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Summary Pharmacology - Drugs for Seizures/Epilepsy

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DRUGS FOR SEIZURES/EPILEPSY
Epilepsy
• Sudden, excessive, and synchronous discharge of cerebral neurons → may result to loss of consciousness, abnormal movements, atypical or odd behavior, and
distorted perceptions that are of limited duration but recur if untreated.
• An excitatory effect which affects another neuron.
• Symptoms depends on the site of firing the neurons.
§ If the origin is from the Parietal & Occipital Lobes → patient may experience: Visual hallucination, Auditory hallucination, or Olfactory hallucination.
Etiology
Primary Seizure Genetic Epilepsy
- Cannot pinpoint where exactly it came from and why the patient is experiencing seizure. - Comes from genetic mutations.
• No specific anatomical cause for the seizure and most common • Inherited abnormality in the CNS
o Sometimes, it can come from trauma or neoplasm
Secondary Seizure Structural/Metabolic Epilepsy
- Can pinpoint possible precipitating factors. - The causes are related to secondary seizures. Same factors may cause the development of
• Precipitated by several reversible disturbances such as tumors, head injury, meningeal structural/metabolic epilepsy.
infection, rapid withdrawal from alcohol • Illicit drug use, tumor, head injury, hypoglycemia, meningeal infection, rapid withdrawal from
alcohol
o If the cause can be determined or corrected → sometimes medication is not
necessary

Classification
Focal Seizure
Only one lobe of the brain hemisphere is affected or that causes the focal seizure.
May progress to become a generalized tonic-clinic seizure
Simple Partial Complex Partial
- Usually, sensory distortion happens/shown - More on mental aspect which causes mental distortions → hallucination (sensory hallucinations)
• Caused by a group of hyperactive neurons exhibiting abnormal electrical activity and are followed by consciousness that is altered
confined to a single locus in the brain. • Complex sensory hallucination and mental distortion
• Electrical discharge does not spread, and patient does not lose consciousness or awareness. • Motor dysfunction may involve chewing movements, diarrhea, and/or urination
• Abnormal activity of a single limb or muscle group that controlled by the region of the brain • Consciousness is altered
experiencing the disturbance.
Generalized Seizure
May begin locally and then progresses to include abnormal electrical discharges throughout both hemispheres.
May be convulsive or non-convulsive and patient usually has an immediate loss of consciousness
Tonic-Clonic (Grand Mal) Absence (Petit Mal)
- Most dramatic form of seizure - Cannot easily be detected
- Has Tonic phase and Clonic phase: • Ex. The patient is speaking then suddenly he stopped then blinks for 3 – 5 seconds before he
• Tonic → continuous contraction (convulsion) normally speaks again.

, • Clonic → Convulsion speeds up then immediately falls (relaxes) - Brief, abrupt, and self-limiting loss of consciousness
o May result to loss of consciousness. - Patient stares and exhibits rapid eye-blinking, which lasts for 3 – 5 seconds
- Seizures may be followed by a period of confusion and exhaustion due to depletion of glucose and - Distinct three-per-second spike and wave discharge seen on electroencephalogram
energy stores
Myoclonic Febrile
- Short episodes of muscle contractions that may recur for several minutes - Generalized tonic-clonic convulsions of short duration with accompanying high fever.
• Rapid jerking which mostly focuses on the hands • Tonic-clonic + high temperature
- Generally, occur after awakening and exhibit as brief jerking of the limbs - Mostly seen in children
Status Epilepticus
- Rapidly recurrent
- Seizure that lasts longer than 5 minutes or having more than 1 seizure within a 5-minute period without returning to a normal level of consciousness
• Convulsive – jerking motions, grunting, sounds, drooling and rapid eye movements or
• Non-convulsive – appear confused as like daydreaming, unable to speak and behaving in an irrational way.
o More distressful jerking + drooling

Antiseizure Drugs: MOA
• The only thing that seizure medications do is to suppress (manage) it; it does not actually treat/cure.
• Reduces seizures through mechanisms as blocking voltage-gated channels (Na+ or Ca+2) enhancing inhibitory y-aminobutyric acid (GABA)-ergic impulses and
interfering with excitatory glutamate transmission.
• What triggers seizures is the excessive firing of the neurons → inhibit the excessive firing (depolarization) by preventing the excitatory response
• GABA – promotes GABA → influx of chloride → hyperpolarization → decreases firing
• NMDA (excitatory receptor) – involved in the entry of calcium
• AMPA (excitatory receptor) – involved in the entry of sodium
§ If glutamate binds to either NMDA or AMPA receptor → triggers entry of either sodium or calcium
§ Sodium and calcium are both involved in action potential
• If sodium and calcium entered the cell → propagation of action potential
o Must be inhibited so that there will be no excessive firing of neurons
• Some drugs have multiple targets within the CNS.
Blocks Na Blocks Ca GABA inhibitory Mixed
ANTISEIZURES DRUGS
Medication Specific Information General (MOA, Side Effects, Interaction) Indications, Side Effect Management & More
1. Benzodiazepines Specific drugs MOA
• Clonazepam and Clobazam Binds to GABA inhibitory receptors → reduced
o Adjunctive therapy for particular firing rate.
types of seizure
• Diazepam

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