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34 Cards in this Set
- Front
- Back
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epilepsy
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symptom characterized by complex recurrent
paradoxysmal aberrations of brain functions, usually brief and self-limited. |
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epilepsy- mechanism (3)
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• --excessive neuronal discharge
• --brought on by a disturbance of physicochemical function • --and electrical activity in the brain |
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etiology of epilepsy (3)
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--loss of the normal inhibitory mechanism
• --chemical supersensitivity that increases excitability • --of neuronal elements |
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epilepsy categories - how categorized (3)
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• -Clinical seizure-type
• -Ictal electroencephalographic expression • -Interictal electroencephalographic expression |
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primary use of anticonvulsants
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the prevention and
control of epileptic seizures. |
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Ideal epileptic drug (3)
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completely suppress seizures
doses do not cause sedation or other undesired CNS toxicity well tolerated and highly effective against various types of seizures devoid of undesirable side effects |
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first effective remedy for epilepsy
replaced by? |
KBr
KBr was replaced by Phenobarbital in 1912 (discovered by chance) |
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new drugs were introduced after KBr. what was the purpose (goals) of these new drugs? (3)
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Introduced with the aim that they might be
anticonvulsant, non sedative, and non-toxic. |
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4 MoAs of anti-epileptics
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Inactivation of voltage-dependent Na+ channels in a
use-dependent fashion B. Increase the effectiveness of inhibitory GABA transmission via the GABAA receptor C. Inhibition of Ca2+ currents through T-type Ca2+ channels D. Inhibition of excitatory glutamate transmission via ionotropic receptors |
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Inactivation of voltage-dependent Na+ channels in a
use-dependent fashion: Mechanism "A" drugs |
Phenytoin
Carbamazepine Lamotrigine Phenobarbital Oxcarbazepine Valproate Topiramate zonisamide |
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GABAa modulators (3)
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Benzodiazepines
Barbiturates (incl phenonbarbital) Topiramate |
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inhibitors of Ca++ channels (3)
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Ethosuximide
Oxazolidinediones Zonisamide |
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phenobarb mechanisms (3)
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glutamate transmission
GABAa modulator inactivation of voltage gated Na++ channels |
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inhibitors of glut transmission (3)
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Felbamate
Phenobarbital Topiramate |
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structures of anticonvulsants
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Containing the Ureide Structure (non aromatic heterocyclic moleclues)
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ureide structure (2)
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part of a 6 member ring- but with N (attached to methyl) flanked by 2 carbonyls
2 R groups coming off of it |
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5 structure categories of anticonvulsants
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barbiturates
hydantoins glutarimides (imide refers to the ureide) oxazolidinedione succimide |
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indicate which 3 anticonvulsant categories are 5 membered rings
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succimide
oxazoidinedione hydantoin |
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primidone - SAR (2)
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NOT A PRODRUG- data suggests its activity is independent of phenobarb levels
but oxidized to phenobarbital by CYP (not a barbiturate initially- missing the carbonyl) |
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primidone- type of structure
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deoxybarbituric acid that is not acidic...
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chemical name for primidone
class |
1,3,diaza 4,6 dione
barbiturate |
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example of hydantoin
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phenytoin
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hydantoin (phenytoin mostly) drug of choice for what type of seizure
other 2 options? |
tonic clonic
valproic acid and carbamazepin (CBZ) |
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unique AE of phenytoin
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Gingival hyperplasia is a use-dependent side effect of Phenytoin.
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oxazolidinedoines (2)
usage |
trimethadone
paramethadone not clinically used |
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succinamides
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-suxamide
ETHOSUXAMIDE |
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ethosuxamide- indication
alternate drug |
petit mal seizures (absence) in kids
valproic acid |
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AE of ethosuxamide
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morphological changes in liver/kidney
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metabolism of succimides
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oxidation of methyl group = inactive
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MoA of succimides
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closes Ca++ channels
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bdz that was discovered by "chance"
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chlordiazepoxide
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most prescribed bzd
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valium (diazepam)
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diazepam is drug of choice for...
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status epilepticus- given IV
brain in persistent seizure |
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definition of status epilepticus (2)
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one continuous seizure or recurrent seizures without regaining consciousness between
seizures for greater than 30 minutes. Many doctors, however, believe that 5 minutes is sufficient to damage neurons and that seizures are unlikely to self-terminate by that time. |
