Chapter 12 Opioids Used for Mild to Moderate Pain Flashcards
World Health Organization Analgesic Ladder- Step 1
Mild pain is usually treated with over-the-counter (OTC) analgesics such as aspirin, ibuprofen, or acetaminophen. These agents exert their effect by mitigating the “algogenic soup” that follows tissue injury.
World Health Organization Analgesic Ladder- Step 2
For mild to moderate pain, the WHO analgesic ladder
advocates the use of short-acting opioids (SAOs) either
alone or in conjunction with OTC analgesics. In addition,
adjunctive therapy such as acupuncture, transcutaneous
electrical nerve stimulation, and/or psychotherapy may be brought into play at this stage
World Health Organization Analgesic Ladder- Step 3
The third step, to relieve moderate to severe pain, entails the use of high-potency SAOs or long-acting opioids (LAOs), either alone or with adjunctive therapy
The duration of action of SAOs ranges from
2 to 4 hr, and they are available as single entity medication or in combination with a nonopioid, such as acetaminophen or a nonsteroidal anti-inflammatory drug (NSAID)
Advantages or Disadvantages of Combination therapy (nonopioid, such as acetaminophen or a nonsteroidal anti-inflammatory drug (NSAID) with opioid)
Combination therapy offers drug-sparing effects since a lower dose of each medication is used, avoiding side effects associated with higher doses. However, a potential problem is created by combining an opioid, which can produce tolerance and that has no dose ceiling, with acetaminophen or an NSAID, which may cause toxicity beyond a certain dosage
“Weak Opioids.”
When opioids are administered with aspirin, acetaminophen, or ibuprofen
Oxycodone
Oxycodone is a semisynthetic opioid processed from thebaine, an organic chemical found in opium.
Oxycodone compared to Morphine
oral administration has high bioavailability (60%); oxycodone is 1.5 to 2 times more as potent as morphine. High abuse potential
Oxycodone metabolism
Unlike morphine and hydromorphone, oxycodone
is metabolized by the cytochrome P450 enzyme
system in the liver, making it vulnerable to drug
interactions.
Federal Controlled Substance Schedule I
Have no currently accepted medical use and high potential for abuse, addiction, or physical dependence.
Ex: Heroin, lysergic acid, marijuana, mescaline, methaqualone
- Federal Controlled Substance Schedule II
Have accepted medical use and high potential for abuse, addiction, or physical dependence
Ex: Morphine, hydromorphone, methadone, oxycodone,
cocaine, amphetamine, methlphenidate
- Federal Controlled Substance Schedule III
Have accepted medical use and potential for abuse, addiction, or physical dependence less than drugs in Schedules I and II.
Ex: Opioids combined with non-narcotic drugs (e.g.,
hydrocodone/acetaminophen, codeine combination),
dronabinol, anabolic steroids, benzphetamine
Federal Controlled Substance Schedule IV
Have accepted medical use and potential for abuse, addiction, or physical dependence less than drugs in Schedules I–III.
Ex: Benzodiazepines, chloral hydrate, dextropropoxyphene, phenobarbital, fenfluramine
Federal Controlled Substance
Schedule V
Have accepted medical use and potential for abuse, addiction, or physical dependence less than drugs in Schedules I–IV.
Ex: Diphenoxylate in combination with atropine (antidiarrheals), antitussives with limited amounts of narcotics (e.g., codeine)
Hydrocodone
Hydrocodone is an opium derivative and is Schedule III
when in combination with acetaminophen or ibuprofen
and Schedule II when used as a single entity product
Hydrocodone vs. Morphine
Morphine Equivalent Conversion Factor
per Milligram of Opioid is 1.0
Hydrocodone metabolism
Hydrocodone is metabolized by the liver into several metabolites, and has a serum half-life of 3.8 hr
CODEINE
Codeine is an opioid metabolized to active analgesic compounds, including morphine.
How is Codeine administered?
This opioid is frequently administered in combination with acetaminophen, butalbital, and caffeine intended for the treatment of headache and commonly employed as an antitussive
Codeine vs. Morphine
Morphine Equivalent Conversion Factor per Milligram of Opioid is 0.15
Metabolism of Codeine
Unlike morphine and hydromorphone, oxycodone
Is metabolized by the cytochrome P450 enzyme
system in the liver, making it vulnerable to drug interactions
*Tramadol (Ultram) mechanisms of action
agonist activity at the mu opioid receptor as well as Inhibition of the reuptake of norepinephrine and serotonin. (SNRI)
How is Tramadol (Ultram) used in children?
Tramadol 1 to 2 mg/kg is an effective oral agent in
the postoperative period in children ready to be transitioned from patient-controlled analgesia
Adverse events with Tramadol (Ultram)
Nausea, dizziness, somnolence, and headache
association of seizure activity (This risk is increased by a history of alcohol abuse, stroke, head injury, or renal compromise.)