Exam 3 Review Pharm Spring 2025 PDF

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Joyce University

2025

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opioids pharmacology NSAIDs analgesics

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This document is a review for a pharmacology exam, covering topics such as opioids, NSAIDs, and different types of analgesics. The review includes questions on treatment options for opioid overdose and migraines, as well as discussions of adverse effects and drug mechanisms.

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Exam 3 Review What are the adverse effects of opioid agonists? Opioids q Therapeutic Effects: q Adverse Effects: M yosis (pinpoint pupils) -Analgesia (pain relief) O ut of it (sedation) -Coug...

Exam 3 Review What are the adverse effects of opioid agonists? Opioids q Therapeutic Effects: q Adverse Effects: M yosis (pinpoint pupils) -Analgesia (pain relief) O ut of it (sedation) -Cough suppression R espiratory depression -Sedation P ruritis (itching) -Slowed GI motility H ypotension -Euphoria I nfrequency (constipation, urinary retention) -Relaxation N ausea E mesis (vomiting) // Euphoria © Joyce University What are the treatment options for acute opioid overdose? Naloxone Nal x ne Therapeutic Class Narcotic antagonist Mechanism of Action Competitive antagonism of CNS opioid receptors Indication Opioid induced respiratory depression, opioid reversal agent Contraindication Tachycardia, tachypnea, cramping, hypertension, vomiting, analgesia reversal Adverse Effects Tachycardia, seizure, hypertension, cardiac arrest, diaphoresis, vomiting Specials May need to re-administer, monitor respiration © Joyce University What are the adverse effects of non-steroidal anti-inflammatory drugs (NSAIDs)? Ibuprofen (NSAID prototype) Therapeutic Class NSAID Mechanism of Action Reduces prostaglandin signaling by inhibiting COX 1 and COX 2 enzymes Indication Inflammatory suppression, mild to moderate pain, fever, arthritis Contraindication Hypertension, peptic ulcer disease, bleeding disorders, aspirin use, ACEIs/ARBs use, asthmatics Adverse Effects GI discomfort, impaired kidney function, hypertension, heart attack, peptic ulcer disease (GI bleed) © Joyce University How does the pharmacological treatment differ for an acute migraine compared to the prophylaxis of migraines? Migraine Treatment ACUTE TREATMENT Aspirin- NSAID, Acetaminophen, Caffeine -Sumatriptan Triptan medications (Serotonin receptor agonists) - Ergotamine Ergot medications (less common) PROPHYLACTIC Beta-blockers – Propranolol- TREATMENT Preventitall Tricyclic antidepressants – © Joyce University Amitriptyline- Define opioid agonist, opioid partial agonist, and opioid antagonist. Give examples of drugs in each pharmacological category. Opioids Agonist Partial Agonist Antagonist https://www.cannify.us/education/cannabis-and-the-body/cannabinoid-clinical-pharmacology/pharmacodynamics/ligand-binding-to-receptors/ © Joyce University Opioids Substances that interact with the opioid receptor and produce morphine-like effects q Opioid Agonist: Substances that will bind to the receptor and produce a response q Opioid Partial Agonist: Substances that will bind to a receptor and can produce a response q Opioid Antagonist: Substances that will bind to the receptor and NOT produce a response (and also prevent agonists from binding) Agonist A go nist Antagonist tag oo nist A nno 12 Opioid agonists Activate opioid receptors fully, resulting in the full opioid effect. Examples include heroin, oxycodone, methadone, hydrocodone, and morphine. Partial agonists Activate opioid receptors to a lesser degree than a full agonist. Examples include buprenorphine and tramadol. Opioid partial agonists Mixed agonist-antagonists: Have both agonist and antagonist properties. Depending on the dose, they activate some opioid receptor sites while blocking others. Opioid antagonists: Block opioids by attaching to the opioid receptors without activating them. Produce no effect. Examples include naltrexone and naloxone. Morphine- Opioid agonist Therapeutic Class Narcotic analgesic Mechanism of Action Activates μ receptors (alters pain sensation) and κ receptors (decreases GI motility) Indication Moderate / severe pain, reduce bowel motility, cough suppression Contraindication Respiratory disorders, obesity, bowel motility disorders, urinary retention Adverse Effects Pruritis, respiratory depression, constipation, urinary retention, sedation, orthostatic hypotension Specials Avoid alcohol Fentanyl, codeine, methadone: similar to morphine © Joyce University Tramadol-Opioid partial agonist Therapeutic Class Narcotic analgesic Mechanism of Action Activates μ receptors (alters pain sensation) and inhibits reuptake of norepinephrine / serotonin Indication Moderate to severe pain Contraindication -Respiratory disorders, obesity, bowel motility disorders, urinary retention -epilepsy, use alongside of TCAs, SSRIs, SNRIs, MAOIs Adverse Effects Pruritis, respiratory depression, constipation, urinary retention, sedation, orthostatic hypotension, serotonin syndrome, seizures © Joyce University Buprenorphine- Opioid partial agonist Therapeutic Class Narcotic analgesic Mechanism of Action Partial agonist-partial antagonist at certain opioid receptors Indication Opioid withdrawal and maintenance Contraindication Active opioid use, clients NOT in withdrawal Adverse Effects Pruritis, respiratory depression, constipation, urinary retention, sedation, orthostatic hypotension, diaphoresis Specials Can be combined with naloxone to prevent abuse © Joyce University Opioid antagonist Naloxone Nal x ne Therapeutic Class Narcotic antagonist Mechanism of Action Competitive antagonism of CNS opioid receptors Indication Opioid induced respiratory depression, opioid reversal agent Contraindication Tachycardia, tachypnea, cramping, hypertension, vomiting, analgesia reversal Adverse Effects Tachycardia, seizure, hypertension, cardiac arrest, diaphoresis, vomiting Specials May need to re-administer, monitor respiration © Joyce University Fibromyalgia 18 Pregabalin Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, reduces seizure activity Indication Neuropathic pain, fibromyalgia, restless leg syndrome, seizures, epilepsy Contraindication Caution in pregnancy Adverse Effects Somnolence, impaired cognition, blurry vision, weight gain, peripheral edema, dry mouth 19 Amitriptyline Therapeutic Class Antidepressant Mechanism of Action Inhibits re-uptake of norepinephrine and serotonin Indication Fibromyalgia, chronic pain, depression, insomnia Contraindication Seizures, urinary/bowel retention, BPH, glaucoma, hyperthyroidism Adverse Effects Anticholinergic effects, DUCCT-dry mouth, urinary retention, constipation, confusion, tachycardia, sedation, decreased seizure threshold, orthostatic hypotension Adjuvant: A drug that enhances or supports another drug (used in combination with something) 20 Non-Opioid Analgesics 21 Acetaminophen (NOT a NSAID) Therapeutic Class Analgesic Mechanism of Action Slows production of prostaglandins in the CNS Indication Mild pain, fever Contraindication Severe liver disease, chronic alcohol use Adverse Effects Complications rare if taking appropriate dose Acute liver toxicity: nausea/vomiting/diarrhea, sweating, abdominal discomfort à liver failure, coma, death 22 NSAIDS (Non-steroidal anti-inflammatory agents) All are very similar, so understand them as a group and then anything that is unique among them NSAIDs are Nephrotoxic with risk of GI bleeds (and general increased bleeding risk) 23 Aspirin (a salicylate) Therapeutic Class NSAID (Antiplatelet) Mechanism of Action Reduces prostaglandin signaling by inhibiting COX 1 and COX 2 enzymes Indication Inflammatory suppression, mild to moderate pain, fever, anti-platelet blood thinner Contraindication Pregnancy, hypertension, bleeding disorders, children under 19 who have viral illness, surgery, asthmatics Adverse Effects Salicylism (tinnitus, sweating, headache, dizziness) Reye Syndrome (Rare): vomiting, brain dysfunction, seizures Specials Effects are irreversible (have to wait it out) 24 Ibuprofen (NSAID prototype) Therapeutic Class NSAID Mechanism of Action Reduces prostaglandin signaling by inhibiting COX 1 and COX 2 enzymes Indication Inflammatory suppression, mild to moderate pain, fever, arthritis Contraindication Hypertension, peptic ulcer disease, bleeding disorders, aspirin use, ACEIs/ARBs use, asthmatics Adverse Effects GI discomfort, impaired kidney function, hypertension, heart attack, peptic ulcer disease (GI bleed) 25 Celecoxib Therapeutic Class NSAID (Selective COX 2 inhibitor) Mechanism of Action Reduces prostaglandin signaling by selectively inhibiting COX 2 enzymes Indication Inflammatory suppression, mild to moderate pain, fever Contraindication Clients at risk of MI/stroke, sulfonamide allergy, asthmatics, ACEIs/ARBs use Adverse Effects GI discomfort, impaired kidney function, increased risk of heart attack / stroke (lower incidence of ulcers) 26 Neurodegenerative Disease Muscle Relaxants 27 Baclofen- Back-lo-fen Therapeutic Class Central Spasmolytic Mechanism of Action Central action: Enhances GABA effects Indication Muscle spasms in neurologic disorders, cerebral palsy, MS, strokes Contraindication Renal disease, epilepsy, CNS depressants Adverse Effects Sedation, fatigue, constipation, urinary retention, seizures, headache Do NOT discontinue abruptly 28 Dantrolene Therapeutic Class Peripheral Spasmolytic Mechanism of Action Peripheral action: inhibits muscle contraction (by preventing calcium release from skeletal muscle) Indication Malignant hyperthermia, neuroleptic malignant syndrome, muscle spasticity Adverse Effects Hepatotoxicity, photosensitivity, sedation Specials Monitor LFTs Do NOT discontinue abruptly 29 Opioid Analgesics 30 Opioids Substances that interact with the opioid receptor and produce morphine-like effects q Opioid Agonist: Substances that will bind to the receptor and produce a response q Opioid Partial Agonist: Substances that will bind to a receptor and can produce a response q Opioid Antagonist: Substances that will bind to the receptor and NOT produce a response (and also prevent agonists from binding) Agonist A go nist Antagonist tag oo nist A nno 31 Morphine Therapeutic Class Narcotic analgesic Mechanism of Action Activates μ receptors (alters pain sensation) and κ receptors (decreases GI motility) Indication Moderate / severe pain, reduce bowel motility, cough suppression Contraindication Respiratory disorders, obesity, bowel motility disorders, urinary retention Adverse Effects Pruritis, respiratory depression, constipation, urinary retention, sedation, orthostatic hypotension Specials Avoid alcohol Fentanyl, codeine, methadone: similar to morphine 32 Tramadol Therapeutic Class Narcotic analgesic Mechanism of Action Activates μ receptors (alters pain sensation) and inhibits reuptake of norepinephrine / serotonin Indication Moderate to severe pain Contraindication -Respiratory disorders, obesity, bowel motility disorders, urinary retention -epilepsy, use alongside of TCAs, SSRIs, SNRIs, MAOIs Adverse Effects Pruritis, respiratory depression, constipation, urinary retention, sedation, orthostatic hypotension, serotonin syndrome, seizures 33 Buprenorphine Therapeutic Class Narcotic analgesic Mechanism of Action Partial agonist-partial antagonist at certain opioid receptors Indication Opioid withdrawal and maintenance Contraindication Active opioid use, clients NOT in withdrawal Adverse Effects Pruritis, respiratory depression, constipation, urinary retention, sedation, orthostatic hypotension, diaphoresis Specials Can be combined with naloxone to prevent abuse 34 Naloxone Nal x ne Therapeutic Class Narcotic antagonist Mechanism of Action Competitive antagonism of CNS opioid receptors Indication Opioid induced respiratory depression, opioid reversal agent Contraindication Tachycardia, tachypnea, cramping, hypertension, vomiting, analgesia reversal Adverse Effects Tachycardia, seizure, hypertension, cardiac arrest, diaphoresis, vomiting Specials May need to re-administer, monitor respiration 35 Substance Abuse ALCOHOL 36 Substance Abuse Treatment Opioids § Acute overdose – naloxone § Acute withdrawal – clonidine, methadone, buprenorphine § Abstinence – naltrexone, methadone, buprenorphine Alcohol § Acute withdrawal - diazepam/lorazepam, clonidine § Abstinence – disulfiram, naltrexone Nicotine § Withdrawal/abstinence – NRT, bupropion, varenicline Clonidine- helps with the increased BP associated with withdrawal by decreasing the BP. 37 Disulfiram Therapeutic Class Alcohol deterrent Mechanism of Action Reacts with alcohol to form acetaldehyde which induces unpleasant sensations Indication Alcohol abstinence Contraindication Alcohol use Adverse Effects Headache, metallic taste, hepatitis Specials Monitor liver function tests (LFTs) -If client ingests alcohol Nausea, vomiting, flushing, dizziness, headache, chest while on disulfiram… pain, abdominal discomfort, hypotension NOT FOR WITHDRAWAL! This is used AFTER when the client is needs assistance avoiding alcohol use 38 Substance Abuse TOBACCO 39 Bupropion (relating to smoking cessation) Therapeutic Class Antidepressants Mechanism of Action Inhibits norepinephrine and dopamine uptake Indication Smoking cessation Contraindication Seizures, eating disorder Adverse Effects Restlessness, seizures, dry mouth 40 Varenicline Therapeutic Class Smoking cessation aid Mechanism of Action Promotes dopamine release Indication Smoking cessation Contraindication Schizophrenia, manic-depression, suicidal ideation, stimulant use Adverse Effects Nausea, nightmares, headache, insomnia, depression, suicidal ideation Specials Caution in diabetics: can cause hypoglycemia: Monitor glucose 41 Quick Recap Smoking Cessation “I give you PROPs for stopping smoking” “Since you stopped smoking you have VERY CLEAN teeth” (buPROPion) (VAREniCLINE) 42 Migraines 43 Antimigraine Sumatriptan Therapeutic Class Antimigraine Mechanism of Action Vasoconstriction (of CNS blood vessels) Indication Migraine Headaches Contraindication Liver failure, ischemic heart disease, history of myocardial infarct, uncontrolled hypertension Adverse Effects Chest pressure/pain, angina, dizziness, vertigo Specials Report chest pain/pressure immediately 44 Neurodegenerative Disease Parkinson’s 45 Used to treat Parkinson’s Levodopa/Carbidopa Therapeutic Class Antiparkinsonian Mechanism of Action Increases dopamine Indication Parkinson’s Disease, restless leg syndrome Contraindication Psychosis, delusions Adverse Effects Dose dependent: nausea/vomiting, drowsiness, dyskinesia, psychosis, orthostatic hypotension, discolored sweat/urine 46 Used to treat Parkinson’s Pramipexole Therapeutic Class Antiparkinsonian Mechanism of Action Activates dopamine receptors Indication Parkinson’s Disease Adverse Effects Psychosis delusions, dyskinesia, drowsiness, orthostatic hypotension 47 Used to treat Parkinson’s Entacapone (COMT inhibitor) Therapeutic Class Antiparkinsonian Mechanism of Action Prevents levodopa breakdown* (administered with levodopa/carbidopa) Indication Parkinson’s Disease- treats signs and symptoms. Contraindication Liver failure Adverse Effects Dyskinesia, vomiting, diarrhea, sleepiness, urine discoloration (orange-yellow) 48 Used to treat Parkinson’s Benztropine Therapeutic Class Antiparkinsonian Mechanism of Action Anticholinergic that blocks effect of acetylcholine Indication Parkinson’s Disease-treats signs and symptoms Adverse Effects Anticholinergic effects, nausea/vomiting, blurry vision, sedation, confusion Treats these symptoms. Such as tremors 49 Used to treat Parkinson’s Selegiline (MAO-B inhibitor) Therapeutic Class Antiparkinsonian Mechanism of Action Prevents breakdown of dopamine Indication Parkinson’s Disease- treats signs and symptoms. Contraindication MAOIs, anti-depressants, decongestants Adverse Effects Hypertensive crisis with foods high in tyramine, serotonin syndrome with certain medications, nausea, diarrhea 50 Parkinson’s Drugs Recap “eLEV ators lift up DOPA mine” (LEVoDOPA increases dopamine) and “CAR bidopa is the CAR to get it to the brain” “Park your PRAM while the baby naps” (PRAM ipexole is a Parkinson’s drug that causes sleepiness) “Park your BENZ ” (BENZ tropine is a Parkinson’s drug) “Your Parkinson’s is getting worse, no CAP ” (Without entaCAP one, Parkinson’s will worsen) “Don’t SEL L your PARKing spot” (SELegiline is a Parkinson’s drug) 51 Neurodegenerative Disease Alzheimer’s 52 Alzheimer’s Disease A common type of dementia characterized by progressive memory loss, confusion, and inability to communicate effectively “AL’z DOME” (Alzheimer’s drugs: DOnepezil and MEmantine) 53 Used to treat Alzheimer’s Donepezil-1st line Therapeutic Class Anti-Alzheimer’s Mechanism of Action Increases acetylcholine (ACh) levels in the brain (preventing its breakdown by acetylcholinesterase (AChE)) Increases levels in the synapses Indication Alzheimer’s Disease Contraindication Caution in clients with heart disease Adverse Effects Appetite loss, nausea/vomiting/diarrhea, muscle cramping, fatigue, cardiac arrythmia, BP dysregulation 54 Used to treat Alzheimer’s Memantine- add on Therapeutic Class Anti-Alzheimer’s Mechanism of Action Reduces overexcitation of neurons by blocking glutamate from binding to NMDA receptors Indication Alzheimer’s disease (used in combination, not by itself) Contraindication Liver disease, severe renal disease Adverse Effects Hypertension, constipation, nausea/vomiting, headache, dizziness, confusion 55 What are the pharmacological treatment options for anxiety disorders? 56 Alprazolam Therapeutic Class Anxiolytic / Sedative / Hypnotic Mechanism of Action Enhances GABA effects Indication Panic attacks, anxiety disorders, acute stress disorder, PTSD, insomnia Contraindication Respiratory depression, sleep apnea, glaucoma Adverse Effects CNS depression, anterograde amnesia, paradoxical response, withdrawal effects, *respiratory depression if overdose, sedation Specials Avoid grapefruit / alcohol, high-risk activities when using Reversed by activated charcoal / flumazenil 57 Diazepam Therapeutic Class Anxiolytic / Sedative / Hypnotic Mechanism of Action Enhances GABA effects Indication Seizure disorder, agitation, insomnia, muscle spasm, alcohol withdrawal, inducing anesthesia Contraindication Respiratory depression, sleep apnea, hypotension, breastfeeding, substance abuse, renal or live disease, BEERS list Adverse Effects CNS depression, paradoxical response, anorexia, *respiratory depression if overdose, dependence, sedation Specials Avoid grapefruit / alcohol, high-risk activities when using Lorazepam: similar to Diazepam 58 Buspirone Therapeutic Class Anxiolytic Mechanism of Action Unknown: binds to serotonin / dopamine receptors Indication Panic disorder, socialized anxiety disorder, obsessive- compulsive disorder, PTSD, generalized anxiety disorder Contraindication St. John’s Wort, erythromycin, ketoconazole, MAOIs Adverse Effects Suicidal ideation, constipation, headache, GI upset, dependence Specials Avoid grapefruit, NOT sedating 59 What are the risk factors for developing serotonin syndrome? What signs and symptoms are associated with serotonin syndrome? What are the risk factors for developing serotonin withdrawal (serotonin discontinuation syndrome)? What signs and symptoms are associated with serotonin withdrawal? 60 Serotonin Syndrome Toxic state caused by increased serotonin activity in the brain. Too much serotonin. HARMFUL Hyperthermia, Anticognitive, Reflexes, Myoclonus, Fast Heart Rate, Unconsciousness, Loss of GI control Agitation, sweating, hyperreflexia Treatment: Benzodiazepine à Cyproheptadine à ICU SSRI/SNRI Discontinuation Syndrome (Adults) (R E M EM BE R TO TAPE R !) Caused by withdrawal of SSRI/SNRI medications FINISH Flu-like symptoms, Insomnia, Nausea, Imbalance, Sensory disturbance, Hyperarousal 61 What clinical features are associated with extrapyramidal symptoms? 62 Commonly referred to as a drug-induced Extrapyramidal Symptoms (EPS) Haloperidol, chlorpromazine movement disorder Muscle spasms Muscle rigidity Lip smacking n) io ot s) gm or in m ew re ch gt g, in in st re ick ia, st ia) es ue this kin ng a dy (to ak ra ia of ,b es ple ait in gg sk a m in dy x ffl ve n e ng) hu di ss (a cki ,s ar o re ne g, r tu ss D-E-P-A-R-T s tle cin po es pa d n) a( pe ct io isi oo ra th st nt ka s( co sm cle ni us so kin ym ar ar nt lu PS vo in 63 a( ni to ys What signs and symptoms are associated with neuroleptic malignant syndrome? 64 Neuroleptic Malignant Syndrome (NMS) Fever A life-threatening neurological disorder caused by an adverse reaction to antipsychotic drugs A gitation S weating Haloperidol, clozapine, chlorpromazine T achycardia L E ad Pipe (more likely to induce NMS) HypoR eflexia 65 How do the expected adverse effects differ between first generation and second-generation antipsychotic medications? What are Pharmacology Treatment Options for Schizophrenia? 66 1st and 2nd Generation Antipsychotics 1st Generation (Typical) Antipsychotics: Chlorpromazine , Haloperidol Messier, higher risk of EPS, NMS, Anticholinergic effects 2nd Generation (Atypical) Antipsychotics: Risperidone, Olanzapine, Clozapine Less adverse effects, higher risk of metabolic dysfunction (which includes diabetes, weight gain, and increased lipids), lower risk for EPS, NMS, Anticholinergic effects 67 Which medications are indicated for the treatment of both bipolar disorder and seizure disorders? 68 Carbamazepine Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Epilepsy, seizure disorders, trigeminal neuralgia, mania, rapid cycling bipolar disorders Contraindication Immunosuppressed, bleeding disorders, breast feeding Adverse Effects Bone marrow suppression, Steven-Johnson Syndrome, anticonvulsant hypersensitivity syndrome, photosensitivity, nystagmus, hepatotoxicity Specials Monitor CBC, LFTs, serum concentration, avoid grapefruit “Stay in the CAR with CARbamazepine if you don’t want to get sunburned and exposed to bacteria” 69 VaLProic acid Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Seizures, Migraines Mania, rapid cycling bipolar disorders Contraindications Pregnancy, Liver disorders, Phenytoin / Phenobarbital use Adverse Effects Hepatotoxicity, pancreatitis, thrombocytopenia, CNS effects, teratogenic Specials Monitor serum concentration, monitor amylase/lipase, monitor LFTs vaLProic acid à Liver / Pancreas 70 LAmotrigine Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Seizures Mania, rapid cycling bipolar disorders Contraindication Do NOT use with valproic acid, breastfeeding, drug- interactions with other mood stabilizers/antiepileptics Adverse Effects CNS effects, sedation, aseptic meningitis, Steven-Johnson Syndrome, anticonvulsant hypersensitivity syndrome “Keep vALproic acid and LAmotrigine in opposite corners” 71 During general anesthesia, which medications provide sedation and which medications provide pain relief? 72 Propofol- Propofall Therapeutic Class Hypnotic Mechanism of Action Strongly enhances GABA effects to the point of loss of consciousness Indication Deep sedation, intubation, mechanical ventilation Contraindication Hypotension, respiratory compromise Adverse Effects Propofol infusion syndrome, bacterial infection*, hypotension, apnea Propofol infusion syndrome: Occurs after prolonged, high-dose infusions: Metabolic acidosis, hyperkalemia, rhabdomyolysis, cardiac/renal failure * Bacteria grows rapidly in vial when left out 73 Ketamine Therapeutic Class Sedative Mechanism of Action Induces loss of consciousness and elimination of pain sensation, complete dissociation of mind / body Indication Procedures requiring deep sedation / amnesia / analgesia Contraindication Substance abuse, mental illness, cold/cough Adverse Effects Mental confusion upon awakening, hallucinations Specials Can be used in children Hospital-based Midazolam (a benzodiazepine) is often given to address the agitation associated with the mental confusion / hallucinations 74 Local Anesthetics LIDOCAINE TETRACAINE / PROCAINE Type Amide Ester Allergic Reaction Potential Low High Onset 2-5 min (topical) 3-10 min (topical) Examples Topical Topical Epidural / Spinal Spinal Eye conjunctiva Nose / Throat Adverse Effects Lidocaine Toxicity Pruritis, pain, burning, edema, rash, erythema Lidocaine Toxicity (SAMS): Slurred Speech, Altered CNS, Muscle twitching, Seizures 75 Anxiolytics- Medication for anxiety 76 76 Joyce University Alprazolam Therapeutic Class Anxiolytic / Sedative / Hypnotic Mechanism of Action Enhances GABA effects Indication Panic attacks, anxiety disorders, acute stress disorder, PTSD, insomnia Contraindication Respiratory depression, sleep apnea, glaucoma Adverse Effects CNS depression, anterograde amnesia, paradoxical response, withdrawal effects, *respiratory depression if overdose, sedation (Drowsy do not operate heavy machinery or drive Specials Avoid grapefruit / alcohol, high-risk activities when using Reversed by activated charcoal / flumazenil 77 Diazepam Therapeutic Class Anxiolytic / Sedative / Hypnotic Mechanism of Action Enhances GABA effects Indication Seizure disorder, agitation, insomnia, muscle spasm, alcohol withdrawal, inducing anesthesia Contraindication Respiratory depression, sleep apnea, hypotension, breastfeeding, substance abuse, renal or live disease, BEERS list Adverse Effects CNS depression, paradoxical response, anorexia, *respiratory depression if overdose, dependence, sedation Specials Avoid grapefruit / alcohol, high-risk activities when using Lorazepam: similar to Diazepam 78 Buspirone Therapeutic Class Anxiolytic Mechanism of Action Unknown: binds to serotonin / dopamine receptors Indication Panic disorder, socialized anxiety disorder, obsessive- compulsive disorder, PTSD, generalized anxiety disorder Contraindication St. John’s Wort, erythromycin, ketoconazole, MAOIs Adverse Effects Suicidal ideation, constipation, headache, GI upset, dependence Specials Avoid grapefruit, NOT sedating 79 RECAP Anxiety Note: Some antidepressants can also be used to treat anxiety Anxiolytic Benzodiazepine Azapirones “Ben’s LADs”- causes “You can drive the BUS with BUSpirone” sedation Not sedating Lorazepam / Alprazolam / Diazepam (and sometimes Midazolam)- used in addition to ketamine 80 sometimes in children (agitation and confusion. Insomnia 81 81 Joyce University Zolpidem Therapeutic Class Hypnotics Mechanism of Action Enhances GABA effects Indication Insomnia (short term) Contraindication Breastfeeding, Renal and liver disease, respiratory disease, CNS depressants, Geriatrics Adverse Effects Daytime sleepiness, lightheadedness, headache, dependence 82 Antidepressants 1st Generation 83 83 Joyce University Phenelzine (a monoamine oxidase inhibitor MAOI)) Therapeutic Class Antidepressant 1st generation Mechanism of Action Block MAO enzymes in brain: increases NE, DA, Serotonin, and Tyramine Indication Severe resistant depression Contraindication Pheochromocytoma, heart failure, cardiovascular/cerebral vascular disease, SSRI, SNRI, TCAs Adverse Effects CNS overstimulation, orthostatic hypotension, hypertensive crisis, serotonin syndrome, suicidal ideation Specials Monitor BP, suicidal ideation Selegiline: similar to phenelzine 84 Antidepressants 1st Generation: TCAs, MAOIs Many adverse effects and drug-drug / drug-food interactions, greater risk of toxicity MAOIs: avoid eating anything high in Tyramine (aged cheese, cured or processed meats, bananas) Can cause hypertensive crisis. Avoid stimulants and other antidepressants and opioids. 2nd Generation: SSRI, SNRI Much safer to use, less adverse effects, less risk of toxicity, less interactions 85 Antidepressants SNRI Smoking Cessation Amitriptyline Increases risk of hypertension Fluoxetine Tricyclic Antidepressants Venlafaxine SSRI Bupropion Increased risk of sexual dysfunction Can be used for both smoking cessation and antidepression. Anticholinergic Effects 86 Amitriptyline: Tricyclic / Anticholinergic effects Fluoxetine / Paroxetine: SSRI / Bleeding Risk Venlafaxine: SSNRI / HTN Risk (stress the 5HT / NE reuptake inhibition) à risk of serotonin syndrome Antidepressants 2nd Generation 87 87 Joyce University Fluoxetine (SSRI) Therapeutic Class Antidepressants Mechanism of Action Selective serotonin reuptake inhibitor (SSRI) Indication Depression, Anxiety disorders Contraindication MAOI / TCA use, liver disease, Caution with anticoagulants, epilepsy, renal and liver disease, caution in heart disease Adverse Effects Sexual dysfunction, agitation, serotonin syndrome, withdrawal syndrome, weight changes, suicidal ideation, bleeding risk, hyponatremia 88 Venlafaxine (SNRI) Therapeutic Class Antidepressants Mechanism of Action Selective serotonin and norepinephrine reuptake inhibitor Indication Major depression, generalized anxiety disorder, fibromyalgia pain, diabetic neuropathy Contraindication SSRIs, MAOIs, recent MI, St. John’s Wort, Kava, Valerian, caution in bipolar, mania, seizures Adverse Effects Hypertension, insomnia, anxiety, tachycardia, blurred vision, withdrawal syndrome, sexual dysfunction, serotonin syndrome, suicidal ideation (adolescents) Duloxetine: similar to Venlafaxine 89 Anesthetics 90 90 Joyce University Local Anesthetics LIDOCAINE TETRACAINE / PROCAINE Type Amide Ester Allergic Reaction Potential Low High Onset 2-5 min (topical) 3-10 min (topical) Examples Topical Topical Epidural / Spinal Spinal Eye conjunctiva Nose / Throat Adverse Effects Lidocaine Toxicity Pruritis, pain, burning, edema, rash, erythema Lidocaine Toxicity (SAMS): Slurred Speech, Altered CNS, Muscle twitching, Seizures 91 Propofol Therapeutic Class Hypnotic Mechanism of Action Strongly enhances GABA effects to the point of loss of consciousness Indication Deep sedation, intubation, mechanical ventilation Contraindication Hypotension, respiratory compromise Adverse Effects Propofol infusion syndrome, bacterial infection*, hypotension, apnea Propofol infusion syndrome: Occurs after prolonged, high-dose infusions: Metabolic acidosis, hyperkalemia, rhabdomyolysis, cardiac/renal failure * Bacteria grows rapidly in vial when left out 92 Sedatives 93 93 Joyce University Ketamine Therapeutic Class Sedative Mechanism of Action Induces loss of consciousness and elimination of pain sensation, complete dissociation of mind / body Indication Procedures requiring deep sedation / amnesia / analgesia Contraindication Substance abuse, mental illness, cold/cough Adverse Effects Mental confusion upon awakening, hallucinations Specials Can be used in children Hospital-based Midazolam (a benzodiazepine) is often given to address the agitation associated with the mental confusion / hallucinations 94 Antiepileptics 95 95 Joyce University Phenytoin Therapeutic Class Anticonvulsant Mechanism of Action Slows / suppresses neuronal firing, slows neuronal action potentials Indication Epilepsy, seizure disorders Contraindication Allergy, anticonvulsant hypersensitivity syndrome Adverse Effects Gum swelling and overgrowth, sedation, fatigue, nystagmus, confusion, hirsutism, Steven-Johnson Syndrome, toxicity Anticonvulsant hypersensitivity syndrome: fever, rash, hepatitis 96 Gabapentin Therapeutic Class Anticonvulsant Mechanism of Action Unknown Indication Epilepsy, Seizures, Diabetic neuropathy, restless leg syndrome Contraindication Renal failure Adverse Effects Somnolence, dizziness, ataxia, fatigue, nystagmus, peripheral edema, dry mouth Specials Monitor serum creatinine 97 Pregabalin Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Seizures, epilepsy, neuropathic pain, fibromyalgia, restless leg syndrome Adverse Effects Somnolence, dizziness, impaired cognition, headache, blurred vision, weight gain, peripheral edema, angioedema 98 Antiepileptics/Mood Stabilizer Combo Drugs 99 99 Joyce University Carbamazepine Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Epilepsy, seizure disorders, trigeminal neuralgia, mania, rapid cycling bipolar disorders Contraindication Immunosuppressed, bleeding disorders, breast feeding Adverse Effects Bone marrow suppression, Steven-Johnson Syndrome, anticonvulsant hypersensitivity syndrome, photosensitivity, nystagmus, hepatotoxicity Specials Monitor CBC, LFTs, serum concentration, avoid grapefruit.. Report fevers/cough “Stay in the CAR with CARbamazepine if you don’t want to get sunburned and exposed to bacteria” 100 VaLPproic acid Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Seizures epilepsy, Migraines Mania, rapid cycling bipolar disorders Contraindications Pregnancy, Liver disorders, Phenytoin / Phenobarbital use Adverse Effects Hepatotoxicity, pancreatitis, thrombocytopenia, CNS effects, teratogenic Specials Monitor serum concentration, monitor amylase/lipase, monitor LFTs, skin rash vaLProic acid à Liver / Pancreas 101 LAmotrigine Therapeutic Class Anticonvulsant Mechanism of Action Enhances GABA effects, suppresses neuronal firing Indication Seizures, epilepsy Mania, rapid cycling bipolar disorders Contraindication Do NOT use with valproic acid, breastfeeding, drug- interactions with other mood stabilizers/antiepileptics Adverse Effects CNS effects, sedation, aseptic meningitis, Steven-Johnson Syndrome, anticonvulsant hypersensitivity syndrome “Keep vALproic acid and LAmotrigine in opposite corners” 102 Lithium Carbonate 103 103 Joyce University Lithium Carbonate Therapeutic Class Antimanic Mechanism of Action Modulates neurochemical changes in the brain Reduces norepinephrine AND increases serotonin Indication Mania (acute), Bipolar disorders, epilepsy Contraindication Breastfeeding, renal disease, hyponatremia Adverse Effects GI distress, Diabetes Insipidus, fine hand tremors, mild thirst, weight gain, renal toxicity, goiter, hypothyroidism, bradycardia, hypotension, electrolyte imbalance (hyponatremia) Specials Caution with diuretics and NSAIDs Monitor serum lithium levels, TSH levels, sodium, Serum creatinine, electrolytes Therapeutic levels: 0.6-1.2mEq/L (if exceeded becomes toxic: initial effects being hand tremor, GI upset) 104 Antipsychotics 105 105 Joyce University 1st and 2nd Generation Antipsychotics 1st Generation (Typical) Antipsychotics: Chlorpromazine (Haloperidol) Messier, higher risk of EPS, NMS, Anticholinergic effects 2nd Generation (Atypical) Antipsychotics: Risperidone (Clozapine) Less adverse effects, higher risk of metabolic dysfunction, lower risk for EPS, NMS, Anticholinergic effects 106 Chlorpromazine Therapeutic Class 1st Generation Antipsychotic Mechanism of Action Blocks dopamine thereby inhibiting psychotic manifestations Indication Psychotic disorders, schizophrenia, bipolar, nausea/vomiting Contraindication Parkinson’s, hypotension, renal and liver disease, seizure disorder, anticholinergic drug use, CNS depressants, dopamine agonists Adverse Effects Higher risk of Extrapyramidal symptoms, neuroleptic malignant syndrome, anticholinergic effects, sexual dysfunction, agranulocytosis, hepatotoxicity, galactorrhea Haloperidol / Fluphenazine: similar to Chlorpromazine 107 Risperidone Therapeutic Class 2nd Generation Antipsychotic Mechanism of Action Blocks serotonin and dopamine receptors Indication Schizophrenia spectrum disorders, psychotic episodes, bipolar, impulse control disorders Contraindication Dementia, CNS depressants, seizures, cardiovascular disease Adverse Effects Diabetes mellitus, hyperglycemia, weight gain, hypercholesterolemia, galactorrhea, anticholinergic effects, sedation, EPS, sexual dysfunction Olanzapine: similar to Risperidone 108 Clozapine Therapeutic Class Antipsychotics Mechanism of Action Unknown, binds to dopamine receptors Indication Schizophrenia unresponsive to other treatments Contraindication Cardiac / respiratory disease, epilepsy, severe neutropenia (BLACK BOX WARNING), CNS depressants, Opioid use Adverse Effects Seizures, CNS depressants, anticholinergic effects, leukopenia (neutropenia), NMS Specials Monitor CBC (obtain CBC BEFORE initiating treatment) 109 CNS Stimulants And Anti-Narcoleptics 110 110 Joyce University ADHD Multiple medications are used to treat ADHD Stimulant: Methylphenidate, Amphetamine Non-stimulant: Atomoxetine, Guanfacine Due to effects on sleep and appetite it is important to monitor changes in sleep patterns (hours) and weight changes (especially in pediatric clients) 111 Methylphenidate Therapeutic Class CNS stimulant Mechanism of Action Increases norepinephrine and dopamine Indication ADHD, Narcolepsy, Obesity Contraindication Hyperthyroidism, hypertension, heart disease, anxiety, psychosis, stimulant use, MOAIs Adverse Effects Insomnia, restlessness, reduced appetite, weight loss, dysrhythmia, dependence, withdrawal 112 Atomoxetine Therapeutic Class ADHD drug Mechanism of Action Blocks norepinephrine reuptake Indication ADHD, depression Contraindication Cardiovascular disorder, hepatic disorders, hypotension, hypertension, angle-closure glaucoma Adverse Effects Appetite suppression, weight loss, growth suppression, hepatotoxicity, seizure activity Specials Not a stimulant. Monitor child behavior, administer early in day 113

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