Tilidine is an inactive precursor of the drug nortilidine. The conversion takes place in the liver. Therefore, how long it takes for the effect to take effect depends on the dosage form. For drops it took 5-10 minutes, for tablets 15-20 minutes. The average duration of the effect is three to five hours in both cases. The analgesic effect is based on the activation of the body’s own opioid receptors. The endorphins in the body also bind to these receptors. These act as the body’s own painkillers, so to speak. By activating the opioid receptors, tilidine indirectly inhibits the neuronal pain-transmission systems in the body.
Tilidin is used to relieve moderate to severe pain. Doctors mainly prescribe it when lighter painkillers are no longer of sufficient help. These include, for example, various non-opioid painkillers such as ibuprofen, diclofenac or paracetamol. The active substance is administered in the form of drops or tablets. To prevent illegal use as a drug, naloxone is added to products in Germany. If the dosage is greatly inflated or if the drug is injected, naloxone inhibits the effect. Withdrawal symptoms then appear immediately in opiate addicts. However, a certain potential for dependency remains. Tilidine preparations with rapid release of the active ingredient are therefore subject to the Narcotics Act.
The main dosage forms of this active substance are tablets with a delayed release of the active substance and drops. Retard tablets release the active substance only slowly and thus prolong the duration of the effect. This has the advantage that the patient has to take the medication less often. While the tablets only have to be taken once or twice a day, the drops require up to six individual doses. Because the body gets used to Tilidin over time, withdrawal symptoms may occur if you stop taking it abruptly. Therefore, weaning should not be sudden, but rather slow. Doctors call this tapering off. The dosage is determined by the attending physician both during treatment and during weaning and must be strictly adhered to.
Side effects may occur when using Tilidin. Dizziness, a drop in blood pressure, drowsiness, fatigue, headaches and restlessness are often described. Some patients experience hallucinations and euphoria, which plays a large role in drug abuse. Constipation, nausea and a respiratory depressive effect are rarely observed when the analgesic is administered in the usual combination with naloxone. Another undesirable effect mentioned is increased sweating.
Children under the age of two should not take Tilidin. Alcohol should be avoided while using Tilidin. Side effects of Tilidin can include dizziness and lightheadedness. This can limit the safe handling of machines and vehicles. Tilidin should not be used by people dependent on opiates or opioids or who have a history of dependence. The rare metabolic disease porphyria is also one of the contraindications.
The effect and side effects can be increased in the case of liver dysfunction and the simultaneous use of sedatives or sleeping pills (e.g. benzodiazepines). In the case of severe liver diseases, another painkiller should therefore be selected. Caution is also required in the case of limitations in respiratory functions and gastrointestinal disorders. In addition to alcohol, the combination with certain other medications can also dangerously slow down breathing and gastrointestinal activity. Due to a lack of experience, tilidin should only be used during pregnancy and breastfeeding if necessary. Better tested alternatives such as paracetamol or tramadol are available, especially for pregnant women.
In Germany and Switzerland, the active ingredient is a prescription drug in a fixed combination with naloxone. Without naloxone, it is a narcotic in both countries, with correspondingly stricter prescription requirements. None of these forms are available in Austria. Some foreign Internet pharmacies offer Tilidin without a prescription. However, experts advise against taking advantage of such offers.