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[3.3.1.02,4]nonane
Identifiers
CAS number 186691-13-4
ATC code R03BB04
PubChem 131950
Chemical data
Formula C19H22NO4S2+
Mol. mass 490.4
SMILES eMolecules & PubChem
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) -only(US)

Routes inhalation (oral)

Tiotropium (pronounced /ˌtaɪəˈtroʊpiəm/) (administered as tiotropium bromide) 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".

Contents

[edit] Mode of delivery

The patient removes one tiotropium capsule from the blister pack, places it into the piercing chamber of the inhalation device and closes the mouthpiece.

The capsule is manually pierced, and the medication is inhaled through the mouthpiece. It is recommended that inhalations are repeated 2 to 3 times to ensure all medication is drawn from the capsule. When properly done, the capsule will make a distinctive flutter or rattle, audible to the patient.

Once the powder capsules are removed from the blister pack, it should immediately taken, via through the inhalation device. If a capsule is exposed to the air it will rapidly degrade to the point the dose will become ineffective. Any previously exposed capsules should be discarded.

The capsules cannot be taken orally - they will not be effective as respiratory medication if absorbed through the gastrointestinal tract and may have side effects if absorbed via this route.

[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 as a daily, 24 hour, 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

[edit] See also

[edit] External links

[edit] Image collection

Front view
Front view
A previously pierced Spiriva capsule
A previously pierced Spiriva capsule
Open (cleaning) view
Open (cleaning) view
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