Baclofen 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 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 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 stabilized.
Paediatric population
Baclofen 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 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.

Dosage
Baclofen is given orally in either tablet or liquid form. These two formulations are bioequivalent.
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 it is prudent to realistically assess the overall extent of
the 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 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 regime 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 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 only at night to counteract painful flexor spasm. Similarly a single
dose given approximately 1 hour prior to the 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. Small doses should therefore be used at the start of the 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.
Baclofen tablets are not suitable for use in children below 33 kg body weight.

Patients with renal impairment:
In patients with impaired renal function or undergoing chronic haemodialysis, a particularly low
dosage of baclofen should be selected i.e. approximately 5 mg daily.
Baclofen 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 sections 4.4 and
4.9).
 

Patients with hepatic impairment:
No studies have been performed in patients with hepatic impairment receiving baclofen
therapy. The liver does not play a significant role in the metabolism of baclofen after oral
administration of baclofen (see section 5.2). However, baclofen has the potential of elevating
liver enzymes. Baclofen 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 cautious dosage schedule be adopted and that patients be kept under appropriate
surveillance.
 

Method of administration
Baclofen should be taken during meals with a little liquid.

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. Patients suffering from
these conditions should therefore be treated cautiously and kept under close surveillance.

Suicide and suicide-related events have been reported in patients treated with baclofen. In
most cases, the patients had additional risk factors associated with an increased risk of suicide
including alcohol use disorder, depression and/or a history of previous suicide attempts. Close
supervision of patients with additional risk factors for suicide should accompany drug therapy.
Patients (and caregivers of patients) should be alerted about the need to monitor for clinical
worsening, suicidal behaviour or thoughts or unusual changes in behaviour and to seek
medical advice immediately if these symptoms present.
Cases of misuse, abuse and dependence have been reported with baclofen. Caution should
be exercised in patients with a history of substance abuse and the patient should be monitored
for symptoms of baclofen misuse, abuse or dependence e.g. dose escalation, drug-seeking
behaviour, development of tolerance.
 

Epilepsy
Baclofen may also exacerbate epileptic manifestations but can be employed provided
appropriate supervision and adequate anticonvulsive therapy are maintained.
 

Others
Baclofen should be used with extreme care in patients already receiving antihypertensive
therapy (see section 4.5).
Baclofen should be used with caution in patients suffering from cerebrovascular accidents or
from respiratory or hepatic 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
Baclofen should be used with caution in patients with renal impairment and should be
administered to end stage renal failure patients only if the expected benefit outweighs the
potential risk (See section 4.2 Posology and method of administration). Neurological signs and
symptoms of overdose including clinical manifestations of toxic encephalopathy (e.g.
confusion, disorientation, somnolence and depressed level of consciousness) have been
observed in patients with renal impairment taking oral baclofen at doses of more than 5mg per
day and at doses of 5mg per day in patients with end stage renal failure being treated with
chronic hemodialysis. Patients with impaired renal function should be closely monitored for
prompt diagnosis of early symptoms of toxicity.
Particular caution is required when combining Baclofen to drugs or medicinal products that
can significantly affect renal function. Renal function should be closely monitored and Baclofen
daily dosage adjusted accordingly to prevent baclofen toxicity.
Cases of baclofen toxicity have been reported in patients with acute renal failure (see section
4.9).

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, neurogenic disturbances affecting emptying of the bladder may
show an improvement. In patients with pre-existing sphincter hypertonia, acute retention of
urine may occur; the drug should be used with caution in such patients.
 

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.
 

Abrupt withdrawal
Treatment should always, (unless serious adverse effects occur), be gradually discontinued
by successively reducing the dosage over a period of about 1-2 weeks. Anxiety and
confusional state, delirium, hallucination, psychotic disorder, mania or paranoia, convulsion
(status epilepticus), dyskinesia, tachycardia, hyperthermia, rhabdomyolysis and temporary
aggravation of spasticity as a rebound phenomenon have been reported with abrupt
withdrawal of baclofen, especially after long term medication.
Neonatal convulsions have been reported after intrauterine exposure to oral baclofen (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.
 

Posture and balance
Baclofen should be used with caution when spasticity is needed to sustain upright posture and
balance in locomotion (see section 4.2).
 

Paediatric patients
There is very limited clinical data on the use of baclofen 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.

Drugs causing Central Nervous System (CNS) depression

Increased sedation may occur when baclofen 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 muscles weakness.
Pre-treatment with baclofen may prolong the duration of fentanyl induced anaesthesia.
 

Lithium
Concomitant use of oral baclofen and lithium resulted in aggravated hyperkinetic symptoms.
Thus, caution should be exercised when baclofen is used concomitantly with lithium.
 

Antidepressants
During concomitant treatment with tricyclic antidepressants, the effect of baclofen may be
potentiated, resulting in pronounced muscular hypotonia.
 

Antihypertensives
Since concomitant treatment with baclofen and anti-hypertensives is likely to increase the fall
in blood pressure, the dosage of anti-hypertensive 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).
 

Levodopa/dopa decarboxylase (DDC) inhibitor (Carbidopa)
In patients with Parkinson's disease receiving treatment with baclofen 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 concomitant administration of
baclofen and levodopa/carbidopa.

Pregnancy
During pregnancy, especially in the first 3 months, baclofen 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 crosses the placental barrier.
 

Foetal/neonatal adverse reactions

Drug withdrawal syndrome including postnatal convulsions in neonates has also been
reported after intra-uterine exposure to oral baclofen (see section 4.4).
 

Breast-feeding
In mothers taking baclofen 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.

Baclofen may be associated with adverse effects such as dizziness, sedation, somnolence
and visual impairment (see section 4.8) which may impair the patient's reaction. Patients
experiencing these adverse reactions should be advised to refrain from driving or operating
machinery.

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 be
ingested with food or a milk beverage.
Lowering of the convulsion threshold and convulsions may occur, particularly in epileptic
patients.
In patients with a 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.
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).
Adverse reactions (Table 1) are ranked under the heading of frequency, the most frequent
first, using the following convention: 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) and
Not known (frequency cannot be estimated from the available data).

*Drug withdrawal syndrome including postnatal convulsions in neonates has also been
reported after intra-uterine exposure to oral baclofen.
* Cases of central sleep apnoea syndrome have been observed with baclofen at high doses
(≥ 100 mg) in patients who are alcohol dependent.

Symptoms: Prominent features are signs of central nervous depression: somnolence,
depressed level of consciousness, respiratory depression, coma. Also liable to occur are:
confusion, hallucinations, agitation, accommodation disorder, impaired pupillary reflex,
generalised muscular hypotonia, myoclonus, hyporeflexia or areflexia, convulsions, abnormal
electroencephalogram (burst suppression pattern and triphasic waves), peripheral
vasodilation, hypotension or hypertension, bradycardia, tachycardia or cardiac arrhythmia,
hypothermia, nausea, vomiting, diarrhoea, salivary hypersecretion, increased hepatic
enzymes, SGOT and AP values, rhabdomyolysis. Patients with renal impairment can develop
signs of overdose even on low doses of oral baclofen (see sections 4.2 and 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, gastrointestinal disorders and 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).

Pharmacotherapeutic group: Antispastic with spinal site attack, ATC code: M03B X01
Baclofen is an antispastic agent acting at the spinal level. A gamma-aminobutyric acid (GABA)
derivative, chemically unrelated to other antispastic agents.
Baclofen depresses monosynaptic and polysynaptic reflex transmission, probably by
stimulating the GABAB-receptors. This stimulation in turn inhibits 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 their
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.

Absorption
Baclofen is rapidly and completely absorbed from the gastrointestinal tract. Following oral
administration of single doses (10-30 mg) 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. The protein binding rate is approximately
30% and is constant in the concentration range of 10 nanogram/ml to 300 microgram/ml. 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-(pchlorophenyl)-
4-hydroxybutyric acid, which is pharmacologically inactive.
Elimination
The plasma elimination half-life of baclofen averages 3 to 4 hours.
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 (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 2.5 mg Baclofen tablet in children (aged 2 to12 years), Cmax
of 62.8±28.7 nanogram/ml, and Tmax in the range of 0.95-2h have been reported. Mean
plasma clearance (Cl) of 315.9 ml/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. 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. 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

Baclofen increases the incidence of omphaloceles (ventral hernias) in the foetuses of rats
given approximately 13 times the maximum oral dose (on 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.

• MICROCRYSTALLINE CELLULOSE AVICEL PH-101
• MICROCRYSTALLINE CELLULOSE AVICEL PH-102
• MAIZE STARCH (CORN STARCH)
• POVIDONE (KOLLIDONE30)
• COLLOIDAL SILICONE DIOXIDE AEROSIL 200 PHARMA
• MAGNESIUM STEARATE VEGETABLE GRADE
• PURIFIED WATER

Not applicable.

Store below 30 ºC and keep in the original pack to protect from light, in a dry place.

LOANTA 10 mg tablets White to off-white, circular, flat face, beveled edge uncoated tablet,
debossed with JS45 and break-line on one side and plain on the other side.
LOANTA 10 mg tablets pack contain TEN tablets per blister, FIVE blisters each pack (Total
50 tablets per pack).

Any unused medicinal product or waste material should be disposed of in accordance with
local requirements, Keep out of the reach & sight of children