CHAPTER 24

ANALGESICS

Analgesic group of pain medications each with very different mechanisms
of action for relieving pains of wide array of causes

Drug Classes
a. Opioids (narcotic analgesic) relief of acute pain and in the
management of moderate to severe chronic pain
b. NSAIDs and Acetaminophen most widely used analgesic drugs for
relieving mild to moderate pain and reducing fever
c. Triptans (antimigraine medications) designed and targeted for acute
and abortive treatment of migraine and cluster headaches
d. Analgesic adjuvants new emerging class of analgesics

PAIN AND PAIN MANAGEMENT
Origin of Pain
1. Physiological (Nociceptive) most common often caused by an injury
to body organs or tissues
Source of Pain:
a. Cutaneous pain skin and surface tissues
b. Somatic pain ligaments, tendons, bones, blood vessels
c. Visceral pain body organs and internal cavities
2. Inflammatory pain from an infection or inflammation as a result of
the initial tissue or organ damage
3. Neuropathic pain complex, chronic pain resulting from injury of the
nervous system
- Limb amputation, spiral surgery, viral infections, multiple sclerosis, DM,
AIDS

Acute and Chronic Pain
1. Acute Pain often severe but usually lasts only until the removal of the
source that triggered the pain
- Includes nociceptive, somatic, visceral,postoperative, posttraumatic,
burn, childbirth, HA
2. Chronic Pain pain lasting longer than 6 months that persists even
when the initial cause has been resolved through appropriate medical
intervention
a. Chronic malignant pain CA, HIV, amyotrophic lateral sclerosis,
multiple sclerosis, end-stage organ failure
b. Chronic non-malignant pain lower-back pain, chronic
degenerative arthritis, OA, RA, migraine and chronic HA, bond
pain
- Often associated with behavior and psychological
component making it subjective and is difficult to resolve
- Leading cause of disability among the elderly


Approaches to Pain Management


OPIOIDS
Opioid Receptor Discovery and Endogenous Ligands
1970s Goldstein et al; radiolabeled levorphanol bound stereospecifically to
certain mouse brain fractions which was hypothesized as an opioid receptor
1973 Pert; opioid agonists and antagonists compete for the same binding
site
1975 confirmed the existence of an opioid receptor and intensifies the SAR
studies of the analgesic opioids
*encephalin first endogenous peptide found to be a mixture of 2
pentapeptides (Met-enkephalin and Leu-enkephalin) that only differ in their
amino acids; inhibit contraction of electrically stimulated guinea pig ileum
(GIP) and mouse vas deferens (MVD)

SARs of Enkephalins
Tyr
1

Gly
2

Gly
3

Phe
4

Met
5
/Leu
5

Opioid Receptors


DRUG MONOGRAPHS
1. 4,5-Epoxymorphinans
a. Morphine isolated by Seturner, German Pharmacist in 1806
- Papaver somniferum unripe pod, collect then dry latex
- Morphine, codeine, thebaine, papaverine, noscapine
- Analgesia as its primary use, severe pain
- Metabolized via Phase II conjugation
- IV dose: 3-5mg q 4 hrs
- PO immediate release: 30mg q 4 hrs
- PO sustained release: 30mg q 12-24hrs