Tilidine is a pain reliever. It is one of the opioids.
What is Tilidine.
Tilidine is a pain reliever. It is one of the opioids. Tilidine belongs to the group of opioid analgesics. Opioids have analgesic properties. However, they have the disadvantage of posing a potential risk of dependence. To counteract such dependence and undesirable side effects, a combination of tilidine and its antagonist naloxone is usually used. The synthetic drug tilidine was developed in the late 1960s by the German pharmaceutical company Gödecke, which today belongs to the Pfizer Group. Initially, the active ingredient was marketed in the form of drops. In this way, the drops made it easier to dose the painkiller. Over time, however, it became apparent that tilidine could cause dependence in patients. For this reason, the drug was no longer used in people who had a drug addiction. Finally, to prevent the risk of addiction, naloxone was added. Thus, naloxone represents an opioid antagonist that cancels the effect of opioids. It has the ability to bind to the same receptors as tilidine, but without triggering a corresponding effect. In this way, naloxone is also suitable for treating opioid intoxication.
Pharmacologic action
Tilidine’s mode of action is based on the fact that it activates opioid receptors within the body. The body’s endorphins, which also act as analgesics, also bind to these receptors. Because of tilidine’s activation of the receptors, there is an indirect inhibition of the neural systems from which pain is transmitted in the body. It takes approximately 15 minutes for the analgesic effect of tilidine to take hold. During this period, the conversion of the active ingredient into nortilidine, which is actually responsible for the analgesic effect of the drug, takes place within the liver. Overall, tilidine works for about 3 to 5 hours. Tilidine not only has the effect of relieving pain, but also affects its perception. For this reason, the patient feels pain less intensely and is put in a more positive mood. Thus, the mode of action of tilidine is similar to morphine, which is considered the most important representative of opioids. The combination of tilidine and naloxone is intended to prevent misuse of the painkiller by overdosing or injecting it into the arm. The active ingredient combination can only develop its positive properties if it enters the gastrointestinal tract via drops, capsules or tablets. In this way, naloxone is largely inactivated in the stomach, leaving only the effect of tilidine. When injected into the arm, as is often the case with drug addicts, the euphoric effect of tilidine is omitted because this property is suppressed by naloxone.
Medical application and use
For use, tilidine is used for the treatment of moderate to severe pain. Here, the period of use is limited to prevent habituation to the opioid, but this is not always possible. Thus, especially people suffering from chronic pain are often dependent on tilidine for a longer period of time. The most common indications for tilidine include pain from cancer, pain after surgery, pain from accidents, and pain after a heart attack. The active ingredient is also suitable for the treatment of inflammatory rheumatic diseases. It can also be useful to take tilidine as a preventive measure if severe pain is already to be expected. In Germany, tilidine is taken in the form of sustained-release tablets and drops and in combination with naloxone. In this combination, the analgesic does not fall under the Narcotic Prescription Regulation (BtMVV) in this country, as the potential for dependence and abuse can be prevented in this way. However, the BtMVV has applied to tilidine preparations in which the active ingredient is released immediately since 2013. The combination of tilidine + naloxone is also available as a generic. Since tilidine is subject to prescription, it can only be obtained through a specific doctor’s BTM prescription.
Risks and side effects
Taking tilidine can have several side effects. For example, nausea and vomiting often occur when using sustained-release tablets.In some cases, drowsiness, fatigue, dizziness, headache, increased sweating, abdominal pain and diarrhea are also possible. Nausea, vomiting, drowsiness and dizziness may also occur when taking drops. The undesirable side effects are especially apparent at the beginning of the therapy. However, the longer the treatment lasts, the more the side effects decrease. To prevent side effects, patients are advised to avoid physical exertion. Tilidine should not be taken at all in the event of hypersensitivity to the active substance. People who are dependent on opiates must also avoid tilidine + naloxone, as the naloxone can cause severe withdrawal symptoms. Other contraindications to tilidine include liver dysfunction and cirrhosis. Tilidine should be taken during pregnancy and lactation only after a thorough weighing of risks and benefits by the physician. For children, tilidine is suitable from the age of two years. Taking Tilidine at the same time as sedatives or alcohol may increase the effect of the painkiller. There is even a risk of respiratory arrest. Because of interactions that are difficult to assess, concomitant administration of tilidine and other opioids should be avoided.
