Tramadol: an Analgesic
Tramadol, also know as Saliva ER, Saliva Flashdose, Ultram, Ultram ER, and Ultram ODT, is an synthetic, centrally acting opioid analgesic. Ultracet is a combination drug of acetaminophen and tramadol. Tramadol can be taken orally four times daily. Extended-release tablet called Tramadol ER may be administered once daily (Hair, Curran, & Keam 2006). The recommended dose of tramadol is 50-100 mg (immediate release tablets) every 4-6 hours as needed for pain. The maximum dose is 400 mg/day. To improve tolerance patients should be started at 25 mg/day, and doses may be increased by 25 mg every 3 days to reach 100 mg/day (25 mg 4 times daily). Thereafter, doses can be increased by 50 mg every 3 days to reach 200 mg day (50 mg 4 times daily). Tramadol may be taken with or without food. Recommended dose for extended release tablets is 100 mg daily which may be increased by 100 mg every 5 days but not to exceed 300 mg /day. Extended release tablets should be swallowed whole and not crushed or chewed.” (Ogbru & Marks 2010, p. 1)
Ultracet is indicated for short-term therapy of acute pain and should not be taken for long term. Tramadol is used to manage moderate to severe pain in adults. It has been indicated that tramadol is significantly more effective than placebo drugs (Hair, Curran & Keam 2007). Tramadol is less effective than morphine but just as effective as codeine when combined with acetaminophen or aspirin (Lehne 2010).
Tramadol is a white, bitter, crystalline and odorless powder which is almost completely absorbed rapidly after oral administration and reaches peak plasma levels in two hours. The absolute bioavailability is 75% when using a 100 mg tablet and is not affected by food. Tramadol has a steady state distribution of two days when using 100 mg four times daily. The plasma half-life of tramadol for single or multiple dosing is six to seven hours. It is metabolized extensively in the liver and may cross the blood-brain barrier. Ninety percent of tramadol and its metabolites are excreted in the urine and about thirty percent of the unchanged portion is also excreted in the urine. It is readily soluble in water and ethanol and has a pKa of 9.41 (www.rxlist.com/ultram-drug.htm). Tramadol is metabolized via the CYP2D6 isoenzyme of cytochrome P450 to an active metabolite which binds to µ receptors. Patients who metabolize drugs poorly via CYP2D6 may get less benefit from tramadol due to reduced formation of its active metabolite. Tramadol is also metabolized by CYP3A4 so its activity is reduced by drugs which induce CYP3A4, such as rifabutin, rifampicin, rifapentine, carbamazepine, phenobarbital, phenytoin or St. John’s Wort (Kaye 2004). Indicators of effectiveness include: relief of acute or chronic pain, relief of stiffness, increase in physical mobility and a decrease in the pain scale. Therapeutic index is usually reached within one hour of dosage, when aspirin and/or paracetamol alone are inappropriate or have failed.
Like most drugs, tramadol has its own set of side effects, interactions, and contradictions. tramadol side effects are caused from re-uptake of serotonin and noradrenaline and stimulation of opiate receptor (Close 2005). Side effects related to the central nervous system include dizziness, drowsiness (excluding vertigo), headache, anxiety, confusion, flushing, hallucinations and euphoria. Cardiovascular side effects are vasodilation, orthostatic hypotension, tachycardia and hypertension. Nausea, vomiting, dry mouth, diarrhea, anorexia flatulence, GI bleed and constipation are common gastrointestinal side effects. Regarding the urinary tract, menstrual disorder, dysuria, menopausal symptoms, urinary frequency and urinary retention are side effects. Patient could have problems with pruritus, urticaria and rashes. Significant adverse affects consist of seizures, anaphylaxis, serotonin syndrome, hypersensitivity reactions, toxic epidermal necrosis and Steven-Johnson...
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