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(zye loot' on)


Pregnancy Category C

Drug classes
Leukotriene formation inhibitor

Therapeutic actions
Selectively and competitively blocks the receptor that inhibits leukotriene formation, thus
blocking many of the signs and symptoms of asthma (neutrophil and eosinophil
migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary
permeability, and smooth muscle contraction). These actions contribute to inflammation,
edema, mucus secretion and bronchoconstriction caused by cold air challenge in patients
with asthma.

• Prophylaxis and long-term treatment of bronchial asthma in adults and children >
12 yr

Contraindications and cautions

• Contraindicated with hypersensitivity to zileuton or any of its components; acute
asthma attacks; status asthmaticus; pregnancy and lactation, severe hepatic
• Use cautiously with hepatic impairment.

Available forms
Tablets—600 mg

600 mg PO qid for a total of 2,400 mg/day.
Use caution, contraindicated if liver enzymes > 3 times normal.

Route Onset Peak
Oral Rapid 1.7 hr

Metabolism: Hepatic; T1/2: 2.5 hr

Distribution: Crosses placenta; enters breast milk
Excretion: Metabolism

Adverse effects
• CNS: Headache, dizziness, myalgia
• GI: Nausea, diarrhea, abdominal pain, vomiting, elevation of liver enzymes
• Other: Generalized pain, fever, myalgia

• Increased effects of propranolol, theophylline, warfarin; monitor patient and
decrease dose as appropriate
• Bioavailability decreased markedly by the presence of food; administer at least 1
hr before or 2 hr after meals

Nursing considerations
• History: Hypersensitivity to zileuton; impaired hepatic function; lactation;
pregnancy; acute asthma or bronchospasm
• Physical: T; orientation, reflexes; R, adventitious sounds; GI evaluation; liver
function tests

• Obtain baseline hepatic function tests before beginning therapy; monitor liver
enzymes on a regular basis during therapy; discontinue drug and consult
prescriber if enzymes rise more than three times normal.
• Administer without regard to food.
• Ensure that drug is taken continually for optimal effect.
• Do not administer for acute asthma attack or acute bronchospasm.

Teaching points
• Take this drug regularly as prescribed; do not stop taking this drug during
symptom-free periods; do not stop taking this drug without consulting your health
care provider. Continue taking any other antasthmatics that have been prescribed
for you.
• Do not take this drug for an acute asthma attack or acute bronchospasm; this drug
is not a bronchodilator; routine emergency procedures should be followed during
acute attacks.
• Avoid the use of over-the-counter drugs while you are using this medication;
many of them contain products that can interfere with or cause serious side effects
when used with this drug. If you feel that you need one of these products, consult
your nurse or physician.
• These side effects may occur: Dizziness (use caution when driving or performing
activities that require alertness); nausea, vomiting (eat frequent small meals; take
drug with food); headache (analgesics may be helpful).
• Report fever, acute asthma attacks, flulike symptoms, lethargy, pruritus, changes
in color of urine or stool.

Adverse effects in Italic are most common; those in Bold are life-threatening.