Dilaxa - Instructions For The Use Of Capsules, Price, Reviews, Analogues

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

Dilax

Dilaxa: instructions for use and reviews

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

Latin name: Dilaxa

ATX code: M01AH01

Active ingredient: Celecoxib (Celecoxib)

Manufacturer: KRKA-RUS LLC (Russia)

Description and photo update: 18.10.2018

Prices in pharmacies: from 164 rubles.

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Dilaxa is an NSAID (non-steroidal anti-inflammatory drug) with anti-inflammatory, analgesic and antipyretic activity.

Release form and composition

Dilaxa dosage form - capsules filled with granular powder from white to almost white color:

• 100 mg: size No. 3, hard gelatinous, body and lid - white;
• 200 mg: size No. 1, hard gelatinous, body and lid - brownish yellow.

10 pcs. in blisters (blister packs), in a cardboard box 1–6, 9 or 10 blisters (packs).

Composition for 1 capsule:

• active substance: celecoxib - 100 mg or 200 mg;
• auxiliary ingredients: magnesium stearate, croscarmellose sodium;
• body and lid: gelatin capsule 100 mg: titanium dioxide - 2%, gelatin - up to 100%; 200 mg gelatin capsule: titanium dioxide - 1%, dye iron oxide yellow - 1%, gelatin - up to 100%.

Pharmacological properties

Pharmacodynamics

The anti-inflammatory, analgesic and antipyretic effect of celecoxib is due to its blocking of the formation of inflammatory prostaglandins (Pg), mainly due to inhibition of cyclooxygenase-2 (COX-2). In response to inflammation, the induction of COX-2 occurs, leading to the synthesis and accumulation of Pg (primarily PgE ₂), causing an increase in the symptoms of inflammation (edema and pain).

Celecoxib, taken in therapeutic doses, does not significantly inhibit cyclooxygenase-1 (COX-1) and does not affect the concentration of Pg synthesized as a result of COX-1 activation, and the natural physiological processes associated with it in tissues (primarily in the intestine, stomach and platelets).

Pharmacodynamic action of celecoxib in some cases:

• chronic renal failure (CRF), old age: celecoxib does not cause a decrease in the glomerular filtration rate, but transiently reduces the excretion of sodium from the body;
• Renal function: celecoxib decreases renal excretion of prostaglandin PgE ₂ and metabolite of prostacyclin 6-keto-PgFl, it does not affect the products of COX-1 - serum concentration of thromboxane B ₂ (TxB ₂) and renal excretion of the metabolite thromboxane 11-Dehydro-TxB ₂;
• arthritis: the incidence of arterial hypertension, peripheral edema, heart failure was comparable to that of non-selective COX inhibitors with inhibitory activity against COX-1 and COX-2. This effect was most pronounced in patients receiving diuretic therapy, but they did not have an increase in the incidence of increased blood pressure (BP) and the development of heart failure, and peripheral edema of mild severity resolved on its own.

Pharmacokinetics

• absorption: celecoxib is well absorbed when taken on an empty stomach, its maximum concentration (C _max) in blood plasma reaches 2–3 hours and is 705 ng / ml after taking 200 mg; the absolute bioavailability of the substance has not been studied; the values of C _max and the area under the concentration-time curve (AUC) are practically proportional to the amount of celecoxib taken in the range of therapeutic doses (2 times a day at a dose of up to 200 mg), but with an increase in its doses, this correlation is violated;
• distribution: about 97% of celecoxib binds to plasma proteins, regardless of its concentration in plasma; celecoxib does not bind to erythrocytes, it penetrates through the blood-brain barrier;
• metabolism: celecoxib is metabolized mainly by the cytochrome P450 (CYP) CYP2C9 isoenzyme by hydroxylation, partial glucuronidation and oxidation in the liver, with the formation of pharmacologically inactive metabolites with respect to COX-1 and COX-2; in patients with genetic polymorphism (for example, polymorphism homozygous for the CYP2C9 * 3 isoenzyme), the activity of the CYP2C9 isoenzyme is reduced, which reduces the effectiveness of the enzymes;
• excretion: celecoxib is excreted in the form of metabolites through the gastrointestinal tract (GIT) - 57% and with urine - 27%, less than 1% of the dose taken is excreted unchanged; for repeated use, the half-life (T _1/2) is from 8 to 12 hours, and the clearance is ~ 500 ml / min, equilibrium plasma concentrations are reached by the 5th day of administration. The main pharmacokinetic parameters (C _max, AUC, T _1/2) vary within 30%; at steady state in healthy young patients, the average volume of distribution is approximately 500 L / 70 kg, which is evidence of a wide distribution of celecoxib in tissues;
• food intake: simultaneous intake of celecoxib with fatty foods increases absorption by ~ 20% and the time to reach C _max ~ by 4 hours.

Indications for use

• osteoarthritis, rheumatoid arthritis, ankylosing spondylitis - for symptomatic therapy;
• pain syndrome (musculoskeletal, postoperative, back pain and other types of pain) - for relief;
• primary dysmenorrhea - for therapy.

Contraindications

Absolute:

• condition after CABG (coronary artery bypass grafting) of the vessels;
• erosive and ulcerative lesions of the gastric mucosa or duodenal ulcer in the active phase, gastrointestinal bleeding, gastric ulcer and duodenal ulcer in the acute phase;
• intestinal inflammation (ulcerative colitis, Crohn's disease) in the acute stage;
• heart failure II – IV functional class according to NYHA classification;
• clinically confirmed coronary artery disease (ischemic heart disease), peripheral arterial disease, severe cerebrovascular pathology;
• subarachnoid hemorrhage;
• hemorrhagic stroke;
• period of pregnancy and lactation;
• severe liver failure;
• severe renal failure, confirmed hyperkalemia, progressive kidney disease;
• age <18 years;
• aspirin triad (including history data);
• lactase deficiency, glucose-galactose malabsorption syndrome, lactose intolerance;
• hypersensitivity to celecoxib, other sulfonamide derivatives and any components of Dilaxa.

The drug is recommended to be taken with caution in case of diseases of the gastrointestinal tract (stomach or duodenal ulcer, Crohn's disease, history of bleeding, ulcerative colitis), known slow metabolism or suspicion of such a condition, fluid retention and edema, moderate liver dysfunction severity, a history of liver disease, hepatic porphyria, impaired renal function with creatinine clearance (CC) = 30-60 ml / min, a significant decrease in circulating blood volume (including conditions after surgery), the presence of Helicobacter pylori infection, diseases of the cardiovascular system (including coronary heart disease, arterial hypertension), cerebrovascular pathologies, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, long-term use of NSAIDs,severe somatic diseases, in old age (including patients with low body weight, weakened, receiving diuretics), with tuberculosis, alcoholism, smoking, as well as simultaneously with anticoagulants (warfarin), antiplatelet agents (clopidogrel, acetylsalicylic acid), glucocorticosteroids (GCS) for oral administration (prednisolone), selective serotonin reuptake inhibitors (fluoxetine, paroxetine, citalopram, sertraline), diuretics, digoxin, inhibitors of the isoenzyme CYP2C9.selective serotonin reuptake inhibitors (fluoxetine, paroxetine, citalopram, sertraline), diuretics, digoxin, inhibitors of the CYP2C9 isoenzyme.selective serotonin reuptake inhibitors (fluoxetine, paroxetine, citalopram, sertraline), diuretics, digoxin, inhibitors of the CYP2C9 isoenzyme.

Instructions for use of Dilaxa: method and dosage

Dilax capsules are taken orally, regardless of food intake, without chewing and drinking water or other neutral liquid.

Due to the fact that the chance of cardiovascular complications directly depends on the dose and duration of taking Dilaxa, patients should take the lowest effective dose for the shortest possible course. For a long course, the recommended maximum daily dose is 400 mg.

Dilaxa dosage regimen depending on the disease:

• osteoarthritis (symptomatic therapy): 200 mg per day for 1-2 doses;
• rheumatoid arthritis (symptomatic therapy): 100-200 mg per day for 2 doses;
• ankylosing spondylitis (symptomatic therapy): 200 mg per day for 1-2 doses; for some patients, the use of 400 mg per day in 2 doses is effective;
• pain syndrome and primary dysmenorrhea (therapy): the initial dose is 400 mg, if necessary, an additional dose of 200 mg can be taken on the first day; on the following days - 200 mg 2 times a day (if necessary).

Side effects

The incidence of side effects from systems and organs according to the scale of the World Health Organization (> 0.1 - very often; 0.01-0.1 - often; 0.001-0.01 - infrequently; 0.0001-0.001 - rarely; < 0.0001 - extremely rare):

• cardiovascular system: often - increased blood pressure (blood pressure), including aggravation of arterial hypertension, peripheral edema; infrequently - a feeling of palpitations, hot flashes; rarely - arrhythmia, CHF (chronic heart failure), tachycardia, myocardial infarction, ischemic stroke;
• digestive system: often - abdominal pain, dyspepsia, flatulence, diarrhea, vomiting; infrequently - dental diseases (including post-extraction alveolar alveolitis); rarely - peptic ulcer of the stomach and duodenal ulcer, ulceration of the esophagus; extremely rare - perforation of the small / large intestine, pancreatitis;
• nervous system: often - insomnia, dizziness; infrequently - increased muscle tone, anxiety, increased secretion of nasal mucus; rarely - psychosis, confusion;
• urinary system: often - urinary tract infection;
• respiratory system: often - cough, bronchitis, sinusitis, upper respiratory tract infections; infrequently - runny nose, inflammation of the mucous membrane and lymph of the pharynx;
• skin: often - rash, itching of the skin (including generalized); infrequently - ecchymosis, urticaria; rarely - alopecia;
• hematopoietic organs: infrequently - anemia; rarely, thrombocytopenia;
• sense organs: infrequently - blurred vision, tinnitus;
• laboratory data: infrequently - increased activity of liver enzymes (including ALT (alanine aminotransferase) and AST (aspartate aminotransferase);
• hypersensitivity reactions: rarely - angioedema; very rarely - a bullous rash (bullous dermatosis);
• other reactions: infrequently - exacerbation of allergic diseases (hypersensitivity), accidental injuries, flu-like syndrome, facial edema.

Based on the results of post-marketing research:

• nervous system: rarely - hallucinations; extremely rare - aseptic meningitis, cerebral hemorrhage, ageusia, anosmia;
• sense organs: infrequently - conjunctivitis;
• cardiovascular system: rarely - PE (pulmonary embolism); extremely rare - vasculitis;
• digestive system: rarely - hepatitis, gastrointestinal bleeding; extremely rare - liver dysfunction, fulminant hepatitis, jaundice, cholestasis, liver necrosis, cholestatic hepatitis;
• skin: rarely - photosensitivity; extremely rare - Stevens-Johnson syndrome, exudative erythema multiforme, acute generalized exanthematous pustulosis, Lyell's syndrome, drug rash in combination with eosinophilia and systemic symptoms of DRESS syndrome, exfoliative dermatitis;
• urinary system: rarely - acute renal failure (acute renal failure), hyponatremia; extremely rare - nephrotic syndrome, interstitial nephritis, minimal renal dysfunction;
• reproductive system: rarely - violation of the menstrual cycle; frequency unknown - decreased fertility in women (the studies did not include women planning a pregnancy);
• hypersensitivity reactions: extremely rare - anaphylaxis;
• other reactions: infrequently - chest pain.

Overdose

Data on Dilaxa overdose are limited. A single dose of the drug in a dose of up to 1200 mg and repeated use in a dose of up to 1200 mg 2 times a day were not accompanied by clinically significant adverse reactions.

If an overdose is suspected, symptomatic therapy should be carried out. Since up to 97% of celecoxib binds to plasma proteins, dialysis is assumed to be ineffective.

special instructions

With its antipyretic effect, Dilaxa can reduce the clinical and diagnostic value of fever and complicate the recognition of infection.

Taking Dilaxa, like other drugs of the coxib group, may increase the likelihood of developing such serious complications from the cardiovascular system as myocardial infarction, stroke and blood clots, which can be fatal. The chance of developing such reactions increases with an increase in the dose of the drug and the duration of the course of treatment, as well as in patients with pathologies of the cardiovascular system or in the presence of risk factors for the development of cardiovascular diseases. To reduce the risk of these side effects, Dilax should be used in the shortest possible short course in the minimum effective doses. The patient is required to be informed about the symptoms of serious adverse reactions from the cardiovascular system and the necessary safety measures if they occur.

The use of NSAIDs (selective COX-2 inhibitors) for the treatment of pain in patients in the postoperative period in the first 10-14 days after coronary artery bypass grafting can increase the incidence of myocardial infarction and cerebrovascular accident.

Since celecoxib does not have an antiplatelet effect on platelets, it should not replace acetylsalicylic acid for the prevention of thromboembolism. In this regard, when treating with Dilaxa, it is also impossible to cancel antiplatelet therapy, for example, with acetylsalicylic acid, for patients at risk of developing thromboembolic complications.

Celecoxib, like all NSAIDs, can increase blood pressure, increasing the risk of complications from the cardiovascular system, and therefore, in patients with arterial hypertension, it should be used with caution, under blood pressure control at the beginning and during treatment.

Cases of ulceration, perforation and bleeding from the gastrointestinal tract were extremely rare on the part of the digestive system during Dilaxa therapy. The risk of developing such complications is highest in old age, in the presence of cardiovascular diseases, concomitant use of acetylsalicylic acid, and in the presence of gastrointestinal diseases such as bleeding, ulcers, exacerbation of inflammatory processes and their history. Also, risk factors for the development of gastrointestinal bleeding are simultaneous oral administration of GCS, the use of anticoagulants, prolonged treatment with NSAIDs, smoking, alcohol consumption. In most cases of registration of spontaneous episodes of serious side effects with a fatal outcome, debilitated and elderly patients were reported.

With the simultaneous use of celecoxib with warfarin and other anticoagulants, serious (up to fatal) bleeding was recorded. Given the lengthening of the prothrombin time, after starting treatment with Dilax or changing its dose, it is necessary to monitor blood coagulation indicators.

In patients who are slow metabolizers, or if such a condition is suspected, Dilax should be used with caution, since this can lead to the accumulation of high concentrations of celecoxib in the blood plasma; the initial recommended dose of Dilaxa should be halved.

Like other inhibitors of Pg synthesis, in some cases, celecoxib can cause fluid retention and edema, so patients with conditions predisposing or worsening due to fluid retention should be careful when using the drug. Patients with hypertension or a history of heart failure should be closely monitored.

When taking Dilaxa, cases of anaphylactic reactions have been recorded.

Due to the presence of lactose in the capsules, Dilax is contraindicated in patients with lactose intolerance, glucose-galactose malabsorption syndrome or lactase deficiency.

Careful monitoring of renal function is required in patients with heart failure, impaired renal / hepatic function, taking diuretics and ACE inhibitors / angiotensin II receptor blockers, as well as in the elderly. Caution is necessary in patients with dehydration; it is advisable to rehydrate before starting therapy.

Very rarely, due to celecoxib therapy, such serious skin reactions as Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis were noted. Some of these have been reported to be fatal. The risk of developing these reactions is higher at the beginning of treatment, mainly during the first month of using Dilaxa. In case of changes in the mucous membranes, skin rash, and other signs of hypersensitivity, the course must be interrupted.

In the treatment of glucocorticosteroid insufficiency, GCS therapy should not be replaced with Dilax.

Influence on the ability to drive vehicles and complex mechanisms

According to the instructions, Dilaxa can cause dizziness and other side effects that can affect the speed of psychomotor reactions and concentration. For this reason, care must be taken when driving and engaging in other potentially hazardous work.

Application during pregnancy and lactation

The experience of using celecoxib in pregnant women is insufficient, and although the potential risk of using Dilaxa during pregnancy has not been established, it cannot be ruled out either.

NSAIDs, including Dilax, due to inhibition of Pg synthesis, can cause in some women the development of changes in the ovaries that threaten complications during pregnancy. Therefore, when planning conception or during a survey on infertility, it is necessary to consider the possibility of canceling NSAIDs, including celecoxib.

Drugs of the Pg synthesis inhibitor group (including celecoxib) when taken during pregnancy, especially in the third trimester, can cause weakness in labor and premature closure of the ductus arteriosus, and their use in the early stages can negatively affect the course of pregnancy.

There are limited data on the penetration of celecoxib into breast milk. Given the threat of side effects in a child, if it is necessary to use Dilaxa for a nursing mother, it is required to assess the feasibility of continuing breastfeeding.

Pediatric use

There is no experience with the use of Dilaxa in children and adolescents under the age of 18, and therefore the use of the drug in this age group is contraindicated.

With impaired renal function

Patients with mild to moderate renal impairment do not require dose adjustment of celecoxib. In elderly patients with a glomerular filtration rate> 65 ml / min / 1.73 m ² (due to age-related changes) and in patients with a glomerular filtration rate of 35-60 ml / min / 1.73 m ^{2, the} pharmacokinetics of celecoxib is unchanged. The correlation between celecoxib clearance and CK (creatinine clearance) has not been reliably proven.

It is assumed that severe renal failure does not affect the clearance of celecoxib, since it is mainly transformed in the liver into inactive metabolites that are easily excreted from the body. But there is no experience of using Dilaxa in severe renal failure with CC <30 ml / min, progressive kidney disease and confirmed hyperkalemia.

For violations of liver function

• mild liver failure (Child-Pugh classification: class A): plasma concentration of celecoxib changes slightly - no dose adjustment is required;
• moderate hepatic impairment (Child-Pugh classification: class B): it is possible to increase the plasma concentration of celecoxib by almost 2 times - therapy should be started with the minimum recommended doses;
• severe hepatic impairment (Child-Pugh classification: class C): no experience with use.

In rare cases, severe liver dysfunctions have been observed, including fulminant hepatitis and liver necrosis, sometimes with a fatal outcome or the need for liver transplantation. Most of these reactions developed a month after starting Dilaxa.

In the case of signs of liver failure or in the detection of liver dysfunction by laboratory tests, during treatment with Dilax, patients should be carefully monitored for the development of more severe liver reactions.

Racial features of the application

For representatives of the Negroid race, the AUC of celecoxib is ~ 40% higher than in patients of the Caucasian race. The clinical significance of this fact, as well as its reasons, is unknown, therefore, treatment of patients of the Negroid race should be started with the minimum recommended dose of Dilaxa.

Use in the elderly

In old age (> 65 years), the average values of C _max and AUC of celecoxib can increase by 1.5-2 times, to a greater extent this is due to a change in the patient's body weight, and not age (as a rule, in old age there is a decrease in the average body weight in comparison with younger patients, due to which, other things being equal, their celecoxib concentrations reach higher values). Similarly, plasma concentrations of celecoxib in the blood plasma are higher in older women than in older men. Dose adjustments, as a rule, do not require such pharmacokinetic features, but if the body weight in elderly patients is <50 kg, Dilaxa treatment should be started with the minimum recommended dose.

Drug interactions

• warfarin and other anticoagulants: prolongation of prothrombin time is possible;
• fluconazole: the simultaneous use of 200 mg of fluconazole 1 time per day with celecoxib can increase the concentration of the latter in the blood plasma by 2 times; during fluconazole therapy, celecoxib should be taken in the minimum recommended dose;
• ketoconazole: no clinically significant effect on the metabolism of celecoxib;
• ACE (angiotensin-converting enzyme) inhibitors / angiotensin II receptor blockers: in the case of simultaneous use with celecoxib in some groups of patients, a possible deterioration in renal function should be considered, including to acute renal failure, which usually passes after the withdrawal of NSAIDs; lisinopril when used with Dilaxa does not have a significant pharmacodynamic interaction on blood pressure;
• thiazide diuretics, furosemide: it is possible to reduce their natriuretic effect by inhibiting renal Pg synthesis;
• oral contraceptives: celecoxib does not have a clinically significant effect on the pharmacokinetics of a complex contraceptive drug containing 1000 μg norethisterone / 35 μg ethinylestradiol;
• lithium: the use of lithium salts 2 times a day at a dose of 450 mg and celecoxib at a dose of 200 mg increases the plasma concentration of lithium by ~ 17%, which requires careful monitoring of patients in the course of combined treatment or in case of celecoxib withdrawal;
• other NSAIDs: concomitant use of celecoxib and other NSAIDs (not including acetylsalicylic acid) should be avoided, as the risk of side effects increases;
• antacids (magnesium / aluminum hydroxide), omeprazole, methotrexate, glibenclamide, phenytoin or tolbutamide: there were no clinically significant interactions with celecoxib;
• acetylsalicylic acid in low doses: celecoxib does not reduce platelet aggregation, therefore, it is ineffective to replace acetylsalicylic acid with it for the prevention of cardiovascular diseases;
• digoxin: there is no information on its interaction with celecoxib, but given the effect of the latter on the cardiovascular system, Dilax should be taken with digoxin with caution, carefully monitoring adverse reactions.

Analogs

Dilaxa analogues are: Celebrex, Roucoxib-Routek, Celecoxib-Vial, etc.

Terms and conditions of storage

Store in original packaging at temperatures up to 25 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Dilax

According to reviews, Dilaxa, at a moderate cost, relieves pain well, is easy to use and has practically no side effects if the recommended dosage is observed.

Of the shortcomings, some patients noted a mild anti-inflammatory effect of Dilaxa and an adverse reaction in the form of nausea.

Dilaxa price in pharmacies

Dilaxa's price for a blister (10 capsules): for a dose of 100 mg is approximately 218 to 415 rubles, for a dose of 200 mg - from 220 to 450 rubles.

Dilaxa: prices in online pharmacies

Drug name Price Pharmacy

Dilaxa 100 mg capsule 10 pcs. 164 RUB Buy

Dilaxa capsules 100mg 10 pcs. 245 RUB Buy

Dilaxa 200 mg capsule 10 pcs. 274 r Buy

Dilaxa 200 mg capsule 30 pcs. RUB 635 Buy

Dilaxa capsules 200mg 30 pcs. 707 r Buy

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!