Shared Flashcard Set

Details

Dental Theraputics
Intramodual exam
9
Medical
Graduate
11/19/2007

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Cards

Term
Meperidine (Demerol)
Definition
•    Mu agonist
   MYDRIASIS
•    Less potent than morphine (1/10)
•    Shorter duration of action
•    Better oral:parenteral ratio
•    High doses more likely to produce excitation; tremors and seizures may occur due to accumulation of the metabolite
•    Contraindicated with MAO inhibitors (seizures)
•    Should be used with caution in asthmatic patients

Term
 Propoxyphene (dextropropoxyphene, Darvon)
Definition
•    Less selective mu agonist
•    Orally effective but less potent than codeine
•    Uses to produce analgesia similar to codeine
•    Combined with aspirin for enhanced effect
•    Excitatory in high doses
•    Abuse liability like codeine
•    Deaths from propoxyphene overdose: respiratory and circulatory collapse, pulmonary edema, cardiac arrhythmias, convulsions, coma.
•    Respiratory depression from propoxyphene is antagonized by naloxone.

Term
    Naltrexone (Trexan; ReVia)
Definition
•    Also relatively "pure" antagonist
•    More effective orally than naloxone due to slower metabolism (24-hour duration of action with moderate oral doses)
•    Can cause hepatic toxicity (monitor liver function with chronic use to treat compulsive abuse; concomitant use with disulfiram not recommended; could have synergistic effects with ethanol)
•    Will precipitate withdrawal; will block analgesic effect of opioids

Term
Heroin
Definition
    Heroin substitutes acetyl groups on the phenolic and alcoholic OH (3,6 positions) to become diacetylmorphine). It is deacetylated in the body to acetylmorphine and morphine.
  • PURE AGONIST
  • Most Lipophilic of all Opioid (crosses BB barrier)
  • Opioid withdrawl is NOT fatal
  • Withdrawl symptoms: mydriasis, diarrhea, vasoconstriction, dysphoria
Term
Methadone (Dolophine)
Definition
•    Mu agonist
•    Similar to morphine in action, duration and potency, when given parenterally
•    High oral efficacy with resulting longer duration of action
•    Methadone maintenance in opioid dependence. Addict is dependent upon methadone rather than morphine or heroin.
•    Cumulation can occur due to binding to tissue proteins
•    Side effects and toxicity similar to morphine

Term
    Pentazocine (Talwin)
Definition
•    Weak antagonist or partial agonist at mu receptor; agonist at kappa receptor
•    Specifically synthesized to find analgesic without abuse potential
•    Has both agonist and antagonist properties
•    Less potent than morphine
•    Naloxone will antagonize the respiratory depression.
•    Anxiety, nightmares and hallucinations with repeated high dose (kappa and/or sigma receptor).
•    Abuse potential lower than codeine, but is compulsively abused. Type of dependence differs in some
        respects from morphine. 
          
Term
Codeine
Definition
•    Effective orally
•    Often combined with aspirin for increased effectiveness
•    Used extensively for antitussive action
•    10% demethylated to morphine (responsible for analgesic effect); mu agonist
•    Excitatory effects in children and some adults
•    Less potent than morphine

Term
Fentanyl (Sublimaze), Sufentanil (Sufenta), and Remifentanil (Ultiva)
Definition
•    Mu Agonists
•    High potency and short duration of action (due to high lipid solubility and redistribution)
•    Used in anesthesia and postoperative analgesia; fentanyl is available in transdermal (patch) formulation for severe chronic pain
•    Do not cause histamine release

Term
Buprenorphine
Definition
  • Agonist- antagonist and Partial Agonist Drug (mixed)
    •  Drugs in this group are either competitive antagonists or partial agonists at the mu receptor and generally possess agonist activity at kappa receptors.
  • Produces less respiratory depression in overdose (lower "ceiling") and less bile duct spasm
  • Advantages= reduced abuse liability and reduction of some adverse effects while retaining strong analgesic
        properties.
  • Disadvantages = most have more "psychotomimetic" activity (kappa and sigma receptor) and will precipitate
        withdrawal in opioid-dependent person.
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