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pharmacology > opioids > Flashcards

opioids Flashcards

1
Q

opium

A

-drugs derived from poppy juice

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2
Q

opiod drugs

A

-mainly synthetic drugs, act as opioid receptors, produce analgesia and other effects used for perioperative and acute pain in vet med

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3
Q

opiates

A

-naturally occuring from opium

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4
Q

narcosis

A

analgesia and stupor bordering on anesthesia

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5
Q

neuroleptanalgesia

A
  • analgesia and amnesiac state produced by administration of neuroleptic and narcotic
  • deep sedation, possible unconciousness
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6
Q

effects of opiods on nociception

A

-perception, modulation, transduction

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7
Q

opioid receptors

A
  • mu, kappa, delta
  • G-coupled protein, inhibition of signal transmission
  • location- brain, spinal cord, endogenous ligand
  • mu: beta endorphins, endomorphins, main effect is analgesia, sedation, respiratory and GI depression
  • kappa- dynorphin main effects are analgesia and sedation
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8
Q

mu 1 and mu 2 receptors

A
  • most common, most affected by opioids
  • supraspinal analgesia- mu 1
  • spinal analgesia- mu 2
  • respiratory depression
  • euphoria
  • sedation
  • GI motility
  • physical dependence
  • brain, spinal cord, joint capsule
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9
Q

kappa receptor

A
  • weakly affected by opioids
  • brain and spinal cord
  • spinal/supraspinal sedation
  • analgesia/antinociception
  • dysphoria
  • GI motility
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10
Q

delta receptor

A
  • spinal/supraspinal antinociception
  • CV depression
  • mild analgesia
  • minimally affected by opiod drugs
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11
Q

full mu agonist (affinity and activity)

A
  • morphine
  • oxymorphine
  • hydromorphine
  • methadone
  • fentanyl
  • remifentanil
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12
Q

partial mu agonist (affinity, partial activity)

A

-buprenorphine

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13
Q

mixed agonist-antagonist- affinity but no activity

A

-K agonist and mu antagonists

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14
Q

full mu agonist

A

naloxone

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15
Q

schedule I drugs

A

-most addictive- heroin

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16
Q

schedule II drugs

A

-full mu agonists, oral drugs in human med

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17
Q

schedule III drugs

A

-buprenorphine, codone with NSAID, hydrocodone

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18
Q

schedule IV drugs

A

butorphanol, tramadol

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19
Q

schedule V drugs

A

-cough suppressants

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20
Q

MOA of opioids

A
  • activation of mu opioid receptor- inhibits excitatory NT release and substance P
  • opioid coupling with membrane-associated Gi/o proteins- hyperpolarization of neurons, block of substance P, decrease in NT activity, decrease of calcium influx
  • inhibit neurotransmission
  • opioid tolerance and resistance of Ca+ channels open in presence of opioid
21
Q

opioid pharmacokinetics

A
  • absorption- readily absorbed from all tissues
  • IV/IM most common routes of administration, commonly given as CRI (fentanyl)
  • SQ/TM (buprenorphine)
  • transdermal (fentanyl patch)
  • epidural (morphine)
  • distribution- widely dist., depends on lipid solubility (morphine one of least lipid soluble), cross specialized barriers (BBB, placenta)
  • metabolism and elimination- mainly conjugation to glucuronic acid (what cats are deficient in so they metabolize slower), metabolites are renally excreted
22
Q

full opioid mu receptor agoinists

A
  • morphine
  • hydromorphone
  • oxymorphone
  • fentanyl
  • cerfantanil/etorphine
23
Q

morphine

A
  • prototypical analgesic, onset 5-15 minutes, lasts several hours, used in epidurals
  • may have histamine release
24
Q

hydromorphone

A

-less histamine released, used in IV instead of morphine, similar onset and duration to morphine

25
Q

oxymorphone

A
  • similar to hydromorphone, may be less emetogenic

- may have smoother sedation in cats and peds

26
Q

fentanyl

A

-potent onset ~1 min, lasts ~30 minutes so suitable for CRI administration, available as transdermal patch

27
Q

cerfantanil/etorphine (M99)

A
  • very potent

- wild life tranquilizer

28
Q

partial opioid mu receptor agonist

A

-Buprenorphine

29
Q

Buprenorphine

A
  • semisynthetic partial mu agonist
  • 30-50% more potent than morphine
  • strongly binds to opioid receptors, not at every site
  • ceiling effect- at certain point dose increases won’t have effect
  • slower onset (about 45 mins), longer duration- up to 8 hrs in cats
  • less apparent adverse side effects
  • IV, IM, SC, TM
30
Q

mixed opioid receptor agonist-antagonist

A

-Butorphanol

31
Q

Butorphanol

A
  • synthetic K agonist and mu antagonist
  • analgesic in dogs, cats, horses, antitussive in dogs
  • lower ceiling effect, visceral pain, less apparent negative effects
  • commonly used in equines
  • IV, IM, SC, PO
  • antitussive effect is greater than pure mu agonist
  • anxiolytic effects in upper airway crisis
  • recovery from anesthesia
32
Q

opiod agonists main effects

A
  • CNS- behavioral changes -depression (dogs), stimulation (cats, horses, ruminants, pigs), interacts with dopamine and NE pathway in brain
  • motor activity- decrease motor area in dogs, increase locomotor in horses
  • thermoregulation- hypothermia in dogs, hyperthermia in cats
  • pupil size- miosis in dogs, mydriasis in cats and horses
  • antitussive
  • dyspnea/excitement
33
Q

opioid agonists- respiratory system

A
  • dose dependent respiratory depression
  • reduced sensitivity to increased CO2
  • decreased respiratory drive, hypoventilation
  • panting in dogs sometimes
  • risk factors for more severe resp effects- ill patients, upper airway obstruction, severe acidemia, use with respiratory depressants
34
Q

CV effects of opioid agonists

A
  • less CV effect than other sedatives
  • dogs:may have bradycardia and hypotension
  • coronary artery vasoconstriciton in dogs
  • cerebral vasodilation and increased intracranial pressure
  • opioids may cause hypotension IV because of histamine release
35
Q

GI effects of opioid agonists

A
  • nausea, vomiting, regurgitation
  • apomorphine–> emetic in dogs, toxic in cats
  • salivation
  • hydromorphone= nausea
  • methadone= less emetogenic
  • ileus and constipation- increase intestinal wall tone, sphincter tone, and non-propulsive rhythmic contractions, decrease propulsive motility
  • delayed gastric emptying, constipation, and ileus
36
Q

urinary tract effects of opioid agonists

A

-urinary retention and increased sphincter tone

37
Q

immunological effects of opioid agonists

A
  • histamine release
  • uticaria
  • WBC funciton and immunity
38
Q

addiction and abuse potential

A

-schedule II-IV

39
Q

opioid agonist clinical uses

A
  • analgesia
  • sedation
  • preanesthetic/ premedication
  • antitussive
  • emetic
  • antidiarrheal
40
Q

full opioid mu agonists

A
  • competitively antagonize opioid agonist effects
  • indications: overdose, toxicity, opioid induced respiratory depression, prolonged anesthetic recovery, imminent cardiac arrest, cardiorespiratory arrest
41
Q

Naloxone

A
  • full opioid mu agonist
  • competitive receptor agonist, reversal of opioid induced adverse effects
  • rapid onset (minutes), short duration (1-2 hrs), repeat dose until gone
  • reverse analgesics as well
42
Q

other opioid antagonists

A
  • naltrexone, diprenorphine

- methylnatrexone- doesn’t cross BBB

43
Q

other opioids

A
  • tramadol
  • hydrocodone
  • apomorphine
  • loperamide
44
Q

tramadol

A
  • weak opioid mu agonist, inhibits serotonin and NE reuptake
  • risk of serotonin syndrome if with MAOIs or SSRIs
  • oral/post op, sometimes IV
  • schedule IV
  • may lower seizure threshold
45
Q

hydrocodone

A
  • antitussive

- schedule II

46
Q

apomorphine

A

emetic in dogs, toxic to cats

47
Q

Loperamide

A

-anti-diarrheal

48
Q

precautions for opioid use

A
  • pre-existing ileus
  • conditions with increased intracranial pressure
  • severe cardiac/hypoventilation
  • renal injury/failure
  • may recover special training
  • history of opioid intolerance/hypersensitivity
  • always address underlying cause of pain
  • full mu agonists may be fully reversed
  • cats can get hyperthermia

pharmacology (5 decks)

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