Tapentadol is a drug for pain. It was approved by the US FDA for the treatment of moderate to severe pain. The FDA news release was dated 24 November 2008, although the actual approval was a few days earlier.

Tapentadol acts on μ-opioid receptors, making it similar to morphine and its ilk. Do we need another opioid agonist? And if so, why? Suspicions deepen because it was produced by the same company that makes tramadol. Indeed, it is similar to tramadol in many ways. Tramadol is the active ingredient in Ultram®, now available as a generic. This is sounding like a familiar me-too drug story.

On the other hand, chronic pain is a common problem:

Chronic pain prevalence estimates were 10.1% for back pain, 7.1% for pain in the legs/feet, 4.1% for pain in the arms/hands, and 3.5% for headache. Chronic regional and widespread pain were reported by 11.0% and 3.6% of respondents, respectively.

Existing treatments often are not satisfactory. With opioid medications, there is risk of psychological dependence and various kinds of diversion and misuse. People put it in their noses and veins and things like that. Perhaps more importantly, though, the drug tramadol, is the fact that some people develop adverse effects at the doses required to achieve adequate pain control.

So what makes tapentadol different?


Much of the information presented here comes from this article:

(-)-(1R,2R)-3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol Hydrochloride (Tapentadol HCl): a Novel µ-Opioid Receptor Agonist/Norepinephrine Reuptake Inhibitor with Broad-Spectrum Analgesic Properties

First, let's look at tramadol. Tramadol is an agonist for μ-opioid receptors, but it also inhibits reuptake of serotonin and norepinephrine (monoamines). It appears that the effect on monoamines is something that is important for the analgesic effect of tramadol. After all, tramadol is a rather weak agonist of opioid receptors.

Tramadol, however, has several problems. The weakness of its effect on opioid receptors means that it would not be expected to have a robust effect on acute pain. The fact that tramadol depends upon the monoamine effect for its action, means that it often works better for chronic pain. (Note that the use of weasel words, e.g. "expected," "often" is intentional; it reflects the fact that different people respond differently.)

Furthermore, soma pill description, tramadol by itself is not very effective unless some of it is metabolized to O-desmethyl-tramadol. This requires an enzyme, soma pill description, cytochrome P450 2D6 (CYP2D6). Persons who are relatively deficient in CYP2D6 activity, or who are also taking a drug that blocks CYP2D6, may not get the full effect.

Lastly, tramadol is a racemic mixture; that is, it comes in left- and right-handed versions. The actions of the two versions are different, and the actions of the two versions of the metabolite are different, the drug tramadol. This is not necessarily a problem, but it is a complicating factor.

With the understand on tramadol, we now can take a look at tapentadol to see if it offers any meaningful advantage.

The key differences are: tapentadol has a stronger effect on the reuptake of norepinephrine than serotonin, it does not depend on CYP2D6 activity, and it is not a racemic mixture. All of these factors are advantageous, at least theoretically, karachi. Based upon these findings, one would expect that tapentadol would be less prone to cause adverse effects, and that it would be much less likely to be involved in drug interactions. Premarketing data are encouraging, though.

Additionally, tapentadol is more potent than tramadol at the μ-opioid receptor, but less potent than morphine. Note, however, that higher potency does not necessarily translate into higher clinical utility.

I tend to think that the advantages are great enough to justify the development of tapentadol for the market, karachi. There are so caveats, however. It is not possible to make any firm assessment of a risks of a drug, prior to its release into the wider market. That is, soma pill description, the basic pharmacology suggests that most patients will be less likely to have adverse effects, patient education tramadol, but this remains to be seen.

Also, as is the case with any opioid agonist, the potential for diversion and abuse cannot be assessed fully. There are examples of drugs that were thought to present a minimal risk of abuse, prior to being released into the wild, but for which that turned out not to be the case. Talwin, Stadol, and of course Oxycontin, come to mind in this respect, soma pill description. Iwould be very cautious about making any assumptions about the potential for diversion and abuse with tapentadol. In fact, the DEA has yet to assign the drug into one of its schedules.

As for what I think of tapentadol, I suspect that it will turn out to be useful, but not a blockbuster. If the safety profile is significantly better than that for tramadol, it may be possible to use it at higher doses, which might translate into greater clinical utility, soma pill description.

I do have two big questions, though, soma pill description. One: is this drug really any better than a combination of a medium-strength opioid, say hydrocodone, along with a norepinephrine reuptake inhibitor, say nortriptyline? Both are pretty inexpensive, the drug tramadol, so for the tapentadol to have a rational place in our pharmacopoeia, it would have to have some benefit that cannot be gotten for less money. (Not that markets are always rational, soma pill description, but still...)

Two: what it is potential for lowering the seizure threshold? Tramadol does this. It usually is not an issue unless a person takes a great deal more than what was prescribed, or it there is a drug interaction. The drug interaction should not be a problem with tapentadol, but we can assume that many persons will take doses that are larger than prescribed, soma pill description. Tapentadol presumably will come with a warning about that, but that won't stop many people. Note that I do not consider this a reason to keep the drug off the market, tramacet migraines side effects, but I do think that clinicians should keep the possibility in mind.
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Disclosure: I don't own any pharmaceutical stocks (not directly, anyway; I probably have some small bit in a mutual fund somewhere), nor do I work for any company that has anything to do with any of the products mentioned, soma pill description.






Synthetic marijuana consists of smokeable leaves of plants that have been covered in chemicals that mimic THC, the active ingredient in actual marijuana. Considered to be one of the newest designer drugs, fake pot makers market the substances as “herbal”. However, little credible evidence exists to back up the assertion. Popular among young people, patient education tramadol, fake pot is typically sold in drug paraphernalia shops and on the Internet, soma pill description. Fake pot is marketed under the brands Spice, K2, soma pill description, Blaze, Mr. Nice Guy and Red X Dawn and it typically referred to as “incense”. The products also claim to be undetectable during drug tests and retail for even more than real pot.

Law enforcement officials, hospitals and even poison control centers have documented many reports of adverse reactions to the synthetic marijuana, including seizures and hallucinations, soma pill description. Evidence also exists that synthetic marijuana may actually be addictive. The American Association of Poison Control Centers claims to have received over fifteen hundred calls nationwide concerning use of fake pot, soma pill description. A seventeen year old boy recently smoke synthetic marijuana and had to be rushed to the emergency room for muscle contractions, low blood pressure (BP) and a racing heart.

The US Drug Enforcement Agency (DEA) recently initiated an emergency lockdown on fake pot, soma pill description, focusing on five chemicals use to create the substances, karachi. Over the next thirty days, soma pill description, the DEA will try to have the chemicals classified in the same category as illicit drugs such as heroin and cocaine. The emergency action is quickest way the DEA can legally get the products off the shelves. The federal government first became aware of the drugs in the fall of ’08, tramacet migraines side effects, when a CBP (Customs & Border Protection) officer evaluated an incoming shipment of “Spice”, soma pill description. In early 2010, patient education tramadol, CBP took possession of over 100 pounds of two of the five target chemicals.

Although the DEA is just now taking action, over fifteen states have already taken steps to regulate the chemicals present in fake pot. In a perverse twist, it turns out that the man who invented three of the five chemicals did so as part of a government-sponsored research project two decades ago;

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Real marijuana typically results in sleepiness and, tramacet migraines side effects, occasionally, paranoia, patient education tramadol. Users of synthetic pot, soma pill description, however, report dizziness, nausea, karachi, agitation, fast heartbeat, the drug tramadol, and hallucinations. Other users have fallen into comas or have heart arrhythmias, tramacet migraines side effects. One team reported having hallucinated that he was standing at the edge of a cliff, getting ready to jump. It turns out that he was actually standing at the edge of a curb and dove off it, injuring his mouth and chin. In addition, he experienced shortness of breath and seizure-like symptoms for about 6 hours.

After the thirty days is up, karachi, the DEA will likely ban fake pot for one year, soma pill description. A ban on fake pot means that anyone found to possess or to have sold the products or chemicals within the product will be guilty of a crime.