Medchem, Anticonvulsants

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a disorder of the brain function characterized by periodic and unpredictable occurrences of seizures

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epilepsy

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epilepsy is a disorder of the brain function characterized by ------ and ----- occurrences of seizures

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periodic

unpredictable

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a seizure is a transient alteration of behavoir due to ----, a ---- and ------- firing of pop of brain neurons

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disordered

synchoronous

rhythmic

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w/ seizures where do the firing usu come from

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cerebral cortex

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t/f

epilepsy is a particular disease

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f

cluster of symptoms arising from various dysfunctional events of the brain

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all forms of epilepsy originate in the -----, likely as a result of changes in ---- activity

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brain

neuronal

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two classification of causes of epilepsy

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symptomatic

idiopathic

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symptomatic epilepsy arise from --- abnormality

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physiologic

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idiopathich is of unknown origin, presumbly ----

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genetic

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so physiologic abnormality that can cause symptomatic epilepsy

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brain lesions

injury

tumor

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what can contribute to hyperexcitable neurons

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loss of inhibitory control

enhanced chem supersensitivity

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loss of inhibitory control and enhanced chem supersensitivity can lead to increase in ---- of neurons

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excitability

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the -- and --- --- --- determines the type of epilepsy

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location

extent of firing

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consciousness not imparied in which seizure

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simple partial

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psychomotor seizures and consciousness impaired for which seizure

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complex partial

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by decreasing intracellular ------- you can cause a seizure

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negativity

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how do you increase intracellular negativity

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stop Na from going into cell

move k out of the cell

inhibit flow of Ca from out to in

increase Cl going into the cell

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epilepsy is associated w/ ----- in ion channels

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mutations

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mutation of GABAa can lead to less --- inside cell and therefore a seizure

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Cl-

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increase flow of Na inside cell due to mutation in ---- can lead to a seizure

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SCN

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goal of antiseizure meds

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decrease excitability of neurons

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how do you decrease the excitabiltiy of neurons

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modulate ion flow thru ion channels

modulate synpatic transmission

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to decrease excitability

modulate --- flow thru ion channels

modulate ----- transmission

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ion

synaptic

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what's blocked in voltage gated channels w/ antiseizure meds

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Na

Ca

K

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what's increased decreased in ligand gated channels w/ antiseizure meds

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increase synapatic inhibition

decrease synaptic inhibition

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what inhibited in synaptic inhibtion

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increase GABA or/and GABAa mediated inhibition

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increase GABA or/and GABAa mediated inhibition will increase --- influx, and cause

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Cl

hyperpolarization

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decrease synaptic excitation will decrease or block --- receptors

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glutamate receptors

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some glutamate receptors that are blocked by antiseizure meds

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NMDA

AMPA/KA

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channel blockers will stabilize --- site of voltage gated Na channels

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inactive

this will prevent spread of seizures

for partial seizures

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channel blockers will reduc -- flow

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Ca

for generalized seizures

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channel openers will activate --- channels

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potassium

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how would you increase GABA

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inhibit GABA T; this slows GABA metabolism

inhibit GAT-1 transporter for the reuptake of GABA

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what do you upregulate to increase GABA conc

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GAD

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hydantoins are --- channel blockers

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Na

Phenytoin

Fosphenytoin

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hydantoins have -- soluability at --- pH

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poor

neutral

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how do barbiurates works

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probably block Na channels and enhance GABA inhibition

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core structure of barbiturates

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substituted pyridmidine

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how do oxazolidineiones work

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decrease Ca current

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how do iminostilbenes work

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acts on voltage dependent Na channels

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valproic acid and derivatives stabilize inactivated state of -- channels

blocks -- currents

increases inhibitory effects of --------

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Na

Ca

GABA

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zonisamide blocks --- and --- currents

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Na

Ca

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what investigational drug will open the K channels

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Retigabine

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how would you increase Cl influx

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increase GABA conc

inhibit GABA transport

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benzodiazepine enhance the effect of --- on ----Cl channles

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GABA

GABA

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examples of benzodiazepines

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diazepam

lorazepam

midazolam

clonazepam

clorazepate dipotassium

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gabapentin may alter ----- metabolism/release

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GABA

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gabapentin activates GABA and opens - channels

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Cl

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tiagabine works by

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binding to gaba transporter GAT1

preventing reuptake of GABA into neurons/glia

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bis-carbamates antagonizes --- receptor

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NMDA

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antagonizing the NMDA receptors will affect the -- currents

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Ca

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lamotrigine modulates --- channels and prevents --- release

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Na

glutamate

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toprimate blocks --- channels and enhances ---- mediated ---- influx and antagonist of ---- and Ka

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Na

GABA

Cl

AMPA

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Levetiracetam binds to synaptic vescile protein ---

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2A

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Levetiracetam blocks release of ---- neurotransmitter from secretory ------ from nerve cells

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excitatory

vesicles

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what nerves cells are blocked by levetiracetam

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glutamate

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--- upregulated in epilepsy

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SYN2