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Tiotropium



Tiotropium
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
Identifiers
CAS number 186691-13-4
ATC code R03BB04
PubChem 131950
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

Prescription Only (S4)(AU) POM(UK)

Routes inhalation (topical)

Tiotropium (pronounced /ˌtaɪəˈtroʊpiəm/) is a long-acting, 24 hour, 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.

Additional recommended knowledge

Contents

Mode of delivery

The patient removes from the blister pack one Spiriva capsule and places it into the piercing chamber of the proprietary HandiHaler device and closes the mouthpiece.

The capsule is manually pierced, and the medication is then inhaled through the mouthpiece. It is recommended to be repeat the inhalations, 2 to 3 times, to make sure all medication is drawn from the capsule. When properly done, the capsule will make a distinctive flutter or rattle, to be heard and sensed by the patient.

The manufacturer warns users to only remove the capsule when ready to immediately take. Any advance removal of capsule, or exposing an additional capsule, is to be discarded. This is because any advanced removal will exposed capsule to the air, of which will render the medication ineffective.

Do not take the capsule orally

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.

Clinical use

Indications

Tiotropium is indicated as a daily, 24 hour, maintenance treatment of chronic obstructive pulmonary disease (COPD).

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).

References

See also

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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Tiotropium". A list of authors is available in Wikipedia.
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