Cisatracurium besilate

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Cisatracuronium synthesis

Cisatracurium besilate is a neuromuscular-blocking drug or muscle relaxant used in modern anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. It is a bisbenzylisoquinolinium agent with the chemical formula C₅₃H₇₂N₂O₁₂. Cisatracurium besilate is one of the ten isomers of the parent compound atracurium besilate, and it is often preferred due to its superior side effect profile.

Pharmacology

Cisatracurium besilate acts by competitively binding to the nicotinic acetylcholine receptors at the neuromuscular junction, inhibiting acetylcholine from binding to these receptors, which are crucial for muscle contraction. This action leads to muscle paralysis. The drug undergoes Hofmann elimination and ester hydrolysis as its primary routes of elimination, which are independent of renal and hepatic functions, making it particularly useful in patients with organ dysfunction.

Clinical Use

Cisatracurium is widely used in the operating room to provide muscle relaxation for procedures that require immobility, and in intensive care units to facilitate mechanical ventilation. Its onset of action is relatively rapid, and its duration of action is intermediate, making it suitable for both short and long procedures. The drug's hemodynamic profile is remarkably stable, with minimal effects on heart rate or blood pressure, which is advantageous in patients with cardiovascular instability.

Side Effects

While cisatracurium is generally well-tolerated, potential side effects include hypotension, hypertension, bronchospasm, and anaphylaxis, although these are rare. Its use may also be associated with the release of histamine but to a lesser extent compared to atracurium.

Dosage and Administration

The dosage of cisatracurium besilate varies depending on the desired degree of muscle relaxation and the duration of the surgical procedure or mechanical ventilation. It is administered intravenously, either as a bolus injection or continuous infusion. Dose adjustments may be necessary in patients with neuromuscular diseases or electrolyte imbalances.

Comparison with Other Neuromuscular-blocking Drugs

Cisatracurium besilate is often compared with other neuromuscular-blocking drugs such as rocuronium bromide and vecuronium bromide. Its unique pharmacokinetic profile, characterized by Hofmann elimination, makes it particularly useful in patients with renal or hepatic impairment. Additionally, its minimal cardiovascular effects make it a preferred choice in certain patient populations.