Posts Tagged ‘Opioids’

The Unique Pain Medication

June 17th, 2010
Yury Bayarski asked:




Tramadol has been used as an analgesic since the late 1970s, and became one of the most popular analgesics of its class in Germany. International interest for the drug has been renewed when it was discovered that tramadol not only acts like opioids, but also inhibits serotonin and noradrenaline reuptake.

Mechanism of action

Tramadol is a unique medication. Its mode of action and safety profile distinguishes it from other opioids. It is classified as an atypical centrally acting analgesic, and has opioid and non-opioid properties. Tramadol is a synthetic analogue of codeine that has weak opioid agonist properties. It also inhibits the neuronal reuptake of norepinephrine and serotonin as do the antidepressant drugs

Tramadol has strong structural similarities to the antidepressant venlafaxine. Because of its similarities to venlafaxine, tramadol may possibly exert a degree of antidepressant effect in certain patients, particularly those with chronic pain.

Side effects

Tramadol is generally well tolerated, the most common side effects being nausea and vomiting. In contrast to agents such as morphine and pethidine, respiratory depression rarely occurs during tramadol treatment at equipotent doses. But large doses of tramadol may increase the respiratory effects of other drugs. It is also associated with a low incidence of cardiac depression and significantly less dizziness and drowsiness than morphine.

Finally, dependence and abuse potential is relatively low because it has only a weak opioid effect. The low abuse potential of tramadol has been demonstrated by postmarketing surveillance data.

Tramadol appears to carry the same risk of urinary disorders (difficulty in micturition, urinary retention) as other opiates.

The medication should be avoided in persons with epilepsy and used cautiously in those taking medications which lower the threshold for seizures.

Tramadol uses

It is effective in different types of moderate-to-severe pain, including neuropathic pain. This medication has a dose-dependent efficacy that lies between that of codeine and morphine, with a parenteral potency comparable to that of pethidine.

Comparative studies have demonstrated that tramadol is more effective than NSAIDs for controlling post operative pain. Moreover, as the mode of action of tramadol does not overlap with that of NSAIDs, it is a useful agent to be combined with these drugs. Use of a combination of tramadol and NSAIDs allows the tramadol dose to be reduced and results in a lower incidence of side effects.

Tramadol may be particularly useful for elderly population suffering from osteoarthritis because, unlike NSAIDs, it does not aggravate high blood pressure and cardiovascular complications, nor does it have the potential to cause peptic ulcer disease.

Tramadol has been used with good results for the management of labour pain without respiratory depression of the neonate. It is effective for the treatment of pain from myocardial ischaemia, renal colic and acute trauma.

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The Unique Pain Medication

March 13th, 2010

Tramadol has been used as an analgesic since the late 1970s, and became one of the most popular analgesics of its class in Germany. The international appeal of the drug was renewed his tramadol was discovered that not only acts as the opiates, but also inhibits the reuptake of serotonin and norepinephrine.

Mechanism of action

Tramadol is a unique product. Its mode of action and safety profile distinguishes it from other opioids. It is classified as a centrally acting analgesic atypical and non-opioid and opioid properties. Tramadol is a synthetic analogue of codeine, which has a weak opioid agonist properties. It also inhibits the neuronal reuptake of norepinephrine and serotonin as antidepressants

Tramadol has strong structural similarities to the antidepressant venlafaxine. Because of its similarities to venlafaxine, tramadol May possibly exercise some degree of antidepressant effect in some patients, particularly those suffering from chronic pain.

Side effects

Tramadol is generally well tolerated, the most common side effects are nausea and vomiting. Unlike agents such as morphine and pethidine, respiratory depression rarely occurs during tramadol to equipotent doses of treatment. But high doses of tramadol in May increased the respiratory system, the effects of other drugs. It is also associated with a low incidence of cardiac depression and significantly less dizziness and drowsiness than morphine.

Finally, the potential for abuse and dependence is relatively low because it has only a weak opioid. The low abuse potential of tramadol has been shown by data from post-marketing surveillance.

Tramadol appears to have the same risk of urinary tract (difficulty urinating, urinary retention) than other opiates.

The drug should be avoided in people with epilepsy and used with caution in those taking drugs that lower the threshold for seizures.

Tramadol uses

It is effective in different types of moderate to severe pain, including neuropathic pain. This drug has a dose-dependent efficacy that lies between that of codeine and morphine, with a parenteral power comparable to that of pethidine.

Comparative studies have shown that tramadol is more effective than NSAIDs for controlling post-operative pain. Moreover, as the mode of action of tramadol does not overlap with that of NSAIDs, it is an agent to be combined with these drugs. Using a combination of tramadol and NSAIDs allows the tramadol dose reduced and results in a lower incidence of side effects.

Tramadol May be particularly useful for elderly people suffering from osteoarthritis because, unlike NSAIDs, it does not aggravate hypertension and cardiovascular complications, has not the potential to cause peptic ulcers.

Tramadol has been used successfully to manage labor pain without respiratory depression in the newborn. It is effective for the treatment of pain of myocardial ischemia, renal colic and acute trauma.



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Assessment of Tramadol in the Management of Pain

January 2nd, 2010

Tramadol is a cyclohexanol derivative with mu-agonist activity. It has been used as an analgesic for postoperative or chronic pain since the late 1970s, and became one of the most popular analgesics of its class in Germany. International interest has been renewed during the past few years, when it was discovered that tramadol not only acts on opioid receptors, but also inhibits serotonin (5-hydroxytryptamine; 5-HT) and noradrenaline (norepinephrine) reuptake. This review aims to provide a risk-benefit assessment of tramadol in the management of acute and chronic pain syndromes.

Tramadol has been used intraoperatively as part of balanced anaesthesia. Such use is under discussion, however, as it was associated with a high incidence of intraoperative recall and dreaming, and postoperative respiratory depression has been described after intraoperative administration of high doses. Postoperatively, intravenous and intramuscular tramadol has been used with good efficacy. Analgesic doses were comparable with pethidine (meperidine) and 10 times higher than morphine. Nausea and vomiting were the most frequently reported adverse effects.

In controlled studies, haemodynamic and respiratory parameters were only minimally impaired. The risk of severe respiratory depression in typical dosages is negligible in comparison with other opioids used for postoperative pain management. Tramadol has been used with good results for the management of labour pain without respiratory depression of the neonate. It was also effective for the treatment of pain from myocardial ischaemia, ureteric colic and acute trauma. Good results have been published for cancer pain management with tramadol in several studies.

The potential for abuse or addiction seems to be minimal, and serious complications have not been reported. For patients with severe pain, the efficacy of morphine is superior, and most patients with adequate analgesia from tramadol had to be changed to a more potent opioid after a few weeks due to increased nociceptive input during tumour progression.

Tramadol can be recommended as a safe and efficient drug for step II according to the World Health Organization guidelines for cancer pain management.

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