Friday, May 27, 2016

4:54:00 PM

Epilepsy Medications

This post is puplished to help people with epilepsy (seizure disorders) become more familiar with the medications they are taking. Any change in physical or mental health in someone taking these epilepsy medications should be reported promptly to the doctor.

If you are unhappy with your level of seizure control or are having unpleasant side effects from the epilepsy medications, do not assume you have to put up with it. Tell your doctor. Ask about other medications or treatments which may be appropriate for you.
Epilepsy Medications or seizure medications are drugs which decreases the frequency of seizures in people with epilepsy. Treats the symptom of seizures, not the underlying epileptic condition
Epilepsy Medications

Epilepsy Medications or Seizure Medications


  • Carbamazepine (Tegretol, Carbatrol)


A favorite partial seizure medicine in the developed world. Carbamazepine affects sodium channels, and inhibits rapid firing of brain cells.

Long-acting forms such as:
  1. Carbatrol or 
  2. Tegretol-XR can be given once a day. 
Potential side effects include: 
  1. GI upset, 
  2. weight gain, 
  3. blurred vision, 
  4. low blood counts, 
  5. low blood sodium (hyponatremia). 
Carbamazepine causes a rash rate of a few percent, sometimes even the dangerous rash called Stevens-Johnson syndrome. People of Asian descent with HLA-B*1502 antigen are more at risk. 
Typical adult dose is 400 mg tid. Patients start with 200 mg bid and each week, and increase by 200 mg daily to about 400 mg three times a day.

  • Clonazepam (Klonopin)


Clonazepam is a member of the epilepsy medications class known as benzodiazepines, to which
  1. diazepam (Valium), 
  2. lorazepam (Ativan), 
  3. clorazepate (Tranxene), 
  4. alprazolam (Xanax) also belong. 
Benzodiazepines are used as:
  1. anti-seizure drugs(epilepsy medications), 
  2. sedatives, 
  3. tranquilizers 
  4. and muscle relaxants. 
Benzodiazepines increase the effectiveness of GABA, the brain’s main inhibitory neurotransmitter. Clonazepam is more long-acting against seizures than are diazepam or lorazepam. 
Side effects of clonazepam include: 
  1. sedation, 
  2. thinking/memory impairment, 
  3. mood changes, 
  4. addiction. 
More so than most, its effects wear off over time. 
A typical adult dose is 0.5-1.0 mg three times a day. Patients usually start with 0.5 mg at night, and if they are not too sleepy the next day, increase to 0.5 mg twice a day. A week later, if seizures persist, Increase to 0.5 mg three times a day. 

  • Gabapentin (Neurontin)


Gabapentin has the reputation of being a safe but not particularly powerful anti epileptic medication. The effectiveness criticism probably is because it is often prescribed at too low a dose.
The drug probably works by influencing transport of GABA and effects on calcium channels. It has no drug interactions, is not metabolized in the liver and it does not bind to blood proteins.

Side effects are:
  1. unsteadiness, 
  2. weight gain, 
  3. fatigue, 
  4. dizziness. 
Typical adult dose is 300-600 mg three times a, but doses can be up to 1200 mg three times a day. I often start at 300 mg per day, sometimes in one dose or with 100 mg pills, and increase over a month or two to the full dose. Gabapentin often is used also for chronic pains of certain types.

  • Lacosamide (Vimpat)


Lacosamide is a new antiepileptic drug , for partial and secondarily generalized seizures. It is chemically related to the amino acid, serine. Vimpat blocks sodium channels (but in a different way from other seizure medicines), and this block reduces brain excitability.

Side effects include:
  1. dizziness, 
  2. headache, 
  3. nausea or 
  4. vomiting, 
  5. double vision, 
  6. fatigue, 
  7. memory or mood problems. 
Vimpat may affect the internal organs, blood counts or heart rhythm, but these potentially serious side effects are infrequent. 
The recommended starting dose is 50 mg twice daily, increased each week by an extra 100 mg, to the recommended maintenance dosage of 100-200 mg twice a day.

  • Lamotrigine (Lamictal)


A broad-spectrum alternative to VPA, with a better side effect profile. However, Lamotrigine may not be as effective for myoclonic seizures. Lamotrigine works by several mechanisms including blocking release of glutamate, the brain’s main excitatory neurotransmitter.

It has the usual side effects of:
  1. dizziness 
  2. and fatigue, 
  3. usually mild cognitive (thinking) impairment. 
Severe medical side effects are unusual. The practical side effect issue is rash, occurring in several percent of people who take it, especially if the dose is increased too fast. Therefore, it takes a couple of months to get up to the typical adult dose of 200 mg twice a day. 
Patients usually start at low doses, adding one 25 mg pill daily each week on a two-times-a-day schedule until taking 100 mg twice a day. If there is no rash at that time, one is unlikely. I then switch my patients to 100 mg pills and increase to 200 mg twice a day over the next few weeks. This is slower than the package insert suggested starting dose, however, a slow starting dose is especially important if the patient also takes valproic acid (Depakote), to reduce risk for rash. Lamotrigine is also used for mood stabilization.

  • Levetiracetam (Keppra)


Levetiracetam is one of the more used medicines in seizure clinics because it probably is effective for a broad-spectrum of seizures types, has a relatively low incidence of causing thinking/memory problems, and can be started at 500 mg twice a day, which is an effective dose. It has no drug interactions, is not metabolized in the liver and it does not bind to blood proteins.

The most common side effects are:
  1. dizziness, 
  2. fatigue, 
  3. insomnia, but the more troublesome problem can be irritability and mood changes. 
This may occur to some degree in up to a third of those taking the medicine. A typical adult dose is 500 - 1500 mg twice a day. Patients usually start with 250 mg twice a day and increase the next week to 500 mg twice a day, then the next week to 1000 mg in the am plus 500 mg in the pm, then the week after to 1000 mg twice a day. This is slower than the package insert suggested starting dose.

  • Lorazepam (Ativan)


Lorazepam is similar to clonazepam in dosage and action, but it is not as long-acting. It is usually used as a ‘rescue medication’ for patients who frequently have clusters of seizures. It works reasonably quickly when taken orally and anti-seizure effect lasts for 2-6 hours.

Typical adult dose is 0.5-2.0 mg orally or as needed. A lorazepam concentrate, 2 mg per ml, can be taken as 1 ml liquid under the tongue in urgent situations.

  • Oxcarbazepine (Trileptal)


Slightly different from carbamazepine, it is at least as effective, and may have fewer side effects, except for more risk for low blood sodium (hyponatremia). It is more expensive than generic carbamazepine.

A typical adult dose is 600 mg twice a day. Patients start with 150 mg twice a day, and increase by 150 mg daily each week. This is slower than the package insert suggested starting dose. An immediate switch from carbamazepine to full-dose oxcarbazepine is possible in some cases.

  • Phenobarbital (Luminal)


The old-timer: very inexpensive and effective in a single daily dose. Phenobarbital increases the effect of GABA, the main inhibitory neurotransmitter in the brain.

Watch for sedation, thinking/memory problems and depression. Phenobarbital can cause long-term bone problems. Phenobarbital is mildly addictive and requires slow withdrawal. During pregnancy, there is a significant rate of birth defects.

Typical adult dose is around 100 mg per day. I start my patients with 30 mg pills, 2 or 3 at bedtime, to allow for future dosage flexibility. The target serum level is 10-40 mcg per ml. See information on phenobarbital.

  • Phenytoin (Dilantin)


The most used anti epileptic medication by general physicians in the US, less so by epilepsy doctors, because of the side effects. Phenytoin alters brain cell sodium channels, which has the effect of limiting rapid firing of the brain cells. It is inexpensive.

Common side effects are:
  1. unsteadiness and moderate cognitive problems. 
  2. There are long-term potential cosmetic (body/face hair growth, skin problems), 
  3. and bone problems (osteoporosis). 
  4. Phenytoin causes a rash rate of a few percent, sometimes even the dangerous rash called Stevens-Johnson syndrome. 

Typical adult dose is 300-400 mg per day, usually with 100 mg pills. Phenytoin can be started quickly in an emergency with intravenous administration, or a large dose of capsules if an immediate effect is required. Small changes in phenytoin dose can cause large changes in serum drug levels, so the blood levels can be hard to regulate. The target serum level is 10-20 mcg per ml.

  • Pregabalin (Lyrica)


A relative of gabapentin, it may be better, and can be given twice a day. Some believe that it is more effective against seizures than is gabapentin. Pregabalin has no drug interactions, no liver metabolism, no protein binding, and similar side effects to gabapentin.

Typical adult dose is 150 - 600 mg bid. Patients start with 50 mg daily, adding 50 mg each week on a twice a day basis until taking 300 - 600 mg per day. This is slower than the package insert suggested starting dose, but avoid sedation. Pregabalin often is used also for chronic pains of certain types. 

  • Rufinamide (Banzel, Inovelon in Europe)


Banzel is approved for add-on treatment of children age 4 and older and adults with the Lennox Gastaut Syndrome. This syndrome can include seizure types such as atonic (drop) seizures, tonic (stiffening) seizures, myoclonic (brief jerking) seizures, or staring (absence) seizures, as well as partial seizures. Banzel works on sodium channels in brain cells, in a way to make them less excitable.

Common side effects include:
  1. headache, 
  2. dizziness, 
  3. fatigue and sleepiness, 
  4. double vision and tremor (trembling). 
People who have the “short QT syndrome,” a rare heart rhythm irregularity, should not take Banzel. The drug comes as 200 and 400 mg tablets. Children will usually be started at doses of approximately 10 mg/kg/day administered in two equally divided doses. Dosing can increase by adding additional 10 mg/kg amounts every two days, until the child is taking 45 mg/kg/day or a maximum of 3200 mg/day, divided into two doses each day. See information on Banzel.

  • Topiramate (Topamax)


A good broad-spectrum anti epileptic medication (i.e., treats all types of seizures). Topiramate has several mechanisms, including blocking the enzyme carbonic anhydrase, which affects the acidity of brain tissue. More acidity (to a point) suppresses seizures.

Side effects include:
  1. thinking and memory problems in about 1/3rd, 
  2. renal stones in 1-2%, 
  3. rare cases of glaucoma (increased eye pressure) 
  4. and weight loss. 
Typical adult dose is 150-200 mg twice a day. Patients usually start with one 25 mg pill daily, adding another pill each week on a two-times-a-day schedule until taking 100 mg twice a day. If there are no significant side effects, then switch to 100 mg pills and increase to 200 mg twice a day over the next few weeks. Topiramate also is used for migraine headache prevention.

  • Valproic acid (Depakote)


This is the standard broad-spectrum anti epileptic medication (treats all types of seizures) and no other epilepsy medication is more effective for generalized seizure types. VPA has effects on GABA (at least in very high doses), and a neurotransmitter called NPY to block seizures, and maybe also on calcium channels.

VPA has significant side effects:
  1. weight gain, 
  2. tremor, 
  3. hair loss, 
  4. GI upset, 
  5. blood count decreases, 
  6. hepatic or pancreatic injury, 
  7. bone weakness over time (osteoporosis), 
  8. birth defects in up to 10% (folic acid can help to prevent them). 
Typical adult dose is 250 mg - 500 mg three times a day, but dose can be higher. An extended release form can be taken once a day.

  • Vigabatrin (Sabril)


Vigabatrin is approved in the US, but official package insert information has not become available. Vigabatrin is a “designer drug,” made to block metabolism of GABA, the brain’s main inhibitory neurotransmitter. Sabril has been used for over a decade in many countries, and it is effective for partial seizures, with or without secondary generalization. It also may be very effective for infantile spasms, a serious type of seizures in young children.

Release in the US was delayed because the drug is toxic to the retina of the eye in up to 30% of people who take it long-term. This toxicity can result in permanent loss of peripheral vision. Regular vision testing is recommended for all people on this drug.

A typical regimen begins with 500 mg twice a day, and can increase over a month or two to 1500 mg twice a day.

  • Zonisamide (Zonegran)


Zonisamide is rather similar in its coverage and side effects to topiramate, except glaucoma is not usually listed. Some find less cognitive impairment than with topiramate but this is individual and dose-dependent.

Typical adult dose is 100-300 mg twice a day. Patients usually start with one 25 mg pill daily, adding 25 mg each week on a two-times-a-day schedule until taking 100 mg twice a day. If there are no significant side effects, Then switch to 100 mg pills and increase to 200 mg twice a day over the next few weeks.

Others:
  1. acetazolamide (Diamox), 
  2. diazepam rectal gel (Diastat), 
  3. ethosuximide (Zarontin), 
  4. felbamate (Felbatol), 
  5. primidone (Mysoline), 
  6. tiagabine (Gabitril)
Taking Control
  • There are several important things people with epilepsy can do to give their treatment the best chance of success.
    • Do take your epilepsy medications regularly.
    • Do learn about your epilepsy medications. Ask your doctor or pharmacist for information about the epilepsy medications and possible side effects. If you obtain information from other sources, such as friends or the Internet that causes you concern, check with your doctor or pharmacist.
    • Do not change the dose without consulting your doctor. Too much epilepsy medications may lead to side effects. Too little epilepsy medications may increase your seizures.
    • Be honest. If you have been missing doses or having side effects, say so. If you are not honest with your doctor, he or she cannot properly help you.
    • Do not ever stop your epilepsy medications abruptly. This can result in a dramatic increase in your seizures, which can be dangerous to you.
    • Do ask your doctor what to do if you miss a dose of epilepsy medications. Do not assume if you miss a few doses that you can make them up by taking them all at once, or when you feel a seizure coming on. What you need is a certain amount of epilepsy medications, taken regularly, to keep a constant level of epilepsy medications in your blood.
    • Do not try other people’s pills, even if a friend says they are working well for her. Instead, get the name of the epilepsy medications and ask your doctor if it might be right for you.
    • Never mix large amounts of alcohol with epilepsy medications. Ask your doctor if it would be safe for you to consume small amounts of alcoholic beverages.
    • Be cautious when starting a new medication or making a major change in dose. Do not drive until you know how the new drug or different dose will affect you. It may make you drowsy.
    • Give your memory some help if you have trouble remembering to take your epilepsy medications. Reminders include daily or weekly pill boxes, watches with alarms, notes where you can see them, and computer calendar reminders. It may be helpful to take your epilepsy medications at the same time you regularly perform other daily tasks, such as brushing your teeth, after meals or before bedtime. 
    • Do not run out of epilepsy medications. Set up a schedule for reordering so it becomes automatic. Request refills several days in advance. If ordering epilepsy medications by mail, leave enough time for delays in delivery.
    • Take enough epilepsy medications with you when going on vacation to last until you return. Carry a separate copy of your prescription and the phone number of your doctor so you can easily replace any medicine that gets lost. Do not keep pills in checked baggage when traveling by plane. Take them with you.
    • Keep all epilepsy medications out of reach of young children. Keep epilepsy medications in the drug store bottle with a childproof cap and label on it. If using a pill box, keep it in a safe place if there are children around. Grandparents and others should remember that toddlers can be very curious.
    • Know the name, strength of pills and dosage of your medication. Write it down so you can refer to it.
    • Keep all epilepsy medications away from direct sunlight, dampness and high humidity. A bathroom cabinet or windowsill over the kitchen sink are usually not good places to keep medicines.
Remember to tell all your doctors, as well as dentists and pharmacists, that you are taking an antiepileptic medications. It is a good idea to bring all your epilepsy medications' bottles with you to doctor visits.