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Active ingredient: Atomoxetine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antidepressants
  • Central Nervous System Agents

Dosage Forms

  • Capsule

Brands / Synonyms

Strattera; Tomoxetina [Spanish]; Tomoxetine; Tomoxetine [Inn]; Tomoxetinum [Latin]

Indications

For the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD).

Pharmacology

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.

Absorption

Not Available

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

Not Available

Drug Interactions

Drug-Drug Interactions

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 atomoxetine alone.

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.

 

 

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