Trospium (Regurin) - Uses, Dose, MOA, Brands, Side effects

Trospium is a medication used to treat overactive bladder (OAB) symptoms such as frequent or urgent urination, incontinence, and urinary frequency. It belongs to a class of drugs called antimuscarinics, which work by relaxing the bladder muscles to reduce bladder contractions and control symptoms.

People with overactive bladder experience sudden, involuntary contractions of the bladder muscles, leading to symptoms like urgency, frequency, and incontinence. Trospium helps alleviate these symptoms by blocking the action of acetylcholine, a neurotransmitter that stimulates muscle contractions, particularly in the bladder.

Trospium (Regurin) decreases the tone of smooth muscles resulting in the relaxation of the bladder muscles. This enhances the urine flow relieving the symptoms of urgency, incontinence, and increased urinary frequency.

Trospium (Regurin) Uses:

  • Overactive bladder:
    • It is indicated for the treatment of overactive bladder in patients with symptoms of urgency, incontinence, and increased urinary frequency.

Trospium (Regurin) Dose in Adults

Trospium (Regurin) Dose in the treatment of Overactive bladder: Oral:

  • Immediate release:
    • Take 20 milligrams (mg) two times a day. This means you'd take it once in the morning and once in the evening.
  • Extended release:
    • Take 60 mg once a day, specifically in the morning.

Dose in Children:

Not indicated. 

Pregnancy Risk Factor C

  • Trospium has a pregnancy risk factor of C, which means there have been adverse effects noted in animal studies.
  • However, there haven't been enough studies done on pregnant women to determine its safety conclusively.
  • Doctors may prescribe it during pregnancy only if the benefits outweigh the potential risks, and there are no better alternatives available.

Use during breastfeeding:

  • It's unclear whether trospium is excreted in breast milk.
  • According to the manufacturer, when deciding whether to continue or stop breastfeeding while using trospium, it's essential to consider both the potential risk to the infant from exposure to the medication and the benefits of treatment for the mother.

Trospium (Regurin) Dose in Kidney Disease:

Patient with a Creatinine Clearance (CrCl) equal to or greater than 30 mL/minute:

  • No dosage adjustment is specified in the manufacturer's labeling.
  • However, it's important to note that renal impairment can lead to higher levels of trospium in the body, potentially increasing the risk of side effects.
  • Therefore, it's recommended to monitor for any signs of increased adverse effects in these individuals.

In cases where the CrCl is less than 30 mL/minute, the dosage recommendations differ:

  • Immediate release: Take 20 mg once daily at bedtime.
  • Extended release: It's not recommended to use the extended-release formulation in individuals with a CrCl less than 30 mL/minute.

Dose in Liver disease:

Patient with Mild hepatic impairment:

  • For patient with mild hepatic impairment, no dosage adjustment is specified in the manufacturer's labeling.

Patient with Moderate to severe hepatic impairment:

  • Patient with moderate to severe hepatic impairment, no specific dosage adjustment is recommended, but caution is advised when using trospium in these cases.

Common Side Effects of Trospium (Regurin):

  • Gastrointestinal:
    • Xerostomia

Less Common Side Effects of Trospium (Regurin):

  • Cardiovascular:
    • Tachycardia
  • Central Nervous System:
    • Headache
    • Fatigue
  • Dermatologic:
    • Skin Rash
    • Xeroderma
  • Gastrointestinal:
    • Constipation
    • Abdominal Pain
    • Dyspepsia
    • Flatulence
    • Abdominal Distention
    • Nausea
    • Dysgeusia
    • Vomiting
  • Genitourinary:
    • Urinary Tract Infection
    • Urinary Retention
  • Infection:
    • Influenza
  • Ophthalmic:
    • Dry Eye Syndrome
    • Blurred Vision
  • Respiratory:
    • Nasopharyngitis
    • Dry Nose

Contraindications to Trospium (Regurin):

  • Trospium should not be used by individuals who have a known hypersensitivity to trospium itself or any component of the formulation.
  • Additionally, it is contraindicated in patients with, or those at risk of, urinary retention (difficulty urinating), gastric retention (delayed emptying of the stomach), and uncontrolled narrow-angle glaucoma (a type of eye condition).
  • These conditions can be exacerbated by trospium and may lead to serious complications.

Warnings and precautions

Angioedema

  • Angioedema, which involves swelling in areas like the face, lips, tongue, and throat, has been reported in some cases with trospium use.
  • If you experience swelling in your tongue, hypopharynx (the area behind the tongue), or larynx (voice box), it's crucial to stop taking trospium immediately and seek medical help right away.
  • Angioedema can be serious and may require urgent treatment to prevent complications.
  • If you notice any signs of swelling or have difficulty breathing, don't hesitate to seek medical attention.

CNS effects

  • Trospium can affect the central nervous system (CNS), potentially causing side effects such as drowsiness, confusion, dizziness, hallucinations, and blurred vision.
  • These effects can impair both physical and mental abilities.
  • Patients should be advised to use caution when engaging in activities that require mental alertness, such as operating machinery or driving vehicles.
  • If you experience any of these side effects, it's essential to avoid activities that could be dangerous until you know how trospium affects you individually.

Alzheimer's disease

  • Trospium should be used with caution in patients with Alzheimer's disease.
  • This caution is important because trospium can affect cognitive function and may exacerbate cognitive impairment in individuals with Alzheimer's disease.

Bladder flow obstruction

  • Trospium should be used cautiously in patients with bladder flow obstruction.
  • This caution is necessary because trospium can potentially increase the risk of urinary retention in individuals with obstructive conditions affecting the bladder.

Gastrointestinal obstructive disorders:

  • Trospium should be used with caution in patients with gastrointestinal obstructive disorders, such as pyloric stenosis.
  • This caution is important because trospium may potentially increase the risk of gastric retention, a condition where the stomach does not empty properly.
  • Patients with gastrointestinal obstructive disorders are already at risk of complications related to impaired stomach emptying, and trospium could exacerbate this condition.

Glaucoma:

  • Trospium should be used cautiously in patients with controlled narrow-angle glaucoma.
  • Although it's treated and controlled, narrow-angle glaucoma is a condition where the fluid in the eye doesn't drain properly, leading to increased pressure inside the eye.
  • Trospium can potentially worsen this condition by causing certain eye-related side effects.

Hepatic impairment

  • Trospium should be used cautiously in patients with moderate or severe hepatic impairment.
  • The liver plays a crucial role in metabolizing medications like trospium, and impaired liver function can affect how the body processes the drug.

Myasthenia gravis:

  • Trospium should be used with caution in patients with myasthenia gravis, a condition characterized by muscle weakness, including the muscles involved in gastrointestinal (GI) motility.
  • Trospium works by relaxing the bladder muscles, but it can also affect other smooth muscles in the body, potentially leading to decreased GI motility.
  • In individuals with myasthenia gravis, whose GI motility may already be compromised, trospium could exacerbate this condition.

Renal impairment

  • In patients with renal impairment, caution should be exercised when using the immediate-release formulation of trospium.
  • Dosage adjustment is necessary in these cases to ensure safe and effective use of the medication.
  • However, the extended-release formulation of trospium is not recommended for individuals with severe renal impairment, where the creatinine clearance (CrCl) is less than 30 mL/minute.

Ulcerative colitis

  • Trospium should be used with caution in patients with ulcerative colitis due to its potential to decrease gastrointestinal (GI) motility.
  • Ulcerative colitis is a condition characterized by inflammation and ulcers in the colon and rectum, which can already disrupt normal bowel function.
  • Trospium, by reducing GI motility, may exacerbate symptoms in individuals with ulcerative colitis.

Trospium: Drug Interaction

Risk Factor C (Monitor therapy)

Acetylcholinesterase Inhibitors

May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors.

Amantadine

May enhance the anticholinergic effect of Anticholinergic Agents.

Anticholinergic Agents

May enhance the adverse/toxic effect of other Anticholinergic Agents.

Botulinum Toxin-Containing Products

May enhance the anticholinergic effect of Anticholinergic Agents.

Cannabinoid-Containing Products

Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol.

Chloral Betaine

May enhance the adverse/toxic effect of Anticholinergic Agents.

Gastrointestinal Agents (Prokinetic)

Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic).

Glucagon

Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased.

Itopride

Anticholinergic Agents may diminish the therapeutic effect of Itopride.

MetFORMIN

May decrease the serum concentration of Trospium.

Mianserin

May enhance the anticholinergic effect of Anticholinergic Agents.

Mirabegron

Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron.

Nitroglycerin

Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption.

Opioid Agonists

Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination.

Ramosetron

Anticholinergic Agents may enhance the constipating effect of Ramosetron.

Thiazide and Thiazide-Like Diuretics

Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics.

Topiramate

Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate.

Risk Factor D (Consider therapy modification)

Alcohol (Ethyl)

May enhance the CNS depressant effect of Trospium. Alcohol (Ethyl) may increase the serum concentration of Trospium. Specifically, alcohol may increase the peak (maximum) serum concentration of trospium when consumed within 2 hours of taking extendedrelease trospium. Management: Avoid consuming any alcohol within 2 hours of taking a dose of trospium XR.

Pramlintide

May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract.

Secretin

Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin.

Risk Factor X (Avoid combination)

Aclidinium

May enhance the anticholinergic effect of Anticholinergic Agents.

Cimetropium

Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium.

Eluxadoline

Anticholinergic Agents may enhance the constipating effect of Eluxadoline.

Glycopyrrolate (Oral Inhalation)

Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation).

Glycopyrronium (Topical)

May enhance the anticholinergic effect of Anticholinergic Agents.

Ipratropium (Oral Inhalation)

May enhance the anticholinergic effect of Anticholinergic Agents.

Levosulpiride

Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride.

Oxatomide

May enhance the anticholinergic effect of Anticholinergic Agents.

Potassium Chloride

Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride.

Potassium Citrate

Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate.

Revefenacin

Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin.

Tiotropium

Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium.

Umeclidinium

May enhance the anticholinergic effect of Anticholinergic Agents.

Monitoring parameters:

Considerations Before Starting Trospium Therapy:

  • Anticholinergic Effects: Trospium may cause side effects like dry mouth, constipation, and dizziness due to its anticholinergic properties.
  • Renal Function: Before starting trospium, it's important to assess renal function, especially in individuals with kidney problems, as dosage adjustments may be necessary.
  • Postvoid Residual (PVR) Urine Volume: Monitoring PVR urine volume is essential to ensure proper bladder emptying. Trospium may increase PVR urine volume, which could indicate urinary retention.
  • Urinary Tract Infection (UTI) Risk: Assessing for urinary tract infections prior to initiating trospium therapy is crucial to prevent potential complications or worsening of symptoms.

How to administer Trospium (Regurin)?

Immediate Release:

  • Administer with water.
  • Take on an empty stomach.
  • Take at least 1 hour before meals.

Extended Release:

  • Administer with water.
  • Take in the morning.
  • Take on an empty stomach.
  • Take at least 1 hour before a meal.

Mechanism of action of Trospium (Regurin):

  • Trospium works by blocking the effects of acetylcholine on muscarinic receptors in organs that are controlled by the nervous system.
  • Specifically, it targets cholinergically innervated organs, where acetylcholine plays a role in muscle contraction.
  • By blocking these receptors, trospium reduces the smooth muscle tone of the bladder.
  • This action helps to relax the bladder muscles, leading to a decrease in bladder contractions and an improvement in symptoms associated with overactive bladder, such as urgency and frequency of urination.

Absorption:

  • Less than 10% of trospium is absorbed.
  • Absorption is reduced when taken with a high-fat meal.

Distribution:

  • Volume of distribution ranges from 395 to over 600 liters.
  • Trospium is primarily distributed in plasma.

Protein Binding:

  • In vitro, trospium binds to proteins in the range of 48% to 85%.

Metabolism:

  • Trospium is hypothesized to undergo esterase hydrolysis and conjugation, leading to the formation of metabolites.

Bioavailability:

  • Immediate release formulation has a bioavailability of approximately 10%, ranging from 4% to 16%.

Half-life Elimination:

  • Immediate release formulation: 20 hours.
  • In severe renal insufficiency (CrCl <30 mL/minute): Approximately 33 hours for immediate release formulation and around 35 hours for extended release formulation.

Time to Peak, Plasma:

  • Trospium reaches peak plasma concentration in 5-6 hours after administration.

Excretion:

  • Approximately 85% of trospium is excreted in the feces.
  • Around 6% is excreted in urine, primarily as unchanged drug via active tubular secretion.

International Brand Names of Trospium:

  • MAR-Trospium
  • Sanctura XR
  • Trosec
  • Ceris
  • Descalon
  • Flotros
  • Inkotan
  • Prometrium
  • Regurin
  • Spasium
  • Spasmed
  • Spasmex
  • Spasmo-Lyt
  • Spasmo-Urgenin Neo
  • Spasmolyt
  • Spasmoplex
  • Stocpium
  • Tiromax
  • Tospin
  • Trosmolyt
  • Trospas
  • Uracare
  • Uraplex
  • Urivesc
  • Urivesc BID
  • Urivesc SR

Trospium Brand Names in Pakistan:

No Brands Available in Pakistan

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