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Medication Class Examples Indications Characteristics Pharmacokinetics Mechanism of Action Adverse Effcts Contraindications

May exacerbate myoclonic


and absence seizures.
Highly bound to plasma
proteins—low
Drugs that compete for
bioavailability.
protein binding sites can
increase levels of free
Hepatic elimination
phenytoin.
(conversion to inactive Coarsening of facial
Non-sedative. metabolites) varies with features, gingival
Drugs that induce or inhibit
dose, such that above hyperplasia, osteomalacia,
Phenytoin Many types of seizures. Inhibits voltage-gated sodium channels. hepatic enzymes can
Fosphenytoin (prodrug) the therapeutic range, and fetal developmental
impact plasma
can be used parenterally. small dose incremements abnormalities (category D
concentrations of
produce disproportional teratogen).
phenytoin.
rises in serum drug
concentration and
Phenytoin induces
hepatic elimination
hepatic enzymes to
follows zero-order
decrease the plasma
kinetics.
concentrations of other
drugs.

May exacerbate myoclonic


or absence seizures.
Hyponatremia, leukopenia,
fetal developmental
Patients with blood or liver
anomalies (category D
Highly bound to plasma disorders.
teratogen), and Stevens-
proteins—low
Johnson syndrome (life-
bioavailability. Drugs that induce hepatic
threatening rash).
Inhibits voltage-gated sodium channels by enzymes may increase
Carbamazepine Many types of seizures.
Engages in auto- prolonging the inactivation period. carbamazepine
Patients of Asian origin are
induction, causing the metabolism.
more likely to develop
half-life of the drug to fall
carbamazepine-induced SJS
significantly over time. Carbamazepine induces
(HLA B*1502 ) and should be
hepatic enzymes to
screened before initiating
Modifiers of Ionic decrease the plasma
treatment.
Conductance concentrations of other
drugs.

Fewer adverse effects than


Patients taking diuretic
Oxcarbazepine Many types of seizures. Similar to above. Similar to above. carbamazepine, but more
drugs.
likely to cause hyponatremia.

Patients with liver disease.

Drugs that induce hepatic


enzymes may increase
Highly bound to plasma
Alopecia, weight gain, valproate metabolism.
proteins—low Inhibits voltage-gated sodium channels and T-
Highly effective for thrombocytopenia,
bioavailability. type calcium channels.
photosensitive epilepsy hepatotoxicity (fulminant Valproate can displace
Valproate Many types of seizures.
and juvenile myoclonic hepatitis), hyperammonemia, drugs that compete for
Hepatic elimination Increases GABA production and decreases
epilepsy. and neural tube defects protein binding sites.
(conversion to inactive GABA metabolism.
(category D teratogen).
metabolites).
Valproate inhibits hepatic
enzymes to increase
plasma concentrations of
other drugs.

May exacerbate myoclonic


Inhibits voltage-gated sodium channels seizures.
Does not induce or inhibit (prolongs the inactivation period) and voltage-
Lamotrigine Many types of seizures. Hepatic elimination. CNS effects and rash.
hepatic enzymes. gated calcium channels. Inhibits glutamate Drugs that induce hepatic
release. enzymes may increase
lamotrigine metabolism.
Leukopenia,
Inhibits T-type calcium channels, thereby
thrombocytopenia,
Ethosuximide Absence seizures. Hepatic elimination. reducing pacemakers currents that contribute
pancytopenia, aplastic
to epileptiforms in absence seizures.
anemia, and skin reactions.

Gabapentin and Adjunct therapy for focal and Originally designed to be Inhibits voltage-gated calcium channels Weight gain and May exacerbate myoclonic
Renal elimination.
Pregabalin secondary generalized seizures. GABA-analogs. containing the alpha-2-delta-1 subunit. somnolence. and absence seizures.

Sedation, cognitive Phenobarbital induces


First line treatment for Primarily binds to the GABA-A receptor to
Good oral absorption. impairment, hyperactivity in hepatic enzymes to
status epilepticus. prolong the opening of chloride channels,
Phenobarbital Many types of seizures. children (paradoxical effect), decrease plasma
however there are reports of multiple
Hepatic elimination. CNS depression, and concentrations of other
Low toxicity and cost. mechanisms of action.
cardiorespiratory depression. drugs.

Diazepam and Lorazepam are


Benzodiazapines first line treatment for status
Diazepam epilepticus. Limitations are sedative Sedation, dependence,
Binds to the GABA-A receptor to increase the
Enhancers of Inhibitory Lorazepam effect and tolerance Hepatic elimination. aggression, hyperactivity,
frequency of chloride channel opening.
Neurotransmission Clonazepam Clonazepam and Clobazam are development. and irritability.
Clobazam approved for chronic treatment of
several types of seizures.

Inhibits GAT-1 to reduce the reuptake of


Tiagabine Adjunct therapy for focal seizures. GABA-analog Renal elimination. GI and CNS distress.
GABA.

Monotherapy for infantile spasms. Weight gain and retinal


Inhibits GABA transaminase to reduce the
Vigabatrin GABA-analog Renal elimination. toxicity (can lead to
breakdown of GABA.
Adjunct therapy for focal seizures. permanent vision loss).

Adjunct therapy for primary


generalized seizures. Binds to SVP2A protein in vesicles of pre- Agitation, irritability, and Patients with renal
Levetiracetam Renal elimination.
synaptic neurons to inhibit glutamate release. lethargy. dysfunction.
Inhibitors of Excitatory Monotherapy for focal seizures.
Neurotransmission Adjunct therapy for primary
generalized seizures. Non-competitive Black-box warning and CNS
Perampanel Hepatic elimination. Binds to AMPA receptors.
antagonist of glutamate. effects.
Monotherapy for focal seizures.