Term
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Definition
| a complex experience that consists of 2 components: as a physiological sensation and as an emotional & psychological reaction to a painful sensation |
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Term
| Emotional & Psychological Component of Pain |
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Definition
| the most important component of pain because it represents pain as "suffering" |
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Term
| Places where morphine acts in the brain |
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Definition
| limbic system, spinal cord, and thalamus |
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Term
| Types of Pain Morphine is effective against |
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Definition
| more effective against dull, constant visceral pain then against sharp, intermittent, somatic pain; a pt's ability to tolerate pain is markedly increased without altering perception of other sensations and does not cause loss of consciousness |
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Term
| Morphine's actions at molecular & cellular level |
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Definition
| agonist at receptors for endogenous opioid peptides (endorphins & enkephalins) and modifies processing of pain information in CNS & in periphery |
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Term
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Definition
| opioid receptors found primarily in brainstem, spinal cord, & limbic areas & mediate supraspinal analgesia, some spinal analgesia, sedation, respiratory depression, euphoria, & dependence |
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Term
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Definition
| opioid receptors found mainly in brainstem & spinal cord; mediates some spinal analgesia, some supraspinal analgesia, meiosis, sedation, & dysphoria |
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Term
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Definition
| opioid receptors that are located in brainstem & limbic system; mediates dysphoria & hallucinations & plays a role in development of tolerance to mu receptor agonists |
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Term
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Definition
| strong agonist at mu receptors, moderate agonist at kappa receptors, and weak agonists at delta receptors |
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Term
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Definition
| strong agonists at kappa receptors, partial agonists or antagonists at mu receptors |
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Term
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Definition
| antagonist at all types of opioid receptors |
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Term
| Pharmacological Actions of Morphine |
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Definition
| analgesia, sedation & mental clouding, relief of anxiety & apprehension, euphoria (usually) or dysphoria (occasionally), nausea, depression of respiration, constriction of pupils, antitussive effect, lowering of seizure threshold, endocrine disturbances, effects on smooth muscle, cardiovascular effects, skeletal muscle rigidity, immunosuppression (chronic use) |
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Term
| Sedative & mental clouding aspect of morphine pharmacology |
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Definition
| therapeutic doses provied a floating, dream-like state (easily woken up from); in OD situations, cause graded depreesion of cortical function which can lead to hypnosis/stupor to coma to death |
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Term
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Definition
| unpleasant subjective effects that include fear, anxiety, restlessness, hallucinations, & nausea when taking morphine |
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Term
| Nausea caused by morphine |
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Definition
| due to stimulation of chemoreceptor trigger zone (CRTZ) in medulla; more common in ambulatory patients than hospitalized patients; tolerance does develop |
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Term
| Depression of Respiration due to Morphine use |
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Definition
| major toxic effect - usual cause of death in opioid poisoning; decreased sensitivity to CO2 at chemoreceptors in medulla; use with caution in pts with impaired respiratory function; may be used in treatment of pulmonary edema due to its frightening & unpleasant symptoms or air hunger |
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Term
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Definition
| tell-tale signs of opioid poisoning; due to severe constriction of pupils (meiosis) |
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Term
| Effects of Morphine on Smooth Muscle |
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Definition
| increased tone of circular smooth muscle, decrease in propulsive movements of longitudinal muscle; decreased intestinal motility (constipation), urine retention, bronchoconstriction, increased biliary pressure |
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Term
| postural (orthostatic) hypotension |
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Definition
| cardiovascular effect of morphine that is due to release of histamine & interference with hemostatic reflexes |
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Term
| Cardiovascular Effects of Morphine |
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Definition
| postural (orthostatic) hypotension, cutaneous vasodilation, increased CSF pressure (use with caution in pts with head injuries) |
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Term
| Routes of Adminstration of Morphine |
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Definition
| IM, SC, or oral (becoming more widely used); snorted = abuse |
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Term
| Gold Standard Therapeutic Dose of Morphine |
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Definition
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Term
| Amount of morphine metabolized if taken orally under first pass effect |
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Definition
| 75% of dose is metabolized, reason why oral was generally not popular (can give high doses to provide a therapeutic oral dose) |
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Term
| Duration of Analgesic Effect of Morphine |
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Definition
| duration is usually 4-6 hrs, longer in elderly pts |
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Term
| Major Drug Interactions with Morphine |
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Definition
| additive effects of other CNS depressants; MAO inhibitors; abuse with amphetamines & cocaine ("speedballing"); enhanced analgesic effect when used in combinations with NSAIDs; certain antihistamines (hydroxyzine) enhance analgesic effects of opioids; tricyclic antidepressants enhance analgesic effects |
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Term
| Triad Symptoms of Opioid Poisoning |
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Definition
| CNS depression (stupor or coma); depressed depth & rate of respiration; pin point pupils (note: if ppt is severely hypoxic, pupils may be DILATED!) |
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Term
| Treatment of Opioid Poisoning |
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Definition
| support respiration; administer a narcotic antagonist like naloxone (NARCAN) |
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Term
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Definition
| moderate-severe pain; treatment of chronic pain; adjuncts to surgical anesthesia; antitussive; antidiarrheals; dyspnea of left heart failure & pulmonary edema; abuse |
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Term
| 3 Important Developments in use of Morphine and related opioids |
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Definition
| 1) infusion & autoinjector systems; 2) PCA (patient controlled analgesia); 3) spinal analgesia |
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Term
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Definition
| oral, SC, IM, or IV; absorbed from GI tract but not as effective orally due to first pass metabolism; GOLD STANDARD Dose: 10 mg SC or IM or 10-30 mg PO; used for more severe pain |
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Term
| codeine (phosphate of sulfate salt) |
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Definition
| orally effective; 1/12th potency of morphine; common doses: 30-60 mg PO; used as analgesic for mild-moderate pain and as an antitussive; has only weak opioid agonist activity |
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Term
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Definition
| similar to morphine but more potent |
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Term
| oxycodone (Roxicodone, Percodan, Percocet, OxyContin) |
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Definition
| a cross between morphine & codeine; used orally (alone or in combination with acetaminophen, ibuprofen) for moderate-severe pain; one is a sustained-release oral tab for management of severe chronic pain |
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Term
| hydrocodone (Lortab, Lorcet, Vicodin, Norco) |
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Definition
| similar to both codeine & oxycodone; used orally in combination with acetaminophen for mild-moderate pain and as an antitussive; one of most widely prescribed opioids |
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Term
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Definition
| synthetic oral and parenteral administered drug with 1/10th potency of morphine; reported to have weaker effects on smooth muscle with less constipation & urine retention but studies show it does not; used for moderate to severe pain; commonly used in obstetrics; relatively short acting (1-3 hrs), not appropriate for chronic pain becuase of buildup of normeperidine which can cause seizures; falling into disfavor |
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Term
| heroin (diacetylmorphine) |
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Definition
| more potent & more euphoric than morphine; duration of action 4-6 hrs; not available for use in US; major drug of abuse; can be injected, snorted, or smoked |
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Term
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Definition
| less euphoric & longer duration of action than heroin or morphine; used as an analgesic & in treating opioid addiction; dosing can be tricky, needs to be done carefully with close monitoring |
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Term
| levo-alpha-acetylmethadol (ORLAAM) |
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Definition
| newer drug approved for treatment of opioid dependence; similar to methadone except given every other day; can only be dispensed through approved drug abuse treatment programs |
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Term
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Definition
| much less potent than other agents; has little analgesic activity; does have potential for serious toxicity at high doses; widely used but not a particularly good drug |
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Term
| fentanyl (Sublimaze, Duragesic, Actiq) |
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Definition
| very potent mu agonist (100x more potent than morphine); given parenterally to supplement surgical anesthesia; also has a transdermal patch for management of chronic pain; also comes in lozenge form for treatment of "breakthrough" pain |
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Term
| fentanyl + droperidol (Innovar) |
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Definition
| combination preparation that induces a state called neuroleptic analgesia --> various diagnostic or minor surgical procedures may be carried out even though patient might not completely lose consciousness; administering NO with this product will produce a state called neuroleptic anesthesia |
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Term
| sufentanil (Sufenta) and alfentanil (Alfenta) |
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Definition
| similar to fentanyl; used IV as adjuncts for surgical anesthesia |
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Term
| pentazocine (Talwin, Talwin NX) |
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Definition
| mixed agonist-antagonist with agonist effects dominant - kappa agonist, partial mu agonist(lower doses) & mu antagonist (high doses); less effective than morphine for severe pain; less sedation & respiratory depression than morphine; more CNS stimulation & hallucinations than morphine; can precipitate withdrawal symptoms in opioid addicts |
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Term
| buprenorphine (Buprenex, Subutrex, Suboxone) |
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Definition
| partial agonist at mu-receptors, very high doses cause mu-antagonist actions; abuse potential is much lower than morphine; reduces craving in heroin addicts, used in treatment of heroin addiction; one form also contains nalaxone and is designed for sublingual use; primary agent used for "office based" treatment of opioid addiction |
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Term
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Definition
| newer drug used for mild to moderate pain; a weak mu agonist & inhibits synaptic reuptake of NE and SE; produces good analgesia with supposedly mild side effects; Side effects include: dizziness, sedation, nausea, constipation; claimed to have lower abuse potential but still has opioid-like abuse potential |
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Term
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Definition
| pure opioid antagonist; drug of choice for opioid poisoning, can reverse respiratory depression of opioids; not effective orally, must be given parenterally; included in combination with oral narcotic analgesics to prevent abuse via injection; short duration of action (1-2 hrs); can precipitate withdrawal in addicts |
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Term
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Definition
| orally effective, long-acting antagonist (24 hrs); used in "immunizing" addicts (preventing high produced by opioid agonists); risk of hepatotoxicity; patient compliance is a major problem; opioid addict must first be detoxified (brought through withdrawal) before therapy can be initiated; decreases craving for alcohol in alcoholics, approved for use in treatment of alcoholism |
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Term
| methylnaltrexone (Relistor) |
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Definition
| quaternary salt used for treatment/prevention of opioid-induced constipation; must be given parenterally (subcutaneously); only appropriate for serious constipation resulting from opioid use in more severe types of pain |
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Term
| Therapeutic Uses of Opioid Antagonists |
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Definition
| treat opioid-induced overdose toxicity; diagnose opioid physical dependence; treat compulsive opioid abuseers; reduce cravings for alcohol in recovering alcoholics |
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Term
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Definition
| tolerance + withdrawal syndrome |
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Term
| Characteristics of Acute Withdrawal Syndrome |
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Definition
| craving for drug; anxiety, hostility, insomnia, yawning, rhinorrhea, hyperventilation; dilation of pupils; GI hypermotility (diarrhea, nausea, vomiting, cramping); hypertension; "goose flesh", chills |
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Term
| Duration & Intensity of short acting drugs (i.e. heroin) |
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Definition
| intense withdrawal symptoms, short duration (3-7 days) |
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Term
| Duration & intensity of long acting drugs (i.e. methadone) |
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Definition
| moderate withdrawal symptoms, long duration (1-2 weeks) |
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Term
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Definition
| quit "cold turkey"; weaning patient off drug; methadone (substitution or maintenance methods); buphenorphine; naltrexone; clonidine; anti-depressants |
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Term
| Opioid dependence in medical setting |
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Definition
| pts become dependent while chronically receiving opioids for medically valid reasons; they receive known doses of pure drug under strictly controlled conditions; usually, pts can be weaned off drug with minimal discomfort & little potential for continuing dependence |
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Term
| Opioid Addiction in street setting |
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Definition
| in this setting, drug abuser actively seeks illegal drug for its mind altering effects; pattern of addiction involves taking unknown doses of impure drugs under very unsanitary conditions; must often resort to crime or prositution to support their habit |
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Term
| Health Hazards Associated with Street Use of Opioids |
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Definition
| hepatitis, miscellaneous infections (abcesses, endocarditis, tuberculosis), AIDS |
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