Rapent Rapid - instructions for use, doses, side effects, contraindications

Excipients: silicon dioxide colloid - 4 mg, calcium hydrophosphate - 110 mg, corn starch - 45 mg, povidone-KZO - 2 mg, magnesium stearate - 1 mg, sodium carboxymethyl starch - 18 mg, shell: acacia gum - 2,95 mg, sucrose - 46.6 mg, talc - 27.1 mg, aluminum varnish based on the dye crimson [Ponso 4R] [E124] - 11.5 mg, povidone-K25 - 1.5 mg, macrogol 6000 - 0.22 mg.

Description:Round biconvex tablets covered with a shell of red color, with small impregnations of a lighter color, on a break from white to almost white.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:

Non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid. Diclofenac has anti-inflammatory, analgesic, antiplatelet and antipyretic effect.By indiscriminately inhibiting cyclooxygenase I and 2 (COX1 and COX2), it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. 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. With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling.

Pharmacokinetics:Eating does not affect the absorption of the drug. The drug is quickly and completely absorbed when taken orally. Diclofenac Potassium in comparison with the sodium salt of diclofenac is rapidly absorbed. Absorption begins in the stomach, the maximum concentration of the drug in the blood plasma: 1.3-1.5 μg / ml is reached approximately 40 minutes after administration. The concentration in the plasma is linear in the dose of the drug administered. Changes in the pharmacokinetics of diclofenac against a background of repeated use do not occur.When observing the recommended interval between doses of the drug, its cumulation does not occur. The half-life of plasma is 1-2 hours.

The drug is quickly distributed in the body through tissues and liquids. Penetrates into the synovial fluid. The maximum concentration of diclofenac in synovial fluid is noted 2-4 hours later than in plasma. The half-life of diclofenac from the synovial fluid is 3-6 hours, and its concentration in the synovial fluid 4-6 hours after the administration of the drug remains higher than in the plasma for another 12 hours.

The connection with plasma proteins is high (up to 99%) and most of it is associated with albumins.

The drug is metabolized in the liver: 50% of the active substance is metabolized during the "first pass" through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugation. The enzyme system P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.

The drug is excreted mainly through the kidneys. Systemic clearance is 260 ml / min.About 60% of the administered dose is excreted through the kidneys in the form of metabolites and less than 1% - in unchanged form. The rest of the drug is excreted as metabolites with bile. It is noted that the pharmacokinetics of the drug does not change depending on the age of the patient.

In patients with severe renal insufficiency (clearance of creatinine KK less than 10 ml / min), 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 cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.

Indications:

Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, osteoarthritis, exacerbation of gout, ankylosing spondylitis), post-traumatic pain syndrome, accompanied by inflammation, postoperative pain. Lumbago, sciatica, neuralgia, myalgia, tenosynovitis. bursitis. Toothache, migraine.

Inflammatory diseases of the pelvic organs, primary algodismenorea, proctitis. As part of the complex therapy of infectious and inflammatory diseases of ENT organs with severe pain syndrome (pharyngitis, tonsillitis,otitis).

The drug reduces pain and inflammation during the treatment period, without affecting the progression of the disease.

Contraindications:

- Hypersensitivity to the active substance (including other NSAIDs) or ancillary components;

- Anamnestic data on an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, bronchial asthma);

- Erosive-ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;

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

- Period after aortocoronary bypass surgery;

- III trimester of pregnancy, the period of breastfeeding;

- Decompensated heart failure;

- Violations of hematopoiesis, hemostasis disorders (including hemophilia);

- Severe hepatic impairment or active liver disease;

- Severe renal insufficiency (creatinine clearance less than 30 ml / min); progressive kidney disease, incl.confirmed hyperkalemia;

- Children up to 15 years.

Carefully:

Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency (creatinine clearance less than 60ml / min), dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, condition after extensive surgical interventions, induced porphyria, diverticulitis, systemic connective tissue diseases, pregnancy I-I1 trimester.

Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAID. frequent use of alcohol, severe physical illness. Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Dosing and Administration:

The drug is used for short-term treatment (up to 7 days)!

Inside. Tablets are taken before meals, washed down with water.

The dose is set individually, taking into account the severity of the disease.

Adults usually appoint 100-150 mg per day in 2-3 doses, not more than 150 mg / day.

The maximum daily dose for migraine is 200 mg (not more than 1-2 days).

For children over 15 years of age, the daily dose is 100 mg divided into 2 divided doses.

For the elderly, especially for the depleted and debilitated, the appointment is recommended

the minimum effective dose (50 mg), not exceeding the daily dose of 100 mg.

Side effects:

Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.001%, including individual cases.

From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorcsy, increased activity of aminotransferases; rarely gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, dysfunction of the liver; 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 sense organs: 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 (BP) and shock; 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; very rarely - pneumonitis.

From the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

Overdose:

Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, seizures, increased blood pressure, respiratory depression, with a significant overdose - acute renal failure, hepatotoxic effect.

Treatment: gastric lavage, Activated carbon, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).

Interaction:

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, thrombolytic agents (altlimlaz, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract). Reduces the effects of hypotensive and hypnotics.

Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac. Reduces the effect of hypoglycemic agents.

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 with ethanol, colchicine, corticotropin, serotonin reuptake inhibitors and St. John's wort preparations increases the risk of bleeding in the gastrointestinal tract.

Diclofenac enhances the effect of drugs that cause photosensitivity.Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

Antibacterial drugs from the quinolone group - the risk of seizures. Effect on the results of laboratory tests: diclofenac can affect serum trances and naz (if this effect is long-lasting or if complications occur, treatment must be stopped), and may also cause an increase in potassium concentration.

Special instructions:

Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful when administered to patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, decrease in circulating blood volume is observed (eg , after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), the 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 liver function, the picture of peripheral blood, the analysis of feces for latent blood.

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.

Care must be taken when combined with ACE inhibitors, beta-blockers; digoxin; in the treatment of non-steroidal drugs, zidovudine.

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. When taking pills for people with diabetes should take into account the content in the preparation of sucrose (in 1 tablet - 46.6 mg of sucrose).

Patients taking the drug should refrain from drinking alcohol.

Effect on the ability to drive transp. cf. and fur:

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 hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

The coated tablets are 50 mg.

Packaging:10 tablets per contour cell pack. 1 contour pack together with instructions for use in a cardboard pack.

Storage conditions:

List B.

Store in a dry, protected light place at a temperature of 15 to 25 "C. Keep out of reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015137 / 01

Date of registration:15.12.2009

The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia

Manufacturer: & nbsp

HEMOFARM, A.D. Serbia

Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia

Information update date: & nbsp19.02.2016

Illustrated instructions

Instructions

Rapent Rapid (Rapten rapid)