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Chapter 6 Psychotropic Medications

6.1. INTRODUCTION

Learning Objectives

  • Relate the anatomy and physiology of the central nervous system to mental health disorders and psychotropic medications
  • Describe patient education for classes of psychotropic medications

Psychotropic medications are medications that affect the mind, emotions, and behavior. This chapter will review the anatomy and physiology of the central nervous system (CNS) as it relates to mental health disorders and medications and then discuss several classes of psychotropic medications.

References

1.
2.
MedlinePlus. About us. https://medlineplus​.gov/
3.
National Alliance on Mental Illness. (n.d.). Mental health medications. https://nami​.org/About-Mental-Illness​/Treatments​/Mental-Health-Medications.

6.2. REVIEW OF THE CENTRAL NERVOUS SYSTEM

To understand how psychotropic medications work, it is important to understand the anatomy and physiology of the central nervous system. The nervous system is divided into the central and peripheral nervous systems. The central nervous system (CNS) is the brain and spinal cord, and the peripheral nervous system includes everything else in the nervous system. See Figure 6.1 [1] for an illustration of the central and peripheral nervous systems.

Figure 6.1

Figure 6.1

The Central and Peripheral Nervous Systems

The peripheral nervous system consists of sensory neurons and motor neurons. Sensory neurons sense the environment and conduct signals to the brain that become a person’s conscious perception of that stimulus. This conscious perception may lead to a motor response that is conducted from the brain to the peripheral nervous system via motor neurons. Motor neurons are part of the somatic nervous system that stimulates voluntary movement of muscles and the autonomic nervous system that controls involuntary responses.

Sympathetic and Parasympathetic Nervous System

The autonomic nervous system is divided into the sympathetic nervous system (SNS) and the parasympathetic nervous system (PNS). Homeostatic mechanisms are regulated by the body through a balance of SNS and PNS stimulation. For example, stimulation of SNS receptors increases the heart rate, increases blood pressure via the constriction of blood vessels, and causes bronchodilation, whereas stimulation of the PNS slows the heart, lowers blood pressure due to vasodilation, and causes bronchoconstriction. Due to these effects, the SNS is associated with the “fight-or-flight” response, and the PNS is often referred to as the “rest and digest” system. See Figure 6.2 [2] to compare the effects of PNS and SNS stimulation on target organs.

Figure 6.2

Figure 6.2

Effects of SNS and PNS Stimulation

SNS Receptors

SNS receptors include Alpha-1, Alpha-2, Beta-1, and Beta-2 receptors that are stimulated by epinephrine and norepinephrine. Medications that stimulate these receptors are referred to as adrenergic agonists because they mimic the effects of the body’s natural SNS stimulation. For example, stimulants like methylphenidate are adrenergic agonists used to treat attention deficit hyperactivity disorder (ADHD). Conversely, adrenergic antagonists block SNS receptors. For example, propranolol is a Beta-2 antagonist used to treat the physical symptoms of severe anxiety (e.g., trembling, rapid heartbeat, and sweating).

PNS Receptors

PNS receptors include nicotinic and muscarinic receptors that are stimulated by acetylcholine (ACh). Drugs that stimulate nicotinic and muscarinic receptors are called cholinergics. For example, nicotine in tobacco products stimulates nicotinic receptors. Stimulation of muscarinic receptors primarily causes smooth muscle contraction. An example of a muscarinic agonist is bethanechol used to treat urinary retention by increasing the tone of the detrusor muscle to increase bladder emptying. [3] Drugs that block the effects of PNS receptors are called anticholinergics. For example, benztropine is an anticholinergic used to treat muscle spasms associated with extrapyramidal symptoms from antipsychotic medications. [4] Many psychotropic medications cause anticholinergic adverse effects that can be especially hazardous for older adults. SLUDGE is a mnemonic for anticholinergic side effects: Salivation decreased, Lacrimation decreased, Urinary retention, Drowsiness/dizziness, GI upset, and Eyes (blurred vision/dry eyes). See Figure 6.3 [5] for an illustration of the “SLUDGE” effects caused by anticholinergics.

Figure 6.3

Figure 6.3

SLUDGE Effects of Anticholinergics

Opioid System

The opioid system in the brain controls pain, reward, and addictive behaviors. There are three types of opioid receptors called mu, delta, and kappa receptors. Opioid receptors are stimulated by endogenous peptides released by neurons (such as endorphins) and exogenous opiates. Opiates include powerful analgesics (such as morphine and oxycodone) prescribed to treat moderate to severe pain. Opiates also include illicit drugs (such as heroin). Chronic use of prescribed and illicit opiates can be highly addictive because of their actions on the reward system of the brain. [6] Read more about the addictive cycle in the “Substance Use Disorders” chapter.

Neurotransmitters

Neurotransmitters are chemical substances released at the end of a neuron by the arrival of an electrical impulse. They diffuse across the synapse and cause the transfer of the impulse to another nerve fiber, a muscle fiber, or other structure. Neurotransmitters interact with specific receptors like a key and a lock. See Figure 6.4 [7] for an illustration of neuron communication with neurotransmitters and receptors.

Figure 6.4

Figure 6.4

Neuron Communication With Neurotransmitters

There are several types of neurotransmitters associated with mental health disorders and psychoactive medications, including acetylcholine, glutamate, GABA, glycine, dopamine, serotonin, norepinephrine, and histamine [8],[9]:

  • Acetylcholine: Acetylcholine stimulates nicotinic and muscarinic receptors in the parasympathetic nervous system. Other substances also bind to these receptors. For instance, nicotine (in tobacco products) binds to nicotinic receptors, and muscarine (products of specific mushrooms used as a hallucinogenic) binds to muscarinic receptors.
  • Glutamate: Glutamate is an excitatory neurotransmitter. Elevated levels of glutamate are associated with psychosis symptoms that can occur with schizophrenia, as well as with illicit drug use such as methamphetamines. Conversely, lamotrigine, a medication used to treat bipolar disorder, inhibits glutamate.
  • Gamma-Aminobutyric Acid and Glycine: Gamma-aminobutyric acid (GABA) and glycine are inhibitory neurotransmitters that act like brakes in a car by slowing down overexcited nerve cells. Low levels of GABA are associated with seizures, anxiety, mania, and impulse control. Pregabalin is an anticonvulsant that mimics the effects of GABA and is used to treat generalized anxiety disorder.
  • Dopamine: Dopamine plays an essential role in several brain functions, including learning, motor control, reward, emotion, and executive functions. It is associated with several mental health disorders and is targeted by many psychotropic medications. For example, bupropion is an antidepressant that inhibits dopamine reuptake, leading to increased dopamine levels in the synapse and relieving the symptoms of depression. Conversely, chlorpromazine blocks dopamine receptors and is used to treat psychosis, but this blockade can cause extrapyramidal side effects (involuntary and uncontrolled muscle movements).
  • Serotonin: Serotonin modulates multiple neuropsychological processes such as mood, sleep, libido, and temperature regulation. Abnormal levels of serotonin have been linked to many mental health disorders such as depression, bipolar disorder, and anxiety. Many psychotropic medications target serotonin. For example, fluoxetine belongs to a class of antidepressants called selective serotonin reuptake inhibitors (SSRIs). SSRIs prevent the reuptake of serotonin at the synapse, making more of the chemical available in the brain and relieving depression.
  • Norepinephrine and Epinephrine: Norepinephrine and epinephrine stimulate alpha- and beta-receptors in the sympathetic nervous system. Their release exerts effects on a variety of body processes, including stress, sleep, attention, and focus. Many psychotropic medications target these neurotransmitters. For example, venlafaxine belongs to a class of antidepressants called norepinephrine reuptake inhibitors (NRIs). NRIs are prescribed to treat depression by preventing the reuptake of norepinephrine at the synapse and boosting levels of norepinephrine in the brain.
  • Histamine: Histamine mediates homeostatic functions in the body, promotes wakefulness, modulates feeding behavior, and controls motivational behavior. For example, diphenhydramine, a histamine antagonist, causes drowsiness and is also used to treat extrapyramidal symptoms.

View a YouTube [10] video called the Receptor Debate that compares the effects of neurotransmitters.

References

1.
2.
Updated SNS-PNS image.png” by Meredith Pomietlo for Open RN is licensed under CC BY 4.0.
3.
This work is a derivative of StatPearls by Padda and Derian and is licensed under CC BY 4.0.
4.
This work is a derivative of StatPearls by Ahuja and Abdijadid and is licensed under CC BY 4.0.
5.
“SLUDGE effects of Anticholinergics” by Dominic Slausen at Chippewa Valley Technical College is licensed under CC BY 4.0.
6.
This work is a derivative of StatPearls by Dhaliwal and Gupta and is licensed under CC BY 4.0.
7.
8.
This work is a derivative of Anatomy and Physiology by OpenStax and is licensed under CC BY 4.0. Access for free at https://openstax​.org​/books/anatomy-and-physiology​/pages/1-introduction.
9.
This work is a derivative of StatPearls by Sheffler, Reddy, and Pillarisetty and is licensed under CC BY 4.0.
10.
NEI Psychopharm. (2016, November 3). Receptor Debate. [Video]. YouTube. All rights reserved. https://youtu​.be/GqX_J5h4aBw.

6.3. ANTIDEPRESSANTS

Antidepressants are commonly used to treat depression but are also used to treat other conditions, such as anxiety, chronic pain, and insomnia. According to a research review by the Agency for Healthcare Research and Quality, antidepressant medications work relatively equally as well to improve symptoms of depression and to keep depression symptoms from coming back. [1] For reasons not yet well understood, some people respond better to certain antidepressant medications than to others, so an individual may have to try different types of antidepressants before finding one that effectively treats their symptoms. [2] Additionally, it may take antidepressants two or more weeks to achieve peak effect.

There are several classes and types of antidepressants, including selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), norepinephrine and dopamine reuptake inhibitors (NDRIs) , serotonin antagonist and reuptake inhibitors, tricyclic antidepressants (TCAs), and monoamine oxidase inhibitors (MAOIs). TCAs and MAOIs are often referred to as first-generation antidepressants because they were first marketed in the 1950s. They have many side effects and are not prescribed as frequently to treat depression as are SSRIs, SNRIs, and bupropion that have fewer side effects.

Selective Serotonin Reuptake Inhibitors

Selective serotonin reuptake inhibitors (SSRIs) prevent the uptake of serotonin at the synapse, causing the serotonin neurotransmitter to stay in the synapse longer and overall raise the level of serotonin in the brain. SSRIs are primarily used to treat depression but are also used to treat bipolar disorder, obsessive-compulsive disorder, bulimia, panic disorder, post-traumatic stress disorder, anxiety, premenstrual syndrome, and migraines. Examples of common SSRIs include fluoxetine, citalopram, sertraline, paroxetine, and escitalopram. [3]

Serotonin Norepinephrine Reuptake Inhibitor (SNRI)

Serotonin norepinephrine reuptake inhibitors (SNRI) prevent the reuptake of serotonin and norepinephrine, with weak inhibition of dopamine reuptake. Examples of SNRIs are venlafaxine and duloxetine. [4]

Norepinephrine and Dopamine Reuptake Inhibitor (NDRI)

Bupropion is an example of a norepinephrine and dopamine reuptake inhibitor. It is used to treat depressive disorders, seasonal affective disorder, attention deficit disorder and to help people stop smoking. [5]

Serotonin Antagonist and Reuptake Inhibitor

Trazodone is an example of a serotonin antagonist and reuptake inhibitor. It is an antidepressant but most commonly prescribed off-label for anxiety or as a hypnotic. Trazodone reduces levels of the neurotransmitters associated with arousal effects, such as serotonin, noradrenaline, dopamine, acetylcholine, and histamine. Low-dose trazodone use exerts a sedative effect for sleep, so is typically administered in the evening. [6]

Tricyclic Antidepressants

Tricyclic antidepressants (TCAs) are older first-generation antidepressants that block the reuptake of serotonin and norepinephrine in the synapse, which leads to increased concentration of these neurotransmitters in the brain. They are now more commonly used to treat neuropathic pain and insomnia. An example of a TCA is amitriptyline. [7]

TCAs are often administered at bedtime due to sedating effects. Older adults are particularly sensitive to the anticholinergic side effects of tricyclic antidepressants (e.g., tachycardia, urinary retention, constipation, dry mouth, blurred vision, confusion, psychomotor slowing, sedation, and delirium). Elderly clients should be started on low doses of amitriptyline and observed closely because they are at increased risk for falls. Blockage of adrenergic receptors can cause cardiac conduction disturbances and hypotension. [8]

Death may occur from overdosage with this class of drugs. Multiple drug ingestion (including alcohol) is common in deliberate tricyclic antidepressant overdose. If overdose occurs, call 911 in an outpatient setting or rapid response in an inpatient setting. Responders can consult with a Certified Poison Control Center (1-800-222-1222) or go to https://www.poisonhelp.org/help for the latest treatment recommendations. [9]

Monoamine Oxidase Inhibitors (MAOI)

Monoamine oxidase inhibitors (MAOIs) are an older first-generation antidepressant. MAOIs are contraindicated with all other classes of antidepressants. Monoamine oxidase is an enzyme that removes the neurotransmitters norepinephrine, serotonin, and dopamine from the brain. By inhibiting this enzyme, MAOIs cause the levels of these transmitters to increase. Tranylcypromine is an example of an MAOI. [10]

A significant disadvantage to MAOIs is their potential to cause a hypertensive crisis when taken with stimulant medications or foods or beverages containing tyramine. Examples of foods containing tyramine are aged cheese, cured or smoked meats, alcoholic beverages, and soy sauce. Older adults are at increased risk for postural hypotension and serious adverse effects. [11]

Read additional information about mechanism of action, potential adverse effects, and related patient education regarding antidepressants in the “Treatments for Depression” section of the “Depressive Disorders” chapter.

References

1.
Volpi-Abadie J., Kaye A. M., Kaye A. D. Serotonin syndrome. The Ochsner Journal. 2013;13(4):533–540. [PMC free article: PMC3865832] [PubMed: 24358002] [CrossRef]
2.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services.https://www.nimh.nih.gov/health/topics/mental-health-medications.
3.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services. https:​//www​.nimh.nih.gov/health​/topics/mental-health-medications.
4.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services. https:​//www​.nimh.nih.gov/health​/topics/mental-health-medications.
5.
MedlinePlus [Internet]. Bethesda (MD): National Library of Medicine (US); [updated 2022, Mar 16]. Bupropion; [reviewed 2018, Feb 15; cited 2022, Mar 25]. https://medlineplus​.gov​/druginfo/meds/a695033.html.
6.
This work is a derivative of StatPearls by Shin and Saadabadi and is licensed under CC BY 4.0.
7.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.
8.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.
9.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.
10.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.
11.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.

6.4. MOOD STABILIZERS

Mood stabilizers are used primarily to treat bipolar disorder. They are also used to treat depression (usually in combination with an antidepressant), schizoaffective disorder, and disorders of impulse control. Lithium is an example of a mood stabilizer. Anticonvulsant medications are also used as mood stabilizers. [1] Antipsychotics, antianxiety, and antidepressants may also be used to treat bipolar disorders.

Lithium

Lithium reduces excitatory neurotransmission (dopamine and glutamate) and increases inhibitory neurotransmission (GABA). It also alters sodium transport in nerve and muscle cells and causes a shift in metabolism of catecholamines. When administered to a client experiencing a manic episode, lithium may reduce symptoms within 1 to 3 weeks. It also possesses unique antisuicidal properties that sets it apart from antidepressants. However, lithium toxicity can occur at doses close to therapeutic levels so lithium levels must be monitored regularly. [2],[3]

Read additional information about mechanism of action and adverse effects of medications used to treat bipolar disorder in the “Treatments for Bipolar Disorder” in the “Bipolar Disorders” chapter.

References

1.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services. https:​//www​.nimh.nih.gov/health​/topics/mental-health-medications.
2.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.
3.
Malhi G. S., Tanious M., Das P., Coulston C. M., Berk M. Potential mechanisms of action of lithium in bipolar disorder. Current understanding. CNS Drugs. 2013;27(2):135–153. [PubMed: 23371914] [CrossRef]

6.5. ANTIANXIETY MEDICATIONS

Antianxiety medications help reduce the symptoms of anxiety, panic attacks, or extreme fear and worry. The most common class of antianxiety medications is benzodiazepines. Benzodiazepines are used to treat generalized anxiety disorder, although SSRIs or other antidepressants are typically used to treat panic disorder or social phobia (i.e., social anxiety disorder). Beta-blockers and buspirone may also be prescribed for anxiety. [1]

Benzodiazepines

Benzodiazepines are used to treat anxiety and are also used for their sedation and anticonvulsant effects because they bind to GABA receptors and stimulate the effects of GABA (an inhibitory neurotransmitter). Benzodiazepines include clonazepam, alprazolam, and lorazepam. Benzodiazepines are a Schedule IV controlled substance because they have a potential for misuse and can cause dependence. Short-acting benzodiazepines (such as lorazepam) and beta-blockers are used to treat the short-term symptoms of anxiety. Lorazepam is available for oral, intramuscular, or intravenous routes of administration. [2]

Beta-Blockers

Beta-blockers (such as propranolol) block sympathetic nervous system stimulation of Beta-1 receptors. They may be prescribed to manage the physical symptoms of anxiety (such as trembling, rapid heartbeat, and sweating) for a short period of time or used “as needed” to reduce acute physical symptoms. [3]

Read additional information about medications used to treat anxiety in the “Treatments for Anxiety” section of the “Anxiety Disorders” chapter.

References

1.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services. https:​//www​.nimh.nih.gov/health​/topics/mental-health-medications.
2.
This work is a derivative of DailyMed by U.S. National Library of Medicine and is available in the Public Domain.
3.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services. https:​//www​.nimh.nih.gov/health​/topics/mental-health-medications.

6.6. ANTIPSYCHOTICS

Antipsychotic medicines are primarily used to manage psychosis (i.e., a loss of contact with reality that may include delusions or hallucinations). Psychosis can be a symptom of a physical condition (such as a high fever, head injury, or substance intoxication) or a mental disorder (such as schizophrenia, bipolar disorder, or severe depression). Antipsychotic medications may also be used in combination with other medications to treat the symptoms of other mental health conditions, including attention deficit hyperactivity disorder (ADHD), eating disorders, post-traumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), and generalized anxiety disorder. [1]

First-generation antipsychotics (also called typical antipsychotics) have several potential adverse effects, and medication is prescribed based on the client’s ability to tolerate the adverse effects. Second-generation antipsychotics (also referred to as atypical antipsychotics) have fewer adverse effects and are generally better tolerated. Clients respond differently to antipsychotic medications, so it may take several trials of different medications to find the one that works best for their symptoms. [2]

First-Generation (Typical) Antipsychotics

Common first-generation antipsychotic medications (also called “typical” antipsychotics) include chlorpromazine, haloperidol, perphenazine, and fluphenazine. [3]

First-generation antipsychotics work by blocking dopamine receptors in certain areas of the CNS, such as the limbic system and the basal ganglia. These areas are associated with emotions, cognitive function, and motor function. As a result, blockage produces a tranquilizing effect in psychotic clients. However, several adverse effects are caused by this dopamine blockade, such extrapyramidal side effects (e.g., involuntary or uncontrollable movements, tremors, and muscle contractions) and tardive dyskinesia (a syndrome of movement disorders that persists for at least one month and can last up to several years despite discontinuation of the medications).

Second-Generation (Atypical) Antipsychotics

Second-generation antipsychotics (also called atypical antipsychotics) work by blocking specific D2 dopamine receptors and serotonin receptors. Second-generation medications include risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, paliperidone, and lurasidone. Several atypical antipsychotics have a “broader spectrum” of action than the older medications and are used for treating bipolar depression or depression that has not responded to an antidepressant medication alone. They have a significantly decreased risk of extrapyramidal side effects but are associated with weight gain and the development of metabolic syndrome. [4Metabolic syndrome increases the risk of heart disease, stroke, and type 2 diabetes. Clinical symptoms of metabolic syndrome include high blood glucose, symptoms of diabetes (i.e., increased thirst and urination, fatigue, and blurred vision), obesity with a large abdominal girth, hypertension, elevated triglyceride, and lower levels of HDL.

Clozapine

Clients with treatment-resistant schizophrenia may be prescribed clozapine, a specific atypical antipsychotic medication that binds to serotonin, as well as dopamine receptors. Clozapine also has strong anticholinergic, sedative, cardiac, and hypotensive properties and frequent drug-drug interactions. [5]

View a supplementary YouTube video [6] explaining how clozapine binds to additional neuroreceptors compared to other antipsychotic medications: The Pines, the Dones, Two Pips and a Rip

Read additional information about the mechanism of action, adverse side effects, and patient education regarding antipsychotic medications in the “Schizophrenia” section of the “Psychosis and Schizophrenia” chapter.

References

1.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health & Human Services. https:​//www​.nimh.nih.gov/health​/topics/mental-health-medications.
2.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health and Human Services. https://www​.nimh.nih​.gov/health/topics/mental-health-medications#part_2362.
3.
National Institute of Mental Health. (2016, October). Mental health medications. U.S. Department of Health and Human Services. https://www​.nimh.nih​.gov/health/topics/mental-health-medications#part_2362.
4.
This work is a derivative of StatPearls by Chokhawala and Stevens and is licensed under CC BY 4.0.
5.
Jibson, M. D. (2021). Second-generation antipsychotic medications: Pharmacology, administration, and side effects. UpToDate. Retrieved January 14, 2022, from https://www​.uptodate.com/
6.
NEI Psychopharm. (2014, March 18). The pines, the dones, two pips, and a rip [Video]. YouTube. All rights reserved. https://youtu​.be/kuYGJOcloH8.

6.7. STIMULANTS

Stimulant medications are prescribed to treat children, adolescents, or adults diagnosed with attention deficit hyperactivity disorder (ADHD). Stimulants block the reuptake of norepinephrine and dopamine in the synapse and increase the overall level of these substances in the brain, but they have a paradoxical calming effect and improve the ability to focus and concentrate for individuals diagnosed with ADHD. Common stimulants used to treat ADHD include methylphenidate, amphetamine, dextroamphetamine, and lisdexamfetamine dimesylate. Stimulant medications are safe when prescribed with close supervision, but they are a Schedule II controlled substance because they have a high potential for misuse and dependence.

Read more information about medications used to treat attention deficit hyperactivity disorder (ADHD), adverse side effects, and patient education in the “Common Disorders and Disabilities in Children and Adolescents” section of the “Childhood and Adolescent Disorders” chapter.

6.8. PSYCHOACTIVE SUBSTANCES AND MEDICATIONS TO TREAT SUBSTANCE USE AND WITHDRAWAL

Information about the effects of substances such alcohol, cannabis, and illicit drugs is discussed in the “Substances: Use, Intoxication, and Overdose” section of the “Substance Use Disorders” chapter.

Medications to treat alcohol use disorder and opioid disorder include buprenorphine-naloxone, methadone, naltrexone, acamprosate, and disulfiram. These medications are discussed in the “Treatment and Recovery Services” subsection of the “Substance Use Disorders” chapter.

Medications used to manage symptoms of substance withdrawal/detoxification include buprenorphine, methadone, and Alpha-2 adrenergic agonists (such as clonidine and lofexidine). Read more about these medications in the “Withdrawal Management/Detoxification” section of the “Substance Use Disorders” chapter.

6.9. LEARNING ACTIVITIES

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VI. GLOSSARY

Acetylcholine

A neurotransmitter that stimulates nicotinic and muscarinic receptors in the parasympathetic nervous system.

Adrenergic agonists

Substances that stimulate SNS receptors and cause effects similar to epinephrine and norepinephrine.

Adrenergic antagonists

Substances that block SNS receptors.

Agranulocytosis

Extremely low white blood cell count and an adverse effect of clozapine and antipsychotic medication.

Anticholinergics

Substances that block the effects of PNS receptors.

Black Box Warning

A significant warning from the Food and Drug Administration (FDA) that alerts the public and health care providers to serious side effects, such as injury or death.

Catecholamines

Substances that include epinephrine, norepinephrine, and dopamine and are responsible for the body’s “fight-or-flight” response.

Central nervous system (CNS)

The brain and spinal cord.

Cholinergics

Substances that stimulate nicotinic and muscarinic receptors and cause effects similar to acetylcholine (ACh).

Controlled substance

Drugs regulated by federal law that can cause dependence and abuse.

Dopamine

A neurotransmitter that plays an essential role in several brain functions, including learning, motor control, reward, emotion, and executive functions.

Extrapyramidal side effects

Involuntary or uncontrollable movements, tremors, and muscle contractions that can occur with antipsychotic medications.

Gamma-aminobutyric acid and Glycine

Inhibitory neurotransmitters that act like brakes in a car by slowing down overexcited nerve cells. Low levels of GABA are associated with seizures, anxiety, mania, and impulse control. Pregabalin is an anticonvulsant that mimics the effects of GABA and is used to treat generalized anxiety disorder.

Glutamate

An excitatory neurotransmitter. Elevated levels of glutamate are associated with psychosis that can occur with schizophrenia, as well as with illicit drug use such as methamphetamines. Conversely, lamotrigine, a medication used to treat bipolar disorder, inhibits glutamate.

Histamine

A substance that mediates homeostatic functions in the body, promotes wakefulness, modulates feeding behavior, and controls motivational behavior. For example, diphenhydramine, a histamine antagonist, causes drowsiness.

Hypertensive crisis

A condition that can be caused by MAOIs with severe hypertension (blood pressure greater than 180/120 mm Hg) and evidence of organ dysfunction. Symptoms may include occipital headache (which may radiate frontally), palpitations, neck stiffness or soreness, nausea or vomiting, sweating, dilated pupils, photophobia, shortness of breath, or confusion.

Lithium toxicity

Lithium has a narrow therapeutic range of 0.8 to 1.2 mEq/L. Levels above this range cause lithium toxicity. Signs of early lithium toxicity include diarrhea, vomiting, drowsiness, muscular weakness, and lack of coordination. At higher levels, giddiness, ataxia, blurred vision, tinnitus, and a large output of dilute urine may occur.

Neuroleptic malignant syndrome (NMS)

A rare but fatal adverse effect that can occur at any time during treatment with antipsychotics. It typically develops over a period of days to weeks and resolves in approximately nine days with treatment. Signs include increased temperature, severe muscular rigidity, confusion, agitation, hyperreflexia, elevation in white blood cell count, elevated creatinine phosphokinase, elevated liver enzymes, myoglobinuria, and acute renal failure.

Neurotransmitters

Chemical substances released at the end of a neuron by the arrival of an electrical impulse. They diffuse across the synapse and cause the transfer of the impulse to another nerve fiber, a muscle fiber, or other structure. Neurotransmitters interact with specific receptors like a key and a lock.

Norepinephrine and Epinephrine

Substances that stimulate alpha- and beta-receptors in the sympathetic nervous system.

Opiates

Powerful analgesics prescribed to treat moderate to severe pain (such as morphine and oxycodone). Opiates also include illicit drugs (such as heroin).

Opioid receptors

Mu, delta, and kappa receptors that are stimulated by endogenous peptides released by neurons (such as endorphins) and exogenous opiates.

Opioid system

A system in the brain that controls pain and reward and addictive behaviors.

Parasympathetic Nervous System (PNS) receptors

Nicotinic and muscarinic receptors that are stimulated by acetylcholine (ACh).

Serotonin

A neurotransmitter that modulates multiple neuropsychological processes such as mood, sleep, libido, and temperature regulation. Abnormal levels of serotonin have been linked to many mental health disorders such as depression, bipolar disorder, and anxiety. Many psychotropic medications target serotonin.

Serotonin syndrome

A syndrome caused by the combination of multiple medications that affect serotonin. It typically develops within 24 hours from the combination of medication and can range from mild to a life-threatening syndrome. Signs of serotonin syndrome include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), incoordination, or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea). Serotonin syndrome, in its most severe form, can resemble neuroleptic malignant syndrome (NMS).

SLUDGE

A mnemonic for anticholinergic side effects: Salivation decreased, Lacrimation decreased, Urinary retention, Drowsiness/dizziness, GI upset, Eyes (blurred vision/dry eyes).

Sympathetic Nervous System (SNS) receptors

Alpha-1, Alpha-2, Beta-1, and Beta-2 receptors that are stimulated by epinephrine and norepinephrine.

Tardive dyskinesia

A syndrome of movement disorders associated with antipsychotic medications that persists for at least one month and can last up to several years despite discontinuation of the medications.

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Licensed under a Creative Commons Attribution 4.0 International License. To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/.

Bookshelf ID: NBK590034

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