Miscellaneous Quiz / Opioids

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QUIZ: Can you name the Opioids?

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

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