Tiotropium bromide
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| Systematic (IUPAC) name | |
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(1α,2β,4β,7β)-
7-[(hydroxidi-2-thienylacetyl)oxy]-9,9-dimethyl- 3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide |
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| Clinical data | |
| MedlinePlus | a604018 |
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| Routes of administration |
Inhalation (oral) |
| Pharmacokinetic data | |
| Bioavailability | 19.5% (inhalation) |
| Metabolism | Hepatic 25% (CYP2D6, CYP3A4) |
| Biological half-life | 5–6 days |
| Excretion | Renal |
| Identifiers | |
| CAS Number | 136310-93-5 Template:CAS (cation) |
| ATC code | R03BB04 (WHO) |
| PubChem | CID: 5487426 |
| IUPHAR/BPS | 367 |
| DrugBank | DB01409 |
| ChemSpider | 10482095  |
| UNII | XX112XZP0J |
| ChEMBL | CHEMBL1201307 |
| Chemical data | |
| Formula | C19H22BrNO4S2 |
| Molecular mass | 472.416 g/mol |
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Tiotropium bromide (INN) is a long-acting, 24-hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Tiotropium bromide capsules for inhalation are co-promoted by Boehringer-Ingelheim and Pfizer under the trade name Spiriva. It is also manufactured and marketed by Cipla under trade name Tiova.
Tiotroprium was discovered in 1991 and came to market in 2004.[1]
Contents
Medical uses
Tiotropium is used for maintenance treatment of chronic obstructive pulmonary disease (COPD) which includes chronic bronchitis and emphysema.[2] It is not however used for acute exacerbations.[2]
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 (notably supraventricular tachycardia and atrial fibrillation) and/or allergy (rash, angioedema, anaphylaxis).[3]
Tiotropium and another member of its class ipratropium were linked to increased risk of heart attacks, stroke and cardiovascular death.[4] The FDA requested further trials; these are now complete, and adequately resolve the previous safety concerns.[5]
Tiotropium mist inhaler (Respimat) has been found to be associated with an increase of all cause mortality in people with COPD.[6]
Dosage
The standard dose of tiotropium is 18 mcg which is administered by a HandiHaler inhalation device.[7]
Mechanism 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, 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.
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 be 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 be taken immediately via 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.
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File:Spiriva3.png
Front view
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File:"Spiriva HandiHaler"-brand dry powder inhaler (open).png
Open (cleaning) view
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References
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
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- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ FDA. Follow-Up to the October 2008 Updated Early Communication about an Ongoing Safety Review of Tiotropium (marketed as Spiriva HandiHaler). FDA 2010
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ Wise RA, Anzueto A, Cotton D, Dahl R, Devins T, Disse B, et al. Tiotropium respimat inhaler and the risk of death in COPD. N Engl J Med. 2013 08/30; 2013/10.
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
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