Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsp
    capsules set: capsules with prolonged release (diclofenac), enteric-soluble capsuleslansoprazole)
    Composition:

    Diclofenac, sustained-release capsules, 75 mg

    Composition per one capsule

    Diclofenac sodium, substance - pellets, coated with enteric-soluble

    shell 80.40 mg

    The composition of 80.40 mg of substance-pellet

    [Active substance:

    Diclofenac sodium 25.00 mg

    Excipients: sugar crockery [sucrose, molasses starch]1 32.00 mg, giprolose 1.87 mg, hypromellose 2.50 mg, magnesium carbonate 3.20 mg, methacrylic acid and ethyl acrylate copolymer (1: 1), 30% dispersion2,3 6.90 mg, triethyl citrate 0.68 mg, talc 6.80 mg, titanium dioxide 0.85 mg, carmellose sodium 0.27 mg, macrogol 0.27 mg, sodium hydroxide 0.06 mg]

    1 Contains up to 92% sucrose

    2 In terms of dry polymer

    3 The polymer dispersion contains 0.7% sodium lauryl sulfate and 2.3% polysorbate-80, as emulsifiers. Diclofenac sodium, prolonged-release substance pellets 130.20 mg

    The composition of 130.20 mg of substance-pellet

    [Active substance: Diclofenac sodium 50.00 mg Excipients: sugar crockery [sucrose, molasses starch]1 64.00 mg, giprolose 3.74 mg, triethyl citrate 0.47 mg, talc 9.49 mg, methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [2: 0, 1: 1] type A, 30% dispersion2 2.00 mg, methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [2: 0, 2: 1] type B, 30% dispersion2 0.50 mg] Excipients: talc 0.42 mg Composition of an empty capsule Cap: titanium dioxide (E171) 0.488 mg, indigocarmine (E132) 0.022 mg, gelatin 23.890 mg Housing: titanium dioxide (E171) 0.732 mg, gelatin 35.868 mg

    1Contains up to 92% sucrose

    2In terms of dry polymer

    Lansoprazole, enteric-soluble capsules, 15 mg

    Composition per one capsule

    Lansoptol, pellets 166.03 mg

    Composition for 166.03 mg of pellets

    [Active substance: Lansoprazole 15.00 mg

    Excipients: sugar crockery [sucrose, molasses starch]1 50,915 mg, giprolose 1,390 mg, magnesium hydroxycarbonate 17,915 mg, sucrose 27,775 mg, corn starch 17,355 mg, sodium lauryl sulfate 1.365 mg, hypromellose 4.845 mg, methacrylic acid and ethyl acrylate copolymer (1: 1)2'3 21,760 mg, talc 4,260 mg, macrogol 6000 2,170 mg, titanium dioxide 1,280 mg, sodium hydroxide 0.135 mg]

    Excipients: talc 0.33 mg

    Composition of an empty capsule

    Cap: gelatin 18.698 mg, titanium dioxide (E171) 0.384 mg, iron dye red oxide (E172) 0.118 mg

    Housing: gelatin 28.224 mg, titanium dioxide (E171) 0.576 mg

    1Contains up to 92% sucrose

    2 In terms of dry polymer

    3The polymer dispersion contains 0.7% sodium lauryl sulfate and 2.3% polysorbate-80, as emulsifiers.

    Description:

    Diclofenac, sustained-release capsules, 75 mg

    Capsules number 2, the capsule body is white, the lid is blue. Contents of my capsules: pellets from white to cream color.

    Lansoprazole, enteric-soluble capsules, 15 mg

    Capsules No. 3, capsule body white, cap of red-brown color. Contents of capsules: pellets from white to white with a slightly yellowish or slightly pink tinge.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID) + proton pump inhibitor
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:

    Diclofenac - Non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid.Has anti-inflammatory, analgesic, antipyretic and antiplatelet effect. Indiscriminately inhibiting cycloxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) in the focus of inflammation, suppresses the exudative and proliferative phases of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the joint condition.

    Lansoprazole - a drug from a group of proton pump inhibitors. Does not show anticholinergic or antihistaminic properties, binds specifically to H+/TO+- ATPase (also called a proton pump) on the secretory surface of parietal cells of the stomach and prevents the final stage of secretion of gastric juice.

    Lansoprazole reduces basal, day and night secretion of gastric juice, which prevents food-stimulated gastric juice secretion and increased secretion caused by other factors such as gastrin and pentagastrin, and also prevents insulin-induced increase in gastric acid volume and acidity.Reduces the acidity of gastric juice and the duration of time during which the pH value> 4, The effect is proportional to the amount of the dose.

    After stopping therapy with lansoprazole, the pH of the gastric juice decreases gradually and returns to normal within 2-4 days. There were no cases of a significant increase in secretion of gastric juice after discontinuation of treatment.

    Lansoprazole increases the activity of pepsinogen in the serum and lowers the activity of pepsin below the basal values ​​after stimulation with food. During treatment with lansoprazole, the average activity of gastrin in serum increases by a factor of 1.5-2. Concentration rises during the first 8 weeks treatment, after which it reaches a plateau and at the completion of therapy after 4 weeks to initial values.

    Pharmacokinetics:

    Absorption

    Absorption is fast and complete, food slows down the absorption rate. The maximum concentration is noted 30-60 minutes after ingestion. The concentration in the blood plasma is linear depending on the amount of oral dose. Changes in the pharmacokinetics of diclofenac against a background of repeated use are not noted. Bioavailability - 50%.

    Distribution

    Do not cumulate while respecting the recommended interval between doses. The connection with plasma proteins is more than 99% (most of it is associated with albumins).

    Metabolism

    50% is metabolized during the "first pass" effect through the liver. Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. In the metabolism of diclofenac is also involved isoenzyme CYP2C9. The pharmacological activity of metabolites is lower than that of diclofenac.

    Elimination

    Systemic clearance is 260 ml / min. The half-life (T1/2) from the blood plasma -2 h. The excretion from the synovial fluid is slower than from the plasma.

    70% of the administered dose is excreted as metabolites through the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile. In patients with severe renal dysfunction, excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood. In patients with chronic hepatitis or compensated liver cirrhosis, pharmacokinetic parameters are the same as in patients without liver disease.

    Diclofenac penetrates into breast milk.

    Lansoprazole

    Absorption

    Absorption is high, bioavailability is 80%. Food intake reduces absorption and bioavailability (by 50%), but the inhibitory effect on gastric secretion remains the same, regardless of food intake. The time to reach the maximum concentration (0.75-1.15 mg / l) is 1.7 hours. The maximum plasma concentration and the area under the concentration / time curve (AUC) are approximately proportional to the dose taken.

    Distribution

    Cumulation does not occur. The connection with plasma proteins is 97%. Good penetrates into tissues, incl. in the lining cells of the gastric mucosa. The volume of distribution is 0.5 l / kg. Metabolism

    It is actively metabolized at the "first passage" through the liver with the participation of the isoenzyme CYP2C19 with the formation of sulfonyl-, sulfone- and hydroxy derivatives. Inhibits activity CYP2C19.

    Elimination

    T1/2 lansoprazole less than 2 hours and does not reflect the duration of gastric secretion inhibition. When a violation of liver function T1/2 increases 3-4 times. Lansoprazole is released as metabolites; approximately one third of lansoprazole is excreted by the kidneys and two-thirds - with bile through the intestine (renal failure is not significantly affected by the rate of excretion).

    Indications:Symptomatic therapy of inflammatory and degenerative diseases of the musculoskeletal system in patients with the risk of developing gastric and / or duodenal ulcers associated with NSAID administration: rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Bekhterev's disease); gouty arthritis, rheumatic soft tissue damage, osteoarthritis of peripheral joints and spine, including with radicular syndrome, tendovaginitis, bursitis.
    Contraindications:

    -Hypersensitivity to the drug components (including other NSAIDs);

    -complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa, paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);

    -inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the phase of exacerbation;

    -State after aortocoronary bypass surgery;

    -active gastrointestinal bleeding;

    -Birth, the period of breastfeeding;

    - cardiac failure in the stage of decompensation;

    -hepal hemopoiesis, hemostasis disorder (incl.hemophilia);

    - marked hepatic impairment or active liver disease;

    - kidney failure (creatinine clearance less than 30 ml / min), progressive kidney disease, hyperkalemia;

    -Sugarase / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;

    -Children under 18 years of age.

    Carefully:

    Erosive-ulcerative lesions of the mucous membrane of the stomach or duodenum (diclofenac apply only in case of carefully assessing the need for use, at a dose of not more than 75 mg / day), malignant neoplasms of the gastrointestinal tract. Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, alcoholism, severe physical illnesses.

    Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, chronic heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic and / or renal insufficiency (QL 30-60 ml / min), liver disease in history, dyslipidemia / hyperlipidemia , diabetes mellitus, smoking, inflammatory bowel disease, a significant decrease in BCC (incl.after extensive surgical intervention), induced porphyria, diverticulitis, systemic connective tissue diseases. Simultaneous reception of glucocorticosteroids (for example, prednisolone), anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

    Pregnancy and lactation:Application of the drug Naklofen Protect (kit) is contraindicated during pregnancy and during breastfeeding.
    Dosing and Administration:

    The kit is designed for combined intake of two kinds of capsules. Separate application of diclofenac capsules is possible only in the absence of ulcerative lesions of the stomach and / or duodenum and the risks of its development.

    Diclofenac

    Inside, squeezed a small amount of liquid, during or immediately after a meal. The initial dose is 1 capsule (75 mg) once a day. The maximum daily dose is 2 capsules / day (150 mg). At the expressed painful syndrome, it is possible to accept at once a daily dose of a preparation (2 capsules 1 time a day).In case of erosive-ulcerative lesions of the mucous membrane of the stomach or duodenum, one capsule (75 mg) per day should be limited to no more than 8 weeks.

    Lansoprazole

    Inside, whole, preferably in the morning, before eating.

    The initial dose is 15 mg / day (1 capsule). The maximum dose is 30 mg / day (2 capsules). In case of erosive-ulcerative lesions of the mucous membrane of the stomach or duodenum, 30 mg / day (2 capsules) should be used. Elderly patients, as well as patients with impaired renal and / or liver function, do not need dose adjustment.

    If it is impossible to swallow the capsule entirely, it must be opened, the contents mixed with a small amount of apple juice and swallowed without chewing.

    The same actions are possible if the substance is injected through a nasogastric tube. Duration of dose 30 mg / day (2 capsules) not more than 8 weeks. A dose of 15 mg / day (1 capsule) can be used up to 12 months.

    Side effects:

    Classification of the incidence of side effects recommended by the World

    Health Organization (WHO):

    Very often (from ≥1/10)

    Often (from ≥1 / 100 to <1/10)

    Infrequently (from ≥1 / 1000 to <1/100)

    Rarely (from ≥1 / 10000 to <1/1000)

    Very rarely (from <1/10000)

    Frequency is unknown (can not be estimated from available data)

    Diclofenac

    From the digestive system:

    often: epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases;

    rarely: gastritis, proctitis, bleeding from the digestive tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function;

    very rarely: stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis;

    From the nervous system:

    often: headache, dizziness; rarely: drowsiness;

    very rarely: a violation of sensitivity (including paresthesia), memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders;

    From the sense organs:

    often: vertigo;

    very rarely: visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disorders;

    From the urinary system:

    very rarely: acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis;

    From the hematopoiesis:

    very rarely: thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis;

    Allergic reactions:

    very rarely: angioedema (including facial), anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock;

    From the cardiovascular system.

    very rarely: palpitation, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction;

    From the respiratory system.

    rarely: exacerbation of bronchial asthma (including dyspnea);

    very rarely: pneumonitis;

    From the skin:

    often: skin rash;

    rarely: urticaria;

    very rarely: bullous rash, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

    Lansoprazole

    From the digestive system:

    often: constipation; infrequently: abdominal pain, diarrhea, nausea, dryness of the oral mucosa, dyspepsia, taste disorders, flatulence; very rarely: colitis, ulcerative colitis, candidiasis of the gastrointestinal tract, increase activity of "liver" enzymes, hyperbilirubinemia; rarely: jaundice, hepatitis;

    From the nervous system:

    often: headache;

    infrequently: dizziness, anxiety, fear, confusion, depression, confusion;

    From the respiratory system:

    rarely: cough, pharyngitis, rhinitis, upper respiratory tract infection, flu-like syndrome;

    On the part of the hematopoiesis system:

    very rarely: leukopenia, thrombocytopenia, eosinophilia, pancytopenia or agranulocytosis;

    Allergic reactions:

    rarely: urticaria, angioedema, photosensitization; very rare: anaphylactic reactions;

    Metabolic and nutritional disorders:

    rarely: anorexia, increased appetite;

    From the sense organs:

    very rarely: visual impairment (blurred vision), tinnitus;

    From the skin: often: skin rash;

    rarely: purpura, petechiae, hair loss;

    very rarely: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme;

    From the musculoskeletal system:

    rarely: pain in the joints, muscles and bones;

    From the genitourinary system:

    infrequently: increased concentration of creatinine.

    very rarely: interstitial nephritis, renal failure, urogenital impaired, impotence, gynecomastia;

    Other:

    infrequently: feeling tired; very rarely: peripheral edema;

    Overdose:

    Diclofenac

    Symptoms: vomiting, bleeding from the gastrointestinal tract, pain in the epigastric region, diarrhea, dizziness, tinnitus, lethargy, convulsions; rarely - increased blood pressure, acute renal failure, hepatotoxic effect, respiratory depression, coma, melena, convulsions, irritability.

    Treatment: gastric lavage, the reception of activated charcoal, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, respiratory depression.

    Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism). There is no specific antidote.

    Lansoprazole

    At present, no cases of an overdose of lansoprazole have been reported. In case of taking high doses of the drug, medical supervision is indicated, if necessary, symptomatic therapy. Hemodialysis is ineffective.

    Interaction:

    Diclofenac

    The simultaneous use of diclofenac with:

    - Lithium or digoxin can increase their concentration in blood plasma;

    - with some diuretics can reduce their diuretic effect; potassium-sparing diuretics can cause hyperkalemia;

    - Acetylsalicylic acid, glucocorticosteroids and other non-steroidal anti-inflammatory drugs increases the risk of side effects (bleeding in the gastrointestinal tract);

    - cyclosporine increases the nephrotoxicity of cyclosporine; methotrexate increases the toxicity of methotrexate;

    - hypotensive drugs - reduces their effectiveness.

    Reduces the effect of hypoglycemic agents.

    Against the background of simultaneous use with anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often the gastrointestinal tract). Reduces the effect of hypnotic drugs. Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

    Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.

    Gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which is manifested by increased nephrotoxicity.

    Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.

    Simultaneous use with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract. Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to UV irradiation.

    Drugs that block tubular secretion, increase the concentration of diclofenac in the blood plasma, thereby increasing its effectiveness and toxicity. Antibacterial drugs from the quinolone group increase the risk of seizures.

    Lansoprazole

    Lansoprazole lowers the acidity of the gastric juice, which can lead to a change in the absorption of certain substances, for example, the bioavailability of ketoconazole, ampicillin esters and iron salts is reduced. The bioavailability of digoxin rises by approximately 10%, which is clinically insignificant for most patients. There may be interaction with drugs that are metabolized in the liver by isozymes CYP3A and CYP2C19. Thus, with the simultaneous use of lansoprazole and theophylline (in the metabolism isoenzyme participates CYP3A) there was a moderate increase in the clearance of theophylline (10%). It is unlikely that this interaction is of clinical significance. However, in some patients, additional titration of the theophylline dose at the beginning and at the end of therapy with lansoprazole is required to achieve clinically effective concentrations of lansoprazole in the blood.

    Lansoprazole has no clinically significant interaction with phenazone, diazepam, ibuprofen, phenytoin, indomethacin, clarithromycin, prednisolone, propranolol, terfenadine, or warfarin.

    Lansoprazole can stimulate the secretion of theophylline (by 10%), but this effect is not clinically significant.

    Since the interaction with phenytoin, theophylline or warfarin may be significant in individual patients at risk, the drug should be taken with caution. Sucralfate and antacids can reduce the absorption of lansoprazole. Since the interaction is not clinically significant, patients can take sucralfate or antacids, at least 30 minutes prior to taking lansoprazole or 1 hour after.

    Special instructions:

    Prolonged use of diclofenac can very rarely cause serious undesirable effects on the part of the liver, which requires periodic monitoring of "hepatic" enzymes.

    With infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac should be taken into account, as they can lubricate the clinical picture of the diseases.

    When performing long-term therapy, it is necessary to monitor the picture of peripheral blood, the analysis of feces for latent blood.

    In connection with the negative effect on fertility, women planning pregnancy, the drug is not recommended.

    Like all medicines, diclofenac should be used in elderly patients in a minimally effective dose.

    Symptomatic improvement during therapy with lansoprazole does not exclude the possible development of neoplasms in the digestive tract. Care should be taken in the sudden occurrence or worsening of dyspeptic symptoms, especially in patients older than 45 years. Cardiovascular and cerebrovascular effects

    The use of diclofenac, especially in high doses (150 mg / day), can cause a slight increase in the risk of developing arterial thrombosis (eg, myocardial infarction or stroke).

    Patients with uncontrolled hypertension, congestive heart failure, ischemic heart disease, peripheral vascular disease and / or cerebrovascular disorders should take diclofenac only after a thorough examination. A thorough examination should be performed before the onset of prolonged therapy in patients at risk of cardiovascular disease (hypertension, hyperlipidemia, diabetes, smoking). It is not recommended simultaneous use of lansoprazole and atazanavir. Before and after treatment, endoscopic control is necessary to exclude malignant neoplasm, because treatment can mask symptoms and delay correct diagnosis. In patients receiving lansoprazole, ulcerative colitis may develop.

    Effect on the ability to drive transp. cf. and fur:Care must be taken when driving vehicles and other technical devices,requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Capsule set: prolonged-release capsules (diclofenac) 75 mg, enteric-soluble capsules (lansoprazole) 15 mg.
    Packaging:

    For 10 capsules (5 capsules of diclofenac and 5 capsules of lansoprazole) into a contiguous cell pack from the combined material OPA / Al / PVC and aluminum foil.

    For 2, 4 or 6 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

    Storage conditions:At a temperature of no higher than 25 ° C, in the original packaging. Keep out of the reach of children.
    Shelf life:

    2 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002077
    Date of registration:28.05.2013 / 25.11.2013
    Expiration Date:28.05.2018
    Date of cancellation:2018-02-06
    The owner of the registration certificate:KRKA-RUS, LLC KRKA-RUS, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp28.05.2018
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