Darifenacin

Registered South African indications:

• Overactive bladder

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe hepatic impairment
• Urinary retention
• Gastric retention
• Uncontrolled narrow angle glaucoma
• Myasthenia gravis
• Severe ulcerative colitis
• Toxic megacolon
• Coadministration with potent CYP3A4 inhibitors

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Mild to moderate hepatic impairment
• Elderly
• Autonomic neuropathy
• Hiatus hernia
• Clinically significant bladder outflow obstruction
• Risk of urinary retention
• Severe constipation
• Gastrointestinal obstructive disorders
• Treated narrow angle glaucoma
• Other causes of frequent urination
• Risk of decreased gastrointestinal motility
• Gastro-oesophageal reflux
• Neurogenic cause of detrusor overactivity
• Cardiac disease

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

Overactive bladder

• Oral (tab): Initial: 7.5mg, dly; Increase to 15mg, dly after 2 weeks if inadequate response

Do not cut/ crush/ chew/ dissolve

Not established for use in children below 18 years

Pregnancy

• Caution
• There are limited amount of data from the use of darifenacin in pregnant women. Studies in animals have shown toxicity to parturition. Darifenacin is not recommended during pregnancy

Breastfeeding

• Caution; not recommended
• Darifenacin is excreted in the milk of rats. It is not known whether darifenacin is excreted in human milk. A risk to the nursing child cannot be excluded. A decision whether to avoid breastfeeding or to abstain from darifenacin therapy during breastfeeding should be based on a benefit and risk comparison

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Mild (Child-Pugh class A): Caution; no dose adjustment recommended
• Moderate (Child-Pugh class B): Caution; dose adjustment recommended
  Max: 7.5mg/24hrs
• Severe(Child-Pugh class C): Contraindicated

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Abnormal thinking
• Headache
• Dizziness
• Somnolence
• Asthenia

Cardiovascular Disorders

• Hypertension
• Peripheral oedema

Respiratory Disorders

• Nasal dryness
• Dyspnoea
• Cough
• Rhinitis

Gastrointestinal Disorders

• Dysgeusia
• Constipation
• Dry mouth
• Abdominal pain
• Nausea
• Dyspepsia
• Flatulence
• Diarrhoea
• Mouth ulceration

Hepatobiliary Disorders

• Increased aspartate aminotransferase
• Increased alanine aminotransferase

Genitourinary Disorders

• Urinary tract infection
• Urinary retention
• Urinary tract disorder
• Bladder pain
• Erectile dysfunction
• Vaginitis

Skin and Subcutaneous Tissue Disorders

• Rash
• Dry skin
• Pruritus
• Hyperhidrosis
• Angioedema
• Facial oedema

Sensory Disorders

• Dry eye
• Visual disturbances
• Blurred vision

• CYP2D6 inhibitors
• CYP2D6 substrates
• CYP3A4 inhibitors
• CYP3A4 inducers
• CYP3A4 substrates
• Digoxin
• Agents with antimuscarinic properties

Hepatic function

Darifenacin is a selective muscarinic M3 receptor antagonist. The M3 receptor is the major subtype that controls urinary bladder muscle contraction. M3 receptors are also involved in the contraction of gastrointestinal smooth muscle, saliva production, and iris sphincter function.

Tablet SRT 7.5mg

• Enablex (Pharmacare) originator

Tablet SRT 15mg

• Enablex (Pharmacare) originator