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BACLOFEN 5 MG/5 ML ORAL SOLUTION

Active substance(s): BACLOFEN / BACLOFEN / BACLOFEN

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SUMMARY OF PRODUCT CHARACTERISTICS
1

NAME OF THE MEDICINAL PRODUCT
Baclofen 5 mg/5 mL Oral Solution

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 5 ml of oral solution contains 5 mg Baclofen.
For a full list of excipients, see section 6.1.

3

PHARMACEUTICAL FORM
Oral Solution
Clear, very slightly yellow solution.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Baclofen 5 mg/5 mL Oral Solution is indicated for the relief of spasticity of
voluntary muscle resulting from such disorders as: multiple sclerosis, other
spinal lesions, e.g. tumours of the spinal cord, syringomyelia, motor neurone
disease, transverse myelitis, traumatic partial section of the cord.
Baclofen 5 mg/5 mL Oral Solution is also indicated in adults and children for
the relief of spasticity of voluntary muscle arising from e.g. cerebrovascular
accidents, cerebral palsy, meningitis, traumatic head injury.
Patient selection is important when initiating Baclofen 5 mg/5 mL Oral
Solution therapy; it is likely to be of most benefit in patients whose spasticity
constitutes a handicap to activities and/or physiotherapy. Treatment should not
be commenced until the spastic state has become stabilised.
Paediatric population
Baclofen 5 mg/5 mL Oral Solution is indicated in patients 0 to <18 years for
the symptomatic treatment of spasticity of cerebral origin, especially where
due to infantile cerebral palsy, as well as following cerebrovascular accidents
or in the presence of neoplastic or degenerative brain disease.
Baclofen 5 mg/5 mL Oral Solution is also indicated for the symptomatic
treatment of muscle spasms occurring in spinal cord diseases of infectious,
degenerative, traumatic, neoplastic, or unknown origin such as multiple
sclerosis, spastic spinal paralysis, amyotrophic lateral sclerosis, syringomyelia,
transverse myelitis, traumatic paraplegia or paraparesis, and compression of
the spinal cord.

4.2

Posology and method of administration
Baclofen 5mg/5mL Oral Solution is given orally in liquid form. The liquid
may be particularly suitable for children or those adults who are unable to take
tablets. Dosage titration can be more precisely managed with the liquid. The
lowest dose compatible with an optimal response is recommended.
Before starting treatment with Baclofen 5 mg/5 mL Oral Solution it is prudent
to realistically assess the overall extent of clinical improvement that the patient
may be expected to achieve. Careful titration of dosage is essential
(particularly in the elderly) until the patient is stabilised. If too high a dose is
initiated or if the dosage is increased too rapidly side effects may occur. This
is particularly relevant if the patient is ambulant in order to minimise muscle
weakness in the unaffected limbs or where spasticity is necessary for support.
Once the maximum recommended dose has been reached, if the therapeutic
effect is not apparent within 6 weeks a decision whether to continue with
Baclofen 5 mg/5 mL Oral Solution should be taken.
Discontinuation of the treatment should always be gradual by successively
reducing the dosage over a period of approximately 1 to 2 weeks, except in
overdose-related emergencies, or where serious adverse effects have occurred
(see section 4.4).
Adults:
Treatment should be started with a dosage of 15 mg daily, preferably in
divided doses. The following gradually increasing dosage regimen is
suggested, but should be adjusted to suit individual patient requirements.
5 mg three times a day for three days
10 mg three times a day for three days
15 mg three times a day for three days
20 mg three times a day for three days
Satisfactory control of symptoms is usually obtained with doses of up to 60
mg daily, but a careful adjustment is often necessary to meet the requirements
of each individual patient.
The dose may be increased slowly if required, but a maximum daily dose of
more than 100 mg is not advised unless the patient is in hospital under careful
medical supervision. Small frequent dosage may prove better in some cases
than larger spaced doses.
Also some patients benefit from the use of Baclofen 5 mg/5 mL Oral Solution
only at night to counteract painful flexor spasm. Similarly a single dose given
approximately 1 hour prior to performance of specific tasks such as washing,
dressing, shaving, physiotherapy, will often improve mobility.
Special populations
Elderly patients (aged 65 years or above):
Elderly patients may be more susceptible to side effects, particularly in the
early stages of introducing Baclofen 5 mg/5 mL Oral Solution. Small doses

should therefore be used at the start of treatment, the dose being titrated
gradually against the response, under careful supervision. There is no evidence
that the eventual average maximum dose differs from that in younger patients.
Paediatric population (0 to < 18 years):
Treatment should usually be started with a very low dose (corresponding to
approximately 0.3 mg/kg a day), in 2-4 divided doses, preferably in 4 divided
doses.
The dosage should be cautiously raised at about 1 week intervals, until it
becomes sufficient for the child's individual requirements. The usual daily
dosage for maintenance therapy ranges between 0.75 and 2mg/kg body
weight. The total daily dose should not exceed a maximum of 40mg/day in
children below 8 years of age. In children over 8 years of age, a maximum
daily dosage of 60mg/day may be given.
Patients with impaired renal function:
In patients with impaired renal function or undergoing chronic haemodialysis,
a particularly low dosage of Baclofen 5 mg/5 mL Oral Solution should be
selected i.e. approx. 5 mg daily.
Baclofen 5mg/5mL Oral Solution should be administered to end stage renal
failure patients only if the expected benefit outweighs the potential risk. These
patients should be closely monitored for prompt diagnosis of early signs
and/or symptoms of toxicity (e.g. somnolence, lethargy) (see section 4.4 and
section 4.9).
Patients with hepatic impairment:
No studies have been performed in patients with hepatic impairment receiving
Baclofen 5mg/5mL Oral Solution therapy. The liver does not play a significant
role in the metabolism of baclofen after oral administration of Baclofen
5mg/5mL Oral Solution (see section 5.2). However, Baclofen 5mg/5mL Oral
Solution has the potential of elevating liver enzymes. Baclofen 5mg/5mL Oral
Solution should be prescribed with caution in patients with hepatic impairment
Patients with spastic states of cerebral origin:
Unwanted effects are more likely to occur in these patients. It is therefore
recommended that a very cautious dosage schedule be adopted and that
patients be kept under appropriate surveillance.
Method of administration
Baclofen 5mg/5mL Oral Solution should be taken during meals with a little
liquid.
4.3

Contraindications
• Hypersensitivity to baclofen or to any of the excipients listed in section
6.1


Peptic ulceration.

4.4

Special warnings and precautions for use
Psychiatric and nervous system disorders
Psychotic disorders, schizophrenia, depressive or manic disorders, confusional
states or Parkinson's disease may be exacerbated by treatment with Baclofen 5
mg/5 mL Oral Solution. Patients suffering from these conditions should
therefore be treated cautiously and kept under close surveillance.
Epilepsy
Baclofen 5 mg/5 mL Oral Solution may also exacerbate epileptic
manifestations but can be employed provided appropriate supervision and
adequate anticonvulsive therapy are maintained.
Others
Baclofen 5 mg/5 mL Oral Solution should be used with extreme care in
patients already receiving antihypertensive therapy, (see section 4.5).
Baclofen 5 mg/5 mL Oral Solution should be used with caution in patients
suffering from cerebrovascular accidents or from respiratory, hepatic or renal
impairment.
Since unwanted effects are more likely to occur, a cautious dosage schedule
should be adopted in elderly and patients with spasticity of cerebral origin (see
section 4.2).
Renal impairment
Signs of overdose have been observed in patients with renal impairment taking
oral baclofen at doses of more than 5 mg per day. Baclofen 5 mg/5 mL Oral
Solution should be used with caution in patients with renal insufficiency and
should only be administered to patients with end-stage renal failure (CKD
stage 5, GFR < 15mL/min) when benefit outweighs risk (see Section 4.2).
Cases of baclofen toxicity have been reported in patients with acute renal
failure (see Section 4.9).
Particular caution is required when combining Baclofen 5 mg/5 mL Oral
Solution to drugs or medicinal products that can significantly affect renal
function. Renal function should be closely monitored and Baclofen 5 mg/5 mL
Oral Solution daily dosage adjusted accordingly to prevent baclofen toxicity.
Besides discontinuing treatment, unscheduled haemodialysis might be
considered as a treatment alternative in patients with severe baclofen toxicity.
Haemodialysis effectively removes baclofen from the body, alleviates clinical
symptoms of overdose and shortens the recovery time in these patients.
Urinary disorders
Under treatment with Baclofen 5 mg/5 mL Oral Solution neurogenic
disturbances affecting emptying of the bladder may show an improvement. In
patients with preexisting sphincter hypertonia, acute retention of urine may
occur; the drug should be used with caution in such cases.
Laboratory tests
In rare instances elevated aspartate aminotransferase, blood alkaline
phosphatase and blood glucose levels in serum have been recorded.
Appropriate laboratory tests should be performed in patients with liver

diseases or diabetes mellitus in order to ensure that no drug induced changes in
these underlying diseases have occurred.
Excipients
Baclofen 5mg/5mL Oral Solution syrup contains methyl hydroxybenzoate and
propyl hydroxybenzoate, which may cause allergic reactions (possibly
delayed). Baclofen Oral Solution syrup contains sorbitol. Patients with rare
hereditary problems of fructose intolerance should not take this medicine.
Baclofen 5mg/5mL Oral Solution syrup also contains 0.65 to 1.08 mg of
sodium per 1 mL of syrup.
Abrupt withdrawal:
Anxiety and confusional states, hallucinations, psychotic, manic or paranoid
states, convulsions (status epilepticus), dyskinesia, tachycardia, hyperthermia
and as rebound phenomenon temporary aggravation of spasticity have been
reported with abrupt withdrawal of baclofen, especially after long term
medication.
Neonatal convulsions have been reported after intrauterine exposure to oral
Baclofen 5 mg/5 mL Oral Solution (see Section 4.6).
Treatment should always, (unless serious adverse effects occur), therefore be
gradually discontinued by successively reducing the dosage over a period of
about 1-2 weeks.
Paediatric patients
There is very limited clinical data on the use of Baclofen 5 mg/5 mL Oral
Solution in children under the age of one year. Use in this patient population
should be based on the physician's consideration of individual benefit and risk
of therapy.
Posture and balance
Baclofen 5 mg/5 mL Oral Solution should be used with caution when
spasticity is needed to sustain upright posture and balance in locomotion (see
section 4.2).
4.5

Interaction with other medicinal products and other forms of interaction
Levodopa/dopa decarboxylase (DDC) inhibitor (Carbidopa)
In patients with Parkinson's disease receiving treatment with Baclofen 5 mg/5
mL Oral Solution and levodopa (alone or in combination with DDC inhibitor,
carbidopa), there have been reports of mental confusion, hallucinations,
nausea and agitation. Worsening of the symptoms of Parkinsonism has also
been reported. Hence, caution should be exercised during concommitant
administration of Baclofen 5 mg/5 mL Oral Solution and levodopa/carbidopa.
Drugs causing Central Nervous System (CNS) depression
Increased sedation may occur when Baclofen 5 mg/5 mL Oral Solution is
taken concomitantly with other drugs causing CNS depression including other
muscle relaxants (such as tizanidine), with synthetic opiates or with
alcohol(see section 4.7).
The risk of respiratory depression is also increased. In addition, hypotension
has been reported with concomitant use of morphine and intrathecal baclofen.

Careful monitoring of respiratory and cardiovascular functions is essential
especially in patients with cardiopulmonary disease and respiratory muscle
weakness.
Antidepressants
During concomitant treatment with tricyclic antidepressants, the effect of
Baclofen 5 mg/5 mL Oral Solution may be potentiated, resulting in
pronounced muscular hypotonia.
Lithium
Concomitant use of oral Baclofen 5mg/5mL Oral Solution and lithium resulted
in aggravated hyperkinetic symptoms. Thus, caution should be exercised when
Baclofen 5 mg/5 mL Oral Solution is used concomitantly with lithium.
Antihypertensives
Since concomitant treatment with Baclofen 5 mg/5 mL Oral Solution and
antihypertensives is likely to increase the fall in blood pressure, the dosage of
antihypertensive medication should be adjusted accordingly.
Agents reducing renal function
Drugs or medicinal products that can significantly affect renal function may
reduce baclofen excretion leading to toxic effects (see Section 4.4).
4.6

Fertility, pregnancy and lactation
During pregnancy, especially in the first 3 months, Baclofen 5 mg/5 mL Oral
Solution should only be employed if its use is of vital necessity. The benefits
of the treatment for the mother must be carefully weighed against the possible
risks for the child. Baclofen 5 mg/5 mL Oral Solution crosses the placental
barrier.
One case of suspected withdrawal reaction (generalised convulsions) has been
reported in a week-old infant whose mother had taken oral baclofen 80 mg
daily throughout her pregnancy. The convulsions, which were refractory to
standard anticonvulsant treatment, ceased within 30 minutes of giving
baclofen to the infant.
In mothers taking Baclofen 5 mg/5 mL Oral Solution in therapeutic doses, the
active substance passes into the breast milk, but in quantities so small that no
undesirable effects on the infant are to be expected.

4.7

Effects on ability to drive and use machines
Baclofen 5mg/5mL Oral Solution may be associated with adverse effects such
as dizziness, sedation, somnolence and visual disturbances (See section 4.8)
which may impair the patient's reaction. Patients experiencing these adverse
reactions should be advised to refrain from driving or using machines.

4.8

Undesirable effects
Adverse reactions (Table 1) are ranked under heading of frequency, the most
frequent first, 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).
Adverse effects occur mainly at the start of treatment (e.g. sedation,
somnolence and nausea) if the dosage is raised too rapidly, if large doses are
employed, or in elderly patients. They are often transitory and can be
attenuated or eliminated by reducing the dosage; they are seldom severe
enough to necessitate withdrawal of the medication.
Should nausea persist following a reduction in dosage, it is recommended that
Baclofen 5 mg/5 mL Oral Solution be ingested with food or a milk beverage.
In patients with a case history of psychiatric illness or with cerebrovascular
disorders (e.g. stroke) as well as in elderly patients, adverse reactions may
assume a more serious form.
Lowering of the convulsion threshold and convulsions may occur, particularly
in epileptic patients.
Table 1 Tabulated summary of adverse drug reactions
Nervous system disorders
Very common:
Sedation, somnolence
Common:
Respiratory depression, confusional state,
dizziness, hallucination, depression,
fatigue, insomnia, euphoric mood,
muscular weakness, ataxia, tremor,
nightmares, myalgia, headache,
nystagmus, dry mouth.
Rare:
Paraesthesia, dysarthria, dysgeusia
Eye Disorders
Common:
Visual impairment, accommodation
disorder
Cardiac disorders
Common:
Cardiac output decreased
Not known:
Bradycardia
Vascular disorders
Common:
Hypotension
Gastrointestinal disorders
Very common:
Nausea
Common:
Gastrointestinal disorder, constipation ,
diarrhoea, retching, vomiting
Rare:
Abdominal pain
Hepatobiliary disorders
Rare:
Hepatic function abnormal
Skin and subcutaneous tissue disorders
Common:
Rash, hyperhidrosis
Not known
Urticaria
Renal and urinary disorders

Common:
Pollakiuria, enuresis, dysuria
Rare:
Urinary retention
Reproductive system and breast disorders
Rare:
Erectile dysfunction
General disorders and administration site conditions
Very rare
Hypothermia
Not known
Drug withdrawal syndrome (see section
4.4)
Investigations
Not known:
Blood glucose increased
Certain patients have shown increased spasticity as a paradoxical reaction to
the medication.
An undesirable degree of muscular hypotonia - making it more difficult for
patients to walk or fend for themselves - may occur and can usually be
relieved by re-adjusting the dosage (i.e. by reducing the doses given during the
day and possibly increasing the evening dose).
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 Yellow Card Scheme at:
www.mhra.gov.uk/yellowcard.
4.9

Overdose
Symptoms:
Prominent features are signs of central nervous depression: somnolence,
depressed level of consciousness, respiratory depression, coma. Also liable to
occur are: confusion, hallucination, agitation, accommodation disorder,
impaired pupillary reflex; generalised muscular hypotonia, myoclonus,
hyporeflexia or areflexia; convulsion, abnormal electroencephalogram (burst
suppression pattern and triphasic waves); peripheral vasodilatation,
hypotension or hypertension, bradycardia, tachycardia or cardiac arrhythmia;
hypothermia; nausea, vomiting, diarrhoea, salivary hypersecretion; increased
hepatic enzymes. Patients with renal impairment can develop signs of
overdose even on low doses of oral Baclofen 5 mg/5 mL Oral Solution (see
section 4.2 and section 4.4)
A deterioration in the condition may occur if various substances or drugs
acting on the central nervous system (e.g. alcohol, diazepam, tricyclic
antidepressants) have been taken at the same time.
Treatment:
No specific antidote is known.
Supportive measures and symptomatic treatment should be given for
complications such as hypotension, hypertension, convulsions, respiratory or
cardiovascular depression.

Since the drug is excreted chiefly via the kidneys, generous quantities of fluid
should be given, possibly together with a diuretic. Haemodialysis (sometimes
unscheduled) may be useful in severe poisoning associated with renal failure
(see Section 4.4).

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Pharmacotherapeutic group: Antispastic with spinal site attack, ATC code:
M03B X01
Baclofen is an antispastic agent acting at the spinal level. A gammaaminobutyric acid (GABA) derivative, baclofen is chemically unrelated to
other antispastic agents.
Baclofen depresses monosynaptic and polysynaptic reflex transmission,
probably by stimulating the GABAB receptors, this stimulation in turn
inhibiting the release of the excitatory amino acids glutamate and aspartate.
Neuromuscular transmission is unaffected by baclofen.
The major benefits of baclofen stem from its ability to reduce painful flexor
spasms and spontaneous clonus thereby facilitating the mobility of the patient,
increasing independence and helping rehabilitation.
Baclofen also exerts an antinociceptive effect. General well being is often
improved and sedation is less often a problem than with centrally acting drugs.
Baclofen stimulates gastric acid secretion.

5.2

Pharmacokinetic properties
Absorption:
Baclofen is rapidly and completely absorbed from the gastro-intestinal tract.
No significant difference between the solution and tablet formulations is
observed in respect of tmax, cmax and bioavailability. Following oral
administration of single doses (10-30mg) peak plasma concentrations are
recorded after 0.5 to 1.5 hours and areas under the serum concentration curves
are proportional to the dose.
Distribution:
The volume of distribution of baclofen is 0.7 l/kg and the protein binding rate
is approximately 30%. In cerebrospinal fluid active substance concentrations
are approximately 8.5 times lower than in the plasma.
Biotransformation:
Baclofen is metabolised to only a minor extent. Deamination yields the main
metabolite, β-(p-chlorophenyl)-4-hydroxybutyric acid, which is
pharmacologically inactive.

Elimination/excretion:
The plasma elimination half-life of baclofen averages 3 to 4 hours. The serum
protein binding rate is approximately 30%.
Baclofen is eliminated largely in unchanged form. Within 72 hours, about 75%
of the dose is excreted via the kidneys with about 5% of this amount as
metabolites.
Special populations
Elderly patients (aged 65 years or above)
The pharmacokinetics of baclofen in elderly patients are virtually the same as
in patients below 65 years of age. Following a single oral dose, elderly patients
have slower elimination but a similar systemic exposure of baclofen compared
to adults below 65 years of age. Extrapolation of these results to multi-dose
treatment suggests no significant pharmacokinetic difference between patients
below 65 years of age and elderly patients.
Paediatric patients
Following oral administration of 2.5mg Baclofen tablet in children (aged 2 to12
years), Cmax of 62.8±28.7 nanogram/mL, and Tmax in the range of 0.95-2 h have been
reported. Mean plasma clearance (Cl) of 315.9mL/h/kg; volume of distribution (Vd)
of 2.58 L/kg; and half-life (T1⁄2) of 5.10 h have been reported.

Hepatic impairment
No pharmacokinetic data are available in patients with hepatic impairment after
administration of Baclofen 5 mg/5 mL Oral Solution. However, as the liver does not
play a significant role in the disposition of baclofen, it is unlikely that baclofen
pharmacokinetics would be altered to a clinically significant level in patients with
hepatic impairment.
Renal impairment
No controlled clinical pharmacokinetic study is available in patients with renal
impairment after administration of Baclofen 5 mg/5 mL Oral Solution. Baclofen is
predominantly eliminated unchanged in urine. Sparse plasma concentration data
collected only in female patients under chronic hemodialysis or compensated renal
failure indicate significantly decreased clearance and increased half-life of baclofen in
these patients. Dosage adjustment of baclofen based on its systemic levels should be
considered in renal impairment patients, and prompt hemodialysis is an effective
means of reversing excess baclofen in systemic circulation.

5.3

Preclinical safety data
Baclofen increases the incidence of omphaloceles (ventral hernias) in the
foetuses of rats given approximately 13 times the maximum oral dose (on a
mg/kg basis) recommended for human use. This was not seen in mice or
rabbits.

An apparently dose related increase in the incidence of ovarian cysts, and a
less marked increase in enlarged and/or haemorrhagic adrenals have been
observed in female rats treated for 2 years. The clinical relevance of these
findings is not known.
Experimental evidence to date suggests that baclofen does not possess either
carcinogenic or mutagenic properties.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Liquid Sorbitol (Non-Crystallising) (E420)
Methyl Paraben (E218)
Propyl Paraben (E216)
Flavour raspberry
Carmellose Sodium (E466)
Purified Water

6.2

Incompatibilities
Not Applicable

6.3

Shelf life
Unopened bottles: 2 years
Opened bottles: 60 days

6.4

Special precautions for storage
This medicinal product does not require any special storage conditions.
See section 6.3 for details of shelf life once opened. Protect from light. Do not
refrigerate.

6.5

Nature and contents of container
Clear, very slightly yellow solution with a raspberry flavour
Type III Amber Glass bottles of 300ml with child resistant polypropylene
closures containing tamper evident ring.

6.6

Special precautions for disposal
No special requirements.

7

MARKETING AUTHORISATION HOLDER
Strides Arcolab International Limited
Unit 4, Metro Centre,
Tolpits Lane,
Watford, Hertfordshire
WD 189 SS
United Kingdom

8

MARKETING AUTHORISATION NUMBER(S)
PL 28176/0162

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
01/05/2015

10

DATE OF REVISION OF THE TEXT
01/05/2015

Expand Transcript

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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