China
Africa
Explore chapters and articles related to this topic
Cholinergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Vishal S. Gulecha, Manoj S. Mahajan, Aman Upaganlawar, Abdulla Sherikar, Chandrashekhar Upasani
Oxybutynin, a nonselective muscarinic blocker, is the drug of choice for UI. This agent has direct smooth muscle relaxant properties. The other drug, terodiline, possesses additional Ca2+ channel-blocking activity that makes it important in the treatment of UI (Langtry and McTavish, 1990). A newer nonselective anti-muscarinic tolterodine has bladder selectivity over salivary secretions. Therefore, it is well tolerated and effective in patients with UI with reduced tendency to cause xerostomia (Chapple et al., 2004; Oyasu et al., 1994).
Antagonists at Muscarinic Cholinergic Receptors
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Terodiline exhibits muscarinic blocking activity in animal and human isolated detrusor muscle, the (−)-isomer being more potent. Additionally, it has Ca2+ blocking properties, since it inhibits K+-induced contractions which are due to Ca2+ influx through voltage-operated L-type Ca2+ channels. This effect appears to be specific for the bladder. Terodiline is well tolerated, the only side-effects arising from muscarinic receptor blockade. It is rapidly absorbed after oral administration and has an elimination half-life of -60 hr. It has been found to be effective in reducing diurnal and nocturnal micturition frequency and episodes of incontinence, and has gained a valuable place in therapy (Langtry & McTavish 1990). However, it has now been withdrawn worldwide after reports of serious heart rhythm disturbances in people taking the drug. It appears to depress the SA node and is therefore probably unrelated to muscarinic receptor blockade and not likely to occur with other agents in this class.
Cardiovascular effects of antimuscarinic agents and beta3-adrenergic receptor agonist for the treatment of overactive bladder
Published in Expert Opinion on Drug Safety, 2018
Gian Marco Rosa, Danilo Baccino, Alberto Valbusa, Carolina Scala, Fabio Barra, Claudio Brunelli, Simone Ferrero
Another AM drug that was related with different reports of TdP is terodiline. This drug is an hERG channel inhibitor that was associated with QTc prolongation in a concentration-dependent manner. Due to this fact and to different reports of cardiac dysrhythmia including advanced AV block, TdP, and ventricular fibrillation, it was withdrawn in 1991 [72,73]. The withdrawal of this drug might be also due to the finding of an increased dispersion of the ventricular repolarization duration, which has an important pro-arrhythmic role [72].