budesonide (systemic)

REMS

3-mg Delayed-Release Capsules

Treatment of mild to moderate active Crohn’s disease involving ileum and/or ascending colon.

3-mg Delayed-Release Capsules

Maintenance of clinical remission for up to 3 mo of mild to moderate Crohn's disease involving ileum and/or ascending colon.

Uceris

Induction of remission of active mild to moderate ulcerative colitis.

Tarpeyo

Reduction in loss of kidney function in patients with primary immunoglobulin A nephropathy who are at risk for disease progression.

Eohilia

Eosinophilic esophagitis.

Action ⬆ ⬇

Has high local anti-inflammatory activity in the lumen of the GI tract, but is rapidly inactivated following absorption. Action in Crohn's disease and ulcerative colitis is primarily local. Modulates activity of B-cells in ileum to decrease production of galactose-deficient IgA1 antibodies, which cause IgA nephropathy. Inhibits effects of numerous mediators (e.g., mast cells, macrophages, histamine) of allergic response that could affect pathogenesis of eosinophilic esophagitis.

Therapeutic effects:

Improvement in symptoms/sequelae of Crohn’s disease.
Induction of remission of ulcerative colitis
Reduction in loss of kidney function.
Reduction in eosinophil count in esophageal tissue and reduction in dysphagia.

Pharmacokinetics ⬆ ⬇

Absorption: 9–21% absorbed following oral administration.

Distribution: Widely distributed to extravascular tissues.

Protein Binding: 85–90%.

Metabolism/Excretion: Rapidly and extensively metabolized during first pass hepatic metabolism by the CYP3A4 isoenzyme to inactive metabolites that are excreted in urine and feces.

Half-Life: 2.0–3.6 hr; Tarpeyo: 5–6.8 hr; Eohilia: 3.3 hr.

Time/Action Profile ⬆ ⬇

(improvement in symptoms of Crohn’s disease or induction of remission of ulcerative colitis)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Severe hepatic impairment;
Moderate hepatic impairment (Uceris only).

Use Cautiously in:

History of diabetes (or family history), tuberculosis, osteoporosis, hypertension, peptic ulcer, glaucoma (or family history), or cataracts (conditions may be exacerbated);
Stress, including surgery or infections—supplemental doses of corticosteroid may be needed;
Active untreated infections;
Immunosuppression;
Potential infections (may mask signs such as fever or inflammation);
Moderate hepatic impairment (3-mg delayed-release capsules and Tarpeyo only) (↓ dose of 3-mg delayed-release capsules);
OB: Use during pregnancy only if maternal benefit outweighs potential fetal risk;
Lactation: Use while breastfeeding only if maternal benefit outweighs potential risk to infant;
Pedi: Safety and effectiveness not established in children 18 yr (Tarpeyo and Uceris), 11 yr (Eohilia), and 8 yr (3-mg delayed-release capsules);
Geri: risk of adverse reactions in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, hypertension, palpitations, tachycardia

Derm: acne, easy bruising, hirsutism, alopecia, dermatitis, eczema, flushing, striae, sweating

EENT: abnormal vision, conjunctivitis

Endo: ADRENAL SUPPRESSION, hypokalemia

GI: nausea, abdominal pain, dyspepsia, erosive esophagitis, flatulence, vomiting

GU: dysuria, irregular menses, nocturia, urinary frequency

Hemat: leukocytosis

Metab: ↑appetite, weight gain

MS: back pain, cramps, myalgia

Neuro: headache, agitation, confusion, dizziness, drowsiness, fatigue, hyperkinesia, insomnia, malaise, nervousness, paresthesia, tremor, vertigo

Resp: bronchitis, dyspnea

Misc: infection, cushingoid appearance, flu-like syndrome, KAPOSI'S SARCOMA

Interactions ⬆ ⬇

Drug-drug:

CYP3A4 inhibitors, including ketoconazole, itraconazole, ritonavir, and erythromycin, may ↑ levels and the risk of toxicity; ↓ dose may be necessary.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness.

Grapefruit juice may ↑ levels and the risk of toxicity; avoid concurrent use.

Route/Dosage ⬆ ⬇

Treatment of Active Crohn's Disease

PO (Adults ): 3-mg delayed-release capsules: 9 mg once daily in the morning for up to 8 wk; recurring episodes of active disease can be treated with a repeat 8-wk course of therapy.
PO (Children ≥8 yr and >25 kg): 3-mg delayed-release capsules: 9 mg once daily in the morning for up to 8 wk; then 6 mg once daily in the morning for 2 wk.

Hepatic Impairment

(Adults ): Moderate hepatic impairment: 3 mg once daily in the morning.

Maintenance of Remission of Crohn's Disease

PO (Adults ): 3-mg delayed-release capsules: Following treatment of active disease and once patient's symptoms are controlled, continue treatment with 6 mg once daily for up to 3 mo. If symptom control maintained at 3 mo, dose should be tapered to complete discontinuation. Continuing treatment for >3 mo does not produce significant clinical benefit.

Hepatic Impairment

(Adults ): Moderate hepatic impairment: 3 mg once daily in the morning.

Induction of Remission of Ulcerative Colitis

PO (Adults ): Uceris: 9 mg once daily in the morning for up to 8 wk.

Reduction in Loss of Kidney Function Associated with Primary Immunoglobulin A Nephropathy

PO (Adults ): Tarpeyo: 16 mg once daily in the morning for 9 mo; then 8 mg once daily in the morning for 2 wk.

Eosinophilic Esophagitis

PO (Adults and Children ≥11 yr): Eohilia: 2 mg twice daily for 12 wk.

Availability ⬆ ⬇

(Generic available)

Delayed-release capsules: 3 mg
Delayed-release capsules (Tarpeyo): 4 mg
Extended-release tablets (Uceris): 9 mg
Orally disintegrating tablets (Jorveza): 1 mg
Oral suspension (Eohilia) cherry flavor: 2 mg/10 mL

Assessment ⬆ ⬇

Inflammatory Bowel Disease:Assess signs and symptoms of Crohn’s disease or ulcerative colitis (diarrhea, abdominal pain, fever, rectal bleeding) during therapy. Monitor frequency and consistency of bowel movements periodically during therapy
Eosinophilic Esophagitis:Monitor for signs and symptoms of exacerbation (heartburn, chest discomfort, regurgitation, sensation of something stuck in esophagus) during therapy.
Monitor for signs and symptoms of adrenal insufficiency (fatigue, weakness, nausea and vomiting, low BP); budesonide should be tapered more slowly.
Monitor for signs and symptoms of hypercorticism (moon face, buffalo hump, stretch marks, obesity, bruising, hyperglycemia, elevated BP) every 6 mo; temporary discontinuation, dose reduction, or slowed taper may be needed.
Assess for signs of infection (fever, chills, sore throat, wound that will not heal).
Assess for signs and symptoms of Kaposi's sarcoma (purple, red, or brown skin blotches on skin or inside the mouth) with long-term use.
Pedi: Evaluate growth of children periodically during therapy. Monitor linear growth and weight gain. Adjust doses accordingly.

Lab Test Considerations:

Monitor CBC, electrolytes, serum and urine glucose, and lipid panel routinely during therapy. May cause hyperglycemia, especially in persons with diabetes. May cause hypokalemia, hypocalcemia, hypernatremia. May ↓ WBC counts. May ↑ lipid values.
- May suppress reactions to allergy skin tests.
- Guaiac test stools. Promptly report presence of guaiac-positive stools.
- May ↓ uptake of thyroid ¹²³I or ¹³¹I.
- Periodic adrenal function tests may be ordered to assess degree of hypothalamic-pituitary-adrenal axis suppression in systemic and chronic topical therapy.
Monitor microalbuminuria and urine protein to creatinine ratio (UPCR) in IgA nephropathy.

Implementation ⬆ ⬇

Periods of stress, such as surgery, may require supplemental systemic corticosteroids.
- If dose is ordered daily or every other day, administer in the morning to coincide with the body's normal secretion of cortisol.
- Patients with mild to moderate Crohn’s disease may be switched from oral prednisolone without adrenal insufficiency by gradually decreasing prednisolone doses and adding budesonide.
PO: Administer once daily in the morning, not with grapefruit juice. Administer Tarpeyo at least 1 hr before a meal. Do not take Eohiliawith food or liquid at the time of ingestion. Ucerisshould be taken with a full glass of water without regard to food. DNC: Swallow capsules and extended-release tablets whole; do not open, crush, break, or chew. For patients unable to swallow capsules, generic delayed-release capsules can be opened and granules poured onto one tablespoonful of applesauce. Mix and consume entire contents within 30 min. Do not chew or crush. Follow with 8 oz of water.
Eohilia is available as an oral suspension in individual stick packs. Do not mix the suspension with food or liquid. Shake the stick pack for at least 10 sec before opening. To use, squeeze the stick pack from the bottom to the top directly into the mouth. Repeat 2–3 times until the stick pack is empty. Wait for at least 30 min to eat or drink after taking Eohilia. After 30 min, rinse mouth with water and spit out the contents without swallowing.

Patient/Family Teaching ⬆ ⬇

Educate patient on reason for budesonideand side effects. Instruct them to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose. Do not double doses. Do not share medication with others, even if they have similar symptoms; may be harmful. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
- Explain need for continued medical follow-up to assess effectiveness and possible side effects of medication. Periodic lab tests and eye exams may be needed.
- Stopping the medication suddenly may result in adrenal insufficiency (anorexia, nausea, weakness, fatigue, dyspnea, hypotension, hypoglycemia). If these signs appear, notify health care professional immediately. This can be life-threatening. Medical ID should be worn in case of emergencies.
- Advise patient to avoid grapefruit juice during therapy.
- Advise patient to notify health care professional of signs and symptoms of hypercorticism (acne; thicker or more hair on body and face; bruising easily; fatty pad or hump between shoulders [buffalo hump]; rounding of face [moon face]; pink or purple stretch marks on skin of abdomen, thighs, breasts, and arms; ankle swelling), adrenal suppression (tiredness, weakness, nausea and vomiting, low blood pressure), worsening of allergies (eczema, rhinitis), or infection (fever, chills, pain, feeling tired, aches, nausea and vomiting).
- May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Instruct patient to inform health care professional promptly if severe abdominal pain or tarry stools occur.
- Corticosteroids cause immunosuppression and may mask symptoms of infection. May worsen existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex. Notify health care professional immediately if exposed to chicken pox or measles.
- Caution patient to avoid vaccinations without first consulting health care professional.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications, especially St. John's wort.
- Advise parents that use may cause shortened stature.
- Instruct patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Hypoadrenalism may occur in infants born to mothers receiving corticosteroids during pregnancy. Observe infant for signs of hypoadrenalism (poor feeding, irritability, weakness, vomiting).

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Classifications ⬆ ⬇

Indications ⬆ ⬇