Pregabalin

Pregabalin is an antiepileptic drug that exerts anticonvulsant and analgesic pharmacological effects.

Used as an additional therapy for partial seizures with secondary generalization and neuropathic pain. Also, this drug helps in the treatment of generalized anxiety disorders. The medicine was developed as a more powerful replacement for Gebapentin.

Before you start taking the drug, you should consult a doctor and also carefully read the instructions for using the drug.

Clinical and pharmacological group

Anticonvulsant drug.

Conditions of leave from pharmacies

It is released on prescription.

Price list

How much is Pregabalin in pharmacies? The average price is at the level of250 rubles.

Form of issue and composition

Pregabalin is available in the form of a capsule for oral administration. They have a dense lid of yellow or brown color (depending on the dosage of the active substance), inside is a white crystalline fine powder.

The composition of Pregabalin (capsules 25/75/100/150/300 mg, respectively):

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active substance: pregabalin - 25/75/100/150/300 mg;
auxiliary components: magnesium stearate - , / , / , / , / , mg; talc 1.6 / 1.6 / 1.6 / 2.95 / 5.9 mg; silicon dioxide colloidal - 3.3 / 3.3 / 3.3 / 5.9 / 11.8 mg; potato starch - 9.95 / 4.93 / 2.42 / 7.565 / 15.13 mg; calcium carbonate - 89.55 / 44.37 / 21.78 / 68.085 / 136.17 mg; sodium lauryl sulfate - , / , / , / , / , mg;
lid: gelatin - up to 100%; titanium dioxide - 1% (capsules of 25 or 75 mg) or 2% (capsules of 100, 150 or 300 mg); capsules on 25 mg - a dye of a jelly oxide yellow - , 143%, indigokarmin - , %; capsules of 75 mg - indigocarmine - 0.1333%;
body: gelatin - up to 100%, titanium dioxide - 2%.

Capsules Pregabalin is packaged in a blister pack of 14 pieces. The cardboard bundle contains 1 or 4 blisters, as well as instructions.

Pharmacological effect

Pregabalin, the active substance of the preparation, is an analogue of gamma-aminobutyric acid of [(S) -3- (aminomethyl) -5-methylhexanoic acid].

It is known that the drug binds to α2-delta-protein, which is an additional subunit of potential-dependent calcium channels in the central nervous system (CNS), irreversibly replaces [3H] -gabapentin. It is believed that such binding can promote the manifestation of analgesic and anticonvulsant properties of the drug.

Mechanism of action of the drug during therapy according to indications:

Epilepsy: when treated with the drug for 12 weeks, a different frequency of reception (2 or 3 times a day) does not affect the effectiveness therapy and threat of development of undesirable reactions; decrease in the frequency of seizures is noted from the first week of the course.
Neuropathic pain: the drug is effective in the presence of diabetic neuropathy and postherpetic neuralgia; when using pregabalin 3 times a day course of up to 8 weeks and 2 times a day until 13 weeks, the same therapeutic effect and the risk of adverse reactions; on the background of taking the drug to 13 weeks The pain syndrome decreases during the first week, and the effect persists until the end of therapy; in 18% of patients who received placebo and 35% of patients who received the drug, it was recorded a decrease in the pain index by 50%; in those taking placebo in 16% of cases and taking pregabalin in 48%, the occurrence of drowsiness was noted.
Fibromyalgia: when doses within 300-600 mg / day are used, the drug shows a significant reduction in pain symptoms due to fibromyalgia; the effectiveness of a daily dose of 450 mg is comparable to a dose of 600 mg, but usually when taking the last pregabalin is worse; at a dose of 600 mg per day, it also contributes to noticeable improvements in the functional activity of patients and a decrease in the severity of sleep disorders when compared with a daily dose of 300-450 mg.
Generalized anxiety disorder: weakening of symptoms of this disease is observed already in the first week of therapy; taking the drug for 8 weeks provides a reduction in symptoms on the Hamilton anxiety scale by 50% in 38% of patients taking placebo, and in 52% who received pregabalin.

In the course of clinical studies in patients who constantly took the drug, reduced visual acuity or blurred vision, vision and other visual impairment were noted more frequently than in patients receiving placebo (except for changes in the fundus).

Indications for use

What helps? Pregabalin is recommended for use in adult patients with the following diseases:

neuropathic pain;
fibromyalgia;
generalized anxiety disorder;
epilepsy (if necessary, additional treatment for patients with partial convulsive seizures, with secondary generalization or without).

Contraindications

Absolute:

children and adolescents under 17;
increased individual sensitivity to pregabalin or auxiliary components of the drug.

Relative (Pregabalin is used with caution):

kidney failure;
heart failure;
drug dependence in the anamnesis.

Use in pregnancy and lactation

Adequate data on the use of the drug during pregnancy are absent. In animal experiments Pregabalin showed a toxicity with respect to reproductive function, so its use in pregnant women is possible only in exceptional cases, when the expected benefit for the mother substantially outweighs the potential risk to the fetus. During treatment with Pregabalin, women of childbearing age should use reliable methods of contraception.

The drug is excreted in breast milk, therefore during the period of Pregabalin's application breastfeeding should be stopped.

Data of clinical studies on the effect of the drug on the fertility of women of reproductive age are absent.

Dosage and route of administration

The instructions for use indicate that Pregabalin is administered orally, regardless of food intake, at a dose of 150 to 600 mg / day in 2 or 3 divided doses. In case of missing a dose of pregabalin, the next dose should be taken as soon as possible. Do not take a double dose of the drug. Resume the usual medication the next day.

Epilepsy:

The initial dose of pregabalin is 150 mg / day. Taking into account the achieved effect and tolerability after 1 week, the dose can be increased to 300 mg / day, and in a week - up to a maximum dose of 600 mg / day.

Neuropathic pain:

The initial dose of pregabalin is 150 mg / day. Depending on the effect achieved and tolerance in 3-7 days, the dose can be increased to 300 mg / day, and, if necessary, after 7 days - up to a maximum dose of 600 mg / day.

Generalized anxiety disorder:

The initial dose of pregabalin is 150 mg / day. Depending on the effect achieved and the tolerability after 7 days, the dose can be increased to 300 mg / day. In the absence of a positive effect, the dose is increased to 450 mg / day, and if necessary, after 7 days - up to a maximum dose of 600 mg / day.

Fibromyalgia:

The initial dose of pregabalin is 75 mg 2 times / day (150 mg / day). Depending on the effect achieved and the tolerance in 3-7 days, the dose can be increased to 300 mg / day. In the absence of a positive effect, the dose is increased to 450 mg / day, and if necessary, after 7 days - up to a maximum dose of 600 mg / day.

Abolition of the drug:

If treatment with pregabalin should be stopped, it is recommended to do this gradually for at least 1 week.

Patients with impaired renal function dose are individually selected with regard to CC (tab. 1), which is calculated by the following formula:

CK (ml / min) = (140 - age in years) × body weight (kg) / 72 × serum creatinine (mg / dl)

For women, the result should be multiplied by 0.85.

Patients who are undergoing hemodialysis receive a daily dose of pregabalin given the kidney function. Immediately after each 4-hour hemodialysis session, an additional dose is prescribed.

In patients with impaired liver function, dose adjustment is not required.

Older patients (over 65 years of age) may need to reduce the dose of pregabalin due to a decrease in kidney function.

Side effects

Drowsiness and dizziness often disturb patients who have started the course of this medication. In addition, asthma attacks and ataxia, confusion, peripheral edema, loss of visual acuity, attention disturbance and coordination of movements may unexpectedly appear. Pregabalin Canon can provoke other side effects, which remind themselves of themselves at the very beginning of the course:

from the side of metabolism: anorexia, hypoglycemia;
from the hematopoiesis: neutropenia, spasms of the vascular walls;
from the urinary system: renal failure, dysuria, urinary retention, oliguria;
from the cardiovascular system: sinus tachycardia and arrhythmia, heart failure;
from the side of the vessels: hyperemia, arterial hypertension and hypotension, hot flashes, cold extremities;
on the part of the organs of vision: diplopia, dry eye syndrome, irritation of the mucous membrane, loss of sharpness, asthenopia, photopsy;
from the musculoskeletal system: arthralgia, back and limb pain, myalgia, limb tremor, muscle cramps, dysarthria;
on the part of the digestive tract: anorexia, signs of dyspepsia, hypersecretion of the salivary glands, ascites, tongue edema, dysphagia, dryness of the oral mucosa;
from the side of the central nervous system: confusion, euphoria, insomnia, disorientation, panic attacks, increased irritability, apathy, propensity to depression, disturbance of psychomotor functions, agitation;
from the side of the reproductive system: erectile dysfunction, dysmenorrhea, gynecomastia, anemorrhoea, increased libido in the absence of orgasm;
others: weight gain, increased creatinine concentration in the blood and other vital indicators of the biological fluid.

Overdose

With overdose Pregabalinum possible development:

confusion of consciousness;
depressive state;
affective disorders;
drowsiness;
agitation and anxiety.

Such cases require gastric lavage, maintenance therapy, and sometimes hemodialysis.

special instructions

Some patients with diabetes mellitus in case of weight gain on the background of treatment with pregabalin may require correction of doses of hypoglycemic agents. If the symptoms of angioedema develop (such as facial edema, perioral edema, or swelling of the upper respiratory tract), pregabalin should be discontinued.

Antiepileptic drugs, including pregabalin, may increase the risk of suicidal thoughts or behavior. Therefore, patients receiving these drugs should be carefully monitored for the appearance or deterioration of depression, the appearance of suicidal thoughts or behavior.

Treatment with pregabalin was accompanied by dizziness and drowsiness, which increases the risk of accidental injuries (falls) in elderly patients. In the course of the post-marketing application of pregabalin, there were also cases of loss of consciousness, confusion, and cognitive impairment. Therefore, as long as patients do not evaluate the possible effects of the drug, they should be careful.

The information about the possibility of canceling other anticonvulsants after achieving seizure control against the background of the use of pregabalin, as well as the advisability of monotherapy with pregabalin, is not enough.

There are reports of the development of seizures, including. epileptic status and small seizures on the background of the use of pregabalin or immediately after the termination of therapy.

When there appear in response to the use of pregabalin such undesirable reactions as blurred vision or other disturbances on the part of the organ of vision, cancellation of the drug may contribute to the disappearance of these symptoms.

There have also been reported cases of development of renal failure against the background of pregabalin therapy; in some cases, after the drug was discontinued, the kidney function was restored.

As a result of cancellation of pregabalin after prolonged or short-term therapy, the following undesirable effects were observed: insomnia, headache, nausea, diarrhea, flu-like syndrome, depression, sweating, dizziness, convulsions and anxiety. Information on the frequency and severity of manifestations of "withdrawal syndrome" of pregabalin, depending on its dose and the duration of therapy, are absent.

During post-marketing application of pregabalin, chronic heart failure was reported in some patients receiving pregabalin. Most of these reactions were observed in elderly patients with impaired heart function and who received pregabalin for neuropathy. Therefore, pregabalin should be used with caution in this category of patients. After the abolition of pregabalin, the disappearance of manifestations of such reactions is possible.

In the treatment of central neuropathic pain caused by spinal cord injury, there was an increase in the frequency of unwanted reactions from the CNS, such as drowsiness. This may be due to the additive effect on the background of the simultaneous use of pregabalin and other medications (for example, antispastic). This circumstance should be taken into account in prescribing pregabalin for the treatment of central neuropathic pain.

There were reported cases of development of dependence when using pregabalin. Patients with drug dependence in a history need careful medical observation for symptoms of dependence on pregabalin.

There were cases of encephalopathy, especially in patients with concomitant diseases, which could contribute to its development.

Drug Interactions

When using the drug, it is necessary to take into account the interaction with other drugs:

In patients taking pregabalin and drugs, depressing the central nervous system, there were cases of respiratory failure and coma.
The use of oral contraceptives containing norethisterone and / or ethinylestradiol simultaneously with pregabalin does not affect the equilibrium pharmacokinetics of the drugs.
There were no signs of a clinically significant pharmacokinetic interaction between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone and ethanol. It has been established that oral hypoglycemic agents, diuretics, insulin, phenobarbital, tiagabine and topiramate have no clinically significant effect on the clearance of pregabalin.
Since pregabalin is mainly excreted by the kidneys unchanged, it undergoes minimal metabolism in man (in the form of metabolites, less than 2% of the dose is excreted by the kidneys), does not inhibit the metabolism of other drugs in vitro and does not bind to blood plasma proteins, it is unlikely to be able to enter a pharmacokinetic interaction.
There have been reports of negative effects of pregabalin on gastrointestinal function (including the development of intestinal obstruction, paralytic ileus, constipation) with simultaneous use with drugs that cause constipation (such as non-narcotic analgesics).
The repeated use of pregabalin with oxycodone, lorazepam or ethanol did not have a clinically significant effect on respiration. It is suggested that pregabalin enhances cognitive and motor function disorders caused by oxycodone. Pregabalin can enhance the effects of ethanol and lorazepam.

Reviews

We picked up some reviews of people who used the drug Pregabalin:

Elena. He treated them with inflammation of the trigeminal nerve. It helped, but the withdrawal syndrome is nightmarish. I've been dizzy for a month now.
Anna. Tablets are taken with increased anxiety, they are excellent for using in full course. Once I violated the recommended dose, I regretted so much. It is very important to observe the dosage, otherwise side effects only increase, provide poisoning of the body. It is still impossible to accelerate treatment with such unauthorized methods.
Marina. With a spinal cord injury, my doctor prescribed such a medical preparation, but I did not complete the course. Too many side effects arose, and it was not just eternal insomnia. There was a tremor in the limbs, trembling hands, a headache, constantly dizzy. It's terrible to live like this, so I switched to Lyric.

Analogues

Structural analogs for the active substance:

Algerian;
Lyrics;
Prabiegin;
Pregabalin Zentiva;
Pregabalin Canon;
Pregabalin Richter;
Pregabalin S3;
Pregabio;
Prigabilon.

Before using analogues, consult your doctor.

Storage conditions and shelf life

The shelf life of the capsules is 2 years from the date of manufacture. The drug should be stored in the original packaging, protected from humidity place at an air temperature of not more than + 25 ° C. Keep away from children.