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Pronunciation

TRA-ma-dol

Classifications

Therapeutic Classification: analgesics (centrally acting), opioid analgesics

Pharmacologic Classification: opioid agonists

Indications

High Alert

Action

Therapeutic Effects:

Pharmacokinetics

Absorption: Immediate-release: 75% absorbed after oral administration; Extended-release: 85–90% (compared with immediate-release).

Distribution: Crosses the placenta; enters breast milk.

Metabolism/Excretion: Mostly metabolized by the liver (primarily by the CYP2D6 and CYP3A4 isoenzymes); primarily metabolized by the CYP2D6 isoenzyme 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. 1–10% of Whites, 3–4% of Blacks, and 1–2% of East Asians may be CYP2D6 ultra-rapid metabolizers and have significantly concentrations of M1 metabolite. 30% eliminated unchanged in the urine.

Half-life: Tramadol (immediate release): 6–8 hr, Extended release: 7.9 hr; Active metabolite: 7–9 hr; both are in renal or hepatic impairment.

Time/Action Profile

(analgesia)

ROUTEONSETPEAKDURATION
PO-immediate release1 hr2–3 hr4–6 hr
PO-extended releaseunknown12 hr24 hr

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

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: dizziness, headache, somnolence, anxiety, confusion, coordination disturbance, euphoria, hypertonia, malaise, nervousness, SEIZURES, sleep disorder, stimulation, weakness.

Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).
Misc: physical dependence, psychological dependence, tolerance.

Interactions

Drug-Drug:

Drug-Natural Products:

Route/Dosage

Immediate Release

Renal Impairment

Hepatic Impairment

Extended Release

Availability

(Generic available)

Assessment

Lab Test Considerations: Toxicity and Overdose:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

ConZip, Qdolo, Ultram, Ultram ER

Canadian Brand Names

Durela, Ralivia, Tridural, Zytram XL

Contr. Subst. Schedule

Schedule IV (C-IV)

Pill Image

tramadol_hcl_195_8991.jpg