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What is Diclazepam?
Diclazepam is basically a synthetic depressant substance that belongs to a chemical class of benzodiazapines, and is related to diazepam in its properties.
The benzodiazepines contain a basic benzene ring that is linked with a seven membered diazepine ring, having two nitrogen constituents located at R1 and R4. Chemically, the Diclazepam has same structure, instead at R1 position, the Diclazepam is replaced with a methyl group.
The benzodiazepine ring is linked to a ring of 2-chlorinated phenyl at R5, and also a chlorine group is attached at R7 of benzyl ring. The Diclazepam also contains a ketone group that is formed by the double bonding of oxygen group to diazepine ring at R2 position.
This characteristic oxygen substitution at R2 position is similar in all benzodiazepine drugs, hence the suffix –azepam is given to them.
In 1960 at Hoffman-La Roche, Leo Sternbach with his team work together to first conduct its synthesizes.
At present, it is only accessible through online as a research chemical. It is currently not available in market as a medicated compound because extensive investigations of potency after administration in humans aren’t been analyzed, though its two metabolites were found to be closely related to lometazepam, and potency value of ×10 greater than diazepam.
It has low toxicity relative to dose but it is an extremely potent drug, so it is dispensed as volumetric liquid dosing in a non-polar solvent to avoid inaccurate dosing and expected harm is reduced. It becomes poisonous when mixed with other depressants like opioids or alcohol.
As it belongs to benzodiazepine class, it shares the same physically and psychologically addictive and tolerance potential, so sudden discontinuation of Diclazepam produces life-threatening withdrawal symptoms. So, it is advisable that taper one dose gradually by lowering the quantity taken each day over a span of time.
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Bioactivity of Diclazepam
The Diclazepam is related to diazepam and is considered its structural analogue. But, this compound has proven to be 10 times more potent than diazepam in animal models.
It has a wide range of activities on nervous system and acts to produce hypnosis, sedation, skeletal muscle relaxation, disinhibition, anxiety suppression and anticonvulsant effects and also possesses amnestic properties.
The mechanism of action of benzodiazepines is to induce effects by binding to a benzodiazepine receptor site, that is likely to enhance the activity of a neurotransmitter GABA (Gamma Aminobutyric acid) on its
receptor sites. As it is known that this receptor site is the most abundant inhibitory set present in brain nervous system, this results in immediate sedative effect of Diclazepam.
The anti-convulsant effect exhibited by Diclazepam is based on mechanism other than binding to benzodiazepines receptors site, as it tends to bind to voltage-dependant sodium (Na) channel either completely or partially.
Expected Physical effects of Chlorodiazepam
Diclazepam tends to affect various physical and cognitive functions in a number of ways. This includes muscle relaxation, loss of motor and impulse control, dizziness, sedation, respiratory depression. The sedation potential is dangerously strong enough to induce prolong lethargic state and drag them to unconsciousness if repeated doses are given.
It provokes irritability, aggression, violence and suicidal thoughts; though it is rare and can only occur in less than 1% of general population.
Due to their effects on cognitive abilities, pronounced amnesia, disinhibition, emotionality suppression, delusions of sobriety, dream potentiation, thoughts deceleration, analysis suppression, decreased ability to process information under the influence of this drug likely to occur.
Due to these subjective effects, an urge to compulsive redosing also increases, that ultimately causes extreme dependence, rebound anxiety, residual sleepiness and decreased thinking ability. This compulsive redosing potential is seen in habitual/ recreational abusers, children or when high dose regimes are given to patients with mental disorders.
Dosage Information for Diclazepam
The Diclazepam minimum threshold dose to produce its effects starts from 0.5 – 1 mg. The dose can be increased to 1 – 2 mg to obtain mild effects, while the commonly administered dose is from 2 – 3 mg. A strong anti-depressant effect can be obtained by slightly increasing the dose to 3 – 4 mg, for the reason of being highly potent drug.
Overdose is likely to occur when taken above 4 mg, which is a medical emergency and may lead to life-threatening conditions like coma and permanent brain injury if not immediately treated. Overdose can also cause death.
After oral administration, the Diclazepam total duration of action is expected to be between 8 – 12 hours. The onset of action is achieved within 10 – 45 minutes.
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*The information contained in this article is for educational purposes only. We have tried to be as factual as possible but this doesn’t mean that the information is 100% accurate.