Gerard Laboratories

Baclopar 10 mg tablets

Each tablet contains 10 mg of Baclofen.

Excipients: Each tablets contains 40mg of lactose monohydrate

For a full list of excipients, see section 6.1.

Tablets.

White flat bevel-edge tablet, marked “BN” breakline “10” on one side and “G” on the reverse.

4.1.1 Relief of voluntary muscle spasticity as occurs in conditions such as multiple sclerosis and spinal cord lesions including syringomyelia, transverse myelitis and motor neurone disease.

4.1.2 Management of spasticity of cerebral origin including meningitis, cerebral palsy, traumatic head injury, cerebrovascular accident.

Baclofen is of most benefit in relief of spasticity which is seriously interfering with activity.

For oral administration only.

Relief of voluntary muscle spasticity in spinal cord lesions and management of spasticity of cerebral origin.

Adults: A gradually increasing dosage regimen of baclofen is recommended which should be adjusted to achieve satisfactory symptom control.

5mg three times a day for three days

10mg three times a day for three days

15mg three times a day for three days

20mg three times a day for three days

25mg three times a day for three days

Symptoms are usually adequately controlled with doses up to 60mg daily. However, in order to meet individual patient needs, dosage adjustments should be slow and careful. The dose should not exceed 100mg per day unless the patient is in hospital under medical supervision. If therapeutic effect is not achieved within 6 weeks of reaching the maximum recommended dose, a decision of whether to continue with therapy should be taken. In some cases, mobility is improved with small frequent doses, especially if given 1 hour prior to performing manual tasks, rather than larger spaced doses. Some patients benefit from only taking baclofen at night to reduce painful muscle spasms.

Elderly: Side effects are more common in the elderly and are noticed most particularly at the beginning of baclofen therapy. Elderly patients should be treated under careful medical supervision and initially receive a low dose of baclofen which can gradually be titrated upwards according to the therapeutic response. Most elderly patients are able to tolerate the same average maximum dose as for younger patients.

Children: A dosage range of 0.75 - 2mg/kg body weight should be used. In children over 10 years of age however, a maximum daily dosage of 2.5mg/kg body weight may be given. The dosage should be cautiously raised at the same rate indicated for adults until satisfactory symptom control is achieved. The recommended daily dosages for maintenance therapy are as follows:-

Patients with impaired renal function: A particularly low dosage of baclofen should be used in patients with impaired renal function or those undergoing haemodialysis.

Patients with spastic states of cerebral origin: Such patients are more likely to experience unwanted side effects and should be kept under close surveillance. Therapy and subsequent dosage changes should be initiated with caution.

Hypersensitivity to baclofen and pulmonary insufficiency.

Use in patients with pulmonary insufficiency.

Baclofen should only be used with great caution in patients with porphyria, history of alcoholism, hypertension, epilepsy, history of convulsions, psychotic disorders, schizophrenia depressive or manic disorders or confusional states since exacerbation of such conditions may occur.

Patients with acute cerebrovascular ischaemia, a history of/or existent peptic ulcers, or those on anti-hypertensive therapy or with renal impairment should receive baclofen only under careful supervision.

Baclofen should be used with extreme care in patients already receiving antihypertensive therapy.

Use of the drug should always, (unless adverse effects occur), be gradually discontinued by successively reducing the dosage over a period of 1-2 weeks. Anxiety and confusional states, hallucinations, psychotic, manic or paranoid sates, convulsions (state epilepticus), dyskinesia, tachycardia, hyperthermia and temporary aggravation of spasticity as rebound phenomenon have been reported with abrupt withdrawal of Baclofen, especially after long-term medication.

For the intrathecal formulation of Baclopar, it has been reported that clinical characteristics of withdrawal may resemble autonomic dysreflexia, infection (sepsis), malignant hyperthermia, neuroleptic-malignant syndrome, or other conditions associated with a hypermetabolic state or widespread rhabodomyolysis.

Baclofen may interfere with micturition and associated functions. Patients with neurogenic disturbances affecting emptying may show improvement but those with pre-existing sphincter hypertonia may experience acute urinary retention.

Raised AST, AP and blood glucose levels have been noted rarely. Liver function tests should be performed in patients with liver disease and diabetic patients monitored to ensure that no underlying drug induced changes have occurred in these diseases.

Patients with renal hereditaryproblems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

In concomitant administration with other drugs acting on the CNS or with alcohol, increased sedation may occur.

Concurrent use of baclofen with MAO inhibitors may result in increased CNS-depressant and hypotensive effects; caution is recommended and dosage of one or both agents may require reduction.

Prolongation of fentanyl induced anaesthesia may occur in patients pre-treated with baclofen.

The effect of baclofen may be prolonged if co-administered with tricyclic anti-depressants resulting in marked muscle hypotonia.

The risk of respiratory depression is also increased. Careful monitoring of respiratory and cardiovascular functions is essential especially in patients with cardiopulmonary disease and respiratory muscle weakness.

The risk of hypotension occurring is increased in patients receiving both baclofen and anti-hypertensive therapy. Adjustments to the dosage of anti-hypertensive medication should be made accordingly.

Mental confusion, hallucinations and agitation has been reported in patients concurrently treated with baclofen and levodopa plus carbidopa for Parkinson's Disease.

Drugs which may produce renal insufficiency e.g. ibuprofen may reduce baclofen excretion leading to toxic effects.

Since balcofen may increase blood glucose concentrations, dosage adjustments of insulin and/or oral hypoglycemic agents may be necessary during and after concurrent therapy.

Aggravation of hyperkinetic symptoms may possibly occur in patients taking lithium.

Genotoxicity has not been reported with baclofen.

An increased incidence of ventral hernias has been noted in the foetuses of rats receiving high doses of baclofen during the period of organogenesis. Studies in rats and rabbits suggest that baclofen may inhibit foetal bone ossification.

Female rats, treated with baclofen for 2 years have developed enlarged and/or haemorrhagic adrenals and a dose related increase of ovarian cysts. The clinical relevance of these findings is not known.

As baclofen crosses the placenta it should be avoided in pregnancy, especially in the first trimester, unless the benefit of treatment for the mother outweighs the risks to the foetus. A case of withdrawal in a neonate manifesting as generalised convulsions following intrauterine baclofen exposure has been recorded.

Baclofen is excreted in breast milk, but the amount present is considered to be too small to harm the infant.

Baclofen may induce sedation and will affect voluntary muscle tone. If affected, patients should not drive or operate machinery.

Side-effects: Unwanted effects occur mainly at the start of treatment, 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 Baclopar be ingested with food or a milk beverage.

Lowering of the convulsion threshold and convulsions may occur, particularly in epileptic patients.

Certain patients have shown increased muscle spasticity as a paradoxical reaction to the medication.

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.

Adverse reactions are ranked under heading of frequency, the most frequent first, using the following convention: very common (1/10); common (1/100, < 1/10); uncommon (1/1,000, <1/100); rare (1/10,000, < 1/1,000) very rare (< 1/10,000), including isolated reports.

Nervous System Disorders:

Very common: Sedation, somnolence.

Common: Respiratory depression, light-headedness, lassitude, exhaustion, mental confusion, dizziness, headache, insomnia, euphoria mood, depression, muscular weakness, ataxia, tremor, hallucinations, nightmares, myalgia, nystagmus, dry mouth.

Rare: Paraesthesia, dysarthria, dysgeusia. Lowering of the convulsion threshold and convulsions may occur, particularly in epileptic patients.

Very rare: Hypothermia

Eyes disorders:

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 (ie. By reducing the doses given during the day and possibly increasing the evening dose).

Common: Accommodation disorders, visual disturbance.

Gastro-intestinal disorders:

Very common: Nausea.

Common: Mild gastro-intestinal disturbances constipation, diarrhoea, retching and vomiting.

Rare: Abdominal pain

Cardiac Disorders:

Common: Diminished cardiovascular function.

Vascular disorders:

Common: Hypotension

Renal and urinaire disorders:

Common: Pollakiuria, enuresis, dysuria

Rare: Urinary retention

Reproductive system and brest disorders:

Rare: Erectile dysfunction

Hepatobiliary disorders:

Rare: Hepatic function abnormal.

Skin and subcutaneous tissue disorders:

Common: Hyperhidrosis, skin rash.

Symptoms: Central nervous depression: drowsiness, impairment of consciousness, respiratory depression and coma.

Other possible symptoms are: confusion, hallucinations, agitation, accommodation disorders, absent pupillary reflex; generalised muscular hypotonia, myoclonia, hyporeflexia or areflexia: convulsions; peripheral vasodilatation, hypotension, bradycardia; hypothermia; nausea, vomiting, diarrhoea, hypersalivation; elevated LDH, AST and AP values.

The condition may be aggravated if various substances or drugs acting on the central nervous system (e.g. alcohol, diazepam, tricyclic antidepressants) were taken at the same time.

Treatment: There is no specific antidote.

The drug should be removed from the gastro-intestinal tract by induction of vomiting, gastric lavage (comatose patients should be intubated prior to gastric lavage) and administration of activated charcoal; if necessary saline aperient. In respiratory depression, administration of artificial respiration, also measures in support of cardiovascular functions should be given. Excretion is chiefly via the kidneys so generous quantities of fluid should be given. In the event of convulsions, i.v. diazepam may be administered cautiously.

Baclofen is a chlorophenyl analogue of gamma-aminobutyric acid (GABA) and is chemically unrelated to other antispastic agents. It acts at the spinal level depressing monosynaptic and polysynaptic reflex transmission, most probably by stimulating the GABA_β receptors. This, in turn inhibits the release of the excitatory amino acids (glutamate and aspartate). Baclofen does not affect neuromuscular transmission.

Baclofen is well absorbed and excreted mostly unmetabolised in the urine with a T½ of about 5 hours.

Animal studies suggest a relatively low level of toxicity. Repeated dosing schedules demonstrated a dose-related increase in the incidence of ovarian cysts. No associated microscopic abnormalities were reported with the increased incidence of ovarian cysts. Increased levels of ALT were also demonstrated but were not associated with histopathological changes. Two year rat studies show no increases in either hyperplasia or neoplasia with baclofen treatment.

Lactose monohydrate

Microcrystalline cellulose

Calcium hydrogen phosphate, anhydrous

Sodium starch glycolate (Type A)

Colloidal anhydrous silica

Magnesium stearate

Not applicable.

3 years

Do not store above 25°C.

6.5.1 Securitainers

Polypropylene tablet containers with polyethylene caps and polyethylene ullage filler. Pack contents of 50 or 100 tablets.

6.5.2 Blister strips

Polyvinylchloride blisters sealed onto aluminium foil. Pack contents of 100 tablets.

Not all pack sizes may be marketed.

No special requirements.

Generics [UK] Limited

12 Station Close

Potters Bar

Hertfordshire, EN6 1TL

UK

PA 405/29/1

Date of first authorisation: 21^st November 1989

Date of last renewal: 21^st November 2009

June 2011