How tilidine works
Opioids such as tilidine achieve their pain-relieving (analgesic) effect by activating opioid receptors in the human body. The body’s own endorphins (endogenous painkillers), which are not structurally related, also bind to the same receptors. By activating the opioid receptors, tilidine indirectly inhibits the pain-mediating neuronal systems in the body.
The time to onset of action depends on the dosage form used (drops or tablets). In the body, tilidine is converted into the actual active substance nortilidine in the liver. The average duration of action is approximately three to five hours.
When is tilidine used?
The active ingredient tilidine is used to relieve moderate to severe pain. Doctors prescribe the drug primarily when non-opioid analgesics (e.g. ibuprofen, diclofenac, paracetamol, metamizole) are not sufficiently effective.
The active ingredient is available in drop or tablet form. To prevent misuse, tilidine is combined with naloxone in Germany. At very high doses or when the medication is injected, naloxone inhibits the effect of tilidine. Opiate or opioid addicts develop withdrawal symptoms.
How tilidine is used
In most cases, tilidine drops and prolonged-release tablets are used. Prolonged-release tablets release the active ingredient only slowly, which prolongs the duration of action. This has the advantage that the patient has to use the medication less often. Tilidine prolonged-release tablets are only taken once or twice a day, depending on the dosage, whereas tilidine drops are taken up to six times a day.
As the opioid can lead to habituation and withdrawal symptoms can occur if tilidine is discontinued abruptly, the painkiller should be discontinued gradually rather than suddenly if treatment is to be ended. Doctors call this “tapering off” the therapy.
The dosage is determined individually by the treating doctor and should be strictly adhered to.
What side effects does tilidine have?
The use of the painkiller can lead to side effects that affect the nervous system, among other things. Dizziness, drops in blood pressure, drowsiness, tiredness, headaches, nervousness and occasionally hallucinations and euphoric mood often occur. The last two side effects play a major role in the misuse of tilidine.
The body becomes accustomed to tilidine after prolonged use. Chronic use can be addictive. Abrupt discontinuation is very likely to cause withdrawal symptoms.
What should be considered when taking tilidine?
The effect of tilidine on the nervous system can cause dizziness and drowsiness, among other things, which may make it impossible to operate machinery and vehicles safely. Patients should be aware of this.
Tilidine is not suitable for people who are (or were) already dependent on opiates/opioids. The rare metabolic disorder porphyria is also a contraindication. In addition, children under two years of age must not take tilidine.
The effects and side effects can be increased by liver dysfunction and the simultaneous use of sedatives or sleeping pills. Tilidine can therefore not be used in cases of severe liver disease.
Side effects can also be considerably increased by taking tilidine and alcohol at the same time. For this reason, alcohol should be avoided during therapy with tilidine.
Pregnancy and breastfeeding
Due to limited experience, tilidine should only be used during pregnancy and breastfeeding if absolutely necessary. For pregnant women in particular, better-proven alternatives such as paracetamol or tramadol are available.
How to obtain medication with tilidine
Tilidine is a prescription-only medication in Germany and Switzerland. The active ingredient is not available in Austria.
In non-retarded dosage forms, tilidine is considered a narcotic (BTM) and as such requires a special prescription (BTM prescription). The reason for the BTM prescription requirement is that tilidine has a high potential for abuse and can lead to addiction if used unnecessarily frequently. Prolonged-release tablets are not subject to the Narcotics Act.
How long has tilidine been known?
Tilidine was developed as a synthetic active ingredient in the early 1970s. Initially, drops were marketed because the dosage of tilidine is easier to handle with drops.
Other interesting facts about tilidine
Tilidine is a weak opioid. Its potency is around a fifth of that of morphine. For this reason, tilidine was long regarded as a painkiller not subject to BTM. Due to increasing abuse and the resulting withdrawal symptoms, the desire for stricter handling was expressed and finally implemented in 2013 – at least for non-retarded tilidine/naloxone.