Медикаментозне лікування астми*

Drug

Form

Dosage

Comments

Children

Adults

Short-acting beta agonists

Albuterol

HFA: 90 mcg/puff

Same as adults

2 puffs every 4–6 hours as needed and 2 puffs 15–30 minutes before exercise

Albuterol is used mainly as a rescue drug.

It is not recommended for maintenance treatment.

Regular use indicates diminishing asthma control and need for additional drug.

MDI-DPI is as effective as nebulized therapy if patients can coordinate the inhalation maneuver using the spacer and holding chamber.

Nebulized albuterol can be mixed with other nebulizer solutions.

DPI: 90 mcg/puff

≥ 4 years: Same as adults

< 4 years: Not used

2 puffs every 4–6 hours as needed and 2 puffs 15–30 minutes before exercise

Nebulized solution: 5 mg/mL and 0.63, 1.25, and 2.5 mg/3 mL

< 5 years: 0.63–2.5 mg in 3 mL of saline every 4–6 hours as needed

≥ 5 years: 0.05 mg/kg in 3 mL saline every 4–6 hours as needed (minimum 1.25 mg, maximum 2.5 mg)

1.25–5 mg in 3 mL saline every 4–6 hours as needed

Levalbuterol

HFA: 45 mcg/puff

< 5 years: Not established

≥ 5 years: Same as adults

2 puffs every 4–6 hours as needed

Levalbuterol is the R-isomer of albuterol. 0.63 mg is equivalent to 1.25 mg racemic albuterol.

Levalbuterol may have fewer adverse effects.

Nebulized solution: 0.31, 0.63, and 1.25 mg/3 mL and 1.25 mg/0.5 mL

< 5 years: 0.31–1.25 mg in 3 mL every 4–6 hours as needed

5–11 years: 0.31–0.63 mg every 8 hours as needed (maximum 0.63 mg every 8 hours)

12 years: Same as adults

0.63–1.25 mg every 6–8 hours as needed

Long-acting beta agonists (not to be used as monotherapy)

Arformoterol

Nebulized solution: 15 mcg/2 mL

Not established

15–25 mcg every 12 hours

Arformoterol is the R-isomer of formoterol.

Formoterol

Nebulized solution: 20 mcg/2 mL

Not established

20 mcg every 12 hours

DPI form is no longer available.

Salmeterol

HFA: 21 mcg/puff (not available in the US)

12 years: Same as adults

2 puffs every 12 hours; when taken before exercise, should be taken 30–60 minutes before exercise

Duration of action is 12 hours.

One dose nightly is helpful for nocturnal asthma.

Salmeterol is not to be used for acute symptom relief in an exacerbation.

DPI: 50 mcg/puff

< 4 years: Not established

4 years: Same as adults

1 puff every 12 hours and 30 minutes before exercise

Ultra–long-acting beta agonists (not to be used as monotherapy)

Indacaterol

DPI: 75 mcg/puff

Not established

1 puff once a day

Olodaterol

SMI: 2.5 mcg/puff

Not established

2 puffs once a day

Vilanterol

DPI: 25 mcg/puff

Not established

1 puff once a day

Vilanterol is available only in combination with fluticasone 100 mcg or 200 mcg.

Anticholinergics

Ipratropium

HFA: 17 mcg/puff

< 12 years: Not established

12 years: Same as adults

2 puffs every 6 hours as needed (maximum 12 puffs/day)

Ipratropium may be mixed in the same nebulizer as albuterol.

It should not be used as first-line therapy.

Regular use provides no clear benefit for long-term maintenance therapy but should be added for treatment of acute symptoms.

Nebulized solution: 500 mcg (0.02%, 2 mL)

< 12 years: Not established

12 years: Same as adults

500 mcg every 6–8 hours as needed

Tiotropium

SMI: 1.25 mcg/puff

< 6 years: Not established

6 years: Same as adults

2 puffs once a day (max 2 puffs/day)

Tiotropium is longer acting than ipratropium.

The lower dose SMI tiotropium is the only dose recommended for use in asthma.

DPI: 18 mcg/capsule

Not established

18 mcg (1 capsule) once a day

Corticosteroids (inhaled)

Beclomethasone

HFA: 40–80 mcg/puff

< 4 years: Not established

4–11 years: 1 puff every 12 hours (usual maximum 80 mcg twice a day)

12 years: Same as adults

1–2 puffs every 12 hours (usual maximum 320 mcg twice a day)

Doses depend on severity and range from 1–2 puffs to whatever dose is needed to control asthma.

All may have systemic effects when used long term.

Maximum threshold is that above which hypothalamic- pituitary-adrenal suppression is produced.

If higher doses are necessary for asthma control, specialist consultation is recommended.

Budesonide

DPI: 90 or 180 mcg/puff

< 6 years: Not recommended

6 years: Initial dose of 180 mcg twice a day (maximum 360 mcg twice a day)

Initial dose of 360 mcg twice a day (maximum 720 mcg twice a day)

Nebulized solution: 0.25, 0.5, or 1.0 mg (each in 2 mL solution)

1–8 years only: If previously taking bronchodilators alone, initial dose of 0.5 mg once a day or 0.25 mg twice a day (maximum 0.5 mg/day)

If previously taking inhaled corticosteroids, initial dose of 0.5 mg once a day or 0.25 mg twice a day

If previously taking oral corticosteroids, initial dose of 0.5 mg twice a day or 1 mg once a day (maximum 1 mg/day)

Not indicated for adults

Ciclesonide

HFA: 80 or 160 mcg/puff

≤ 5 years: 160 mcg daily

6–11 years: Low dose 80 mcg once a day, medium dose > 80 to 160 mcg once a day, high dose > 160 mcg once a day

≥ 12 years: Same as adult

If previously taking bronchodilators alone, initial dose of 80 mcg twice a day (maximum 320 mcg twice a day)

If previously taking inhaled corticosteroids, initial dose of 80 mcg twice a day (maximum 640 mcg twice a day)

If previously taking oral corticosteroids, initial dose of 320 mcg twice a day (maximum 640 mcg twice a day)

Flunisolide

HFA: 80 mcg/puff

< 5 years: Not established

5–11 years: 1 puff twice a day (maximum 2 puffs twice a day [320 mcg/day])

12 years: Same as adults

2 puffs twice a day (maximum 4 puffs twice a day [640 mcg/day])

Fluticasone propionate

HFA: 44, 110, or 220 mcg/puffs

0--4 years: 50 mcg/day

5–11 years: usually 44–220 mcg total daily dose

12 years: Same as adults

If previously taking bronchodilators alone, initial dose of 88 mcg twice a day (maximum 440 mcg twice a day)

If previously taking inhaled corticosteroids, initial dose of 88–220 mcg twice a day (maximum 440 mcg twice a day)

If previously taking oral corticosteroids, initial dose of 440–880 mcg twice a day (maximum 880 mcg twice a day)

DPI: 50, 100, or 250 mcg/puff

0–4 years: not established

5–11 years: usually 50–200 mcg total daily dose (usual maximum 100 mcg twice a day)

12 years: Same as adults

If previously taking bronchodilators alone, initial dose of 100 mcg twice a day (maximum 500 mcg twice a day)

If previously taking inhaled corticosteroids, initial dose of 100–250 mcg twice a day (maximum 500 mcg twice a day)

If previously taking oral corticosteroids, initial dose of 500–1000 mcg twice a day (maximum 1000 mcg twice a day)

Fluticasone furoate

DPI: 50, 100, or 200 mcg/puff

0–4 years: Not established

5–11 years: 1 puff (50 mcg) once a day

≥ 12 years: Same as adults

If previously taking bronchodilators alone, initial dose of 100 mcg once a day (maximum 200 mcg/day)

If previously taking inhaled corticosteroids, initial dose of 100-200 mcg once a day (maximum 200 mcg/day)

Mometasone

DPI: 110 or 220 mcg/puff

< 4 years: Not established

4–11 years: 110 mcg once a day in the evening

12 years: Same as adults

If previously taking bronchodilators alone or inhaled corticosteroids, initial dose of 220 mcg once a day in the evening (maximum 220 mcg twice a day or 440 mcg once a day in the evening)

If previously taking oral corticosteroids, initial dose of 440 mcg twice a day (maximum 880 mcg twice a day)

HFA: 50, 100, or 200 mcg/puff

< 12 years: Not established

12 years: Same as adults

If previously taking bronchodilators alone, initial dose of 220 mcg (delivering 200 mcg) once or twice a day (maximum 440 mcg/day)

If previously taking inhaled corticosteroids, initial dose of 110–220 mcg (delivering 100 or 200 mcg) twice a day (maximum 800 mcg/day)

If previously taking oral corticosteroids, initial dose of 440 mcg (delivering 400 mcg) twice a day (maximum 800 mcg/day)

Systemic corticosteroids (oral)

Methylprednisolone

Tablets: 2, 4, 8, 16, or 32 mg

0–11 years: Short-course burst: 1–2 mg/kg once a day (maximum 60 mg) for 3–10 days

12 years: Same as adults

7.5–60 mg once a day in the morning or every other day in the morning

Short-course burst: 40–60 mg once a day (or 20–30 mg twice a day) for 3–10 days

Maintenance doses should be given in a single dose in the morning every day or every other day as needed for control.

Some evidence suggests clinical effectiveness increases with no increase in adrenal suppression when dose is given at 3 PM.

Short-course burst doses are effective for establishing control when initiating therapy or during a period of gradual deterioration.

The burst should be continued until PEF = 80% of personal best or symptoms resolve, possibly requiring > 3–10 days of therapy.

Prednisolone

Tablets: 5 mg

Solution: 5 mg/5 mL or 15 mg/5 mL

Prednisone

Tablets: 1, 2.5, 5, 10, 20, or 50 mg

Solution: 5 mg/mL or 5 mg/5 mL

Combination drugs

Ipratroprium and albuterol

SMI: 20 mcg/puff ipratropium and 100 mcg/puff albuterol

Not established

1 puff qid (maximum 6 puffs/day)

Ipratroprium prolongs bronchodilator effect of albuterol.

Nebulized solution: 0.5 mg ipratropium and 2.5 mg albuterol in a 3-mL vial

3-mL vial via nebulization 4 times a day for ambulatory rescue therapy (maximum 6 doses/24 hours)

Fluticasone and salmeterol

DPI: 100, 250, or 500 mcg fluticasone and 50 mcg salmeterol

< 4 years: Not established

4–11 years: 1 puff (100/50) twice a day

12 years: Same as adults

1 puff twice a day

The 250/50 dose is indicated for asthma not controlled by low-to-medium doses of inhaled corticosteroids.

The 500/50 dose is indicated for asthma not controlled by medium-to-high doses of inhaled corticosteroids.

HFA: 45, 115, or 230 mcg fluticasone and 21 mcg salmeterol

< 12 years: Not established

12 years: Same as adults

2 puffs twice a day

Budesonide and formoterol

HFA: 80 or 160 mcg budesonide and 4.5 mcg formoterol

< 12 years: 1-2 puffs budesonide 80 mcg/formoterol 4.5 mcg twice daily (not to exceed 2 puffs twice daily as maintenance dose)

12 years: 2 puffs twice a day and as needed

Maximum total daily maintenance and rescue of 8 puffs (36 mcg)

2 puffs twice a day and as needed Maximum total daily maintenance and rescue of 12 puffs (54 mcg).

The 80/4.5 dose is indicated for asthma not controlled by low-to-medium doses of inhaled corticosteroids.

The 160/4.5 dose is indicated for asthma not controlled by medium-to-high doses of inhaled corticosteroids.

Mometasone and formoterol

HFA: 100 mcg or 200 mcg mometasone and 5 mcg formoterol; 50 mcg mometasone and 5 mcg formoterol for children < 5 years

< 5 years: 2 puffs twice a day as needed and do not exceed this dose for maintenance therapy

≥ 5 years: 2 puffs twice a day and as needed

Maximum total daily maintenance and rescue of 8 puffs (36 mcg)

2 puffs twice a day and as needed

Maximum total daily maintenance and rescue of 12 puffs (54 mcg)

The 100/5 dose is recommended for asthma not controlled by low-to-medium–dose inhaled corticosteroids.

The 200/5 dose is recommended for asthma not controlled by high-dose inhaled corticosteroids.

Fluticasone and vilanterol

DPI: 100 or 200 mcg fluticasone and 25 mcg vilanterol

Not established

1 puff once/day

Recommended starting dose is based on asthma severity.

Mast cell stabilizers

Cromolyn

Nebulized solution: 20 mg/ampule

< 2 years: Not established

2 years: Same as adults

1 ampule 3 or 4 times a day

Cromolyn should be taken before exercise or allergen exposure.

One dose provides effective prophylaxis for 1–2 hours.

Leukotriene modifiers

Montelukast

Tablets, chewable tablets, and granules: 4, 5, or 10 mg

12 mo–5 years: 4 mg orally once a day in the evening

6–14 years: 5 mg orally once a day in the evening

15 years: Same as adults

10 mg orally once a day in the evening

Exercise-induced asthma: 10 mg orally 2 hours before exercise

Montelukast is a leukotriene receptor antagonist that is a competitive inhibitor of leukotrienes D4 and E4.

Zafirlukast

Tablet: 10 or 20 mg

< 5 years: Not established

5–11 years: 10 mg orally twice a day

12 years: Same as adults

20 mg orally in the evening

Zafirlukast is a leukotriene receptor antagonist that is a competitive inhibitor of leukotrienes D4 and E4.

It must be taken 1 hour before or 2 hours after meals.

Zileuton

Tablet, immediate-release: 600 mg

< 12 years: Not established

12 years: Same as adults

600 mg orally 4 times a day

Zileuton inhibits 5-lipoxygenase.

Dosing may limit adherence.

Zileuton may cause liver enzyme elevations and inhibit metabolism of drugs processed by CYP3A4, including theophylline.

Extended-release: 1200 mg

< 12 years: Not established

≥ 12 years: Same as adults

1200 mg orally twice a day within 1 hour after morning and evening meals

Methylxanthines

Theophylline

Capsule, extended-release: 100, 200, 300, and 400 mg

Elixir: 80 mg/15 mL

Tablet, extended-release: 100, 200, 400, 450, or 600 mg

Initial dose of 10 mg/kg/day up to 600 mg/day, then adjusted to achieve a serum concentration of 5–15 mcg/mL at steady state

Initial dose of 10 mg/kg/day up to 600 mg/day, then adjusted to achieve a serum concentration of 5–15 mcg/mL at steady state

The wide variability in metabolic clearance, drug interactions, and potential for adverse effects mandate routine serum level monitoring.

Availability of safer alternatives has led to declining use of this drug.

Safety may be better with a target level < 10 mcg/mL.

Immunomodulators

Benralizumab

Subcutaneous injection: 30 mg/mL

< 12 years: Not established

> 12 years: Same as adults

30 mg subcutaneously every 4 weeks for 3 doses then every 8 weeks thereafter

Benralizumab is used as an add-on treatment for patients with the eosinophilic phenotype.

Dupilumab

Subcutaneous injection: 300 mg/2mL or 200 mg/1.14 mL

< 6- years: Not established

6–11 years: Refer to specialist for dose adjustment

≥ 12 years: Same as adults

400 mg subcutaneously once then 200 mg every 2 weeks or 600 mg subcutaneously once then 300 mg every 2 weeks

The initial dose should be given as two injections.

Dupilumab is used as an add-on treatment for patients with the eosinophilic phenotype.

Mepolizumab

Subcutaneous injection: 100 mg

< 6 years: Not established

6–12 years: Refer to specialist for dose adjustment

≥ 12 years: Same as adults

100 mg subcutaneously once every 4 weeks

Omalizumab

Subcutaneous injection: 150 mg/1.2 mL

< 12 years: 75–375 mg subcutaneously every 2–4 weeks, depending on body weight and pretreatment serum IgE level

≥ 12 years: Same as adults

150–375 mg subcutaneously every 2–4 weeks, depending on body weight and pretreatment serum IgE level

Maximum dose per injection site is 150 mg.

Reslizumab

Intravenous: 100 mg/10 mL

Not established

3 mg/kg IV once every 4 weeks

* All ages unless specified differently.

DPI = dry-powder inhaler; HFA = hydrofluoroalkane; MDI = metered-dose inhaler; SMI = soft mist inhaler; PEF = peak expiratory flow.

Adapted from the National Heart, Lung, and Blood Institute: Expert Panel Report 3, Guidelines for the diagnosis and management of asthma—full report 2007. August 28, 2007. Available at www.nhlbi.nih.gov/guidelines/asthma/asthgdln.pdf.