Journal List > J Korean Orthop Assoc > v.55(1) > 1142182

Se-Jin, Woo, and Taedong: Opioids and Antidepressants for Pain Control in Musculoskeletal Disease

Abstract

The progression of aging and the increase in musculoskeletal diseases have led to an increase in invasive treatment methods, including various surgical methods, but conservative treatment should be attempted before surgical treatment in musculoskeletal diseases. Medication for pain control, such as acetaminophen, non-steroidal anti-inflammatory drugs, steroid, opioids, antidepressants, etc., is one of the most popular methods for pain control. If the pain receptors on peripheral organ are stimulated, pain is transmitted to the brain by the ascending pathway, and the brain then secretes endogenous opioids, such as endorphin, by the descending pathway for pain control. Opioids are substances that act on the opioid receptors, and there are three receptors for opioids. The affinity for each receptor varies according to the tissue and the patient’s systemic status. Antidepressants work on the synapses in the central nervous system and its main mechanism is regulation of the ascending pathway. This is mainly effective in chronic pain and neuropathic pain, which is similar in effectiveness to opioids. This review focuses on the effectiveness, method of use, and side effects of opioids and antidepressants.

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Table 1.
Types and Effects of Opioids
Opioid Conversion factor
Codeine (mg) 0.15
Fentanyl transdermal (mg/h) 2.4
Hydrocodone (mg) 1
Hydromorphone (mg) 4
Methadone (mg)
1–20 mg/d 4
21–40 mg/d 8
41–60 mg/d 10
≥61–80 mg/d 12
Morphine (mg) 1
Oxycodone (mg) 1.5
Oxymorphone (mg) 3
Tapentadol (mg) 0.4
Table 2.
Type, Specificity, and Distribution of Opioid Receptor
Receptor type Receptor distribution (musculoskeletal system) Specificity
m-opioid receptor Synovium, articular cartilage The main receptor on which opioid work. The action of morphine and narcotic analgesics used clinically in moderate, severe, acute and chronic pain is the major agonist of mu receptors.
d-opioid receptor Synovium The expression of d-opioid receptor in the synovium of knee joints from patients with RA and OA was demonstrated. The density of d-opioid receptor immunoreactive nerve fibers was significantly greater in RA and OA synovium than on normal synovium.
k-opioid receptor Synovium k-opioid receptor were detected in normal human fibroblast-like synoviocytes. Although there is still limited information on the occurrence and distribution of k-opioid receptor in musculoskeletal tissues, pharmacological evidence on the presence and activation of peripheral k-opioid receptor located in arthritic joint tissues comes from preclinical studies. than on normal synovium.

RA, rheumatoid arthritis; OA, osteoarthritis.

Table 3.
Types and Dose of Antidepressants
Antidepressants Dose
TCAs  
  Amitriptyline 10–75 mg at bedtime
  Nortriptyline 10–50 mg at bedtime
  Imipramine 10–50 mg at bedtime
  Desipramine 10–50 mg at bedtime
  Doxepin 10–75 mg at bedtime
SNRI  
  Milnacipran 25–50 mg twice a day
  Duloxetine Maximum 30 mg twice a day
SSRI  
  Fluoxetine 5 mg/Kg/d

TCAs, tricyclic antidepressants; SNRI, serotonin-norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor.

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