Drugs for the Treatment of Pain Dr. Steven I. Dworkin

Narcotic Analgesics Used to treat mild to severe pain Opiate Activity and Effects related to occupation of three opiate receptor subtypes. Mu morphine-like supraspinal analgesia, respiratory and physical depression, miosis, reduced gastrointestinal motility. Delta Dysphoria, psychotomimetic effects. Kappa Sedation and miosis Dr. Steven I. Dworkin

Narcotic Analgesics Actions related to receptor binding or occupancy Agonists - binds to receptor produces an effect Partial agonists – binds to receptor produces limited response Antagonist – binds to receptor blocks effect of agonist * partial agonist can antagonize the effects of a full agonist by binding to the site. Dr. Steven I. Dworkin

Dr. Steven I. Dworkin

Dr. Steven I. Dworkin

Dr. Steven I. Dworkin

Uses of Narcotic Analgesics Manage moderate to severe acute and chronic pain Analgesic effects depend on several factors Drug, dose, route of administration, type of pain, the patient. Lessen anxiety and sedate a patient before surgery Support anesthesia Obstetrical analgesia Treat severe diarrhea To relieve severe, persistent cough Manage opioid dependence Dr. Steven I. Dworkin

Adverse Reactions to Narcotic Analgesics Most common Light-headedness, dizziness, sedation, constipation, anorexia, nausea, vomiting, sweating. Other adverse effects include: CNS - euphoria, weaknesses, pinpoint pupils, insomnia, agitation, tremor, impairment of activity. Gastrointestinal – dry mouth, biliary tract spasms. Cardiovascular – flushing, tachycardia, bradycardia, and palpitations Genitourinary – spasm of ureters and bladder sphincter, urinary retention or hesitancy. Allergic – pruritus, rash Narcotic drug dependence Dr. Steven I. Dworkin

Dr. Steven I. Dworkin