Naklofen SR - instructions for use, dose, side effects, contraindications

SHELL: hypromellose 4.20 mg, ferric iron oxide red (E172) 0.20 mg, titanium dioxide 0.70 mg, macrogol 6000 0.36 mg, polysorbate 80 0.18 mg, talc 3.64 mg.

Description:

Round, biconcave, smooth tablets, covered with a film shell of a reddish-brown color.

Type of tablet on the break: the mass of white or almost white color, covered with a film shell of reddish-brown color.

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

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:Diclofenac 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 synthesis of prostaglandins in the kidneys, mucous membrane of the stomach 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. With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling. Like all non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac has antiaggregant activity. In therapeutic doses diclofenac practically does not affect the time of bleeding. With prolonged treatment, the analgesic effect of diclofenac does not decrease.

Pharmacokinetics:As a result of sustained release of the drug, the maximum concentration (Cmax) in the plasma is lower than that produced when a short-acting drug is administered; however, it remains high for a long time after administration. Cmax 0.5 μg / ml, the time required to reach the maximum concentration (TCmax) -5 h after taking 100 mg of prolonged-release tablets. The concentration in the plasma is linear depending on the amount of the administered dose. 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 breast milk, synovial fluid; Stax in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life (T1 / 2) of the synovial fluid is 3-6 hours (the concentration of the drug in the synovial fluid 4-6 hours after its administration is higher than in the plasma, and remain higher for another 12 hours).

50% of the drug is metabolized during the "first pass" through the liver; the area under the concentration-time curve (AUC) is 2 times lower after oral administration of the drug than after parenteral administration of the same dose.Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The isozyme CYP2C9 also participates in the metabolism of the drug. Pharmacological activity of metabolites is less than diclofenac.

Systemic clearance is 260 ml / min. T1 / 2 from the plasma -1-2 hours. 60% 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 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, the pharmacokinetic parameters do not change.

Indications:

- Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis (in case of an acute attack it is preferable to use high-speed medicinal forms), arthritis in Reiter's disease, rheumatic soft tissue damage

tissues, osteoarthrosis of peripheral joints and spine, including with 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 (in case of an acute attack it is preferable to use high-speed medicinal

forms), 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).

- Feverish syndrome.

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

Contraindications:

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

- The period after aortocoronary bypass surgery.

- Erosive-ulcerous changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding.

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

- Cerebrovascular bleeding or other bleeding and hemostasis disorders.

- Severe hepatic impairment or active liver disease.

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

- Decompensated heart failure.

- Inhibition of bone marrow hematopoiesis.

- III trimester of pregnancy, the period of breastfeeding.

- Children's age (up to 18 years).

Carefully:ischemic 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 gastrointestinal ulcer, presence of Helicobacter pylori infection, advanced age, long-term use of non-steroidal anti-inflammatory drugs (NSAIDs),frequent alcohol use, severe physical illnesses, induced porphyria, epilepsy, old age, diverticulitis, systemic connective tissue diseases, a significant decrease in the volume of circulating blood (BCC) (including after massive surgery), elderly patients (prescribed in lower doses) (including those receiving diuretics, weakened patients and low body weight), concomitant therapy with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (e.g., acetylsalicylic acid, clopidogrel), fibrinolytics, oral glucocorticoids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, 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 I-II trimester.

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 it is not recommended to use during the last trimester of pregnancy. Although diclofenac is found in breast milk in small amounts, its use during breastfeeding is not recommended.

Dosing and Administration:

Inside, the tablets should be swallowed whole, not liquid, squeezed enough water during or after a meal.

Naklofen CP, prolonged-action tablets, 100 mg should be used for long-term therapy.

The initial and maintenance doses are 1 tablet per day.

If necessary, increase the dose to 150 mg per day Naklofen CP should be combined with tablets or suppositories of Naclofen 50 mg.

Side effects:

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

On the part of the digestive system, often - epigastric pain, abdominal cramps, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, 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,dryness of the mucous membranes (including the mouth), damage to the esophagus, diaphragm-like intestinal strictures (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, tremor, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, agitation, 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, edema.

On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, eosinophilia, hemolytic and aplastic anemia, agranulocytosis. Allergic reactions: anaphylactic / anaphylactoid reactions, including marked reduction in blood pressure (BP) and shock; very rarely - angioedema (including face), in some cases vasculitis.

From the side of the cardiovascular system: very rarely - palpitation, tachycardia, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

From the respiratory system: rarely - cough, bronchial asthma (including dyspnea); very rarely - pneumonitis, laryngeal edema.

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, nausea, abdominal pain, bleeding from the gastrointestinal tract, diarrhea, headache, dizziness, tinnitus, increased excitability, hyperventilation with increased convulsive readiness, convulsions, 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 (significant association 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; on the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often the gastrointestinal tract).

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.

Hypoglycemic agents - hypo- or hyperglycemia can be observed.With this combination of funds, it is necessary to monitor the concentration of glucose in the blood. 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.

Special instructions:

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 in such cases appoint diclofenac, it is recommended as a precaution to monitor kidney function.

Caution should be given diclofenac in patients with severe renal or hepatic insufficiency, heart failure, with blood clotting disorders, porphyria, epilepsy, as well as in patients receiving anticoagulants or fibrinolytics.

When performing long-term therapy, it is necessary to control the picture

peripheral blood, analyze 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 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.

The amount of sucrose contained in the preparation does not affect patients with the following conditions: lactase enzyme deficiency, galactosemia, and glucose / galactose uptake syndrome.

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 engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of prolonged action, covered with a film coat of 100 mg.

Packaging:10 tablets in a blister pack.2 blisters per pack of cardboard along with instructions for use.

Storage conditions:Store in a dry place, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N013166 / 05

Date of registration:14.03.2008

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp09.03.2016

Illustrated instructions

Instructions

Naklofen SR (Naklofen SRX)