Buprenorphine: Pain therapy & substitution


Niklas Bergmann, M.A.
Biochemist, specialist author
Inhaltsverzeichnis: Buprenorphine: Pain therapy & substitution
Buprenorphine is a versatile medication that plays a central role in both pain therapy and substitution therapy for opioid addiction. As a partial opioid agonist, it offers an effective treatment option while at the same time harbouring a lower risk of abuse and overdose. However, in order to achieve the best possible effects, it is crucial to familiarise yourself with the correct dosage, directions for use and duration of action.
In this article, you will find out how buprenorphine works, what the dosage guidelines are and what you should look out for when taking it. We also look at the combination with naloxone and compare the use of buprenorphine with other substitution substances such as methadone.
If you are also interested in related topics, you can find useful information in our article on Tilidin .
What is buprenorphine?
Buprenorphine is a highly effective medication that is primarily used in two areas: pain therapy and the treatment of opioid addiction. It belongs to the opioid group, but acts as a partial agonist at the so-called µ-opioid receptors in the brain. This means that it has similar effects to other opioids, but less strong and with a lower risk of dependence or respiratory depression.
The special thing about buprenorphine is its long duration of action and the so-called ceiling-effects: after a certain dose, the effects no longer intensify, which reduces the risk of overdose. Thanks to these properties, buprenorphine has proven itself both in medicine and in substitution therapy.
Dosage of buprenorphine
The correct dosage of buprenorphine is crucial in order to achieve an optimal effects and avoid side effects. It depends on various factors, such as the area of application, the patient's state of health and previous drug tolerance.
Dosage recommendations:
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For pain therapy:
- Starting dose: 0.2 to 0.4 mg sublingually.
- Adjustment: The dose can be gradually increased depending on the intensity of the pain.
- Maximum daily dose: 2 mg (depending on individual requirements and medical assessment).
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In substitution therapy:
- Initial dose: 2 to 4 mg sublingually, usually on the first day.
- Top-up dosage: Up to 8 mg on the second day, depending on withdrawal symptoms.
- Maintenance dose: Usually between 8 and 16 mg daily, individually adjusted.
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Special features:
- The dosage must be adjusted for elderly patients or people with impaired liver function.
- Avoid overdosing: Buprenorphine shows no further increase in effect at higher doses (ceiling effect).
Close coordination with the attending physician is essential to ensure safe and effective treatment.
Taking buprenorphine: how to do it properly
Taking buprenorphine correctly is crucial to ensure its full effectiveness and avoid risks. Buprenorphine is administered in different dosage forms depending on the treatment goal, including sublingual tablets, transdermal patches or injections. Each form has specific requirements that must be observed.
Sublingual tablets must be dissolved under the tongue, as the active ingredients are absorbed through the mucous membranes. It is important not to chew or swallow the tablet, as this can significantly reduce the effects. You should not eat or drink while taking the tablet to ensure complete absorption.
For transdermal patches, correct placement on clean, dry skin is required. The skin site should be changed regularly to avoid irritation. Injections, on the other hand, are only administered by healthcare professionals to ensure precise dosing.
Regardless of the dosage form, buprenorphine should always be taken exactly as prescribed by a doctor, as incorrect use can not only impair its effectiveness but can also lead to dangerous side effects.
How long does buprenorphine last?
The duration of action of buprenorphine is one of the greatest advantages of this medication and makes it particularly suitable for long-term treatment. After ingestion, buprenorphine usually releases its effects within 30 minutes to an hour. However, the duration of effects can vary greatly depending on the dosage, dosage form and individual metabolism.
In pain therapy, the effects of sublingual tablets usually lasts 6 to 8 hours. With transdermal patches, on the other hand, the duration of action is several days, as the active ingredient is continuously released into the body via the skin. In substitution therapy, buprenorphine is often dosed so that a daily dose is sufficient, as its effects can last for more than 24 hours.
Another important factor is the ceiling effect of buprenorphine: from a certain dosage, the effects no longer increases, regardless of whether the dose is increased. This not only reduces the risk of overdosing, but also ensures consistent efficacy over longer periods of time.
Side effects and risks of buprenorphine
As with any medication, side effects can also occur with buprenorphine. These often depend on the dosage, the duration of use and individual factors such as age or state of health. It is important to be aware of possible risks so that action can be taken at an early stage if necessary.
Typical side effects:
- Nausea and vomiting: Especially common at the beginning of therapy.
- Schläfrigkeit: May impair concentration and reaction time.
- Kopfschmerzen: An occasionally reported side effect.
- Verstopfung: Typical for opioids and often in need of treatment.
- Schwindel: Especially possible when standing up suddenly.
Rare but serious side effects:
- Atemdepression: Especially at high doses or in combination with other sedative substances.
- Liver dysfunction: Should be checked regularly during prolonged use.
- Allergic reactions: Skin rashes or itching are rare, but possible.
Risikofaktoren:
- Combination with alcohol or tranquillisers can increase the sedative effects.
- People with impaired liver function should be dosed with particular care.
- Withdrawal symptoms may occur if the drug is stopped abruptly, which is why it must be gradually phased out.
Serious risks:
In combination with alcohol or tranquillisers, serious side effects such as respiratory depression can occur.
Buprenorphine in substitution therapy
Buprenorphine plays a central role in substitution therapy for opioid addiction, as it enables an effective reduction in withdrawal symptoms and at the same time reduces the craving for other opioids. It binds to the µ-opioid receptors as a partial agonist, thereby blocking the effects of stronger opioids and preventing relapses. Through this mechanism, it not only alleviates the physical symptoms of withdrawal, but also helps to stabilise the mental state. Especially in combination with naloxone, buprenorphine offers additional safety, as the risk of abuse is reduced. In addition, the long duration of action means that it can be taken once a day, which gives patients more flexibility in everyday life and increases adherence to treatment. Buprenorphine is therefore considered a reliable and effective option for the long-term treatment of addiction disorders.
Conclusion: The correct handling of buprenorphine
Buprenorphine is an effective and versatile medication that is convincing both in pain therapy and in substitution therapy. It offers a safe treatment option thanks to its long duration of action, ceiling effect and low dependency potential.
Correct use and medical supervision are essential to achieve the best results.