Brands, Medical Use, Clinical Data
- Central Nervous System Agents
Brands / Synonyms
Strattera; Tomoxetina [Spanish]; Tomoxetine; Tomoxetine [Inn]; Tomoxetinum [Latin]
For the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD).
Atomoxetine is an amphetamine used to treat ADD/ADHD in children and adults. Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity. It increases motor activity and mental alertness, and reduces drowsiness and a sense of fatigue, decreasing motor restlessness and improves one's ability to focus. Peripheral actions include elevation of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action. There is neither specific evidence which clearly establishes the mechanism whereby amphetamine produces mental and behavioral effects in children, nor conclusive evidence regarding how these effects relate to the condition of the central nervous system. Atomoxetine activates the brain stem arousal system and cortex to produce its stimulant effect.
Mechanism of Action
Amphetamines release stores of norepinephrine and dopamine from nerve endings by converting the respective molecular transporters into open channels. Amphetamines also releases stores of serotonin from synaptic vesicles. Like methylphenidate (Ritalin) amphetamines also prevent the monoamine transporters for dopamine and norepinephrine from recycling them (called reuptake inhibition) which leads to increased amounts of dopamine and norepinephrine in synaptic clefts. These combined effects rapidly increases the concentrations of the respective neurotransmitters in the synaptic cleft, which promotes nerve impulse transmission in neurons that have those receptors.
Biotrnasformation / Drug Metabolism
Albuterol ¾ STRATTERA should be administered with caution to patients
being treated with systemically-administered (oral or intravenous) albuterol (or other beta2 agonists)
because the action of albuterol on the cardiovascular system can be potentiated resulting in increases in heart rate
and blood pressure.
CYP2D6 inhibitors ¾ Atomoxetine is primarily metabolized by the CYP2D6
pathway to 4-hydroxyatomoxetine. In EMs, selective inhibitors of CYP2D6 increase atomoxetine steady-state plasma
concentrations to exposures similar to those observed in PMs. Dosage adjustment of STRATTERA may be necessary when
coadministered with CYP2D6 inhibitors, e.g., paroxetine, fluoxetine, and quinidine (see DOSAGE AND ADMINISTRATION). In EM individuals treated with paroxetine or fluoxetine, the
AUC of atomoxetine is approximately 6- to 8-fold and Css,max is about 3- to 4-fold greater than
In vitro studies suggest that coadministration of cytochrome P450 inhibitors to PMs will not increase the plasma
concentrations of atomoxetine.
Monoamine oxidase inhibitors ¾ See CONTRAINDICATIONS.
Pressor agents ¾ Because of possible effects on blood pressure, STRATTERA
should be used cautiously with pressor agents.