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Tiotropium bromide
CasNo: 136310-93-5
ProductName:

Tiotropium bromide

MolecularFormula: C19H22BrNO4S2
Molecular Weight: 472.42
Boiling Point: 218-220 °C
Assay: >99%
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Product Name: Tiotropium bromide

Molecular Weight: 472.41628 [g/mol] 

Molecular Formula: C19H22BrNO4S2 

H-Bond Donor: 1 

H-Bond Acceptor: 5 

Product Categories: API; Heterocycles; Intermediates & Fine Chemicals; Pharmaceuticals; Sulfur & Selenium Compounds; Tiotropium 

Appearance: White Solid

Melting Point: 218-220 °C

Classification Code of 3-Oxa-9-azoniatricyclo[3.3.1.02,4]nonane,7-[(2-hydroxy-2,2-di-2-thienylacetyl)oxy]-9,9-dimethyl-, bromide (1:1), (1a,2b,4b,5a,7b)- (CAS NO.136310-93-5): Anti-Asthmatic Agents; Autonomic Agents; Bronchodilator agents; Cholinergic Agents; Cholinergic antagonists; Neurotransmitter Agents; Parasympatholytics; Peripheral Nervous System Agents; Respiratory System Agents


Tiotropium bromide(casno.136310-93-5) is a long-acting, 24-hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Tiotropium bromide(casno.136310-93-5) 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.


Tiotropium bromide(casno.136310-93-5) 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.


Tiotropium bromide(casno.136310-93-5) 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).

Tiotropium and another member of its class ipratropium were linked to increased risk of heart attacks, stroke and cardiovascular death.The FDA requested further trials; these are now complete, and adequately resolve the previous safety concerns.

Tiotropium mist inhaler (Respimat) has been found to be associated with an increase of all cause mortality in people with COPD.


Tiotropium bromide(casno.136310-93-5) Dosage


The standard dose of tiotropium is 18 mcg which is administered by a HandiHaler inhalation device.

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 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.


Tiotropium bromide(casno.136310-93-5) 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.


Tiotropium bromide(casno.136310-93-5) Inhalation Powder and Capsules


SPIRIVA HANDIHALER consists of SPIRIVA capsules and a HANDIHALER device. Each light green, hard gelatin SPIRIVA capsule contains a dry powder consisting of 18 mcg tiotropium (equivalent to 22.5 mcg Tiotropium bromide(casno.136310-93-5) monohydrate) blended with lactose monohydrate (which may contain milk proteins).

The contents of SPIRIVA capsules are intended for oral inhalation only, and are intended for administration only with the HANDIHALER device.

The active component of SPIRIVA HANDIHALER is tiotropium. The drug substance, Tiotropium bromide(casno.136310-93-5) monohydrate, is an anticholinergic with specificity for muscarinic receptors. It is chemically described as (1α, 2β, 4β, 5α, 7β)-7-[(Hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide monohydrate. It is a synthetic, non-chiral, quaternary ammonium compound. Tiotropium bromide(casno.136310-93-5) is a white or yellowish white powder. It is sparingly soluble in water and soluble in methanol. The structural formula is:


Tiotropium bromide(casno.136310-93-5)


Tiotropium bromide(casno.136310-93-5) (monohydrate) has a molecular mass of 490.4 and a molecular formula of C19H22NO4S2Br •H2O.


What are the precautions when taking Tiotropium bromide(casno.136310-93-5) (Spiriva)?


Before using tiotropium, tell your doctor or pharmacist if you are allergic to it or to ipratropium; or to atropine or other belladonna-type drugs; or if you have any other allergies. This product may contain inactive ingredients (such as milk proteins), which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, personal or family history of glaucoma (angle-closure type), difficulty urinating (for example, due to enlarged prostate).


Uses for Tiotropium bromide(casno.136310-93-5)


COPD


Long-term treatment of reversible bronchospasm associated with COPD, including chronic bronchitis and emphysema.


A long-acting bronchodilator (e.g., orally inhaled salmeterol, formoterol, tiotropium) or an inhaled corticosteroid recommended for maintenance monotherapy in patients with moderate to severe COPD (e.g., FEV1 30 to <80% of predicted or, alternatively, <60% of predicted) who have persistent symptoms not relieved by as-needed therapy with a selective, short-acting inhaled β2-adrenergic agonist. Maintenance therapy with long-acting bronchodilators in such patients more effective and more convenient than regular therapy with short-acting bronchodilators. Insufficient data to favor one maintenance monotherapy over another in patients with moderate to severe COPD. In selected patients with inadequate response, may use a combination of several long-acting bronchodilators, such as tiotropium, and a long-acting β2-adrenergic agonist.


In patients with severe to very severe COPD (e.g., FEV1 <30 to <50% of predicted), some clinicians recommend addition of an inhaled corticosteroid to one or more long-acting bronchodilators, given separately or in fixed combination; however, benefits of combination therapy over monotherapy not consistently established. If inadequate response or limiting adverse effects occur, may consider the addition or substitution of extended-release oral theophylline.

Not indicated for the initial treatment of acute episodes of bronchospasm or acute exacerbations of COPD;a drug with a more rapid onset of action (e.g., a short-acting β-adrenergic agonist) preferred.


Tiotropium bromide(casno.136310-93-5) Dosage


Available as Tiotropium bromide(casno.136310-93-5) monohydrate; dosage expressed in terms of anhydrous tiotropium.

Each capsule contains 18 mcg of tiotropium as an inhalation powder.1 However, the precise amount of drug delivered to the lungs depends on factors such as the patient’s inspiratory flow.


Cautions for Tiotropium bromide(casno.136310-93-5)


Contraindications

Known hypersensitivity to Tiotropium bromide(casno.136310-93-5) or any ingredient in the formulation.

Known hypersensitivity to atropine or its derivatives (e.g., ipratropium).


Interactions for Tiotropium bromide(casno.136310-93-5)

Metabolized by CYP isoenzymes, principally CYP2D6 and CYP3A4

Does not inhibit CYP1A1, 1A2, 2B6, C29, 2C19, 2D6, 2E1, or 3A4.


Tiotropium bromide(casno.136310-93-5) Pharmacokinetics

Absorption

Bioavailability

Following inhalation, absolute bioavailability is 19.5%. Most of a dose is swallowed and minimally absorbed into systemic circulation;the fraction reaching the lungs appears to be readily absorbed. Peak plasma concentrations following oral inhalation are attained within 5 minutes.


Advice to Patients

Importance of providing patient a copy of manufacturer’s patient information.

Importance of informing a clinician of allergies to any medications prior to initiation of Tiotropium bromide(casno.136310-93-5) therapy.

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