CLONAZEPAM 2MG 300TABS

Clonazepam exhibits pharmacological properties that are common to benzodiazepines, including anticonvulsant, sedative, muscle relaxant, and anxiolytic effects. As with other benzodiazepines, its effects are believed to be primarily due to GABA-mediated postsynaptic inhibition, although some animal studies also show an effect on serotonin.

Data from animal models and some electroencephalographic studies in man have shown that clonazepam rapidly suppresses many types of paroxysmal activity, including spike-and-wave discharge in absence seizures (petit mal), slow spike waves, slow spike waves, generalized spikes, spikes with temporal or other locations, as well as irregular waves and spikes.

Generalized EEG normalities are suppressed more regularly than focal abnormalities. In agreement with this, clonazepam has beneficial effects in generalized and focal epilepsies.

Clonazepam is well absorbed from the gastrointestinal tract. In one study, peak blood concentrations found after 1 to 2 hours were 6.5-13.5 ng/mL when a single 2 mg oral dose of micronized clonazepam was administered to healthy adults. However, in some individuals the maximum concentration was found between 4 to 8 hours. Although the concentration of clonazepam required in plasma to obtain a therapeutic effect has not been established, some studies indicate that it may be between 20-80 ng/ml. Plasma concentrations in this range can be maintained in adults by administering clonazepam 6 mg daily in three divided doses and in children 6 to 13 years of age with 1.5-4 mg of the drug daily in three divided doses. Usually, the action starts at 20 to 60 minutes. Its duration is 6 to 8 hours in infants and young people and more than 12 hours in adults.

There is very little information on the distribution of clonazepam and it is similar to other benzodiazepines. The drug appears to cross the placenta and the blood-brain barrier.

Clonazepam is metabolized in the liver to various metabolites including 7-aminoclonazepam, 7-acetaminoclonazepam and 3-hydroxy derivatives of these metabolites, and clonazepam. Clonazepam metabolites are excreted in the urine, mainly by a first order reaction and together with their glucuronic and/or sulfate conjugates. A minimal amount of the drug is excreted unchanged.