Solifenacin (Vesicare) is an antimuscarinic drug that is used to treat patients with symptoms of overactive bladder manifesting as urgency, frequency, and urinary incontinence.

Solifenacin Uses:

• Overactive bladder:

  • Treatment of overactive bladder with symptoms of increased urinary frequency, urgency, and/or urge incontinence.

Solifenacin (Vesicare) Dose in Adults

Solifenacin (Vesicare) Dose in the treatment of Overactive bladder:

• 5 mg orally once a day initially,
• if tolerated, the dose may be increased to 10 mg once daily.

Solifenacin dose adjustment with concomitant potent CYP3A4 inhibitors (eg, ketoconazole):

• Maximum dose: 5 mg/day

Solifenacin (Vesicare) Dose in Childrens

Not recommended for use in children.

Pregnancy Risk Factor C

• In some studies on animal reproduction, adverse events were reported.

Solifenacin use during breastfeeding:

• It is unknown if the drug is found in breast milk.
• Manufacturer suggests that a decision is made about whether to withhold nursing care or discontinue using the drug.

Vesicare Dose in Kidney Disease:

• CrCl ≥30 mL/minute:

  • There are no dosage adjustments provided in the drug manufacturer's labeling;
  • use with caution.

• CrCl <30 mL/minute:

  • Maximum dose: 5 mg/day

Vesicare Dose in Liver disease:

• Mild impairment (Child-Pugh class A):

  • No dosage adjustment necessary;
  • use with caution.

• Moderate impairment (Child-Pugh class B):

  • Maximum dose: 5 mg/day.

• Severe impairment (Child-Pugh class C):

  • Use is not recommended.

Common Side Effects of Solifenacin (Vesicare):

• Gastrointestinal:

  • Xerostomia
  • Constipation

Less Common Side Effects of Vesicare:

• Cardiovascular:

  • Hypertension
  • Lower Extremity Edema

• Central Nervous System:

  • Fatigue
  • Depression

• Gastrointestinal:

  • Dyspepsia
  • Nausea
  • Upper Abdominal Pain
  • Vomiting

• Genitourinary:

  • Urinary Tract Infection
  • Urinary Retention

• Ophthalmic:

  • Blurred Vision
  • Dry Eye Syndrome

• Respiratory:

  • Cough

• Miscellaneous:

  • Influenza

Contraindications to Solifenacin (Vesicare):

• Hypersensitivity to solifenacin and any component of the formulation
• Urinary retention
• gastric retention
• Uncontrolled narrow-angle glaucoma
• Dialysis

Warnings and precautions

• Angioedema

  • Reports of angioedema in the lips, face, tongue, or larynx were reported.
  • Some cases occurred even after the first dose.
  • Allergies can be life-threatening.
  • If you are concerned about your tongue, hypopharynx or larynx, stop immediately and start supportive care.

• CNS effects

  • There have been reports of CNS side effects (eg headache, confusion, hallucinations and somnolence).
  • Monitor for CNS effects at treatment initiation and dose increases;
  • If necessary, reduce or stop taking the medication.
  • This may cause blurred or drowsy vision and/or drowsiness, which can impair mental and physical abilities.
  • It is important to warn patients about tasks that require mental alertness, such as operating machinery or driving.

• Heat prostration:

  • It may occur when the environment temperature is elevated
  • Take care when exercising or in hot weather.

• Hypersensitivity reactions

  • Rarely have anaphylactic reactions been reported.
  • If an anaphylactic reaction occurs, stop taking the medication immediately.

• Alzheimer disease

  • Preliminary data suggests that anticholinergics could potentially have an adverse effect on the clinical course Alzheimer's disease in patients who are taking cholinesterase inhibitors.
  • Patients with dementia who are receiving dual therapy (acetylcholinesterase inhibitor, bladder anticholinergic) should be monitored for any changes in cognition or functional abilities.

• Bladder outflow obstruction

  • Patients with bladder obstruction (eg BPH) should be cautious.
  • It could increase your risk of having urinary retention.

• Gastrointestinal Disease:

  • Patients with reduced GI motility (severe colitis, ulcerative colitis), or GI obstructive conditions (pyloric stenosis) should be cautious.
  • It could increase the risk for gastric retention.

• Glaucoma:

  • Patients with narrow-angle glaucoma that has been treated (controlled) should be cautious.
  • Uncontrolled narrow-angle vision impairment is a reason to avoid its use.

• Hepatic impairment

  • Patients with moderate hepatic impairment (Child Puugh class B) should be cautious.
  • Patients with severe hepatic impairment (Child Pugh class C) may need to adjust their dosage.

• Extension of QT

  • Use with caution in patients with a known history of QT prolongation or other risk factors for QT prolongation (eg, concomitant use of medications known to prolong QT interval, and electrolyte abnormalities).
  • Dose-related QT prolongation risk

• Renal impairment

  • Patients with impaired renal function should be cautious.
  • For severe renal impairment (CrCl 30mL/minute), dosage adjustment is necessary.

Solifenacin: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

• Anticholinergic effects including:
  • CNS effects such as headache, confusion, hallucinations, somnolence),
  • fixed and dilated pupils
  • blurred vision
  • tremors
  • dry skin
• creatinine clearance
• hepatic function
• post-void residuals when added to alpha-blocker therapy for BPH.

How to administer Solifenacin (Vesicare)?

• Administer with water without regard to food.
• Swallow whole. Do not crush or chew.

Mechanism of action of Solifenacin (Vesicare):

• It blocks the muscarinic receptors, resulting in decreased bladder contraction, increased urine volume, and decreased muscle pressure.

Protein binding:

• 98%, mainly due to alpha-acid glycoprotein

Metabolism:

• Hepatic disease; forms active and inactive metabolites via N-oxidation, 4 R-hydroxylation and 1 R-hydroxylation. Primary route for elimination is via CYP3A4.

Bioavailability:

• 90%

Half-life elimination:

• Chronic dosing can take 45-68 hours; prolongation in severe renal impairment (CrCl 30mL/minute) and moderate hepatic impairment (Child Pugh class B).

Plasma peak time:

• 3-8 hours

Excretion:

• Urine (69.2%; 15% as an unchanged drug);
• feces (22.5%)

International Brands of Solifenacin:

• VESIcare
• ACT-Solifenacin
• APO-Solifenacin
• Auro-Solifenacin
• JAMP-Solifenacin
• MED-Solifenacin
• MINT-Solifenacin
• PMS-Solifenacin
• RAN-Solifenacin
• SANDOZ Solifenacin
• TEVA-Solifenacin
• VESIcare
• Asolfena
• Bispec
• Slowurge
• Sofcare
• Solficare
• Solicin
• Soliten
• Somfen
• Tormeel
• Urisol
• Utrobin
• Vesicare
• Vesiker
• Vesikur
• Vesitrim
• Vesizen
• Zevesin

Solifenacin Brand Names in Pakistan: