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40 Cards in this Set
- Front
- Back
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MA of Phenytoin (Dilantin, Diphenylan)
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Inhibits Na+ channels
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Pharmacokinetics of Phenytoin
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Nonlinear between dose and [plasma] due to saturable liver metabolism
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Protein binding of Phenytoin
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High protein binding (including thyroid hormone-binding globulin)
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Adverse effects of phenytoin
OH MY GOD!!! |
Lymphadenopathy, lupus, gigival hyperplasia, hirsutism, corsened facial features, endocrine abnormalities--osteomalacia, hyperglycemia, decrease ADH, tetratogen
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Lab tests for Phenytoin
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Monitor T.I. and thyroid fxn tests
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Carbamazepine (Tegretol)MA
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(-) Na+ channels and decreases synaptic transmission
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Metabolism of Carbamazepine
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Induction of own metabolism
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Adverse effects of Carbamazepine
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Liver damage, leukopenia-rarely aplastic anemia and agranulocytosis, hyponatremia, ostoeporosis, teratogen
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Lab test for Carbamazepine
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Liver fxn test- REQUIRED
Monitor T.I. Hematology and serum Na+ Renal fxn |
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Oxcarbazepine (Trileptal) MA
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(-) Na+ and high voltage Ca2+ channels, enhances K+ currents
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Metabolism of Oxcarbazepine
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Prodrug, 10 monohydroxycarbazepine is active, fewer drug interxns
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Why does Oxcarbazepine have fewer adverse effects?
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No epoxide intermediate
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Adverse effects of Oxcarbazepine?
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Hyponatremia
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Lab tests for Oxcarbazepine
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Monitor serum Na+
*Decreases T4 |
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Barbituates used in partial or gen TC seizures
(there are 8) |
Phenobarbital
Primidone Gabapentin Tiagabine Zonisamide Levetiracetam Felbamate Vigabatrin |
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Phenobarbital MA
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Modulates GABA a receptors, (-) Ca2+ channels, and decreases glutamate transmission
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Adverse effects of phenobarbital
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Sedation and possibly coma leading to death
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Primidone (2-desoxyphenobarbital) MA
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Like phenytoin
Split into phenobarbital and phenylethylmalonamide (PEMA) |
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Pharmokinetics of Primidone
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Primidone and PEMA high clearance
Phenobarbital high clearance *during chronic treatment can be 2-3X higher than primidone levels |
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Adverse effects of Primidone
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Acute intoxication
Sedation Lupus like syndrome Blood dyscrasias Osteoporosis |
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Gabapentin (Neurontin) MA
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Unknown
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Gabapentin Pharmokinetics
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Excreted unexchanged
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Gabapentin Adverse Effects
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Peripheral edema
Behavior and though disorders in kids 3-12 |
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Tiagabine (Gabatril)MA
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GABA uptake (GAT-1) inhibitor
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Tiagabine pharmokinetics
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Highly bound to plasma proteins
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Side effects of Tiagabine
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Nonconvulsive status epilepticus
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Zonisamide (Zonegran)MA
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(-) Na+ and T-type Ca2+
Weak carbonic anhydrase inhibitor |
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Side effects of Zonisamide
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Allergic rxn to Sulfa
Hypohydrosis and hyperthermia in peds pts. Renal caliculi Photosensitivity Teratogen Irritability |
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Levetiracetam (Keppra) MA
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Inhibits delayed rectifier K+ channel and N-type Ca2+ channels, (-) negative modulation of GABA a receptors by Zn2+ and beta-carboine
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Side effects of Keppra
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Irritability
Behavioral Changes |
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Felbamate (Felbatol) MA
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(-) NMDA receptors and (+) GABA transmission
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Felbamate side effects
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Aplastic anemia and severe hepatitis--hepatic failure
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Lab tests for Felbamate
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REQUIRED LIVER FXN TESTS
Hematology |
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Vigabatrin (Sabril) MA
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Irreversibly (-) of GABA degradation enzyme and GABA transaminase
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Vigabatrin side effects
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CONTRAINDICATION: preexisting mental illness, may cause psychosis
Long term visual field deficits in 1/3 of pts may be irreversible |
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FDA required liver fxn testing for these drugs
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Carbamazepine
Felbamate Valproic Acid/sodium valproate |
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Which antiseizure drugs do we have to know lab tests for?
(There are 5) |
Phenytoin- monitor T.I.
Carbamazepine- liver fxn Oxcarbazepine- Na+ and T4 Felbamate- liver fxn Valproic acid- liver fxn |
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General use Anti-seizure drugs?
(3) |
Valproate
Lamotrigine Topiramate |
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Absence seizure drug
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Ethosuximide
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Non-barbituate partial and generalized TC drugs?
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Phenytoin
Carbamazepine Oxcarbazepine |
