NUR 426 Lecture Notes - Lecture 15: Opioid Antagonist, Opioid Receptor, Levorphanol

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5 Jan 2018
Department
Course
Professor
Narcotic Analgesics
Prototypes Categories and Medicines
Narcotic Agonist
Morphine Sulfate
Methadone
Fentanyl
Meperidine (Demerol)
Tramadol (Ultram)
Opioid Agonist/Antagonist
Pentazocine
Buprenorphine
Narcotic Antagonist
Naloxone
What Is Pain?
Definition:
sensory and emotional experience associated with actual or potential tissue damage
tissue injury: release of kinins and prostaglandins stimulate sensory nerves
Nociceptive direct stimulus to a pain receptor
Neuropathic nerve injury
Psychogenic emotional, psychological or behavioral stimuli
Acute pain response to recent tissue damage/injury
Chronic pain constant or intermittent pain that occurs long past time of injury
Pain causes a release of epinephrine and has an effect on the sympathetic nervous system.
Pain location and Intensity
Location:
- Site of injury
- Referred pain often follows a predictable pathway
- Generalized or poorly localized pain
Neural Pathways of pain
A-delta fibers (fast): small, myelinated fibers respond quickly to acute pain and send messages
to spinal cord (motor)
C fibers: unmyelinated and slow conducting; transmit messages to spinal cord
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A fibers: large diameter sensory nerves that enter the dorsal horn of the spinal cord transmit
touch and temperature (not pain);
Opioid receptors
Receptors that respond to endorphins and enkephalins
Pain blocking
Respiratory depression
Euphoria
Decreased GI activity
Pupil constriction and physical dependence
Pain
Nociceptive
- Somatic visceral
Neuropathic
Pain threshold level od stimulus needed to produce pain
Pain tolerance amount of pain that can be endured without interfering with functioning
Drug tolerance
Physical dependence
Addition
Narcotic Agonist
Actions
- Act at opioid receptor sites
- Produce analgesia, sedation and a sense of well-being (euphoria)
- Ex: Codeine, Fentanyl, hydrocodone, hydromorphone, levorphanol, meperidine, methadone
Actions
- Antitussives
- Adjuncts to general anesthesia
- EX: Morphine, Oxycodone, oyxmorphone, Propoxyphene, remifentanil, sufentanil, tramadol
Life span Implications
- Children: safety and effectiveness not established; dose recommendations established
for codeine, fentanyl (not transdermal), hydrocodone, meperidine and morphine
- Adults: reassure that additions are unlikely during treatment for acute pain;
contraindicated or caution in pregnancy; drugs enter breastmilk; morphine, meperidine,
oxymorphone used for analgesia during labor
- Oxycodone Category B; all other category C
- Older adults: more susceptible to adverse effects on CNS, GI, CV system; hepatic or
renal impairments, may increase risk of toxicity; implement fall precautions in hospital.
Pharmacokinetics
- IV most reliable way to achieve therapeutic response
- IM and subq rate of absorption varies
- IM and Subq absorption is slower in female patients
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