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 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The general pharmacological properties of 1-(m-methoxyphenyl)-2-(dimethylaminomethyl)-cyclohexan-1-ol (tramadol; Tramal) are described and compared with those of other strong narcotic analgetics. In behavioral studies tramadol in high doses had a primarily stimulating effect in mice and rats and a sedative effect in rabbits and dogs. The Straub tail phenomenon, a reaction typical for mice administered morphine, was observed only after subtoxic doses of tramadol. In i.v. doses tramadol generally caused a weak central inhibition of non-stimulated and electrically stimulated brain activity in unanesthetized rabbits. Muscle tone and motor coordination in rats and mice were only slightly affected by the drug, in contrast to the effect of morphine. Unlike other strong analgesics tramadol in doses of 5--20 mg/kg i.v. did not cause respiratory depression and even clearly increased respiratory volume and rate in conscious rabbits and anesthetized dogs. In cats and dogs i.v. doses of tramadol up to 10 mg/kg were well tolerated in the cardiovascular system. Tramadol has a slight, papaverine-like spasmolytic effect and no effect on gastrointestinal motility or urinary and electrolyte excretion. The drug showed no antipyretic properties in rabbits. It inhibited edema in rats and guinea pigs but had no antiproliferative effect in the cotton pellet test in rats. Tramadol did not inhibit monoamine oxidase activity or cause enzyme induction in the rat liver.
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PMID:[General pharmacological studies on tramadol, a potent analgetic agent (author's transl)]. 30 47

The effect of tramadol on laryngeal reflex activity was assessed in a double-blind cross-over study in six volunteers receiving single oral doses of either codeine 50 mg, tramadol 50 mg or tramadol 100 mg. Laryngeal reactivity was measured by the response to the inhalation of dilute ammonia vapour. The minimum ammonia concentration required to induce a glottic stop was recorded prior to drug administration, and at 15, 30, 45, 60, 90, 120, 150 and 180 min thereafter. Psychometric tests were performed at 0, 45 and 105 min to detect any relationship between central sedation and changes in laryngeal reflex activity. The concentration of ammonia required to induce a glottic stop increased in all treatment groups, but more so in the tramadol groups. The time course suggested that the codeine effect peaked early, and had returned to normal within 2 h. For tramadol 100 mg, laryngeal depression appeared to be still increasing at the end of the 3-h study period. No correlation was found between laryngeal and sedative effects. Tramadol is produced as a racemic mixture, in which one isomer acts through an opioid receptor pathway whilst the other affects noradrenergic and serotonergic mechanisms. Both of these routes of action may be involved in the suppression of the response to experimentally induced cough.
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PMID:A comparison of the effects of codeine and tramadol on laryngeal reactivity. 155 50

Accidental rectal administration of 27 mg/kg of the narcotic analgesic Tramadol to a five-week-old infant resulted in severe cerebral depression, which had to be treated with Naloxone during 48 hours. The severity and the duration of this intoxication are not explained solely by the high dosage of Tramadol. A decreased elimination kinetics and an increased permeability of the blood-cerebrospinal fluid barrier probably also account for the pattern of the present intoxication.
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PMID:[Acute poisoning with a narcotic (Tramadol) in an infant of five weeks]. 322 Jul 91

The analgesic agent, tramadol, was tested on motor and sensory responses of the nociceptive system in rats. The tail-flick response to radiant heat was dose dependently depressed by tramadol (1-10 mg/kg i.p.), and the antinociceptive effect of the drug was reduced by naloxone in the same range of doses that antagonized the effect of morphine. Tramadol (100 micrograms) microinjected into the periaqueductal grey (PAG) prolonged the tail-flick latency and this effect was abolished by naloxone (0.2 mg/kg i.p.). Aminophylline (25 mg/kg i.p.) did not prevent the antinociceptive effect of tramadol (5 mg/kg i.p.). Tramadol (20 and 40 mg/kg injected i.v.; 100 and 200 micrograms injected intrathecally (i.t.); 100 micrograms injected into the PAG) depressed both the spontaneous activity in ascending axons and their activity due to stimulation of afferent C fibres and co-activation from afferent A delta fibres in the sural nerve. Naloxone injected i.v. at a dose (0.2 mg/kg) that had proven fully effective against the effects of morphine antagonized only the effect on spontaneous activity caused by i.v. injection of tramadol. A high dose of naloxone (1 mg/kg i.v.) not only abolished the depression of spontaneous activity caused by an i.t. injection of tramadol (200 micrograms) but also significantly reduced (but did not abolish) the activity in ascending axons evoked from afferent C fibres while the depression of co-activation from afferent A delta fibres remained unchanged. Aminophylline (50 micrograms i.t.) failed to abolish the depression by tramadol of ascending nociceptive activity. The activity elicited in ascending axons by stimulation of afferent A beta fibres was not changed by i.t. injection of tramadol (200 micrograms), which was evidence that the antinociceptive effect of tramadol is not due to a local anaesthetic action. It is concluded that tramadol produces its antinociceptive and analgesic effects through spinal and supraspinal sites of action. Since the effects of tramadol and morphine differ in some respects, it must be assumed that they are due to binding to different opiate receptors or that some of the effects of tramadol are not mediated by opiate receptors alone.
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PMID:Effects of tramadol on motor and sensory responses of the spinal nociceptive system in the rat. 365 36

A variety of opioids is available for treatment of acute pain. Sometimes administration is limited due to typical side effects such as respiratory depression or pressure increase in the pulmonary circulation. Tramadol, a synthetic opioid, was investigated in a dosage of 1.5 mg/kg body weight i.v. with regard to changes in haemodynamic parameters and in blood gases. The haemodynamic parameters generally remained stable; all changes were statistically non significant. There were no signs of respiratory depression. The risk of pain therapy with opioids seems to be reduced further by the introduction of this agent.
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PMID:[Effects of tramadol on haemodynamics and blood gases in the early postoperative period]. 681 68

The author reports a new technique of balanced anaesthesia using a pump-controlled 0.1% solution of Tramadol instead of the inhalation of halothane, enflurane or infusion of neuroleptanalgetic agents. Tramadol (Tramal) is a new analgetic drug without side effects: no postnarcotic respiratory depression, sickness or vomiting do not occur, and it does not interfere with the cardiovascular system. The other great advantage is the ultrashort recovery of the patient, mostly with 30-60 s, even after long lasting surgical procedures over several hours. The author has been convinced for more than 15 years that the future of anaesthesia no longer lies in the inhalation of chloroformoids, but in the infusion of analgesic substances. His experience has shown that the analgesic drug Tramadol, which has practically no side-effects, is a considerable advance into this direction. Last but not least this also applies to the prompt post-anaesthetic recovery and the absence of postoperative complications. This technique has been used in the last two years in 7500 patients, So far we have not seen an contraindications to Tramadol infusion. On the contrary, the greater the risk, the more this form of anaesthesia was found to be indicated.
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PMID:[Infusion-controlled Tramal-anaesthesia (author's transl)]. 721 51

Tramadol-HCl was used clinically in the form of a continuous infusion as the analgesic component of a balanced anaesthetic technique. In over 90% of the anaesthetics a further injection of barbiturate and/or supplementary muscle relaxant was necessary because the patients did not tolerate the operative procedure. Although a higher dosage of Tramadol reduces significantly the supplementary barbiturate dosage per kilogram bodyweight per minute which is required, it has no effect on the incidence of reflex movements, nor does it prevent the marked intraoperative rise of diastolic blood pressure. The balanced anaesthetic with Tramadol-HCl is characterized by prompt awakening, total amnesia, good post-operative analgesia and minimal side effects (occasional nausea). In particular, there was no case in which there was noticeable respiratory depression. As insufficient analgesia and hypnosis is provided by Tramadol-HCl, making the administration of muscle relaxants and barbiturates obligatory, there is no significant advance in our technique of using Tramadol-HCl, despite the advantages which have been outlined.
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PMID:[The clinical usefulness of Tramadol-infusion anaesthesia (author's transl)]. 733 89

Tramadol is effective in treating both acute and chronic pain, exhibiting a potency equivalent to that of pethidine, and it has an acceptable adverse event profile. Whilst the most common adverse events are nausea, vomiting, drowsiness and dizziness, as would be expected from an opioid, there is a noticeable lack of respiratory depression. This latter property, together with its low potential for the development of tolerance and dependence, make tramadol a most interesting agent for clinical use. The studies reported in this article illustrate the beneficial and adverse effects of tramadol to enable the clinician to judge the value of this agent.
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PMID:Chronic pain--challenge and response. 751 24

Tramadol (Zydol-Searle) is a centrally acting opioid analgesic newly marketed in the UK for use by mouth or injection. It is licensed for the prevention and treatment of moderate to severe pain. The manufacturer claims that it causes less constipation and respiratory depression than conventional opioids and that it offers a special "dual action". We examine the claims and consider the place of tramadol.
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PMID:Tramadol--a new analgesic. 763 11

Tramadol is a centrally acting analgesic which possesses opioid agonist properties and activates monoaminergic spinal inhibition of pain. It may be administered orally, rectally, intravenously or intramuscularly. In patients with moderate to severe postoperative pain, intravenous or intramuscular tramadol has generally proved to be of equivalent potency to pethidine (meperidine) and one-fifth as potent as nalbuphine. Intravenous tramadol 50 to 150mg was equivalent in analgesic efficacy to morphine 5 to 15mg in patients with moderate pain following surgery; however, when administered epidurally tramadol was one-thirtieth as potent as morphine. Tramadol has demonstrated efficacy in a few studies in the short term treatment of chronic pain of various origins. Orally administered tramadol was found to be an effective analgesic in step 2 of the World Health Organization's guidelines for the treatment of patients with cancer pain. Tramadol is well tolerated in short term use with dizziness, nausea, sedation, dry mouth and sweating being the principal adverse effects. Respiratory depression has been observed in only a few patients after tramadol infusion anaesthesia. When used for pain relief during childbirth, intravenously administered tramadol did not cause respiratory depression in neonates. The tolerance and dependence potential of tramadol during treatment for up to 6 months appears to be low, although the possibility of dependence with long term use cannot be entirely excluded. Thus, evidence to date of the analgesic effectiveness of tramadol combined with a low respiratory depressant effect and low dependence potential in short term use, suggests that the drug may become a useful alternative to the opioid analgesics currently available for the treatment of patients with moderately severe acute or chronic pain.
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PMID:Tramadol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute and chronic pain states. 769 19


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