Baclofen online in Australia

What is Baclofen used for?

Adult

Baclofen is indicated as a treatment for:

· Spastic contractures of multiple sclerosis.

Spastic contractures of spinal disorders (infectious, degenerative, traumatic, neoplastic).

Spastic contractions of cerebral origin.

Pediatric population (6 to 18 years old)

Baclofen is indicated as symptomatic treatment for:

Spastic contractions of cerebral origin (infantile cerebral palsy, cerebrovascular accident, neoplastic or degenerative cerebral disease).

Muscular spasticity that occurs in spinal cord diseases of infectious, degenerative, traumatic, neoplastic, or secondary origin due to multiple sclerosis, spastic spinal palsy, amyotrophic lateral sclerosis, syringomyelia, transverse myelitis.

Conditions for which this medicine may be prescribed

• Spastic contraction of multiple sclerosis.
• Spinal contracture of the spinal cord.
• Spastic contraction of cerebral origin.
• Muscular spasticity

Method of administration and dosage of the drug Baclofen

Dose

Individually adapted, the dose is slowly progressive.

The lowest possible dose consistent with an optimal response is recommended.

The optimal dose should be individually adjusted to reduce clones, flexor / extensor muscle spasms and spasticity, while minimizing the occurrence of side effects.

To prevent excessive weakness and falls, Baclofen should be used with caution when spasticity is required to stand upright, balance the musculoskeletal system, or other functions. A certain degree of muscle cloning and occasional spasms may be important in supporting circulatory functions and possibly preventing deep vein thrombosis.

If the therapeutic goal is not reached after 6 to 8 weeks of treatment at maximum doses, the treatment will be re-evaluated.

With the exception of emergency situations related to overdose or the appearance of serious adverse effects, treatment interruption should always be gradual (in 1 to 2 weeks, in increments of 10 or 15 mg) (see section warnings and precautions for use ). If symptoms return, treatment should be resumed with the previous dose.

Adults

Start treatment with 15 mg per day, preferably in 2 to 3 doses, and increase doses gradually with caution (for example, 15 mg every 3-4 days) until the optimal daily dose is obtained, which is generally between 30 and 80 mg per day. An intake may be recommended at bedtime in cases of painful night spasticity.

In some particularly drug-sensitive patients, it is preferable to start with a lower daily dose (5 or 10 mg) and increase this dose very gradually (see Warnings and precautions for use section).

In hospitals, daily doses of up to 100 to 120 mg can be administered under close clinical supervision.

During the rehabilitation of neurological spasticity, a daily dose of 30 to 40 mg is usually sufficient.

Special populations

Pediatric population (6 to 18 years old)

Treatment is started with very low doses of the order of 0.3 mg / kg / day divided into 2 to 4 doses (preferably 4 doses). Given the recommended doses and available presentations, Baclofen is not suitable for children weighing less than 33 kg. The daily dose should be carefully increased from one to two weeks to the optimum dose for the child.

As an indication, the usual daily maintenance dose ranges from 0.75 to 2 mg / kg of body weight in three doses. The total daily dose should not exceed 40 mg / day in children younger than 8 years. In children older than 8 years, a maximum dose of 60 mg / day can be administered.

Elderly and patients with spasticity of cerebral or medullary origin:

To decrease the frequency of occurrence of side effects, the administration of a lower starting dose and its gradual increase under supervision is recommended.

Kidney failure or dialysis:

Choose an initial daily dose of approximately 5 mg / day. Signs and symptoms of overdose have been reported at doses greater than 5 mg per day.

The baclofen dose should be adjusted according to its plasma concentration in patients with renal impairment. A short hemodialysis is an effective way to remove excess baclofen from the bloodstream.

Liver failure

No studies have been conducted in patients with hepatic impairment treated with Baclofen. The liver does not play a major role in the metabolism of orally administered baclofen (see section Pharmacokinetic properties). However, Baclofen can cause an increase in liver enzymes. Baclofen should be administered with caution to patients with hepatic impairment (see section 4.4).

Administration form

Oral use.

The tablets should be absorbed during meals with a glass of water.

Due to its pharmaceutical form, Baclofen is not suitable for children under 6 years (approximately 33 kg).

Possible side effects of the drug Baclofen

• Sedation
• Drowsiness
• Confusion
• Vertigo
• Headache
• Insomnia
• Ataxia
• Shaking
• Paresthesia
• Dysarthria
• Dysgeusia
• Tinnitus
• Lowering the epileptogenic threshold
• Paradoxical increase in spasticity.
• Euphoric state
• Depression
• Hallucination
• Accommodation disorder
• Muscular hypotonia
• Bradycardia
• Respiratory depression
• Hypotension
• Sickness
• Vomiting
• Constipation
• Diarrhea
• Dry mouth
• Abdominal pain
• Anorexy
• Abnormal liver function
• Increased alkaline phosphatases.
• Increased transaminases.
• Hyperhidrosis
• Acne
• Hives
• Worsening of dysuria.
• Asthenia
• Hypothermia
• Abstinence syndrome
• Decreased cardiac output
• Increased blood sugar.
• Death
• Neuromuscular disorder
• Spasticity
• Dyskinesia
• Rhabdomyolysis
• Seizures
• Epilepticus status
• Skin itching
• Dysautonomia
• Hyperthermia
• Disorder of consciousness
• Behavioral disorder
• Anxiety
• Psychotic state
• Manic state
• Paranoid reaction
• Coagulopathy
• Delirium
• Psychotic disorder
• Paranoid idea
• Tachycardia

Show more Occurring more frequently at the start of treatment (for example, sedation) when the dose is increased too quickly or when the doses are used too high, they are more often transient and can be reduced or eliminated by reducing the dose Rarely require discontinuation of treatment.

Sometimes they are more serious in the elderly, or with a psychiatric history or cerebrovascular disorders.

The epileptogenic threshold can be lowered, seizures can occur particularly in epileptics.

The undesirable effects are presented below in decreasing order of frequency using the following categories: very common (³ 1/10), common ((³ 1/100 and minus 1/10), uncommon ((³ 1/1000 and minus 1/100), rare ((³ 1/10000 and minus 1/1000), very rare (minus 1/10000), frequency unknown (cannot be estimated from the available data).

* Withdrawal syndrome, including postnatal seizures, has also been reported after intrauterine exposure to Baclofen orally.

** Cases of sleep apnea syndrome have been observed with high doses of baclofen (≥100 mg) in patients with alcohol dependence.

Additional undesirable effects have been observed with the injectable solution for intrathecal injection of baclofen: altered alertness (very common), anxiety, disorientation, hypersalivation, dyspnea, bradypnea, pruritus, facial and peripheral edema, pyrexia, pain, chills, incontinence urinary and urinary retention (common), suicide attempt, lethargy, hypertension, venous thrombosis, reddening of the skin, paleness, muscle hypertonia, dysphagia, nystagmus (uncommon), suicidal ideation, agitation, paranoid reactions, ileus, dehydration, alopecia , erectile dysfunction (rare), memory impairment, pneumonia, inhalation pneumonia (frequency not known).

Abstinence syndrome

Stopping treatment, especially if it is abrupt, can induce a sometimes fatal withdrawal syndrome. The most frequent withdrawal reactions (by analogy with that observed with intrathecal administration) are the following: neuromuscular disorders (spasticity, dyskinesia, rhabdomyolysis, paresthesia, seizures or even epilepticus), pruritus, dysautonomia (hyperthermia, hypotension), disorders of the awareness and behavior (state of confusion, anxiety, manic or paranoid psychotic state) and coagulopathy.

Except in the case of an emergency related to overdose or the appearance of serious undesirable effects, treatment should always be discontinued gradually (see sections Dosage and method of administration and Warnings and precautions for use).

Contraindications: when not to use this medicine?

• Baclofen hypersensitivity
• Child under 6
• Child under 33 kg
• Lack of effective female contraception
• Alcohol consumption
• Porphyria
• Pregnancy
• Breastfeeding
• Galactose intolerance
• Lactase deficiency
• Galactose malabsorption syndrome
• Glucose malabsorption syndrome
• End-stage kidney disease (Clcr minus 15 ml / min)

Show more This medication is contraindicated in the following cases:

Hypersensitivity to the active substance or to any of the excipients included in the Composition section.

Presentation of this medicine

30 slotted tablets in blister (aluminum / PVC / PVDC) Appearance and shape

Breakable tablet

Composition of the drug Baclofen

* per unit dose Active ingredients: Baclofen Excipients with known effects? : Lactose monohydrate Other excipients: Microcrystalline cellulose (AVICEL PH 102), Calcium anhydrous hydrogen phosphate, Sodium carboxymethyl starch, Colloidal anhydrous silica, Magnesium stearate Effects on ability to drive and use machines

Baclofen has a moderate influence on the ability to drive and use machines. Undesirable effects such as sedation, dizziness and visual disturbances are associated with taking baclofen (see section Undesirable effects).

Patients should be warned about the importance of avoiding driving or using machines if they experience these side effects.

Warnings and precautions for use

• Multi-deficient
• Woman of childbearing age
• Stroke
• Cardiopulmonary disease
• Partial paralysis of the respiratory muscles.
• Kidney failure (15 min Clcr minus 80 ml / min)
• Epileptic
• Sphincter hypertonia
• Liver disease
• Diabetes
• History of psychotic disorders.
• History of the confusional state.
• History of depression
• Cerebrovascular disease
• History of cerebrovascular disease.
• Respiratory insufficiency.
• History of respiratory failure.
• Peptic ulcer
• Gastroduodenal ulcer history
• Parkinson's disease
• Newborn mother treated
• Old subject

Show more Special warnings

Baclofen will be administered only if the benefit outweighs the risk. The occurrence of undesirable effects (in particular drowsiness and lethargy) should be controlled in patients at risk (multiple deficient severe stroke, end-stage renal failure).

Pediatric population

Clinical experience with the use of baclofen in children younger than 1 year is very limited.

Women of childbearing age

In view of the potential risk of exposure during pregnancy, women of childbearing potential should use effective contraception during treatment (see section Fertility, pregnancy and lactation).

Treatment interruption

Do not stop treatment suddenly because of the risk of withdrawal syndrome. In fact, a sudden interruption of treatment (by analogy with what has been observed in the case of intrathecal administration) can lead to a withdrawal syndrome that is sometimes fatal with the following symptoms in relation to a probable elevation of serotonergic tone: neuromuscular disorders (spasticity, dyskinesia, rhabdomyolysis, paresthesia, seizures, or even epilepticus), pruritus, dysautonomia (hyperthermia, hypotension), disorders of consciousness and behavior (confused state, hallucinations, manic or paranoid psychotic state), and coagulopathy .

Withdrawal symptoms, including postnatal seizures in the newborn, have been reported after intrauterine exposure to Baclofen orally. The administration of Baclofen to newborns with withdrawal syndrome, with gradual dose reduction, may help to control withdrawal reactions (see section Fertility, pregnancy and lactation).

Unless there is an emergency related to overdose or the appearance of serious adverse effects, treatment should always be discontinued gradually, gradually reducing the dose over a period of approximately 1 to 2 weeks. The following side effects have been reported during the sudden discontinuation of Baclofen, especially after prolonged pharmacological treatment: anxiety and confusion, delirium, hallucinations, psychotic, manic or paranoid disorders, seizures (state of epilepsy), dyskinesia, tachycardia, hyperthermia , rhabdomyolysis and temporary worsening of spasticity as a rebound effect.

Respiratory problems

The risk of respiratory depression is increased when CNS depressant medications are prescribed together. Particular monitoring of respiratory and cardiovascular functions is essential in patients suffering from cardiopulmonary disease or paresis of the respiratory muscles.

Porphyria

The use of this medicine is not recommended in patients with porphyria, by extrapolation from animal data.

This medicine contains lactose. Its use is not recommended in patients with galactose intolerance, Lapp lactase deficiency, or malabsorption of glucose or galactose (rare inherited diseases).

Employment precautions

Renal insufficiency

Baclofen should be used with caution in patients with renal impairment and should only be administered to patients with end-stage renal disease if the expected benefit outweighs the risk involved (see section 4.2). Neurological signs and symptoms of overdose, including clinical manifestations of toxic encephalopathy (eg, confusion, disorientation, drowsiness, and altered level of consciousness) have been observed in patients with renal impairment taking baclofen orally in doses greater than 5 mg per day. Patients with renal dysfunction should be closely monitored for a rapid diagnosis of early signs and / or symptoms of toxicity.

Special precautions are needed when Baclofen is combined with drugs or pharmaceuticals that can have a significant impact on kidney function. Kidney function should be closely monitored and the daily dose of Baclofen should be adjusted to prevent baclofen toxicity.

Epilepsy

In epileptic patients suffering from spasticity, comitia attacks can occur at therapeutic doses or in overdose or during withdrawal. In these patients, continue antiepileptic treatment and reinforce monitoring (see section Adverse effects).

Urinary problems

In pre-existing sphincter hypertonia, the possible occurrence of acute urine retention requires the careful use of baclofen.

Biological analysis

In case of liver disease or diabetes, regular checks for transaminases, serum alkaline phosphatases, or blood sugar are necessary.

Psychiatric disorders

Use with caution in patients with a history of psychotic disorders, confusion and depression.

Other situations that require careful use in patients with or with a history of

Cerebrovascular disease,

Respiratory insufficiency

Gastric or duodenal ulcer,

Parkinson's disease.

Mechanism of action: how does it work?

Pharmacotherapeutic group: OTHER CENTRAL ACTION DRUGS, ATC code: M03BX01

Mechanism of action

Baclofen is a structural analogue of gamma-aminobutyric acid (GABA). This product has an antispastic action with an impact point on the spinal cord: it slows down the transmission of mono and polysynaptic reflexes by stimulating GABA B receptors in the spinal cord.

Pharmacodynamic effects

Neuromuscular transmission is not affected by baclofen. Baclofen has an antinociceptive action: in neurological disorders accompanied by spasms of skeletal muscles, Baclofen produces a favorable clinical effect on reflex muscle contractions and considerably attenuates painful spasms, automatisms and clones.

Baclofen has been shown to cause depression of the central nervous system, accompanied by sedation, drowsiness, and respiratory and cardiovascular depression.

Interactions: do not take this medicine with ..

Associations not recommended

+ Alcohol (drink or excipient)

Increased alcohol sedative effect of baclofen. Impaired alertness can make driving and using machines dangerous.

Avoid drinking alcoholic beverages and drugs that contain alcohol.

Associations subject to precautions for use.

+ Antihypertensive drugs

Risk of increased hypotension, especially orthostatic. Blood pressure control and dose adjustment of the antihypertensive if necessary.

Associations to consider

+ Imipramine antidepressants

Risk of increased muscle hypotonia.

+ Other sedative drugs:

Morphine derivatives (pain relievers, cough suppressants, and substitution treatments), neuroleptics, barbiturates, benzodiazepines, anxiolytics other than benzodiazepines (eg, meprobamate), hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimistamine) , trimistamine, trimistamine, trimistamine central antihypertensive drugs, thalidomide.

Increased central depression. Impaired alertness can make driving and using machines dangerous.

+ Dapoxetine

Risk of increased unwanted effects, particularly with dizziness or fainting.

+ Levodopa

Risk of worsening Parkinson's syndrome or central adverse effects (visual hallucinations, confusion, headache).

+ Drugs that lower blood pressure

Risk of increased hypotension, especially orthostatic.

Incompatibilities

Aimlessly.

How to react in case of overdose?

Clinical signs of an overdose:

· Disorders of consciousness that can lead to coma,

Sometimes generalized muscle hypotonia that can last 72 hours, which can reach the respiratory muscles,

It can also occur: dizziness, confusion, hallucinations, agitation, seizures, abnormal electroencephalogram (suppression of bursts and triphasic waves), accommodation disorders, alteration of pupillary reflexes, myoclonus, hyporeflexia or areflexia, peripheral vasodilation, hypotension or hypertension. , bradycardia or tachycardia, or cardiac arrhythmia, hypothermia, nausea, vomiting, diarrhea, salivary hypersecretion, elevated liver enzymes (AST, alkaline phosphatase), and rhabdomyolysis.

What to do:

· There is not a specific antidote.

Immediate cessation of treatment,

· Immediate transfer to the hospital,

· Quick elimination of the ingested product.

After ingestion of a potentially toxic amount, administration of activated charcoal may be considered, especially in the first hours after ingestion. Gastric lavage can be considered on a case-by-case basis, particularly within 60 minutes of ingestion of a life-threatening overdose.

Comatose or seizure patients should be intubated before starting gastric evacuation. In addition to discontinuation of treatment, unscheduled hemodialysis may be considered as an alternative in patients with severe toxicity due to baclofen. Hemodialysis facilitates the elimination of baclofen, alleviates the clinical symptoms of overdose and shortens the healing time in these patients.

Symptomatic treatment of visceral failures,

· When using diazepam IV for seizures, give it with caution.

BACLOFEN ZENTIVE: pregnancy, lactation and fertility

Women of childbearing age

Women of childbearing potential should use effective contraception during treatment.

Pregnancy

Animal studies have shown a teratogenic effect of oral baclofen. Administered orally in animals, baclofen crosses the placenta.

Limited clinical data are available, but cases of malformations have been reported in children exposed to baclofen in utero, with types of malformations consistent with those observed in animals (central nervous system, skeletal abnormalities, and omphalocele).

If baclofen is used orally until delivery, cases of withdrawal syndrome (including postnatal seizures) have been reported in newborns (see section 4.4). ) This syndrome can be delayed for several days after birth.

Therefore, baclofen should not be used during pregnancy unless absolutely necessary. Women of childbearing potential should use effective contraception during treatment.

In the event of exposure during pregnancy, specialized prenatal surveillance should be implemented, geared towards the malformations described above. In the event of exposure at the end of pregnancy, adequate monitoring and management of the newborn should be implemented.

Breastfeeding

Very little data is available on the use of baclofen during lactation. Consequently, breastfeeding should be avoided.

Fertility

There are no data available on the effect of baclofen on human fertility. In rats, baclofen administered to the mother in non-toxic doses did not affect male or female fertility.