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45 Cards in this Set
- Front
- Back
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Morphine Clinical application |
Treats moderate-severe pain 1st line treatment |
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Morphine Mechanism of action |
Opiate agonist Spinal effect: inhibits ascending pathway by activating MOR in dorsal horn = inhibit neurotransmitter release from pain fiber Supraspinal effect: activate descending pain pathway by activating MOR in PAG |
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Morphine Metabolites |
Morphine-6-glucuronide: full agonist at MOR Morphine-3-glucuronide: does not bind to MOR = no analgesic effects but has neurotoxicity activity in brain |
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Morphine Common/serious adverse reactions |
Respiratory depression Histamine release: hypotension, pruritis, bronchoconstriction Confusion, abuse potential, constipation, nausea, sedation, urinary retention |
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Morphine Methadone Contraindications |
Contraindicated in severe asthma, paralytis ileus, respiratory depression, upper airway obstruction |
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Morphine Routes of administration |
Controlled release oral preps reduce number of daily doses but associated with high abuse potential IV and SC commonly used in patient-controlled devices Epidural and intrathecal administration = highly effective analgesia |
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Methadone Clinical application |
Used to treat severe pain 1st line treatment Used to detox. patients with opioid addiction (opioid use disorder) Due to long duration of action, used to achieve long-lasting pain relief in cancer patients |
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Methadone Meperidine Mechanism of action |
Synthetic opioid agonist Spinal effect: inhibit ascending pathway by activating MOR in dorsal horn = inhibit neurotransmitter release from pain fiber Supra-spinal effect: activate descending pain pathway by activating MOR in PAG |
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Methadone Common/serious adverse reactions |
Similar to morphine (miosis, constipation, respiratory depression, sedation) Little-no histamine release = less pruritus, hypotension, bronchoconstriction Delayed respiratory depression, prolonged QT interval |
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Methadone Metabolism |
Inactivated by CYP2D6 Poor metabolizer polymorphism associated with potential overdose |
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Fentanyl Clinical application |
Used to treat moderate to severe pain 1st line treatment Useful for chronic and breakthrough pain |
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Fentanyl Mechanism of action |
Synthetic opioid agonist Short-acting Spinal effect: inhibit ascending pathway by activating MOR in dorsal horn to inhibit neurotransitter release from pain fiber Supra-spinal effect: activate descending pain pathway by activating MOR in PAG |
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Fentanyl Common/serious adverse reactions |
Similar to morphine, but thought to be lower in severity Little to no histamine release = less pruritus, less CV effects (hypotension), less bronchospasm |
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Fentanyl Potency Routes of administration |
More potent than morphine Several routes of administration Lozenges used for pediatric patients Ideal as primary general anesthetic due to low cardiac deression |
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Meperidine Clinical application |
Treat moderate to severe pain 2nd line treatment |
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Meperidine Common/serious adverse reactions |
Similar to morphine: histamine release (pruritis, hypotension, bronchoconstriction), constipation, respiratory depression, sedation No miosis Unlike other opioids, causes mydriasis (instead of miosis) and tachycardia due to antimuscarinic activity |
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Meperidine Contraindications |
Contraindicated in patients on recent or concomitant SSRI or MAOI due to life-threatening serotonin syndrome |
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Meperidine Metabolite |
Toxic metabolite = normeperidine = causes CNS convulsions/seizures |
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Codeine Clinical application |
Low-medium efficacy Used to treat mild-moderate pain Antitussive agent Antidiarrheal effects |
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Codeine Mechanism of action |
Opiate agonist Does not need to be converted to morphine for antitussive effects Spinal effect: inhibit ascending pathway by activating MOR in dorsal horn to inhibit neurotransitter release from pain fiber Supra-spinal effect: activate descending pain pathway by activating MOR in PAG |
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Codeine Metabolism |
Metabolized by CYP2D6 to activate morphine for analgesia About 10% converted to morphine in patients with 2 wild type CYP2D6 alleles |
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Codeine Commmon/serious adverse reactions |
Similar to morphine (e.g. miosis, constipation, respiratory depression, sedation) Significant histamine release (pruritis, hypotension, bronchospasm) Seizures with excessive dose |
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Codeine Hydrocodone Oxycodone CYP2D6 |
CYP2D6 gene is polymorphic "Poor metabolizers" (2 inactive alleles) are unresponsive "Ultra metabolizers" (gene duplication allele) are otential candidates for toxicity Avoid with opioids not metabolized by CYP2D6 (morphine, hydromorphone, buprenorphine) |
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Hydrocodone Oxycodone Clinical application |
Low-medium efficacy Used to treat mild-moderate pain |
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Hydrocodone Oxycodone Mechanism of action |
Semi-synthetic agonists Spinal effect: inhibit ascending pathway by activating MOR in dorsal horn = inhibit neurotransmitter release from pain fiber Supra-spinal effect: activate descending pain pathway by activating MOR in PAG |
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Hydrocodone Oxycodone Metabolism |
Partially metabolized by CYP2D6 to more active metabolites Metabolized to additional metabolites by other hepatic enzymes |
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Hydrocodone Oxycodone Common/serious adverse reactions |
Similar to morphine (e.g. miosis, constipation, respiratory depression, sedation, histamine release - pruritus, hypotension, bronchoconstriction) |
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Hydrocodone Oxycodone Combined with drug |
Combined with acetominophen (Vicodin and Percocet) Risk of liver toxicity due to acetominophen |
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Hydrocodone Oxycodone Rank in treatment of pain with codeine |
Oxycodone > hydrocodone > codeine |
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Buprenorphine Clinical application |
Used to treat moderate-severe pain Used to treat patients with opioid addiction (opioid use disorder) |
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Buprenorphine Mechanism of action |
Semi-synthetic agonist Partial MOR agonist Spinal effect: inhibit ascending pathway by activating MOR in dorsal horn = inhibit neurotransmitter release from pain fiber Supra-spinal effect: activate descending pain pathway by activating MOR in PAG |
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Buprenorphine Common/serious adverse reactions |
Respiratory depression, miosis, hypotension (due to CNS depression), dizziness, sedation Little-no histamine release |
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Buprenorphine Potency |
25-50x more potent than morphine Morphine-like analgesia but with milder euphoria |
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Buprenorphine Combo drug |
+ naloxone formation given sublingual for pain Prevents illicit IV use Also used for treatment of opioid addiction |
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Pentazocine Clinical application |
Used to treat moderate to severe pain |
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Pentazocine Mechanism of action |
Synthetic mixed agonist/antagonist activity Kappa opioid receptor (KOR) agonist MOR antagonist Analgesia due to KOR stimulation at spinal and supra-spinal sites |
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Pentazocine Common/serious adverse reactions |
Less risk of respiratory depression compared to many mu agonists (but dose-dependent)' Can elicit dysphoric and psychotomimetic effects due to KOR activation |
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Pentazocine Dependence |
Has lower dependence/abuse liability (but not zero) since MOR is not activated in reward pathway Can precipitate withdrawal in mu opioid agonist-dependent patients |
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Naloxone Clinical application |
Treat acute opioid toxicity |
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Naloxone Mechanism of action |
MOR antagonist Short-acting |
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Naloxone Common/serious adverse reactions |
Cardiac arrhythmia, hypertension or hypotension, pulmonary edema, hepatotoxicity |
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Dextromethorphan Clinial application |
Cough suppression |
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Dextromethorphan Mechanism of action |
Synthetic opioid D-isomer Acts on "DM receptor" (likely sigma1 receptor) NMDA receptor antagonist Antitussive mechanism believed to be due to DM receptor |
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Dextromethorphan Common/serious adverse reactions |
Rare but serious allergic reaction |
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Dextromethorphan Analgesic effect |
No effects on opioid receptors = little-no analgesic properties and lower abuse liability |
