Miorel

baclofen

Miorel baclofen is a medication that helps with cramps and abnormally increased tone. It works on GABA receptors in the spinal cord and in the cerebellum. Baclofen is similar to benzodiazepines in terms of effectiveness, but baclofen works mostly in the spinal cord and not as much in the brain. Since baclofen does not work as much in the brain, there tend to be fewer side effects compared with the benzodiazepines.

Miorel is a derivative of gamma-aminobutyric acid, and is an agonist specific to mammalian but not fruit fly (Drosophila) GABAB receptors. It is used for the treatment of spastic movement, especially in instances of spinal cord injury, spastic diplegia, multiple sclerosis, amyotrophic lateral sclerosis (Lou Gehrig's Disease) and trigeminal neuralgia. Its beneficial effects result from actions at spinal and supraspinal sites. Baclofen can also be used to treat hiccups.

This medication relaxes muscles and relieves pain and discomfort due to certain nerve disorders. The drug is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low and the drug is predominantly excreted in the unchanged form by the kidneys.

Baclofen affects the spinal cord, which is the main connection between the brain and the rest of the body. The spinal cord plays a role as a reflex system that functions as a feedback loop. Our most obvious reflex is the withdrawal of our appendages from extreme heat. Baclofen works on this reflex circuit's Renshaw cells. These cells are very sensitive to a neurotransmitter produced by the nervous system, GABA (gamma-amino-butyric-acid), which slows this reflex circuit down. Baclofen mimics the effects of GABA.

Baclofen is a direct agonist of GABAB receptors, which upon activation utilize a G-protein coupled mechanism to increase transmembrane potassium conductance through specific ion channels. Since potassium has a positive charge, and since intracellular potassium concentrations are normally at least ten times that of the extracellular environment, opening potassium channels has an inhibitory, hyperpolarizing effect on a cell's resting electrochemical potential. This tends to decrease the rate of neuronal action potentials, which accounts for Baclofen's anti-spastic effects.

This drug is taken by mouth, usually three times daily. Dosage is based on your condition and response. Do not increase your dose or take it more often than prescribed. Do not suddenly stop taking this drug without your doctor's approval. It may take 1 to 2 months for full benefit to be noticed.

The determination of optimal dosage requires individual titration. Start therapy at a low dosage and increase gradually until optimum effect is achieved (usually between 40 to 80 mg daily). The following dosage schedule is suggested: 5 mg for 3 days, 10 mg for 3 days, 15 mg for 3 days, 20 mg for 3 days. Thereafter additional increases may be necessary but the total daily dose should not exceed a maximum of 80 mg daily.

The lowest dose compatible with an optimal response is recommended. If benefits are not evident after a reasonable trial period, patients should be slowly withdrawn from the drug.

If you miss a dose, take it as soon as remembered if it is within an hour or so. If you do not remember until later, skip the missed dose and resume your usual dosing schedule. Do not "double-up" the doses.

May cause drowsiness, dizziness, weakness, confusion, headache, nausea, constipation or diarrhea. If these effects persist or worsen, notify your doctor. Unlikely to occur but report promptly: mental/mood changes, seizures, vision changes, muscle stiffness, stomach pain, vomiting, trouble breathing, painful urination, change in urine amount. Very unlikely but report promptly: impotence, chest pain, black stools, fainting, unsteadiness. If you notice other effects not listed above, contact your doctor or pharmacist.

Older adults may be more sensitive to the effects of this medicine. Do not give this medication to a child younger than 12 years old.

Avoid using other medicines that make you sleepy (such as cold medicine, pain medication, muscle relaxers, and medicine for seizures, depression or anxiety). They can add to sleepiness caused by baclofen. Do not use Miorel at a time when muscle tone is needed to assure safe balance and movement for certain activities. In some situations, it may endanger your physical safety to be in a state of reduced muscle tone.

Store at room temperature between 59 and 86 degrees F (between 15 and 30 degrees C) away from moisture and heat. Do not store in the bathroom.