Tiotropium bromide

Inhalation/Respiratory
Asthma, Chronic obstructive pulmonary disease

CrCl (mL/min)	Dosage
≤50	Use w/ caution.

Hypersensitivity to tiotropium bromide, atropine or its derivatives.

Patient w/ narrow-angle glaucoma, prostatic hyperplasia/bladder neck obstruction, cystic fibrosis. History of MI (<6 mth), or unstable or life threatening cardiac arrhythmia w/in the past yr. Not intended for use as initial treatment for acute bronchospasm and as monotherapy for asthma. Moderate to severe renal impairment (CrCl ≤50 mL/min). Pregnancy and lactation.

Dry mouth, upper resp tract infection, pharyngitis, sinusitis, rhinitis, epistaxis, non-specific chest pain, UTI, dyspepsia, hypersensitivity reactions (e.g. urticaria, angioedema, rash, itching), dizziness, dysphagia, hoarseness, intestinal obstruction, increased intraocular pressure, palpitations, tachycardia; application site irritation (e.g. glossitis, mouth ulceration, pharyngolaryngeal pain).
Potentially Fatal: Paradoxical bronchospasm, anaphylaxis.

This drug may cause dizziness and blurred vision, if affected, do not drive or operate machinery.

Monitor pulmonary function.

Additive effect w/ other anticholinergic drugs.

Description:
Mechanism of Action: Tiotropium bromide antagonises the cholinergic effects of acetylcholine by reversibly and competitively binding to type 3 muscarinic (M₃) receptors, resulting in bronchial smooth muscle relaxation.
Pharmacokinetics:
Absorption: Systemically absorbed from the lungs. Bioavailability: Approx 20% (dry powd inhalation); approx 33% (inhalation soln). Time to peak plasma concentration: 5 min (dry powd inhalation); 5-7 min (inhalation soln).
Distribution: Volume of distribution: 32 L/kg. Plasma protein binding: Approx 72%.
Metabolism: Undergoes minimal hepatic metabolism by non-enzymatic cleavage and by CYP2D6 and CYP3A4 isoenzymes.
Excretion: Via urine as unchanged drug. Half-life: 5-6 days (dry powd inhalation).

Source: National Center for Biotechnology Information. PubChem Database. Tiotropium bromide, CID=5487426, https://pubchem.ncbi.nlm.nih.gov/compound/Tiotropium-bromide (accessed on Jan. 23, 2020)

Inhalation cap: Store at 25°C. Protect from excessive heat and moisture. Do not store in inhaler device. Inhalation soln: Store at 25°C. Do not freeze.

Antiasthmatic & COPD Preparations

R03BB04 - tiotropium bromide ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, anticholinergics.

Anon. Tiotropium. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/07/2015.

Buckingham R (ed). Tiotropium Bromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/07/2015.

Spiriva Capsule (Boehringer Ingelheim Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/07/2015.