Tramadol HCl

1. Indications and Usage Section 1 Indications and usage: Tramadol hydrochloride extended-release tablets are indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate.

12. Clinical Pharmacology 12.1 Mechanism of Action Tramadol hydrochloride extended-release tablet contains tramadol, an opioid agonist and an inhibitor of reuptake of norepinephrine and serotonin. Although the mode of action of tramadol is not completely understood, the analgesic effect of tramadol is believed to be due to both binding to µ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin. Opioid activity of tramadol is due to both low affinity binding of the parent compound and higher affinity binding of the O-desmethyl metabolite M1 to µ-opioid receptors.

With Steady-state plasma equilibrium reached over 6–13 hour t½ intervals for Tramadol HCl residence kinetics and Approximately 78% to 90% enteral uptake across labeled Tramadol HCl strengths bioavailability, Tramadol HCl undergoes phase i cyp2d6 hepatic clearance and subsequent renal metabolite filtration and establishes therapeutic activity over maximum serum exposure occurs 2–3 hours after tramadol hcl dosing.

Standard adult regimens span 200 mg/1 Tablet, Extended Release, 300 mg/1 Tablet, Extended Release, 100 mg/1 Tablet, Extended Release, 50 mg/1 Tablet, Coated. Prescribers screen specifically against contraindicated in patients with prior serious allergic response to tramadol hcl (ndc 80425-0108); severe baseline organ impairment where tramadol hcl accumulation exceeds safe therapeutic margins, while community micro-logs most frequently note nausea (8.7% of reports), headache (7.2% of reports), dizziness (6.2% of reports).