Budesonide


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Crohn's disease For induction of remission in patients with mild to moderate active disease affecting the ileum and/or ascending colon: 9 mg daily either as a single dose before breakfast or in 3 divided doses about 30 minutes before meals (depending on preparation) for up to 8 weeks. Recurring episodes of active disease: May repeat an 8-week course. Maintenance of remission: 6 mg once daily for up to 3 months. Collagenous colitis For induction of remission in patients with active disease: 9 mg once daily in the morning for up to 8 weeks. Autoimmune hepatitis As gastro-resistant cap: In combination with azathioprine (only if patients are tolerant with azathioprine): Induction of remission: 3 mg tid until remission is achieved. Maintenance of remission: 3 mg bid for at least 24 months, may be increased to 3 mg tid if ALT/AST elevates during maintenance treatment. Microscopic colitis For induction of remission in patients with active disease: As controlled-release cap: 9 mg once daily in the morning for up to 8 weeks. Maintenance: 6 mg once daily in the morning, or the lowest effective dose. Ulcerative colitis As modified-release tab: For induction of remission in patients with mild to moderate active disease, where 5-aminosalisylic acid (5-ASA) is insufficient: 9 mg once daily in the morning for up to 8 weeks. Eosinophilic oesophagitis As orodispersible tab: 1 mg bid for 6 weeks, may be extended for up to 12 weeks for unresponsive patients. Inhalation Asthma As dry powder inhaler: 200-800 mcg as a single dose or in 2 divided doses. Max: 800 mcg bid. As nebuliser susp: Severe asthma, or while reducing or stopping oral corticosteroids: Initial: 1-2 mg bid. Maintenance: 0.5-1 mg bid. Nasal Allergic rhinitis; Vasomotor rhinitis As metered-dose spray (64 mcg/dose): Initial: 2 sprays into each nostril once daily in the morning or 1 spray into each nostril bid, may be decreased to 1 spray into each nostril once daily if desired effect is achieved. Nasal polyps As metered-dose spray (64 mcg/dose): Initial: 1 spray into each nostril bid. Rectal Ulcerative colitis For cases involving the rectum and sigmoid colon: As retention enema: 2 mg in 100 mL given daily at bedtime for 4 weeks, may be extended to 8 weeks if the patient is not in remission after the initial 4-week treatment. As rectal foam: 2 mg once daily for up to 6-8 weeks.
Dosage Details
Inhalation/Respiratory
Croup
Child: As nebuliser susp: 2 mg as a single dose, or in 2 divided doses of 1 mg administered in an interval of 30 minutes. Doses may be repeated 12 hourly for up to 36 hours or until clinical improvement is observed.

Inhalation/Respiratory
Asthma
Adult: As dry powder inhaler: 200-800 mcg daily as a single dose or in 2 divided doses. Max: 800 mcg bid. As nebuliser susp: Severe asthma, or while reducing or stopping oral corticosteroids: Initially, 1-2 mg bid. Maintenance: 0.5-1 mg bid. Dosing should be individualised and reduced to the minimum effective dose to maintain good asthma control.
Child: As dry powder inhaler: 5-12 years 200-800 mcg daily in 2 divided doses. >12 years Same as adult dose. As nebuliser susp: 3 months to 12 years Initially, 0.5-1 mg bid. Maintenance: 0.25-0.5 mg bid. >12 years Same as adult dose. Dosing should be individualised and reduced to the minimum effective dose to maintain good asthma control.

Nasal
Allergic rhinitis, Vasomotor rhinitis
Adult: As metered-dose spray (64 mcg/dose): Initially, 2 sprays into each nostril once daily in the morning or 1 spray into each nostril bid, may be decreased to 1 spray into each nostril once daily if desired effect is achieved. Doses must be titrated to the lowest effective dose to maintain adequate control of symptoms.
Child: ≥6 years Same as adult dose.

Nasal
Nasal polyps
Adult: As metered-dose spray (64 mcg/dose): Initially, 1 spray into each nostril bid. Doses must be titrated to the lowest effective dose to maintain adequate control of symptoms.
Child: ≥6 years Same as adult dose.

Oral
Crohn's disease
Adult: For induction of remission in patients with mild to moderate active disease affecting the ileum and/or ascending colon: 9 mg daily either as a single dose before breakfast or in 3 divided doses about 30 minutes before meals (depending on preparation) for up to 8 weeks. Reduce dose 2-4 weeks before stopping therapy. Recurring episodes of active disease: May repeat an 8-week course. Maintenance of remission: 6 mg once daily for up to 3 months, gradually reduce dose before stopping treatment.

Oral
Autoimmune hepatitis
Adult: As gastro-resistant cap: In combination with azathioprine (only if patients are tolerant with azathioprine): Induction of remission: 3 mg tid until remission is achieved. Maintenance of remission: 3 mg bid for at least 24 months, may be increased to 3 mg tid if ALT/AST elevates during maintenance treatment.

Oral
Microscopic colitis
Adult: For induction of remission in patients with active disease: As controlled-release cap: 9 mg once daily in the morning for up to 8 weeks. Maintenance: 6 mg once daily in the morning, or the lowest effective dose.

Oral
Collagenous colitis
Adult: For induction of remission in patients with active disease: 9 mg once daily in the morning for up to 8 weeks. Reduce dose gradually during the last 2 weeks of therapy.

Oral
Eosinophilic oesophagitis
Adult: As orodispersible tab: 1 mg bid for 6 weeks, may be extended for up to 12 weeks for unresponsive patients.

Oral
Ulcerative colitis
Adult: As modified-release tab: For induction of remission in patients with mild to moderate active disease, where 5-aminosalisylic acid (5-ASA) is insufficient: 9 mg once daily in the morning for up to 8 weeks.

Rectal
Ulcerative colitis
Adult: For cases involving the rectum and sigmoid colon: As retention enema: 2 mg in 100 mL given daily at bedtime for 4 weeks, may be extended to 8 weeks if the patient is not in remission after the initial 4-week treatment. As rectal foam: 2 mg once daily for up to 6-8 weeks.
Renal Impairment
Oral
Eosinophilic oesophagitis
Severe: Not recommended.
Administration
May be taken with or without food. Take in the morning. Swallow whole, do not chew/crush. For patients w/ difficulty swallowing, cap may be carefully opened & entire contents mixed in a tbsp of applesauce. Swallow mixt w/o chewing w/in 30 min after prep. Avoid grapefruit juice.
Contraindications
Oral, rectal: Hepatic cirrhosis. Oral inhalation: Primary treatment of status asthmaticus or other acute episodes of asthma requiring intensive measures.
Special Precautions
Patients with diabetes mellitus, myasthenia gravis, thyroid disease, COPD, CV disease (e.g. CHF, hypertension, acute MI), gastrointestinal disease (e.g. diverticulitis, fresh intestinal anastomoses, active or latent peptic ulcer), infections (e.g. oral, nasal or ocular herpes simplex, active or quiescent TB, untreated fungal, bacterial, systemic viral or parasitic infections), cataracts, glaucoma, seizure disorders, and severe affective disorders (e.g. manic-depressive illness, previous steroid-induced psychosis); major risk factors for decreased bone mineral count (e.g. prolonged immobilisation, osteoporosis, postmenopausal status, tobacco use, poor nutrition); recent nasal surgery or trauma. Avoid abrupt withdrawal. Renal and hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Adrenal suppression (e.g. suppression of hypothalamic-pituitary-adrenal axis, hypercortisolism, Cushing’s syndrome), immunosuppression (prolonged use), growth retardation in children, hyperglycemia, fluid retention, decreased bone mineral density, Kaposi sarcoma (prolonged use), acute myopathy, pneumonia, delayed wound healing, visual disturbances (e.g. blurred vision, glaucoma, cataract, central serous chorioretinopathy), oral candidiasis. Rarely, vasculitis or other systemic eosinophilic conditions, psychiatric disturbances (e.g. psychomotor hyperactivity, insomnia, euphoria, mood swings, personality changes, anxiety, depression, aggression or psychotic manifestations), hypersensitivity reactions (e.g. anaphylaxis, angioedema, bronchospasm, contact dermatitis, rash, urticaria).
Cardiac disorders: Palpitation.
Gastrointestinal disorders: Nausea, abdominal pain, abdominal distension, dry mouth, dyspepsia, flatulence, diarrhoea, GERD, constipation.
General disorders and admin site conditions: Fatigue, malaise.
Infections and infestations: Oesophageal or oropharyngeal candidiasis, influenza.
Investigations: Blood cortisol decreased.
Metabolism and nutrition disorders: Hypokalaemia.
Musculoskeletal and connective tissue disorders: Myalgia, back pain, muscle spasms.
Nervous system disorders: Headache, dizziness, tremor.
Reproductive system and breast disorders: Menstrual disorder.
Respiratory, thoracic and mediastinal disorders: Cough, hoarseness, throat irritation, nasal ulcer, nasal septum perforation, epitaxis, nasal mucosa irritation.
Skin and subcutaneous tissue disorders: Acne, pruritus, exanthema, petechiae, bruising.
Vascular disorders: Hypertension.
Potentially Fatal: Adrenal insufficiency, paradoxical bronchospasm; chickenpox or measles infection (in immunosuppressed patients).
PO/Rectal: C; Inhalation/Respiratory/Nasal: B
MonitoringParameters
Monitor blood pressure, serum glucose and electrolytes; peak flow, FEV1, and other pulmonary function tests, bone mineral density, LFTs, growth in children. Assess for signs and symptoms of adrenal suppression, infection, ocular changes, and oral candidiasis (prolonged use).
Overdosage
Symptoms: Adrenal suppression and hypercorticism. Management: Symptomatic and supportive treatment. May consider immediate gastric lavage or emesis (oral).
Drug Interactions
Diminished therapeutic effects of vaccines. Increased systemic exposure and side effects with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, HIV protease inhibitors, clarithromycin, cobicistat). Decreased systemic exposure with CYP3A4 inducers (e.g. carbamazepine, rifampicin). Enhanced K excretion and aggravated hypokalaemia with diuretics. May potentiate effects of cardiac glycosides. May reduce uptake with colestyramine or antacids.
Food Interaction
Oral, rectal: Increased systemic exposure and risk of systemic adverse effects with grapefruit or grapefruit juice.
Lab Interference
May cause false low value results in ACTH stimulation test.
Action
Description: Budesonide is a corticosteroid with potent glucocorticoid activity. It controls the rate of protein synthesis, inhibits the migration of polymorphonuclear leukocytes and fibroblasts, reverses the capillary permeability and lysosomal stabilisation at the cellular level to prevent or control inflammation.
Onset: 24 hours (inhalation); 2-8 days (nebulisation); within 10 hours (nasal).
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability: 9-21% (oral); 39% (oral inhalation); approx 34% (nasal); 3-27% (rectal enema). Time to peak plasma concentration: 0.5-10 hours (oral); 10 minutes (oral inhalation); 30 minutes (nasal); 1.5 hours (rectal enema).
Distribution: Enters breast milk. Volume of distribution: 2.2-3.9 L/kg. Plasma protein binding: 85-90%.
Metabolism: Extensively metabolised in the liver by CYP3A4 isoenzyme to 2 major inactive metabolites, 16-α-hydroxyprednisolone and 6-β-hydroxybudesonide.
Excretion: Mainly via urine (60%) and faeces, as metabolites. Elimination half-life: Approx 2-3.6 hours.
Chemical Structure

Chemical Structure Image
Budesonide

Source: National Center for Biotechnology Information. PubChem Database. Budesonide, CID=5281004, https://pubchem.ncbi.nlm.nih.gov/compound/Budesonide (accessed on Jan. 22, 2020)

Storage
Tab, cap: Store at 25°C. Protect from light and moisture. Dry powder inhaler, nebule, nasal spray, rectal foam: Store between 20-25°C. Do not refrigerate or freeze. Protect from light, heat or direct sunlight.
ATC Classification
A07EA06 - budesonide ; Belongs to the class of corticosteroids acting locally. Used in the treatment of intestinal inflammation.
R01AD05 - budesonide ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
D07AC09 - budesonide ; Belongs to the class of potent (group III) corticosteroids. Used in the treatment of dermatological diseases.
R03BA02 - budesonide ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
References
Anon. Budesonide (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2019.

Anon. Budesonide (Oral Inhalation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2019.

Anon. Budesonide (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2019.

Anon. Budesonide (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2019.

Buckingham R (ed). Budesonide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/10/2019.

Budesonide Capsule (Mylan Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 16/07/2015.

Budesonide Extended Release Tablet (Oceanside Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/10/2019.

Joint Formulary Committee. Budesonide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/10/2019.

Disclaimer: This information is independently developed by MIMS based on Budesonide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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