What is the composition of Spiolto (tiotropium and olodaterol)?

Spiolto Composition

Spiolto Respimat is a fixed-dose combination inhaler containing tiotropium bromide 2.5 mcg and olodaterol 2.5 mcg per actuation, delivering a total dose of 5 mcg tiotropium and 5 mcg olodaterol per complete dose (two actuations). 1

Active Pharmaceutical Ingredients

Tiotropium Component:

• Each dose delivers 5 mcg of tiotropium (equivalent to 6.247 mcg tiotropium bromide monohydrate) 1
• Tiotropium is a long-acting muscarinic antagonist (LAMA) that provides anticholinergic bronchodilation 1, 2
• Chemical name: (1α, 2ß, 4ß, 5α, 7ß)-7-[(Hydroxydi-2-thienylacetyl)oxy]-9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane bromide monohydrate 1
• Molecular formula: C19H22NO4S2Br ∙ H2O with molecular mass of 490.4 1

Olodaterol Component:

• Each dose delivers 5 mcg of olodaterol (equivalent to 5.473 mcg olodaterol hydrochloride) 1
• Olodaterol is a long-acting beta2-adrenergic agonist (LABA) 1, 2
• Chemical name: 2H-1,4-Benzoxazin-3H(4H)-one, 6-hydroxy-8-[(1R)-1-hydroxy-2-[[2-(4-methoxyphenyl)-1-dimethylethyl]-amino]ethyl]-, monohydrochloride 1
• Molecular formula: C21H26N2O5 × HCl with molecular weight of 422.9 g/mole (salt) 1

Inactive Ingredients (Excipients)

The sterile aqueous solution contains: 1

• Benzalkonium chloride (preservative)
• Edetate disodium
• Hydrochloric acid
• Water for injection

Delivery System Specifications

Respimat Soft Mist Inhaler:

• Each cartridge contains 4 grams of sterile aqueous solution 1
• Each complete dose requires two actuations 1
• Each actuation delivers 22.1 mcL of solution from the mouthpiece 1
• The inhaler uses mechanical energy to generate a slow-moving aerosol cloud 1
• Spray duration is 1.5 seconds 1

Clinical Pharmacology Context

Dual Bronchodilator Mechanism:

• This LAMA/LABA combination provides complementary bronchodilation through two distinct pathways 2, 3
• Tiotropium blocks muscarinic receptors to reduce cholinergic bronchoconstriction 4
• Olodaterol stimulates beta2-adrenergic receptors to relax airway smooth muscle 4
• The combination demonstrates superior lung function improvement compared to either monocomponent 2, 3

Dosing Regimen:

• Administered once daily at the same time each day 1
• Two actuations constitute one complete dose 1
• The fixed-dose combination eliminates the need for multiple inhalers 2