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Anticonvulsants

Anticonvulsants are used to treat seizures which result from abnormal neuronal firing in the brain. Seizures can cause loss of consciousness, abnormal movements, or perceptual changes depending on their origin. They are classified based on their origin, cause, electrophysiology, or presentation. Generalized seizures include tonic-clonic, absence, myoclonic, febrile, and status epilepticus seizures. Anti-seizure drugs work via different mechanisms like blocking sodium channels, enhancing GABA, or blocking glutamate. Common classes include hydantoins like phenytoin, valproate derivatives, barbiturates, benzodiazepines, and succinimides. Status epileptic

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0% found this document useful (0 votes)
96 views34 pages

Anticonvulsants

Anticonvulsants are used to treat seizures which result from abnormal neuronal firing in the brain. Seizures can cause loss of consciousness, abnormal movements, or perceptual changes depending on their origin. They are classified based on their origin, cause, electrophysiology, or presentation. Generalized seizures include tonic-clonic, absence, myoclonic, febrile, and status epilepticus seizures. Anti-seizure drugs work via different mechanisms like blocking sodium channels, enhancing GABA, or blocking glutamate. Common classes include hydantoins like phenytoin, valproate derivatives, barbiturates, benzodiazepines, and succinimides. Status epileptic

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Deema Abuasi
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Anticonvulsants

Seizures
D Abnormal or uncontrolled neuronal discharges in the brain
D Affect
C Consciousness
C Motor activity
C Sensation
D Symptom of an underlying disorder
Convulsion

D Involuntary violent spasm of large muscles of face, neck,


arms, and legs
D Not synonymous with seizure
Epilepsy
D Seizures occurring chronically
D International Classification of Epileptic Seizures
C Partial (focal)
C Generalized
C Special epileptic syndromes
Epilepsy
D Epilepsy can cause
IJ Loss of consciousness
IJ Abnormal movements
IJ Atypical or odd behavior
IJ Distorted perceptions
D The site of origin of the abnormal neuronal firing determines
the symptoms that are produced
D If the motor cortex is involved, the patient may experience
abnormal movements or a generalized convulsion
D Seizures originating in the parietal or occipital lobe may
include visual, auditory, and olfactory hallucinations
Classification of seizures
D Seizure classification determines
treatment

D Seizures have been classified by:


IJ Site of origin
IJ Etiology

IJ Electrophysiologic correlation

IJ Clinical presentation
Generalized seizures

1.  Tonic-clonic seizures:


D Result in loss of consciousness, followed by tonic (continuous

contraction) and clonic (rapid contraction and relaxation)


phases
2.  Absence seizures:
D Involve a brief, abrupt, and self-limiting loss of
consciousness
D The patient stares and exhibits rapid eye-blinking for 3-5
seconds
Generalized seizures

3. Myoclonic seizures:
D Short episodes of muscle contractions that may recur for
several minutes
4. Febrile seizures:
D Young children may develop seizures with illness
accompanied by high fever
5. Status epilepticus:
D Life-threatening and requires emergency treatment

D Two or more seizures occur without recovery of full


consciousness between them
Known Causes of Seizures
D Infectious diseases
D Trauma
D Metabolic disorders
D Vascular diseases
D Pediatric disorders
D Neoplastic disease
Additional Known Causes of Seizures

D Medications
D High doses of local anesthetics
D Eclampsia
D Drug abuse
D Withdrawal syndromes from alcohol or sedative-
hypnotic drugs
Seizures of Unknown Etiology
D Lower tolerance to environmental triggers
IJ Sleep deprivation
IJ Flickering lights

IJ Fluid and electrolyte imbalances


Seizures in Neonates, Infants, and Children

D Congenital abnormalities of CNS


D Perinatal brain injury
D Metabolic imbalances
Later-Childhood Etiology
D CNS infections
D Neurological degenerative disorders
Adult Etiology
D Cerebral trauma or neoplasm
D Cerebrovascular disorders
EEG recordings showing the differences between normal,
absence seizure, and generalized tonic-clonic seizure tracings.
Choice of Drug Depends Upon
D Type of seizure
D Client’s history and diagnostic studies
D Pathologic process causing seizures
Mechanism of action of antiepileptic drugs
•  Blocking voltage gated channels (Na+ or Ca2+)
•  Blocking excitatory glutamate transmission
•  Enhancing inhibitory GABA impulses

•  Some antiepileptic drugs appear to have multiple


targets in CNS

•  Antiepileptic drugs (AED) suppress seizures but do not


“cure” or “prevent” epilepsy
Hydantoins
D Prototype drug: phenytoin (Dilantin)
D Mechanism of action: to densitize sodium channels
D Primary use: treating all types of epilepsy except
absence seizures
D Adverse effects: CNS depression, gingival hyperplasia,
skin rash, cardiac dysrhythmias, and hypotension
Phenytoin-Like Drugs
D Prototype drug: valproic acid
D Mechanism of action: to desensitize sodium channels
D Primary use: for absence seizures
D Adverse effects: limited CNS depression, visual
disturbances, ataxia, vertigo, headache
D Additional adverse reactions: gastrointestinal effects,
hepatotoxicity, pancreatitis
Valproic acid and divalproex
D Mechanisms of action:

IJ Sodium channel blockade


IJ Blockade of GABA transaminase (The enzyme that metabolizes
GABA)
D Broad spectrum of activity against seizures
Examples of Phenytoin-like Drugs

D Carbamazepine (for tonic-clonic and partial seizure)


D Felbamate (Broad spectrum anticonvulsant)

D Lamotrigine (effective for a wide variety of seizures)

D Valproic acid (Broad spectrum, can be used for absence


seizures)
Hydantoins and Phenytoin-like Drugs

D Desensitize sodium channels


D Sodium movement is factor that determines whether neuron
will undergo an action potential
Drugs That Potentiate GABA Action

D Include barbiturates, benzodiazepines, and miscellaneous


GABA agents
D Suppress the firing ability of neurons
Barbiturates
D Prototype drug: phenobarbital (Luminal)
D Mechanism of action: changing the action of
GABA
D Primary use: controlling seizures

D Adverse effects: dependence, drowsiness, vitamin


deficiencies, laryngospasm
Examples of Barbiturates
D Phenobarbital
D Amobarbital
D Secobarbital
D Pentobarbital
Barbiturates & primidone:
D Only long-acting ones useful in epilepsy: phenobarbital &
mephobarbital
D Can be usefully combined with phenytoin
D Broad spectrum
D More depressant than phenytoin
D Some tolerance develops
D Elevated seizure liability during withdrawal
D Primidone is second-line due to risk of agranulocytosis
Benzodiazepines
D Prototype drug: diazepam
D Mechanism of action: similar to that of barbiturates
but safer
D Primary use: for short-term seizure control
D Adverse effects: drowsiness and dizziness
Examples of Benzodiazepines
D Clonazepam
D Clorazepate
D Lorazepam
D Diazepam
Examples of Miscellaneous GABA Agents

D Gabapentin
D Primidone
D Tiagabine
D Topiramate
Succinimides
Suppress seizures by delaying calcium influx into neurons
Examples of succinimides
}  Ethosuximide Effective in treating only primary generalized absence seizures
}  Methsuximide
}  Phensuximide
Adverse effects of
an/-seizure drugs
Status epilepticus

•  Two or more seizures occur without recovery of full


consciousness in between episodes
•  May be focal or primary generalized, convulsive or
nonconvulsive
•  Requires emergency treatment
•  Fast-ac/ng medica/on such as a benzodiazepine
•  Slower-acting medication such as phenytoin,
•  Phenytoin is not compa/ble with most IV solu/ons, especially
those containing dextrose.

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