Lyrica tablets are an antiepileptic drug derived from gamma-aminobutyric acid.
Hard gelatin capsules from light red brown to red brown, containing white or almost white powder
Actively acting component:
Antiepileptic and anticonvulsant
Lyrica® belongs to the group of drugs with anticonvulsant and antiepileptic activity.
Pregabalin (an active component) binds to the alpha-2-delta subunits of calcium channels (P / O and N-type), and, in response to the action potential, helps to reduce calcium transport to neuron cells.
With postoperative pain and pain of neuropathic origin, the https://anticonvulsants-info.com/ has an analgesic effect. It is well tolerated in therapeutic doses, and even when the dosage is exceeded by 2 times, it does not cause toxic, carcinogenic and teratogenic effects.
After internal use, Lyrica® capsules are well adsorbed in the digestive tract. The peak concentration of the active component in blood plasma occurs an hour after taking the drug.
With repeated use, the time to reach maximum plasma concentration remains the same. The bioavailability of the drug, regardless of the dose taken, is 90%. The equilibrium concentration of the drug with repeated administration is achieved after 24-48 hours.
The degree and rate of absorption of the active component decreases with food intake, however, this does not have a significant (clinically significant) effect on the absorption volume.
Pregabalin has good penetration through the blood-brain and blood-brain barrier, can be excreted in breast milk, does not bind to plasma proteins.
The drug practically does not lend itself to metabolism (about 98% is excreted along with urine unchanged). The half-life of the drug is 6.3 hours.
The drug is approved for use only in adulthood.
Relative contraindications include renal and heart failure, pregnancy and lactation, as well as a history of drug dependence.
Lyrica® is a drug for internal (oral) use. The capsule is recommended to be swallowed without chewing, washed down with plenty of water, regardless of the meal. The dosage and duration of course use is prescribed individually, depending on the clinical features and nature of the disease.
The initial dose for neuropathic pain is 75 mg (2 times a day). If necessary, the dosage is increased to 150 mg (this amount is considered the most optimal for neuropathy). According to medical indications, the daily dosage of the drug can be increased to 300 mg, divided into 2 doses. The maximum daily dose is 600 mg.
The therapeutic effect of taking the drug develops after a week from the start of capsule use. When finishing treatment, the dose of the drug is gradually reduced over a period of 7 days.
The daily dosage for patients with epilepsy is 75 mg (2 times a day). After a week, according to medical indications, the dose can be increased to 150 mg. A further increase in dosage is carried out after another week (if necessary). The maximum dose is 600 mg per day, divided by 2 times.
Lyrica® does not affect the pharmacological effects of other anticonvulsants; therefore, dose adjustment is not required. In the treatment of patients with impaired renal function, the dosage is prescribed taking into account creatinine clearance indicators.
Due to the fact that the active component of the drug is practically not metabolized and does not bind to plasma proteins, its pharmacokinetic effect with other drugs is unlikely.
With concomitant use with lorazepam and ethanol, pregabalin enhances their action. Concomitant use with oxycodone can cause impaired motor function.
From the digestive tract: nausea, dryness in lying, vomiting, impaired appetite, flatulence, constipation or diarrhea. In rare cases, the development of oral hypoesthesia (decreased sensitivity), increased secretory function of the salivary glands, gastroesophageal reflux, dysphagia, hypoglycemia, pancreatitis and ascites are possible.
From the side of the central nervous system and PNS: drowsiness, dizziness, headache, decreased attention, ataxia, euphoria, impaired coordination of movements, confusion, increased irritability, aggressiveness.
In some cases, impaired memory, praxis and speech, the development of tremor, paresthesia.
Depersonalization, insomnia, hallucinations, apathy, decreased reflexes, acute anxiety, panic reactions, etc. can also be observed.
uncontrolled muscle contractions (fasciculation), muscle stiffness, cramps, pain in the back and limbs. In rare cases, spasm of the cervical muscles, rhabdomyolysis (destruction of muscle cells).
An overdose of the drug is almost impossible (no side effects were observed even when the recommended doses were exceeded several times).
In the event that the patient develops negative symptoms, he is given symptomatic treatment, and, if necessary, gastric lavage is performed and enterosorbents are given.
If the recommended dose is repeatedly exceeded, hemodialysis is indicated.
Information on the effect of Lyrica® on the ability to drive a car or perform work that requires an increased concentration of attention and speed of psychomotor reactions has not been identified.
The drug is dispensed by prescription.
Store in a dry, dark place, out of the reach of children, at a temperature not exceeding 25 C. Shelf life 3 years.
Pfizer Manufacuring Deutschland GmbH. Germany.
The average cost of Lyrica capsules in pharmacies in Moscow is:
An antiepileptic drug whose active ingredient is an analogue of gamma-aminobutyric (gamma-aminobutyric) acid (GABA).
It was found that pregabalin binds to an additional subunit (α2-delta protein) of voltage-dependent calcium channels in the central nervous system, irreversibly replacing [3H] -gabapentin. It is believed that such binding may contribute to the manifestation of its analgesic and anticonvulsant effects.
A decrease in the pain index by 50% was noted in 35% of patients receiving pregabalin, and in 18% of patients taking placebo. Among patients who did not experience drowsiness, the effect of this reduction in pain was observed in 33% of patients in the pregabalin group and 18% of patients in the placebo group. In 48% of patients taking pregabalin, and in 16% of patients receiving placebo, drowsiness occurred.
A pronounced decrease in pain symptoms associated with fibromyalgia is noted with the use of pregabalin in doses from 300 mg to 600 mg per day. The effectiveness of doses of 450 mg and 600 mg per day is comparable, however, dose tolerance of 600 mg / day is usually worse.
The use of pregabalin is associated with a marked improvement in the functional activity of patients and a decrease in the severity of sleep disturbances.
The use of pregabalin at a dose of 600 mg / day led to a more pronounced improvement in sleep, compared with a dose of 300-450 mg / day.
When using the drug for 12 weeks, 2 or 3 times / day, the noted risk of side effects and the effectiveness of the drug under these dosing regimens are the same. The decrease in the frequency of seizures began during the first week.
Generalized Anxiety Disorder
The decrease in symptoms of generalized anxiety disorder is noted in the first week of treatment. When using the drug for 8 weeks, 52% of patients receiving pregabalin and 38% of patients receiving placebo showed a 50% decrease in symptoms on the Hamilton anxiety scale (NAM-A).
The pharmacokinetics of pregabalin in the range of recommended daily doses is linear, interindividual variability is low (
Lyrica – a drug with antiepileptic and anticonvulsant activity.
The active component of the drug is pregabalin, an alkyl analogue of gamma-aminobutyric acid, however, despite the structural similarity of the molecules, pregabalin does not have the activity characteristic of gamma-aminobutyric acid.
Pregabalin has neither a direct nor indirect GABAergic effect.
The mechanism of action of the drug is based on its ability to bind to the alpha-2-delta subunits of calcium channels of neurons (calcium channels of N- and P / O-type), as a result of which there is a decrease in calcium transport to neuron cells in response to the action potential.
The drug is characterized by a high degree of affinity for the alpha-2-delta protein located in the tissues of the central nervous system. The use of the drug leads to a decrease in the release of pain neurotransmitters (including glutamate, norepinephrine and substance P) into the synaptic cleft upon excitation of neurons. Due to such changes, the impulse is selectively suppressed under the influence of the drug, it should be noted that the Lyrica drug suppresses the excitability of the network of neurons only in pathological conditions.
The drug has an analgesic effect for pains of neuropathic etiology and postoperative pain, including in conditions such as hyperalgesia and alodynia.
The drug in a therapeutic dose is well tolerated by patients; during the studies, there was a lack of teratogenic effects when using the drug in doses 2 times higher than therapeutic. As a result of a number of studies, the absence of the carcinogenic and genotoxic effects of pregabalin was noted.
After oral administration, the drug is well absorbed in the gastrointestinal tract, the peak concentration of the active substance in the blood plasma is observed 1 hour after oral administration of the drug. With repeated use of the drug Lyrica, the time to reach the maximum plasma concentration of the active substance does not change.
The bioavailability of the drug does not depend on the dose taken and is about 90%. With repeated use of the drug, equilibrium concentrations of pregabalin are reached within 24-48 hours.
Eating reduces the speed and degree of absorption of pregabalin, so while taking the drug with food, the time to reach the peak of the active substance in plasma increases by 2.5 hours, and the maximum plasma concentrations of the drug are reduced by 25-30% (compared with the data obtained after administration fasting drug).
It should be noted that eating does not have a clinically significant effect on the volume of absorption.
The drug is not characterized by binding to plasma proteins. Pregabalin penetrates well through the blood-brain and hematoplacental barriers, and is also excreted in breast milk.
An insignificant part of the drug (less than 1%) is metabolized to form an N-methylated compound. The drug is excreted unchanged in urine. About 1% of the drug is excreted in the urine as a metabolite. The half-life of the drug is 6.3 hours. It should be noted that pregabalin clearance is directly proportional to creatinine clearance.
In patients taking antiepileptic drugs and patients suffering from chronic pain, the pharmacokinetics are similar to those in healthy volunteers.
In patients with impaired renal function, dose adjustment is necessary. A decrease in pregabalin clearance in patients suffering from renal failure is directly proportional to a decrease in creatinine clearance.
Patients with reduced creatinine clearance need a reduction in the dose of Lyrica drug, and patients on hemodialysis, after a hemodialysis session, it is necessary to increase the dose of pregabalin (after 4 hours of hemodialysis, about 50% of the taken dose of the drug is removed from blood plasma).
In addition, the drug is used to treat patients with generalized anxiety disorders and epilepsy. In patients with epilepsy, Lyrica is used as an additional treatment for partial (partial) seizures, including partial seizures, which are accompanied by secondary generalization.
The drug Lyrica is taken orally, it is recommended to swallow the capsule whole, without chewing and not crushing, drinking plenty of water. The drug is taken regardless of the meal. The duration of the course of treatment and the dose of the drug is determined by the attending physician individually for each patient, depending on the nature of the disease and personal characteristics of the patient.
Adult patients suffering from neuropathic pain are usually prescribed an initial dose of 75 mg 2 times a day. If necessary, the dose is gradually increased to 150 mg 2 times a day (this dose is optimal for most patients with pain of neuropathic etiology).
Depending on the individual sensitivity to pregabalin and the severity of the disease, some patients require higher doses of the drug.
In this case, the dose is initially gradually increased to 150 mg 2 times a day, then the dose can be increased to 300 mg of the drug 2 times a day (an interval of at least 7 days must be observed between each increase in dose).
The maximum daily dose of the drug is 600 mg.
The therapeutic effect develops within a week after the start of the drug. The duration of treatment is determined by the attending physician. After the end of the course of treatment, the drug is canceled, gradually reducing the dose for at least 7 days.
Adults and adolescents over the age of 12 years with epilepsy are usually prescribed the drug in an initial dose of 75 mg 2 times a day.
A week after the start of therapy, if necessary, the dose of the drug can be increased to 150 mg 2 times a day.
A further dose increase, if necessary, is carried out 7 days after the previous dose increase.
The maximum daily dose of the drug is 600 mg.
The duration of the drug treatment is determined by the attending physician. Patients taking other anticonvulsant drugs do not require dose adjustment of pregabalin, since the drug does not affect the concentration and pharmacological effects of other anticonvulsants. The withdrawal of the drug Lyrica should take place gradually over a period of at least 7 days.
For patients with impaired renal function, the dose of the drug is determined depending on the creatinine clearance indicators:
Patients with creatinine clearance greater than 60 ml / min are usually prescribed a drug in an initial daily dose of 150 mg. The maximum daily dose of the drug is 600 mg. The daily dose of the drug is recommended to be divided into 2 doses.
Patients with creatinine clearance from 30 to 60 ml / min are usually prescribed the drug in an initial daily dose of 75 mg. The maximum daily dose of the drug is 300 mg. The daily dose of the drug is recommended to be taken at a time or divided into 2 doses.
Patients with creatinine clearance of 15 to 30 ml / min are usually prescribed the drug in an initial daily dose of 25-50 mg. The maximum daily dose of the drug is 150 mg. The daily dose of the drug is recommended to be taken at a time or divided into 2 doses.
Patients with creatinine clearance less than 15 ml / min are usually prescribed a drug in an initial daily dose of 25 mg. The maximum daily dose of the drug is 75 mg. The daily dose of the drug is recommended to be taken at a time.
Patients suffering from impaired renal function, who are on hemodialysis, it is recommended to prescribe an additional dose of Lyrica after a hemodialysis session (since within a 4-hour hemodialysis session, about 50% of the accepted dose of pregabalin is removed from the blood plasma).
Usually, at the beginning of treatment, the additional dose of pregabalin after hemodialysis is 25 mg, however, depending on the individual sensitivity of the patient to the drug, the dose can be gradually increased to 100 mg.
Patients suffering from impaired liver function do not need dose adjustment of Lyrica.
If it is necessary to use the drug in elderly patients, it is recommended to check kidney function before using pregabalin. Elderly patients with normal renal function do not require dose adjustment of pregabalin.