lesson 11

• Opioids


  Are regulated substances because they are at risk of addiction
• Opioids


  Are regulated substances because they are at risk of addiction
• Opioids


  Classified as Narcotics
• Opioids


  Classified as Narcotics
• Opioids


  S2 prescription is required for buying
• Opioids


  S2 prescription is required for buying
• Opioids


  Controlled substances by PDEA

  
• Outline


  • Opioid Analgesics and Antagonists
  • Non-Opioid Analgesics
  • Drugs for Arthritic Disorders

  
• Opioids


  Controlled substances by PDEA

  
• Outline


  • Opioid Analgesics and Antagonists
  • Non-Opioid Analgesics
  • Drugs for Arthritic Disorders

  
• Pain


  An unpleasant sensory and emotional experience that serves to alert an individual to actual or potential tissue damage

  
• Pain


  An unpleasant sensory and emotional experience that serves to alert an individual to actual or potential tissue damage

  
• Types of Pain


  • Nociceptive Pain (Detected through stimuli)
  • Neuropathic Pain (Damage neurons involved in pain transmission)

  
• Types of Pain


  • Nociceptive Pain (Detected through stimuli)
  • Neuropathic Pain (Damage neurons involved in pain transmission)

  
• Nociceptive Pain


  • Somatic Pain (Skin, muscles, joints)
  • Visceral Pain (Visceral organs)
• Nociceptive Pain


  • Somatic Pain (Skin, muscles, joints)
  • Visceral Pain (Visceral organs)
• Pain Pathway


  • Ascending Pain
  • Descending Inhibitory
• Endogenous Opioid Peptides


  • Enkephalins
  • B-endorphins
  • Dynorphins
• Opioid Receptors


  • μ (mu)
  • δ (delta)
  • κ (kappa)

  
• Pain Pathway


  • Ascending Pain
  • Descending Inhibitory
• Mechanism of Action


  Activation of opioid receptors leads to the inhibition of Adenylyl Cyclase thereby reducing concentration of cAMP

  
• Endogenous Opioid Peptides


  • Enkephalins
  • B-endorphins
  • Dynorphins
• Consequences of Mechanism of Action

  • Hyperpolarization (K+ efflux)
  • Blocked Ca++ influx
• Opioid Receptors


  • μ (mu)
  • δ (delta)
  • κ (kappa)

  
• Neuronal Effects


  • Inhibition of presynaptic NT release
  • Postsynaptic inhibition of membrane depolarization

  
• Mechanism of Action


  Activation of opioid receptors leads to the inhibition of Adenylyl Cyclase thereby reducing concentration of cAMP

  
• General Effect of Opioid Uses
• Consequences of Mechanism of Action

  • Hyperpolarization (K+ efflux)
  • Blocked Ca++ influx
• Effects of Opioids (per organ system)

  • CNS (Analgesia, Sedation, Euphoria, Miosis, Inhibition of cough reflex, Respiratory depression)
  • Cardiovascular (Vasodilation)
  • Gastrointestinal (Constipation, Increased biliary sphincter tone and pressure)
  • Genitourinary (Urinary retention)
  • Neuroendocrine (Anti Diuretic Hormones release stimulation, Prolactin release stimulation)
  • Others (LH release inhibition, Suppression of lymphocyte activity)

  
• Neuronal Effects


  • Inhibition of presynaptic NT release
  • Postsynaptic inhibition of membrane depolarization

  
• General Effect of Opioid Uses
• Tolerance


  Primarily a result of the down-regulation of the opioid receptors due to the chronic use of opioids

  
• Physical Dependence


  Physiological state in which a person's continued use of a drug is required for the individual's well-being
• Effects of Opioids (per organ system)

  • CNS (Analgesia, Sedation, Euphoria, Miosis, Inhibition of cough reflex, Respiratory depression)
  • Cardiovascular (Vasodilation)
  • Gastrointestinal (Constipation, Increased biliary sphincter tone and pressure)
  • Genitourinary (Urinary retention)
  • Neuroendocrine (Anti Diuretic Hormones release stimulation, Prolactin release stimulation)
  • Others (LH release inhibition, Suppression of lymphocyte activity)

  
• Withdrawal


  • Abrupt discontinuation upon chronic use
  • Antagonist precipitated withdrawal/sudden administration of opioid antagonist
  • Mother to baby transmission/vertical transmission/baby can manifest the withdrawal symptoms
• Adverse Effects


  • Respiratory depression (usually the cause of death)
  • Increased intracranial pressure (ICP)
  • Nausea & Vomiting (Due to CTZ Stimulation)
  • Hypersensitivity reactions
• Tolerance


  Primarily a result of the down-regulation of the opioid receptors due to the chronic use of opioids

  
• Physical Dependence


  Physiological state in which a person's continued use of a drug is required for the individual's well-being
• Classification Based on Intrinsic Activity

  • Strong Opioid Agonists
  • Moderate Opioid Agonists
  • Partial Opioid Agonists
  • Opioid Antagonists
  • Other Opioid Agonists

  
• Withdrawal


  • Abrupt discontinuation upon chronic use
  • Antagonist precipitated withdrawal/sudden administration of opioid antagonist
  • Mother to baby transmission/vertical transmission/baby can manifest the withdrawal symptoms