Before changing treatment check the patient’s concordance and inhaler technique.

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If FEV1 ≥ 50% - Choose a Long-acting beta-2 agonist (LABA) - They have a prolonged affect due to prolonged receptor occupancy, with a duration of action of 12 hours.

 

Mechanism of action: The same as SABA (see first-line treatments).

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Formoterol

• Aerosol inhalation — 12 micrograms twice daily. Additional doses may be taken to a total maximum of 48 micrograms daily (maximum single dose is 24 micrograms).

• Dry powder inhalation — 12 micrograms twice daily.

Pharmacodynamics: A potent selective beta-2-adrenergic stimulant with a rapid effect (within 1-3minutes) lasting 12hours.

Pharmacokinetics: It has a plasma protein binding of 61-64% (around 34% to albumin).  At therapeutic doses it does not inhibit cytochrome P450 enzymes and the kinetics are similar after single and repeated administration. Around 7-10% is eliminated in the urine as unchanged drug. It has a renal clearance of 150ml/min.

 

Salmetarol

• Aerosol inhalation — 50 micrograms (2 puffs) twice daily.

• Dry powder inhalation — 50 micrograms (1 blister) twice daily. (The recommended doses may vary slightly for the different brands available.)

Pharmacodynamics: A selective long-acting (usually 12 hours) beta-2 adrenoceptor agonist, acting on the reversible component of COPD. It has been shown to improve symptoms, pulmonary function and quality of life. It has a long side chain that binds to the exo-site of the receptor.

Pharmacokinetics: It acts locally in the lung so plasma levels do not predict therapeutic effect.

 

Indacaterol

• Dry powder inhalation — 150 micrograms or 300 micrograms once daily.

Pharmacodynamics: Its pharmacological effect is partly due to the stimulation of adenyl cyclase (an enzyme catalysing the conversion of ATP to cAMP).  Increased cAMP relaxes bronchial smooth muscle.  It has a rapid onset of around 5minutes.

Pharmacokinetics: Bioavailability is around 43-45%.

 

Olodaterol - Licensed for the maintenance treatment of COPD. It is a Black Triangle drug subject to intense surveillance by the Medicines and Healthcare products Regulatory Agency (MHRA).

 

Combination products with ICS (see below for details)

Formoterol plus budesonide - Symbicort Turbohaler, DuoResp Spiromax

Salmeterol plus fluticasone propionate, Seretide 500 Accuhaler, AirFluSal Forspiro

 

Cautions and interactions: Same as SABA (see first-line treatments).

 

Side effects: Same as SABA. Can also cause muscle cramps.

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OR a Long-acting muscarinic antagonist (LAMA) (discontinue SAMA)

 

Pharmacology: Same as SAMA (see first-line treatments).

 

Tiotropium

• Inhalation powder, hard capsule (18 micrograms tiotropium bromide monohydrate) for use with Handihaler® device — 18 micrograms once daily (at the same time of the day).

• Nebulized solution (Spiriva Respimat®) — 5 micrograms (2 puffs) once daily (at the same time of the day). [Spiriva Respimat® should be reserved for use in people with chronic obstructive pulmonary disease (COPD) who have difficulties using the Handihaler® device.]

Pharmacodynamics: A long-acting specific muscarinic antagonist (sometimes called an anticholinergic). It binds to muscarinic receptors in bronchial smooth muscle inhibiting the effects of acetylcholine causing airway relaxation.

Pharmacokinetics: Is a non-chiral quaternary ammonium compound which is sparingly soluble in water and as such is delivered by dry powder inhalation. A lot of the dose is deposited in the GI tract not the lung where its intended.

 

Aclidinium and glycopyrronium – licensed for the maintenance treatment of COPD.

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Cautions and side effects: Same as SAMA (see first-line treatments).

 

Interactions: Not usually a problem due to low systemic absorption.