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Narcotic Analgesics
1.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Chapter 7Chapter 7 Opioid (Narcotic) AnalgesicsOpioid (Narcotic) Analgesics and Antagonistsand Antagonists By Gaurang Chauhan 7th sem.,B.ph L.J.I.P
2.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Opioid (nonnarcotic) analgesics are usedOpioid (nonnarcotic) analgesics are used to manage dental pain in patients whoto manage dental pain in patients who cannot tolerate NSAIDS or when NSAIDscannot tolerate NSAIDS or when NSAIDs are contraindicated.are contraindicated. Opioid analgesics are divided into threeOpioid analgesics are divided into three groupsgroups——opioid agonists, mixed opioids,opioid agonists, mixed opioids, and antagonists.and antagonists. 2
3.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Mechanism of ActionMechanism of Action Opioid analgesics bind to several differentOpioid analgesics bind to several different opioid receptors in the CNS and spinal cord toopioid receptors in the CNS and spinal cord to produce therapeutic and adverse effects.produce therapeutic and adverse effects. These drugs alter the patient’s perception orThese drugs alter the patient’s perception or reaction to pain.reaction to pain. Opioids can be complete agonists, partialOpioids can be complete agonists, partial agonists, agonist-antagonists, or antagonists atagonists, agonist-antagonists, or antagonists at the receptor site.the receptor site. 3
4.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Mechanism of ActionMechanism of Action Stimulation ofStimulation of μμ receptors produces analgesia,receptors produces analgesia, sedation, miosis, pruritus, respiratory depression,sedation, miosis, pruritus, respiratory depression, euphoria, physical dependence, constipation.euphoria, physical dependence, constipation. Stimulation ofStimulation of κκ receptors produces analgesia,receptors produces analgesia, sedation, and myosis.sedation, and myosis. Stimulation ofStimulation of δδ is thought to produce analgesia.is thought to produce analgesia. Stimulation ofStimulation of σσ receptors produces autonomicreceptors produces autonomic stimulation, dysphoria, hallucinations,stimulation, dysphoria, hallucinations, nightmares, and anxiety.nightmares, and anxiety. Stimulation ofStimulation of εε receptors produces analgesia.receptors produces analgesia. 4
5.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics PharmacokineticsPharmacokinetics Most opioid analgesics are well absorbed fromMost opioid analgesics are well absorbed from the gastrointestinal tract.the gastrointestinal tract. Absorption also occurs from the lungs, nasal andAbsorption also occurs from the lungs, nasal and oral mucosa, and the skin.oral mucosa, and the skin. Opioids are bound to plasma protein to varyingOpioids are bound to plasma protein to varying degrees and are also distributed to the placenta.degrees and are also distributed to the placenta. These drugs are metabolized in the liver andThese drugs are metabolized in the liver and undergo variable first-pass metabolism.undergo variable first-pass metabolism. These drugs are excreted by the kidneys.These drugs are excreted by the kidneys. 5
6.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Pharmacologic EffectsPharmacologic Effects These drugs produce varying degrees of analgesiaThese drugs produce varying degrees of analgesia depending on the strength of the individual drug.depending on the strength of the individual drug. Morphine is the opioid agonist by which all othersMorphine is the opioid agonist by which all others are measured.are measured. Opioid analgesics produce euphoria and sedationOpioid analgesics produce euphoria and sedation at usual therapeutic doses.at usual therapeutic doses. Opioid analgesics depress the cough center in theOpioid analgesics depress the cough center in the medulla and produce an antitussive effect.medulla and produce an antitussive effect. Opioid analgesics increase smooth muscle toneOpioid analgesics increase smooth muscle tone and decrease propulsive contractions and motility.and decrease propulsive contractions and motility. This effect makes them useful for treating diarrhea.This effect makes them useful for treating diarrhea. 6
7.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Adverse ReactionsAdverse Reactions Adverse reactions are an extension of theAdverse reactions are an extension of the opioids’ pharmacologic effects.opioids’ pharmacologic effects. Adverse reactions are proportional to opioidAdverse reactions are proportional to opioid analgesic strength.analgesic strength. Adverse reactions are many and includeAdverse reactions are many and include respiratory depression, nausea and emesis,respiratory depression, nausea and emesis, constipation, myosis, urinary retention, CNSconstipation, myosis, urinary retention, CNS depressant effects, and histamine release.depressant effects, and histamine release. 7
8.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics 8
9.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics AddictionAddiction The degree of addiction is related to opioidThe degree of addiction is related to opioid analgesic strength.analgesic strength. Addiction is usually not a problem in dentistryAddiction is usually not a problem in dentistry because the duration of action is short andbecause the duration of action is short and weaker opioids are used.weaker opioids are used. The rate of development of tolerance is relatedThe rate of development of tolerance is related to the strength of the opioid and the frequencyto the strength of the opioid and the frequency of use.of use. 9
10.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Overdose and WithdrawalOverdose and Withdrawal The major symptoms of opioid analgesic overdoseThe major symptoms of opioid analgesic overdose include respiratory depression, pinpoint pupils, andinclude respiratory depression, pinpoint pupils, and coma.coma. Withdrawal occurs with the abrupt discontinuationWithdrawal occurs with the abrupt discontinuation of opioid analgesics.of opioid analgesics. Symptoms include yawning, lacrimation,Symptoms include yawning, lacrimation, perspiration, rhinorrhea, gooseflesh, irritability,perspiration, rhinorrhea, gooseflesh, irritability, nausea, vomiting, tachycardia, tremors, chills.nausea, vomiting, tachycardia, tremors, chills. Addiction, overdose, and withdrawal can be treatedAddiction, overdose, and withdrawal can be treated with opioid antagonists.with opioid antagonists. 10
11.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Red Flags of AddictionRed Flags of Addiction Asks for the opioid analgesic by name and saysAsks for the opioid analgesic by name and says that this is the only drug that works for themthat this is the only drug that works for them Patient claims allergies to NSAIDs or lowerPatient claims allergies to NSAIDs or lower potency opioid analgesicspotency opioid analgesics Calls with a request for an opioid analgesic justCalls with a request for an opioid analgesic just as the office is closing or after hoursas the office is closing or after hours Cancels dental appointment but still requests theCancels dental appointment but still requests the opioid analgesic even though they will be “out ofopioid analgesic even though they will be “out of town on business”town on business” Continually changing practitionersContinually changing practitioners 11
12.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Red Flags of AddictionRed Flags of Addiction Claims a “low pain threshold”Claims a “low pain threshold” Experiences pain for days after scaling andExperiences pain for days after scaling and root planingroot planing Needs refills several days after anNeeds refills several days after an uncomplicated dental procedureuncomplicated dental procedure 12
13.
Mosby items and
derived items © 2007 by Mosby, Inc., an affiliate of Elsevier Inc. Opioid AnalgesicsOpioid Analgesics Allergic ReactionsAllergic Reactions The most common allergic reactions are skin rashThe most common allergic reactions are skin rash and urticaria.and urticaria. They are due to the histamine-releasing propertiesThey are due to the histamine-releasing properties of opioid analgesics.of opioid analgesics. Drug InteractionsDrug Interactions Opioid analgesics produce additive CNSOpioid analgesics produce additive CNS depressant effects when given with other drugsdepressant effects when given with other drugs that depress the CNS.that depress the CNS. 13
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