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Clonazepam

HOME >> API >> API List1 >> Clonazepam >> Pharmalogy

PHARMALOGY
Clonazepam CAS Number 1622-61-3

The precise mechanism by which clonazepam exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Convulsions produced in rodents by pentylenetetrazol or, to a lesser extent, electrical stimulation are antagonized, as are convulsions produced by photic stimulation in susceptible baboons. A taming effect in aggressive primates, muscle weakness and hypnosis are also produced. In humans, clonazepam is capable of suppressing the spike and wave discharge in absence seizures (petit mal) and decreasing the frequency, amplitude, duration and spread of discharge in minor motor seizures.

Clonazepam's primary mechanism of action is via modulating GABA function in the brain, via the benzodiazepine receptor which in turn leads to enhanced GABAergic inhibition of neuronal firing. In addition clonazepam decreases the utilization of 5-HT (serotonin) by neuronsand has been shown to bind tightly to central type benzodiazepine receptors.Because of its strong anxiolytic and anticonvulsant properties, it is said to be among the class of "highly potent" benzodiazepines.The anticonvulsant properties of benzodiazepines are due to enhancement of synaptic GABA responses and inhibition of sustained high frequency repetitive firingBenzodiazepines, including clonazepam, bind to mouse glial cell membranes with high affinity.Clonazepam decreases release of acetylcholine in cat brainand decreases prolactin releaseBenzodiazepines inhibit cold-induced thyroid stimulating hormone (also known as TSH or thyrotropin) releaseBenzodiazepines acted via micromolar benzodiazepine binding sites as Ca2+ channel blockers and significantly inhibit depolarization-sensitive calcium uptake in experimentation on rat brain cell components.

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