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QuickView for Atomoxetine (compound)

Summary
General Info

PubChem

PubChem Compound 11162189

Name:	atomoxetine
PubChem Compound ID:	11162189
Molecular formula:	C₁₇H₂₂ClNO
Molecular weight:	293.808 g/mol

DrugBank

Identification

Name:	atomoxetine
Name (isomeric):	DB00289
Drug Type:	small molecule
Synonyms:	Tomoxetine; Tomoxetine [INN]; Tomoxetina [Spanish]; Tomoxetinum [Latin]
Brand:	Strattera
Category:	Antidepressants, Adrenergic Uptake Inhibitors, Central Nervous System Agents
CAS number:	82248-59-7

Pharmacology

Indication:	For the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) alone or in combination with behavioral treatment, as an adjunct to psychological, educational, social, and other remedial measures.
Pharmacology:	Atomoxetine is the first non-stimulant drug approved for the treatment of attention-deficit hyperactivity disorder (ADHD). Atomoxetine is classified as a norepinephrine reuptake inhibitor, and is approved for use in children, adolescents, and adults. However, its efficacy has not been studied in children under six years old. Its advantage over stim... show more » Atomoxetine is the first non-stimulant drug approved for the treatment of attention-deficit hyperactivity disorder (ADHD). Atomoxetine is classified as a norepinephrine reuptake inhibitor, and is approved for use in children, adolescents, and adults. However, its efficacy has not been studied in children under six years old. Its advantage over stimulants for the treatment of ADHD is that it has less abuse potential than stimulants, is not scheduled as a controlled substance and has proven in clinical trials to offer 24 hour coverage of symptoms associated with ADHD in adults and children. show less «
Mechanism of Action:	The precise mechanism by which atomoxetine produces its therapeutic effects in Attention-Deficit/Hyperactivity Disorder (ADHD) is unknown, but is thought to be related to selective inhibition of the pre-synaptic norepinephrine transporter, as determined through in-vitro studies. Atomoxetine appears to have minimal affinity for other noradrenergic r... show more » The precise mechanism by which atomoxetine produces its therapeutic effects in Attention-Deficit/Hyperactivity Disorder (ADHD) is unknown, but is thought to be related to selective inhibition of the pre-synaptic norepinephrine transporter, as determined through in-vitro studies. Atomoxetine appears to have minimal affinity for other noradrenergic receptors or for other neurotransmitter transporters or receptors. show less «
Absorption:	Atomoxetine is rapidly absorbed after oral administration, with absolute bioavailability of about 63% in EMs and 94% in PMs. Drugs that elevate gastric pH (magnesium hydroxide/aluminum hydroxide, omeprazole) have no effect on atomoxetine bioavailability. Absorption is minimally affected by food.
Protein binding:	At therapeutic concentrations, 98% of atomoxetine in plasma is bound to protein, primarily albumin.
Biotransformation:	Atomoxetine is primarily metabolized by the CYP2D6 pathway to 4-hydroxyatomoxetine. 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).
Half Life:	5 hours
Clearance:	0.35 L/hr/kg [after oral administration in adult extensive metabolizers] 0.03 L/hr/kg [administration of atomoxetine to poor metabolizers]
Toxicity:	The most commonly reported symptoms accompanying acute and chronic overdoses are somnolence, agitation, hyperactivity, abnormal behavior, and gastrointestinal symptoms.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

In the presence of food, the absorption rate is reduced, without the quantity absorbed being affected.

Take without regard to meals.

Drug interaction:

Phenelzine	Possible severe adverse reaction with this combination
Perphenazine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Cocaine	CYP2D6 Inhibitors (Strong) such as cocaine may increase the serum concentration of atomoxetine. Initiate atomoxetine at a reduced dose (patients up to 70kg: 0.5mg/kg/day; patients 70kg or more: 40mg/day) in patients receiving a strong CYP2D6 inhibitor. The dose should only be increased to usual doses if symptoms fail to improve after 4 weeks. Patients established on atomoxetine therapy may require dosage reductions and should be monitored for increased levels/adverse effects with initiation/dose increase of a strong CYP2D6 inhibitor.
Quinacrine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Fluphenazine	Risk of additive CNS depressant effects. Monitor for increased CNS depression during concomitant therapy.

Phenelzine	Possible severe adverse reaction with this combination
Perphenazine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Cocaine	CYP2D6 Inhibitors (Strong) such as cocaine may increase the serum concentration of atomoxetine. Initiate atomoxetine at a reduced dose (patients up to 70kg: 0.5mg/kg/day; patients 70kg or more: 40mg/day) in patients receiving a strong CYP2D6 inhibitor. The dose should only be increased to usual doses if symptoms fail to improve after 4 weeks. Patients established on atomoxetine therapy may require dosage reductions and should be monitored for increased levels/adverse effects with initiation/dose increase of a strong CYP2D6 inhibitor.
Quinacrine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Fluphenazine	Risk of additive CNS depressant effects. Monitor for increased CNS depression during concomitant therapy.
Fluoxetine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Tranylcypromine	The MAO inhibitor, Tranylcypromine, may increase the central neurotoxic effects of the Atomoxetine. These agents should not be administered within 14 days of each other.
Isocarboxazid	Possible severe adverse reaction with this combination
Quinine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Mibefradil	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Thioridazine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Rasagiline	Possible severe adverse reaction with this combination
Propoxyphene	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Ritonavir	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Haloperidol	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Paroxetine	The CYP2D6 inhibitor, paroxetine, may increase the effect and toxicity of atomoxetine.
Terbinafine	Terbinafine, a CYP2D6 inhibitor, may reduce the metabolism and clearance of Atomoxetine. Consider alternate therapy or monitor for therapeutic/adverse effects of Atomoxetine if Terbinafine is initiated, discontinued or dose changed.
Amiodarone	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Diphenhydramine	Diphenhydramine, a moderate CYP2D6 inhibitor, may increase the therapeutic and adverse effects of atomoxetine by decreasing its metabolism.
Chloroquine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Quinidine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Quinidine barbiturate	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Yohimbine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Triprolidine	The CNS depressants, Triprolidine and Atomoxetine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Vinorelbine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Lomustine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine

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Targets

Sodium-dependent noradrenaline transporter

Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals

UniProt ID:

P23975

Gene:

SLC6A2

Actions:

yes

References:

Biederman J, Heiligenstein JH, Faries DE, Galil N, Dittmann R, Emslie GJ, Kratochvil CJ, Laws HF, Schuh KJ: Efficacy of atomoxetine versus placebo in school-age girls with attention-deficit/hyperactivity disorder. Pediatrics. 2002 Dec;110(6):e75.
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Spencer T, Heiligenstein JH, Biederman J, Faries DE, Kratochvil CJ, Conners CK, Potter WZ: Results from 2 proof-of-concept, placebo-controlled studies of atomoxetine in children with attention-deficit/hyperactivity disorder. J Clin Psychiatry. 2002 Dec;63(12):1140-7.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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Sodium-dependent serotonin transporter

Enzymes

Cytochrome P450 2D6

Cytochrome P450 2C19

Cytochrome P450 3A4