What is Clonazolam?
Clonazolam, also known as clonitrazolam, belongs to benzodiazepine class. Benzodiazepines compounds typically has a central benzene ring that is fused with a seven membered diazepene ring, having two nitrogen groups located at position R1 and R4. In clonazolam, the benzyl ring at R8 is replaced with an NO2- (nitro) group and the diazepine ring is linked to a 2-chlorinated phenyl ring at R6 while a 1-methylated triazole ring is linked with a diazepine ring. This fused triazole ring is characteristic class of benzodiazepine, known as triazolobenzodiazepines and identified with the “-zolam” suffix. Clonazolam also belongs to a subclass of benzodiazepine, known as nitrobenzodiazepine, as the name indicates that contains a nitro group (NO2-). This class also includes drugs such as clonazepam and flunitrazepam.
Clonazolam is basically a novel research chemical compound, which has been derived from the two FDA-approved drugs clonazepam and alprazolam. Its first synthesis can be dated back to 1971, where it was regarded as the most active compound out of a series of tested compounds. No detailed information is present about this substance, but it has lately become easily accessible from online chemical vendors for research purposes, under the popular name of ‘designer drug’. It is mostly found as volumetric dosed solution or on blotter-paper, for the reason being extremely potent. Clonazolam and flubromazolam were reported to pose greater risks, in contrast to other designer benzodiapenes drugs due to their substantial sedative effect on an oral dosage of as low as 0.5mg.
It has been regarded as a highly potent drug, showing its effects as small as in micrograms, which may prove harmful for human consumption. As it belongs to the benzodiazepine class, it has same dependence and addiction-causing potential and life-threatening withdrawal effects may occur on discontinuation of drug, so it is advisable to gradually lower the dose taken per day.
Bioactivity of Clonazolam
It possesses anxiolytic, sedative, hypnotic, muscle relaxing, amnesic properties and produce anti-convulsant effects on administration.
Being a benzodiazepine, it exhibits a number of effects when bound to the receptor site of benzodiazepine. They potentiate the effects of the neurotransmitter GABA (gamma amino butyric acid), due to which inhibitory effects occurs, causing sedation.
The mechanism of anti-convulsant action has been linked to binding to voltage-dependant sodium (Na) channels completely or partially, rather than binding to benzodiazepine receptor as seen when causing sedation.
It is also reported to antagozises the convulsive effects induced by thiosemicarbazide and pentobarbital.
Expected Physical Effects of Clonazolam
The clonazolam have effects on nervous system causing sedation, dizziness, , respiratory depression, loss of motor control, muscle relaxation, increased libido and have ability to reduce severity or frequency of seizures (in epilepsy). Due to its effects on nervous system, an increase in aggressive behavior, anxiety, irritability, violent and suicidal thoughts may likely occur in less than 1% of general population. These effects are intensified while following high-dosage regimes in patients having mental disorders, children or if habitually used, such as by recreational abusers.
It can also have effect on cognition, causing amnesia (memory loss), difficulty thinking and processing information, impulsivity, decreased consciousness and sleepiness. Also it can manifest delusions of sobriety in individuals under the effects of this drug.
The after-effects of this drug are reported, such as rebound anxiety, dreamy state potentiation or suppression, residual sleepiness, altered mental activity, thought deceleration and disorganization, irritability and lack of motivation.
Dosage Information for Clonazolam
The primal route of administration is oral. Its total duration of action is expected to be between 6-10 hours, with onset of action showing within 10-30 minutes of dose administration.
The dosage range can be described as starting from a threshold level of 50 – 75 µg, light dose of 75 – 200 µg, common dose of 200 – 400 µg, strong dose of 400 – 1000 µg and heavy dose which is above 1000 µg.
Overdose of benzodiazepine is treated as medical emergency as it leads to coma, brain injury or death if left untreated or not treated properly.
Other Names for Clonazolam
Clonitrazolam, 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-1][1,4]benzodiazepine, designer drug, sledgehammer.