Source: Health Products Regulatory Authority (ZA) Publisher: Dr. Reddys Laboratories (Pty) Ltd, The Place, Third Floor, 1 Sandton Drive, Sandton, 2196
A1.2 Psychoanaleptics
Atomoxetine is a selective inhibitor of the presynaptic norepinephrine transporter, without directly affecting the serotonin or dopamine transporters. Atomoxetine has minimal affinity for other noradrenergic receptors or for other neurotransmitter transporters or receptors.
The pharmacokinetics of atomoxetine in children and adolescents are similar to those in adults. The pharmacokinetics of atomoxetine have not been evaluated in children under the age of 6 years.
Atomoxetine is well absorbed after oral administration and reaches a mean maximal observed plasma concentration (Cmax) approximately 1 to 2 hours after dosing.
Atomoxetine can be administered with or without food.
Atomoxetine is widely distributed. Atomoxetine is extensively bound to plasma proteins, primarily albumin.
Atomoxetine undergoes biotransformation primarily through the cytochrome P450 2D6 (CYP2D6) enzymatic pathway.
4-hydroxyatomoxetine is the major oxidative metabolite formed, that is glucuronidated.
4-hydroxyatomoxetine is equipotent to atomoxetine but circulates in plasma at much lower concentrations. As 4-hydroxyatomoxetine is primarily formed by CYP2D6, in individuals that lack CYP2D6 activity, 4-hydroxyatomoxetine is still formed by several other cytochrome P450 enzymes, but at a slower rate.
The CYP2D6 pathway is not inhibited or induced by atomoxetine.
In extensive metabolisers the mean elimination half-life of atomoxetine after oral administration is 3,6 hours and in poor metabolisers it is 21 hours. Atomoxetine is excreted primarily as 4-hydroxyatomoxetine-O-glucuronide, mainly in the urine.
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