Formoterol

Formoterol is a long-acting beta-2 agonist (LABA) used as a dry powder inhaler for the maintenance treatment of asthma and COPD. It is characterized by an unusually rapid onset of action, which is already noticeable after 1-3 minutes.

Unlike most LABAs, formoterol combines a rapid onset of action with a long duration of action (12 hours). The single-ingredient product is used as an add-on to inhaled corticosteroids.

Well-known brand names are Formoterol STADA® and Oxis® Turbuhaler. Formoterol is also a component of the combination inhalers Symbicort, Bufori Easyhaler® and Foster.

Formoterol activates the beta-2 receptors in the bronchi:

Mechanism of action: 1. Binds to beta-2 adrenoceptors in the bronchial muscles 2. Activates adenylate cyclase and increases cAMP 3. The smooth muscle of the bronchi relaxes 4. The airways are widened

Special features:

• Rapid onset of action (1-3 minutes) – unusual for a LABA
• Full intrinsic activity (full agonist)
• Duration of action: 12 hours
• Lipophilic anchoring in the cell membrane

Additional effects:

• Inhibition of the release of histamine and leukotrienes from passively sensitized human lung cells
• Improvement of mucociliary clearance
• Protection against bronchoconstrictive stimuli

Formoterol single-ingredient products are suitable for:

• Asthma from step 3 onward (always together with ICS!)
• Maintenance treatment of COPD
• Prevention of exercise-induced asthma

Important – safety information: In asthma, formoterol must NEVER be used alone without an inhaled corticosteroid (ICS)! LABA monotherapy in asthma increases the risk of severe exacerbations.

Advantages of the single-ingredient product:

• Flexible dosing independent of the ICS
• Rapid onset of action
• Suitable for as-needed use before exercise

Not suitable as:

• Sole asthma therapy (without ICS!)
• Acute treatment as the only measure

Formoterol STADA:

• 12 µg per single dose

Dosage for asthma:

• 1 inhalation (12 µg) 2 times daily
• If needed: up to 2 inhalations 2 times daily
• Before exercise: 1 inhalation 15 minutes beforehand

Dosage for COPD:

• 1 inhalation (12 µg) 2 times daily
• Maximum: 48 µg per day

Note: Always use in combination with an inhaled corticosteroid!

Formoterol STADA (hard capsules with powder for inhalation):

• Inhale the capsules only with the enclosed inhaler, do not swallow them
• Press the button only once (reduces the risk of the capsule shattering)
• For detailed handling, see the operating instructions in the pack

Easyhaler (dry powder inhaler): 1. Remove the protective cap 2. Hold the device upright and shake it once 3. Press and release (the dose is loaded) 4. Breathe out deeply (not into the inhaler) 5. Close your lips tightly around the mouthpiece 6. Breathe in forcefully and deeply 7. Hold your breath for 5-10 seconds 8. Breathe out slowly

Important notes:

• Always at the same time of day (morning and evening)
• Use regularly
• Do not stop abruptly
• In addition to the inhaled corticosteroid – never alone!

Do not use in case of:

• Hypersensitivity to formoterol or lactose
• As sole therapy for asthma (without ICS!)

Use with caution in:

• Severe cardiovascular diseases
• QT prolongation
• Hyperthyroidism
• Diabetes mellitus (may raise blood sugar)
• Hypokalemia
• Pheochromocytoma

Pregnancy: Only if clearly indicated. Asthma control is more important than theoretical risks.

Breastfeeding: It is not known whether formoterol passes into breast milk in humans. Use during breastfeeding should only be considered if the expected benefit for the mother outweighs the possible risk to the child.

Common (1-10%):

• Tremor (shaking of the hands)
• Palpitations
• Headache

Uncommon:

• Tachycardia
• Muscle cramps
• Restlessness, nervousness
• Sleep disturbances
• Dry mouth

Rare:

• Nausea
• Cardiac arrhythmias
• Hypokalemia (at high doses)
• Allergic reactions

Very rare:

• Paradoxical bronchospasm

Note: Side effects are considerably less pronounced with inhaled use than with oral administration.

Interactions:

• Beta blockers – may cancel out the effect of formoterol
• Avoid non-selective beta blockers in asthma!
• QT-prolonging medicines – increased risk of arrhythmia
• MAO inhibitors, tricyclic antidepressants – enhanced effects on the heart
• Corticosteroids, diuretics – risk of hypokalemia

Useful combination:

• Inhaled corticosteroids (mandatory in asthma)
• Anticholinergics (e.g. tiotropium)