CNS Medications and Neurotransmitters
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Questions and Answers

Which age group has an increased risk of suicidal thinking and behavior when using antidepressants?

  • Children and adolescents (correct)
  • Elderly patients over 65
  • Adults aged 25-34
  • Adults aged 35-44
  • Adults over the age of 24 have an increased risk of suicidal thoughts when taking antidepressants.

    False

    What is the primary mechanism of action for selective serotonin reuptake inhibitors (SSRIs)?

    Inhibit presynaptic serotonin reuptake by inhibition of the 5-HT transporter

    SSRIs help to increase the level of serotonin in the ______.

    <p>synaptic cleft</p> Signup and view all the answers

    Match the following SSRIs with their respective adverse effects:

    <p>GI adverse effects = Take with small snack/meal Headache = Adjust dose to evening Insomnia/Sedation = Adjust dose to morning or evening as necessary Anxiety = Slow dose titration</p> Signup and view all the answers

    What is the primary mechanism of action of Valbenazine?

    <p>Inhibits vesicular monoamine transporter 2 (VMAT2)</p> Signup and view all the answers

    Valbenazine can cause coma, seizures, or even death at toxic doses.

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

    List one medication class known to affect lithium concentration.

    <p>Thiazide diuretics</p> Signup and view all the answers

    Valbenazine is indicated for the treatment of __________.

    <p>tardive dyskinesia</p> Signup and view all the answers

    Match the following medications with their potential effects or interactions:

    <p>Valbenazine = Regulates monoamine uptake Lithium = Requires monitoring for toxicity Furosemide = Can increase lithium levels NSAIDs = May affect serum sodium levels</p> Signup and view all the answers

    Which medication is specifically used for absence seizures?

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

    Valproic acid is contraindicated in the treatment of absence seizures.

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

    What is the therapeutic level range for Ethosuximide?

    <p>50-100 mcg/ml</p> Signup and view all the answers

    The _____ are often treatment resistant and may require special attention.

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

    Match the following medications with their specific use:

    <p>Ethosuximide = Absence seizures Valproic acid = Multiple seizure types Clonazepam = Anxiety disorders Topiramate = Generalized seizures</p> Signup and view all the answers

    Which drug should be avoided in the treatment of myoclonic seizures?

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

    Ethosuximide has significant drug interactions with other medications.

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

    What are some common adverse effects of Ethosuximide?

    <p>GI distress, lethargy, fatigue, headache, dizziness, hiccup, euphoria, psychosis</p> Signup and view all the answers

    What is a common side effect associated with cholinergic agonists at M4 receptors in the mouth?

    <p>Excessive salivation</p> Signup and view all the answers

    Clozapine should be prescribed to patients with adherence issues.

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

    What are the initial dosing considerations for clozapine after the patient has missed a dose for more than 48 hours?

    <p>The dose must be re-titrated from the initial 25 mg QHS.</p> Signup and view all the answers

    In the treatment of EPS, __________ is used at a dose of 25-50 mg po or IM.

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

    Which of the following antipsychotics carries a high risk of EPS?

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

    Tardive dyskinesia is a permanent condition that may occur with long-term antipsychotic usage.

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

    Match the following treatments with their appropriate effects for EPS:

    <p>Diphenhydramine = 25-50 mg po or IM for EPS Benztropine = 0.5 – 4 mg po, usually BID Propranolol = May help with akathisia Clonazepam = Adjunctive treatment for tardive dyskinesia</p> Signup and view all the answers

    What are some symptoms of tardive dyskinesia?

    <p>Repetitive, involuntary movements such as tongue movements, facial grimacing, and limb dyskinesia.</p> Signup and view all the answers

    What is the common adverse effect of Lamotrigine (Lamictal)?

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

    Valproic Acid (Depakote) is considered a liver enzyme inhibitor.

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

    What is the therapeutic level range for Valproic Acid in mcg/ml?

    <p>50-100</p> Signup and view all the answers

    Lamotrigine should be titrated _____ to reduce the risk of rash.

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

    Match the following adverse effects with their classification (common or rare):

    <p>Dizziness = Common Hepatic failure = Rare Skin rash including TENS/SJS = Rare Nausea = Common</p> Signup and view all the answers

    What is the loading dose range for Valproic Acid?

    <p>15-45 mg/kg</p> Signup and view all the answers

    Somnolence is a rare adverse effect of Lamotrigine.

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

    What mechanism of action describes how Valproic Acid works on sodium channels?

    <p>prolong inactivated state</p> Signup and view all the answers

    Which receptor blockade in the nigrostriatal pathway can lead to movement disorders?

    <p>D2 receptors</p> Signup and view all the answers

    Antipsychotics can be used effectively in patients with dementia-related psychosis.

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

    Name a common anticholinergic medication that may be required as adjunct therapy for high-potency FGAs.

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

    The first generation antipsychotic chlorpromazine is classified as a ______ potency agent.

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

    Match the following first generation antipsychotics with their potency:

    <p>Chlorpromazine = Low Haloperidol = High Trifluoperazine = High Perphenazine = Mid</p> Signup and view all the answers

    What is a major adverse effect associated with second generation antipsychotics compared to first generation?

    <p>Weight gain</p> Signup and view all the answers

    All antipsychotics have the same level of cardiovascular risk.

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

    What effect does smoking have on the CYP450 1A2 pathway?

    <p>Induces it by 20-30%</p> Signup and view all the answers

    Patients treated with _______ need to be monitored for extrapyramidal symptoms (EPS).

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

    Which of the following is a side effect associated with long-term use of FGAs?

    <p>Tardive dyskinesia</p> Signup and view all the answers

    Prolactin elevation can occur with the blockade of D2 receptors in the tuberoinfundibular pathway.

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

    Which drug is primarily used for treating acute agitation in hospitalized patients?

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

    Match the following SGA with their trade name:

    <p>Aripiprazole = Abilify Clozapine = Clozaril Olanzapine = Zyprexa Risperidone = Risperdal</p> Signup and view all the answers

    The medication _________ is associated with metabolic abnormalities including weight gain and hyperlipidemia.

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

    Study Notes

    Central Nervous System Medications

    • Objectives for the presentation include reviewing mechanisms of action and adverse effects of commonly used CNS agents, identifying important counseling points for patients prescribed CNS agents, developing an optimal psychotropic regimen, summarizing clinically significant drug interactions, and reviewing key monitoring parameters and contraindications for CNS agents.

    Neurotransmitters

    • GABA and Glycine are major inhibitory neurotransmitters in the CNS.
    • Glycine is present in the spinal cord and brainstem.
    • GABA is present throughout the CNS.
    • Glutamate is the major excitatory neurotransmitter in the CNS.
    • It interacts with multiple receptors (AMPA, KA, NMDA).
    • NMDA receptors are a crucial pharmacological target for glutamate.
    • Serotonin (5-HT) has multiple pathways originating in the raphe nuclei or midline region of the pons/upper brainstem.
    • It's involved in varied functions like perception, mood, and pain.
    • It's a target for antidepressants and antipsychotics.
    • Noradrenaline (NE) is involved in vasoconstriction, tachycardia, increased cardiac output, increased peripheral resistance, and hypertension.
    • It's a target for drugs aimed at improving attention deficit hyperactivity disorder (ADHD).
    • Dopamine (DA) has multiple pathways with different functions including higher-order cognitive functions, reward pathway, and motor function.
    • The tuberoinfundibular pathway regulates prolactin.
    • Acetylcholine (ACh) interacts with muscarinic and nicotinic receptors, exhibiting both excitatory and inhibitory effects.
    • Presynaptic nicotinic receptors regulate neurotransmitter release of glutamate, 5-HT, GABA, DA and NE in the CNS.
    • ACh is hydrolyzed by acetylcholinesterase (AChE).

    Cholinergic Effects/Toxidrome

    • Cholinergic effects display the symptoms of DUMBELS.
    • For examples, diarrhea and sweating are some effects of cholinergic effects.

    ACh Effects

    • Acetylcholine (ACh) affects various bodily systems
    • Ocular: Affects pupil constriction (miosis) and alters the activity of the heart's conduction, inotropy, and dromotropy through reflex.
    • Cardiac: alters sympathetic effects to help decrease peripheral vascular resistance.
    • Respiratory: influences bronchoconstriction and increased secretions.
    • Gastrointestinal influence motility and sphincter activity.
    • Urinary: influences the detrusor muscle and sphincter action.
    • Endocrine: impacts secretions like diaphoresis, siallorrhea, lacrimation and nasopharyngeal activity.

    ANTI-cholinergic Effects

    • Symptoms of ANTI-cholinergic effects display the opposite symptoms of DUMBELS
    • For an example, dry mouth is a symptom of anti-cholinergic effects.

    CNS & Psychiatric Medications

    • The presentation covers a variety of medications with different purposes and classifications
    • Antidepressants, antipsychotics, mood stabilizers, and anxiolytics are among the discussed classifications.

    Treatment of Major Depressive Disorder (MDD)

    • Treatment options for MDD include pharmacotherapy, psychotherapy, and somatic therapies.
    • Somatic therapies encompass electroconvulsive therapy (ECT) and transcranial magnetic stimulation (TMS)
    • Treatment decisions are guided by comorbid conditions, anticipated side effects, medication properties, previous response, and patient preference.

    Antidepressants: Overview

    • This section details different classes of antidepressants including Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs), Atypical antidepressants, Tricyclic antidepressants (TCAs), and Monoamine oxidase inhibitors (MAOIs)
    • It includes a pharmacological diagram describing the mechanism of action of antidepressants.

    Selective Serotonin Reuptake Inhibitors (SSRIs)

    • SSRIs inhibit the presynaptic serotonin reuptake, increasing serotonin levels in the synaptic cleft.
    • Common adverse effects include GI effects, headache, insomnia/sedation, anxiety, sexual dysfunction, SIADH, and discontinuation syndrome.
    • Treatment strategies include taking with small meals, adjusting dosages, switching medications, and slow tapering, among others.

    Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs)

    • SNRIs inhibit the reuptake of both serotonin and norepinephrine, increasing neurotransmitter levels in the synaptic cleft.
    • Clinically significant adverse effects include increased blood pressure when doses are higher.

    Atypical Antidepressants

    • These medications have diverse mechanisms and adverse effects, presenting various approaches to treatment.

    Tricyclic Antidepressants (TCAs)

    • These medications inhibit the reuptake of norepinephrine and serotonin.
    • Adverse effects include orthostatic hypotension, dry mouth, blurry vision, urinary retention, and sedation.

    Monoamine Oxidase Inhibitors (MAOIs)

    • MAOIs inhibit the enzyme monoamine oxidase, increasing the concentration of neurotransmitters like serotonin, norepinephrine, and dopamine in the synapse.
    • These drugs require a tyramine-restricted diet, as interaction with tyramine can lead to a hypertensive crisis.

    Antipsychotics

    • Blockade of D2 receptors in the brain is central to antipsychotic medications' mechanisms of action.
    • Typical antipsychotics (FGAs) primarily block dopamine (D2) receptors.
    • Atypical antipsychotics (SGAs) block both dopamine (D2) and serotonin (5-HT2A) receptors.
    • Blockage of D2 receptors can result in extrapyramidal symptoms (EPS).
    • Increased mortality in dementia-related psychosis has been linked to antipsychotic use.

    SGA Prescribing Considerations

    • Clozapine is often reserved for treatment-resistant cases, necessitating REMS registration.
    • Aripiprazole and lurasidone have higher rates of akathisia.
    • Cost is generally higher for SGAs compared to FGAs.

    Mood Stabilizers

    • Lithium, valproate, lamotrigine, carbamazepine, and oxcarbazepine.

    Lithium

    • Lithium is a monovalent ion similar to sodium, primarily excreted via the kidneys.
    • Its therapeutic index is narrow, requiring careful monitoring of blood levels to avoid toxicity.
    • Common adverse effects include Gl distress, tremor, mental status changes, coma, and seizures.

    Benzodiazepines (BDZs)

    • BDZs enhance the activity of GABA, promoting inhibitory effects in the central nervous system.
    • These medications are categorized by their elimination half-life, which impacts their duration of action.
    • Withdrawal should be tapered to mitigate the risk of seizures in some cases.

    Alternative Anxiolytics

    • These medications offer alternative approaches to managing anxiety.
    • Common choices include hydroxyzine (Atarax), gabapentin (Neurontin), pregabalin (Lyrica), and buspirone (Buspar).
    • Adverse effects can include somnolence, ataxia, weight gain, and peripheral edema.

    Anticonvulsants

    • Anticonvulsants are medications that help manage seizures.
    • Several factors influence medication selection including seizure type, comorbid conditions, safety, tolerability, pharmacokinetics, ease of use, and cost.

    Epilepsy: Seizure Classification

    • Partial seizures are confined to one side of the brain.
    • Generalized seizures involve both hemispheres of the brain.

    Anticonvulsants: Mechanism of Action

    • The mechanism of action of anticonvulsants entails modulation of voltage-gated ion channels, enhancement of synaptic inhibition, and inhibition of synaptic excitation.

    GABA

    • GABA is a neurotransmitter regulating inhibitory effects.

    Glutamate

    • Glutamate is a neurotransmitter predominantly responsible for excitatory effects in the brain.

    Topiramate (Topamax)

    • Topiramate is a carbonic anhydrase inhibitor.
    • Adverse effects may include metabolic acidosis, weight loss, somnolence, fatigue, dizziness, cognitive slowing, paresthesias, nervousness, and confusion.

    Levetiracetam (Keppra)

    • Levetiracetam affects vesicular release of GABA and glutamate.
    • Adverse effects include somnolence, asthenia, ataxia, agitation, and psychosis.

    Lacosamide (Vimpat)

    • Lacosamide preferentially affects slow inactivation of sodium channels, potentially having neurotrophic effects.
    • Adverse effects may include dizziness, headache, nausea, diplopia, and prolonged PR interval, necessitating slow titration.

    Generalized Seizures

    • Myoclonic seizures lack a specific treatment unless they coexist with other seizure types.
    • Atonic seizures often need treatment resistant approaches.

    Ethosuximide (Zarontin)

    • Ethosuximide specifically targets inhibitory pathways on calcium channels.
    • Adverse effects are usually transient, with the possibility for improvement over time or with dose reduction.

    Felbamate (Felbatol)

    • Its mechanism includes inhibition of NMDA receptors and potentiation of GABAergic responses.
    • Adverse effects may involve aplastic anemia and severe hepatitis.

    Valproic Acid (Depakote, Depakene)

    • It prolongs the inactivated state of sodium channels and increases GABA.
    • Common adverse effects include Gl upset, sedation, fine tremor, weight gain, increased appetite, and hair loss, as well as hepatotoxicity.

    Zonisamide (Zonegran)

    • Its mechanism of action involves regulating sodium and calcium channels.
    • Adverse effects can range from drowsiness to cognitive impairment, confusion, poor concentration, and rash.

    Benzodiazepines

    • These agents mainly potentiate the effects of GABA, suppressing nerve activity, and are commonly used to manage acute seizures, especially status epilepticus, with their short half-lives.

    Cannabinoids for Seizures

    • Cannabinoids are used to normalize neuronal function through modulation of intracellular calcium and adenosine signaling.
    • Adverse effects may include vomiting, fatigue, upper respiratory tract infection, and decreased appetite.

    Status Epilepticus and Emergent Seizure Management

    • Emergency measures to manage status epilepticus involve administering benzodiazepines (lorazepam, diazepam, midazolam), phenytoin or fosphenytoin, or valproic acid.
    • Phenobarbital, levetiracetam, lacosamide, and IV midazolam or propofol/ketamine infusion are also possible treatments, depending on the patient's specific response.
    • Safety protocols during seizures include positioning to prevent aspiration, and ensuring the person's safety.

    Anticonvulsants and Pregnancy

    • When considering anticonvulsant use during pregnancy, close monitoring of efficacy and potential adverse effects is necessary.
    • Single-agent therapy, minimizing dosage, and avoiding specific drugs like valproic acid, phenytoin, and phenobarbital, are essential strategies.

    Oral Hypoglycemics

    • Metformin, SGLT-2 inhibitors and DPP-4 inhibitors have varied mechanisms of action, associated side effects, and clinical uses.

    Sulfonylureas

    • These medications stimulate insulin release through beta-cells, reducing blood glucose levels.
    • Adverse effects include weight gain and hypoglycemia, and caution is needed in patients with renal impairment.

    Meglinitides

    • Meglinitides simulate insulin release through direct interaction with beta cells, often used for rapid-acting postprandial hyperglycemia control.
    • Hypoglycemia and potential weight gain are frequently observed, and appropriate dosing or consideration for meal skipping is crucial.

    Alpha-Glucosidase Inhibitors

    • These drugs inhibit the absorption of carbohydrates from the gut, lowering postprandial blood glucose levels, although there is no hypoglycemia risk.
    • Main adverse effects include GI distress.

    Thiazolidinediones (TZDs)

    • These drugs increase peripheral insulin sensitivity, offering a significant impact on reducing HbA1C.
    • Common adverse effects include edema, anemia, heart failure, and weight gain, sometimes increasing bone fracture risk.

    Summary: Pharmacotherapy Considerations

    • Factors like sedation, appetite, pain type, comorbid conditions, pharmacokinetics, and drug-drug/food interactions are important when evaluating treatment strategies.

    Diabetes Mellitus

    • The presentation covers the definitions, prevalence, impact, treatment goals, and recommendations related to diabetes treatment, emphasizing the importance of considering specific patient factors..

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    Description

    This quiz explores the pharmacology of central nervous system (CNS) medications, focusing on their mechanisms of action, adverse effects, and key counseling points for patients. Additionally, it reviews important neurotransmitters like GABA and glutamate, their roles within the CNS, and their relevance in psychotropic regimens.

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