Buprenorphine

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient buprenorphine is a highly effective pain reliever from the opioid group. It is used on the one hand for pain therapy, on the other hand for weaning in the treatment of opioid addiction. Here you can read everything you need to know about the effects and forms of use of buprenorphine (patches, tablets, etc.) as well as possible side effects.

This is how buprenorphine works

The active ingredient buprenorphine, as an opioid active ingredient, does not occur naturally in the poppy plant like opiates, but is chemically and pharmacologically modeled on them. Thanks to the targeted change in structure, opioids are more beneficial than opiates in terms of effects and side effects.

Like other opioids and opiates, buprenorphine works via opioid docking sites (receptors) in the central nervous system, i.e. the brain and spinal cord. They mainly have an analgesic effect and usually have a stronger effect on the receptors than the body's own endorphins, which also dock there.

The opiate morphine, which is also used in pain therapy, serves as the standard active ingredient with which all other opiates and opioids are compared with regard to their potency. Compared to this, the active ingredient buprenorphine is about 25 to 50 times more potent.

Buprenorphine shares some effects with other opioids and opiates, such as relieving pain and coughing, slowing breathing, causing nausea and constipation. Nevertheless, it has a very beneficial spectrum of side effects. In contrast to the other active ingredients, for example, it shows a so-called "ceiling effect" (saturation effect) for respiratory suppression: above a certain dosage, respiratory suppression does not become even stronger, as is the case with morphine, for example.

In addition, buprenorphine is not a so-called full agonist (in which the effect increases more and more with increasing dosage), but a partial agonist that has a certain percentage of effect, but not more - even in combination with other opioids. This effect is particularly important for weaning off addiction, since it can effectively alleviate the withdrawal symptoms, but does not lead to dose increases and overdoses.

Uptake, breakdown and excretion of buprenorphine

Depending on the dosage form, it is absorbed either through the skin (plaster) or the mucous membranes (sublingual tablets). Via the mucous membranes, the active ingredient reaches the highest blood values ​​after about one and a half hours. The active ingredient buprenorphine enters the body more slowly via the patch and reaches effective concentrations in the blood after four to twelve hours, but the maximum values ​​only after about one and a half days. About two thirds of the buprenorphine is excreted unchanged with the bile via the intestine, one third is broken down in the liver and excreted in the urine.

When is buprenorphine used?

The opioid buprenorphine is used to treat severe and very severe pain (such as pain after surgery, heart attack and tumor pain) and in combination with addiction therapy for substitution therapy in opioid addicts.

For the treatment of addicts who have consumed opioids intravenously, there are also combination preparations with the active ingredient naloxone, which are intended to prevent the buprenorphine sublingual tablets from being misused (by dissolving and injecting).

This is how buprenorphine is used

To treat pain, buprenorphine can be given by the doctor by injection, which leads to the fastest onset of action. Otherwise, sublingual tablets are used, which dissolve in the oral cavity after a short time. Their dosage depends on the severity of the pain and must be determined by the doctor; Dosages of 0.2 to 0.4 milligrams of buprenorphine every six to eight hours, i.e. three to four times a day, are common.

Buprenorphine patches (also called transdermal patches) are stuck on for several days (depending on the manufacturer, usually three to four days) and continuously release buprenorphine through the skin into the body. This dosage form is often chosen for long-term therapy. When changing the patch, care must be taken that no buprenorphine-containing residues of the patch stick to the skin. The new patch must be put on a new, suitable area of ​​skin.

To wean opioid addicts, the buprenorphine dose has to be set individually, but it is usually a lot higher than for pain therapy. The maximum daily dose is 24 milligrams of buprenorphine (equivalent to eight milligrams three times a day).

What are the side effects of buprenorphine?

The use of buprenorphine is associated with side effects similar to those of other opioids. More than ten percent of patients experience nausea, headaches, insomnia, increased sweating, weakness and withdrawal symptoms.

Furthermore, buprenorphine side effects such as inflammation of the respiratory tract, loss of appetite, restlessness, anxiety, depression, drowsiness, dizziness, tremors, changes in heart rhythm, drop in blood pressure, shortness of breath, indigestion, constipation, vomiting, rashes, , Bone and muscle pain.

The buprenorphine side effects mentioned occur more frequently at high doses, such as those used for addiction cessation therapy.

What should be considered when taking buprenorphine?

If buprenorphine is taken with other substances that depress the central nervous system, it can have excessively strong sedative, depressant, and soporific effects. Such substances include sedatives and sleeping pills from the benzodiazepine group (such as diazepam, lorazepam), other pain relievers, antiallergics (doxylamine, diphenhydramine), antipsychotics / neuroleptics (haloperidol, chlorpromazine, olanzapine) and alcohol.

Buprenorphine is broken down in the liver by a specific enzyme (cytochrome P450 3A4). If active substances that stimulate the activity of this enzyme (so-called enzyme inducers) are taken at the same time, buprenorphine can be broken down more quickly. As a result, it only has a weakened effect or no longer works at all. Examples of such enzyme inducers are agents against epilepsy and convulsions (carbamazepine, phenytoin, phenobarbital) and the antibiotic rifampicin.

Buprenorphine should not be taken during pregnancy and breastfeeding, as the active ingredient can increasingly enter the child's circulation, especially when taken shortly before birth and during breastfeeding. This can lead to the "floppy infant syndrome", whereby the newborn or the infant has hardly any body tension, reacts little to its environment and only breathes shallowly, which can be life-threatening.

How to get medication with buprenorphine

Preparations with the active ingredient buprenorphine are classified as narcotics and may only be prescribed by a specialist doctor using a special narcotic prescription. With this prescription you can get the appropriate medication in the pharmacy.

How long has buprenorphine been known?

Buprenorphine was discovered and patented by the pharmaceutical company Reckitt & Colman (now Reckitt Benckiser) in 1968. Since then, it has developed into a valuable active ingredient in pain therapy and has even been included in the list of essential medicines of the World Health Organization (WHO). Since the patent protection has now expired, there are now numerous generics with the active ingredient buprenorphine.

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