darifenacin


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Related to darifenacin: Tolterodine, darifenacin hydrobromide

darifenacin

(dar-i-fen-a-sin) ,

Enablex

(trade name)

Classification

Therapeutic: urinary tract antispasmodics
Pharmacologic: anticholinergics
Pregnancy Category: C

Indications

Overactive bladder with symptoms (urge incontinence, urgency, frequency).

Action

Acts as a muscarinic (cholinergic) receptor antagonist; antagonizes bladder smooth muscle contraction.

Therapeutic effects

Decreased symptoms of overactive bladder.

Pharmacokinetics

Absorption: 15–19% absorbed.
Distribution: Unknown.
Protein Binding: 98%.
Metabolism and Excretion: Extensively metabolized by the CYP2D6 enzyme system in most individuals; genetic implication poor metabolizers (7% of Caucasians, 2% of African Americans) have less CYP2D6 activity with less metabolism occurring. Some metabolism via CYP3A4 enzyme system. 60% excreted renally as metabolites, 40% in feces as metabolites.
Half-life: 13–19 hr.

Time/action profile

ROUTEONSETPEAKDURATION
POunknown7 hr24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Urinary retention;Gastric retention;Uncontrolled angle-closure glaucoma;Severe hepatic impairment.
Use Cautiously in: Concurrent use of CYP3A4 inhibitors (use lower dose/clinical monitoring may be necessary);Moderate hepatic impairment (lower dose recommended);Bladder outflow obstruction;GI obstructive disorders, ↓ GI motility, severe constipation or ulcerative colitis;Myasthenia gravis;Angle-closure glaucoma; Lactation / Pediatric: Safety not established; Obstetric: Use only if maternal benefit outweighs fetal risk.

Adverse Reactions/Side Effects

Central nervous system

  • confusion
  • dizziness
  • drowsiness
  • hallucinations
  • headache

Ear, Eye, Nose, Throat

  • blurred vision

Gastrointestinal

  • constipation (most frequent)
  • dry mouth (most frequent)
  • dyspepsia
  • nausea

Metabolic

  • heat intolerance

Miscellaneous

  • angioedema (life-threatening)

Interactions

Drug-Drug interaction

Blood levels and risk of toxicity are ↑ by concurrent use of strong CYP3A4 inhibitors including ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, and nefazodone ; daily dose should not exceed 7.5 mg.Concurrent use of moderate inhibitors of CYP3A4, especially those with narrow therapeutic indices, including flecainide, thioridazine, and tricyclic antidepressants, should be undertaken with caution.

Route/Dosage

Oral (Adults) 7.5 mg once daily, may be ↑ after 2 wk to 15 mg once daily.

Availability

Extended-release tablets: 7.5 mg, 15 mg Cost: All strengths $599.48 / 90

Nursing implications

Nursing assessment

  • Monitor voiding pattern and assess symptoms of overactive bladder (urinary urgency, urinary incontinence, urinary frequency) to and periodically during therapy.

Potential Nursing Diagnoses

Impaired urinary elimination (Indications)

Implementation

  • Oral: Administer once daily without regard to food. Extended-release tablets must be swallowed whole; do not break, crush, or chew.

Patient/Family Teaching

  • Instruct patient to take darifenacin as directed. Advise patient to read the Patient Information before starting therapy and with each prescription refill. If a dose is missed, skip dose and take next day; do not take 2 doses in same day.
  • Do not share darifenacin with others; may be dangerous.
  • Inform patient of potential anticholinergic side effects (constipation, urinary retention, blurred vision, heat prostration in a hot environment).
  • May cause dizziness, drowsiness, confusion, and blurred vision. Caution patient to avoid driving and other activities that require alertness until response to medication is known.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Decrease in symptoms of overactive bladder (urge urinary incontinence, urgency, frequency).

darifenacin

Therapeutics An agent in clinical trials for treating irritable bowel syndrome and overactive bladder
References in periodicals archive ?
was comparable for darifenacin, fesoterodine, transdermal oxybutynin,
Gegen and darifenacin together attained synergism for detrusor overactivity treatment via the neurogenic pathway.
According to Merus Labs, Darifenacin is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
Darifenacin is to be used for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
There are seven anticholinergics that are used as antispasmodics for the treatment of overactive bladder: darifenacin (Enablex) [C], fesoterodine (Toviaz) [C], flavoxate (Urispas) [B], oxybutynin (Ditropan) [B], solifenacin (Vesicare) [C], tolterodine (Detrol) [C], and trospium (Sanctura) [C].
Five pharmacologic therapies have been approved for the treatment of OAB: oxybutynin, approved in immediate-release, extended-release, (11) and transdermal patch (12) formulations; immediate- and extended-release tolterodine (11); trospium chloride (13); solifenacin (14); and darifenacin.
Pharmacotherapy (anticholinergic medication) includes any form of oxybutynin, tolterodine, trospium chloride, solfenacin, or darifenacin.
The parties have therefore agreed to sell off Darifenacin.
For urge UI, anticholinergic medications, such as tolterodine (Detrol), darifenacin (Enablex), and solifenacin (Vesicare) are used.
revealed 12-month adherence rates of 26% for oxybutynin extended-release (ER), 28% for tolterodine ER, 26% for trospium, 35% for solifenacin, and 17% for darifenacin.
Anticholinergic agents which are prescribed for OAB symptoms include oxybutynin (Ditropan[R], Gelnique[R], Oxytrol[R]), tolterodine (Detrol[R], Detrol LA[R]), solifenacin (VESIcare[R]), darifenacin (Enablex[R]), and fesoterodine (Toviaz[R]).