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hydromorphone; dihydromorphinone (Dilaudid, Palladone)

Tradenames: Dilaudid, Palladone [5]. DEA-controlled substance: class 2. Indications: 1) management of moderate to severe pain [11] - useful in patients with renal failure [13] - useful in patients with end-stage renal disease 2) cough, antitussive agent at lower doses Dosage: 1) 1-2 mg IV/IM/SC every 4-6 hours (7x as potent as morphine) 2) 2 mg PO* every 4-6 hours. 3) 3 mg PR every 6-8 hours. 4) extended-release* (Palladone) QD dosing Tabs: 1, 2, 3, 4 mg. * Palladone (extended-release) [4] - do NOT chew, crush, dissolve - use ONLY in opiate-tolerant patients Suppositories: 3 mg. * Oral doses 20% to 50% as potent as parenteral administration. marketing & sales suspended due to alcohol interactions [7] Pharmacokinetics: 1) bioavailability 62% 2) metabolized in the liver 3) elimination in the urine as glucuronides - cleared by hemodialysis 4) elimination 1/2 life of 3-4 hours Adverse effects: 1) common (> 10%) - dizziness, lightheadedness, drowsiness, hypotension, anorexia 2) less common (1-10%) - shortness of breath, troubled breathing, tachycardia, weakness, tiredness, bradycardia, flushing of the face, trembling, decreased urination, dry mouth, stomach cramps,headache, nausea/vomiting, nervousness, restlessness, ureteral spasm 3) uncommon (< 1%) - skin rash, hives, hallucinations, mental depression, paralytic ileus 4) other - increased all-cause mortality after 180 days of exposure [10] Drug interactions: 1) CNS depressants 2) phenothiazines 3) tricyclic antidepressants (TCA) 4) alcohol in combination - increased CNS depression - increased release of Palladone resulting in high serum & tissue levels leading to overdose (marketing & sales suspended) [5] Laboratory: 1) methods: GC-MS, GLC, RIA, EIA 2) labs with Loincs - hydromorphone in specimen - hydromorphone in hair - hydromorphone in gastric fluid - hydromorphone in meconium - hydromorphone in saliva - hydromorphone in serum/plasma - hydromorphone in urine - hydromorphone free in blood - hydromorphone free in serum/plasma - hydromorphone free in stool - hydromorphone free in urine - hydromorphone free in vitreous fluid Mechanism of action: opiate

Interactions

drug interactions drug adverse effects (more general classes)

General

opiate opioid receptor agonist (narcotic)

Properties

MISC-INFO: elimination route LIVER 1/2life 1.5-4 HOURS therapeutic-range 1-30 NG/ML toxic-range >100 NG/ML protein-binding 14% pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  4. Prescriber's Letter 12(3): 2005 Palladone (Hydromorphone Extended-release Capsules) Detail-Document#: 210308 (subscription needed) http://www.prescribersletter.com
  5. FDA Medwatch http://www.fda.gov/medwatch/SAFETY/2005/safety05.htm#Palladone
  6. Department of Veterans Affairs, VA National Formulary
  7. Prescriber's Letter 13(2): 2006 Detail-Document#: 220215 (subscription needed) http://www.prescribersletter.com
  8. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  9. Chang AK et al, Safety and efficacy of hydromorphone as an analgesic alternative to morphine in acute pain: A randomized clinical trial. Ann Emerg Med 2006, 48:164 PMID: 16857467
  10. Solomon DH et al. The comparative safety of opioids for nonmalignant pain in older adults. Arch Intern Med 2010 Dec 13/27; 170:1979. PMID: 21149754 - Becker WC, O'Connor PG. The safety of opioid analgesics in the elderly: New data raise new concerns: Comment on "The Comparative Safety of Opioids for Nonmalignant Pain in Older Adults". Arch Intern Med 2010; 170(22):1986-1988. PMID: 21149755 - Papaleontiou M, Henderson CR, Turner BJ, et al. Outcomes associated with opioid use in the treatment of chronic noncancer pain in older adults: a systematic review and meta-analysis. J Am Geriatr Soc 2010; 58(7):1353-1369. Epub 2010 Jun 1. PMID: 20533971
  11. Chang AK et al. Randomized clinical trial of efficacy and safety of a single 2-mg intravenous dose of hydromorphone versus usual care in the management of acute pain. Acad Emerg Med 2013 Feb; 20:185 PMID: 23406078
  12. Pfizer and Acura Announce FDA Approval of Oxectatm (Oxycodone HCL, USP) CII http://www.pfizer.com/news/press_releases/pfizer_press_releases.jsp#guid=20110620005857en&source=RSS_2011&page=1
  13. Medical Knowledge Self Assessment Program (MKSAP) 17, 19 American College of Physicians, Philadelphia 2015, 2021

Component-of

bupivacaine/hydromorphone guaifenesin/hydromorphone