Budesonide

Updated on Nov 05, 2023

Edit

Comment

AHFS/Drugs.com Monograph Molar mass 430.534 g/mol		MedlinePlus a608007 CAS ID 51333-22-3

Trade names Pulmicort, Rhinocort, others Pregnancy category US: B (No risk in non-human studies) Routes of administration By mouth, nasal, tracheal, rectal ATC code A07EA06 (WHO) D07AC09 (WHO), R01AD05 (WHO), R03BA02 (WHO)

How to pronounce budesonide pulmicort memorizing pharmacology flashcard

Budesonide (BUD), sold under the brand name Pulmicort among others, is a medication of the corticosteroid type. It is available as an inhaler, pill, nasal spray, and rectal forms. The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease (COPD). The nasal spray is used for allergic rhinitis and nasal polyps. The pills in a delayed release form and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis and microscopic colitis.

Common side effects with the inhaled form include respiratory infections, cough, and headaches. Common side effects with the pills include feeling tired, vomiting, and joint pains. Serious side effects include an increased risk of infection, loss of bone strength, and cataracts. Long-term use of the pill form may cause adrenal insufficiency. Stopping the pills suddenly following long-term use may therefore be dangerous. The inhaled form is generally safe in pregnancy. Budesonide is mainly a glucocorticoid.

Budesonide was initially patented in 1973. Commercial use as an asthma medication began in 1981. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Some forms are available as a generic medication. The wholesale price in the developing world for an inhaler containing 200 doses is about 5 to 7 USD as of 2014. As of 2015 the cost for a typical month of medication in the United States is 100 to 200 USD.

How to pronounce budesonide formoterol symbicort memorizing pharmacology flashcard

Asthma

Budesonide is nebulized for maintenance and prophylactic treatment of asthma including patients who require oral corticosteroids and those who may benefit from a systemic dose reduction.

Inflammatory bowel disease

Formulations of delayed-release Budesonide can be effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon. A Cochrane review found evidence for up to 3 months (but not longer) of maintenance of remission Crohn's disease.

Budesonide assists in the induction of remission in people with active ulcerative colitis.

Allergic rhinitis

Nasal spray budesonide is a treatment for allergic rhinitis.

Side-effects

Budesonide may cause:

Nose irritation or burning

Bleeding or sores in the nose

Lightheadedness

Upset stomach

Cough

Hoarseness

Dry mouth

Rash

Sore throat

Bad taste in mouth

Change in mucus

In addition, the following symptoms should be reported immediately:

Difficulty breathing or swelling of the face

White patches in the throat, mouth, or nose

Irregular menstrual periods

Severe acne

On rare occasions, behavioral changes (mostly affecting children)

Contraindications

Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required. It is also contraindicated for patients who have hypersensitivity to budesonide.

Mechanism of action

Budesonide:

Controls the rate of protein synthesis.

Depresses the migration of polymorphonuclear leukocytes and fibroblasts.

Reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation.

Has a potent glucocorticoid activity and weak mineralocorticoid activity.

Dietary considerations

Those taking tablets or capsules orally should avoid grapefruit juice and echinacea.

Grapefruit juice may double bioavailability of oral budesonide.

Echinacea diminishes bioavailability.

Also, high fat meals delay absorption but do not impede absorption.

Pharmacokinetics

Onset of action: Nebulization: 2–8 days; Inhalation: 24 hours

Peak effect: Nebulization: 4–6 weeks; Inhalation: 1–2 weeks

Distribution: 2.2-3.9 L/kg

Protein binding: 85% to 90%

Metabolism: Hepatic via CYP3A4 to two metabolites: 16 alpha-hydroxyprednisolone and 6 beta-hydroxybudesonide; minor activity

Bioavailability: Limited by high first-pass effect; Capsule: 9% to 21%; Nebulization: 6%; Inhalation: 6% to 13%

Half-life elimination: 2-3.6 hours

Time to peak: Capsule: 0.5–10 hours (variable in Crohn's disease); Nebulization: 10–30 minutes; Inhalation: 1–2 hours; Tablet: 7.4-19.2 hours

Excretion: Urine (60%) and feces as metabolites.

Brand names

Aeronide (TH); Aquacort (DE); B Cort (CO); Bronex (PH); Budair (MY); Budecort DP (MY); Budenofalk (DE, GB, HK, KP, PH, SG); Budeson (AR); Budeson Aqua (AR); BudeSpray (TH); Budiair (KP); Budicort Respules (IL); Bunase (TH); Clebudan (CN); Cycortide (HK); Denecort (PH); Duasma (TW); Eltair (MY); Entocort (AR, AT, BE, BR, CH, CZ, DK, FI, FR, GB, HK, IE, IL, IT, KP, NL, NO, PL, PT, SE, TR); Giona Easyhaler (MY, SG, TH); Inflammide (PE); Miflonid (CZ); Miflonide (BE, DE, IL, IT, NZ, PT); Neumocort (PY); Novopulmon (DE, FR); Pulmicon Susp for Nebulizer (KP); Pulmicort (AT, BE, BG, BR, CH, CL, CN, CO, CR, CZ, DE, DK, DO, EE, FI, FR, GB, GR, GT, HN, ID, IN, NI, NL, NO, PA, PK, PL, PT, RU, SE, SV, TR, TW, UY, VE, ZA); Pulmicort Nasal Turbohaler (CL, KE, MU, NG); Pulmicort Turbuhaler (KE, MU, NG); Rafton (FR); Rhinocort (AU); Rhinocort Aqua (HK); Rhinoside (GR); Symbicort (FR, US, ZA) Uceris (US)