional2009-04-30Completed
Measurement Of Urethral Function In Healthy Female Volunteers - Evaluation Of The Sensitivity of Urethral Reflectometry Compared To Urethral Pressure Profilometry, Using [S,S]-Reboxetine. [NCT00444548]12 participants (Actual)Interventional2007-05-31Completed
[S,S]-Reboxetine Dose-Range Finding Trial: A 16-Week, Randomized, Double-Blind, Placebo And An Active Comparator Controlled, Multi-Center Trial Of [S,S]-Reboxetine In Patients With Postherpetic Neuralgia (PHN) [NCT00288652]Phase 2280 participants Interventional2006-03-31Completed
Comparative Responses to 15 Different Antidepressants in Major Depressive Disorder - Results From a Long-term Nation-wide Population-based Study Emulating a Randomized Trial [NCT05952713]73,336 participants (Actual)Observational2022-10-01Completed
Phase 3 Reboxetine Treatment in Depressed Children and Adolescents an 8-Week, Open Study [NCT00426946]Phase 460 participants Interventional2005-01-31Recruiting
Augmentation of the Antidepressant Action of Sertraline With Triiodothyronine (T3)and Reboxetine: Clinical Efficacy, Adverse Effects and Predictors of Response. [NCT00421369]35 participants (Actual)Interventional2007-09-30Completed
An 8-Week, Randomized, Double-Blind, Placebo-Controlled, Multi-Centre Study of [S,S]-Reboxetine Administered Once Daily in Patients With Fibromyalgia [NCT00357825]Phase 2246 participants Interventional2006-08-31Completed
Efficacy of Hydroxyzine Versus Treatment as Usual for Panic Disorder: An Eight-Week, Open Label, Pilot, Randomized Controlled Trial. [NCT05737511]Phase 480 participants (Anticipated)Interventional2023-12-30Not yet recruiting
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
The Role of Dopaminergic and Noradrenergic Neurotransmission in Value- and Salience-based Decision-Making [NCT04371146]120 participants (Actual)Interventional2019-07-03Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT03881852 (1) [back to overview]Change From Baseline in the Weekly Average Total Number of Cataplexy Attacks

Change From Baseline in the Weekly Average Total Number of Cataplexy Attacks

Presented as LSmeans. A positive change is indicative of improvement. (NCT03881852)
Timeframe: 2 weeks

Interventionweekly cataplexy attacks (Least Squares Mean)
AXS-12 (Reboxetine)13.0
Placebo-0.28

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