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Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
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Depolarizing blockers are administered through intravenous injection. Succinylcholine is the most common choice of depolarizing blockers in emergency clinical practices. Although they have a rapid onset, they readily diffuse away from the motor end plate into the extracellular fluid. They are metabolized by enzymes such as liver butyrylcholinesterase and plasma pseudocholinesterases. This produces a short duration of action, typically 5-10 minutes long, unlike nondepolarizing blockers, which...
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Related Experiment Video

Updated: Apr 2, 2026

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Intramuscular Generic Injection (QLG2072) versus Haloperidol in Chinese Patients with Acute Agitation: A Phase 3

Fang Dong1,2, Zhonggang Wang3, Chao Li4

  • 1Department of Psychiatry, Beijing Anding Hospital, Capital Medical University, Beijing, People's Republic of China.

Drug Design, Development and Therapy
|March 4, 2026
PubMed
Summary

Generic olanzapine injection (QLG2072) effectively managed acute agitation in Chinese patients with schizophrenia or bipolar I disorder, showing non-inferiority to haloperidol with fewer neurological side effects.

Keywords:
acute agitationbipolar I disorderhaloperidolintramuscularolanzapineschizophrenia

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Area of Science:

  • Psychiatry
  • Clinical Pharmacology
  • Neuroscience

Background:

  • Acute agitation in schizophrenia and bipolar I disorder poses significant clinical challenges.
  • Effective and safe management options are crucial for patient stabilization and treatment adherence.

Purpose of the Study:

  • To evaluate the efficacy and safety of generic olanzapine injection (QLG2072) compared to haloperidol for acute agitation in Chinese patients.
  • To establish non-inferiority of QLG2072 to haloperidol.

Main Methods:

  • A multicenter, randomized, double-blind, phase 3 trial involving 318 Chinese patients.
  • Patients received intramuscular injections of either QLG2072 (10 mg) or haloperidol (7.5 mg) within 24 hours.
  • The primary endpoint was the change in Positive and Negative Syndrome Scale-Excited Component (PANSS-EC) score at 2 hours post-injection.

Main Results:

  • QLG2072 demonstrated non-inferiority to haloperidol, with comparable mean reductions in PANSS-EC scores (-9.37 vs -9.40).
  • Efficacy was similar across secondary endpoints, including response rates.
  • QLG2072 showed a numerically lower incidence of extrapyramidal symptoms (10.1% vs 27.2%) with comparable overall adverse events.

Conclusions:

  • Generic olanzapine injection (QLG2072) is a non-inferior alternative to haloperidol for managing acute agitation.
  • QLG2072 offers favorable neurological tolerability, supporting its use in Chinese psychiatric populations.