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OXYBUTYNIN HYDROCHLORIDE 5MG/5ML ORAL SOLUTION

Active substance(s): OXYBUTYNIN HYDROCHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS
1

NAME OF THE MEDICINAL PRODUCT
Oxybutynin hydrochloride 5mg/5ml Oral Solution

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 5ml solution contains 5mg oxybutynin hydrochloride.
Excipients with known effect: Each 5ml of solution contains 1.3gm liquid
sorbitol (non-crystallising) (E420) and 6.0mg methyl parahydroxybenzoate
(E218).
For the full list of excipients, see section 6.1

3

PHARMACEUTICAL FORM
Oral solution
Clear, colourless solution with raspberry odour

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Urinary incontinence, urgency and frequency in the unstable bladder, whether
due to neurogenic bladder disorders (detrusor hyperreflexia) in conditions such
as multiple sclerosis and spina bifida, or to idiopathic detrusor instability
(motor urge incontinence).

Paediatric population
Oxybutynin hydrochloride is indicated in children over 5 years of age for:

4.2

-

Urinary incontinence, urgency and frequency in unstable bladder
conditions due to idiopathic overactive bladder or neurogenic bladder
disorders (detrusor overactivity).

-

Nocturnal enuresis associated with detrusor overactivity, in conjunction
with non-drug therapy, when other treatment has failed.

Posology and method of administration
Adults:

The usual dose is 5mg (5ml) two or three times a day. This may be increased
to a maximum of 5mg (5ml) four times a day to obtain a clinical response
provided that the side effects are tolerated.
Elderly (including frail elderly):
The elimination half-life is increased in the elderly. Therefore, a dose of 2.5mg
(2.5ml) twice a day, particularly if the patient is frail, is likely to be adequate.
This dose may be titrated upwards to 5mg (5ml) twice a day to obtain a
clinical response provided that the side effects are tolerated.
Children (under 5 years of age):

Not recommended
Children (over 5 years of age):

Neurogenic bladder instability:
The usual dose is 2.5mg (2.5ml) twice a day. This dose may be titrated upwards to
5mg (5ml) two or three times a day to obtain a clinical response provided that the side
effects are tolerated.
Nocturnal enuresis:
The usual dose is 2.5mg (2.5ml) twice a day. This dose may be titrated upwards to
5mg (5ml) two or three times a day to obtain a clinical response provided that the side
effects are tolerated. The last dose should be given before bedtime.

Method of administration

For oral administration.
Measure the prescribed dose with the 2.5-5ml double ended spoon provided in
the pack.

4.3

Contraindications
-

4.4

Hypersensitivity to oxybutynin or to any of the excipients listed in section
6.1
Myasthenia gravis.
Narrow-angle glaucoma or shallow anterior chamber.
Gastrointestinal obstruction including paralytic ileus, intestinal atony.
Patients with toxic megacolon, severe ulcerative colitis.
Patients with bladder outflow obstruction where urinary retention may be
precipitated.

Special warnings and precautions for use
Oxybutynin should be used with caution in the frail elderly and in children
who may be more sensitive to the effects of the product and in patients with
autonomic neuropathy (such as those with Parkinson’s disease), hepatic or
renal impairment and severe gastro-intestinal motility disorders (also see
section 4.3).
Anticholinergics should be used with caution in elderly patients due to the risk
of cognitive impairment.
Gastrointestinal disorders: Anticholinergic medicinal products may decrease
gastrointestinal motility and should be used with caution in patients with
gastrointestinal obstructive disorders, intestinal atony and ulcerative colitis.
Oxybutynin may aggravate tachycardia (and thus hyperthyroidism, congestive
heart failure, coronary heart disease, cardiac arrhythmias, hypertension),
cognitive disorders and symptoms of prostatic hypertrophy.
Anticholinergic CNS effects (e.g. hallucinations, agitation, confusion,
somnolence) have been reported; monitoring recommended especially in first
few months after initiating therapy or increasing the dose; consider

discontinuing therapy or reducing the dose if anticholinergic CNS effects
develop.
Since oxybutynin can cause narrow-angle glaucoma, patients should be
advised to contact a physician immediately if they are aware of a sudden loss
of visual acuity or ocular pain.
Oxybutynin may reduce salivary secretions which could result in dental caries,
parodontosis or oral candidiasis.
Anticholinergic medicinal products should be used with caution in patients
who have hiatus hernia/gastro-oesophageal reflux and/or who are concurrently
taking medicinal products (such as bisphosphonates) that can cause or
exacerbate esophagitis.
When oxybutynin is used in high environmental temperatures, this can cause
heat prostration due to decreased sweating.
Paediatric population
Oxybutynin hydrochloride is not recommended for use in children below age 5
years due to insufficient data on safety and efficacy.
There is limited evidence supporting the use of Oxybutynin in children with
monosymptomatic nocturnal enuresis (not related to detrusor overactivity).
In children over 5 years of age, Oxybutynin hydrochloride should be used with
caution as they may be more sensitive to the effects of the product, particularly
the CNS and psychiatric adverse reactions.
Excipient Warnings
This product contains:
Methyl parahydroxybenzoate (E218): This may cause allergic reactions
(possibly delayed).
Liquid sorbitol (non-crystallising) (E420): Patients with rare hereditary
problems of fructose intolerance should not take this medicine.

4.5

Interaction with other medicinal products and other forms of interaction
Care should be taken if other anticholinergic agents are administered together
with Oxybutynin, as a potentiation of anticholinergic effects could occur.

The anticholinergic activity of oxybutynin is increased by concurrent use of
other anticholinergics or medicinal products with anticholinergic activity, such
as amantadine and other anticholinergic antiparkinsonian medicinal products
(e.g. biperiden, levodopa), antihistamines, antipsychotics (e.g. phenothiazines,
butyrophenones, clozapine), quinidine, digitalis, tricyclic antidepressants,
atropine and related compounds like atropinic antispasmodics and
dipyridamole.
By reducing gastric motility, oxybutynin may affect the absorption of other
drugs.
Oxybutynin is metabolised by cytochrome P450 isoenzyme CYP 3A4.
Concomitant administration with a CYP3A4 inhibitor can inhibit oxybutynin
metabolism and increase oxybutynin exposure.
Oxybutynin may antagonise prokinetic therapies.
Concomitant use with cholinesterase inhibitors may result in reduced
cholinesterase inhibitor efficacy.
Patients should be informed that alcohol may enhance the drowsiness caused
by anticholinergic agents such as oxybutynin (see section 4.7).

4.6

Fertility, pregnancy and lactation
Pregnancy
There are no adequate data from the use of Oxybutynin hydrochloride in
pregnant women. Animal studies are insufficient with respect to effects on
pregnancy, embryonic/foetal development, parturition or postnatal
development. The potential risk for humans is unknown. Oxybutynin should
not be used during pregnancy unless clearly necessary.
Breast-feeding
When oxybutynin is used during lactation, a small amount is excreted in the
mother's milk. Use of oxybutynin during breast feeding is therefore not
recommended.

4.7

Effects on ability to drive and use machines

As Oxybutynin hydrochloride oral solution may produce drowsiness or blurred
vision, the patient should be cautioned regarding activities requiring mental
alertness such as driving, operating machinery or performing hazardous work
while taking this drug.

4.8

Undesirable effects
Adverse effects have been listed under headings of body systems and their
frequencies as follows, where possible: very common (≥ 1 / 10), common (≥ 1
/ 100 to <1 / 10), uncommon (≥ 1 /1000 to <1 / 100), rare (≥ 1 / 10, 000 to <1 /
1000), very rare (<1/10,000), not known (cannot be estimated from the
available data).
Table 1: Adverse effects and their frequencies:
Body
systems

Very
common
(≥1/10)
-

Common
(≥1/100 to
<1/10)
-

Uncommon
(≥ 1 /1000
to <1 / 100)
-

constipation,
nausea, dry
mouth

diarrhoea,
vomiting

abdominal
discomfort,
anorexia,
decreased
appetite,
dysphagia

gastroesophageal
reflux disease

Psychiatric
disorders

-

confusional
state

-

Nervous
system
disorders
Cardiac
disorders
Injury,
poisoning
and
procedural
complications
Eye disorders

dizziness,
headache,
somnolence
-

-

-

-

-

-

-

-

agitation,
anxiety,
hallucinations,
nightmares,
paranoia,
cognitive
disorders in
elderly
cognitive
disorders,
convulsions
tachycardia,
arrhythmia
heat stroke

-

dry eyes

-

Angle closure

Infections
and
infestations
Gastro intestinal
disorders

Not known

urinary tract
infection

Renal and
urinary
disorders

-

urinary
retention

-

glaucoma,
mydriasis, ocular
hypertension,
vision blurred
-

Vascular
disorders
Skin and
subcutaneous
tissue
disorders
Immune
system
disorders

-

flushing

-

-

dry skin

-

-

angioedema,
rash, urticaria,
hypohidrosis

-

-

-

hypersensitivity

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:
Yellow Card Scheme
Website: www.mhra.gov.uk/yellowcard

4.9

Overdose
The symptoms of overdose with oxybutynin progress from an intensification
of the usual side effects of CNS disturbances (from restlessness and
excitement to psychotic behaviour), circulation changes (flushing, fall in blood
pressure, circulatory failure etc), respiratory failure, paralysis and coma.
Measures to be taken are:
1) Immediate gastric lavage
2) physostigmine by slow intravenous injection

Adults: 0.5 to 2.0mg of physostigmine by slow intravenous administration.
Repeat after 5 minutes, if necessary up to a maximum total dose of 5mg.
Children: 30micrograms/kg of physostigmine by slow intravenous
administration. Repeat after 5 minutes, if necessary up to a maximum total
dose of 2mg.

Fever should be treated symptomatically with tepid sponging or ice packs.

In pronounced restlessness or excitation, diazepam 10mg may be given by
intravenous injection, tachycardia may be treated by intravenous injection of
propranolol and urinary retention can be managed by catheterisation.
In the event of progression of the curare- like effect to the paralysis of the
respiratory muscles, mechanical ventilation will be required.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties

Pharmacotherapeutic group: anticholinergic as well as antispasmodic, ATC Code:
G04B D04

Oxybutynin has both direct antispasmodic action on the smooth muscle of the
bladder detrusor muscle as well as an anticholinergic action in blocking the
muscarinic effects of acetylcholine on smooth muscle. These properties cause
relaxation of the detrusor muscle of the bladder in patients with an unstable
bladder. Oxybutynin increases bladder capacity and reduces the incidence of
spontaneous contractions of the detrusor muscle.

5.2

Pharmacokinetic properties
Absorption
Oxybutynin is rapidly absorbed from the gastrointestinal tract following oral
administration with maximum plasma concentrations reached in less than 1
hour. First-passage effect is high and less than 10% of the administered dose
reaches the circulation unchanged.
Distribution
Oxybutynin is widely distributed in body tissues following systemic
absorption. The volume of distribution was estimated to be 193 l after
intravenous administration of 5mg oxybutynin hydrochloride.
Metabolism

Oxybutynin is extensively metabolised by the liver, primarily by the
cytochrome P450 enzyme system, particularly CYP 3A4 found mostly in the
liver and gut wall. Metabolites include phenylcyclohexylglycolic acid, which
is pharmacologically inactive, and N-desethyloxybutynin, which is
pharmacologically active.

Excretion
Oxybutynin is extensively metabolised in the liver, see above, with less than
0.1% of the administered dose excreted unchanged in the urine. Also, less than
0.1% of the administered dose is excreted as the metabolite Ndesethyloxybutynin.
Elderly
Bioavailability is higher in elderly patients; AUC is 2-4-fold higher after
repeated administration and half-life 3-5 times longer (see section 4.2).

5.3

Preclinical safety data
No data of therapeutic relevance.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Citric acid monohydrate (E330)
Sodium citrate (E331)
Liquid sorbitol (non-crystallising) (E420)
Glycerol (E422)
Methyl parahydroxybenzoate (E218)
Raspberry flavour (containing propylene glycol (E1520))
Purified water

6.2

Incompatibilities

In the absence of compatibility studies, this medicinal product must not be
mixed with other medicinal products.

6.3

Shelf life
24 months.
Discard after 30 days of first opening. Store in the original packaging after first
opening.

6.4

Special precautions for storage
Do not store above 25°C.
For storage conditions after first opening of the medicinal product, see section
6.3.

6.5

Nature and contents of container
Bottle: Ph. Eur Type III Amber glass
Closure: Tamper evident, child resistant, plastic (Polypropylene/
Polyethylene) cap with EPE liner
Pack size: 100ml and 150ml.
Not all pack sizes may be marketed.
Dosing device: Double ended white polypropylene plastic spoon with 2.5ml
and 5ml measuring ends.

6.6

Special precautions for disposal
Any unused medicinal product or waste material should be disposed of in
accordance with local requirements.

7

MARKETING AUTHORISATION HOLDER
Syri Limited, t/a Thame Laboratories,
Unit 4, Bradfield Road,
Ruislip, Middlesex,
HA4 0NU, UK

8

MARKETING AUTHORISATION NUMBER(S)
PL 39307/0023

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
26/03/2015

10

DATE OF REVISION OF THE TEXT
27/09/2017

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