Pain management, especially chronic, is often a challenge for physicians and patients due to adverse effects associated with commonly prescribed analgesics. Opioid analgesics such as morphine or codeine are effective for many different types of pain, but side effects such as respiratory depression, constipation, tolerance, and dependence can be very worrisome.
Tramadol ultram is a centrally acting analgesic that has been shown to be effective in a variety of acute and chronic pain states. Unlike other centrally acting analgesics, it exerts a dual action by binding to the opioid receptor site in the central nervous system and by weakly inhibiting the reuptake of biogenic amines.
This medicine is rapidly and almost completely absorbed, with an onset of action occurring within 1 hour of oral administration. The recommended dosage is 50 to 100 mg every 4 to 6 hours; however, regular administration is an alternative, particularly for chronic pain states such as osteoarthritis, where the use of the recently developed sustained release formulation may represent an important advantage.
Tramadol is a synthetic 4-phenylpiperidine analog of codeine with pure opiate activity. The parent compound has low affinity for the mu opioid receptor, however, the active M1 metabolite has a higher affinity for the receptor with six times the analgesic activity. In addition to its analgesic activity at the opioid receptor, tramadol hcl inhibits the reuptake of norepinephrine and serotonin through negative and positive enantiomer activity. Inhibiting the reuptake of mono-amines in the central nervous system seems to have an antinociceptive effect. Absorption of this drug is rapid and complete following oral administration, and is unaffected by food. After a single 100 mg dose peak plasma concentrations occur in approximately 2 hours.
Tramadol ultram produces clinical analgesia 1.5 to 3 times less potent than morphine, as effectively as codeine, pentazocine, or propoxyphene against multiple pain conditions, and produces a greater antitussive effect than codeine. But, unlike typical opioid analgesics, it has not been associated with significant respiratory depression, constipation, or addiction.
Non-steroidal anti-inflammatory drugs are effective for many disorders where inflammation and pain are present, but can produce gastrointestinal adverse effects due to prostaglandin inhibition.
All cases exhibited symptoms within 4 hours of tramadol ingestion. Several cases of moderate toxicity have been associated with a mild serotonin syndrome, which could include agitation, confusion, tachycardia, and hypertension. An overload of monoamines was considered to be the most likely cause of the symptoms of toxicity rather than the opioid agonist effects. Treatments used for the symptoms of overdose were naloxone, benzodiazepines, nifedipine, and droperidol. The symptoms in one case report of possible serotonin syndrome associated with the coadministration of tramadol and sertraline were confusion, diaphoresis, tremor, and mental status changes. The mental status changes resolved with in 24 to 36 hours after the medicine was discontinued and the sertraline dose was decreased.
