methadone (Dolophine, Methadose, Physeptone, Algolysin)

From Aaushi
Jump to navigation Jump to search

Introduction

Tradenames: Dolophine, Methadose. (methadone hydrochloride) DEA-controlled substance: class 2.

Indications

* policies discouraging use of methadone for treating pain have reduced opioid overdoses[16]

Contraindications

pregnancy category = c

pregnancy category = +

safety in lactation = ?

Dosage

* minimum lethal dose is 50 mg; opiate addicts may tolerate > 200 mg

Tabs: 5 & 10 mg; 40 mg tablets (opiate withdrawal only)*

* methadone 40 mg is only available to hospitals & facilities authorized for detoxification & maintenance treatment of patients with opioid addiction

* patients taking methadoned for maintenance treatment are more likely to maintain remission & less likely to experience overdose if they continue methadone[17]

Solution: 5 & 10 mg/5 mL.

Injection: 10 mg/mL (20 mL).

10 mg PO = 30 mg morphine PO

Pharmacokinetics

elimination via liver

1/2life = 15-25 hours

protein binding = 88-90 %

elimination by hemodialysis = -

elimination by peritoneal dialysis = -

Monitor

  • EKG for QTc[8][11] (all patients when daily dose > 30 mg)[17]
    • before treatment begins
    • after 30 days
    • annually during treatment
      • more often if daily dose is > 100 mg, QTc is 450-500 ms, or if unexplained syncope or seizures develop
    • with dose increase
    • consider discontinuation, reducing the dose, or eliminating contributing factors if QTc > 500 ms[13]

Adverse effects

Drug interactions

Laboratory

Mechanism of action

More general terms

Additional terms

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
  6. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
  7. 7.0 7.1 Bruce Ferrell, Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 25-28, 2002
  8. 8.0 8.1 8.2 Ehret GB et al, Drug-induced long QT syndrome in injection drug users receiving methadone: High frequency in hospitalized patients and risk factors. Arch Intern Med 2006; 166:1280 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16801510
  9. Prescriber's Letter 13(9): 2006 Methadone: Focus on Safety Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220902&pb=PRL (subscription needed) http://www.prescribersletter.com
  10. 10.0 10.1 10.2 FDA Medwatch http://www.fda.gov/medwatch/safety/2006/safety06.htm#Methadone
  11. 11.0 11.1 11.2 Krantz MJ et al QTc interval screening in methadone treatment. Ann Intern Med 2009 Jan 20 PMID: https://www.ncbi.nlm.nih.gov/pubmed/19153406
  12. 12.0 12.1 Ansermot N et al. Substitution of (R,S)-methadone by (R)-methadone: Impact on QTc interval. Arch Intern Med 2010 Mar 22; 170:529. PMID: https://www.ncbi.nlm.nih.gov/pubmed/20308640
  13. 13.0 13.1 13.2 13.3 13.4 13.5 Geriatric Review Syllabus, 7th edition Parada JT et al (eds) American Geriatrics Society, 2010
    Geriatric Review Syllabus, 8th edition (GRS8) Durso SC and Sullivan GN (eds) American Geriatrics Society, 2013
  14. 14.0 14.1 14.2 14.3 Centers for Disease Control and Prevention (CDC) Vital Signs: Risk for Overdose from Methadone Used for Pain Relief - United States, 1999-2010 MMWR. July 6, 2012 / 61(26);493-497 http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6126a5.htm
  15. 15.0 15.1 Vallecillo G et al. Risk of QTc prolongation in a cohort of opioid-dependent HIV-infected patients on methadone maintenance therapy. Clin Infect Dis 2013 Aug 14 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23899678 <Internet> http://cid.oxfordjournals.org/content/early/2013/08/14/cid.cit467
  16. 16.0 16.1 Jones CM, Baldwin GT, Manocchio T, White JO, Mack KA Trends in Methadone Distribution for Pain Treatment, Methadone Diversion, and Overdose Deaths - United States, 2002-2014. MMWR Morb Mortal Wkly Rep 2016;65:667-671 https://www.cdc.gov/mmwr/volumes/65/wr/mm6526a2.htm
  17. 17.0 17.1 17.2 NEJM Knowledge+ Pain Management and Opioids: Recharge

Database