Tilidin (Ethyl-trans-2-dimethylamino-1-phenyl-cyclohex-3-en-1-carboxylat) belonged to the group of the Opioide and is the active substance of the pain means Valoron N (among other things). N stands for the admixture of Naloxon. This combination is to dam the abuse of Tilidin in the drug scene. Success is however moderately, only the injection and high doses with oral application is to a large extent prevented.
Tilidin is assigned to the stage 3 according to WHO as pain means, which means that this medicine is subject to the
Tilidin is a Opioid with Phenylaminocyclohexenyl structure. Tilidin is only relatively weakly effective as so-called Prodrug (a material that is thus obtained no or only small effect, but transferred in the body into a more strongly effective substance). The actual active substance, the Nortilidin, results from the amplifier off changing from Tilidin in the liver, particularly with the first passage of the material. One speaks here frequently also of roofridge passport. In the today usual trade preparations such as Tilidalor", Tilidin FindolN", Andolor etc.) is fixed combined Tilidin with the Opioid antagonist Naloxon.
Tilidin can be ordered according to the red list for strong to very strong pain. with very strong pain Tilidin is not sufficient however mostly. The next step are mostly morphines or morphine similar materials.
Naloxon is used e.g. for the treatment of acute Opioid poisonings. It is to be noted that with a dangerous withdrawal syndrome can be released. In the combination with Naloxon Tilidin is not subject to the Tilidin preparations without Naloxon are no longer available on the German market, until approximately 2002 gave it still the Valoron without Naloxon.
Only by the admixture of Naloxon (a Opiatantagonist) tilidinhaltige preparations are assigned to the stage 2 after WHO. One tried by this admixture to limit the abuse of Tilidin by drug-dependent. It came and comes nevertheless frequently to prescription falsifications and abuse into connection with Tilidin. Tilidin actually has hardly opioidtypische effect and becomes only with its first passage by the liver to Nortilidin - which actual opioiden active substance - amplifier-off-changes. Nortilidin is on the one hand a on the other hand one it is transferred in the further process into the again active until Nortilidin, which likewise opioide effects obtain. After the income of Tilidin the Opioidwirkung builds itself comparatively fast on (about 10-20 minutes).
That the Tilidin mixed Naloxon is nearly completely diminished and inactivated generally with its first passage by the liver. Since however a relatively large quantity of Naloxon is mixed to the Tilidin, of it only one part in the liver is deactivated and it remains - with the income of a larger quantity of Tilidin - still always enough in order to unfold its antagonistic effect and to restrain or destroyed make the effect of the taken Tilidin and/or further Opioide. A privileged position does not have the Opioid Buprenorphin, this normally by Naloxon antagonisiert, there the receptor affinity ("attraction" simplifies to the receptor) of the Buprenorphins is higher, than those of the Naloxon. With intravenous gift large parts of the Naloxons become immediately effective, which can be attributed quite simply to the fact that most Naloxon reaches the crucial receptor populations, before it can be inactivated, whereby also only one part could be inactivated at all. The liver passage is ignored by the direct intravenous gift to a large extent at the appropriate time.
Of an abuse of Tilidin urgently one warns, since this means can lead a strong dependence potential combined with Naloxon still to substantial euphoric conditions and thus offers.
The combination is not protection from dependence, because a Durschschnittserwachsener could take for instance 300-400mg Tilidin (and thus 24-32mg Naloxon, more Naloxon can be not sufficiently inactivated and becomes more strongly effective therefore). First euphorisierenden effects however already arise with 25-50mg Tilidin.
Tilidin is available as solution in the form of drop, caps as well as retardierte tablet form on prescription.
In principle all of the opioidtypischen side effects (see opioid, section side effects). The rapid effect entrance favours nausea and a vomiting contrary to sedating Opioiden such as morphine frequently a drive increase is observed.
To the liver and kidney damage criticized by various media: With humans with existing of the liver the fixed combination Tilidin/Naloxon is not the first choice, with kidney insufficiencies can it however be used. Opioide are besides generally quite compatible and load the organs compared with other pain means few.
Explicit Tilidin deaths are unknown, but each medicament income saves risks (15.000-20.000 deaths per year in Germany, dark number probably very highly).
In the past in different media was maintained, Tilidin makes aggressive. It is however like that that the consumption of Tilidin makes very extroverted and one shows feelings openly. The aggression must be already present thus and it develops not by the consumption of Tilidin.
Due to the fact that Tilidin has nearly no opioidtypische effect, it prevails under expert disagreement over it whether Tilidin is to be called Opioid or only as preliminary stage (Prodrug) to a work-strong Opioid (Nortilidin). The whole is not actually a faith question, a clear "correctly" or "wrongly" gives it here.