Ch 48 Drug Therapy With Opioids

Front 1

Pain

Back 1

unpleasant, sensory, emotional sensation that is associated with actual or potential tissue damage

Front 2

Breakthrough pain

Back 2

episodic bursts of intense pain that “breaks through” the pain control of the medication regime

Front 3

ceiling effect

Back 3

a phenomenon of certain drugs that limits the ability to produce a further effect above a particular dosage level

Front 4

endogenous analgesia system

Back 4

nerve signals that relieve pain by suppressing the transmission of pain signals from peripheral nerves; can be activated by nerve signals entering the brain or by morphine-like drugs

Front 5

endorphins

Back 5

peptides (i.e., endorphins, enkephalins, and dynorphins) that interact with receptors to inhibit perception and transmission of pain signals

Front 6

nociceptors

Back 6

nerve endings that selectively respond to painful stimuli and send pain signals to the brain and spinal cord

Front 7

analgesics

Back 7

drugs that provide pain relief by affecting people’s perception and tolerance of moderate to severe pain.

Front 8

mnemonic device (SOCRATES)

Back 8

* Site
* Onset
* Character
* Radiation
* Associations with other symptoms
* Time course (pattern)
* Exacerbating/relieving factors
* Severity

Front 9

preemptive analgesia

Back 9

used to reduce postsurgical pain by simultaneously administering medications from different drug classes to suppress pain by blocking multiple pain pathways

Front 10

Morphine sulfate

Back 10

Opioid Agonists prototype, an opium alkaloid used mainly to relieve moderate to severe pain

Front 11

Morphine

Back 11

______________ is well absorbed after oral (PO), intramuscular (IM), subcutaneous, and intravenous (IV) administration. PO formulations undergo significant first-pass metabolism in the liver, which means that PO doses must be larger than injected doses to have equivalent therapeutic effects. After PO administration of fast-acting (e.g., immediate-release) formulations, peak activity occurs in about 60 minutes. After IV injection, maximal analgesia and respiratory depression usually occur within 10 to 20 minutes. After IM injection, these effects occur in about 30 minutes. After subcutaneous injection, its effects may be delayed up to 60 to 90 minutes. ______________ is extensively metabolized in the liver, and metabolites are excreted in urine. ______________ is about 30% bound to plasma proteins, and its half-life is 2 to 4 hours. The duration of action is 5 to 7 hours.

Front 12

Morphine

Back 12

relieves pain by binding to receptors in the brain, spinal cord, and peripheral tissues. When bound to the drug, receptors function like gates that close and thereby block or decrease transmission of pain impulses from one nerve cell to the next.

Front 13

major types of receptors

Back 13

mu, kappa, and delta

Front 14

effects of morphine attributed to activation of the mu receptors

Back 14

analgesia; CNS depression, with respiratory depression and sedation; euphoria; decreased gastrointestinal [GI] motility; and physical dependence

Front 15

kappa

Back 15

Analgesia, sedation, and decreased GI motility occur with activation of ______________ receptors.

Front 16

delta

Back 16

The endogenous analgesia system involves the______________ receptors, which may not bind with opioid drugs.

Front 17

Opioid Agonists other drugs in class

Back 17

Codeine fentanyl (Actiq, Duragesic, and others)

Hydrocodone (Lortab, Vicodin)

Hydromorphone (Dilaudid)

Meperidine (Demerol)

Methadone (Dolophine)

Oxycodone (OxyContin)

Oxymorphone (Numorphan, Opana)

Tramadol (Ultram)

Front 18

Opioid Agonists /antagonists other drugs in class

Back 18

Butorphanol (Stadol)

Nalbuphine (Nubain)

Front 19

Pentazocine (Talwin)

Back 19

Opioid Agonists /antagonists Prototype

Front 20

Naloxone (Narcan)

Back 20

Opioid Antagonists Prototype

Front 21

opioid Antagonists Other Drugs in the Class

Back 21

Naltrexone (Depade, ReVia)

Front 22

morphine

Back 22

main indication for __________ is to prevent or relieve acute or chronic pain. Specific conditions for __________ include acute myocardial infarction, biliary colic, renal colic, burns and other traumatic injuries, postoperative states, and cancer. Health care providers usually give__________ for chronic pain, such as that associated with terminal cancer, only when other measures and milder drugs are ineffective.

Front 23

Other clinical uses of morphine include the following:

Back 23

* Before and during surgery to promote sedation, decrease anxiety, facilitate induction of anesthesia, and decrease the amount of anesthesia required
* During labor and delivery (obstetric analgesia)
* Treatment of GI disorders, such as abdominal cramping and diarrhea
* Treatment of acute pulmonary edema
* Treatment of severe, unproductive cough (codeine may be used)
* Unlabeled use: relief of dyspnea associated with acute left ventricular failure and pulmonary edema

Front 24

morphine Use in Older Adults

Back 24

* Start with low doses and increase doses gradually, if necessary.
* Give morphine less frequency than for younger adults because the duration of action may be longer.
* Monitor carefully for sedation or confusion. In addition, monitor voiding and urine output because acute urinary retention is more likely to occur in older adults.

Front 25

Naloxone

Back 25

__________ is known to reverse the effects of morphine.

Front 26

increase

Back 26

Herbs such as kava, valerian, and St. John’s wort may__________ the sedative effect of morphine.

Front 27

Drugs That Increase the Effects of Morphine Sulfate

Back 27

Alcohol
Increases sedation

Antihistamines
Increase sedation and the risk of constipation and urinary retention

Antidepressants
Increase the risk of drowsiness, confusion, memory loss, or respiratory distress

Antipsychotics
Increase the risk of drowsiness, confusion, memory loss, or respiratory distress

Barbiturates
Increase the risk of drowsiness, confusion, memory loss, or respiratory distress

Benzodiazepines
Increase the risk of drowsiness, confusion, memory loss, or respiratory distress

Monoamine oxidase (MAO) inhibitors
Increase the risk of hypotension, respiratory depression, or coma; patients should not take morphine and an MAO inhibitor within 14 days of each other.

Other narcotics or opiates
Increase the risk of hypotension, respiratory depression, or coma

Sedatives
Increase sedation

Front 28

all opioid analgesics

Back 28

The U.S. Food and Drug Administration (FDA) has issued BLACK BOX WARNINGS ♦ for __________ because of the potentially fatal adverse effects of respiratory depression, coma, and death, as well as the risks of drug abuse and dependence.

Front 29

morphine adverse effects

Back 29

profound drowsiness, respiratory depression, hypotension, constipation, and nausea and vomiting

Front 30

morphine

Back 30

With __________ , withdrawal symptoms begin within a few hours of the last dose, reach peak intensity in 36 to 72 hours, and subside over 8 to 10 days.

Front 31

methadone

Back 31

With __________ , withdrawal symptoms begin in 1 to 2 days, peak in about 3 days, and subside over several weeks.

Front 32

naloxone (Narcan)

Back 32

If an antagonist such as __________ is given, withdrawal symptoms occur rapidly and are more intense but of shorter duration.

Front 33

Methadone

Back 33

Another technique is to substitute a long-acting opioid (e.g., __________ ) for a short acting. __________ is usually given in an adequate dose to control symptoms, once or twice daily, and then is gradually tapered over 5 to 10 days.

Front 34

methadone

Back 34

In neonates undergoing withdrawal, __________ or paregoric may be used.

Front 35

Codeine

Back 35

__________ is an opium alkaloid used for analgesic and antitussive effects. This Schedule II drug produces weaker analgesic and antitussive effects and milder adverse effects than morphine.

Front 36

codeine

Back 36

Compared with other opioid analgesics, __________ is more effective when given orally and is less likely to lead to abuse and dependence.

Front 37

codeine

Back 37

The injected __________ drug is more effective than the oral drug in relieving pain, but onset (15–30 minutes), peak (30–60 minutes), and duration of action (4–6 hours) are about the same. Half-life is about 3 hours. Larger doses are required for analgesic than for antitussive effects.

Front 38

Fentanyl

Back 38

__________ (Duragesic, Sublimaze, others) is a potent opioid agonist that is widely used for preanesthetic medication, postoperative analgesia, and chronic pain that requires an opioid analgesic.

Front 39

Fentanyl

Back 39

__________ is commonly given intravenously and may also be given intramuscularly.

Front 40

Ionsys

Back 40

* __________ is for short-term treatment of acute postoperative pain in hospitalized adults who require opioid analgesics. An adhesive skin patch, it uses a tiny electric current to deliver a dose of fentanyl through intact skin and into the bloodstream. The patch, which is placed on the patient’s upper arm or chest, has a button the patient can press for a preset dose of 40 mcg. Only the patient should activate the patch (to avoid overdosing). After removal of the Ionsys patch, serum drug levels decline gradually.

Front 41

Duragesic

Back 41

__________ is for treatment of chronic and severe malignant pain. After deposition of active drug in the skin, systemic absorption slowly occurs. __________ has a slow onset of action (12–24 hours), but it lasts about 72 hours. When a __________ patch is removed, the drug continues to be absorbed from the skin deposits for 24 hours or longer.

Front 42

30 to 60 minutes

Back 42

Sit or lie down at least __________ minutes after receiving an opioid by injection. Injected drugs may cause dizziness, drowsiness, and falls when walking around. If it is necessary to stand up, ask someone for assistance.

Front 43

constipation

Back 43

Avoid __________ , a common adverse effect of opioid analgesics. It may be prevented or managed by eating high-fiber foods, such as whole-grain cereals, fruits, and vegetables; drinking 2 to 3 quarts of fluid daily; and being as active as tolerated.

Front 44

6 to 8

Back 44

Take oral opioid analgesics with __________ ounces of water, with or after food to reduce nausea.

Front 45

Morphine

Back 45

Route:

IV

subcutaneous

intramuscular

oral

rectal

intrathecal

Front 46

Oxycodone

Back 46

No IV form available in the United States.

Oxycodone: morphine 1:1 to 1:1.5

Front 47

Fentanyl patch (Duragesic)

Back 47

Also available in buccal and oral formulations

Front 48

Hydromorphone

Back 48

Sustained-release preparation available

Front 49

Methadone

Back 49

Use only by experienced prescriber is suggested.

Front 50

Hydrocodone (Lortab, Vicodin)

Back 50

__________ , a Schedule III drug, is similar to codeine in its analgesic and antitussive effects. It is available only in oral combination products for cough and with acetaminophen or ibuprofen for pain. Its half-life is about 4 hours, and its duration of action is 4 to 6 hours.

Front 51

Meperidine (Demerol)

Back 51

a synthetic drug similar to morphine in action and adverse effects. After injection, analgesia occurs in 10 to 20 minutes, peaks in 1 hour, and lasts 2 to 4 hours. After an oral dose, about half is metabolized in the liver and never reaches the systemic circulation.

Front 52

meperidine

Back 52

Prescribers order __________ infrequently for therapeutic purposes, mainly because it produces a neurotoxic metabolite (normeperidine). Normeperidine accumulates with chronic use, large doses, or renal failure and produces CNS stimulation characterized by agitation, hallucinations, and seizures. The half-life of normeperidine is 15 to 30 hours, depending on renal function, and the effects of normeperidine are not reversible with opioid antagonist drugs. __________ is not recommended for use in older adults.

Front 53

Methadone (Dolophine)

Back 53

a synthetic drug similar to morphine but with a longer duration of action. It is usually given orally, and onset and peak of action occur in 30 to 60 minutes. Effects last 4 to 6 hours initially and longer with repeated use. Half-life is 15 to 30 hours, and this also lengthens with repeated use.

Front 54

methadone

Back 54

Prescribers order__________ for severe pain and in the detoxification and maintenance treatment of opiate addicts. In 2006, the FDA issued an alert about serious adverse effects (e.g., death, overdose, and serious cardiac dysrhythmias) reported

Front 55

Oxycodone (Roxicodone, others)

Back 55

a derivative of codeine used to relieve moderate pain; its pharmacologic actions are similar to those of other opioid analgesics. It is a Schedule II drug of abuse. With oral administration, action starts in 15 to 30 minutes, peaks in 60 minutes, and lasts 4 to 6 hours. Its half-life is unknown.

Front 56

Oxycodone

Back 56

an agonist narcotic that is used, alone or in combination with acetaminophen, for the treatment of moderate to severe pain. Several years ago, controlled-release tablets (OxyContin) in 10-, 20-, 40-, and 80-mg sizes became available for extended treatment of such pain (only patients who have developed drug tolerance through long-term use of smaller doses should take the 80-mg tablets).

Front 57

Tramadol (Ultram)

Back 57

an oral, synthetic, centrally active analgesic for moderate to severe pain. It is effective and well tolerated in older adults and in people with acute or chronic pain, back pain, fibromyalgia, osteoarthritis, and neuropathic pain.

Front 58

Tramadol (Ultram)

Back 58

Because it has a low potential for producing tolerance and abuse, it may be used long term for the management of chronic pain. It is not chemically related to opioids and is not a controlled drug.

Front 59

Tramadol (Ultram)

Back 59

Its mechanism of action includes binding to mu opioid receptors and inhibiting reuptake of norepinephrine and serotonin in the brain, actions that interfere with transmission of pain signals. Analgesia occurs within 1 hour of administration and peaks in 2 to 3 hours with immediate-release tablets.

Front 60

Tramadol

Back 60

__________ causes significantly less respiratory depression than morphine but may cause other morphine-like adverse effects (e.g., drowsiness, nausea, constipation, orthostatic hypotension).

Front 61

Tramadol

Back 61

available in oral immediate-release tablets alone and in combination with acetaminophen (Ultracet) as well as an extended-release tablet (Ultram ER) that can be given once daily.

Front 62

Opioid agonists/antagonists

Back 62

__________ act on the same pain receptors in the CNS as morphine and other opiates, resulting in interference with pain transmission and/or pain sensation. These agents have agonist activity at some receptors and antagonist activity at others.

Front 63

Pentazocine

Back 63

__________ s well absorbed from the GI tract. After oral administration, onset of significant analgesia usually occurs in 15 to 30 minutes, and the duration of action is usually 3 hours or longer. Concentrations in plasma coincide closely with the onset, duration, and intensity of analgesia. One study found that the time to mean peak concentration in 24 normal subjects was 1.7 hours (range, 0.5–4 hours) after oral administration and that the mean plasma elimination half-life was 3.6 hours (range, 1.5–10 hours).

Front 64

Pentazocine

Back 64

like morphine, __________ has sedative effect. It is a synthetic analgesic with potency that is one third of morphine. Large doses increase blood pressure and heart rate. It weakly antagonizes the analgesic effects of morphine and meperidine. In addition, it produces incomplete reversal of cardiovascular, respiratory, and behavioral depression induced by morphine and meperidine.

Front 65

Pentazocine (Talwin)

Back 65

is used to treat moderate to severe pain. Pentazocine (Talwin NX; a Talwin and naloxone combination) has been shown to be beneficial in managing chronic pain. It is also used before, during, and after surgery for short-term sedating effects.

Front 66

pentazocine

Back 66

The adverse effects of __________ are similar to those of morphine (confusion, respiratory depression, and risk of dependence), but it may be more likely to cause hallucinations.

Front 67

pentazocine

Back 67

Unlike morphine, the respiratory depressant action of __________ is subject to a ceiling effect; this causes no further effect (in this case respiratory depression) above a particular dosage level. The drug can be used as an analgesic for dental extractions except in patients dependent on opioid agonists.

Front 68

pentazocine

Back 68

Caution is necessary when administering to patients with hypothyroidism, adrenocortical insufficiency, prostate hypertrophy, inflammatory or obstructive bowel disease, acute abdominal syndromes of unknown etiology, cholecystitis, pancreatitis, or acute alcohol intoxication and delirium tremens.

Front 69

pentazocine

Back 69

Administration of__________ is by IM and IV injection. Rarely, administration is by subcutaneous injection (lactate). It is essential to give the drug at regular intervals exactly as directed.

Front 70

pentazocine

Back 70

The signs of withdrawal from __________ include tremors and anxiety. The BLACK BOX WARNING ♦ issued for morphine also applies to pentazocine because of its potentially fatal adverse effects of respiratory depression, coma, and death, as well as risks of drug abuse and dependence.

Front 71

pentazocine

Back 71

The nurse ensures that patients are instructed to notify the prescriber if the pain does not disappear, becomes worse, or changes in location or type. Patients should not stop taking __________ abruptly, and they should take care when changing positions quickly or operating equipment that requires mental alertness.

Front 72

An antagonist (antidote)

Back 72

__________ reverses analgesia and the CNS and respiratory depression caused by agonists.

Front 73

opioid antagonist

Back 73

__________ does not relieve the depressant effects of other drugs, such as sedative–hypnotic, antianxiety, and antipsychotic agents. The chief clinical use is to relieve opioid-induced CNS and respiratory depression.

Front 74

Naloxone

Back 74

Therapeutic effects occur within minutes after IV, IM, or subcutaneous injection and last 1 to 2 hours. __________ has a shorter duration of action than opioids, and repeated injections are usually necessary. To combat the effects of a long-acting drug such as methadone, patients may need injections for 2 to 3 days.

Front 75

Naloxone (antidote)

Back 75

__________ reverses analgesia and the CNS and respiratory depression caused by agonists. It competes with opioids for receptor sites in the brain and thereby prevents binding with receptors or displaces opioids already occupying receptor sites. When opioids cannot bind to receptor sites, they are “neutralized” and cannot exert their effects on body cells.

Front 76

Naloxone

Back 76

__________ has long been the drug of choice to treat respiratory depression caused by an overdose of opioids. Given intravenously, naloxone begins to reverse CNS and respiratory depression induced by opioids in minutes.

Front 77

naloxone

Back 77

Critically ill patients who have increased intracranial pressure, seizure disorders, head trauma, or respiratory depression should not receive __________ . However, people with coma of unknown origin may receive the drug to determine if the cause of the mental status change could result from opioids.

Front 78

naloxone

Back 78

Adverse effects of__________ include tremors, drowsiness, sweating, decreased respirations, hypertension, and nausea and vomiting. Naloxone itself has minimal toxicity.