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Epileptic Drugs
BCP 401 Stony Brook
25
Pharmacology
Undergraduate 4
12/05/2017

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Cards

Term
Phenytoin
Definition
Sodium channel blocking antiseizure drug with reduced sedative effects. Effective against tonic clonic, but not absence seizures. Stabilizes inactive state of sodium channels. Undesirable phenotypic side effects like gum enlargement, hair growth. Non linear pharmacokinetics
Term
Fosphenytoin
Definition
Greater water solubility than phenyotin, effective for tonic clonic seizures for IV use.
Term
Lamotrigine
Definition
Blocks sodium channels and effective against both seizure types. Effective against a broad range of seizures and has additional activity. Inhibits glutamate release by inhibiting calcium channel and presynaptic nuerons
Term
Valproate
Definition
Anti-seizure drug, inhibit T-type Ca channel, reduce pacemaker current that belies absence seizures. Weak carboxylic acid that is a clear liquid at room temp. Increase GABA by stimulating synthesis, inhibiting its breakdown. Broad effects, can treat all major seizures
Term
Ethosuximide
Definition
Inhibit the T-Type Calcium Channel in thalamus. Effective against absence seizures. Is a specific Ttype Calcium channel blocker.
Term
Phenobarbitol
Definition
Barbiturate, allosteric modulate of GABAa, but in higher doses, can be an agonist. Effective for tonic clonic as it immediately depresses activity. Can lead to suppressed CNS function, sedation eventually.
Term
Clonazepam
Definition
BDZ used for managing epilepsy, specialized for absence seizures. Indirectly inhibits Ttype Calcium currents.
Term
Gabapentin
Definition
Antiseizure medication, management of pain, and other things. Increases biosynthesis of GABA, Gaba potentiator, Main action, binds to subunit of calcium channel, reduce current of calcium decrease NT release.
Term
Methaqualone
Definition
Quinazolone, has sedative, hypnotic effects.
Term
Diazepam
Definition
First BDZ
Term
Propofol
Definition
Used to initiate and maintain general anesthesia. Potentiates GABAa receptors. Respiratory depressant, frequently produces apnea. No reversal agent other than time
Term
GABA
Definition
Binds to GABA Receptor, chloride ion influx.
Term
GABAa receptor
Definition
Has subunit a1, 2b2, and 1y2 subunit.
Term
Flumazenil
Definition
Competitive antagonist, Decrease BDZ stimulated Cl current. Reversal agent for BDZs
Term
B Carboline
Definition
Blocks Basal Cl- Current
Term
Midazolam
Definition
Short acting BDZ. Used against anxiety, for amnesia and hypnosis.
Term
Lorazapam
Definition
Intermediate acting BDZ. In addition to all Midazolam does, it also is a muscle relaxant
Term
Diazepam
Definition
Long acting, has active metabolites
Term
Busipirone
Definition
Agonist of serotonin receptor, does not bind to GABAa receptors
Term
Zolpidem
Definition
Z drug, effective at initiating sleep, but not at sustaining it. Short acting nonBDZ, increases GABA activity by binding to GABAa, can be reversed with flumazenil
Term
Melatonin
Definition
Normally produced in pineal gland, can be beneficial in managing insomnia, but tolerance develops quick. No convincing evidence that it can treat it
Term
Ramelteon
Definition
Agonist of melatonin Mt1 and MT2 to promote sleep. Chronohypnotic influences SCN master clock to promote sleep.
Term
Orexin A
Definition
Peptides that provide signal for wakefulness. A binds OX1R and OX2R
Term
Orexin B
Definition
only binds OX2R, these are GPCRs
Term
Suvorexant
Definition
Antagonist for both OX1R and OX2R, good for insomnia
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