Miscellaneous Quiz / Opioids

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Can you name the Opioids?

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Receptor subtype: Mu (--) and Kappa (++)
Receptor subtype: Mu (+++) and Kappa (+)
Efficacy: very low; abuse potential: low
Drug use: acute opioid OD
Addiction/Withdrawal: No tolerance develops, no abstinence symptoms after withdrawal of antagonists after chronic administration
Hydrocodone class
Efficacy: low; abuse potential: medium
Butorphanol class
Medium oral bioavailability. DOA: 2-4 hours
Parenteral. DOA: > 0.75 hours
Codeine class
Tramadol class
Transdermal, low oral bioavailability. DOA: >1.5 hours
Receptor subtype: Mu (++) [10% to morphine] and Delta (+)
SE: Neuroendocrine effects (stimulate the release of ADH, prolactin, somatotropin, inhibit the release of LH), pruritis, flushing, warm skin, sweating.
Codeine w/ aspirin
Parenteral only. DOA: 4-8 hours
Drug use: Analgesia, pre-sx anxiolytic, epidural & spinal analgesia, balanced anesthesia (buprenorphine may be > effective than methadone in detox & maintenance tx in heroin users
Codeine w/acetaminophen
Low oral bioavailability. DOA: 3-4 hours
Naloxone class
Efficacy: high; abuse potential: low
Receptor subtype: Mu (P) and Kappa (--)
Medium oral potency. DOA 3-4 hours
Efficacy: high; abuse potential: high
Oral only. DOA 4-5 hours
Receptor subtype: Mu (+++)
Dezocine class
SE: Analgesia, euphoria (floating sensation, no anxiety or distress), rarely dysphoria (restlessness, malaise), sedation, drowsiness.
Receptor subtype: Mu (+++), Delta (+), and Kappa (+)
Efficacy: moderate. Abuse Potential: low
Nalbuphine class
Dihydrocodone class
Drug use: Mild to moderate analgesia
Medium oral bioavailability, not SC (irritant). DOA: 3-4 hours
SE: Itching (via histamine release), immune modulation
SE: Constriction of Oddi sphincter (--> reflex of bile and pancreatic juice --> elevated plasma amylase, lipase), depressed renal function.
Fentanyl class
Efficacy: moderate; abuse potential: medium
Parenteral or SL only. DOA: > 8 hours. Long half life (20-70 hours)
SE: Peripheral arterial & venous dilation, may increase ICP when pCO2 rises, constipation, decreased motility, increase in GI tone & spasms, biliary colic
Receptor subtype: Mu (P) and Kappa (++)
Non-opioid effects: MAO inhibition, blocks NMDA (neuropathic pain)
Drug use: mild to moderate analgesia, anti-tussives
Parenteral. DOA: > 0.05 hours
SE: seizures, neuropathic pain. Little respiratory effects
Receptor subtype: Mu (+)
Drug MOA: Weak mu-receptor agonist. Serotonin and NE transporter inhibition
Nalmefene class
Receptor subtype: Mu (P) and Delta (++)
Oxycodone w/ acetaminophen
High oral bioavailability.DOA: 4-6 hours
Well absorbed orally. Strong first pass effect. DOA: up to 48 hours
Drug use: Mild analgesia, 1/2 as potent as codeine
Parenteral only. DOA: 3-4 hours
Hydrocodone w/ acetaminophen
SE: Increased tone of the ureter, bladder, and sphincter (--> urinary retention), decreased uterine tone (may prolong labor).
Methadone class
Drug use: acute opioid OD, possible use in decreasing ETOH cravings in addicts
Drug use: detox tx for heroine addicts, tolerance develops slower -- analgesic rotation. Withdrawal milder; maintenance tx for heroin addicts
SE: in dependent pts --> instant abstinence (withdrawal syndrome)
Oxycodone w/ aspirin
Pentazocine class
Parenteral. DOA: > 1.5 hours
Hydrocodone w/ ibuprofen
Levorphanol class
Naltrexone class
Low oral bioavailability. DOA: 4-5 hours
Drug: Poor oral efficacy. Glucoronidation. DOA: 1-2 hours (IV). Repeated injected may be needed
Drug use: Analgesia (especially severe acute pain)
Drug use: Analgesia (severe acute pain), pre-sx anxiolytic, epidural & spinal analgesia, balanced anesthesia, chronic pain (patches, lollipops)
Oxycodone class
High oral potency. DOA 3-4 hours
IV only with DOA longer than naloxone
Meperidine class
Drug Effects: Almost inert in the absence of an agonist. Reverses opioid effect completely in 1 - 3 minutes. Normalizes resp, consciousness, pupil size, & bowel activity.
Receptor subtype: Mu (P) and Kappa (+++)
Analgesia (severe acute pain), pre-sx anxiolytic, epidural & spinal regional analgesia, balanced anesthesia, dyspnea.
SE: Resp depression (increased PaCO2 & depressed response to CO2 challenge), cough suppression, miosis, truncal rigidity, n/v, little effect on BP or HR (some exceptions)
Buprenorphine class
Non-opioid effects: Antimuscarinic, (tachycardia), blocks serotonin reuptake (contraindicated w/ MAOIs), active metabolite can produce seizure in pts w/ renal failure

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