Pregabalin

Pharmacological action Lyrica

Lyrica – a drug that has antiepileptic and anticonvulsant activity. The active component of the drug is pregabalin – alkylated analogue of gamma-aminobutyric acid, however, despite the structural similarity of molecules, pregabalin does not have the characteristic gamma-aminobutyric acid activity. Pregabalin does not have any direct or indirect GABA-ergic action. The mechanism of drug action based on its ability to bind to alpha-2-delta subunits of neuronal calcium channels (calcium channels, N-and P / O-type), resulting in a decline in transport of calcium cells in response to neuronal action potential. To a high degree of drug affinity for the alpha-2-delta protein, located in the tissues of the central nervous system. Use of the drug reduces the release of neurotransmitters, pain (including glutamate, noradrenaline and substance P) into the synaptic cleft during excitation of neurons. Because of these changes under the action of the drug selectively suppressed impulse conduction, it should be noted that the drug inhibits the excitability of the lyrics are a network of neurons only in pathological states.

The drug has analgesic effect in neuropathic pain etiology and postoperative pain syndrome, including conditions such as hyperalgesia and alodiniya.

The drug at a therapeutic dose is well tolerated by patients in the studies noted a lack of teratogenic effects when using the drug at doses 2 times greater than therapeutic. As a result, a number of studies have noted the lack of carcinogenic and genotoxic action of pregabalin.

After oral administration of the drug is well absorbed from the gastrointestinal tract, peak concentrations of the active substance in plasma was 1 hour after oral dosing. Repeated use of the drug Lyrica time to reach maximum plasma concentration of the active substance does not change. Bioavailability does not depend on the dose and about 90%. Repeated use of the drug pregabalin equilibrium concentrations are attained within 24-48 hours. Food intake decreases the rate and extent of absorption of pregabalin, so while taking the drug with food during the peak of the active substance in the plasma increases by 2.5 hours and the maximum plasma drug concentrations are reduced by 25-30% (compared with data obtained after administration medication on an empty stomach). It should be noted that food intake has no clinically significant effect on the amount of absorption.

For the drug is not characteristic of binding to plasma proteins. Pregabalin well penetrates the blood-brain barrier and gematoplatsentarny and is excreted in breast milk.

A small part of the preparation (less than 1%) is metabolized to form N-methylated compounds. Output unchanged drug in urine. About 1% of the drug is excreted in the urine as metabolites. The half-life of the drug is 6.3 hours. It should be noted that pregabalin clearance is directly proportional to creatinine clearance.

Patients taking antiepileptic drugs, and patients suffering from chronic pain syndrome, pharmacokinetic parameters are similar to those in healthy volunteers.

Patients with impaired renal function, dosage adjustment is necessary. Reduced clearance of pregabalin in patients with renal insufficiency is directly proportional reduction in creatinine clearance. Patients with reduced creatinine clearance is necessary to decrease the dose of the drug Lyrica, and patients on hemodialysis, after hemodialysis is necessary to increase the dose of pregabalin (after 4 hours of hemodialysis of blood plasma derived approximately 50% of the dose of the drug).

Patients suffering from hepatic failure, dose adjustment is not usually required, since pregabalin in small quantities is metabolized, and hepatic dysfunction has no significant effect on the pharmacokinetics of the drug.

In elderly patients there is a decrease in creatinine clearance and pregabalin, it is recommended to adjust the dose of the drug Lyrica for patients with age-related impaired renal function.

Indications Lyrica

The drug is used to relieve pain in patients with fibromyalgia and neuropathic pain etiology.

In addition, the drug used to treat patients with generalized anxiety disorders and epilepsy. In patients with epilepsy drug Lyrica is used as adjunctive therapy of partial means of (partial) seizures, including partial seizures, which are accompanied by secondary generalization.

How to use Lyrica

The drug is taken orally, it is recommended to swallow the capsule whole without chewing or crushing, drinking plenty of water. The drug is taken regardless of meals. The duration of treatment and the dose determined by the attending physician for each patient depending on the nature of the disease and personal characteristics of the patient.

Adult patients suffering from neuropathic pain, are usually given medication in an initial dose of 75 mg 2 times a day. If necessary, gradually increase the dose to 150 mg 2 times a day (this is the optimal dose for most patients with neuropathic pain etiology). For some patients, depending on individual sensitivity to pregabalin and severity of the disease requires higher doses of the drug. In this case the first dose is gradually increased to 150 mg 2 times a day, then the dose may be increased to 300 mg 2 times a day (between each dose increase is necessary to observe an interval of at least 7 days).

The maximum daily dose is 600 mg.

The therapeutic effect develops within weeks after starting the drug. The duration of treatment determined by the attending doctor. After treatment abolition of the drug produced, gradually reducing the dose for at least 7 days.

Adults and adolescents over the age of 12 years with epilepsy are usually given medication in an initial dose of 75 mg 2 times a day. One week after initiation of therapy, if necessary, the dose may be increased to 150 mg 2 times a day. Further increasing the dose, if necessary, spend 7 days after the last dose increase.

The maximum daily dose of 600 mg.

Duration of the course of drug treatment determined by the attending doctor. Patients taking other antiepileptic drugs, pregabalin dose adjustment is required, as the drug has no effect on the concentration and pharmacological effects of other anticonvulsants. Removal of the drug Lyrica should take place gradually over a period of at least 7 days.

Patients with impaired renal function, dosage is determined depending on the performance of creatinine clearance:

Patients with creatinine clearance 60 ml / min is usually prescribed drug in the initial daily dose of 150 mg. The maximum daily dose is 600 mg. Recommended daily dose divided into two doses.

Patients with creatinine clearance of 30 to 60 ml / min is usually prescribed drug in the initial daily dose of 75 mg. The maximum daily dose is 300 mg. The daily dose is recommended to take at one time or divided into two doses.

Patients with creatinine clearance of 15 to 30 ml / min is usually prescribed drug in the initial daily dose of 25-50 mg. The maximum daily dose is 150 mg. The daily dose is recommended to take at one time or divided into two doses.

Patients with creatinine clearance below 15 ml / min is usually prescribed drug in the initial daily dose of 25 mg. The maximum daily dose is 75 mg. The daily dose is recommended to take at one time.

Patients suffering from impaired renal function who are on hemodialysis is recommended to appoint an additional dose of the drug Lyrica after the hemodialysis session (as in within 4 hours of hemodialysis blood plasma displays about 50% of the dose pregabalin). Usually early in treatment an extra dose pregabalin after hemodialysis is 25 mg, but depending on the patient’s individual sensitivity to the drug dose may be gradually increased to 100 mg.

Patients with impaired liver function, the correct dose of the drug Lyrica is not needed.

If necessary, use in elderly patients is advisable to check renal function prior to the application of pregabalin. Elderly patients with normal renal function, dosage adjustment of pregabalin is not required.

Side effects Lyrica

The drug is generally well tolerated, but in rare cases may develop after effects (it is possible that the development of side effects associated with the passage of the underlying disease):

Gastro-intestinal tract: violation of appetite (perhaps as increased appetite and anorexia), dry mouth, nausea, vomiting, disturbances of stool, bloating. In addition, the possible development of hypersalivation, oral gipoestezii and gastroesophageal reflux. In rare cases, patients experienced the development of pancreatitis, hypoglycemia, ascites, and dysphagia.

Cardio-vascular system and hematopoietic system: tachycardia, neutropenia, redness and flushing, atrioventricular block first degree, changes in blood pressure. In a few cases may develop sinus arrhythmia (mentioned development as tachycardia and bradycardia).

From the central and peripheral nervous system: dizziness, headache, drowsiness, ataxia, decreased attention, impaired coordination, euphoria, irritability, confusion. In addition, violations may develop mnestic function, memory loss, tremors, dysarthria, paresthesias, speech disturbances, difficulties with the selection of words, anxiety, depersonalization. Some patients have noted the development of sleep disorders including insomnia and abnormal dreams. Using the drug in patients observed mood swings, depression, anxiety wanton, hallucinations, apathy, elation, psychomotor hyperactivity, giperesteziya, reduced reflexes, dyskinesia, the development of acute anxiety with panic reaction. In a few cases may develop hypokinesia, diplopia and parsomii.

From the senses: taste disturbance sensitivity, hyperacusis, visual disturbances, including diplopia, dry eyes, reduced vision, tearing, eye-strain, eye pain. In a few cases noted the development of fotopsii, eye irritation, mydriasis, disorders of peripheral vision, and strabismus ostsilopsii.

The respiratory system: respiratory failure, dry mucous membranes, cough, rhinitis, nasopharyngitis, snoring. In addition, the possible development of nasal bleeding and a sense of contraction in the throat.

On the part of the musculoskeletal system: muscle fasciculations, cramps, pain in muscles and joints, swelling of joints, muscle stiffness, pain in back and limbs. In a few cases noted the development of spasm of the neck muscles and rhabdomyolysis.

Urogenital system: reduction of urine, renal failure, urinary incontinence, erectile dysfunction, ejaculation disorders, amenorrhea, dysmenorrhea, decreased or increased libido, and anorgasmia.

Allergic reactions: skin rash, itching, rash, papular rash.

Other: increased sweating, pain and hypertrophy of the breast, discharge from the breast.

Using the drug observed changes in some indicators of laboratory tests, including elevated liver transferase, increased concentrations of creatinine and glucose in the blood, reducing the number of platelets and white blood cell count, hypokalemia.

Contraindications Lyrica

Increased individual sensitivity to the drug.

In the absence of reliable data on the safety of the drug pregabalin in pediatric patients is not indicated for children under the age of 12 years.

The drug is recommended with caution during pregnancy and lactation, as well as patients with impaired renal function.

Pregnancy

In the absence of reliable data on the safety of pregabalin during pregnancy, the drug can only be used under strict control physician, before prescribing the drug that must be carefully weighed the expected benefits to the mother and the potential risks to the fetus.

Before starting the drug Lyrica is recommended to exclude pregnancy during therapy pregabalin is recommended that women use reliable contraception.

In the experiments it was found in rats pregabalin selection through breast milk. Data on the allocation of the drug in breast milk in humans do not. If necessary, use during lactation is recommended to resolve the issue of termination of breastfeeding.

Interactions with other drugs

Pregabalin to a small extent is metabolized in the body and almost not bound to plasma proteins, so pharmacokinetic interaction of the drug Lyrica with other drugs is unlikely.

The drug, while the application increases the effects of ethanol and lorazepam.

With simultaneous use of pregabalin and oxycodone has increased, violations mnestic functions and basic motor functions, which are caused by taking oxycodone.

The drug has no effect on the pharmacological effects of other anticonvulsants, as well as to the effectiveness of oral contraceptives, diuretics, oral antidiabetic agents or insulin.

Overdose Lyrica

An overdose of the drug is unlikely, since even when using the drug in doses several times greater than recommended not mentioned the development of new side effects.

If necessary, gastric lavage, in addition, appoint reception enterosorbents and symptomatic therapy.

In the case of the drug in doses many times higher than recommended, it is shown hemodialysis.

Storage

The drug should be stored in a dry, dark place at a temperature of 15 degrees to 25 degrees Celsius.

Shelf life – 3 years.

Ingredients

1 capsule of the drug Lyrica 50 includes:

Pregabalin – 50 mg;

Excipients, including lactose monohydrate.

1 capsule of the drug Lyrica 75 contains:

Pregabalin – 75 mg;

Excipients, including lactose monohydrate.

1 capsule of the drug Lyrica 150 contains:

Pregabalin – 150 mg;

Excipients, including lactose monohydrate.

1 capsule contains 300 drug Lyrica:

Pregabalin – 300 mg;

Excipients, including lactose monohydrate.

Attention!

Before using the drug Lyrica, you should consult with a physician. This instruction is given a free transfer and is designed for educational purposes only. For more information, please contact the manufacturer annotations.

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