Bac-10

Baclofen (BAC-10) 10 mg Tablet is a white to off-white, round, biconvex, uncoated tablet, plain on both sides.
Each tablet contains: Baclofen, USP 10 mg.

Skeletal Muscle Relaxant.
Pharmacology: Pharmacodynamics and Pharmacokinetics: Baclofen, an analogue of gamma-aminobutyric acid, is a centrally acting skeletal muscle relaxant. It interferes with the release of excitatory neurotransmitters and inhibits monosynaptic and polysynaptic transmission at the spinal cord level. It may also act at supraspinal sites producing CNS depression.
Baclofen is rapidly and almost completely absorbed from the gastrointestinal tract after an oral dose. Peak plasma concentrations occur about 0.5 to 3 hours after ingestion, but the rate and extent of absorption vary between patients, and may vary inversely with the dose. After oral doses some baclofen crosses the blood-brain barrier, with concentrations in CSF about 12% of those in the plasma. About 30% of baclofen is bound to plasma proteins. About 70% to 80% of a dose is excreted in the urine mainly as unchanged drug; 15% metabolised in the liver. The elimination half-life of baclofen is about 3 to 4 hours in plasma and about 1 to 5 hours in CSF. Baclofen crosses the placenta and is distributed into breast milk.

It is used for the symptomatic relief of severe chronic spasticity associated with variety of conditions.

Baclofen is given orally in divided doses, preferably with or after food or milk. The initial dose of baclofen is 5 mg three times daily for 3 days, increased to 10 mg three times daily for 3 days, then in similar increments and intervals until either a dose of 20 mg three times daily is reached or until the desired therapeutic effect is obtained. Or as prescribed by a physician.
The recommended daily maintenance doses are: 12 months to 2 years, 10 mg to 20 mg; 2 to 6 years, 20 mg to 30 mg; 6 to 10 years, 30 mg to 60 mg.
Elderly patients should receive lower initial doses, although final maintenance doses may be in the same range as younger adults.

Overdosage may lead to muscular hypotonia, hypothermia, drowsiness, respiratory depression, coma, and convulsions.
Treatment of Baclofen overdosage is symptomatic. Consideration should be given to the use of activated charcoal in adults who have ingested more than 100 mg and children who have taken more than 5 mg/kg, within an hour of presentation. Alternatively, gastric lavage may be considered in adults within an hour of ingesting a life-threatening overdose. Haemodialysis should be considered in severe cases.

Baclofen is considered unsafe in patients with porphyria because it has been shown to be porphyrinogenic in in-vitro system.

Baclofen stimulates gastric acid secretion and should be used with caution in patients with a history of peptic ulcer and avoided in those patients with active peptic ulcer disease. It should also be used with caution in patients with severe psychiatric disorders or epilepsy or convulsive disorders since these disorders may be exacerbated by baclofen. Liver function should be monitored in patients with liver disease; patients with renal impairment need a reduced dose. Baclofen should be used with caution in patients with respiratory impairment. Observations of increased blood sugar concentrations suggest caution in patients with diabetes mellitus.
Care is also required in the elderly, in whom adverse effects may be more common, and in patients with cerebrovascular disease (who tolerate baclofen poorly). It should be used with caution in patients who use their spasticity to maintain posture or to increase function. Urine retention may be exacerbated in patients with hypertonic bladder sphincters. Baclofen may cause drowsiness; patients affected should not drive or operate machinery.
Abrupt withdrawal of baclofen may result in a withdrawal syndrome and exacerbation of spasticity; dosage should be reduced gradually over at least 1 to 2 weeks, or longer if symptoms occur.

Baclofen is excreted into breast milk. No adverse effects have been observed in breast-fed infants whose mothers were receiving baclofen.

The most common adverse effects include drowsiness, nausea, dizziness, lassitude, lightheadedness, confusion, fatigue, muscular pain and weakness and hypotension. Other adverse effects include euphoria, hallucinations, depressions, headache, tinnitus, convulsions, paresthesias, slurred speech, dry mouth, taste alterations, vomiting, diarrhea or constipation, ataxia, nystagmus, tremors, insomnia, visual disturbances, skin rashes, pruritus, increased sweating, urinary disturbances, respiratory or cardiovascular depression, blood sugar changes, alterations in liver function values, and a paradoxical increase in spasticity.
ADR Reporting: Patient should seek medical attention immediately at the first sign of any adverse drug reaction.

Alcohol and other CNS depressants may exacerbate the CNS effects of baclofen and should be avoided; severe aggravation of hyperkinetic symptoms may possibly occur in patients taking lithium. There may be increased weakness if baclofen is given to patients taking tricyclic antidepressant and there may be increased hypotensive effects if it is given to patients receiving antihypertensive therapy. Ibuprofen and other drugs that produce renal insufficiency may reduce baclofen excretion leading to toxicity.

Store at temperatures not exceeding 30°C.

Muscle Relaxants

M03BX01 - baclofen ; Belongs to the class of other centrally-acting muscle relaxants.

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