Opioids
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| Opioid MoA = ? | * Produces analgesia through actions at G protein-coupled receptors in the CNS and spinal cord
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| Opioids can be ? | * Full agonists, partial agonists, or antagonists
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| Opioids have actions at ? | * µ (mu) -, κ (kappa)-, or δ (delta)-receptors
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| Another special things opiods can do ? | * can be agonists at one receptor AND antagonist at another
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| Receptor for Euphoria and Receptor for Dysphoria = ? | * Mu = euphoris..... * Kappa = Dysphoria
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| Identify sites of opioid action in the ascending pain pathway = ? | * Afferent Nociceptor, Dorsal Horn, and Ventral Caudal Thalamus
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| Systemic distribution of exogenous opioids does ? | * causes the release of endogenous peptides.... * Overall effect is an INCREASE of analgesic effect (numbing the pain)
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| Opiod action on the Descending pain pathway = ? | * Inhibits release of GABA, inhibiting pain neuron transmission.... * Sites: Periaqueductal gray, Rostral Ventral Medulla, and Dorsal Horn
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| Since opioids undergo an intense first-pass effect, the ____ Dose needs to be higher than the ____ Dose ? | * ORAL.... * Parental..... * Exceptions (poor first pass): codeine and oxycodone
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| Main reservoir of drug = ? | * Skeletal muscle
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| Metabolism of Morphine = ? | * UGT makes Morphine-3 = inhibitory/GABA actions and can cause seizures, and makes Morphine-6 = longer analgesic affects
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| One Opiod that has NO active metabolite, and can ware off quickly = ? | * Fentanyl
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| Turns Codeine in to Morphine = ? | * CYP-2D6 -- can see ultra-rapid metabolizers (need less drug bc morphine is gets in to the system a lot faster) see more pronounced effect
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| CNS effects of opioids ? | * Analgesia, Euphoria, Dysphoria, Sedation, Resp Depression (watch in COPD ppl), Cough Suppression, Miosis (pin prick pupils), Truncal rigidity (treat with NeuroMusc Blocker), Temp issues ( Mu agonists = hyperthermia, and Kappa agonists= hypo)
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| Peripheral effects of opioids = ? | * bradycardia (except for meperidine = Tachy), slows down renal function, Uterus = prolongs labor, Neuroendocrine = ADH-prolactin, and Flushing/Warming Skin
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| Clinical use Example = ? | * Used in CV and other high risk surgeries where goal is to minimize CV depression
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| **STRONG Agonist Drug List = ? ** | * Morphine -- Hydromorphone -- Heroin -- Methadone -- Meperidine -- Fentanyl
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| **MILD/MOD Agonist Drug List = ? ** | * Codeine -- Hydrocodone -- Oxycodone -- Loperamide -- Diphenoxylate
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| **MIXED Receptor Agonist = ? ** | * Buprenorphine
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| **Antagonist Drug List = ? ** | * Naloxone -- Naltrexone
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| **Miscellaneous Drug List = ? ** | * Tramadol -- Dextromethorphan
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| Methadone uses = ? | * To alleviate long term/chronic pain due to its long t 1/2.... * Withdrawal CxSx less likely too (can use for withdrawal pts too)
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| Fentanyl = ? | * widely used and is safe since no active metabolite
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| Meperidine = ? | * Has significant anti-muscarinic effects (anti-DUMBBELSS).... * Negative inotropic action on the heart (CI in Tachy).... * Can cause Seizures or renal failure
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| Codeine = ? | * antitussive (cough).... * Watch monoamine oxidase inhibitor use with this drug.... * Consider a NO GO in kids due to metabolism
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| Hydrocodone and Oxycodone = ? | * Less efficacious than morphine.... *Often combined with acetaminophen for mild to moderate pain..... * HYDROS = NOT used in Migraines
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| Diphenoxylate and Loperamide = ? | * Used in the treatment of diarrhea.... * used with atropine (anti-musc) to stop abuse potential
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| Antagonists primarily through µ-opioid receptors = ? | * Naloxone - IV and Naltrexone - Oral (Used for addicts in treatment programs and has use with alcoholics)
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| Patient has a an opioid overdose and alcohol overdose, what do you give them = ? | * use Naltraxone....* Naloxone = use in OPIOD ONLY !
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| Naloxone SE = ? | * A severely depressed (resp/CV) patient may recover for 1-2 hours then relapse – so monitor tmt
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| Buprenorphine = ? | * SUBLINGUAL route.... * Potent and long-acting partial µ-receptor agonist and κ-receptor antagonist
..... * Use: analgesia and maintenance therapy during opioid withdrawal
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| Tramadol = ? | * serotonin re-uptake blocker.... * is an adjunct.... * watch use in other serotonin re-uptake blockers bc = Serotonin Syndrome
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| Dextromethorphan = ? | * Antitussive (cough)... * Kids Under 6 = BANNED
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| Contraindications/Cautions = ? | * Pure agonists with weak partial agonists – risk of diminished analgesia or inducing a withdrawal state (bc partial gets there first).... * don't give if there is an increase in intracranial pressure
.... * NO in Pregnants
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| Some things that we never develop tolerance too ? | * Miosis (pin prick pupil) and Constipation
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| Tolerance is minimized by ? | * giving smaller doses with longer intervals between dosing..... * tolerance is also usu to Mu-Rec... * also depends on the individual
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| Dependence/ Withdrawal CxSx of a PURE agonist = ? | * yawning, mydriasis, anxiety, hostility
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| Mixed = ? | * appetite and weight loss, abdominal cramps
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