Universal reference book for medicines
Product name: NAKLOFEN (NAKLOFEN)

Active substance: diclofenac

Type: NSAIDs

Manufacturer: KRKA (Slovenia)
Composition, form of production and packaging
The tablets covered with an enteric film coat of
brownish-yellow color, round, slightly biconvex, smooth.

1 tab.

diclofenac sodium 50 mg

Excipients: lactose monohydrate, corn starch, microcrystalline cellulose, povidone, silicon dioxide colloidal anhydrous, magnesium stearate.

Ingredients of enteric film coating: hypromellose, iron dye red oxide (E172), iron oxide yellow (E172), titanium dioxide, methacrylic acid-ethyl acrylate copolymer, propylene glycol, talc.

10 pieces.
- blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Diclofenac sodium is a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects.

The main mechanism of its action and associated side effects are indiscriminate inhibition of the activity of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2), which leads to a disruption of the metabolism of arachidonic acid, a decrease in the synthesis of prostaglandins, prostacyclin and thromboxane.
The level of various prostaglandins in urine, gastric mucosa and synovial fluid decreases. 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. Like all non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac has antiplatelet activity. In therapeutic doses, diclofenac sodium has virtually no effect on bleeding time. With prolonged treatment, the analgesic effect of diclofenac sodium does not decrease.
PHARMACOKINETICS

Absorption is fast and complete, the food slows the absorption rate by 1-4 hours and reduces the maximum concentration by 40%.
After oral administration, 50 mg ofCmax - 1.5 μg / ml is achieved after 2-3 hours. The concentration in the plasma is linear depending on the amount of the dose taken. 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. Bioavailability - 50%.
The connection with plasma proteins is more than 99% (most of it is associated with albumins).
Penetrates into the synovial fluid; C max in the synovial fluid is observed 2-4 hours later than in the plasma. T 1/2 of 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). The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug has not been elucidated.
Metabolism: 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. 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 systemic clearance is 260 ml / min, the volume of distribution is 550 ml / kg. T 1/2 from the plasma - 2 hours. About 70% of the administered dose is excreted as pharmacologically inactive metabolites by the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile.
In patients with severe renal failure (creatinine clearance less than 10 ml / min), the 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 of the liver, as well as elderly patients, the pharmacokinetic parameters of diclofenac do not change.Diclofenac penetrates into breast milk.

INDICATIONS

- inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis, arthritis in Reiter's disease, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine, including radicular syndrome, tendovaginitis, periarthritis, bursitis, myositis, synovitis);

- pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache, renal and biliary colic;

- in the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis);

febrile syndrome.

Diclofenac is intended for symptomatic therapy and does not affect the progression of the disease.

DOSING MODE

Inside, without chewing, during or after a meal, with a small amount of water.

Adults and adolescents with 15 years (and weighing more than 45 kg) - 50 mg 2-3 times a day.
When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 100 mg / day. The maximum daily dose is 150 mg.
SIDE EFFECT

Often -1-10%;
sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.01%, including individual cases.
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, dryness of the mucous membranes (including the mouth), damage to the esophagus, diaphragm-like bowel strains (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.

On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, eosinophilia, hemolytic and aplastic anemia, agranulocytosis.

Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure (BP) and shock;
very rarely angioedema (including facial).
From the cardiovascular system: very rarely - palpitations, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

On the part of the respiratory system: rarely - cough, bronchial asthma (including dyspnea);
very rarely - pneumonitis, laryngeal edema.
On the part of the skin: often - skin rash;
rarely - hives; very rarely, bulbar eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.
CONTRAINDICATIONS

- period after aortocoronary shunting;

- erosive and ulcerative changes in the mucosa of the stomach or duodenum, active gastrointestinal bleeding;

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

- cerebrovascular bleeding or other bleeding and hemostasis disorders;

- severe hepatic impairment or active liver disease;

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

Decompensated heart failure;

- oppression of bone marrow hematopoiesis;

- III trimester of pregnancy, the period of breastfeeding;

- this dosage form is contraindicated in children weighing less than 45 kg (or at the age of 15 years);

hypersensitivity to diclofenac;
with 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, asthma).
With caution: coronary heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min;
anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, advanced age, long-term use of NSAIDs, frequent alcohol use, severe somatic diseases, induced porphyria, epilepsy, advanced age, diverticulitis, systemic connective tissue diseases, including after massive surgery), elderly patients (including those receiving diuretics, weakened patients and with low body weight), concomitant therapy with the following reparative: anticoagulants (eg, warfarin), antiplatelet agents (e.g., aspirin, clopidogrel), oral corticosteroids (e.g., prednisone), selective serotonin reuptake inhibitor (such as citalopram, fluoxetine, paroxetine, sertraline). To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as little as possible.
PREGNANCY AND LACTATION

The use of diclofenac in pregnant women is possible only when the expected benefit exceeds the potential risk to the fetus.
Diclofenac is not recommended for use during the last trimester of pregnancy.
Despite the fact that diclofenac is found in breast milk in small amounts, its use during breast-feeding is not recommended.

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in severe renal failure (CK less than 30 ml / min), including confirmed hyperkalemia, progressive kidney disease.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe hepatic insufficiency or active liver disease.

APPLICATION FOR CHILDREN

Contraindicated for children under 15 years.

APPLICATION IN ELDERLY PATIENTS

Use with caution in elderly patients.

SPECIAL INSTRUCTIONS

In order to quickly achieve the desired therapeutic effect, take the drug 30 minutes before meals.
In other cases, take before, during or after a meal wholly, with plenty of water.
To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Caution should be used for ulcerative colitis and Crohn's disease because of a possible exacerbation of the disease.

With long-term use of diclofenac, it is possible, although in rare cases, the development of serious hepatotoxic reactions, and therefore it is recommended to regularly examine the function of the liver.

Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when administering the drug to patients with cardiac or renal insufficiency, as well as in the treatment of elderly people taking diuretics and patients who for any reason have a decrease in circulating blood volume (for example , after a major surgical intervention).
If diclofenac is prescribed in such cases, it is recommended to monitor kidney function as a precautionary measure.
Caution should be given to diclofenac in patients with violations of blood coagulation, porphyria, epilepsy, as well as in patients receiving anticoagulants or fibrinolytics.

When carrying out long-term therapy, it is necessary to monitor the picture of peripheral blood, to conduct a fecal occult blood test.

In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended.
In patients with infertility (including undergoing examination) it is recommended to cancel the drug.
Patients taking the drug should refrain from drinking alcohol.

In infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac sodium can mask the symptoms of these diseases.

Influence on the ability to manage motor vehicles and work with mechanisms

During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, convulsions, with a significant overdose - acute renal failure, hepatotoxic effect.

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 (significant association with proteins and intensive metabolism).
DRUG INTERACTION

Increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.

Reduces the effect of diuretics, against the background of potassium-sparing diuretics, the risk of developing gyerkalemia increases;
against the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more gastrointestinal).
Reduces the effect of hypotensive and hypnotic drugs.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (bleeding from 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 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 is manifested by increased nephrotoxicity.
Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.
Simultaneous administration with ethanol, colchicine, corticotropin and preparations of 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.
Antibacterial drugs from the quinolone group - the risk of seizures.

TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

Store in a dry place at a temperature of no higher than 25 ° C.
Keep out of the reach of children. Shelf life - 5 years.
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