卢非酰胺(Rufinamid)的药物相互作用都有哪些？

Author: Medicalhalo

Release time: 2025-10-19 11:44:20

(Rufinamid) has drug interactions with sodium 2-propylvalerate and hormonal contraceptives. Use together will reduce the effects of the two drugs. The drug interactions of Rufinamid are explained in detail below.

About Rufinamid

Rufinamide is a triazole derivative. It was approved by the US FDA in 2008 and was launched on the market. It is mainly used for the adjuvant treatment of epileptic seizures related to Lennox Gastant syndrome (LGS) in children and adults aged 4 years and above. Relevant studies have proven that rufinamide is effective in bipolar disorder. During the treatment of epilepsy, as the dosage of rufinamide increases, the patient's cognitive function will not be significantly affected, which has become one of the main advantages of the drug.

It is currently believed that rufinamide mainly exerts clinical effects by regulating the activity of brain sodium ion channels. When the concentration is greater than 10 mol/L, it has no significant effect on monoamines, epinephrine, histamine, acetylcholine, AMPA kainate, glycine, NMDA or GA-BA neurotransmitter receptor systems.

Drug interactions of rufinamide

1. Effects of rufinamide on other anti-epileptic drugs

Population pharmacokinetic analysis of steady-state average concentrations of carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate and sodium valproate showed that typical rufinamide Cavss levels have little effect on the pharmacokinetics of other AEDs. Any effects, when they occur, are more pronounced in the pediatric population.

Table 1 summarizes drug interactions between Rufinamid and other AEDs.

Table 1: Summary of drug interactions between Rufinamid and other anti-epileptic drugs

Automated external defibrillator jointly managed	Effects of Rufinamide on AED concentration a)	Effects of AED on the concentration of rufinamide
amide carbamide	Reduce7% to 13%b)	Reduce19% to 26% Dependent on carbamazepine dose
lamotrigine	No effect
Sedative and Sleeping Agent	Increase8% to 13%b)	Reduce25% to 46%c) d) ' Independent of the dose or concentration of phenobarbital
phenytoin	Increase7% to 21%b)	Reduce25% to 46%c) d) ' Not related to dose or concentration Phenytoin
topiramate	No effect	No effect
Sodium 2-propylvalerate	No effect	Increase< 16% to 70%c) Depends on the concentration of sodium valproate
predione	Not investigated	Reduce25% to 46%c) d) ' Not related to the dose or concentration of primidone
Benzodiazepinese)	Not investigated	No effect

2. Effects of other anti-epileptic drugs on rufinamide

Powerful cytochrome P450 enzyme inducers, such as carbamazepine, phenytoin, primidone and phenobarbital, appear to increase the clearance of Banzel (see Table 1). Given that most of the clearance of rufinamid occurs via CYP-independent pathways, it is unlikely that the decreases in plasma concentrations of carbamazepine, phenytoin, phenobarbital, and primidone are entirely attributable to the induction of P450 enzymes. Other factors explaining this interaction are unclear. Any effects, regardless of where they occur, are likely to be more pronounced in the pediatric population.

Patients who are stable on rufinamid before taking sodium valproate should start treatment with low-dose sodium valproate and gradually increase to a clinically effective dose. Likewise, patients taking sodium valproate should start rufinamid at a dose less than 10 mg/kg per day (pediatric patients) or 400 mg per day (adults).

3. Effect of Rufinamid on hormonal contraceptives

Female patients of childbearing age should be warned that Rufinamid and hormonal contraceptives may reduce the effectiveness of this contraceptive method. It is recommended to use other non-hormonal forms of contraception while using Rufinamid.

Use of rufinamide in special populations

1. Use in the elderly

Since the clinical studies of Rufinamid did not include a sufficient number of subjects aged 65 and above, it is not yet possible to determine whether elderly patients respond to the drug differently from younger subjects. In general, careful dosage selection is required when using drugs in elderly patients, usually starting at the lower end of the dosage range, because elderly patients may have decreased liver, renal, or cardiac function and may have more frequent concomitant medical conditions or other medications. However, the pharmacokinetics of rufinamid in the elderly are similar to those in younger subjects.

2. Kidney damage

For patients with severe renal impairment (creatinine clearance < 30 mL/min), the pharmacokinetics of rufinamid are similar to those in healthy subjects. Therefore, dose adjustments should be considered when administering rufinamid to patients receiving dialysis therapy.

3. Liver damage

Rufinamid is not recommended for patients with severe hepatic impairment (Child-Pugh score 10 to 15). Rufinamid should be used with caution in patients with mild (Child-Pugh score 5 to 6) to moderate (Child-Pugh score 7 to 9) hepatic impairment.