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 ?
Darifenacin, oxybutynin, solifenacin, tolterodine, and trospium are indicated for the treatment of OAB with symptoms of urge urinary incontinence, urgency, and urinary frequency (3-13).
Darifenacin is effective in improving the major symptoms of overactive bladder: A pooled analysis of phase III studies.
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.
Darifenacin, a selective muscarinic M3 receptor antagonist being developed for treatment of overactive bladder, does not affect cognition in the elderly at clinically effective doses, Richard B.
A pooled analysis of three phase III studies to investigate the efficacy, tolerability and safety of darifenacin, a muscarinic M3 selective receptor antagonist, in the treatment of overactive bladder.
Three new medications aimed at OAB sufferers, darifenacin, solifenacin, and trospium, are awaiting FDA approval.
The same or a slightly smaller percentage of surveyed urologists selected darifenacin (Novartis/Bayer's Enablex/Emselex), ER trospium chloride (Allergan/Madaus/Speciality European Pharma/Rottapharm's Sanctura XR/Urivesc/Regurin XR, generics) or ER oxybutynin (McNeil/Janssen-Cilag's Ditropan XL/Lyrinel XL, generics) as the most efficacious drug for the indication.
Solifenacin and oxybutynin, for example, are metabolized through the CYP3A4 pathway, while tolterodine and darifenacin are metabolized through both CYP3A4 and CYP2D6 (Table 2).
He provided clinical leadership to a number of programs including darifenacin, Viagra and lasofoxifene, including the submission of two New Drug Applications (NDAs).
The available pharmacological treatment includes oxybutinin immediate release (IR), extended release (ER) or transdermal, tolterodine (IR or ER), solifenacin, darifenacin, trospium chloride and fesoterodine.
Oxybutynin, a non-selective muscarinic receptor antagonist, and darifenacin, selective for M[sub.
solifenacin, darifenacin, fesoterodine) and alternative routes of delivery of oxybutynin (e.