Anticonvulsants and Seizure Classification

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Questions and Answers

Which medication is a prodrug of gabapentin not affected by transporter saturation?

  • Gralise
  • Pregabalin
  • Horizant (correct)
  • Vigabatrin

What is the primary mechanism of action for Vigabatrin?

  • Mimicking GABA at the receptor
  • Inhibition of voltage-gated Ca channels
  • Inhibition of glutamate release
  • Inhibition of GABA transaminase (correct)

Which of the following adverse drug reactions is associated with Pregabalin?

  • Fatigue
  • Ataxia
  • Sedation
  • Weight gain (correct)

Gabapentin has an unlabeled use for which of the following conditions?

<p>Migraine (B)</p> Signup and view all the answers

Which of the following is true regarding Pregabalin's pharmacokinetics?

<p>It is more than 90% bioavailable. (B)</p> Signup and view all the answers

Which type of seizure is characterized by impaired consciousness and lack of response to commands?

<p>Complex partial seizures (A)</p> Signup and view all the answers

What are Jacksonian motor seizures specifically associated with?

<p>Frontal lobe foci (A)</p> Signup and view all the answers

In which type of seizure do individuals typically experience a blank stare and are unable to recall events during the seizure?

<p>Complex partial seizures (A)</p> Signup and view all the answers

What symptoms typically characterize seizures originating from the parietal lobe?

<p>Altered sensations such as tingling or pain (C)</p> Signup and view all the answers

Which seizure type is more commonly observed in children and often misinterpreted as daydreaming?

<p>Typical absence seizures (B)</p> Signup and view all the answers

What phenomenon occurs when a seizure starts in one localized area of the brain and spreads to neighboring areas?

<p>Jacksonian march (D)</p> Signup and view all the answers

Which type of seizure is distinguished by the absence of consciousness impairment?

<p>Simple partial seizures (B)</p> Signup and view all the answers

Which adverse drug reaction (ADR) is commonly associated with Mephobarbital?

<p>Sedation (B)</p> Signup and view all the answers

What is a significant pharmacokinetic characteristic of Phenytoin?

<p>Undergoes dose dependent kinetics (D)</p> Signup and view all the answers

Which of the following statements about Primidone is true?

<p>It converts into Phenobarbital among other metabolites (B)</p> Signup and view all the answers

Which adverse effect can be seen during chronic therapy with Phenytoin?

<p>Confusion (B)</p> Signup and view all the answers

Which characteristic distinguishes Fosphenytoin from Phenytoin?

<p>Water soluble pro-drug formulation (D)</p> Signup and view all the answers

What is a potential side effect of acute overdose on Phenytoin?

<p>Dizziness (D)</p> Signup and view all the answers

What effect does Primidone have when used in combination with Phenytoin?

<p>Increases the conversion to Phenobarbital (C)</p> Signup and view all the answers

What common withdrawal reaction is seen in children treated with certain AEDs?

<p>Agitation (A)</p> Signup and view all the answers

Which drug is a prodrug that is metabolized to an active form in the liver?

<p>Mephobarbital (C)</p> Signup and view all the answers

Which PK property of Phenytoin must be considered during therapy due to its potential effects?

<p>It is highly protein bound (C)</p> Signup and view all the answers

Which of the following anticonvulsants is primarily associated with interaction with the GABA receptor?

<p>Phenobarbital (D)</p> Signup and view all the answers

What is the primary mechanism of action for drugs affecting T-type Calcium channels used to control absence seizures?

<p>Slow the influx of calcium into the cell (A)</p> Signup and view all the answers

Which drug is primarily used for absence seizures by interacting with calcium channels?

<p>Ethosuximide (B)</p> Signup and view all the answers

Which characteristic is NOT true about barbiturates and hydantoins used for seizure control?

<p>Only effective for absence seizures (D)</p> Signup and view all the answers

Which statement best describes the metabolism of phenobarbital?

<p>Induces CYP3A4 and glucuronyl transferase (A)</p> Signup and view all the answers

What role do aromatic rings play in the structure of anticonvulsant compounds like hydantoins and barbiturates?

<p>Reduce activity of the compound (C)</p> Signup and view all the answers

Which of the following statements is true regarding the pharmacokinetics of phenobarbital?

<p>Around 50% is protein bound (B)</p> Signup and view all the answers

Which anticonvulsants gain some of their effects via GABA receptor interaction?

<p>Valproic acid and Topiramate (D)</p> Signup and view all the answers

What distinguishes succinimides and oxazolidinediones from barbiturates?

<p>Only effective for absence seizures (A), Lack of aromatic rings (C)</p> Signup and view all the answers

GABA acts mainly as an inhibitory neurotransmitter. What happens when it binds to its receptor?

<p>Allows chloride to enter the cell (C)</p> Signup and view all the answers

Which of the following AEDs belong to the group of sulfamate/sulfonamide?

<p>Topiramate (D)</p> Signup and view all the answers

Which type of seizure is characterized by sudden loss of postural tone, with sagging of the head and limb drooping?

<p>Atonic seizures (C)</p> Signup and view all the answers

Which of the following AEDs is classified as a benzodiazepine?

<p>Clonazepam (A)</p> Signup and view all the answers

What is the primary mechanism of action of AEDs that interact with sodium channels?

<p>Stabilizing sodium channels in the inactive state (D)</p> Signup and view all the answers

Which type of seizure is characterized by sudden brief jerking contractions that may involve the whole body or just the face and neck?

<p>Myoclonic seizures (C)</p> Signup and view all the answers

Which of the following is NOT a characteristic of atypical absence seizures?

<p>Usually accompanied by a loss of consciousness (A)</p> Signup and view all the answers

What is the effect of AEDs that interact with GABA receptors?

<p>They enhance the inhibitory effects of GABA (A)</p> Signup and view all the answers

Which of the following AEDs is known to be effective in the treatment of absence seizures?

<p>Ethosuximide (A)</p> Signup and view all the answers

What is the significance of T-type calcium channels in the context of seizures?

<p>They are involved in the regulation of neuronal excitability (C)</p> Signup and view all the answers

Flashcards

Atypical absence seizures

Seizure attacks with slower onset lasting several minutes, may involve clonic motions and autonomic symptoms.

Myoclonic seizures

Sudden brief jerking contractions, involving individual muscle groups, with no loss of consciousness.

Clonic seizures

Seizures with loss of consciousness, characterized by tonic contractions followed by symmetrical jerking, often in children.

Tonic seizures

Seizures where there's increased tone in extensor muscles, leading to loss of consciousness and falling to the ground.

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Atonic seizures

Sudden loss of postural tone causing head sagging or limb drooping, resulting in falls.

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Tonic-clonic seizures

Major convulsions with a sequence of tonic spasms followed by clonic jerking and prolonged depression of central functions.

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Anti-epileptic drugs (AEDs)

Various drugs used to treat seizures, classified by their mechanism of action.

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Sodium channel interaction

AEDs stabilize voltage-dependent sodium channels in the inactive state, decreasing seizure activity.

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GABA receptor interaction

AEDs can enhance the action of GABA, an inhibitory neurotransmitter, or increase its availability to prevent seizures.

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Partial Seizures

Seizures that originate in one part of the brain, affecting local areas.

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Simple Partial Seizures

Seizures where consciousness is preserved; symptoms depend on the brain area affected.

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Complex Partial Seizures

Seizures involving impaired consciousness, characterized by staring and unresponsiveness.

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Jacksonian Motor Seizures

A type of simple partial seizure with motor symptoms starting in one body part and spreading.

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Gabapentin

AED designed as a GABA analogue that promotes GABA release and regulates glutamate release via Ca channels.

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Vigabatrin

Inhibits GABA transaminase, increasing GABA levels; used as adjunct for complex seizures.

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Pregabalin

GABA analogue that interacts with Ca channels, used for seizures and neuropathic pain, high bioavailability.

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Horizant®

Prodrug of gabapentin for RLS and post-herpetic neuralgia, doesn't saturate transporters.

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Lamotrigine

Initially designed as anti-folate; used for seizures despite mistaken mechanism.

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Seizure Threshold

The level at which seizure activity can begin.

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Sedation (ADR)

Drowsiness or sleepiness caused as a side effect of AEDs.

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Mephobarbital

A prodrug of phenobarbital that is less well absorbed.

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Primidone

Anticonvulsant effective for most seizure types except absence; has active metabolites.

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Phenytoin

AED effective for all seizure types except absence; has slow absorption.

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Protein Binding in Phenytoin

Phenytoin is 90% protein bound in the bloodstream.

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Dose Dependent Kinetics

As the dose of phenytoin increases, the half-life also increases.

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Oral Toxicity Signs

Nystagmus, ataxia, and gingival hyperplasia are signs of phenytoin toxicity.

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Fosphenytoin

Water soluble pro-drug of phenytoin used for IV treatment.

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Common ADRs of AEDs

Includes sedation, ataxia, vertigo, and hyperactivity.

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GABA

An inhibitory neurotransmitter that decreases neurons' excitability.

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GABA receptor

A ligand-gated ion channel that allows chloride ions into the cell.

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T-type Calcium channels

Channels that act as pacemakers in the CNS, particularly in the thalamus.

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Absence seizures

Seizures that often originate from thalamic spiking activity.

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Ether compounds

Includes hydantoins, oxazolidinediones, and succinimides, effective against seizures.

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Phenobarbital

A long-acting anticonvulsant with a half-life of 100 hours.

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Hydantoins

Used for partial and generalized seizures, linked to barbiturates' structure.

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Aromatic rings in AEDs

Aromatic rings can decrease effectiveness of certain anticonvulsants.

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Anticonvulsant activity of Phenobarbital

Relative non-selectivity in its anticonvulsant effects.

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2C9 enzyme

Major metabolizing enzyme for Phenobarbital.

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Study Notes

Anticonvulsants

  • Anticonvulsants (AEDs) are used to treat seizures
  • They work by various mechanisms, influencing sodium channels, GABA receptors, and calcium channels.

Seizure Classification

  • Partial Seizures (focal or local):

    • These seizures originate in a specific area of the brain (focus). Symptoms depend on the location of the focus.
    • Simple Partial Seizures: Symptoms can include sensory changes (tingling, numbness), motor symptoms (jerking), or psychic symptoms (fear, hallucinations). Awareness is generally maintained.
    • Complex Partial Seizures: These seizures involve impaired consciousness. The person may stare blankly and not respond to commands. There's often an inaccurate recall or amnesia of events during the seizure.
    • Partial Seizures Secondarily Generalized: Partial seizures can spread to involve both hemispheres of the brain, leading to generalized seizure activity.

  • Generalized Seizures (both hemispheres involved):

    • Absence Seizures (petite mal): Often characterized by a sudden brief lapse of awareness and a blank stare. Brief, and rapid onset and cessation.
    • Typical Absence Seizures: Rapid onset and cessation, appearing as brief lapses in awareness, characterized by a vacant stare, often misinterpreted as daydreaming. Brief periods of unconsciousness.
    • Atypical Absence Seizures: Slower onset and cessation, lasting more than a few seconds. May include clonic motions, automatisms (repetitive, involuntary movements), and autonomic disturbances (sweating, flushing).
    • Myoclonic Seizures: Brief, sudden jerking movements that may involve the whole body or only certain parts (face, neck). Absence of loss of consciousness.
    • Clonic Seizures: Repetitive, rhythmic jerking movements of the body. Loss of consciousness may or may not occur.
    • Tonic Seizures: Sudden, sustained increase in muscle tone, causing the body to stiffen. Often leads to falling. Loss of Consciousness.
    • Atonic Seizures: Sudden loss of muscle tone, leading to drooping or falling.
    • Tonic-Clonic Seizures (grand mal): Characterized by a sudden loss of consciousness, stiffening of muscles (tonic phase), followed by violent, rhythmic jerking movements (clonic phase). This is often accompanied by autonomic changes (breathing problems, cyanosis).

AEDs (Anti-epileptic Drugs)

  • Mechanisms of Action: AEDs can target various points in the seizure pathway to prevent or control seizures.
  • Specific Drug Information (Examples): Further notes on individual drugs like phenytoin, carbamazepine, oxcarbazepine, ethosuximide, valproic acid, etc. are included in the following sections. Specific details about each drug, such as mechanism of action, typical use, adverse effects, and interactions, are found in the various sections dedicated to each drug.

Note: This is a condensed summary. Further detail on specific AEDs is provided in the document.

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