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, these drugs are also used for other neurological and psychiatric conditions such as anxiety disorders and bipolar disorder due to their ability to modulate neural transmission. Physicians select appropriate medications based on seizure type, patient age, and health status. Some drugs are additionally approved for migraine prophylaxis.

Types and Mechanisms of Treatment

Anticonvulsants are mainly divided into first-generation and second-generation drugs. 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 regulation 3. Enhancement of gamma-aminobutyric acid (GABA). Some drugs, such as levetiracetam, have mechanisms that are not fully understood but have been clinically proven to reduce abnormal synaptic transmission. Second-generation drugs tend to have higher specificity and generally fewer neurological side effects.

Indications

Main indications include various types of epileptic seizures, such as generalized, partial, and absence seizures. In emergencies like status epilepticus, intravenous formulations are used for urgent treatment. Additionally, carbamazepine is used for trigeminal neuralgia, while pregabalin is indicated for pain caused by peripheral neuropathy.

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

Usage and Dosage

Most medications are administered orally, requiring adherence to fixed dosages and timing to maintain therapeutic blood concentrations. For example, the starting dose of lamotrigine is usually 25-50 mg daily, gradually increased based on efficacy. In emergency situations like status epilepticus, fosphenytoin can be administered intravenously under close monitoring of blood pressure and cardiopulmonary function.

Children's doses are calculated based on weight, and adjustments are necessary for patients with liver or kidney impairment. It may take 2-4 weeks to achieve 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

The 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 high specificity, generally have a better side effect risk-benefit profile.

Extended benefits include:

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

Risks and Side Effects

Common side effects include:

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

Severe side effects: 0.1-2% of patients may develop serious skin reactions such as Stevens-Johnson syndrome, requiring immediate discontinuation. Long-term use may lead to osteoporosis or hormonal disturbances; regular bone density and adrenal function tests 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 anomaly risks; 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 doses on their own; abrupt discontinuation can trigger status epilepticus.

Interactions with Other Treatments

Concurrent use with anticoagulants (e.g., warfarin) may reduce efficacy; INR levels should be monitored. Combining with antiarrhythmic drugs (e.g., 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 inform healthcare providers of all medications taken.

Therapeutic Outcomes and Evidence

Clinical trials show that monotherapy controls seizures in 60-70% of patients, with combination therapy achieving success rates of up to 85%. Second-generation drugs like levetiracetam have a 65-75% success rate in partial seizures and less impact on cognition. Randomized controlled trials 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. Drug choice should be based on EEG patterns and seizure types; for example, valproic acid is more effective for generalized seizures than partial 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 implantation therapies
  • Nutritional therapy: ketogenic diet, effective in about 50% of children with refractory epilepsy
These alternatives should be evaluated by 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 for personalized medication selection
Discussion with the treating physician regarding risks and benefits is essential.

 

Frequently Asked Questions

Should anticonvulsant drugs be started only during seizures?

Anticonvulsants are usually taken regularly at fixed times and should not be used only during seizures. Doctors prescribe a daily fixed dose to maintain therapeutic blood levels; even if no seizures occur, continuous use is necessary. Stopping medication abruptly can 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 and often resolve after a few weeks. If symptoms are severe, contact your doctor immediately, as dose adjustment or medication change may be necessary. Avoid activities like driving or operating machinery until side effects subside. Keep a record of side effects to assist your healthcare provider's assessment.

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

Some anticonvulsants may interact with certain foods or vitamins (e.g., grapefruit, vitamin K), affecting efficacy or side effects. Patients should inform their doctors of their dietary habits and avoid self-medicating with supplements. Your doctor will provide personalized dietary advice based on your medication.

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

Regular exercise can improve physical and mental health but should avoid high-intensity or collision-prone activities, especially during initial treatment or if side effects are not stabilized. Before driving, ensure no dizziness or coordination issues are present, and follow local regulations. Some regions require seizure-free periods and medical approval before driving.

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

The duration of treatment varies; typically, medication should be continued for at least 2-4 years without seizures before gradually tapering under medical supervision. Do not stop medication abruptly, as this can cause severe rebound seizures. Before discontinuation, EEG and blood level monitoring are recommended, and a gradual reduction plan should be followed by your healthcare provider.