Tolterodine

Registered South African indications: 

• Overactive bladder syndrome

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Urinary retention
• Uncontrolled narrow angle glaucoma
• Myasthenia gravis
• Severe ulcerative colitis
• Toxic megacolon

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Significant bladder outlet obstruction at risk of urinary retention
• Gastrointestinal obstructive disorders
• Autonomic neuropathy
• Hiatus hernia
• Risk of decreased gastrointestinal motility
• Congenital or acquired QT prolongation
• Electrolyte disturbances 
• Bradycardia
• Pre-existing cardiac diseases 
• Diabetes mellitus
• Sodium-controlled diet 
• Galactose intolerance
• Lapp lactase deficiency 
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: cap

Overactive bladder syndrome 

• Oral (cap): Initial: 4mg, dly; Maintenance: 2-4mg, dly

Do not cut/crush/chew/dissolve

The need for continued treatment should be reconsidered at regular intervals

Not established for use in children

Pregnancy

• Caution
• There are no adequate data from the use of tolterodine in pregnant women. Studies in animals have shown reproductive toxicity. The potential risk for humans is unknown. Consequently, tolterodine is not recommended during pregnancy

Breastfeeding

• Caution; not recommended
• No data concerning the excretion of tolterodine into human milk are available. Tolterodine should be avoided during breastfeeding

Renal Impairment

• Mild to moderate: Caution; no dose adjustment recommended 
• Severe: Caution; dose adjustment recommended 

Hepatic Impairment

• Caution; dose adjustment recommended
  Mild to moderate (Child-Pugh Class A and B): 2mg dly
  Severe (Child-Pugh Class C): Avoid use, has not been studied

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Nervousness
• Confusion
• Hallucinations
• Disorientation
• Dizziness
• Somnolence
• Headache
• Paraesthesia
• Memory impairment
• Fatigue

Cardiovascular Disorders

• Palpitations
• Cardiac failure
• Arrhythmia
• Tachycardia
• Flushing
• Chest pain

Gastrointestinal Disorders

• Dry mouth
• Dyspepsia
• Constipation
• Abdominal pain
• Flatulence
• Diarrhoea
• Gastroesophageal reflux
• Vomiting

Genitourinary Disorders

• Dysuria
• Urinary retention

Skin and Subcutaneous Tissue Disorders

• Angioedema
• Dry skin
• Peripheral oedema

Immune, Blood and Lymphatic System Disorders

• Sinusitis
• Hypersensitivity
• Anaphylactoid reactions

Sensory Disorders

• Dry eyes
• Abnormal vision
• Vertigo

• Potent CYP3A4 inhibitors 
• Antimuscarinics
• Muscarinic cholinergic receptor agonists
• Metoclopramide
• Cisapride 
• QT prolonging agents

• Renal function
• Hepatic function

Tolterodine is a competitive, specific muscarinic receptor antagonist, which shows selectivity for the urinary bladder over salivary glands. It results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

Capsule 2mg

• Detrusitol SR (UpJohn) originator

Capsule 4mg

• Detrusitol SR (UpJohn) originator