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Questions and Answers
Which age group has an increased risk of suicidal thinking and behavior when using antidepressants?
Which age group has an increased risk of suicidal thinking and behavior when using antidepressants?
Adults over the age of 24 have an increased risk of suicidal thoughts when taking antidepressants.
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)?
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 ______.
SSRIs help to increase the level of serotonin in the ______.
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Match the following SSRIs with their respective adverse effects:
Match the following SSRIs with their respective adverse effects:
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What is the primary mechanism of action of Valbenazine?
What is the primary mechanism of action of Valbenazine?
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Valbenazine can cause coma, seizures, or even death at toxic doses.
Valbenazine can cause coma, seizures, or even death at toxic doses.
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List one medication class known to affect lithium concentration.
List one medication class known to affect lithium concentration.
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Valbenazine is indicated for the treatment of __________.
Valbenazine is indicated for the treatment of __________.
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Match the following medications with their potential effects or interactions:
Match the following medications with their potential effects or interactions:
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Which medication is specifically used for absence seizures?
Which medication is specifically used for absence seizures?
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Valproic acid is contraindicated in the treatment of absence seizures.
Valproic acid is contraindicated in the treatment of absence seizures.
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What is the therapeutic level range for Ethosuximide?
What is the therapeutic level range for Ethosuximide?
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The _____ are often treatment resistant and may require special attention.
The _____ are often treatment resistant and may require special attention.
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Match the following medications with their specific use:
Match the following medications with their specific use:
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Which drug should be avoided in the treatment of myoclonic seizures?
Which drug should be avoided in the treatment of myoclonic seizures?
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Ethosuximide has significant drug interactions with other medications.
Ethosuximide has significant drug interactions with other medications.
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What are some common adverse effects of Ethosuximide?
What are some common adverse effects of Ethosuximide?
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What is a common side effect associated with cholinergic agonists at M4 receptors in the mouth?
What is a common side effect associated with cholinergic agonists at M4 receptors in the mouth?
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Clozapine should be prescribed to patients with adherence issues.
Clozapine should be prescribed to patients with adherence issues.
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What are the initial dosing considerations for clozapine after the patient has missed a dose for more than 48 hours?
What are the initial dosing considerations for clozapine after the patient has missed a dose for more than 48 hours?
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In the treatment of EPS, __________ is used at a dose of 25-50 mg po or IM.
In the treatment of EPS, __________ is used at a dose of 25-50 mg po or IM.
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Which of the following antipsychotics carries a high risk of EPS?
Which of the following antipsychotics carries a high risk of EPS?
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Tardive dyskinesia is a permanent condition that may occur with long-term antipsychotic usage.
Tardive dyskinesia is a permanent condition that may occur with long-term antipsychotic usage.
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Match the following treatments with their appropriate effects for EPS:
Match the following treatments with their appropriate effects for EPS:
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What are some symptoms of tardive dyskinesia?
What are some symptoms of tardive dyskinesia?
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What is the common adverse effect of Lamotrigine (Lamictal)?
What is the common adverse effect of Lamotrigine (Lamictal)?
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Valproic Acid (Depakote) is considered a liver enzyme inhibitor.
Valproic Acid (Depakote) is considered a liver enzyme inhibitor.
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What is the therapeutic level range for Valproic Acid in mcg/ml?
What is the therapeutic level range for Valproic Acid in mcg/ml?
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Lamotrigine should be titrated _____ to reduce the risk of rash.
Lamotrigine should be titrated _____ to reduce the risk of rash.
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Match the following adverse effects with their classification (common or rare):
Match the following adverse effects with their classification (common or rare):
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What is the loading dose range for Valproic Acid?
What is the loading dose range for Valproic Acid?
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Somnolence is a rare adverse effect of Lamotrigine.
Somnolence is a rare adverse effect of Lamotrigine.
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What mechanism of action describes how Valproic Acid works on sodium channels?
What mechanism of action describes how Valproic Acid works on sodium channels?
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Which receptor blockade in the nigrostriatal pathway can lead to movement disorders?
Which receptor blockade in the nigrostriatal pathway can lead to movement disorders?
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Antipsychotics can be used effectively in patients with dementia-related psychosis.
Antipsychotics can be used effectively in patients with dementia-related psychosis.
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Name a common anticholinergic medication that may be required as adjunct therapy for high-potency FGAs.
Name a common anticholinergic medication that may be required as adjunct therapy for high-potency FGAs.
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The first generation antipsychotic chlorpromazine is classified as a ______ potency agent.
The first generation antipsychotic chlorpromazine is classified as a ______ potency agent.
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Match the following first generation antipsychotics with their potency:
Match the following first generation antipsychotics with their potency:
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What is a major adverse effect associated with second generation antipsychotics compared to first generation?
What is a major adverse effect associated with second generation antipsychotics compared to first generation?
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All antipsychotics have the same level of cardiovascular risk.
All antipsychotics have the same level of cardiovascular risk.
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What effect does smoking have on the CYP450 1A2 pathway?
What effect does smoking have on the CYP450 1A2 pathway?
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Patients treated with _______ need to be monitored for extrapyramidal symptoms (EPS).
Patients treated with _______ need to be monitored for extrapyramidal symptoms (EPS).
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Which of the following is a side effect associated with long-term use of FGAs?
Which of the following is a side effect associated with long-term use of FGAs?
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Prolactin elevation can occur with the blockade of D2 receptors in the tuberoinfundibular pathway.
Prolactin elevation can occur with the blockade of D2 receptors in the tuberoinfundibular pathway.
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Which drug is primarily used for treating acute agitation in hospitalized patients?
Which drug is primarily used for treating acute agitation in hospitalized patients?
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Match the following SGA with their trade name:
Match the following SGA with their trade name:
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The medication _________ is associated with metabolic abnormalities including weight gain and hyperlipidemia.
The medication _________ is associated with metabolic abnormalities including weight gain and hyperlipidemia.
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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.