Clonazepam exhibits pharmacological properties that are common to benzodiazepines, including anticonvulsant, sedative, muscle relaxant, and anxiolytic effects.
The central actions of benzodiazepines are mediated through enhancement of GABAergic neurotransmission at inhibitory synapses. In the presence of benzodiazepines, the affinity of the GABA receptor for the neurotransmitter is enhanced through positive allosteric modulation that results in increased action of released GABA on postsynaptic transmembrane chloride ion flux.
There are also some animal studies that 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, generalized spike waves. , spikes with temporal or other locations, as well as waves and irregular spikes.
Generalized EEG abnormalities are suppressed more regularly than focal abnormalities. According to this, clonazepam has beneficial effects in generalized and focal epilepsies.
Clonazepam is rapidly and almost completely absorbed after oral administration of Rivotril®. Peak plasma concentrations of clonazepam are reached within 1-4 hours. The absorption half-life is about 25 minutes. Absolute bioavailability is around 90% with large differences between individuals. Rivotril® tablets are 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. Severe toxic effects including increased seizure frequency developed in most patients with steady-state plasma concentrations greater than 100 ng/mL. In patients with panic disorders; effective concentrations of clonazepam to reduce the frequency of panic attacks were about 20 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-acetamido-clonazepam. Hydroxylation also occurs at the C-3 position. Hepatic cytochrome P450 3A4 is involved in the nitro reduction of clonazepam to pharmacologically inactive or weakly active metabolites.
The metabolites are present in the urine as free and conjugated compounds (glucuronide and sulfate).
The average elimination half-life is 30 to 40 hours and is independent of dose. Clearance is close to 55 mL/min regardless of gender, but weight-normalized values decreased with increasing body weight.
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:
Renal impairment does not affect the pharmacokinetics of clonazepam. Based on pharmacokinetic criteria, no dose adjustment is required in patients with renal insufficiency.
Hepatic insufficiency: The binding of clonazepam to plasma proteins in cirrhotic patients is significantly different from that in healthy subjects (free fraction 17.1 ± 1.0% vs 13.9 ± 0.2%).
Although the influence of hepatic insufficiency on the pharmacokinetics of clonazepam has not been further investigated, experience with another closely related nitrobenzodiazepine (nitrazepam) indicates that the clearance of unbound clonazepam might be reduced in hepatic cirrhosis.
BRAND NAME
KLONOPIN (RIVOTRIL IN MEXICO)
ACTIVE INGREDIENT
CLONAZEPAM 2MG
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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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