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Pharm28

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robbypowell's version from 2016-11-08 05:17

antiepilieptics and anticonvulsants

Question Answer
Define: group of disorders characterized by periodic and uncontrolled excessive neuronal discharge in either part or all of the CNS/brainEpileptic disorders
define: violent involuntary muscle contractions (characterizing most forms of epilepsy)convulsions
_____ ______: Generalized seizure occurring as repeated or continuous attacks (longer than 5 minutes or repeated occurrences within 5 minutes), usually treated with IV Lorazepam (benzodiazipene)Status Epilepticus
______ ______: Most common type of seizure, responsive to pharmacotherapyGrand Mal
t/f: epilepsy has no definitive causetrue (but it does have risk factors: • Premature infants, brain infections, cerebral palsy, hypoxia/trauma, brain tumors, stroke, drugs, genetics)
list 8 risk factors for epileptic disorderspremature infancy, brain infection, cerebral palsy, hypoxia (trauma), brain tumor, stroke, drugs, genetics
_______ seizures involve one side of the brain, consciousness not impaired or may be impaired depending on locale involvedPartial (focal, localized)
_______ seizures involve both sides of brain at onsetTonic/clonic (aka Grand Mal)
what muscle reaction associated with grand mal seizures?bilateral sharp tonic muscle contractions
in this type of seizure, consciousness is impaired, both sides of brain are involved at onset, but postural muscles are not involvedPetit Mal (absence seizures)
T/f: Status epilepticus seizures are rare but life-threateningTrue
what is the drug of choice for tonic-clonic and partial seizures?Phenytoin (hydantoin)
what is the drug of choice for trigeminal neuralgia?Phenytoin (hydantoin)
T/F: Hydantoins (like phenytoin) prevent spread of abnormal neuronal depolarization from source, but doesn't effect discharge at sitetrue
T/F: Hydantoins (like phenytoin) prevent spread of abnormal neuronal depolarization from source, and lowers discharge at siteFalse (does not affect discharge at site)
T/F: Hydantoins (like phenytoin) suppress normal neuronal activity, in addition to abnormal activity, resulting in a sedative effectFalse (does not affect normal neuronal activity)
T/F: Hydantoins (like phenytoin) Normal neural activity is unaffected, does not cause excessive sedationTrue
What is the major site of action/receptor for Hydantoins (e.g. Phenytoin)Na channel (reversibly binds to inactivated sodium channels, thereby delaying neural recovery)
High extracellular ____ levels (which occur in epilepsy) increase the effectiveness of Hydantoins (e.g. Phenytoin)K (extracellular potassium)
High dose of Phenytoin (or any of the Hydantoins) interferes with pre-synaptic _____ channelsCalcium (→ inhibits NT release)
How is Phenytoin eliminated?urine & saliva
t/f: Phenytoin (and all other Hydantoins) are metabolized in the livertrue
t/f: phenytoin (and all other Hydantoins) are metabolized in the bloodstreamfalse (liver)
Phenytoin is metabolized in the _____liver
t/f: phenytoin induces P450true
t/f: phenytoin does not induce P450false (it does)
t/f: phenytoin has teratogenic effects during pregnancytrue
list 2 anti epileptics appropriate for use during pregnancyphenobarbital, carbamazapine
Primidone is a prodrug that is endogenously metabolized to ______phenobarbitol
t/f: barbiturates such as Phenobarbital (barbituate anti epileptic) induce P450TRUE***
t/f: barbiturates such as Phenobarbital (barbiturate anti epileptic) do not induce P450False*** (they DO)
what is the major site of action/receptor for Phenobarbital?GABA activated Cl channels (enhances binding of GABA-A receptors)
drug of choice for absence seizuresEthosuximide (Succinimide)
the classic anti epileptic classes (hydantoins, barbiturates & succinimides) have what adverse effects in common?GIT distress, P450 induction, fatigue, skin rashes, & hematological disorders (megaloblastic anemia)
t/f: carbamazepine has active site and effects similar to succinimides (e.g. ethosuximide)false (similar to hydantoins e.g. phenytoin)
t/f: carbamazepine has active site and effects similar to hydantoins (e.g. phenytoin)true (inactivated na channels)
carbamazepine is effective against what types of seizures?tonic-clonic and partial seizures; also trigeminal neuralgia
Valproic acid is most effective against what types of seizures?Absence seizures and Partial seizures
which anti epileptic has been reported to accumulate in bone?Valproic acid
t/f: Valproic acid has adverse effect on platelet aggregation which results in gingival bleedingTrue ***
what class of anti epileptic drug is appropriate to treat Status Epilepticus?Benzodiazepines (diazepam; lorazepam)
what drug should be given for seizures induced by local anesthetics?Diazepam
what receptors are targeted by benzodiazepines?GABA-A receptors
t/f: Valproic acid can induce P450false (can inhibit)
t/f: valproic acid can inhibit P450true
t/f: Gabapentin targets GABA-A receptorFalse (gaba analouge that does not interact with receptor)
what is the main use of gabapentin?Adjunct for Refractory Epilepsy
what is the mechanism of Vigabantin?Increases GABA concentrations by inhibiting GABA transaminase (targets GABA-Transaminase)
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