Zonik (pregabalin) hard capsules 75 mg. №28

$24.00

Neuropathic pain. Zonic is indicated for the treatment of neuropathic pain of peripheral or central origin in adults. Epilepsy. Generalized anxiety disorder.

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Description

Composition and form of release
active substance: pregabalin

1 capsule contains 150 mg of pregabalin;

excipients: corn starch, magnesium stearate, hard gelatin capsule (gelatin, purified water, titanium dioxide (E 171)).

Release form
Hard capsules (14 capsules in a blister. 1 or 2 or 4 or 6 blisters in a carton box).

Basic physical and chemical properties
Size 2 hard gelatin capsules with a white body and an opaque white lid containing a white to off-white powder.

Pharmachologic effect
The active ingredient of Zonic is pregabalin, which is an analogue of gamma-aminobutyric acid [(S) -3- (aminomethyl) -5-methylhexanoic acid].

Mechanism of action.

Pregabalin binds to an additional subunit (a 2 -d protein) of voltage-gated calcium channels in the central nervous system (CNS).

Clinical efficacy and safety.

Neuropathic pain.
Pregabalin is effective in patients with diabetic neuropathy, postherpetic neuralgia, and spinal cord injury. The effectiveness of the drug in other types of neuropathic pain did not go away.

It was found that the safety and efficacy profiles of pregabalin treatment for a duration of up to 13 weeks with a dosing regimen twice a day and a duration of up to 8 weeks with a dosing regimen three times a day are similar.

When pregabalin was used to treat neuropathic pain for up to 12 weeks, pain relief of peripheral and central origin was observed after the first week and persisted throughout the treatment period.

Epilepsy.
Complementary treatment. The safety and efficacy profiles of pregabalin were similar when taken for 12 weeks with a twice or thrice daily dosing regimen. A decrease in the frequency of seizures was observed already in the first week.

Children. The efficacy and safety of pregabalin as an adjuvant for epilepsy in children under 12 years of age and in adolescents has not been established. The adverse reactions that were observed in patients aged 3 months to 16 years were similar to those in adults. It has been established that pyrexia and upper respiratory tract infections in children aged 3 months to 16 years are observed more often than in adults.

Monotherapy (in patients with newly diagnosed disease). Pregabalin and lamotrigine were equally safe and well tolerated.

Generalized anxiety disorder.
A reduction in the symptoms of generalized anxiety disorder according to the Hamilton Anxiety Scale (HAM-A) was observed as early as the first week of pregabalin use.

Fibromyalgia.
The efficacy (pain reduction according to the visual analogue scale) of pregabalin in patients diagnosed with fibromyalgia was established.

Children. The efficacy of pregabalin in children 12-17 years old with fibromyalgia, who used pregabalin at a dose of 75-450 mg per day, was established. The most common adverse reactions were dizziness, nausea, headache, weight gain, and fatigue. The overall safety profile in adolescents was similar to that of adults with fibromyalgia.

Pharmacokinetics
Equilibrium pharmacokinetic parameters of pregabalin were similar in healthy volunteers, patients with epilepsy who took antiepileptic drugs, and patients with chronic pain.

Absorption.

Pregabalin is rapidly absorbed when taken on an empty stomach and reaches its maximum plasma concentration within 1:00 after a single or multiple use. The calculated oral bioavailability of pregabalin is ≥ 90% and does not depend on the dose. With repeated use, the equilibrium state is reached after 24-48 hours. The rate of absorption of pregabalin decreases when taken simultaneously with food, leading to a decrease in the maximum concentration (C max) by about 25-30% and an increase in tmax values ​​up to about 2.5 hours. However, dietary intake of pregabalin did not have a clinically significant effect on absorption.

Distribution.

Pregabalin crosses the blood-brain barrier in mice, rats and monkeys. It was found that pregabalin crosses the placenta in rats and enters the milk of rats during lactation. In humans, the volume of distribution of pregabalin after oral administration is approximately 0.56 L / kg. Pregabalin does not bind to blood plasma proteins.

Metabolism.

In humans, pregabalin undergoes minor metabolism. After the administration of a dose of radiolabeled pregabalin, about 98% of the radioactive substance was excreted in the urine as unchanged pregabalin. The proportion of N-methylated derivative of pregabalin, the main metabolite of the drug was determined in urine, was 0.9% of the administered dose. During preclinical studies, there was no racemization of the S-enantiomer of pregabalin to the R-enantiomer.

Pregabalin is excreted from the systemic circulation unchanged, mainly by the kidneys. The half-life of pregabalin is 6.3 hours. Plasma and renal clearance of pregabalin are directly proportional to creatinine clearance.

Indications for use
Neuropathic pain.

Zonic is indicated for the treatment of neuropathic pain of peripheral or central origin in adults.

Epilepsy.

Zonik is indicated for adults as an adjunctive treatment for partial seizures with or without secondary generalization.

Generalized anxiety disorder.

Zonic is indicated for the treatment of generalized anxiety disorder in adults.

Fibromyalgia.

Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in the “Composition” section.

Method of administration and dosage
Take the drug Zonik regardless of food intake.

This medicinal product is intended for oral use only.

The dose range of the drug can vary from 150 to 600 mg per day. The daily dose is divided into 2 or 3 doses.

In the case of a single dose of less than 150 mg, apply in the appropriate dosage.

Neuropathic pain.

Pregabalin therapy can be started with a dose of 150 mg per day, divided into 2 or 3 doses. Depending on the individual response and the tolerability of the drug, the dose can be increased to 300 mg per day after 3-7 days, and, if necessary, up to a maximum dose of 600 mg per day after 7 days.

In the case of a single dose of less than 150 mg, apply in the appropriate dosage.

Epilepsy.

Pregabalin therapy can be started with a dose of 150 mg per day, divided into 2 or 3 doses. Depending on the individual response and the patient’s tolerability of the drug, the dose can be increased to 300 mg per day after the first week of treatment. After one week, the dose can be increased to a maximum of 600 mg per day.

In the case of a single dose of less than 150 mg, apply in the appropriate dosage.

Generalized anxiety disorder.

The dose, which is divided into 2 or 3 doses, can vary in the range of 150-600 mg per day. The need for continued therapy should be reviewed periodically.

Pregabalin therapy can be started with a dose of 150 mg per day. Depending on the individual response and the patient’s tolerability of the drug, the dose can be increased to 300 mg per day after the first week of treatment. After another week of administration, the dose can be increased to 450 mg per day. After one week, the dose can be increased to a maximum of 600 mg per day.

In the case of a single dose of less than 150 mg, apply in the appropriate dosage.

Fibromyalgia.

The recommended dose for the treatment of fibromyalgia is 300 to 450 mg per day. Treatment should be started with a dose of 75 mg twice daily (150 mg daily). Depending on efficacy and tolerability, the dose can be increased to 150 mg twice a day (300 mg per day) for one week. For patients for whom the use of a dose of 300 mg per day is not effective enough, you can increase the dose to 225 mg twice a day (450 mg per day) *. Although there are studies on the 600 mg daily dose, there is no evidence that this dose would have an additional benefit; also such a dose should be worse tolerated. Taking into account the dose-dependent adverse reactions, the use of doses of 450 mg per day is not recommended. Since pregabalin is excreted by the kidneys, the dose should be adjusted in patients with impaired renal function.

In the case of a single dose of less than 150 mg, apply in the appropriate dosage.

Cancellation of pregabalin.

According to current clinical practice, it is recommended to discontinue pregabalin therapy gradually, over at least one week, regardless of the indication.

Overdose
The most common adverse reactions in pregabalin overdose have been reported to be drowsiness, confusion, agitation, and anxiety. There have also been reports of seizures.

Cases of coma have been rarely reported.

Treatment of pregabalin overdose consists of general supportive measures and, if necessary, may include hemodialysis.

Side effects
The most common adverse reactions leading to discontinuation of pregabalin use were dizziness and drowsiness.

These side reactions can also be associated with the course of the underlying disease and (or) the concomitant use of other drugs.

During the treatment of neuropathic pain of central origin caused by a lesion of the spinal cord, the incidence of adverse reactions in general, the incidence of adverse reactions from the central nervous system, and especially drowsiness increased.

Infections and invasions: nasopharyngitis.

On the part of the blood and lymphatic system: neutropenia.

From the immune system: hypersensitivity, angioedema, allergic reactions, anaphylactoid reactions.

From the side of metabolism, metabolism: increased appetite, loss of appetite, hypoglycemia.

From the side of the psyche: euphoria, confusion, irritability, disorientation, insomnia, decreased libido, hallucinations, panic attacks, anxiety, agitation, depression, depressed mood, high spirits, aggression, mood changes, depersonalization, difficulty finding words, pathological dreams, amplification libido, anorgasmia, apathy, disinhibition.

From the nervous system: dizziness, drowsiness, headache, ataxia, impaired coordination, tremor, dysarthria, amnesia, memory impairment, impaired attention, paresthesia, hypesthesia, sedation, imbalance, lethargy, fainting, stupor, myoclonus, loss of consciousness, psychomotor hyperactivity, dyskinesia, postural dizziness, intentional tremor, nystagmus, impaired cognitive functions, mental disorders, speech disorders, hyporeflexia, hyperesthesia, burning sensation, ageusia, general malaise, apathy, navkolortova paresthesia, myoclonus, convulsion , hypalgesia, addiction, cerebellar syndrome, cogwheel syndrome, coma, delirium, encephalopathy, extrapyramidal symptoms, Guillain-Barré syndrome, intracranial hypertension, manic reactions, paranoid reactions, sleep disorders.

From the side of the organs of vision: blurred vision, diplopia, conjunctivitis, loss of peripheral vision, blurred vision, eye edema, visual field defects, decreased visual acuity, eye pain, asthenopia, photopsia, dry eyes, increased lacrimation, eye irritation, blepharitis, accommodation disorders, hemorrhage in the eye, photophobia, retinal edema, loss of vision, keratitis, osclopsia, changes in visual depth perception, mydriasis, strabismus, vision brightness, anisocoria, corneal ulcers, exophthalmos, paralysis of the eye muscle, iritis, keratocon “junctivitis, night blindness, ophthalmoplegia, optic atrophy, edema of the optic nerve head, ptosis, uveitis.

On the part of the hearing and balance organs: vertigo, hyperacusis.

From the heart: tachycardia, first-degree block, sinus bradycardia, congestive heart failure, prolongation of the QT interval, sinus tachycardia, sinus arrhythmia,

From the side of the vessels: arterial hypotension, arterial hypertension, hot flashes, hyperemia, feeling of coldness in the extremities.

From the respiratory system, chest and mediastinum: pharyngolaryngeal pain, shortness of breath, epistaxis, cough, rhinitis, snoring, dry nasal mucosa, pulmonary edema, constriction in the throat, laryngospasm, apnea, atelectasis, bronchiolitis, hiccups, pulmonary fibrosis, yawning …

From the gastrointestinal tract: nausea, vomiting, constipation, diarrhea, flatulence, bloating, dry mouth, gastroenteritis, gastroesophageal reflux disease, salivary hypersecretion, oral hypoesthesia, cholecystitis, cholelithiasis, bleeding, gastrointestinal, gastrointestinal tongue edema, rectal bleeding, ascites, pancreatitis, tongue edema, dysphagia, stomatitis, esophageal ulcer, periodontal abscess.

Skin and subcutaneous tissue disorders: pressure sores, papular rash, urticaria, hyperhidrosis, pruritus, alopecia, dry skin, eczema, hirsutism, skin ulcers, vesicle-bullous rash, Stevens-Johnson syndrome, cold sweat, exfoliative dermatitis, lichenoidal dermatitis , nail disorders, petechial rash, purpura, pustular rash, skin atrophy, skin necrosis, cutaneous and subcutaneous nodules.

On the part of the musculoskeletal system and connective tissue: muscle cramps, arthralgia, back pain, pain in the extremities, neck muscle spasms, joint swelling, myalgia, muscle twitching, neck pain, muscle stiffness, rhabdomyolysis.

From the kidneys and urinary tract: urinary incontinence, dysuria, albuminuria, hematuria, kidney stones, nephritis, renal failure, oliguria, urinary retention, acute