Pregabalin

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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 pregabalin is used to treat generalized anxiety disorder, neuropathic pain and as an add-on therapy for focal epileptic seizures. Read more about the effects and use of pregabalin, side effects and other interesting information here!

This is how pregabalin works

Pregabalin belongs to the group of active substances called anti-epileptic drugs and blocks voltage-dependent calcium channels in the central and peripheral nervous system. It specifically binds to certain subunits of these calcium channels and in this way inhibits the calcium-mediated release of nerve messenger substances (neurotransmitters).

These subunits occur mainly in the cerebellum (cerebellum), the cerebral cortex, the hippocampus and the back horn of the spinal cord. Pregabalin ensures that less calcium gets into cells, which reduces their activity. As a result, they release fewer messenger substances such as glutamate (a messenger substance that stimulates nerve cells), norepinephrine (a stress messenger substance) and substance P (a messenger substance that transmits pain).

In the case of epileptic seizures and anxiety disorders, it can often be achieved that fewer or no more seizures occur or fears decrease. Nerve pain during and after shingles (herpes zoster infection), fibromyalgia (fiber muscle pain), diabetes (diabetic polyneuropathy) or after spinal cord injuries can often be positively influenced by pregabalin.

Pregabalin uptake, breakdown and excretion

The highest blood levels are reached within an hour of taking pregabalin. The active ingredient is able to cross the blood-brain barrier. Pregabalin is then excreted unchanged via the kidneys with the urine. After about six hours, half of the active ingredient is removed from the blood.

When is pregabalin used?

The active ingredient pregabalin is approved:

• for the treatment of central and peripheral neuropathic pain
• for the treatment of generalized anxiety disorder (persistent anxiety that is not related to a specific situation or object)
• as additional therapy for focal epileptic seizures with / without secondary generalization

In some countries, pregabalin is approved for the treatment of fibromyalgia. Outside of the approved areas of application, pregabalin is also sometimes used to relieve withdrawal symptoms in opiate addicts and to relieve symptoms of restless legs syndrome.

The application is usually long-term, but should be checked regularly to determine whether it is necessary.

This is how pregabalin is used

Pregabalin is usually taken in the form of capsules. An oral solution is also available for patients who cannot swallow capsules or who are fed through a tube. Depending on the type and severity of the disease, between 150 and 600 milligrams of pregabalin are taken daily, divided into two to three individual doses.

If the low dosage used at the beginning turns out to be too weak, the dosage can be increased in stages on a weekly basis, depending on the doctor's judgment. Even when discontinuing treatment after consultation with a doctor, the dose should be reduced gradually (so-called “gradual dosage”) in order to keep side effects to a minimum.

Do not just stop taking pregabalin. This can cause severe withdrawal symptoms.

What are the side effects of pregabalin?

The most common side effects during treatment with pregabalin are drowsiness, sleepiness, and headache in more than ten percent of patients.

Other pregabalin side effects in one in ten to a hundred people treated are, for example, inflammation of the nasopharynx, increased appetite, weight gain, increased mood, confusion, dizziness, irritability, insomnia, decreased libido, erectile dysfunction, coordination and movement disorders, memory disorders, Parasitic sensations, blurred vision, vomiting, nausea, indigestion, cramps, muscle and joint pain.

Pregabalin can affect your ability to drive and react.

What should be considered when taking pregabalin?

Since most of the pregabalin is not metabolized in the body, there are few interactions with additional medication.

Pregabalin can increase the effect of central depressant substances and stimulants. This applies, for example, to sedatives and sleeping pills (benzodiazepines such as lorazepam and diazepam), strong pain relievers (opiates and opioids such as morphine, fentanyl and oxycodone) and alcohol. Caution is therefore required, particularly when handling heavy machinery and when actively participating in road traffic.

The dose may need to be reduced in elderly patients and patients with impaired renal function. Pregabalin also increases the risk of falls in the elderly. Weight gain due to pregabalin may make it necessary for people with diabetes to adjust the dosage of blood sugar lowering medication.

pregnancy and breast feeding period

Pregabalin should not be taken by pregnant or breastfeeding women, as animal experiments have shown teratogenic effects and the active ingredient has been found in breast milk. If possible, more suitable alternatives such as amitriptyline (neuropathic pain) or lamotrigine and levetiracetam (focal seizures) should be used.

The safety of use in children and adolescents has also not been proven, which is why the active ingredient should only be taken by adults.

How to get pregabalin medication

In Germany, Austria and Switzerland, the active ingredient pregabalin requires a prescription in every dosage and form of administration and is only available in pharmacies after a doctor's prescription.

Since when is pregabalin known?

The active ingredient is the direct further development of the active ingredient gabapentin, which was patented in 1976. After the manufacturing company was taken over by a large pharmaceutical company, the researchers there finally developed the successor pregabalin, which was approved in the EU and the USA in 2004. The patent protection expired in 2014, and generics with the active ingredient have been available since then.

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