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Related Concept Videos

Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

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Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
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Cholinergic Antagonists: Therapeutic Uses01:26

Cholinergic Antagonists: Therapeutic Uses

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Antimuscarinic drugs have various therapeutic applications by inhibiting parasympathetic stimulation in different systems. Here are the key therapeutic uses of antimuscarinics:    
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal...
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Antiasthma Drugs: Muscarinic Receptor Antagonists01:20

Antiasthma Drugs: Muscarinic Receptor Antagonists

2.0K
Muscarinic receptor antagonists, also known as antimuscarinic agents, are a class of bronchodilators used to treat asthma, although they are more commonly used to treat COPD. They work by inhibiting the action of acetylcholine (ACh), a neurotransmitter, on muscarinic receptors found in the airways.
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
2.0K
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

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Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren...
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Antiasthma Drugs: β2-Adrenoceptor Agonists01:25

Antiasthma Drugs: β2-Adrenoceptor Agonists

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Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce...
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Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

2.5K
Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
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Related Experiment Video

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Dry Powder and Nebulized Aerosol Inhalation of Pharmaceuticals Delivered to Mice Using a Nose-only Exposure System
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Tiotropium formulations and safety: a network meta-analysis.

Mario Cazzola1, Luigino Calzetta2, Paola Rogliani2

  • 1Department of Systems Medicine, University of Rome Tor Vergata, Via Montpellier 1, 00133 Rome, Italy.

Therapeutic Advances in Drug Safety
|February 17, 2017
PubMed
Summary

Tiotropium HandiHaler generally shows a superior safety profile compared to the Respimat Soft Mist Inhaler (SMI), though no statistical differences were found. Individual patient cardiovascular responses to antimuscarinic drugs are key.

Keywords:
COPDhandihalermeta-analysisrespimat SMIsafetytiotropium

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Area of Science:

  • Pharmacology
  • Respiratory Medicine
  • Clinical Evidence Synthesis

Background:

  • Tiotropium is available via two inhaler devices: HandiHaler (18 µg) and Respimat Soft Mist Inhaler (SMI) (5 µg).
  • Previous trials suggested similar safety profiles, but further evaluation is warranted.
  • Understanding device-specific safety is crucial for optimal patient care in respiratory diseases.

Purpose of the Study:

  • To conduct a safety evaluation comparing tiotropium HandiHaler 18 µg versus tiotropium Respimat SMI (5 µg and 2.5 µg).
  • To systematically review and meta-analyze existing clinical evidence on tiotropium inhaler safety.
  • To identify potential differences in safety profiles between the two delivery devices.

Main Methods:

  • Systematic review and network meta-analysis of available clinical trial data.
  • Inclusion of a large number of patients to ensure robust statistical power.
  • Safety outcome assessment, including serious adverse events (AEs) and cardiovascular (CV) responses.

Main Results:

  • The meta-analysis indicated a generally superior safety profile for tiotropium HandiHaler compared to tiotropium Respimat SMI.
  • No statistically significant difference in safety was detected between the HandiHaler and Respimat SMI devices.
  • A Specialized Utility-Based Reliability Assessment (SUCRA) analysis favored tiotropium Respimat SMI for serious adverse events.

Conclusions:

  • While HandiHaler may have a generally superior safety profile, current evidence does not suggest higher risks with Respimat SMI.
  • Individual patient variability in cardiovascular response to muscarinic receptor blockade is a significant factor.
  • Proactive identification of patients at increased risk for cardiovascular adverse events with antimuscarinic therapy is essential.