Clonazepam

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Cat Number

API0233025

CAS Number

1622-61-3

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Product Detail Description Scientific Support Customer Q&A

CAS Number

1622-61-3

EINECS

216-596-2

Synonyms

Klonopin; Rivotril; Ro 5-4023

Molecular Formula

C15H10ClN3O3

Molecular Weight

315.71

Smiles

C1C(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])C(=N1)C3=CC=CC=C3Cl

Appearance

White to off-white crystalline powder

Melting Point

237-240℃

Boiling Point

524.5℃

General Description

Clonazepam is a long-acting, high-potency benzodiazepine approved for treating seizure and panic disorders. As a Schedule IV controlled substance, it carries boxed warnings regarding risks of concomitant use with opioids, abuse potential, and dependence.

Mechanism of Action

Clonazepam acts as a positive allosteric modulator of GABA-A receptors, enhancing the inhibitory effects of gamma-aminobutyric acid by increasing chloride channel opening frequency. This produces neuronal hyperpolarization and reduced firing, decreasing CNS excitability.

Application

Clonazepam is FDA-approved for monotherapy or adjunctive treatment of Lennox-Gastaut syndrome, akinetic, and myoclonic seizures, and for panic disorder with or without agoraphobia.

Nour SA, et al. developed and optimized clonazepam-loaded polymeric micelles for intranasal delivery to enable rapid brain targeting in status epilepticus. Using a central composite design, formulations incorporating Pluronic® P123 and L121 were optimized for entrapment efficiency, particle size, and release characteristics. The optimized formulation demonstrated significantly enhanced brain targeting in biodistribution studies using 99mTc-radiolabeled clonazepam, with a drug targeting efficiency of 242.3% and a nose-to-brain direct transport percentage of 99.30%. Pharmacodynamic studies showed prolonged seizure protection compared to intranasal solution, with minimal histopathological changes.

Fig. 1 DSC thermograms of CZ, Pluronic® P123, Pluronic® L121, and the optimized polymeric micelle (PM7). (Nour SA, et al., 2016)

References

Nour SA, et al. Intranasal brain-targeted clonazepam polymeric micelles for immediate control of status epilepticus: in vitro optimization, ex vivo determination of cytotoxicity, in vivo biodistribution and pharmacodynamics studies. Drug Deliv. 2016;23(9):3681-3695.

Does Clonazepam require protection from light during long-term storage?

Yes, it is photosensitive. Prolonged exposure to light can cause degradation and discoloration. It must be stored in amber or opaque containers in a dark environment.

What is the recommended storage temperature for Clonazepam?

Store at controlled room temperature, between 15°C and 30°C. Avoid refrigeration unless specified, as condensation upon warming could introduce moisture and cause hydrolysis.

Is Clonazepam prone to hydrolysis of its nitro group?

The nitro group is stable in the solid state. However, in solution, particularly under light, reduction or other transformations can occur. Formulated products require strict pH and light control.

How is the purity of Clonazepam verified as a controlled substance?

We use a validated HPLC method to monitor related benzodiazepine impurities, ensuring compliance with pharmacopoeial standards and regulatory requirements for Schedule IV drugs.