Anticonvulsants

Overview of Treatment

Anticonvulsant drugs are a class of medications specifically used to treat epileptic seizures and control abnormal neuronal discharges. Their primary goal is to suppress excessive excitation of neurons in the brain, preventing seizures from impacting patients' lives. Since the 20th century, anticonvulsants have become the cornerstone of epilepsy treatment, suitable for patients of all ages, and can also serve as adjunct therapy before and after epilepsy surgery.

In addition to epilepsy treatment, these drugs are also expanded in application due to their ability to modulate neural transmission, including conditions such as anxiety disorders and bipolar disorder. Physicians select appropriate medications based on seizure type, patient age, and health status. Some drugs are also approved for migraine prophylaxis.

Types and Mechanisms of Treatment

Anticonvulsant drugs are mainly divided into first-generation and second-generation medications. First-generation drugs, such as Phenytoin and Carbamazepine, primarily work by blocking sodium channels to reduce neuronal hyperexcitability. Second-generation drugs, like Lamotrigine and Gabapentin, target the regulation of neurotransmitters (such as GABA and glutamate) or stabilize cell membrane potentials.

The mechanisms of action can be categorized into three main types: 1. Sodium channel blockade 2. Calcium channel modulation 3. GABA enhancement. Some drugs, such as Levetiracetam, have mechanisms that are not fully understood but have been clinically proven to reduce abnormal synaptic transmission. Due to their higher specificity, second-generation drugs generally have fewer neurological side effects.

Indications

The primary indications include various types of seizures, such as generalized seizures, focal seizures, and absence seizures. For emergency conditions like status epilepticus, intravenous medications are used for urgent management. Additionally, carbamazepine is used for trigeminal neuralgia, while Pregabalin is suitable for pain management caused by peripheral neuropathy.

Second-line indications include treatment of manic episodes in bipolar disorder, relief of anxiety symptoms, and prophylactic treatment of migraine headaches. Physicians tailor personalized treatment plans based on core symptoms and comorbidities.

Usage and Dosage

The vast majority of these drugs are administered orally, requiring adherence to fixed dosages and timing to maintain therapeutic blood concentrations. For example, the starting dose of Lamotrigine is typically 25-50 mg daily, gradually increased based on efficacy. In emergency situations, such as status epilepticus, fosphenytoin can be administered intravenously, with close monitoring of blood pressure and cardiopulmonary function.

Children’s doses are calculated based on body weight, and adjustments are necessary for patients with liver or kidney dysfunction. It may take 2-4 weeks to reach therapeutic effects; physicians will adjust treatment based on seizure diaries and EEG results. Due to differences in half-life, short-acting drugs require multiple doses per day, while long-acting formulations can be taken once daily.

Benefits and Advantages

Main therapeutic effects include:

  • Reducing seizure frequency by 70-90%
  • Improving cognitive function and daily activity capacity
  • Some drugs have multiple mechanisms of action, suitable for complex epilepsy
Second-generation drugs, due to their higher specificity, generally have a better side effect risk-benefit profile.

Extended benefits include:

  • Reducing accidents caused by seizures
  • Enhancing social functioning and mental health
  • Some medications can also improve comorbid anxiety or depression symptoms associated with epilepsy

Risks and Side Effects

Common side effects include:

  • Dizziness, drowsiness, or coordination disturbances
  • Skin rashes (especially with first-generation drugs)
  • Hepatic dysfunction or hematological effects
Some drugs may induce suicidal tendencies or mood swings, requiring regular psychological monitoring.

Serious side effects: 0.1-2% of patients may develop severe skin reactions such as Stevens-Johnson syndrome, requiring immediate discontinuation. Long-term use may lead to osteoporosis or hormonal imbalances; regular checks of bone density and adrenal function are recommended.

Precautions and Contraindications

Contraindications include:

  • Allergy to active ingredients or excipients
  • Severe hepatic or renal failure
  • Use with certain drugs like vitamin D deficiency or warfarin (contraindicated)
Use during pregnancy may increase congenital abnormalities; women of childbearing age should consult before conception.

During treatment, alcohol intake should be avoided, and blood drug levels should be monitored regularly. Patients with epilepsy should not adjust dosages independently; abrupt discontinuation may trigger status epilepticus.

Drug Interactions

Concurrent use with anticoagulants (such as warfarin) may reduce efficacy; INR levels should be monitored. Combining with antiarrhythmic drugs (like amiodarone) may enhance sedative effects. Some drugs induce hepatic enzymes, reducing the effectiveness of oral contraceptives.

When combined with antipsychotics, caution is needed for drug accumulation toxicity; for example, combining with olanzapine may increase drowsiness. Herbal medicines like St. John’s Wort may lower drug concentrations; patients should disclose all medications used.

Therapeutic Efficacy and Evidence

Clinical trials show that monotherapy controls seizures in 60-70% of patients, with combination therapy achieving success rates up to 85%. Second-generation drugs like LEV have a treatment success rate of 65-75% for focal seizures and have less impact on cognition. RCTs confirm that Lamotrigine can reduce migraine attack frequency by 50%.

Long-term follow-up indicates that regular medication use can lead to seizure freedom in 70% of patients, but 10-20% have drug-resistant epilepsy. Choice of medication should be based on EEG patterns and seizure types; for example, valproic acid is more effective for generalized seizures than focal seizures.

Alternative Options

When medications are ineffective, consider:

  • Neurostimulation therapies: Vagus nerve stimulation (VNS) or deep brain stimulation
  • Surgical treatments: Resection of epileptogenic focus or multiple site implantation
  • Nutritional therapy: Ketogenic diet, effective in about 50% of children with refractory epilepsy
Alternative options should be evaluated at epilepsy centers.

Non-pharmacological options include:

  • Repetitive transcranial magnetic stimulation (rTMS) for focal epilepsy
  • Traditional Chinese medicine acupuncture as an adjunct for symptom relief
  • Genetic testing to guide personalized medication choices
Discussion of risks and benefits with the treating physician is essential.

 

Frequently Asked Questions

Should anticonvulsant drugs only be started during an epileptic seizure?

Anticonvulsant medications are typically taken regularly at fixed times and should not be used only during seizures. Physicians prescribe a fixed daily dose to maintain therapeutic blood levels. Discontinuing medication without guidance may increase seizure risk. Patients should set reminders to ensure timely medication intake.

What should I do if I experience side effects like dizziness or drowsiness from anticonvulsants?

Mild dizziness or drowsiness may be initial side effects that usually improve after a few weeks. If symptoms are severe, contact your doctor immediately, as dose adjustments or medication changes may be necessary. Avoid high-altitude activities or driving until side effects subside, and keep a record of symptoms for physician assessment.

Are there dietary restrictions or supplements to consider while taking anticonvulsants?

Some anticonvulsants interact with certain foods or vitamins (such as grapefruit or vitamin K), affecting efficacy or side effects. Patients should inform their doctors of their dietary habits and avoid self-medicating with supplements. Dietary advice will be tailored based on the medication used.

Do I need to be cautious about exercise or driving during anticonvulsant therapy?

Regular exercise can improve physical and mental health, but high-intensity activities or those prone to collisions should be avoided, especially early in treatment or when side effects are not stable. Before driving, ensure no dizziness or coordination issues, and follow local regulations. Some regions require medical approval for epileptic patients to drive.

How long do I need to continue anticonvulsant medication? Can I stop on my own?

The treatment duration varies; generally, medication should be taken regularly for at least 2-4 years without seizures before considering gradual withdrawal. Do not stop medication abruptly, as this can trigger severe rebound seizures. Before discontinuation, EEG and blood level monitoring are necessary, and a gradual tapering plan should be developed by a healthcare professional.