The whole truth about tramadol

Tramadol Abuser.png File Photo

Fri, 23 Nov 2018 Source: Joel Savage

Tramadol is an old anesthetic the German pharmaceutical company Gr ?nenthal GmbH, developed in 1962. In therapeutic doses, tramadol is practically safe. At the same time, tramadol abuse is on the rise, taking its toll on those addicted.

In order to prevent the uncontrolled use of tramadol, it is widely ranked as prescription drugs. Ukraine is the first country to include tramadol in the list of narcotic drugs, psychotropic substances, and precursors

Tramadol - one of the four most commonly prescribed analgesics - is used in 70 countries around the world for cancer pain and non-cancer genesis, which is generally not surprising, since the drug has proven itself in postoperative anesthesia.

It is quite effective in fibromyalgia syndrome (a rheumatological disease characterized by diffuse musculoskeletal pain, fatigue and a decrease in the pain threshold during palpation in the so-called pain points).

Three to five days after the start of tramadol in a daily dose of 100 mg decreases pain in most patients, while long-term therapy with tramadol (for 4-6 months) reduces the severity of autonomic and functional disorders, as well as normalizes the level of pain threshold in painful points.

In addition, daily doses of 50 to 200 mg of tramadol can relieve severe and moderate pain in osteoarthritis of large joints as effectively as diclofenac or meloxicam, without causing the side effects of NSAIDs. And in higher doses (up to 400 mg per day), it eliminates chronic pain in cancer patients.

Since 1989, tramadol has been used with a slightly different purpose to relieve muscle tremor in the post-anesthesia period. What is the reason for the "unconventional" effect is difficult to say? But it is authentically known that the analgesic effect of the drug is realized through the effect on mu-opiate receptors and monoaminergic mechanisms.

In other words, like narcotic analgesics, the same morphine, for example, tramadol selectively binds to opiate mu-receptors, but unlike narcotic analgesics, it simultaneously suppresses the reverse neuronal seizure of serotonin and noradrenaline, thereby disrupting the transmission of pain impulses to the gelatin substance of the spinal cord.

The effect of each mechanism is rather weak. In particular, tramadol is 6000 times less than morphine in binding to mu-opioid receptors and codeine 10 times less; nevertheless, its analgesic activity is twice as high as that of codeine and only five times lower than that of morphine.

As it turned out, the reason for the relatively high efficiency of tramadol lies in the synergistic, complementary action of the mu-opioid and monoaminergic mechanisms. But the most curious thing is that in the early stages of the study when the ability of tramadol to selectively bind to mu-opioid receptors was discovered, it was ranked as a narcotic analgesic.

It fell into the category of potent non-narcotic drugs later, after it was possible to prove that:

- Therapeutic (100 mg) and even three times therapeutic doses (300 mg) of tramadol cause depression of breath, euphoria, development of drug dependence and tolerance incomparably less often than doses of morphine equivalent to the analgesic effect.

- With long-term use of tramadol (again in therapeutic doses) nausea, dizziness, vomiting, and dry mouth are observed in about 5% of cases, and the likelihood of tolerance to the drug and dependence on it actually reduces to zero.

- In former drug addicts and people with opiate addiction, long-term use of therapeutic doses of tramadol rarely leads to the development of tolerance and drug dependence.

- Tramadol cannot be used with a substitutionary purpose with dependence on heroin and morphine.

At the same time, the FDA received 83 reports of epileptic morphic seizures and convulsions in patients taking tramadol in the first year of the sale of the drug in the United States. The following year, the number of such messages increased almost two and a half times.

Many reports noted that convulsions occurred on the day of admission, mainly in healthy young people between the ages of 20 and 39; that therapeutic side effects of tramadol caused this adverse reaction, but overdose increased the risk of its development, as did the simultaneous use of antidepressants, including new selective inhibitors of reverse neuronal uptake and old tricyclic antidepressants.

After the launch of tramadol on the market in the first one and a half years, the frequency of development of dependence reached a peak - approximately two cases per 100,000 patients, in the next year and a half, this figure dropped by about half.

It is characteristic that in 97% of cases, dependence developed in patients with a history of drug dependence on other drugs. Moreover, for some addicts, only one dose of tramadol was enough for some patients.

It is worth noting that, according to a careful assessment by the FDA, there are a dozen unrecorded cases per one reported adverse drug reaction.

Many of the introduction to tramadol accounted for adolescence. Someone first took a few capsules of the drug out of curiosity, someone from the desire to feel free, relax, and someone - under the influence of friends.

For the sake of completeness, it should be noted that patients who abused tramadol for several years usually looked 15–20 years older than their peers and were inferior to them in the growth and volume of the chest.

They had no motivation to get rid of dependence; they succumbed to treatment worse than opium addicts. Quite a few adolescents, starting with regular intake of tramadol, gradually switched to injecting the consumption of artisan-made opiates or heroin.

On top of that, the long-term tramadol dependence, which proceeds without remission, inevitably leads to a general depletion with systemic inhibition of the functions of vital organs.

Columnist: Joel Savage