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Budesonide

Pronunciation

Pronunciation: bue-DES-oh-nide
Class: Corticosteroid, Glucocorticoid, Intranasal steroid

Trade Names

Entocort EC
- Capsules, oral 3 mg (micronized)

Pulmicort Flexhaler
- Powder for inhalation 90 mcg
- Powder for inhalation 180 mcg

Pulmicort Respules
- Inhalation suspension 0.25 mg per 2 mL
- Inhalation suspension 0.5 mg per 2 mL
- Inhalation suspension 1 mg per 2 mL

Rhinocort Aqua
- Nasal spray 32 mcg/spray

Entocort Capsules (Canada)
Gen-Budesonide AQ (Canada)
Pulmicort Nebuamp (Canada)
Rhinocort Turbuhaler (Canada)

Pharmacology

Exhibits wide range of inhibitory activities against multiple cell types and mediators involved in allergic-mediated inflammation.

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Pharmacokinetics

Absorption

Oral

T max is 1 to 2 h. Absolute bioavailability is 6% to 13%.

Inhalation

T max is 1 to 2 h, absolute bioavailability is 6% to 13% (powder for inhalation). T max is 20 min; absolute bioavailability is 6% (inhalation suspension).

Intranasal

Approximately 34% reaches systemic circulation. T max is approximately 0.7 h.

Distribution

Vd is 2 to 3 L/kg (or 200 L). Budesonide is 85% to 90% protein bound.

Metabolism

Rapidly metabolized; CYP3A4 is involved in the formation of 2 metabolites (less than 1% of budesonide activity).

Elimination

The half-life is 2 to 3 h. Budesonide is excreted in the urine (approximately 60%) and feces as metabolites; no unchanged drug is detected in the urine.

Special Populations

Renal Function Impairment

No data regarding use in patients with renal impairment.

Hepatic Function Impairment

Reduced liver function may affect the elimination of budesonide. Patients with compromised liver function had doubled systemic availability after oral ingestion.

Elderly

No pharmacokinetic differences have been identified.

Children

Plasma half-life is shorter than in adults. In asthmatic children 4 to 6 y of age, the terminal half-life of budesonide after nebulization is 2.3 hours, and the systemic Cl is 0.5 L/min, which is approximately 50% greater than in healthy adults after adjustment for differences in weight.

Gender

No pharmacokinetic differences have been identified.

Race

No pharmacokinetic differences have been identified.

Indications and Usage

Intranasal

Management of seasonal and perennial allergic rhinitis symptoms in adults and children.

Powder for inhalation

For the maintenance treatment of asthma as prophylactic therapy in adults and children 6 y and older.

Inhalation suspension

For the maintenance treatment of asthma and as prophylactic therapy in children 12 mo to 8 y of age.

Oral capsule

Crohn disease.

Unlabeled Uses

Inhalation suspension

Eosinophilic esophagitis.

Contraindications

Untreated localized infections involving the nasal mucosa; relief of acute bronchospasm; primary treatment of status asthmaticus or other acute episodes of asthma when intensive measures are required; hypersensitivity to the drug or any component of the product; severe hypersensitivity to milk proteins (powder for inhalation). Not recommended for treatment of nonallergic rhinitis because of lack of data.

Dosage and Administration

Nasal Spray
Adults and Children 12 y and older

Spray Start with 64 mcg/day administered as 1 spray in each nostril daily.

Maintenance

Spray Titrate to minimum effective dose (max, 256 mcg/day administered as 4 sprays in each nostril daily).

Adults and Children 6 to younger than 12 y

Spray Start with 64 mcg/day administered as 1 spray in each nostril daily.

Maintenance

Spray Titrate to minimum effective dose (max, 128 mcg/day administered as 2 sprays in each nostril daily).

Powder for inhalation
Adults

Inhalation 360 mcg twice daily (max, 720 mcg twice daily).

Children 6 to 17 y of age

Inhalation 180 mcg twice daily (max, 360 mcg twice daily).

Inhalation suspension
Children 12 mo to 8 y of age Patients receiving bronchodilators alone

Inhalation 0.5 mg/day administered daily or twice daily in divided doses (max, 0.5 mg/day).

Patients receiving inhaled corticosteroids

Inhalation 0.5 mg/day administered daily or twice daily in divided doses (max, 1 mg/day).

Patients receiving oral corticosteroids

Inhalation 1 mg/day administered as 0.5 mg twice daily or 1 mg daily (max, 1 mg/day). For patients who are maintained on long-term oral corticosteroids, the usual maintenance dose should be used concurrently with the initial budesonide therapy. After approximately 1 week, gradual withdrawal of the systemic corticosteroid is started by reducing the daily or alternate daily dose. The next reduction is made after 1 or 2 weeks, depending on the response of the patient. Generally, these decrements should not exceed 25% of the prednisone dose or its equivalent. A slow rate of withdrawal is strongly recommended.

Oral Capsules
Adults

PO 9 mg daily in the morning for up to 8 wk (Crohn disease); can be tapered to 6 mg daily for up to 3 mo for maintenance of clinical remission.

General Advice

  • Nasal Spray
  • For intranasal use only. Avoid spraying into the eyes, mouth, or directly into the nasal septum.
  • Shake gently before each use.
  • Actuate the pump 8 times to prime before first use. If pump has not been used for 2 consecutive days, reprime the pump with 1 spray. If pump has not been used for more than 14 days, rinse the applicator and reprime the pump with 2 sprays.
  • Clear nasal passages of secretions prior to use. If patient is congested, use topical, short-acting decongestant just before administration to ensure adequate penetration of spray. Saline nasal lavage may help remove secretions.
  • Place nasal adapter into 1 nostril, gently close other nostril with finger. While inhaling from nostril, activate canister. Repeat process on other side. Patient should not blow nose immediately after administration.
  • If 2 sprays per nostril are ordered, administer 1 spray in each nostril, wait a few seconds, and administer second spray into each nostril.
  • Powder for inhalation
  • For inhalation only. Inhale deeply and forcefully each time the unit is used.
  • Prime the unit before the first use.
  • Have patient rinse mouth with water without swallowing after each use.
  • Inhalation suspension
  • Administer only via jet nebulizer connected to an air compressor. Not for administration by ultrasonic nebulizer.
  • Medication requires no dilution before administration and is added directly into the nebulizer reservoir.
  • Do not mix with other nebulized medications unless ordered by health care provider.
  • Oral Capsules
  • Administer prescribed dose daily in the morning. Administer without regard to meals but administer with food if GI upset occurs.
  • Have patient swallow capsules whole. Do not crush, chew, or break capsules.

Storage/Stability

Nasal Spray

Store nasal spray between 68° and 77°F with the valve up. Protect from freezing and light. Discard bottle when labeled number of sprays have been used, even if bottle is not completely empty.

Inhalation

Store upright between 68° and 77°F in a dry place. Protect from light. Do not refrigerate or freeze. For the inhalation suspension, after opening the foil pouch, return unused ampules to the pouch to protect from light. Unused inhalation suspension must be used within 14 days after the pouch has been opened. Any opened inhalation suspension must be used promptly. Discard any unused suspension.

Oral Capsules

Store capsules at ambient room temperature (59° to 86°F).

Drug Interactions

Anticoagulants (eg, warfarin)

The anticoagulant effect of warfarin may be increased. Hemorrhagic episodes have been reported. Monitor coagulation parameters and adjust the warfarin dose as needed.

Barbiturates, carbamazepine, rifamycins

Budesonide pharmacologic effects may be decreased. Monitor patient response and adjust the budesonide dose as needed.

CYP3A4 strong inhibitors (eg, atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin)

May increase budesonide plasma levels, increasing the pharmacologic and adverse effects. Use with caution. Monitor for budesonide adverse reactions (eg, adrenal insufficiency) and adjust the dose as needed.

Hormonal contraceptives

Budesonide therapeutic effects and risk of adverse reactions may be increased. A lower dose of budesonide may be needed. Monitor the patient response and adjust the budesonide dose as needed.

Hydantoins (eg, phenytoin)

Budesonide and phenytoin plasma concentrations and pharmacologic effects may be decreased. Higher doses of both agents may be needed during coadministration. Monitor the patient response and phenytoin concentrations. Adjust treatment as needed.

Interleukins (eg, aldesleukin)

Pharmacologic effects of interleukins may be decreased. Avoid coadministration.

Mifepristone

Administration of mifepristone for the termination of pregnancy is contraindicated in patients receiving long-term corticosteroid therapy.

Quinolones (eg, levofloxacin)

The risk of tendon rupture may be increased when a quinolone is given concomitantly with a corticosteroid. Avoid coadministration.

Salicylates (eg, aspirin)

Salicylate plasma concentrations and effectiveness may be decreased. Monitor salicylate concentrations and the patient response when starting or stopping budesonide. Adjust the salicylate dose as needed.

Adverse Reactions

Cardiovascular

Hypertension, migraine, palpitations, syncope, tachycardia (less than 5%).

CNS

Dizziness, fatigue, headache (at least 3%); agitation, amnesia, asthenia, dysphonia, emotional lability, hyperkinesia, hypertonia, insomnia, malaise, nervousness, paresthesia, sleep disorder, somnolence, tremor, vertigo (less than 5%); aggressive reactions, anxiety, depression, irritability, psychosis, restlessness (postmarketing).

Dermatologic

Hirsutism, rash (at least 3%); acne, alopecia, dermatitis, eczema, flushing, increased sweating, pruritus, purpura, pustular rash, skin disorder, skin striae (less than 5%); facial skin irritation, skin bruising (postmarketing).

EENT

Otitis media, rhinitis (12%); nasopharyngitis (9%); ear infection (5%); conjunctivitis, epistaxis (4%); nasal congestion, pharyngitis, rhinitis (at least 3%); nasal irritation (at least 2%); abnormal vision, earache, external ear infection, eye abnormality, eye infection, pharynx disorder (less than 5%); cataracts, glaucoma, loss of smell, septum perforation, throat irritation (postmarketing).

GI

Gastroenteritis (5%); diarrhea, vomiting (4%); abdominal pain, dyspepsia, flatulence, nausea, oral candidiasis (at least 3%); aggravated enteritis, anorexia, anus disorder, Crohn disease, dry mouth, epigastric pain, GI fistula, glossitis, hemorrhoids, increased appetite, intestinal obstruction, taste perversion, tongue edema, tooth disorder (less than 5%).

Genitourinary

Dysuria, intermenstrual bleeding, menstrual disorder, micturition frequency, nocturia, UTI (less than 5%).

Hematologic-Lymphatic

Cervical lymphadenopathy, ecchymosis, leukocytosis (less than 5%).

Lab Tests

Adrenal insufficiency, anemia, hematuria, hypokalemia, increased alkaline phosphatase, increased atypical neutrophils, increased erythrocyte sedimentation rate, pyuria (at least 1%).

Metabolic-Nutritional

Hypokalemia, weight increase (less than 5%).

Musculoskeletal

Arthralgia, back pain (at least 3%); aggravated arthritis, cramps, fracture, myalgia, neck pain (less than 5%); avascular necrosis of the femoral head, growth suppression, osteoporosis (postmarketing).

Respiratory

Respiratory tract infection (38%); coughing (9%); respiratory infection, sinusitis (at least 3%); viral upper respiratory tract infection (2%); bronchitis, bronchospasm, dyspnea, stridor (less than 5%); wheezing (postmarketing).

Miscellaneous

Moniliasis, viral infection (4%); fever, flu syndrome, moon face, pain, swollen ankles (at least 3%); abscess, allergic reaction, buffalo hump, chest pain, dependent edema, face edema, herpes simplex, increased C-reactive protein, infection, oral candidiasis (less than 5%); angioedema, hypersensitivity reactions, intracranial hypertension, symptoms of hypocorticism and hypercorticism (postmarketing).

Precautions

Monitor

Ensure that therapy is periodically reviewed to determine if it needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated. Monitor patients being weaned from oral to inhalation for signs and symptoms of adrenal insufficiency (fatigue, lassitude, weakness, hypotension). Monitor growth velocity in children. Monitor bone mineral density (BMD) in patients at major risk for decreased bone mineral content. Monitor for the development of glaucoma or cataracts in patients who experience changes in vision or have a history of increased IOP, glaucoma, and/or cataracts.


Pregnancy

Category B (inhalation); Category C (oral, intranasal).

Lactation

Excreted.

Children

Safety and efficacy not established for children younger than 6 y (intranasal, powder for inhalation); safety and efficacy not established for children younger than 12 mo or older than 8 y (inhalation suspension); safety and efficacy not established in children for Entocort EC . Corticosteroids may suppress growth in children and adolescents, particularly with higher doses over extended periods. Plot growth in children on prolonged therapy.

Elderly

Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and comorbidity.

Hypersensitivity

Immediate hypersensitivity reactions have occurred. The powder for inhalation contains lactose. It is possible that cough, wheeze, or bronchospasm may occur in patients who have a severe milk protein allergy.

Special Risk Patients

Use with caution in patients with tuberculosis (TB) infection, hypertension, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, a family history of diabetes or glaucoma, renal or hepatic impairment, or any condition in which glucocorticoids may have unwanted effects. Use inhaled corticosteroids with caution in patients with active or quiescent TB infection; untreated systemic fungal, bacterial, parasitic, or viral infections; or ocular herpes simplex.

Acute asthma

Not for rapid relief of acute episodes of asthma or bronchospasm.

Allergy

Transfer of patients from systemic steroid therapy to inhalation therapy may unmask allergic conditions previously suppressed by systemic steroid therapy (eg, rhinitis).

Bone mineral density

Decrease in BMD may occur with long-term administration.

Bronchospasm

Bronchospasm may occur with an immediate increase in wheezing following dosing, which may require immediate treatment with a fast-acting inhaled bronchodilator.

Eosinophilic conditions

May occur. These events usually, but not always, have been associated with the reduction and/or withdrawal of oral corticosteroid therapy following the introduction of inhaled corticosteroids.

Fungal infections

Antifungal treatment or discontinuation of corticosteroid therapy may be necessary.

Immunology

Patients receiving immunosuppressant agents are more susceptible to infections than healthy adults. If a patient is exposed to measles or chickenpox, appropriate prophylaxis and treatment may be indicated.

Local effects

Localized infections with Candida albicans occurred in the mouth and pharynx in some patients after inhaled budesonide use.

Prior corticosteroid use

Transfer from oral corticosteroids to inhaled corticosteroids has resulted in death caused by adrenal insufficiency related to a lower systemic availability. A number of months are required for recovery of hypothalamic-pituitary-adrenal (HPA) axis suppression. Patients maintained on 20 mg or more of prednisone daily may be at higher risk. During periods of stress or severe asthma attack, instruct patients who have been withdrawn from systemic corticosteroids to resume oral steroids immediately.

Systemic effects

Use cautiously in patients taking daily or alternate-day steroid therapy; may increase likelihood of HPA suppression. Exceeding recommended dose may cause systemic effects.

Wound healing

Because of inhibitory effect of corticosteroids on wound healing, patients with recent nasal septal ulcers, nasal surgery, or nasal trauma should not use nasal corticosteroids until healing has occurred.

Overdosage

Symptoms

Adrenal suppression, growth suppression, hypercorticism.

Patient Information

  • Advise patient to read the patient information leaflet before starting therapy and again with each refill.
  • Advise patient to continue taking other medications for the same condition as prescribed by health care provider.
  • Advise patients that their dose may be changed periodically, depending on how well symptoms are controlled.
  • Explain that effects of this drug are not immediate. Benefit requires daily use as instructed, and usually begins to occur within 1 or 2 days, but full benefit may take 1 to 2 wk depending on the condition being treated and the dose and route of administration of medication being used.
  • Caution patients not to increase their dose and to inform heir health care provider if symptoms are not improving or are worsening.
  • If patient is being converted from oral corticosteroids to inhaled or intranasal corticosteroids, review the signs and symptoms of adrenal insufficiency, which may occur days or weeks after conversion is complete. Advise patient to carry medical identification (eg, card, bracelet) indicating they may need supplemental systemic corticosteroids during periods of stress or a severe asthma attack.
  • Instruct diabetic patients to monitor their blood glucose more frequently when the drug is started or the dose is changed, and to inform their health care provider of significant changes in readings.
  • Advise patients to immediately notify their health care provider if any of the following occur: swelling of feet or ankles; muscle weakness; black, tarry stools; vomiting of blood; fever, sore throat, or other signs of infection.
  • Advise patient to avoid exposure to chickenpox and measles and to seek medical advice immediately if exposed.
  • Advise women to notify their health care provider if they are pregnant, planning to become pregnant, or are breast-feeding.
  • Caution patients not to take any prescription or OTC medications, herbal preparations, or dietary supplements unless advised by their health care provider.
  • Advise patient that follow-up visits may be required to monitor therapy, and to keep appointments.
  • Powder for Inhalation
  • Review proper administration technique. Have patient demonstrate technique to ensure effective use of the delivery system.
  • Warn patient that drug is an asthma controller and is not to be used to treat an acute asthma attack. Rescue medication (bronchodilator) must be used to obtain rapid relief of asthma symptoms.
  • Instruct patient not to stop the medication once symptoms have been controlled. Continued daily use is necessary to continue to control symptoms.
  • Advise patient to discard the inhaler when the red mark appears at bottom of indicator window.
  • Instruct patients to carry medical identification (eg, card, bracelet) if they experience acute, severe asthma attacks requiring rapid systemic treatment.
  • Advise patients to report the following symptoms to their health care provider: sore throat or mouth, cough, dry mouth, rash, facial swelling, or worsening asthma symptoms (eg, increasing need for bronchodilator).
  • Inhalation Suspension
  • Ensure that the caregiver can prepare, use, and clean the nebulizer without difficulty.
  • Instruct the caregiver not to mix with other nebulizer medications unless advised by a health care provider.
  • Instruct the caregiver to use nebulizer solution immediately after opening. If solution is not used immediately, advise patient or caregiver to discard the solution.
  • Advise the caregiver to discard any unused nebulizer solution.
  • Advise the caregiver to rinse the child's mouth and wash face after each treatment.
  • Nasal Inhalation
  • Review the proper administration technique. Have patient demonstrate the technique to ensure effective use of the nasal spray.
  • Instruct patient not to stop the medication once symptoms have been controlled. Continued daily use is necessary to continue to control symptoms.
  • Instruct patient to use with caution if sores develop or injuries occur in nasal passages. Drug may prevent or slow proper healing.
  • Advise patients to report the following symptoms to their health care provider: sneezing, nasal irritation, or nosebleed.
  • Advise patient to discard bottle when labeled number of sprays have been used, even if bottle is not completely empty.
  • Oral
  • Advise patient to take prescribed dose once daily in the morning.
  • Advise patient that mediation can be taken without regard to meals, but to take with food if stomach upset occurs.
  • Advise patient to swallow capsules whole and not to chew, crush, or break the capsule.
  • Caution patient to avoid consumption of grapefruit juice for duration of therapy.
  • Advise patients to carry medical identification (eg, card, bracelet) indicating they are on corticosteroids, the condition(s) being treated, and possible need for supplemental systemic corticosteroids during periods of stress.
  • Caution patient not to suddenly stop taking this medication if therapy has continued for longer than 1 mo. Advise patient that if medication needs to be discontinued after prolonged therapy (eg, greater than 1 mo), it will be slowly withdrawn to prevent adrenal insufficiency.
  • Review the following signs and symptoms of adrenal insufficiency: nausea; fatigue; dizziness; hypotension; depression; or abdominal, joint, or muscle pain. Instruct patient to immediately seek medical care if symptoms suggestive of adrenal insufficiency develop.

Copyright © 2009 Wolters Kluwer Health.

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