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44 Cards in this Set

  • Front
  • Back
Where in the brain are mu receptors located?
Dorsal spinal cord, PAG, thalamus, cortex, limbic areas
Where in the brain are kappa receptors located?
Ventral spinal cord, PAG, thalamus, cortex, limbic areas
Where in the brain are delta receptors located?
Dorsal and ventral spinal cord, PAG, thalamus, cortex, limbic areas
What receptor is responsible for respiratory depression?
Mu
How does respiratory depression occur?
Mu receptors decrease the breathing rate and the body's response to CO2 build-up.
What effect do mu receptors have on dopamine levels?
Mu receptors block GABA interneurons, INCREASING dopamine
What receptor is responsible for dysphoria?
Kappa
How does dysphoria occur?
Kappa receptors directly on the dopamine neuron inhibit dopamine
What receptors are responsible for miosis?
Mu and kappa (increased parasympathetic activity)
What receptors are responsible for sedation?
Mu and kappa (both decrease NE levels)
What receptors are responsible for muscular rigidity?
Mu, kappa and delta (inhibition of dopamine neurons in the nigrostriatal tract)
What receptors are responsible for cough suppression?
None (naloxone insensitive)
What receptor is responsible for nausea?
Mu receptor in the CTZ in the area postrema
How do opiates affect hormone levels?
Mu receptors in the hypothalamus decrease testosterone and estrogen
What protein are opioid receptors coupled to?
Gi
What effects do opioids have on the molecular level?
Inhibit cAMP, open K+ channels, decrease Ca2+ channels
What effect do enkephalin neurons have?
Decrease the release of Substance P
What effects do dynorphin neurons have?
Increase K+ conductance, cause hyperpolarization, slow pain impulses
What effect does blocking opioid receptors in the thalamus have?
Blocks the impulses to the cortex and limbic system, blunting the emotional response to pain
What receptor is responsible for constipation?
Mu (decreases motility and secretions, increases tone)
What receptors affect smooth muscle?
Mu and delta
What receptors affect the immune system?
Mu and delta (suppress lymphocytes, esp. T-Killer cells)
What is the primary type of metabolism opiates undergo in the liver?
Glucuronidation
What are the contraindications for opioids?
Head injury, resp. depression, pregnancy, allergies/asthma, impaired liver/kidney function
What happens when you combine opioids with anything that increases NE or 5HT?
Increased activation of enkephalin and dynorphin neurons
What happens when you combine opioids with CNS depressants?
Increased sedation
What happens when you combine opioids with antihistamines?
Increased analgesia and some sedation
What happens when you combine opioids with NSAIDs?
Increased analgesia
What classes of drugs increase NE and 5HT?
TCAs, SSRIs, NSRIs, stimulants, MAO inhibitors
What is the opiate "overdose triad"?
Stupor, respiratory depression, pinpoint pupils
What drug do you give to counteract an opioid overdose?
Naloxone (non-selective opioid antagonist)
What is the active metabolite of morphine?
Morphine-6-glucuronidate
What is the active metabolite of heroin?
Morphine
Which opioid may be a little safer in babies?
Meperidine
Which opioid may be a SSRI?
Meperidine
Which enzyme converts codeine to morphine?
CYP2D6
Dextromethophan is a stereoisomer of what drug?
Levorphanol
What opioid receptors does pentazocine interact with?
Partial mu, full kappa agonist
What opioid receptors does nalbuphine interact with?
Mu antagonist, full kappa agonist
What opioid receptors does butorphanol interact with?
Partial mu, full kappa agonist
What opioid receptors does buprenorphine interact with?
Partial mu, full kappa antagonist
What opioid receptors does buprenorphine interact with?
Partial mu agonist
What opioid receptors does spiradoline interact with?
Selective kappa agonist
What opioid receptors does nalmefene interact with?
Pure mu antagonist