Identification

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Name
Atomoxetine
Accession Number
DB00289  (APRD00614)
Type
Small Molecule
Groups
Approved
Description

Atomoxetine is a selective norepinephrine (NE) reuptake inhibitor used for the treatment of attention deficit hyperactivity disorder (ADHD). Also known as the marketed product Strattera, atomoxetine is used with other treatment modalities (psychological, educational, cognitive behaviour therapy, etc) to improve developmentally inappropriate symptoms associated with ADHD including distractibility, short attention span, hyperactivity, emotional lability, and impulsivity. Although the underlying pathophysiology that causes ADHD remains unclear, evidence suggests that dysregulation in noradrenergic and dopaminergic pathways plays a critical role in suboptimal executive functioning within prefrontal regions of the brain, which are involved in attention and memory 5. Atomoxetine has been shown to specifically increase NA and DA within the prefrontal cortex, but not in the nucleus accumbens (NA) or striatum 8. DA activation in the subcortical NA and striatum is associated with many stimulant-associated side effects and an increase in abuse potential, which is a limiting factor associated with the use of stimulant medications such as Methylphenidate, Dextroamphetamine, and Lisdexamfetamine 8. Use of non-stimulant medications such as atomoxetine is therefore thought to offer a clinical advantage over the use of traditional medications for the management of ADHD. More recently, positron emission tomography (PET) imaging studies in rhesus monkeys have shown that atomoxetine also binds to the serotonin transporter (SERT)9, and blocks the N-methyl-d-aspartate (NMDA) receptor 10, indicating a role for the glutamatergic system in the pathophysiology of ADHD.

Long-acting formulations of psychostimulants (such as Methylphenidate, Dextroamphetamine, and Lisdexamfetamine) are typically considered the most effective and first-line treatment for ADHD in adults and children as recommended by CADDRA (Canadian ADHD Resource Alliance) 16. However, these stimulant medications are limited by dose-related side effects and concerns of abuse. Many contain a blackbox warning stating that CNS stimulants, including methylphenidate-containing products and amphetamines, have a high potential for abuse and dependence. In particular, increased dopamine in key areas caused by these stimulant medications is associated with their reinforcing and addictive properties, and even amplifies the potency and reinforcing effects of other drugs of abuse such as amphetamines, making ADHD sufferers more susceptible to their addictive effects6. Concerns about abuse potential have spurred research into medications with fewer effects on DA and the use of non-stimulant ADHD medications including atomoxetine, Modafinil and Guanfacine. The non-stimulant norepinephrine/dopamine reuptake inhibitor Bupropion (commonly used for the treatment of depression and for smoking cessation) has also been shown to be effective in the treatment of ADHD 7.

Structure
Thumb
Synonyms
  • (-)-Tomoxetine
  • Atomoxetina
  • Atomoxetine
  • Tomoxetina
  • Tomoxetine
  • Tomoxetinum
Product Ingredients
IngredientUNIICASInChI Key
Atomoxetine hydrochloride57WVB6I2W082248-59-7LUCXVPAZUDVVBT-UNTBIKODSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AtomoxetineCapsule40 mgOralPro Doc Limitee2012-11-29Not applicableCanada
AtomoxetineCapsule25 mgOralSanis Health Inc2018-01-15Not applicableCanada
AtomoxetineCapsule100 mgOralSanis Health Inc2018-01-15Not applicableCanada
AtomoxetineCapsule10 mgOralSivem Pharmaceuticals Ulc2015-10-07Not applicableCanada
AtomoxetineCapsule25 mgOralPro Doc Limitee2012-11-29Not applicableCanada
AtomoxetineCapsule18 mgOralSanis Health Inc2018-01-15Not applicableCanada
AtomoxetineCapsule80 mgOralSanis Health Inc2018-01-15Not applicableCanada
AtomoxetineCapsule60 mgOralSivem Pharmaceuticals Ulc2015-10-07Not applicableCanada
AtomoxetineCapsule18 mgOralPro Doc Limitee2012-11-29Not applicableCanada
AtomoxetineCapsule10 mgOralSanis Health Inc2018-01-15Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-atomoxetineCapsule10 mgOralApotex Corporation2011-03-15Not applicableCanada
Apo-atomoxetineCapsule60 mgOralApotex Corporation2011-07-19Not applicableCanada
Apo-atomoxetineCapsule40 mgOralApotex Corporation2011-07-19Not applicableCanada
Apo-atomoxetineCapsule25 mgOralApotex Corporation2011-03-15Not applicableCanada
Apo-atomoxetineCapsule100 mgOralApotex Corporation2011-07-19Not applicableCanada
Apo-atomoxetineCapsule80 mgOralApotex Corporation2011-07-19Not applicableCanada
Apo-atomoxetineCapsule18 mgOralApotex Corporation2011-03-15Not applicableCanada
AtomoxetineCapsule40 mg/1OralTeva Pharmaceuticals USA, Inc.2017-05-30Not applicableUs
AtomoxetineCapsule60 mg/1OralCadila Healthcare Limited2017-12-06Not applicableUs
AtomoxetineCapsule40 mg/1OralMajor Pharmaceuticals2018-02-23Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
StratteraAtomoxetine hydrochloride (10 mg/1) + Atomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1) + Atomoxetine hydrochloride (60 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1) + Atomoxetine hydrochloride (60 mg/1) + Atomoxetine hydrochloride (80 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1) + Atomoxetine hydrochloride (60 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (10 mg/1) + Atomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1) + Atomoxetine hydrochloride (60 mg/1) + Atomoxetine hydrochloride (80 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (10 mg/1) + Atomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1) + Atomoxetine hydrochloride (60 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1) + Atomoxetine hydrochloride (60 mg/1) + Atomoxetine hydrochloride (80 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
StratteraAtomoxetine hydrochloride (10 mg/1) + Atomoxetine hydrochloride (18 mg/1) + Atomoxetine hydrochloride (25 mg/1) + Atomoxetine hydrochloride (40 mg/1)KitOralEli Lilly and Company2009-03-162009-11-03Us
International/Other Brands
Tomoxetin (Torrent Pharmaceuticals Ltd)
Categories
UNII
ASW034S0B8
CAS number
83015-26-3
Weight
Average: 255.3547
Monoisotopic: 255.162314299
Chemical Formula
C17H21NO
InChI Key
VHGCDTVCOLNTBX-QGZVFWFLSA-N
InChI
InChI=1S/C17H21NO/c1-14-8-6-7-11-16(14)19-17(12-13-18-2)15-9-4-3-5-10-15/h3-11,17-18H,12-13H2,1-2H3/t17-/m1/s1
IUPAC Name
methyl[(3R)-3-(2-methylphenoxy)-3-phenylpropyl]amine
SMILES
CNCC[C@@H](OC1=CC=CC=C1C)C1=CC=CC=C1

Pharmacology

Indication

Atomoxetine is indicated for the treatment of attention deficit hyperactivity disorder (ADHD) in children and adults.

Associated Conditions
Pharmacodynamics

Atomoxetine is a selective norepinephrine (NE) reuptake inhibitor used for the treatment of attention deficit hyperactivity disorder (ADHD). Atomoxetine has been shown to specifically increase NA and DA within the prefrontal cortex, which results in improved ADHD symptoms, but not in the nucleus accumbens or striatum 8,8. More recently, positron emission tomography (PET) imaging studies in rhesus monkeys have shown that atomoxetine also binds to the serotonin transporter (SERT) in addition to the norepinephrine transporter (NET) 9. Due to atomoxetine's noradrenergic activity, it also has effects on the cardiovascular system such as increased blood pressure and tachycardia 11.

Mechanism of action

Atomoxetine is known to be a potent and selective inhibitor of the norepinephrine transporter (NET)2, which prevents cellular reuptake of norepinephrine throughout the brain, which is thought to improve the symptoms of ADHD. More recently, positron emission tomography (PET) imaging studies in rhesus monkeys have shown that atomoxetine also binds to the serotonin transporter (SERT)9, and blocks the N-methyl-d-aspartate (NMDA) receptor 10, indicating a role for the glutamatergic system in the pathophysiology of ADHD.

TargetActionsOrganism
ASodium-dependent noradrenaline transporter
inhibitor
Humans
USodium-dependent serotonin transporter
binder
Humans
UNMDA receptor
blocker
Humans
UG protein-activated inward rectifier potassium channel 1
inhibitor
Humans
UKappa-type opioid receptor
partial agonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

The pharmacokinetic profile of atomoxetine is highly dependent on cytochrome P450 2D6 genetic polymorphisms of the individual 1. A large fraction of the population (up to 10% of Caucasians and 2% of people of African descent and 1% of Asians) are poor metabolizers (PMs) of CYP2D6 metabolized drugs. These individuals have reduced activity in this pathway resulting in 10-fold higher AUCs, 5-fold higher peak plasma concentrations, and slower elimination (plasma half-life of 21.6 hours) of atomoxetine compared with people with normal CYP2D6 activity.

Atomoxetine is rapidly absorbed after oral administration, with absolute bioavailability of about 63% in extensive metabolizers (EMs) and 94% in poor metabolizers (PMs). Mean maximal plasma concentrations (Cmax) are reached approximately 1 to 2 hours after dosing with a maximal concentration of 350 ng/ml with an AUC of 2 mcg.h/ml1.

Volume of distribution

The reported volume of distribution of oral atomoxetine was 1.6-2.6 L/kg. The steady-state volume of distribution of intravenous atomoxetine was approximately 0.85 L/kg.1

Protein binding

At therapeutic concentrations, 98.7% of plasma atomoxetine is bound to protein, with 97.5% of that being bound to albumin, followed by alpha-1-acid glycoprotein and immunoglobulin G1.

Metabolism

Atomoxetine undergoes biotransformation primarily through the cytochrome P450 2D6 (CYP2D6) enzymatic pathway. People with reduced activity in the CYP2D6 pathway (also known as poor metabolizers or PMs) have higher plasma concentrations of atomoxetine compared with people with normal activity (also known as extensive metabolizers, or EMs). For PMs, the AUC of atomoxetine at steady-state is approximately 10-fold higher and Cmax is about 5-fold greater than for EMs.

The major oxidative metabolite formed regardless of CYP2D6 status is 4-hydroxy-atomoxetine, which is rapidly glucuronidated. 4-Hydroxyatomoxetine is equipotent to atomoxetine as an inhibitor of the norepinephrine transporter, but circulates in plasma at much lower concentrations (1% of atomoxetine concentration in EMs and 0.1% of atomoxetine concentration in PMs).

In individuals that lack CYP2D6 activity, 4-hydroxyatomoxetine is still the primary metabolite, but is formed by several other cytochrome P450 enzymes and at a slower rate. Another minor metabolite, N-Desmethyl-atomoxetine is formed by CYP2C19 and other cytochrome P450 enzymes, but has much less pharmacological activity than atomoxetine and lower plasma concentrations (5% of atomoxetine concentration in EMs and 45% of atomoxetine concentration in PMs).

Route of elimination

Atomoxetine is excreted primarily as 4-hydroxyatomoxetine-O-glucuronide, mainly in the urine (greater than 80% of the dose) and to a lesser extent in the feces (less than 17% of the dose). Only a small fraction (less than 3%) of the atomoxetine dose is excreted as unchanged atomoxetine, indicating extensive biotransformation Label.

Half life

The reported half-life depends on the CYP2D6 genetic polymorphisms of the individual and can range from 3 to 5.6 hours.1

Clearance

The clearance rate of atomoxetine depends the CYP2D6 genetic polymorphisms of the individual and can range of 0.27-0.67 L.h/kg.1

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3(-;-)2549delAEffect Directly StudiedThe presence of this genotype in CYP2D6 may be associated with reduced metabolism of atomoxetine and more frequent occurrence of adverse events.Details
Cytochrome P450 2D6CYP2D6*4(A;A)A Allele, homozygoteEffect Directly StudiedThe presence of this genotype in CYP2D6 is associated with poor metabolism of atomoxetine and more frequent occurrence of adverse events.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole Gene DeletionEffect Directly StudiedThe presence of this genotype in CYP2D6 is associated with poor metabolism of atomoxetine and more frequent occurrence of adverse events.Details
Cytochrome P450 2D6CYP2D6*6(-;-) / (-;T)T deletion, homozygoteEffect Directly StudiedThe presence of this genotype in CYP2D6 is associated with poor metabolism of atomoxetine and more frequent occurrence of adverse events.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, increased side effects.Details
Cytochrome P450 2D6CYP2D6*3Not AvailableG alleleEffect Directly StudiedThe presence of this genotype in CYP2D6 may be associated with reduced metabolism of atomoxetine and more frequent occurrence of adverse events.Details
Cytochrome P450 2D6CYP2D6*4Not Available3877G>AEffect Directly StudiedThe presence of this genotype in CYP2D6 may be associated with reduced metabolism of atomoxetine and more frequent occurrence of adverse events.Details

Interactions

Drug Interactions
DrugInteraction
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hypertension can be increased when Atomoxetine is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Atomoxetine is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of hypertension can be increased when Atomoxetine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of hypertension can be increased when Atomoxetine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of hypertension can be increased when Atomoxetine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Atomoxetine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Atomoxetine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Atomoxetine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Atomoxetine.
AbacavirAtomoxetine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity
    Severity

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  • Evidence Level
    Evidence Level

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  • Action
    Evidence Level

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Food Interactions
  • In the presence of food, the absorption rate is reduced, without the quantity absorbed being affected.
  • Take without regard to meals.

References

Synthesis Reference
US20060211772
General References
  1. Yu G, Li GF, Markowitz JS: Atomoxetine: A Review of Its Pharmacokinetics and Pharmacogenomics Relative to Drug Disposition. J Child Adolesc Psychopharmacol. 2016 May;26(4):314-26. doi: 10.1089/cap.2015.0137. Epub 2016 Feb 9. [PubMed:26859445]
  2. Hutchison SL, Ghuman JK, Ghuman HS, Karpov I, Schuster JM: Efficacy of atomoxetine in the treatment of attention-deficit hyperactivity disorder in patients with common comorbidities in children, adolescents and adults: a review. Ther Adv Psychopharmacol. 2016 Oct;6(5):317-334. doi: 10.1177/2045125316647686. Epub 2016 May 20. [PubMed:27721971]
  3. Aman MG, Smith T, Arnold LE, Corbett-Dick P, Tumuluru R, Hollway JA, Hyman SL, Mendoza-Burcham M, Pan X, Mruzek DW, Lecavalier L, Levato L, Silverman LB, Handen B: A review of atomoxetine effects in young people with developmental disabilities. Res Dev Disabil. 2014 Jun;35(6):1412-24. doi: 10.1016/j.ridd.2014.03.006. Epub 2014 Apr 16. [PubMed:24732041]
  4. Kratochvil CJ, Heiligenstein JH, Dittmann R, Spencer TJ, Biederman J, Wernicke J, Newcorn JH, Casat C, Milton D, Michelson D: Atomoxetine and methylphenidate treatment in children with ADHD: a prospective, randomized, open-label trial. J Am Acad Child Adolesc Psychiatry. 2002 Jul;41(7):776-84. doi: 10.1097/00004583-200207000-00008. [PubMed:12108801]
  5. Del Campo N, Chamberlain SR, Sahakian BJ, Robbins TW: The roles of dopamine and noradrenaline in the pathophysiology and treatment of attention-deficit/hyperactivity disorder. Biol Psychiatry. 2011 Jun 15;69(12):e145-57. doi: 10.1016/j.biopsych.2011.02.036. Epub 2011 May 6. [PubMed:21550021]
  6. Marshall CA, Brodnik ZD, Mortensen OV, Reith MEA, Shumsky JS, Waterhouse BD, Espana RA, Kortagere S: Selective activation of Dopamine D3 receptors and norepinephrine transporter blockade enhances sustained attention. Neuropharmacology. 2019 Apr;148:178-188. doi: 10.1016/j.neuropharm.2019.01.003. Epub 2019 Jan 8. [PubMed:30633928]
  7. Verbeeck W, Bekkering GE, Van den Noortgate W, Kramers C: Bupropion for attention deficit hyperactivity disorder (ADHD) in adults. Cochrane Database Syst Rev. 2017 Oct 2;10:CD009504. doi: 10.1002/14651858.CD009504.pub2. [PubMed:28965364]
  8. Bymaster FP, Katner JS, Nelson DL, Hemrick-Luecke SK, Threlkeld PG, Heiligenstein JH, Morin SM, Gehlert DR, Perry KW: Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder. Neuropsychopharmacology. 2002 Nov;27(5):699-711. [PubMed:12431845]
  9. Ding YS, Naganawa M, Gallezot JD, Nabulsi N, Lin SF, Ropchan J, Weinzimmer D, McCarthy TJ, Carson RE, Huang Y, Laruelle M: Clinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD. Neuroimage. 2014 Feb 1;86:164-71. doi: 10.1016/j.neuroimage.2013.08.001. Epub 2013 Aug 9. [PubMed:23933039]
  10. Ludolph AG, Udvardi PT, Schaz U, Henes C, Adolph O, Weigt HU, Fegert JM, Boeckers TM, Fohr KJ: Atomoxetine acts as an NMDA receptor blocker in clinically relevant concentrations. Br J Pharmacol. 2010 May;160(2):283-91. doi: 10.1111/j.1476-5381.2010.00707.x. [PubMed:20423340]
  11. Coleman J., Cox A. and Cowley N. (2011). Side Effects of Drugs Annual. Elsevier.
  12. Waller D., and Sampson A. (2018). Medical Pharmacology and Therapeutics (5th ed.). Elsevier.
  13. Kolevzon A. (2013). The neuroscience of autism spectrum disorders. Elsevier.
  14. FDA approvals [Link]
  15. NIH [Link]
  16. CADDRA - Canadian ADHD Practice Guidelines [Link]
External Links
Human Metabolome Database
HMDB0014434
KEGG Drug
D07473
PubChem Compound
54841
PubChem Substance
46506160
ChemSpider
49516
BindingDB
50366567
ChEBI
127342
ChEMBL
CHEMBL641
Therapeutic Targets Database
DAP000721
PharmGKB
PA134688071
Wikipedia
Atomoxetine
ATC Codes
N06BA09 — Atomoxetine
AHFS Codes
  • 28:92.00 — Miscellaneous Central Nervous System Agents
FDA label
Download (363 KB)
MSDS
Download (108 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
0RecruitingTreatmentParkinson's Disease, Idiopathic1
1CompletedNot AvailableAutonomic Failure / Idiopathic orthostatic hypotension1
1CompletedBasic ScienceChanges in Striatal [11C]ORM-13070 Binding1
1CompletedBasic ScienceDependence, Cocaine1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
1CompletedTreatmentCocaine-Related Disorders1
1CompletedTreatmentContinuous Methamphetamine Dependence / Methamphetamine Dependence in Remission1
1RecruitingTreatmentOrthostatic Intolerance1
1TerminatedBasic ScienceAlcohol Craving / Emotional Instability1
1TerminatedBasic ScienceAlcohol Sensitivity / Alcohol-induced Cue-craving1
1TerminatedTreatmentMethamphetamine Abuse / Methamphetamine Dependence1
1, 2Active Not RecruitingTreatmentChronic Orthostatic Intolerance / Tachycardia1
1, 2CompletedBasic ScienceAttention Deficit Disorder With Hyperactivity (ADHD)1
1, 2CompletedTreatmentMethamphetamine Dependence1
1, 2CompletedTreatmentObstructive Sleep Apnea (OSA)1
1, 2CompletedTreatmentSchizophrenic Disorders1
1, 2CompletedTreatmentStress1
1, 2CompletedTreatmentStress, Physiological1
1, 2Not Yet RecruitingTreatmentSleep Apnea Syndrome1
1, 2SuspendedTreatmentNicotine Dependence1
2CompletedBasic ScienceMild Cognitive Impairment (MCI)1
2CompletedTreatmentAdult Attention Deficit Hyperactivity Disorder (ADHD)1
2CompletedTreatmentAtomoxetine Hydrochloride / Placebos1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)3
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Attention-Deficit/Hyperactivity Disorder1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Deficient Emotional Self-Regulation (DESR)1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Substance Use Disorder (SUD)1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity / Cocaine-Related Disorders1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity / Marijuana Abuse2
2CompletedTreatmentAttention-Deficit/Hyperactivity Disorder1
2CompletedTreatmentCannabis Dependence1
2CompletedTreatmentChorea / Huntington's Disease (HD)1
2CompletedTreatmentCognition / Schizophrenic Disorders / Smoking1
2CompletedTreatmentCognitive Impairments / Parkinson's Disease (PD)1
2CompletedTreatmentDisseminated Sclerosis / Memory Disorders1
2CompletedTreatmentOpiate Dependence / Stimulant Dependence1
2CompletedTreatmentSubstance Abuse1
2CompletedTreatmentSyncope, Vasovagal2
2RecruitingTreatmentNeurogenic Orthostatic Hypotension1
2TerminatedTreatmentCognition Disorders / Memory Disorders / Schizophrenic Disorders1
2WithdrawnTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
2, 3CompletedTreatmentAlzheimer's Disease (AD)1
2, 3CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
2, 3CompletedTreatmentGeneralized Social Phobia1
3Active Not RecruitingTreatmentAttention Deficit Disorder With Hyperactivity1
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity3
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)18
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Oppositional Defiant Disorder2
3CompletedTreatmentAttention-Deficit/Hyperactivity Disorder1
3CompletedTreatmentAutism, Early Infantile1
3CompletedTreatmentFreezing of Gait / Parkinson's Disease (PD)1
3Enrolling by InvitationTreatmentAutonomic Nervous System Diseases / Dopamine Beta-Hydroxylase Deficiency / Idiopathic orthostatic hypotension / Orthostatic Intolerance1
3Unknown StatusTreatmentAttention Deficit Disorder (ADD) / Attention Deficit Disorder With Hyperactivity (ADHD) / Fetal Alcohol Syndrome (FAS)2
3WithdrawnTreatmentCognitive Late Effects / Malignancies1
4CompletedNot AvailableAttention Deficit Disorder With Hyperactivity (ADHD)1
4CompletedNot AvailableBinge Eating Disorder (BED)1
4CompletedNot AvailableInjuries, Whiplash1
4CompletedDiagnosticAttention Deficit Disorder With Hyperactivity (ADHD)1
4CompletedHealth Services ResearchAttention Deficit Disorder With Hyperactivity (ADHD)1
4CompletedTreatmentADHD NOS2
4CompletedTreatmentAsperger's Disorder / Attention Deficit Disorder With Hyperactivity (ADHD) / Autism, Early Infantile / Pervasive Development Disorder1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity3
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)17
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Comorbid Alcohol Abuse1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Comorbid Social Anxiety Disorder1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Dyslexia2
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Oppositional Defiant Disorder1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Post Traumatic Stress Disorder (PTSD)1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Reading Disability1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Reading Disorder1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Sleeplessness1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity / Autistic Disorder1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity / Substance-Related Disorders1
4CompletedTreatmentAttention-Deficit/Hyperactivity Disorder2
4CompletedTreatmentAttention-Deficit/Hyperactivity Disorder / Comorbid Dyslexia1
4CompletedTreatmentCognition in Schizophrenia1
4CompletedTreatmentDepressive Disorders / Parkinson's Disease (PD)1
4CompletedTreatmentDepressive Symptoms1
4CompletedTreatmentExecutive Dysfunction1
4CompletedTreatmentNeurogenic Orthostatic Hypotension1
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
4CompletedTreatmentSchizophrenic Disorders1
4Not Yet RecruitingBasic ScienceAttention Deficit Disorder With Hyperactivity (ADHD)1
4RecruitingTreatmentAttention-Deficit/Hyperactivity Disorder1
4TerminatedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)2
4TerminatedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Cannabis Abuse1
4Unknown StatusNot AvailableAttention Deficit Disorder (ADD) / Attention Deficit Disorders With Hyperactivity / Attention Deficit/Hyperactivity Disorder1
4Unknown StatusBasic ScienceAttention Deficit Disorder With Hyperactivity (ADHD)1
4Unknown StatusTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Sleeplessness1
4Unknown StatusTreatmentParkinson's Disease (PD)1
4WithdrawnTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Substance Use Disorder (SUD)1
Not AvailableActive Not RecruitingTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)2
Not AvailableCompletedNot AvailableAnorexia Nervosa (AN) / Attention Deficit Disorder With Hyperactivity (ADHD) / Depression1
Not AvailableCompletedNot AvailableAttention Deficit Disorder With Hyperactivity (ADHD)1
Not AvailableCompletedNot AvailableAttention Deficit Disorder With Hyperactivity (ADHD) / Cerebrovascular Accidents / Transient Ischaemic Attack (TIA)1
Not AvailableCompletedTreatmentAddictions1
Not AvailableCompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)2
Not AvailableCompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Substance Abuse1
Not AvailableCompletedTreatmentCognitive Impairments / Menopause1
Not AvailableCompletedTreatmentParkinson's Disease (PD)1
Not AvailableCompletedTreatmentSchizophrenic Disorders1
Not AvailableCompletedTreatmentTraumatic Brain Injury (TBI)1
Not AvailableEnrolling by InvitationNot AvailableAttention Deficit Disorder With Hyperactivity (ADHD)1
Not AvailableNot Yet RecruitingTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
Not AvailableRecruitingNot AvailableAttention Deficit Disorder With Hyperactivity1
Not AvailableRecruitingNot AvailableAttention Deficit Disorder With Hyperactivity (ADHD)2
Not AvailableRecruitingNot AvailableObesity, Morbid1
Not AvailableRecruitingTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
Not AvailableTerminatedTreatmentDependence, Cocaine / Opiate Dependence1

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
Packagers
  • Atlantic Biologicals Corporation
  • Cardinal Health
  • Eli Lilly & Co.
  • Lake Erie Medical and Surgical Supply
  • Lilly Del Caribe Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Pharmacy Service Center
  • Physicians Total Care Inc.
  • Remedy Repack
Dosage forms
FormRouteStrength
CapsuleOral10 mg/1
CapsuleOral100 mg/1
CapsuleOral18 mg/1
CapsuleOral40 mg/1
CapsuleOral60 mg/1
CapsuleOral80 mg/1
CapsuleOral10 mg
CapsuleOral100 mg
CapsuleOral18 mg
CapsuleOral25 mg
CapsuleOral25 mg/1
CapsuleOral40 mg
CapsuleOral60 mg
CapsuleOral80 mg
KitOral
Prices
Unit descriptionCostUnit
Strattera 80 mg capsule6.94USD capsule
Strattera 100 mg capsule6.83USD capsule
Strattera 40 mg capsule6.43USD capsule
Strattera 60 mg capsule6.43USD capsule
Strattera 18 mg capsule6.03USD capsule
Strattera 25 mg capsule5.85USD capsule
Strattera 10 mg capsule5.84USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2209735No2002-10-012016-01-04Canada
US5658590Yes1997-08-192017-05-26Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)161-165 ºC'MSDS'
boiling point (°C)64-65 ºC at 0.760 mmHg'MSDS'
water solubility27.8 mg/mLYu G., Li G. and Markowitz J. 2016. J Child Adolesc Psychopharmacol.
logP0.676'MSDS'
pKa10.13Atomoxetine. Eli Lilly product monograph.
Predicted Properties
PropertyValueSource
Water Solubility0.0039 mg/mLALOGPS
logP3.95ALOGPS
logP3.81ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)9.8ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area21.26 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity79.44 m3·mol-1ChemAxon
Polarizability29.79 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.964
Caco-2 permeable+0.852
P-glycoprotein substrateSubstrate0.6133
P-glycoprotein inhibitor IInhibitor0.7771
P-glycoprotein inhibitor IINon-inhibitor0.8003
Renal organic cation transporterInhibitor0.5929
CYP450 2C9 substrateNon-substrate0.7443
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.6216
CYP450 1A2 substrateInhibitor0.9324
CYP450 2C9 inhibitorNon-inhibitor0.957
CYP450 2D6 inhibitorInhibitor0.9037
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8122
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7371
Ames testNon AMES toxic0.7738
CarcinogenicityNon-carcinogens0.8493
BiodegradationNot ready biodegradable0.8013
Rat acute toxicity2.5166 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7132
hERG inhibition (predictor II)Inhibitor0.7974
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-0900000000-456e1257123470a131c2
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0190000000-0f4cf059747adb026b96
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-ecaeebd63dc195659e57
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-0900000000-6da1a9a3edfed770c2cd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00xs-0900000000-d71f5b857319380ce595
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01bc-2900000000-37eb3191934e545cc338
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014l-6900000000-6be893f7d4702639eac2
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0190000000-c2030f3f981d83eacf57
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0190000000-3c27da7fa8c958a76be1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-0900000000-133c9cb2f2383aa0fe8a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00r5-1900000000-b68a2013855cb02e4512
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01bd-1900000000-c4fd6863785e44cc724e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014l-3900000000-4529fcb6c89f3acafac9
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-0900000000-06348bdc8d24fed52e75
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0690000000-494128ae0f3b90b415b3

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenol ethers
Sub Class
Not Available
Direct Parent
Phenol ethers
Alternative Parents
Phenoxy compounds / Toluenes / Aralkylamines / Alkyl aryl ethers / Dialkylamines / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Phenoxy compound / Phenol ether / Alkyl aryl ether / Toluene / Aralkylamine / Monocyclic benzene moiety / Secondary aliphatic amine / Ether / Secondary amine / Organooxygen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
aromatic ether, secondary amino compound, toluenes (CHEBI:127342)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da
References
  1. Michelson D, Adler L, Spencer T, Reimherr FW, West SA, Allen AJ, Kelsey D, Wernicke J, Dietrich A, Milton D: Atomoxetine in adults with ADHD: two randomized, placebo-controlled studies. Biol Psychiatry. 2003 Jan 15;53(2):112-20. [PubMed:12547466]
  2. Wernicke JF, Faries D, Girod D, Brown J, Gao H, Kelsey D, Quintana H, Lipetz R, Michelson D, Heiligenstein J: Cardiovascular effects of atomoxetine in children, adolescents, and adults. Drug Saf. 2003;26(10):729-40. [PubMed:12862507]
  3. Wernicke JF, Adler L, Spencer T, West SA, Allen AJ, Heiligenstein J, Milton D, Ruff D, Brown WJ, Kelsey D, Michelson D: Changes in symptoms and adverse events after discontinuation of atomoxetine in children and adults with attention deficit/hyperactivity disorder: a prospective, placebo-controlled assessment. J Clin Psychopharmacol. 2004 Feb;24(1):30-5. [PubMed:14709944]
  4. Garnock-Jones KP, Keating GM: Atomoxetine: a review of its use in attention-deficit hyperactivity disorder in children and adolescents. Paediatr Drugs. 2009;11(3):203-26. doi: 10.2165/00148581-200911030-00005. [PubMed:19445548]
  5. Kaplan S, Heiligenstein J, West S, Busner J, Harder D, Dittmann R, Casat C, Wernicke JF: Efficacy and safety of atomoxetine in childhood attention-deficit/hyperactivity disorder with comorbid oppositional defiant disorder. J Atten Disord. 2004 Oct;8(2):45-52. [PubMed:15801334]
  6. Purper-Ouakil D, Fourneret P, Wohl M, Reneric JP: [Atomoxetine: a new treatment for Attention Deficit/Hyperactivity Disorder (ADHD) in children and adolescents]. Encephale. 2005 May-Jun;31(3):337-48. [PubMed:16142049]
  7. Gaillez C, Sorbara F, Perrin E: [Atomoxetine (Strattera), an alternative in the treatment of attention-deficit/hyperactivity disorder (ADHD) in children]. Encephale. 2007 Sep;33(4 Pt 1):621-8. [PubMed:18033153]
  8. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
  9. Yu G, Li GF, Markowitz JS: Atomoxetine: A Review of Its Pharmacokinetics and Pharmacogenomics Relative to Drug Disposition. J Child Adolesc Psychopharmacol. 2016 May;26(4):314-26. doi: 10.1089/cap.2015.0137. Epub 2016 Feb 9. [PubMed:26859445]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin:sodium symporter activity
Specific Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
Molecular Weight
70324.165 Da
References
  1. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
  2. Yu G, Li GF, Markowitz JS: Atomoxetine: A Review of Its Pharmacokinetics and Pharmacogenomics Relative to Drug Disposition. J Child Adolesc Psychopharmacol. 2016 May;26(4):314-26. doi: 10.1089/cap.2015.0137. Epub 2016 Feb 9. [PubMed:26859445]
  3. Ding YS, Naganawa M, Gallezot JD, Nabulsi N, Lin SF, Ropchan J, Weinzimmer D, McCarthy TJ, Carson RE, Huang Y, Laruelle M: Clinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD. Neuroimage. 2014 Feb 1;86:164-71. doi: 10.1016/j.neuroimage.2013.08.001. Epub 2013 Aug 9. [PubMed:23933039]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Blocker
General Function
Voltage-gated cation channel activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...

Components:
References
  1. Ludolph AG, Udvardi PT, Schaz U, Henes C, Adolph O, Weigt HU, Fegert JM, Boeckers TM, Fohr KJ: Atomoxetine acts as an NMDA receptor blocker in clinically relevant concentrations. Br J Pharmacol. 2010 May;160(2):283-91. doi: 10.1111/j.1476-5381.2010.00707.x. [PubMed:20423340]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
G-protein activated inward rectifier potassium channel activity
Specific Function
This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their...
Gene Name
KCNJ3
Uniprot ID
P48549
Uniprot Name
G protein-activated inward rectifier potassium channel 1
Molecular Weight
56602.84 Da
References
  1. Kobayashi T, Washiyama K, Ikeda K: Inhibition of G-protein-activated inwardly rectifying K+ channels by the selective norepinephrine reuptake inhibitors atomoxetine and reboxetine. Neuropsychopharmacology. 2010 Jun;35(7):1560-9. doi: 10.1038/npp.2010.27. Epub 2010 Mar 10. [PubMed:20393461]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. Creighton CJ, Ramabadran K, Ciccone PE, Liu J, Orsini MJ, Reitz AB: Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect. Bioorg Med Chem Lett. 2004 Aug 2;14(15):4083-5. doi: 10.1016/j.bmcl.2004.05.018. [PubMed:15225731]

Enzymes

Details
1. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Purper-Ouakil D, Fourneret P, Wohl M, Reneric JP: [Atomoxetine: a new treatment for Attention Deficit/Hyperactivity Disorder (ADHD) in children and adolescents]. Encephale. 2005 May-Jun;31(3):337-48. [PubMed:16142049]
  2. Garnock-Jones KP, Keating GM: Atomoxetine: a review of its use in attention-deficit hyperactivity disorder in children and adolescents. Paediatr Drugs. 2009;11(3):203-26. doi: 10.2165/00148581-200911030-00005. [PubMed:19445548]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Sauer JM, Long AJ, Ring B, Gillespie JS, Sanburn NP, DeSante KA, Petullo D, VandenBranden MR, Jensen CB, Wrighton SA, Smith BP, Read HA, Witcher JW: Atomoxetine hydrochloride: clinical drug-drug interaction prediction and outcome. J Pharmacol Exp Ther. 2004 Feb;308(2):410-8. doi: 10.1124/jpet.103.058727. Epub 2003 Nov 10. [PubMed:14610241]
  5. Yu G, Li GF, Markowitz JS: Atomoxetine: A Review of Its Pharmacokinetics and Pharmacogenomics Relative to Drug Disposition. J Child Adolesc Psychopharmacol. 2016 May;26(4):314-26. doi: 10.1089/cap.2015.0137. Epub 2016 Feb 9. [PubMed:26859445]
  6. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Yu G, Li GF, Markowitz JS: Atomoxetine: A Review of Its Pharmacokinetics and Pharmacogenomics Relative to Drug Disposition. J Child Adolesc Psychopharmacol. 2016 May;26(4):314-26. doi: 10.1089/cap.2015.0137. Epub 2016 Feb 9. [PubMed:26859445]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Aman MG, Smith T, Arnold LE, Corbett-Dick P, Tumuluru R, Hollway JA, Hyman SL, Mendoza-Burcham M, Pan X, Mruzek DW, Lecavalier L, Levato L, Silverman LB, Handen B: A review of atomoxetine effects in young people with developmental disabilities. Res Dev Disabil. 2014 Jun;35(6):1412-24. doi: 10.1016/j.ridd.2014.03.006. Epub 2014 Apr 16. [PubMed:24732041]
  2. Hutchison SL, Ghuman JK, Ghuman HS, Karpov I, Schuster JM: Efficacy of atomoxetine in the treatment of attention-deficit hyperactivity disorder in patients with common comorbidities in children, adolescents and adults: a review. Ther Adv Psychopharmacol. 2016 Oct;6(5):317-334. doi: 10.1177/2045125316647686. Epub 2016 May 20. [PubMed:27721971]
Kind
Protein group
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...

Components:
References
  1. Hutchison SL, Ghuman JK, Ghuman HS, Karpov I, Schuster JM: Efficacy of atomoxetine in the treatment of attention-deficit hyperactivity disorder in patients with common comorbidities in children, adolescents and adults: a review. Ther Adv Psychopharmacol. 2016 Oct;6(5):317-334. doi: 10.1177/2045125316647686. Epub 2016 May 20. [PubMed:27721971]
  2. Aman MG, Smith T, Arnold LE, Corbett-Dick P, Tumuluru R, Hollway JA, Hyman SL, Mendoza-Burcham M, Pan X, Mruzek DW, Lecavalier L, Levato L, Silverman LB, Handen B: A review of atomoxetine effects in young people with developmental disabilities. Res Dev Disabil. 2014 Jun;35(6):1412-24. doi: 10.1016/j.ridd.2014.03.006. Epub 2014 Apr 16. [PubMed:24732041]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Receptor signaling protein activity
Specific Function
High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
Gene Name
FCGR1A
Uniprot ID
P12314
Uniprot Name
High affinity immunoglobulin gamma Fc receptor I
Molecular Weight
42631.525 Da
References
  1. Hutchison SL, Ghuman JK, Ghuman HS, Karpov I, Schuster JM: Efficacy of atomoxetine in the treatment of attention-deficit hyperactivity disorder in patients with common comorbidities in children, adolescents and adults: a review. Ther Adv Psychopharmacol. 2016 Oct;6(5):317-334. doi: 10.1177/2045125316647686. Epub 2016 May 20. [PubMed:27721971]
  2. Aman MG, Smith T, Arnold LE, Corbett-Dick P, Tumuluru R, Hollway JA, Hyman SL, Mendoza-Burcham M, Pan X, Mruzek DW, Lecavalier L, Levato L, Silverman LB, Handen B: A review of atomoxetine effects in young people with developmental disabilities. Res Dev Disabil. 2014 Jun;35(6):1412-24. doi: 10.1016/j.ridd.2014.03.006. Epub 2014 Apr 16. [PubMed:24732041]

Drug created on June 13, 2005 07:24 / Updated on May 20, 2019 14:46