Instructions for use and marketing status of landiolol

Landiolol is an ultra-short-acting β1 receptor selective blocker, mainly used for heart rate control, especially suitable for postoperative or acute arrhythmia management. Because of its rapid onset of action, short half-life and high degree of controllability, it plays an important role in intensive care, perioperative management and the treatment of acute arrhythmias.

1. Pharmacological effects and mechanism of action

Landiolol is a selectiveβ1 receptor antagonist, which can effectively reduce heart rate while having a relatively small effect on blood pressure. Its main mechanism of action is to reduce the excitatory effect of sympathetic nerves on the heart by blocking cardiac β1 receptors, thereby reducing the ventricular rate in patients with sinus rhythm and atrial fibrillation. Due to its ultra-short-acting properties, the half-life of landiolol is only about four minutes, allowing it to take effect quickly in a short period of time and is rapidly metabolized after drug withdrawal without causing drug accumulation. This property makes landiolol ideal for rate control in perioperative and acute arrhythmia patients.

2. Clinical indications

Landiolol is mainly used for the following types of patients:

1. Postoperative and perioperative arrhythmias: After cardiac surgery or other major surgeries, patients may develop postoperative arrhythmias, such as postoperative atrial fibrillation (POAF). Landiolol can quickly control ventricular rate, reduce cardiac load, and reduce the risk of cardiovascular complications.

2. Acute atrial fibrillation/Atrial flutter with rapid ventricular rate: For patients with rapid ventricular rate caused by atrial fibrillation or atrial flutter, landiolol can take effect quickly and help patients restore a stable heart rate.

3. Other post-operative high heart rate states: For example, high heart rate after non-cardiac surgery due to pain, anxiety or increased sympathetic nerve activity Landiolol can effectively lower the heart rate and reduce cardiac oxygen consumption in a short period of time.

3. Usage and dosage

Landiolol is generally administered as an intravenous infusion. Common dosing regimens are as follows:

1. Patients with normal heart function:

The starting dose is9mcg/kg/minute; according to clinical indications, the dose can be increased by 9mcg/kg/minute at 10-minute intervals to a maximum dose of 36mcg/kg/minute.

2. Patients with impaired cardiac function:

The starting dose is1mcg/kg/minute; according to clinical indications, the dose can be increased by 1mcg/kg/minute at 15-minute intervals to a maximum dose of 36mcg/kg/minute.

4. Adverse reactions and precautions

Although landiolol is safer than otherbeta blockers, it may still cause some adverse reactions, including:

1. Hypotension: Due to its effect of lowering heart rate, in some patients with hypovolemia or hypotension, it may cause blood pressure to further drop.

2. Bradycardia: For some patients with a low basal heart rate, landiolol may cause excessive heart rate reduction.

3. Exacerbation of heart failure: For patients with basic cardiac dysfunction, they should be used with caution to avoid aggravation of heart failure.

4. Bronchospasm: Although its effect onβ2 receptors is weak, it should still be used with caution in patients with asthma or chronic obstructive pulmonary disease (chronic obstructive pulmonary disease).

5. Current status of listing

Landiolol was first developed by Japan's Astela Pharmaceutical Company and is marketed in Japan, Europe and some Asian countries. Landiolol was first launched in Japan in September 2002 and is sold under the brand name Onoact. It is mainly used for perioperative and acute arrhythmia management. In 2016, landiolol was approved for marketing in many European countries under the trade name Rapibloc for heart rate control after cardiac surgery; in the United States, it was approved for marketing in November 2024 and sold under the brand name Rapiblyk.

References:https://www.drugs.com/newdrugs/fda-approves-rapiblyk-landiolol-atrial-fibrillation-atrial-flutter-critical-care-setting-6410.html