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35 Cards in this Set
- Front
- Back
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Opioid Receptor types & effects
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mu -> supraspinal & spinal
morphine-like analgesia, respiratory depression, euphoria, physical dependence delta -> spinal analgesia -> enkephaline selective interaction kappa -> spinal analgesia -> miosis, sedation (pentazocine-like) |
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Morphine Physiological Actions
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"HECk of a DREAM"
↑Histamine & hormonal (↑Prolactin, ↓ GRH, CRH, CH, FSH, ACTH) Emesis Contract smooth mm (biliary & bladder/ureter) CV changes (orthostat hypo) Decreased cough, GI motility, uterine tone, Depress mental (sedation) Respiratory depression (also causes dilation of cerebral vasculature -> ↑ICP) Euphoria Analgesia Miosis |
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Morphine acts on which receptors
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mu (strong), delta (weak), kappa (weak)
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Heroin differences from morphine and metabolism
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lipid soluble -> CROSS BBB
glucuronide conjug -> urine & bile |
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Treatment of morphine OD
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atropine + naloxone (also diagnostic c/o reverses effects)
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Codeine effects
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same as morphine except:
anti-tussic less euphoria more effective orally |
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Opioid alkaloid mnemonic
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"CODE LEVels call for MORe HEROIN"
Codein, Levorphanol, Morphine/Hydromorphone, Heroin |
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Codeine acts on which receptors
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kappa (weak) and delta (weak)
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Levorphanol what is it
routes of admin |
Strong opioid agonist
oral or parenteral |
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Cross-tolerance to morphine
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meperidine & codeine
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Effects cannot get tolerance to w/ opioids
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miosis & constipation
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Meperidine mnemonic
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"Me poor mom had me in labor & pushed w/ anti-muscles wide eyed w/ amazement"
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Meperidine uses, DOA & Admin
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Use: labor & moderate/severe pain
Action: SHORT DOA, weaker than morphine ORAL (no 1st pass metab) |
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Meperidine acts on which receptor
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mu agonist
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Meperidine actions, SE, admin
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Anti-SLUD/anti-muscarinic
Depress repiration DILATES PUPIL Blurred vision TACHYCARDIA (c/o decrease TPR) |
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Diphenoxylate use
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Diarrhea (diphenoxylate + atropine)
"Diarrhea is not too (di) phen atropine all" |
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Fentanyl acts at which receptor
DOA metabolism |
mu agonist
RAPID onset Short DOA (Fentanyl is Fast) |
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Fentanyl use
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Labor, Post-Op, Pre-op (Anaesthesia), Chronic pain (e.g. cancer)
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Sufentanyl properties
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analogue of fentanyl; short duration
high addiction and OD toxicity |
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Methadone acts on which receptors? for how long? How is it used & administered?
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mu agonist, Oral admin
LONG DOA: 15-40 hrs (lipid soluble -> cross BBB) Tx for heroin addicts: long doa decrease withdrawal & blocks reinforcement/criminal activity NOTE: Very addictive |
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Oxycodone acts on which receptors
Use? |
Mu agonist
Moderate/severe pain; opioid tolerant pt -> sustained release tablets (#1 killer of abusers) (Note: oxy + aspirin + acetaminophen = Percocet) |
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Propoxyphene site of action
Use Side effects |
mu receptors
mild/moderate analgesia, anti-tussic Nausea, anorexia, constipation (Toxic dose: resp depress, pulmonary edema, cardiotoxic, delusions/HALLUCINATIONS - like EtOH withdrawal) |
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Pentazocine site of action & MOA
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mixed agonist:
kappa agonist mu antag/partial agonis MOA: Release NE from Sympathetic fibers |
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Pentazocine mnemonic
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Pentagrams seen breathing on ceiling BUT not on PHAN AT ALL (Butorphanol = less halluc)
Krazy? Maybe (Kappa, Mu) |
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Pentazocine Side effects
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Psychomimetic (hallucinations)
High dose: increase BP & HR (from NE) Ceiling effect for resp. depression |
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Buprenorphine site of action
DOA |
Partial mu agonist
Long DOA |
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Buprenorphine use
Side effects |
Office detox (Bupre + Naltrexone)
Can precip. withdrawal Resp depression RESISTS Naloxone ("Bupre No Naloxone work") MORE potent than morphine (25-50x) |
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Butorphanol site of action
Side effects |
Kappa (strong)
Mu (antagonist or partial agonist) Less psychomimetic effects Ceiling for resp. depression |
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Tramodol site of action
MOA |
mu (weak) (synthetic codeine analogue)
Inhibits reuptake of NE & 5-HT ("One way tram to exciting (NE), feel-good (serotonin) land") |
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Tramodol use
side effects |
moderate pain
OD can -> respiratory depression |
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Naloxone use
Site of action/MOA DOA |
Opioid OD (DOC); possible for shock, eating disorder
Mu, kappa, delta ANTAGONIST (binds w/o activating) Short DOA (addict can relapse) |
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Naloxone route of admin
metabolism |
IV c/o 1st pass metabolism
Glucuronide (rapidly) Use lower dose titrated slow to avoid withdrawal effects |
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Naltrexone use
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Opioid abuse (Naltrexone + clonidine or buprenorphine)
ALCOHOLISM (1x/month) |
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Naltrexone route of admin
DOA Metabolism |
Oral
Long DOA 1st pass metabolism |
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Dextromethorphan
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Anti-tussic (oral, OTC)
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