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Analgesia (Pain (Symptoms associated with pain (insomnia, lack of energy,…

- - - - contain presynaptic opioid receptors, which
        a are predominant site of action of opioids
    - - 5HT and NA descending pathways have inhibitory
        modulative effect on the nociceptive neurons
    - - Cortex is also the place where, we
        perceive the sensation of pain as we know it
  - - - surgery
      - arthritis
        
        persistent
        inflammatory pain
      - cancer
      - trauma
    - - NSAIDS and COXIBS are drug, which
        inhibit COX1/2 activity, thereby reducing pain
      - Is an enzyme mediating, Prostaglandin release.
        Prostaglandins mediate nociceptive signalling
    - - Is a pain mediator
      - Triptans work by modulating the activity of 5HT,
        thereby controlling pain in the periphery
        
        Only used for migranes
    - - blocked by LA like Lignocaine
    - - another pain mediator
      - cannot be targeted for therapeutic use,
        as it is too wide-spread across the organism and too
        important for the functioning of the whole organism
  - - - diabetes
      - post herpetic neuralgias
      - HIV
      - alcohol abuse
      - chronic pain after surgery
      - cancer
        
        surgical removal of tissues with
        tremor can damage nerves
      - trauma
    - - blocks the v.g. Ca channels in the CNS --> blocking the propagation of noxious APs
    - - block the v.g. Na channels --> blocking the propagation of noxious APs
- - - - side effects
        
        Nausea and vomiting - ati-emetic - CTZ
        
        dependence - rare in patients
        
        inhibit GABAergic neurons projecting to VTA, causing
        disinhibition and triggering of the reward pathway
        
        Pain blocks the reward pathway -> rare in patients compared to street use
        
        Constipation - peripheral-enteric
        
        Anti-tussive - brain
        
        respiratory depression - brainstem
      - Morphine
      - Codeine
      - Heroine
        
        diacetylmorphine
        
        Acetyl group makes it inactive and
        able to quickly penetrate to the CNS
        
        converts into morphine in the CNS
      - mechanism of action
        
        stimulate opioid receptors
        
        Mu receptors
        
        Endogenous agonist: Endomorphine
        
        Exogenous agonist: Morphine, Codeine
        
        mechanism: Opens K+ channels
        
        most clinically used drug targets
        
        Drugs
        
        Morphine
        
        Oral and intravenous administration
        
        slow release
        
        Codeine
        
        weak effects
        
        pro-drug for morphine
        
        Fentanyl
        
        Rapid onset and offset
        
        Pethidine
        
        used in childbirth
        
        Heroin
        
        pro-drug for morphine
        
        rapid effects
        
        Naloxone
        
        Mu antagonist
        
        used to reverse opioid effects e.g. in overdose
        
        genetic component
        
        differences in receptor sequence
        
        lack of enzyme converting codeine to morphine
        
        Slower metabolism of morphine
        
        Delta receptors
        
        Endogenous agonist: Enkephalins
        
        Exogenous agonist: DPDPE
        
        mechanism: Opens K+ channels
        
        Similar to Mu, but no drugs available
        
        Kappa receptors
        
        Endogenous agonist: Dynorphin
        
        Exogenous agonist: U50488H
        
        mechanism: Closes Ca2+ channels
        
        odd side effects
        
        ORL-1
        
        Endogenous agonist: Nociceptine
        
        mechanism: Opens K+ channels
        
        analgesic, bu can also enhance pain
        
        exerted effects
        
        Block Ca channels (no polarisation)
        
        Open K+ channels (hyperpolarisation)
        
        location
        
        Brain
        
        Brainstem
        
        elevated mood and emotions
        
        sleep
        
        appetite
        
        Spinal Cord
        
        Peripheral tissues - side effects
        
        INHIBITION
        
        75% of action through presynaptic inhibititory
        receptors on the pain fibres in the SC
        
        25% through postsynaptic inhibitory
        receptors in the SC
      - Endogenous opioids
        are all peptide NTs