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112 Cards in this Set

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This drug is effective against all seizure types except absence (petit mal).
Phenobarbital
These drugs are useful in status elepticus
Phenobarbital, Phenytoin, Benzodiazepines (old AED's)
This is the mechanism of phenobarbital
GABA receptor agonist, opening Cl- channels to hyperpolarize neurons.
Administration of phenobarbital
IV and oral
Metabolism of phenobarbital
Hepatic
Clearance of phenobarbital
Renal
Half life of phenobarbital
Long. 100 hours
Without loading, it takes this many half-lives for any drug to reach steady-state blood levels
Five half lives
This drug tends to increase phenobarbital levels
Valproate (Divalproex)
This drug is a CYP-450 inducer that therefore decreases the levels and effectiveness of most other drugs
Phenobarbital
Hyperactivity in children and sedation in adults is a toxicity of this drug
Phenobarbital
This drug must be withdrawn slowly (over weeks) or status ellepticus may result
Phenobarbital
These are the side effects of phenobarbital
Allergic rash, joint and CT problems
This drug is effective against all seizure types except absence (petit mal), but is better for partial and secondarily generalized seizures
Phenytoin
Mechanism of Phenytoin
Blocks Na+ channels
This drug blocks seizures spread from epileptic foci to normal neurons, with relatively little effect on seizure Tz
Phenytoin
This drug has variable oral absorption that is worse in children
Phenytoin
This drug has zero-order kinetics at high concentration because of enzyme saturation, which can lead to sudden toxicity
Phenytoin
Half-life of Phenytoin
6-24 hrs (at low doses)
Clearance of phenytoin
Urine and bile
This drug is mostly protein bound in the blood, and binding may be lowered in uremia, hypoalbuminemia and co-administration of Valproate (Divalproex)
Phenytoin
Unbound levels of this drug should be monitored to avoid OD and toxicity
Phenytoin
This drug induces the metabolism of most drugs, making them less effective
Phenytoin
This drug increases vitamin K turnover; therefore it should be supplemented in pregnant women
Phenytoin
This drug is a folate antagonist
Phenytoin
Phenytoin toxicity can result from administration of these drugs
INH disulfiram, cimetidine
These are the side effects of phenytoin
Gingival hyperplasia, osteomalacia, cerebellar ataxia, allergic rash
This drug is effective against absence seizures only
Ethosuxide
Mechanism of ethosuxide
T-type Ca++ channel blocker
Administration of ethosuxide
Oral only. No IV formulation available
Half-life of ethosuxide
24-48 hrs (med).
Metabolism of ethosuxide
Hepatic, metabolized to inactive glucoronide
Clearance of ethosuxide
Some is excreted unchanged in urine
This drug is a mild enzyme inducer, so other drug levels may fall off
Ethosuxide
These are the side effects of ethosuxide
Sedation, GI upset, behavior changes in children, allergic reaction
These are the uses of benzodiazepines
Sedatives, hypnotics, anxiolytics, acute anti-epileptic
This drug is effective against all seizure types, but resistence develops quickly
Benzodiazepines
This class of drugs is the treatment of choice for initial treatment of status epilepticus
Benzodiazepines
This class of drugs is used to treat EtOH withdrawal and delirium tremens
Benzodiazepines
Mechanism of benzodiazepines
Noncompetitive GABA-A receptor agonist; different binding site than phenobarbital
Administration of benzodiazepines
Good oral absorption, and can be given IV
This benzodiazepine has no active metabolites
Lorazepam (Ativan)
Metabolism and clearance of benzodiazepines
Metabolized by CYP in the liver, and excreted in urine as glucoronides
This drug has high lipid solubility, and therefore a higher volume of distribution and therefore shorter duration of action in status epilepticus
Diazepam
T/F: Lorazepam has a longer half-life than Diazepam
False. Diazepam has a longer half life even though it has a shorter duration of action due to its lipid solubility
Cimetidine inhibits the metabolism of these drugs, thereby increasing their duration of activity
Benzodiazepines
These are the side effects of benzodiazepines
Sedation, disinhibition (esp in the demented), falls, tolerance & dependence
These drugs should be withdrawn gradually
Phenobarbital, Benzodiazepines
This is the drug of choice for partial and secondarily generalized seizures
Carbamazepine
This drugs makes some types of primary generalized seizures worse
Carbamazepine
This drug is very useful for the treatment of trigeminal neuralgia and painful peripheral neuropathy
Carbamazepine
This drug is a good second line drug (after lithium and Valproate (Divalproex)) for chronic treatment of bipolar disorder
Carbamazepine
Mechanism of carbamazepine
Blocks Na+ channels
This drug has variable oral absorption; it is very insoluble and there is no IV preparation
Carbamazepine
Because this drug is not available in IV formation, it is not a treatment for acute seizures
Carbamazepine
Half-life of carbamazepine
12 hrs (short)
Metabolism of carbamazepine
Hepatic (CYP)
This drug induces its own metabolism, so blood levels and effectiveness may fall after several weeks of use
Carbamazepine
10-11 epoxide is an active metabolite of this drug
Carbamazepine
Excretion of carbamazepine and its metabolite
Renal, after glucoronidation
This drug decreases the effectiveness of birth-control pills
Carbamazepine
Macrolide (lactone) antibiotics are best avoided in patients taking this drug
Carbamazepine
Erythromycin and CEB's raise levels of this drug in the blood
Carbamazepine
These are the side effects of carbamazepine
Sedation, ataxia, blurred vision, hyponatremia and SIADH, neutropenia, allergic reactions
This is a wide spectrum drug that is effective in treating all seizure types
Valproate (Divalproex)
This is the drug of choice for absence seizures and all other primary generalized seizures
Valproate (Divalproex)
This AED is also used to treat bipolar disorder
Valproate (Divalproex)
This AED is also used in prophylactic treatment of migraines
Valproate (Divalproex)
Mechanism of Valproate (Divalproex)
Not well understood. Possibly Na channels, indirect GABA agonist, Ca and K conductances
Half-life of Valproate (Divalproex)
15 hours
Administration of Valproate (Divalproex)
IV and oral. Valproate (Divalproex) is well-absorbed orally
Metabolism and clearance of Valproate (Divalproex)
Hepatic metabolism, also excreted renally without metabolism after glucoronidations
These drugs tends to drop levels of Valproate (Divalproex)
Phenytoin, phenobarbital
These are the side effects of Valproate (Divalproex)
GI upset, acute pancreatitis, wt gain, tremor, hair loss, thrombocytopenia, menstrual irregularities
Retarded children are susceptible to liver damage caused by this drug
Valproate (Divalproex)
This drug can cause elevated ammonia levels and encephalopathy
Valproate (Divalproex) (in retarded children)
This is used to treat elevated ammonia levels and encephalopathy when they occur in the context of Valproate (Divalproex)
Carnitine supplementation
This drug was developed as a GABA receptor agonist, but it is not
Gabapentin
Mechanism of gabapentin
Unknown
This drug is weakly effective against partial and secondarily generalized seizures
Gabapentin
This drug may make absence and myoclonic seizures worse
Gabapentin
This AED is relatively safe-it has a benign side effect profile, and almost no drug interactions
Gabapentin
This AED is useful for neuropathic pain and fibromyalgia, and may also be effective against tremor
Gabapentin
This drug has a short half-life and therefore requires 3-4 times a day dosing
Gabapentin
Administration of gabapentin
Well absorbed orally
Metabolism and clearance of gabapentin
Excreted renally without metabolism
These are the side effects of gabapentin
Sedation, esp in the elderly; behavioral problems in retarded children
This AED is also used to treat mood disorders and sleep disturbances
Lamotrigine
This drug is effective against all seizure types
Lamotrigine
This drug is a weak anti-folate, but its main mechanism is probably interaction with Na channels to decrease sustained repetitive firing, and prevention of abnormal release of glutamate
Lamotrigine
Half-life of lamotrigine
24 hrs
Metabolism and clearance of lamotrigine
Renal, after glucoronidation. Not significantly metabolized
This drug has its levels doubled by interactions with this drug, which itself is unaffected
Lamotrigine levels are doubled by Valproate (Divalproex)
These are the side effects of lamotrigine
Allergic rash (dose dependent, which is unusual among allergies); also dizziness, HA, diplopia, ataxia, nausea, etc
The side effects of this drug are circumvented by introducing the drug slowly over 4-8 weeks
Lamotrigine
Mechanism of topiramate
Multiple: GABA and glutamate receptors, blockage of Na channels
Half-life of topiramate
24 hrs
These are the side effects of topiramate
Can cause paresthesias, kidney stones and wt loss; confusion, speech problems
These are novel, new drugs with a broad spectrum of use for focal and generalized seizures
Topiramate, levetiracetam
Mechanism of levetiracetam
Unknown (may block Ca channels, bind to vessicles to block release)
Metabolism and clearance of levetiracetam
Excreted renally without metabolism
Half-life of levetiracetam
12 hrs (short)
Administration of levetiracetam
IV and oral
This drug is metabolized by an enzyme found in RBC membranes
Levetiracetam
These are the side effects of levetiracetam
Virtually no physical side effects; mental side effects include cognitive effects and behavioral problems
This drug was developed as an analog of piracetam which is a brain stimulant and anti-myoclonus drug
Levetiracetam
These AED's are Na channel blockers
Phenytoin, carbamazepine, valproate, topiramate and lamotrigine.
T-type Ca channels are found here
Thalamus
This drug blocks Na channels, and is a GABA agonist and glutamate antagonist
Topiramate
These drugs are GABA agonists
Barbiturates, benzodiazepines, topiramate
These drugs are (direct and indirect) glutamate antagonists
Lamotrigine (blocks glutamate release), topiramate (glutamate antagonist)
This drug blocks Na channels, and blocks glutamate release
Lamotrigine