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

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:

    • 20 mg twice daily
  • Extended-release:

    • 60 mg once a day in the morning

Dose in Children:

Not indicated. 

Pregnancy Risk Factor C

  • Animal reproduction studies have shown adverse pregnancy outcomes.
  • Its use in human pregnancies has not been proven.
  • However, there are limited data. It should only be used with caution, and only when clearly indicated.

Use during breastfeeding:

  • It is unknown if the drug is found in breastmilk. 
  • Manufacturers recommend that you stop breastfeeding or discontinue the drug.
  • This is based on the potential risks for the baby and the benefits to the mother.

Trospium (Regurin) Dose in Kidney Disease:

  • CrCl ≥30 mL/minute:
    • No dosage adjustment provided in the manufacturer's labeling.
    • However, patients should be monitored for adverse events as renal impairment increases the drug's systemic exposure.
  • CrCl <30 mL/minute:
    • Immediate-release: 20 mg once a day at bedtime.
    • Extended-release: Avoid using the extended-release formulation.

Dose in Liver disease:

  • Mild impairment:
    • No dosage adjustment provided in the manufacturer's labeling.
  • Moderate to severe impairment:
    • No dosage adjustment provided in the manufacturer's labeling;
    • Use with caution.

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):

 

  • Allergy reactions to any component of the drug or the drug itself
  • Patients who might develop gastric or urinary retention
  • Patients suffering from uncontrolled narrow-angle vision impairment

Warnings and precautions

  • Angioedema
    • This condition can lead to severe allergic reactions. 
    • Angioedema can occur in the lips, face, tongue, larynx, and/or lips. 
    • The treatment should be stopped immediately if the patient experiences facial swelling, hypopharynx or larynx swelling.
  • CNS effects

    • People who work with heavy machinery, such as operators of heavy machinery, should be cautious about using it.
    • It can cause CNS depression, confusion, hallucinations, blurred vision.
  • Alzheimer's disease

    • Alzheimer's patients should be cautious when taking the drug.
  • Bladder flow obstruction

    • Urinary retention may occur. Patients with obstruction of the urinary tract should not use it.
  • Gastrointestinal obstructive disorders:

    • Gastric retention may be increased by taking the drug. Patients with obstructive gastro-intestinal disorders, such as pyloricstensis, should not take the drug.
  • Glaucoma:

    • Patients with narrow-angle glaucoma (controlled) should be cautious.
  • Hepatic impairment

    • Patients with severe or moderate liver impairment should be cautious when taking the drug.
  • Myasthenia gravis:

    • Patients with myasthenia Gravis should be cautious when taking the drug due to reduced gastrointestinal motility.
  • Renal impairment

    • Extended-release formulations should be avoided by patients with severe renal impairment. 
    • Patients with severe renal impairment should be cautious when using the immediate-release formulation.
  • Ulcerative colitis

    • Patients with ulcerative colitis should use it with caution due to the decreased GI motility.

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:

  • Monitor the anticholinergic effects such as dry mouth, constipation, and dizziness.
  • Monitor renal functions, postvoid residual (PVR) urine volume, and urinary tract infection before treatment initiation. 

How to administer Trospium (Regurin)?

Immediate-release:

  • It may be administered before (at least one hour) meals with a glass of water.

Extended-release:

  • The extended-release formulation is administered at least one hour before meals on an empty stomach with a glass of water.

Mechanism of action of Trospium (Regurin):

It decreases the tone and smoothness of the bladder's smooth muscles by blocking the action of Acetylcholine at muscarinic nerves. It is most harmful to organs innervated by cholinergic neuron.

Absorption:

  • Below 10%
  • Absorption is decreased with a high-fat meal.

Protein binding:

  • 48% to 85% in vitro

Metabolism:

  • It is metabolized via esterase hydrolysis and conjugation.

Bioavailability:

  • Immediate-release formulation:
    • About 10% (range: 4% to 16%)

Half-life elimination:

  • Immediate-release formulation:
    • 20 hours
    • Severe renal insufficiency (CrCl <30 mL/minute): about 33 hours;
  • extended-release formulation:
    • about 35 hours

Time to peak plasma concentration: 5-6 hours

Excretion:

  • 85% of the drug is excreted in feces;
  • The rest is excreted in urine (about 6% mostly as unchanged drug) primarily via the process of 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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