Effect of Lyrica®
General
Lyrica® (trade name; active ingredient name: Pregabalin) belongs to the newer anti-epileptic drugs and is used to treat:
- focal epilepsies (seizures) or the
- Combination treatment, including generalized seizures,
- for complementary therapy of generalized anxiety disorders and
- neuropathic pain
These are nerve pain that can occur as a result of diabetic foot syndrome, shingles (inflammation of the nerve endings by herpes viruses) or a spinal cord injury.
Effect of anti-epileptic drugs
All Anti-epileptic drugs (Seizure medication) work on several Receptors and Ion channels.
Lyrica® in particular blocks the voltage-dependent Calcium channels and thus interrupts repetitive discharges.
The channels consist of 4 subunits and mediate the influx of Calcium ions in the Nerve cell. This usually leads to the release of various Neurotransmitters and forwarding the Action potential about the Synapse.
By binding Lyrica® to the GABA receptor, inhibitory chloride channels are activated and the actual effect of the calcium channels does not occur. So will the distribution of this Neurotransmitters prevents:
- Norepinephrine,
- Glutamate and
- Substance P
Through the simultaneous inhibition All three substances explain the relatively large area of application.
Glutamate belongs to the Messenger substances of the brain and is involved in the mediation of nerve stimuli Sensory perception, of the Motor skills and the memory involved.
Norepinephrine is a neurotransmitter in the body and is used to transmit important information. For example, it increases the Blood pressure through a vasoconstriction. This happens especially in stressful situations.
Substance P however, is a neurotransmitter of pain- Receptors and nerve fibers that conduct pain. If such a receptor is more strongly excited, it releases substance P. But also with Inflammation Substance P is increasingly released. When released, the substance causes a strong expansion of the blood vessels and increases them Permeability the vessel wall. In addition, the sensitivity of pain-conducting nerves in the Spinal cord increased.
How Lyrica® works
The individual However, the mode of action in individual patients cannot always be explained purely physiologically. This is particularly due to the very individual creation epileptic seizures and the special anti-epileptic mechanisms, which are very complex.
For this reason, it is difficult to draw conclusions about the individual mode of action of the drugs. However, much has improved in the development of some drugs:
In contrast to the classic Anti-epileptic drugs are the newer drugs (for example Lyrica®) clearly better tolerated.
However, you are not more effectivebut own one greater therapeutic breadth and call fewer side effects emerged.
In addition to the main effects mentioned above and the associated area of application, Lyrica® also works sedating. In some cases, for example for epileptic Seizure therapy or for treatment neuropathic pain the sedative effect is undesirable.
In case of Anxiety disorders one can however cause this side effect Reassurance use. The sedative effect arises from the general neuronal inhibition and inhibition of neuronal excitation. This will make the Sensory impressions from the outside muffled, because the nerve cells can no longer pass the information on quickly enough.
The excretion of the drug takes place via the Kidneys with a Half-life of 6 hours.
Onset of action
The onset of action of Lyrica® usually happens within a week. This is already possible with a starting dose of 150 mg per day. The dose can be administered in 2 or 3 divided doses. It can be taken during or between meals. Individually, in consultation with the doctor, the dose can be increased to 300 mg after one week. The maximum dose is usually 600 mg daily. In some cases it is higher. This can be achieved in a further week if necessary. Lyrica® is quickly absorbed by the body regardless of the dose. It has a so-called bioavailability of 90%. As a result, maximum concentrations in the body can be reached on average after about an hour.
Lyrica® is hardly metabolized or bound to proteins in the plasma. Therefore about 98% of it can be excreted unchanged via the kidneys with the urine. The time span in which the plasma concentration of the active ingredient has decreased by half is about 6 hours. Because Lyrica® is eliminated via the kidneys, the dose must be adjusted in people with impaired kidney function and in the elderly. The dose must therefore be reduced according to the functions. Since Lyrica® is not metabolized via the liver, the dose is largely independent of the liver functions. In addition, the effect cannot be influenced by interactions with other drugs that are processed by the liver. This means, for example, that no interactions with other anti-epileptic drugs, certain antibiotics or the birth control pill are to be expected.
Effect on fear
Lyrica® acts on the cells of the so-called cerebellum. These cells are called Purkinje cells. It inhibits calcium channels at a specific point. This means that less calcium gets inside the cell. As a result, fewer exciting messenger substances such as glutamate, noradrenaline and substance P are released. These messenger substances can, among other things, intensify the development of fears. By inhibiting their effects, fears can be (biochemically) throttled in some cases. This effect of the drug is known as the anxiolytic effect.
Read more on the topic: Lyrica® for anxiety disorder
Effect on pain
Lyrica® has shown in several controlled clinical studies that it can also work against so-called peripheral, neuropathic pain. This chronic pain is often described as tingling, burning, severe, or shock-like. Peripheral neuropathic pain can occur in diseases such as shingles, the so-called herpes zoster virus, in spinal cord injuries or diabetic neuropathy. According to some studies, Lyrica® had a soothing effect in this context. According to this, 47% of people who suffered from neuropathic pain experienced an average pain reduction of 50%. In addition, pain-related sleep disorders were significantly fewer.
You might also be interested in this topic: Side effect of Lyrica®
Effect on MS
Lyrica® is used in multiple sclerosis for the symptomatic treatment of nerve pain. Here, the mechanism of action is used with regard to the inhibitory effect on certain messenger substances. Since these messenger substances have an influence on nerve pain, Lyrica® comes in here. Successful pain relief has been recorded. In other cases the side effects predominate. Individual treatment for multiple sclerosis is essential.
Read more on the topic: multiple sclerosis
Can you increase the effects of Lyrica®?
The effect of Lyrica® can be increased by changing the dose. In addition, sedating substances (calming substances) can strengthen the active ingredient. Alcohol can also, in an unpredictable way, intensify the effects and thus the side effects in a life-threatening way.
Read more on the topic: Lyrica® and alcohol
Particular caution is required with previous illnesses and weakness or limitations of the heart, especially in old age. In addition, you should be very careful with a combination of drugs that prolong the so-called QT time (in the ECG). In the case of impaired renal function, lower doses must be given. A reinforcement of Lyrica® should therefore not be carelessly focused. If the effect of Lyrica® does not bring the desired results, you should always consult your doctor first.
What can I do when the effects of Lyrica® wear off?
The dose of Lyrica® can be increased gradually as instructed by the attending physician. However, it should be noted that any increase in dose can also increase the risk of side effects. Increasing the dose too quickly can cause side effects such as drowsiness and drowsiness. These side effects were observed very frequently in this context.
Find out more about the topic: Side effect of Lyrica®
It is imperative to first find out the reasons why the effect has waned before increasing the dose. The dose of Lyrica® should never be changed on your own. If the effect wears off, this should always be discussed with the doctor.
