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Adv Pharm > Chapter 24: Opioid Analgesics, Opioid Antagonist, and Nonopioid Centrally Acting Analgesics > Flashcards

Chapter 24: Opioid Analgesics, Opioid Antagonist, and Nonopioid Centrally Acting Analgesics Flashcards

1
Q

analgesics and opioids

A

Analgesics are drugs that relieve pain without causing the loss of consciousness​

Opioids are the most effective pain relievers available​

​

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2
Q

opioid

A

A general term that is defined as any drug, natural or synthetic, that has actions similar to those of morphine

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3
Q

opiate

A

A term that applies only to compounds present in opium

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4
Q

endogenous opioid peptides

A

Three families of peptides​:

Enkephalins​

Endorphins​

Dynorphins​

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5
Q

opioid receptors

A

Three main classes of opioid receptors​

Mu receptors: Analgesia, respiratory depression, euphoria, sedation, and physical dependence​

Kappa receptors: Analgesia and sedation; kappa activation may underlie psychotomimetic effects seen with certain opioids​

Delta receptors​

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6
Q

Classification of Drugs That ​
Act as Opioid Receptors​

A

Agonist, partial agonist, or antagonist​:

Pure opioid agonists​

Agonist-antagonist opioids​

Pure opioid antagonists

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7
Q

Pure Opioid Agonists​

A

Activate mu receptors and kappa receptors​

Can produce analgesia, euphoria, sedation, respiratory depression, physical dependence, constipation, and other effects​

2 groups: strong and mod-to-strong agonist:

Morphine: Strong opioid agonists and moderate to strong opioid agonists​

Codeine: Moderate to strong agonists

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8
Q

Agonist-Antagonist Opioids​

A

Pentazocine, nalbuphine, butorphanol, and buprenorphine​

When administered alone, produce analgesia​

If administered with a pure opioid agonist, can antagonize analgesia caused by the pure agonist

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9
Q

Pure Opioid Antagonists​

A

Naloxone [Narcan]: Prototype of the pure opioid antagonists​

Antagonists at mu and kappa receptors​

Do not produce analgesia or any of the other effects caused by opioid agonists​

Reversal of respiratory and central nervous system (CNS) depression caused by overdose with opioid agonists​

Methylnaltrexone: Used to treat opioid-induced constipation​

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10
Q

basic pharm of the opioids

A

Strong opioid agonists​:
Morphine​
Other strong opioid agonists​

Moderate to strong opioid agonists​

Agonist-antagonist opioids​

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11
Q

source of morphine

A

Seedpod of the poppy plant​

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12
Q

morphine: overview of pharm actions

A

Pain relief​

Drowsiness​

Mental clouding​

Anxiety reduction​

Sense of well-being

Respiratory depression​

Constipation​

Urinary retention​

Orthostatic hypotension​

Emesis​

Miosis​

Cough suppression​

Biliary colic​

Tolerance and physical dependence​​

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13
Q

morphine therapeutic use

A

Relief of pain​ -mod to severe. post-op pain, L&D pain, chronic pain caused by cancer and other conditions.

more effective against constant, dull pain than against sharp, intermittent pain. however, sharp pain can be relieved by large doses

Relieves pain without affecting other senses (e.g., sight, touch, smell, and hearing)​

No loss of consciousness​

Relieves pain by mimicking the actions of endogenous opioid peptides, primarily at mu receptors​

sched 2

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14
Q

morphine ADR: resp depression

A

Infants and the elderly are especially sensitive​

Onset: ​
Intravenous, 7 minutes; intramuscular, 30 minutes; subcutaneous, up to 90 minutes; may persist 4 to 5 hours​
Spinal injection: Response may be delayed by hours​
PO: 90 min

Tolerance to respiratory depression can develop​

Increased depression with concurrent use of other drugs that have CNS depressant actions (e.g., alcohol, barbiturates, and benzodiazepines) ​

Can compromise patients with impaired pulmonary function ​

Asthma, emphysema, kyphoscoliosis, chronic cor pulmonale, and extreme obesity​

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15
Q

morphine ADR: constipation

A

Cause: Suppressed propulsive intestinal contractions, intensified nonpropulsive contractions, increased tone of the anal sphincter, and inhibited secretion of fluids into the intestinal lumen​

Complications of constipation include fecal impaction, bowel perforation, rectal tearing, and hemorrhoids​

Treatment includes physical activity, increased intake of fiber and fluids, stimulant laxatives, stool softeners, and polyethylene glycol

last resort: methylnaltrexone -cant cross BBB so won’t reverse pain relief

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16
Q

morphine ADR: ortho hypotension

A

Morphine-like drugs lower blood pressure by blunting the baroreceptor reflex and by dilating peripheral arterioles and veins​

Patient teaching: Symptoms of hypotension (e.g., lightheadedness and dizziness) and instructions to sit or lie down if they occur​

Hypotension can be minimized by moving slowly when changing from a supine or seated position to an upright position​

hypotensive medications can exacerbate opioid induced hypotension

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17
Q

morphine ADR: urinary retention and hesitancy

A

Increases tone in the bladder sphincter​

Increases tone in the detrusor muscle, thereby elevating pressure within the bladder and causing a sense of urinary urgency​

May interfere with voiding by suppressing awareness of bladder stimuli​

encourage pt to void every 4 hr

likely in pt with BPH. anticholinergic meds can exacerbate

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18
Q

morphine ADR: emesis

A

Promotes nausea and vomiting through the direct stimulation of the chemoreceptor trigger zone of the medulla​

Emetic reactions are greatest with the initial dose and then diminish with subsequent doses​

Nausea and vomiting are uncommon in recumbent patients but occur in 15% to 40% of ambulatory patients​

Nausea and vomiting can be reduced by pretreatment with an antiemetic (e.g., prochlorperazine) and by having the patient remain still

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19
Q

morphine ADR: euphoria/dysphoria

A

Euphoria: An exaggerated sense of well-being caused by the activation of mu receptors​

Dysphoria: A sense of anxiety and unease​

Dysphoria is uncommon among patients in pain, but it may occur when morphine is taken in the absence of pain​

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20
Q

morphine ADR: sedation

A

Drowsiness and some mental clouding​

Avoid hazardous activities​

Sedation can be minimized:​
Take smaller doses more often ​
Use opioids that have short half-lives​
Give small doses of a CNS stimulant (e.g., methylphenidate or dextroamphetamine)​
Nonamphetamine stimulants such as modafinil [Provigil, Alertec] or armodafinil [Nuvigil] may also be tried​

​

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21
Q

morphine ADR: neurotoxicity

A

Delirium, agitation, myoclonus, hyperalgesia, and other symptoms​

Risk factors include renal impairment, preexisting cognitive impairment, and prolonged high-dose opioid use​

Management: Hydration and dose reduction​, opioid rotation for long term user is helpful

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22
Q

morphine ADR: tolerance

A

Tolerance​

Increased doses needed to obtain the same response​

Develops with analgesia, euphoria, sedation, and respiratory depression​

Cross-tolerance to other opioid agonists​

No tolerance to miosis or constipation develops

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23
Q

morphine ADR: physical dependence

A

Abstinence syndrome with abrupt discontinuation​

About 10 hours after last dose, the initial reaction occurs and includes yawning, rhinorrhea, and sweating​

Progresses to violent sneezing, weakness, nausea, vomiting, diarrhea, abdominal cramps, bone and muscle pain, muscle spasms, and kicking movements​

Lasts 7 to 10 days if untreated​

Withdrawal is unpleasant but not lethal, as it may be with CNS depressants

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24
Q

morphine pharmakinetics

A

Administered by several routes: oral, intramuscular, intravenous, subcutaneous, epidural, and intrathecal​

Not very lipid-soluble​

Does not cross blood-brain barrier easily​

Only small fraction of each dose reaches site of analgesic action​

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25
Q

morphine precautions

A

Abuse liability​

Use cautiously in pt with:
Decreased respiratory reserve​
Pregnancy​
Labor and delivery​
Head injury​
Other precautions

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26
Q

morphine drug interactions

A

CNS depressants​

Anticholinergic drugs​

Hypotensive drugs​

Monoamine oxidase inhibitors​

Agonist-antagonist opioids​

Opioid antagonists​

Other interactions​

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27
Q

morphine toxicity s/sx

A

Classic triad​:

Coma​

Respiratory depression​ -may be as low as 2-4 breath/min

Pinpoint pupils -can dilate secondary to resp depression

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28
Q

morphine tox tx

A

Ventilatory support​

Antagonist: Naloxone [Narcan]

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29
Q

morphine admin general guidelines

A

Monitor vital signs before giving​

Give on a fixed schedule​

30
Q

morphine: general guidelines for dosage and admin

A

​

Morphine/naltrexone [Embeda]: Designed to discourage morphine abuse​

Dosage and routes of administration​
Oral​
Intramuscular and subcutaneous​
Intravenous​
Epidural and intrathecal​
Extended-release liposomal formulation [DepoDur]​

31
Q

fentanyl [Duragesic, Abstral, Actiq, Fentora, Onsolis, Lazanda, Subsys]

A

100 times the potency of morphine​

Formulations given via three routes​:
Parenteral ​
Surgical anesthesia

Transdermal [Duragesic]​ -Patch: Heat acceleration​, Iontophoretic system: Needle-free

Transmucosal​
Lozenge on a stick [Actiq]​
Buccal film [Onsolis]​
Buccal tablets [Fentora]​
Sublingual tablets [Abstral]​
Sublingual spray [Subsys]​

sched 2

32
Q

codeine: actions and uses

A

10% converts to morphine in liver​

Pain (mild to mod) and cough suppression​ (sch 5)

Preparations, dosage, and administration​
Usually oral (formulated alone or with aspirin or acetaminophen)​
30 mg produces same effect as 325 mg of acetaminophen​

metabolized by p450 system in liver

tox to breast fed infants whose mothers take codeine

sched 2
combo sched 3

33
Q

oxycodone

A

Analgesic actions equivalent to those of codeine​

Long-acting analgesics​:
Immediate-release ​
Controlled-release [OxyContin]​
Abuse: Crushes and snorts or injects medication​
2010 OP formulation much harder to crush and does not dissolve into an injectable solution to decrease risk of abuse​

high risk for abuse

sched 2

34
Q

hydrocodone

A

Most widely prescribed drug in the United States​

pain relief and cough suppressant

Combined with aspirin, acetaminophen, or ibuprofen​

sched 2

35
Q

tapentadol

A

Analgesic effects equivalent to oxycodone​n (mod to severe pain)

Causes less constipation than traditional medications​

blocks reuptake of NE

high abuse potential

sched 2

36
Q

Pentazocine

A

agonist (K receptors) -antagonist (mu receptors) opioid
mild - mod pain
less effective than morphine

resp depression is limited, produces little to none euphoria

low potential for abuse

sched 2-5 depending on state

if admin to a pt physically dependent on pure agonist, will withdrawal

physically dependence can occur

reversed with naloxone

37
Q

nalbuphinal

A

opioid agonist-antagonist
IM, IV, SQ

38
Q

Buprenorphine

A

IM, IV
agonist (mu) antagonist (k)
if admin to a pt physically dependent on pure agonist, will withdrawal
prolongs QT
sched III
7-day patch: Butrans​
Sublingual film: Suboxone

39
Q

Butorphanol

A

agonist antagonist
nasal spray

40
Q

pain assessment

A

Pain assessment​

Essential component of management​

Based on patient’s description​

Evaluate:​
Pain location, characteristics, and duration​
Things that improve or worsen pain​
Status before taking drug and 1 hour after​

41
Q

dosing guideline

A

Assessment of pain​
Pain status should be evaluated before opioid administration and about 1 hour after​

Dosage determination​
Opioid analgesics must be adjusted to accommodate individual variation​
start lowest dose
Using a standard 10 mg dose of morph only 70% of adults will have pain relief
older adults metabolize slowly and need lower doses
newborns need smaller dose dt immature BBB

Dosing schedule​
As a rule, opioids should be administered on a fixed schedule​
want lowest effective dose for shortest time possible
as pain diminishes, switch to nonopioid analgesic (asa, tyl)

Avoiding withdrawal​
when opioids are admin in high doses for 20 days or more, physical dependence may develop. under these conditions abstinence syndrome will develop, to min opioid to be withdrawn slowly by tapering the dose over 3 days. if the degree of dependence is high, withdrawn over 7-10 days. ​

42
Q

physical dependence

A

State in which an abstinence syndrome will occur if the dependence-producing drug is abruptly withdrawn; it is NOT equated with addiction​

Withdrawal drug over longer period of time

43
Q

abuse

A

Drug use that is inconsistent with medical or social norms

before prescribing, identify at risk abuse pt using NIDA-modified ASSISR. next become familiar with state prescription drug monitoring program (see all drugs prescribed to pt, who prescribed and how much). check this at initiation of tx and periodically thruout. before starting therapy, get a urine drug test.

in ohio, every script requires DEA number and to be registered with DEA in order to scribe sch 2 and above.

OAARs -run pt thru before writing script

44
Q

addiction

A

Behavior pattern characterized by continued use of a psychoactive substance despite physical, psychologic, or social harm​

45
Q

pt education for opioids

A

Balance the need to provide pain relief with the desire to minimize abuse​

Minimize fears about the following:​
Physical dependence​
Addiction​

46
Q

prescribing guidelines for opioids

A

use opioids only after nonopioids fail
discuss benefits and risks of long term opioid tx
use only 1 prescriber and 1 pharm
ensure comp follow up to assess efficacy and SE and monitor for abuse
stop opioids after an attempt at opioid rotation has produced inadequate benefit
fully document the entire process

47
Q

PCA

A

Patient-controlled analgesia devices​

Drug selection and dosage regulations​ exist -monitor

Comparison of patient-controlled analgesia with traditional intramuscular therapy​ -pt feel more in control with PCA
Multiple intramuscular injections: Painful to the patient; cause negative side effects, including bruising and hematoma formation​

Patient education​ and Family education​ are a good thing

48
Q

Using opioids in specific settings​

A

Postoperative pain​

Obstetric analgesia​

Myocardial infarction​

Head injury​

Cancer-related pain​

Chronic noncancer pain

49
Q

REMs

A

Risk evaluation and mitigation strategy (REMS)​

Developed by the U.S. Food and Drug Administration​

Designed to reduce opioid-related injuries and deaths​

central component to edu prescriber and pt -edu all providing care for pt in pain

50
Q

principal uses for opioid antagonists

A

Treatment of opioid overdose and relief of opioid-induced constipation​

Reversal of postoperative opioid effects​

Reversal of neonatal respiratory depression​

Management of opioid addiction​

51
Q

naloxone therapeutic uses

A

Reversal of opioid overdose​
Drug of choice with pure opioid agonist overdose​
Titrated cautiously with physical dependence​

Reversal of postoperative opioid effects​
Titrated to achieve adequate ventilation and to maintain pain relief
​
Reversal of neonatal respiratory depression​
Opioids given during labor and delivery may cause respiratory depression in neonate​

52
Q

naloxone prep and admin

A

IM or SQ
onset 2-5 min
duration several hours
half-life 2 hr (may need repeat doses)
cant be given orally dt first pass
careful titration to prevent abrupt withdrawal
may need higher doses to reverse agonist-antagonist tox

53
Q

Methylnaltrexone

A

Selective opioid antagonist​

Treatment of opioid-induced constipation in late-stage disease for patients receiving constant opioids​

Block mu opioid receptors in the gastrointestinal tract​

54
Q

Alvimopan

A

Peripherally acting mu opioid antagonist developed​

Counteracts the adverse effects of opioids on bowel function​

Does not reduce opioid-mediated analgesia: Limited ability to cross the blood-brain barrier​

Short-term therapy of opioid-induced ileus after partial small or large bowel resection with primary anastomosis​

55
Q

naltrexone

A

Pure opioid antagonist​

Opioid and alcohol abuse​

Opioid abuse: Prevents euphoria if the abuser takes an opioid​

Candidates for treatment must be rendered opioid free before naltrexone is started​

Does not prevent craving for opioids​

PO or IM

can cause hepatocellular injury with excessive dosage, contraindicated for hepatitis pt, educate pt on r/o liver injury and signs of hepatitis

less effective than methdone (suppresses cravings and euphoria)

56
Q

nonopioid centrally acting analgesics

A

Relieve pain by mechanisms largely or completely unrelated to opioid receptors​

Do not cause respiratory depression, physical dependence, or abuse​

Not regulated under the Controlled Substances Act​

Tramadol [Ultram]​

Suicide risk​

Clonidine [Duraclon]​

Ziconotide [Prialt]​

Dexmedetomidine [Precedex]​

57
Q

tramadol MOA

A

weak agonist activity at mu receptors. block uptake of NE and serotonin, thereby activating monoaminergic spinal inhibition of pain. BC of this, naloxone only partially blocks effects

58
Q

tramaol therapeutic uses

A

mod- mod severe pain
less effective than morphine, more effective then codeine combo

59
Q

tramadol ADRs

A

resp depression min
sedation, dizziness, HA, dry mouth, constipation
sz

60
Q

tramadol drug interactions

A

intensify responses to CNS depressants (alc, benzo)
hypertensive crisis with MAOI
serotonin syndrome with SSRI, SNRI, TCA, MAOIs

61
Q

abuse liability of tramadol

A

very low
sched 4

62
Q

tramadol prep, dosage, and admin

A

PO IM onset 1 hr, peak 2 hr, duration 6 hr. half life 5-6 hr
PO ER

63
Q

clonidine

A

Treatment of hypertension and relief of severe pain​

Mechanism of pain relief​
Alpha2-adrenergic agonist​

Analgesic use​
Used in combination with opioid analgesics​

Adverse effects​
Cardiovascular: Severe hypotension, rebound hypertension, and bradycardia​

Contraindication: hypot​ension

​

64
Q

Ziconotide MOA

A

Selective antagonist at N-type voltage-sensitive calcium channels on neurons​

Blocks calcium channels on primary nociceptive afferent neurons in dorsal horn of the spinal cord​

65
Q

Ziconotide pharmakinetics

A

Distributed through cerebrospinal fluid and then transported to systemic circulation

66
Q

Ziconotide ADRs

A

CNS and muscle injury​

67
Q

Ziconotide drug interactions

A

Formal studies not done​

68
Q

Ziconotide prep, dosage, admin

A

Intrathecal administration

69
Q

Dexmedetomidine

A

Selective alpha2-adrenergic agonist​

Acts in the CNS to cause sedation and analgesia​

70
Q

Dex uses

A

Short-term sedation in critically ill patients who are initially intubated and undergoing mechanical ventilation​

Sedation for nonintubated patients before or during surgical and other procedures​

71
Q

dex ADRs

A

Hypotension​

Bradycardia

Adv Pharm (76 decks)

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