Christian Sinclair, MDKansas City Hospice

& Palliative Care

OpioidsApril 22, 2010

DISCLAIMER

• The information included in this slidedeck is for informational purposes only and should NOT be used to guide individual medical decisions and is NOT a marker of a doctor-patient relationship.

• Please contact your personal doctor regarding any personal health decisions.

Creative Commons

• http://creativecommons.org/licenses/by-nc-sa/3.0/us/

PAIN

SUFFERING

Opioid Receptors

• Mu• Delta• Kappa• ORL-1• All opioid receptors are inhibitory• Pre and post-synaptically

HPCF-USA 2nd ed.

HPCF-USA 2nd ed.

Chronic Opioid Use

• Affects hypothalamic-pituitary fxn– Decreased testosterone/estrogen– Decreased cortisol release– Inhibition of growth hormone– Also impacts immune function

• As quickly as one week

Components of Opium

Name Your Opioids

• Name• Extended Release version?• Route

Codeine

• FDA Indications– Mild-mod pain, cough, diarrhea

• AKA methylmorphine• ‘Weak’ opioid• More constipating than propoxyphene

and tramadol• Must be metabolized by CYP2D6

– Rapid (<10%) and slow metabolizers (40%)

HPCF-USA, Wikipedia

Propoxyphene

• FDA Indications:– Mild-moderate pain

• Synthetic derivative of methadone• Mu and NMDA effects• Effective?• Less drowsiness, dry mouth, n/v• Increases half-life with alprazolam• Increased overdose riskHPCF USA, Wikipedia

Tramadol

• FDA indication: – Mod-sever pain

• Synthetic opioid with serotonin and noepinepherine effects

• Based off codeine so a pro-drug– Converted to M1 (CYP2D6)

• NNT (n-pain) = 3.8 (TCA 2.3)• Equivalent to codeine for cough

Tramadol

• Onset: 30min-1hr• Time to Peak: 2h (SR 4-8hr)• Duration of action: 4-9h• Lowers seizure threshold• Reduced by ondansetron

– Because Zofran blocks….5HT3

• $$$

Hydrocodone

• FDA Indications: mod-sev pain, cough• Less histamine release• Active and prodrug (P450, CYP2D6)

– Hydromorphone

HPCF-USA

HPCF-USA 2nd ed

HPCF-USA 2nd ed

Morphine

Fentanyl Patch

Oxycodone

• Semi-synthetic opioid (thebaine)• Long acting formulation controversial

– And expensive

• Equianalgesic to morphine?– MS 30 = Oxy 20– MS 20 = Oxy 20

ChristianSinclair, MD

csinclair@kchospice.org

References

• HPCF-USA 2nd edition, www.palliativedrugs.com• Dame Cicely Saunders• Eric Cassell, The Nature of Suffering and the

Goals of Medicine.• Ross, J.R., Riley, J., Taegetmeyer, A.B., Sato, H.,

Gretton, S., du Bois, R.M., Welsh, K.I. (2008). Genetic variation and response to morphine in cancer patients. Cancer DOI: 10.1002/cncr.23292

• Nadler et al. The physiologic basis and clinical applications of cryotherapy and thermotherapy for the pain practitioner. Pain Physician. 2004 Jul;7(3):395-9. (free pdf online)

References

• Opioid Conversion Tables, Adapted from Resident and Staff Physician

• Hallenbeck J. Palliative Care Perspectives. Chapter 4. http://www.mywhatever.com/cifwriter/library/70/4932.html

• Mercadante S. Intrathecal treatment in cancer patients unresponsive to multiple trials of systemic opioids. Clin J Pain. 2007 Nov-

Dec;23(9):793-8.