UMLS:C0011570 - FACTA Search

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Query: UMLS:C0011570 (depression)
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The need for analgesia to overcome pain in labour is highly requested by women today. Various ways either non pharmachologic e.g. Emotional sustain, psycho-prophylactic preparation, yoga and hypnosis or pharmachologic such as epidural blockade or parenteral are used. Therefore in our study we evaluated the efficacy and tolerability of the two opioids usually used today in parenteral analgesia to reduce pain during labour: Tramadol and Meperidine. We studied two groups of patients each made up of 20 women in labour, all at term and with a physiologic course of pregnancy. 75 mg i.m. of Meperidine chloryhydrate were somministered in the first group while in the second group 100 mg i.m. of tramadol chloryhydrate were somministered. Various maternal, fetal and neonatal parameters were then monitored demonstrating--A moderate maternal analgesic effect in both drugs (evaluated through the analogic grading of pain). In the group to whom Meperidine was given, sedative effects on the mother were observed associated with respiratory depression in the newborn (the latter evaluated through the Apgar index at 1st and 5th minute of life and pH of the blood obtained at the umbilical cord. The data obtained permitted us to conclude that Tramadol in accordance to the obtained in literature gives an analogous analgesic effect, with better tolerability for the absence of collateral effects on the mother, fetus and newborn.
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PMID:[Evaluation of the peripartum effects of 2 analgesics: meperidine and tramadol, used in labor]. 1142 77

An ideal analgesic for patients after craniotomy should neither cause respiratory depression, nor affect intracranial pressure (ICP) and cerebral perfusion pressure (CPP). The aim of the study was to evaluate the effect of Tramadol (T) on ICP and CPP, as well as to determine its analgetic efficacy in patients (pts) after craniotomy. Thirty five pts aged 16 divided by 78 years (mean 46) entered the study. Twelve had GCS (Glasgow Coma Scale) scores < or = 8 and 23 pts had scores > or = 12. Fourteen pts were mechanically ventilated and 21 pts were breathing spontaneously (BS). Tramadol was injected i.v. at a dose of 0.75 mg/kg over 3 minutes in 11 pts (Group 1), 1.0 mg/kg over 5 minutes in 13 pts (Group 2) and 1.0 mg/kg over 10 minutes in 11 pts (Group 3) PaCO2 was measured before T in all pts and at 8 minute after injection in 21 BS pts. Heart rate (HR), mean arterial blood pressure (MBP), ICP, CPP and respiratory frequency (f) were registered before and in the 1st, 3rd, 8th, and 15th minute after T. Analgetic effect was evaluated in 22 conscious pts by comparing the pain intensity before and 30 minutes after T using a five-point verbal response scale. Mean control ICP was 17 mmHg. ICP over 15 mmHg was diagnosed in 15 pts (mean ICP equal 26 mmHg). Mean CPP for all 35 pts was 85 mmHg. There were no statistically significant changes in HR, MBP, ICP, and CPP after T in any particular group, nor were there changes in ICP in subgroups with normal and elevated ICP. No significant changes in PaCO2 and f were found in BS pts. Satisfactory analgesia was obtained in 50% of pts of Group 1, and in 88% of pts of Groups 2 and 3. We conclude that tramadol in doses of 0.75 mg/kg and 1.0 mg/kg i.v. does not affect ICP and CPP in adult postcraniotomy patients and seems to be a safe and effective analgesic at a dose of 1.0 mg/kg for postcraniotomy pain control.
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PMID:Tramadol for postoperative analgesia in intracranial surgery. Its effect on ICP and CPP. 1145 59

Tramadol hydrochloride is a centrally-acting, synthetic analgesic with a dual mechanism of action-weak opioid and monoaminergic effects. Tramadol is a racemic mixture and its mechanism of action via opioid and noradrenergic/serotonergic mechanisms is related to the independent effects of its two enantiomers. Interestingly, the enantiomers act synergistically to achieve better antinociceptive effect without enhancing side effects, moreover, lowering respiratory depression and tolerance/dependence. In several post-marketing surveillance studies tramadol is showed as effective as codeine, penthazocine, pethidine and morphine with good tolerability. Tramadol might be analgesic of choice for a wide variety of painful conditions.
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PMID:[Tramadol in the treatment of pain]. 1155 11

Tramadol hydrochloride is a racemic mixture of two enantiomers. It has analgesic activity suitable for mild to moderate pain, part of its analgesic activity being modulated via mu receptors. Adult studies have raised the question of increased electroencephalographic activity. The study examined the analgesic efficacy, respiratory effects, and behavior plus recovery-influencing properties of tramadol in the pediatric patient. Day-case dental extraction children, aged 4-7 years having 6 or more extractions, were studied. Tramadol drops, 3 mg/kg, plus oral midazolam, 0.5 mg/kg, were administered 30 minutes prior to a sevoflurane in N2O and O2 anesthetic. Forty children received this premedication treatment (T) and 10 entered a placebo control group (P), where no tramadol was administered. Entry was random, double blind, and parallel. Analgesic efficacy was measured using the Oucher face pain scale (OFPS), with responders scoring three or less. Respiration was measured by rate and oxygen saturation. Behavior and ease of mask induction were assessed on a 4-point scale. Recovery was measured with the Aldrete scale. Parameters were measured from 30 minute preanesthetic to 120 minute postanesthetic. Analgesic efficacy was shown, with an OFPS score of 11.42 (SD 18.66) (T) and 29.80 (SD 25.14) (P) (P < .05). Responders on tramadol were 77.5% versus 0% on placebo (P < .05). No respiratory depression was seen; rates and oxygen saturations were the same preanesthetic and postanesthetic. Similarly, the two groups had no cardiovascular differences. Preanesthetic behavior patterns were the same (P > .05), with 85% of the tramadol group being drowsy but awake versus 90% in the placebo group. Similarly satisfactory induction behavior was seen in 95% of the tramadol group and 90% of the placebo group. Recovery times were 48.6 minutes (SD 32.3) (T) and 43.1 minutes (SD 32.5) (P) (P > .05). It is concluded that tramadol at 3 mg/kg has no clinical respiratory depressant effect and that behavior and recovery times are unaffected. Analgesic efficacy is demonstrated.
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PMID:Tramadol drops in children: analgesic efficacy, lack of respiratory effects, and normal recovery times. 1169 48

Tramadol, an analgesic with mean potency one tenth that of morphine is used regularly for the treatment of chronic and postoperative pain. Previous reports have indicated that tramadol may induce seizure activity when given together with a selective serotonin reuptake inhibitor (SSRI). Therefore, its major mode of action may be questioned which purportedly is due to binding with the opioid receptor and partly due to the inhibition of monoamine reuptake. We therefore set out to study its potential in inducing seizure activity and to quantify its effect on EEG-power spectra and on the central modulation of sensory afferents in awake and trained dogs (n=7). In order to demonstrate if opioid receptors mediated these effects, incremental doses of tramadol were given which was followed by naloxone for possible reversal. After a wash-out period the same animals were exposed to graded doses of alfentanil, a pure mu-receptor agonist. Again this was followed by the opioid antagonist naloxone for reversal.The electroencephalogram (EEG) and the event-related evoked potentials (SEP) were used to demonstrate possible excitatory effects. In order to derive the SEP the front paw was stimulated electrically (Digi Stim II trade mark ) while the evoked potentials were picked up contralaterally from the somatosensory cortex using stick-on electrodes. 256 sweeps were averaged (Lifescan) and the peak-to-peak amplitude was measured to demonstrate CNS excitation compared to control (%). Additionally, the raw electroencephalogram was viewed for epileptogenic changes and its power computed into the various power bands alpha, beta, delta und theta using FFT over a time epoch of 60 s. Following control, graded doses of either tramadol (2-5-10 mg/kg i.v.) or alfentanil (10-30-60 microg/kg i.v.) were given every 15 min while the EEG and the SEP were recorded. Thereafter naloxone (20 microg/kg i.v.) was injected for reversal. Tramadol did not suppress the amplitude of the SEP at any dose. High doses (>5 mg/kg i.v.) resulted in an increase (+100%) of the amplitude of the evoked potential. This was accompanied by short-term muscle fibrillations, and a short-term spike-and-wave activity in the EEG followed by a long-lasting theta-dominance. These effects could not be reversed by naloxone. In contrast to tramadol, alfentanil induced a dose-related depression of amplitude in the SEP with a maximum of 82% suggesting a depressive effect of modulation of afferents in the sensory cortex. This effect was fully naloxone reversible and was followed by a rebound in amplitude of the SEP together with an increase in fast beta-waves in the EEG. Tramadol very little mediates its central action via the mu-opioid receptor as the present effects were not naloxone reversible. Consistent with the results is the very low affinity of tramadol to the opioid receptor which is several thousand times less than that of morphine. Most likely, inhibition of central norepinephrine and serotonin reuptake as well as the reduction in 5-HT-turnover may contribute to the effects of tramadol. Due to the monoamine reuptake inhibition an increase in transmission may result, triggering off excitatory phenomena with spike-and-wave activity in the CNS. Such excitatory effects, however, may only be seen when tramadol is used in doses exceeding the therapeutic range.
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PMID:[The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]. 1279 88

Tramadol is a centrally acting synthetic analgesic with mu-opioid receptor agonist activity, it is a widely prescribed analgesic used in the treatment of moderate to severe pain and as an alternative to opiates. Tramadol causes less respiratory depression than morphine at recommended doses. Its efficacy and low incidence of side effects lead to its unnecessary prescribing in patients with mild pain. Tramadol was classified as a "controlled drug" long after its approval for use in Jordan. Analysis of drugs of abuse in hair has been used in routine forensic toxicology as an alternative to blood in studying addiction history of drug abusers. A method for the determination of tramadol in hair using solid phase extraction and gas chromatography-mass spectrometry (GC-MS) is presented, the method offers excellent precision (3.5-9.8%, (M)=6.77%), accuracy (6.9-12%, M=9.4%) and limit of detection 0.5 ng/mg. The recovery was in the range of 87-94.3% with an average of 90.75%. The calibration curve was linear over the concentration range 0.5-5.0 ng/mg hair with correlation coefficient of 0.998. The developed method was tested on 11 hair samples taken from patients using tramadol as prescribed by their physician along with other different drugs in treating chronic illnesses. Tramadol was detected in all hair samples at a concentration of 0.176-16.3 ng/mg with mean concentration of 4.41 ng/mg. The developed method has the potential of being applied in forensic drug hair testing. In Jordan, hair drug testing started to draw the attention of legal authorities which stimulated forensic toxicologists in recent years to develop methods of analysis of drugs known or have the potential to be abused.
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PMID:Determination of tramadol in hair using solid phase extraction and GC-MS. 1292 14

An analysis of the treatment of nonmalignant pain in the elderly at a long-term facility was conducted to allow development of a pain management program that complies with both JCAHO guidelines for pain management and with the Tennessee Medicaid (TennCare) reimbursement schedule, and to determine if tramadol can meet the standards of pain management under these new guidelines. Inclusion criteria were residence in our long-term care facility; a pain intensity score > 4 on a modified Wong Baker Pain Scale; the patient having prescription orders for one or more of the following drugs: propoxyphene, meperidine, or high dosages of acetaminophen (approaching 4 g/day); suspected neuropathic or mixed nociceptive/neuropathic pain; and/or a diagnosis of diabetes, osteoarthritis, or degenerative joint disease. Exclusion criteria were history of seizures, history of opioid or alcohol abuse, and demonstrated hypersensitivity to tramadol or opioids. Tramadol administration began at a dose of 25 mg/day titrated up to a maximum of 300 mg/day over a 16-day period. Data were collected from computer records, dispensing reports, medication administration reports (MARs), current federal minimum data set (MDS) data, and weekly care plan meetings. Data were tabulated at baseline and 4-6 weeks after a stable dose of tramadol had been established. Fourteen residents (mean age 85 years, 1 male, 13 female) met the criteria and received tramadol up to 300 mg/day (qid). Tramadol reduced the residents' pain scores from an average of 6 to 2 using the Modified Wong Baker Pain Scale, reduced the percentage of residents taking propoxyphene from 50% to 14%, and reduced those taking high doses of APAP or APAP products from 43% to 14%. Tramadol reduced the percentage of residents falling, losing weight, showing no change or decline in activities in daily living (ADLs), displaying inappropriate behavioral symptoms, suffering depression, and/or taking psychotropic medications. In the state of Tennessee, new reimbursement schedules by TennCare have allowed our hospital to comply with the JCAHO standards of "optimal achievable care" for the treatment of pain by allowing the hospital staff to treat patients with newer, safer, more effective analgesics such as tramadol. Early results from this ongoing study have shown that tramadol can provide a safe and effective treatment on non-malignant pain in a long-term care facility and improve adherence to JCAHO and TennCare standards for proper pain management.
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PMID:Pain management in a long-term care facility: compliance with JCAHO standards. 1464 89

Tramadol (CAS 36282-47-0) plays an important role in the management of pain. With its dual mechanism of action (opioid agonist; weak noradrenaline and serotonin reuptake inhibitor) tramadol provides a kind of combined/adjuvant pain therapy. Besides its proven clinical efficacy tramadol is a safe drug as respiratory depression, cardiovascular side effects, drug abuse and dependence are of minor clinical relevance, unlike some other opioids. Following oral administration the bioavailability of tramadol is high (70-90%) and with new slow release preparations twice daily administration enables effective pain control. Tramadol is characterised by low plasma protein binding (20%) and quite extensive tissue distribution (apparent volume of distribution about 3 l/kg). Elimination is primarily by the hepatic route (metabolism by CYP2D6 to an active metabolite and by CYP3A4 and CYP2B6) and partly by the renal route (up to 30% of dose). Elimination half-lives of the active agents range between 4.5 and 9.5 h and total plasma clearance of tramadol is moderately high (600 ml/min). The interaction potential of tramadol is neglectable, as it does not affect the disposition of other drugs. It should be taken into account that inducers (e.g. carbamazepine) or inhibitors (e.g. quinidine for CY2D6) of drug metabolism might modify the elimination of tramadol. Likewise, if kidney (creatinine clearance below 30 ml/min) or hepatic function is severely impaired, some dosage reduction (approximately by 50%) or extension of the dosage interval should be considered. In conclusion, tramadol is an effective and safe analgesic with a very low interaction potential. Therefore it represents a drug of first choice if moderate to severe pain states have to be treated in pediatric, adult and elderly patients including those with poor cardiopulmonary function.
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PMID:Tramadol--the impact of its pharmacokinetic and pharmacodynamic properties on the clinical management of pain. 1465 Mar 59

Tramadol ((+/-)-tramadol) is an analgesic agent formulated as a racemic mixture (1:1) of (-)- and (+)-tramadol, which differ in their potency to bind to mu-opioid receptors and to inhibit monoamine-reuptake. We investigated the stereoselectivity of in vitro tramadol-induced vasodilatation of aortic rings and its effect on the arterial blood pressure measured in conscious Wistar rats. (+)-Tramadol, but not (-)-tramadol, produced a concentration-dependent relaxation of aorta precontracted with phenylephrine. The concentration-response curve was significantly altered by the removal of endothelium. Vascular relaxation was also inhibited by pre-incubation of endothelium-intact aorta with naloxone, suggesting the involvement of opioid receptors. The vasodilatation produced by tramadol was stereoselective, and the (+)-tramadol-induced vasodilatation was mediated by mu-opioid receptors and partially dependent on endothelium integrity. The hypotensive response induced by (+)-tramadol was also observed after bolus injection of 5.0 and 10.0 mg/kg. The results indicate that only high doses of tramadol cause cardiac depression and hypotension, indicating that it can be used safely.
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PMID:In vitro and in vivo vasodilator activity of racemic tramadol and its enantiomers in Wistar rats. 1637 Dec 27

Tramadol, a centrally acting analgesic, consists of two enantiomers, both of which contribute to analgesic activity via different mechanisms. (+) Tramadol and the metabolite (+) -O- desmethyl-tramadol (M1) are agonists of the mu opioid receptor. (+) Tramadol also stimulates presinaptic release of serotonin and inhibits serotonin reuptake whereas (-) tramadol inhibits norepinephrine reuptake. Thus tramadol enhances inhibitory effects on pain transmission both by opioid and monoaminergic mechanisms. The complementary and synergistic actions of the two enantiomers improve the analgesic efficacy and tolerability profile of the racemate. Following oral administration the bioavailability of tramadol is high and with new slow release preparations twice daily administration enables effective pain control. The recommended maximum daily dose of tramadol is 400 mg/day. Tramadol is characterised by low plasma protein binding and quite extensive tissue distribution. Elimination is primarily by the hepatic route (metabolism by CYP2D6) and partly by the renal route. It is effective in different types of moderate-to-severe acute and chronic pain, including neuropathic pain, low back pain, osteoarthritis pain and breakthrough pain. It also causes fewer opioid-type adverse effects, e.g. nausea, drowsiness, vomiting, dry mouth and constipation. Although trials in literature demonstrate immune-stimulating effects of tramadol, there are also trials suggesting immunesuppressive effects that are lesser than morphine. Owing to its pharmacological properties, tramadol is more appropriate than NSAIDs for patients suffering from gastrointestinal and renal problems. Besides its proven clinical efficacy tramadol is a safe drug as respiratory depression, cardiovascular side effects, drug abuse and dependence are of minor clinical relevance, unlike some other opioids.
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PMID:[An atypical opioid analgesic: tramadol]. 1678 63

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