Opioids in Medicine

The book centers on the treatment of pain using the appropriate opioid and a suitable co-medication whenever necessary. While many physicians or health care providers either subscribe or advocate analgesics in response to a painful situation, their basic knowledge when and how to apply them frequently is scarce. And often there is a lack of sufficient knowledge on their potential side-effects, their mode of action, 2+ their possible interactions with other agents such as ß-blockers, Ca -antagonists, ACE inhibitors and/or benzodiazepines. In addition, not all analgesics are equivalent or equally proficient at alleviating certain painful ailments. Although there have been many of articles and books written on the subject of effective pain treatment, very few have centered on the rational use of opioids. In fact opiophobia is still around with some caregivers who consider an opioid not to be the first-line drug in severe pain. On the contrary, the myth is still around that an opioid is potentially dangerous even when used in serious painful situations, and although the WHO has stated that opioids are elementary in therapeutic strategy taking into account that they are used by mouth, by the ladder, at fixed time intervals and advocating a time consistent release formulation, they are not available in every country.

Stressing key concepts and essential information on pain and its treatment Providing one-step review of the important concepts in the mode of action of opioids Summary of symptoms and modalities available for treatment of major pain syndromes Written for everyone who needs detailed information on practical use on opioid pharmacology Broad review for everyone preparing for the board examination

Inhalt

Introduction. Part I Rational for the Use of Opioids in Nociceptive Transmission. The Nociceptive System, an Elementary Part of the Body's Protective Scheme. Acute Pain Sequence of Changes in the Body. Differences in Pain Quality. Anatomy of Pain and Analgesia. Significance of C-Fibers in Pain Transmission. Significance of Aß-Fibers in Pain Modulation. Transmission of Pain with Different Qualities. Substance P, a Mediator of Pain and a Member of the Tachykinine Family. Supraspinal Processing of Pain. Transduction of Nociception Via the Spinothalamic Tracts. The Descending Antinociceptive System. Neurophysiology of Pain Type of Receptor Sites Involved in Therapy. Transduction of Nociceptive Afferences Via Ascending Pathways. Different Therapeutic Approaches in Pain Therapy. Significance of Bradykinins in Inflammatory Pain. Cox Inhibitors in the Alleviation of Pain. The Opioid Receptor System Main Target in Pain Therapy. Inhibitory and Excitatory Effects of Nociception at the Spinal Cord Level. Neurohormones In Transmission of Nociception. Melanocortins. Cholecystokinins. Calcitonin-Gene-Related Neuropeptide. Galanin. Nitric Monoxide, Mediator for Chronic Pain. The Cannabinoid System. Ion Channel Modulators Resulting in Facilitation/Inhibition of Nociception. The P2X and P2Y Receptor System. The Vanilloid Receptor System. Voltage-Gated Sodium Channels as Ion Conduit Modulators. Non Voltage-Gated Potassium Channels. Ionotropic Glutamate Receptor Ion Channel Modulators. Excitatory Glutamate Receptor; Mediator of Pronociceptive Effects. The Nicotinic/Acetylcholine (NAchR) Receptors. Nerve Growth Factor (NGF) in Mediating Hyperalgesia. Significance of the Immune System and Microglia in Chronic Pain. Reflectory, Segmental Mediation of Pain Afferents. Sequence of Resulting in Neuropathic Pain. Causes of Potentiation and Transition From Acute to Chronic Pain. Neurophysiological Changes Taking Effect During Evolution of Pain. Supraspinal Engrams Relevant inTransition from Acute to Chronic Pain. Preventing Transition from Acute to Chronic Pain Use of Analgesics with Different pharmacology. Rationale for the Use of Opioids. Reasons for Insufficient Opioid use The 11 Myths in Opioid Therapy. Alternative Therapeutic Targets in Pain Therapy. Proton Channels as Therapeutic Targets in Pain Therapy. Adjuvant Analgesics in Pain Therapy. Difference in Receptor Activation/Inhibition as Drug Targets. Mechanism of Action of Tricyclic Antidepressants. Pharmacologically Resistant Psychologically Conditioned Pain. The Malingering Patient with Compensatory Pain Behavior. References. Part II Mechanism of Action of Opioids and Clinical Effects. Conversion of Morphine to Heroin (Diacetylmorphine). Major Classes of Opioid Analgesics in Clinical Practice. Mode of Action of Opiates/Opioids. Overview of the Different Opioid Receptors and their Subtypes. Agonists, Antagonists, their Potency and Mode of Action. Relative Potency and Equianalgesic Doses. Specific Binding Sites for Opioids in the CNS. Reasons for Difference in Potency of Opioids. Intracellular Signaling Following Opioid Binding. G-Protein Coupled Receptors and the Adenylate Cyclase Signaling System, Mediators of Opioid Action. Significance of the Heterotrimeric G-Proteins in Intracellular Transmission. Differences in Clinical Effects of Various Opioids. Opioid-Refractory Painful Conditions. Opioid-Related Side Effects. Opioid-Induced Respiratory Depression. Significance of the Different Opioid Receptors in the Mediation of Respiratory Depression. Vigilance, Leading Parameter in Opioid-Related Respiratory Depression. Reasons for Prolongation of Opioid-Related Respiratory Depression in Patients. Difference in Sedative-Hypnotic Effect of Opioids. Difference in the Hypnosedative and Analgesic Effect of Potent Opioids. Potential Epileptogenic Potency of Opioids. The Antitussive Action of Opioids (Blockade of Cough Reflex). Dependence Liability of Opioids Pharmacological Principles of Addiction. Neurobiological Changes with Addiction. Opioids Inducing Nausea and Emesis. Opioids and Muscular Rigidity. The Pupillary Effect of Opioids. Opioids and Gastrointestinal Inhibition (Constipation). Clinical Relevance of Opioid-Induced Constipation. Opioids and the Cardiovascular System. References. Part III Opioids, an Integrative Part in Perioperative Medicine. Intraoperative Use of Opioids for Anesthesia. Potentiation of Opioid-Based Anesthesia. Pharmacokinetics of Opioids: Significance for Clinical Use in Anesthesia. Significance of Pharmacokinetic Data for Practical Use. Advantages of "Maintenance Phase" Infusions Compared to Intermittent Bolus Dose. Use of Target Controlled Infusion (TCI) Systems in Anesthesia. "On-Top"-Dose of Either Alfentanil or Remifentanil in an Opioid-Based Anesthetic Regimen. Recommendations for the Use of Remifentanil. The Pharmacology of Sufentanil. Respiratory Depression After Sufentanil. The Hypnosedative Effect of Sufentanil. Sufentanil and Muscular Rigidity. Sufentanil in Selective Operations. Neurosurgery. Sufentanil in Open-Heart Surgery. Interaction of Sufentanil. Volatile Aspects. Muscle Relaxants. Barbiturates. Practical Considerations for the Use of Sufentanil. Examples for the Use of Sufentanil in Anesthesia. Opioids for Use in Postoperative Pain Management. Addiction Liability by Use of Opioids for Postoperative Pain. Time-Contingent Dosing of Opioids for Postoperative Pain. Selection of the Appropriate Agent in Postoperative Pain Management. Choice of Opioid Agents for Post-Operative Pain Treatment. Dosage of Opioid Analgesics in Post-Operative Pain Treatment. Implications of Agonist/Antagonists in Postoperative Pain Management. Patient-Controlled Analgesia (PCA) for Postoperative Pain Therapy. Opioids On-Demand, Without Use of a PCA System. New Techniques for Postoperative Pain Management. Selective Opioid Antagonists for Postoperative Reversal of Opioid Side Effects. PostoperativeOpioids Summary and Outlook. Neuraxial Administration of Opioids for Pain Therapy. Side Effects of Epidural Opioids. Lipophilic or Hydrophilic Opioids for Neuraxial Use. Extended-Release Epidural Morphine for Postoperative Pain. Combination of an Epidural Opioid with a Local Anesthetic. Continuou…