Baclofen (Tablets) Instructions for Use

Marketing Authorization Holder

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

ATC Code

M03BX01 (Baclofen)

Active Substance

Baclofen (Rec.INN registered by WHO)

Dosage Forms

	Baclofen	Tablets 10 mg: 10, 20, 30, 40 or 50 pcs.
		Tablets 25 mg: 10, 20, 30, 40 or 50 pcs.

Dosage Form, Packaging, and Composition

Tablets white, round, biconvex, with a score line.

Excipients: lactose monohydrate – 60 mg, potato starch – 34.75 mg, gelatin – 2.25 mg, talc – 1 mg, magnesium stearate – 0.5 mg, ethylcellulose – 1.5 mg.

10 pcs. – contour cell blisters – cardboard packs.
10 pcs. – contour cell blisters (2) – cardboard packs.
10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (4) – cardboard packs.
10 pcs. – contour cell blisters (5) – cardboard packs.
10 pcs. – contour cell blisters (100) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (200) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (300) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (400) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (600) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (800) – cardboard boxes (for hospitals).

Tablets white, round, biconvex.

Excipients: lactose monohydrate – 50 mg, potato starch – 29.75 mg, gelatin – 2.25 mg, talc – 1 mg, magnesium stearate – 0.5 mg, ethylcellulose – 1.5 mg.

10 pcs. – contour cell blisters – cardboard packs.
10 pcs. – contour cell blisters (2) – cardboard packs.
10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (4) – cardboard packs.
10 pcs. – contour cell blisters (5) – cardboard packs.
10 pcs. – contour cell blisters (100) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (200) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (300) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (400) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (600) – cardboard boxes (for hospitals).
10 pcs. – contour cell blisters (800) – cardboard boxes (for hospitals).

Clinical-Pharmacological Group

Centrally acting muscle relaxant

Pharmacotherapeutic Group

Centrally-acting muscle relaxant

Pharmacological Action

Centrally acting muscle relaxant; GABA_B receptor agonist. It inhibits mono- and polysynaptic reflexes, apparently by reducing the release of excitatory amino acids (glutamate and aspartate) from nerve terminals, which occurs as a result of stimulation of presynaptic GABA receptors.

It does not affect impulse transmission at neuromuscular synapses. It reduces skeletal muscle tone. It has a moderate analgesic effect.

Pharmacokinetics

After oral administration, Baclofen is rapidly and completely absorbed from the gastrointestinal tract. C_max in blood plasma is reached 2-3 hours after administration.

Plasma protein binding is about 30%. Baclofen crosses the placental barrier and is excreted in breast milk. It is metabolized in the liver. It is excreted in the urine, mainly unchanged.

Indications

Skeletal muscle spasticity in multiple sclerosis. Spastic conditions in diseases of the spinal cord of infectious, degenerative, traumatic origin, as well as in cerebral palsy.

ICD codes

Dosage Regimen

Orally for adults at the beginning of treatment – 5 mg 3 times/day. Every 4th day of treatment, the dose is increased by 5 mg 3 times/day until the optimal therapeutic effect is achieved.

The average daily dose is 30-75 mg; if necessary, it can be increased to 100-120 mg. The final daily dose is set individually so that, along with a reduction in clonus and muscle spasm, sufficient muscle tone for active movements is maintained.

For patients with increased sensitivity to drugs, the initial daily dose may be 5-10 mg with a subsequent slower increase.

For patients with renal failure, as well as those undergoing hemodialysis, the daily dose is 5 mg.

For children under 10 years of age, the daily dose is 0.75-2 mg/kg, over 10 years – 2.5 mg/kg. Treatment begins with a dose of 2.5 mg 4 times/day.

The daily dose, as in adults, is selected individually, increasing it every 3 days, in accordance with the clinical course of the disease. The maintenance dose for children aged 1-2 years is 10-20 mg/day, for children aged 2-10 years – 30-60 mg/day.

Adverse Reactions

From the nervous system: drowsiness, dizziness (especially at the beginning of treatment); sometimes – apathy, feeling of fatigue, sleep disorders, confusion; rarely – euphoria, depression, paresthesia, myalgia, muscle weakness, ataxia, tremor, nystagmus, accommodation disturbances, hallucinations; possible increase in the frequency of seizures and a decrease in the threshold of their occurrence (especially in epilepsy).

From the digestive system: nausea; sometimes dry mouth, constipation, diarrhea are observed; in some cases – impaired liver function.

From the cardiovascular system: sometimes – arterial hypotension, deterioration of cardiovascular system activity.

Other: sometimes – respiratory depression; rarely – dysuria, enuresis.

Adverse effects occur mainly at the beginning of treatment, with a rapid dose increase, when prescribed at a dose of more than 60 mg/day, as well as in elderly patients.

Contraindications

Hypersensitivity to baclofen.

Use in Pregnancy and Lactation

During pregnancy (especially in the first trimester), Baclofen should be used only for vital indications.

Baclofen is excreted in breast milk. If it is necessary to use during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

Use with caution in cases of impaired liver function. In patients with liver disease, the level of liver transaminases and alkaline phosphatase should be periodically monitored.

Use in Renal Impairment

Use with caution in cases of impaired renal function.

For patients with renal failure, as well as those undergoing hemodialysis, the daily dose is 5 mg.

Pediatric Use

For children under 10 years of age, the daily dose is 0.75-2 mg/kg, over 10 years – 2.5 mg/kg. Treatment begins with a dose of 2.5 mg 4 times/day.

The daily dose, as in adults, is selected individually, increasing it every 3 days, in accordance with the clinical course of the disease. The maintenance dose for children aged 1-2 years is 10-20 mg/day, for children aged 2-10 years – 30-60 mg/day.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Selection of an individual daily dose is recommended to be carried out in a hospital setting.

Adverse effects are often transient and may disappear or decrease when the dose is reduced. The need to interrupt therapy rarely arises. The side effects of baclofen should be distinguished from the symptoms of the disease for which the treatment is being carried out.

Discontinuation of baclofen should be carried out gradually, reducing the dose over 1-2 weeks (except in cases of serious adverse effects).

Use with caution in cerebrovascular disorders, psychotic conditions, schizophrenia, peptic ulcer of the stomach and duodenum, respiratory disorders, impaired liver and kidney function, as well as in elderly patients.

In case of concomitant epilepsy, treatment should be carried out under strict medical supervision and without interruption of adequate anticonvulsant therapy.

In patients with dysuria during treatment with baclofen, hypertonicity of the bladder sphincter and urinary retention may be observed.

In patients with liver disease and diabetes mellitus, the levels of liver transaminases, alkaline phosphatase and blood glucose should be periodically monitored.

Effect on the ability to drive vehicles and mechanisms

During treatment, one should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug Interactions

With simultaneous use, Baclofen enhances the effect of antihypertensive agents and ethanol.

With simultaneous use with tricyclic antidepressants, a significant decrease in muscle tone is possible.

A case of toxic reactions due to the action of baclofen (impaired consciousness, disorientation, bradycardia, blurred vision, arterial hypotension, hypothermia) has been described with simultaneous use with ibuprofen in an elderly patient with impaired renal function.

With simultaneous use with lithium preparations, severe manifestations of hyperkinetic symptoms are possible.

In patients with Parkinson’s disease, with simultaneous use of baclofen with levodopa and carbidopa, hallucinations, confusion, and agitation may occur.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.