Solifenacin

Registered South African indications:

• Symptomatic treatment of overactive bladder syndrome: symptoms of urinary urgency, frequent micturition and/or urge incontinence

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Urinary retention
• Uncontrolled narrow angle glaucoma
• Myasthenia gravis
• Toxic megacolon
• Patients undergoing haemodialysis
• Patients with severe hepatic impairment
• Patients with severe renal impairment (ClCr < 30ml/min) and on treatment with a strong CYP3A4 inhibitor, e.g. ketoconazole
• Patients with moderate hepatic impairment and on treatment with a strong CYP3A4 inhibitor, e.g. ketoconazole
• Patients with a prolonged QT interval, either congenital or acquired
• Pregnancy
• Lactation

Contraindications registered in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Solifenacin is contraindicated in patients with the following condition or at risk for these conditions
  • Urinary retention
  • Severe gastro-intestinal conditions (including toxic megacolon)
  • Myasthenia gravis
  • Narrow-angle glaucoma
• Patients undergoing haemodialysis
• Patients with severe hepatic impairment
• Patients with severe renal impairment or moderate hepatic impairment and who are on treatment with a potent CYP3A4 inhibitor, e.g. ketoconazole

• Pregnancy (Recommendations in other jurisdictions)
• Breastfeeding (Recommendations in other jurisdictions)
• Severe renal impairment
• Moderate hepatic impairment
• Clinically significant bladder outflow obstruction at risk of urinary retention
• Gastrointestinal obstructive disorders
• Risk of decreased gastrointestinal motility
• Hiatus hernia
• Gastroesophageal reflux
• Autonomic neuropathy
• Risk factors to QT prolongation and Torsade de Pointes
• Pre-existing long QT syndrome
• Neurogenic cause for detrusor overactivity
• Hypokalaemia
• Concomitantly taking medicinal products that can cause or exacerbate oesophagitis
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• Driving and the ability to use machinery

Forms avail. in SA and covered in this monograph: fct, tab, chu

Symptomatic treatment of overactive bladder syndrome: symptoms of urinary urgency, frequent micturition and/or urge incontinence

• Oral (fct, tab, chu): 5mg, once daily; If needed the dose may be increased: 10mg, once daily

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Solifenacin tablets (fct, tab) should be taken orally and should be swallowed whole with liquids. It can be taken with or without food

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Solifenacin chewable tablets (chu) should be taken orally and chewed. It can be taken with or without food, as is convenient

Not established for use in children

Pregnancy

South African recommendations

• Contraindicated
• The use of solifenacin is contraindicated during pregnancy
• No clinical data are available from women who became pregnant while taking solifenacin. Foetal toxicity has been shown in rodents

Recommendations in other jurisdictions

• Caution
• No clinical data are available from women who became pregnant while taking solifenacin. Animal studies do not indicate direct harmful effects on fertility, embryonal / foetal development or parturition. The potential risk for humans is unknown. Caution should be exercised when prescribing to pregnant women

Breastfeeding

South African recommendations

• Contraindicated
• Solifenacin is excreted into breastmilk. Women taking solifenacin should not breastfeed their infants

Recommendations in other jurisdictions

• Caution; not recommended
• No data on the excretion of solifenacin in human milk are available. In mice, solifenacin and/or its metabolites was excreted in milk, and caused a dose dependent failure to thrive in neonatal mice. The use of solifenacin should therefore be avoided during breastfeeding

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• No data are available on the effect of solifenacin on fertility

Recommendations below are applicable to South Africa and other jurisdictions

• CrCl>30 ml/min: No dose adjustment recommended
• CrCl≤30 ml/min: Caution; no dose adjustment recommended
  Patients should be treated with caution and receive not more than 5mg once daily

Recommendations below are applicable to South Africa and other jurisdictions

• Mild: No dose adjustment recommended
• Moderate: Caution; no dose adjustment recommended
  Patients should be treated with caution and receive not more than 5 mg once daily
• Severe: Contraindicated

Recommendations below are applicable to South Africa and other jurisdictions

• No dose adjustment recommended

Central Nervous System Disorders

• Hallucinations
• Confusional state
• Delirium
• Somnolence
• Dysgeusia
• Dizziness
• Headache
• Fatigue

Cardiovascular Disorders

• Torsade de Pointes
• QT prolongation
• Atrial fibrillation
• Palpitations
• Tachycardia

Respiratory Disorders

• Nasal dryness
• Dysphonia

Gastrointestinal Disorders

• Dry mouth
• Constipation  
• Nausea and vomiting
• Dyspepsia
• Abdominal pain
• Gastroesophageal reflux disease
• Dry throat
• Colonic obstruction
• Faecal impaction
• Ileus
• Abdominal discomfort

Hepatobiliary Disorders

• Hepatic disorder
• Abnormal hepatic function test

Genitourinary Disorders

• Urinary tract infection
• Cystitis
• Difficulty in micturition
• Urinary retention
• Renal impairment

Endocrine and Metabolic Disorders

• Decreased appetite
• Hyperkalaemia

Musculoskeletal Disorders

• Muscular weakness

Skin and Subcutaneous Tissue Disorders

• Dry skin
• Pruritus
• Rash
• Erythema multiforme
• Urticaria
• Angioedema
• Exfoliative dermatitis
• Peripheral oedema

Immune, Blood and Lymphatic System Disorders

• Anaphylactic reaction

Sensory Disorders

• Blurred vision
• Dry eyes
• Glaucoma

• Metoclopramide
• Cisapride
• Anticholinergic agents
• CYP3A4 inhibitors
• CYP3A4 inducers
• QT-prolonging agents
• Potassium chloride
• Potassium citrate
• Ketoconazole
• Ritonavir
• Nelfinavir
• Itraconazole
• Verapamil
• Diltiazem
• Rifampicin
• Phenytoin
• Carbamazepine

None routine. Specific cases may require

• Hepatic function
• Renal function

Solifenacin is a competitive, specific cholinergic receptor antagonist. The urinary bladder is innervated by parasympathetic cholinergic nerves. Acetylcholine contracts the detrusor smooth muscle through muscarinic receptors of which the M3 subtype is predominantly involved. In vivo studies demonstrated that solifenacin binds to muscarinic M3 subtype receptors, with high affinity. In addition, solifenacin showed to be a specific antagonist for muscarinic receptors by displaying low or no affinity for various other receptors and ion channels tested.

Tablet 5mg

• Fenence 5mg (Austell Laboratories)
• Floloc 5 (Cipla Medpro)
• Solifenacin 5 Teva (Teva Pharmaceuticals)
• Solirest 5 (iPharma)
• Utroves 5 (Forrester Pharma)
• Vesicare (Astellas) originator
• Vesicont 5mg (Ranbaxy Pharmaceuticals)
• Vesifin 5mg (Pharma Dynamics)

Tablet 10mg

• Fenence 10mg (Austell Laboratories)
• Floloc 10 (Cipla Medpro)
• Solifenacin 10 Teva (Teva Pharmaceuticals)
• Solirest 10 (iPharma)
• Utroves 10 (Forrester Pharma)
• Vesicare (Astellas) originator
• Vesicont 10mg (Ranbaxy Pharmaceuticals)
• Vesifin 10mg (Pharma Dynamics)