receptors Delta MU low affinity MU Antagonist effects MU high affinity 50x > MSO4 Kappa Kappa moderate affinity Slow dissociation = action Sigma minimal affinity Resistant to Antagonism of Naloxone (Narcan) effects Agonist effects Antagonized by Agonist effects 20 x > than Equal potency Analgesia to MSO4 Very Potent Naloxone (Narcan) Pentazocine Analgesia Onset and Duration 0.3mg IM = 10mg Morphine Antagonist effects Withdrawal Antagonist effects 10 - 30 times Similar to Morphine (MSO4) greater Nubain 10mg IM uses Treatment of: Good for: 10-20mg IV reverses the respiratory Good for: Chronic Pain Acute Pain rather than Chronic depression of Fentanyl postop Moderate to Severe Pain Relieves Moderate Pain But maintains Analgesia dose Dose 10-30mg IV or 50mg Available in parenteral form > 30mg “CEILING EFFECT” d/t 50mg = 60mg Codeine 2 -3 mg IM = 10mg Morphine antagonist activity Extensive 1st-Pass Hepatic Hepatic metabolism to inactive Metabolized in the Liver Onset = 30 min Metabolism metabolites Morphine-like Drugs Inactive Duration 8-10 hours Metabolized to an inactive metabolite Excreted in Urine E ½ x = 3 - 6 hours Highly Soluble and Excreted in E ½ x = 2.5 - 3.5 hours E ½ x = 2- 3 hours Rapidly &Completely absorbed after IM metabolism side effects Sedation Sedation Abuse potential LOW Drowsiness Diaphoresis Diaphoresis Incidences of Pulmonary Edema Dizziness Nausea Nausea/Vomiting Dysphoria Respiratory Depression Respiratory Depression Crosses the Placenta Fetal Attenuates Opioid Agonist Activity** Depression Does NOT cause Catecholamines HR HR BP BP PAP PAP LVEDP Opioid Antagonists structure Minor changes in structure of Opioid Agonist changes the Drug to an ANTAGONIST Substitute an Alkyl Group for a Methyl Group receptor Displaces Opioid agonist from the MU receptors Pure Antagonist DOES NOT activate the receptor Antagonism Naloxone (Narcan) receptor ANTAGONIZES Mu Receptors ***
receptors Delta Kappa MU low affinity Kappa moderate affinity Sigma minimal affinity MU Antagonist effects MU high affinity 50x > MSO4 Slow dissociation = action Resistant to Antagonism of Naloxone (Narcan) effects Agonist effects Antagonized by Naloxone (Narcan) Antagonist effects Withdrawal Agonist effects 20 x > than Pentazocine Antagonist effects 10 - 30 times greater Equal potency Analgesia to MSO4 Analgesia Onset and Duration Similar to Morphine (MSO4) Nubain 10mg IM Very Potent 0.3mg IM = 10mg Morphine uses Treatment of: Chronic Pain Relieves Moderate Pain Good for: Acute Pain rather than Chronic 10-20mg IV reverses the respiratory depression of Fentanyl postop But maintains Analgesia Good for: Moderate to Severe Pain dose Dose 10-30mg IV or 50mg 50mg = 60mg Codeine Available in parenteral form 2 -3 mg IM = 10mg Morphine > 30mg “CEILING EFFECT” d/t antagonist activity and metabolism Extensive 1st-Pass Hepatic Metabolism Metabolized to an inactive metabolite Excreted in E ½ x = 2- 3 hours Hepatic metabolism to inactive metabolites Excreted in Urine E ½ x = 2.5 - 3.5 hours Rapidly &Completely absorbed after IM Metabolized in the Liver Morphine-like Drugs Inactive E ½ x = 3 - 6 hours Onset = 30 min Duration 8-10 hours Highly Soluble side effects Sedation Diaphoresis Dizziness Dysphoria Crosses the Placenta Fetal Depression Catecholamines HR BP PAP LVEDP Sedation Diaphoresis Nausea Respiratory Depression Attenuates Opioid Agonist Activity** Abuse potential LOW Does NOT cause HR BP PAP Drowsiness Incidences of Pulmonary Edema Nausea/Vomiting Respiratory Depression Opioid Antagonists structure Minor changes in structure of Opioid Agonist changes the Drug to an ANTAGONIST Substitute an Alkyl Group for a Methyl Group receptor Displaces Opioid agonist from the MU receptors Pure Antagonist DOES NOT activate the receptor Antagonism Naloxone (Narcan) receptor ANTAGONIZES Mu Receptors ***
new%20opioid%20charts.docx