budesonide inhaled (Rx)

>10%

Respiratory infection (34-38%)

Rhinitis (7-12%)

Otitis media (1-12%)

1-10%

Nasopharyngitis (10%)

Nasal congestion (3%)

Pharyngitis (3%)

Allergic rhinitis (2%)

Viral gastroenteritis (2%)

Viral upper respiratory tract infection (2%)

Oral candidiasis (1%)

Contraindications

Hypersensitivity

Status asthmaticus, acute bronchospasm

Cautions

Respiratory tract tuberculosis, untreated fungal or bacterial infections, viral or parasitic infections, ocular herpes simplex

Risk of more serious or fatal course of chickenpox or measles in susceptible patients (eg, unvaccinated or immunologically unexposed individuals); care must be taken to avoid exposure

Localized infections with Candida albicans in mouth and pharynx in some patients; mouth must be rinsed after inhalation to reduce risk

Deaths from adrenal insufficiency have occurred after abrupt withdrawal of oral steroids; taper withdrawal gradually

Potential decrease in growth velocity in children

Immunocompromised patients

Hepatic impairment

Risk of infections of nose and pharynx, including C albicans

Decrease in bone mineral density after long-term administration of corticosteroids; monitor patients at risk

Excessive use may suppress hypothalamic-pituitary-adrenal function; monitor closely, especially postoperatively or during periods of stress

During periods of stress or severe status asthmaticus, supplementary systemic corticosteroids may be immediately required

Not to be administered for rapid relief of acute bronchospasm (agent is not a bronchodilator)

Nasal septum perforation, wheezing

Cataracts, glaucoma, increased intraocular pressure

Risk of systemic eosinophilic conditions, some consistent with Churg-Strauss syndrome

Pregnancy

There are no adequate well-controlled studies in pregnant women; however, there are published studies on use of budesonide, in pregnant women; studies of pregnant women have not shown that inhaled budesonide increases risk of abnormalities when administered during pregnancy

There are no well-controlled human studies that have investigated effects of therapy during labor and delivery

Animal data

• In animal reproduction studies, therapy, administered by subcutaneous route, caused structural abnormalities, was embryocidal, and reduced fetal weights in rats and rabbits at less than maximum recommended human daily inhalation dose (MRHDID), but these effects were not seen in rats that received inhaled doses approximately 2 times the MRHDID; experience with oral corticosteroids suggests that rodents are more prone to structural abnormalities from corticosteroid exposure than humans
• In women with poorly or moderately controlled asthma, there is increased risk of several perinatal adverse outcomes such as preeclampsia in the mother and prematurity, low birth weight, and small for gestational age in neonate; pregnant women with asthma should be closely monitored and medication adjusted as necessary to maintain optimal asthma control

Lactation

There are no available data on effects of therapy on breastfed child or on milk production; budesonide, is present in human milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Anti-inflammatory corticosteroid; has potent glucocorticoid activity and weak mineralocorticoid activity

Absorption

Bioavailability: 6-13%

Onset: 24 hr to 2 wk

Peak plasma time: 1-2 hr

Distribution

Protein bound: 85-90%

Vd: 3 L/kg

Metabolism

Metabolized in liver by CYP3A4

Metabolites: 16-Alpha hydroxyprednisolone, 6-beta hydroxybudesonide

Elimination

Half-life: 2-3 hr

Excretion: Urine (60%), feces (40%)