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Pharmacology > Ch. 28 > Flashcards

Ch. 28 Flashcards

1
Q

Opiate

A
  • applies only to compounds present in opium
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2
Q

Endogenous Opioid Peptides

A

3 families:

  • enkephalins
  • endorphins
  • dynorphins
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3
Q

Opioid Receptors

A

Mu receptors: Analgesia, respiratory depression, euphoria, sedation, and physical dependence
Kappa receptors: Analgesia and sedation; kappa activation may underlie psychotometic effects seen with certain opioids
Delta receptors

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4
Q

Pure Opioid Agonists

A
  • activate mu receptors and kappa receptors
  • can produce analgesia, euphoria, sedation, respiratory depression, physical dependence, constipations, and other effects
  • morphine: strong opioid agonist and moderate to strong opioid agonists
  • codeine: moderate to strong agonists
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5
Q

Agonist-Antagonist Opioids

A
  • pentazocine, nalbuphine, butorphanol, and buprenorphine
  • when administered alone, produce analgesia
  • if administered, can antagonize analgesia caused by the pure agonist
  • rarely used
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6
Q

Pure Opioid Antagonists

A
  • Nalozone (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 depression caused by overdose with opioid agonists
  • Methylnaltrexone: used to treat opioid-induced constipation
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7
Q

Morphine

A
  • source: seedpod of the poppy plant
  • actions: 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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8
Q

Morphine: Therapeutic Use

A
  • relief of pain
  • without affecting other senses
  • no loss of consciousness
  • relieve pain by mimicking the actions of endogenous opioid peptides, primarily at mu receptors
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9
Q

Morphine: Adverse Effect- Resp. Depression

A

resp. depression:
- infants and elderly are sensitive
- onset: IV, 7 mins; IM, 30 mins; SubQ, 90 mins; may persist 4-5 hours; spinal injection; delayed for hours
- tolerance to resp. depression can develop
- increased depression with concurrent use of other drugs that have CNS depressant actions
- can compromise patients with impaired pulmonary function

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10
Q

Morphine: Constipation

A
  • cause: supressed propulsive intestinal contractions, intensified nonpropulsive contractions, increased ton of 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
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11
Q

Morphine: Othrostatic Hypotension

A
  • morphine-like drugs lower bp by blunting the baroreceptor relfex and by dilating peripheral arterioles and veins
  • patient teaching: symptoms of hypotension (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
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12
Q

Morphine: Urinary Retention and Hesitancy

A
  • increases tone in bladder sphincter
  • increases tone in detrusor muscle, thereby elevating pressure within bladder and causing sense of urinary urgency
  • may interfere with voiding by suppressing awareness of bladder stimuli
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13
Q

Morphine: Cough Supression

A
  • acts at opioid receptors in the medulla to suppress cough
  • suppression of spontaneous cough ma lead to the accumulation of secretion in airway
  • patients should be instructed to actively cough at regular intervals
  • codeine-based and hydrocodone-based cough remedies
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14
Q

Morphine: Biliary Colic

A
  • induces spasm of common bile duct
  • epigastric distress to biliary colic
  • may intensify rather than relieve pain in patients with pre-existing biliary colic
  • meperidine causes less smooth muscle spasm than morphine
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15
Q

Morphine: Emesis

A
  • promotes nausea and vomiting through direct stimulation of chemoreceptor trigger zone of medulla
  • emetic reactions are greatest with initial dose and then diminish
  • nausea and vomiting is uncommon in recumbent patients but occur 15%-40% of ambulatory patients
  • can be reduced by pretreatment with an antimetic and by having patient remain still
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16
Q

Morphine: Elevation of Intracranial Pressure

A
  • supressed resp., morphine increases carbon dioxide content of blood, which dilates cerebral vasculuature and causes intracranial pressure to rise
  • if resp. is maintained at a normal rate, intracranial pressure will remain normal
17
Q

Morphine: Euphoria/Dysphoria

A
  • exaggerated sense of well-being caused by activation of mu receptors
  • a sense of anxiety and unease; uncommon among patients in pain, but may occur when morphine is taken in absence of pain
18
Q

Morphine: Sedation

A
  • drowsiness and some mental clouding

- avoid hazardous activities

19
Q

Morphine: Miosis

A
  • cause pupilary constriction
  • toxic doses: pupils constrict to pinpoint size
  • bright lights
20
Q

Morphine: Neurotoxicity

A
  • delirum, agitation, hyperalgesia
  • renal impairment, prolonged high-dose opioid use
  • manage: hydration and dose reducation
21
Q

Adverse Effects From Prologned Morphine Use

A
  • hormonal changes: declinein cortisol levels, increase in prolactin, decrease in LH and FH, testosterone and estrogen
  • altered and suppressed immune function
22
Q

Morphine: Pharacokinetics

A
  • admin by several routes
  • not very lipid-soluble
  • does not cross BBB easily
  • only small fraction of each dose reaches site of analgesic action
23
Q

Morphine: Tolerance

A
  • increased doses needed to obtain same response
  • develops with analgesia, euphoria, sedation, and resp. depression
  • cross-tolerance to other opioid agonists
  • no tolerance to miosis or constipation develops
24
Q

Morphine: Physical Dependence

A
  • abstinence sydnrome with abrupt discontinuation
  • about 10 hours after last dose, the intial reaction occurs and includes yawning, rhinorrhea, and sweating
  • progressing to sneezing, weakness, nausea, vomiting, diarhea, abdominal crmaps, bone and muscle pain, spasms, and kicking movements
  • lasts 7-10 days if untreated
  • withdrawl is unpleasent but not lethal
25
Q

Morphine: Drug Interactions

A
  • CNS depressants: intesnify sedation and resp. depression
  • Anticholinergic drugs
  • Hypotensive drugs
  • MAO inhibitors
  • agonist-anatagonist opiods
  • opioid antagonist
26
Q

Morphine: Toxicity

A
  • clinical manifestation: classic triad (coma, resp. depression, pimpoint pupils)
  • treat: vent support; anatagonist (Narcan)
  • guidelines: monitor vital signs before giving, give on a fixed schedule
27
Q

Codeine

A
  • 10% converts to morphine in liver
  • pain and cough supression
  • orally usually
28
Q

Oxycodone

A
  • analgesic actions = to those of codeine
  • long-acting analgesics
  • immediate release
29
Q

Fentanyl

A
  • 100x more potent than morphine
30
Q

Dosing Guidelines

A
  • assessment of pain: should be evaluated before opioid admin and about 1 hour after
  • dosage determination: opioid analgesic must be adjusted to accomodate individual variation
  • dosing schedule: as a rule, opioid should be admin on a fixed schedule
  • avoiding withdrawal
31
Q

Clinical Use of Opioids

A
  • physical dependence: state in which an abstinence sydnrome will occur if the dependence-producing drug is abruptly withdrawn; it is NOT equated with addiction
  • abus: drug use that is inconsistent with medical social norms
  • addiction: behaviour pattern characterized by continued use of a psychoactive substance despite physical, psychologic, or social harm
32
Q

Patient-controlled analgesia

A
  • drug selection and dosage regulations
  • comparision of patient-controoled analgesia with traditional intramuscular therapy
  • IM painful to patient; cause negative side effects (bruising and hematoma formation)
  • patient education and family education
33
Q

Indications for Clinical Use

A
  • postoperative pain
  • obstetric analgesia
  • myocardinal infarction
  • head injury
  • cancer-related pain
  • chronic noncancer pain
34
Q

Opiod Anatagonist: Principle Use

A
  • treat opioid overdose and relief of opiod-induced constipation
  • reversal of postoperative opioid effects
  • reversal of neonatal resp. depression
  • management of opiod addiction
35
Q

Pure Opioid Antagonists

A
  • Narcan (Naloxone)
36
Q

Naloxone

A
  • action: competitive antagonist
  • pharmacolgic effects
  • pharmacokinetics
  • therapeutic uses: reversal of opioid overdose; reversal of postoperative opioid effects; reversal of neonetal resp. depression (during labour and delivery)
37
Q

Naltrexone

A
  • pure opiod antagonist
  • opioid and alcohol abuse
  • opioid abuse: prevents euphoria if abuser takes and opiod
  • candidates for treatment must be rendered opioid free before naltrexone is started
  • does not prevent craving for opioids
38
Q

Nonopioid Centrally Acting Analgesics

A
  • relieve pain by mechanism largely or completely unrelated to opioid receptors
  • do not cause resp. depression, physical dependence or abuse
  • not regulated under controlled substances act
    ex. Tramadol (suicide risk), Clonidine, Ziconotide, Dexmedetomidine

Pharmacology (21 decks)

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