NR565 ADVANCED PHARMACOLOGY FUNDAMENTALS MIDTERM AND FINAL EXAM STUDY GUIDE| 300 QUESTIO, Exams of Nursing

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NR565 ADVANCED PHARMACOLOGY FUNDAMENTALS MIDTERM AND FINAL EXAM STUDY GUIDE| 300 QUESTIONS AND 100 % CORRECT ANSWERS | RATED A QUIZ BANK | LATEST, 2024 / 2025| CHAMBERLAIN COLLEGE The process by which drugs are absorbed, distributed within the body, metabolized, and excreted. - CORRECT ANSWER>>Pharmacokinetics The study of what the drug does to the body - CORRECT ANSWER>>Pharmacodynamics Rate of dissolution Surface area Blood flow Lipid solubility pH partitioning - CORRECT ANSWER>>Factors Affecting Drug Absorption Blood flow to tissues Ability to exit the vascular system Blood-brain barrier Protein-binding capacity - CORRECT ANSWER>>Factors Affecting Drug Distribution substances that are foreign to the body, usually synthetic chemical compounds; medications are a common example - CORRECT ANSWER>>Xenobiotics xenobiotic-metabolizing enzymes necessary for the production of cholesterol and steroids and the detoxification of chemicals and drug metabolism. - CORRECT ANSWER>>Cytochrome P450 (CYP450) responsible for phase 1 metabolism in which drugs are oxidized, reduced, or hydrolyzed - CORRECT ANSWER>>Function of Cytochrome P450 (CYP450) Oxidation; Reduction; Hydrolysis - CORRECT ANSWER>>Phase 1 Metabolism of Drugs via P450 -Drug becomes completely inactive -Drug becomes partially inactive but one or more metabolites remain active -Original drug is not pharmacologically active but one metabolite remains active - CORRECT ANSWER>>Three possible outcomes of phase 1 drug metabolism. Medications that can increase the rate of another drug's metabolism by elevating CYP450 enzyme activity via increasing enzyme synthesis. decreasing the concentration of the "parent drug" - CORRECT ANSWER>>CYP450 Inducers CRAPGPS Carbamazepine Rifampin Alcohol Phenytoin Griseofulvin Phenobarbital Sulfonylureas - CORRECT ANSWER>>CYP450 Inducer Medications Medications that inhibit the metabolic activity of one or more of the CYP450 enzymes. Higher risk for toxicity; prolongs the pharmacological effect of the "parent drug". - CORRECT ANSWER>>CYP450 Inhibitors VISACKGQ Valproate Isoniazid Sulfonamides Amiodarone Chloramphenicol Ketoconazole Grapefruit Juice Quinidine - CORRECT ANSWER>>CYP450 Inhibitor Medications -potentially Inappropriate Medication (PIM) use in older adults Pain in the internal organs and abdomen Poorly localized (C-fibers) Radiates Most responsive to opiates May also use corticosteroids, NSAIDs - CORRECT ANSWER>>Acute Visceral Pain any drug, natural or synthetic, that has actions similar to those of morphine - CORRECT ANSWER>>Opioids Mu (μ) Kappa (k) Delta (δ) - CORRECT ANSWER>>Opioid Receptor Families (1) pure opioid agonists, (2) agonist-antagonist opioids, (3) pure opioid antagonists. - CORRECT ANSWER>>At each type of receptor, a drug can act in one of three ways: Opioid receptor most responsible for mediating analgesic properties - CORRECT ANSWER>>Mu (u) Receptor activate µ receptors and κ receptors. produce analgesia, euphoria, sedation, respiratory depression, physical dependence, constipation, and other effects Prototype Drug: MORPHINE - CORRECT ANSWER>>Pure opioid agonists Prototype drug of pure opioid agonist; Strong Opioid Agonist - CORRECT ANSWER>>Morphine A strong opioid analgesic with a high milligram potency (about 100 times that of morphine). - CORRECT ANSWER>>Fentanyl strong opioid agonists; moderate to strong opioid agonists - CORRECT ANSWER>>Subcategory of Pure Opioid Agonist Oxycodone (Roxicodone, Oxycontin); Hydrocodone (Vicodin) - CORRECT ANSWER>>Moderate to Strong Pure Opioid Agonists The actions of these drugs at µ and κ receptors When administered alone, produce analgesia. However, if given to a patient who is taking a pure opioid agonist, can antagonize analgesia Prototype Drug: Pentazocine - CORRECT ANSWER>>Agonist-Antagonist Opioids drug is indicated for mild to moderate pain and is much less effective than morphine against severe pain. acts as an agonist at κ receptors and as an antagonist at µ receptors. the drug produces analgesia, sedation, and respiratory depression. If administered to a patient who is physically dependent on a pure opioid agonist, can precipitate withdrawal; this is due to agonist effect at (mu) receptor which this drug antagonizes. - CORRECT ANSWER>>Pentazocine (Talwin) act as antagonists at µ and κ receptors; Their principal use is reversal of respiratory and CNS depression caused by overdose with opioid agonists. methylnaltrexone—is used to treat opioid-induced constipation. Naloxone (Narcan) is the prototype of the pure opioid antagonists. - CORRECT ANSWER>>Pure opioid antagonists Moderate to Severe Pain - CORRECT ANSWER>>Opioid Pain Consideration Referral to a pain specialist is required for patients who take this dose of Morphine Milligram Equivalents - CORRECT ANSWER>>120 mg per day of morphine milligram equivalents Sedation, Nausea/Vomiting, Constipation, Urinary Retention, Potential for Addiction, Respiratory Depression; Pupillary Dilation - CORRECT ANSWER>>Adverse Effects of Opioids classic triad of signs: coma, respiratory depression, and pinpoint pupils. Coma is profound, and the patient cannot be aroused. - CORRECT ANSWER>>Opioid Toxicity/Overdose ventilatory support and giving an opioid antagonist. Naloxone (Narcan) is the traditional antagonist (opioid reversal) of choice. *Administering NARCAN can induce withdrawal effect in an individual who is chronically dependent on opioids. - CORRECT ANSWER>>Opioid Overdose Treatment Pure Opioid Agonist, used to relieve pain but also treat opioid addiction. Use to treat opioid addicts restricted to opioid treatment programs approved by the designated state authority and certified by the federal Substance Abuse and Mental Health Services Administration. - CORRECT ANSWER>>Methadone Opioid Reversal; Can cause QT prolongation and fatal dysrhythmias - CORRECT ANSWER>>Naloxone (Narcan) Agonist-Antagonist Opioid; promotes analgesia similar to morphine; used for treatment of opioid addiction; prolongs QT interval and hence may pose a risk for potentially fatal dysrhythmia can be prescribed and dispensed in general medical settings, such as primary care offices. - CORRECT ANSWER>>Buprenorphine 1) Improving access to treatment and recovery services 2)Promoting use of overdose-reversing drugs 3)Strengthening our understanding of the epidemic through better public health surveillance 4)Providing support for cutting-edge research on pain and addiction 5)Advancing better practices for pain management - CORRECT ANSWER>>Strategies to Address Opioid Crisis can lead to physical dependence in only 4-8 weeks. - CORRECT ANSWER>>Opioids Dependency Pain Assessment; Patient education; Initiating Therapy w/ non-opioid/non- pharmacologics; assess risk of abuse; safe dose consideration (lowest possible initial dose); withdrawal risk - CORRECT ANSWER>>Safe Opiate Prescribing Considerations Utilize assessment tools such as NIDA-Modified ASSIST; evaluate state prescription drug monitoring program (PDMP); obtaining a urine drug test for controlled -Examples of drugs included in Schedule IV are alprazolam, clonazepam, and diazepam. - CORRECT ANSWER>>Controlled Substances Act Class 4 -The drug or other substance has a low potential for abuse relative to the drugs or other substances in Schedule IV. -The drug or other substance has a currently accepted medical use in treatment in the United States. -Abuse of the drug or other substances may lead to limited physical dependence or psychological dependence relative to the drugs or other substances in Schedule IV. -Cough medicines with codeine are examples of Schedule V drugs. - CORRECT ANSWER>>Controlled Substances Act Class 5 Prescriptions may be oral, written, or electronic - CORRECT ANSWER>>schedules III and IV drugs may be dispensed without a prescription provided certain restrictions apply. - CORRECT ANSWER>>Schedule V Drugs all have approved applications in the United States - CORRECT ANSWER>>Schedule II-V Drugs Only prescribers registered with this agency are authorized to prescribe controlled drugs - CORRECT ANSWER>>DEA When dispensed their containers must bear this label: Caution—Federal law prohibits the transfer of this drug to any person other than the patient for whom it was prescribed. - CORRECT ANSWER>>Schedule II, III, and IV Drugs Anxiolytic medication; Does not produce Analgesia/antipsychotic effects; Decrease anxiety; Mild sedation - CORRECT ANSWER>>Benzodiazepines work on GABA receptors as an AGONIST; anxiolytic; decrease anxiety; Mild Sedative Effect - CORRECT ANSWER>>Benzodiazepine PD Drowsiness and Confusion are main AE; - CORRECT ANSWER>>Benzodiazepine AE GABA receptor antagonist; Reversal for Benzodiazepine overdose; - CORRECT ANSWER>>Flumazenil Reduction of the frequency and intensity of anginal attacks. Prototype Nitrate Drug; Acts directly on vascular smooth muscle (VSM) to promote vasodilation - CORRECT ANSWER>>Nitroglycerin decreasing cardiac oxygen demand. decreases venous return to the heart and thereby decreases ventricular filling; the resultant decrease in wall tension (preload) decreases oxygen demand. - CORRECT ANSWER>>Nitrates: Mechanism of Action highly lipid soluble - CORRECT ANSWER>>Nitroglycerin: Pharmacokinetics & Pharmacodynamics headache, hypotension, and tachycardia; All secondary to vasodilation. - CORRECT ANSWER>>Nitroglycerin: AE β blockers, CCBs, diuretics, and all other drugs that can lower blood pressure, Also, patients should be advised to avoid alcohol. phosphodiesterase type 5 inhibitors (sildenafil) is contraindicated. - CORRECT ANSWER>>Nitroglycerin: Contraindications β blockers, verapamil, and diltiazem - CORRECT ANSWER>>Drugs that suppress nitroglycerin-induced tachycardia No routine blood monitoring necessary - CORRECT ANSWER>>Nitroglycerin: Monitoring keep a record of the frequency and intensity of anginal attacks and the factors that precipitate these attacks; phosphodiesterase type 5 inhibitors (sildenafil) is contraindicated. - CORRECT ANSWER>>Nitroglycerin: Patient Teaching Indications include; hypertension, angina pectoris, heart failure, and cardiac dysrhythmias. Other uses include hyperthyroidism; migraine prophylaxis; performance anxiety, phechromocytoma; and glaucoma; Prototype drug includes: Propanolol/Metoprolol - CORRECT ANSWER>>β Blockers Blockade of β1 receptors in the heart. 1) reduced heart rate; (2) reduced force of contraction; and (3) reduced velocity of impulse conduction through the atrioventricular (AV) node. β1 receptors in the heart. - CORRECT ANSWER>>β- Adrenergic Antagonists Mechanism of Action Bradycardia; Reduced Cardiac Output; Precipitation of Heart Failure; AV Block; Rebound cardiac excitation; - CORRECT ANSWER>>Adverse Effects of β1 Blockade Blockade of β2 receptors in the lungs can cause constriction of the bronchi; Hypoglycemia - CORRECT ANSWER>>Adverse effects of β2 blockade propranolol and metoprolol. - CORRECT ANSWER>>Prototype β Blockers first-generation β blockers, produces a nonselective β blockade; blocks both β1- and β2-adrenergic receptors - CORRECT ANSWER>>Propranolol blocking cardiac β1 receptors; reduce the heart rate, decrease the force of ventricular contraction, and suppress impulse conduction through the AV node; net effect is a reduction in cardiac output. - CORRECT ANSWER>>β1 effects of Propanolol (1) bronchoconstriction (through β2 blockade in the lungs); (2) vasoconstriction (through β2 blockade on certain blood vessels); (3) reduced glycogenolysis(through β2 blockade in skeletal muscle and liver) - CORRECT ANSWER>>β2 effects of propranolol high lipid solubility; penetrates the blood-brain barrier with ease; and (2) eliminated primarily by hepatic metabolism. - CORRECT ANSWER>>Propanolol Pharmacokinetics β1 blockade: Bradycardia, Heart Failure, Rebound Cardiac Excitation; Does not effect heart muscle directly and therefore no AE as that of Verapamil/Diltiazem - CORRECT ANSWER>>Dihydropyridine Blockade at peripheral arterioles causes dilation and thereby reduces arterial pressure. • Blockade at arteries and arterioles of the heart increases coronary perfusion. • Blockade at the SA node reduces heart rate. • Blockade at the AV node decreases AV nodal conduction. • Blockade in the myocardium decreases force of contraction - CORRECT ANSWER>>Verapamil Effects Angina pectoris; Essential hypertension; Cardiac dysrhythmias - CORRECT ANSWER>>Verapamil Therapeutic Uses Constipation; dizziness, facial flushing, headache, and edema of the ankles and feet - CORRECT ANSWER>>Verapamil Adverse Effects SA Node block->bradycardia; AV Node Block>partial/complete AV block; Myocardium>decrease contractility; - CORRECT ANSWER>>Calcium Channel Blockers Cardiac Adverse Effects -Digoxin; increase risk of AV block and raises plasma digoxin levels when combined: -β-adrenergic blocking agents due to similar effects of decrease heart rate, AV conduction, and contractility - CORRECT ANSWER>>Verapamil/Diltiazem Drug Contraindication Grapefruit juice can inhibit the intestinal and hepatic metabolism of many drugs and thus raise their levels. - CORRECT ANSWER>>Verapamil/Diltiazem Food Contraindication -blocks calcium channels in the heart and blood vessels; -lower blood pressure through arteriolar dilation; -used for angina pectoris, essential hypertension, and cardiac dysrhythmias - CORRECT ANSWER>>Diltiazem Actions and Uses Orally well absorbed and then extensively metabolized on its first pass through the liver; bioavailability is only about 50% - CORRECT ANSWER>>Verapamil/Diltiazem Pharmacokinetics CONTRINDICATED in patients with hypotension, sick sinus syndrome, and second- or third-degree atrioventricular block. - CORRECT ANSWER>>Verapamil and Diltiazem High Risk Patients hypertension, angina, and cardiac dysrhythmias. - CORRECT ANSWER>>Verapamil and Diltiazem Therapeutic Indication No routine blood monitoring required. - CORRECT ANSWER>>Verapamil and Diltiazem Monitoring -Dihydropyridine; -blocks calcium channels in VSM of arteriole; promotes vasodilation; -produces very little blockade of calcium channels in the heart - CORRECT ANSWER>>Nifedipine HTN; Angina; Not indicated for cardiac dysrhythmias - CORRECT ANSWER>>Nifedipine Indication No heart specific effects; edema, flushing, headache, dizziness reflex tachycardia AE: Secondary to arteriole vasodilation - CORRECT ANSWER>>Nifedipine Adverse Effects approved for essential hypertension and angina - CORRECT ANSWER>>Dihydropyridines/Nifedipine Therapeutic Goal hypotension, use cautiously w/ sick sinus syndrome, heart failure, and second- or third-degree atrioventricular block. - CORRECT ANSWER>>Dihydropyridines/Nifedipine High Risk Patients Reflex tachycardia can be suppressed with a β blocker. Peripheral edema can be reduced with a diuretic - CORRECT ANSWER>>Dihydropyridines/Nifedipine Adverse Effects well absorbed after oral administration but undergoes extensive first-pass metabolism; only about 50% of an oral dose reaches the systemic circulation. - CORRECT ANSWER>>Nifedipine Pharmacokinetics systolic blood pressure < 90 mm Hg sick sinus syndrome recent myocardial infarction (MI) or pulmonary congestion second- or third-degree AV block (unless the patient has a pacemaker) concurrent use with rifampin (Rifadin®) - CORRECT ANSWER>>Calcium Channels Blockers Contraindications Used with precautions in patient with: heart failure aortic stenosis severe hepatic impairment (reduction in dose recommended) advanced age, older adults, due to increased risk of hypotension secondary to decrease in body mass, hepatic, renal, and cardiac function - CORRECT ANSWER>>Calcium Channel Blocker Prescribing Considerations Hypertension; Edema; referred agent for treating stage 1 hypertension; Preferred initial HTN therapy for treating African Americans Reduce BLOOD VOLUME; VENOUS PRESSURE; PRELOAD - CORRECT ANSWER>>Thiazide Diuretics Treatment Goal/Therapeutic Use promotes urine production by blocking the reabsorption of sodium and chloride in the early segment of the distal convoluted tubule - CORRECT ANSWER>>Thiazide Diuretic Mechanism of Action Hydrochlorothiazide - CORRECT ANSWER>>Thiazide Diuretic Prototype Drug Diuresis begins about 2 hours after oral administration. Effects peak within 4 to 6 hours and may persist up to 12 hours. - CORRECT ANSWER>>Hydrochlorothiazide Pharmacokinetics patients with cardiovascular disease, renal impairment, diabetes mellitus, history of gout; patients taking digoxin, lithium, or antihypertensive drugs. block the actions of angiotensin II at receptor site; block access of angiotensin II to its receptors in blood vessels, the adrenals, and all other tissues. - CORRECT ANSWER>>Angiotensin II Receptor Blockers Mechanism of Action Reduce blood pressure in patients with hypertension, improve hemodynamics in patients with heart failure, slow progression of established diabetic nephropathy, reduce mortality, and treat heart failure after myocardial infarction - CORRECT ANSWER>>Angiotensin II Receptor Blockers Therapeutic Goal do not inhibit kinase II and hence do not increase levels of bradykinin in the lung. a lower risk for cough; do not cause clinically significant hyperkalemia - CORRECT ANSWER>>Angiotensin II Receptor Blockers Difference from ACE Inhibitors Angioedema; can cause renal failure in patients with bilateral renal artery stenosis or stenosis in the artery to a single remaining kidney; - CORRECT ANSWER>>ARBs Adverse Effects Fetal Toxicity; Cannot be taken during pregnancy - CORRECT ANSWER>>ARBs/ACE Inhibitor Black Box Warning Other antihypertensive agents - CORRECT ANSWER>>ARBs Drug Interaction Renal Montioring; - CORRECT ANSWER>>Angiotensin II Receptor Blockers Monitoring Losartan - CORRECT ANSWER>>ARBs Prototype Drug third generation β blocker; act on both alpha and beta receptors; acts on β1, β2, α1 causing vasodilation - CORRECT ANSWER>>Labetalol asthma, hypotensive, 2nd/3rd degree "AV block," uncontrolled heart failure, bradycardia. - CORRECT ANSWER>>Labetalol Contraindication most significant adverse effect is orthostatic hypotension; other adverse effects include reflex tachycardia, nasal congestion, inhibition of ejaculation; sodium retention and increased blood volume - CORRECT ANSWER>>Adverse Effects of α Blockade Hepatic - CORRECT ANSWER>>Metabolism of Labetalol, Propanolol, Metoprolol Moderate - CORRECT ANSWER>>Labetalol Lipid Solubility (1) agents that inhibit the RAAS (ACE Inhibitors/ARBs), (2) diuretics (3) β blockers. - CORRECT ANSWER>>Drugs Used to Treat Heart Failure RAAS Inhibitors: Captopril (angiotensin-converting enzyme inhibitor) Losartan (angiotensin II receptor blocker) Eplerenone (aldosterone antagonist) Diuretics: Hydrochlorothiazide Furosemide Inotropic Agent: Digoxin (a cardiac glycoside) β Blocker: Metoprolol - CORRECT ANSWER>>Prototype Drugs for HF NSAIDS, Alcohol, CCB, - CORRECT ANSWER>>Drugs that precipitate or exacerbate Heart Failure Inhibit ANG1-->ANG2; Decrease preload/afterload and increase cardiac output; Decrease VSM tone =decrease BP; Decrease Aldosterone production = Decrease NA/H20 retention - CORRECT ANSWER>>HF ACE Inhibitor Mechanism of Action Captopril (angiotensin-converting enzyme inhibitor) Losartan (angiotensin II receptor blocker) Eplerenone (aldosterone antagonist) - CORRECT ANSWER>>HF: RAAS Inhibitors Cough; Angioedema; First Dose Hypotension; Hyperkalemia - CORRECT ANSWER>>ACE Inhibitor Main AE Decrease pulmonary congestion; peripheral edema Decrease preload/Afterload Hydrochlorothiazide (mild diuretic) Furosemide (Lasix) (strong diuretic) - CORRECT ANSWER>>HF: Diuretics Furosemide; Preferred for HF due to profound diuresis or patient w/ renal insufficiency - CORRECT ANSWER>>HF: Loop Diuretic hypotension; hypokalemia; increase digitalis toxicity OH DANG! Ototoxicity Hypokalemia Dehydration Allergy (Sulfa) Nephritis Gout - CORRECT ANSWER>>Loop Diuretic AE Digoxin (a cardiac glycoside) - CORRECT ANSWER>>HF: Inotropic Agent Metoprolol; Selective blockade of B1 receptor - CORRECT ANSWER>>HF: β Blocker Decrease conversion of ANG1-->ANG2 ACEIs cause dilation of arterioles and veins Decrease the release of aldosterone=decrease NA/H20 retention; Decrease VSM=Decrease BP - CORRECT ANSWER>>HF: ACEIs Therapeutic Second line choice for HF if ACE Inhibitor cannot be tolerated due to cough/angioedema; valsartan (Diovan); candesartan (Atacand) - CORRECT ANSWER>>HF: ARBs Block aldosterone receptor; Increase NA/H20 excretion; Increase K+ retention eplerenone and spironolactone - CORRECT ANSWER>>HF: Aldosterone Antagonist used for patients with high LDL levels, specifically in patients with heterozygous familial hypercholesterolemia or atherosclerotic heart problems who need additional lowering of LDL cholesterol. Examples; Alirocumab (Praluent) and Evolocumab (Repatha) - CORRECT ANSWER>>Monoclonal Antibodies (Proprotein Convertase Subtilisin/Kexin Type 9 [PCSK9] Inhibitors) Cholesterol Absorption Inhibitors; Most used non-statin medication - CORRECT ANSWER>>Ezetimibe -myopathy, rhabdomyolysis, hepatitis, pancreatitis, and thrombocytopenia; - CORRECT ANSWER>>Ezetimibe Adverse Effects should not be used in patients with severe hepatic impairment - CORRECT ANSWER>>Ezetimibe Prescribing Concerns Statins, Fibrates, Bile Acid Sequestrants, Cyclosporins; - CORRECT ANSWER>>Ezetimibe Drug Interactions Used primarily to prevent thrombosis in veins and the atria of the heart; decrease formation of fibrin; Three Classes: vitamin K antagonist; direct factor Xa inhibitor; direct thrombin inhibitor; - CORRECT ANSWER>>Anticoagulants Inhibits synthesis of vitamin K-dependent clotting factors, including prothrombin and factor X - CORRECT ANSWER>>Warfarin (Coumadin) (1) anticoagulants, (2) antiplatelet drugs, and (3) thrombolytic drugs, also known as fibrinolytic drugs - CORRECT ANSWER>>Drugs for Thromboembolic Disorders inhibit platelet aggregation; Examples: Aspirin, Clopidogrel (Plavix) - CORRECT ANSWER>>Antiplatelet drugs promote the lysis of fibrin, causing the dissolution of thrombi. (Alteplase-TPA) - CORRECT ANSWER>>Thrombolytic Drugs Heparin and all other anticoagulants pose a risk for spinal or epidural hematoma in patients undergoing spinal puncture or spinal or epidural anesthesia - CORRECT ANSWER>>Spinal or Epidural Hematoma Prevention of thrombosis; - CORRECT ANSWER>>Heparins Therapeutic Goals aPTT Values - CORRECT ANSWER>>Heparin Monitoring patients with severe thrombocytopenia or uncontrollable bleeding - CORRECT ANSWER>>Heparin High Risk Patients Bleeding - CORRECT ANSWER>>Heparin Adverse Effects Prevention of Thrombus - CORRECT ANSWER>>Warfarin Therapeutic Goal PT/INR should be monitored frequently at the onset of therapy;INR on a weekly basis, monthly monitoring is reasonable. - CORRECT ANSWER>>Warfarin Monitoring Pregnancy; Uncontrollable Bleeding; Vitamin K deficient; Liver Disease - CORRECT ANSWER>>Warfarin High Risk Patients Activates antithrombin, which then inactivates thrombin and factor Xa - CORRECT ANSWER>>Heparin Mechanism of Action Apixaban (Eliquis), Rivaroxaban (Xarelto), Dabigatran (Pradaxa); - CORRECT ANSWER>>Direct Oral Anticoagulants Dabigatran (Pradaxa) - CORRECT ANSWER>>Direct Oral Anticoagulants (DOACs)>Direct Thrombin Inhibitors Rivaroxaban (Xarelto); Apixaban (Eliquis) - CORRECT ANSWER>>Direct Oral Anticoagulants (DOACs)>Direct Factor Xa Inhibitor Prevention and treatment of thrombosis - CORRECT ANSWER>>DOACs Therapeutic Goal No routine monitoring is required with these drugs. - CORRECT ANSWER>>DOACs Monitoring uncontrolled bleeding. Use with caution in patients with high risk for bleeding or renal dysfunction. - CORRECT ANSWER>>DOACs High Risk Patients Poor "Metabolizers": Patients with variant forms of the CYP2C19 gene cannot reliably convert clopidogrel to its active form. - CORRECT ANSWER>>Clopidogrel Black Box Warning suppress platelet aggregation; principal indication for the is the prevention of thrombosis in arteries Prevent blockage of coronary artery stents and reduce thrombotic events - CORRECT ANSWER>>Antiplatelet Drugs Therapeutic Intent antiplatelet drugs: prevention of thrombosis in arteries: anticoagulants (e.g., heparin, warfarin) prevention of thrombosis in veins. - CORRECT ANSWER>>Antiplatelet vs. Anticoagulant Aspirin, a Cyclooxygenase Inhibitor; P2Y12 ADP Receptor Blockers; PAR-1 Antagonists - CORRECT ANSWER>>Major Classes of Antiplatelet Drugs Salicylate Medication Irreversibly inhibits cyclooxygenase and thereby blocks synthesis of thromboxane A2; suppresses platelet aggregation by causing irreversible inhibition of cyclooxygenase, an enzyme required by platelets to synthesize TXA2; - CORRECT ANSWER>>Aspirin Mechanism of Action Prevention of CV disease; Colorectal Cancer; Acute Coronary Syndrome; Primary prevention of myocardial infarction; Prevention of Stroke; TIA; MI; Angina; - CORRECT ANSWER>>Aspirin Indication Irreversibly blocks receptors for ADP - CORRECT ANSWER>>Clopidogrel (Plavix) Prasugrel (Effient) Ticagrelor (Brilinta) Mechanism Prevent blockage of coronary artery stents and reduce thrombotic events. - CORRECT ANSWER>>Antiplatelet Medications Therapeutic Goals For Gout: appropriate for patients younger than 60 years old who do not have a history of renal, cardiovascular, or active GI disease - CORRECT ANSWER>>NSAIDS May increase the risk for myocardial infarction, stroke, and other thromboembolic events. May increase the risk for dangerous gastrointestinal adverse effects such as bleeding, ulceration, and perforation. - CORRECT ANSWER>>NSAIDS Black Box Warning -Use with extreme caution in patients with peptic ulcer disease, bleeding disorders, and those taking anticoagulants. -Caution is also needed when treating older adult patients with heart failure, renal dysfunction, or angina pectoris. -Long-term therapy, start with a proton pump inhibitor to decrease risk of GI bleeding. - CORRECT ANSWER>>NSAIDs NSAIDS; Colchicine - CORRECT ANSWER>>Treatment for acute gout Allopurinol; Febuxostat - CORRECT ANSWER>>Treatment for recurrent/chronic gout Urate Lower Drugs/Anti-Hyperuricemia Inhibits xanthine oxidase, interfering with conversion of hypoxanthine and xanthine to uric acid. Decreases the production of Uric Acid - CORRECT ANSWER>>Allopurinol and Febuxostat drug of choice for patients with renal dysfunction or who overproduce uric acid; current drug of choice for chronic tophaceous gout - CORRECT ANSWER>>Allipurinol Caution in African American pts (incr. HLA-B 5801 allele prevalence); caution in patients of Han Chinese, Korean, Thai, Native Hawaiian, Pacific Islander ancestry (incr. HLA-B 5801 allele prevalence); caution if HLA-B 5801 allele; caution if renal impairment; caution if renal impairment risk; caution if hepatic impairment - CORRECT ANSWER>>Allopurinol Prescribing Consideration -Caution if CrCl 15-29; caution if severe hepatic impairment; caution if cardiovascular disease -Patients should receive prophylactic NSAIDs or colchicine for up to 6 months after starting treatment. - CORRECT ANSWER>>Febuxostat Prescribing Consideration Renal and hepatic impairment (gout prophylaxis use); caution in elderly or debilitated patients; caution if renal impairment; caution if hepatic impairment; caution if biliary obstruction - CORRECT ANSWER>>Colchicine Prescribing Consideration Rash, diarrhea, nausea, gout exacerbation, pruritus, urticaria, somnolence, alkaline phosphatase elevated (ALP), ALT or AST elevated, and eosinophilia - CORRECT ANSWER>>Allopurinol AE LFTs elevated and gout exacerbation - CORRECT ANSWER>>Febuxostat AE Creatinine (Cr) at baseline; CBC if used long-term - CORRECT ANSWER>>Cochichine Monitoring Obtain BUN/Cr at baseline and periodically if there is current or chronic renal infection or disease, LFTs during early treatment if there is hepatic disease - CORRECT ANSWER>>Allopurinol Monitoring Acquire LFTs at baseline - CORRECT ANSWER>>Febuxostat Monitoring Parameters may inhibit hepatic drug-metabolizing enzymes; specific concern when taking warfarin - CORRECT ANSWER>>Allopurinol NSAID; relieve moderate to severe pain, tenderness, swelling, and stiffness caused by osteoarthritis (arthritis caused by a breakdown of the lining of the joints), rheumatoid arthritis (arthritis caused by swelling of the lining of the joints), and ankylosing spondylitis - CORRECT ANSWER>>Indomethacin The goal is to prevent and treat osteoporosis by improving bone density and preventing bone loss. - CORRECT ANSWER>>Bisphosphonates (Aledronate/Ibandronate) prevention and treatment of osteoporosis in postmenopausal women, in whom benefits derive from decreasing bone resorption by osteoclasts. suppresses resorption of bone by decreasing both the number and activity of osteoclasts. - CORRECT ANSWER>>Aledronate (Fosamax) MOA Esophagitis, sometimes resulting in ulceration, is the most serious adverse effect; atypical fractures of the femur, - CORRECT ANSWER>>Aledronate (Fosamax) AE After 5 years of use, evaluate annually the need for continued treatment. - CORRECT ANSWER>>Bisphosphonates Monitoring Prevention and treatment of postmenopausal osteoporosis; Benefits derive from inhibiting osteoclast-mediated resorption of bone - CORRECT ANSWER>>Ibandronate (Boniva) minimize the risk for esophagitis, instruct patients to swallow the tablet whole with a full glass of water while sitting or standing upright. Explain that it is important to remain upright for at least 30 min-60mins - CORRECT ANSWER>>Bisphosphonates Patient Education can cause severe esophagitis, sometimes resulting in ulceration. Avoid these drugs in patients with esophageal disorders that could impede swallowing and in patients who are unable to sit or stand for 30 min - CORRECT ANSWER>>Bisphosphonates AE symmetric joint stiffness and pain - CORRECT ANSWER>>Rheumatoid arthritis (1) Relieve RA symptoms (pain, inflammation, and stiffness), (2) maintain joint function and range of motion, (3) minimize systemic involvement, and (4) delay disease progression. - CORRECT ANSWER>>DMARDS (Methotrexate/Leflunomide)