Antiepileptic Drugs: Mechanisms and Strategies
20 Questions
0 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to Lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

A patient experiencing refractory focal seizures is being evaluated for adjunctive therapy. Considering the diverse mechanisms of action among antiepileptic drugs, which of the following agents, when added to an existing regimen of phenytoin and valproate, would MOST likely introduce redundancy in sodium channel blockade, potentially limiting additional efficacy?

  • Gabapentin
  • Ethosuximide
  • Lamotrigine (correct)
  • Levetiracetam

An investigator is studying novel anticonvulsant compounds. A promising lead demonstrates both enhancement of slow inactivation of sodium channels and a discernible impact on calcium channel modulation. Based on the currently available antiepileptic drugs, which agent's mechanism MOST closely resembles this novel compound's activity?

  • Tiagabine
  • Lacosamide
  • Phenobarbital
  • Lamotrigine (correct)

A researcher is designing an experiment to evaluate the efficacy of various antiepileptic strategies in a neuronal cell culture model exhibiting hyperexcitability. To comprehensively address the underlying mechanisms, the researcher intends to simultaneously target multiple pathways. Which of the following combination of interventions would MOST effectively block neuronal hyperexcitability?

  • Blocking calcium channels, decreasing GABA activity.
  • Enhancing glutamate receptors, blocking potassium channels.
  • Blocking sodium channels, inhibiting glutamate receptors.
  • Enhancing GABA activity, opening potassium channels (correct)

A patient is prescribed ramelteon for chronic insomnia. During a follow-up visit, the patient reports inconsistent drug efficacy. Which of the following instructions is MOST critical to emphasize to optimize ramelteon's therapeutic effect?

<p>Administer the medication 30 minutes before bedtime on an empty stomach or low fat meal. (D)</p> Signup and view all the answers

In a clinical toxicology scenario involving an unconscious patient, the ingested substance is suspected to be either a benzodiazepine or a barbiturate. Rapid clinical differentiation is crucial. Which of the following considerations is MOST pertinent in guiding immediate therapeutic intervention?

<p>The absence of a specific antagonist for barbiturates necessitates primarily supportive care, while flumazenil can reverse benzodiazepine effects. (A)</p> Signup and view all the answers

An analytical chemist is tasked with identifying an unknown hypnotic drug based on its molecular structure. Upon analysis, the compound is found to contain a pyrazolopyrimidine core. Based on this structural characteristic, which of the following drugs is MOST likely the unknown compound?

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

In a metabolic study, researchers are investigating the impact of specific enzyme deficiencies on neurotransmitter synthesis. A particular cell line exhibits a complete absence of tyrosine hydroxylase activity. Which of the following neurotransmitters would be DIRECTLY affected by this enzymatic defect?

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

A researcher is investigating the effects of a novel enzyme inhibitor on catecholamine synthesis in neuronal cells. The inhibitor selectively targets aromatic L-amino acid decarboxylase (AADC). Which of the following pairs of compounds would MOST directly accumulate in the presence of this inhibitor?

<p>L-DOPA and Dopamine (A)</p> Signup and view all the answers

An investigator is studying the metabolic pathways of catecholamine synthesis and identifies a novel compound that specifically inhibits dopamine β-hydroxylase (DBH). Which of the following changes in neurotransmitter concentrations would MOST likely be observed in neuronal cells treated with this DBH inhibitor?

<p>Increased levels of dopamine and decreased levels of norepinephrine (D)</p> Signup and view all the answers

A genetic study identifies a novel mutation that results in a complete loss of function of glutaminase in a specific neuronal population. Which of the following neurotransmitter imbalances would MOST directly result from this mutation in the affected neurons?

<p>Decreased levels of glutamate (A)</p> Signup and view all the answers

A patient with a history of generalized anxiety disorder is prescribed buspirone. Which of the following considerations is MOST critical when initiating and managing this patient's treatment, given buspirone's complex pharmacology and potential for drug interactions?

<p>Careful assessment of concomitant medications metabolized by CYP3A4, alongside a comprehensive review for any serotonergic agents or MAO inhibitors, due to the risk of serotonin syndrome or altered buspirone metabolism. (C)</p> Signup and view all the answers

Considering the pharmacological properties of spironolactone, a potassium-sparing diuretic, which of the following drug combinations presents the GREATEST risk of inducing severe hyperkalemia, demanding vigilant electrolyte monitoring and possible dosage adjustments?

<p>Concomitant use of a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin II receptor blocker (ARB), and an angiotensin-converting enzyme inhibitor (ACEI). (D)</p> Signup and view all the answers

In the treatment of advanced prostate cancer, non-steroidal anti-androgen receptor antagonists like flutamide are frequently combined with GnRH agonists. What critical strategy minimizes the risk of initial disease flare and disease progression?

<p>Administering the non-steroidal anti-androgen receptor antagonist as monotherapy prior to initiating GnRH agonist therapy to mitigate the effects of the luteinizing hormone (LH) surge. (D)</p> Signup and view all the answers

A novel estrogen receptor modulator is being developed for the treatment of osteoporosis and breast cancer prevention. Elucidation of which structural features is MOST critical for achieving selective estrogen receptor agonist activity in bone tissue while maintaining antagonist activity in breast tissue?

<p>Preservation of the aromatic A-ring and C3-OH group, coupled with strategic modifications at the C17 position to modulate the interaction with co-regulatory proteins in a tissue-specific manner. (B)</p> Signup and view all the answers

A female patient on combined hormonal contraceptives presents with persistent breakthrough bleeding and reports experiencing increased fibroid growth. Based on this clinical presentation, which of the following adjustments to her contraceptive regimen is MOST appropriate, considering the differential effects of estrogen and progestin?

<p>Increasing the estrogen dosage in the combined hormonal contraceptive formulation to stabilize the endometrium and reduce breakthrough bleeding. (C)</p> Signup and view all the answers

A postmenopausal woman with a history of breast cancer is being considered for treatment to prevent further bone loss. Which of the following agents exhibits selective estrogen receptor agonist activity in bone tissue while demonstrating antagonist activity in breast tissue, thereby offering a dual benefit in this clinical scenario?

<p>Tamoxifen, a selective estrogen receptor modulator (SERM) that acts as an antagonist in breast tissue and an agonist in bone. (D)</p> Signup and view all the answers

A patient with estrogen-dependent breast cancer is being treated with an aromatase inhibitor. What is the MOST critical mechanism of action through which aromatase inhibitors exert their therapeutic effect in this context?

<p>Inhibiting the conversion of androgens to estrogens, thereby decreasing estrogen concentration and depriving breast cancer cells of hormonal stimulation. (C)</p> Signup and view all the answers

Which of the following represents the MOST significant advantage of utilizing sulfate-conjugated estrogens, such as estrone sulfate, compared to unconjugated 17β-estradiol in hormone replacement therapy?

<p>Prolonged half-life, improved bioavailability, and greater overall stability, leading to more consistent and predictable hormonal effects. (B)</p> Signup and view all the answers

A patient taking a Z-drug for insomnia is also prescribed an antiepileptic drug (AED) that is known to induce CYP3A4 enzymes. What clinically significant outcome should be anticipated in this scenario?

<p>The AED will induce CYP3A4, resulting in decreased plasma concentrations and reduced efficacy of the Z-drug, potentially exacerbating the patient's insomnia. (D)</p> Signup and view all the answers

In the context of local anesthetics, which of the following statements accurately describes the relationship between lipophilicity, diffusibility, and clinical implications for anesthetic action?

<p>Lipophilicity is directly proportional to diffusibility, where more lipophilic anesthetics diffuse more readily across lipid membranes, resulting in faster onset, increased potency, and potentially greater systemic toxicity. (C)</p> Signup and view all the answers

Flashcards

Synthesis of GABA

GABA is synthesized from glutamate via glutamate decarboxylase.

Buspirone

An anxiolytic that is a 5-HT1A agonist and does not act on GABAa receptors.

Spironolactone Drug Interactions

Interacts with NSAIDs, ARBs, and ACE inhibitors.

Non-steroidal Androgen Receptor Antagonists

Include Flutamide and Bicalutamide; used for prostate cancer.

Signup and view all the flashcards

Estrogen Receptor Agonists

Tamoxifen and Raloxifene; useful in treating certain cancers.

Signup and view all the flashcards

Adverse Effects of Hormonal Contraceptives

Too much estrogen leads to thromboembolic risk; too little causes fibroids.

Signup and view all the flashcards

Aromatase Inhibitors Effects

Drugs like Anastrazole decrease estrogen concentration in the body.

Signup and view all the flashcards

Mechanism of Action of AEDs

Includes blockade of Na+ and Ca2+ channels and enhancing GABA transmission.

Signup and view all the flashcards

Local Anesthetics: Esters vs Amides

Esters include Benzocaine; Amides include Lidocaine, distinguished by chemical structure.

Signup and view all the flashcards

Bupivacaine Fatality Risk

Bupivacaine can be fatal if administered intravenously.

Signup and view all the flashcards

Antiepileptic drug strategies

Different strategies used to manage epilepsy include GABA activation, NMDA receptor modulation, and Na/Ca channel blockade.

Signup and view all the flashcards

GABA activators

Drugs that enhance GABA activity include benzodiazepines and phenobarbital, which help in seizures.

Signup and view all the flashcards

NMDA blockers

Felbamate and Topiramate are drugs that block NMDA receptors and reduce hyperexcitability.

Signup and view all the flashcards

Na channel blockers

Drugs like Carbamazepine and Phenytoin block Na+ channels to prevent neuronal depolarization.

Signup and view all the flashcards

Lacosamide

Lacosamide enhances slow inactivation of Na channels and is considered an antiepileptic drug.

Signup and view all the flashcards

Levetiracetam

Levetiracetam acts as a GABA enhancer and blocks Ca channels; it has multiple mechanisms of action.

Signup and view all the flashcards

Ramelteon administration

Ramelteon should not be taken with a high-fat meal and is taken 30 minutes before bed.

Signup and view all the flashcards

BZD vs Barbs overdose treatment

Benzodiazepines can be treated with Flumazenil, while barbiturates cannot due to lack of specific antagonists.

Signup and view all the flashcards

Catecholamine synthesis

Tyrosine is converted to L-dopa by tyrosine hydroxylase, which is the first step in catecholamine synthesis.

Signup and view all the flashcards

Neurotransmitter amino acids

Epinephrine, dopamine are synthesized from Tyrosine; serotonin from Tryptophan, and GABA from Glutamate.

Signup and view all the flashcards

Study Notes

Antiepileptic Strategies and Drugs

  • GABA Activation: Benzodiazepines (e.g., lorazepam, diazepam), Phenobarbital, Primidone, Levetiracetam
  • GABA Inhibition: Tiagabine, Vigabatrin
  • NMDA Receptor Blockade: Felbamate, Topiramate
  • Calcium Channel Blockade: Oxcarbazepine, Levetiracetam, Pregabalin, Gabapentin, Ethosuximide
  • Sodium Channel Blockade: Carbamazepine, Oxcarbazepine, Phenytoin, Fosphenytoin, Lamotrigine, Valproate, Zonisamide, Lacosamide, Topiramate

Multiple Mechanisms of Action

  • Lacosamide: Enhances slow inactivation of sodium channels
  • Lamotrigine: Blocks sodium channels; affects calcium channels
  • Levetiracetam: GABA activator; blocks calcium channels

Blocking Neuronal Hyperexcitability

  • Sodium Channel Blockade: Prevents depolarization
  • Calcium Channel Blockade: Prevents depolarization
  • Glutamate Receptor Inhibition: Glutamate is a stimulatory neurotransmitter
  • GABA Activity Enhancement: GABA is an inhibitory neurotransmitter
  • Potassium Channel Opening: Promotes hyperpolarization

Ramelteon Administration

  • Dietary Restrictions: Avoid high-fat meals
  • Timing: Take 30 minutes before bedtime
  • Mechanism: Melatonin receptor agonist

Benzodiazepine Overdose Treatment

  • Treatment: Flumazenil (competitive GABAa receptor agonist)
  • Reasoning: Barbituates lack a specific antagonist; different binding site on GABAa receptor

Z-Drug Parent Structures

  • Zolpidem: Imidazopyridine (2 nitrogens)
  • Zaleplon: Pyrazolopyrimidine (3 nitrogens)
  • Eszopiclone: Cyclopyrrolone (4 nitrogens)

Neurotransmitter Synthesis

  • Epinephrine, Norepinephrine, Dopamine: Tyrosine
  • Serotonin: Tryptophan
  • GABA: Glutamate (from Glutamine)
  • Glutamate: Glutamine

Catecholamine Synthesis

  • Tyrosine Hydroxylase: Converts tyrosine to L-DOPA
  • Aromatic Amine Decarboxylase: Converts L-DOPA to dopamine
  • Dopamine Beta Hydroxylase/COMT: Converts dopamine to norepinephrine
  • Final step: Norepinephrine to epinephrine

GABA Synthesis

  • Glutamate Decarboxylase: Converts glutamate to GABA

Buspirone

  • Mechanism: 5-HT1A and 5-HT2 receptor agonist; affinity for D2 receptors; not a GABAa receptor agonist
  • Metabolism: CYP3A4
  • Onset: Longer onset
  • Drug Interactions: MAOIs, CYP3A4 inhibitors/inducers, serotonergic agents

Spironolactone Drug Interactions

  • NSAIDs, ARBs, ACE-Is

Non-Steroidal Androgen Receptor Antagonist

  • Flutamide, Apalutamide, Bicalutamide, Nilutamide
  • Use: Prostate cancer (in combination with GnRH)
  • Adverse Effects: Liver toxicity
  • Route of Administration: Oral, Parenteral, Transdermal

Estrogen Receptor Agonist/Antagonist

  • Estogen Receptor Structure: Aromatic A ring, C3-OH, C17-OH; Fluvestrant is an antagonist
  • General indication: Tamoxifen, Toremifene, Raloxifene, Bazedoxifene: Agonist in bones, antagonists in breast tissue (cancer)

Aromatase Inhibitor Effect on Estrogen [ES]

  • Mechanism: Exemestane, Anastrazole, Letrozole decrease estrogen concentration

Selective Estrogen Receptor Modulator (SERM)

  • Mechanism: Antagonist in breast tissue, agonist in bone
  • Examples: Tamoxifen, Toremifene, Raloxifene, Bazedoxifene

Sulfate-Conjugated Estrogens

  • Advantages: Longer half-life, higher bioavailability, more stable and predictable

Drug Interactions (Z-Drugs, AEDs)

  • Z-Drugs: CYP3A4 inhibitors/inducers, cigarettes, CNS depressants (Benzodiazepines)
  • AEDs: CYP3A4 inhibitors/inducers, benzodiazepines, CNS depressants

Antiepileptic Drugs (AEDs) Mechanisms of Action

  • Sodium Channel Blockade
  • GABAergic Transmission Enhancement
  • Calcium Channel Blockade
  • Glutamate Receptor Blockade

NMDA Receptor Blockade as Antiepileptic Strategy

  • Drugs: Felbamate, Topiramate

Depolarization/Hyperpolarization Mechanisms

  • Depolarization: Sodium channel opening
  • Repolarization: Sodium channel closing, potassium channel opening
  • Hyperpolarization: Potassium channels remain open after potential reaches resting level

General Anesthesia Drugs

  • Inhaled: Nitrous oxide, Desflurane, Enflurane, Halothane, Isoflurane, Sevoflurane (lowest to highest half-life)

  • IV: Methohexital, Midazolam, Diazepam, Propofol, Ketamine, Etomidate

Local Anesthetics

  • Esters: Benzocaine, Cocaine, Procaine
  • Amides: Articaine, Bupivacaine, Lidocaine, Mepivacaine, Prilocaine, Ropivacaine

Local Anesthetics and Lipophilicity

  • Relationship: Lipophilicity directly proportional to diffusability

Local Anesthetic Contraindications with Antibiotics

  • Ester-type local anesthetics: Avoid with sulfonamide antibiotics (due to PABA metabolite)
  • Aminoglycoside antibiotics: Can enhance neuromuscular blockade

Fatal IV Local Anesthetic

  • Bupivacaine

Studying That Suits You

Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

Quiz Team

Description

Overview of antiepileptic drugs and their mechanisms of action. Includes GABA activation and inhibition, NMDA receptor blockade, calcium and sodium channel blockade. Also covers drugs with multiple mechanisms and those blocking neuronal hyperexcitability.

More Like This

Antiepileptic Drugs and Seizure Types Quiz
30 questions
Central Nervous System - Antiepileptic Drugs
16 questions
Antiepileptic Drugs and Strategies
48 questions

Antiepileptic Drugs and Strategies

RetractableAsteroid3303 avatar
RetractableAsteroid3303
Antiepileptic Drugs and Mechanisms
20 questions

Antiepileptic Drugs and Mechanisms

WarmheartedGyrolite2317 avatar
WarmheartedGyrolite2317
Use Quizgecko on...
Browser
Browser