Ultram, ZydolClassification: Central nervous system agent, opiate agonist; Narcotic Analgesic
Prototype: Morphine sulfate
Pregnacy Type: C
Availability: 50mg tablets
Actions: Centrally acting opiate receptor agonist that inhibits the uptake of norepinephrine and serotonin, suggesting both opioid and nonoptioid mechanism of pain relief. May produce opoiod-like effects, but causes less respiratory depression than morphine.
Theraputic Effects:
Effective agent for control of moderate to moderate severe pain.
Use: Management of moderate to moderately severe pain.
Contraindication: Hypersensitivity to tramadol or other opoiod analgesics: patients in MAO inhibitors; patients acutely intoxicated with alcohol, hypnotics, centrally acting analgesics, opoiods, or psyctropic drugs; patients on obstretric preoperative medication; lactation.
Cautious Use: Debilitated patients; chronic respiratory disorders; Liver disease; renal impairment; myxedema, hypothyroidism, or hypoadrenalism; acute abdominal conditions; increased ICP or head injury; history of siezures; pregnancy (category C); patients >75y. Safely and efficacy i children are not established.
Route and Dosage:
Pain
Adult: PO 50-100mg q4-6h prn(max: 400mg/d), may start with 25mg/d if not well tolerated, and increase by 25mg q3d up to 200mg/d
Geriatric:PO 50-100mg q4-6h prn (max:300mg/d), may start with 25mg/d if not well tolerated, and increase by 25 mg q3d up to 200mg/d
Renal Impairment:
Clcr <30mL/min: decrease to 50-100mg q 12h
Hepatic Impairment cirrhosis decrease to 50-100 mg q12h.
Administration:
Oral
Note: Dosage reduction is recomended for patients with renal insufficientcy and hepatic impairment.
Store at 15 to 30degrees C (59 to 86degrees F).
Adverse Effects: CNS: Drowsiness, dizziness, vertigo, fatigue, headache, somnolence, restlessness. euphoria, confusion, anxiety, coordination disturbance, sleep disturbances, siezures. CV: palpitations, vasodilation. GI: Nausea, constipation, vomiting, xerostomia, dyspepsia, diarrhea, abdominal pain, anorexia, flatylence. Body as a Whole: Sweating, anaphylactics reaction (even with first dose).
Skin: Rash Special senses: Visual disturbances. Urogenital: Urinary retention/frequency, menopausal symptoms.
Diagnostic Test Interference: Increased creatinine, liver enzymes; decreased hemoglobin; protienuria.
Interactions Drug: Carbamazepine significantly decreases tramadol level (may need up to twice usual dose). Tramadol may increase adverse effects of MAO INHIBITORS. TRICYCLIC ANTIDEPRESANTS, cyclobenzaprine, PHENOTHIAZINES, SELECTIVE SEROTONIN-REUPTAKE INHIBITORS (SSRIS), MAO INHIBITORS may enhance seizure risk with tramadol. May increase CNS adverse effects when used with other CNS DEPRESANTS. Herbal: St. John's Wort may increase sedation.
PHARMACOKINETICS Absorption:
Rapidly absorbed from GI tract; 75% reaches systemic circulation.
Onset: 30-60 min.
Peak: 2h
Duration: 3-7hrs
Distribution: Approximately 20% bound to plasma proteins; probably crosses blood-brain barrier; crosses placenta; 0.1% excreted into breast milk.
Metabolism: Metabolized extensively in liver by cytocrome P450 system.
Elimination: Excreted primarily in urine.
Half Life: 6-7h.
