Tramadol The route of healing

What does “mechanism of action” mean? This phrase refers to the effect that a drug substance causes on a living organism or in a biochemical system. The drug substance can produce four main actions: depressing, stimulating, destroying cells and replacing substances.

The desired activities may be cellular membrane disruption, chemical reaction, interaction with enzyme proteins, interaction with structural proteins, interaction with carrier proteins, interaction with ion channels, binding to receptors, hormone receptors, neuromodulator receptors and neurotransmitter receptors.

Although there are many studies performed on thousands of volunteers to know more about analgesics, Tramadol mechanism of action is not completely understood. From studies with animals, at least two complementary mechanisms seem to be valid: binding of parent and M1 metabolite to µ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin. The comparative contribution of both Tramadol and M1 to human analgesia depends on the plasma concentrations of each compound. Apart from analgesia, Tramadol may cause a group of symptoms similar to that of an opioid.

The mechanism explained above seems to be a little bit complicated if you are not a scientist but its objective is to clarify why Tramadol can work for treating pain. The different way in which Tramadol provides analgesia with less side effects than the ones caused by other similar products may be explained by Tramadol dual mechanism of action.

In animal and human models both opioid and monaminergic mechanisms contribute to the analgesic efficacy of Tramadol, with the monaminergic mechanism likely accounting for more than half of the analgesic effect.

Tramadol is related to the uptake inhibition of the neurotransmitters noradrenaline and serotonin. Its dual mechanism of action differentiates it from prototypic opioids such as morphine or codeine. This mechanism of action allows Tramadol to have a significant therapeutic importance to improve pain. Tramadol has no clinically related effect on respiratory or cardiovascular parameters. Tramadol may demonstrate particularly useful in patients with poor cardiopulmonary function and in other special patient groups.

Drugs may be classified like any other chemical agent that affects life process. The relationship between the dose administered to a patient and the usefulness on the treatment of the disease he or she suffers from.

Differences between Pharmacokinetics and Pharmacodynamics: The first one is focused on drug quantitative performance in the body. The second one studies the biochemical and physiological effects of the drugs and their mechanism of actions. So, Tramadol mechanism of action explains the effect that Tramadol has on human body functions. In general, drugs can’t create new functions but they are able to modulate the ones that already exist. It has been observed that the drug effects are the result of their relationship with molecules.

Tramadol mechanism of action allows pharmaceutical products that contained Tramadol to produce analgesia that can be compared to Codeine or Dextropropoxyphene. In addition, it produces the beneficial effects that may improve post-surgical pain, obstetric pain, cancer pain and chronic pain of mechanical and neurogenic origin.

Since 2004, there has been a state of uncertainty and controversy about the use of nonsteroidal anti-inflamatory medications and cyclooxygenase (COX)-2 inhibitors, so other analgesics have started to be used for treating moderate to severe pain. This is Tramadol case. Although it was launched in 1977, new uses have been discovered for this active principle.

At the same time, products manufactured with Tramadol may be habit forming. Patients should not take more doses than the ones recommended by their physicians. On the other hand, if they feel that Tramadol mechanism of action is not acting properly, they should contact their healthcare providers immediately.

Because of its mechanism of action, Tramadol may be coadministered with other analgesics, especially those with peripheral action. Drug substances that depress CNS function may enhance the sedative result of Tramadol. When facing a treatment to get pain management, patients should know everything about the drug they will use. Physicians are in charge of providing them with the necessary information to make them feel more confident.

Tramadol mechanism of action is available for those patients who need relief for their pain and suffering. This “mechanism” seems to really “act” as a loyal ally.

Benefits and Side effects of Tramadol

TRAMADOL

 Ultram^®) is a prescription medication licensed for the treatment of pain. Specifically, tramadol benefits include treating moderate to moderately severe pain in adults (age 16 and older).

Tramadol is classified as a "centrally acting opioid analgesic." This means that it works in the central nervous system (the brain and spinal cord), acts much like morphine in the body, and relieves pain. Tramadol also works in a similar manner as someantidepressant medications by inhibiting the reuptake of certain brain chemicals (serotonin and norepinephrine).

Originally, tramadol was marketed as a medication with weak narcotic effects and little potential for abuse. However, research has since demonstrated that this drug works primarily through morphine-like activity, and numerous cases of abuse and dependence have been reported.



Throughout all the clinical trials and the accumulating years of experience after launch, Tramadol has proved a remarkably reliable and effective painkiller:

• it treats and relieves pain no matter what the cause;
• it works equally well across the age range from 16 years upwards although the dosage may be changed to reflect different body weights;
• there’s no difference in its effectiveness in all the different races;
• it’s equally effective in both sexes;
• there are side effects but, in most people, they last only a short period of time and are not serious; and
• there’s only a low level risk of it proving habit-forming.

SIDE EFFECTS

Tramadol Side Effects:  Brand name Ultram. Tramadol is available as 50 and 100 mg dose tablets. There are also sustained release formulations, and formulations that also contain acetaminophen.   Tramadol is a synthetic opioid-like drug that has its effects primarily as an agonist (stimulator) of the  mu opioid receptor site.  Tramadol is used primarily for moderate to severe pain control.  It has many properties in common with other opioid medications, but is different in that it acts more specifically on the opioid mu receptor than most other opioids. (there are other opioid receptors)  Like other opioids is potentially habit forming, although some experts feel this is a less severe and common problem with tramadol than with other opioids.  Tramadol is also used for treatment of restless legs syndrome and fibromyalgia, and has additional properties that affect neurotransmitter release and reuptake.

Common Tramadol Side Effects:  Tramadol side effects include many of the gastrointestinal side effects of opioid agonists including constipation, nausea, vomiting, dyspepsia and occasionally diarrhea.  These are due to the opioid mu receptors in the GI tract that lead to increased stimulation of the circular muscles and decreased stimulation of the longitudinal muscles of the colon wall.  This leads to poor propulsive effect of the bowel content and increased churning of the bowel content, and caused dryer and firmer stool, and slower transit time.  It can also lead to decreased feeling of fullness in the distal colon and reduced urge to defecate. Non GI tramadol side effects that are common include somnolence, itching, dizziness, sweating and flushing.

Life Threatening Tramadol Side Effects:  Seizures are the most important tramadol side effect to consider. They are more common in people with a history of seizures, and if you have a history of seizures you should be sure your physician knows about this history, and if used tramadol dosing should be minimized.  The other serious side effects can be primarily grouped into the allergic side effects including angioedema, anaphylaxis, severe rashes including the Stevens-Johnson Syndrome and toxic epidermal necrolysis, and those side effects shared with most opioids including withdrawal syndrome if discontinued suddenly, dependency and abuse, respiratory depression, and depression/suicide  Other serious tramadol side effects can be the serotonin syndrome, and orthostatic hypotension (drop in blood pressure on sitting or standing)

Unusual Tramadol Side Effects:  Seizures are the most unusual tramadol side effect that is occasionally seen.

Drug Interactions:  Tramadol is contraindicated for use with alcohol (don’t drink alcohol while taking tramadol), some HIV drugs, and any MAO inhibitors (mono-amine oxidase inhibitors)  Tramadol is metabolized extensively in the liver using the cytochrome P-450 pathway including several specific enzyme processes (2B6, 2D6, and 3A4).   This leads to many drug interactions including bupropion, digoxin, warfarin and such a long list of other medications that it is not realistic to discuss them all here.  Refer to the manufacturers prescriber information for more details.

Pregnancy and Lactation Class:  Tramadol is pregnancy Category C and is considered possibly unsafe in lactation.

Special Considerations:  Tramadol is generally considered to be less addicting than many other opioid analgesics, but it is still an opioid mu receptor and has the potential for abuse.  Do not share this medication with others, and certainly do not crush the pills for inhalation or injection.  Seizures are the unique tramadol side effect and is especially a concern if used taken in higher than the recommended dosage or if you have a history of seizures.

About tramadol

Tramadol or Ultram® is a German invented pain reliever created in the 1970s. It is quite different than other prescribed pain relievers like codeine or hydrocodone, and generally considered far less addictive, though people can become addicted to it. The drug has similar action to certain antidepressants, particularly the medication Effexor® which is a selectedserotonin reuptake inhibitor (SSRI). Most often tramadol is prescribed to treat pain associated with various forms of neuralgia. Other conditions for which tramadol might be used are called off-label or investigational and these include restless legs syndrome, migraines, withdrawal of other more addictive medications, fibromyalgia, and obsessive compulsive disorder.

The medication may be a preferred drug for people suffering from chronic pain conditions because it tends to be well tolerated without huge risk of addiction or serious side effects when used appropriately. However, there are dangers, as with any medicine in overusing Ultram®, and many people who stop using the medication suddenly do suffer withdrawal symptoms. Ultram® is a central nervous system depressant and it shouldn’t be used in combination with other things that can depress the central nervous system. Those who take tramadol should avoid using alcohol, taking tranquilizers, or any other medications that can suppress breathing.

Common side effects in regular dosage can include nausea, diarrhea, headache, dizziness, drowsiness and constipation. Withdrawal symptoms if the medication has been taken for a long time can include sweating, anxiety, poor sleep, pain and tremors. If people have taken tramadol for a long period of time, they should work with a doctor to plan safe withdrawal from the medication. Allergy or sensitivity to Ultram® is very rare but may include hives, trouble breathing and dizziness. Symptoms of chest pain, depressed breathing, seizures or rapid heart rate are medical emergencies, but again are extremely rare.

Certain medications are contraindicated when Ultram® is used. It should never be used with other SSRIs (Prozac®, Zoloft®, Paxil®, Luvox® for example) since this can cause a rare complication called serotonin syndrome. Severe cases of this condition may result in seizures and death. As much as having serotonin is a good thing, too much in the body is potentially deadly. Other drugs that hazard some risk of creating serotonin syndrome include monoamine oxidase inhibitors, or first generation antidepressants. When patients take any type of antidepressant they should make sure doctors are aware of this fact before they take tramadol.

Using this medication is also not advised for women who are pregnant or nursing babies. Others who should avoid this drug include those with heart or kidney disease. People with recurrent or chronic breathing conditions should inform doctors prior to taking Ultram®.

Some common drugs lower the effectiveness of tramadol. These include carbamazepine, an anti-seizure medication that is also widely used as a mood stabilizer in patients with bipolar disorder. Quinidine, which regulates heart rhythm, may make the pain fighting action of Ultram® less effective too.

There are several ways to take tramadol. It comes in capsules, tablets, suppositories, and in injectable forms. Some preparations of the medication include other analgesics like acetaminophen or anti-inflammatory agents like aspirin. Recommended dose is usually no more than 400 mg per day. It is especially important to use this medication exactly as prescribed, for the length of time prescribed. It should never be shared with others or used in a manner unadvised by a physician.