Clonazepam

Clonazepam (Klonopin) is one of the most popular benzodiazepines on the market. This blockbuster drug was the 46th most prescribed medication in 2019. Google Trend data suggests interest in Klonopin is only continuing to grow. This compound is one of the easiest to find on designer drug markets.

A lot of young people are abusing Klonopin for its intoxicating effects. It’s considered more euphoric, more intoxicating, and less sedative than many of the other members of this class.

Clonazepam was first patented in 1960 by Roche, so the patents have long since expired. Many different companies now produce this drug on a commercial scale.

Clonazepam is 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively.

IUPAC Name: 5-(2-chlorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one

Cloniprazepam is a benzodiazepine drug and prodrug of the more common benzodiazepine, clonazepam (Klonopin).

Benzodiazepines like clonazepam are primarily used for treating panic disorders, anxiety, and seizures. Because of the accessibility and low price of designer benzodiazepines, people often self-prescribe or take benzodiazepines recreationally too.

There are not enough clinical studies for this drug to prove it’s safe for human consumption and carries significant risk for people looking to use this drug recreationally or off-label.

Cloniprazepam has never been approved as medicine in any country and is a designer drug [1].

IUPAC Name: 5-(2-chlorophenyl)-1-(cyclopropylmethyl)-7-nitro-3H-1,4-benzodiazepin-2-one

Metabolism: Cloniprazepam is metabolized into 7-amino-cloniprazepam, hydroxy-cloniprazepam, 3-keto-cloniprazepam, clonazepam, hydroxy-clonazepam and 7-amino-clonazepam. The active metabolites are biotransformed into inactive metabolites by the cytochrome P450 enzymes, including the CYP3A4 enzyme [2].

Duration of Effects: It starts to work in 15 to 45 minutes, and the effects of the drug last for 6 to 9 hours [2].

What Is the Dose Of Cloniprazepam?

There is no approved dose of cloniprazepam.

However, for the sake of providing as much information about this drug as possible, here are some dosage recommendations for people taking this drug off-label. This information is based on user experience and binding affinity research involving cloniprazepam.

• Light dose — 0.5 to 1 mg
• Common dose — 1 to 2 mg
• Strong dose — 2 to 4 mg

How Does Cloniprazepam Work?

Like most other benzodiazepines, cloniprazepam works by binding and attenuating GABA A.

GABA is the body’s primary inhibitory molecule. When the mind becomes anxious and active, GABA steps in to slow things down.

GABA works by binding to the receptor, causing rapid hyperpolarization and reduction in neuronal excitation [3]. In other words, it inhibits the neurons’ ability to transmit information, thus stopping the transmission of messages throughout the brain and slowing down activity.

GABAergic drugs like cloniprazepam also lead to a variety of other effects — including sedation and skeletal muscle relaxation. This occurs because GABA receptors are located throughout the peripheral and central nervous systems (throughout the body and brain) [4].

Additionally, it reduces nerve transmission in the motor cortex, suppressing the spike and wave-like brain electrical patterns and minimizing the occurrence of seizures [5, 6].

Cloniprezapam is largely metabolized into the active compound clonazepam (Klonopin).

Is Cloniprazepam Safe? Risks & Side-Effects

Cloniprazepam has never been clinically tested or approved for medical use. It’s a research chemical and carries all the same risks as other research chemicals (unknown side effects and safety profile, issues with adulteration or impurities, etc.).

Although the pharmacological profile of the drug is similar to that of other benzodiazepines like clonazepam, it has not been studied properly or confirmed to be safe.

The side effects of the drug are likely very similar to its active metabolite, clonazepam. In high concentrations, clonazepam can result in sedation, breathing problems, intoxication, and coma.

Side Effects of Cloniprazepam

Common side effects of cloniprazepam include:

• Blurred vision
• Cognition problems, such as problems with memory, thinking, and attention
• Frequent urination
• Increased salivation
• Lightheadedness, drowsiness, and dizziness
• Low mood
• Muscle weakness, balance problems, and increased risk of fall
• Sexual issues such as reduced sex drive
• Sleep disturbances

Serious side effects appear to be rare but are not impossible. If you experience any of the following side effects, visit your doctor immediately.

Serious side effects of cloniprazepam:

• Anaphylaxis
• Coma
• Confusion and slurring of speech
• Delirium
• Dementia
• Disinhibition and increased risk-taking behavior
• Extreme sedation or dizziness
• Respiratory distress
• Signs of liver problems, such as yellowish discoloration of the skin and eyes

Harm Reduction: Cloniprazepam

Since the drug is not approved for clinical use, it is better to use other approved benzodiazepines under prescription, such as clonazepam, alprazolam, and diazepam. However, the following instructions can reduce the risk associated with cloniprazepam.