Tiotropium Bromide Spiriva

Structural Formula Ball-and-Stick Model Space-filling Model

= Carbon = Hydrogen M = Oxygen A = Nitrogen = Sulfur

Year of discovery: 1991; Year of Introduction: 2004 (Pfizer, Boehrlnger Ingelheim); Drug category: Long-acting antimuscarinic bronchodilator; Main uses: Treatment of chronic obstructive pulmonary disease (COPD); Related drugs: Ipratropium bromide (Atrovent).

Chronic obstructive pulmonary disease (COPD) is an umbrella term used to describe a set of chronic lung diseases in which there is obstruction or deficiency of airflow. Included are chronic bronchitis (inflamed and narrowed bronchial tubes) and emphysema, a condition in which the air sacs (alveoli) in the lungs are inelastic and weakened as a result of long-term damage. COPD is a serious illness that, according WHO estimates, affects 80 million people worldwide and over 10 million people in the US. It is the fourth leading cause of death (responsible for 2.75 million deaths globally and over 100 thousand deaths in the US in 2000) after heart disease, cancer and stroke, and is projected to be the third leading cause of death by 2020. The economic burden is also significant; COPD was estimated to cost about $32 billion in the US in 2002.

The most common cause of COPD is tobacco smoke. An estimated 15% of smokers develop the disease, and smoking is responsible for 90% of COPD cases. Other risk factors are intense and prolonged exposure to occupational dusts and chemicals, as well as high levels of urban air pollution. A history of severe childhood respiratory infection and low birth weight predispose to the development of the disease.

COPD is a progressive disease; the symptoms develop so gradually that they generally are not troublesome. Early telltale signs include shortness of breath, development of a chronic cough, increased sputum production, wheezing and a feeling of chest tightness. The first symptoms typically appear at age 40-50. Heavy smokers often loose 50% of their lung function by the age 50, and most of those with COPD die before reaching 65.

COPD is not curable, but it is possible to control the symptoms and reverse acute exacerbation. The most commonly used medications include inhaled bronchodilators that work by relaxing the muscles around the airways (see salmeterol, page 50) and inhaled anti-inflammatory corticosteroids (see fluticasone, page 51). Tiotropium bromide is a long-acting antimuscarinic agent that exerts its pharmacological effect by inhibiting the M3 muscarinic receptors at the smooth muscles in the airways leading to bronchodilation. Tiotropium bromide capsules are comarketed by Boehringer Ingelheim and Pfizer under the trade name Spiriva and are self-administered by a commercial inhalation device.12

An earlier, structurally related bronchodilator, ipratropium, was introduced in 1986 by Boehringer Ingelheim under the name Atrovent. Ipratropium is a nonselective muscarinic receptor antagonist. It is also sold in combination with albuterol (Combivent, Duoneb).

h3c h3c

Ipratropium (Atroventâ„¢)

Ipratropium (Atroventâ„¢)

1. Treatments in Resp. Med. 2004, 3, 247-268; 2. Nat. Rev. Drug Discov. 2004, 3, 643-644; Rets. p. 82


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