Tuesday 15 November 2011

Tramadol: dosage and administration

For the treatment of painful conditions Tramadol? 50 mg to 100 mg can be administered as needed for relief every four to six hours, not to exceed 400 mg per day. For moderate pain Tramadol 50 mg may be adequate as the initial dose, and for more severe pain Tramadol 100 mg is usually more effective as the initial dose.

Tramadol: drug abuse and overdosage

Although tramadol can produce drug dependence of the ?-opioid type (like codeine or dextropropoxyphene) and potentially may be abused, there has been little evidence of abuse in foreign clinical experience. In clinical trials, tramadol produced effects similar to an opioid, and at supratherapeutic doses was recognized as an opioid in subjective/behavioral studies. Tolerance development has been reported to be relatively mild and withdrawal when present, is not considered to be as severe as that produced by other opioids. Part of tramadol's activity and some extension of the duration of ?-opioid activity. Delayed ?-opioid activity is believed to reduce a drug's abuse liability.

An assay for tramadol is not included in routine urine screens for drugs of abuse.

Tramadol: Drug interaction

Tramadol does not appear to induce its own metabolism in humans, since observed maximal plasma concentrations after multiple oral doses are higher than expected based on single-dose data. Tramadol is a mild inducer of selected drug metabolism pathways measured in animals.

Concomitant administration of Tramadol? with carbamazepine causes a significant increase in tramadol metabolism, presumably through metabolic induction by carbamazepine. Patients receiving chronic carbamazepine doses of up to 800 mg daily may require up to twice the recommended dose of Tramadol.

Tramadol: Indications

INDICATIONS
Tramadol is indicated for the management of moderate to moderately severe pain.

CONTRAINDICATION
Tramadol should not be administered to patients who have previously demonstrated hypersensitivity to tramadol or in cases of acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids or psychotropic drugs.

Tramadol: description

Tramadol? is a centrally acting analgesic. The chemical name for tramadol hydrochloride is (?)cis-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl cyclohexanol hydrochloride.

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The molecular weight of tramadol hydrochloride is 299.8. Tramadol hydrochloride is a white, bitter, crystalline and odorless powder. It is readily soluble in water and ethanol and has a pKa of 9.41. The water/n-octanol partition coefficient is 1.35 at pH 7. Tramadol tablets contain 50 mg of tramadol hydrochloride and are white in color. Inactive ingredients in the tablet are corn starch, hydroxypropyl methylcellulose, lactose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, sodium starch glycolate, titanium dioxide and wax

Tramadol compatibility with drugs

Tramadol hydrochloride is a centrally acting synthetic analgesic with a dual mechanism of action. Tramadol and its Odesmethyl metabolite (M1) bind to opioid receptors, with M1 having a 200-fold higher affinity for binding to these receptors. Tramadol has also been shown to inhibit the uptake of norepinephrine and serotonin, suggesting that its antinociceptive activity is mediated by both opioid and nonopioid mechanisms. In patients with diabetic neuropathy, therapy with oral tramadol resulted in low pain scores and high painrelief scores. Tramadol produced effective analgesia with minimal adverse effects in cancer patients with chronic pain.
Tramadol is also a useful alternative in patient-controlled epidural analgesia when patients cannot receive combined spinal? epidural analgesia for labor pains. There are some clinical situations in which tramadol must be combined with other drugs, such as for patients with postoperative pain who require both a painkiller and an antibiotic or when tramadol is used as an adjunct to analgesic-supplemented anesthesia for certain surgical procedures. In addition, patients receiving tramadol are likely to receive other i.v. medications concurrently. There may be a need for tramadol and other agents to be administered through the same intravenous line.
Tramadol can be administered by i.v. bolus injection and by i.v. infusion. The objective of this study was to investigate the compatibility of tramadol injection with different infusion solutions and in admixtures

Tramadol and hiccups

Since 1993 tramadol (Tramal?, Tramagetic?) is available in the Netherlands and since 2003 tramadol is also available in combination with paracetamol (Zaldiar?). Tramadol is a centrally acting analgesic, which is indicated for acute and chronic pain, such as pain due to surgery or trauma, and malignant diseases. Tramadol is a racemate of two enantiomers. The cis-enantiomer binds to the μ-opiatereceptor and inhibits the serotonin-reuptake. The trans-enantiomer inhibits the norepinephrine-reuptake and stimulates *2-receptors. Nausea, vomiting, constipation, sweating, dry mouth and headache are the most frequently occurring adverse drug reactions. Respiratory depression may occur only when high dosages of tramadol are used or when concomitant drugs with centrally inhibiting effects are used. Tramadol has almost no effect on the gastrointestinal motility.