Central Nervous System Overview and Neurotransmitters
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Questions and Answers

Which antiepileptic drug is specifically noted for its efficacy against absence seizures?

  • Gabapentin
  • Felbamate
  • Ethosuximide (correct)
  • Eslicarbazepine
  • Which medication has the potential for severe adverse effects such as aplastic anaemia and hepatitis?

  • Ethosuximide
  • Felbamate (correct)
  • Carisbamate
  • Lamotrigine
  • What characterizes Lennox-Gastaut Syndrome (LGS)?

  • Complete independence from treatments
  • Resistance to medication (correct)
  • Cognitive enhancement
  • Single type of seizure
  • Which drug listed is considered safer for use in the elderly due to its lower adverse effects?

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

    Which of the following drugs has multiple proposed mechanisms including blocking NMDA-glutamate receptors?

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

    What is a common adverse effect of Ethosuximide?

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

    Which of the following is an analogue of GABA and primarily acts on P/Q type calcium channels?

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

    Which drug is noted for requiring blood counts due to the risk of eosinophilia?

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

    Which neurotransmitter is primarily known for its role as an inhibitory neurotransmitter in the brain?

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

    What is the primary therapeutic use of Diazepam in the treatment of epilepsy?

    <p>Febrile convulsions in infants (D)</p> Signup and view all the answers

    Which of the following drugs blocks the sodium channels as part of its mechanism for treating epilepsy?

    <p>Carbamazepine (B), Oxcarbazepine (D)</p> Signup and view all the answers

    Which of the following is NOT a common adverse effect associated with the use of benzodiazepines in epilepsy management?

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

    What pharmacokinetic property of Carbamazepine can lead to variations in its serum concentrations?

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

    Which of the following antiepileptic drugs is least likely to induce the CYP3A4 and UGT systems?

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

    Which part of the central nervous system is primarily responsible for processing sensory information?

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

    What does GABA primarily bind to in the brain as part of its function?

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

    What is the main mechanism of action of Phenytoin?

    <p>Blocks voltage-gated Na channels (C)</p> Signup and view all the answers

    What are the primary side effects associated with Phenytoin?

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

    Which statement about Levetiracetam is true?

    <p>It is excreted mostly unchanged in urine (C)</p> Signup and view all the answers

    Which antiepileptic medication is most likely to increase the serum concentration of Rufinamide?

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

    What distinguishes Fosphenytoin from Phenytoin?

    <p>Fosphenytoin can be administered intramuscularly (C)</p> Signup and view all the answers

    What is the therapeutic range for Phenytoin plasma concentration?

    <p>40-100 μmol/l (C)</p> Signup and view all the answers

    Which antiepileptic drug primarily acts as a positive allosteric modulator of GABA-A receptors?

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

    Which of the following is a life-threatening hypersensitivity reaction associated with antiepileptic drugs?

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

    What is the mechanism of action for Lacosamide?

    <p>Slow inactivation of Na channels (D)</p> Signup and view all the answers

    What is the mechanism of action for Stiripentol?

    <p>Prolongs GABAergic transmission (B)</p> Signup and view all the answers

    Which adverse effect is associated with retigabine when used as an antiepileptic agent?

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

    Which of the following is NOT a treatment use of antiepileptic drugs?

    <p>Cognitive behavioral therapy (C)</p> Signup and view all the answers

    What is a common side effect of antiepileptic drugs that can affect the skeletal system?

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

    Which antiepileptic agent is known for its teratogenic effects when taken during pregnancy?

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

    Which mechanism is primarily targeted by Tiagabine in order to exert its antiepileptic effects?

    <p>Increase of GABA availability (B)</p> Signup and view all the answers

    Which of the following drugs is NOT used for the treatment of painful conditions?

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

    What is the primary mechanism of action of Zonisamide?

    <p>Block Na and T-type Ca channels (C)</p> Signup and view all the answers

    Which side effect is NOT associated with Zonisamide?

    <p>Neural tube defects (C)</p> Signup and view all the answers

    For what condition is Tiagabine mainly used?

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

    What is a significant unwanted effect of Topiramate?

    <p>Weight loss due to appetite suppression (C)</p> Signup and view all the answers

    What characterizes the mechanism of Valproic acid?

    <p>Inhibition of GABA transaminase (B)</p> Signup and view all the answers

    Which condition should NOT use Tiagabine?

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

    What is a potential side effect of Vigabatrin?

    <p>Peripheral visual field defects (D)</p> Signup and view all the answers

    Which statement about Topiramate is true?

    <p>It has similar action to phenytoin but with less severe side effects. (D)</p> Signup and view all the answers

    Flashcards

    What is the cerebrum?

    The cerebrum is the largest part of the brain, responsible for higher-level functions like thinking, memory, and language.

    What is the hypothalamus?

    The hypothalamus controls many vital functions, including body temperature, hunger, thirst, and sleep.

    What is the thalamus?

    The thalamus is a relay center for sensory information, sending it to the appropriate parts of the cerebrum.

    What are benzodiazepines?

    Benzodiazepines are a class of drugs that enhance the effects of GABA, a neurotransmitter that inhibits nerve activity.

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    What is Clonazepam?

    Clonazepam is a potent and long-acting benzodiazepine used for epilepsy and panic disorders.

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    What is Diazepam?

    Diazepam is a benzodiazepine used for short-term therapy of epilepsy and muscle spasms.

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    How does Carbamazepine work?

    Carbamazepine blocks sodium channels, preventing nerve impulses from firing too rapidly, which can be helpful in managing epilepsy.

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    How does Oxcarbazepine differ from Carbamazepine?

    Oxcarbazepine is similar to carbamazepine, but it's a less potent inducer of liver enzymes, making it a good choice for people with liver problems.

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    Phenobarbital

    A long-acting barbiturate (1-2 days) that enhances the inhibitory effects of GABA-mediated neurons. It is used to treat generalized tonic-clonic seizures. The mechanism of action is to enhance the effect of GABA, a neurotransmitter that has an inhibitory effect on the brain.

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    Carbamazepine

    This medication is metabolized by the UGT pathway, which could lead to drug interactions with other medications like antiepileptic agents. It is important to note that the levels of the drug are decreased by carbamazepine and phenytoin, while it is increased by valproate.

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    What is the mechanism of action of Phenytoin?

    The main mechanism of action is to block voltage-gated Na channels. This medication is effective in treating partial and generalized tonic-clonic seizures but is not effective for absence epilepsy. It is important to note that the therapeutic range of phenytoin is quite narrow and needs close monitoring of plasma concentrations.

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    What is Fosphenytoin and how does it compare to phenytoin?

    This medication is an alternative to Phenytoin. It can be administered intramuscularly unlike phenytoin. It is also used to treat partial and generalized tonic-clonic seizures.

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    Rufinamide

    The main mechanism of action is to inactivate Na channels. It is used as an adjunctive treatment for Lennox-Gastaut syndrome. It is important to note that the serum concentrations are affected by food, other medications like carbamazepine and phenytoin, and even birth control tablets.

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    Stiripentol

    It is a newer antiepileptic drug that works by prolonging GABAergic transmission. It is used as adjunctive therapy in children with epilepsy. It is important to note that it has some efficacy in children.

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    What is Lennox-Gastaut Syndrome (LGS)?

    A type of epilepsy characterized by frequent, varied seizures with medication resistance, behavioral issues and cognitive impairment.

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    Eslicarbazepine

    Eslicarbazepine is an antiepileptic drug primarily used for partial seizures, but is also effective for trigeminal neuralgia (TN).

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    Ethosuximide

    Ethosuximide is most effective against absence seizures (petit mal) with little effect on other seizure types.

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    Felbamate

    Felbamate is an anti-epileptic drug with a broad spectrum of activity, effective against various seizure types. It was used for Lennox-Gastaut Syndrome (LGS). But its use is limited due to its associated risks of aplastic anemia and hepatitis.

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    Carisbamate

    Carisbamate is a newer drug in clinical trials for epilepsy. It has a lower risk of aplastic anemia compared to Felbamate.

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    Gabapentin and Pregabalin

    Gabapentin and Pregabalin are anticonvulsant medications that work primarily by affecting P/Q type Ca channels.

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    Lamotrigine

    Lamotrigine is a broad-spectrum antiepileptic drug, effective against various types of seizures including absence seizures. It's also used for bipolar disorder.

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    What is Hyponatremia?

    Hyponatremia is a medical condition characterized by a low sodium level in the blood. It can be a side effect of some medications, including eslicarbazepine.

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    Antiepileptic Drugs (AEDs)

    A group of medications used to prevent or reduce the frequency of seizures in people with epilepsy.

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    How do AEDs like Valproic Acid work?

    AEDs can increase the activity of GABA, an inhibitory neurotransmitter, by inhibiting GABA transaminase, which breaks down GABA. This results in more GABA available to bind to GABA receptors and reduce neuronal activity.

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    How do Phenytoin and Carbamazepine work?

    AEDs like Phenytoin and Carbamazepine block sodium channels, reducing the influx of sodium ions into neurons, thus decreasing neuronal excitability and preventing seizure activity.

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    How does Lacosamide work?

    AEDs like Lacosamide slow the inactivation of sodium channels, prolonging their closed state and reducing neuronal excitability.

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    Zonisamide's Mechanism

    Zonisamide is an antiepileptic drug that blocks sodium and T-type calcium channels and enhances GABAergic transmission.

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    How do AEDs like Ethosuximide and Zonisamide work?

    AEDs can also work by blocking calcium channels. This reduces the influx of calcium ions into neurons, which are essential for neurotransmitter release and neuronal excitability.

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    How do AEDs like Topiramate and Felbamate work?

    AEDs can also modulate glutamate receptors, which are crucial for excitatory neurotransmission. Reducing glutamate activity helps control neuronal hyperactivity and seizures.

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    Zonisamide's Uses and Side Effects

    Zonisamide is approved for use in patients with partial epilepsy, but it can cause adverse effects like ataxia, confusion, sedation, and concentration issues.

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    What are some common side effects of AEDs?

    AEDs can cause adverse effects such as nausea, vomiting, sedation, ataxia (loss of coordination), rash, hyponatremia (low sodium), weight changes, osteoporosis, and teratogenicity (birth defects).

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    Tiagabine's Mechanism and Use

    Tiagabine inhibits the GABA transporter-1, increasing GABA levels in the brain. It is typically used as an add-on therapy for partial seizures.

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    What are some other uses of AEDs besides epilepsy?

    AEDs can also be used to treat a variety of other conditions, including neuropathic pain, migraine, and bipolar disorder, due to their effects on neurotransmission.

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    Topiramate's Multifaceted Action

    Topiramate is a broad-spectrum antiepileptic drug that affects multiple neurotransmitter systems, including sodium channels, calcium channels, GABA receptors, and glutamate receptors.

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    Topiramate vs Phenytoin

    Topiramate has similar effectiveness to phenytoin but with fewer side effects and a distinct pharmacokinetic profile.

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    Valproic Acid and Divalproex's Mechanisms

    Valproic acid and divalproex are antiepileptic drugs that inhibit T-type calcium channels, block sodium channels, and inhibit GABA transaminase.

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    Vigabatrin's Action and Efficacy

    Vigabatrin is a powerful and irreversible inhibitor of GABA transaminase, significantly increasing GABA levels in the brain. It is effective for many types of epilepsy, particularly in patients resistant to other treatments.

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    Vigabatrin's Side Effects

    While vigabatrin is effective against epilepsy, it can cause unwanted side effects, including peripheral visual field defects, sedation, depression, psychotic disturbances, and hallucinations.

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    Study Notes

    Central Nervous System (CNS) Overview

    • The CNS comprises the cerebrum, diencephalon, brainstem, and cerebellum.
    • The cerebrum is responsible for higher-level cognitive functions.
    • The diencephalon includes the hypothalamus (regulates hormones and body functions) and the thalamus (relay center for sensory information).
    • The pineal gland is part of the epithalamus and involved in hormone secretion.
    • The brainstem contains the midbrain, pons, and medulla oblongata, controlling vital functions such as breathing and heart rate.
    • The cerebellum coordinates movement and balance.
    • The spinal cord connects the brain to the rest of the body.

    Neurotransmitters

    • Neurotransmitters are chemical messengers in the brain.
    • Over 100 unique neurotransmitters are identified.
    • Well-known neurotransmitters include dopamine, serotonin, GABA, glutamate, glycine, acetylcholine, norepinephrine/noradrenaline, and epinephrine/adrenaline.

    Central Nervous System Pharmacology: Antiepileptic Drugs

    • The study details anti-epileptic drugs, their mechanisms, side effects, and other uses.
    • The chapter focuses on benzodiazepines, carbamazepine, oxcarbazepine, ethosuximide, felbamate, levetiracetam, phenobarbital, phenytoin, rufinamide, stiripentol, zonisamide, and tiagabine.

    Benzodiazepines

    • Benzodiazepines bind to GABA receptors.
    • Clonazepam, diazepam, clorazepate, and lorazepam are potent benzodiazepines.
    • Diazepam is used in short-term epilepsy therapy, effective for treating febrile convulsions in infants and children (rectal administration).
    • Sedation is a common side effect and shouldn't be stopped abruptly.

    Carbamazepine

    • Carbamazepine blocks sodium channels.
    • It treats various epilepsy types (excluding absence and myoclonic).
    • It's also useful for neuropathic pain (trigeminal neuralgia), bipolar disorders, and cancer pain.
    • Serum concentrations vary considerably due to absorption and metabolism variations.
    • Some metabolites are active and may not be well-tolerated by the elderly.
    • Commonly observed side effects include gastrointestinal issues, neurological problems, hematological problems, allergic reactions, anticholinergic effects, and cardiac issues like edema.

    Oxcarbazepine and Ethosuximide

    • Oxcarbazepine is a less potent inducer of specific enzyme systems (CYP3A4 and UGT).
    • It's effective for partial onset seizures and is associated with a higher risk of hyponatremia.
    • Ethosuximide primarily targets T-type calcium and potassium channels and is particularly effective for absence seizures.
    • Nausea, vomiting, and anorexia are common side effects of ethosuximide.

    Felbamate

    • Felbamate's mechanism involves blocking voltage-gated sodium channels and potentiating GABA actions, as well as blocking NMDA receptors.
    • It's indicated for treating specific, potentially refractory, epilepsy types like Lennox-Gastaut syndrome.
    • Common side effects include nausea, irritability, and insomnia, and more serious side effects such as aplastic anemia and hepatitis.

    Levetiracetam and Phenobarbital and Brivaracetam

    • Levetiracetam acts by affecting a specific protein, SV2A. It is used in partial and generalized tonic-clonic seizures.
    • Phenobarbital is a long-acting barbiturate that enhances the impact of GABA activity, commonly used for status epilepticus.
    • Brivaracetam has higher binding affinity to SV2A.

    Phenytoin and Fosphenytoin

    • Phenytoin and Fosphenytoin block voltage-gated sodium channels, effective against partial and generalized tonic-clonic seizures. Phenytoin is usually taken orally while Fosphenytoin can be given intravenously or intramuscularly.
    • Phenytoin's metabolism is saturable, requiring careful monitoring of serum levels, to avoid adverse effects and to maintain it in a therapeutic range.
    • Potential side effects include nystagmus, ataxia, vertigo, headache, and increased seizure frequency.

    Rufinamide and Stiripentol

    • Rufinamide's mechanism involves sodium channel inactivation and GABA reuptake inhibition making it effective as an adjunctive therapy for Lennox-Gastaut syndrome.
    • Serum concentration levels are influenced by food intake, as well as other antiepileptic agents.
    • Stiripentol prolongs GABAergic transmission and is an adjunctive therapy for use in children.

    Zonisamide and Tiagabine

    • Zonisamide affects sodium and calcium ion channels and increases GABA transmission and is effective in treating partial epilepsy.
    • Side effects include weight loss, loss of appetite, oligohidrosis, elevated body temperature, and kidney stones.
    • Tiagabine, an inhibitor of GABA transporter, is primarily used in add-on therapy for partial seizures.

    Topiramate

    • Topiramate acts on voltage-gated sodium channels, blocking calcium currents and enhancing GABA-A receptors.
    • It's effective against varied types of epilepsy and migraines.
    • Side effects include lessened sedation, and drug interactions.

    Valproic Acid and Divalproex

    • Valproic acid and divalproex are effective in several epilepsy types, including absence and myoclonic seizures.
    • They influence GABA transaminase (similar to vigabatrin) and block sodium channels.
    • They're used to treat bipolar disorders, and a notable concern is potential teratogenicity.

    Vigabatrin

    • Vigabatrin is an irreversible inhibitor of GABA transaminase, increasing GABA levels in the brain.
    • It's suitable for treating a wide range of epilepsy types.
    • Potential side effects include peripheral visual field defects.

    Novel Mechanisms for New Antiepileptic Agents

    • Retigabine activates neuronal potassium channels.
    • Lacosamide slowly inactivates sodium channels.
    • Tonabersat inhibits neuronal gap junctions.
    • Ganaxolone is a positive allosteric modulator.

    Adverse Effects of Antiepileptic Agents

    • Common adverse effects include nausea, vomiting, sedation, ataxia, rash, hyponatremia, body weight changes, and osteoporosis.

    Pregnancy and Antiepileptic Drugs

    • Antiepileptic medications can induce hepatic enzymes, affect oral contraceptive efficacy, and result in vitamin K deficiency in newborns.
    • Teratogenic risks exist, and pregnancy planning is essential. Adjusting the lowest effective dose during pregnancy may be needed.

    Other Uses of Antiepileptic Drugs

    • Antiepileptic drugs are used for neuropathic pain, migraine prophylaxis, bipolar disorders, and anxiety disorders.

    The End

    • The study concludes with a statement that the end of one chapter is the start of another.

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    Description

    This quiz covers key aspects of the Central Nervous System (CNS), including its major components like the cerebrum, diencephalon, brainstem, and cerebellum. It also explores neurotransmitters, their functions, and their significance in brain activity. Test your knowledge on these fundamental topics in neuroscience.

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