Tramadol hydrochloride
Tramadol hydrochloride (Ultram)
Tramadol hydrochloride
( TRAM-ah-dol)
Pregnancy Category: C Ultram (Rx)

Classification: Analgesic, centrally acting

Action/Kinetics: A centrally acting analgesic not related chemically to opiates. Precise mechanism is not known. It may bind to mu-opioid receptors and inhibit reuptake of norepinephrine and serotonin. The analgesic effect is only partially antagonized by the antagonist naloxone. Causes significantly less respiratory depression than morphine. In contrast to morphine, tramadol does not cause release of histamine. Produces dependence of the mu-opioid type (i.e., like codeine or dextropropoxyphene); however, there is little evidence of abuse. Tolerance occurs but is relatively mild; the withdrawal syndrome is not as severe with other opiates. Rapidly absorbed after PO administration. Food does not affect the rate or extent of absorption. Onset: 1 hr. Peak effect: 2-3 hr. Peak plasma levels: 2 hr. t 1/2, plasma: Approximately 7 hr after multiple doses. Extensively metabolized by one of the P-450 isoenzymes. Excreted in the urine, with about 30% excreted unchanged and 60% as metabolites. The M-metabolite is active.

Uses: Management of moderate to moderately severe pain.

Contraindications: Hypersensitivity to tramadol. In acute intoxication with alcohol, hypnotics, centrally acting analgesics, opiates, or psychotropic drugs. Use in clients with past or present addiction or opiate dependence or in those with a prior history of allergy to codeine or opiates. Use for obstetric preoperative medication or for postdelivery analgesia in nursing mothers. Use in children less than 16 years of age, as safety and efficacy have not been determined.

Special Concerns: Use with great caution in those taking MAO inhibitors, as tramadol inhibits norepinephrine and serotonin uptake. Dosage reduction is recommended with impaired hepatic or renal function and in clients over 75 years of age. Use with caution in increased intracranial pressure or head injury, in epilepsy, or in clients with an increased risk for seizures, including head trauma, metabolic disorders, alcohol or drug withdrawal, and CNS infections. Tramadol may complicate the assessment of acute abdominal conditions.

Side Effects: CNS: Dizziness, vertigo, headache, somnolence, CNS stimulation, anxiety, confusion, incoordination, euphoria, nervousness, sleep disorders, seizures paresthesia, cognitive dysfunction, hallucinations, tremor, amnesia, concentration difficulty, abnormal gait, migraine, development of drug dependence. GI: Nausea, constipation, vomiting, dyspepsia, dry mouth, diarrhea, abdominal pain, anorexia, flatulence, GI bleeding, hepatitis, stomatitis, dysgeusia. CV: Vasodilation, syncope, orthostatic hypotension, tachycardia, abnormal ECG, hypertension, myocardial ischemia, palpitations. Dermatologic: Pruritus, sweating, rash, urticaria, vesicles. Body as a whole: Asthenia, malaise, allergic reaction, accidental injury, weight loss, suicidal tendency. GU: Urinary retention, urinary frequency, menopausal symptoms, dysuria, menstrual disorder. Miscellaneous: Anaphylaxis visual disturbances, cataracts, deafness, tinnitus, hypertonia, dyspnea.

Laboratory Test Alterations: Creatinine, liver enzymes. Hemoglobin. Proteinuria.

Overdose Management: Symptoms: Extension of side effects, especially respiratory depression and seizures. Treatment: Naloxone will reverse some, but not all, of the symptoms of overdose. General supportive treatment, with special attention to maintenance of adequate respiration. Diazepam or barbiturates may help if seizures occur. Hemodialysis is not helpful.

Drug Interactions: Alcohol / Respiratory depression Anesthetics, general / Respiratory depression Carbamazepine / Tramadol effect R/T metabolism CNS depressants / Additive CNS depression MAO Inhibitors / Risk of seizures Naloxone / Risk of seizures if naloxone used for tramadol overdose. Quinidine / Levels of tramadol and levels of M1 R/T inhibition of metabolism Warfarin PT and INR

How Supplied: Tablet: 50 mg

Dosage
?Tablets Management of pain.
Adults: 50-100 mg q 4-6 hr, as needed, but not to exceed 400 mg/day. For moderate pain, 50 mg, initially, may be adequate, and for severe pain, 100 mg, initially, is often more effective. For clients over 75 years of age, the recommended dose is no more than 300 mg/day in divided doses. In impaired renal function with a C _CR less than 30 mL/min, the dosing interval should be increased to 12 hr, with a maximum daily dose of 200 mg. The recommended dose for clients with cirrhosis is 50 mg q 12 hr.