Pregabalin Canon

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Pregabalin Canon: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Pregabalin Canon

ATX code: N03AX16

Active ingredient: pregabalin (Pregabalin)

Producer: Kanonpharma production, CJSC (Russia)

Description and photo update: 2019-08-07

Pregabalin Canon is an antiepileptic drug with anticonvulsant activity.

Release form and composition

The drug is available in the form of capsules: gelatinous, with a hard structure, Pregabalin Canon 25 mg - No. 3, blue, Pregabalin Canon 50 mg - No. 3, yellow, Pregabalin Canon 75 mg - No. 2, dark yellow, Pregabalin Canon 100 mg - No. 1, blue, Pregabalin Canon 150 mg - No. 1, white body, yellow cap, Pregabalin Canon 200 mg - No. 0, white, Pregabalin Canon 300 mg - No. 0, yellow; the contents of the capsules are a powdery mass of almost white color with inclusions in the form of small compressed pieces or a compressed mass of almost white color, crumbling when pressed (in blisters: 7 pcs., in a cardboard box 2, 4, 6 or 8 packages; 10 or 14 pcs., in a cardboard box 1-4 packs; 15 pcs., in a cardboard box 2 packs; 56 pcs. in a can, in a cardboard box 1 can. Each pack also contains instructions for the use of Pregabalin Canon).

Composition of 1 capsule:

active substance: pregabalin - 25, 50, 75, 100, 150, 200 or 300 mg;
auxiliary components: mannitol, pregelatinized corn starch, magnesium stearate, talc;
capsule body and cap: gelatin, titanium dioxide.

In addition, the capsule shell contains:

dosage 25 mg: indigotine dye;
dosage of 50 and 300 mg: quinoline yellow dye, sunset yellow dye;
dosage 75 mg: iron dye yellow oxide;
dosage 100 mg: proprietary blue V dye;
dosage 150 mg: cap - quinoline yellow dye, sunset yellow dye.

Pharmacological properties

Pharmacodynamics

Pregabalin Canon is an antiepileptic drug with anticonvulsant activity. Its active ingredient, pregabalin, is an analogue of GABA (gamma-aminobutyric acid). The mechanism of action of the drug is due to the ability of pregabalin to bind to alpha ₂ -delta-protein, which is an additional subunit of voltage-gated calcium channels (calcium channels N, P or O type) in the central nervous system, which leads to irreversible substitution of [3H] -gabapentin. Presumably, this binding can contribute to the manifestation of the anticonvulsant and analgesic effects of Pregabalin Canon.

Pharmacokinetics

When taken orally before meals, pregabalin is rapidly absorbed from the gastrointestinal tract (GIT). Its maximum concentration (C _max) in blood plasma is achieved after 1 hour both with a single dose and with regular use of Pregabalin Canon. The bioavailability of pregabalin is at least 90% and does not depend on the dose taken. With repeated administration, equilibrium concentrations of pregabalin are reached within 24-48 hours. Simultaneous food intake reduces the rate of absorption, increasing the time to reach the maximum plasma concentration by about 2.5 times and reducing _Cmax by 25-30%. It should be noted that food intake does not have a clinically significant effect on the total absorption of pregabalin.

Pregabalin does not bind to plasma proteins.

The apparent volume of distribution is approximately 0.56 L / kg.

It overcomes the blood-brain and hematoplacental barriers, excreted in breast milk.

Pregabalin is almost not metabolized. 0.9% of the dose taken is metabolized to form an N-methylated compound, which is the main metabolite, which is excreted by the kidneys. No signs of racemization of the S-enantiomer of pregabalin into the R-enantiomer were noted.

It is excreted mainly unchanged through the kidneys. The half-life averages 6.3 hours. Plasma and renal clearance of pregabalin are directly proportional to creatinine clearance.

In the range of therapeutic doses, the pharmacokinetics of pregabalin is linear; with repeated use of the drug, it does not change. Therefore, there is no need for regular monitoring of the pregabalin concentration level.

The gender of the patient has no clinically significant effect on the concentration of pregabalin in plasma.

In case of impaired renal function, a dose reduction is required. During hemodialysis, pregabalin is intensively removed from the plasma; after a hemodialysis session lasting 4 hours, its concentration in plasma decreases by approximately 50%. Therefore, after hemodialysis, it is necessary to take an additional dose of Pregabalin Canon.

With impaired liver function, the pharmacokinetics of pregabalin does not change significantly.

In patients over the age of 65 with impaired renal function, a dose reduction of Pregabalin Canon may be required.

The equilibrium pharmacokinetic parameters of pregabalin in patients with epilepsy on antiepileptic therapy are similar to those in patients with chronic pain syndromes or healthy volunteers.

Indications for use

epilepsy - as an adjunctive therapy in patients with partial seizures, which are accompanied or not accompanied by secondary generalization;
neuropathic pain;
generalized anxiety disorder;
fibromyalgia.

Contraindications

Absolute:

breast-feeding;
age up to 18 years;
individual intolerance to the components of the drug.

Pregabalin Canon should be prescribed with caution in case of impaired renal function, heart failure, diabetes mellitus, a history of encephalopathy, concomitant therapy with lorazepam, oxycodone, ethanol-containing oral agents, a history of drug dependence, patients over the age of 65 years.

During pregnancy, the use of the drug is possible only in cases where the benefits of therapy for the mother are much higher than the possible risk to the fetus.

Pregabalin Canon, instructions for use: method and dosage

Capsules Pregabalin Canon are taken orally, regardless of food intake, swallowing whole (the integrity of the shell must not be violated) and washed down with a sufficient amount of water.

The doctor determines the dose and duration of treatment taking into account the nature of the disease and the individual characteristics of the patient.

The prescribed daily dose of Canon Pregabalin should always be divided into 2–3 doses.

Recommended dosage:

neuropathic pain: starting dose 150 mg daily. With good tolerance and positive dynamics of therapy, after 3–7 days, the dose, if necessary, can be increased to 300 mg, and after another 7 days - to a maximum daily dose of 600 mg;
epilepsy: starting dose 150 mg daily. Considering the tolerance of Pregabalin Canon and the degree of effectiveness of treatment after 7 days, the initial daily dose can be increased to 300 mg, and after another 7 days - to 600 mg;
fibromyalgia: the initial dose is 150 mg per day for 3-7 days, then, taking into account the individual tolerance and the achieved effect, an increase in the dose of Canon Pregabalin to 300 mg is shown. In the absence of positive dynamics, the dose is increased to 450 mg, then, if necessary, after 7 days - up to 600 mg;
generalized anxiety disorder: 150 mg per day for 7 days, then, depending on tolerance and the effect achieved, the dose can be increased to 300 mg. In the absence of the desired effect, the dose is increased to 450 mg, after 7 days, if necessary, up to 600 mg.

You can not stop treatment with Pregabalin Canon abruptly, if necessary, the drug should be discontinued by gradually reducing the dose for at least 7 days.

In case of impaired liver function, dose adjustment of the drug is not required.

In case of impaired renal function, the dose should be prescribed taking into account the CC (creatinine clearance), which is determined by calculation using the serum creatinine indicator.

So to calculate the QC, it is necessary to multiply the patient's body weight in kilograms by the difference, in which the reduced is 140, and the subtracted is his age in years. The result is divided by 72 and multiplied by the individual serum creatinine.

For women, the result is additionally multiplied by a factor of 0.85.

Recommended daily dosage of Canon Pregabalin for the treatment of patients with impaired renal function, taking into account CC:

CC more than 60 ml / min: initial dose - 150 mg, maximum dose - 600 mg, frequency of administration - 2-3 times a day;
CC from 30 to 60 ml / min: initial dose - 75 mg, maximum dose - 300 mg, frequency of administration - 2-3 times a day;
QC from 15 to 30 ml / min: initial dose - 25-50 mg, maximum dose - 150 mg, frequency of administration - 1-2 times a day;
CC less than 15 ml / min: the initial dose is 25 mg, the maximum dose is 75 mg, the frequency of administration is 1 time per day.

The dose for patients on hemodialysis is selected individually, taking into account the CC and immediately after the end of the hemodialysis session, the patient is additionally prescribed from 25 to 100 mg of pregabalin.

For patients over the age of 65 years with CC above 60 ml / min, dosage adjustment is not required.

If you accidentally skip the next dose of Pregabalin Canon, the missed dose can be taken if the time for the next dose has not yet arrived, and this will not correspond to the simultaneous reception of two doses.

Side effects

In the course of clinical studies and post-marketing observation, the following adverse reactions from systems and organs were recorded (according to the frequency of occurrence, they are classified as follows: very often - ≥ 1/10 prescriptions; often - from ≥ 1/100 to <1/10 appointments; infrequently - from ≥ 1/1000 to <1/100 appointments; rarely - from ≥ 1/10 000 to <1/1000 appointments; very rarely - <1/10 000 appointments; frequency not established - based on available data it is impossible to establish the frequency of occurrence adverse reactions):

infections and invasions: infrequently - nasopharyngitis;
from the nervous system: very often - drowsiness, dizziness; often - headache, impaired attention, memory impairment, ataxia, impaired coordination, dysarthria, paresthesia, tremor, imbalance, lethargy, sedation; infrequently - speech impairment, cognitive disorders, loss of taste, myoclonic seizures, hypesthesia, nystagmus, weakening of reflexes, psychomotor agitation, postural dizziness, dyskinesia, hyperesthesia, burning sensation on the mucous membranes and skin, intentional tremor, fainting, stupor; rarely - dysgraphia, hypokinesia, parosmia; frequency not established - loss of consciousness, convulsions;
on the part of the psyche: often - confusion, euphoria, insomnia, irritability, disorientation, decreased libido; infrequently - anxiety, depersonalization, mood lability, anorgasmia, difficulty in finding words, agitation, depressed mood, unusual dreams, hallucinations, panic attacks, apathy, depression, increased libido; rarely - high spirits, disinhibition; frequency not established - aggression;
from the lymphatic system and blood: infrequently - thrombocytopenia; rarely - leukopenia, neutropenia;
from the side of the heart: infrequently - atrioventricular block of the 1st degree, tachycardia; rarely - sinus arrhythmia, sinus tachycardia, sinus bradycardia; frequency not established - prolongation of the QT interval, chronic heart failure;
from the side of the vessels: infrequently - hot flashes, flushing of the skin, lowering blood pressure (BP), increased blood pressure; rarely - coldness of the extremities;
on the part of the organ of hearing and labyrinthine disorders: often - vertigo; infrequently - hyperacusis;
on the part of the organ of vision: often - diplopia, blurred vision; infrequently - dry eyes, decreased visual acuity, increased lacrimation, narrowing of the visual fields, asthenopia, eye pain, eye puffiness; rarely - eye irritation, flickering sparks in front of the eyes, mydriasis, oscillopsia or a sensation of vibrations of the objects in question, loss of peripheral vision, impaired perception of visual depth, increased brightness of visual perception, strabismus; frequency not established - keratitis, loss of vision;
on the part of metabolism and nutrition: often - increased appetite, increased body weight; infrequently - hypoglycemia, anorexia; rarely - a decrease in body weight;
from the digestive system: often - dry mouth, flatulence, constipation, vomiting; infrequently - increased salivation, hypesthesia of the oral mucosa, gastroesophageal reflux, bloating; rarely - nausea, diarrhea, ascites, dysphagia, tongue edema, pancreatitis;
on the part of the musculoskeletal system and connective tissue: infrequently - muscle twitching, muscle stiffness, back pain, muscle spasms, pain in the limbs, joint swelling, myalgia, arthralgia; rarely - neck pain, neck muscle spasm, rhabdomyolysis;
on the part of the respiratory system, chest and mediastinal organs: infrequently - dryness of the nasal mucosa, shortness of breath; rarely - snoring, nasal congestion, cough, rhinitis, feeling of tightness in the throat, nosebleeds; frequency not established - pulmonary edema;
from the urinary system: infrequently - urinary incontinence, dysuria; rarely - renal failure, oliguria; frequency not established - urinary retention;
on the part of the reproductive function: often - erectile dysfunction; infrequently - sexual dysfunction, delayed ejaculation; rarely - pain in the mammary glands, an increase in the volume of the mammary glands, discharge from the mammary glands, amenorrhea, dysmenorrhea; frequency not established - gynecomastia;
from the immune system: the frequency has not been established - allergic reactions, angioedema, hypersensitivity reactions;
dermatological reactions: infrequently - papular rash, sweating; rarely - urticaria, cold sweat; frequency not established - itching, facial edema, Stevens-Johnson syndrome;
laboratory and instrumental parameters: infrequently - increased activity of alanine aminotransferase, aspartate aminotransferase, creatine phosphokinase; rarely - an increase in the concentration of glucose and creatinine in the blood plasma, a decrease in the level of potassium in the blood;
others: often - gait disturbance, fatigue, drunkenness, edema (including peripheral edema); infrequently - thirst, asthenia, chest tightness, falls, pain, chills, pathological sensations; rarely - hyperthermia, generalized edema.

Overdose

Symptoms: drowsiness, agitation and anxiety, confusion, affective disorders, depression.

Treatment: immediate gastric lavage, intake of activated carbon, the appointment of supportive therapy. Hemodialysis is used if necessary.

special instructions

Dizziness and drowsiness occur most often with the use of the drug. Adverse events are usually mild to moderate. Depending on the subjective tolerance of Pregabalin Canon, the side effects requiring discontinuation of treatment include: severe dizziness or drowsiness, confusion, ataxia, asthenia, blurred vision, impaired attention and / or coordination, peripheral edema.

Reception of Pregabalin Canon causes in some cases drug dependence, which, when canceled after long or short-term therapy, can manifest itself with the following undesirable phenomena: headache, sweating, dizziness, nausea, insomnia, diarrhea, flu-like syndrome, depression, convulsions and anxiety. The dependence of the frequency and severity of the manifestations of pregabalin withdrawal syndrome on the duration of treatment or dose has not been established.

It should be borne in mind that with an increase in body weight in patients with diabetes mellitus during therapy with the drug, it may be necessary to consider the issue of adjusting the doses of hypoglycemic agents.

Due to the fact that treatment may be accompanied by drowsiness and dizziness, confusion or loss of consciousness, impaired cognitive functions, which increase the risk of falls and accidental injury, it is recommended to exercise caution until the patient evaluates the possible individual effects of Pregabalin Canon.

There is insufficient information on the possibility of discontinuing other anticonvulsants when seizures are suppressed with pregabalin and the advisability of monotherapy with this drug.

When prescribing Pregabalin Canon for the treatment of central neuropathic pain caused by a lesion of the spinal cord, one should take into account the existing risk of an increased incidence of adverse events from the central nervous system, including those caused by the summation of the effects of simultaneously taken drugs and pregabalin.

Violations of the organ of vision in most cases are transient, they go away on their own.

Renal failure arising during therapy with pregabalin is reversible; after discontinuation of the drug, renal function is restored.

It should be borne in mind that when using Canon Pregabalin in elderly patients suffering from cardiac dysfunction and receiving the drug for neuropathy, the risk of developing chronic heart failure increases.

If it is necessary to combine therapy with opioid analgesics, it is recommended to simultaneously carry out preventive measures to prevent constipation and intestinal obstruction, especially in elderly patients.

With the development of symptoms of angioedema (edema of the face, perioral edema or edema of the tissues of the upper respiratory tract), the administration of Pregabalin Canon should be immediately discontinued.

When prescribing the drug, the doctor should inform the patient about the possible development of addiction during treatment with pregabalin. Close medical supervision of patients with a history of drug dependence is required.

During therapy with Pregabalin Canon, the risk of suicidal thoughts or behavior increases. In this regard, patients need close monitoring by loved ones for the appearance and worsening of depression, including suicidal thoughts or behavior.

Influence on the ability to drive vehicles and complex mechanisms

When treating with Pregabalin Canon, patients are advised to refrain from performing potentially hazardous activities, including driving vehicles and mechanisms that require an increased concentration of attention and a high speed of psychomotor reactions, for a period until the individual effect of the drug on the development of side effects from the nervous system becomes clear and the organ of vision.

Application during pregnancy and lactation

The efficacy and safety of using pregabalin during pregnancy have not been reliably established. Therefore, prescribing Pregabalin Canon during gestation is recommended only in cases where the expected therapeutic effect for the mother is much higher than the possible risk to the fetus.

Women of reproductive age during the period of drug treatment must use reliable methods of contraception.

The use of Canon Pregabalin during breastfeeding is contraindicated. If pregabalin is prescribed during lactation, breastfeeding should be suspended.

Pediatric use

The use of Canon Pregabalin for the treatment of patients under the age of 18 is contraindicated.

With impaired renal function

Pregabalin Canon should be prescribed with caution in case of impaired renal function.

When determining the dose, it is necessary to take into account the patient's QC.

For violations of liver function

In case of impaired liver function, dose adjustment of Pregabalin Canon is not required.

Use in the elderly

Pregabalin Canon should be prescribed with caution to patients over the age of 65 years.

Drug interactions

Given the pharmacokinetic properties of pregabalin, clinically significant drug interactions with other drugs are unlikely.

Nevertheless, due to the individual characteristics of the body, there are reports that when pregabalin is combined with drugs that depress the central nervous system, respiratory failure and coma may occur.

Pregabalin Canon, when used concomitantly with opioid analgesics and other constipation-causing agents, can adversely affect the gastrointestinal tract, contributing to the development of constipation, intestinal obstruction, or paralytic ileus.

It is possible to enhance the effects of ethanol and lorazepam, aggravate the impairment of cognitive and motor functions caused by oxycodone. With repeated combination of pregabalin with lorazepam, oxycodone or ethanol, there is no clinically significant effect on respiration.

The simultaneous use of oral contraceptives containing norethisterone and / or ethinyl estradiol does not cause changes in the equilibrium pharmacokinetics of pregabalin and the contraceptive.

Diuretics, oral hypoglycemic agents, insulin, tiagabine, topiramate, phenobarbital do not have a clinically significant effect on pregabalin clearance.

Signs of a clinically significant interaction were not found when pregabalin was taken together with phenytoin, lamotrigine, carbamazepine, valproic acid, gabapentin, lorazepam, oxycodone and ethanol.

Analogs

Analogues of Pregabalin Canon are: Pregabalin, Pregabalin Zentiva, Pregabio, Replica, Algerica, Lyrica, Prabegin, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C, protected from moisture and light.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Pregabalin Canon

The few reviews about Pregabalin Canon are mostly positive. Patients indicate the effectiveness of the drug when used according to indications. The absence of perceptible undesirable effects during therapy with minimal doses of the drug is noted.

The disadvantages of Pregabalin Canon include the risk of developing drug dependence.

Price for Pregabalin Canon in pharmacies

The price of Pregabalin Canon can be: for a package containing 14 capsules, a dosage of 25 mg - from 79 rubles, a dosage of 50 mg - from 145 rubles, a dosage of 75 mg - from 348 rubles, a dosage of 150 mg - from 440 rubles., dosage 200 mg - from 465 rubles, dosage 300 mg - from 734 rubles; for a package containing 56 capsules - dosage 25 mg - from 300 rubles, dosage 50 mg - from 550 rubles, dosage 200 mg - from 1,767 rubles, dosage 300 mg - from 2,620 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!