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Pharmacology, An Issue of Anesthesiology Clinics E-Book

Pharmacology, An Issue of Anesthesiology Clinics E-Book

Alan D. Kaye

(2017)

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Abstract

This issue of Anesthesiology Clinics focuses on Pharmacology. Editor Alan Kaye has assembled an expert team of authors on topics such as: Ketorolac, Oxymorphone and Tapentadol; Anticoagulation and Neuraxial/Peripheral Anesthesia; Pharmacologic Update on Antiemetics: Total parenteral nutrition/enteral nutrition in the ICU, Evolving Concepts; Reversal of Anticoagulants and Anesthesia Considerations; Non-opioids  Intravenous or Oral Analgesics for Perioperative  Pain Management, Update; Uterotonic Medications and Anesthesia Considerations: oxytocin, misoprostol, methylergonovine, carboprost; Pulmonary Vascular Mediating Drugs, Evolving Concepts; Alpha 2 Modulators and Anesthesia Considerations; Pharmacologic Considerations of Anesthetic Agents in the Obese Patient; Pharmacologic Considerations of Anesthetic Agents in the Geriatric Patient; Pharmacologic Considerations of Anesthetic Agents in the Pediatric Patient; Anesthesia CV Drug Update; Pharmacogenomics: Anesthesia; Pharmacogenomics: Pain; Novel anticoagulants; Novel anesthetic agents; Novel opioids; Pharmacology of Newer Local anesthetics; Pharmacology of Nonsteroidal Antiinflammatory and Steroid Medications.  Implications for Anesthesia or Unique Associated Risks; Pharmacology of Octreotide.  Implications for Anesthesia and Associated Risks.

Table of Contents

Section Title Page Action Price
Front Cover Cover
Pharmacology\r i
Copyright\r ii
Contributors iii
CONSULTING EDITOR iii
EDITOR iii
AUTHORS iii
Contents ix
Foreword: Pharmacology ix
Preface: The Future of Pharmacology in Anesthesia Practice ix
Ketorolac, Oxymorphone, Tapentadol, and Tramadol: A Comprehensive Review\r ix
Anticoagulation and Neuraxial/Peripheral Anesthesia ix
Pharmacology of Antiemetics: Update and Current Considerations in Anesthesia Practice ix
Total Parenteral and Enteral Nutrition in the ICU: Evolving Concepts x
Anticoagulant Reversal and Anesthetic Considerations x
An Update on Nonopioids: Intravenous or Oral Analgesics for Perioperative Pain Management x
Uterotonic Medications: Oxytocin, Methylergonovine, Carboprost, Misoprostol xi
Pulmonary Vasodilators and Anesthesia Considerations xi
Alpha-2 Agonists xi
Perioperative Pharmacologic Considerations in Obesity xi
Pharmacologic Considerations of Anesthetic Agents in Geriatric Patients xii
Pharmacologic Considerations of Anesthetic Agents in Pediatric Patients: A Comprehensive Review xii
Cardiovascular Pharmacology: An Update and Anesthesia Considerations xii
Pharmacogenomics in Anesthesia xii
Pharmacogenomics in Pain Management xiii
Novel Anticoagulant Agents in the Perioperative Setting xiii
New Hypnotic Drug Development and Pharmacologic Considerations for Clinical Anesthesia xiii
Essential Elements of Multimodal Analgesia in Enhanced Recovery After Surgery (ERAS) Guidelines xiii
Pharmacologic Properties of Novel Local Anesthetic Agents in Anesthesia Practice xiv
Pharmacology of Acetaminophen, Nonsteroidal Antiinflammatory Drugs, and Steroid Medications: Implications for Anesthesia or ... xiv
Pharmacology of Octreotide: Clinical Implications for Anesthesiologists and Associated Risks xiv
Revisiting Oxycodone Analgesia: A Review and Hypothesis xv
An Analysis of New Approaches and Drug Formulations for Treatment of Chronic Low Back Pain xv
ANESTHESIOLOGY CLINICS\r xvi
FORTHCOMING ISSUES xvi
September 2017 xvi
December 2017 xvi
March 2018 xvi
RECENT ISSUES xvi
March 2017 xvi
December 2016 xvi
September 2016 xvi
Pharmacology xvii
The Future of Pharmacology in Anesthesia Practice xix
Ketorolac, Oxymorphone, Tapentadol, and Tramadol e1
Key points e1
INTRODUCTION e1
KETOROLAC e2
Background e2
Pharmacology e2
Adverse Events e2
Drug Interactions e3
Routes of Administration e3
Intramuscular/Intravenous e3
Oral e4
Intranasal e4
Subcutaneous e4
OXYMORPHONE e4
Background e4
Pharmacology e4
Oxymorphone Immediate Release e5
Oxymorphone Extended Release e5
Postoperative Pain e6
Multimodal Analgesia e6
Contraindications/Adverse Events e6
Adverse effects e6
Kidney disease e6
Liver disease e6
TAPENTADOL e7
Background e7
Pharmacology e7
Indications/Benefits e8
Contraindications/Adverse Events e9
TRAMADOL e9
Background e9
Mechanism of Action e10
Pharmacokinetics e10
Dosage e11
Adult e11
Pediatric e11
Adverse Effects e11
Serotonin syndrome e12
Seizures e12
Respiratory depression e12
Hyperalgesia e13
Psychiatric e13
Hypersensitivity e13
Gastrointestinal e13
Nervous system e13
Dermatologic e13
Genitourinary e14
Cardiovascular e14
Other e14
Metabolic e14
Endocrine e14
Hematologic e14
Hepatic e14
Ocular e14
Renal e14
Musculoskeletal e14
Contraindications e15
Overdose e15
Physical Dependence and Withdrawal e15
REFERENCES e15
Anticoagulation and Neuraxial/Peripheral Anesthesia e21
Key points e21
Introduction e21
Potential advantages of regional anesthetic techniques e22
Antiplatelet agents e23
The American Society of Regional Anesthesia recommendations and morbidities e23
Mechanisms e24
Monitoring e24
Reversal e25
Heparin e25
Pharmacokinetics e25
Monitoring e26
Adverse effects e26
Reversal e26
American Society of Regional Anesthesia recommendations e26
Low-Molecular-Weight Heparin e27
Monitoring and dosing e27
Reversal e27
American Society of Regional Anesthesia recommendations e27
Vitamin K Antagonists e28
Dosing and precautions e28
Monitoring e28
Reversal e28
American Society of Regional Anesthesia recommendations e29
Novel Anticoagulants (Direct Thrombin Inhibitors and Factor Xa Inhibitors) e29
Prevalence e29
Monitoring of novel anticoagulants e30
Reversal of novel anticoagulants e30
Direct Thrombin Inhibitors e30
Review of mechanism of anticoagulation, and comparisons with heparin e30
Pharmacokinetics e31
American Society of Regional Anesthesia recommendations and safety investigations e31
Direct Thrombin Inhibitor Reversal e32
Factor Xa Inhibitors e32
Review of mechanism of anticoagulation e32
American Society of Regional Anesthesia recommendations for injectable factor Xa inhibitors and safety investigations e32
American Society of Regional Anesthesia recommendations for oral factor Xa inhibitors and safety investigations e32
Factor Xa inhibitor reversal e33
Summary e33
References e36
Pharmacology of Antiemetics e41
Key points e41
Introduction e42
Socioeconomic factors of postoperative nausea and vomiting e42
Risk factors for nausea and vomiting—factors that contribute e42
Patient factors e43
Surgery and anesthesia factors e43
Scoring e43
Definitions, physiology, and anatomy of nausea and vomiting e44
Pharmacologic prophylaxis e44
Serotonin Receptor Antagonists e44
Ondansetron e45
Palonosetron e45
Dopamine antagonists e46
Droperidol e46
Metoclopramide e46
Novel agents e46
Aprepitant (Neurokinin-1) e46
Corticosteroids e47
Dexamethasone e47
Anticholinergics e48
Dimenhydrinate e48
Scopolamine e48
H1 antagonists e48
Promethazine e48
Diclectin e49
Combination therapies for postoperative nausea and vomiting e50
Alternative therapies for the prevention of postoperative nausea and vomiting e50
Isopropyl Alcohol Inhalation e50
Recommended strategies for postoperative nausea and vomiting prophylaxis e51
Discussion e52
References e52
Total Parenteral and Enteral Nutrition in the ICU 181
Key points 181
INTRODUCTION 181
INITIATION AND ADVANCEMENT OF NUTRITIONAL SUPPORT 182
Benefits of Early Enteral Nutrition 182
Estimating Energy Needs 182
Initiation and Maintenance 183
When to Use Parenteral Nutrition 184
ADJUNCTIVE THERAPY 184
Fiber 184
Probiotics 184
Antioxidants and Trace Minerals 185
Glutamine, Arginine, Eicosapentaenoic Acid, Docosahexaenoic Acid, and Nucleic Acid 185
DRUG INTERACTIONS 185
SIDE EFFECTS 186
Side Effects of Enteral Nutrition 187
Side Effects of Parenteral Nutrition 187
Comparison of Enteral Nutrition and Parenteral Nutrition Side Effects 188
SUMMARY 188
REFERENCES 188
Anticoagulant Reversal and Anesthetic Considerations 191
Key points 191
INTRODUCTION 191
AVAILABLE AGENTS 192
HEPARINS 192
Indications 192
Kinetics 192
Reversal 194
VITAMIN K ANTAGONISTS 195
Indications 195
Kinetics 196
Interactions 196
Adverse Effects 196
Reversal 196
DIRECT THROMBIN INHIBITORS 197
Monitoring 198
Kinetics 198
Reversal 198
DIRECT FACTOR XA INHIBITORS 199
Indications 199
Kinetics 199
Monitoring 200
Reversal 200
Prothrombin Complex Concentrates 200
Andexanet Alfa 200
Kinetics 201
Availability 201
Cirapirantag 201
APPLICATIONS FOR THE ANESTHESIOLOGIST 201
REFERENCES 202
An Update on Nonopioids e55
Key points e55
General introduction e55
Acetaminophen e56
Nonsteroidal anti-inflammatory drugs e57
N-methyl-d-aspartate receptor antagonists e58
Ketamine e58
Memantine e59
Amantadine e60
Dextromethorphan e60
Magnesium e60
Gabapentin (Neurontin) oral capsule, tablet, solution e61
Gabapentin (Gralise) tablet oral once daily e61
Gabapentin enacarbil (Horizant) extended-release oral tablet e62
Perioperative pain management of gabapentin e62
Pregabalin (Lyrica) e62
Perioperative pain management of pregabalin e63
Steroids e64
Glucocorticoids e64
Dexamethasone e64
Alpha-2 agonists e64
Clonidine e64
Dexmedetomidine e65
Consequences of undermanaged acute pain e66
Summary e66
References e67
Uterotonic Medications 207
Key points 207
OXYTOCIN 207
Introduction 207
Structure/Activity 208
Pharmacokinetics 208
Clinical Role 209
Routes and Dosages 209
Side Effects and Contraindications 210
Summary 210
METHYLERGONOVINE 210
Introduction 210
Structure/Activity 210
Pharmacokinetics 211
Clinical Role 211
Route and Dosage 211
Side Effects and Contraindications 212
Summary and Discussion 212
CARBOPROST 212
Introduction 212
Structure/Activity 212
Pharmacokinetics 213
Clinical Role 213
Routes and Dosage 213
Side Effects and Contraindications 213
Summary and Discussion 214
MISOPROSTOL 214
Introduction 214
Structure/Activity 214
Pharmacokinetics 214
Clinical Role 215
Routes and Dosage 215
Side Effects and Contraindications 216
Summary and Discussion 216
SUMMARY 216
REFERENCES 216
Pulmonary Vasodilators and Anesthesia Considerations 221
Key points 221
INTRODUCTION 221
STRUCTURE OF PULMONARY VESSELS AND THE ROLE OF ENDOTHELIUM AND NEURAL MECHANISMS 222
PATHOPHYSIOLOGY 224
CRITERIA AND DIAGNOSIS OF PULMONARY HYPERTENSION 225
VASODILATORS 226
TYPES OF VASODILATORS 227
Calcium Channel Blockers 227
Inhaled Nitric Oxide 227
Prostacyclin 227
Endothelin Blockers 227
Diuretics 228
Oxygen 228
Exercise 228
Pregnancy 228
ANESTHETIC CONSIDERATIONS IN PULMONARY HYPERTENSION 229
Preoperative 229
Perioperative 229
Postoperative 230
SUMMARY 230
REFERENCES 230
Alpha-2 Agonists 233
Key points 233
CLONIDINE 233
Introduction 233
Mechanism of Action 234
Pharmacokinetics and Pharmacodynamics 235
Anesthetic Considerations 235
Central nervous system 235
Cardiovascular system 235
Respiratory system 235
Renovascular system 235
Endocrine 235
Anesthetic Applications 236
Sedation 236
Anesthesia and analgesia adjuvant 236
Topical applications 236
Premedication 236
Adverse Effects 236
Contraindications 237
Summary 237
DEXMEDETOMIDINE 237
Introduction 237
Mechanism of Action 238
Pharmacokinetics and Pharmacodynamics 238
Anesthetic Considerations 239
Anesthetic Applications 239
Sedation 239
Anxiolysis and premedication 239
Procedural sedation and monitored anesthesia care 240
Pediatric sedation 240
Adjuvant to general anesthesia 240
Intraoperative and postoperative analgesia 241
Locoregional techniques 241
Postoperative shivering 241
Emergence delirium/agitation 241
Adverse Effects 241
Airway obstruction 241
Bradycardia and hypotension 242
Contraindications 242
Summary 242
REFERENCES 242
Perioperative Pharmacologic Considerations in Obesity 247
Key points 247
INTRODUCTION 247
EPIDEMIOLOGY 248
DEFINITIONS 248
PHYSIOLOGIC CHANGES IN OBESITY 250
GENERAL DOSING STRATEGIES 250
ANESTHETIC INDUCTION AGENTS 251
NEUROMUSCULAR BLOCKING AGENTS 252
REVERSAL AGENTS 253
INHALED ANESTHETIC AGENTS 253
ANALGESICS 254
SUMMARY 254
REFERENCES 255
Pharmacologic Considerations of Anesthetic Agents in Pediatric Patients e73
Key points e73
Introduction and pediatric considerations e73
Pharmacokinetic considerations in pediatric patients e75
Individual drugs e76
Inhaled Agents e76
Intravenous Agents e77
Total Intravenous Anesthesia Induction Agents e79
Benzodiazepines and Opioids e79
Sedative-Hypnotics: Benzodiazepines and Other Agents e80
Special Pharmacologic Considerations for Opioids e82
Local anesthetics e85
Postoperative pain control strategies in pediatric patients e86
Neuromuscular blockers e87
Physiology, Mechanism of Action, and Pharmacology e87
Neuromuscular drug blocker classification e88
Individual drugs based on duration of action e88
Nondepolarizing (competitive) drugs e89
Long-Acting Neuromuscular Blockers e89
Intermediate-acting neuromuscular blocking drugs e89
Short-acting nondepolarizing neuromuscular blocking drugs e90
Indications for use of neuromuscular blocking drugs e90
Potential risks/complications e90
Anesthetic Agents to Use with Caution in Pediatric Patients e90
References e91
Cardiovascular Pharmacology 273
Key points 273
INTRODUCTION 273
ANATOMY OF CARDIAC MUSCLE FIBER AND SARCOMERES 274
EXCITATION-CONTRACTION COUPLING: THE CARDIAC ACTION POTENTIAL 276
DRUGS FOR THE MANAGEMENT OF HEMODYNAMIC INSTABILITY 277
VASOPRESSORS 278
Vasopressin 278
Methylene Blue 278
Intravenous Antihypertensive Drugs 278
Nicardipine 279
Clevidipine 280
Inotropes and Inodilators 280
Omecamtiv Mecarbil 281
Sarcoplasmic Reticulum Calcium Adenosine Triphosphatase Gene Therapy 281
Levosimendan: A Calcium Sensitizer 281
Inhaled Agents 282
Nitric Oxide 282
Epoprostenol 283
REFERENCES 283
Pharmacogenomics in Anesthesia 285
Key points 285
INTRODUCTION 285
NEUROMUSCULAR BLOCKING AGENTS 286
OPIOIDS 287
Metabolism 287
Receptors 288
Transporters 288
LOCAL ANESTHETICS 288
INHALATION ANESTHETICS 288
MALIGNANT HYPERTHERMIA 289
BENZODIAZEPINES 289
POSTOPERATIVE NAUSEA AND VOMITING 290
CARDIOVASCULAR GENOMICS 290
Coagulation Variability 290
Atrial Fibrillation 291
SUMMARY 292
REFERENCES 292
Pharmacogenomics in Pain Management 295
Key points 295
INTRODUCTION 295
METABOLISM VARIABILITY 296
WEAK OPIOIDS 296
Codeine 296
Hydrocodone 297
Tramadol 297
STRONG OPIOIDS 297
Morphine 297
Diamorphine 298
Fentanyl 298
Buprenorphine 298
Oxycodone and Oxymorphone 299
OPIOID RECEPTORS 299
Mu-Opioid Receptor 299
Kappa-Opioid Receptor 300
Delta-Opioid Receptor 300
CATECHOL-O-METHYLTRANSFERASE 300
KETAMINE 301
NONSTEROIDAL ANTI-INFLAMMATORY DRUGS 301
SUMMARY 302
REFERENCES 302
Novel Anticoagulant Agents in the Perioperative Setting 305
Key points 305
INTRODUCTION 305
DIRECT THROMBIN INHIBITORS 306
Dabigatran Etexilate 306
FACTOR XA INHIBITORS 306
Rivaroxaban 306
Apixaban 307
Edoxaban 307
Betrixaban 308
NOVEL ORAL ANTICOAGULANTS AND REGIONAL ANESTHESIA 308
ANTIPLATELET AGENTS 309
Clopidogrel 310
Prasugrel 310
Ticagrelor 310
ANTIPLATELET AGENTS AND REGIONAL ANESTHESIA 310
SUMMARY 311
REFERENCES 311
New Hypnotic Drug Development and Pharmacologic Considerations for Clinical Anesthesia e95
Key points e95
Introduction e95
Novel agents e96
Phenols e96
PF0713 e96
Fospropofol e97
Imidazoles e97
Methoxycarbonyl etomidate and cyclopropyl methoxycarbonyl etomidate e97
Carboetomidate e100
Methoxycarbonyl carboetomidate e101
Benzodiazepines and Benzodiazepine-Like Agents e101
Remimazolam (CNS 7056) e101
JM-1232 e101
Phencyclidines e104
Norketamine ester analogues e104
Alternative ketamine derivatives e104
Halogenated Ethers e105
Emulsified isoflurane e105
Emulsified sevoflurane e105
Barbiturates e106
Ultra-short-acting barbiturates e106
Nucleosides e106
N3-phenacyluridine e106
Phenylacetates e107
AZD3043 e107
Pharmacoeconomics and future directions e107
Summary e108
References e109
Essential Elements of Multimodal Analgesia in Enhanced Recovery After Surgery (ERAS) Guidelines e115
Key points e115
Introduction e116
Components of multimodal, opiate-sparing analgesia e117
Systemic Analgesia e117
Nonsteroidal anti-inflammatory drugs e122
Acetaminophen e122
Opiates e122
N-Methyl d-Aspartate receptor antagonists e123
Gabapentin and pregabalin e123
Local anesthetics e123
Nonsystemic Anesthesia or Analgesia e124
Thoracic Epidural Anesthesia or Analgesia and Spinal Anesthesia e124
Transversus Abdominis Plane Blocks and Continuous Wound Infiltration e124
Future directions for Enhanced Recovery After Surgery Society Guidelines and bundled care in delivering multimodal analgesia e124
Procedure-specific multimodal analgesia e125
Emergency surgery e125
Specific patient groups e125
Cancer recurrence to measure impact of enhanced recovery or multimodal strategy e125
Chronic postsurgical pain prevention with adequate acute pain management? e132
Audit, evaluation of outcomes, and long-term follow-up of patients on Enhanced Recovery After Surgery Society Guideline–com ... e132
Summary e133
References e133
Pharmacologic Properties of Novel Local Anesthetic Agents in Anesthesia Practice 315
Key points 315
INTRODUCTION 315
NATURALLY OCCURRING SITE-1 SELECTIVE SODIUM CHANNEL BLOCKERS 316
NOVEL LOCAL ANESTHETIC DELIVERY SYSTEMS 317
NOVEL ADJUVANTS OF LOCAL ANESTHETICS 319
SUMMARY 321
REFERENCES 322
Pharmacology of Acetaminophen, Nonsteroidal Antiinflammatory Drugs, and Steroid Medications: Implications for Anesthesia or ... e145
Key points e145
Acetaminophen e146
Nonsteroidal antiinflammatory drugs e149
Corticosteroids e153
Summary e157
References e158
Pharmacology of Octreotide 327
Key points 327
BACKGROUND 327
CLINICAL PHARMACOLOGY 327
PHARMACOKINETICS 328
FORMS 329
Octreotide Acetate 329
Octreotide Acetate Long-Acting Release 329
DOSAGE AND ADMINISTRATION 329
DOSAGE FOR SPECIFIC CONDITIONS 329
Acromegaly 329
Carcinoid Tumors 330
Vasoactive Intestinal Peptide Tumors 330
Carcinoid Crisis, Prevention 330
Esophageal Varices Bleeding 330
Malignant Bowel Obstruction 330
ROLE OF OCTREOTIDE IN MEDICINE 330
Acromegaly 330
Carcinoid Tumors 331
Vasoactive Intestinal Peptide Tumors 331
Pain Control 331
Esophageal Varices Bleeding 331
Malignant Bowel Obstruction 331
Refractory and Chylous Ascites 331
Off-Label Uses 331
NEW STUDIES AND NEW ROLES FOR OCTREOTIDE 332
Transfusion Requirements During Orthotopic Liver Transplantation 332
Postoperative Chylothorax 332
CONTRAINDICATIONS 332
ANESTHETIC CONSIDERATIONS 332
Preoperative Evaluation and Optimization 333
Anesthetic Techniques 333
Postoperative Care 334
OCTREOTIDE USE DURING ANESTHESIA 334
CARCINOID CRISIS: IS IT PREVENTABLE? 336
DRUG INTERACTIONS 336
CAUTIONS 336
SIDE EFFECTS 337
OCTREOTIDE AND PREGNANCY 337
OCTREOTIDE AND BREAST FEEDING 337
OCTREOTIDE AND PEDIATRIC USE 337
OCTREOTIDE AND GERIATRIC USE 337
SUMMARY 338
REFERENCES 338
Revisiting Oxycodone Analgesia e163
Key points e163
Introduction e163
Basic pharmacokinetics e164
Pharmacogenetic variation or metabolite contribution e164
Pharmacodynamic dilemma e165
The role of peripheral opioid receptors in peripheral oxycodone analgesia e166
Oxycodone and its active metabolites binding sites e168
References e170
An Analysis of New Approaches and Drug Formulations for Treatment of Chronic Low Back Pain 341
Key points 341
INTRODUCTION 341
Anatomy and Pathophysiology 342
CURRENT TREATMENTS 342
Chemonucleolysis 343
Collagenase 343
Chondroitinase ABC 343
Matrix Metalloproteinases 344
Ethanol 345
Platelet-Rich Plasma Injections 345
Artemin 346
Tanezumab 346
Stem Cell Therapy 347
SUMMARY 347
REFERENCES 347
Index 351