Tramadol
Opioid analgesic (atypical, weak μ-agonist with serotonin/norepinephrine reuptake inhibition), Schedule IV controlled substance, Analgesic
Tramadol
Ultram (IR), Ultram ER, ConZip ER
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Summary
Classes
Common uses
Moderate to moderately severe pain (FDA)0, Chronic pain in opioid-sparing regimens (off-label)0, Restless legs syndrome (off-label, second-line)0, Neuropathic pain (off-label)0
Pharmacy
Starting dose
IR: 25-50 mg PO every 4-6 hours as needed, titrate as tolerated. ER: 100 mg PO once daily, titrate by 100 mg every 5 days
Preparations
IR tablets 50 mg; ER tablets 100, 200, 300 mg (Ultram ER, ConZip); oral solution 5 mg/mL; combination products with acetaminophen (Ultracet)
US FDA Max
400 mg/day (IR, adult); 300 mg/day (ER); 300 mg/day in elderly >75 years
Pharmacology
Routes
Oral
Onset
30-60 minutes (IR)
Duration
4-6 hours (IR); 24 hours (ER)
Half-life
Tramadol 6-7 hours; M1 active metabolite 7-9 hours[2]
Bioavailability
~75% (IR, rises with multi-dose administration due to saturable first-pass)[2]
Pregnancy
Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.[citation needed]
Legal status
Schedule IV controlled substance in US (federally scheduled 2014); some states schedule higher[2]
Purported mechanism
Weak μ-opioid receptor agonist whose major analgesic activity comes from CYP2D6 conversion to O-desmethyltramadol (M1), a ~6-fold more potent μ-agonist. Tramadol also inhibits serotonin and norepinephrine reuptake (the SNRI-like component), which contributes meaningfully to analgesia and distinguishes the agent from traditional opioids. CYP2D6 ultra-rapid metabolizers produce dangerously high M1 levels with risk of fatal respiratory depression, particularly in children; CYP2D6 poor metabolizers get reduced opioid analgesic benefit and rely on the SNRI component.0 Serotonin syndrome risk with SSRIs, SNRIs, MAOIs, and other serotonergic agents. Seizure risk is dose-dependent and elevated in patients with epilepsy, head trauma, or concurrent serotonergic medicines. CPIC provides CYP2D6 genotype-guided opioid selection guidance[1].
References
- ↑ CPIC Guideline for CYP2D6, OPRM1, and COMT and Opioid Use, 2021. https://cpicpgx.org/guidelines/cpic-guideline-for-codeine-and-cyp2d6/
- ↑ 2.0 2.1 2.2 FDA Prescribing Information, Ultram (tramadol hydrochloride), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020281s048lbl.pdf