Miscellaneous Drugs Flashcards

1
Q

Nontraditional analgesic agents

A

-Classified as adjuvant analgesics
-part of multimodal treatment plan
-used to treat acute and chronic pain

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2
Q

Functions of adjuvant analgesics

A
  1. to potentiate effect of traditional analgesics
  2. To reduce dose and side effects of primary drugs
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3
Q

Chronic Pain definition

A

-Pain persisting longer than normal tissue healing time… pain without apparent biological value

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4
Q

Components of chronic pain

A

`1. inflammatory pain
2. Neuropathic pain

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5
Q

Neuropathic pain

A

-pain caused by a disease of lesion leading to damage and dysfunction of the somatosensory system

Leads to abnormal pain sensations: hyperalgesia and allodynia

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6
Q

Phantom limb pain

A

Common in human amputees (immediately post-op to several years later)
-complex neuropathic pain syndrome
-excessive pain conditions= allodynia and hyperalgesia

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7
Q

Phantom limb pain mechanism

A

Associated with direct nerve injury, central sensitization and changes in cortical recognition of pain and sensitization

-excessive c-fiber firing
-results in ongoing dorsal horn stimulation
-stimulation of NMDA receptors
-development of new sympathetic nerve fibers

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8
Q

Antiepileptic drugs

A

-Gabapentin

-Pregabalin

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9
Q

Gabapentin

A

Structural analogue of GABA with little activity on GABA receptor. Used to treat seizures and neuropathic pain

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10
Q

Gabapentin mechanism

A

1.Blocks calcium influx into presynaptic membrane by inhibition of voltage gated calcium channels
2. results in decreased release of excitatory neurotransmitters

**acts on descending noradrenergic inhibitory system

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11
Q

Gabapentin doses

A

-Dose and frequency varies amojng individuals

-Oral variability is high but variable (dogs: 80%, cats 90-95%)

**pharmacokinetics not linear= means double dose does not equal double the effect because receptors are already saturated

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12
Q

Gabapentin formulations

A

-capsules, tablets, liquids
*avoid formulations with xylitol

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13
Q

Gabapentin half life

A

3-4 hrs

Therefore need 3-20 mg/kg BID-TID
-give every 6-8 hrs to sustain plasma concentrations

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14
Q

Adverse effects of gabapentin

A

**Sedation (and ataxia) is most common side effects BUT improvement of quality of life due to decrease in pain

To minimize side effects, start with lower dose that could be titrated up until a balance between sedation and efficacy

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15
Q

Human gabapentin

A

-evidence it reduces opioid consumption post op OR acute pain

**not proven in animals/vet med but there may be some effect

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16
Q

Pregabalin structure and pharmacokinetics

A

Structurally similar to gabapentin but higher bioavailability. Therefore potentially more effective.

Linear pharmacokinetics- double dose= double effects

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17
Q

Pregabalin effects and dosing

A

Cats: 1-2mg/kg BID
Dogs: 4mg/kg BID

May be linked to sedation

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18
Q

NMDA receptor

A

N-methyl D-asparate receptors
-located in dorsal horn of spinal cord
-activated by excitatory NTs during sustained nociception in dorsal horn
**usually in chronic pain NOT acute

-involved in central sensitization and wind-up effects

19
Q

Amantadine and Ketamine

A

-Can antagonize NMDA receptors and produce antihyperalgesic effects

20
Q

Ketamine

A

-dissociative anesthetic used for anesthesia induction. Subanesthetic dose used for analgesia/antihyperalgesia
**not a classic stand around analgesic
=considered a multimodal anesthesia (combine opiods and other analgesics with ketamine)

21
Q

What receptor effects does ketamine have?

A

-mu-opioid
-muscarinic
-monoaminergic
-GABA receptors

22
Q

Ketamine metabolism

A

metabolized in liver, excreted in kidneys

22
Q

Ketamine use

A

IV as a variable or constant rate infusion (CRI) for pain
-post-op analgesia
-decreased opioid requirements
-chronic management- SQ doses or continuous rate infusions for pain breakthrough

23
Q

Different types of patients for ketamine use

A
  1. chronic pain- intervertebral disc disease, OA, cancer patients
  2. Severe pain procedures (sternotomy, limb and spine procedures)
  3. An adjuvant to opioid analgesics in perioperative analgesic

4.Behavioual side effects

24
Q

Amandatine

A

Antihyperalgesic used with multimodal protocol
-enhances effects of NSAIDs, gabapentin, opioids
-decreases central sensitization

Good oral bioavailability

25
Q

Amandatine treatment

A

-influenza virus A infection and Parkinson’s in humans
-Neuropathic pain

26
Q

Tricyclic antidepressants (TCAs)

A

-Serotonin and NE reuptake inhibitors. They block reuptake of serotonin and NE in CNS resulting in increased concentrations of serotonin and NE in synaptic cleft and enhancing the descending inhibition of nociception

-Antagonize voltage gated Na channels

-NMDA antagonism

27
Q

Side effects of TCAs

A

-sedation
-excitability
-vomiting
-arrthymias
-increased appetite
-weight gain

28
Q

Amitriptyline

A

-serotonin and NE reuptake inhibitor
-3-4 mg/kg every 12 hrs

**TCAs are other inhibitors but no clinical trials and experiments in vet med

29
Q

Acetaminophen (paracetamol)

A

Analgesic and antipyretic effects but weak anti-inflammatory activity
*Analgesic effects not well understood
*antipyretic effects mediated by cerebral COX inhibition

Contraindicated in cats= hepatotoxicity or methemoglobinemia

30
Q

Cannabinoids

A

-sativa or indica products used; reported first use in China

-includes tetrahydrocannabinol (THC) and cannabidol (CBD)

31
Q

THC

A

major psychoactive cannabinoid

32
Q

CBD

A

primary non-psychoactive cannabinoid

33
Q

Endocannabinoid System

A

-Cannabinoid receptor (CB1)
-Cannabinoid Receptor (CB2)
-endogenous ligands (endocannabinoids) including anadamine and 2-arachidonoul glycerol

34
Q

Effects of Endocannabinoid system

A

Lipid signalling system modulates broad range of physiological processes and behaviours

-pain
-mood
-appetite
-emesis
-neuronal activity
-memory
-immunity

35
Q

CBD products

A

-hemp based products
-readily available
-Cannibinoids: group of 60 different active products
-no quality control; varying concentrations, contamination

36
Q

CBD uses

A

-anxiety
-seizures
-anorexia
-vomiting
-pain
-sleep

37
Q

Canine osteoarthritis study with CBD

A

Saw that there was decreased pain and increased activity

2mg/kg was effective, higher doses (8mg/kg) for large dogs is costly

38
Q

Nerve Growth Factor

A

-inflammatory mediator produced by the tissue damage of osteoarthritis

Receptor: tropomyosin kinase A (TrkA)

39
Q

What does NGF binding to TrkA result in?

A

-Elicits release of other inflammatory mediators
-increases nerves sensitivity
-causes phenotypic (physical and biochemical) changes in the nerve.

40
Q

Phenotypic changes in the nerve from NGF binding

A

-increases pain receptors, proinflammatory mediators and ion channel production

-neurogenic inflammations (osteoarthritis pain)

41
Q

Anti-NGF mAbs

A

Use monoclonal antibodies to capture the free NGF

Results in:
-lower amount of NGF available to bind nociceptors
-help normalize changes to nerves seen with chronic pain
-reduce nerve sensitivity and alleviate OA pain

42
Q

Anti-NGF mAbs dosing

A

-need to be species specific with very specific actions

-no significant adverse events associated with treatment

-single SC injection potentially providing 4 weeks pain relief

-non narcotic, non sedating

-function like naturally occurring antibodies

43
Q

Inhalant sparing effects of ketamine

A

allows dose dependent decreases of inhalant anesthetics plus reduction of side effects of inhalant anesthetics