Ipratropium drug class
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Ipratropium Drug Class: An Overview
Anticholinergic Bronchodilator
Ipratropium bromide is classified as an anticholinergic bronchodilator. It works by inhibiting cholinergic bronchomotor tone, which leads to bronchodilation, making it effective in treating obstructive airways diseases such as asthma and chronic obstructive pulmonary disease (COPD)1 4 7.
Mechanism of Action
Ipratropium achieves its bronchodilatory effect by blocking the action of acetylcholine on muscarinic receptors in the bronchial smooth muscle. This inhibition reduces cyclic guanosine monophosphate (cGMP) levels, leading to muscle relaxation and airway dilation1 4. Unlike beta-adrenergic agonists, which primarily act on smaller airways, ipratropium tends to affect larger and intermediate-sized airways7.
Pharmacokinetics
When administered via inhalation, ipratropium has a low systemic absorption rate, with about 30% of the drug being absorbed orally and even less when inhaled. Peak plasma concentrations are reached approximately three hours post-administration. The drug is metabolized into eight metabolites, which are excreted equally in feces and urine. The elimination half-life of ipratropium is between 3.2 to 3.8 hours1.
Therapeutic Efficacy
Asthma and Chronic Bronchitis
Ipratropium is somewhat less effective than beta2-adrenoceptor agonists like salbutamol in asthma patients but is equally effective in treating chronic bronchitis1. It provides significant bronchodilation within minutes of inhalation, with maximum effects occurring between 1.5 to 2 hours and lasting for about 4 to 6 hours1 4.
Chronic Obstructive Pulmonary Disease (COPD)
In COPD patients, ipratropium has shown to be effective in improving lung function. Studies comparing ipratropium with other bronchodilators like metaproterenol and albuterol have demonstrated that ipratropium often provides a longer duration of action and greater improvement in forced expiratory volume (FEV1) and forced vital capacity (FVC)2 3 5.
Combination Therapy
Combining ipratropium with beta2-agonists, theophylline, or sodium cromoglycate often results in a greater bronchodilatory response than using a single drug. This combination therapy is particularly beneficial for patients who do not respond adequately to a single drug regimen1 6 9.
Safety and Side Effects
Ipratropium is generally well-tolerated with minimal systemic effects. Common side effects include dryness of the mouth, a "scratching" sensation in the trachea, and a bad taste in the mouth. Unlike beta-agonists, ipratropium does not cause tremors or significant cardiovascular changes1 3 7.
Conclusion
Ipratropium bromide is a valuable anticholinergic bronchodilator used primarily for managing asthma and COPD. Its mechanism of action, pharmacokinetics, and therapeutic efficacy make it a suitable alternative or adjunct to beta2-agonists, especially in patients who experience side effects or inadequate response to other treatments. The drug's safety profile further supports its use in long-term management of obstructive airway diseases.
Sources and full results
Most relevant research papers on this topic
Ipratropium Bromide: A Review of its Pharmacological Properties and Therapeutic Efficacy in Asthma and Chronic Bronchitis
Ipratropium bromide is a suitable alternative to 2-adrenoceptor agonist drugs for patients not fully responding to these agents, and may be useful in patients with side effects from 2-adrenoceptor agonists.
Literature ReviewA randomised controlled comparison of tiotropium and ipratropium in the treatment of chronic obstructive pulmonary disease
Tiotropium significantly improves lung function and peak expiratory flow more effectively than ipratropium in chronic obstructive pulmonary disease patients.
RCT
Highly CitedComparison of the anticholinergic bronchodilator ipratropium bromide with metaproterenol in chronic obstructive pulmonary disease. A 90-day multi-center study.
Inhaled ipratropium bromide is more effective and safer than metaproterenol for long-term treatment of chronic obstructive pulmonary disease (COPD).
RCTHighly CitedBronchodilator action of the anticholinergic drug, ipratropium bromide (Sch 1000), as an aerosol in chronic bronchitis and asthma.
Ipratropium bromide is an effective bronchodilator for both asthma and chronic bronchitis, with optimal doses of 40 to 80 mcg, and shows prolonged efficacy compared to isoproterenol.
RCTHighly CitedComparison of ipratropium bromide and albuterol in chronic obstructive pulmonary disease: a three-center study.
Ipratropium bromide has longer duration of action and may be effective when beta 2 agonists are not effective in treating chronic obstructive pulmonary disease.
RCTThe role of ipratropium bromide in the emergency management of acute asthma exacerbation: a metaanalysis of randomized clinical trials.
Ipratropium bromide combined with beta-agonists effectively improves airflow and reduces hospitalizations in adults with acute asthma exacerbation.
Meta-AnalysisHighly CitedClinical pharmacology and toxicology of ipratropium bromide.
Ipratropium bromide is a promising anticholinergic drug for treating airflow obstruction, with promising effects on large- and intermediate-size airways without toxic effects.
Transport of ipratropium, an anti-chronic obstructive pulmonary disease drug, is mediated by organic cation/carnitine transporters in human bronchial epithelial cells: implications for carrier-mediated pulmonary absorption.
Ipratropium and tiotropium are primarily taken up by OCTN2, with a lesser extent by OCTN1, in human bronchial epithelial cells, resulting in carrier-mediated pulmonary absorption.
In Vitro StudyHighly CitedA meta-analysis of the effects of ipratropium bromide in adults with acute asthma.
Ipratropium bromide adds modest improvement in pulmonary function and reduces hospital admissions in adults with acute asthma treated with beta-agonists.
Meta-AnalysisHighly CitedNebulized ipratropium in the treatment of acute asthma.
Ipratropium alone or combined with salbutamol does not significantly improve peak flow rates in acute asthma patients.
RCTHighly Cited