Epilepsy is a chronic neurological disorder characterized by recurrent seizures due to abnormal neuronal excitability and hypersynchronous cortical activity. Antiepileptic drugs (AEDs) remain the cornerstone of epilepsy management, functioning primarily by modulating ion channels, neurotransmitter systems, and synaptic excitability to suppress seizure activity. This study investigates the physiological mechanisms, clinical efficacy, and future directions of AED therapy, with a focus on novel agents offering improved safety and efficacy profiles. A randomized controlled trial was conducted on 200 epilepsy patients to compare conventional AEDs (carbamazepine, valproate) with novel AEDs (brivaracetam, cenobamate). The novel AED group demonstrated a statistically significant reduction in seizure frequency (68.5% vs. 47.3%, p<0.01) and superior cognitive preservation (MoCA score 26.5 ± 2.2 vs. 24.1 ± 2.4, p=0.02) compared to conventional AEDs. Furthermore, the incidence of adverse effects such as fatigue, dizziness, and weight gain was significantly lower in the novel AED group (p<0.05). These findings suggest that novel AEDs selectively target neuronal ion channels and neurotransmitter systems with greater precision, leading to enhanced therapeutic outcomes. Despite these advantages, drug resistance remains a challenge, affecting up to 30% of epilepsy patients. Future research should focus on precision medicine, pharmacogenomics, and emerging neuromodulation strategies such as optogenetics and brain stimulation techniques. This study provides new insights into optimizing AED therapy for improved seizure control and patient quality of life.