Beklo Oral Solution

Beklo Oral Solution 5 mg/5 ml is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant used for the relief of painful and uncomfortable muscle spasms caused by a variety of conditions. It is known to be particularly useful in treating muscle spasticity associated with spinal cord injury .

This drug has recently been studied for the management of alcohol withdrawal, however, a conclusion has not been made regarding baclofen efficacy in this condition .

This drug was initially approved by the FDA in 1992 . It is available in tablet form , injection form , and powder form (for suspension) .

Beklo Oral Solution 5 mg/5 ml is a GABA-ergic agonist used to manage severe spasticity of cerebral or spinal origin in adult and pediatric patients.

Beklo Oral Solution 5 mg/5 ml is administered for the relief of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and associated pain and clonus, in addition to muscular rigidity .

Patients receiving this drug should have reversible spasticity for baclofen to promote the restoration of residual function. This drug is not indicated in the treatment of skeletal muscle spasm caused by rheumatic disorders. The efficacy of baclofen in stroke, cerebral palsy, and Parkinson's disease has not been determined and, therefore, baclofen is not recommended for these conditions .

• Joint Pain
• Soreness
• Muscle
• Flexor spasm
• Reversible Spasticity
• Severe cerebral origin Spasticity
• Severe spinal cord origin Spasticity

In neurological diseases associated with spasm of the skeletal muscles, the clinical effects of baclofen occur due to baclofen action on reflex muscle contractions and of significant relief from painful spasm, automatism, as well as clonus. Beklo Oral Solution 5 mg/5 ml, when used as indicated, improves mobility, increasing levels of independence, and facilitates both passive and active physiotherapy. Beklo Oral Solution 5 mg/5 ml also stimulates gastric acid secretion .

GABA-B receptor activation by baclofen may produce protective neurological effects. Beklo Oral Solution 5 mg/5 ml also possesses anti-inflammatory properties that may be of interest in the study of addiction treatment . Preclinical studies have shown that GABA-B receptors have roles in memory storage and retrieval, reward, motivation, mood, as well as anxiety. Neuroimaging studies in humans indicate that baclofen produces region-specific alterations in brain activity.

The exact mechanism of action of baclofen is not fully understood at this time , . Many studies indicate that baclofen is a GABA-B receptor agonist , , , , . Despite this, there is no conclusive evidence that the effects of baclofen on GABA systems are involved in the production of its clinical effects .

Beklo Oral Solution 5 mg/5 ml is an effective and widely used antispastic agent with a spinal site of action. Its mechanism of action and pharmacological properties are different from the effects of other antispastic agents. In addition, baclofen has central sites of action, shown by its adverse event profile and general CNS depressant properties . GABA-B receptors interact with signal transduction pathways and neurotransmitter systems. Beklo Oral Solution 5 mg/5 ml exerts an antinociceptive effect. The clinical significance of this warrants further research data for clarification.

Beklo Oral Solution 5 mg/5 ml depresses monosynaptic and polysynaptic reflex transmission, by various actions, and possibly including the stimulation of GABAβ-receptors. This stimulation results in the inhibition of excitatory neurotransmitter (glutamate and aspartate) release, which may normally contribute to pain and spasticity. Although baclofen is an analog of the inhibitory neurotransmitter gamma-amino-butyric acid (GABA), there are no conclusive data indicating GABA systems are involved in its clinical effects .

Rapidly and almost completely absorbed from the gastrointestinal tract. Absorption may be dose-dependent, being reduced with increased doses .

Beklo Oral Solution 5 mg/5 ml, when introduced directly into the intrathecal space, allows for effective CSF concentrations to be achieved with resulting plasma concentrations 100 times less than concentrations occurring with oral administration , .

Apparent volume of distribution: 59 liters .

Beklo Oral Solution 5 mg/5 ml does not readily cross the blood-brain barrier .

30%

Beklo Oral Solution 5 mg/5 ml is rapidly and extensively eliminated from the body. There is significant intersubject variation in elimination rates. Beklo Oral Solution 5 mg/5 ml is excreted mainly by the kidney as unchanged drug. Seventy to eighty (70 - 80%) of a dose is measured in the urine as unchanged drug. The remainder of the dose is excreted as unchanged drug in the feces or as metabolites in the urine and feces. Excretion is complete within 72 hours after administration .

Elimination half-life: Approximately 5.5 hours .

Total systemic clearance: 180 mL/min Renal clearance: 103 mL/min

Beklo Oral Solution 5 mg/5 ml is primarily excreted unchanged by the kidneys. It should be administered cautiously, and it may be necessary to reduce the dosage in patients with reduced renal function .

LD50 after oral administration in rats: 145 mg/kg

Overdosage: Vomiting, muscular hypotonia, drowsiness, accommodation disorders, coma, respiratory depression, and seizures may occur with overdosage .

Pregnancy: This drug is a pregnancy category C drug. There are no adequate and well-controlled studies that have been performed with pregnant women. Beklo Oral Solution 5 mg/5 ml should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus .

Excretion in breastmilk: It is unknown whether this drug is excreted in human breast milk. Because many drugs are excreted in human milk, caution is warranted when baclofen is administered to a nursing woman .

• Avoid alcohol.
• Take with food. Take with food or milk to reduce gastric irritation.

• 12 month-2 years: 10-20 mg (10-20 ml)
• 2 years-6 years: 20-30 mg (20-30 ml)
• 6 years-10 years: 30-60 mg (30-60 ml)