Anticonvulsant drugs

Overview
Summary
Anticonvulsant drugs are classified as either classic or newer anticonvulsants. Newer anticonvulsants are usually better tolerated and have a broader
therapeutic range than classic anticonvulsant drugs. The choice of drug is guided by the type of seizure. First-line treatment for focal
seizures includes e.g., lamotrigine or levetiracetam, while valproate is used for generalized seizures. All anticonvulsants have dose-dependent side
effects on the central nervous system such as somnolence and nausea, but some agents have more specific side effects (e.g., gingival
hyperplasia caused by phenytoin).

Besides their importance in anti-epileptic therapy, anticonvulsants are also used for pain

management (e.g., carbamazepine or gabapentin as coanalgesics) or as mood stabilizers in bipolar disorders (valproate).

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Agent Indication Mechanism of action Side effects

Classic
anticonvulsants
First-line long-
term treatment
for tonic-
clonicgeneralized
Valproate seizures
Partial (focal) seizures
Absence seizures
Myoclonic seizures
Bipolar disorder
Gastrointestinal upset (e.g.,
abdominal discomfort)
Hepatotoxicity (rare)
Teratogenicity (see pharmacotherapy
Inhibits GABA during pregnancy)
transaminase→ ↑ GABA→ Tremor
decreased neuronal excitability Sedation
Ataxia
Inactivates Na+ channels Alopecia
Pancreatitis
Skin rash
Agranulocytosis
Weight gain

First-linetreatment
for tonic-
clonicgeneralized
Carbamazepine and focal seizures
First-linetreatment
of trigeminal
neuralgia
Nausea
Skin rash
Hyponatremia, hyperhydration,
and edema (due to SIADH)
Blood count abnormalities
(e.g., agranulocytosis, aplastic
anemia)
Inactives Na+channels Teratogenicity during the first
trimester (see pharmacotherapy
during pregnancy)
Diplopia
Ataxia
Hepatotoxicity
Stevens-Johnson syndrome
Induces cytochrome P-450

Gastrointestinal symptoms
Allergic skin reactions
Inhibition of voltage-gatedcalcium
First-line for absence (urticaria, Stevens-
Ethosuximide channels (T-type) in neurons of
seizures Johnson syndrome)
the thalamus
Fatigue
Headache

First-linetreatment
for tonic-
clonicseizures and
for status
Phenytoin epilepticusprophylaxis
Only rarely used
for long-
term treatment
of focal seizures.
Gingival hyperplasia
Stevens-Johnsonsyndrome
Hirsutism
Drug-induced lupus erythematosus
Osteopathies
Inactivation of Na+ channels Megaloblastic anemia
Zero-orderelimination(i.e., Nystagmus, diplopia, ataxia
constant rate of drug eliminated) Peripheral neuropathy
Teratogenic: fetal hydantoin
syndrome
Induction of cytochrome P-
450 enzymes
 Agent Indication Mechanism of action Side effects
First-line for status Indirect Sedation and dependence
Benzodiazepine epilepticus GABAAagonist → ↑ GABA action (See benzodiazepines for details)
Overview
First-
linetreatment for long-
Exanthema,
termtherapy of focal
exfoliative dermatitis, Stevens-
seizures
Johnson syndrome (slow dose
Second-line treatment
increase necessary to prevent skin
Lamotrigine for generalized
and mucous membrane reactions)
seizures and absence
Rarely hepatotoxic or nephrotoxic
seizures
Blurry vision
Mood
Gastrointestinal symptoms
stabilizerfor bipolar
disordertreatment

First-linetreatment
in neonates Sedation
Tonic- GABAAagonist → ↑ GABA action Tolerance and dependence
Phenobarbital clonicgeneralized Cardiorespiratory depression
seizures Induces cytochrome P-450
Focal seizures

First-
linetreatment for long- Somnolence, nausea
Levetiracetam termtherapy of focal Psychiatric symptoms (e.g., changes
Newer seizures in personality)
anticonvulsants Generalized seizures

Second-linetreatment
Inhibition of voltage-gatedcalcium Dry mouth
for focal seizures
channels (T-type and L-type) Somnolence, nausea
Gabapentin Polyneuropathy
in neurons of the thalamus Ataxia
Post-herpeticneuralgia

Refractory focal Inhibits GABA
Irreversible vision loss
Vigabatrin seizures transaminase→ ↑ GABA

Focal and
generalized tonic- Somnolence
Blocks voltage-gatedNa+
clonicepilepticseizures Glaucoma
Topiramate channels
Migraineprophylaxis Weight loss
Idiopathic intracranial ↑ GABA Kidney stones
hypertension

Gastrointestinal upset: nausea,

Focal seizures, with or vomiting, diarrhea
Inhibits GABAreuptake
Tiagabine without impairment of → ↑ GABA Insomnia
consciousness Drowsiness
Weight changes