Composition, form of production and packaging
Modified-release tablets are round, biconvex, two-layered; one layer of orange, the second - from white to yellowish white, with small impregnations of white and orange on the orange and white layers, respectively.
diclofenac sodium 75 mg,
in t.ch. diclofenac sodium (in granules intestine-soluble) 25 mg
diclofenac sodium (in enteric-granular granules with sustained release) 50 mg
[PRING] granules intestinal soluble - corn starch, lactose monohydrate, sodium carboxymethyl starch, acryl from white (methacrylic acid and methyl methacrylate copolymer (1: 1), talc, titanium dioxide, triethyl citrate, silicon dioxide colloid, sodium bicarbonate, sodium lauryl sulfate), simethicone emulsion 30%, magnesium stearate, silicon colloidal dioxide; granules intestine-soluble with prolonged release - corn starch, lactose monohydrate, carboxymethyl starch sodium, acrylic-from white (methacrylic acid and methyl methacrylate copolymer (1: 1), talc, titanium dioxide, triethyl citrate, silicon dioxide colloid, sodium bicarbonate, sodium lauryl sulfate), simethicone emulsion 30%, hypromellose, magnesium stearate, silicon dioxide colloid, aluminum lacquer based on the dye solar sunset yellow (E110).
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
NSAID, a derivative of phenylacetic acid. Diclofenac has anti-inflammatory, analgesic, antiplatelet and antipyretic effects. By indiscriminately inhibiting cyclooxygenase 1 and 2 (COX-1 and COX-2), it breaks the metabolism of arachidonic acid, reduces the amount of prostaglandins in a hotbed of inflammation. The most effective for inflammatory pain.
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 functional state of the joint. In injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema.
The drug removes or reduces pain and inflammation during the treatment of diseases of the musculoskeletal system, while does not affect the progression of the disease.
The drug Rapten Duo is a form of diclofenac (sodium salt) in the form of two-layer tablets.
After oral administration of diclofenac rapidly and completely absorbed from the digestive tract. After a single administration of C max in plasma is achieved through 20-60 min by releasing 25 mg of diclofenac from the first acid-fast layer . From the second layer slowly released 50 mg of diclofenac for? 6 hours, which provides a lasting effect (12-24 hours). Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted. Do not cumulate while observing the recommended interval between meals.
With plasma proteins 99% of the applied dose binds. The drug is well distributed in tissues and tissue fluids. Penetrates into the synovial fluid; C max in synovial fluid is observed 2-4 hours later than in plasma. T 1/2 from the synovial fluid 3-6 hours (the concentration of active substance in the synovial fluid 4-6 hours after the administration of the drug is higher than in the plasma, and remains higher for another 12 hours). Relationship of drug concentration in synovial fluid with clinical efficacy drug is not clear.
The drug penetrates through the BBB and placental barrier, in small amounts excreted in breast milk.
50% of the active substance is metabolized during the "first pass" through the liver. Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. In the metabolism of the drug takes part enzyme system P450 CYP2C9. The pharmacological activity of metabolites is lower than that of diclofenac. Systemic clearance is about 260 В± 50 ml / min, V d - 550 ml / kg.
T 1/2 from the plasma averages about 2.5 hours. 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is excreted unchanged, the rest of the dose (less than 35%) is excreted as metabolites with bile.
Pharmacokinetics in special clinical cases
In patients with chronic hepatitis or compensated cirrhosis, the pharmacokinetic parameters of diclofenac do not change.
- symptomatic treatment of diseases of the musculoskeletal system (including rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis / Bechterew's disease), gouty arthritis, osteoarthrosis of peripheral joints and spine, including with radicular syndrome, tendovaginitis , bursitis);
- pain syndrome of mild or moderate severity: neuralgia, myalgia, lumbago, sciatica, ossalgia, post-traumatic and postoperative pain syndrome, accompanied by inflammation, pain in cancer, headache, migraine, algodismenorea, adnexitis, toothache;
- in the complex therapy of infectious and inflammatory diseases of the ENT organs with severe pain syndrome (pharyngitis, tonsillitis, otitis).
Tablets are taken orally, without chewing, during or after a meal, with a sufficient amount of liquid.
The daily dose for adults is 75 mg (1 tab.). The maximum daily dose is 150 mg (1 tablet 2 times / day - preferably the first tablet before breakfast, and the second after 12 hours).
To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.
Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.001%, including individual cases.
From the side of 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, incl. paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.
From the senses: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.
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: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock; rarely - hives; very rarely - angioedema (including face).
From the cardiovascular system: very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
From the respiratory system: rarely - exacerbation of bronchial asthma, shortness of breath; very rarely - pneumonitis.
Dermatological reactions: often - skin rash; very rarely - bullous eruptions, erythema including. multiform, Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.
Other: rarely - swelling.
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);
- erosive and ulcerative changes in the mucosa of the stomach or duodenum, active gastrointestinal bleeding;
- Inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the phase of exacerbation;
- period after aortocoronary shunting;
Decompensated heart failure;
- violations of hematopoiesis, hemostasis disorders (including hemophilia);
- severe hepatic impairment or active liver disease;
- marked renal failure (QC less than 30
ml / min), progressive kidney disease, incl. confirmed hyperkalemia;
- rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
- III trimester of pregnancy;
- the period of lactation (breastfeeding);
- children's age till 18 years;
- Hypersensitivity to the active substance (including other NSAIDs) or ancillary components.
With caution should prescribe the drug for anemia, bronchial asthma, cerebrovascular diseases, IHD, stagnant heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency (CK 30-60 ml / min), liver disease in history, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, a significant decrease in BCC including after extensive surgery), hepatic porphyria, diverticulitis, systemic connective tissue diseases, in the I-II trimesters of pregnancy, with gastric ulcer and duodenal ulcer (including history), in the presence of Helicobacter pylori infection, in elderly patients (including those receiving diuretics, weakened patients and low body weight), with prolonged use of NSAIDs, frequent alcohol consumption, severe somatic diseases, simultaneous therapy with anticoagulants (eg, warfarin), antiplatelet agents (eg, acetylsalicylic acid, clopidogrel), oral GCS (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
PREGNANCY AND LACTATION
Contraindicated use of the drug in the III trimester of pregnancy and lactation. Care should be taken when prescribing the drug in the first and second trimesters of pregnancy.
In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended.
In patients with infertility (including those undergoing examination) it is recommended to cancel the drug.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication: marked renal failure (QC less than 30 ml / min), progressive kidney disease, incl. confirmed hyperkalemia.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: severe hepatic impairment or active liver disease.
APPLICATION FOR CHILDREN
Contraindicated: children under 18 years.
In order to quickly achieve the desired therapeutic effect, diclofenac is taken 30 minutes before meals. In other cases, take before, during or after eating, without chewing, squeezed with enough water.
Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised in appointing patients with cardiac or renal insufficiency, as well as in the treatment of elderly patients taking diuretics, and patients who for any reason have a reduced BCC (for example, after extensive surgical interventions). When appointing such patients diclofenac is recommended to monitor the kidney function (as a precaution).
Patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), kinetics and metabolism do not differ from similar processes in patients with normal liver function.
When performing long-term therapy, it is necessary to monitor the liver function, the picture of peripheral blood, to conduct a fecal occult blood test.
If the increase in hepatic transaminase activity persists or increases during the administration of the drug, if clinical signs of hepatotoxicity are noted (including nausea, fatigue, drowsiness, diarrhea, itching, jaundice), treatment should be discontinued.
Diclofenac (like other NSAIDs) can cause hyperkalemia.
Patients taking the drug should refrain from drinking alcohol.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure; with a significant overdose - acute renal failure, hepatotoxic effect, oppression breathing, coma.
Treatment: gastric lavage, activated charcoal, symptomatic therapy aimed at eliminating blood pressure increase, renal dysfunction, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
Diclofenac with simultaneous application increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.
Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia.
Against the background of anticoagulants, antiplatelet agents and thrombolytic agents (alteplase, streptokinase, urokinase), the risk of bleeding increases (more often from the digestive tract).
Diclofenac with simultaneous application reduces the effects of hypotensive and hypnotic drugs.
Increases the likelihood of side effects of other NSAIDs and GCS (bleeding in the gastrointestinal tract).
With simultaneous use with diclofenac, the toxicity of methotrexate and the nephrotoxicity of cyclosporine increases.
Acetylsalicylic acid reduces the concentration of diclofenac in the blood.
Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.
Diclofenac with simultaneous use reduces the effect of hypoglycemic drugs.
Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.
Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.
Simultaneous administration of diclofenac with ethanol, colchicine, corticotropin, selective serotonin reuptake inhibitors and St. John's wort increases the risk of bleeding in the digestive tract.
Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.
Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.
With the simultaneous use of antibacterial drugs from the group quinolone increases the risk of seizures.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light, out of reach of children at temperature from 15 В° to 25 В° C. Shelf life - 3 years.