Lorazepam

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Cat Number

API0233186

CAS Number

846-49-1

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Product Detail Description Scientific Support Customer Q&A

CAS Number

846-49-1

EINECS

212-687-6

Synonyms

Ativan, Temesta, Loraz

Molecular Formula

C15H10Cl2N2O2

Molecular Weight

321.16

Smiles

C1=CC=C(C(=C1)C2=NC(C(=O)NC3=C2C=C(C=C3)Cl)O)Cl

Appearance

White crystalline powder

Melting Point

166-168℃

Boiling Point

533.8℃

General Description

Lorazepam is an intermediate-acting benzodiazepine approved for short-term relief of anxiety symptoms, anxiety-related insomnia, anesthesia premedication, and status epilepticus.

Mechanism of Action

Lorazepam acts as a positive allosteric modulator of GABA-A receptors, potentiating the inhibitory effects of gamma-aminobutyric acid in the central nervous system. This enhances chloride channel conductance, producing neuronal hyperpolarization and decreased excitability in limbic and reticular formations.

Application

Lorazepam is FDA-approved for management of anxiety disorders, preoperative sedation and amnesia, and treatment of status epilepticus. For status epilepticus, the recommended IV dose is 4 mg administered at 2 mg/minute, with onset of action within 1 to 3 minutes.

Gonzalez D, et al. combined data from two pediatric clinical trials to characterize the population pharmacokinetics of intravenous lorazepam in 145 infants and children (aged 3 months to 17 years) with status epilepticus. A two-compartment model with allometric scaling based on body weight best described the data, with younger age associated with slightly higher weight-normalized clearance. Typical parameter estimates were as follows: central volume of distribution 0.879 L/kg, clearance 0.115 L/h/70 kg (age-adjusted), peripheral volume 0.542 × central volume, and intercompartmental clearance 1.45 L/h/70 kg. Simulations confirmed that uniform dosing of 0.1 mg/kg (maximum 4 mg) achieves plasma concentrations of 50–100 ng/mL, a range previously associated with effective seizure control.

Fig. 1 Observations versus population and individual predictions from the final population pharmacokinetic model. (Gonzalez D, et al., 2017)

References

Gonzalez D, et al. Population Pharmacokinetics and Exploratory Pharmacodynamics of Lorazepam in Pediatric Status Epilepticus. Clin Pharmacokinet. 2017;56(8):941-951.

Does Lorazepam require protection from both light and moisture?

Yes, it is sensitive to both. Light can cause photodegradation, and moisture can lead to hydrolysis of the imine bond. Storage in tightly sealed, light-resistant containers is essential.

What is the recommended storage temperature for Lorazepam?

Controlled room temperature (20-25°C) is suitable. Avoid temperature extremes, as heat can accelerate degradation and cold can cause condensation upon warming.

Is Lorazepam stable in propylene glycol-based formulations?

Yes, it is commonly formulated in propylene glycol for injectable solutions. We provide compatibility data to support formulation development, including stability at various temperatures.

How is the degradation product 2-amino-2',5-dichlorobenzophenone monitored?

This primary hydrolysis product is specifically quantified using a stability-indicating HPLC method, ensuring it remains below the established limit throughout the product's shelf life.