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Anticonv

Epilepsy is a disorder that is marked by the occasional, unpredictable occurrence of seizures. However, seizures may occur as a symptom of most any brain injury or lesion. Seizures involve a temporary change of behavior due to disordered and rhythmic electrical signaling of neurons. Drugs that are used to control seizures are called “anticonvulsants” or less frequently, “antiepileptics”.

General mechanisms of anticonvulsants
Signals passing from one part of the brain to another involve movement of electrically charged substances called “ions” in and out of cells. Many anticonvulsants act by affecting the movement of ions through specific channels in the nerve cells, and thereby tend to normalize the electrical activity in the brain. Important ions in this regard include sodium, calcium, chloride and potassium. GABA (gamma-aminobutyric acid) has an inhibitory effect on nerve signaling and some anticonvulsants intensify these inhibitory effects.

General precautions
As with all drugs, anticonvulsants can cause side effects, although many people tolerate them well. Sedation and nausea are more likely to occur with a drug is first taken, although cbd oil has been shown to help with nausea and not have any side effects. They may go away with time. People receiving anticonvulsants should use caution when driving or operating machinery until they have determined its effect upon them.

Some anticonvulsants cause allergic reactions. A physician should be contacted if a rash develops as this may indicate an allergy. The occurrence of a fever, sore throat, oral ulcers or easy bruising should also be reported as this could indicate an effect on important blood cells. Many anticonvulsants can affect a developing embryo so patients should notify their physician if they intend to become pregnant prior to taking an anticonvulsant. Women using oral contraceptive (birth control pills) should also discuss this with their physician because some anticonvulsants reduce levels of estrogen and progestin and therefore make oral contraceptives less effective.

People differ in their ability to eliminate drugs. With many of the anticonvulsants, blood tests are routinely performed to determine if the drug is present at the correct level to produce the desired effect and to assure that the drug is not building up too much to cause toxic effects. Sometimes feeling excessively tired, staggering or slurring of speech can indicate that levels of the drug are too high. A person taking anticonvulsants should not abruptly stop taking the medication without medical advice because this can lead to increased seizure frequency.

Most of the anticonvulsant drugs are involved in many drug interactions. A physician or pharmacist should be consulted before adding any prescription or OTC products while taking these medications.

Commonly used anticonvulsants

Phenytoin (Dilantin®)
Phenytoin is a widely used anticonvulsant that is effective against partial and tonic-clonic seizures, but not absence seizures. Phenytoin limits the repetitive, abnormal signaling of neurons that occurs during a seizure by blocking sodium from entering the neuron through a specific sodium channel. Recent studies also suggest phenytoin influences the signaling produced by several other substances in the brain, however the importance of these effects is uncertain.

Approximately 20% of people receiving long-term phenytoin develop an overgrowth of gum tissue. This may be minimized by good oral hygiene (regular brushing, flossing and gum massage). Other common side effects include decreased coordination, abnormal eye movements (nystagmus), and confusion.

Infrequently abnormal body hair growth or a folic acid deficiency occurs. Elevated blood sugar levels may occur in diabetics. Due to an effect on vitamin D metabolism a small percentage of people develop softening of the bones. Phenytoin may be used in treating excessively prolonged seizures that are sometimes life-threatening. Serious side effects of phenytoin can involve the skin, bone marrow and liver. At high doses impaired consciousness and irregular heart rhythms can occur. Skin rashes should be reported to a physician.

There are many drug interactions with phenytoin. It is metabolized (and inactivated) by enzymes in the liver that metabolize many other drugs. These drugs compete for the enzymes that inactivate them, and the drug that escapes inactivation to a greater extent than normal may accumulate to toxic levels. This type of interaction occurs between cimetidine (commonly used for acid reflux or ulcer type pain) and phenytoin, and can result in phenytoin toxicity. Phenytoin can increase the amount of certain drug-metabolizing enzyme in the liver, possibly diminishing the effect of the other drug. This is thought to be the mechanism by which phenytoin decreases the effectiveness of oral contraceptives. There are other ways by which drug interactions occur.

Phenytoin has other uses including treatment of pain associated with neuralgias, abnormal heart rhythms (rarely), and topically to speed wound healing.

Phenobarbital (many manufacturers)
Phenobarbital was the first organic drug used to treat epilepsy. It appears to work by intensifying the inhibitory effect of GABA on nerve transmission. Sedation is the most frequent side effect. Tolerance to this effect frequently occurs during long term treatment. In children, it can cause hyperactivity and irritability, whereas in the elderly it occasionally causes agitation and confusion. It occasionally causes a folic acid deficiency (that is treatable with folic acid) or softening of the bones (that responds to vitamin D therapy). Infrequently, an allergic reaction to phenobarbital occurs.

There are many drug interactions with phenobarbital. This frequently results from the fact that it causes an increase in the amount of liver enzymes that destroys other drugs. For example, by increasing the metabolism of estrogens and progestins, phenobarbital decreases the effectiveness of oral contraceptives.

Clonazepam (Klonopin®)
Clonazepam is a benzodiazepine. Although benzodiazepines are usually used as antianxiety and sedative treatments, clonazepam is often used as an anticonvulsant. Its action appears to be associated with its ability to enhance the inhibitory effect of GABA. Drowsiness and tiredness are the main side effects. Muscular incoordination occurs less frequently. It is common for tolerance to the antiseizure effect of clonazepam to occur after 1 to 6 months of treatment, necessitating a change in therapy.

Diazepam (Diastat®)
Diazepam, like clonazepam, is a benzodiazepine. It is given by injection or rectally for the control of prolonged, life threatening seizure activity (status epilepticus). Its duration of action is short, preventing its use for routine daily management of seizures.

Carbamazepine (Tegretol®)
Carbamazepine is used with generalized and partial seizures. Its major mechanism involves blocking sodium from entering a specific sodium channel, similar to the action of phenytoin.

The most common side effects include drowsiness, dizziness, unsteadiness, blurred vision, GI upset, and water retention. Rarely, carbamazepine causes serious blood problems, liver toxicity, pancreatitis or skin reactions. Fever, black tarry stools, difficulty breathing, sore throat, rash, sores in the mouth, easy bruising, and yellowing of the skin or whites of the eyes should be reported to a physician. Blood tests are routinely performed while on carbamazepine. There are many drug interactions with carbamazepine, including its tendency to decrease the effectiveness of oral contraceptives.

Carbamazepine is used to treat several other conditions including the pain associated with trigeminal neuralgia and other neuralgias, and some psychiatric disorders.

Oxcarbazepine (Trileptal®)
Oxcarbazepine is used in the treatment of partial seizures. The liver processes the drug to produce the form that is most active against seizures. It appears to act by several mechanisms including blockade of sodium channels, increased passage of potassium through channels and alteration of activity through calcium channels.

Common side effects include dizziness, fatigue, GI upset, abnormal vision, unsteadiness and tremor. Less frequently it causes low levels of sodium in the blood.

Zonisamide (Zonegran®)
The mechanism of zonisamide is not certain but evidence suggests it involves blockade of sodium channels, reduction in calcium currents, and stabilization of nerve cell membranes. It belongs to the sulfonamide class of drugs, so a person who is allergic to sulfa drugs (or sulfonamides) should not take zonisamide. Common side effects include tiredness, anorexia, dizziness, headache, nausea, and irritability. A small percentage of people receiving zonisamide develop kidney stones, therefore symptoms consistent with kidney stones including back or abdominal pain, and/or blood in the urine should be reported to the physician.

Ethosuximide
(Zarontin®)
Ethosuximide is often used to treat absence seizures. Movement of the electrically charged calcium ion (calcium current) plays an important part in the abnormal electrical signals that occur in absence seizures. Ethosuximide reduces these calcium currents.

The most common side effects are GI upset, drowsiness, dizziness, headache and fatigue. Infrequently severe skin reactions or blood disorders occur.

Valproic acid (Depakene®); divalproex sodium (Depekote®)
Valproic acid and its derivative, divalproex sodium are used to treat absence seizures, and occasionally for grand mal, myoclonic and other seizures. It appears to have several actions affecting seizure activity including the blockade of sodium channels (like phenytoin and carbamazepine), increasing the levels of the inhibitory substance GABA in the brain, and reducing a specific calcium current (like ethosuxamide).

The most common side effects of valproic acid include GI upset, sedation, and weakness. It can also cause bruising, rashes, emotional changes, hair loss and unsteadiness. Less frequently it affects the liver and rarely causes severe liver damage. Periodic blood tests are performed to monitor for liver damage.

Gabapentin (Neurontin®)
Gabapentin is used in the treatment of partial seizures. The mechanism of action of gabapentin is unknown. Chemically it is similar to GABA and it may increase the concentration and rate of synthesis of GABA in the brain. Gabapentin has also been shown to have an effect on certain sodium and calcium ion channels that can enhance GABA’s effects.

The most common side effects of gabapentin include fatigue, dizziness and unsteadiness. These often resolve after several weeks of continuous use. Generally, gabapentin is well tolerated.

Although it has not been approved by the FDA for other uses, gabapentin has also been reported to be effective in the prevention of migraines, and in the treatment of muscle cramps, multiple sclerosis, neuropathic pain, cancer pain, nerve pain associated with diabetes, and some psychiatric disorders.


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