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1. Pharmacology > Opiods > Flashcards

Opiods Flashcards

1
Q

Pain

A

Unpleasant sensory and emotional experience with actual or potential tissue damage

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2
Q

Nociceptors (pain receptors)

A

Free nerve ending with cells bodies outside the SC —> certain threshold reached before signal triggered —> threshold reached and signal passes along axon into the SC

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3
Q

What sense pain/ primary target of opioids!

A

Dorsal root ganglion

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4
Q

Opioid receptors and natural pain chemicals

A

Mu (MOP) receptors- endorphins
Kappa (KOP)- dynorphin
Delta (DOP)- encephalin

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5
Q

Opioid receptor locations

A

MOP and KOP- brain, SC and peripheral sensory neurons
DOP- brain and peripheral sensory neurons

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6
Q

Major effect of opioids receptors

A

Analgesia (spinal and supraspinal)

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7
Q

MOP effects

A

Respiratory depression
Decreased GI motility, biliary secretions, urine voiding reflex, uterine contractions
Increased appetite
Euphoria
Antidiuresis
Miosis/ mydriasis
Nausea/ vomiting
Immunimodulation

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8
Q

KOP receptor major effects

A

Decreased GI motility
Increased appetite
Sedation
Diuresis (increased ADH release)
Miosis / mydriasis

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9
Q

DOP receptor major effects

A

Increased appetite
Immunomodulation

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10
Q

Opioids MOA

A

Opioids bind to spinal and supraspinal receptors —> inhibit adenylyl cyclase (decrease CAMP) —> activation of K+ ion channels and hyperpolarization —> inhibits excitatory NT release

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11
Q

Opioid therapeutic uses

A

Analgesia
Sedation
Calming and euphoria
Diarrhea, decreased GI motility
Induction and maintenance of anesthesia

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12
Q

Agonist opioids

A

Morphine
Methadone
Hydromorphone
Fentanyl
Tramadol

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13
Q

Mixed agonist/ antagonist opioids

A

Butorphanol
Buprenorphine

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14
Q

Antagonist/ reversal of opioids

A

Naloxone

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15
Q

Morphine PE

A

Analgesia, emetics , miosis, decreased GI motility

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16
Q

Morphine therapeutic uses

A

Acute pain, anesthetic premedication, antitussive

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17
Q

Adverse effects of morphine

A

Hyperexcitability, hypotension, cerebral hemorrhage or edema
Anaphyloid rx (mast cell degranulation)

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18
Q

Methadone

A

Synthetic OPIOD
Slower elimination than morphine

19
Q

Methadone therapeutic uses

A

Preanesthetic, algesia

20
Q

Methadone adverse effects

A

Sedation, vomiting, constipation, respiratory depression

21
Q

Hydromorphone

A

5x analgesia potency of morphine
Replaced oxymorphone

22
Q

Hydromorphone therapeutic uses

A

Analgesia, preanesthetic and anesthetic

23
Q

Hydromorphone adverse effects

A

Panting (cool down) and bradycardia, dose dependent excitement, cerebral hemorrhage or edema

24
Q

Fentanyl PK

A

More rapid onset than morphine but shorter duration
75-125 x more potent

25
Q

How do you measure fentanyl?

A

MICROGRAMS!!

26
Q

Fentanyl therapeutic uses

A

Analgesia (continuous infusion), anesthetic induction in dogS
Neuroletanalgesia

27
Q

Adverse affects of fentanyl

A

Motor response
Panting, defecation, flatulence, bradycardia, salivation

28
Q

Tramadol

A

Synthetic analog of codeine
MOP agonist (weak) and inhibits serotonin and NE uptake @ synapse

29
Q

Tramadol PK

A

Active metabolite is desmethyltramadol

30
Q

Tramadol therapeutic affects

A

Analgesic, antitussive in dogs and cats

31
Q

Butorphanol

A

Agonist-Antagonist
High affinity for MOP receptors but not activity (antagonist)
High affinity for KOP receptors

32
Q

Butorphanol therapeutic uses

A

Opiod reversal (antagonist), analgesic, antitussive
short duration of efficacy limits its use as a primary

33
Q

Buprenorphine

A

Most generally useful analgesic in dogs and cats (30x potency of morphine)
Longer duration of action than other opiods

34
Q

Buprenorphine MOA

A

High affinity for MOP but only partial agonist
KOP antagonist

35
Q

Buprenorphine therapeutic uses

A

Analgesia for mild to moderate pain in small animals (buccal/ transmucosal admin in cats)

36
Q

Simbadol for Cats

A

Buprenorphine long acting SQ
Slow release SQ prep
Offers 24 hour surgical pain control for cats (1x/day)

37
Q

Zorbium for Cats

A

Buprenorphine Transdermal
First FDA approved long acting transdermal for bupren for cats
4 days, single dose

38
Q

Naloxone

A

Pure opiate antagonist
High affinity for MOP receptors
High doses will reverse DOP and KOP

39
Q

Naloxone PK

A

Duration of action less than agonists
Repeated administration for opioid reversal (monitor and redose)

40
Q

Naloxone therapeutic uses

A

Reversal of opioid induced respiratory depression
Treat shocks (IV and IM, nasal)
Extralabel use in dogs and cats

41
Q

Adverse effects of naloxone

A

CNS sedation
Respiratory and cardiac depression

42
Q

Naloxone contraindicated

A

Shock
Severe cranial trauma and diseases associated with respiratory compromise

43
Q

Continuous opioid use

A

If given longer than 5-7 days they’ll get withdrawal signs (nausea, aggregation, vocalization, vomting, hyperactivity) after discontinuing the drug or antagonist administered

44
Q

Opioid scheduling

A

Morphine and other pure: 2
Bupren: 3
Buto: 4
(2-5, low potential of abuse)

1. Pharmacology (29 decks)

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