How Pregabalin Works

Pregabalin (Lyrica) is an antiepileptic drug that reduces the excitability of nerve cells but also has analgesic, antianxiety, and sedative effects. It is used in epilepsy therapy for focal seizures, as well as for various nerve pain, generalized anxiety disorder, and social phobia. It is also approved in the United States for the treatment of fibromyalgia. To learn exactly how pregabalin works, what dosage is appropriate, and what side effects may occur, read this article.

What is pregabalin?

Pregabalin is an active ingredient from the group of antiepileptic drugs, also called anticonvulsants, and is sold in Germany under the trade name Lyrica, among others. In the meantime, however, there are also many generics on the market. Antiepileptics lower the excitability of nerve cells and are used to treat epilepsy.

Treating epilepsy with pregabalin

Pregabalin plays a role in the long-term treatment of so-called focal seizures with or without secondary generalization, which are specific forms of epilepsy. It is always administered as an add-on medication in combination with other epilepsy medications, such as lamotrigine. Pregabalin has been shown to reduce seizure frequency or even achieve seizure freedom.

Pregabalin vs. gabapentin

Pregabalin is the successor drug to gabapentin, an established epilepsy medication. Its advantage over other antiepileptic drugs is that it causes fewer side effects, is more easily metabolized in the body, and attacks its target more effectively. In addition, unlike gabapentin, it is approved for the treatment of other conditions, such as nerve pain and anxiety disorders.

Also used for pain and anxiety

Another major area of use is nerve pain. Nerve pain is characterized by tingling and burning sensations and is caused by certain neurotransmitters, the release of which pregabalin inhibits. Therefore, it is an alternative for other antiepileptic drugs such as carbamazepine and gabapentin. It is used, for example, to treat pain caused by herpes zoster disease or post-herpetic neuralgia syndrome, diabetic neuropathy and spinal cord injuries. Furthermore, it is used in the therapy of generalized anxiety disorder and social phobia. Other possible drugs in the therapy of generalized anxiety disorder include duloxetine and venlafaxine. In the United States, pregabalin is also approved in the treatment of fibromyalgia. It has been shown to have a pain-relieving effect and, although it is already used in Germany for patients with fibromyalgia, it does not yet have official approval. Alternatively, old proven agents such as amitriptyline can be used to treat fibromyalgia.

Dosing and discontinuing pregabalin

Pregabalin comes in capsule or solution form. It can be taken independently of meals. Importantly, pregabalin must be phased in over a period of at least two weeks. The normal starting dose of 150 mg a day is divided into two to three individual doses, and the maximum dose is 600 mg a day. The doctor treating you must determine which dosage is actually suitable for you. How quickly does pregabalin take effect? The first effects usually become apparent after one week. If therapy is discontinued, Pregabalin must also be gradually phased out again, otherwise severe side effects may occur. Sudden discontinuation of pregabalin may cause symptoms to return worse than before.

Side effects of pregabalin

The most common adverse effects of pregabalin are:

  • Drowsiness
  • Drowsiness
  • Dizziness
  • Headache

Attention may also be impaired. Therefore, driving a car is not allowed while taking pregabalin and operating complex machinery is prohibited. In addition, blurred vision, double vision and erectile dysfunction may occur as side effects. Some patients taking pregabalin also report weight gain. There is also evidence that pregabalin can be addictive, especially if there is a history of addiction.

Drug interactions with pregabalin

Because pregabalin is hardly metabolized in the body and is excreted almost unchanged by the kidneys, it has few interactions with other medications.However, caution is advised when taking it simultaneously with depressant substances such as alcohol, benzodiazepines or opioids. In this combination, respiratory arrest and even coma may occur.

Contraindications of the active substance

The main contraindications of pregabalin are:

  • Hypersensitivity to the active substance
  • Pregnancy and lactation
  • Use in children
  • Severely impaired renal function

How does pregabalin work?

Pregabalin has a similar chemical makeup to the nerve cell messenger GABA, an inhibitory hormone. It docks onto the same calcium channels of nerve cells in the brain and body, thereby reducing the release of activating neurotransmitters such as glutamate, norepinephrine, and substance P. The effect is to reduce nerve cell excitation, which has pain-relieving and anxiety-reducing effects, as well as reducing the risk of epileptic seizures.