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Questions and Answers
What is the mechanism of action of iminostilbenes on NaV channels?
What is the mechanism of action of iminostilbenes on NaV channels?
What is the consequence of alkylation at the urea group of the dibenzazepine core in iminostilbenes?
What is the consequence of alkylation at the urea group of the dibenzazepine core in iminostilbenes?
What is the significance of carbamazepine (CBZ) in the context of AEDs?
What is the significance of carbamazepine (CBZ) in the context of AEDs?
What is the effect of higher doses of older iminostilbenes like CBZ and OXC on selectivity for hyperfunctioning neurons?
What is the effect of higher doses of older iminostilbenes like CBZ and OXC on selectivity for hyperfunctioning neurons?
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What is the functional moiety of iminostilbenes?
What is the functional moiety of iminostilbenes?
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What is the significance of the ethylene group in iminostilbenes?
What is the significance of the ethylene group in iminostilbenes?
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What is the effect of iminostilbenes on NaV channels?
What is the effect of iminostilbenes on NaV channels?
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What is the therapeutic significance of carbamazepine (CBZ)?
What is the therapeutic significance of carbamazepine (CBZ)?
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What is a potential contribution of lamotrigine's inhibition of dihydrofolate reductase to its adverse effect profile?
What is a potential contribution of lamotrigine's inhibition of dihydrofolate reductase to its adverse effect profile?
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What is a characteristic of lacosamide compared to older NaV channel blockers?
What is a characteristic of lacosamide compared to older NaV channel blockers?
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What is the mechanism of action of lamotrigine, carbamazepine, and phenytoin?
What is the mechanism of action of lamotrigine, carbamazepine, and phenytoin?
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What is the class of voltage-gated calcium channel modulators that are structural analogues of GABAA?
What is the class of voltage-gated calcium channel modulators that are structural analogues of GABAA?
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What is the year in which lacosamide was approved by the FDA as an adjuvant for partial-onset seizures in adults?
What is the year in which lacosamide was approved by the FDA as an adjuvant for partial-onset seizures in adults?
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What is the therapeutic use of lamotrigine, carbamazepine, and phenytoin?
What is the therapeutic use of lamotrigine, carbamazepine, and phenytoin?
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What is the chemical structure similarity between lamotrigine and phenytoin?
What is the chemical structure similarity between lamotrigine and phenytoin?
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What is the characteristic of lamotrigine that contributes to its unique adverse effect profile?
What is the characteristic of lamotrigine that contributes to its unique adverse effect profile?
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What is the mechanism of action of gabapentinoids in reducing excessive hyperactivity associated with seizures?
What is the mechanism of action of gabapentinoids in reducing excessive hyperactivity associated with seizures?
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What is the pharmacophore for gabapentinoids?
What is the pharmacophore for gabapentinoids?
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What is gabapentin approved to treat?
What is gabapentin approved to treat?
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What is pregabalin approved to treat?
What is pregabalin approved to treat?
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What is the structural relationship between gabapentinoids and older classes of CaV blockers?
What is the structural relationship between gabapentinoids and older classes of CaV blockers?
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What is the common feature of gabapentin and pregabalin?
What is the common feature of gabapentin and pregabalin?
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What is the mechanism of action of gabapentinoids in reducing excessive hyperactivity associated with seizures, not related to?
What is the mechanism of action of gabapentinoids in reducing excessive hyperactivity associated with seizures, not related to?
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What is the functional effect of gabapentinoids on CaV channel gating?
What is the functional effect of gabapentinoids on CaV channel gating?
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Study Notes
Voltage-Gated Sodium Channel Modulators
- Lamotrigine (Lamictal) is an inhibitor of presynaptic fast NaV channels and dihydrofolate reductase.
- Lamotrigine's mechanism of action is similar to that of carbamazepine (CBZ) and phenytoin.
- The two aromatic rings of lamotrigine occupy a similar chemical space as the two aromatic rings of CBZ.
Miscellaneous
- Lacosamide (Vimpat) is a third-generation AED approved by the FDA in 2008 as an adjuvant for partial-onset seizures in adults.
- Lacosamide has an improved safety profile over older NaV channel blockers, with minimal drug-drug interactions (DDIs) or induction of metabolic enzymes.
Voltage-Gated Calcium Channel Blockers
Gabapentinoids
- Gabapentinoids are structural analogues of GABA that modulate CaV channel gating, causing a net reduction in glutamate release.
- Gabapentinoids reduce excessive hyperactivity associated with seizures by attenuating the release of the excitatory neurotransmitter glutamate.
- The pharmacophore for gabapentinoids consists of a weakly acidic carboxylic acid or bioisostere, cyclic or acyclic hydrocarbons attached to the 3-position, and a weakly basic primary amine.
Gabapentinoids
- Gabapentin (Neurontin) was FDA approved in 1993 as adjunctive treatment of partial seizures and is also approved to treat neuralgia.
- Pregabalin (Lyrica) was approved in 2005 as adjunctive treatment of partial-onset seizures, and is also approved to treat neuropathic pain, generalized anxiety disorder, and diabetic peripheral neuropathy.
Succinimides and Oxazolidinediones
- Succinimides and oxazolidinediones are older classes of CaV blockers that are structurally related to the ureides.
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Description
Learn about lamotrigine, a medication that works similarly to CBZ and phenytoin, inhibiting presynaptic fast NaV channels and dihydrofolate reductase.
