Pharmacology: Voltage-Gated Sodium Channel Modulators
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Questions and Answers

What is the mechanism of action of iminostilbenes on NaV channels?

  • Blocking the inactivation of NaV channels
  • Activating the resting state of NaV channels
  • Stabilizing the active state of NaV channels
  • Preventing transition to the resting state of NaV channels (correct)

    • What is the consequence of alkylation at the urea group of the dibenzazepine core in iminostilbenes?

  • Unchanged anticonvulsant activity
  • Increased anticonvulsant activity
  • Dramatic loss of anticonvulsant activity (correct)
  • No effect on anticonvulsant activity

    • What is the significance of carbamazepine (CBZ) in the context of AEDs?

  • It is the gold standard for comparing new AEDs (correct)
  • It is a newly developed AED
  • It is no longer used due to ineffectiveness
  • It is rarely prescribed due to adverse effects

    • What is the effect of higher doses of older iminostilbenes like CBZ and OXC on selectivity for hyperfunctioning neurons?

    <p>Loss of selectivity</p> Signup and view all the answers

    What is the functional moiety of iminostilbenes?

    <p>Dibenzazepine core</p> Signup and view all the answers

    What is the significance of the ethylene group in iminostilbenes?

    <p>It can be metabolically oxidized without loss of activity</p> Signup and view all the answers

    What is the effect of iminostilbenes on NaV channels?

    <p>They stabilize the inactive state of NaV channels</p> Signup and view all the answers

    What is the therapeutic significance of carbamazepine (CBZ)?

    <p>It was initially designed as an antidepressant and antipsychotic</p> Signup and view all the answers

    What is a potential contribution of lamotrigine's inhibition of dihydrofolate reductase to its adverse effect profile?

    <p>Unique adverse effect profile</p> Signup and view all the answers

    What is a characteristic of lacosamide compared to older NaV channel blockers?

    <p>Improved safety profile</p> Signup and view all the answers

    What is the mechanism of action of lamotrigine, carbamazepine, and phenytoin?

    <p>Inhibition of presynaptic fast NaV channels</p> Signup and view all the answers

    What is the class of voltage-gated calcium channel modulators that are structural analogues of GABAA?

    <p>Gabapentinoids</p> Signup and view all the answers

    What is the year in which lacosamide was approved by the FDA as an adjuvant for partial-onset seizures in adults?

    <p>2008</p> Signup and view all the answers

    What is the therapeutic use of lamotrigine, carbamazepine, and phenytoin?

    <p>Treatment of partial-onset seizures</p> Signup and view all the answers

    What is the chemical structure similarity between lamotrigine and phenytoin?

    <p>Similarity in the chemical space of the two aromatic rings</p> Signup and view all the answers

    What is the characteristic of lamotrigine that contributes to its unique adverse effect profile?

    <p>Inhibition of dihydrofolate reductase</p> Signup and view all the answers

    What is the mechanism of action of gabapentinoids in reducing excessive hyperactivity associated with seizures?

    <p>By attenuating the release of glutamate</p> Signup and view all the answers

    What is the pharmacophore for gabapentinoids?

    <p>A weakly acidic carboxylic acid or bioisostere, cyclic or acyclic hydrocarbons, and a weakly basic primary amine</p> Signup and view all the answers

    What is gabapentin approved to treat?

    <p>Partial seizures and neuralgia</p> Signup and view all the answers

    What is pregabalin approved to treat?

    <p>Generalized anxiety disorder, diabetic peripheral neuropathy, and partial-onset seizures</p> Signup and view all the answers

    What is the structural relationship between gabapentinoids and older classes of CaV blockers?

    <p>Gabapentinoids are structurally related to the succinimides and oxazolidinediones</p> Signup and view all the answers

    What is the common feature of gabapentin and pregabalin?

    <p>Both contain a GABA amino acid core</p> Signup and view all the answers

    What is the mechanism of action of gabapentinoids in reducing excessive hyperactivity associated with seizures, not related to?

    <p>Modulating CaV channel gating</p> Signup and view all the answers

    What is the functional effect of gabapentinoids on CaV channel gating?

    <p>Decrease the release of glutamate</p> Signup and view all the answers

    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.

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