BUDESONIDE FORMOTEROL (Symbicort): What is used for?

What is Budesonide and Formoterol?

Budesonide and Formoterol (inhalation) is an active ingredient used for treatment of pseudo croup, bronchial asthma and COPD.

The brand name of Budesonide and Formoterol (inhalation) in United States is Symbicort.

Budesonide formoterol Mechanism of Action (MOA)

Local anti-inflammatory, inhibits the release of inflammatory mediators and the cytokine mediated immune response.

Therapeutic indications, uses and benefits of Budesonide and Formoterol

Maintenance treatment for underlying airway inflammation in bronchial asthma and COPD.
Treatment of very severe pseudo croup (subglottic laryngitis) in which hospitalization is indicated.

Dosage of Budesonide/Formoterol

INHALATION ROUTE: Formoterol fumarate (4.5 ug/1) + Budesonide (160 ug/1), Formoterol fumarate (4.5 ug/1) + Budesonide (80 ug/1), Budesonide (100 mcg) + Formoterol fumarate (6 mcg), Formoterol fumarate (6 mcg) + Budesonide (200 mcg), Formoterol fumarate (12 mcg) + Budesonide (400 mcg).

– Nebulizer suspension: at the onset of glucocorticoid therapy, periods of severe asthma, reduction or discontinuation of oral glucocorticoids.

Adults, the elderly and children > 12 years: 0.5-2 mg/day, maximum 4 mg/day.
Children > 6 months: 0.25-1 mg/day, maximum 2 mg/day.
Maintenance, adults, the elderly and children > 12 years: 0.5-4 mg/day; Children > 6 months: 0.25-2 mg/day.
Administer 1 or 2 times/day, consider 1 time/day in mild-moderate stable asthma with maintenance 0.25-1 mg/day.

Pseudo croup in infants and children: 2 mg/day or in 2 doses 30 minutes apart. If there is no improvement, the dosage can be repeated every 12 hours, maximum every 36 hours.

– Suspension for inhalation.
Adults and the elderly: 200-1,600 mcg/day.
Children > 7 years: 200-800 mcg/day.
Children 2-7 years: 200-400 mcg/day.
Daily dose divided into 2-4 administrations.

– Solution for inhalation: 200 mcg 2 times/day.
In period of severe asthma up to 1,600 mcg/day.
Well controlled patients: 200 mcg/day.

– Inhalation powder. Bronchial asthma, initial:
Adults and the elderly: Not previously treated or treated with inhaled glucocorticoids 200-400 mcg/24 hours, or 100-400 mcg/12 hours. Maximum dose 800 mcg/12 hours.
Adults and the elderly: Treated with oral glucocorticoids 400-800 mcg/12 hours. Maximum dose 800 mcg/12 hours.
Children > 6 years: Not previously treated or treated with inhaled glucocorticoids 200-400 mcg/24 hours, or 100-200 mcg/12 hours. Maximum dose 400 mcg.
Children > 6 years: Treated with oral glucocorticoids 200-400 mcg/12 hours. Maximum dose 400 mcg.

Maintenance, adults and the elderly: 100-1,600 mcg/day.
Children: 100-800 mcg/day.
Administer 1 or 2 times/day, consider 1 time/day with maintenance 100-400 mcg/day.
COPD: 400 mcg/12 h.
Adjust dose to minimum effective and, in general, in maintenance treatment with oral glucocorticoids, use inhaled therapy together 7-10 days, then gradually reduce the oral dose, if possible until complete withdrawal.

Mode of administration 

After each administration it is convenient to rinse the mouth with water and then spit out the rinse water.

Contraindications of Budesonide Formoterol 

  • Hypersensitivity.
  • Children under 6 years of age.
  • Active pulmonary tuberculosis.

Warnings and precautions with Budesonide Formoterol

  • Control and special care with pulmonary tuberculosis, and viral, fungal, or other respiratory tract infection.
  • Bronchiectasis and pneumoconiosis.
  • Severe hepatic insufficiency, monitor adrenocortical pituitary hypothalamic axis function.
  • To monitor possible alteration of adrenal function in the change from oral to inhaled corticoid, in subjects who required emergency treatment with parenteral corticoid at high doses, or in inhaled treatment at high doses for long periods.
  • Possible need for additional oral corticosteroid treatment in situations of severe stress or elective surgery.
  • Risk of paradoxical bronchospasm.
  • Long-term high doses increase risk of systemic effects: s. Cushing’s, cushingoid characteristics, inhibition of adrenal function, growth retardation in children and adolescents (growth monitoring), decreased bone mineral density, cataracts, glaucoma, and psychological and behavioral effects particularly in children.
  • Avoid concomitance with ketoconazole, itraconazole, ritonavir or other potent CYP3A4 inhibitors (azolic antifungals, protease inhibitors, macrolide antibiotics, amiodarone), if spacing is not possible.
  • Rinse mouth with water after administration to reduce risk of oropharyngeal candidiasis.
  • Not indicated for dyspnea or acute episodes but as a long-term treatment.
  • Do not stop treatment abruptly (after 10 days reduce daily dose gradually).
  • In case of worsening, re-evaluate the patient and consider increasing the dose and frequency of daily use as needed.
  • Respiratory disease with COPD component due to increased risk of pneumonia.
  • Risk of visual alterations such as blurred vision, cataracts, glaucoma or central serous chorioretinopathy (CRSC).
  • In addition, in COPD: risk of pneumonia (take into account other factors such as smoking, advanced age, low BMI and severity of COPD).

Liver failure

Caution with severe liver failure, risk of systemic effects, monitor adrenocortical pituitary hypothalamic axis function.

Interactions with Budesonide 

  • Increased metabolism and reduced systemic exposure by: potent CYP3A4 inducers (e.g. rifampicin), not known to affect lung exposure.
  • ACTH stimulation test for diagnosis of pituitary insufficiency may show false positives (lower values).

Pregnancy and Budesonide Formoterol

Evaluate benefit/risk.
The results of an extensive prospective epidemiological study and extensive post-authorization experience indicate that budesonide inhaled during pregnancy has no adverse effects on the health of the fetus and the newborn.

Breastfeeding

Budesonide passes into breast milk. However, at therapeutic doses no effect on the infant is expected.
Budesonide can be used during lactation. Maintenance treatment with inhaled budesonide (200 or 400 micrograms twice daily) in lactating asthmatic women results in systemic exposure to negligible budesonide in lactating children. In a pharmacokinetic study, the estimated daily dose in children 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 in children. Budesonide concentrations in children’s plasma samples were below the limit of quantification.

Based on data from inhaled budesonide and the fact that budesonide has linear FC properties within the therapeutic dose intervals after nasal, inhaled, oral and rectal administrations at the therapeutic dose of budesonide, it can be anticipated that infant exposure is low.

Adverse reactions and side effects of Budesonide Formoterol

  • Mild irritation of the throat and oral mucosa.
  • Dysphonia.
  • Difficulty swallowing.
  • Oropharyngeal candidiasis.
  • Hoarseness.
  • Cough.
  • Blurred vision.

⭐⭐⭐⭐⭐ VIDEO OF BUDESONIDE AND FORMOTEROL/SYMBICORT (DRUG)

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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