BUDESONIDE (Pulmicort, Uceris): What is used for?

What is Budesonide?

Budesonide is an active ingredient used for the treatment of Crohn’s disease, autoimmune hepatitis, ulcerative colitis, active collagenous colitis.

The brand names of Budesonide in the United States are: Uceris, Pulmicort Turbuhaler, Pulmicort Flexhaler, Pulmicort Respules.

Budesonide Mechanism of Action (MOA)

Local anti-inflammatory glucocorticosteroid.
Inhibits the release of mediators of inflammation and immune responses mediated by cytokines.

Therapeutic Indications of Budesonide

Oral:

  • Induction of remission in patients with mild to moderate active Crohn’s disease with involvement of the ileum and/or ascending colon.
  • Induction of remission in patients with active collagenous colitis.
  • Autoimmune hepatitis.
  • In adults for induction of remission in patients with mild to moderate active ulcerative colitis (UC), where 5-ASA treatment is not sufficient.

Rectal:

  • Ulcerative colitis affecting the rectum and the sigmoid and descending colon.

Dosage of Budesonide

1) Oral:

– Induction of remission in patients with mild to moderate active Crohn’s disease with involvement of the ileum and/or ascending colon:

Adults > 18 years old, 9 mg once/day in the morning ½ time before breakfast (capsules or gastroresistant granulate) or 3 mg 3 times/day ½ time before meals (gastroresistant capsules) or adults and children ≥ 8 years old with body weight greater than 25 kg, 9 mg once/day in the morning (modified release capsules); maximum 8 weeks.

– Induction of remission in patients with active collagenous colitis.

Adults > 18 years: 3 mg 3 times/day ½ hour before meals (gastroresistant capsules) or 9 mg 1 time/day in the morning ½ hour before breakfast (gastroresistant granulate).

– Autoimmune hepatitis (gastro-resistant capsules).

Adults > 18 years: induction of remission, 3 mg 3 times/day ½ hour before meals until remission; maintenance: 3 mg 2 times/day, minimum 24 months, conclude if biochemical remission is maintained and there are no symptoms of inflammation in liver biopsy (if ALT and/or AST increase during maintenance treatment, increase dose to 3 mg 3 times/day); combine with azathioprine in patients with tolerance to it.

– In adults for induction of remission in patients with mild to moderate active ulcerative colitis (UC), where treatment with 5-ASA is not sufficient (prolonged release tablets).

Adults: 9 mg in the morning, up to 8 weeks.

2) Rectal:

Ulcerative colitis affecting the rectum and sigmoid and descending colon: 2 mg once/day before bedtime (rectal foam morning or night); maximum 8 weeks.

Mode of administration of Budesonide

Oral use: Capsules should be taken approximately ½ one hour before meals, whole and with plenty of liquid (e.g. a glass of water).
For children and adults with swallowing difficulties, the capsules can be opened and their contents swallowed after mixing with a tablespoon of applesauce. It is important that the contents of the capsules are not crushed or chewed.

The contents of 1 sachet should be taken before breakfast. The granules should be placed on the tongue and swallowed whole, with plenty of liquid (e.g. a glass of water). These granules should not be chewed or crushed to prevent destruction of the gastroresistant coating of the granules. Premature disintegration would affect the disposition of the drug in an unpredictable manner.

Take prolonged release tablets in the morning, with or without food. They should be swallowed with a glass of water and should not be broken, crushed or chewed, as the tablet coating is intended to ensure prolonged release.

Contraindications of Budesonide

Hypersensitivity.
Cirrhosis of the liver.

Warnings and Cautions with Budesonide

  • Limited experience in the elderly and children.
  • Kidney failure.
  • Liver failure.
  • Not indicated for patients with Crohn’s disease of the upper gastrointestinal tract.
  • Infections, tuberculosis, BPH, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma, cataracts or family history of diabetes or glaucoma.
  • Monitor bacterial, fungal, amoebic and viral infection for risk of worsening, especially chickenpox and measles.
  • Administer passive immunization with varicella-zoster immunoglobulin (IGVZ) to all non-immune exposed patients who receive systemic glucocorticosteroids or have received them in the previous 3 months (must be administered within 10 days following exposure to varicella).
  • Patients with compromised immune systems exposed to measles should receive normal immunoglobulin as soon as possible after exposure.
  • High doses over time may cause systemic corticosteroid effects (Cushing syndrome, adrenal suppression, growth retardation, decreased bone mineral density, cataracts, glaucoma, and psychiatric/behavioral effects.
  • When replacing systemic glucocorticoid of greater effect may cause adrenocortical suppression, monitor.
  • Suspend gradually.
  • Administer complementary systemic treatment with glucocorticoids in case of surgery or stress.
  • Increased exposure in concomitance with: ketoconazole or other CYP3A4 inhibitors and grapefruit juice, avoid.
  • Do not administer live vaccines.
  • In treatment of autoimmune hepatitis: monitor ALT and AST every 2 weeks during the first month and then at least every 3 months. Possible increase in systemic availability of budesonide in patients with advanced primary biliary cirrhosis (PBC) with liver cirrhosis.
  • Risk of visual disturbances such as blurred vision, cataracts, glaucoma, or central serous chorioretinopathy (CRSC); regularly monitor the stature of children under long-term or prolonged treatment.

Liver failure

Caution.
Increases systemic bioavailability of budesonide.

Kidney failure

Caution.

Interactions with Budesonide

  • Power action of: cardiac glycosides.
  • Increases excretion of K with: saluretic diuretics.
  • Increases risk of systemic adverse reactions with: CYP3A inhibitors (including cobicistat-containing drugs); assess risk/benefit.
  • Increased exposure with: ketoconazole, other CYP3A4 inhibitors (ritonavir, itraconazole, clarithromycin) and grapefruit juice; avoid.
  • Plasma levels decreased by: CYP3A4 inducers (carbamazepine and rifampicin); adjust dose.
  • Plasma levels increased with: CYP3A4 substrates (estrogens or oral contraceptives); dose adjustment.
  • Decrease in effect with: steroid binding compounds (cholestyramine, antacids), respect interval between doses of at least 2 hours.
  • Lab: the ACTH stimulation test for the diagnosis of pituitary insufficiency may show false + (lower values).

Pregnancy and Budesonide

In pregnant animals it is associated with anomalies in fetal development. Unknown relevance in humans, avoid.

Breastfeeding

Oral use:
Budesonide is excreted through breast milk (excretion data available after inhalation use). However, only minor effects are predictable in the infant after ingestion of oral budesonide administered within therapeutic limits.
A decision must be made whether to discontinue lactation or to discontinue/abstention with budesonide treatment after considering the benefit of lactation for the infant and the benefit of treatment for the mother.

Rectal route:
No information is available on the transition from budesonide to breast milk. Maintenance treatment with inhaled budesonide (200 or 400 micrograms twice daily) in lactating asthmatic women results in negligible system exposure for budesonide in lactating children.

In a pharmacokinetic study the estimated daily dose was 0.3% of the daily maternal dose for both dose levels, and the mean plasma concentration in children was estimated at 1/600 of the observed concentrations in maternal plasma, assuming complete oral bioavailability of the infant. Budesonide concentrations in infant plasma samples were below the limit of quantification.
Based on data from inhaled budesonide and the fact that it shows linear pharmacokinetic properties at therapeutic dose intervals after inhaled administration, exposure after oral and rectal administrations of budesonide to therapeutic doses is expected to be low in the infant.
These data support the continued use of budesonide, oral and rectal administration, during lactation.

Effects on driving ability

No studies have been conducted on the ability to drive and use machines. When driving vehicles or using machines it should be noted that dizziness or fatigue may occasionally occur,

Adverse reactions and side effects of Budesonide

Oral use:
Cushing syndrome (full moon face, trunk obesity, decreased glucose tolerance, diabetes mellitus, hypertension, sodium retention with edema, increased potassium excretion, inactivity or atrophy of the adrenal cortex, red striae, steroid acne, alterations in the secretion of sex hormones (amenorrhea, hirsutism or impotence). Dyspepsia; increased risk of infection. Muscle and joint pain, muscle weakness and cramps, osteoporosis; headache; depression, irritability, euphoria; allergic rash, petechiae, delayed wound healing, contact dermatitis.

Rectal use: burning and pain in the rectum.

Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).

In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.

Resources:

UNII: Q3OKS62Q6X
ChemIDplus
DrugPortal
NCI Thesaurus: C1027

 

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