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QuickView for Atomoxetine (compound)

Name: atomoxetine
PubChem Compound ID: 11162189
Molecular formula: C17H22ClNO
Molecular weight: 293.808 g/mol
Name: atomoxetine
Name (isomeric): DB00289
Drug Type: small molecule
Tomoxetine; Tomoxetine [INN]; Tomoxetina [Spanish]; Tomoxetinum [Latin]
Brand: Strattera
Category: Antidepressants, Adrenergic Uptake Inhibitors, Central Nervous System Agents
CAS number: 82248-59-7
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.
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...
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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...
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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
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:
PhenelzinePossible severe adverse reaction with this combination
PerphenazineThe CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
CocaineCYP2D6 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.
QuinacrineThe CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
FluphenazineRisk of additive CNS depressant effects. Monitor for increased CNS depression during concomitant therapy.
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