Term
|
Definition
Generalized (entire brain)
Unilateral (one side of the brain)
Partial (or focal)
Erratic (new born)
Unclassified (high mortality) |
|
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Term
| Anticonvulsants Mechanism of Action |
|
Definition
Allosteric modulation of GABAA receptors (Benzodiazepine)
Blocking voltage-gated sodium channel (Phenobarbital, phenyl
succinimide and hydantoins).
Blocking calcium T channel (5,5-dialkyl members of barbiturates,
oxazolidine-2,4-diones and succinimide ) |
|
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Term
|
Definition
IV for rapid response
(Status epilepticus) |
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Term
|
Definition
Use for many types of seizure
EXCEPT grand mal |
|
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Term
|
Definition
Rapid response (Status
Epilepticus)
IV or IM
Use combination with Dilantin |
|
|
Term
| Tranxene (Clorazepate dipotassium) |
|
Definition
Prodrug (decarboxylation)
Use in combination for partial seizures |
|
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Term
| General SARs for Anticonvulsants. |
|
Definition
R and R’ are hydrocarbon.
If R and R’ are lower alkyl, tendency is to
active against petit mal seizures.
If R or R’ is a phenyl, activity tend to be against
grand mal seizures and partial seizures |
|
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Term
|
Definition
Barbiturate
Use for grand mal and partial seizures
Less effective than phenytoin and Tegretol
Adminster IV as sodium salt
May be in combination with a benzodiazepine
Metabolism p-hydroxylation followed
by conjugation (glu or sulf).
Block sodium channels and GABA-A receptors |
|
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Term
|
Definition
| Blocks Na channel and GABA-A receptors |
|
|
Term
|
Definition
2-deoxy of Barbiturate
Use for all types of seizure
except petit mal
Less effective than Dilantin
Associated with sedation
Overall safe |
|
|
Term
| Dilantin (Phenytoin and Phenytoin sodium) |
|
Definition
Hydantoins
Block Sodium channel
(decrease presynaptic
glutamic acid release)
Activity against all seizures except
petit mal.
Metabolism involves p-hydroxylation
and conjugation. |
|
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Term
|
Definition
Hydantoins Disodium phospate ester prodrug of Dilantin IV or IM (phenytoin sodium has poor water solubility
Indication same as Dilantin = Activity against all seizures EXCEPT petit mal
Side effect include severe bradycardia |
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Term
|
Definition
Relatives of barbiturates but lack 6-oxo group.
Weaker acid than barbiturates therefore forms strong basic salts.
Phenyl ring indicates active against grand mal seizure |
|
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Term
|
Definition
Hydantoins
Use grand mal and complex
Partial seizures
Less active than Dilantin and
More sedating
Use in combination therapy |
|
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Term
|
Definition
Replacement of NH of hydantoin to oxygen yields oxazolidine-2,4-dione. Oldest drugs used to treat
Petit mal seizures (1940s) |
|
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Term
|
Definition
Oxazolidinedione
Prodrug undergoes N-demethylation
To active metabolite (water soluble)
Use Petit mal
Blocks Calcium T-channel |
|
|
Term
|
Definition
Due to toxicity of oxazolidinediones,
these drugs were develop for
treatment of petit mal seizure (1950s).
CH2 replaces the O of
oxazolidine-2,4-dione |
|
|
Term
|
Definition
Succinimide
Use for petit mal seizure (worsen grand mal seizure)
Block calcium T channel
Toxicity involves skin and blood. Metabolism oxidation (hydroxyl) of ethyl group |
|
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Term
|
Definition
Succinimide
Primarily use for petit mal seizure
Phenyl group indicates some activity
against grand mal seizure
N-demethylation to yield active
metabolite which is deactivated
by p-hydroxylation and conjugation
Turn urine to pink or red color
Less active than Zarontin |
|
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Term
|
Definition
Succinimide
Use for petit mal and
complex partial seizures
(does not worsen grand mal
seizure)
Metabolism in p-hydroxylation
and conjugation |
|
|
Term
| Tegretol (CBZ, Carbamazepine) |
|
Definition
Block sodium channel
Use for grand mal and partial seizures
Hematological toxicity ( rare aplastic anemia)
Metabolism involve epoxidation at
double bond convert to Trans diol
It is one of the safest and effective anti-
convulsant alone with Dilantin.
Tricyclic structure similar imipramine |
|
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Term
| Trileptal (Oxcarbazepine) |
|
Definition
Block sodium channel
Use partial seizures
Metabolism involve reduction of
ketone to active metabolite. |
|
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Term
|
Definition
Block sodium channel and increase GABA
Active as anion available as sodium salts (IV)
Metabolism involves conjugation of
carboxylic acid
and oxidation of hydrocarbon chains.
Side effects are mild, but potentially
fatal fulminate hepatitis. |
|
|
Term
|
Definition
Blocks sodium channels and
release of glutamate
Use for refractory partial seizures
Clinical trial for amyotrophic
lateral sclerosis (ALS) |
|
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Term
|
Definition
Design to mimetic GABA
May alter metabolism or release
of GABA
Bind to calcium channels?
Use grand mal, partial seizures
as single drug therapy |
|
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Term
|
Definition
Pipiderine 3-carboxylic acid
Know to inhibit GABA uptake
Binding GABA transporter GAT1
Blocks GABA reuptake
Use partial seizures |
|
|
Term
| S-(-)Levetiracetam (Keppra) |
|
Definition
Use partial, grand mal and
Myoclonic seizures. |
|
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Term
|
Definition
Dicarbamate
Blocks NMDA receptor
Blocks sodium channel.
Interact with GABAA receptor
Side effects aplastic anemia. |
|
|
Term
|
Definition
Carbonic acid anhydrase
inhibitor |
|
|
Term
|
Definition
Blockage of sodium channels
Blockage of voltage-gate calcium channels |
|
|
Term
| Anticonvulsant that tx all seizures EXCEPT petit mal |
|
Definition
2-deoxy barb: Primidone (Mysoline)
Hydantoins: Phenytoin (Dilantin) and Fosphenytoin (Cerebyx) |
|
|
Term
| BZD used for all seizures EXCEPT grand mal |
|
Definition
|
|
Term
| BZD that has rapid IV response for status epilepticus |
|
Definition
Diazepam (Valium)
Lorazepam (Ativan)-IM as well but in combination with Dilantin |
|
|
Term
| Barbs used for grand mal and partial seizures |
|
Definition
Phenobartital (Luminal)
Mephobarbital (Mebaral) |
|
|
Term
| Hydatoin used for GRAND mal and partial complex seizures |
|
Definition
|
|
Term
| Succinimide for PETITE mal and complex partial seizures |
|
Definition
|
|
Term
| Trimethyl oxazolidinedione prodrug used to treat Petit mal seizure by blocking T-Ca2+ channels |
|
Definition
|
|
Term
| All __________(Class of drugs) treat petit mal seizures |
|
Definition
|
|
Term
| Give brand name of Ethosuximide |
|
Definition
|
|
Term
| Give brand name of Methsuximide |
|
Definition
|
|
Term
| Give brand name of Phensuximide |
|
Definition
|
|
Term
| Succimide generic names end in the suffix ______ and brand names end in the suffix _______ |
|
Definition
|
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Term
| Hydratoin generic names ends in _______ |
|
Definition
|
|
Term
| Metabolism involves epoxidation at the double bond convert to Trans diol |
|
Definition
| Carbamazepine, CBZ (Tegretol, carbatrol, Epitol) |
|
|
Term
| Anticonvulsant agent with risk of fatal fulminate hepatitis (acute liver failure) |
|
Definition
|
|
Term
| Miscellaneous anticonvulsant used for refractory partial seizures |
|
Definition
|
|
Term
| Miscellaneous dicarbamate with the side feect of aplastic anemia |
|
Definition
|
|
Term
| Carbonic anhydrase inhibitor used as an anticonvulsant |
|
Definition
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