Flashcards in Opioids Deck (25)
Phenantherane Alkaloids drugs
Morphine, Codeine (Natural) Hydromorphone, Tramadol (Semisynthetic):
Derived from opium poppy
Phenylpiperidines derrivtives (synthetic)
Meperidine, fent, sufent, alefent, remi
Most likely to cause histamine release?
Morphine, codeine, meperidine
Cross-sensitivity exists within classes, however, no cross-sensitivity between the 3 classes
Gold standard for potency comparison?
Morphine sulfate (=1) - purely serve as guideline because each patient response can vary drastically
Highest concentration of opioid receptors in the body?
Likely in the GI nervous system compared to CNS
High dose opioids?
Only provide analgesia, additional drugs needed to provide anesthesia/amnesia/unconsciousness/relaxation
Duration: 2-4 hr
Analgesic Dose: 100 mg
Duration: 1-1.5 hr
Analgesic Dose: 100 mcg
Duration: 48-78 min
Analgesic Dose: 10-20 mcg
Duration: 15-25 min
Analgesic Dose: 500-1,000 mcg
Potency: 100 (same as fentanyl)
Duration: 2-5 min
Analgesic Dose: infusion
Duration: 2-4 hrs
Analgesic Dose: 2 mg
Duration: 3-5 hrs
Analgesic Dose: 10 mg
Chronic effects of opioids
Tolerance, physical dependence, constipation
Never develop a tolerance to (2)?
Effect on breathing?
Shift the CO2 response curve to the right, decreased respiratory response to elevated CO2 levels
Stronger the opioid?
Higher the likelihood of physical dependence
Mu receptor effects
Analgesia (supraspinal and spinal), euphoria, sedation, skeletal muscle rigidity, biliary spasm
Kappa receptor effects
Analgesia (supraspinal and spinal), dysphoria, sedation, antishivering
Opioid MOA specifics
Binds to G-protein coupled receptor - cAMP activation, depression of voltage gated Ca channels, activated inward rectifier K channels (K efflux)
Opioid MOA general
Activate opiate receptors on pre-synaptic (1st order) sensory neurons resulting in a decreased amount of substance P (excitatory NT) to be released into synaptic cleft - blocks transmission of pain signal
Endogenous opioid peptides
Enkephalins, endorphins, dynorphins