Podcast
Questions and Answers
A patient with a known seizure disorder is taking carbamazepine. Which potential adverse effect is most important to monitor for, especially in the initial stages of treatment?
A patient with a known seizure disorder is taking carbamazepine. Which potential adverse effect is most important to monitor for, especially in the initial stages of treatment?
- Gingival hyperplasia
- Hyponatremia (correct)
- Hepatotoxicity
- Peripheral neuropathy
Which antiepileptic drug (AED) requires careful monitoring for serious skin rashes, especially when co-administered with valproic acid?
Which antiepileptic drug (AED) requires careful monitoring for serious skin rashes, especially when co-administered with valproic acid?
- Oxcarbazepine
- Lamotrigine (correct)
- Phenytoin
- Clonazepam
Which of the following antiepileptic drugs has a multi-faceted mechanism of action, including sodium channel blockade, AMPA/glutamate receptor antagonism, and enhancement of GABAa channel activity?
Which of the following antiepileptic drugs has a multi-faceted mechanism of action, including sodium channel blockade, AMPA/glutamate receptor antagonism, and enhancement of GABAa channel activity?
- Topiramate (correct)
- Levetiracetam
- Zonisamide
- Lacosamide
Which of the following is the primary mechanism of action of benzodiazepines in the treatment of seizures?
Which of the following is the primary mechanism of action of benzodiazepines in the treatment of seizures?
A patient experiencing status epilepticus is unresponsive to initial treatment with lorazepam. Which of the following medications would be most appropriate as a second-line agent in this situation?
A patient experiencing status epilepticus is unresponsive to initial treatment with lorazepam. Which of the following medications would be most appropriate as a second-line agent in this situation?
Flumazenil is indicated for the reversal of which of the following drug overdoses?
Flumazenil is indicated for the reversal of which of the following drug overdoses?
Which of the following AEDs is known to bind to synaptic vesicle protein SV2A, thereby modulating synaptic transmission?
Which of the following AEDs is known to bind to synaptic vesicle protein SV2A, thereby modulating synaptic transmission?
A patient taking topiramate develops hyperkalemia. Which class of diuretics, if taken concurrently, could potentially contribute to this electrolyte imbalance?
A patient taking topiramate develops hyperkalemia. Which class of diuretics, if taken concurrently, could potentially contribute to this electrolyte imbalance?
Which inhaled anesthetic is LEAST likely to cause respiratory irritation due to its less pungent nature?
Which inhaled anesthetic is LEAST likely to cause respiratory irritation due to its less pungent nature?
A patient with a history of QT prolongation needs anesthesia. Which inhaled anesthetic should be avoided?
A patient with a history of QT prolongation needs anesthesia. Which inhaled anesthetic should be avoided?
Which intravenous anesthetic is most suitable for rapid sequence intubation due to its rapid onset of action and direct muscle relaxation properties?
Which intravenous anesthetic is most suitable for rapid sequence intubation due to its rapid onset of action and direct muscle relaxation properties?
A patient with significant cardiovascular disease requires sedation for a minor procedure. Which intravenous anesthetic would be the MOST appropriate choice?
A patient with significant cardiovascular disease requires sedation for a minor procedure. Which intravenous anesthetic would be the MOST appropriate choice?
A patient receiving ketamine experiences vivid dreams and hallucinations post-operatively. Which of the following actions would be MOST appropriate?
A patient receiving ketamine experiences vivid dreams and hallucinations post-operatively. Which of the following actions would be MOST appropriate?
Which local anesthetic is LEAST likely to cause an allergic reaction because it is not metabolized to PABA (para-aminobenzoic acid)?
Which local anesthetic is LEAST likely to cause an allergic reaction because it is not metabolized to PABA (para-aminobenzoic acid)?
Epinephrine is often co-administered with lidocaine to achieve which of the following effects?
Epinephrine is often co-administered with lidocaine to achieve which of the following effects?
Why is bupivacaine not recommended for IV regional anesthesia (Bier block)?
Why is bupivacaine not recommended for IV regional anesthesia (Bier block)?
A patient is taking a sulfonamide antibiotic. Which topical anesthetic should be avoided?
A patient is taking a sulfonamide antibiotic. Which topical anesthetic should be avoided?
What property of local anesthetics is MOST directly related to their potency?
What property of local anesthetics is MOST directly related to their potency?
Which of the following medications blocks T-type calcium channels in the thalamus, making it a primary treatment option for absence seizures?
Which of the following medications blocks T-type calcium channels in the thalamus, making it a primary treatment option for absence seizures?
A patient is prescribed a medication that irreversibly inhibits GABA-transaminase. What effect would this medication have on GABA levels in the central nervous system?
A patient is prescribed a medication that irreversibly inhibits GABA-transaminase. What effect would this medication have on GABA levels in the central nervous system?
Which of the following antiepileptic drugs has a dual mechanism of action involving both blocking calcium channels and stimulating GABA transmission?
Which of the following antiepileptic drugs has a dual mechanism of action involving both blocking calcium channels and stimulating GABA transmission?
Which of the following strategies is LEAST likely to effectively block neuronal hyperexcitability in the treatment of epilepsy?
Which of the following strategies is LEAST likely to effectively block neuronal hyperexcitability in the treatment of epilepsy?
A patient taking ramelteon for insomnia reports that the medication is not working effectively. Which of the following instructions should the healthcare provider give to improve the drug's efficacy?
A patient taking ramelteon for insomnia reports that the medication is not working effectively. Which of the following instructions should the healthcare provider give to improve the drug's efficacy?
Why is flumazenil effective in reversing benzodiazepine overdoses, while there is no equivalent antidote for barbiturate overdoses?
Why is flumazenil effective in reversing benzodiazepine overdoses, while there is no equivalent antidote for barbiturate overdoses?
Which of the following 'Z drugs' shares a parent structure with cyclopyrrolones?
Which of the following 'Z drugs' shares a parent structure with cyclopyrrolones?
Which amino acid serves as the direct precursor for the synthesis of GABA?
Which amino acid serves as the direct precursor for the synthesis of GABA?
What is the correct enzymatic sequence involved in the synthesis of norepinephrine from tyrosine?
What is the correct enzymatic sequence involved in the synthesis of norepinephrine from tyrosine?
What enzyme directly facilitates the conversion of glutamate to GABA?
What enzyme directly facilitates the conversion of glutamate to GABA?
What is the primary mechanism of action of buspirone in treating generalized anxiety disorder?
What is the primary mechanism of action of buspirone in treating generalized anxiety disorder?
A patient is prescribed spironolactone. Concurrent use of which of the following medication classes would increase the risk of hyperkalemia?
A patient is prescribed spironolactone. Concurrent use of which of the following medication classes would increase the risk of hyperkalemia?
Flutamide is often used in combination with a GnRH agonist for the treatment of prostate cancer. What is flutamide's mechanism of action?
Flutamide is often used in combination with a GnRH agonist for the treatment of prostate cancer. What is flutamide's mechanism of action?
A patient on hormonal contraceptives reports breakthrough bleeding early in the cycle and light menses. Which hormonal imbalance is MOST likely the cause?
A patient on hormonal contraceptives reports breakthrough bleeding early in the cycle and light menses. Which hormonal imbalance is MOST likely the cause?
In what clinical scenario are estrogen receptor agonists commonly indicated?
In what clinical scenario are estrogen receptor agonists commonly indicated?
Which of the following is the primary mechanism of action for aromatase inhibitors?
Which of the following is the primary mechanism of action for aromatase inhibitors?
Which of the following aromatase inhibitors is considered irreversible?
Which of the following aromatase inhibitors is considered irreversible?
A post-menopausal woman with tamoxifen-resistant breast cancer is prescribed an aromatase inhibitor. What is the most likely mechanism by which this drug will exert its therapeutic effect?
A post-menopausal woman with tamoxifen-resistant breast cancer is prescribed an aromatase inhibitor. What is the most likely mechanism by which this drug will exert its therapeutic effect?
Raloxifene is described as a selective estrogen receptor modulator (SERM). What accurately describes its activity at the estrogen receptor in bone tissue?
Raloxifene is described as a selective estrogen receptor modulator (SERM). What accurately describes its activity at the estrogen receptor in bone tissue?
What is the primary rationale for using sulfate-conjugated estrogens instead of 17β-estradiol in certain hormone therapies?
What is the primary rationale for using sulfate-conjugated estrogens instead of 17β-estradiol in certain hormone therapies?
Which of the following represents the correct enzymatic conversion in the biosynthesis of catecholamines?
Which of the following represents the correct enzymatic conversion in the biosynthesis of catecholamines?
Which of the following amino acids serves as the direct precursor for the synthesis of GABA?
Which of the following amino acids serves as the direct precursor for the synthesis of GABA?
A patient is taking zolpidem for insomnia. Which of the medication combinations would raise a concern for a drug-drug interaction (DDI)?
A patient is taking zolpidem for insomnia. Which of the medication combinations would raise a concern for a drug-drug interaction (DDI)?
A patient is starting carbamazepine therapy. What should the healthcare provider consider as a significant contraindication?
A patient is starting carbamazepine therapy. What should the healthcare provider consider as a significant contraindication?
A patient is prescribed lamotrigine for bipolar disorder. Which concurrent medication could increase the risk of serious skin rashes, and what action should be taken?
A patient is prescribed lamotrigine for bipolar disorder. Which concurrent medication could increase the risk of serious skin rashes, and what action should be taken?
A patient taking phenytoin is also prescribed a new medication that induces CYP2C9 enzymes. What effect would this enzyme induction likely have on phenytoin serum concentrations?
A patient taking phenytoin is also prescribed a new medication that induces CYP2C9 enzymes. What effect would this enzyme induction likely have on phenytoin serum concentrations?
Which of the following is a key mechanism of action for many antiepileptic drugs (AEDs)?
Which of the following is a key mechanism of action for many antiepileptic drugs (AEDs)?
Felbamate can be used as an antiepileptic drug because of its ability to block which type of receptor?
Felbamate can be used as an antiepileptic drug because of its ability to block which type of receptor?
Which of the following best describes how neuronal depolarization is achieved?
Which of the following best describes how neuronal depolarization is achieved?
Which of the following is a characteristic of inhaled anesthetics regarding their mechanism of action?
Which of the following is a characteristic of inhaled anesthetics regarding their mechanism of action?
Flashcards
Isoflurane
Isoflurane
Inhalation anesthetic causing decreased blood pressure and increased ICP.
Sevoflurane
Sevoflurane
Medium high potency inhalation anesthetic, avoid in QT prolongation.
Desflurane
Desflurane
Fastest onset inhalation anesthetic, low potency, provides muscle relaxation.
IV Anesthetics
IV Anesthetics
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Methohexital
Methohexital
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Ketamine
Ketamine
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Local Anesthetics
Local Anesthetics
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Ester vs Amide Anesthetics
Ester vs Amide Anesthetics
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Bupivacaine
Bupivacaine
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Lipid Solubility
Lipid Solubility
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Carbamazepine
Carbamazepine
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Oxcarbazepine
Oxcarbazepine
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Lamotrigine
Lamotrigine
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Valproic Acid
Valproic Acid
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Benzodiazepines
Benzodiazepines
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Phenobarbital
Phenobarbital
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Levetiracetam
Levetiracetam
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Topiramate
Topiramate
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Calcium Channel Blockade
Calcium Channel Blockade
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Gabapentin
Gabapentin
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Felbamate
Felbamate
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Ethosuximide
Ethosuximide
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Tiagabine
Tiagabine
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Vigabatrin
Vigabatrin
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Flumazenil
Flumazenil
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Z Drugs
Z Drugs
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GABA Synthesis
GABA Synthesis
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Buspirone
Buspirone
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Hormonal Contraceptives Effects
Hormonal Contraceptives Effects
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Catecholamine Synthesis
Catecholamine Synthesis
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Aromatase Inhibitors
Aromatase Inhibitors
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Tamoxifen
Tamoxifen
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Exemestane
Exemestane
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GABA Biosynthesis
GABA Biosynthesis
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Catecholamines
Catecholamines
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Serotonin
Serotonin
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Norepinephrine DDI
Norepinephrine DDI
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Phenytoin
Phenytoin
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Sulfate-Conjugated Estrogens
Sulfate-Conjugated Estrogens
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Stimulation of GABAergic Transmission
Stimulation of GABAergic Transmission
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NMDA Receptor Blockade
NMDA Receptor Blockade
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Depolarization
Depolarization
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Hyperpolarization
Hyperpolarization
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Inhaled Anesthetics
Inhaled Anesthetics
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Study Notes
Antiepileptic Strategies and Drugs
- Sodium Channel Blockade: Drugs like carbamazepine, oxcarbazepine, lamotrigine, phenytoin, valproic acid, zonisamide, lacosamide, and topiramate target sodium channels to prevent neuronal hyperexcitability.
- GABAergic Stimulation: Benzodiazepines (lorazepam, diazepam, clonazepam, clorazepate), phenobarbital, and levetiracetam enhance GABAergic transmission, the primary inhibitory neurotransmitter.
- Calcium Channel Blockade: Oxcarbazepine, levetiracetam, pregabalin, and gabapentin are examples of drugs that block calcium channels, reducing neuronal excitability.
- Glutamate Receptor Blockade: Felbamate and perampanel act as antagonists at glutamate receptors (NMDA and AMPA), reducing excitatory signaling.
- T-type Calcium Channel Blockade: Ethosuximide specifically blocks T-type calcium channels in the thalamus, targeting particular seizure types.
- GABA Metabolism Inhibitors: Tiagabine blocks GABA transporter; vigabatrin inhibits GABA-transaminase (GABA-T), preventing GABA breakdown.
Multiple MOA Drugs
- Levetiracetam inhibits calcium influx and enhances GABA transmission.
Neuronal Hyperexcitability Blockade Strategies
- Voltage-gated channel blockade: Sodium and calcium channel blockers.
- Inhibitory neurotransmitter enhancement: GABAergic stimulation.
- Excitatory neurotransmitter reduction: Glutamate receptor blockade.
Ramelteon Use
- Ramelteon is a melatonin receptor agonist used for insomnia, taken 30 minutes before sleep.
Benzodiazepine Overdose Treatment
- Flumazenil is a competitive benzodiazepine antagonist, reversing benzodiazepine overdose effects.
Z-Drugs Parent Structures
- Zolpidem (imidazopyridine), zaleplon (pyrazolopyrimidine), zopiclone and eszopiclone (cyclopyrrolone).
Neurotransmitter Synthesis
- Dopamine: Synthesized from tyrosine.
- Serotonin: Synthesized from tryptophan.
- Norepinephrine: Synthesized from tyrosine, a precursor to dopamine.
- GABA: Derived from glutamate by glutamate decarboxylase.
- Glutamate: Synthesized from glutamine.
- Acetylcholine: Synthesized from choline and acetyl CoA.
Catecholamine Synthesis
- Tyrosine → L-DOPA → Dopamine → Norepinephrine → Epinephrine (enzymes sequential).
GABA Synthesis
- Glutamate → GABA (via glutamate decarboxylase).
Buspirone (Buspar)
- Anxiolytic with 5-HT1A and 5-HT2 receptor agonist action, but different from GABA-receptor targets.
Spironolactone Drug Interactions
- Increased risk of hyperkalemia with NSAIDs, ARBs, and ACE inhibitors.
Androgen Receptor Antagonists
- Flutamide, apalutamide, bicalutamide, and nilutamide are non-steroidal androgen receptor antagonists used in prostate cancer treatment.
Estrogen Receptor Agonists/Antagonists
- Tamoxifen, bazedoxifene, and raloxifene are examples of selective estrogen receptor modulators (SERMs).
Aromatase Inhibitors
- Aromatase inhibitors (exemestane, anastrozole, letrozole) inhibit aromatase, reducing estrogen levels.
Sulfate-Conjugated Estrogens
- Sulfate-conjugated estrogens offer advantages in oral bioavailability and sustained release compared to 17β-estradiol.
Local Anesthetics: Ester vs. Amide
- Esters: Benzocaine, procaine, tetracaine (more allergenic, rapid onset, short duration).
- Amides: Lidocaine, mepivacaine, bupivacaine, levobupivacaine, ropivacaine, articaine, prilocaine (less allergenic, slower onset, longer duration).
Local Anesthetics and Antibiotics
- Some local anesthetics can reduce antibiotic permeability.
Fatal IV Local Anesthetic
- Bupivacaine.
Lipophilicity and Diffusability
- Local anesthetic diffusability correlates with its lipid solubility.
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Description
This article provides an overview of antiepileptic drugs and their mechanisms of action. It covers sodium channel blockade, GABAergic stimulation, calcium channel blockade, glutamate receptor blockade and GABA metabolism inhibitors. Specific drugs like carbamazepine, lamotrigine, benzodiazepines, and ethosuximide are mentioned.
