Tiotropium bromide

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Tiotropium
Tiotropium.svg
Tiotropium-3D-balls.png
Clinical data
Trade names Spiriva
MedlinePlus a604018
Pregnancy
category
Routes of
administration
Inhalation (oral)
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability 19.5% (inhalation)
Metabolism Hepatic 25%
(CYP2D6, CYP3A4)
Elimination half-life 5–6 days
Excretion Renal
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
ECHA InfoCard 100.234.575 Edit this at Wikidata
Chemical and physical data
Formula C19H22BrNO4S2
Molar mass 472.416 g/mol
3D model (JSmol)
  (verify)

Tiotropium bromide, originally marketed as Spiriva,[1] is a long-acting, 24-hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD).

Tiotroprium was discovered in 1991 by Boehringer Ingelheim and came to market in 2004.[2]

Medical uses[edit]

Tiotropium is used for maintenance treatment of chronic obstructive pulmonary disease (COPD) which includes chronic bronchitis and emphysema.[3] It is not however used for acute exacerbations.[3]

Adverse effects[edit]

Adverse effects are mainly related to its antimuscarinic effects. Common adverse drug reactions (≥1% of patients) associated with tiotropium therapy include: dry mouth and/or throat irritation. Rarely (<0.1% of patients) treatment is associated with:urinary retention, constipation, acute angle closure glaucoma, palpitations (notably supraventricular tachycardia and atrial fibrillation) and/or allergy (rash, angioedema, anaphylaxis).[4]

Tiotropium and another member of its class ipratropium were linked to increased risk of heart attacks, stroke and cardiovascular death.[5] The FDA requested further trials; these are now complete, and adequately resolve the previous safety concerns.[6]

Tiotropium mist inhaler (Respimat) has been found to be associated with an increase of all cause mortality in people with COPD.[7]

Mechanism of action[edit]

Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, when topically applied it acts mainly on M3 muscarinic receptors[8] located on smooth muscle cells and submucosal glands. This leads to a reduction in smooth muscle contraction and mucus secretion and thus produces a bronchodilatory effect.

References[edit]

External links[edit]