卢非酰胺(Rufinamid)的适应症及功效与副作用是什么？

Indications of Rufinamid

It is a new anti-epileptic drug with a triazole ring structure. It is suitable for the adjuvant treatment of epileptic seizures related to Lennox-Gastaut syndrome in children aged 1 year and above and adults.

Efficacy of Rufinamid

1. Control of epileptic seizures:

Rufinamid (Rufinamid) provides an effective and well-tolerated adjuvant treatment for patients with partial epilepsy and Lennox-Gastaut syndrome (LGS). At LGS, rufinamid is effective in controlling many types of seizures and reducing their severity.

2. Reduce the severity of epileptic seizures:

Rufinamid has good tolerance and efficacy in significantly reducing the frequency of fall attacks and total epileptic seizures. The efficacy, safety, and tolerability of rufinamide in the treatment of seizures associated with Lennox-Gastaut syndrome have been demonstrated in several other clinical trials and long-term extension studies.

3. Improve quality of life:

Rufinamid has been proven to be effective and well-tolerated in one-year-old children and adults, and can improve patients' quality of life. It is particularly effective in the treatment of fall seizures and generalized tonic-clonic seizures, and it has been suggested that it may be superior to other antiepileptic drugs as a second-line treatment for Lennox-Gastaut syndrome in patients with frequent fall attacks.

The mechanism of action of Rufinamide

Epilepsy is a brain dysfunction syndrome caused by excessive excitability of nerves in local lesions of the brain, producing paroxysmal discharges and spreading to the surroundings.

Rufinamid, a triazole derivative, was analyzed for anticonvulsant activity at the National Institutes of Health and has shown broad-spectrum anticonvulsant properties in animal models at non-toxic doses.

The main mechanism of action of Rufinamide is believed to be to inhibit sodium-dependent action potentials and regulate the activity of sodium channels, especially prolonging the inactive state of the channels.

Dosage

1. Pediatric patients (1 to 17 years old):

The recommended starting day is 10 mg/kg, administered in two equal doses. The maximum daily dose is 45g/kg, not exceeding 3200mg.

2. Adults (17 years and above):

The recommended starting daily dose is 400 to 800 mg per day, administered in two equal doses. The dose should be increased by 400-800 mg every other day, with the maximum daily dose being 3200 mg.

Side effects

The most common side effects of Rufinamide are headache, dizziness, fatigue, drowsiness and nausea. In addition, patients may also experience adverse reactions such as nystagmus, blurred vision, anxiety, constipation, indigestion, and vomiting during treatment.

Notes

1. Suicidal behavior and ideation:

Anti-epileptic drugs (AEDs), including rufinamide (Rufinamid), increase the risk of suicidal thoughts or behaviors in patients taking these drugs for any indication. Therefore, patients should be monitored during treatment for abnormal changes in mood or behavior or for depression, suicidal thoughts or behaviors.

2. Central nervous system reactions:

Caution should be exercised when combining Rufinamid with other drugs that shorten the QT interval. Patients are advised not to drive or operate machinery during treatment.

3. Allergic reaction:

If multiple organ allergic reactions occur, use of Rufinamid should be stopped.

4. Drug withdrawal reactions:

Gradually discontinue Rufinamid to minimize the risk of sudden seizures, worsening of seizures, or status epilepticus.

5. Status epilepticus persisting:

Because no standard definition is used, it is difficult to estimate the incidence of treatment-emergent status epilepticus in patients receiving rufinamide. In a controlled Lennox-Gastaut syndrome trial, status epilepticus occurred in 3 of 74 patients (4.1%) treated with rufinamid, compared with none of 64 patients treated with placebo.

6. Leukopenia:

Rufinamid has been shown to reduce white blood cell count. Leukopenia (white blood cell count < 3x109 L) was more common in 43 of 1171 patients (3.7%) treated with Bansai than in patients treated with placebo and occurred in 7 (1.2%) of all controlled trials.

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