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Nondepolarizing (Competitive) Neuromuscular Blockers: Mechanism of Action

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Nondepolarizing neuromuscular blockers induce paralysis by competitively blocking nicotinic acetylcholine receptors at the muscle end plate. Examples include pancuronium, mivacurium, vecuronium, and rocuronium. These quaternary ammonium derivatives are administered intravenously, are poorly absorbed, and are excreted via the kidneys.
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Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacological Actions

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Nondepolarizing neuromuscular blockers prevent the membrane depolarization of muscle cells and inhibit muscle contraction. These are usually administered with anesthetics to achieve complete muscle relaxation. Upon administration, these drugs first block the small, rapidly contracting muscles of the face and hands, followed by the larger muscles of the trunk and the intercostal muscles. The diaphragm is the last muscle to be affected.
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Direct-Acting Cholinergic Agonists: Therapeutic Uses

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Depolarizing Blockers: Mechanism of Action

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Depolarizing blockers act on skeletal muscle fibers' membranes and induce their depolarization. Most depolarizing blockers have two quaternary N+ atoms that bind the nicotinic acetylcholine receptors and cause neuromuscular blockade within minutes.
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Directly Acting Muscle Relaxants: Dantrolene and Botulinum Toxin

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Related Experiment Video

Updated: Jul 4, 2026

3D-Neuronavigation In Vivo Through a Patient's Brain During a Spontaneous Migraine Headache

3D-Neuronavigation In Vivo Through a Patient's Brain During a Spontaneous Migraine Headache

Published on: June 2, 2014

Maximum effect of triptans in migraine? A comment.

P Tfelt-Hansen¹

¹Danish Headache Centre, Department of Neurology, University of Copenhagen, Glostrup Hospital, Glostrup, Denmark. tfelt@inet.uni2.dk

Cephalalgia : an International Journal of Headache

|June 13, 2008

Summary

High-dose subcutaneous naratriptan (10 mg) achieved an 88% pain-free response in migraine patients. This demonstrates its potential to overcome central sensitization, even in long-lasting migraine attacks.

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Area of Science:

Neurology
Pharmacology

Background:

The effectiveness of triptans for migraine treatment has been questioned.
Understanding the maximum efficacy of triptans is crucial for treatment guidelines.

Purpose of the Study:

To determine the maximum effect of a triptan in migraine treatment.
To evaluate the efficacy of high-dose subcutaneous naratriptan.

Main Methods:

A study involving subcutaneous naratriptan at a 10 mg dose was conducted.
Patient response was measured by pain-free rates.

Main Results:

An 88% pain-free response rate was observed after administration of subcutaneous naratriptan 10 mg.
This high efficacy was noted even in patients with migraine duration exceeding 4 hours.

Conclusions:

Subcutaneous naratriptan, at a high dose, can effectively manage migraine symptoms.
This treatment may overcome central sensitization associated with prolonged migraine attacks.