darifenacin

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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).
Drug Guide, © 2015 Farlex and Partners

darifenacin

Therapeutics An agent in clinical trials for treating irritable bowel syndrome and overactive bladder
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.
References in periodicals archive ?
* Anticholinergic drugs, such as oxybutynin (Ditropan, Oxytrol), tolterodine (Detrol), darifenacin (Enablex), trospium (Sanctura) or solifenacin (Vesicare)
Repovic adds that some medications commonly prescribed for bladder dysfunction (Ditropan, Detrol, Vesicare and Enablex) can contribute to memory loss, somnolence and confusion, although these effects typically occur more suddenly than when they are MS-related.
Medications for Overactive Bladder (OAB) DRUG BRAND(S) RECOMMENDED ORAL DOSE Darifenacin Enablex 7.5 mg once daily.
in terms of dollars--by Novartis' sale of the rights to Enablex
One-off items in the quarter included charges totalling USD789m, partially offset by a gain of USD392m from the divestment of Enablex.
P&G's key pharmaceutical brands include Actonel--a $1 billion brand--along with Intrinsa, Enablex and Asacol.
Darifenacin (Enablex) was approved for the treatment of overactive bladder by the Food and Drug Administration at the end of last year.
Darifenacin (Enablex) thus stands in marked contrast to traditional antimuscarinic agents, which are effective for overactive bladder but have a high rate of limiting cognitive side effects due to their broad spectrum of action.
"For urge UI, medications that reduce contractions in the bladder, such as tolterodine (Detrol), darifenacin (Enablex), and solifenacin (Vesicare), are used.
Mis au point en 2003 et commercialise aux Etats-Unis et en Europe, puis en Grande Bretagne, le darifenacine (ENABLEX 7,5 mg et 15 mg, EMSELEX 7,5 mg et 15 mg, Novartis) a obtenu l'homologation de la FDA pour le traitement de l'HAV en decembre 2004.
M2 EQUITYBITES-October 19, 2010-Warner Chilcott plc acquires US rights to Enablex for USD400m(C)2010 M2 COMMUNICATIONS http://www.m2.com
The impairment charges are expected to be partially offset through the proceeds received from the sale of the US rights for Enablex (darifenacin) to Warner Chilcott (NASDAQ) for USD400m, as announced on 24 September 2010.