What is Tramadol (Ultram) and where do I buy generic Tramadol online?
Tramadol, sold under the brandnames Ultram and Tramal among others, is an opioid pain medication used to treat moderate to moderately severe pain. It has two different mechanisms. First, it binds to the μ-opioid receptor. Second, it inhibits the reuptake of serotonin and norepinephrine.
Its analgesic effects take about one hour to come into effect and 2–4 hours to peak after oral administration with an immediate-release formulation.On a dose-by-dose basis Tramadol has about one-tenth the potency of morphine and is approximately equally potent when compared to pethidine and codeine.
Mechanism Of Action
ULTRAM and generic Tramadol is a centrally acting synthetic opioid analgesic. Although its mode of action is not completely understood, from animal tests, at least two complementary mechanisms appear applicable: binding of parent and M1 metabolite to μ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin.
Opioid activity is due to both low affinity binding of the parent compound and higher affinity binding of the O-demethylated metabolite M1 to μ-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in μ-opioid binding. Tramadol-induced analgesia is only partially antagonized by the opiate antagonist naloxone in several animal tests. The relative contribution of both tramadol and M1 to human analgesia is dependent upon the plasma concentrations of each compound (see Pharmacokinetics).
Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin in vitro, as have some other opioid analgesics. These mechanisms may contribute independently to the overall analgesic profile of ULTRAM. Analgesia in humans begins approximately within one hour after administration and reaches a peak in approximately two to three hours.
Apart from analgesia, ULTRAM and generic Tramadol administration may produce a constellation of symptoms (including dizziness, somnolence, nausea, constipation, sweating and pruritus) similar to that of opioids. In contrast to morphine, tramadol has not been shown to cause histamine release. At therapeutic doses, ULTRAM has no effect on heart rate, left-ventricular function or cardiac index. Orthostatic hypotension has been observed.
For pain moderate in severity its effectiveness is equivalent to that of morphine; for severe pain it is less effective than morphine.These painkilling effects peak at about 3 hours, post-oral administration and last for approximately 6 hours.These analgesic effects are only partially reversed by naloxone, hence indicating that its opioid action is unlikely the sole contributing factor; Tramadol's analgesic effects are also partially reversed by α2 adrenergic receptor antagonists like yohimbine and the 5-HT3 receptor antagonist, ondansetron.
Pharmacologically, Tramadol is similar to levorphanol and tapentadol in that it not only binds to the mu opioid receptor, but also inhibits the reuptake of serotonin and norepinephrinedue to its action on the noradrenergic and serotonergic systems, such as its "atypical" opioid activity. Available dosage forms include liquids, syrups, drops, elixirs, effervescent tablets and powders for mixing with water, capsules, tablets including extended release formulations, suppositories, compounding powder, and injections.
Tramadol may also be used for purposes not listed in this medication guide.
©24hrspharma - 2018