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Diclazepam

Diclazepam
Diclazepam
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Product Code : Nutritional-Elements
Product Description

Also known as Choloradiazepam, Diclazepam is a benzodiazepine drug that is an analogue of Diazepam. This compound was first synthesized by Leo Sternbach and his respective team at Hoffman-La Roche back in 1960`s. The effects of Diclazepam are identical to those of diazepam as it possessed Anxiolytic, hypnotic, sedative, and skeletal muscle relaxant with a few amnestic properties. When it comes to animal models, this compound has ten times more potency as compared to diazepam. 

At this moment, Diclazepam is not marketed as medication. Instead, it’s just sold as a research chemical. The potency of this compound has not been tested in humans so far. Its closest relatives are metabolite and lormetazepam. Lormetazepam itself has the potency value of x10-12 diazepam and delorazepam. 

Having the chemical name Chlorodiazepam, our offered Diclazepam acts as a synthetic depressant that is derived from the benzodiazepine class for producing various a number of effects that includes anxiety suppression, muscle relaxing, dis-inhibition, hypnotic, amnesia and anticoagulant. It was introduced to the world of medicines by Leo Sternbach with the help of his team members in the year 1960 at Hoffman-La Roche. When given to animals, properties similar to that of diazepam can be observed.

The aforementioned medicine has not yet been marketed as a medication but as a chemical for conducting various researches. This is not tested on humans, however, it comprises lormetazepam, having ten to twelve times delorazepam potency and ten times potency of diazepam. One of the important things to note is that sudden discontinuation of such medicine may cause dangerous side effects to the patient who have been consuming this on regular basis and for longer time period. If the patient wants to stop the usage then he can do this by gradually tapering the dosage and stopping the use.

Composition

As mentioned above, Diclazepam is a derivative of Benzodiazepine class. This being the reason, it contains a benzene ring with the fusion of another rings called diazepine. It contains seven members in its ring containing a couple of nitrogen constituents located at the position R1 (where the substitution is done with methyl group) and R4. Diazepine is also bonded at the position R5 to a ring called as 2-chlorinated phenyl. The position R7 is also substituted using chlorine group. An oxygen group is double bonded to the position R2 so that a ketone can be formed and this oxygen is shared by various other benzodiazepine drugs having suffix -azepam.

Chemistry

Diclazepam belongs to the class of Benzodiazepine. The Benzodiazepine has a benzene ring that is fused to a diazepine ring. Collectively, all of them forms a seven-membered ring with two nitrogen constituents which are located at R1 and R4. In R1, the Diclazepam substitute with Methyl Group. Furthermore, the Benzodiazepine ring bonds at R5 to a 2 chlorinated phenyl ring. 

The R7 of benzyl ring is substituted with a chlorine group. Apart from that, Diclazepam contains an oxygen group that is double bonded with R2 of its diazepam ring to form a ketone. Whereas oxygen substitution of R2 has been shared with other Benzodiazepine drugs with suffix azepam.

Pharmacology

The Diclazepam produces a broad array of effects as it binds to benzodiazepine receptor site and magnifies efficiency and effects of neurotransmitter gamma-aminobutyric acid by acting on its receptor. The receptor site proves to be the most beneficial inhibitory site in the brain. The modulation of this site leads to sedating effects of this drug right on the nervous system.

Subjective Effects

The following effects are based on subjective effects index and personal experiences of a few tested subjects. These effects are bound to occur only once, rarely, but that can change if the subject takes a heavy dosage of the compound. 

Physical Effects

Physical effects of Diclazepam are broken down into different elements which are progressively proportional to the dose, these effects include the names of:

  • Sedation
  • Loss of Motor Control
  • Respiratory Depression 
  • Music Relaxation
  • Dizziness

Cognitive Effects

These effects are also proportional to the taken dose. The headspace here can be described by intense sedation and controlled inhibition. Moreover, Diclazepam has a bunch of typical depressant cognatic effects that are given as below. 

  • Amnesia
  • Anxiety Suppression 
  • Thought Deceleration 
  • Disinhibition
  • Compulsive Redosing 
  • Delusion of Sobriety 
  • Information Processing Suppression

Paradoxical Effects

The Paradoxical reactions to benzodiazepines are increased seizures, aggression, anxiety, violent behavior, impulse control loss, suicidal behavior and irritability. The fact is, paradoxical effects of Diclazepam are bound to occur frequently in recreational abusers, people who are dealing with some mental disorders, children, and patients who are on high dose regimes.

So far, this compound is legalized in United Sate but in some European countries, namely the United Kingdom, it is currently unscheduled.

Physical effects

One of the most important physical effect of the aforementioned pharmaceutical product is Sedation. If alterations to the energy level is considered, this chemical has the capability for sedating and resulting in the state of lethargy. When consumed in larger quantity, the patients may feel as if they are deprived of sleep. This increases with the increase in the dosage and can result in the unconscious state of mind.

Tolerance and Addiction Potential

The patient consuming Diclazepam not only physically but mentally gets addicted to this chemical. His tolerance level will lead to the sedative-hypnotic effects within a couple of days of consuming it. This level of tolerance returns to the baseline of seven to fourteen days after the cessation. However, while observing some cases, it can be said that the effects and potential of addiction and tolerance depends upon the dosage of the patient.

Occurrence of rebound and withdrawal symptoms can be observed after steady dosage of few weeks. In order to have more information about how to taper the effect of benzodiazepines in a controlled and effective manner, kindly go through the following guide:

Discontinuation of the aforementioned product is not an easy task; it can be very risky for the patients who are on continuous and regular dosage. Sudden discontinuation can lead to seizure or hypertension or even death. Pharmaceuticals such as tramadol, which is used for minimizing the seizure threshold should be avoided while trying to discontinue the usage of Benzodiazepine. When consumed with GABAergics, it can show the effects of cross-tolerance.


Overdose

When consumed in heavier dosage or with other depressants, the condition of Benzodiazepine overdose occurs. However, it is dangerous with some depressants such as GABAergic such as alcohol, barbiturates because their working is similar, except from that it binds itself to the distinct allosteric site where GABAA receptor is present. This results in the potentiating effect on each other.

Benzodiazepines help in increasing the frequency of chlorine ion pores that are present on the GABAA receptor, however, with the help of barbiturates ion pore can be frequently opened and for longer duration of time. The overdose of such pharmaceuticals may lead to the conditions like permanent injury of brain, coma or even death of the patient, if the condition is not treated with a proper facility and on time. Apart from these, the symptoms also include slurred speech, delusions, deceleration, confusion, respiratory depression, etc. Based on certain observations, it can be said that such overdose can be treated in the hospital environment using flumaxenil, which is a GABAA antagonist.


Dangerous Interactions

Combining this product with other can be helpful but still the risk of death may persist. Bulletined below list mentions some harmful combinations, some of which may be safer when consumed in lower doses. A thorough research should be conducted for ensuring that a combination of two or more pharmaceuticals is safe for the consumption.

  • Depressants: These are combination of opioids, GHB/GBL, alcohol, 1,4-Butanediol, barbiturates, methaqualone and 2-methyl-2-butanol. The mentioned combination if consumed in excess quantity can result in respiratory depression. It relaxes muscles, increases sedation and amnesia and the patient can reach to the state of unconsciousness and vomiting with suffocation.

  • Dissociatives: The symptoms and effects are similar to that of the depressants.

  • Stimulants: One of the main reasons for combining stimulants with benzodiazepines is that it can minimize the sedative effect of benzodiazepines. But in this case, after wearing off the effect of stimulant, benzodiazepines effect highly rises.



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