Pregabalin - instructions for use, reviews, analogs and formulations (capsules or tablets 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg and 300 mg Richter, Canon) drugs for the treatment of epilepsy, seizures and convulsions in adults , children and pregnancy

In this article, you can read the instructions for using the drug Pregabalin. The visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Pregabalin in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Pregabalin in the presence of existing structural analogues. Use for the treatment of epilepsy, seizures, seizures, neuropathic pain in adults, children, as well as during pregnancy and lactation.

Pregabalin - An anticonvulsant, an analogue of gamma-aminobutyric acid ((S) -3- (aminomethyl) -5-methylhexanoic acid).

It was established that pregabalin binds to the additional subunit (alpha2-delta protein) of potential-dependent calcium channels in the CNS, irreversibly replacing [3H] -gabapentin. It is suggested that such binding can promote the manifestation of analgesic and anticonvulsant effects of pregabalin.

Neuropathic pain

Pregabalin is effective in patients with diabetic neuropathy and postherpetic neuralgia.

It has been established that when taking pregabalin with courses up to 13 weeks 2 times a day and up to 8 weeks 3 times a day, the risk of side effects and the effectiveness of the drug when taking 2 or 3 times a day are the same.

When taking a course of up to 13 weeks, the pain decreased during the first week, and the effect persisted throughout the course of therapy.

In 35% of patients with pregabalin and 18% of patients receiving placebo, the pain index was reduced by 50%. Among patients who received pregabalin and did not show drowsiness, a 50% reduction in the pain index was noted in 33% of cases; among patients who received placebo, this figure was 18%.Drowsiness was noted in 48% of patients receiving pregabalin, and in 16% of patients receiving placebo.

Fibromyalgia

The expressed decrease in pain symptoms in fibromyalgia was noted in patients receiving pregabalin at a dose of 300-600 mg per day. The efficacy of doses of 450 mg and 600 mg per day was comparable, but a dose of 600 mg per day was usually worse tolerated. In addition, against the background of the use of pregabalin, there was an improvement in the functional activity of patients, as well as a decrease in the severity of sleep disturbances. The use of pregabalin at a dose of 600 mg per day led to a more pronounced improvement in sleep, compared with a dose of 300-450 mg per day.

Epilepsy

When taking the drug for 12 weeks, 2 or 3 times a day, the risk of unwanted reactions and the effectiveness of the drug at these dosing regimes are the same. Reduction in the frequency of seizures is noted already during the first week of taking the drug.

Generalized anxiety disorder

Reduction of symptoms of generalized anxiety disorder is noted in the first week of treatment. After 8 weeks of treatment, a 50% reduction in Hamilton anxiety symptoms (NAM-A) was observed in 52% of patients treated with pregabalin and 38% of patients receiving placebo.

Composition

Pregabalin + excipients.

Pharmacokinetics

In healthy volunteers, patients with epilepsy, who received antiepileptic therapy, and in patients who received pregabalin for relief of chronic pain syndromes, similar indicators of the pharmacokinetics of pregabalin in equilibrium were observed.

Pregabalin is rapidly absorbed after ingestion on an empty stomach. Cmax in blood plasma is achieved after 1 h both with a single and repeated application. The intake of food reduces Cmax by about 25-30%, and the time to reach Cmax increases to about 2.5 hours. However, eating does not have a clinically significant effect on the overall absorption of pregabalin.

Pregabalin does not bind to blood plasma proteins. Virtually does not undergo metabolism. After taking labeled pregabalin, approximately 98% of the radioactive label was detected in the urine unchanged. The proportion of the N-methylated derivative of pregabalin, which is the main metabolite found in the urine, was 0.9% of the dose. There were no signs of racemization of the S-enantiomer of pregabalin into the R-enantiomer.

Pregabalin is excreted mainly by the kidneys in unchanged form.

The clearance of pregabalin with age tends to decrease,which reflects the age-related decline in QC. Elderly patients (over 65 years) with impaired renal function may need to reduce the dose of the drug.

The sex of the patient does not have a clinically significant effect on the concentration of pregabalin in the blood plasma.

Indications

Neuropathic pain:

• treatment of neuropathic pain in adult patients.

Epilepsy:

• as additional therapy in adult patients with partial convulsive seizures, accompanied or not accompanied by secondary generalization.

Generalized anxiety disorder:

• treatment of generalized anxiety disorder in adult patients.

Fibromyalgia:

• treatment of fibromyalgia in adult patients.

Forms of release

Capsules 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg and 300 mg (sometimes mistakenly referred to as tablets).

Instructions for use and dosing regimen

The drug is used inside, regardless of food intake, at a dose of 150 to 600 mg per day in 2 or 3 doses.

Neuropathic pain

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

Epilepsy

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

Fibromyalgia

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

Generalized anxiety disorder

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

Abolition of the drug

If treatment with pregabalin should be stopped, it is recommended to do this gradually for at least 1 week (possibly the development of withdrawal syndrome).

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

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.

Side effect

• nasopharyngitis;
• neutropenia;
• increased appetite;
• anorexia;
• hypoglycemia;
• euphoria;
• confusion of consciousness;
• decreased libido;
• insomnia;
• irritability disorientation;
• depersonalization;
• anorgasmia;
• anxiety;
• depression;
• agitation;
• mood lability;
• depressed mood;
• difficulties in the selection of words;
• hallucinations;
• unusual dreams;
• increased libido;
• panic attacks;
• apathy;
• increased insomnia;
• disinhibition;
• a good mood;
• dizziness;
• drowsiness;
• ataxia;
• violation of attention;
• lack of coordination;
• memory impairment;
• tremor;
• dysarthria;
• paresthesia;
• disturbance of balance;
• amnesia;
• sedation;
• lethargy;
• cognitive disorders;
• hypoesthesia;
• nystagmus;
• speech impairment;
• myoclonic cramps;
• hyporeflexion;
• dyskinesia;
• psychomotor agitation;
• postural dizziness;
• hyperesthesia;
• loss of taste;
• burning sensation on mucous membranes and skin;
• intentional tremor;
• stupor;
• fainting;
• hypokinesia;
• parosmia;
• dysgraphy;
• headache;
• loss of consciousness;
• cognitive impairment;
• convulsions;
• blurred vision;
• diplopia;
• narrowing of the fields of vision;
• decreased visual acuity;
• Pain in the eyes;
• asthenopia;
• dryness in the eyes;
• swelling of the eyes;
• increased lacrimation;
• eye irritation;
• mydriasis;
• Oscilloscopy (subjective sensation of the oscillation of the objects under consideration);
• impaired perception of visual depth;
• loss of peripheral vision;
• strabismus;
• increased brightness of visual perception;
• keratitis;
• loss of vision;
• vertigo;
• tachycardia;
• AV-blockade of 1 degree;
• a decrease in blood pressure;
• coldness of limbs;
• increased blood pressure;
• hyperemia of the skin;
• sinus tachycardia;
• sinus arrhythmia;
• sinus bradycardia;
• chronic heart failure;
• prolongation of the QT interval;
• dyspnea;
• cough;
• dryness of the nasal mucosa;
• nasal congestion;
• bleeding from the nose;
• rhinitis;
• snore;
• pulmonary edema;
• dry mouth;
• constipation, diarrhea;
• nausea, vomiting;
• flatulence;
• bloating;
• increased salivation;
• gastroesophageal reflux;
• hypoesthesia of the oral mucosa;
• ascites;
• dysphagia;
• pancreatitis;
• rare cases of edema of the tongue;
• sweating;
• cold sweat;
• hives;
• rare cases of edema of the face;
• itching;
• Stevens-Johnson syndrome;
• twitching of muscles;
• swelling of the joints;
• muscle spasms;
• myalgia;
• arthralgia;
• backache;
• pain in the limbs;
• stiffness of muscles;
• spasm of the neck muscles;
• pain in the neck;
• dysuria;
• urinary incontinence;
• oliguria;
• kidney failure;
• retention of urine;
• angioedema;
• allergic reactions;
• hypersensitivity;
• erectile disfunction;
• delay in ejaculation;
• sexual dysfunction;
• amenorrhea;
• pain in the mammary glands;
• discharge from the mammary glands;
• dysmenorrhea;
• increase of mammary glands in volume;
• gynecomastia;
• fatigue;
• edema (including peripheral);
• feeling of "intoxication";
• violation of gait;
• asthenia;
• thirst;
• a feeling of restraint in the chest;
• generalized edema;
• chills;
• pain;
• pathological sensations;
• hyperthermia;
• increase in body weight;
• increased activity of ALT, AST, KFK;
• a decrease in the number of platelets;
• increase in the concentration of glucose and creatinine of the blood;
• decrease in the potassium content of blood;
• decreased body weight;
• decrease in the number of leukocytes in the blood.

Contraindications

• rare hereditary diseases, incl.intolerance to galactose, lactase deficiency or glucose-galactose malabsorption;
• children and adolescents under 17 years of age inclusive (due to lack of data);
• hypersensitivity to the active substance or any other component of the drug.

Application in pregnancy and lactation

Data on the use of pregabalin in pregnant women is not enough. In studies using animals, signs of reproductive toxicity of the drug were recorded. Therefore, pregabalin can be used during pregnancy only if the intended benefit for the mother clearly exceeds the possible risk to the fetus.

When using the drug, women of reproductive age should use adequate methods of contraception.

There is no information about the penetration of pregabalin into breast milk in women, however, it is noted that in lactating rats it is excreted with milk. In this regard, during treatment with pregabalinum breastfeeding is not recommended.

Use in children

Safety and efficacy of pregabalin in children under 12 years of age and adolescents (12-17 years of age) is not established. The use of the drug in children is not recommended.

Application in elderly patients

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

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 such undesirable reactions appear as a response to the use of pregabalin, such as blurred vision or other abnormalities on the part of the eye, withdrawal of the drug may help to eliminate 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 phenomena 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.

Impact on the ability to drive vehicles and work with mechanisms with an increased risk of injury

Pregabalin can cause dizziness and drowsiness and, accordingly, affect the ability to drive vehicles and work with mechanisms. Patients should not drive vehicles and mechanisms or perform other potentially hazardous activities until it is clear whether the drug affects the ability to do so.

Drug Interactions

Since pregabalin is mainly excreted by the kidneys unchanged, it undergoes minimal metabolism in humans (in the form of metabolites, less than 2% of the dose is excreted by the kidneys), does not inhibit the metabolism of other medicinal substances and does not bind to blood plasma proteins, it is unlikely to enter into pharmacokinetic interaction.

There were no signs of clinically significant pharmacokinetic interaction of pregabalin with phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone and ethanol (alcohol). It has been established that oral hypoglycemic agents, diuretics, insulin, phenobarbital, tiagabine and topiramate have no clinically significant effect on the clearance of pregabalin.

The use of oral contraceptives containing norethisterone and / or ethinylestradiol simultaneously with pregabalin does not affect the equilibrium pharmacokinetics of the drugs.

In patients taking pregabalin and drugs, depressing the central nervous system, there were cases of respiratory failure and coma.

There have been reports of negative effects of pregabalin on gastrointestinal function (including the development of intestinal obstruction, paralytic ileus, constipation) with concomitant 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 (alcohol) and lorazepam.

Analogues of the drug Pregabalin

Structural analogs for the active substance:

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

Analogues on the curative effect (antiepileptic drugs):

• Actinerval;
• Acetazolamide;
• Benzobarbital;
• Benzon;
• Valparin;
• Valproate sodium;
• Valproic Acid Sandoz;
• Wimpat;
• Gabagamma;
• Gabapentin;
• Habitryl;
• Halodiff;
• Gapentec;
• Hexamidine;
• Depakin;
• Depakin chrono;
• Diazepam;
• Diakarb;
• Diphenine;
• Zonegran;
• Inovevelon;
• Carbamazepine;
• Carbapine;
• Carbasan retard;
• Clonazepam;
• Convulex;
• Convulsant;
• Convulsofin;
• Lameptil;
• Lamitor;
• Lamolope;
• Lamotrigine;
• Levetiracetam;
• Mazepine;
• Mysolin;
• Neuronthin;
• Paglyuferal;
• Primidone;
• Relium;
• Rivotril;
• Sabril;
• Sibazon;
• Suxilep;
• Tegretol;
• Topamax;
• Topiramate;
• Topsaver;
• Trileptal;
• Ficomp;
• Phenobarbital;
• Finlepsin;
• Finlepsin retard;
• Chloracon;
• Exalieff;
• Enkorat;
• Epimax;
• Epitope;
• Eplorontin.

Similar medicines:

Other medicines: