TRAMADOL HYDROCHLORIDE

TRAMADOL HYDROCHLORIDE (tra'ma-dol) Ultram, Zydol  Classifications: analgesic; narcotic (opiate) agonist; Therapeutic: narcotic analgesic; opiate agonist Prototype: Morphine sulfate Pregnancy Category: C

Availability

50 mg tablets; 50 mg orally disintegrating tablets

Action

Centrally acting opiate receptor agonist that inhibits the uptake of norepinephrine and serotonin, suggesting both opioid and nonopioid mechanisms of pain relief. May produce opioid-like effects, but causes less respiratory depression than morphine.

Therapeutic Effect

Effective agent for control of moderate to moderately severe pain.

Uses

Management of moderate to moderately severe pain.

Contraindications

Hypersensitivity to tramadol or other opioid analgesics; patients on MAO inhibitors; patients acutely intoxicated with alcohol, hypnotics, centrally acting analgesics, opioids, or psychotropic drugs; substance abuse; patients on obstetric preoperative medication; abrupt discontinuation; alcohol intoxication; pregnancy (category C); lactation; children <16 y.

Cautious Use

Debilitated patients; chronic respiratory disorders; respiratory depression; older adults; liver disease; renal impairment; myxedema, hypothyroidism, or hypoadrenalism; GI disease; acute abdominal conditions; increased ICP or head injury, increased intracranial pressure; history of seizures; patients >75 y.

Route & Dosage

Pain Adult: PO 50–100 mg q4–6h prn (max: 400 mg/d), may start with 25 mg/d if not well tolerated, and increase by 25 mg q3d up to 200 mg/d Geriatric: PO 50–100 mg q4–6h prn (max: 300 mg/d), may start with 25 mg/d if not well tolerated, and increase by 25 mg q3d up to 200 mg/d Renal Impairment Clcr <30 mL/min: decrease to 50–100 mg q12h Hepatic Impairment Cirrhosis: decrease to 50–100 mg q12h

Administration

Oral

• Note: Dosage reduction is recommended for patients with renal insufficiency and hepatic impairment.
• Store at 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

CNS: Drowsiness, dizziness, vertigo, fatigue, headache, somnolence, restlessness, euphoria, confusion, anxiety, coordination disturbance, sleep disturbances, seizures. CV: Palpitations, vasodilation. GI: Nausea, constipation, vomiting, xerostomia, dyspepsia, diarrhea, abdominal pain, anorexia, flatulence. Body as a Whole: Sweating, anaphylactic reaction (even with first dose), withdrawal syndrome (anxiety, sweating, nausea, tremors, diarrhea, piloerection, panic attacks, paresthesia, hallucinations) with abrupt discontinuation. Skin: Rash. Special Senses: Visual disturbances. Urogenital: Urinary retention/frequency, menopausal symptoms.

Diagnostic Test Interference

Increased creatinine, liver enzymes; decreased hemoglobin; proteinuria.

Interactions

Drug: Carbamazepine significantly decreases tramadol levels (may need up to twice usual dose). Tramadol may increase adverse effects of mao inhibitors. tricyclic antidepressants, 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 depressants. Herbal: St. John's wort may increase sedation.

Pharmacokinetics

Absorption: Rapidly absorbed from GI tract; 75% reaches systemic circulation. Onset: 30–60 min. Peak: 2 h. Duration: 3–7 h. Distribution: Approximately 20% bound to plasma proteins; probably crosses blood–brain barrier; crosses placenta; 0.1% excreted into breast milk. Metabolism: Extensively in liver by cytochrome P450 system. Elimination: Primarily in urine. Half-Life: 6–7 h.

Nursing Implications

Assessment & Drug Effects

• Assess for level of pain relief and administer prn dose as needed but not to exceed the recommended total daily dose.
• Monitor vital signs and assess for orthostatic hypotension or signs of CNS depression.
• Discontinue drug and notify physician if S&S of hypersensitivity occur.
• Assess bowel and bladder function; report urinary frequency or retention.
• Use seizure precautions for patients who have a history of seizures or who are concurrently using drugs that lower the seizure threshold.
• Monitor ambulation and take appropriate safety precautions.

Patient & Family Education

• Exercise caution with potentially hazardous activities until response to drug is known.
• Understand potential adverse effects and report problems with bowel and bladder function, CNS impairment, and any other bothersome adverse effects to physician.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug