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VetMed Pharmacology9

Opioid Pharmacology

Amino-Terminal End of Opioid Peptides Tyr-Gly-Gly-Phe-(Met or Leu)
Classes of Endogenous Opioid Peptides endorphins enkephalins dynorphins nociceptin & orphanin (N/OFQ)
Anatomical Distribution of Endorphins arcuate nucleus nucleus tractus solitarius pituitary pancreatic islet cells
Anatomical Distribution of Enkephalins & Dynorphins distributed widely throughout CNS
Functions of Enkephalins & Dynorphins pain perception behaviour modulation autonomic nervous system regulation motor control neuroendocrine function
Anatomical Distribution of Nociceptin & Orphanin hippocampus cerebral cortex sensory sites
Functions of Nociceptin & Orphanin complex behavioural profile pain sensitivity
Telencephalon amygdaloid body hippocampus cingulum and cingulum gyrus septal region medial forebrain bundle - hypothalamus
Diencephalon thalamus hypothalamus
Mesencephalon intercrural nucleus reticular formation
Opioid Receptor / Opioid Dose Concept compounds that are relatively selective in their binding avidity for u, o, or k receptors at "standard" doses eventually "spill-over" and also bind to other opioid receptors at higher concentration
Location of Opioid u Receptors periaqueductal gray matter (pain) pontine reticular formation median raphe nucleus raphe magnus spinal cord '
Location of Opioid k and o Receptors periaqueductal gray matter (pain) pontine reticular formation median raphe (k) nucleus raphe magnus (k) gigantocellular reticular nucleus spinal cord (dorsal horn)
Location of Opioid N/OFQ Receptors para-aqueduct gray matter median raphe rostral ventral-medial medulla spinal cord (superficial dorsal horn)
Opioid u Receptor Antagonists CTOP naloxone nalorphine
Opioid o Receptor Antagonist natrindole
Opioid k Receptor Antagonist nor BNI
Opioid u&k Receptor Antagonists diprenorphine naltrexone
Opioid Receptor Activation MOA inhibit adenyl cyclase (stops ATP --> cAMP) suppresses voltage-gated Ca2+ currents activates receptor-operated K+ ion channels
Opioid Pathophysical Effects directly inhibit ascending transmission of nociceptive impulses from spinal cord dorsal horn reduce perceived pain, but also improve the ability to emotionally tolerate pain activate
Definition of Nociceptive Pain stimulation of nociceptive neuroreceptors and impulses transmitted over intact neural pathways
Definition of Neuropathic Pain damage or injury to neural structures often involving neural supersensitivity
Opioid Side Effects nausea vomiting drowsiness decreased mentation lower physical activity
Effect of Chronic Opioid Administration u and o receptor internalization (desensitization & tolerance)
Butorphanol Tartrate (Morphinan Congener) used for management of visceral pain frequently in combo with xylazine/detomidine
Clinical Applications of Opioids analgesia for severe pain cough suppression slow GI motility anesthetic/pre-anesthetic agent
Naloxone Effects antagonizes u-opioid receptors and GABA blocks beta-endorphin release elevates arterial blood pressure antagonizes oxymorphone-induced respiratory depression and analgesia reverses fentanyl effects therapeutic management of horse vices vascular shoc
Opioid Routes of Administration parenteral intraspinal (epidural/intrathecal) oral inhalation o
Centrally Acting Opioid Antitussive Agents codeine dextromethorphan levopropoxyphene - l-isomer of dextro nocapine
Centrally Acting Non-Opioid Antitussive Agents caramiphen carbetapentane diphenylhydramine pholcodine benzonatate
Basic MOA of Opioids influences the Limbic System, which influences involuntary responses
Three Basic Types of Opioid-Acting Substances synthetic opioids opiates endogenous peptides (endorphins, enkephalins, dyorphins, endomorphins)
What Kind of Pain is Managed More Effectively with Opioids? continuous dull pain
Precursor Polypeptide of Endorphins pre-pro-opiomelanocortin
Precursor Polypeptide of Enkephalins pre-pro-enkephalin
Precursor Polypeptide of Dyorphins pre-pro-dynorphin
Clinical Significance of Morphine Metabolites have a biological effect indistinguishable from morphine, but are twice as potent
Class of Analgesic Drug Used in Conjunction with Opioids to Reduce Necessary Dose of Opioid barbiturates
Created by: 26509889



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