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Drugs reference index «Budesonide»

Budesonide
Budesonide
Budesonide


Budesonide

Pronunciation: (byoo-DESS-oh-nide)Class: Corticosteroid, Glucocorticoid, Intranasal steroid

Trade Names:Entocort EC- Capsules 3 mg (micronized)

Trade Names:Pulmicort Flexhaler- Inhalation powder 180 mcg- Inhalation powder 90 mcg

Trade Names: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

Trade Names: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.

Pharmacokinetics

Absorption

Oral

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

Oral inhalation (powder)

34% systemically available from lungs. T max is within 10 min. Absolute bioavailability is 39%.

Intranasal

About 34% reaches systemic circulation. T max is about 0.7 h.

Distribution

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

Metabolism

Liver

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

Elimination

The t ½ is 2 to 3 h. Budesonide is excreted in the urine (about 60%) and feces as metabolites; no unchanged drug is detected in the urine.

Special Populations

Hepatic Function Impairment

Doubled systemic availability after oral ingestion.

Children

Plasma half-life is shorter than in adults.

Indications and Usage

Intranasal

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

Oral inhalation

For the maintenance treatment of asthma as prophylactic therapy in adults and children and for patients requiring oral corticosteroid therapy for asthma.

Inhalation suspension

Maintenance treatment of asthma and prophylactic therapy in children 12 mo to 8 yr of age.

Oral capsule

Crohn disease.

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. Not recommended for treatment of nonallergic rhinitis because of lack of data.

Dosage and Administration

Nasal SprayAdults and Children 12 yr of age 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 yr of age

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).

Aerosol, FlexhalerAdults

Oral inhaler 360 mcg twice daily (max, 720 mcg twice daily).

Children at least 6 yr of age

Oral inhaler 180 mcg twice daily (max, 360 mcg twice daily).

RespulesChildren 12 mo to 8 yr of age

Inhalation suspension Administer by inhaled route via jet nebulizer connected to air compressor.

Children receiving bronchodilators alone

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

Children receiving inhaled corticosteroids

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

Children receiving oral corticosteroids

1 mg/day administered as 0.5 mg twice daily or 1 mg daily (max, 1 mg/day).

Oral CapsulesAdults

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. Do 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.
Aerosol, Flexhaler
  • If patient is also receiving bronchodilators by inhalation, administer bronchodilator 5 min before budesonide to enhance penetration of latter drug into bronchial tree.
  • Prime the unit before the first use.
  • Do not shake inhaler. Have patient rinse mouth with water or mouthwash after each use.
  • Do not use with a spacer device (eg, Aerochamber ). Do not bite or chew mouthpiece, exhale into the inhalation device, or wash or attempt to take the inhalation device apart. Replace cover securely after each use.
Respules
  • Administer only via jet nebulizer. Not for injection or oral use or administration by ultrasonic nebulizer.
  • Medication requires no dilution before administration and is added directly into the nebulizer reservoir. Gently shake ampule using circular motion before adding to nebulizer reservoir.
  • Once ampule has been opened, administer promptly or discard.
  • Have patient rinse mouth with water or mouthwash after each use.
  • Discard any unused solution.
  • 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 at 68° to 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.

Aerosol, Flexhaler

Store at 68° to 77°F. Keep tightly capped.

Respules

Store unused ampules in upright position in protective foil pouch at 68° to 77°F. Protect from light. Do not refrigerate or freeze. After opening foil pouch, return unused ampules to pouch to protect from light. Unused ampules must be used within 14 days after pouch has been opened.

Oral Capsules

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

Drug Interactions

Grapefruit juice, CYP3A4 inhibitors (eg, erythromycin, ketoconazole, ritonavir)

May increase budesonide plasma levels, increasing the pharmacologic and adverse effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Oral

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

Nasal

Palpitations (postmarketing).

CNS

Oral

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

Dermatologic

Oral

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

EENT

Oral

Conjunctivitis, ear infection, epistaxis, nasopharyngitis, nasal congestion, otitis media, pharyngitis, rhinitis (at least 3%); earache, eye abnormality, eye infection, abnormal vision, pharynx disorder (less than 5%); glaucoma, cataracts (postmarketing).

Nasal

Epistaxis, nasal irritation, pharyngitis (at least 2%); pharynx disorders (eg, throat irritation, burning, itching), loss of smell, septum perforation (postmarketing).

GI

Oral

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

Genitourinary

Oral

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

Hematologic-Lymphatic

Oral

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

Lab Tests

Oral

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

Local

Oral

Contact dermatitis (less than 5%).

Metabolic-Nutritional

Oral

Hypokalemia, weight increase (less than 5%).

Musculoskeletal

Oral

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

Respiratory

Oral

Coughing, respiratory infection, sinusitis (at least 3%); bronchitis, bronchospasm, dyspnea, stridor (less than 5%); wheezing (postmarketing).

Nasal

Coughing (at least 2%).

Miscellaneous

Oral

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

Nasal

Angioedema (postmarketing).

Precautions

Monitor

Document disease state activity and/or symptoms before starting therapy and periodically during treatment. Notify health care provider if symptoms do not improve or worsen. 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.

Pregnancy

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

Lactation

Excreted.

Children

Not recommended for children younger than 6 yr of age (intranasal, oral inhaler) or younger than 12 mo of age (respules); 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. Inform health care provider if abnormalities noted.

Elderly

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

Hypersensitivity

Immediate hypersensitivity reactions have occurred.

Special Risk Patients

Use with caution in patients with tuberculosis infection, hypertension, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, with a family history of diabetes or glaucoma, renal or hepatic impairment, or with any condition in which glucocorticoids may have unwanted effects. Use inhaled corticosteroids with caution in patients with active or quiescent tuberculosis 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 steroids therapy to inhalation therapy may unmask allergic conditions previously suppressed by systemic steroid therapy (eg, rhinitis).

Bronchospasm

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

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.

Milk protein allergy

Flexhaler contains lactose. It is possible that cough, wheeze, or bronchospasm may occur in patients who have a severe milk protein allergy.

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 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 experiencing recent nasal septal ulcers, nasal surgery, or nasal trauma should not use nasal corticosteroids until healing has occurred.

Overdosage

Symptoms

Hypercorticoidism, adrenal suppression.

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 same condition as prescribed by health care provider.
  • Advise patient that dose may be changed periodically, depending on how well symptoms are controlled.
  • Explain that effects of 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 patient not to increase dose and to inform 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 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 patient to monitor blood glucose more frequently when drug is started or dose is changed and to inform health care provider of significant changes in readings.
  • Advise patient to immediately notify 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 health care provider if pregnant, planning to become pregnant, or breastfeeding.
  • Caution patient not to take any prescription or OTC medications, herbal preparations, or dietary supplements unless advised by health care provider.
  • Advise patient that follow-up visits may be required to monitor therapy and to keep appointments.
  • Oral Inhalation Powder
  • 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 red mark appears at bottom of indicator window.
  • Instruct patient to carry medical identification (eg, card, bracelet) if he or she experiences acute severe asthma attacks requiring rapid systemic treatment.
  • Advise patient to report the following symptoms to health care provider: sore throat or mouth, cough, dry mouth, rash, facial swelling, or worsening asthma symptoms (increasing need for bronchodilator).
  • Inhalation Suspension
  • Ensure caregiver can prepare, use, and clean the nebulizer without difficulty.
  • Instruct caregiver not to mix with other nebulizer medications unless advised by health care provider.
  • Instruct caregiver to use nebulizer solution immediately after opening. If solution is not used immediately, advise patient or caregiver to discard the solution.
  • Advise caregiver to discard any unused nebulizer solution.
  • Advise caregiver to rinse child's mouth and wash face after each treatment.
  • Nasal Inhalation
  • Review proper administration technique. Have patient demonstrate 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 patient to report the following symptoms to 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 patient 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 been 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.

  • Budesonide Powder MedFacts Consumer Leaflet (Wolters Kluwer)
  • Budesonide Detailed Consumer Information (PDR)
  • budesonide Advanced Consumer (Micromedex) - Includes Dosage Information
  • budesonide Concise Consumer Information (Cerner Multum)
  • Entocort EC Prescribing Information (FDA)
  • Entocort EC Detailed Consumer Information (PDR)
  • Entocort EC Sustained-Release Capsules MedFacts Consumer Leaflet (Wolters Kluwer)
  • Pulmicort Flexhaler Prescribing Information (FDA)
  • Pulmicort Flexhaler Advanced Consumer (Micromedex) - Includes Dosage Information
  • Pulmicort Flexhaler Concise Consumer Information (Cerner Multum)
  • Pulmicort Respules Suspension MedFacts Consumer Leaflet (Wolters Kluwer)
  • Pulmicort Respules Prescribing Information (FDA)
  • Pulmicort Turbuhaler Detailed Consumer Information (PDR)
  • Pulmicort Turbuhaler Powder MedFacts Consumer Leaflet (Wolters Kluwer)

See Also...

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