Tiotropium

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Tiotropium
Systematic (IUPAC) name
(1α,2β,4β,7β)- 7-[(hydroxidi-2-thienylacetyl)oxy]-9,9-dimethyl- 3-oxa-9-azoniatricyclo[3.3.1.0^2,4]nonane
Identifiers
CAS number	186691-13-4
ATC code	R03 BB04
PubChem	131950
Chemical data
Formula	C₁₉H₂₂N O₂⁺
Mol. weight	392.51
Pharmacokinetic data
Bioavailability	19.5% (inhalation)
Metabolism	hepatic 25% (CYP2D6, CYP3A4)
Half life	5–6 days
Excretion	renal
Therapeutic considerations
Pregnancy cat.	B1(AU)
Legal status	S4(AU) POM(UK)
Routes	inhalation (topical)

Tiotropium (IPA: [ˌtaɪəˈtropiəm]) is a long-acting anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Tiotropium bromide (INN) capsules for inhalation are co-marketed by Boehringer-Ingelheim and Pfizer under the trade name Spiriva. Capsules are inhaled via a proprietary HandiHaler device.

1 Mode of action
2 Clinical use
- 2.1 Indications
- 2.2 Adverse effects
3 References
4 See also
5 External links

[edit] Mode of action

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, on topical application it acts mainly on M₃ muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect.

[edit] Clinical use

[edit] Indications

Tiotropium is indicated for maintenance treatment of chronic obstructive pulmonary disease (COPD).

[edit] Adverse effects

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, and/or allergy (rash, angioedema, anaphylaxis) (Rossi, 2006).

[edit] References

Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.

[edit] See also

Chronic obstructive pulmonary disease

[edit] External links

MedlinePlus drug information: Tiotropium (Inhalation–Local) – information from USP DI Advice for the Patient
Spiriva online

Medications commonly used in asthma and COPD (primarily R03) edit
Anticholinergics:	Ipratropium, Tiotropium
Short acting β₂-agonists:	Salbutamol, Terbutaline
Long acting β₂-agonists (LABA):	Clenbuterol, Formoterol, Salmeterol
Corticosteroids:	Beclometasone, Budesonide, Fluticasone
Leukotriene antagonists:	Montelukast, Pranlukast, Zafirlukast
Xanthines:	Aminophylline, Theobromine, Theophylline
Mast cell stabilizers:	Cromoglicate, Nedocromil
Combination products:	Budesonide/formoterol, Fluticasone/salmeterol, Ipratropium/salbutamol