Anticonvulsant

Definition

Anticonvulsant drugs are medicines used to prevent or treat convulsions (seizures).

Purpose

Anticonvulsant drugs are used to control seizures in people with epilepsy. Epilepsy is not a single disease—it is a set of symptoms that may have different causes in different people. The common thread is an imbalance in the brain's electrical activity. This imbalance causes seizures that may affect part or all of the body and may or may not cause a loss of consciousness. Anticonvulsant drugs act on the brain to reduce the frequency and severity of seizures.

Some cases of epilepsy are brought on by head injuries, brain tumors or infections, or metabolic problems such as low blood sugar. But in some people with epilepsy, the cause is not clear.

Anticonvulsant drugs are an important part of the treatment program for epilepsy. Different kinds of drugs may be prescribed for different types of seizures. In addition to taking medicine, patients with epilepsy should get enough rest, avoid stress, and practice good health habits.

Some physicians believe that giving the drugs to children with epilepsy may prevent the condition from getting worse in later life. However, others say the effects are the same, whether treatment is started early or later in life.
Determining when treatment begins depends on the physician and his assessment of the patient's symptoms.
Physicians also prescribe certain anticonvulsant drugs for other conditions, including bipolar disorder and migraine headaches.

Description

Anticonvulsant drugs may be divided into several classes. The hydantoins include pheytoin (Dilantin) and mephenytoin (Mesantoin.) Ther succimides include ethosuximide (Zarontin) and methsuccimide (Celontin.) The benzodiazepines, which are better known for their use as tranquilizers and sedatives, include clonazepam (Klonopin), clorazepate (Tranxene) and diazepam (Valium.) There are also a large number of other drugs which are not related to larger groups. These include carbamazepine (Tegretol), valproic acid (Depakote, Depakene) gabapentin (Neurontin), topiramate (Topamax), felbamate (Felbatol) and several others. Phenobarbital has been used as an anticonvulsant, and is still useful for some patients. The drugs are available only with a physician's prescription and come in tablet, capsule, liquid, and "sprinkle" forms.

Recommended dosage

The recommended dosage depends on the type of anticonvulsant, its strength, and the type of seizures for which it is being taken. Check with the physician who prescribed the drug or the pharmacist who filled the prescription for the correct dosage.

Do not stop taking this medicine suddenly after taking it for several weeks or more. Gradually tapering the dose may reduce the chance of withdrawal effects.
Do not change brands or dosage forms of this medicine without checking with a pharmacist or physician. If a prescription refill does not look like the original medicine, check with the pharmacist who filled the prescription.

Precautions

Patients on anticonvulsant drugs should see a physician regularly while on therapy, especially during the first few months. The physician will check to make sure the medicine is working as it should and will note unwanted side effects. The physician may also need to adjust the dosage during this period.

Valproic acid can cause serious liver damage, especially in the first 6 months of treatment. Children are particularly at risk, but anyone taking this medicine should see their physician regularly for tests of liver function and should be alert to symptoms of liver damage, such as yellow skin and eyes, facial swelling, loss of appetite, general feeling of illness, loss of appetite, and vomiting. If liver problems are suspected, call a physician immediately.

Felbatol has caused serious liver damage and aplastic anemia, a condition in which the bone marrow stops producing blood cells. Patients taking this drug should have regular blood counts, and should stop taking the drug if there are too few red blood cells.

While taking anticonvulsant drugs, do not start or stop taking any other medicines without checking with a physician. The other medicines may affect the way the anticonvulsant medicine works.

Because anticonvulsant drugs work on the central nervous system, they may add to the effects of alcohol and other drugs that slow down the central nervous system, such as antihistamines, cold medicine, allergy medicine, sleep aids, other medicine for seizures, tranquilizers, some pain relievers, and muscle relaxants. Anyone taking anticonvulsant drugs should check with his or her physician before drinking alcohol or taking any medicines that slow the central nervous system.

Anticonvulsant drugs may interact with medicines used during surgery, dental procedures, or emergency treatment. These interactions could increase the chance of side effects. Anyone who is taking anticonvulsant drugs should be sure to tell the health care professional in charge before having any surgical or dental procedures or receiving emergency treatment.

Some people feel drowsy, dizzy, lightheaded, or less alert when using these drugs, especially when they first begin taking them or when their dosage is increased. Anyone who takes anticonvulsant drugs should not drive, use machines or do anything else that might be dangerous until they have found out how the drugs affect them.

Anticonvulsant drugs may affect the results of certain medical tests. Before having medical tests, people who take anticonvulsant drugs should make sure that the medical professional in charge knows what they are taking.
Children may be more likely to have certain side effects from anticonvulsant drugs, such as behavior changes; tender, bleeding, or swollen gums; enlarged facial features; and excessive hair growth. Problems with the gums may be prevented by regularly brushing and flossing, massaging the gums, and having the teeth cleaned every 3 months whether the patient is a child or an adult.

Children who take high doses of this medicine for a long time may have problems in school.

Older people may be more sensitive to the effects of anticonvulsant drugs. This may increase the chance of side effects and overdoses.

Special conditions

People with certain medical conditions or who are taking certain other medicines can have problems if they take anticonvulsant drugs. Before taking these drugs, be sure to let the physician know about any of these conditions:

ALLERGIES. Anyone who has had unusual reactions to anticonvulsant drugs or to tricyclic antidepressants such as imipramine (Tofranil) or desipramine (Norpramin) in the past should let his or her physician know before taking the drugs again. The physician should also be told about any allergies to foods, dyes, preservatives, or other substances.

PREGNANCY. Birth defects have been reported in babies born to mothers who took anticonvulsant drugs during pregnancy. Women who are pregnant or who may become pregnant should check with their physicians about the safety of using anticonvulsant drugs during pregnancy.

Some anticonvulsant drugs taken during pregnancy may cause bleeding problems in the mother during delivery and in the baby after delivery. This problem can be avoided by giving vitamin K to the mother during delivery and to the baby after birth.

Pregnancy may affect the way the body absorbs anti-convulsant drugs. Women who are prone to seizures may have more seizures during pregnancy, even though they are taking their medicine regularly. If this happens, they should check with their physicians about whether the dose needs to be increased.

BREASTFEEDING. Some anticonvulsant drugs pass into breast milk and may cause unwanted effects in babies whose mothers take the medicine. Women who are breastfeeding should check with their physicians about the benefits and risks of using anticonvulsant drugs.

DIABETES. Anticonvulsant drugs may affect blood sugar levels. Patients with diabetes who notice changes in the results of their urine or blood tests should check with their physicians.

OTHER MEDICAL CONDITIONS. Before using anti-convulsant drugs, people with any of these medical problems should make sure their physicians are aware of their conditions:

* liver disease
* kidney disease
* thyroid disease
* heart or blood vessel disease
* blood disease
* brain disease
* problems with urination
* current or past alcohol abuse
* behavior problems
* diabetes mellitus
* glaucoma
* porphyria
* systemic lupus erythematosus
* fever higher than 101°F (38.3°C) for more than 24 hours

USE OF CERTAIN MEDICINES. Taking anticonvulsant drugs with certain other drugs may affect the way the drugs work or may increase the chance of side effects.

Side effects

The most common side effects are constipation, mild nausea or vomiting, and mild dizziness, drowsiness, or lightheadedness. These problems usually go away as the body adjusts to the drug and do not require medical treatment. Less common side effects, such as diarrhea, sleep problems, aching joints or muscles, increased sensitivity to sunlight, increased sweating, hair loss, enlargement of facial features, excessive hair growth, muscle twitching, and breast enlargement in males also may occur and do not need medical attention unless they persist or are troublesome.

Other side effects may need medical attention. If any of these side effects occur, check with a physician as soon as possible:

* clumsiness or unsteadiness
* slurred speech or stuttering
* trembling
* unusual excitement, irritability, or nervousness
* uncontrolled eye movements
* blurred or double vision
* mood or mental changes
* confusion
* increase in seizures
* bleeding, tender, or swollen gums
* skin rash or itching
* enlarged glands in neck or armpits
* muscle weakness or pain
* ever

Other side effects are possible. Anyone who has unusual symptoms after taking anticonvulsant drugs should get in touch with his or her physician.

Interactions

Some anticonvulsant drugs should not be taken within two to three hours of taking antacids or medicine for diarrhea. These medicines may make the anticonvulsant drugs less effective. Ask the pharmacist or physician for more information.

Birth control pills may not work properly when anti-convulsant drugs are being taken. To prevent pregnancy, ask the physician or pharmacist if additional methods of birth control should be used while taking anticonvulsant drugs.

Anticonvulsant drugs may interact with many other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Anyone who takes anticonvulsant drugs should let the physician know all other medicines he or she is taking. Among the drugs that may interact with certain anticonvulsant drugs are:

* airway opening drugs (bronchodilators) such as aminophylline, theophylline (Theo-Dur and other brands), and oxtriphylline (Choledyl and other brands)
* medicines that contain calcium, such as antacids and calcium supplements
* blood thinning drugs
* caffeine
* antibiotics such as clarithromycin (Biaxin), erythromycins, and sulfonamides (sulfa drugs)
* disulfiram (Antabuse), used to treat alcohol abuse
* fluoxetine (Prozac)
* monoamine oxidase inhibitors (MAO inhibitors) such as phenelzine (Nardil) or tranylcypromine (Parnate), used to treat conditions including depression and Parkinson's disease
* tricyclic antidepressants such as imipramine (Tofranil) or desipramine (Norpramin)
* corticosteroids
* acetaminophen (Tylenol)
* aspirin
* female hormones (estrogens)
* male hormones (androgens)
* cimetidine (Tagamet)
* central nervous system (CNS) depressants such as medicine for allergies, colds, hay fever, and asthma; sedatives; tranquilizers; prescription pain medicine; muscle relaxants; medicine for seizures; sleep aids; barbiturates; and anesthetics
* alcohol
* other anticonvulsant drugs

Anxiolytics

Definition

Anxiolytics are prescription drugs used to treat and prevent anxiety disorders. Anxiety is an emotional state in which fear dominates a person's life. Drugs that are often prescribed to manage anxiety episodes are known as benzodiazepines. Probably the best-known example of a benzodiazepine is the anxiolytic diazepam. In the United States, diazepam is sold under the brand name Valium.

All together, there are six other anxiolytics approved for use in the United States. All of these medications are similar to diazepam in their chemical structures and the way they exert their beneficial anxiolytic effects. However, these drugs differ from one another in several important ways. Some drugs work faster than others, while other drugs continue their anxiolytic effects for longer periods of time. Additionally, some anxiolytics differ from one another in the way that they are eliminated from the body, and others are involved with more drug-to-drug interactions than others. In 2002, the two most commonly prescribed anxiolytics were the drugs lorazepam, sold under the trade name of Ativan, and alprazolam, sold under the brand name of Xanax.

Purpose

Diazepam and other anxiolytics reduce the frequency, severity, and duration of anxiety symptoms in individuals who have medical or psychiatric disorders associated with anxiety. Illnesses associated with anxiety symptoms include heart disease, gastrointestinal diseases, as well as diseases that affect the lungs and make breathing difficult. Anxiety may also occur in the absence of these diseases and is thought to involve abnormal function of several different neurotransmitters in a region of the brain known as the amygdala. The amygdala plays a critical role in assessing fear and responding to danger. Examples of common anxiety disorders include generalized anxiety disorder, panic disorder, and phobic disorders. Nearly 25% of the population will develop an anxiety disorder at some time during their life.

Description

Benzodiazepine anxiolytics like diazepam have similar chemical structures, including a benzene ring fused to a diazepine ring. This structure is important for anxiolytic activity. In the brain, anxiolytics are believed to enhance the actions of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter. By enhancing GABA's inhibitory actions, brain cells are unable to be stimulated by excitatory neurotransmitters, and this inhibition alleviates symptoms of anxiety.

Although benzodiazepines like diazepam alleviate symptoms of anxiety in a manner similar to older anxiolytics like barbiturates, the distinctive feature that sets benzodiazepines apart from barbiturates is the wide margin of safety associated with benzodiazepines. Unlike barbiturates, benzodiazepine anxiolytics have a wide margin of safety, meaning that the doses of benzodiazepines that cause life-threatening toxicities are considerably larger than the doses that are normally used for alleviating anxiety.

Diazepam and related anxiolytics are safe and effective medications for alleviating anxiety symptoms. Until the 1990s, these drugs were the mainstay of pharmacologic treatment for anxiety-related disorders. However, these anxiolytics do possess some unwanted properties. For example, the Drug Enforcement Administration (DEA) classifies diazepam and related anxiolytics as controlled substances because the drugs are sometimes abused, or used for recreational purposes due to their desirable anxiolytic effects. Additionally, physical dependence develops when these medications are used at high doses or for prolonged periods of time. This means that people experience unpleasant withdrawal symptoms if they abruptly stop taking their medication. Common withdrawal symptoms include anxiety, insomnia, restlessness, agitation, muscle tension, and irritability, although seizures and depression may sometimes occur. The unpleasant withdrawal effects that are experienced when discontinuing these medications cause people to continue using the drugs to avoid unpleasant effects. Because these drugs are sometimes used for non-medicinal purposes and are associated with unpleasant withdrawal symptoms, benzodiazepine anxiolytics are now typically prescribed only for short-term treatment of anxiety disorders, until other anxiolytics like buspirone or selective serotonin reuptake inhibitors (SSRIs) begin working.
Recommended dosage

The usual adult dosage of diazepam is 2–10 mg taken by mouth two to four times a day. In addition to oral tablets, diazepam is also available as an oral liquid or as an injection that can be given either intramuscularly or intravenously to individuals with severe anxiety symptoms.

Dosages for anxiolytics that are chemically related to diazepam vary. Examples include alprazolam given by mouth in dosages of 0.25–0.5 mg three times a day, or lorazepam taken by mouth in dosages of 0.5–2 mg two or three times a day.

The anxiolytic effects of diazepam occur in as little as 15 minutes, but only last for two or three hours. These features make diazepam an ideal drug for quickly eliminating acute anxiety attacks. On the other hand, lorazepam's anxiolytic effects are a little slower in onset but tend to persist for more than six hours. As a result, lorazepam may be better suited to prevent anxiety in people with generalized anxiety disorder.

Elderly patients may be more sensitive to the side effects of diazepam and related anxiolytics than younger adults. As a result, initial doses are usually reduced and increased slowly in the elderly to avoid excessive sedation and other unwanted side effects.

Precautions

Paradoxically, excitement, rage, anger, or hostility may occur in individuals taking anxiolytics for their calming effects. These reactions may occur secondarily to the relief of anxiety and usually occur within the first two weeks of therapy. If these reactions occur, anxiolytic therapy should be stopped.

Because suicidal tendencies may be present in patients who also have accompanying depressive disorders, only small amounts of anxiolytic agents should be dispensed at any given time to minimize the likelihood of intentional drug overdoses.

Side effects

Diazepam and related anxiolytics are often associated with drowsiness, sedation, confusion, and difficulty maintaining balance. These effects are more pronounced at the beginning of therapy and after dosage increases. People should avoid driving or performing tasks that require alertness until they know how the drugs will affect them.

When using anxiolytics like diazepam, fainting or dizziness sometimes occurs when a person stands up suddenly. Blurred vision may also occur.

When anxiolytics are used in high doses or taken with other drugs that depress the actions of the brain, such as alcohol or barbiturates, the normal breathing responses of the body may be interrupted and patients may stop breathing. For this reason, alcohol and other CNS depressants should be avoided in people taking diazepam and related anxiolytics. It is also best to avoid anxiolytics in those persons with a prior history of drug abuse or those who are suicidal.

Withdrawal symptoms will occur if patients stop taking anxiolytics suddenly. Patients should only discontinue using diazepam and related anxiolytics at the advice of their physician and the dosage of the drugs should be reduced slowly to avoid withdrawal effects.

Interactions

Diazepam will increase the drowsiness or sedative effects of other central nervous system depressants like alcohol or barbiturates. These combinations should be avoided.

Certain drugs, especially those eliminated by the liver, may interfere with the elimination of diazepam from the body. Anticonvulsants, antidepressants, numerous antibiotics, and cimetidine inhibit the elimination of most anxiolytics from the body, causing higher blood levels and increased side effects.