Tiotropium
From Wikipedia, the free encyclopedia
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Tiotropium
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| Systematic (IUPAC) name | |
| (1α,2β,4β,7β)- 7-[(hydroxidi-2-thienylacetyl)oxy]-9,9-dimethyl- 3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane |
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| Identifiers | |
| CAS number | |
| ATC code | R03 |
| PubChem | |
| Chemical data | |
| Formula | C19H22NO4S2+ |
| Mol. mass | 490.4 |
| 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 | |
| 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.
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[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
[edit] External links
[edit] Image collection
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| Medications commonly used in asthma and COPD (primarily R03) | |
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| Anticholinergics | Ipratropium, Tiotropium |
| Short acting β2-agonists | Salbutamol, Terbutaline |
| Long acting β2-agonists (LABA) | Bambuterol, Clenbuterol, Fenoterol, Formoterol, Salmeterol |
| Corticosteroids | Beclometasone, Budesonide, Ciclesonide, Fluticasone |
| Leukotriene antagonists | Montelukast, Pranlukast, Zafirlukast |
| Xanthines | Aminophylline, Theobromine, Theophylline |
| Mast cell stabilizers | Cromoglicate, Nedocromil |
| Combination products | Budesonide/formoterol, Fluticasone/salmeterol, Ipratropium/salbutamol |
