Absorption: Immediate-release 75% absorbed after oral administration; Extended-release (Ultram) 8590% (compared with immediate-release).
Distribution: Crosses the placenta; enters breast milk.
Metabolism/Excretion: Mostly metabolized by the liver (primarily by CYP2D6 and CYP3A4); primarily metabolized by CYP2D6 to active metabolite with analgesic activity (M1); CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers and may have significantly ↑ concentrations of tramadol and ↓ concentrations of M1 metabolite. 110% of Whites, 34% of Blacks, and 12% of East Asians may be ultrarapid metabolizers of CYP2D6 and have significantly ↑ concentrations of M1 metabolite. 30% eliminated unchanged in the urine.
Half-life: Tramadol 68 hr, ER 7.9 hr; active metabolite 79 hr; both are ↑ in renal or hepatic impairment.
Contraindicated in:
Use Cautiously in:
CV: vasodilation.
Derm: pruritus, sweating.
EENT: visual disturbances.
Endo: hypoglycemia.
F and E: hyponatremia.
GI: constipation, nausea, abdominal pain, anorexia, diarrhea, dry mouth, dyspepsia, flatulence, vomiting.
GU: ↓fertility, menopausal symptoms, urinary retention/frequency.
Neuro: hypertonia , SEIZURES, dizziness, headache, somnolence, anxiety, confusion, coordination disturbance, euphoria, malaise, nervousness, sleep disorder, stimulation, weakness.
Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).
Misc: physical dependence, psychological dependence, tolerance.
Drug-Drug:
Drug-Natural Products:
Immediate-release
Renal Impairment
Hepatic Impairment
Extended-release
ConZip, Qdolo, Ultram, Ultram ER
(Generic available)
NDC Code*