Tilidine - medicine - 2022 (2022)



Tilidine - medicine - 2022 (1)


  • What is tilidine?
  • General
  • Mode of action
  • application areas
  • Correct application
  • Medication
  • Trade names
  • Indications
  • Contraindications
  • Risks and Side Effects
  • Interactions
  • Important instructions
  • Dispensing regulations
  • history
  • Warning notices
  • swell
  • swell

The substance tilidine belongs to the group of opioids and is best known for its analgesic effect. The substance is produced synthetically and is used when there is severe or even very severe pain.

To avoid misuse of the substance, tilidine is combined with the substance naloxone in Germany.

Tilidine - medicine - 2022 (3)What is tilidine?

The active ingredient tilidine is used when patients suffer from severe or very severe pain and this needs to be treated.

For example, after an operation or in the case of very serious illnesses such as cancer, such treatment with tilidine is necessary.

The active ingredient is able to inhibit the perception of pain in the brain so that the pain no longer feels as severe to the patient as it would without the treatment.

Tilidine belongs to the so-called opiates, i.e. to the group of agents that have a similar effect to morphine. Although these remedies are very effective in combating pain, since they have a large number of points of attack they also have a few other effects on the human body.

For example, the psyche or mood can be influenced by the material. This effect is one reason that the active ingredient is misused by some people.

To prevent this abuse of tilidine, the substance is often combined directly with the active ingredient naloxone.

What is the purpose of this drug?

The active ingredient is used for treatment in the following cases:

  • Pain after surgery
  • Pain in a serious illness, such as cancer
  • impaired function of the kidneys or liver


other names
  • (1RS,2SR) -2- (Dimethylamino) -1-phenylcyclo-hex-3-ene-carboxylic acid ethyl ester
  • (±)-(E.) -2- (Dimethylamino) -1-phenyl-cyclohex-3-en-1-carboxylic acid ethyl ester
  • rac-(E.) -2- (Dimethylamino) -1-phenyl-cyclohex-3-en-1-carboxylic acid ethyl ester
Molecular formulaC.17H23NO2
Drug classOpioid analgesic

Mode of action

This is how Tilidin works

Tilidine achieves its analgesic, i.e. its analgesic effect, just like other substances from the group of opioids, by activating the specific opioid receptors in the human body.

Among other things, the endorphins, which are produced by the body itself, but are not related to the opiods in their structure, also bind to these receptors.

Because the receptors are activated by the ingested tilidine, the neuronal systems in our body are also indirectly inhibited. These neural systems are responsible for ensuring that the pain is passed on in the organism.

After the active ingredient has been ingested, it takes about ten to 15 minutes for this effect to occur. During this time, the active ingredient is converted into the actual active ingredient, the tilidine becomes the so-called nortilidine.

This conversion to the active substance takes place in the liver. After the effects of tilidine have set in, they last for about three to five hours.

Uptake, breakdown and excretion of tilidine

When tilidine is ingested, the first thing in our body is the liver. There, the active ingredient is metabolized to nortilidine through the process of demethylation.

This nortilidine is the actual active ingredient. After this process, the effect sets in, that means after about ten to 15 minutes. Compared to other options, the onset of action for the drug is relatively early.

In Germany, as mentioned, naloxone is added to tilidine to prevent the active ingredient from being misused. This naloxone is broken down directly in the liver.

The drug then works for about three to five hours in our body, after which it is also broken down by the liver and excreted from the body.

application areas

When is Tilidine used?

The tilidine is prescribed as a pain reliever when there is moderate or even severe pain.

Treatment with the active ingredient is used, among other things, if a patient experiences pain after an operation or if the pain occurs due to a serious illness such as cancer.

Attempts are always made to only use tilidine for the treatment of this pain for a very short time in order to avoid that the patients get used to the active ingredient or even become dependent on it.

However, it is not always possible to use the substance only for a short time. Especially in patients who suffer from severe chronic pain, the agent must be used long-term in order to suppress the pain.

In some cases it is even necessary to use other pain relievers in addition to the tilidine in order to combat the pain that occurs.

If the active ingredient is misused, i.e. taken or injected in a very high dose for a long time, this can have very serious effects on the human body.

To prevent this abuse, tilidine is very often combined with naloxone. Naloxone is a kind of antagonist of tilidine and, if the dose is too high, the effect of the substance is inhibited. In addition, withdrawal symptoms are triggered in this case.

Correct application

This is how tilidine is used

There are three different forms in which Tilidine can be used. The active ingredient is available as an injection, i.e. as a syringe, as a tablet, optionally also as an extended-release tablet, and also in the form of drops.

Your doctor will tell you the dose to take in each case. In order to avoid serious side effects or possible addiction, you should absolutely keep this dose.


Which drugs contain the active ingredient tilidine?

In some countries, products containing only tilidine are allowed to be sold. This is not allowed in Germany, here the active ingredient must always be combined with naloxone.

The following drugs contain a combination of these two active ingredients:

  • TILICOMP beta 100/8 mg prolonged-release tablets
  • TILICOMP-beta 150/12 mg prolonged-release tablets
  • TILICOMP beta 50/4 mg prolonged-release tablets
  • TILIDIN-100/8 mg retard-1A Pharma Tabl.
  • TILIDIN-150/12 mg retard-1A Pharma Tabl.
  • TILIDIN-200/16 mg retard-1A Pharma Tabl.
  • TILIDIN-50/4 retard-1A Pharma Tabl.
  • TILIDIN-AbZ drops 50 mg / 4 mg per 0.72 ml
  • TILIDIN-AL comp. 100 mg / 8 mg prolonged-release tablets
  • TILIDIN-AL-comp. 150 mg / 12 mg prolonged-release tablets

Trade names


There is a risk of tilidin becoming addictive if misused. For this reason, Tilidine is subject to the provisions of the Narcotics Act as a monopreparation and may therefore not be sold and used as such in Germany.

Combination preparations

Tilidine is only available in Germany as a combination preparation, which means that it is combined with naloxone. The proportion of naloxone in such preparations is 8%.


Tilidine is indicated when the effect of non-opiods is insufficient in an acceptable dosage. The indication takes place in the case of moderate, severe or very severe pain.


When should Tilidin not be used?

Under certain circumstances Tilidin should not be used. This applies, for example, if the patient has an allergic reaction to the active ingredient.

Even patients who have already suffered from an addiction disorder should not take the active ingredient.

In addition, in patients with impaired liver function, the pain reliever may not work for you.

What should I watch for pregnancy and breastfeeding?

Although there are no exact results from systematic studies in this area, there is so far no evidence that taking tilidine during pregnancy poses a risk of harm to the embryo. This generally applies to the group of opioids.

When it comes to breastfeeding, there are still no precise studies as to whether tilidine can be harmful. However, if possible, the active ingredient should only be used for a short time during breastfeeding. No restriction is required for single doses.

What to consider with children

There are also some remedies for children that can combat pain.

However, not all products containing tilidine are approved for use in children. Therefore, you should check the package insert for each drug to see whether the drug can also be taken by children without risk.

Children under two years of age should not be treated with tilidine, as tests with tilidine have not yet been carried out in children of this age and therefore under certain circumstances undetected and possibly very dangerous side effects can occur.

Risks and Side Effects

What are the side effects of tilidine?

When using tilidine, side effects that affect the nervous system are common.

After taking the pain reliever, people often feel dizzy, blood pressure drops, feel drowsy and tired, have headaches, become nervous, notice hallucinations or fall into a euphoric mood for no reason.

Hallucinations or an inexplicable change of mood play a major role, especially if the Tilidine is misused and taken even when there is no need for such ingestion.

Side effects that are rarely observed are problems in the gastrointestinal tract, for example nausea or constipation and impaired breathing, i.e. a respiratory depressive effect. Increased sweating is also often observed as a side effect.


What interactions does tilidine show?

When taking tilidine, you should be particularly careful if you are taking other medications at the same time, which cause you to become tired.

Because of these drugs it can happen that the side effects of tilidine occur much more frequently and also more strongly.

It does not matter whether the cause of fatigue is a main or a side effect of the medication. Drugs that make you tired include various antidepressants and sleeping pills.

If you take anticoagulants such as phenprocoumon in addition to tilidine, your coagulation should be checked closely by a doctor and the dose of the anticoagulant may be adjusted on the advice of a doctor.

In addition, patients taking Tilidine should avoid alcohol.

Important instructions

What should be considered when taking Tilidine?

As Tilidine may make you feel drowsy or tired, or you may experience severe dizziness when using it, you should be very careful if you:

  • have to control a vehicle in traffic
  • Need to operate machines
  • Have to do work for which you do not have a secure hold

Especially if you are just starting to use tilidine, or even if your dose of pain reliever is increased, you may no longer be able to do all of these things.

However, these effects are different for each person, so we recommend that you have a doctor assess your ability to drive after taking tilidine.

Dispensing regulations

How to get medicines with tilidine

Since Tilidine can be highly addictive, attempts are often made to combat severe pain with other means.Only when a doctor sees no other way to control the pain will you be prescribed tilidine to relieve your severe pain.


Since when is Tilidin known?

Tilidine was developed as a synthetic active ingredient in the early 1970s. Since the dosage of the active ingredient in the form of drops is easier, the active ingredient was initially only sold in drops.

Since tilidine, like all other opiods, can also be addictive, various preparations were made in the following period, for example the combination with naloxone or the requirement that tilidine should no longer be given to drug addicts in order to prevent misuse of the agent.

Warning notices

Warnings and Precautions

Tilidine can be highly addictive and cause serious side effects that may greatly affect your perception.

For this reason, it is important to adhere to the prescribed dose and also the prescribed duration of intake that your doctor will give you at the beginning of use, in order not to run the risk of becoming dependent on the active ingredient.



  • Aktories, K. et al .: General and special pharmacology and toxicology, 11th edition, Urban & Fischer Verlag / Elsevier GmbH, 2013.
  • Waldvogel, H. H .: Analgesics, Antinociceptives, Adjuvants: Manual for pain practice, Springer-Verlag Berlin Heidelberg GmbH, 2nd edition, 2001.
  • Pharmacovigilance and advice center for embryonic toxicology at the Charité - Universitätsmedizin Berlin: www.embryotox.de (accessed: December 30, 2013)
  • Thomm, M .: Pain Management in Nursing, Springer Verlag, 2012.

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