Budesonide (Capsules, Inhaler) - Uses, Dose, MOa, Brands, Side effects

Budesonide is a high potency topical glucocorticoid that suppresses the inflammatory mediators. It is used to treat the following conditions:
    • For the maintenance and prophylactic treatment of patients with Asthma
    • Mild to moderately active Crohn disease involving the ileum and the ascending colon in patients older than 8 years of age
    • For the induction of remission in patients with mild to moderately active ulcerative colitis.
    • Off-label use for the treatment of eosinophilic esophagitis and protein-losing enteropathy.
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Budesonide Dose in adults:

For the inhalational therapy in patients with Asthma:

    • 400 - 2400 mcg in two to four divided doses initially, followed by a maintenance dose of 200 to 400 mcg twice a day.
    • According to the NIH Asthma guidelines:
      • Low dose: 180 - 600 mcg per day
      • Medium dose: 600 - 1200 mcg per day
      • High dose: more than 1200 mcg per day

Budesonide use in the treatment of mild to moderately active Crohn disease:

    • 9 mg orally once a day of an oral capsule in the morning for up to eight weeks
    • A repeat course may be required.
    • After the induction phase, a lower dose of 6 mg may be given for another 3 months.

Budesonide use in the treatment of active Ulcerative colitis:

    • 9 mg orally once a day of budesonide tablet in the morning for up to eight weeks

Off label use in the treatment of Eosinophilic esophagitis:

    • 2 mg/day orally as an oral budesonide viscous liquid or suspension in one or two divided doses.
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Budesonide Dose in Children:

For the treatment of Asthma in Children:

  • Children 6 - 11 years of age:
    • 200 - 400 mcg in two divided doses initially, followed by the lowest effective maintenance dose.
    • According to the NIH Asthma guidelines:
      • Low dose: 180 - 400 mcg per day
      • Medium dose: 400 - 800 mcg per day
      • High dose: more than 800 mcg per day
  • For nebulization in young children (12 months - 8 years):

    • 0.25 mg/day. The lowest effective dose should be used.
    • Patients previously treated with bronchodilators alone:
      • 0.5 mg/day administered in one or two divided doses.
    • Previously treated with inhaled corticosteroids:
      • 0.5 mg/day administered in one or two divided doses to a maximum dose of 1 mg daily.
    • Previously treated with oral corticosteroids:
      • 1 mg/day administered in one or two divided doses to a maximum daily dose of 1 mg daily.
    • According to the NIH Asthma Guidelines:

      • Children 0-4 years:
        • Low dose: 0.25-0.5 mg/day
        • Medium dose: 0.5 - 1 mg/day
        • High dose: more than 1 mg/day
      • Children 5-11 years:
        • Low dose: 0.5 mg/day
        • Medium dose: 1 mg/day
        • High dose: 2 mg/day

Use in the treatment of mild to moderate Crohn disease:

  • Manufacturer's labeling:
    • Children older than 8 years and Adolescents weighing more than 25 kgs:
      • 9 mg orally once a day of enteric coated capsule for up to 8 weeks then 6 mg once a day for 2 weeks
  • Alternate dosing:
    • Children older than 6 years and Adolescents:
      • Induction: 9 mg orally once a day of enteric coated capsule or in divided doses three times a day for 7 to 8 weeks
      • Maintenance dose: 6 mg once a day for 3 - 4 weeks

Budesonide use in the treatment of Eosinophilic esophagitis: 

  • Children less than 10 years:
    • Viscous liquid or suspension (using the inhalational suspension):
      • 1 mg orally once a day or divided twice a day.
  • Children older than 10 years and Adolescents:
    • Viscous liquid or suspension (using inhalation suspension):
      • 2 mg orally once a day or divided twice a day.

Budesonide use in the treatment of Protein-losing enteropathy following Fontan:

  • Children older than 7 years and Adolescents:
    • Enteric coated capsule:
      • 9 mg orally once a day or in divided doses thrice a day
      • The dose may be reduced over several weeks to 3 mg once a day after clinical improvement and albumin of more than 3 gms/dL may
    • up to 6 mg has been used in studies.
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Pregnancy Risk Factor B (Inhalational use), C (oral capsules and tablets)

    • Steroids administered in the first trimester can cause adverse effects.
    • Steroids can influence fetal growth, causing neonatal hypoadrenalism.
    • Budesonide can be used to induce remission for pregnant women suffering from inflammatory bowel diseases.
Use of budesonide while breastfeeding
    • Budesonide can be absorbed into breastmilk.
    • It is important to weigh the benefits of maternal therapy and neonatal steroids exposure.
    • After the maternal administration of Budesonide, breastfeeding can be continued for up to 4 hours.
   

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Budesonide dose in Liver disease:

  • Oral capsule:
    • Mild hepatic impairment (Child-Pugh class A):
      • Dose adjustment is not necessary.
    • Moderate hepatic impairment (Child-Pugh class B):
      • Reduce the dose to 3 mg once a day.
      • Monitor for hypercortisolism.
    • Severe hepatic impairment (Child-Pugh class C):
      • Avoid using in severe liver disease.
  • Oral tablet:
    • Mild hepatic impairment:
      • Use with caution.
      • Adjustment in the dose is not recommended.
    • Moderate to severe hepatic impairment:
      • The manufacturer has not recommended any dose adjustment.
      • Monitor for clinical features of hypercortisolism
      • May consider discontinuing it.
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Common Side Effects of Budesonide Include:

  • Central Nervous System:
    • Headache
  • Dermatologic:
    • Acne Vulgaris
  • Endocrine & Metabolic:
    • Decreased Cortisol
    • Bruise
    • Moon Face
  • Gastrointestinal:
    • Nausea
  • Respiratory:
    • Respiratory Tract Infection

Less Common Side Effects Of Budesonide Include:

  • Cardiovascular:
    • Chest Pain
    • Edema
    • Facial Edema
    • Flushing
    • Hypertension
    • Palpitations
    • Tachycardia
  • Central Nervous System:
    • Dizziness
    • Fatigue
    • Agitation
    • Amnesia
    • Confusion
    • Drowsiness
    • Insomnia
    • Malaise
    • Nervousness
    • Paresthesia
    • Sleep Disorder
    • Vertigo
  • Dermatologic:
    • Alopecia
    • Dermatitis
    • Dermatological Disease
    • Diaphoresis
    • Eczema
  • Endocrine & Metabolic:
    • Hirsutism
    • Hypokalemia
    • Intermenstrual Bleeding
    • Menstrual Disease
    • Weight Gain
    • Adrenocortical Insufficiency
    • Redistribution Of Body Fat
  • Gastrointestinal:
    • Diarrhea
    • Dyspepsia
    • Anal Disease
    • Enteritis
    • Epigastric Pain
    • Exacerbation Of Crohn's Disease
    • Gastrointestinal Fistula
    • Glossitis
    • Hemorrhoids
    • Increased Appetite
    • Intestinal Obstruction
    • Oral Candidiasis
    • Upper Abdominal Pain
    • Flatulence
    • Abdominal Distention
    • Constipation
  • Genitourinary:
    • Urinary Tract Infection
    • Dysuria
    • Nocturia
    • Urinary Frequency
    • Hematuria
    • Pyuria
  • Hematologic & Oncologic:
    • Increase in C-reactive protein
    • Leukocytosis
    • Purpura
    • Abnormal Neutrophils
    • Anemia
    • Increased Erythrocyte Sedimentation Rate
  • Hepatic:
    • Increased Serum Alkaline Phosphatase
  • Hypersensitivity:
    • Tongue Edema
  • Infection:
    • Viral Infection
    • Abscess
  • Neuromuscular & Skeletal:
    • Ankle Edema
    • Arthralgia
    • Arthritis
    • Hyperkinesia
    • Muscle Cramps
    • Myalgia
    • Tremor
    • Weakness
  • Ophthalmic:
    • Eye Disease
    • Visual Disturbance
  • Otic:
    • Otic Infection
  • Respiratory:
    • Sinusitis
    • Bronchitis
    • Dyspnea
    • Flu-Like Symptoms
    • Pharyngeal Disease
    • Rhinitis
  • Miscellaneous:
    • Fever
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Contraindication to Budesonide Include:

 
  • Allergy to Budesonide or any other component of the formulation
  • Active tuberculosis
  • Local active infections, systemic or local (bacterial, fungal, or viral)
  • Hypersensitivity to peanuts, lecithin and soya.
Warnings and Precautions
  • Suppression of the adrenals:
    • High doses of budesonide can cause adrenal suppression in children and patients who are young.
    • Corticosteroids must be reduced slowly to avoid adrenal crises.
    • Patients who are switching from systemic to topical or inhaled formulations should be careful.
    • Patients who take systemic corticosteroids greater than 20 mg daily may be more vulnerable to adrenal suppression.
  • Anaphylactoid reactions
    • Anaphylactic reactions are rare but possible.
  • Immunosuppression:
    • Patients who have been taking corticosteroids for a long time are at greater risk of developing secondary infections, including fungal infections.
    • Response to inactivated and killed vaccines may be blunted.
    • Patients with herpes should avoid ocular administration.
    • Exposure to chickenpox and measles should be avoided.
    • Patients with cerebral malaria, fungal infections and viral hepatitis should avoid corticosteroids.
    • For patients with reactivated tuberculosis, it is important to monitor them.
    • Strongyloides and amebiasis patients should not be treated.
  • Kaposi Sarcoma:
    • Kaposi Sarcoma can be caused by prolonged corticosteroids use.
  • Myopathy
    • Acute myopathy can result in weakness of the respiratory, ocular and limb muscles.
    • You should monitor Creatine Kinase.
  • Psychiatric disorders:
    • Some patients may experience psychiatric disturbances such as mood swings and euphoria, insomnia, personality changes, depression, or psychotic manifestations.
    • It is possible for pre-existing psychiatric disorders to worsen by its use.
  • Cardiovascular disease
    • Hypertension, fluid retention and hypernatremia can all be caused by corticosteroids.
    • Patients with acute myocardial infarction should avoid using steroids because of the risks of myocardial rupture.
  • Diabetes:
    • Patients with diabetes may experience a worsening of their glycemic condition if they take steroids.
  • Gastrointestinal Disease:
    • Steroids should be avoided in patients with diverticulitis and peptic ulcer disease.
  • Hepatic impairment
    • Patients suffering from advanced liver disease should not use it.
    • People with mild or moderate hepatic impairment may need to reduce their dose.
    • Hypercortisolism and fluid retention should be closely monitored.
  • Myasthenia gravis:
    • Patients who are taking steroids for myasthenia Gravis may feel more weak.
  • Ocular disease:
    • It should be used with caution in patients with cataracts and glaucoma as steroids may result in an elevation in the intraocular pressure.
  • Osteoporosis
    • Use of long-term medication can lead to bone loss and osteoporotic injuries.
  • Renal impairment
    • Patients with kidney disease may experience fluid retention.
  • Seizure disorders:
    • Steroids should be used with caution in patients with seizure disorders.
  • Thyroid disease:
    • Dose adjustment may be required in patients with thyroid disease.
    • Patients with hyperthyroidism have a higher clearance of corticosteroids and a lower clearance in those with hypothyroidism.

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Budesonide (systemic): Drug Interaction

Note: Drug Interaction Categories:
  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

    Risk Factor C (Monitor therapy).

    Bile Acid Sequestrants Might decrease the absorption Corticosteroids (Oral)
    Clofazimine High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Coccidioides immitis Skin Test Coccidioides immitis Skin Test may be affected by immunosuppressants.
    Corticorelin Corticosteroids can reduce the therapeutic effects of Corticorelin. Recent or current corticosteroid treatment may affect plasma ACTH responses to Corticorelin.
    Deferasirox Corticosteroids can increase the toxic/adverse effects of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
    Denosumab Might increase the toxic/adverse effects of Immunosuppressants. In particular, there may be an increase in the risk of serious infections.
    Fosaprepitant High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Larotrectinib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Ocrelizumab May increase the immunosuppressive effects of Immunosuppressants.
    Palbociclib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Pidotimod Pidotimod's therapeutic effects may be diminished by immunosuppressants.
    Ritodrine Ritodrine's toxic/adverse effects may be amplified by corticosteroids.
    Simeprevir High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Siponimod Siponimod's immunosuppressive effects may be enhanced by taking immunosuppressants.
    Sipuleucel-T Sipuleucel T's therapeutic effects may be diminished by immunosuppressants
    Tertomotide Tertomotide's therapeutic effects may be diminished by immunosuppressants.
    Trastuzumab May increase the neutropenic effects of Immunosuppressants.

    Risk Factor D (Consider therapy modifications)

    Antacids Could decrease the bioavailability (Oral) of Corticosteroids. Management: It is worth separating doses for at least 2 hours. Budesonide enteric-coated tablets may dissolve prematurely when combined with lower gastric acid drugs, which have unknown effects on the budesonide therapeutic benefits.
    Baricitinib Baricitinib's immunosuppressive effects may be enhanced by immunosuppressants. Baricitinib should not be used in combination with immunosuppressants like azathioprine and cyclosporine. It is permissible to use methotrexate antirheumatically or nonbiologic disease-modifying antirheumatic drug (DMARDs), concurrently.
    Echinacea Might decrease the therapeutic effects of Immunosuppressants.
    Fingolimod Fingolimod may be immunosuppressed by immunosuppressants. When possible, avoid the use of fingolimod with other immunosuppressants. Patients should be closely monitored for any additive immunosuppressant effects, such as infections, if they are used together.
    Hyaluronidase The therapeutic effects of Hyaluronidase may be diminished by corticosteroids. Management: Patients who are taking corticosteroids, especially at higher doses, may not have the desired clinical response to standard doses hyaluronidase. Higher doses of hyaluronidase might be necessary.
    Leflunomide Leflunomide's toxic/adverse effects may be exacerbated by immunosuppressants. The risk of hematologic toxicities such as pancytopenia and agranulocytosis may increase. Patients on immunosuppressants should not be given a leflunomide loading dosage. Patients who are receiving leflunomide or another immunosuppressant must be checked for bone marrow suppression at minimum monthly.
    Nivolumab Nivolumab's therapeutic effects may be diminished by immunosuppressants.
    Roflumilast May increase the immunosuppressive effects of Immunosuppressants.
    Stiripentol High risk of Inhibitors causing an increase in serum concentrations of CYP3A4 substrates. Management: Avoid stiripentol use with CYP3A4 Substrates that have a narrow therapeutic Index. This is to avoid adverse effects and toxicities. Monitoring of any CYP3A4 substrate that is used with stiripentol should be closely done.
    Tofacitinib Tofacitinib's immunosuppressive effects may be enhanced by immunosuppressants. Management: It is permissible to use methotrexate (or nonbiologic disease-modifying antirheumatic drug (DMARDs), concurrently with methotrexate. This warning appears to be particularly targeted at more potent immunosuppressants.
    Vaccines (Inactivated) Immunosuppressants can reduce the therapeutic effects of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. All age-appropriate vaccines must be completed at least two weeks before you start an immunosuppressant. Re-vaccinate anyone who was vaccinated while on immunosuppressant therapy.

    Risk Factor X (Avoid Combination)

    Aldesleukin Aldesleukin's antineoplastic effects may be diminished by corticosteroids.
    BCG (Intravesical). The therapeutic effects of BCG (Intravesical) may be diminished by immunosuppressants
    Cladribine May increase the immunosuppressive effects of Immunosuppressants.
    Conivaptan High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Moderate CYP3A4 inhibitors Might increase serum Budesonide (Systemic) concentrations
    Strong CYP3A4 inhibitors Might increase serum Budesonide (Systemic) concentrations
    Fusidic Acid (Systemic). High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Grapefruit Juice Might increase serum Budesonide (Systemic) concentrations
    Idelalisib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
    Natalizumab Natalizumab's toxic/adverse effects may be exacerbated by immunosuppressants. Particularly, concurrent infections may increase.
    Pimecrolimus May increase the toxic/adverse effects of Immunosuppressants
    Tacrolimus (Topical) May increase the toxic/adverse effects of Immunosuppressants
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Monitor:

  • Serum glucose
  • Serum electrolytes
  • Blood pressure
  • Weight
  • If the drug is administered for more than 6 weeks, monitor:
    • Monitor intraocular pressure
    • Bone mineral density
    • Assess for the suppression of hypothalamic-pituitary axis with ACTH stimulation test, morning plasma cortisol test and urinary free cortisol test.
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How to take Budesonide?

Oral administration:
  • Capsule:
    • Take the drug in the morning without regard to meals. The capsule should be swallowed whole and should not be crushed or chewed.
    • The contents of the capsule may be sprinkled on applesauce and swallowed without chewing.
    • It should not be stored after mixing with the applesauce and the patient should be asked to drink a glass of cool water following its intake.
  • Tablet:
    • It should be swallowed whole, should not be crushed, chewed, or broken.
    • Administer without regard to meals in the morning.
  • Viscous liquid and suspension:
    • Swallow the liquid immediately after preparation
    • After its administration, avoid ingesting any solid or liquid food for at least half an hour.
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Mechanism of action of Budesonide:

Budesonide, a topical glucocorticoid of high potency with few systemic side effects, is highly effective. It suppresses endogenous mediators of inflammation and exerts anti-inflammatory properties. Oral administration can be used to release PH-dependent substances at the target site. It is effective in treating inflammatory bowel diseases. The controlled-release capsule is made up of enteric-coated powdered granules. They dissolve at pH greater than 5.5. It delivers the drug to your ileum and ascending colon. Multi-matrix enteric coated tablets dissolve at pH greater than 7. They deliver budesonide throughout the colon. It is 85 - 90% Protein-bound and is metabolized in the liver via CYP 3A4 to inactive metabolites. The oral tablet goes through extensive first-pass metabolism. It has a half-life eliminationAfter intravenous administration of approximately 1.9 hours for children and adolescents, and 2 – 3.6 hours for adults. Time to get therepeak plasma concentrationChildren and adolescents take approximately 5 hours to digest the tablets, while adults take 0.5-10 hours. Extended-release tablets last 13+/- hours. It is excreted primarily in the urine.

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International Brands:

  • Budenofalk
  • Budeson 3
  • Budeson 9
  • Cortiment
  • Cycortide
  • Entocir
  • Entocort
  • Zentacort
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Budesonide Brand Names in Pakistan:

Budesonide Inhaler 100 mcg in Pakistan

Budeform Hfa Highnoon Laboratories Ltd.

Budesonide Inhaler 200 mcg in Pakistan

Budeform Hfa Highnoon Laboratories Ltd.

Budesonide Inhaler 50 mcg/actu in Pakistan

Pulmicort Barrett Hodgson Pakistan (Pvt) Ltd.

Budesonide Inhaler 200 mcg/actu in Pakistan

Pulmicort Barrett Hodgson Pakistan (Pvt) Ltd.
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