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</p> Signup and view all the answers

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

    <p>Felbamate</p> Signup and view all the answers

    What is a common adverse effect of Ethosuximide?

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

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

    <p>Ethosuximide</p> Signup and view all the answers

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

    <p>GABA</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</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</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</p> Signup and view all the answers

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

    <p>Autoinduction</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</p> Signup and view all the answers

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

    <p>Thalamus</p> Signup and view all the answers

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

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

    What is the main mechanism of action of Phenytoin?

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

    What are the primary side effects associated with Phenytoin?

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

    Which statement about Levetiracetam is true?

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

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

    <p>Carbamazepine</p> Signup and view all the answers

    What distinguishes Fosphenytoin from Phenytoin?

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

    What is the therapeutic range for Phenytoin plasma concentration?

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

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

    <p>Ganaxolone</p> Signup and view all the answers

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

    <p>Rashes</p> Signup and view all the answers

    What is the mechanism of action for Lacosamide?

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

    What is the mechanism of action for Stiripentol?

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

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

    <p>Euphoria</p> Signup and view all the answers

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

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

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

    <p>Osteoporosis</p> Signup and view all the answers

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

    <p>Valproate</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</p> Signup and view all the answers

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

    <p>Ethosuximide</p> Signup and view all the answers

    What is the primary mechanism of action of Zonisamide?

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

    Which side effect is NOT associated with Zonisamide?

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

    For what condition is Tiagabine mainly used?

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

    What is a significant unwanted effect of Topiramate?

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

    What characterizes the mechanism of Valproic acid?

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

    Which condition should NOT use Tiagabine?

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

    What is a potential side effect of Vigabatrin?

    <p>Peripheral visual field defects</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.</p> Signup and view all the answers

    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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    Central Nervous System Pharmacology (Week 10) PDF

    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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