Imidafenacin
Imidafenacin Uses, Dosage, Side Effects, Food Interaction and all others data.
Imidafenacin is an antispasmodic agent with anticholinergic effects. It antagonizes muscarinic receptors in the bladder to reduce the frequency of urination in the treatment of overactive bladder. It is marketed in Japan under the tradenames Staybla by Ono Pharmaceutical and Uritos by Kyojin Pharmaceutical.
Imidafenacin is an antimuscarinic agent which acts to reduce the frequency of urination in patients with overactive bladder .
| Trade Name | Imidafenacin |
| Generic | Imidafenacin |
| Imidafenacin Other Names | Imidafenacin |
| Type | |
| Formula | C20H21N3O |
| Weight | Average: 319.408 Monoisotopic: 319.168462308 |
| Protein binding | Imidafenacin is 88% bounf by human plasma proteins . It binds to serum albumin and α1-acid glycoprotein. |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Imidafenacin is an antispasmodic with anticholinergic effects used to reduce urinary frequency.
Used in the treatment of overactive bladder .
Imidafenacin is also used to associated treatment for these conditions: Urinary Bladder, Overactive, Urinary Incontinence (UI), Urinary Urge Incontinence, Urinary Urgency, Increased frequency of urination
How Imidafenacin works
Imidafenacin binds to and antagonizes muscarinic M1 and M3 receptors with high affinity . It also antagonizes muscarinic M2 receptors but with lower affinity. M3 receptors stimulate contraction of the detrusor muscle in the bladder via release of calcium from the sarcoplasmic reticulum . M2 receptors are also present in the detrusor muscle but serve to inhibit adenylate cyclase which reduces the relaxation mediated by β adrenergic receptors. Finally, M1 receptors are present on the parasympathetic neurons which release acetylcholine in the bladder. They act as an autocrine positive feedback loop and further increase release of acetylcholine. Antagonism of these receptors by imidafenacin prevents contraction of the bladder's detrusor muscle, prevents inhibition of the relation produced by sympathetic tone, and reduces acetylcholine release. Together these reduce the frequency of urination.
Toxicity
Clinically significant adverse reactions to imidafenacin are acute glaucoma (0.06%), urinary retention (0.03%), and heptic dysfunction (0.02%) . The most common adverse effects observed with imidafenacin are thirst (37.7%), constipation (13.6%).
Volume of Distribution
The estimated volume of distribution is 43.9 L .
Elimination Route
The absolute oral bioavailability is 57.8% . Tmax is 1-3 h after administration.
Half Life
The half life of elimination is 3 h .
Clearance
The estimated clearance is 21.2 L/h .
Elimination Route
10% is excreted in the urine as the parent compound . Most is eliminated by metabolism thought to be mediated by CYP3A4 and UGT1A4.
Innovators Monograph
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