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Exam #2 & 3 - Anticonvulsants I & II
n/a
44
Pharmacology
Graduate
10/10/2009

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Term
Anticonvulsant drugs
Definition
treat 1) epileptic seizures and 2) non-epileptic convulsions
Term
Epileptic seizures
Definition
short term alteration in behavior due to disordered synchronous, rhythmic firing of brain neurons
Term
Non-epileptic convulsions
Definition
similar to epileptic seizures but caused by a variety of environmental stimuli such as electroshock therapy, chemicals, hypoglycemia, genetic disorders, & brain damage
Term
Starting Treatment of Epilepsy
Definition
usually, physicians start drug therapy after 2 unexplained seizures
Term
causes of seizures
Definition
stroke, trauma, and genetic disorders
Term
partial (focal) seizure
Definition
seizure activity begins at a SINGLE site within cortex; one arm, leg, or body part is affected
Term
simple partial (focal) seizure
Definition
seizure that lasts 20-60 seconds and has preservation of consciousness; pt may have twitches or other weird responses but DOES NOT lose consciousness
Term
complex partial (focal) seizure
Definition
seizure that has gradual loss of consciousness; it lasts 30 secs to 2 min; may begin with a simple seizure, hallucinations, strong emotions followed by automatisms (lip smacking, hand wringing)
Term
EEG of partial seizures
Definition
shows only 1 or 2 electrodes displaying synchronous activity during a seizure
Term
EEG of generalized seizures
Definition
all 15-20 electrodes used will display synchronous activity during a seizure
Term
generalized seizure
Definition
seizure activity that begins simultaneously in both hemispheres of brain
Term
absence (petit mal) generalized seizure
Definition
seizure that includes sudden loss of consciousness and lasts less than 30 seconds; characterized by staring & blinking (3 blinks per second) while the body may remain active (sitting, walking, biking, etc); more common in children
Term
tonic-clonic (grand mal) seizures
Definition
seizures that result in sudden loss of consciousness and lass 1.5 to 2.5 minutes; initial stage (tonic): 20 seconds of muscle rigidity; followed by: 1-2 min of rhythmic muscle contractions (clonic); most injuries due to falling during tonic stage; associated with loss of control of bowels
Term
myoclonic generalized seizure
Definition
single shock-like contraction wit duration of less than 1 second; whole body or one extremity may contract; more common in children
Term
secondarily generalized seizures
Definition
a combination of both partial and generalized seizures; seizure activity starts in one area (partial) with axonal fibers leaving seizure focus to excite a structure like the thalamus that begins rhythmic asynchronous firing in both hemispheres (generalized)
Term
Kindling
Definition
experimental model of seizures using animal models; repeated low-intensity, brief, electrical stimulation to amygdale-hippocampus; model of partial & generalized seizures
Term
Injection of excitatory neurotransmitters/chemoconvulsants
Definition
experimental models of seizures that use animal models; this is a model for tonic-clonic seizures
Term
Anticonvulsant drug mechanism of action (phenytoin, valproic acid, carbamazepine, oxycarbazepine)
Definition
drugs that act to reduce neuronal activity by blocking voltage-gated sodium channels on neuronal axons
Term
Anticonvulsant drug mechanism of action (ethosuximide & valproic acid)
Definition
drugs that act to reduce neuronal activity by blocking T-type calcium channels located on post-synaptic membranes; used to treat absence seizures
Term
Anticonvulsant drug mechanism of action (barbiturates: phenobarbital & primidone; benzodiazepines: clonazepam, diazepam; tiagapine)
Definition
drugs that all act to reduce neuronal activity by enhancing the inhibitory effects of GABA
Term
Bromides - sodium & potassium bromide
Definition
drugs used at high doses that cause severe sedation resulting in fewer seizures; used in 1800's; side effects: severe sedation, severe skin rash and/or lesions
Term
Lennox-Gustaut Syndrome (LGS)
Definition
childhood-onset epilepsy with severe cognitive dysfunction; pts have multiple seizure types including atonic seizures; resistant to drug therapy and high mortality rate (3-7%); treat with ketogenic diet that is very low in carbs and high in protein and fat; also treated with felbamate (Felbatol)
Term
felbamate (Felbatol)
Definition
drug used as monotherapy & adjunctive therapy for Lennox-Gustaut Syndrome (LGS), partial, & generalized seizures in adults; inhibits Ca & Na channels as well as NMDA & AMPA-kainate receptors
Term
Side Effects of felbamate (Felbatol)
Definition
GI upsets, anorexia, insomnia, aplastic anemia, hepatotoxicity
Term
phenobarbital (Luminal, 1912)
Definition
first anti-seizure drug still used today because it is cheap & effective; Use: monotherapy for generalized tonic-clonic & partial seizures; MOA: enhances inhibitory effect of GABA on synaptic receptors; Pharmacokinetics: mainly metabolized by liver; SE: sedation (adults), irritability/hyperactivity (children), induction of CYP3A4 which leads to increased drug metabolism (oral contraceptives)
Term
primidone (Mysoline, 1949)
Definition
barbiturate metabolized to phenobarbital & PEMA; Use: monotherapy for generalized tonic-clonic, partial, & adolescent myoclonic seizures; less effective than phenobarbital; MOA: enhances inhibitory effects of GABA on synapse receptors; Pharmacokinetics: a lot of variation in absorptoin, distribution; Side Effects: sedation (adults), irritability/hyperactivity (children), dizziness, nausea, nystagmus, ataxia
Term
phenytoin (Dilantin, Diphenylan)
Definition
Use: monotherapy for generalized tonic-clonic & partial seizures; MOA: prolong rate of recovery of voltage-gated Na channels from inactivation; Kinetics: 90% protein bound, drug concentration increases disproportionately as dosage is increased, 95% metabolized in liver; Side Effects: drugs metabolized by CYP2C9/10/19 affected (warfarin), induction of CYP3A4 results in increased drug metabolism (oral contraceptives), minor rash, occasional Stevens-Johnson Syndrome (SJS)
Term
Stevens-Johnson Syndrome
Definition
adverse, immune system-mediated drug reaction characterized by blistering of skin & mucous membranes; starts with flu-like symptoms with persistent fever progressing to blisters then sloughing of skin; Treatment: discontinuation of suspected drug (phenytoin) & possible immunosuppressives; Toxic Epidermal Necrolysis: a more severe form of SJS in which 30% of total skin surface area is covered in blisters with a higher mortality rate
Term
carbamazepine (Tegretol, Carbatrol, 1974)
Definition
Use: monotherapy for generalized tonic-clonic & partial seizures, also used in manic-depressive pts; MOA: prolonged rate of recovery of voltage-gated Na channels from inactivation; Kinetics: metabolized to epoxide that induces its own metabolism, must wait 3 wks for consistent plasma concentrations, metabolism increased by phenobarbital, phenytoin, valproic acid; Side Effects: Acute: stupor, coma, hyperirritability, convulsions; Chronic: drowsiness, vertigo, ataxia, blurred vision; induces CYP3A4 resulting in increased drug metabolism (oral contraceptives)
Term
oxcarbazepine (Trileptal, 2000)
Definition
structurally similar to carbamazepine; Use: monotherapy/adjunctive treatment of partial seizures; MOA: prolongs rate of recovery of voltage-gated Na channels from inactivation; Kinetics: acts as prodrug converted to active form in liver; Side effects: dizziness, nausea, somnolence, ataxia, induces CYP3A4 resulting in increased drug metabolism (oral contraceptives)
Term
ethosuximide (Zarontin, 1960)
Definition
Use: monotherapy of ABSENCE seizures; MOA: inhibits T-type Ca channels; Kinetics: unbound, mainly excreted by liver; SE: nausea, vomiting, anorexia, CNS drowsiness, lethargy, euphoria, SJS, aplastic anemia
Term
valproic acid (Depakote, Depakene, 1978)
Definition
Use: monotherapy of ABSENCE, MYOCLONIC, PARTIAL, and TONIC/CLONIC seizures; MOA: inhibits T-type Ca channels, prolongs inactivation of Na channels, increases GABA synthesis; Kinets: 90% protein bound; SEs: GI nausea, anorexia, CNS sedation, ataxia, tremor, increases hepatic blood enzymes, inhibits CYP2C9 resulting in increased concentrations of phenytoin, phenobarbital
Term
benzodiazepines - clonazepam (Klonopin) & clorazepate (Tranxene-SD)
Definition
Use: adjunctive therapy for ABSENCE seizures & juvenile myoclonic seizures; MOA: increases inhibitory effect of GABA by inhibiting synapses; Kinetics: good oral absorption, fast acting; SEs: drowsiness, lethargy, decrease with time; Children: aggression, hyperactivity, irritability
Term
gabapentin (Neurontin, 1993)
Definition
Use: adjunctive treatment for partial seizures with or without generalized secondary seizures, mostly used for neuropathic pain; MOA: not completely known, binds to L-type Ca channels but no change in Ca conductance, does not act like endogenous GABA; Kinetics: not metabolized, excreted unchanged in urine; SEs: fatigue, ataxia
Term
lamotrigine (Lamictal, 1994)
Definition
Uses: monotherapy & adjunctive therapy for partial & generalized tonic/clonic seizures, LGS; MOA: prolong rate of recovery of voltage-gated Na channels from inactivation, inhibits Ca to lesser extent; Kinetics: long half-life, reduced by phenytoin, carbamazepine, phenobarbital, & primidone; SEs: dizziness, ataxia, blurred vision, nausea
Term
topiramate (Topamax, 1996)
Definition
Use: adjunctive therapy for partial seizures with and without generalized tonic/clonic seizures, LGS; MOA: inhibits Na channels & AMPA-kainate receptors, enhances GABA receptors; Kinetics: excreted mostly unchanged in urine; SE: ataxia, fatigue, somnolence, weight loss
Term
tiagabine (Gabitril, 1997)
Definition
Use: adjunctive therapy for partial seizures with or without secondarily generalized tonic/clonic seizures; MOA: inhibits GABA reuptake at synapse, prolonging actions of GABA; Kinetics: shorter half-life; SEs: dizziness, somnolence, tremor
Term
levetiracetam (Keppra, 1999)
Definition
Use: adjunctive treatment for partial seizures in adults; MOA: prolong rate of recovery of voltage-gated Ca channels from inactivation, inhibits T-type Ca channels; Kinetics: 85% excreted in urine unchanged, minor liver metabolism; SEs: somnolence, dizziness, anorexia, fatigue
Term
AEDs of choice for partial secondarily generalized seizures
Definition
Drugs of Choice: 1) phenytoin, 2) carbamazepine; Alternatives: phenobarbital, primidone, valproic acid
Term
AEDs of choice for generalized absence seizures
Definition
Drug of Choice: ethosuximide, valproic acid; Alternatives: clonazepam, diazepam
Term
AEDs of choice for generalized tonic/clonic seizures
Definition
drugs of choice: phenytoin, carbamazepine, valproic acid; Alternatives: phenobarbital, primidone
Term
Status Epilepticus
Definition
a series of seizures where full recovery from one seizure does not occur before onset of next seizure; medical emergency with 20% mortality rate; give IV diazepam for initial treatment, closely monitor pt avoid hypoventilation & hypotension, once seizures are controlled give fosphenytoin (Cerebryx)
Term
AEDs & Pregnancy
Definition
when taking both meds (AED + oral contraceptives), women have a 3x higher failure rate of contraceptive; also, a 2-3 fold increase in birth defects while taking AEDs during pregnancy (neural tube formation abnormalities, facial & cranial deformities)
Term
Treatment of Pregnant Women on AEDs
Definition
reduce adjunctive therapy to monotherapy; find minimum dose of drug to adequately control seizure activity; give patient folate (0.4 mg/day) throughout pregnancy; also give vitamin K (10 mg/day) during last month of gestation to help reduce newborn blood coagulation problems/vitamin K deficiencies
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