BUDESONIDE

BUDESONIDE (bu-des'o-nide) Entocort EC, Pulmicort Flexhaler, Rhinocort, Rhinocort Aqua, Rhinocort Turbuhaler Classifications: antiinflammatory; adrenal corticosteroid; glucocorticoid; Therapeutic: antiinflammatory; adrenal corticosteroid Prototype: Hydrocortisone Pregnancy Category: B for inhaled; C for oral

Availability

32 mcg/inhalation; 3 mg capsule

Action

Has potent glucocorticoid activity. Its antiinflammatory action on nasal mucosa is thought to be a result of decreased IgE synthesis and decreased arachidonic acid metabolism.

Therapeutic Effect

Glucocorticoids have a wide range of inhibitory activities against multiple cell types (e.g., neutrophils, macrophages) and mediators (e.g., histamine, cytokines) involved in allergic and nonallergic/irritant-mediated inflammation.

Uses

Treatment of allergic and perennial rhinitis, maintain remission in mild to moderate Crohn's disease; prophylaxis for asthma.

Contraindications

Hypersensitivity to budesonide, status asthmaticus, acute bronchospasms; peptic ulcer disease; pregnancy (category C for oral; category B for inhaled), lactation.

Cautious Use

Concomitant administration of systemic oral steroids; active or quiescent tuberculosis; infections of respiratory tract; in sun-treated fungal, bacterial, or systemic viral infections or ocular herpes simplex; recent nasal septal ulcers; recurrent epistaxis; nasal surgery or trauma; psychosis; myasthenia gravis; diabetes mellitus; seizure disorders.

Route & Dosage

Crohn's Disease Adult: PO 9 mg once/d in a.m. for up to 8 wk, may taper to 6 mg q.d. for 2 wk prior to discontinuing. May repeat 8-wk course for recurring episodes of active Crohn's disease. Asthma Prophylaxis, Rhinitis See Appendix A-3.

Administration

Oral

• Ensure that capsules are swallowed whole and not chewed.
• Give only in the morning.
• Patients with moderate to severe liver disease should be monitored for increased signs and/or symptoms of hypercorticism. Reducing the dose of Entocort EC capsules should be considered in these patients.
• Store at 25° C (77° F); excursions permitted to 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

Body as a Whole: Arthralgia, fatigue, fever, hyperkinesis, myalgia, asthenia, paresthesia, tremor. CNS: Dizziness, emotional lability, facial edema, nervousness, headache, agitation, confusion, insomnia, drowsiness. CV: Chest pain, hypertension, palpitations, sinus tachycardia. GI: Abdominal pain, dyspepsia, gastroenteritis, oral candidiasis, xerostomia, diarrhea, nausea, vomiting, cramps. Hematologic: Epistaxis. Metabolic: Hypokalemia, weight gain. Respiratory: Bronchospasms, infections, cough, rhinitis, sinusitis, dyspnea, hoarseness, wheezing. Skin: Eczema, pruritus, purpura, rash, alopecia. Special Senses: Contact dermatitis, reduced sense of smell, nasal pain. Urogenital: Intermenstrual bleeding, dysuria.

Interactions

Drug: Ketoconazole may increase oral budesonide concentrations and toxicity; toxicity may also occur with anastrozole (high doses only), clarithromycin, cyclosporine, danazol, delavirdine, diltiazem, erythromycin, fluconazole, fluoxetine, fluvoxamine, indinavir, isoniazid, INH, itraconazole, mibefradil, nefazodone, nelfinavir, nicardipine, norfloxacin, oxiconazole, quinidine, quinine, ritonavir, saquinavir, troleandomycin, verapamil, and zafirlukast. Food: Grapefruit juice will significantly increase bioavailability of oral budesonide.

Pharmacokinetics

Absorption: 20% (nasal) dose, 6–13% of (orally inhaled) dose, 9% PO dose reaches systemic circulation; PO form is absorbed from duodenum at pH >5.5; oral bioavailability increases 2.5 times in hepatic cirrhosis. Onset: 8–12 h inhaled, 2 wk oral. Peak: 2 wk inhaled, 8 wk oral delayed by high-fat meal. Distribution: 90% protein bound. Metabolism: 85% of absorbed dose undergoes first pass metabolism by CYP3A4. Elimination: 60% in urine, 40% in feces. Half-Life: 2–3.6 h.

Nursing Implications

Assessment & Drug Effects

• Monitor closely for S&S of hypercorticism if concomitant doses of ketoconazole or other CYP3A4 inhibitors (see Drug Interactions) are being given.
• Monitor patients with moderate to severe liver disease for increased S&S of hypercorticism.
• Lab tests: Periodic serum potassium.

Patient & Family Education

• Notify the physician immediately for any of the following: itching, skin rash, fever, swelling of face and neck, difficulty breathing, or if you develop S&S of infection.
• Do not drink grapefruit juice or eat grapefruit regularly.
• Avoid people with infections, especially those with chickenpox or measles if you have never had these conditions.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug