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Related Concept Videos

Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists01:23

Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists

Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
Drugs for Treatment of Constipation-Predominant IBS01:21

Drugs for Treatment of Constipation-Predominant IBS

Pharmacological therapies for IBS-C are designed to alleviate abdominal discomfort and enhance bowel function. In patients with IBS-C, fiber supplements may help soften stools and decrease straining, but may also lead to increased gas production and bloating. Osmotic laxatives like milk of magnesia are frequently used to soften stools and increase stool frequency in IBS-C patients. In addition, two drugs approved for use in severe IBS-C adult cases are linaclotide (Linzess) and lubiprostone...
Drugs for Treatment of Diarrhea-Predominant IBS01:17

Drugs for Treatment of Diarrhea-Predominant IBS

Diarrhea-predominant irritable bowel syndrome (IBS-D) is a subtype of IBS characterized primarily by frequent, loose, or watery stools, abdominal pain, and abdominal discomfort. Therapeutic approaches to managing IBS-D include dietary changes, stress management techniques, and pharmaceutical interventions.
Two specific drugs used in the treatment are alosetron (Lotronex) and eluxadoline (Viberzi). Alosetron, a 5-HT3 antagonist, works by slowing the movement of stools in the gut, reducing bowel...
Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance01:23

Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance

The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
A study on guinea pigs examined the...
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
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Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

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 the conjunctiva.

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Related Experiment Video

Updated: Jun 16, 2026

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
09:34

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells

Published on: February 9, 2019

Solifenacin pharmacology.

Francisco J Morales-Olivas1, Luis Estañ

  • 1Departamento de Farmacología, Facultad de Medicina y Odontología, Universidad de Valencia, Avda. Blasco Ibáñez 15, Valencia, Spain. morales@uv.es

Archivos Espanoles De Urologia
|February 17, 2010
PubMed
Summary
This summary is machine-generated.

Solifenacin, an antimuscarinic, offers a favorable benefit/risk profile for overactive bladder due to its M3 receptor selectivity and limited drug interactions. Its metabolism and excretion support efficacy without dose adjustments in elderly or impaired patients.

Related Experiment Videos

Last Updated: Jun 16, 2026

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
09:34

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells

Published on: February 9, 2019

Area of Science:

  • Pharmacology
  • Urology

Background:

  • Antimuscarinics are primary treatments for overactive bladder (OAB).
  • Drug selectivity for muscarinic receptor subtypes influences efficacy and side effect profiles.
  • Metabolic pathways and drug interactions are critical considerations for antimuscarinic therapy.

Purpose of the Study:

  • To evaluate the selectivity and metabolic profile of solifenacin for OAB treatment.
  • To compare the risk of drug interactions and pharmacokinetic variability of solifenacin with other antimuscarinics.
  • To assess the contribution of solifenacin's metabolites and excretion to its therapeutic effect.

Main Methods:

  • Review of solifenacin's muscarinic receptor selectivity, particularly for M3 bladder receptors.
  • Analysis of solifenacin's metabolic pathways, focusing on cytochrome P450 (CYP) enzyme involvement (CYP3A4 and CYP2D6).
  • Comparison of solifenacin's pharmacokinetic properties and interaction risks with other antimuscarinic agents.

Main Results:

  • Solifenacin exhibits high selectivity for M3 bladder receptors, potentially reducing off-target side effects.
  • Solifenacin is primarily metabolized by CYP3A4 into inactive metabolites, with one active metabolite; it is not a substrate for polymorphic CYP2D6.
  • This metabolic profile results in a low risk of drug interactions, lower than antimuscarinics metabolized by CYP2D6.
  • Unmetabolized solifenacin and its active metabolite contribute to therapeutic effects via urothelial receptors.
  • No dose adjustment is required for solifenacin in elderly patients or those with moderate renal or hepatic impairment.

Conclusions:

  • Solifenacin's M3 receptor selectivity and favorable metabolic profile contribute to an advantageous benefit/risk ratio in OAB management.
  • The limited involvement of CYP2D6 in solifenacin metabolism minimizes pharmacokinetic variability and drug interaction risks.
  • Solifenacin offers a safe and effective treatment option for OAB, including in specific patient populations requiring no dose modification.