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106 Cards in this Set
- Front
- Back
Patients with increased expression of multidrug transporter ____________________, children with progressive ______________ and ____________ in some adults that are refractory to treatment do not respond to ANY treatment. |
P-glycoprotein 170 Brain damage Focal seizures |
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What is the treatment for patients who do not respond to ANY pharmacologic treatment for seizures? |
Vagus nerve stimulation |
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Most anti-seizure drugs are not highly bound to plasma proteins. Three exceptions are: |
Valproic acid Phenytoin Carbemazepine |
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Most older AEDs are inducers of the ___________ enzyme, giving them lots of drug interactions. |
Cytochrome P450 |
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The entire class of anti-epileptic drugs is black boxed for _________________. |
Increased risk of suicidal thoughts |
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This drug alters Na+, Ca++ and K+ conductance, prolonging the inactive state of the Na+ channel and inhibiting the generation of repetitive action potentials. |
Phenytoin |
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Phenytoin increases/decreases glutamate release and increases/decreases GABA release. |
Decreases, increases |
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What types of seizures is phenytoin active against? |
Simple partial Complex partial Partial with secondarily generalized tonic clonic seizures |
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What is the drug that is a more soluble form of phenytoin that is available for parenteral use? |
Fosphenytoin |
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Fosphenytoin is more/less potent than phenytoin and requires/does not require the co-administration of PEG. |
More, does not require |
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Phenytoin is highly bound by protein, but the administration of other highly bound drugs may displace it, resulting in _______________. |
Increased free drug |
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What enzymes metabolize phenytoin into inactive compounds? |
CYP2C9, 2C19 |
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Which two enzymes are induced by phenytoin? |
CYP2C9, CYP3A4 |
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Elimination of _______________ is dose dependent. |
Phenytoin |
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Low levels of phenytoin are eliminated by ________ order kinetics. |
First |
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High levels of phenytoin are eliminated by ______ order kinetics. |
Zero |
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______________ competes with phenytoin for protein binding, increasing plasma levels. |
Valproate |
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Enzyme interactions of phenytoin prevent __________ degradation, resulting in bleeding disorders. |
Warfarin |
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_______ have increased metabolism when given with phenytoin and should be supplemented with other methods. |
Oral contraceptives |
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_________________ enhances metabolism of phenytoin and vice versa. |
Carbemazepine |
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Phenytoin has an affinity for _________ binding globulin, and can confound ___________ function test. |
Thyroid, thyroid |
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What does DANG stand for, and what drug's side effects does it describe? |
Diplopia Ataxia Nystagmus Gingival hyperplasia Phenytoin |
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Which side effects of phenytoin require dose adjustment: diplopia and ataxia, or nystagmus/loss of smooth pursuit? |
Diplopia and ataxia |
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What is the black box warning associated with phenytoin? |
Hypotension Cardiac arrhythmias with rapid infusion of Fosphenytoin |
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This drug blocks Na+ channels, inhibiting high frequency repetitive firing of neurons. It acts pre-synaptically to reduce synaptic transmission. |
Carbamazepine |
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What types of seizures does carbamazepine treat? |
Simple partial Complex partial Partial with secondarily generalized tonic clonic |
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Aside from seizures, carbamazepine also treats ___________ and ___________. |
Bipolar disorder Trigeminal neuralgia |
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Carbamazepine is only administered __________ and is __% plasma bound |
Orally, 70% |
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Carbamazepine induces _______ and auto-induces __________. |
CYP450 CYP3A4 |
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Metabolism of carbamazepine may be decreased by _____________-. |
Valproic acid |
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Metabolism of carbamazepine may be increased by ______________ and ______________. |
Phenytoin Phenobarbital |
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Carbamazepine increases/decreases the metabolism of other drugs such as primidone, phenytoin, ethosuximide, valproic acid and clonazepam. |
Increases |
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What is the first sign of carbamazepine toxicity? |
Diplopia |
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What is the black box warning associated with carbamazepine? |
Blood dyscrasias in elderly patients taking it for trigeminal neuralgia |
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This drug has been associated with mild but persistent leukopenia (requires careful monitoring) and fatal cases of aplastic anemia and agranulocytosis. |
Carbamazepine |
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Patients of Asian descent may possess the ___________ allele, increasing their risk of developing Stevens-Johnson syndrome. |
HLA-B*1502 |
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Patients who are positive for the HLA-B*1502 allele should not take ____________. |
Carbamazepine |
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While the MOA is largely unknown for this drug, it is thought to bind to GABA A and prolong the opening of the Cl- channel to inhibit spread of abnormal firing from the seizure focus. |
Phenobarbital |
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This is the AED of choice in infants. |
Phenobarbital |
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This drug is used for all seizure types when attacks are difficult to control. |
Phenobarbital |
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True or false: phenobarbital is effective against all types of seizures, including absence. |
False. It has no effect on absence seizures, atonic attacks and infantile spasms. |
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This drug is an active parent drug with two active metabolites. |
Primidone |
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What are the two active metabolites of primidone? |
Phenobarbital Phenylethylmalonamide (PEMA) |
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This drug blocks voltage gated Na+ channels and potentiates GABA. |
Primidone |
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What types of seizures is primidone active against? |
Seizures in infants and elderly Simple partial Parital with secondarily generalized tonic clonic Tonic clonic |
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Dose adjustments of primidone must consider steady state of ___________ (rapid) and _____________ (days to weeks). |
Parent drug Metabolites |
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This drug is an irreversible inhibitor of GABA aminotransferase (GABA-T), the enzyme responsible for degrading GABA. It is also an inhibitor of vesicular GABA transporter, and decreases brain glutamate synthetase activity. |
Vigabatrin |
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This drug is used to treat infantile spasms and refractory complex partial seizures. |
Vigabatrin |
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What is the black box warning associated with vigabatrin, leading it to be a highly controlled substance that can only be distributed by certain physicians/pharmacists? |
Permanent vision loss |
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This drug suppresses rapid firing of neurons by producing voltage-and-use-dependent inactivation of Na+ channels. It also inhibits voltage-gated Ca++ channels and may decrease the release of glutamate. |
Lamotrigine |
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This drug is used as an adjunctive therapy for partial seizures, absence and myoclonic seizures in children, and is very effective in focal epilepsy. |
Lamotrigine |
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What is the black box warning associated with lamotrigine? |
Skin rashes Life threatening dermatins |
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This drug blocks voltage of voltage gated Ca++ channels as its main MOA. It also modifies release of GABA, decreases release of glutamate at synapse and inccreaess brain concentration of GABA. |
Gabapentin Pregabalin |
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This drug is used as an adjunct therapy for partial and generalized tonic-clonic seizures. |
Gabapentin |
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This drug is used as an adjunct therapy for partial seizures. |
Pregabalin |
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This drug enhances slow activation of the Na+ channel, blocks actions of neurotrophic factors on axonal and dendritic growth and binds to collapsin-response mediator element (CRMP-2), blocking BDNF and NT3. |
Lacosamide |
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This drug is used as an adjunctive therapy in patients >16 years old who have partial seizures. It is notable because it has no effect on CYP450s, making drug interactions negligible. |
Lacosamide |
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This drug binds selectively to the synaptic vesicle SV2A, which modifies synaptic release of GABA and glutamate. |
Levetiracetam |
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Along with being used for partial, primary generalized tonic-clonic seizures, levetiracetam is also good for myoclonic seizures in________________. |
juvenile myoclonic epilepsy. |
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This drug's adverse effects includde somnolence, asthenia, dizziness, CNS depression. |
Levetiracetam |
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This drug is an inhibitor of GABA uptake in both neurons and glia, producing prolonged activity and increasing tonic inhibition. It also inhibits the GABA transporter 1, increasing synaptic GABA in the forebrain and hippocampus. |
Tiagabine |
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Tiagabine is used as an adjunctive therapy for ___________. |
Partial seizures |
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Patients who take tiagabine may develop severe skin reactions or ________________ syndrome/______________________. |
Steven Johnson Syndrome Toxic epidermal necrolysis |
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This drug blocks repetitive neuronal firing through blockade of Na+ channels, potentiates the inhibitory effects of GABA and interfere with excitation of glutamate receptors. In addition, it is a weak carbonic anhydrase inhibitor. |
Topiramate |
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This is a severe form of epilepsy that develops around 4 years of age. It can be tonic, clonic, atypical absence or myoclonic, and lead to impaired intellectual functioning and information processing as well as developmental delays. |
Lennox-Gastaut Syndrome |
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This drug can be used as a monotherapy to treat Lennox-Gastaut syndrome, absence seizures and migraine headaches. |
Topiramate |
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Development of ____________ when taking topiramate requires prompt drug withdrawal. |
Acute myopia and glaucoma |
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This AED drug can lead to metabolic acidosis and urolithiasis. |
Topiramate |
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This drug provides a dose-dependent block of the NMDA receptor and potentiates the GABA A receptor response. It is NEVER considered first line. |
Felbamate |
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What types of seizures does felbamate treat? |
Refractory partial seizures Lennox-Gastaut Syndrome |
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What is the black box warning associated with felbamate that requires signed consent? |
Aplastic anemia Severe hepatitis |
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This drug is an adjunctive treatment for seizures associated with Lennox-Gastaut syndrome and refractory partial seizures. Its adverse effects include somnolence, vomiting, and shortened QT intervals. |
Rufinamide |
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What AED is associated with shortened QT intervals? |
Rufinamide |
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This drug opens KCNQ2/3 voltage gated potassium channels that typically activate M current, regulating normal neuronal excitability. |
Ezogabine |
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This drug is used as an adjunct for partial seizures and is associated with dizziness, somnolence and urinary retention. |
Ezogabine |
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True or false: absence seizures are exacerbated by phenytoin and carbamazepine. |
True |
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What three drugs are used to treat absence seizures? |
Ethosuximide Valproic acid Benzodiazepines |
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This drug inhibits Ca++ currents of T-type channels. |
Ethosuximide |
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What is the drug of choice for absence seizures? |
Ethosuximide |
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____________ is more toxic than ethosuximide, but __________________ is less effective than ethosuximide. |
Methsuximide Phensuximide |
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This drug blocks high frequency neuronal firing, causing a blockade of Na+ currents. It also causes a blockade of NMDA receptor mediated excitation and increased GABA levels. |
Valproic acid |
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This drug displaces phenytoin from plasma proteins, inhibits metabolism of phenobarbital, phenytoin and carbamazepine and decreases the clearance of lamotrigine. |
Valproic acid |
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What are the black box warnings associated with valproic acid? |
Hepatotoxicity (especially in young patients <2 years old) Pancreatitis Increased risk of spina bifida in fetuses |
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Which AED is associated with spina bifida in babies of pregnant patients? |
Valproic acid |
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How do you treat hepatotoxicity associated with valproic acid? |
L-Carnitine |
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These drugs bind to the allosteric site on GABA a receptors to treat absence seizures. |
Benzodiazapines |
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These drugs are used for status epilepticus. |
Diazepam IV Lorazepam IV |
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Which benzodiazapine can be used to treat Lennox-Gastaut syndrome in patients >2 years old? |
Clobazam |
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Children can develop paradoxical hyperactivity when taking ________________. |
Benzodiazepines |
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This drug is an inhibitor of carbonic anhydrase, leading to mild acidosis of the brain and diminished release of bicarbonate ions from GABAergic neurons. Tolerance develops quickly, so it should not be given continuously. |
Acetazolamide |
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This treatment should be used for patients with refractory seizures or for patients in whom seizure medications are poorly tolerated. |
Vagus nerve stimulation |
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What are the side effects of vagus nerve stimulation? |
Hoarseness, sore throat, voice changes during stimulation |
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This refers to recurrent episodes of tonic-clonic seizures in which the patient remains unconscious without normal muscle movement between episodes. |
Status epilepticus |
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What is the first treatment for status epilepticus? |
IV diazepam or lorazepam until 30-45 minutes of being seizure free |
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What is the second treatment for status epilepticus? |
IV phenytoin |
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Administration of IV phenytoin requires the addition of PEG, which may cause _____________ and requires constant monitoring. |
Cardiotoxicity |
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What drug can be used instead of phenytoin to avoid the side effects caused by PEG? |
Fosphenytoin |
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If there is no response to phenytoin, what drug can be administered in the instance of status epilepticus? |
Phenobarbital |
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For absence status epilepticus, this drug can be used. |
Benzodiazepines |
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What is the exception to the rule that women of childbearing age who are taking AEDs should also use another form of birth control? |
Medroxyprogesterone acetate |
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Which drug causes hypospadias in newborns of women who took it during pregnancy? |
Topiramate |
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Which drug is responsible for fetal hydantoin syndrome? |
Phenytoin |
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What are the signs of fetal hydantoin syndrome? |
Cleft lip/palate Microcephaly Brain malformations Skull/face abnormalities Growth deficiencies Underdeveloped nails Mild developmental delays |
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How long must a patient be seizure free before they can be taken off AEDs? |
Years |
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Which two classes of drugs are difficult to discontinue and may take weeks to months to wean off of? |
Benzodiazepines Barbiturates |
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True or false: generic drugs do not pose a risk for break through seizures because they are just as therapeutically stable as brand name AEDs. |
False. They are not as stable, and may cause breakthrough seizures. |