Chapter 12 Opioids Used for Mild to Moderate Pain

Question 1

World Health Organization Analgesic Ladder- Step 1

Answer 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.

Question 2

World Health Organization Analgesic Ladder- Step 2

Answer 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

Question 3

World Health Organization Analgesic Ladder- Step 3

Answer 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

Question 4

The duration of action of SAOs ranges from

Answer 4

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)

Question 5

Advantages or Disadvantages of Combination therapy (nonopioid, such as acetaminophen or a nonsteroidal anti-inflammatory drug (NSAID) with opioid)

Answer 5

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

Question 6

“Weak Opioids.”

Answer 6

When opioids are administered with aspirin, acetaminophen, or ibuprofen

Question 7

Oxycodone

Answer 7

Oxycodone is a semisynthetic opioid processed from thebaine, an organic chemical found in opium.

Question 8

Oxycodone compared to Morphine

Answer 8

oral administration has high bioavailability (60%); oxycodone is 1.5 to 2 times more as potent as morphine. High abuse potential

Question 9

Oxycodone metabolism

Answer 9

Unlike morphine and hydromorphone, oxycodone
is metabolized by the cytochrome P450 enzyme
system in the liver, making it vulnerable to drug
interactions.

Question 10

Federal Controlled Substance Schedule I

Answer 10

Have no currently accepted medical use and high potential for abuse, addiction, or physical dependence.
Ex: Heroin, lysergic acid, marijuana, mescaline, methaqualone

Question 11

• Federal Controlled Substance Schedule II

Answer 11

Have accepted medical use and high potential for abuse, addiction, or physical dependence
Ex: Morphine, hydromorphone, methadone, oxycodone,
cocaine, amphetamine, methlphenidate

Question 12

• Federal Controlled Substance Schedule III

Answer 12

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

Question 13

Federal Controlled Substance Schedule IV

Answer 13

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

Question 14

Federal Controlled Substance

Schedule V

Answer 14

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)

Question 15

Hydrocodone

Answer 15

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

Question 16

Hydrocodone vs. Morphine

Answer 16

Morphine Equivalent Conversion Factor

per Milligram of Opioid is 1.0

Question 17

Hydrocodone metabolism

Answer 17

Hydrocodone is metabolized by the liver into several metabolites, and has a serum half-life of 3.8 hr

Question 18

CODEINE

Answer 18

Codeine is an opioid metabolized to active analgesic compounds, including morphine.

Question 19

How is Codeine administered?

Answer 19

This opioid is frequently administered in combination with acetaminophen, butalbital, and caffeine intended for the treatment of headache and commonly employed as an antitussive

Question 20

Codeine vs. Morphine

Answer 20

Morphine Equivalent Conversion Factor per Milligram of Opioid is 0.15

Question 21

Metabolism of Codeine

Answer 21

Unlike morphine and hydromorphone, oxycodone
Is metabolized by the cytochrome P450 enzyme
system in the liver, making it vulnerable to drug interactions

Question 22

*Tramadol (Ultram) mechanisms of action

Answer 22

agonist activity at the mu opioid receptor as well as Inhibition of the reuptake of norepinephrine and serotonin. (SNRI)

Question 23

How is Tramadol (Ultram) used in children?

Answer 23

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

Question 24

Adverse events with Tramadol (Ultram)

Answer 24

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.)

Question 25

Avoid combining Tramadol with what medication? Why?

Answer 25

patients receiving serotonin selective reuptake inhibitors should avoid taking tramadol due to the risk of producing the serotonin syndrome. The excess serotonin activity produces a spectrum of specific symptoms including cognitive, autonomic, and somatic effects. mild (shivering and diarrhea) to severe (muscle rigidity, fever and seizures). Severe serotonin syndrome can be fatal if not treated.

Question 26

Tapentadol

Answer 26

a centrally acting analgesic with dual mechanisms of action: μ-opioid receptor: agonist activity and norepinephrine reuptake inhibition

Question 27

Tapentadol dosage

Answer 27

Currently, it is not recommended to exceed more than 700 mg/day of tapentadol on the first day of therapy and no more than 600 mg/day on subsequent days with most patients taking 50 to 100 mg every 4 to 6 hr as needed for pain

Question 28

Federal Controlled Substance Schedules for Tapentadol

Answer 28

Tapentadol is a Schedule II controlled substance with abuse potential similar to other potent opioid analgesic

Question 29

Tapentadol adverse effects

Answer 29

nausea, vomiting, constipation,

dizziness, and somnolence

Question 30

Propoxyphene

Answer 30

Propoxyphene hydrochloride is an odorless, white crystalline powder with a bitter taste that is freely soluble in water.

Question 31

What is Propoxyphene analgesic effect due to?

Answer 31

Although propoxyphene is no stronger than acetaminophen, it remains a relatively popular analgesic with increased interest spurred by the finding that the d-isomer, dextropropoxyphene, is a noncompetitive NMDA receptor antagonist

Question 32

Propoxyphene adverse effects

Answer 32

Are dizziness, sedation, nausea, and vomiting. more
serious potential problems including seizures, cardiac dysrhythmias, and even heart block if taken in excessive amounts, either accidentally or because of suicidal intent

Question 33

Risk factor for accidental overdose

Answer 33

Concomitant use of alcohol, sedatives, tranquilizers, muscle relaxants, or antidepressants

Question 34

NSAIDs should be considered possible first-line agents for

Answer 34

Most acute injuries and minor surgical procedures

Question 35

In postoperative pain management, the basis for using nonopioid analgesic adjuvants is to reduce

Answer 35

Opioid consumption and lessen opioid-related adverse effects

Question 36

In what cases is Opioid analgesics might be advantageous over NSAIDs?

Answer 36

Low platelet count: NSAIDs cause platelet dysfunction,(relatively contraindication) patient with a low threshold for bronchospasm. pregnancy (increase the risk of miscarriage) NSAIDs as a group tend to exacerbate reflux esophagitis and peptic ulcer. also are patients with CHF, intrinsic renal disease, liver failure with ascites, and those receiving diuretics. Opioid analgesics used with caution because most are excreted by the kidneys and metabolized by the liver

Question 37

When analgesia is poorly controlled with acetaminophen, salicylates, or an NSAID add…

Answer 37

A weak opioid (e.g., codeine, oxycodone, tramadol, or hydrocodone) can be added to bring about additional pain relief

Question 38

LAOs are believed to be preferable for chronic pain because they

Answer 38

Provide less variation in blood levels and possibly promote a lower propensity for the development of abusive behaviors