 Medications that relieve pain without causing
loss of consciousness “Painkillers”
 Classes of analgesics:
◦ Opioids (moderate to severe pain)
◦ adjuvant analgesic drugs.
 An unpleasant
sensory and
emotional
experience
associated with
actual or potential
tissue damage
Gate theoryGate theory
 Level of stimulus needed to produce the
sensation of pain
 Pain receptors: mu, kappa, and delta.
 Mu, kappa and delta
 Opioid drugs also react with these receptors and
thus relieve pain, so these receptors also called
OPIOID RECEPTORS.
 Each receptor family exhibits a different specificity
for the drug(s) it binds.
 The analgesic properties of the opioids are primarily
mediated by the μ receptors that modulate
responses to thermal, mechanical, and chemical
nociception.
 The κ receptors in the dorsal horn also contribute
to analgesia by modulating the response to
chemical and thermal nociception.
 Body has endogenous pain killers
◦ Enkephalins
◦ Endorphins
 The goals of pain management include
reducing and controlling pain, improving
body function and quality of life.
 Assist primary drugs in relieving pain, this
produce synergistic effects.
◦ NSAIDs
◦ Antidepressants
◦ Anticonvulsants
◦ Corticosteroids
 Very strong pain relievers
 Pain relievers that contain opium, derived from
the opium poppy or chemically related to
opium.
Opioid
Analgesics
 They can be classified according to:
◦ Their chemical structure.
◦ Their action at specific receptors.
 Of the 20 different natural alkaloids, only three are
clinically useful: morphine, codeine, and papaverine.
 Relatively simple synthetic chemical modifications of
these opium alakaloids are produced the three different
chemical classes of opioids: morphine-like drugs,
meperidine-like drugs, and methadone-like
drugs.
 Agonists: morphine, meperidine (pethidine),
methadone, fentanyl,codeine.
 Partial agonists: pentazocine, nalbuphine,
buprenorphine, butorphanol.
 Antagonists: naloxone, naltrexone.
 Main use: to alleviate moderate to severe pain.
 Opioids are also used for:
◦ Cough center suppression
◦ Treatment of diarrhea
◦ Balanced anesthesia
 Control postoperative and other types of pain.
 Morphine rapidly enters all body tissues, including
the fetuses of pregnant women.
 Short duration of action 4 hours.
 Given usually I.V OR I.M
 Orally given is absorbed buterratic and slow.
 Spasm in sphincter of oddi.
 Lead to spasm in anal sphincter---constipation.
 Cerebral vasodilatation ---increase cerebral pressure.
 Release histamine.
 Decrease the sensitivity of respiratory center to CO2.
 Is a weak analgesic compared to
morphine.
 It should be used only for mild to
moderate pain.
 Dextromethorphan a nonopioid cough
suppressant, is often given instead.
 Derivative from morphine
 Higher addiction potential.
 Higher euphoria.
 Shorter duration of action.
 Higher penetration to the CSF
 Compared to morphine.
 used in Anesthesia.
 Used to management Postoperative and
procedural pain.
 Rapid onset and short duration.
 Sufentanil , alfentanil , and remifentanil are three
synthetic opioid agonists related to fentanyl.
 They differ in potency and metabolic disposition.
 Sufentanil is even more potent than fentanyl,
whereas the other two are less potent and shorter
acting.
 These agents are mainly used for their analgesic
and sedative properties during surgical
procedures requiring anesthesia.
 Used as analgesic.
 Used in the controlled withdrawal of dependent
abusers from heroin and morphine.
 Methadone [METH-a-done] is a synthetic, orally
effective opioid that has variable equianalgesic
potency compared to that of morphine, and the
conversion between the two products is not linear.
 Methadone induces less euphoria and has a
longer duration of action.
 The actions of methadone are mediated by μ
receptors. In addition, methadone is an antagonist
of the N-methyl-d-aspartate (NMDA)
 Used for acute pain.
 Can be administered orally or I.M.
 Meperidine is very lipophilic and has
anticholinergic effects, resulting in an
increased incidence of delirium as
compared to other opioids.
 Meperidine [me-PER-i-deen] is a lower-potency synthetic opioid
 is very lipophilic and has anticholinergic effects, resulting in an increased incidence
of delirium as compared to other opioids.
 The duration of action is slightly shorter than that of morphine and other opioids.
Meperidine also has an active metabolite (normeperidine) that is renally excreted.
 Normeperidine has significant neurotoxic actions that can lead to delirium,
hyperreflexia, myoclonus, and possibly seizures.
 Due to the short duration of action and the potential for toxicity,meperidine should
only be used for short-term (≤48 hours) management of pain. Other agents are
generally preferred.
 Meperidine shouldnot be used in elderly patients or those with renal insufficiency,
hepatic insufficiency, preexisting respiratory compromise, or concomitant or recent
administration of MAOIs.
 Serotonin syndrome has also been reported in patients receiving both
meperidine and selective serotonin reuptake inhibitors (SSRIs).
 partial agonists used for opioid detoxification
 Mixed agonist-antagonist
 Contraindicated in:
 Known drug allergy
 Severe asthma
Use with extreme caution if:
 Respiratory insufficiency
 Elevated intracranial pressure
 Sleep apnea
 Euphoria
 CNS depression
 Nausea and vomiting
 Urinary retention
 Diaphoresis and flushing
 Constipation
 naloxone I.V (Narcan): half-
life is about 1 hour.
 naltrexone oral (Revia), has
longer duration of action.
 These drugs are used in the
management of both opioid
overdose and opioid
addiction( block the effect of
any future opioid dose)
 When treating an opioid overdose or toxicity, the
nurse must recognize the signs and symptoms of
withdrawal.
 A gradual dosage reduction after chronic opioid
use, when possible, generally helps to minimize
the risk and severity of withdrawal symptoms.
 Stimulation of the patient may be adequate to reverse
mild hypoventilation.
 Is this is unsuccessful, ventilator assistance using a bag
and mask or endotracheal intubation may be needed to
support respiration.
 Administration of opioid anatagonists may also
necessary to reverse severe respiratory depression.
 Co-administration of opioids with:
◦ Alcohol.
◦ Antihistamines.
◦ Barbiturates.
◦ Benzodiazepine.
 Can result in additive respiratory depression,
seizures, and hypotension.
 Mechanism of action:
 It blocks peripheral pain impulses by inhibition of
prostaglandin synthesis.
 It also lowers febrile body temperatures by acting on
hypothalamus.
 Mild to moderate pain
 Fever
 Alternative for those who cannot take aspirin
products
 Contraindications: known allergy, severe liver
disease and G-6-PD
 Adverse effects: is generally well tolerated.
Possible adverse effects include rash, nausea
and vomiting.
 Overdose, causes hepatic necrosis:
hepatotoxicity.
 Long-term ingestion of large doses also
causes nephropathy
 Recommended antidote: acetylcysteine
regimen : is more effective when given within 10
hours of overdose. It is available as IV and OP
dose.
 Maximum daily dose for healthy adults is 4000
mg/day
◦ 2000 mg for elderly or those with liver disease
 It is a centrally acting analgesic.
 Weak bond to the mu receptors and inhibit
reuptake of both norepinephrine and serotonin.
 Adverse effects are include drowsiness,
dizziness, headache, nausea, constipation and
respiratory depression.
 Before beginning therapy, perform a thorough
history.
 Assess for potential contraindications and drug
interactions
 Perform a thorough pain assessment, including
pain intensity and character, onset, location,
description, precipitating and relieving factors,
type, remedies, and other pain treatments
◦ Assessment of pain is now being considered a “fifth
vital sign”
◦ Rate pain on a 0 to 10 or similar scale
 Be sure to medicate patients before the pain
becomes severe so as to provide adequate
analgesia and pain control
 Pain management includes pharmacologic and
nonpharmacologic approaches; be sure to
include other interventions as indicated
 Patients should not take other medications or
over-the-counter preparations without checking
with their physician
 Instruct patients to notify physician for signs of
allergic reaction or adverse effects
 Ensure safety measures, such as keeping side
rails up, to prevent injury
 Withhold dose and contact physician if there is
a decline in the patient’s condition or if vital
signs are abnormal, especially if
respiratory rate is less than 10 to 12
breaths/min
 Monitor for adverse effects.
 Monitor for therapeutic effect.

Opioids

  • 2.
     Medications thatrelieve pain without causing loss of consciousness “Painkillers”  Classes of analgesics: ◦ Opioids (moderate to severe pain) ◦ adjuvant analgesic drugs.
  • 3.
     An unpleasant sensoryand emotional experience associated with actual or potential tissue damage
  • 4.
  • 5.
     Level ofstimulus needed to produce the sensation of pain  Pain receptors: mu, kappa, and delta.
  • 6.
     Mu, kappaand delta  Opioid drugs also react with these receptors and thus relieve pain, so these receptors also called OPIOID RECEPTORS.  Each receptor family exhibits a different specificity for the drug(s) it binds.  The analgesic properties of the opioids are primarily mediated by the μ receptors that modulate responses to thermal, mechanical, and chemical nociception.
  • 7.
     The κreceptors in the dorsal horn also contribute to analgesia by modulating the response to chemical and thermal nociception.
  • 8.
     Body hasendogenous pain killers ◦ Enkephalins ◦ Endorphins  The goals of pain management include reducing and controlling pain, improving body function and quality of life.
  • 9.
     Assist primarydrugs in relieving pain, this produce synergistic effects. ◦ NSAIDs ◦ Antidepressants ◦ Anticonvulsants ◦ Corticosteroids
  • 10.
     Very strongpain relievers  Pain relievers that contain opium, derived from the opium poppy or chemically related to opium.
  • 11.
  • 12.
     They canbe classified according to: ◦ Their chemical structure. ◦ Their action at specific receptors.  Of the 20 different natural alkaloids, only three are clinically useful: morphine, codeine, and papaverine.  Relatively simple synthetic chemical modifications of these opium alakaloids are produced the three different chemical classes of opioids: morphine-like drugs, meperidine-like drugs, and methadone-like drugs.
  • 14.
     Agonists: morphine,meperidine (pethidine), methadone, fentanyl,codeine.  Partial agonists: pentazocine, nalbuphine, buprenorphine, butorphanol.  Antagonists: naloxone, naltrexone.
  • 15.
     Main use:to alleviate moderate to severe pain.  Opioids are also used for: ◦ Cough center suppression ◦ Treatment of diarrhea ◦ Balanced anesthesia
  • 16.
     Control postoperativeand other types of pain.  Morphine rapidly enters all body tissues, including the fetuses of pregnant women.
  • 18.
     Short durationof action 4 hours.  Given usually I.V OR I.M  Orally given is absorbed buterratic and slow.  Spasm in sphincter of oddi.  Lead to spasm in anal sphincter---constipation.  Cerebral vasodilatation ---increase cerebral pressure.  Release histamine.  Decrease the sensitivity of respiratory center to CO2.
  • 20.
     Is aweak analgesic compared to morphine.  It should be used only for mild to moderate pain.  Dextromethorphan a nonopioid cough suppressant, is often given instead.
  • 21.
     Derivative frommorphine  Higher addiction potential.  Higher euphoria.  Shorter duration of action.  Higher penetration to the CSF  Compared to morphine.
  • 24.
     used inAnesthesia.  Used to management Postoperative and procedural pain.  Rapid onset and short duration.
  • 25.
     Sufentanil ,alfentanil , and remifentanil are three synthetic opioid agonists related to fentanyl.  They differ in potency and metabolic disposition.  Sufentanil is even more potent than fentanyl, whereas the other two are less potent and shorter acting.  These agents are mainly used for their analgesic and sedative properties during surgical procedures requiring anesthesia.
  • 26.
     Used asanalgesic.  Used in the controlled withdrawal of dependent abusers from heroin and morphine.
  • 27.
     Methadone [METH-a-done]is a synthetic, orally effective opioid that has variable equianalgesic potency compared to that of morphine, and the conversion between the two products is not linear.  Methadone induces less euphoria and has a longer duration of action.  The actions of methadone are mediated by μ receptors. In addition, methadone is an antagonist of the N-methyl-d-aspartate (NMDA)
  • 28.
     Used foracute pain.  Can be administered orally or I.M.  Meperidine is very lipophilic and has anticholinergic effects, resulting in an increased incidence of delirium as compared to other opioids.
  • 29.
     Meperidine [me-PER-i-deen]is a lower-potency synthetic opioid  is very lipophilic and has anticholinergic effects, resulting in an increased incidence of delirium as compared to other opioids.  The duration of action is slightly shorter than that of morphine and other opioids. Meperidine also has an active metabolite (normeperidine) that is renally excreted.  Normeperidine has significant neurotoxic actions that can lead to delirium, hyperreflexia, myoclonus, and possibly seizures.  Due to the short duration of action and the potential for toxicity,meperidine should only be used for short-term (≤48 hours) management of pain. Other agents are generally preferred.  Meperidine shouldnot be used in elderly patients or those with renal insufficiency, hepatic insufficiency, preexisting respiratory compromise, or concomitant or recent administration of MAOIs.  Serotonin syndrome has also been reported in patients receiving both meperidine and selective serotonin reuptake inhibitors (SSRIs).
  • 30.
     partial agonistsused for opioid detoxification  Mixed agonist-antagonist
  • 31.
     Contraindicated in: Known drug allergy  Severe asthma Use with extreme caution if:  Respiratory insufficiency  Elevated intracranial pressure  Sleep apnea
  • 32.
     Euphoria  CNSdepression  Nausea and vomiting  Urinary retention  Diaphoresis and flushing  Constipation
  • 33.
     naloxone I.V(Narcan): half- life is about 1 hour.  naltrexone oral (Revia), has longer duration of action.  These drugs are used in the management of both opioid overdose and opioid addiction( block the effect of any future opioid dose)
  • 34.
     When treatingan opioid overdose or toxicity, the nurse must recognize the signs and symptoms of withdrawal.  A gradual dosage reduction after chronic opioid use, when possible, generally helps to minimize the risk and severity of withdrawal symptoms.
  • 37.
     Stimulation ofthe patient may be adequate to reverse mild hypoventilation.  Is this is unsuccessful, ventilator assistance using a bag and mask or endotracheal intubation may be needed to support respiration.  Administration of opioid anatagonists may also necessary to reverse severe respiratory depression.
  • 38.
     Co-administration ofopioids with: ◦ Alcohol. ◦ Antihistamines. ◦ Barbiturates. ◦ Benzodiazepine.  Can result in additive respiratory depression, seizures, and hypotension.
  • 39.
     Mechanism ofaction:  It blocks peripheral pain impulses by inhibition of prostaglandin synthesis.  It also lowers febrile body temperatures by acting on hypothalamus.
  • 41.
     Mild tomoderate pain  Fever  Alternative for those who cannot take aspirin products  Contraindications: known allergy, severe liver disease and G-6-PD  Adverse effects: is generally well tolerated. Possible adverse effects include rash, nausea and vomiting.
  • 42.
     Overdose, causeshepatic necrosis: hepatotoxicity.  Long-term ingestion of large doses also causes nephropathy  Recommended antidote: acetylcysteine regimen : is more effective when given within 10 hours of overdose. It is available as IV and OP dose.
  • 43.
     Maximum dailydose for healthy adults is 4000 mg/day ◦ 2000 mg for elderly or those with liver disease
  • 44.
     It isa centrally acting analgesic.  Weak bond to the mu receptors and inhibit reuptake of both norepinephrine and serotonin.  Adverse effects are include drowsiness, dizziness, headache, nausea, constipation and respiratory depression.
  • 46.
     Before beginningtherapy, perform a thorough history.  Assess for potential contraindications and drug interactions
  • 47.
     Perform athorough pain assessment, including pain intensity and character, onset, location, description, precipitating and relieving factors, type, remedies, and other pain treatments ◦ Assessment of pain is now being considered a “fifth vital sign” ◦ Rate pain on a 0 to 10 or similar scale
  • 48.
     Be sureto medicate patients before the pain becomes severe so as to provide adequate analgesia and pain control  Pain management includes pharmacologic and nonpharmacologic approaches; be sure to include other interventions as indicated
  • 49.
     Patients shouldnot take other medications or over-the-counter preparations without checking with their physician  Instruct patients to notify physician for signs of allergic reaction or adverse effects
  • 50.
     Ensure safetymeasures, such as keeping side rails up, to prevent injury  Withhold dose and contact physician if there is a decline in the patient’s condition or if vital signs are abnormal, especially if respiratory rate is less than 10 to 12 breaths/min
  • 51.
     Monitor foradverse effects.  Monitor for therapeutic effect.