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Narcotic Analgesic
Aka: Narcotic Analgesic, Opioid Analgesic, Narcotic, Opioid, Opiate, Opioid Abuse Deterrent Agent, Opioid Metabolism
- See Also
- Morphine Milligram Equivalent
- Analgesic
- Pediatric Analgesic
- Acute Pain Management
- Opioid Prescription in Acute Pain
- Opioid Overdose
- Opioid Abuse
- Chronic Pain Management
- Pediatric Analgesics
- Chronic Narcotic Guideline
- Definitions
- Opiate
- Naturally occurring, derived from opium poppy
- Examples: Morphine, Codeine, Heroin
- Opioids
- Includes Opiates (naturally occurring)
- Semi-synthetic Opioids (structurally similar to Opiates)
- Examples: Hydrocodone, Oxycodone, Hydromorphone, Oxymorphone
- Synthetic Opioids
- Examples: Methadone, Buprenorphine, Meperidine, Fentanyl, Tramadol
- Adverse Effects
- See Opioid Adverse Effect
- See Opioid Overdose
- See Opioid Abuse
- See Opioid Withdrawal
- Pharmacology: Metabolism of Opioids
- Common Metabolites
- Codeine: Metabolizes to Hydrocodone and Morphine
- Heroin: Metabolizes to 6-acetylmorphine (6-MAM) and then to Morphine
- Morphine and Hydrocodone: metabolize to Hydromorphone
- Hydrocodone: Metabolizes to Dihydrocodeine
- Oxycodone: Metabolizes to Oxymorphone
- Renal dysfunction
- Safe
- Fentanyl (consider reduced dose)
- Methadone
- Caution (risk of metabolite accumulation)
- Hydromorphone
- Morphine
- Oxycodone
- Unsafe (avoid)
- Codeine
- Hepatic dysfunction
- Safe
- Fentanyl
- Caution
- Hydromorphone (decrease starting dose by 50%)
- Oxycodone (decrease starting dose by 50%)
- Morphine (decreased conversion to active metabolite, increased dosing frequency may be needed)
- Unsafe (avoid)
- Codeine
- Methadone
- References
- Johnson (2007) Opioid Safety in Patients With Renal or Hepatic Dysfunction, Pain Treatment Topics
- http://paincommunity.org/blog/wp-content/uploads/Opioids-Renal-Hepatic-Dysfunction.pdf
- Pharmacology: Mechanism
- Opioid binds Neuron membrane receptor
- Calcium (2+) channels close (blocks calcium entry into cell)
- Potassium (1+) channels open (allows Potassium to leave cell)
- Intracellular cAMP also decreases
- Cell becomes hyperpolarized
- Charge difference increases between intracellular and extracellular fluid
- Decreases likelihood of Neuron activation (firing) in response to a given action potential
- Sensory Neurons decrease activity
- Results in fewer afferent, sensory signals returning to CNS
- Pain Sensation is therefore reduced
- Approach: Quantity Prescribed
- See Opioid Prescribing Quantity
- Precautions: General
- Informed Consent for Opioid Prescription
- See Opioid Prescription in Acute Pain
- Pregnancy
- Neural Tube Defects if Opioids used in early pregnancy
- Newborn Opioid Withdrawal (neonatal abstinence syndrome) if maternal Chronic Opioid use
- No evidence of Tramadol safety
- Buprenorphine (without Naloxone) or Methadone may be used for pregnant women with Opioid Use Disorder
- (2017) Presc Lett 24(11): 64
- (2017) Obstet Gynecol 130(2):e81-e94 +PMID:28742676 [PubMed]
- Reddy (2017) Obstet Gynecol 130(1):10-28 +PMID:28594753 [PubMed]
- Precautions: Ineffective Oral Opioids (Not recommended)
- Darvocet N-100 (Acetaminophen 650, Propoxyphene 100)
- Dose: 1 PO q4-6 hours
- Not available in U.S. as of 2007-2010
- Not recommended due to low efficacy and toxicity risk
- Tylenol #3 (Acetaminophen 300, Codeine 30)
- Dose: 1-2 PO q4-6 hours
- Avoid due to low efficacy and increased toxicity risk
- Precautions: Variable metabolism of oral Opioids
- Most oral Opioids are metabolized to active form (e.g. Morphine) by Cytochrome P450 2D6 (CYP2D6)
- Codeine
- Tramadol (Ultram)
- Hydrocodone
- Oxycodone
- Ultrarapid CYP2D6 Metabolizers
- Accounts for 10% of caucasians (may be as high as 30% in some races)
- Risk of a rapid conversion to toxic levels of active Opioid (e.g., Morphine)
- Slow CYP2D6 Metabolizers
- Accounts for 10% of caucasians (or 3% of other races)
- Renders the oral Opioids less effective in slow metabolizing patients
- References
- (2012) Presc Lett 19(6): 33
- Crews (2012) Clin Pharmacol Ther 91:321-6 [PubMed]
- Precautions: Iatrogenic Opioid Overdose prevention
- Avoid repeat intramuscular Opioid injection
- Risk of dose stacking and secondary CNS/Respiratory depression (esp. Dilaudid)
- Titrate dosing to pain while exercising caution in the elderly and Opioid naive
- See Dilaudid below for specific precautions
- Decrease dose to 50% in the elderly, hepatic insufficiency, Renal Insufficiency
- Opioid tolerant patients may still experience respiratory depression on typical Opioid doses
- Exercise caution when combining CNS Depressants (e.g. Opioids and Benzodiazepines)
- Long-acting Opioids for non-cancer Chronic Pain are associated with significantly increased mortality
- Ray (2016) JAMA 215(22): 215-23 [PubMed]
- References
- Beaudoin (2015) Ann Emerg Med 65(4): 4243-31 [PubMed]
- Preparations: Acute pain IV Opioids (equivalent to Demerol 50 IV)
- Morphine 4 mg IV (2 mg IV in elderly)
- Fentanyl 50 mcg IV (25 mcg IV in elderly)
- Preferred agent in Renal Insufficiency
- Hydromorphone (Dilaudid)
- Moderate pain: 0.5 mg IV
- Start with 0.2 to 0.3 mg IV in the elderly or Opioid naive
- May repeat every 15 to 30 minutes up to 3 doses in the emergency department
- Spread interval to every 2-3 hours on the hospital ward
- Opioid tolerant or severe pain: Start with 1 mg IV
- Dilaudid is a high potency Opioid (1 mg is equivalent to up to 10 mg Morphine)
- Most iatrogenic Opioid Overdoses have occurred with Hydromorphone (Dilaudid)
- Preparations: Oral Opioids by strength
- Weak Opioids (WHO Step 2)
- Vicodin (Hydrocodone 5, Acetaminophen 500)
- Dose: 1-2 PO q4-6 hours
- Hydrocodone 10 mg equivalent to Codeine 60-80 mg
- Vicoprofen (Hydrocodone 7.5, Ibuprofen 200)
- Dose: 1-2 PO q4-6 hours
- Tramadol (Ultram)
- Dose: 50-100 mg PO q4-6 hours
- Tramadol 50 mg equivalent to Codeine 60 mg
- Higher cost, but less effective than other Opioids
- Metabolized by 2D6 and risk of respiratory depression in ultrarapid metabolizers
- Inferior to Vicodin for analgesia
- Turturro (1998) Ann Emerg Med 32:139-143 [PubMed]
- Strong Opioids (WHO Step 3)
- Oxycodone
- Adults (and over age 12 years) 5-10 mg every 4-6 hours as needed
- Child: 0.05 to 0.3 mg/kg/dose (up to 10 mg) every 4-6 hours as needed
- Percocet (Acetaminophen 325, Oxycodone 5)
- Dose: 1 PO q6 hours (adults)
- Hydromorphone (Dilaudid)
- Dose: 2 mg PO q4-6 hours
- Morphine Sulfate (MSIR, MS Contin)
- Fast Release: 15 to 30 mg PO q4 hours
- Sustained Release (MS Contin): 30 mg PO q8-12 hours
- Fentanyl Lollipop (100 ug, 200 ug, 300 ug, 400 ug)
- Dose: 5 to 15 ug/kg (maximum 400 ug)
- Methadone (Dolophine)
- Dose: 15 to 60 mg PO q6 to 8 hours
- Preparations: Oral Opioids by duration
- Short acting Opioids
- Percocet PO every 6 hours
- MSIR 10 mg PO every 4 hours
- Hydromorphone 4 mg PO every 4 hours
- Vicodin PO every 6 hours
- Darvocet N-100 PO every 6 hours
- Long acting Opioids
- Methadone 20 mg PO every 8 hours
- Morphine Sulfate
- Controlled release (MS Contin) 30 mg PO q12 hours
- Sustained release (Oramorph) PO q8-12 hours
- Sustained release (Kadian) PO q12-24 hours
- Extended release (Avinza) PO q24 hours
- Oxycodone (Oxycontin) 20 mg PO every 12 hours
- Preparations: MME - Morphine Equivalent Opioid Doses
- See Morphine Milligram Equivalent
- Preparations: Transdermal Opioid
- Fentanyl (Duragesic) Patch
- Dose: 25 to 100 ug/hour patch q72 hours
- Fentanyl 50 ug/hour equivalent Morphine IV 25 mg/day
- Preparations: Transmucosal Opioid
- Precaution
- Indicated for breakthrough Cancer Pain in those using >60 mg/day of Morphine or equivalent
- Fentanyl
- Sublingual tab (Abstral) 100 mcg
- Sublingual spray (Subsys) 100 mcg
- Nasal spray (Lazanda) 100 mcg
- Preparations: Rectal Opioids
- General
- Do not use lubricant to insert (decreased absorption)
- Morphine suppository or tablet 10 to 30 mg rectally q4h
- MS Contin 30 mg rectally every 12 hours
- Available preparations: 15, 30, 60, 100, 200 mg
- Preparations: By origin (natural Opiates, semi-sythetic and synthetic Opioids)
- Naturally occurring Opiates (opium poppy derivatives, subset of Opioids)
- Morphine
- Codeine
- Heroin (Morphine metabolite)
- Semi-synthetic Opioids (structurally similar to Opiates)
- Hydrocodone
- Oxycodone
- Hydromorphone
- Oxymorphone
- Synthetic Opioids
- Methadone
- Buprenorphine
- Meperidine
- Fentanyl
- Tramadol
- Preparations: Opioid Abuse deterrents (e.g. Tamper resistant)
- Precautions
- Abuse deterrents are inconsistent among products
- Long-acting Hydrocodone (Zohydro) is not tamper resistant
- Abuse deterrents are not shown to reduce abuse
- abuse deterrent may simply offset abuse to other substances (e.g. Heroin)
- Abuse deterrents increase Opioid costs up to four fold
- Agents with abuse deterrents
- Opioids with abuse antagonists
- Buprenorphine with Naloxone (Suboxone, Zubsolv)
- Opioids with tamper resistance (e.g. break into clumps when crushed or thick gel when wet)
- Long-Acting Oxycodone (Oxycontin)
- Extended Release Hydromorphone (Exalgo)
- Implantable Opioids
- Buprenorphine implant (Probiphine)
- References
- (2014) Presc Lett 21(5): 28
- Preparations: Adjunctive medications
- Alternative non-Narcotics
- See Chronic Pain Management
- Acetaminophen (Tylenol)
- NSAIDs
- COX-2 Inhibitors
- Stool Softeners or Laxatives
- See Bowel Regimen in Chronic Narcotic Use
- References
- Dachs (2003) AAFP Board Review, Seattle
- Hipskind and Kamboj (2016) Crit Dec Emerg Med 30(10): 15-23
- (2000) Tarascon Pocket Pharmacopoeia
- (2000) Med Lett Drugs Ther 42(1085):73-8 [PubMed]