Indications
Attention-Deficit/Hyperactivity Disorder (ADHD).
Action
Selectively inhibits the presynaptic transporter of norepinephrine.
Therapeutic Effects: Increased attention
span.
Pharmacokinetics
Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Protein Binding: 98%.
Metabolism and Excretion: Mostly metabolized
by the liver (CYP2D6 enzyme pathway). A small percentage
of the population are poor metabolizers and
will have higher blood levels withqeffects.
Half-life: 5 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
PO unknown 1–2 hr 12–24 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Concurrent
or within 2 wk therapy with MAO inhibitors; Angle-closure
glaucoma; Pheochromocytoma; Hypertension,
tachycardia, cardiovascular, or cerebrovascular disease.
Use Cautiously in: Pre-existing psychiatric illness;
Pedi: Mayqrisk of suicide attempt/ideation especially
during dose early treatment or dose adjustment; risk
may be greater in children or adolescents; Concurrent
albuterol or vasopressors (qrisk of adverse cardiovascular
reactions); OB: Use only if benefits outweigh risks
to fetus; Lactation, Pedi: Safety not established.
Adverse Reactions/Side Effects
CNS: SUICIDAL THOUGHTS, dizziness, fatigue, mood
swings, behavioral disturbances, hallucinations, hostility,
mania, thought disorder; Adults, insomnia. CV: hypertension,
orthostatic hypotension, QT interval prolongation,
syncope, tachycardia. GI: HEPATOTOXICITY,
dyspepsia, nausea, vomiting; Adults, dry mouth, constipation.
Derm:qsweating, rash, urticaria. GU:
Adults—dysmenorrhea, ejaculatory problems, erectile
dysfunction, libido changes, priapism, urinary hesitation,
urinary retention.Metab:pappetite, weight/
growth loss. MS: RHABDOMYOLYSIS. Neuro: Adults—
paresthesia. Misc: allergic reactions including ANGIONEUROTIC
EDEMA and ANAPHYLAXIS.
Interactions
Drug-Drug: Concurrent use with MAO inhibitors
may result in serious, potentially fatal reactions (do not
use within 2 wk of each other).qrisk of cardiovascular
effects with albuterol or vasopressors(use cautiously).
Drugs which inhibit the CYP2D6 enzyme
pathway (quinidine, fluoxetine, paroxetine) will
qblood levels and effects, doseprecommended.
Route/Dosage
PO (Children and adolescents 70 kg): 0.5 mg/kg/
day initially, may beqevery 3 days to a daily target dose
of 1.2 mg/kg, given as a single dose in the morning or
evenly divided doses in the morning and late afternoon/
early evening (not to exceed 1.4 mg/kg/day or 100 mg/
day whichever is less). If taking concurrent CYP2D6
inhibitor (quinidine, fluoxetine, paroxetine)—0.5
mg/kg/day initially, mayqif needed to 1.2 mg/kg/day
after 4 wk.
PO (Adults , adolescents, and children 70 kg):
40 mg/day initially, may beqevery 3 days to a daily target
dose of 80 mg/day given as a single dose in the
morning or evenly divided doses in the morning and
late afternoon/early evening; may be furtherqafter 2–
4 wk up to 100 mg/day. If taking concurrent CYP2D6
inhibitor (quinidine, fluoxetine, paroxetine)—40
mg/day initially, mayqif needed to 80 mg/day after 4
wk.
Hepatic Impairment
PO (Adults and Children): Moderate hepatic impairment
(Child-Pugh Class B)—pinitial and target
dose by 50%; Severe hepatic impairment (Child-
Pugh Class C)—pinitial and target dose to 25% of
normal.
Availability (generic available)
Capsules: 10 mg, 18 mg, 25 mg, 40 mg, 60 mg, 80
mg, 100 mg.
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