Clonazepam is rapidly and almost completely absorbed after oral administration. Peak plasma concentrations of clonazepam are reached within 1-4 hours. The absorption half-life is about 25 minutes. Absolute bioavailability is 90%.
Clonazepam tablets is bioequivalent to an oral solution with respect to the extent of absorption of clonazepam, while the rate of absorption is slightly less from tablets.
Steady-state plasma concentrations of clonazepam are 3-fold higher with a once-daily dosing regimen than after a single oral dose; the predicted accumulation rate for the 2 and 3 times daily regimens are 5 and 7, respectively. Following multiple oral doses of 2 mg 3 times daily, stable pre-dose plasma concentrations of clonazepam averaged 55 ng/mL. The plasma concentration-dose relationship of clonazepam is linear. The desired plasma concentration of clonazepam as an anticonvulsant varies from 20 to 70 ng/ml. The plasma concentration threshold in patients with panic disorder is around 17 ng/ml.
Clonazepam is rapidly distributed in various organs and tissues of the body with preferential reuptake by brain structures. The distribution half-life is approximately 0.5-1 hour. The volume of distribution is 3 L/kg. Protein binding is 82-86%.
Clonazepam is extensively metabolized by reduction to 7-amino-clonazepam and by N-acetylation to 7-acetamino-clonazepam. Hydroxylation also occurs at the C-3 position.
Hepatic cytochrome P450 3A4 is involved in the nitroreduction of clonazepam to pharmacologically inactive metabolites.
The metabolites are present in the urine as free and conjugated compounds (glucuronide and sulfate).
The average elimination half-life is 30-40 hours. The clearance is 55 ml/min. 50-70% of a dose is excreted in the urine and 10-30% in the faeces as metabolites.
The urinary excretion of unchanged clonazepam is usually less than 2% of the administered dose.
The kinetic elimination in children is similar to that observed in adults.
Pharmacokinetics in special clinical situations:
Kidney disease does not affect the pharmacokinetics of clonazepam. Based on pharmacokinetic criteria, no dose adjustment is required in patients with renal insufficiency.
The pharmacokinetic influence of hepatic disease on clonazepam has not been investigated.
The pharmacokinetics of clonazepam in the elderly have not been established.
The elimination half-life and clearance values in neonates are in the same order of magnitude as those reported in adults.
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 abnormalities are suppressed more regularly than focal abnormalities. According to this, clonazepam has beneficial effects in generalized and focal epilepsies.
ACTIVE INGREDIENT
CLONAZEPAM 2MG
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At the moment we offer 1 shipping option:
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Most of the drugs we offer are manufactured in Mexico, some are manufactured in countries such as Germany, England, France and others, all manufactured by large multinational laboratories legally established in Mexico.
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We offer the guarantee that your product will have at least 10 months of use at the time of sale, however most of the drugs we sell have an expiration date greater than 1 to 2 years
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