Zexing Landiolol Hydrochloride for Injection

1. Indications and Usage
Acute Supraventricular Tachycardia:
Emergency treatment of tachyarrhythmias (specifically Atrial Fibrillation, Atrial Flutter, and Sinus Tachycardia) occurring during surgery or in the perioperative period .
Sepsis-Associated Tachycardia:
Management of tachycardia associated with sepsis (depending on regional labeling).
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Recommended Dosage:
Initial Titration: Administer by continuous infusion (typically with a syringe pump).
Standard Rate: Start at 0.01 to 0.04 mg/kg/min.
Titration: Adjust the rate based on heart rate (HR) and blood pressure (BP) response.
Maximum Dose: Generally should not exceed 20 to 40 µg/kg/min (depending on clinical indication) .
Critical Administration Instructions:
Reconstitution: Dissolve the vial content with 5 mL or more of 0.9% Sodium Chloride Injection(Normal Saline) or 5% Dextrose Injection .
Concentration Limit: Do not exceed a concentration of 10 mg/mL to avoid local irritation or skin necrosis .
Equipment: Use a precision infusion pump (syringe pump) for accurate control .
3. Mechanism of Action
Selective Beta-Blockade:
Landiolol is a β1-selective adrenergic receptor antagonist. It has a high affinity for cardiac β1 receptors (approx. 251 times higher than β2 receptors) .
Rapid Onset and Offset:
It blocks the effects of catecholamines (epinephrine/norepinephrine) on the heart, reducing heart rate and myocardial contractility.
Unique Feature: It has an extremely short half-life (approx. 4 minutes) due to rapid hydrolysis by esterases in the blood and liver, allowing for rapid titration and quick offset of effects upon discontinuation .
4. Safety and Warnings
Hypotension and Bradycardia:
The most common adverse reactions are a drop in blood pressure and excessive slowing of heart rate.
Action: Continuous monitoring of ECG and BP is mandatory. Discontinue if severe hypotension or bradycardia occurs .
Contraindications:
Cardiogenic shock.
Second or third-degree AV block and Sick Sinus Syndrome.
Decompensated heart failure.
Untreated pheochromocytoma.
Metabolic acidosis (e.g., diabetic ketoacidosis) .
5.Adverse Reactions and Clinical Research
Most Common Adverse Reactions:
Hypotension, bradycardia, nausea, headache, and injection site reactions.
Serious Adverse Events:
Shock, cardiac arrest, and complete AV block (rare) .
Clinical Research Highlights:
Studies confirm its efficacy in rapidly controlling heart rate in atrial fibrillation/flutter with a safety profile that allows for immediate cessation of effects if hemodynamic instability occurs .
6.Drug Interactions
Calcium Channel Blockers:
Concomitant use with verapamil or diltiazem may have additive effects, increasing the risk of severe hypotension or bradycardia .
General Anesthetics:
May enhance the myocardial depressant effects of anesthetics (e.g., propofol, fentanyl) .
Insulin/Antidiabetics:
May mask signs of hypoglycemia (tachycardia) .
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Landiolol Hydrochloride.
Appearance: White to off-white lyophilized powder.
Packaging: Single-use vial (e.g., 20 mg or 100 mg).
Storage: Store at 2°C to 8°C (Refrigerate), protected from light .