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 ?
Tolterodine use increased 13.7% from Q1-2000 (2.1 users/1,000 beneficiaries) to Q3-2011(15.3 users/1,000 beneficiaries) before the introduction of solifenacin (2011), darifenacin (2011), and mirabegron (2015) led to a steady reduction in tolterodine use.
Method: After daily oral administration of Gegen 30 (Gegen, 30mg/kg); Gegen 300 (Gegen, 300mg/kg); Low_Dar (darifenacin, 3mg/kg); High_Dar (darifenacin, 30mg/kg) Low_Dar+Gegen 30 or High_Dar+Gegen 30 for 3 weeks, bladder detrusor strips of the rats were isolated and assessed with different stimulators for the measurement of tonic and phasic contractile activities (including phasic amplitude and frequency).
* Anticholinergic drugs, such as oxybutynin (Ditropan, Oxytrol), tolterodine (Detrol), darifenacin (Enablex), trospium (Sanctura) or solifenacin (Vesicare)
Available agents include darifenacin, fesoterodine, oxybutynin, solifenacin, tolterodine, and trospium.
Antimuscarinics include darifenacin, fesoterodine, oxybutynin, solifenacin, tolterodine, and trospium, which all have similar efficacy, In general, patients with more severe symptoms have a greater degree of response to medications, regardless of which medication is chosen.
Urinary tract drugs: Darifenacin, Fesoterodine, Solifenacin, Silodosin, Tamsulosin
Pharmaceutical company Merus Labs International Inc (TSX:MSL.TO)(NasdaqCM:MSLI) said on Wednesday that it has acquired the Canadian and European rights (excluding France, Spain and Italy) to manufacture, market and sell the branded prescription medicine product Emselex/Enablex (darifenacin) extended release tablets.
It was reported today that Merus Labs International Inc (TSX:MSL)(NASDAQ:MSLI), a specialty pharmaceutical company engaged in the acquisition and licensing of pharmaceutical products, has acquired the Canadian and European rights to produce, market, and sell the branded prescription medicine product, Emselex(r)/Enablex(r) (darifenacin) extended release tablets, from Novartis Pharma AG.
Among the leading Rx brands that Warner Chilcott receives are Asacol HD (mesalamine) delayed-release tablets for ulcerative colitis, Actonel (risedronate sodium) for osteoporosis and copromotion rights to Enablex (darifenacin) for treatment of overactive bladder.
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. (15) Each of these agents is a muscarinic receptor antagonist, and all have demonstrated substantial efficacy in reducing urinary urgency, frequency, and urinary incontinence.
Pharmacotherapy (anticholinergic medication) includes any form of oxybutynin, tolterodine, trospium chloride, solfenacin, or darifenacin. The pharmacotherapy requirement can be waived if drug therapy is contraindicated or if the patient is intolerant.