Emselex

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ANNEX I 
 

SUMMARY OF PRODUCT CHARACTERISTICS 



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1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 7.5 mg prolonged-release tablets 
 
 
2. QUALITATIVE AND QUANTITATIVE COMPOSITION 
 
Each tablet contains 7.5 mg of darifenacin (as hydrobromide) 
 
For the full list of excipients, see section 6.1. 
 
3. PHARMACEUTICAL FORM 
 
Prolonged-release tablet 
 
White round, convex tablet, debossed with “DF” on one side and “7.5” on the reverse. 
 
4. CLINICAL PARTICULARS 
 
4.1 Therapeutic indications 
 
Symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may 
occur in adult patients with overactive bladder syndrome. 
 
4.2 Posology and method of administration 
 
Posology 
 
Adults 
The recommended starting dose is 7.5 mg daily. After 2 weeks of starting therapy, patients should be 
reassessed. For those patients requiring greater symptom relief, the dose may be increased to 15 mg 
daily, based on individual response. 
 
Elderly patients (≥ 65 years) 
The recommended starting dose for the elderly is 7.5 mg daily. After 2 weeks of starting therapy, 
patients should be reassessed for efficacy and safety. For those patients who have an acceptable 
tolerability profile but require greater symptom relief, the dose may be increased to 15 mg daily, based 
on individual response (see section 5.2). 
 
Paediatric population 
Emselex is not recommended for use in children below 18 years of age due to a lack of data on safety 
and efficacy. 
 
Renal impairment 
No dose adjustment is required in patients with impaired renal function. However, caution should be 
exercised when treating this population (see section 5.2). 
 
Hepatic impairment 
No dose adjustment is required in patients with mild hepatic impairment (Child Pugh A). However, 
there is a risk of increased exposure in this population (see section 5.2). 
 
Patients with moderate hepatic impairment (Child Pugh B) should only be treated if the benefit 
outweighs the risk, and the dose should be restricted to 7.5 mg daily (see section 5.2). Emselex is 
contraindicated in patients with severe hepatic impairment (Child Pugh C) (see section 4.3). 
 
Patients receiving concomitant treatment with substances that are potent inhibitors of CYP2D6 or 
moderate inhibitors of CYP3A4 



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In patients receiving substances that are potent CYP2D6 inhibitors, such as paroxetine, terbinafine, 
quinidine and cimetidine, treatment should start with the 7.5 mg dose. The dose may be titrated to 
15 mg daily to obtain an improved clinical response provided the dose is well tolerated. However, 
caution should be exercised. 
 
In patients receiving substances that are moderate CYP3A4 inhibitors, such as fluconazole, grapefruit 
juice and erythromycin, the recommended starting dose is 7.5 mg daily. The dose may be titrated to 
15 mg daily to obtain an improved clinical response provided the dose is well tolerated. However, 
caution should be exercised. 
 
Method of administration 
Emselex is for oral use. The tablets should be taken once daily with liquid. They can be taken with or 
without food, and must be swallowed whole and not chewed, divided or crushed. 
 
4.3 Contraindications 
 
Emselex is contraindicated in patients with: 
- Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. 
- Urinary retention. 
- Gastric retention. 
- Uncontrolled narrow-angle glaucoma. 
- Myasthenia gravis. 
- Severe hepatic impairment (Child Pugh C). 
- Severe ulcerative colitis. 
- Toxic megacolon. 
- Concomitant treatment with potent CYP3A4 inhibitors (see section 4.5). 
 
4.4 Special warnings and precautions for use 
 
Emselex should be administered with caution to patients with autonomic neuropathy, hiatus hernia, 
clinically significant bladder outflow obstruction, risk for urinary retention, severe constipation or 
gastrointestinal obstructive disorders, such as pyloric stenosis. 
 
Emselex should be used with caution in patients being treated for narrow-angle glaucoma (see 
section 4.3). 
 
Other causes of frequent urination (heart failure or renal disease) should be assessed before treatment 
with Emselex. If urinary tract infection is present, an appropriate antibacterial therapy should be 
started. 
 
Emselex should be used with caution in patients with risk of decreased gastrointestinal motility, 
gastro-oesophageal reflux and/or who are concurrently taking medicinal products (such as oral 
bisphosphonates) that can cause or exacerbate oesophagitis. 
 
Safety and efficacy have not yet been established in patients with a neurogenic cause for detrusor over 
activity. 
 
Caution should be used when prescribing antimuscarinics to patients with pre-existing cardiac 
diseases. 
 
As with other antimuscarinics, patients should be instructed to discontinue Emselex and seek 
immediate medical attention if they experience oedema of the tongue or laropharynx, or difficulty 
breathing (see section 4.8). 
 



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4.5 Interaction with other medicinal products and other forms of interaction 
 
Effects of other medicinal products on darifenacin 
Darifenacin metabolism is primarily mediated by the cytochrome P450 enzymes CYP2D6 and 
CYP3A4. Therefore, inhibitors of these enzymes may increase darifenacin exposure. 
 
CYP2D6 inhibitors 
In patients receiving substances that are potent CYP2D6 inhibitors (e.g. paroxetine, terbinafine, 
cimetidine and quinidine) the recommended starting dose should be 7.5 mg daily. The dose may be 
titrated to 15 mg daily to obtain an improved clinical response provided the dose is well tolerated. 
Concomitant treatment with potent CYP2D6 inhibitors results in an increase in exposure (e.g. of 33% 
with 20 mg paroxetine at the 30 mg dose of darifenacin). 
 
CYP3A4 inhibitors 
Darifenacin should not be used together with potent CYP3A4 inhibitors (see section 4.3) such as 
protease inhibitors (e.g. ritonavir), ketoconazole and itraconazole. Potent P-glycoprotein inhibitors 
such as ciclosporin and verapamil should also be avoided. Co-administration of darifenacin 7.5 mg 
with the potent CYP3A4 inhibitor ketoconazole 400 mg resulted in a 5-fold increase in steady-state 
darifenacin AUC. In subjects who are poor metabolisers, darifenacin exposure increased 
approximately 10-fold. Due to a greater contribution of CYP3A4 after higher darifenacin doses, the 
magnitude of the effect is expected to be even more pronounced when combining ketoconazole with 
darifenacin 15 mg. 
 
When co-administered with moderate CYP3A4 inhibitors such as erythromycin, clarithromycin, 
telithromycin, fluconazole and grapefruit juice, the recommended starting dose of darifenacin should 
be 7.5 mg daily. The dose may be titrated to 15 mg daily to obtain an improved clinical response 
provided the dose is well tolerated. Darifenacin AUC24 and Cmax from 30 mg once daily dosing in 
subjects who are extensive metabolisers were 95% and 128% higher when erythromycin (moderate 
CYP3A4 inhibitor) was co-administered with darifenacin than when darifenacin was taken alone. 
 
Enzyme inducers 
Substances that are inducers of CYP3A4, such as rifampicin, carbamazepine, barbiturates and St 
John’s wort (Hypericum perforatum) are likely to decrease the plasma concentrations of darifenacin. 
 
Effects of darifenacin on other medicinal products 
CYP2D6 substrates 
Darifenacin is a moderate inhibitor of the enzyme CYP2D6. Caution should be exercised when 
darifenacin is used concomitantly with medicinal products that are predominantly metabolised by 
CYP2D6 and which have a narrow therapeutic window, such as flecainide, thioridazine, or tricyclic 
antidepressants such as imipramine. The effects of darifenacin on the metabolism of CYP2D6 
substrates are mainly clinically relevant for CYP2D6 substrates which are individually dose titrated. 
 
CYP3A4 substrates 
Darifenacin treatment resulted in a modest increase in the exposure of the CYP3A4 substrate 
midazolam. However the data available do not indicate that darifenacin changes either midazolam 
clearance or bioavailability. It can therefore be concluded that darifenacin administration does not alter 
the pharmacokinetics of CYP3A4 substrates in vivo. The interaction with midazolam lacks clinical 
relevance, and therefore no dose adjustment is needed for CYP3A4 substrates. 
 
Warfarin 
Standard therapeutic prothrombin time monitoring for warfarin should be continued. The effect of 
warfarin on prothrombin time was not altered when co-administered with darifenacin. 
 
Digoxin 
Therapeutic drug monitoring for digoxin should be performed when initiating and ending darifenacin 
treatment as well as changing the darifenacin dose. Darifenacin 30 mg once daily (two times greater 
than the recommended daily dose) co-administered with digoxin at steady state resulted in a small 



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increase in digoxin exposure (AUC: 16% and Cmax: 20%). The increase in digoxin exposure could be 
caused by competition between darifenacin and digoxin for P-glycoprotein. Other transporter-related 
interactions cannot be excluded. 
 
Antimuscarinic agents 
As with any other antimuscarinic agents, concomitant use of medicinal products that possess 
antimuscarinic properties, such as oxybutynin, tolterodine and flavoxate, may result in more 
pronounced therapeutic and side effects. The potentiation of anticholinergic effects with anti-
parkinson agents and tricyclic antidepressants may also occur if antimuscarinic agents are used 
concurrently with such medicinal products. However, no studies involving the interaction with anti-
parkinson agents and tricyclic antidepressants have been performed. 
 
4.6 Fertility, pregnancy and lactation 
 
Pregnancy 
There are limited amount of data from the use of darifenacin in pregnant women. Studies in animals 
have shown toxicity to parturition (for details, see section 5.3). Emselex is not recommended during 
pregnancy. 
 
Breast-feeding 
Darifenacin is excreted in the milk of rats. It is not known whether darifenacin is excreted in human 
milk. A risk to the nursing child cannot be excluded. A decision whether to avoid breast-feeding or to 
abstain from Emselex therapy during lactation should be based on a benefit and risk comparison. 
 
Fertility 
There are no human fertility data for darifenacin. Darifenacin had no effect on male or female fertility 
in rats or any effect in the reproductive organs of either sex in rats and dogs (for details, see section 
5.3). Women of child bearing potential should be made aware of the lack of fertility data, and Emselex 
should only be given after consideration of individual risks and benefits. 
 
 
4.7 Effects on ability to drive and use machines 
 
As with other antimuscarinic agents, Emselex may produce effects such as dizziness, blurred vision, 
insomnia and somnolence. Patients experiencing these side effects should not drive or use machines. 
For Emselex, these side effects have been reported to be uncommon. 
 
4.8 Undesirable effects 
 
Summary of the safety profile  
Consistent with the pharmacological profile, the most commonly reported adverse reactions were dry 
mouth (20.2% and 35% for the 7.5 mg and 15 mg dose, respectively, 18.7% after flexible dose 
titration, and 8% - 9% for placebo) and constipation (14.8% and 21% for the 7.5 mg and 15 mg dose, 
respectively, 20.9% after flexible dose titration, and 5.4% - 7.9% for placebo). Anticholinergic effects, 
in general, are dose-dependent. 
 
However, the patient discontinuation rates due to these adverse reactions were low (dry mouth: 0% - 
0.9% and constipation: 0.6% - 2.2% for darifenacin, depending on the dose; and 0% and 0.3% for 
placebo, for dry mouth and constipation, respectively). 
 
Tabulated list of adverse reactions 
The adverse reactions are ranked under heading of frequency using the following convention: very 
common (≥1/10), common (≥1/100 to <1/10), uncommon (1/1,000 to <1/100), rare (1/10,000 to 
<1/1,000), very rare (<1/10,000) and not known (cannot be estimated from the available data). Within 
each frequency grouping, adverse reactions are presented in order of decreasing seriousness. 
 
Table 1: Adverse reactions with Emselex 7.5 mg and 15 mg prolonged-release tablets 



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Infections and infestations 
Uncommon Urinary tract infection 
Psychiatric disorders 
Uncommon Insomnia, thinking abnormal 
Nervous system disorders 
Common Headache 
Uncommon Dizziness, dysgeusia, somnolence 
Eye disorders 
Common Dry eye 
Uncommon Visual disturbance, including vision blurred 
Vascular disorders 
Uncommon Hypertension 
Respiratory, thoracic and mediastinal disorders 
Common Nasal dryness 
Uncommon Dyspnoea, cough, rhinitis 
Gastrointestinal disorders 
Very common Constipation, dry mouth 
Common Abdominal pain, nausea, dyspepsia 
Uncommon Flatulence, diarrhoea, mouth ulceration 
Skin and subcutaneous tissue disorders 
Uncommon Rash, dry skin, pruritus, hyperhidrosis 
Not known Angioedema 
Renal and urinary disorders 
Uncommon Urinary retention, urinary tract disorder, bladder pain 
Reproductive system and breast disorders 
Uncommon Erectile dysfunction, vaginitis 
General disorders and administration site conditions 
Uncommon Oedema peripheral, asthenia, face oedema, oedema 
Investigations 
Uncommon Aspartate aminotransferase increased, alanine 

aminotransferase increased 
Injury, poisoning, and procedural complications 
Uncommon Injury 

 
Description of selected adverse reactions  
In the pivotal clinical trials with doses of Emselex 7.5 mg and 15 mg, adverse reactions were reported 
as presented in the table above. Most of the adverse reactions were of mild or moderate intensity and 
did not result in discontinuation in the majority of the patients. 
 
Treatment with Emselex may possibly mask symptoms associated with gallbladder disease. However, 
there was no association between the occurrence of adverse events related to the biliary system in 
darifenacin-treated patients and increasing age. 
 
The incidence of adverse reactions with the doses of Emselex 7.5 mg and 15 mg decreased during the 
treatment period up to 6 months. A similar trend is also seen for the discontinuation rates. 
 
Post-marketing experience 
The following events have been reported in association with darifenacin use in worldwide post-
marketing experience: generalised hypersensitivity reactions including angioedema, depressed 
mood/mood alterations, hallucination. Because these spontaneously reported events are from the 
worldwide post-marketing experience, the frequency of events cannot be estimated from the available 
data. 
 
Reporting of suspected adverse reactions 



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Reporting suspected adverse reactions after authorisation of the medicinal product is important. It 
allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare 
professionals are asked to report any suspected adverse reactions via the national reporting system 
listed in Appendix V. 
 
 
4.9 Overdose 
 
Emselex has been administered in clinical trials at doses up to 75 mg (five times maximum therapeutic 
dose). The most common adverse reactions seen were dry mouth, constipation, headache, dyspepsia 
and nasal dryness. However, overdose with darifenacin can potentially lead to severe anticholinergic 
effects and should be treated accordingly. Therapy should be aimed at reversing the anticholinergic 
symptoms under careful medical supervision. The use of agents such as physostigmine can assist in 
reversing such symptoms. 
 
5. PHARMACOLOGICAL PROPERTIES 
 
5.1 Pharmacodynamic properties 
 
Pharmacotherapeutic group: Urologicals, drugs for urinary frequency and incontinence; ATC code: 
G04BD10. 
 
Mechanism of action  
Darifenacin is a selective muscarinic M3 receptor antagonist (M3 SRA) in vitro. The M3 receptor is 
the major subtype that controls urinary bladder muscle contraction. It is not known whether this 
selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of 
overactive bladder syndrome. 
 
Clinical efficacy and safety  
Cystometric studies performed with darifenacin in patients with involuntary bladder contractions 
showed increased bladder capacity, increased volume threshold for unstable contractions and 
diminished frequency of unstable detrusor contractions. 
 
Treatment with Emselex administered at dosages of 7.5 mg and 15 mg daily has been investigated in 
four double-blind, Phase III, randomised, controlled clinical studies in male and female patients with 
symptoms of overactive bladder. As seen in Table 2 below, a pooled analysis of 3 of the studies for the 
treatment with both Emselex 7.5 mg and 15 mg provided a statistically significant improvement in the 
primary endpoint, reduction in incontinence episodes, versus placebo. 
 
Table 2: Pooled analysis of data from three Phase III clinical studies assessing fixed doses of 7.5 mg 
and 15 mg Emselex 
 

Dose N Incontinence episodes per week 95% CI P value2 
Baseline 
(median) 

Week 12 
(median) 

Change from 
baseline 
(median) 

Differences 
from placebo1 

(median) 

Emselex 
7.5 mg 
once daily 

335 16.0 4.9 -8.8 (-68%) -2.0 (-3.6, -0.7) 0.004 

Placebo 271 16.6 7.9 -7.0 (-54%) -- -- -- 
        
Emselex 
15 mg 
once daily 

330 16.9 4.1 -10.6 (-77%) -3.2 (-4.5, -2.0) <0.001 

Placebo 384 16.6 6.4 -7.5 (-58%) -- -- -- 
1 Hodges Lehmann estimate: median difference from placebo in change from baseline 



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2 Stratified Wilcoxon test for difference from placebo. 
 
Emselex 7.5 mg and 15 mg doses significantly reduced both the severity and number of urinary 
urgency episodes and the number of micturitions, while significantly increasing the mean volume 
voided from baseline. 
 
Emselex 7.5 mg and 15 mg were associated with statistically significant improvements over placebo in 
some aspects of quality of life as measured by the Kings Health Questionnaire including incontinence 
impact, role limitations, social limitations and severity measures. 
 
For both doses of 7.5 mg and 15 mg, the percentage median reduction from baseline in the number of 
incontinence episodes per week was similar between males and females. The observed differences 
from placebo for males in terms of percentage and absolute reductions in incontinence episodes was 
lower than for females. 
 
The effect of treatment with 15 mg and 75 mg of darifenacin on QT/QTc interval was evaluated in a 
study in 179 healthy adults (44% male: 56% females) aged 18 to 65 for 6 days (to steady state). 
Therapeutic and supra-therapeutic doses of darifenacin resulted in no increase in QT/QTc interval 
prolongation from baseline compared to placebo at maximum darifenacin exposure. 
 
5.2 Pharmacokinetic properties 
 
Darifenacin is metabolised by CYP3A4 and CYP2D6. Due to genetic differences, about 7% of the 
Caucasians lack the CYP2D6 enzyme and are said to be poor metabolisers. A few percent of the 
population have increased CYP2D6 enzyme levels (ultrafast metabolisers). The information below 
applies to subjects who have normal CYP2D6 activity (extensive metabolisers) unless otherwise 
stated. 
 
Absorption 
Due to extensive first-pass metabolism darifenacin has a bioavailability of approximately 15% and 
19% after 7.5 mg and 15 mg daily doses at steady state. Maximum plasma levels are reached 
approximately 7 hours after administration of the prolonged-release tablets and steady-state plasma 
levels are achieved by the sixth day of administration. At steady state, peak-to-trough fluctuations in 
darifenacin concentrations are small (PTF: 0.87 for 7.5 mg and 0.76 for 15 mg), thereby maintaining 
therapeutic plasma levels over the dosing interval. Food had no effect on darifenacin pharmacokinetics 
during multiple-dose administration of prolonged-release tablets. 
 
Distribution 
Darifenacin is a lipophilic base and is 98% bound to plasma proteins (primarily to alpha-1-acid-
glycoprotein). The steady-state volume of distribution (Vss) is estimated to be 163 litres. 
 
Metabolism 
Darifenacin is extensively metabolised by the liver following oral administration. 
 
Darifenacin undergoes significant metabolism by cytochrome CYP3A4 and CYP2D6 in the liver and 
by CYP3A4 in the gut wall. The three main metabolic routes are as follows: 
monohydroxylation in the dihydrobenzofuran ring; 
dihydrobenzofuran ring opening and 
N-dealkylation of the pyrrolidine nitrogen. 
 
The initial products of the hydroxylation and N-dealkylation pathways are major circulating 
metabolites but none contribute significantly to the overall clinical effect of darifenacin. 
 
The pharmacokinetics of darifenacin at steady state are dose-dependent, due to saturation of the 
CYP2D6 enzyme. 
 



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Doubling the darifenacin dose from 7.5 mg to 15 mg result in a 150% increase in steady-state 
exposure. This dose-dependency is probably caused by saturation of the CYP2D6 catalysed 
metabolism possibly together with some saturation of CYP3A4-mediated gut wall metabolism. 
 
Excretion 
Following administration of an oral dose of 14C-darifenacin solution to healthy volunteers, 
approximately 60% of the radioactivity was recovered in the urine and 40% in the faeces. Only a small 
percentage of the excreted dose was unchanged darifenacin (3%). Estimated darifenacin clearance is 
40 litres/hour. The elimination half-life of darifenacin following chronic dosing is approximately 
13-19 hours. 
 
Special patient population 
Gender 
A population pharmacokinetic analysis of patient data indicated that darifenacin exposure was 23% 
lower in males than females (see section 5.1). 
 
Elderly patients 
A population pharmacokinetic analysis of patient data indicated a trend for clearance to decrease with 
age (19% per decade based on Phase III population pharmacokinetic analysis of patients aged 60–
89 years), see section 4.2. 
 
Paediatric patients 
The pharmacokinetics of darifenacin have not been established in the paediatric population. 
 
CYP2D6 poor metabolisers 
The metabolism of darifenacin in CYP2D6 poor metabolisers is principally mediated by CYP3A4. In 
one pharmacokinetic study the steady-state exposure in poor metabolisers was 164% and 99% higher 
during treatment with 7.5 mg and 15 mg once daily, respectively. However, a population 
pharmacokinetic analyses of Phase III data indicated that on average steady-state exposure is 66% 
higher in poor metabolisers than in extensive metabolisers. There was considerable overlap between 
the ranges of exposures seen in these two populations (see section 4.2). 
 
Renal insufficiency 
A small study of subjects (n=24) with varying degrees of renal impairment (creatinine clearance 
between 10 ml/min and 136 ml/min) given darifenacin 15 mg once daily to steady state demonstrated 
no relationship between renal function and darifenacin clearance (see section 4.2). 
 
Hepatic insufficiency 
Darifenacin pharmacokinetics were investigated in subjects with mild (Child Pugh A) or moderate 
(Child Pugh B) impairment of hepatic function given darifenacin 15 mg once daily to steady state. 
Mild hepatic impairment had no effect on the pharmacokinetics of darifenacin. However, protein 
binding of darifenacin was affected by moderate hepatic impairment. Unbound darifenacin exposure 
was estimated to be 4.7-fold higher in subjects with moderate hepatic impairment than subjects with 
normal hepatic function (see section 4.2). 
 
5.3 Preclinical safety data 
 
Preclinical data reveal no special hazard for humans based on conventional studies of safety 
pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential. There were no effects 
on fertility in male and female rats treated at oral doses up to 50 mg/kg/day (78 times the AUC0-24h of 
free plasma concentration at maximum recommended human dose [MRHD]). There were no effects 
on reproductive organs in either sex in dogs treated for 1 year at oral doses up to 6 mg/kg/day 
(82 times the AUC0-24h of free plasma concentration at MRHD). Darifenacin was not teratogenic in 
rats and rabbits at doses up to 50 and 30 mg/kg/day, respectively. At the dose of 50 mg/kg/day in rats 
(59 times the AUC0-24h of free plasma concentration at MRHD), delay in the ossification of the sacral 
and caudal vertebrae was observed. At the dose of 30 mg/kg/day in rabbits (28 times the AUC0-24h of 
free plasma concentration at MRHD), maternal toxicity and foetotoxicity (increased post implantation 



10 

loss and decreased number of viable foetuses per litter) were observed. In peri and post-natal studies in 
rats, dystocia, increased foetal deaths in utero and toxicity to post-natal development (pup body weight 
and development land marks) were observed at systemic exposure levels up to 11 times the AUC0-24h 
of free plasma concentration at MRHD. 
 
 
6. PHARMACEUTICAL PARTICULARS 
 
6.1 List of excipients 
 
Tablet core 
Calcium hydrogen phosphate, anhydrous 
Hypromellose 
Magnesium stearate 
 
Film coat 
Polyethylene glycol 
Hypromellose 
Titanium dioxide (E171) 
Talc 
 
6.2 Incompatibilities 
 
Not applicable 
 
6.3 Shelf life 
 
3 years 
 
6.4 Special precautions for storage 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
6.5 Nature and contents of container 
 
Clear PVC/CTFE/aluminium or PVC/PVDC/aluminium blisters in cartons containing 7, 14, 28, 49, 56 
or 98 tablets as unit pack or in multipacks containing 140 (10x14) tablets. 
 
Not all pack sizes may be marketed. 
 
6.6 Special precautions for disposal 
 
No special requirements. 
 
 
7. MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 
8. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/001-006 
EU/1/04/294/013 
EU/1/04/294/015-020 



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EU/1/04/294/027 
 
 
9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 
 
Date of first authorisation: 22 October 2004 
Date of latest renewal: 24 September 2009 
 
 
10. DATE OF REVISION OF THE TEXT 
 
Detailed information on this product is available on the website of the European Medicines Agency 
http://www.ema.europa.eu 
 



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1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 15 mg prolonged-release tablets 
 
 
2. QUALITATIVE AND QUANTITATIVE COMPOSITION 
 
Each tablet contains 15 mg of darifenacin (as hydrobromide) 
 
For the full list of excipients, see section 6.1. 
 
 
3. PHARMACEUTICAL FORM 
 
Prolonged-release tablet 
 
Light peach round, convex tablet debossed with “DF” on one side and “15” on the reverse. 
 
 
4. CLINICAL PARTICULARS 
 
4.1 Therapeutic indications 
 
Symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may 
occur in adult patients with overactive bladder syndrome. 
 
4.2 Posology and method of administration 
 
Posology 
 
Adults 
The recommended starting dose is 7.5 mg daily. After 2 weeks of starting therapy, patients should be 
reassessed. For those patients requiring greater symptom relief, the dose may be increased to 15 mg 
daily, based on individual response. 
 
Elderly patients (≥ 65 years) 
The recommended starting dose for the elderly is 7.5 mg daily. After 2 weeks of starting therapy, 
patients should be reassessed for efficacy and safety. For those patients who have an acceptable 
tolerability profile but require greater symptom relief, the dose may be increased to 15 mg daily, based 
on individual response (see section 5.2). 
 
Paediatric population 
Emselex is not recommended for use in children below 18 years of age due to a lack of data on safety 
and efficacy. 
 
Renal impairment 
No dose adjustment is required in patients with impaired renal function. However, caution should be 
exercised when treating this population (see section 5.2). 
 
Hepatic impairment 
No dose adjustment is required in patients with mild hepatic impairment (Child Pugh A). However, 
there is a risk of increased exposure in this population (see section 5.2). 
 
Patients with moderate hepatic impairment (Child Pugh B) should only be treated if the benefit 
outweighs the risk, and the dose should be restricted to 7.5 mg daily (see section 5.2). Emselex is 
contraindicated in patients with severe hepatic impairment (Child Pugh C) (see section 4.3). 
 



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Patients receiving concomitant treatment with substances that are potent inhibitors of CYP2D6 or 
moderate inhibitors of CYP3A4 
In patients receiving substances that are potent CYP2D6 inhibitors, such as paroxetine, terbinafine, 
quinidine and cimetidine, treatment should start with the 7.5 mg dose. The dose may be titrated to 
15 mg daily to obtain an improved clinical response provided the dose is well tolerated. However, 
caution should be exercised. 
 
In patients receiving substances that are moderate CYP3A4 inhibitors, such as fluconazole, grapefruit 
juice and erythromycin, the recommended starting dose is 7.5 mg daily. The dose may be titrated to 
15 mg daily to obtain an improved clinical response provided the dose is well tolerated. However, 
caution should be exercised. 
 
Method of administration 
Emselex is for oral use. The tablets should be taken once daily with liquid. They can be taken with or 
without food, and must be swallowed whole and not chewed, divided or crushed. 
 
4.3 Contraindications 
 
Emselex is contraindicated in patients with: 
- Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. 
- Urinary retention. 
- Gastric retention. 
- Uncontrolled narrow-angle glaucoma. 
- Myasthenia gravis. 
- Severe hepatic impairment (Child Pugh C). 
- Severe ulcerative colitis. 
- Toxic megacolon. 
- Concomitant treatment with potent CYP3A4 inhibitors (see section 4.5). 
 
4.4 Special warnings and precautions for use 
 
Emselex should be administered with caution to patients with autonomic neuropathy, hiatus hernia, 
clinically significant bladder outflow obstruction, risk for urinary retention, severe constipation or 
gastrointestinal obstructive disorders, such as pyloric stenosis. 
 
Emselex should be used with caution in patients being treated for narrow-angle glaucoma (see 
section 4.3). 
 
Other causes of frequent urination (heart failure or renal disease) should be assessed before treatment 
with Emselex. If urinary tract infection is present, an appropriate antibacterial therapy should be 
started. 
 
Emselex should be used with caution in patients with risk of decreased gastrointestinal motility, 
gastro-oesophageal reflux and/or who are concurrently taking medicinal products (such as oral 
bisphosphonates) that can cause or exacerbate oesophagitis. 
 
Safety and efficacy have not yet been established in patients with a neurogenic cause for detrusor over 
activity. 
 
Caution should be used when prescribing antimuscarinics to patients with pre-existing cardiac 
diseases. 
 
As with other antimuscarinics, patients should be instructed to discontinue Emselex and seek 
immediate medical attention if they experience oedema of the tongue or laropharynx, or difficulty 
breathing (see section 4.8). 
 



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4.5 Interaction with other medicinal products and other forms of interaction 
 
Effects of other medicinal products on darifenacin 
Darifenacin metabolism is primarily mediated by the cytochrome P450 enzymes CYP2D6 and 
CYP3A4. Therefore, inhibitors of these enzymes may increase darifenacin exposure. 
 
CYP2D6 inhibitors 
In patients receiving substances that are potent CYP2D6 inhibitors (e.g. paroxetine, terbinafine, 
cimetidine and quinidine) the recommended starting dose should be 7.5 mg daily. The dose may be 
titrated to 15 mg daily to obtain an improved clinical response provided the dose is well tolerated. 
Concomitant treatment with potent CYP2D6 inhibitors results in an increase in exposure (e.g. of 33% 
with 20 mg paroxetine at the 30 mg dose of darifenacin). 
 
CYP3A4 inhibitors 
Darifenacin should not be used together with potent CYP3A4 inhibitors (see section 4.3) such as 
protease inhibitors (e.g. ritonavir), ketoconazole and itraconazole. Potent P-glycoprotein inhibitors 
such as ciclosporin and verapamil should also be avoided. Co-administration of darifenacin 7.5 mg 
with the potent CYP3A4 inhibitor ketoconazole 400 mg resulted in a 5-fold increase in steady-state 
darifenacin AUC. In subjects who are poor metabolisers, darifenacin exposure increased 
approximately 10-fold. Due to a greater contribution of CYP3A4 after higher darifenacin doses, the 
magnitude of the effect is expected to be even more pronounced when combining ketoconazole with 
darifenacin 15 mg. 
 
When co-administered with moderate CYP3A4 inhibitors such as erythromycin, clarithromycin, 
telithromycin, fluconazole and grapefruit juice, the recommended starting dose of darifenacin should 
be 7.5 mg daily. The dose may be titrated to 15 mg daily to obtain an improved clinical response 
provided the dose is well tolerated. Darifenacin AUC24 and Cmax from 30 mg once-daily dosing in 
subjects who are extensive metabolisers were 95% and 128% higher when erythromycin (moderate 
CYP3A4 inhibitor) was co-administered with darifenacin than when darifenacin was taken alone. 
 
Enzyme inducers 
Substances that are inducers of CYP3A4, such as rifampicin, carbamazepine, barbiturates and St 
John´s wort (Hypericum perforatum) are likely to decrease the plasma concentrations of darifenacin. 
 
Effects of darifenacin on other medicinal products 
CYP2D6 substrates 
Darifenacin is a moderate inhibitor of the enzyme CYP2D6. Caution should be exercised when 
darifenacin is used concomitantly with medicinal products that are predominantly metabolised by 
CYP2D6 and which have a narrow therapeutic window, such as flecainide, thioridazine, or tricyclic 
antidepressants such as imipramine. The effects of darifenacin on the metabolism of CYP2D6 
substrates are mainly clinically relevant for CYP2D6 substrates which are individually dose titrated. 
 
CYP3A4 substrates 
Darifenacin treatment resulted in a modest increase in the exposure of the CYP3A4 substrate 
midazolam. However the data available do not indicate that darifenacin changes either midazolam 
clearance or bioavailability. It can therefore be concluded that darifenacin administration does not alter 
the pharmacokinetics of CYP3A4 substrates in vivo. The interaction with midazolam lacks clinical 
relevance, and therefore no dose adjustment is needed for CYP3A4 substrates. 
 
Warfarin 
Standard therapeutic prothrombin time monitoring for warfarin should be continued. The effect of 
warfarin on prothrombin time was not altered when co-administered with darifenacin. 
 
Digoxin 
Therapeutic drug monitoring for digoxin should be performed when initiating and ending darifenacin 
treatment as well as changing the darifenacin dose. Darifenacin 30 mg once daily (two times greater 
than the recommended daily dose) co-administered with digoxin at steady state resulted in a small 



15 

increase in digoxin exposure (AUC: 16% and Cmax: 20%). The increase in digoxin exposure could be 
caused by competition between darifenacin and digoxin for P-glycoprotein. Other transporter-related 
interactions cannot be excluded. 
 
Antimuscarinic agents 
As with any other antimuscarinic agents, concomitant use of medicinal products that possess 
antimuscarinic properties, such as oxybutynin, tolterodine and flavoxate, may result in more 
pronounced therapeutic and side effects. The potentiation of anticholinergic effects with anti-
parkinson agents and tricyclic antidepressants may also occur if antimuscarinic agents are used 
concurrently with such medicinal products. However, no studies involving the interaction with anti-
parkinson agents and tricyclic antidepressants have been performed. 
 
4.6 Fertility, pregnancy and lactation 
 
Pregnancy 
There are limited amount of data from the use of darifenacin in pregnant women. Studies in animals 
have shown toxicity to parturition (for details, see section 5.3). Emselex is not recommended during 
pregnancy. 
 
Breast-feeding 
Darifenacin is excreted in the milk of rats. It is not known whether darifenacin is excreted in human 
milk. A risk to the nursing child cannot be excluded. A decision whether to avoid breast-feeding or to 
abstain from Emselex therapy during lactation should be based on a benefit and risk comparison. 
 
Fertility 
There are no human fertility data for darifenacin. Darifenacin had no effect on male or female fertility 
in rats or any effect in the reproductive organs of either sex in rats and dogs (for details, see section 
5.3). Women of child bearing potential should be made aware of the lack of fertility data, and Emselex 
should only be given after consideration of individual risks and benefits. 
 
 
4.7 Effects on ability to drive and use machines 
 
As with other antimuscarinic agents, Emselex may produce effects such as dizziness, blurred vision, 
insomnia and somnolence. Patients experiencing these side effects should not drive or use machines. 
For Emselex, these side effects have been reported to be uncommon. 
 
4.8 Undesirable effects 
 
Summary of the safety profile  
Consistent with the pharmacological profile, the most commonly reported adverse reactions were dry 
mouth (20.2% and 35% for the 7.5 mg and 15 mg dose, respectively, 18.7% after flexible dose 
titration, and 8% - 9% for placebo) and constipation (14.8% and 21% for the 7.5 mg and 15 mg dose, 
respectively, 20.9% after flexible dose titration, and 5.4% - 7.9% for placebo). Anticholinergic effects, 
in general, are dose-dependent. 
 
However, the patient discontinuation rates due to these adverse reactions were low (dry mouth: 0% - 
0.9% and constipation: 0.6% - 2.2% for darifenacin, depending on the dose; and 0% and 0.3% for 
placebo, for dry mouth and constipation, respectively). 
 
 



16 

 
Tabulated list of adverse reactions 
The adverse reactions are ranked under heading of frequency using the following convention: very 
common (≥1/10), common (≥1/100 to <1/10), uncommon (1/1,000 to <1/100), rare (1/10,000 to 
<1/1,000), very rare (<1/10,000) and not known (cannot be estimated from the available data). Within 
each frequency grouping, adverse reactions are presented in order of decreasing seriousness. 
 
Table 1: Adverse reactions with Emselex 7.5 mg and 15 mg prolonged-release tablets 
 

Infections and infestations 
Uncommon Urinary tract infection 
Psychiatric disorders 
Uncommon Insomnia, thinking abnormal 
Nervous system disorders 
Common Headache 
Uncommon Dizziness, dysgeusia, somnolence 
Eye disorders 
Common Dry eye 
Uncommon Visual disturbance, including vision blurred 
Vascular disorders 
Uncommon Hypertension 
Respiratory, thoracic and mediastinal disorders 
Common Nasal dryness 
Uncommon Dyspnoea, cough, rhinitis 
Gastrointestinal disorders 
Very common Constipation, dry mouth 
Common Abdominal pain, nausea, dyspepsia 
Uncommon Flatulence, diarrhoea, mouth ulceration 
Skin and subcutaneous tissue disorders 
Uncommon Rash, dry skin, pruritus, hyperhidrosis 
Not known Angioedema 
Renal and urinary disorders 
Uncommon Urinary retention, urinary tract disorder, bladder pain 
Reproductive system and breast disorders 
Uncommon Erectile dysfunction, vaginitis 
General disorders and administration site conditions 
Uncommon Oedema peripheral, asthenia, face oedema, oedema 
Investigations 
Uncommon Aspartate aminotransferase increased, alanine 

aminotransferase increased 
Injury, poisoning, and procedural complications 
Uncommon Injury 

 

Description of selected adverse reactions  
In the pivotal clinical trials with doses of Emselex 7.5 mg and 15 mg, adverse reactions were reported 
as presented in the table above. Most of the adverse reactions were of mild or moderate intensity and 
did not result in discontinuation in the majority of the patients. 
 
Treatment with Emselex may possibly mask symptoms associated with gallbladder disease. However, 
there was no association between the occurrence of adverse events related to the biliary system in 
darifenacin-treated patients and increasing age. 
 
The incidence of adverse reactions with the doses of Emselex 7.5 mg and 15 mg decreased during the 
treatment period up to 6 months. A similar trend is also seen for the discontinuation rates. 
 



17 

Post-marketing experience 
The following events have been reported in association with darifenacin use in worldwide post-
marketing experience: generalised hypersensitivity reactions including angioedema, depressed 
mood/mood alterations, hallucination. Because these spontaneously reported events are from the 
worldwide post-marketing experience, the frequency of events cannot be estimated from the available 
data. 
 
Reporting of suspected adverse reactions 
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It 
allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare 
professionals are asked to report any suspected adverse reactions via the national reporting system 
listed in Appendix V. 
 
 
4.9 Overdose 
 
Emselex has been administered in clinical trials at doses up to 75 mg (five times maximum therapeutic 
dose). The most common adverse reactions seen were dry mouth, constipation, headache, dyspepsia 
and nasal dryness. However, overdose with darifenacin can potentially lead to severe anticholinergic 
effects and should be treated accordingly. Therapy should be aimed at reversing the anticholinergic 
symptoms under careful medical supervision. The use of agents such as physostigmine can assist in 
reversing such symptoms. 
 
 
5. PHARMACOLOGICAL PROPERTIES 
 
5.1 Pharmacodynamic properties 
 
Pharmacotherapeutic group: Urologicals, drugs for urinary frequency and incontinence; ATC code: 
G04BD10. 
 
Mechanism of action  
Darifenacin is a selective muscarinic M3 receptor antagonist (M3 SRA) in vitro. The M3 receptor is 
the major subtype that controls urinary bladder muscle contraction. It is not known whether this 
selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of 
overactive bladder syndrome. 
 
 
Clinical efficacy and safety  
Cystometric studies performed with darifenacin in patients with involuntary bladder contractions 
showed increased bladder capacity, increased volume threshold for unstable contractions and 
diminished frequency of unstable detrusor contractions. 
 
Treatment with Emselex administered at dosages of 7.5 mg and 15 mg daily has been investigated in 
four double-blind, Phase III, randomised, controlled clinical studies in male and female patients with 
symptoms of overactive bladder. As seen in Table 2 below, a pooled analysis of 3 of the studies for the 
treatment with both Emselex 7.5 mg and 15 mg provided a statistically significant improvement in the 
primary endpoint, reduction in incontinence episodes, versus placebo. 
 
Table 2: Pooled analysis of data from three Phase III clinical studies assessing fixed doses of 7.5 mg 
and 15 mg Emselex 
 

Dose N Incontinence episodes per week 95% CI P value2 
Baseline 
(median) 

Week 12 
(median) 

Change from 
baseline 
(median) 

Differences 
from placebo1 

(median) 



18 

Emselex 
7.5 mg 
once daily 

335 16.0 4.9 -8.8 (-68%) -2.0 (-3.6, -0.7) 0.004 

Placebo 271 16.6 7.9 -7.0 (-54%) -- -- -- 
        
Emselex 
15 mg 
once daily 

330 16.9 4.1 -10.6 (-77%) -3.2 (-4.5, -2.0) <0.001 

Placebo 384 16.6 6.4 -7.5 (-58%) -- -- -- 
1 Hodges Lehmann estimate: median difference from placebo in change from baseline 
2 Stratified Wilcoxon test for difference from placebo. 
 
Emselex 7.5 mg and 15 mg doses significantly reduced both the severity and number of urinary 
urgency episodes and the number of micturitions, while significantly increasing the mean volume 
voided from baseline. 
 
Emselex 7.5 mg and 15 mg were associated with statistically significant improvements over placebo in 
some aspects of quality of life as measured by the Kings Health Questionnaire including incontinence 
impact, role limitations, social limitations and severity measures. 
 
For both doses of 7.5 mg and 15 mg, the percentage median reduction from baseline in the number of 
incontinence episodes per week was similar between males and females. The observed differences 
from placebo for males in terms of percentage and absolute reductions in incontinence episodes was 
lower than for females. 
 
The effect of treatment with 15 mg and 75 mg of darifenacin on QT/QTc interval was evaluated in a 
study in 179 healthy adults (44% male: 56% females) aged 18 to 65 for 6 days (to steady state). 
Therapeutic and supra-therapeutic doses of darifenacin resulted in no increase in QT/QTc interval 
prolongation from baseline compared to placebo at maximum darifenacin exposure. 
 
5.2 Pharmacokinetic properties 
 
Darifenacin is metabolised by CYP3A4 and CYP2D6. Due to genetic differences, about 7% of the 
Caucasians lack the CYP2D6 enzyme and are said to be poor metabolisers. A few percent of the 
population have increased CYP2D6 enzyme levels (ultrafast metabolisers). The information below 
applies to subjects who have normal CYP2D6 activity (extensive metabolisers) unless otherwise 
stated. 
 
Absorption 
Due to extensive first-pass metabolism darifenacin has a bioavailability of approximately 15% and 
19% after 7.5 mg and 15 mg daily doses at steady state. Maximum plasma levels are reached 
approximately 7 hours after administration of the prolonged-release tablets and steady-state plasma 
levels are achieved by the sixth day of administration. At steady state, peak-to-trough fluctuations in 
darifenacin concentrations are small (PTF: 0.87 for 7.5 mg and 0.76 for 15 mg), thereby maintaining 
therapeutic plasma levels over the dosing interval. Food had no effect on darifenacin pharmacokinetics 
during multiple-dose administration of prolonged-release tablets. 
 
Distribution 
Darifenacin is a lipophilic base and is 98% bound to plasma proteins (primarily to alpha-1-acid-
glycoprotein). The steady-state volume of distribution (Vss) is estimated to be 163 litres. 
 
Metabolism 
Darifenacin is extensively metabolised by the liver following oral administration. 
 
Darifenacin undergoes significant metabolism by cytochrome CYP3A4 and CYP2D6 in the liver and 
by CYP3A4 in the gut wall. The three main metabolic routes are as follows: 
monohydroxylation in the dihydrobenzofuran ring; 



19 

dihydrobenzofuran ring opening and 
N-dealkylation of the pyrrolidine nitrogen. 
 
The initial products of the hydroxylation and N-dealkylation pathways are major circulating 
metabolites but none contribute significantly to the overall clinical effect of darifenacin. 
 
The pharmacokinetics of darifenacin at steady state are dose-dependent, due to saturation of the 
CYP2D6 enzyme. 
 
Doubling the darifenacin dose from 7.5 mg to 15 mg result in a 150% increase in steady-state 
exposure. This dose-dependency is probably caused by saturation of the CYP2D6 catalysed 
metabolism possibly together with some saturation of CYP3A4-mediated gut wall metabolism. 
 
Excretion 
Following administration of an oral dose of 14C-darifenacin solution to healthy volunteers, 
approximately 60% of the radioactivity was recovered in the urine and 40% in the faeces. Only a small 
percentage of the excreted dose was unchanged darifenacin (3%). Estimated darifenacin clearance is 
40 litres/hour. The elimination half-life of darifenacin following chronic dosing is approximately 
13-19 hours. 
 
Special patient population 
Gender 
A population pharmacokinetic analysis of patient data indicated that darifenacin exposure was 23% 
lower in males than females (see section 5.1). 
 
Elderly patients 
A population pharmacokinetic analysis of patient data indicated a trend for clearance to decrease with 
age (19% per decade based on Phase III population pharmacokinetic analysis of patients aged 60–
89 years), see section 4.2. 
 
Paediatric patients 
The pharmacokinetics of darifenacin have not been established in the paediatric population. 
 
CYP2D6 poor metabolisers 
The metabolism of darifenacin in CYP2D6 poor metabolisers is principally mediated by CYP3A4. In 
one pharmacokinetic study the steady-state exposure in poor metabolisers was 164% and 99% higher 
during treatment with 7.5 mg and 15 mg once daily, respectively. However, a population 
pharmacokinetic analyses of Phase III data indicated that on average steady-state exposure is 66% 
higher in poor metabolisers than in extensive metabolisers. There was considerable overlap between 
the ranges of exposures seen in these two populations (see section 4.2). 
 
Renal insufficiency 
A small study of subjects (n=24) with varying degrees of renal impairment (creatinine clearance 
between 10 ml/min and 136 ml/min) given darifenacin 15 mg once daily to steady state demonstrated 
no relationship between renal function and darifenacin clearance (see section 4.2). 
 
Hepatic insufficiency 
Darifenacin pharmacokinetics were investigated in subjects with mild (Child Pugh A) or moderate 
(Child Pugh B) impairment of hepatic function given darifenacin 15 mg once daily to steady state. 
Mild hepatic impairment had no effect on the pharmacokinetics of darifenacin. However, protein 
binding of darifenacin was affected by moderate hepatic impairment. Unbound darifenacin exposure 
was estimated to be 4.7-fold higher in subjects with moderate hepatic impairment than subjects with 
normal hepatic function (see section 4.2). 
 
5.3 Preclinical safety data 
 



20 

Preclinical data reveal no special hazard for humans based on conventional studies of safety 
pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential. There were no effects 
on fertility in male and female rats treated at oral doses up to 50 mg/kg/day (78 times the AUC0-24h of 
free plasma concentration at maximum recommended human dose [MRHD]). There were no effects 
on reproductive organs in either sex in dogs treated for 1 year at oral doses up to 6 mg/kg/day 
(82 times the AUC0-24h of free plasma concentration at MRHD). Darifenacin was not teratogenic in 
rats and rabbits at doses up to 50 and 30 mg/kg/day, respectively. At the dose of 50 mg/kg/day in rats 
(59 times the AUC0-24h of free plasma concentration at MRHD), delay in the ossification of the sacral 
and caudal vertebrae was observed. At the dose of 30 mg/kg/day in rabbits (28 times the AUC0-24h of 
free plasma concentration at MRHD), maternal toxicity and foetotoxicity (increased post implantation 
loss and decreased number of viable foetuses per litter) were observed. In peri and post-natal studies in 
rats, dystocia, increased foetal deaths in utero and toxicity to post-natal development (pup body weight 
and development land marks) were observed at systemic exposure levels up to 11 times the AUC0-24h 
of free plasma concentration at MRHD. 
 
 
6. PHARMACEUTICAL PARTICULARS 
 
6.1 List of excipients 
 
Tablet core 
Calcium hydrogen phosphate, anhydrous 
Hypromellose 
Magnesium stearate 
 
Film coat 
Polyethylene glycol 
Hypromellose 
Talc 
Titanium dioxide (E171) 
Yellow iron oxide (E172) 
Red iron oxide (E172) 
 
6.2 Incompatibilities 
 
Not applicable 
 
6.3 Shelf life 
 
3 years 
 
6.4 Special precautions for storage 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
6.5 Nature and contents of container 
 
Clear PVC/CTFE/aluminium or PVC/PVDC/aluminium blisters in cartons containing 7, 14, 28, 49, 56 
or 98 tablets as unit pack or in multipacks containing 140 (10x14) tablets. 
 
Not all pack sizes may be marketed. 
 
6.6 Special precautions for disposal 
 
No special requirements. 
 
 



21 

7. MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 
8. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/007-012 
EU/1/04/294/014 
EU/1/04/294/021-026 
EU/1/04/294/028 
 
 
9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 
 
Date of first authorisation: 22 October 2004 
Date of latest renewal: 24 September 2009 
 
 
10. DATE OF REVISION OF THE TEXT 
 
Detailed information on this product is available on the website of the European Medicines Agency 
http://www.ema.europa.eu 
  



22 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX II 
 
A. MANUFACTURER RESPONSIBLE FOR BATCH RELEASE 
 
B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY 

AND USE 
 
C.  OTHER CONDITIONS AND REQUIREMENTS OF THE 

MARKETING AUTHORISATION  
 
D. CONDITIONS OR RESTRICTIONS WITH REGARD TO 

THE SAFE AND EFFECTIVE USE OF THE MEDICINAL 
PRODUCT 



23 

A. MANUFACTURER RESPONSIBLE FOR BATCH RELEASE 
 
Name and address of the manufacturer responsible for batch release 
 
Norgine B. V., 
Antonio vivaldistraat 150, 
1083 HP Amsterdam, 
The Netherlands  
 
B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE  
 
Medicinal product subject to medical prescription 
 
C.  OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING 

AUTHORISATION  
 
 Periodic Safety Update Reports 
 
The requirements for submission of periodic safety update reports for this medicinal product are set 
out in the list of Union reference dates (EURD list) provided for under Article 107c(7) of Directive 
2001/83/EC and any subsequent updates published on the European medicines web-portal. 
 
D.  CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND 

EFFECTIVE USE OF THE MEDICINAL PRODUCT   
 
 Risk Management Plan (RMP) 
 
The MAH shall perform the required pharmacovigilance activities and interventions detailed in 
the agreed RMP presented in Module 1.8.2 of the Marketing Authorisation and any agreed 
subsequent updates of the RMP. 
 
An updated RMP should be submitted: 
 At the request of the European Medicines Agency; 
 Whenever the risk management system is modified, especially as the result of new information 

being received that may lead to a significant change to the benefit/risk profile or as the result of 
an important (pharmacovigilance or risk minimisation) milestone being reached. 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 



24 

 
 
 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX III 
 

LABELLING AND PACKAGE LEAFLET 
  



25 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

A. LABELLING 
  



26 

PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
CARTON OF UNIT PACK 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 7.5 mg prolonged-release tablets 
darifenacin 
 
 

2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each tablet contains 7.5 mg darifenacin (as hydrobromide). 
 
 

3. LIST OF EXCIPIENTS 
 
 

4. PHARMACEUTICAL FORM AND CONTENTS 
 
7 tablets 
14 tablets 
28 tablets 
49 tablets 
56 tablets 
98 tablets 
 
 

5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Oral use. 
Read the package leaflet before use. 
 
 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 
OF THE SIGHT AND REACH OF CHILDREN 

 
Keep out of the sight and reach of children. 
 
 
 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 

8. EXPIRY DATE 
 
EXP 
 
 

9. SPECIAL STORAGE CONDITIONS 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
 



27 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 

11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 

12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/001 7 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/002 14 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/003 28 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/004 49 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/005 56 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/006 98 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/015 7 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/016 14 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/017 28 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/018 49 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/019 56 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/020 98 tablets (PVC/PVDC/alu blisters) 
 
 

13. BATCH NUMBER 
 
Lot 
 
 

14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 

15. INSTRUCTIONS ON USE 
 
 

16. INFORMATION IN BRAILLE 
 
Emselex 7.5 mg 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC:  
SN:  
NN:  
 



28 

 
PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
OUTER CARTON OF MULTIPACKS (INCLUDING BLUE BOX) 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 7.5 mg prolonged-release tablets 
darifenacin 
 
 

2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each tablet contains 7.5 mg darifenacin (as hydrobromide). 
 
 

3. LIST OF EXCIPIENTS 
 
 

4. PHARMACEUTICAL FORM AND CONTENTS 
 
140 tablets 
Multipack comprising 10 packs, each containing 14 tablets. 
 
 

5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Oral use. 
Read the package leaflet before use. 
 
 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 
OF THE SIGHT AND REACH OF CHILDREN 

 
Keep out of the sight and reach of children. 
 
 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 

8. EXPIRY DATE 
 
EXP 
 
 

9. SPECIAL STORAGE CONDITIONS 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 



29 

11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg  
 
 

12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/013 (PVC/CTFE/alu blisters) 
EU/1/04/294/027 (PVC/PVDC/alu blisters) 
 
 

13. BATCH NUMBER 
 
Lot 
 
 

14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 

15. INSTRUCTIONS ON USE 
 
 

16. INFORMATION IN BRAILLE 
 
Emselex 7.5 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC:  
SN:  
NN:  
 
  



30 

PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
INTERMEDIATE CARTON OF MULTIPACKS (WITHOUT BLUE BOX) 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 7.5 mg prolonged-release tablets 
darifenacin 
 
 

2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each tablet contains 7.5 mg darifenacin (as hydrobromide). 
 
 

3. LIST OF EXCIPIENTS 
 
 

4. PHARMACEUTICAL FORM AND CONTENTS 
 
14 tablets 
Component of a multipack, not to be sold separately. 
 
 

5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Oral use. 
Read the package leaflet before use. 
 
 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 
OF THE SIGHT AND REACH OF CHILDREN 

 
Keep out of the sight and reach of children. 
 
 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 

8. EXPIRY DATE 
 
EXP 
 
 

9. SPECIAL STORAGE CONDITIONS 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 

11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 



31 

 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 

12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/013 (PVC/CTFE/alu blisters) 
EU/1/04/294/027 (PVC/PVDC/alu blisters) 
 
 

13. BATCH NUMBER 
 
Lot 
 
 

14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 

15. INSTRUCTIONS ON USE 
 
 

16. INFORMATION IN BRAILLE 
 
Emselex 7.5 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC:  
SN:  
NN:  
 
  



32 

MINIMUM PARTICULARS TO APPEAR ON BLISTERS OR STRIPS 
 
BLISTER 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 7.5 mg prolonged-release tablets 
darifenacin 
 
 

2. NAME OF THE MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
 
 
 

3. EXPIRY DATE 
 
EXP 
 
 

4. BATCH NUMBER 
 
Lot 
 
 

5. OTHER 
 
 
  



33 

PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
CARTON OF UNIT PACK 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 15 mg prolonged-release tablets 
darifenacin 
 
 

2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each tablet contains 15 mg darifenacin (as hydrobromide). 
 
 

3. LIST OF EXCIPIENTS 
 
 

4. PHARMACEUTICAL FORM AND CONTENTS 
 
7 tablets 
14 tablets 
28 tablets 
49 tablets 
56 tablets 
98 tablets 
 
 

5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Oral use. 
Read the package leaflet before use. 
 
 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 
OF THE SIGHT AND REACH OF CHILDREN 

 
Keep out of the sight and reach of children. 
 
 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 

8. EXPIRY DATE 
 
EXP 
 
 

9. SPECIAL STORAGE CONDITIONS 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
 



34 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 

11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 

12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/007 7 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/008 14 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/009 28 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/010 49 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/011 56 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/012 98 tablets (PVC/CTFE/alu blisters) 
EU/1/04/294/021 7 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/022 14 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/023 28 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/024 49 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/025 56 tablets (PVC/PVDC/alu blisters) 
EU/1/04/294/026 98 tablets (PVC/PVDC/alu blisters) 
 
 

13. BATCH NUMBER 
 
Lot 
 
 

14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 

15. INSTRUCTIONS ON USE 
 
 

16. INFORMATION IN BRAILLE 
 
Emselex 15 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC:  
SN:  
NN:  



35 

 
 

PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
OUTER CARTON OF MULTIPACKS (INCLUDING BLUE BOX) 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 15 mg prolonged-release tablets 
darifenacin 
 
 

2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each tablet contains 15 mg darifenacin (as hydrobromide). 
 
 

3. LIST OF EXCIPIENTS 
 
 

4. PHARMACEUTICAL FORM AND CONTENTS 
 
140 tablets 
Multipack comprising 10 packs, each containing 14 tablets. 
 
 

5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Oral use. 
Read the package leaflet before use. 
 
 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 
OF THE SIGHT AND REACH OF CHILDREN 

 
Keep out of the sight and reach of children. 
 
 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 

8. EXPIRY DATE 
 
EXP 
 
 

9. SPECIAL STORAGE CONDITIONS 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 



36 

 
11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 

 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 

12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/014 (PVC/CTFE/alu blisters) 
EU/1/04/294/028 (PVC/PVDC/alu blisters) 
 
 

13. BATCH NUMBER 
 
Lot 
 
 

14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 

15. INSTRUCTIONS ON USE 
 
 

16. INFORMATION IN BRAILLE 
 
Emselex 15 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC:  
SN:  
NN:  
 
 
 
 
  



37 

PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
INTERMEDIATE CARTON OF MULTIPACKS (WITHOUT BLUE BOX) 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 15 mg prolonged-release tablets 
darifenacin 
 
 

2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each tablet contains 15 mg darifenacin (as hydrobromide). 
 
 

3. LIST OF EXCIPIENTS 
 
 

4. PHARMACEUTICAL FORM AND CONTENTS 
 
14 tablets 
Component of a multipack, not to be sold separately. 
 
 

5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Oral use. 
Read the package leaflet before use. 
 
 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 
OF THE SIGHT AND REACH OF CHILDREN 

 
Keep out of the sight and reach of children. 
 
 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 

8. EXPIRY DATE 
 
EXP 
 
 

9. SPECIAL STORAGE CONDITIONS 
 
Keep the blister packs in the outer carton in order to protect from light. 
 
 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 

11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 



38 

 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
 
 

12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/04/294/014 (PVC/CTFE/alu blisters) 
EU/1/04/294/028 (PVC/PVDC/alu blisters) 
 
 

13. BATCH NUMBER 
 
Lot 
 
 

14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 

15. INSTRUCTIONS ON USE 
 
 

16. INFORMATION IN BRAILLE 
 
Emselex 15 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC:  
SN:  
NN:  
 
 
 
 
  



39 

MINIMUM PARTICULARS TO APPEAR ON BLISTERS OR STRIPS 
 
BLISTER 

 
 

1. NAME OF THE MEDICINAL PRODUCT 
 
Emselex 15 mg prolonged-release tablets 
darifenacin 
 
 

2. NAME OF THE MARKETING AUTHORISATION HOLDER 
 
Merus Labs Luxco II S.à R.L. 
 
 

3. EXPIRY DATE 
 
EXP 
 
 

4. BATCH NUMBER 
 
Lot 
 
 

5. OTHER 
 
  



40 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

B. PACKAGE LEAFLET 



41 

Package leaflet: Information for the user 
 

Emselex 7.5 mg prolonged-release tablets 
Darifenacin 

 
Read all of this leaflet carefully before you start taking this medicine because it contains 
important information for you. 
- Keep this leaflet. You may need to read it again. 
- If you have any further questions, ask your doctor or pharmacist. 
- This medicine has been prescribed for you. Do not pass it on to others. It may harm them, even 

if their symptoms are the same as yours. 
- If you get any side effects, talk your doctor or pharmacist. This includes any possible side 

effects not listed in this leaflet. See section 4. 
 
What is in this leaflet 
1. What Emselex is and what it is used for 
2. What you need to know before you take Emselex 
3. How to take Emselex 
4. Possible side effects 
5. How to store Emselex 
6. Contents of the pack and other information  
 
 
1. What Emselex is and what it is used for 
 
How Emselex works 
Emselex reduces the activity of an overactive bladder. This enables you to wait longer before you go 
to the toilet and it increases the amount of urine that your bladder can hold. 
 
What Emselex can be used for 
Emselex belongs to a class of medicines which relax the muscles of the bladder. It is used in adults for 
the treatment of the symptoms of overactive bladder conditions - such as a sudden urge to rush to the 
toilet, needing to go to the toilet frequently and/or not getting to the toilet in time and wetting yourself 
(urge incontinence). 
 
 
2. What you need to know before you take Emselex 
 
Do not take Emselex: 
 if you are allergic to darifenacin or any of the other ingredients of this medicine (listed in 

section 6). 
 if you suffer from urinary retention (inability to empty your bladder). 
 if you have gastric retention (problems emptying the contents of the stomach). 
 if you suffer from uncontrolled narrow-angle glaucoma (high pressure in the eyes with loss of 

eyesight that is not being adequately treated). 
 if you have myasthenia gravis (a disease marked by abnormal tiredness and weakness of 

selected muscles). 
 if you have severe ulcerative colitis or toxic megacolon (acute dilation of the colon due to 

complication of infection or inflammation). 
 if you have severe liver problems. 
 There are some medicines such as ciclosporin (a medicine used in transplantation to prevent 

organ rejection or for other conditions, e.g. rheumatoid arthritis or atopic dermatitis), verapamil 
(a medicine used to lower blood pressure, to correct heart rhythm or to treat angina pectoris), 
antifungal medicines (e.g. ketoconazole and itraconazole) and some antiviral medicines (e.g. 
ritonavir) that must not be taken with Emselex. 

 
 



42 

Warnings and precautions 
Talk to your doctor  before taking Emselex 
 if you have autonomic neuropathy (damage to the nerves that communicate between the brain 

and internal organs, muscles, skin, and blood vessels to regulate vital functions, including the 
heart rate, blood pressure and bowel function) – your doctor will have told you if you have this. 

 if you have heartburn and belching. 
 if you have difficulties in passing urine and a weak stream of urine. 
 if you have severe constipation (less than or equal to 2 bowel movements per week). 
 if you have a digestive motility disorder. 
 if you have an obstructive gastrointestinal disorder (any obstruction of the passage of intestinal 

or gastric contents, such as narrowing of the pylorus, the lower part of the stomach) – your 
doctor will have told you if you have this. 

 if you are taking medicinal products that can cause or worsen inflammation of the oesophagus 
such as oral bisphosphonates (a class of medicinal products that prevent the loss of bone mass 
and are used to treat osteoporosis). 

 if you are receiving treatment for narrow-angle glaucoma. 
 if you have liver problems. 
 if you have kidney problems. 
 if you have heart diseases. 
If any of these apply to you, tell your doctor before you take Emselex. 
 
During treatment with Emselex, tell your doctor straight away and stop taking Emselex if you 
experience swelling of the face, lips, tongue and/or throat (signs of angioedema). 
 
Children and adolescents  
Emselex is not recommended for use in children and adolescents (<18 years). 
 
Other medicines and Emselex 
Tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including 
medicines obtained without a prescription. This is particularly important if you are taking any of the 
following as your doctor may need to adjust your dose of Emselex and/or the other medicine: 
 certain antibiotics (e.g. erythromycin, clarithromycin and rifampicin), 
 antifungal medicines (e.g. ketoconazole and itraconazole), 
 antiviral medicines (e.g. nelfinavir and ritonavir), 
 antipsychotic medicines (e.g. thioridazine), 
 certain antidepressants (e.g. imipramine), 
 certain anticonvulsants (carbamazepine, barbiturates), 
 certain medicines used to treat heart problems (e.g. flecainide, verapamil and digoxin), 
 other antimuscarinic medicines (e.g. tolterodine, oxybutynin and flavoxate). 
Please also inform your doctor if you are taking products containing St John’s wort. 
 
Emselex with food and drink 
Eating food has no effect on Emselex. Grapefruit juice may interact with Emselex. However, the 
adjustment of Emselex doses is not necessary. 
 
Pregnancy and breast-feeding 
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask 
your doctor for advice before taking this medicine. 
Emselex is not recommended during pregnancy. 
Emselex should be taken with caution while breast-feeding. 
 
Driving and using machines 
Emselex may cause effects such as dizziness, blurred vision, trouble sleeping or drowsiness. If you 
have any of these symptoms whilst taking Emselex, consult your doctor for advice on changing the 
dose or considering an alternative treatment. You should not drive or use machines if you are affected 



43 

by these symptoms. For Emselex, these side effects have been reported to be uncommon (see 
section 4). 
 
3. How to take Emselex 
 
Always take Emselex exactly as your doctor has told you. You should check with your doctor or 
pharmacist if you are not sure. If you have the impression that the effect of Emselex is too strong or 
too weak, talk to your doctor or pharmacist. 
 
How much Emselex to take 
The recommended starting dose, including for patients aged over 65 years, is 7.5 mg daily. Depending 
on your response to Emselex, your doctor may increase your dose to 15 mg daily, two weeks after 
starting therapy. 
 
These doses are suitable for people with mild liver problems or people with kidney problems. 
 
Take Emselex tablets once a day with water, at about the same time each day. 
 
The tablet may be taken with or without food. Swallow the tablet whole. Do not chew, split or crush it. 
 
How long to take Emselex 
Your doctor will tell you how long your treatment with Emselex will last. Do not stop treatment early 
because you do not see an immediate effect. Your bladder will need some time to adapt. Finish the 
course of treatment prescribed by your doctor. If you have not noticed any effect by then, discuss it 
with your doctor. 
 
If you take more Emselex than you should 
If you have taken more tablets than you have been told to take, or if someone else accidentally takes 
your tablets, go to your doctor or hospital for advice immediately. When seeking medical advice, 
make sure that you take this leaflet and your remaining tablets with you to show them to the doctor. 
People who have taken an overdose may have dry mouth, constipation, headache, indigestion and 
nasal dryness. Overdose with Emselex may lead to severe symptoms requiring emergency treatment in 
hospital. 
 
If you forget to take Emselex 
If you forget to take Emselex at the usual time, take it as soon as you remember, unless it is the time 
for your next dose. Do not take a double dose to make up for a forgotten dose. 
 
If you stop taking Emselex 
It has been shown that taking all doses at the appropriate times can greatly increase the effectiveness 
of your medicine. Therefore, it is important to keep taking Emselex correctly, as described above. Do 
not stop taking Emselex until your doctor tells you to. You should not experience any effects when 
you stop treatment. 
 
If you have any further questions on the use of this product, ask your doctor or pharmacist. 
 
 
4. Possible side effects 
 
Like all medicines, this medicine can cause side effects, although not everybody gets them. The side 
effects caused by Emselex are usually mild and temporary. 
 
Some side effects could be serious 
Serious allergic reactions including swelling, mainly of the face and throat. 
 
Other side effects 
Very common (may affect more than 1 in 10 people) 



44 

Dry mouth, constipation. 
 
Common (may affect up to 1 in 10 people) 
Headache, abdominal pain, indigestion, feeling sick, dry eyes, nasal dryness. 
 
Uncommon (may affect up to 1 in 100 people) 
Fatigue, accidental injury, facial swelling, high blood pressure, diarrhoea, flatulence, inflammation of 
the mucous membrane of the mouth, increased liver enzymes, swelling, dizziness, sleeplessness, 
drowsiness, abnormal thinking, runny nose (rhinitis), cough, shortness of breath, dry skin, itching, 
rash, sweating, visual disturbance including blurred vision, taste disturbance, urinary tract disorder or 
infection, impotence, discharge and itching in the vagina, bladder pain, inability to empty your 
bladder. 
 
Not known (frequency cannot be estimated from the available data) 
Depressed mood/mood alterations, hallucination. 
 
Reporting of side effects 
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects 
not listed in this leaflet. You can also report side effects directly via the national reporting system 
listed in Appendix V. By reporting side effects you can help provide more information on the safety of 
this medicine. 
 
 
5. How to store Emselex 
 
 Keep this medicine out of the sight and reach of children. 
 Do not use this medicine after the expiry date which is stated on the carton and blister. The 

expiry date refers to the last day of that month. 
 Keep the blister packs in the outer carton in order to protect from light. 
 Do not use if the pack is damaged or shows signs of tampering. 
 Do not throw away any medicines via wastewater or household waste. Ask your pharmacist 

how to throw away medicines you no longer use. These measures will help protect the 
environment. 

 
 
6. Contents of the pack and other information 
 
What Emselex contains 
- The active substance is darifenacin. Each tablet contains 7.5 mg darifenacin (as hydrobromide). 
- The other ingredients are calcium hydrogen phosphate (anhydrous), hypromellose, magnesium 

stearate, polyethylene glycol, titanium dioxide (E171) and talc. 
 
What Emselex looks like and contents of the pack 
Emselex 7.5 mg prolonged-release tablets are round, convex white tablets and are debossed with “DF” 
on one side and “7.5” on the other. 
 
The tablets are available in blister packs containing 7, 14, 28, 49, 56 or 98 tablets or in multipacks 
containing 140 (10x14) tablets. Not all pack sizes may be available in your country. 
 
Marketing Authorisation Holder 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
Tel: +352 26 37 58 78 
 
 



45 

Manufacturer 
Norgine B. V., 
Antonio vivaldistraat 150, 
1083 HP Amsterdam, 
The Netherlands 
 
This leaflet was last revised in 
 
Other sources of information 
Detailed information on this medicine is available on the European Medicines Agency website: 
http://www.ema.europa.eu 
 



46 

Package leaflet: information for the user 
 

Emselex 15 mg prolonged-release tablets 
Darifenacin 

 
Read all of this leaflet carefully before you start taking this medicine because it contains 
important information for you. 
- Keep this leaflet. You may need to read it again. 
- If you have any further questions, ask your doctor or pharmacist. 
- This medicine has been prescribed for you. Do not pass it on to others. It may harm them, even 

if their symptoms are the same as yours. 
If you get any side effects, talk your doctor or pharmacist. This includes any possible side effects not 
listed in this leaflet. See section 4. 
 
What is in this leaflet 
1. What Emselex is and what it is used for 
2. What you need to know before you take Emselex 
3. How to take Emselex 
4. Possible side effects 
5. How to store Emselex 
6. Contents of the pack and other information 
 
 
1. What Emselex is and what it is used for 
 
How Emselex works 
Emselex reduces the activity of an overactive bladder. This enables you to wait longer before you go 
to the toilet and it increases the amount of urine that your bladder can hold. 
 
What Emselex can be used for 
Emselex belongs to a class of medicines which relax the muscles of the bladder. It is used in adults for 
the treatment of the symptoms of overactive bladder conditions - such as a sudden urge to rush to the 
toilet, needing to go to the toilet frequently and/or not getting to the toilet in time and wetting yourself 
(urge incontinence). 
 
 
2. What you need to know before you use Emselex 
 
Do not take Emselex: 
 if you are allergic to darifenacin or any of the other ingredients of this medicine (listed in 

section 6). 
 if you suffer from urinary retention (inability to empty your bladder). 
 if you have gastric retention (problems emptying the contents of the stomach). 
 if you suffer from uncontrolled narrow-angle glaucoma (high pressure in the eyes with loss of 

eyesight that is not being adequately treated). 
 if you have myasthenia gravis (a disease marked by abnormal tiredness and weakness of 

selected muscles). 
 if you have severe ulcerative colitis or toxic megacolon (acute dilation of the colon due to 

complication of infection or inflammation). 
 if you have severe liver problems. 
 There are some medicines such as ciclosporin (a medicine used in transplantation to prevent 

organ rejection or for other conditions, e.g. rheumatoid arthritis or atopic dermatitis), verapamil 
(a medicine used to lower blood pressure, to correct heart rhythm or to treat angina pectoris), 
antifungal medicines (e.g. ketoconazole and itraconazole) and some antiviral medicines (e.g. 
ritonavir) that must not be taken with Emselex. 

 
Warnings and precautions: 



47 

Talk to your doctor before taking Emselex 
 if you have autonomic neuropathy (damage to the nerves that communicate between the brain 

and internal organs, muscles, skin, and blood vessels to regulate vital functions, including the 
heart rate, blood pressure and bowel function) – your doctor will have told you if you have this. 

 if you have heartburn and belching. 
 if you have difficulties in passing urine and a weak stream of urine. 
 if you have severe constipation (less than or equal to 2 bowel movements per week). 
 if you have a digestive motility disorder. 
 if you have an obstructive gastrointestinal disorder (any obstruction of the passage of intestinal 

or gastric contents, such as narrowing of the pylorus, the lower part of the stomach) – your 
doctor will have told you if you have this. 

 if you are taking medicinal products that can cause or worsen inflammation of the oesophagus 
such as oral bisphosphonates (a class of medicinal products that prevent the loss of bone mass 
and are used to treat osteoporosis). 

 if you are receiving treatment for narrow-angle glaucoma. 
 if you have liver problems. 
 if you have kidney problems. 
 if you have heart diseases. 
If any of these apply to you, tell your doctor before you take Emselex. 
 
During treatment with Emselex, tell your doctor straight away and stop taking Emselex if you 
experience swelling of the face, lips, tongue and/or throat (signs of angioedema). 
 
Children and adolescents 
Emselex is not recommended for use in children and adolescents (<18 years). 
 
Other medicines and Emselex 
Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines, 
including medicines obtained without a prescription. This is particularly important if you are taking 
any of the following as your doctor may need to adjust your dose of Emselex and/or the other 
medicine: 
 certain antibiotics (e.g. erythromycin, clarithromycin and rifampicin), 
 antifungal medicines (e.g. ketoconazole and itraconazole), 
 antiviral medicines (e.g. nelfinavir and ritonavir), 
 antipsychotic medicines (e.g. thioridazine), 
 certain antidepressants (e.g. imipramine), 
 certain anticonvulsants (carbamazepine, barbiturates), 
 certain medicines used to treat heart problems (e.g. flecainide, verapamil and digoxin), 
 other antimuscarinic medicines (e.g. tolterodine, oxybutynin and flavoxate). 
Please also inform your doctor if you are taking products containing St John’s wort. 
 
Emselex with food and drink 
Eating food has no effect on Emselex. Grapefruit juice may interact with Emselex. However, the 
adjustment of Emselex doses is not necessary. 
 
Pregnancy and breast-feeding 
If you are pregnant or breast-feeding, think you may be pregnant, or are planning to have a baby, ask 
your doctor for advice before taking this medicine. 
Emselex is not recommended during pregnancy. 
 
 
Emselex should be taken with caution while breast-feeding. 
 
Driving and using machines 
Emselex may cause effects such as dizziness, blurred vision, trouble sleeping or drowsiness. If you 
have any of these symptoms whilst taking Emselex, consult your doctor for advice on changing the 



48 

dose or considering an alternative treatment. You should not drive or use machines if you are affected 
by these symptoms. For Emselex, these side effects have been reported to be uncommon (see 
section 4). 
 
 
3. How to take Emselex 
 
Always take Emselex exactly as your doctor has told you. You should check with your doctor or 
pharmacist if you are not sure. If you have the impression that the effect of Emselex is too strong or 
too weak, talk to your doctor or pharmacist. 
 
How much Emselex to take 
The recommended starting dose, including for patients aged over 65 years, is 7.5 mg daily. Depending 
on your response to Emselex, your doctor may increase your dose to 15 mg daily, two weeks after 
starting therapy. 
 
These doses are suitable for people with mild liver problems or people with kidney problems. 
 
Take Emselex tablets once a day with water, at about the same time each day. 
 
The tablet may be taken with or without food. Swallow the tablet whole. Do not chew, split or crush it. 
 
How long to take Emselex 
Your doctor will tell you how long your treatment with Emselex will last. Do not stop treatment early 
because you do not see an immediate effect. Your bladder will need some time to adapt. Finish the 
course of treatment prescribed by your doctor. If you have not noticed any effect by then, discuss it 
with your doctor. 
 
If you take more Emselex than you should 
If you have taken more tablets than you have been told to take, or if someone else accidentally takes 
your tablets, go to your doctor or hospital for advice immediately. When seeking medical advice, 
make sure that you take this leaflet and your remaining tablets with you to show them to the doctor. 
People who have taken an overdose may have dry mouth, constipation, headache, indigestion and 
nasal dryness. Overdose with Emselex may lead to severe symptoms requiring emergency treatment in 
hospital. 
 
If you forget to take Emselex 
If you forget to take Emselex at the usual time, take it as soon as you remember, unless it is the time 
for your next dose. Do not take a double dose to make up for a forgotten dose. 
 
If you stop taking Emselex 
It has been shown that taking all doses at the appropriate times can greatly increase the effectiveness 
of your medicine. Therefore, it is important to keep taking Emselex correctly, as described above. Do 
not stop taking Emselex until your doctor tells you to. You should not experience any effects when 
you stop treatment. 
 
If you have any further questions on the use of this product, ask your doctor or pharmacist. 
 
4. Possible side effects 
 
Like all medicines, this medicine can cause side effects, although not everybody gets them. The side 
effects caused by Emselex are usually mild and temporary. 
 
Some side effects could be serious 
Serious allergic reactions including swelling, mainly of the face and throat. 
 
Other side effects 



49 

Very common (may affect more than 1 in 10 people) 
Dry mouth, constipation. 
 
Common (may affect up to 1 in 10 people) 
Headache, abdominal pain, indigestion, feeling sick, dry eyes, nasal dryness. 
 
Uncommon (may affect up to 1 in 100 people) 
Fatigue, accidental injury, facial swelling, high blood pressure, diarrhoea, flatulence, inflammation of 
the mucous membrane of the mouth, increased liver enzymes, swelling, dizziness, sleeplessness, 
drowsiness, abnormal thinking, runny nose (rhinitis), cough, shortness of breath, dry skin, itching, 
rash, sweating, visual disturbance including blurred vision, taste disturbance, urinary tract disorder or 
infection, impotence, discharge and itching in the vagina, bladder pain, inability to empty your 
bladder. 
 
Not known (frequency cannot be estimated from the available data) 
Depressed mood/mood alterations, hallucination. 
 
Reporting of side effects 
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects 
not listed in this leaflet. You can also report side effects directly via the national reporting system 
listed in Appendix V. By reporting side effects you can help provide more information on the safety of 
this medicine. 
 
 
5. How to store Emselex 
 
 Keep this medicine out of the sight and reach of children. 
 Do not use this medicine after the expiry date which is stated on the carton and blister. The 

expiry date refers to the last day of that month. 
 Keep the blister packs in the outer carton in order to protect from light. 
 Do not use if the pack is damaged or shows signs of tampering. 
 Do not throw away any medicines via wastewater or household waste. Ask your pharmacist 

how to throw away medicines you no longer use. These measures will help protect the 
environment. 

 
6. Contents of the pack and other information 
 
What Emselex contains 
- The active substance is darifenacin. Each tablet contains 15 mg darifenacin (as hydrobromide). 
- The other ingredients are calcium hydrogen phosphate (anhydrous), hypromellose, magnesium 

stearate, polyethylene glycol, talc, titanium dioxide (E171), red iron oxide (E172) and yellow 
iron oxide (E172). 

 
What Emselex looks like and contents of the pack 
Emselex 15 mg prolonged-release tablets are round, convex light peach tablets and are debossed with 
“DF” on one side and “15” on the other. 
 
The tablets are available in blister packs containing 7, 14, 28, 49, 56 or 98 tablets or in multipacks 
containing 140 (10x14) tablets. Not all pack sizes may be available in your country. 
 
Marketing Authorisation Holder 
Merus Labs Luxco II S.à R.L. 
26-28, rue Edward Steichen 
L-2540 Luxembourg 
Tel: +352 26 37 58 78 
 



50 

Manufacturer 
Norgine B. V., 
Antonio vivaldistraat 150, 
1083 HP Amsterdam, 
The Netherlands  
 
This leaflet was last revised in  
 
Other sources of information 
Detailed information on this medicine is available on the European Medicines Agency website: 
http://www.ema.europa.eu 
 


	SUMMARY OF PRODUCT CHARACTERISTICS
	A. MANUFACTURER RESPONSIBLE FOR BATCH RELEASE
	B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE
	C. OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING AUTHORISATION
	D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND EFFECTIVE USE OF THE MEDICINAL PRODUCT
	A. LABELLING
	B. PACKAGE LEAFLET