Pregabalin: Effect, administration, side effects

How pregabalin works

Pregabalin belongs to the group of antiepileptic drugs and blocks voltage-dependent calcium channels in the central and peripheral nervous system. It binds specifically to certain subunits of these calcium channels and in this way inhibits the calcium-mediated release of neurotransmitters.

These subunits are mainly found in the cerebellum, the cortex, the hippocampus and the posterior horn of the spinal cord. Pregabalin ensures that less calcium enters the cells, thereby reducing their activity. As a result, they release fewer messenger substances such as glutamate (a messenger substance that excites nerve cells), noradrenaline (a stress messenger substance) and substance P (a messenger substance for pain transmission).

In the case of epileptic seizures and anxiety disorders, this can often result in fewer or no more seizures or a reduction in anxiety. Pregabalin can also often have a positive effect on nerve pain during and after shingles (herpes zoster infection), fibromyalgia (fiber-muscle pain), diabetes (diabetic polyneuropathy) or after spinal cord injuries.

Absorption, breakdown and excretion of pregabalin

When is pregabalin used?

The active substance 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 adjunctive therapy for focal epileptic seizures with/without secondary generalization

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

It is usually used on a long-term basis, but its necessity should be reviewed regularly.

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 tube-fed. Depending on the type and severity of the illness, between 150 and 600 milligrams of pregabalin are taken daily, divided into two to three single doses.

Do not simply 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, dizziness and headaches in more than ten percent of patients.

Other pregabalin side effects in one in ten to one hundred people treated include inflammation of the nasopharynx, increased appetite, weight gain, increased mood, confusion, dizziness, irritability, insomnia, decreased libido, impotence, coordination and movement disorders, memory disorders, sensory disturbances, blurred vision, vomiting, nausea, digestive disorders, cramps, muscle and joint pain.

Pregabalin can impair the ability to drive and react.

What should I bear in mind when taking pregabalin?

As pregabalin is largely not metabolized in the body, there are only a few interactions with additional medications taken.

The dosage may need to be reduced in elderly patients and patients with renal dysfunction. In addition, pregabalin increases the risk of falls in elderly patients. Weight gain due to pregabalin may make it necessary to adjust the dosage of blood sugar-lowering medication in people with diabetes.

Pregnancy and breastfeeding

Pregabalin should not be taken by pregnant or breastfeeding women, as animal experiments have shown fruit-damaging effects and the active substance has been detected in breast milk. If possible, more suitable alternatives such as amitriptyline (neuropathic pain) or lamotrigine and levetiracetam (focal seizures) should therefore 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 obtain medication with pregabalin

In Germany, Austria and Switzerland, the active ingredient pregabalin is only available on prescription in any dosage and pharmaceutical form and can only be obtained from pharmacies with a doctor’s prescription.

How long has pregabalin been known?