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Opioids

Uni of Notts, Addiction & The Brain, first year

TermDefinition
Opioids & their effects Compounds similar to those naturally in the opium poppy which agonise inhibitory receptors to cause analgesia but not anaesthesia. Act as incredibly potent painkillers, euphorics, & narcotics
Dangerous side effects of opioids High risk of overdose due to inhibition of cells in medulla oblongata & pons of the brainstem causing respiratory depression leading to hypoxia & blood acidosis
Types of opioids: Direct derivatives Active compounds obtained directly from opium resin e.g., morphine
Types of opioids: Processed opioid derivatives Modifying the chemical structure of compounds found in opium such as codeine or heroin. These modifications make it more lipophilic so more crosses the blood brain barrier to be converted back to morphine
Types of opioids: Synthetic/semi-synthetic opiates Organic compounds similar to opium derivatives except synthesised by different precursor molecules that either don't come from opium (synthetic) or do but aren't morphine (semi-synthetic)
History of opioids Have been used in early civilisations but sale & use was completely unregulated in 19th & 20th centuries. A laudanum (Victoria opioid tincture) habit was more acceptable than alcoholism. Heroin was synthesised by Beyer as an alternative to morphine
Opioid receptors Only recently discovered & named after their exogenous ligand (endogenous opioid system hadn't been discovered) to cause rapid hyperpolarisation of the cell. Are metabotropic GPCRs
Opioid receptor subtypes Mu - widely distributed, associated with pain relief & euphoria Kappa - mediates some effects of mu receptors causing dysphoria Peripheral - in targets in the PNS such as small intestine & oesophagus
Chronic pain Severe physical agony lasting for longer than 3 months, it is considered a disease in itself at this point & opioids can be used to treat
Pain pathway Ascending white matter tract. Stimulus triggers nociceptors, dorsal horns of the spinal cord signal the thalamus then somatosensory cortex. Descending midbrain pathway mediates the pain signal
Opioids in pain relief Inhibits dorsal horn of ascending tract & disinhibits periaqueductal cells in the descending pathway. Is good for acute pain but not efficient in treating non-cancer chronic pain
Opioids in the reward system Increase dopamine in the nucleus accumbens by stimulating mu-receptors on GABAa channels on inhibitory interneurons in the Ventral Tagmental Area (VTA) disinhibiting dopamine release
Ways of measuring effects of opioids on the reward system (3) fMRI shows blood flow in the brain but doesn't directly correlate to activity so microdialysis of nucleus accumbens is used. Behaviourally we see how rats will administer intravenously or intracranially
Dopamine vs enjoyment Dopamine triggers pathways causing wanting rather than pleasure so users might not even enjoy opioids, they just want them. Shown by an experiment comparing facial reactions to sweet & sour stimuli as reference for enjoyment
Pharmacological adaptations of opioids use (7) Psychological & physiological changes to oppose the acute effects of opioids includes anhedonia, tremors, increased heartrate, spontaneous ejaculation, sweating, insomnia, depression etc.
How many people become addicted Legal prescription opioids can cause dependency & can lead individuals to seek stronger opioids to continue the effects through illegal means. Now less opioids are prescribed so dependence comes from illegal sources
Treatment options (3) Detoxification with medication, controlled withdrawal & abstinence in controlled settings, & naloxone treatment for strong willed patients
Created by: Beech47
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