Budesonide

Registered South African indications:

• Inflammatory bowel disease

Contraindication

• Hypersensitivity to the active ingredient or any of its excipients
• Systemic infections
• Hepatic cirrhosis

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment (cap)
• Moderate to severe hepatic impairment (cap)
• Previous systemic glucocorticoid treatment
• Hypertension (cap)
• Diabetes mellitus or family history thereof (cap)
• Osteoporosis (cap)
• Peptic ulcer (cap)
• Glaucoma or family history thereof (cap)
• Cataracts (cap)
• Severe affective disorders or in first degree relative
• Previous steroid-induced psychosis
• High doses
• Prolonged periods
• Physiological stress
• Withdrawal phase
• Children
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• Chickenpox
• Measles
• Live vaccines
• Visual disturbance
• Concomitant treatment with ketoconazole
• Sucrase-isomaltase insufficiency
• Fructose intolerance
• Total lactase deficiency

Forms avail. in SA and covered in this monograph: cap, ene

Crohn's disease involving ileum and/or ascending colon - Mild to moderate

• Oral (cap): 9mg, dly in the morning; Treatment duration: 8 weeks

Full effect usually achieved in 2-4 weeks

Taper dose gradually to discontinue use

Ulcerative colitis involving rectum and sigmoid colon

• Rectal (ene): 2.3mg, dly at night; Treatment duration: 4-8 weeks

Full effect usually achieved in 2-4 weeks

See additional prescribing points for administration directions

Not established for use in children

Pregnancy

• Caution
• The ability of corticosteroids to cross the placenta varies between individual medicines, however, in mice, budesonide and/or its metabolites have been shown to cross the placenta. In pregnant animals, administration of budesonide, like other glucocorticosteroids, is associated with abnormalities in foetal development including cleft palate, intra-uterine growth retardation and effects on brain growth and development. There is no evidence that corticosteroids result in an increased incidence of congenital abnormalities, such as cleft palate/lip in humans. However, when administered for prolonged periods or repeatedly during pregnancy, corticosteroids may increase the risk of intra-uterine growth retardation
• Hypoadrenalism may, in theory, occur in the neonate following prenatal exposure to corticosteroids but usually resolves spontaneously following birth and is rarely clinically important. When corticosteroids are essential, however, patients with normal pregnancies may be treated as though they were in the non-gravid state. As with other medicines the administration of oral and rectal budesonide during pregnancy requires that the benefits for the mother are weighed against the risk for the foetus

Breastfeeding

• Caution
• Budesonide is excreted in breast milk.  Maintenance treatment with inhaled budesonide (200 or 400μg twice daily) in asthmatic nursing women results in negligible systemic exposure to budesonide in breastfed infants. In a pharmacokinetic study, the estimated daily infant dose was 0.3% of the daily maternal dose for both dose levels, and the average plasma concentration in infants was estimated to be 1/600th of the concentrations observed in maternal plasma, assuming complete infant oral bioavailability. Budesonide concentrations in infant plasma samples were all less than the limit of quantification
• Based on data from inhaled budesonide and the fact that budesonide exhibits linear PK properties within the therapeutic dosage intervals after inhaled, oral and rectal administrations, at therapeutic doses of budesonide, exposure to the suckling child is anticipated to be low. Infants of mothers taking higher than recommended doses of budesonide may have a degree of adrenal suppression. This data supports the continued use of budesonide, oral and rectal administrations, during breastfeeding

Fertility

• There is no data on the effect of budesonide on human fertility. Fertility was unaffected following budesonide treatment in animal studies

Renal Impairment

• Oral (cap): Caution; no dose adjustment recommended
• Rectal (ene): No dose adjustment recommended

Hepatic Impairment

• Oral (cap): Mild: No dose adjustment recommended
• Oral (cap): Moderate to severe: Caution; dose adjustment recommended
  Moderate: Reduce dose to 3mg, once daily
  Severe: Avoid use
• Rectal (ene): No dose adjustment recommended

Elderly

• No dose adjustment recommended 

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Prohibited - In competition

Central Nervous System Disorders

• Nervousness
• Insomnia
• Mood swings 
• Depression
• Anxiety
• Aggression
• Tremor
• Psychomotor hyperactivity

Cardiovascular Disorders

• Palpitations

Gastrointestinal Disorders 

• Dyspepsia
• Flatulence (ene)
• Nausea (ene)
• Diarrhoea (ene)
• Duodenal or gastric ulcer (ene)

Genitourinary Disorders

• Menstrual disorders

Endocrine and Metabolic Disorders

• Cushingoid features
• Growth retardation
• Hypokalemia

Musculoskeletal Disorders

• Muscle cramps
• Osteonecrosis

Skin and Subcutaneous Tissue Disorders

• Urticaria
• Exanthema
• Ecchymosis

Sensory Disorders

• Blurred vision
• Glaucoma
• Cataract

Immune, Blood and Lymphatic System Disorders

• Anaphylactic reactions

• Antacids
• Cimetidine
• Cholestyramine
• CYP3A4 inhibitors
• CYP3A4 inducers  
• Digoxin
• Diuretics

None routine. Specific cases may require

• Growth (children)
• Adrenocortical function
• Blood glucose
• Hepatic Transaminsese (ALT, AST)

Administration directions
Enema

• Place tablet into bottle
• Shake bottle until tablet dissolved
• Remove protective cover
• Insert the rectal pipe into the anus and squeeze out the contents of the bottle as fully as possible
• Roll over onto your stomach and remain like that for 5 minutes. Then choose a comfortable sleeping position. The enema should remain in the intestine for as long as possible, preferably overnight

Budesonide is a glucocorticosteroid with a high local anti-inflammatory effect. It produces its anti-inflammatory effect by inhibition of inflammatory mediator release and inhibition of cytokine mediated immune response.

Capsule 3mg

• Entocord (Equity) Originator

Enema (per 100ml) 2mg

• Entocord 0.02mg/ml (Equity) Originator

Also available in the following forms: Inhaler, turbuhaler, novoliser, nebuliser suspension and nasal spray.