Trade Names:Strattera- Capsules 10 mg (as base)- Capsules 18 mg (as base)- Capsules 25 mg (as base)- Capsules 40 mg (as base)- Capsules 60 mg (as base)- Capsules 80 mg (as base)- Capsules 100 mg (as base)
Selective inhibition of the presynaptic norepinephrine transporter is suspected.
C max is reached approximately 1 to 2 h after dosing.
Vd is 0.85 L/kg (IV dose) and 98% is protein bound, primarily to albumin.
Primarily metabolized by CYP2D6; CYP2C19 and other CYP-450 enzymes are involved to a lesser extent. Major metabolite is 4-hydroxyatomoxetine, which is equipotent to atomoxetine but circulates at much lower concentrations.
Cl is approximately 0.35 L/h/kg and half-life is 5.2 h for extensive metabolizers. Cl is approximately 0.3 L/h/kg and half-life is 21.6 h for poor metabolizers. More than 80% is excreted in urine and less than 17% in feces (as metabolite). Less than 3% is excreted as unchanged atomoxetine.
Extensive metabolizers with end-stage renal disease had higher systemic exposure (about a 65% increase), but there was no difference when exposure was corrected for mg/kg dose.Hepatic Function Impairment
AUC is increased in extensive metabolizers with moderate or severe hepatic function impairment. Dosage adjustment is required.Gender
Pharmacokinetics are similar in men and women.Race
Does not affect atomoxetine pharmacokinetics, except poor metabolizing is more common in white patients.
Treatment of attention deficit hyperactivity disorder (ADHD).
Weight reduction in women with obesity.
Narrow-angle glaucoma; MAOIs or within 2 wk after discontinuing an MAOI; hypersensitivity to any component of the product.
PO Start with 40 mg/day and increase the dose after a minimum of 3 days to a target total daily dosage of approximately 80 mg. After 2 to 4 additional wk, the dosage may be increased to a max of 100 mg/day in patients who have not achieved an optimal response. In children more than 70 kg or adults receiving a strong CYP2D6 inhibitor (eg, fluoxetine), increase the 40 mg/day dosage to the target dosage of 80 mg/day if symptoms fail to improve after 4 wk and the initial dosage is well tolerated.Children (up to 70 kg)
PO Start with 0.5 mg/kg/day and increase the dosage after a minimum of 3 days to a target total dosage of approximately 1.2 mg/kg/day (max, 1.4 mg/kg or 100 mg/day, whichever is less). In children up to 70 kg receiving a strong CYP2D6 inhibitor (eg, fluoxetine), increase the 0.5 mg/kg/day dosage to the target dosage of 1.2 mg/kg/day only if symptoms fail to improve after 4 wk and the initial dosage is well tolerated.Hepatic Function Impairment
PO In patients with moderate hepatic function impairment (Child-Pugh class B), reduce initial and target doses to 50% of the normal dose; in patients with severe hepatic function impairment (Child-Pugh class C), reduce initial and target doses to 25% of normal.
Store at controlled room temperature (59° to 86°F).
Use with caution; the CV effects of albuterol may be potentiated.CYP2D6 inhibitors (eg, fluoxetine, paroxetine, quinidine)
The AUC and peak plasma level of atomoxetine may be increased.CYP3A4 substrates (eg, midazolam)
Plasma concentrations may be increased by atomoxetine; however, dosage adjustments are not recommended.MAOIs (eg, isocarboxazid)
Coadministration is contraindicated.Pressor agents (eg, dobutamine, dopamine)
Possible increased BP.
None well documented.
Hot flush (8%); palpitations (3%); QT prolongation, syncope (postmarketing).
Headache (19%); decreased appetite (16%); insomnia (15%); somnolence (11%); fatigue (9%); dizziness, irritability (6%); decreased libido (4%); anorexia, sinus headache, sleep disorder (3%); feeling jittery, mood swings, tremor (2%); seizures (postmarketing).
Sweating (4%); rash (2%).
Dry mouth, nausea (21%); abdominal pain (18%); vomiting (11%); constipation (9%); dyspepsia (4%).
Erectile dysfunction (9%); urinary hesitancy and/or urinary retention (7%); dysmenorrhea (6%); delayed ejaculation and/or ejaculation disorder, dysuria (3%); menstruation irregularities (2%); male pelvic pain, priapism (postmarketing).
Weight decrease (3%).
Chills, unexpected therapeutic response (3%).
Atomoxetine increased the risk of suicidal thinking in short-term studies in children and adolescents. When considering the use of atomoxetine, balance the risk with clinical need. Observe children or adolescents closely for suicidal thinking and behavior, clinical worsening, or unusual changes in behavior. Advise families and caregivers of the need for close observation and communication with the prescriber.
Monitor patients closely for suicidality (suicidal thinking and behavior), clinical worsening, or unusual changes in behavior. Monitor growth during treatment. Monitor pulse and BP following dose increases and periodically during therapy.ADHD symptoms
Assess ADHD symptoms before and periodically throughout therapy.
Category C .
Safety and efficacy not established in children younger than 6 yr of age.
Safety and efficacy have not been evaluated.
No dosage adjustments are needed in patients with renal insufficiency or end-stage renal disease.
Dosage adjustment is recommended in patients with moderate to severe hepatic insufficiency. Discontinue in patients with jaundice or laboratory evidence of liver injury; do not restart.
Aggressive behavior or hostility were observed more frequently among children and adolescents treated with atomoxetine compared with placebo.
Reactions, including angioneurotic edema, rash, and urticaria, can occur.
Use with caution in patients with ADHD and comorbid bipolar disorder because of possible induction of a mixed/manic episode in patients at risk for bipolar disorder.
Sudden death has been associated with atomoxetine treatment at usual doses in children and adolescents with structural cardiac abnormalities or other serious heart problems. Sudden death, stroke, and MI have been reported in adults taking atomoxetine at usual doses for ADHD. In addition, because therapy can increase BP and heart rate, use with caution in patients with hypertension, tachycardia, or CV or cerebrovascular disease.
Poor CYP2D6 metabolizers have a 10-fold higher AUC and 5-fold higher C max to a given dose of atomoxetine compared with extensive metabolizers. The higher plasma levels in the poor metabolizers lead to a higher rate of some adverse reactions.
Monitor growth during treatment; mean weight and growth changes have been reported to be less than those occurring with placebo administration.
Reports of new-onset and exacerbation of Raynaud phenomenon.
Painful and nonpainful penile erection lasting more than 4 h has been reported for adults and children receiving atomoxetine.
Treatment-emergent psychotic or manic symptoms in children and adolescents without a history of psychotic illness or mania can occur.
Rate of occurrence of urinary retention and hesitancy may be increased.
Abnormal behavior, agitation, GI symptoms, hyperactivity, mental changes including disorientation and hallucinations, QT prolongation, somnolence, sympathetic nervous system activation (eg, dry mouth, mydriasis, tachycardia).
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