PHAR450 – Medicinal Chemistry II: Antiseizures and Antiepileptics

These flashcards cover key concepts from PHAR450 lecture notes on Medicinal Chemistry II, focusing on antiseizure medications and epilepsy.

What does the term 'epilepsy' originate from?

Greek word meaning 'to seize'.

What are the characteristics of epilepsy?

Recurrent paroxysmal aberrations of brain functions, usually brief and self-limited.

What is the primary physiological change that leads to epilepsy?

Changes in neuronal activity that result in uncontrolled electric discharge in the cerebral cortex.

Name the two main classes of epileptic seizures.

Partial seizures and generalized seizures.

What is 'Status Epilepticus'?

A condition of prolonged seizures or a series of seizures without recovery between them.

What are partial seizures characterized by?

Abnormal firing that starts in a small number of neurons but may spread to adjacent areas.

What primarily determines the mechanism of action for antiseizure drugs?

Inhibition of Na+ and Ca2+ channels and enhancement of GABA effects.

What is the role of GABA in seizure control?

GABA is the predominant inhibitory neurotransmitter in the brain.

What is the effect of benzodiazepines on GABA?

They enhance the action of GABA on GABAA receptors.

What kind of seizures is carbamazepine effective against?

Complex partial seizures and generalized tonic-clonic seizures.

What is the main adverse effect of phenobarbital?

Drowsiness and sedation.

What is a major active metabolite of valproate?

(E)-2-ene-valproic acid.

Which drug is specifically indicated for absence seizures?

Ethosuximide.

What is the mechanism of action for lamotrigine?

Blockade of Na+ channels.

What distinguishes oxcarbazepine from carbamazepine?

Oxcarbazepine is a 10-keto derivative and has less toxicity.

What serious side effect is associated with felbamate?

Aplastic anemia.

How is gabapentin thought to enhance seizure control?

By increasing GABA levels in the brain.

What is the primary characteristic of generalized seizures?

Virtually the entire brain is affected simultaneously.

What mechanism does topiramate utilize to block seizures?

Blocks repetitive firing on Na+ channels and may enhance GABAA receptor activity.

Which drug is a prodrug that gets converted to phenytoin?

Fosphenytoin.

What is known about the metabolism of valproate?

It is metabolized entirely by the liver.

What is the main action of ethosuximide?

Inhibiting Ca++ channel activity.

How do succinimides function in seizure management?

They decrease Ca++ channel activity.

What type of seizures is clonazepam used for?

Atonic, myoclonic, and absence seizures.