Budemet 100 (DPI)

Budemet 100 (DPI) Uses, Dosage, Side Effects, Food Interaction and all others data.

Budesonide and Formoterol have different mode of action and show additive effects in terms of reduction of asthma exacerbations. The specific properties of Budesonide and Formoterol allow the combination to be used both as maintenance and reliever therapy, and as maintenance treatment for asthma. Budesonide is a glucocorticosteroid which when inhaled has a rapid (within hours) and dose dependent anti-inflammatory action in the airways, resulting in reduced symptoms and fewer asthma exacerbations. Formoterol Fumarate Dihydrate is a long acting β2-adrenoreceptor agonist having rapid onset of action.

Budemet 100 (DPI)
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Budemet 100 (DPI)
Generic	Budesonide + Formoterol Dihydrate
Weight	100mcg + 6mcg
Type	Convicap Capsule
Therapeutic Class	Long-acting selective β2-adrenoceptor stimulants, Respiratory corticosteroids
Manufacturer	Incepta Pharmaceuticals Limited
Available Country	Bangladesh
Last Updated:	September 19, 2023 at 7:00 am

Uses

ASTHMA

Budesonide and Formoterol combination is used for the regular treatment of asthma where use of a combination (inhaled corticosteroid and long acting β2-agonist) is appropriate. This includes:

-patients who are not adequately controlled with inhaled corticosteroid therapy and as needed inhaled --short-acting β2-adrenoceptor agonists.

-patients who are already adequately controlled on regular separate long-acting β2-agonist and inhaled corticosteroid therapies.

COPD

Budesonide and Formoterol combination is used for the regular treatment of adult patients with moderate to severe chronic obstructive pulmonary disease (COPD) with frequent symptoms despite β2-agonist use and a history of exacerbations.

Budemet 100 (DPI) is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Allergies, Asthma, Chronic Obstructive Pulmonary Disease (COPD), Collagenous Colitis, Crohn's Disease (CD), Nasal Congestion, Oesophagitis, Eosinophilic, Polyps, Nasal, Pruritus, Rhinosinusitis, Ulcerative Colitis, Vasomotor Rhinitis, Corticosteroid-responsive dermatoses, Mild Crohn’s Disease, Moderate Crohn’s Disease

How Budemet 100 (DPI) works

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Dosage

Budemet 100 (DPI) dosage

Asthma:

There are two alternative dosage regimens for the treatment of asthma with Budesonide and Formoterol combination.

Budemet 100 & 200 Convicap maintenance and reliever therapy

Adults and adolescents (12 years and older) Maintenance dose: Budemet 100 & 200 Convicap twice daily

Reliever dose: 1 additional Convicap as needed in response to symptoms. If symptoms persist after a few minutes, an additional Convicap should be taken. Not more than 6 Convicaps should be taken on any single occasion. A total daily dose of more than 8 Convicaps is not normally needed, however, a total daily dose of up to 12 Convicaps can be used temporarily.

Children (4 years and older)

Maintenance dose: Budemet 100 Convicap once daily.

Reliever dose: 1 additional Convicap as needed in response to symptoms. If symptoms persist after a few minutes, an additional Convicap should be taken. Not more than 4 Convicaps should be taken on any single occasion. A total daily dose of more than 4 Convicaps is not normally needed, however, a total daily dose of up to 8 Convicaps could be used temporarily.

Budemet 100 & 200 Convicap maintenance therapy

Adults and adolescents (12 years and older)

Budemet 100 Convicap: 1-2 Convicaps once or twice daily

Maximum daily maintenance dose: 4 Convicaps (2 Convicaps twice daily).

Budemet 200 Convicap: 1-2 Convicaps once or twice daily. Maximum daily maintenance dose: 4 Convicaps.

( 2 Convicaps twice daily ).

During worsening of asthma the dose of Budemet 100 Convicap and Budemet 200 Convicap may temporarily be increased to a maximum of 4 Convicaps twice daily in adults.

Budemet 400 Convicap : 1 ConviCap once or twice daily. Maximum daily maintenance dose: 2 ConviCaps (1 ConviCap twice daily).

During the worsening of asthma the dose of Budemet 400 Convicap may temporarily be increased to a maximum of 2 Convicaps twice daily in adults.

Children (4 years and older)

Budemet 100 Convicap: 1-2 Convicaps twice daily. Maximum daily maintenance dose: 4 Convicaps

Budemet 200 Convicap: 1 Convicap twice daily. Maximum daily maintenance dose: 2 Convicaps.

COPD

Adults (40 years and older)

Budemet 200 Convicap: 2 Convicaps twice daily.

Maximum daily maintenance dose: 4 Convicaps

Budemet 400 Convicap: 1 Convicap twice daily.

Maximum daily maintenance dose: 2 Convicaps.

Side Effects

The most common drug related adverse reactions are pharmacologically predictable side effects of β2-agonist therapy, such as tremor and palpitations. Adverse events which have been associated with Budesonide and Formoterol are Palpitations, Candida infections in oropharynx, Headache, Tremor, Coughing, Hoarseness and Tachycardia.

Toxicity

Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression. In the case of overdose, reduce the dosage of corticosteroids temporarily.

A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.

Precaution

Treatment with Budesonide and Formoterol combination should not be initiated to treat a severe exacerbation or if patients have significantly worsening or acutely deteriorating asthma.

Interaction

Concomitant treatment with Ritonavir, Itraconazole, Ketoconazole or other potent CYP3A4 inhibitors should be avoided.

Volume of Distribution

The volume of distribution of budesonide is 2.2-3.9L/kg.

Elimination Route

Extended release oral capsules are 9-21% bioavailable. A 9mg dose reaches a C_max of 1.50±0.79ng/mL with a T_max of 2-8h and an AUC of 7.33ng*hr/mL. A high fat meal increases the T_max by 2.3h but otherwise does not affect the pharmacokinetics of budesonide.

180-360µg metered inhaled doses of budesonide are 34% deposited in the lungs, 39% bioavailable, and reach a C_max of 0.6-1.6nmol/L with a T_max of 10 minutes.

A 1mg nebulized dose is 6% bioavailable, reaching a C_max of 2.6nmol/L with a T_max of 20 minutes.

A 9mg oral extended release tablet reaches a C_max of 1.35±0.96ng/mL with a T_max of 13.3±5.9h and an AUC of 16.43±10.52ng*hr/mL.

Budesonide rectal foam 2mg twice daily has an AUC of 4.31ng*hr/mL.

Half Life

Budesonide has a plasma elimination half life of 2-3.6h. The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.

Clearance

Budesonide has a plasma clearance of 0.9-1.8L/min. The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min. The clearance in asthmatic children 4-6 years old is 0.5L/min.

Elimination Route

Approximately 60% of a budesonide dose is recovered in the urine as the major metabolites 6beta-hydroxybudesonide, 16alpha-hydroxyprednisolone, and their conjugates. No unchanged budesonide is recovered in urine.

Pregnancy & Breastfeeding use

Pregnancy: Budesonide and Formoterol combination should only be used in pregnancy if the potential benefits outweigh the potential risks to the foetus.

Lactation: Administration of Budesonide and Formoterol combination to women who are breastfeeding should only be considered if the expected benefit to the mother is greater than any possible risk to the child.

Contraindication

Hypersensitivity to Budesonide, Formoterol or to Lactose.

Special Warning

It is recommended that the height of children receiving prolonged treatment with inhaled corticosteroids is regularly monitored. If growth is slowed, therapy should be re evaluated with the aim of reducing the dose of inhaled corticosteroid. The benefits of the corticosteroid therapy and the possible risks of growth suppression must be carefully weighed. In addition consideration should be given to referring the patient to a paediatric respiratory specialist.

Acute Overdose

If glucocorticoids are used at excessive doses for prolonged periods, systemic glucocorticoid effects such as hypercorticism and adrenal suppression may occur.

Symptoms: Decreased motor activity, piloerection, generalised oedema. Management: Immediate gastric lavage or emesis followed by supportive and symptomatic treatment.