Trade Names:Entocort EC- Capsules 3 mg (micronized)
Trade Names:Pulmicort Flexhaler- Inhalation powder 180 mcg- Inhalation powder 90 mcg
Trade Names:Pulmicort Respules- Inhalation suspension 0.25 mg per 2 mL- Inhalation suspension 0.5 mg per 2 mL- Inhalation suspension 1 mg per 2 mL
Trade Names:Rhinocort Aqua- Nasal spray 32 mcg/sprayEntocort Capsules (Canada)Gen-Budesonide AQ (Canada)Pulmicort Nebuamp (Canada)Rhinocort Turbuhaler (Canada)
Exhibits wide range of inhibitory activities against multiple cell types and mediators involved in allergic-mediated inflammation.
T max is 1 to 2 h. Absolute bioavailability is 6% to 13%.Oral inhalation (powder)
34% systemically available from lungs. T max is within 10 min. Absolute bioavailability is 39%.Intranasal
About 34% reaches systemic circulation. T max is about 0.7 h.
Vd is 2 to 3 L/kg (or 200 L). Budesonide is 85% to 90% protein bound.
Rapidly metabolized; CYP3A4 is involved in the formation of 2 metabolites (less than 1% of budesonide activity).
The t ½ is 2 to 3 h. Budesonide is excreted in the urine (about 60%) and feces as metabolites; no unchanged drug is detected in the urine.
Doubled systemic availability after oral ingestion.Children
Plasma half-life is shorter than in adults.
Management of seasonal and perennial allergic rhinitis symptoms in adults and children.Oral inhalation
For the maintenance treatment of asthma as prophylactic therapy in adults and children and for patients requiring oral corticosteroid therapy for asthma.Inhalation suspension
Maintenance treatment of asthma and prophylactic therapy in children 12 mo to 8 yr of age.Oral capsule
Untreated localized infections involving the nasal mucosa; relief of acute bronchospasm; primary treatment of status asthmaticus or other acute episodes of asthma when intensive measures are required; hypersensitivity to the drug or any component of the product. Not recommended for treatment of nonallergic rhinitis because of lack of data.
Spray Start with 64 mcg/day administered as 1 spray in each nostril daily.Maintenance
Spray Titrate to minimum effective dose (max, 256 mcg/day administered as 4 sprays in each nostril daily).Adults and Children 6 to younger than 12 yr of age
Spray Start with 64 mcg/day administered as 1 spray in each nostril daily.Maintenance
Spray Titrate to minimum effective dose (max, 128 mcg/day administered as 2 sprays in each nostril daily).Aerosol, FlexhalerAdults
Oral inhaler 360 mcg twice daily (max, 720 mcg twice daily).Children at least 6 yr of age
Oral inhaler 180 mcg twice daily (max, 360 mcg twice daily).RespulesChildren 12 mo to 8 yr of age
Inhalation suspension Administer by inhaled route via jet nebulizer connected to air compressor.Children receiving bronchodilators alone
0.5 mg/day administered daily or twice daily in divided doses (max, 0.5 mg/day).Children receiving inhaled corticosteroids
0.5 mg/day administered daily or twice daily in divided doses (max, 1 mg/day).Children receiving oral corticosteroids
1 mg/day administered as 0.5 mg twice daily or 1 mg daily (max, 1 mg/day).Oral CapsulesAdults
PO 9 mg daily in the morning for up to 8 wk (Crohn disease); can be tapered to 6 mg daily for up to 3 mo for maintenance of clinical remission.
Store nasal spray at 68° to 77°F with the valve up. Protect from freezing and light. Discard bottle when labeled number of sprays have been used, even if bottle is not completely empty.Aerosol, Flexhaler
Store at 68° to 77°F. Keep tightly capped.Respules
Store unused ampules in upright position in protective foil pouch at 68° to 77°F. Protect from light. Do not refrigerate or freeze. After opening foil pouch, return unused ampules to pouch to protect from light. Unused ampules must be used within 14 days after pouch has been opened.Oral Capsules
Store capsules at ambient room temperature (59° to 86°F).
May increase budesonide plasma levels, increasing the pharmacologic and adverse effects.
None well documented.
Hypertension, migraine, palpitations, syncope, tachycardia (less than 5%).Nasal
Dizziness, fatigue, headache (at least 3%); agitation, amnesia, anorexia, dysphonia, increased appetite, asthenia, emotional lability, hyperkinesias, hypertonia, insomnia, malaise, nervousness, paresthesia, sleep disorder, somnolence, tremor, vertigo (less than 5%); depression, aggressive reactions, irritability, anxiety, psychosis (postmarketing).
Hirsutism, rash (at least 3%); acne, alopecia, dermatitis, eczema, flushing, purpura, pustular rash, pruritus, skin disorder, skin striae, increased sweating (less than 5%).
Conjunctivitis, ear infection, epistaxis, nasopharyngitis, nasal congestion, otitis media, pharyngitis, rhinitis (at least 3%); earache, eye abnormality, eye infection, abnormal vision, pharynx disorder (less than 5%); glaucoma, cataracts (postmarketing).Nasal
Epistaxis, nasal irritation, pharyngitis (at least 2%); pharynx disorders (eg, throat irritation, burning, itching), loss of smell, septum perforation (postmarketing).
Abdominal pain, oral candidiasis, diarrhea, dyspepsia, flatulence, gastroenteritis, nausea, vomiting (at least 3%); anus disorder, Crohn disease, aggravated enteritis, epigastric pain, GI fistula, glossitis, hemorrhoids, intestinal obstruction, dry mouth, taste perversion, tongue edema, tooth disorder (less than 5%).
Dysuria, intermenstrual bleeding, menstrual disorder, micturition frequency, nocturia, UTI (less than 5%).
Cervical lymphadenopathy, ecchymosis, leukocytosis (less than 5%).
Hypokalemia, anemia, hematuria, pyuria, increased erythrocyte sedimentation rate, increased alkaline phosphatase, increased atypical neutrophils, adrenal insufficiency (at least 1%).
Contact dermatitis (less than 5%).
Hypokalemia, weight increase (less than 5%).
Arthralgia, back pain (at least 3%); aggravated arthritis, cramps, fracture, myalgia, neck pain (less than 5%); avascular necrosis of the femoral head, osteoporosis (postmarketing).
Coughing, respiratory infection, sinusitis (at least 3%); bronchitis, bronchospasm, dyspnea, stridor (less than 5%); wheezing (postmarketing).Nasal
Coughing (at least 2%).
Fever, flu syndrome, moniliasis, moon face, pain, swollen ankles, viral infection, voice changes (at least 3%); abscess, allergic reaction, buffalo hump, increased C-reactive protein, chest pain, dependent edema, face edema, herpes simplex, oral candidiasis (less than 5%); angioedema, intracranial hypertension, symptoms of hypocorticism and hypersensitivity reactions (postmarketing).Nasal
Document disease state activity and/or symptoms before starting therapy and periodically during treatment. Notify health care provider if symptoms do not improve or worsen. Ensure that therapy is periodically reviewed to determine if it needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated. Monitor patients being weaned from oral to inhalation for signs and symptoms of adrenal insufficiency (fatigue, lassitude, weakness, hypotension). Monitor growth velocity in children.
Category B (inhalation). Category C (oral, intranasal).
Not recommended for children younger than 6 yr of age (intranasal, oral inhaler) or younger than 12 mo of age (respules); safety and efficacy not established in children for Entocort EC . Corticosteroids may suppress growth in children and adolescents, particularly with higher doses over extended periods. Plot growth in children on prolonged therapy. Inform health care provider if abnormalities noted.
Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function and comorbidity.
Immediate hypersensitivity reactions have occurred.
Use with caution in patients with tuberculosis infection, hypertension, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, with a family history of diabetes or glaucoma, renal or hepatic impairment, or with any condition in which glucocorticoids may have unwanted effects. Use inhaled corticosteroids with caution in patients with active or quiescent tuberculosis infection; untreated systemic fungal, bacterial, parasitic, or viral infections; or ocular herpes simplex.
Not for rapid relief of acute episodes of asthma or bronchospasm.
Transfer of patients from systemic steroids therapy to inhalation therapy may unmask allergic conditions previously suppressed by systemic steroid therapy (eg, rhinitis).
Bronchospasm may occur with an immediate increase in wheezing following dosing, which may require immediate treatment with a fast-acting inhaled bronchodilator.
Antifungal treatment or discontinuation of corticosteroid therapy may be necessary.
Patients receiving immunosuppressant agents are more susceptible to infections than healthy adults. If a patient is exposed to measles or chickenpox, appropriate prophylaxis and treatment may be indicated.
Flexhaler contains lactose. It is possible that cough, wheeze, or bronchospasm may occur in patients who have a severe milk protein allergy.
Transfer from oral corticosteroids to inhaled corticosteroids has resulted in death caused by adrenal insufficiency related to a lower systemic availability. A number of months are required for recovery of hypothalamic-pituitary adrenal (HPA) axis suppression. Patients maintained on 20 mg or more prednisone daily may be at higher risk. During periods of stress or severe asthma attack, instruct patients who have been withdrawn from systemic corticosteroids to resume oral steroids immediately.
Use cautiously in patients taking daily or alternate-day steroid therapy; may increase likelihood of HPA suppression. Exceeding recommended dose may cause systemic effects.
Because of inhibitory effect of corticosteroids on wound healing, patients experiencing recent nasal septal ulcers, nasal surgery, or nasal trauma should not use nasal corticosteroids until healing has occurred.
Hypercorticoidism, adrenal suppression.
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