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Depolarizing Blockers: Pharmocokinetics

Depolarizing Blockers: Pharmocokinetics

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...

One-Compartment Open Model for IV Bolus Administration: General Considerations

One-Compartment Open Model for IV Bolus Administration: General Considerations

The one-compartment model is a pharmacokinetic tool that models the body as a single, uniform compartment, facilitating the understanding of drug distribution and elimination. This model is particularly beneficial for intravenous (IV) bolus administration, where the drug rapidly circulates throughout the body.
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant, half-life,...

Two-Compartment Open Model: IV Bolus Administration

Two-Compartment Open Model: IV Bolus Administration

The two-compartment model for intravenous (IV) bolus administration illustrates drug distribution in the body, subdividing it into central and peripheral compartments. This model operates on the concept of two-compartment kinetics. The drug's plasma concentration shows a bi-exponential decline following IV bolus administration, signaling the presence of two disposition processes: distribution and elimination.
The disparity between drug input and the sum of drug transfer rates between...

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...

One-Compartment Open Model for IV Bolus Administration: Estimation of Clearance

One-Compartment Open Model for IV Bolus Administration: Estimation of Clearance

Clearance is a key pharmacokinetic parameter that quantifies the volume of body fluid from which a drug is entirely removed within a specific time frame. It is crucial in assessing how a drug is eliminated from the body and has critical clinical applications.
In the one-compartment open model for intravenous (IV) bolus administration, clearance is estimated by dividing the elimination rate by the plasma drug concentration. This equation leverages the elimination rate constant and the apparent...

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacological Actions

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacological Actions

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.
Although all competitive neuromuscular blockers are designed...

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Related Experiment Video

Updated: Jun 22, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

[Priming versus bolus: a comparative study with different cisatracurium doses.].

Angélica de Fátima de Assunção Braga¹, Glória Maria Braga Potério, Franklin Sarmento da Silva Braga

¹Departamento de Anestesiologia, Faculdade de Ciências Médicas, Universidade de Campinas.

Revista Brasileira De Anestesiologia

|May 29, 2009

Summary

Fractional cisatracurium doses did not accelerate neuromuscular block onset compared to bolus injections. However, both methods provided acceptable tracheal intubation conditions without adverse cardiovascular effects.

Related Experiment Videos

Last Updated: Jun 22, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

Area of Science:

Anesthesiology
Pharmacology
Neuromuscular Blockade

Context:

The priming technique is explored as a method to reduce the onset time of nondepolarizing neuromuscular blockers.
Cisatracurium is a commonly used neuromuscular blocking agent in anesthesia.

Purpose:

To evaluate the onset time of maximum neuromuscular block, tracheal intubation conditions, and cardiocirculatory changes using different single or fractional doses of cisatracurium.
To compare the efficacy of priming doses versus bolus injections of cisatracurium.

Summary:

This study compared fractional versus bolus doses of cisatracurium in 80 patients (ASA I-II).
No significant difference in maximum neuromuscular block onset time was observed between fractional (priming) and bolus cisatratracurium doses.
Both administration methods resulted in acceptable tracheal intubation conditions and no significant cardiovascular changes.

Impact:

Fractional cisatracurium dosing does not offer an advantage in accelerating neuromuscular blockade onset over bolus injections.
Cisatracurium administration, whether fractional or bolus, ensures safe and effective tracheal intubation with stable hemodynamics.