Opioid (Narcotic) Analgesics

and Antagonists

Chapter 6

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 Learning Objectives
Lesson 6.1: Opioid (Narcotic)
Analgesics and Antagonists
(Slide 1 of 2)
1. Explain the classification, mechanism of action,
and pharmacokinetics of opioids.
2. List and describe the pharmacologic effects and
potential adverse reactions of opioids.
3. Discuss the addiction potential of opioids,
including treatment.
4. Name and explain the analgesic actions of the
most common opioid agonists.

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 Learning Objectives
Lesson 6.1: Opioid (Narcotic)
Analgesics and Antagonists
(Slide 2 of 2)
5. Discuss the actions of and provide examples of
the mixed opioids.
6. Summarize the mechanism of action and adverse
reactions of tramadol.
7. Apply the use of opioids to dentistry.

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 Introduction
 Opium: Dried juice from the unripe seed
capsules of the opium poppy
 1800s: Morphine and codeine were isolated from

opium
 Until 1920: Medications containing opium were

promoted
 Oral opioids became unlawful: Injection abuse

began and continues today

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 Classification of Opioid
Analgesics and Antagonists
 Agonists
 Mixed opioids
 Antagonists

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 Mechanism of Action
 Enkephalins
 Endorphins
 Dynorphins
 Important receptors include:
 Mu (μ)
 Kappa (κ)
 Delta (δ)

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 Pharmacokinetics
 ADME
 Absorption
 Distribution
 Metabolism
 Excretion

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 Pharmacologic Effects
(Slide 1 of 3)

 Analgesia
 Sedation and euphoria
 Cough suppression
 Gastrointestinal (GI) effects
 Adverse reactions

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 Pharmacologic Effects
(Slide 2 of 3)

 Sedation and euphoria

 κ-Receptor stimulation
 Potentiate analgesic effect; relieve anxiety
 Additive with other CNS depressants
 Remove pain; euphoria results

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 Pharmacologic Effects
(Slide 3 of 3)

 Cough suppression
 Depresses cough center in medulla
 Antitussive effect requires lower dose
 Gastrointestinal effects
 Increases the smooth muscle tone
 Decreases GI tract’s propulsive contractions and
motility

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 Adverse Effects:
Respiratory Depression
 Cause of death with overdose
 Elderly: Decrease in pulmonary ventilation
 Reduced ventilation produces vasodilation
 Vasodilation results in intracranial pressure
 Mask CNS diagnostic symptoms
 Hyperthyroidism
 Hypothyroidism

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 Adverse Reactions:
Nausea and Emesis
 Constipation
 Miosis
 Urinary retention and antidiuretic effect
 CNS effects
 Anxiety
 Restlessness
 Nervousness
 Dysphoria

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 Adverse Reactions:
Cardiovascular Effects
 Biliary tract constriction
 Histamine release
 Pregnancy and nursing considerations
 FDA pregnancy category C: Morphine, codeine
 Infant born to addict
 Depressed respiration
 Withdrawal symptoms

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 Allergic Reactions
 Dermatologic
 Skin rashes
 Urticaria
 Contact dermatitis
 Some brands of opioid analgesic combinations
are formulated with sodium bisulfate: Be aware
of sulfite hypersensitivity

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 Drug Interactions
 Sedation
 Respiratory depression
 Interact with monoamine oxidase (MAO)

inhibitors
 Interact with antipsychotic agents such as

chlorpromazine

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 Adverse Reactions: Addiction
and Chronic Administration
 Two signs of addiction
 Cravings
 Loss of ability to stop using and loss of ability to
control amount
 Chronic administration
 Tolerance occurs except to miosis and constipation
 Habituation
 Dependence

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 Adverse Reactions: Addiction
 Degree of addiction potential is proportional to
analgesic strength
 Dependent on the drug’s ability to produce

euphoria and reduce anxiety

 Length of administration
 Development of tolerance: Related to drug

strength and frequency of use

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 Treatment
 Substituting oral opioid for injectable form
 Cold turkey: Abrupt withdrawal
 Methadone maintenance
 Administering naltrexone (Trexan)

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 Specific Opioid
Analgesics and Antagonists
 Opioid agonists  Mixed opioids
 Morphine  Agonist-antagonist
 Oxycodone  Partial agonists
 Oxymorphone  Antagonists
 Hydrocodone,  Pentazocine
Hydrocodone ER  Full agonist/reuptake
 Codeine inhibitors
 Meperidine  Tapentadol
 Hydromorphone  Tramadol
 Methadone
 Fentanyl family

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 Specific Opioids: Morphine
 Prototype
 Parenterally: Postoperative pain in hospitalized

patients
 Orally: Treatment of terminal illnesses
 Sustained-release tablets: Outpatient use in

terminally ill

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 Specific Opioids:
Oxycodone, Oxymorphone
 Oxycodone + aspirin = Percodan
 Oxycodone + acetaminophen = Percocet, Tylox
 Oxymorphone

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 Specific Opioids: Hydrocodone
 Hydrocodone > hydromorphone
 Hydrocodone + ibuprofen
 Hydrocodone + acetaminophen
 Hydrocodone ER

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 Specific Opioids: Codeine
 Meperidine (Demerol)
 Hydromorphone (Dilaudid)
 Methadone (Dolophine)
 Fentanyl family
 Fentanyl (Duragesic, Sublimaze)
 Fentanyl (Duragesic) transdermal system
 Sufentanil (Sufenta)
 Alfentanil (Alfenta)

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 Mixed Opioids: Agonist-
Antagonist Opioids
 Pentazocine (Talwin): Oral
 Butorphanol (Stadol): Nasal spray
 Butorphanol (Butrans): Transdermal patch
 50 mg pentazocine + 0.5 mg naloxone = Choice

street drug

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 Mixed Opioids: Partial Agonists
 Buprenorphine (Buprenex, Subutex)
 Schedule III
 Oral and parenteral use

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 Mixed Opioids: Opioid Antagonists
 Naloxone (Narcan)
 Treating agonist or mixed opioid overdoses
 Nalmefene (Revex)
 Reverse opioid overdose
 Naltrexone (Re Via, Vivitrol)
 Maintenance of the opioid-free state in detoxified,
formerly opioid-dependent patients
 Used in management of alcohol abstinence

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 Full Agonist/Reuptake Inhibitors:
Tramadol (Ultram)
 μ-Opioid agonist action
 Inhibition of reuptake of norepinephrine and

serotonin
 No federal scheduling yet; Schedule IV

controlled substance in many states

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Considerations for Dental Rx of Opioids
(Slide 1 of 2)

 Be aware of prescription abuse

 Be aware of illegal selling of Rx drugs
 NSAIDs manage dental pain
 Dispensing excess amount of opioids per Rx
 Codeine or hydrocodone combinations >

oxycodone combinations
 Misconception that limited opioid analgesic use

does not lead to addiction

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Considerations for Dental Rx of Opioids
(Slide 2 of 2)

 Treatment of chronic orofacial pain

 Refer patient, if necessary
 Assess for current signs of drug abuse
 Monitor for potential signs of drug abuse
 Monitor for pain relief
 See patient in office for treatment
 Limit quantity; no refills
 Be aware of demanding patients

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 Dental Hygiene Considerations
 Conduct thorough medication/health history
 Determine contraindications or possible drug

interaction
 Be aware of nonopioid/opioid combinations
 Remind patients to not supplement with OTC

agents
 Avoid use with other sedating drugs
 Patients should avoid making life-changing

decisions
 Be aware of patient positioning
 Be aware of signs of addiction or abuse

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 Patient Instructions for
Use of Opioid Analgesics
 Take with a full glass of water
 Take with food to minimize GI irritation
 Use caution with driving because of likelihood of

dizziness and drowsiness

 Avoid any situations that require thought or

concentration because of the likelihood of

sedation
 These drugs can cause xerostomia. Drink plenty

of water and avoid caffeinated beverages,

juices, and sodas

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Questions?

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