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Analgesics

Pain is an unpleasant sensory (noxious) and


emotional experience associated with actual or
potential tissue damage
Analgesia absence, or reduction of pain in
the presence of a stimulus that would normally
be painful
Analgesic drug that selectively relieves pain by
acting in the CNS or on peripheral pain mechanisms,
Hyperalgesia an increased sensitivity to a
stimulus that is normally painful

Allodynia pain caused by a stimulus that is


not normally painful
Nociception the reception, conduction, and
central nervous processing of nerve signals
resulting in the perception of pain
Somatic pain pain originating from skin,
joints, muscles, and other deep tissues
Visceral pain pain originating from the
internal organs

Types of Pain
Acute Pain

Chronic Pain

Occurs immediately after


a stimulus is received

Persists well past the


initial stimulus (3-6
months)

Responds well to
treatment
Subsides once stimulus
is removed

May or may not respond


well to treatment; may
require a multi-modal
approach
Can result in hyperalgesia

Pain Assessment
You need to be familiar with the species/strain
you are working with to be able to recognize
normal vs. abnormal behavior
Signs of pain will vary not only between various
species, but between strains and individuals
within a species
There is no single sign which will always indicate
a specific amount of pain universally

Signs of Pain
Lethargy
Biting/licking at
injured area
Worried expression
Vocalization
Disuse of limb
Aggression
Hunched posture

Abnormal posture
Ruffled coat
Decreased food/water
consumption
Hiding
Inwardly focused
Disinterest in
environment

Four distinct processes involved in nociception


which can be modulated by analgesics:
1. Transduction translation of the noxious
stimulus into electrical activity at the peripheral
nociceptor
Can be blocked by local anesthetics by injection
either at the site of injury/incision or
intravenously
Can be decreased by use of NSAIDs which
decrease the production of prostaglandins at the
site of injury

2. Transmission the propagation of nerve


impulses through the nervous system
Can be prevented by local anesthetics applied
along peripheral nerves, at nerve plexus, or in
the epidural or subarachnoid spaces
3. Modulation modification of nociceptive
transmission by inhibition of the spinal dorsal
horn cells by endorphins
Can be augmented by injection of local
anesthetics or alpha2-adrenergic agonists;
gabapentin may also effect modulation

4. Perception the final conscious subjective


and emotional experience of pain
Altered by use of general anesthetics or
systemic injection of opioids and/or alpha2agonists
Pre-emptive analgesia: giving analgesics prior
to the noxious stimulus (surgery)
Multimodal or balanced analgesia: using a
combination of analgesics which will impact
more than one portion of the nociceptive
process

Analgesics

Divided into five main classes based on


their modes of action
1.
2.
3.
4.

Opioids
Non-steroidal anti-inflammatory drugs
Local anesthetics
Alpha2-adrenoceptor agonists

OPIOIDS
Narcotic analgesics derived from semi-synthetic
or synthetic sources
Semi-synthetic:
Hydromorphone, Buprenorphine, Hydrocodone,
Oxycodone, Diacetyl morphine (Heroin)
Synthetic:
Methadone, Pethidine, Pentazocine, Fentanyl
OPIATES
Narcotic analgesics derived from opium poppy
plant (natural in origin)
Morphine, Codeine

Classification of Opioids
Full Agonists
Morphine
Methadone
Pethidine (Meperidine)
Fentanyl
Partial Agonists
Codeine
Hydrocodone
Propoxyphene

Classification of Opioids
Mixed Agonist-Antagonist
Buprenorphine
Pentazocine
Antagonists
Naloxone
Naltrexone
Endogenous opioid peptides (Endorphins)
Enkephalins
Dynorphins
-Endorphins

Opioid Analgesics- Effects

Analgesia
Euphoria
Sedation
Emesis
Miosis
Antitussive effect
Release histaminevasodilator

Respiratory centre
Depression
Contraction of smooth
muscle, bladder
sphincter, pyloric
sphincter,
Reduced intestinal
motility
Reduce uterine tone

Functional effects and opioid receptors


Mu

Delta

Kappa

Supraspinal analgesia

+++

Spinal analgesia

++

++

++

Peripheral analgesia

++

++

Respiratory depression +++

++

Miosis

++

GI motility

++

++

Euphoria

+++

Dysphoria

+++

Sedation

++

++

Dependence

+++

Selectivity of Opioid Drugs for receptor


subtypes
Mu

Delta

Kappa

Methadone

+++
++

+
-

+
-

Pethidine

++

Pentazocine

++

Buprenorphine

+++

++

Naloxone

+++

++

Naltrexone

+++

+++

Morphine, Codeine

Agonist + Antagonist +

ADVERSE EFFECTS

Euphoria
Sedation
Nausea and Vomiting
Constipation
Urinary Retention
Tolerance and Dependence
Treatment:
Supportive care
Naloxone

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