Analgesic Agents- Opioids Flashcards

1
Q

Define ‘Pain’

A

An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage.

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2
Q

Define Nociception

A

Perception of pain or injurious stimuli

-Nociception is the sensory nervous system’s process of encoding noxious stimuli. In nociception, intense chemical (e.g., cayenne powder), mechanical (e.g., cutting, crushing), or thermal (heat and cold) stimulation of sensory nerve cells called nociceptors produces a signal that travels along a chain of nerve fibers via the spinal cord to the brain. Nociception triggers a variety of physiological and behavioral responses and usually results in a subjective experience, or perception, of pain in sentient beings.

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3
Q

Define Allodynia

A

a condition where pain is caused by a stimulus that does not normally elicit pain. For example, bad sunburn can cause temporary allodynia, and touching sunburned skin, or running cold or warm water over sunburned skin can be very painful.

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4
Q

Define Hyperalgesia

A

Increased sensitivity to pain

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5
Q

Define Neuropathic Pain

A

Neuropathic pain is pain caused by damage or disease affecting the somatosensory nervous system

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6
Q

Define Central Sensitization

A

Central sensitization is a condition of the nervous system that is associated with the development and maintenance of chronic pain.
When an animal is repeatedly exposed to a painful stimulus, the animal’s pain threshold will change and result in a stronger pain RESPONSE

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7
Q

Define Analgesia

A

The reduction in the intensity of pain perceived

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8
Q

What are the 4 compartments of the pain pathway that can be targeted for pain management?

A

Transduction (PNS)
Transmission (PNS)
Modulation (CNS)
Perception (CNS)

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9
Q

Define an Opiate and an Opioid

A

Opioids refer to all natural, semisynthetic, and synthetic opioids

Opiates refer to only natural opioids such as heroin, morphine and codeine

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10
Q

What is the mechanism of action of opioids?

A
  • Bind to opioid recepters (OP mu, Kappa, delta)
  • Opioid receptors are G-protein coupled receptors and lead to inhibition of adenylate cyclase and reduction in cAMP
  • Leads to K+ channels opening and an efflux of K+, leading to hyperpolarization
  • Ca+ channels are inhibited, causing reduced transmitter release
  • Ultimately this leads to a decrease of nociceptive impulses
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11
Q

Where in the body are opioids metabolized and excreted?

A

Metabolized: Liver
Excreted: Urine and Bile

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12
Q

Where in the nervous system are the opioid receptors found?

A
  • Brain and CTZ
  • Dorsal horn (sensory)
  • Peripheral terminals of nociceptive afferent neurons
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13
Q

With regards to the pupils, what happens in our domestic species upon administration of opioids?

A

Dogs get pupil constriction

Cats, horses and ruminants get pupil dilation

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14
Q

With regards to thermoregulation, what happens in our domestic species upon administration of opioids?

A

Dogs get a hypothermia

Cats, horses and ruminants get a hyperthermia

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15
Q

What are the effects of certain opioids on the CVS?

A
  • Pethidine/ Morphine: can cause a severe histamine release, which can cause severe vasodilation and death if untreated
  • All opioids (except Pethidine) can cause Bradycardia
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16
Q

What are the clinical signs associated with an overdose of opioids in animals?

A
  • Severe respiratory depression
  • Bradycardia and hypotension
  • Altered mental state: depressed and coma-like
  • Hypothermia
  • Mioisis
  • Death
17
Q

What is the reversal agent to opioids?

A

Naloxone

18
Q

How are opioids classified?

A

Based on the opioid receptor they bind to

Mu, Delta and Kappa

19
Q

List the 4 or 5 Mu receptor agonists

A
  • Morphine
  • Methadone
  • Pethidine
  • Fentanyl
  • Tramadol or Tapentadol: has mild Mu receptor activity

All are, except Ketamine, which is a mu antagonist but kappa agonist

20
Q

What are the actions of Tramadol?

A
  • Mild Mu receptor activity
  • Serotonin reuptake inhibitor
  • Noradrenaline reuptake inhibitor: increases activation of descending inhibitory control pathways in the spinal cord
  • Alpha2 receptor agonist
  • Antagonist of muscarinic receptors
21
Q

Is tramadol an appropriate analgesic in the dog?

A

No, the dog doesnt seem to be able to produce high enough quantities of the active metabolite of Tramadol to receive appropriate pain control

22
Q

Where in the body is Tramadol metabolized and excreted?

A

Metabolized: liver- to the active form (M1)
Excreted: urine

23
Q

What are the side effects that can occur with Tramadol administration?
CNS
GI
CVS

A
  • CNS: Sedation, trembling, ataxia, seizures
  • GI: nausea, vomiting and anorexia
  • CVS: Bradycardia
  • Serotonin Syndrome: IF given with tricyclic antidepressants, serotonin reuptake inhibitors or MAO inhibitors
24
Q

Is Tramadol an appropriate analgesic in cats?

A

Yes, for acute pain

25
Q

What are the actions of Tapentadol?

A
  • Mild Mu receptor activity

- Noradrenaline reuptake inhibitor: increases activation of descending inhibitory control pathways in the spinal cord

26
Q

What are the benefits of using Tapentadol over Tramadol in dogs?

A
  • an appropriate analgesic for acute and neuropathic pain
  • No nausea or vomiting reported
  • Less risk of Serotonin Syndrome

Tapentadol is considered an appropriate analgesic in dogs, meanwhile Tramadol is NOT

27
Q

What drug preparation is available and suitable for wild/zoo species for restraint and surgery?

A

Immobilon: a preparation of etorphine (an opioid) and Acepromazine

28
Q

What is the reversal agent to Immobilon?

A

Animals: Diprenorphine aka Revivon

Humans (in case of accidental exposure): Naloxone

29
Q

Where in the body is Immobilon metabolized and excreted?

A

Metabolized: liver
Excretion: Urine and bile

30
Q

What drug is available and suitable for large game species (elephants and rhinos etc.) for sedation?

A

Carfentanil