Antiepileptic Drugs Flashcards
Treatment; Slides 55 onwards
Cause fewer cognitive impairments (2)
Gabapentin and Lamotrigine
May cause substantial cognitive impairments esp. when given at high or rapid doses
Topiramate
Most widely used AEDs (4)
Carbamazepine, Phenobarbital, Phenytoin, Valproic Acid
Superior to valproic acid for efficacy in the treatment of
partial seizures
Carbamazepine
Newer generation agents (3)
Lamotrigine, Oxcarbazepine, Topiramate
Received FDA approval for use as monotherapy in patients
with partial seizures (3)
Lamotrigine, Oxcarbazepine, Topiramate
Lamotrigine, Oxcarbazepine, Topiramate are FDA approved as _____________
monotherapy in patients
with partial seizures
traditional treatment for Tonic-Clonic Seizures
Phenytoin
increasingly used due
to lower incidences of side effects and with equal efficacy compared to phenytoin in treating Tonic-Clonic Seizures (2)
Carbamazepine and Valproic acid
Generally considered the drug of first choice for atonic seizures and for juvenile myoclonic epilepsy
(JME)
Valproic acid
FDA-approved as adjunctive treatment of myoclonic seizures in patients with JME
Levetiracetam
Alternative agents (3)
Lamotrigine, Topiramate, Zonisamide
Levetiracetam is FDA-approved as _________
adjunctive treatment of myoclonic seizures in patients with JME
viewed as a tool with which to optimize therapy for an individual patient not as a therapeutic endpoint in itself
Serum concentrations of the older AEDs
Serum concentration is a target that should be correlated with ______
clinical response
First-line therapy for patients with newly diagnosed partial seizures and for patients with primary generalized convulsive seizures
Carbamazepine
Associated with a 1% risk of spina bifida when ingested during
the first trimester of pregnancy
Carbamazepine
congenital disability condition which affects the spine as a type of neural tube defect; can happen anywhere along the spine if the neural tube does not close entirely in the membranes of the spinal cord
spina bifida
Most Common Adverse Effects include neurosensory side effects (diplopia, blurred vision, nystagmus, ataxia, unsteadiness, dizziness and headache); seen in 35%
to 50% of px
Carbamazepine
Most Common Adverse Effects include Hematologic side effect (leukopenia - 10% incidence)
Carbamazepine
double vision
diplopia
rapid or uncontrollable eye movement
nystagmus
loss of muscle control or coordination
ataxia
Drug Interactions of Carbamazepine are _________
very significant
Drugs that inhibit CYP3A4 potentially may increase this AED’s serum concentrations
Carbamazepine
Second-line agent for patients with partial seizures who have failed initial treatment
Gabapentin
Shown to be useful for chronic pain and other non-epileptic conditions
Gabapentin
we can also find benefits in this AED for px with less severe seizure disorders in the elderly
Gabapentin
Minimal CNS adverse effects and few drug interactions due
to broad therapeutic index
Gabapentin
CNS adverse effects include ataxia, somnolence, dizziness and fatigue
Gabapentin
T/F
Drug Interactions are not likely to occur in Gabapentin since this drug does not induce or inhibit liver enzymes
T
Gabapentin therapeutic index makes it a (safer/less safer) option
safer
Useful as both monotherapy and adjunctive treatment in patients with partial seizures
Lamotrigine
Useful alternative for primary generalized seizure types
Lamotrigine
Adjunctive therapy for primary GTC seizures
Lamotrigine
as monotherapy, it has comparable efficacy with more traditional AEDs such as carbamazepine and phenytoin
Lamotrigine
Most frequently reported A/E: diplopia, drowsiness, ataxia,
headaches
Lamotrigine
A/E are more common when given in combination with other AEDs
Lamotrigine
observed more in carbamazepine + lamotrigine
diplopia
manifested more in lamotrigine + valproic acid
tremors
diplopia is common in the combination of ____________
carbamazepine + lamotrigine
tremors is common in the combination of ____________
lamotrigine + valproic acid
Drug has Low potential for pharmacokinetic drug interactions
and Do not induce or inhibit liver enzymes
Lamotrigine
Indicated for patients with partial seizures who have failed initial therapy
Levetiracetam
Approved for adjunctive treatment of myoclonic seizures in patients with JME
Levetiracetam
Adjunctive treatment of primarily generalized seizures in
patients with idiopathic generalized epilepsy
Levetiracetam
Adverse Effects of this AED Appears to be modest
Levetiracetam
Most common CNS effects (sedation, fatigue, and
coordination difficulties)
Levetiracetam
drug Does not induce or inhibit liver enzymes and does not appear to interact with other AEDs, warfarin, digoxin, or oral contraceptive drugs
Levetiracetam
T/F
Oxcarbazepine is indicated for use as monotherapy
T
Adjunctive therapy in the treatment of partial seizures in adults
and children as young as four years of age
Oxcarbazepine
Potential first-line drug for patients with primary generalized
convulsive seizures
Oxcarbazepine
May also be effective in patients not demonstrating a response
to carbamazepine
Oxcarbazepine
fewer S/E than phenytoin, carbamazepine, and valproic acid
Oxcarbazepine
Most frequently reported S/E: dizziness, nausea, headache,
diarrhea, vomiting, URTI, constipation, dyspepsia, ataxia, and nervousness
Oxcarbazepine
Decreases the bioavailability and pharmacologic activity of ethinyl estradiol and levonorgestrel
Oxcarbazepine
ethinyl estradiol and levonorgestrel drug class
oral contraceptives
Drug of choice for neonatal seizures
Phenobarbital
Reserved for patients who have failed therapy with other AEDs
Phenobarbital
May be useful given IV in refractory status epilepticus
Phenobarbital
life-threatening condition when seizures persist despite administration of both 1st line and 2nd line medications
status epilepticus
advantage: available in Multiple dosage forms available
Phenobarbital
T/F
phenytoin is available in oral solid, oral liquid, IM, IV
F - phenobarbital
Most inexpensive AED
Phenobarbital
primary factors limiting the use of
phenobarbital
CNS side effects
Adverse Effects: Hyperactivity in children
Phenobarbital
May also cause porphyria and rashes as serious as SJS
Phenobarbital
Potent enzyme inducer (increases elimination of any drug
metabolized by CYP450)
Phenobarbital
First-line AED for primary generalized convulsive and partial seizures
Phenytoin
CNS depressant effects (lethargy, fatigue, incoordination,
blurred vision, higher cortical dysfunction, and drowsiness)
Phenytoin
adverse effects on CNS are usually transient, can be minimized by slow dosage titration
Phenytoin
T/F
if newer AEDs are available, phenytoin would be a lower priority
T
T/F
Phenytoin is Associated with minimal drug interaction
F - numerous drug interaction
drug interactions Involve altered absorption, metabolism, protein binding; May enhance or reduce its effects
Phenytoin
Dosing Must be in mg PE
Phenytoin
dosing unit of phenytoin
mg phenytoin
equivalents or PE
75 mg fosphenytoin is equal to ____ mg phenytoin sodium
50
Second-line agent for patients with partial seizures who have failed initial treatment
Pregabalin
Useful for chronic neuropathic pain and generalized anxiety disorder
Pregabalin
Most frequently reported A/E: dizziness, ataxia, blurred vision,
and weight gain
Pregabalin
Drug Interactions are Unlikely to happen, predominantly excreted unchanged in the urine and undergoes negligible metabolism
Pregabalin
First-line AED for partial seizures as an adjunct and/or monotherapy
Topiramate
Approved for the treatment of tonic-clonic seizures in primary generalized epilepsy
Topiramate
T/F
most A/Es occur irregardless of how topiramate is administered; whether in high doses or rapid titration
F
Slow dosage titration and increments (increments must be assessed in 1 to 2 weeks)
Topiramate
Main: ataxia, impaired concentration, memory difficulties, attentional deficits, fatigue, paresthesia, somnolence, and “thinking abnormally” which rarely has included psychosis
Topiramate
Cognitive dysfunctions in concomitant therapy with topiramate, valproic acid, or phenobarbital
Topiramate
Cognitive dysfunctions from
Topiramate arise in concomitant therapy with _________, __________, or ________
topiramate, valproic acid, phenobarbital
First-line therapy for primary generalized seizures including myoclonic, atonic, and absence seizures
Valproic Acid or Divalproex Sodium
Used as both monotherapy and adjunctive therapy for partial seizures
Valproic Acid or Divalproex Sodium
Useful in patients with mixed seizure disorders
Valproic Acid or Divalproex Sodium
Most frequently reported: Gastrointestinal symptoms w/ 20%
incidence (nausea, vomiting, anorexia and weight gain)
Valproic Acid or Divalproex Sodium
T/F
GI complains in valproic acid can be completely alleviated
F
how to Minimize GI complaints from Valproic Acid or Divalproex Sodium?
enteric-coated formulation or by
giving the drug with food
A/E: Alopecia and hair changes (temporary)
Valproic Acid or Divalproex Sodium
Most serious side effect of Valproic Acid or Divalproex Sodium
hepatotoxicity
Highly protein-bound, can be displaced by other drugs
Valproic Acid or Divalproex Sodium
Approved for the adjunctive treatment of partial seizures
Zonisamide
Most common: somnolence, dizziness, anorexia, headache, nausea, agitation, word-finding difficulties, irritability; usually dose, dependent
Zonisamide
T/F
Zonisamide does not induce or inhibit liver enzymes
T
Should be avoided in patients
allergic to sulfa drugs
Zonisamide
