Solifenacin


Generic Medicine Info
Indications and Dosage
Oral
Overactive bladder
Adult: 5 mg once daily; may increase to 10 mg once daily if needed.

Oral
Neurogenic detrusor overactivity
Child: ≥2 years As 1 mg/mL oral susp: 9-15 kg: Initially, 2 mg (Max: 4 mg); >15-30 kg: Initially, 3 mg (Max: 5 mg); >30-45 kg: Initially, 3 mg (Max: 6 mg); >45-60 kg: Initially, 4 mg (Max: 8 mg); >60 kg: Initially, 5 mg (Max: 10 mg). All doses are to be taken once daily. May titrate doses to the lowest effective dose after initiation.
Special Patient Group
Overactive bladder:
Patient taking strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir): Max: 5 mg once daily.

Neurogenic detrusor overactivity:
Patient taking strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir): Do not use more than the recommended initial doses.
Renal Impairment
Overactive bladder:
CrCl (mL/min) Dosage
≤30 Severe: Max: 5 mg once daily.

Neurogenic detrusor overactivity:
CrCl (mL/min) Dosage
≤30 Severe: Do not use more than the recommended initial doses.
Hepatic Impairment
Overactive bladder:
Moderate (Child-Pugh class B): Max: 5 mg once daily. Severe (Child-Pugh class C): Contraindicated.

Neurogenic detrusor overactivity:
Moderate (Child-Pugh class B): Do not use more than the recommended initial doses. Severe (Child-Pugh class C): Contraindicated.
Administration
May be taken with or without food. Swallow whole, do not chew/crush.
Contraindications
Myasthenia gravis, uncontrolled narrow-angle glaucoma, severe gastrointestinal condition (e.g. toxic megacolon, gastric retention); urinary retention (when used for overactive bladder). Patient undergoing haemodialysis. Severe hepatic impairment (Child-Pugh class C). Concomitant use with strong CYP3A4 inhibitors in patients with severe renal or moderate hepatic impairment.
Special Precautions
Patient with controlled narrow-angle glaucoma; Alzheimer's disease; known history of or predisposition to QT prolongation (e.g. hypokalaemia, concomitant use of drugs known to prolong QT interval); significant pre-existing cardiac disease (e.g. CHF, arrhythmia, myocardial ischaemia), risk of decreased gastrointestinal motility, gastrointestinal obstructive disorders; autonomic neuropathy, GERD, hiatus hernia. Not recommended for use in patients with significant bladder outlet obstruction (e.g. BPH) who are being treated for overactive bladder. Patient subjected to hot weather and/or exercise. Patient taking strong CYP3A4 inhibitors. Severe renal (CrCl ≤30 mL/min) and moderate hepatic (Child-Pugh class B) impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: QT prolongation and torsades de pointes (particularly in patients with known risk factors), CNS effects (e.g. headache, confusion, hallucinations, somnolence), heat prostration (in presence of high environmental temperature). Rarely, faecal impaction, colonic obstruction, intestinal obstruction; urinary retention.
Eye disorders: Blurred vision, dry eyes.
Gastrointestinal disorders: Dry mouth, nausea, abdominal pain, dyspepsia, constipation, dysgeusia, GERD, dry throat.
General disorders and administration site conditions: Fatigue, peripheral oedema.
Renal and urinary disorders: Cystitis, UTI, difficulty in micturition.
Respiratory, thoracic and mediastinal disorders: Nasal dryness.
Skin and subcutaneous tissue disorders: Dry skin.
Potentially Fatal: Angioedema associated with swelling of the upper airway. Rarely, anaphylactic reactions.
Patient Counseling Information
This drug may cause blurred vision, and uncommonly, drowsiness and tiredness, if affected, do not drive or operate machinery.
Monitoring Parameters
Evaluate other causes of frequent urination (e.g. heart failure, renal disease) prior to treatment. Monitor creatinine clearance, hepatic function, and urination pattern. Assess for signs and symptoms of anticholinergic effects (e.g. headache, confusion, hallucination, somnolence, fixed and dilated pupils, blurred vision, tremors, dry skin).
Overdosage
Symptoms: Severe anticholinergic effects (e.g. blurred vision, fixed and dilated pupils, tremors, dry skin). Management: Symptomatic and supportive treatment. Administer activated charcoal. Perform gastric lavage within 1 hour of ingestion but vomiting must not be induced. Give physostigmine or carbachol to treat hallucinations or pronounced excitation; benzodiazepines for convulsions; β-blockers for tachycardia. Administer pilocarpine eye drops and/or place the patient in a dark room in case of mydriasis. Employ artificial respiration during respiratory insufficiency and catheterisation for urinary retention. Monitor ECG as necessary.
Drug Interactions
Increased plasma concentration with strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir, nelfinavir, itraconazole). May enhance the therapeutic effects and adverse reactions when used concomitantly with other agents with anticholinergic activity; an interval of approx 1 week between using these drugs is recommended. May reduce efficacy with cholinergic receptor agonists. Efficacy of drugs that stimulate gastrointestinal motility (e.g. metoclopramide, cisapride) may be reduced by solifenacin.
Food Interaction
May increase serum levels with grapefruit juice.
Action
Description: Solifenacin is a selective, competitive inhibitor of the muscarinic M3 subtype receptor, which causes a decrease in urinary bladder contraction and detrusor muscle pressure, and an increase in residual urine volume.
Pharmacokinetics:
Absorption: Absorbed from the gastrointestinal tract. Bioavailability: Approx 90%. Time to peak plasma concentration: 3-8 hours (tab); 4-12 hours (oral susp).
Distribution: Plasma protein binding: Approx 98%, mainly to α1-acid glycoprotein.
Metabolism: Extensively metabolised in the liver, mainly by the CYP3A4 isoenzyme, but alternative metabolic pathways may also contribute; metabolism via N-oxidation and 4R-hydroxylation forms 1 active metabolite (4R-hydroxy solifenacin) and 3 inactive metabolites (N-glucuronide, N-oxide, and 4R-hydroxy-N-oxide solifenacin).
Excretion: Via urine (approx 70%; approx 11% as unchanged drug, 8% as the active metabolite, 9% as the 4R-hydroxy-N-oxide metabolite, 18% as the N-oxide metabolite); faeces (23%). Terminal elimination half-life: 45-68 hours (adults); approx 26 hours (children).
Chemical Structure

Chemical Structure Image
Solifenacin

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 154059, Solifenacin. https://pubchem.ncbi.nlm.nih.gov/compound/Solifenacin. Accessed Nov. 25, 2021.

Storage
Store between 15-30°C. Protect from light (oral susp).
MIMS Class
Other Drugs Acting on the Genito-Urinary System
ATC Classification
G04BD08 - solifenacin ; Belongs to the class of urinary antispasmodics.
References
Anon. Solifenacin. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/10/2021.

Anon. Solifenacin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/10/2021.

Buckingham R (ed). Solifenacin Succinate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2021.

Joint Formulary Committee. Solifenacin Succinate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2021.

Sequirus (NZ) Ltd. Vesicare 5 mg and 10 mg Film-Coated Tablets data sheet June 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 01/10/2021.

Solifenacin Succinate 1 mg/mL Oral Suspension (Glenmark Pharmaceuticals Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 01/10/2021.

Solifenacin Succinate 10 mg Film-Coated Tablets (Ascend Laboratoris [UK] Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 01/10/2021.

Solifenacin Succinate 5 mg Film-Coated Tablets (Ascend Laboratoris [UK] Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 01/10/2021.

Vesicare 10 mg Film-Coated Tablet (Astellas Pharma Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 20/10/2021.

Vesicare 5 mg & 10 mg Tablet (Astellas Pharma Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 01/10/2021.

Vesicare 5 mg Film-Coated Tablet (Astellas Pharma Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 20/10/2021.

Vesicare LS Suspension (Astellas Pharma US, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/10/2021.

Vesicare Tablet, Film Coated (Astellas Pharma US, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/10/2021.

Disclaimer: This information is independently developed by MIMS based on Solifenacin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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