Tramadol: Difference between revisions

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{{MedTemplate

| generic = Tramadol

| brand = Ultram

| brand = Ultram (IR), Ultram ER, ConZip ER

| classes = Opioid, Analgesic

| structure =

| mechanism = Mu-opioid agonist; ~~serotonin–norepinephrine reuptake inhibitor~~

| classes = [[:Category:Opioid analgesics|Opioid analgesic (atypical, weak μ-agonist with serotonin/norepinephrine reuptake inhibition)]], [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]], [[:Category:Analgesics|Analgesic]]

| uses = <vote slug="moderate-severe-pain-use">Moderate to moderately severe pain (FDA)</vote>, <vote slug="chronic-pain-tramadol-use">Chronic pain in opioid-sparing regimens (off-label)</vote>, <vote slug="restless-legs-syndrome-use">Restless legs syndrome (off-label, second-line)</vote>, <vote slug="neuropathic-pain-broad-use">Neuropathic pain (off-label)</vote>

| 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)

| fda_max = 400 mg/day (IR, adult); 300 mg/day (ER); 300 mg/day in elderly >75 years

| pill_id =

| routes = Oral

| onset = 30-60 minutes (IR)

| duration = 4-6 hours (IR); 24 hours (ER)

| halflife = Tramadol 6-7 hours; M1 active metabolite 7-9 hours<ref name="ultram-label">FDA Prescribing Information, Ultram (tramadol hydrochloride), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020281s048lbl.pdf</ref>

| bioavailability = ~75% (IR, rises with multi-dose administration due to saturable first-pass)<ref name="ultram-label" />

| pregnancy = Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.{{citation needed}}

| legal = [[USLegal:Schedule IV|Schedule IV controlled substance]] in US (federally scheduled 2014); some states schedule higher<ref name="ultram-label" />

| mechanism = <vote slug="tramadol-mech-claim">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.</vote> '''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<ref name="cpic-opioid-cyp2d6">CPIC Guideline for CYP2D6, OPRM1, and COMT and Opioid Use, 2021. https://cpicpgx.org/guidelines/cpic-guideline-for-codeine-and-cyp2d6/</ref>.

}}

== References ==

[[Category:Opioid analgesics]]

[[Category:Schedule IV controlled substances]]

[[Category:Analgesics]]

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