Ibuklin - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 120 mg, corn starch 76 mg, glycerol 3 mg, sodium carboxymethyl starch (type A) 7 mg, silicon dioxide colloid 5 mg, talc 8 mg, magnesium stearate 6 mg.

Shell: hypromellose 6 cps 11.32 mg, dye sunset yellow (E110) lacquer aluminum 1.78 mg, macrogol-6000 2.2 mg, talc 4.06 mg, titanium dioxide 0.16 mg, polysorbate-80 0.16 mg, sorbic acid 0.16 mg, dimethicone 0.16 mg.

Description:

Tablets capsular shaped, covered with an orange coating, with a risk on one side; for certain tablets marble color is allowed.

Pharmacotherapeutic group:Analgesic combined (NSAID + analgesic non-narcotic)

ATX: & nbsp

M.01.A.E.51 Ibuprofen in combination with other drugs

Pharmacodynamics:

Combined drug, the effect of which is due to its constituent components.

Ibuprofen - non-steroidal anti-inflammatory drug (NSAID), has analgesic, anti-inflammatory, antipyretic effect. Inhibiting cycloxygenase (COX) 1 and 2, disrupts the metabolism of arachidonic acid, reduces the number of prostaglandins (mediators of pain, inflammation and hyperthermia), both in the inflammatory focus and in healthy tissues, suppresses the exudative and proliferative phases of inflammation.

Paracetamol - non-selectively blocks COX, mainly in the central nervous system, weakly affects water-salt metabolism and mucous membrane of the gastrointestinal tract (GI tract). Has analgesic and antipyretic effect. In inflamed tissues, peroxidases neutralize the effect of paracetamol on COX 1 and 2, which explains the low anti-inflammatory effect.

The effectiveness of the combination is higher than that of the individual components.Relieves arthralgia at rest and during movement, reduces morning stiffness and swelling of joints, promotes an increase in the volume of movements.

Pharmacokinetics:

Ibuprofen.

Absorption is high, quickly and almost completely absorbed from the gastrointestinal tract (GIT). The time to reach the maximum concentration (TCmax) after ingestion is about 1-2 hours. The connection with blood plasma proteins is more than 90%. Half-life (T1 / 2) - about 2 hours Slowly penetrates the joint cavity, accumulates in the synovial fluid, creating higher concentrations in it than in the blood plasma. After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into an active S-form. Exposed to metabolism. More than 90% is excreted by the kidneys (unchanged not more than 1%) and, to a lesser extent, with bile in the form of metabolites and their conjugates.

Paracetamol.

Absorption is high, the association with plasma proteins is less than 10% and slightly increases with an overdose. Sulfate and glucuronide metabolites do not bind to plasma proteins even at relatively high concentrations. The value of Cmax is 5-20 μg / ml, TCmax is 0.5-2 hours. It is evenly distributed in the liquid medium of the body. Penetrates through the blood-brain barrier.

About 90-95% of paracetamol is metabolized in the liver with the formation of inactive conjugates with glucuronic acid (60%), taurine (35%) and cysteine (3%), as well as a small amount of hydroxylated and deacetylated metabolites. A small part of the preparation is hydroxylated by microsomal enzymes with the formation of highly active N-acetyl-l-benzoquinonimine, which binds to the sulfhydryl groups of glutathione. When depletion of glutathione stores in the liver (with an overdose) enzyme systems of hepatocytes can be blocked, leading to the development of their necrosis.

T1 / 2 - 2-3 hours. In patients with cirrhosis of the liver, T1 / 2 slightly increases. In elderly patients the clearance of the drug decreases and T1 / 2 increases. It is excreted by the kidneys, mainly in the form of glucuronide and sulfate conjugates (less than 5% in unchanged form). Breast milk penetrates less than 1% of the accepted dose of paracetamol. In children, the ability to form conjugates with glucuronic acid is lower than in adults.

Indications:

- symptomatic therapy of infectious and inflammatory diseases (cold, flu) accompanied by fever, chills, headache, pain in muscles and joints, sore throat;

- myalgia;

- neuralgia;

- back pain;

- joint pain, pain syndrome with inflammatory and degenerative diseases of the musculoskeletal system;

- pain with bruises, sprains, dislocations, fractures;

- post-traumatic and postoperative pain syndrome;

- toothache;

- algodismenorea (painful menstruation).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Contraindications:Increased individual sensitivity to the components of the drug (including other NSAIDs), gastric ulcer and duodenal ulcer in the exacerbation phase, gastrointestinal bleeding, severe renal failure (QC less than 30 ml / min), complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history), optic nerve damage, genetic absence of glucose-6-phosphate dehydrogenase, syphilis blood levels, period after aortocoronary bypass surgery; progressive kidney disease,severe hepatic insufficiency or active liver disease, confirmed hyperkalemia, active gastrointestinal bleeding, inflammatory bowel disease, children under 12 years of age.

Carefully:Ischemic heart disease, chronic heart failure, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, CC less than 60 ml / min, ulcerative lesions of the gastrointestinal tract in history, presence of Helicobacter pylori infection, advanced age, prolonged use NSAIDs, alcoholism, severe somatic diseases, simultaneous administration of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiaggregants (including chi sp., acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

If you need to use the drug Ibuklin® during pregnancy and lactation (breastfeeding), you should carefully weigh the expected benefit of therapy for the mother and the potential risk to the fetus or child.

If you need to use in the first trimester of pregnancy should be deleted long-term use of the drug Ibuklin ®.

If you need a short-term use of the drug Ibuklin® during lactation, the termination of breastfeeding is usually not required. In experimental studies, embryotoxic, teratogenic and mutagenic effects of the components of the drug Ibuklin® have not been established.

Dosing and Administration:

Inside (before or 2-3 hours after eating), without chewing, squeezed with enough water. Adults and children over 12 years - 1 tablet 2-3 times a day. The minimum interval between taking the drug is 4 hours. The maximum dose for adults: single - 2 tablets, daily - 6 tablets.

In case of violations of the kidney or liver function, for elderly patients, the interval between doses should be at least 8 hours.

The drug should not be taken for more than 5 days as an anesthetic and for more than 3 days as an antipyretic without the supervision of a doctor.

Side effects:

From the digestive system: rarely - dyspeptic phenomena, with prolonged use in high doses - hepatotoxic effect.

On the part of the hematopoiesis system: rarely - thrombocytopenia, leukopenia,

pancytopenia, neutropenia, agranulocytosis.

Allergic reactions: rarely - skin rash, itching, hives.

Overdose:Symptoms: gastrointestinal disorders (diarrhea, nausea, vomiting, anorexia, pain in the epigastric region), an increase in prothrombin time, bleeding after 12-48 hours, retardation, drowsiness, depression, headache, tinnitus, impaired consciousness, cardiac dysfunction rhythm, lowering blood pressure, manifestations of hepato- and nephrotoxicity, seizures, possibly the development of hepatonecrosis. Treatment: gastric lavage for the first 4 hours; alkaline drink, forced diuresis; Activated carbon Inward, administration of donors of SH-groups and precursors of glutathione-methionine synthesis 8-9 hours after overdose and N-acetylcysteine inside or intravenously - after 12 hours, antacid preparations; hemodialysis; symptomatic therapy. The need for additional therapeutic measures (further introduction of methionine, intravenous injection of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction:

With the simultaneous use of the drug Ibuklin® with drugs, it is possible to develop various interaction effects.

Long-term combined use with paracetamol increases the risk of developing nephrotoxic effects.

The combination with ethanol, glucocorticosteroids, corticotropin increases the risk of erosive and ulcerative lesions of the digestive tract.

Ibuprofen enhances the action lines (heparin) and indirect (coumarin and indandione derivatives), anticoagulants, thrombolytic agents (alteplase, anestreplase, streptokinase, urokinase), antiplatelet agents, colchicine - the risk of hemorrhagic complications increases.

Strengthens the hypoglycemic effect of insulin and oral hypoglycemic drugs.

Weaken the effects of antihypertensive drugs and diuretics (by inhibiting the synthesis of renal prostaglandins).

Increases the concentration in the blood of digoxin, lithium and methotrexate. Caffeine enhances the analgesic effect of ibuprofen. Cyclosporin and gold preparations increase nephrotoxicity.

Cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin increase

the frequency of hypoprothrombinemia.

Antacids and colestramine reduce the absorption of the drug.

Myelotoxic drugs promote the manifestation of hematotoxicity of the drug.

Special instructions:

The expediency of using the drug as an antipyretic agent is decided in each case, depending on the severity, nature and tolerability of the febrile syndrome.

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. At simultaneous application of anticoagulants of indirect action it is necessary to supervise parameters of a coagulating system of blood. It is necessary to avoid joint intake of the drug Ibuklin® with other NSAIDs. To avoid possible damaging effects on the liver during the intake of the drug should not drink alcohol.

With prolonged (more than 5 days) drug intake, control of peripheral blood and the functional state of the liver is necessary.

The drug may distort the results of laboratory tests in quantitative determination of glucose, uric acid in the blood serum, 17-ketosteroids (it is necessary to cancel the drug 48 hours prior to the study).

Effect on the ability to drive transp. cf. and fur:During the treatment period, the patient should refrain from engaging in potentially dangerous activities requiring increased attention and speed of psychomotor reactions

Form release / dosage:Tablets coated with a film coat 400 mg + 325 mg.

Packaging:For 10 tablets in PVC / A1 blister. For 1, 2 or 20 blisters packaged in a pack of cardboard along with instructions for use.

Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children!

Shelf life:5 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011252 / 01

Date of registration:07.07.2011

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp03.07.2013

Illustrated instructions

Instructions

Ibuklin® (Ibuclin)