Effects of Tramadol ( Generic Ultram ) on alpha2-adrenergic receptors in the rat brain.Faron-Gorecka A, Kusmider M, Inan SY, Siwanowicz J, Dziedzicka-Wasylewska M.Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, Cracow PL-31-343, Poland.In recent years, it has been postulated that Tramadol ( Generic Ultram ), used mainly for the treatment of moderate to severe pain, might display a potential as an antidepressant drug. The present study investigated the effects of acute and repeated Tramadol ( Generic Ultram ) administration on the binding of [3H]RX 821002, a selective alpha2-adrenergic receptor ligand, in the rat brain. Male Wistar rats were used. Tramadol ( Generic Ultram ) (20 mg/kg, i.p.) administered acutely (single dose), at 24 h after dosing, induced a significant decrease in the alpha2-adrenergic receptors in all brain regions studied. The most pronounced effects were observed in all subregions of the olfactory system, nucleus accumbens and septum, thalamus, hypothalamus, amygdala, and cerebral cortex. Repeated treatment with Tramadol ( Generic Ultram ) (20 mg/kg, i.p., once daily for 21 days) also induced statistically significant downregulation of [3H]RX 821002 binding sites in the rat brain. However, the effect--although statistically significant--was less pronounced than in the group treated acutely with the drug. Since drugs such as mianserin and mirtazapine are potent antagonists of central alpha2-adrenergic receptors and are effective antidepressants, it is tempting to suggest that, in addition to other alterations induced by Tramadol ( Generic Ultram ), downregulation of these receptors may represent a potential antidepressant efficacy. On the other hand, one should be careful to avoid the treatment of chronic pain with Tramadol ( Generic Ultram ) in patients already receiving antidepressant drugs. Tramadol ( Generic Ultram )-induced downregulation of alpha2-adrenergic receptors--when combined with ongoing antidepressant therapy with drugs, which themselves inhibit serotonin reuptake or are antagonists of alpha2-adrenergic receptors--might cause threatening complications.

Ketoprofen (ketonal): a drug for preventing and treating postoperative pain

An inert matrix to control the release of Tramadol ( Generic Ultram ) HCl was prepared using glyceryl behenate as a matrix-forming agent. The matrices were prepared by either direct compression of a physical mixture of the drug and the matrix-forming agent or by compression of granules prepared by hot fusion of the drug and the matrix-forming agent. The hot fusion method was found to be more effective than compression of physical mixtures in retarding the release of the drug from the matrix. Drug release was adjusted by using release enhancers, such as microcrystalline cellulose and lactose, and the results showed that higher release rates were obtained using lactose. However, the release of the drug was independent of the compression force and the pH of the dissolution medium. This study showed that glyceryl behenate is an appropriate waxy material that can be used as a matrix-forming agent to control the release of a water-soluble drug such as Tramadol ( Generic Ultram ) HCl.

Role of epidural Tramadol ( Generic Ultram ) hydrochloride on postoperative pain relief in caesarean section delivery.

Two groups comprising 25 patients in each went for caesarean section delivery under epidural anaesthesia. Group I patients received 50 mg (1 ml) of Tramadol ( Generic Ultram ) hydrochloride with 14 ml of 2% lignocaine with adrenaline (1:200,000) and group II cases received 15 ml of 2% lignocaine with adrenaline (1:200,000). Both the groups of patients were comparable in age and body weight. In both the groups, there were good operative conditions, insignificant changes in pulse and blood pressure. The neonatal status was also similar in both the groups. The patients belonging to group I showed longer duration (15.39 +/- 0.45 hours) of analgesia in comparison to group II patients (2.46 +/- 0.54 hours).

Selegiline: a second look. Six years later: too risky in Parkinson's disease.

(1) The reference treatment for Parkinson's disease is levodopa plus a peripheral dopadecarboxylase inhibitor (benserazide or carbidopa). (2) In 1996, selegiline, a type B MAOI marketed in France since 1988, saw its indications extended to cover single-agent therapy of early-stage Parkinson's disease, and in combination with levodopa, before onset of complications of levodopa therapy. The initial clinical file failed to show that selegiline had any benefit in these indications. (3) Now, in 2002, new data from trials involving hundreds of untreated patients show that selegiline postpones the need for levodopa therapy for a few months but fails to substantially alter the progression of Parkinson's disease. (4) A clinical trial and a retrospective epidemiological study of patients with advanced Parkinson's disease showed excess mortality on selegiline. (5) The side effects of selegiline are similar to those of other antiparkinsonian drugs and amphetamine. Notable side effects include cardiovascular problems (postural hypotension, atrial fibrillation and arterial hypertension). (6) Selegiline can cause a serotoninergic syndrome and arterial hypertension, so must not be combined with pethidine, Tramadol ( Generic Ultram ), bupropion, sumatriptan, zolmitriptan or naratriptan. Concurrent treatment with serotonin reuptake inhibitor antidepressants should also be avoided. (7) Given the only moderate effects of selegiline in Parkinson's disease, and the possibility of a slight increase in mortality, there is no justification for prescribing this medication in patients with Parkinson's disease. (8) Whatever the stage of Parkinson's disease, there is no justification for starting patients on selegiline. Patients who are already taking selegiline should only continue to take it if they feel a clear benefit and are free from risk factors for early mortality, especially cardiovascular disease.

Premedication with Tramadol ( Generic Ultram ) in patients undergoing colonoscopy: a double-blind randomized placebo-controlled study.Grossi L, Cappello G, Marzio L.Department of Medicine and Sciences of Aging, School of Gastroenterology, Unit of Internal Medicine I, Ospedale Spirito Santo, Pescara, Italy.Colonoscopy is often disturbed by poor patient tolerance; benzodiazepines or opiates are routinely used to overcome such problems, despite the possibility of undesired effects. Tramadol ( Generic Ultram ), an opiate analogue with potentially fewer side effects, has not been tested yet to this end. The aim of the study was therefore to evaluate the efficacy of Tramadol ( Generic Ultram ) as a premedication for the colonoscopic procedure. Fifty patients were randomly allocated to receive an i.v. infusion of 100 ml saline, with 100 mg Tramadol ( Generic Ultram ) or alone, before endoscopy. At the end of the procedure patients were asked to score the discomfort experienced and to give an exam evaluation. The endoscopist also analyzed his performance. Tramadol ( Generic Ultram ) patients reported a pain score of 39 +/- 10 (mean +/- SE), compared to 45 +/- 8 for the placebo group (P = 0.25); the evaluation of endoscopy was also similar (Tramadol ( Generic Ultram ), 66 +/- 12; placebo, 70 +/- 9; P = 0.15). The endoscopist also reported a similar score (65 +/- 4 after Tramadol ( Generic Ultram ); 69 +/- 4 after placebo; P = 0.2). No significant sex- or age-related differences were detected. We conclude that Tramadol ( Generic Ultram ), at least as a monotherapy, seems scarcely effective for controlling pain evoked by colonoscopy.

Population pharmacokinetic modelling of Tramadol ( Generic Ultram ) with application of the NPEM algorithms.Gan SH, Ismail R, Wan Adnan WA, Zulmi W, Jelliffe RW.Department of Pharmacology, School of Medical Science, Universiti Sains Malaysia, Kubang Kerian, Kelantan, Malaysia. BACKGROUND AND OBJECTIVE: Although the kinetic behaviour of Tramadol ( Generic Ultram ) has been described, the present study is the first to our knowledge, to report specifically on the population pharmacokinetic modelling of Tramadol ( Generic Ultram ) hydrochloride. METHODS: The parametric Iterative Two-stage Bayesian Population Model (IT2B) program followed by the Non-parametric Expectation Maximization Population Model (NPEM2) program was used to determine population pharmacokinetic parameter values of Tramadol ( Generic Ultram ) in 138 postoperative orthopaedic Malaysian patients. All patients had received a 100 mg intravenous dose of Tramadol ( Generic Ultram ), infused over 2-3 min, as their first postoperative analgesic. Blood was sampled at 0 min and subsequently at 15, 30 min, 1, 2, 4, 8, 16, 20 and 24 h for serum Tramadol ( Generic Ultram ) high-performance liquid chromatography analysis. RESULTS AND DISCUSSION: The one-compartmental model pharmacokinetic parameters--volume of distribution (Vd), elimination rate constant (kel) and the total clearance rates (ClT)--found were: mean Vd = 167.6 +/- 63.84 L; median Vd = 161.48 L; mean kel = 0.1241 +/- 0.056 h(-1); median kel = 0.1138 h(-1); ClT = 19.57 +/- 9.51 L/h; median ClT =18.12 L/h. The interindividual coefficient of variation of ClT (48.56%) was higher than that of Vd (38.09%), indicating the presence of other possible influencing factors on Tramadol ( Generic Ultram )'s ClT such as CYP2D6 polymorphism, gender and age. Overall, NPEM2 suggested more diversity in the population than did IT2B.