Anticonvulsant Drugs PDF

# ANTICONVULSANTS (ANTIEPILEPTIC DRUGS (AEDs)/ ANTISEIZURE DRUGS/ ANTI-SEIZURE MEDICATIONS [ASM]) Mildred T. Castillo, RN, RM, RPR, MAN - drugs/agents used in the treatment of epileptic seizures - used in the treatment of - bipolar disorder - borderline personality disorder - mood stab...

# ANTICONVULSANTS (ANTIEPILEPTIC DRUGS (AEDs)/ ANTISEIZURE DRUGS/ ANTI-SEIZURE MEDICATIONS [ASM]) Mildred T. Castillo, RN, RM, RPR, MAN - drugs/agents used in the treatment of epileptic seizures - used in the treatment of - bipolar disorder - borderline personality disorder - mood stabilizers - neuropathic pain. - suppress the excessive rapid firing of neurons during seizures - prevent the spread of the seizure within the brain ## MOA: Alter electrical activity in nerve cells (neurons) - block or stimulate ion channels, such as sodium, calcium, or potassium channels - increase activity of neurotransmitters, such as GABA ## CONVULSION ("febrile convulsions") - a sudden, violent, irregular movement of a limb or of the body - caused by involuntary contraction of muscles and associated especially with brain disorders - epilepsy - presence of certain toxins - other agents in the blood - fever in children ## SEIZURE - Sudden, uncontrolled electrical disturbance in the brain which can cause changes in behavior, movements, feelings, and consciousness. ### 3 major groups of seizures: 1. Generalized onset seizures affect both sides of the brain. 2. Focal onset seizures affect one area or side of the brain. These were previously known as partial seizures. 3. Unknown onset seizures occur when it's unknown when a seizure began. ## Common Causes Seizures is not always related to an underlying condition, can be caused by other factors as - Lack of sleep - Alcohol or drug use (amphetamines or cocaine) - Medications such as certain pain relievers, antidepressants or smoking cessation therapies, that lower the seizure threshold - Lack of oxygen during birth - High stress ## Common Side Effects Some people may experience unwanted side effects while taking antiepileptic medications, usually mild and short lived - Dizziness - Tiredness - Upset stomach - Blurry vision - Memory problems - Trouble focusing or concentrating Seizure medications can also cause more serious side effects such as: - A low number of white blood cells (cells that fight infections) - A low number of platelets (cells that help control bleeding) - Rashes - Problems with the pancreas - Aplastic anemia (a life-threatening problem with the bone marrow) - Liver damage Older adults can sometimes be at a higher risk for these side effects. ## EPILEPSY (EPILEPTIC FIT, SEIZURE, FIT, CONVULSIONS) - A neurological disorder that causes seizures or unusual sensations and behaviors repeatedly - Occurs in people of all ages Electrical activity allows signals to travel within the brain. Seizures occur when there's a sudden burst of electrical activity between brain cells (neurons). But it can also happen when there's too little activity between neurons. It can range from violently shaking to symptoms that are hardly noticeable. ## Symptoms of Epilepsy - vary greatly between individuals and depend on the type of seizure people experience - can range from violently shaking to symptoms that are hardly noticeable. ### Common symptoms - Fatigue - Depressed mood - Pain - Anxious mood - Excessive daytime sleepiness (somnolence) - can be mild to severe in form - Euphoria during aura (before the episode) - Temporary confusion - Episodes of staring blankly - Uncontrollable jerking movements or twitching of the arms and legs - Loss of consciousness or awareness ### Complications - untreated for a prolonged period it may lead to - Injuries or death due to falls - Drowning during swimming - Increased risk of accidents when driving a vehicle - Complications during pregnancy - Psychological problems such as depression, anxiety, and suicidal tendencies - Frequent and recurrent seizures without regaining consciousness, a condition known as status epilepticus - Sudden unexpected death in epilepsy (SUDEP), a rare but life-threatening complication ## ANTISEIZURE AGENTS ### Focal seizures: - GraliseTM, Horizant) - Tiagabine (Gabitril) Brivaracetam (Briviact) - Eslicarbazepine (Aptiom) - Gabapentin (Neurontin) ### Focal and generalized seizures: - Carbamazepine (Tegretol, Carbatrol, Tegretol XR, Equetro) - Oxcarbazepine (Trileptal, Oxtellar XR) - Perampanel (Fycompa) - Phenytoin (Dilantin, Phenytek) - Pregabalin (Lyrica) ### Focal and epileptic spasms: - Vigabatrin (Sabril) ### Absence seizures: - Ethosuximide (Zarontin) ### Infantile spasms: - Repository corticotropin injection (HP Acthar Gel) ## ANTICONVULSANT DRUGS - Carbamazepine (Tegretol) - Gabapentin (Neurontin) - Lamotrigine (Lamictal) - Oxcarbazepine (Trileptal) - Topiramate (Topamax) - Brivaracetam (Briviact) - Clobazam (Onfi) - Clonazepam (Klonopin) - Eslicarbazepine (Aptiom) - Ethosuximide (Zarontin) - Benzodiazepine - can stop a seizure quickly, especially in an emergency situation. - Diazepam - lorazepam - clonazepam ## ANTICONVULSANTS/ANTISEIZURES Mildred T. Castillo, RN, RM, RPH, MAN ### Aldehydes - Paraldehyde ### Aromatic allylic alcohols - Stiripentol Indicated for the treatment of Dravet syndrome- is a rare type of epilepsy. Seizures usually start in the first year of your child's life. ### Barbiturates - Barbiturates are drugs that act as central nervous system (CNS) depressants, and by virtue of this they produce a wide spectrum of effects, from mild sedation to anesthesia - Phenobarbital (primidone) – main anticonvulsant ; today is rarely used to treat epilepsy coz of sedating effect; used to stop acute convulsions or status epilepticus - Methylphenobarbital ( mephobarbital) - Barbexaclone - Phenobarbital was the main anticonvulsant from 1912 until the development of phenytoin in 1938. Today, phenobarbital in new patients since there are other effective drugs that are less sedating. Phenobarbital sodium injection can be, but a benzodiazepine such as lorazepam, diazepam or midazolam is usually tried first. Other barbiturates only have an anticonvulsant effect at anaesthetic doses. ### BenzodiazepineS - The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsive, amnestic and muscle relaxant properties. Benzodiazepines act as a central nervous system depressant. The relative strength of each of these properties in any given benzodiazepine varies greatly and influences the indications for which it is prescribed. Long-term use can be problematic due to the development of tolerance to the anticonvulsant effects and dependency. Of many drugs in this class, only a few are used to treat epilepsy: - Clobazam Notably, used on a short-term basis around menstruation in women with catamenial epilepsy( a form of epilepsy in women where seizures are exacerbated during certain phases of the menstrual cycle. - Clonazepam - Clorazepate The following benzodiazepines are used to treat status epilepticus: - Diazepam -Can be given rectally by trained care-givers. - Midazolam (N/A). Increasingly being used as an alternative to diazepam. This water-soluble drug is squirted into the side of the mouth but not swallowed. It is rapidly absorbed by the buccal mucosa. - Lorazepam - Given by injection in hospital. - Nitrazepam, temazepam, and especially nimetazepam are powerful anticonvulsant agents, however their use is rare due to an increased incidence of side effects and strong sedative and motor-impairing properties. ### Bromides - Potassium bromide. The earliest effective treatment for epilepsy. It is still used as an anticonvulsant for dogs and cats but is no longer used in humans. ### Carbamates - Felbamate This effective anticonvulsant has had its usage severely restricted due to rare but life-threatening side effects ### Cenobamate ### Carboxamides - Carbamazepine - Carbamazepine A popular anticonvulsant that is available in generic formulations. - Oxcarbazepine A derivative of carbamazepine that has similar efficacy and is better tolerated and is also available generically. - Eslicarbazepine acetate ### Fatty acids - valproates - valproic acid, sodium valproate, and divalproex sodium - Vigabatrin - Progabide - Tiagabine - Vigabatrin and progabide are also analogs of GABA - Fructose derivatives - Topiramate ### Gabapentinoids ### GABA analogues - Voltage-gated calcium channel - Gabapentinoids are used in epilepsy, neuropathic pain, fibromyalgia, restless leg syndrome, opioid withdrawal and generalized anxiety disorder (GAD). Gabapentinoids block voltage-gated calcium channels, mainly the N-Type, and P/Q-type calcium channels. - Pregabalin - Mirogabalin - Gabapentin - Gabapentin enacarbil (Horizant) - Gabapentin extended release (Gralise) - Gabapentinoids are analogs of GABA, but they do not act on GABA receptors. They have analgesic, anticonvulsant, and anxiolytic effects. ### Hydantoins - Ethotoin - Phenytoin - Mephenytoin. - Fosphenytoin ### Oxazolidinediones - Paramethadione. - Trimethadione (1946). - Ethadione. ### Propionates - Beclamide. ### Pyrimidinediones - Primidone ### Pyrrolidines - Brivaracetam - Etiracetam. - Levetiracetam - Seletracetam