darifenacin hydrobromide

(redirected from Emselex)

darifenacin hydrobromide

Action

Competitively antagonizes muscarinic receptors, reducing contractions of urinary bladder smooth muscle

Availability

Tablets (extended-release): 7.5 mg, 15 mg

Indications and dosages

Overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency

Adults: Initially, 7.5 mg P.O. daily; may increase to 15 mg P.O. daily as early as 2 weeks after therapy begins

Dosage adjustment

• Moderate hepatic impairment
• Concurrent use of potent CYP3A4 inhibitors (such as clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, and ritonavir)

Contraindications

• Hypersensitivity to drug or its components
• Urinary retention, gastric retention, uncontrolled angle-closure glaucoma, or increased risk for these conditions

Precautions

Use cautiously in:
• decreased GI motility (such as severe constipation, ulcerative colitis, or myasthenia gravis), controlled angleclosure glaucoma, hepatic impairment
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Administer tablets whole with liquid (with or without food) once daily.
• Make sure patient doesn't chew, crush, or divide them.
• Know that drug isn't recommended for patients with severe hepatic impairment.

Adverse reactions

CNS: dizziness, asthenia

CV: hypertension

EENT: dry eyes, abnormal vision, dry throat, bronchitis, pharyngitis, rhinitis, sinusitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, dry mouth

GU: urinary tract infection or disorder, vaginitis

Musculoskeletal: back pain, arthralgia

Skin: dry skin, rash, pruritus

Other: abnormal taste, weight gain, accidental injury, flulike syndrome, pain, peripheral edema, heat prostration

Interactions

Drug-drug.Anticholinergics: increased frequency or severity of adverse reactions

CYP4502D6 inhibitors: increased darifenacin exposure and blood level

Drugs metabolized by CYP2D6 (such as flecainide, thioridazine, and tricyclic antidepressants): increased blood levels of these drugs

Patient monitoring

• Monitor liver function tests frequently; withdraw drug if liver function tests show severe hepatic impairment.
• Monitor urinary function periodically.

Patient teaching

• Instruct patient to take tablets whole with liquid, with or without food. Tell him not to chew, divide, or crush them.
• Inform patient that some over-the-counter products such as antihistamines may increase risk of side effects.
• Caution patient that drug may cause heat prostration; describe signs and symptoms.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs mentioned above.

References in periodicals archive ?
Emselex demand declined at 5% year-over-year due to intense competition in the overactive bladder market.
Merus has been notified that Emselex will be included in this new class, and was informed today that the proposed maximum reimbursement price will be set at approximately 40% of our current weighed average net selling prices.
Selling expenses decreased in fiscal 2015 when compared to fiscal 2014, driven by right-sizing our contract sales force in Canada and one-time strategic investment made in fiscal 2014 to reclassify Emselex within the prescribing guidelines in the UK for products treating overactive bladder, which drove incremental physician prescribing.
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.
5 and 15 mg once daily won marketing approval for treating overactive bladder in Europe, where it goes by the trade name Emselex.
The approval of Emselex will provide many people in Europe who experience OAB symptoms a safe and effective new treatment option," said Jorg Reinhardt, Global Head of Development, Novartis Pharma AG.
Emselex is a once-daily M3 selective receptive antagonist (M3 SRA) oral treatment that works by selectively inhibiting the detrusor muscle that controls bladder contraction while sparing the M1 and M2 receptors believed to be involved in central nervous system (CNS) and cardiovascular (CV) function, respectively.
To date, 97 clinical trials with Emselex have been carried out involving more than 10,500 subjects and patients, of whom 7,146 were treated with darifenacin.
Our in-market prescription trends are tracking as expected for Emselex and Sintrom.
Upon receipt of the EC approval, Novartis will be able to market Emselex throughout these countries.
Due to its M3 selectivity, Emselex provides effective overactive bladder symptom relief while decreasing the potential risk of safety issues such as cognitive impairment or effects on cardiac function.
The safety and efficacy of Emselex has been extensively studied in over 90 pre-clinical studies and clinical trials, involving more than 5,000 patients.