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Indications ⬇

BEERS REMS, High Alert


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: allodynia, opioid-induced hyperalgesia, physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Drug-Natural Products:

Availability ⬆ ⬇

(Generic available)

Route/Dosage ⬆ ⬇

Immediate Release

Renal Impairment

Hepatic Impairment

Extended Release

US Brand Names ⬆ ⬇

ConZip, Ultram, Ultram ER

Action ⬆ ⬇

  • Acts as a mu-opioid receptor agonist.
  • Inhibits reuptake of serotonin and norepinephrine in the CNS.
Therapeutic effects:
  • Decreased pain.

Classifications ⬆ ⬇

Therapeutic Classification: analgesics (centrally acting), ), opioid analgesics

Pharmacologic Classification: opioid agonists

Pharmacokinetics ⬆ ⬇

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

Distribution: Widely distributed to tissues.

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 White patients, 3–4% of Black patients, and 1–2% of East Asian patients 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.

Contr. Subst. Schedule ⬆ ⬇

Schedule IV (C-IV)

Canadian Brand Names ⬆ ⬇

Durela, Ralivia, Tridural, Zytram XL

Time/Action Profile ⬆ ⬇

( analgesia)

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

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

TRA-ma-dol

Pill Image

tramadol hcl_195-8991.jpg

Code ⬆

NDC Code