Entocort EC, Pulmicort Flexhaler, Rhinocort, Rhinocort Aqua, Rhinocort Turbuhaler
Classifications: antiinflammatory; adrenal corticosteroid; glucocorticoid; Therapeutic: antiinflammatory; adrenal corticosteroid
Pregnancy Category: B for inhaled; C for oral
32 mcg/inhalation; 3 mg capsule
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.
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.
Treatment of allergic and perennial rhinitis, maintain remission in mild to moderate Crohn's disease; prophylaxis for asthma.
Hypersensitivity to budesonide, status asthmaticus, acute bronchospasms; peptic ulcer disease; pregnancy (category C for
oral; category B for inhaled), lactation.
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
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.
- 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
, 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:
Hypokalemia, weight gain. Respiratory:
cough, rhinitis, sinusitis
, hoarseness, wheezing. Skin: Eczema
, pruritus, purpura, rash, alopecia
. Special Senses:
Contact dermatitis, reduced sense of smell, nasal pain. Urogenital:
Intermenstrual bleeding, dysuria.
may increase oral budesonide concentrations and 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.
20% (nasal) dose, 613% 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
812 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:
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.