More info
Active ingredients
Ibuprofen + paracetamol
Release form
Pills
Composition
Active ingredient: ibuprofen 400 mg and paracetamol 325 mg. Excipients: microcrystalline cellulose 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. Concentration of active ingredient (mg): 725 mg
Pharmacological effect
Ibuprofen is a non-steroidal anti-inflammatory drug, phenylpropionic acid derivative, has antiinflammatory, antipyretic and analgesic properties due to inhibition of COX main enzyme responsible for the metabolism of arachidonic acid are precursors of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The analgesic effect is due both to the peripheral (indirectly, through a decrease in prostaglandin synthesis) and to the central mechanism (inhibition of the synthesis of prostaglandins in the central and peripheral nervous system). Suppresses platelet aggregation. Paracetamol is a non-narcotic analgesic, has analgesic, antipyretic and weak anti-inflammatory effect by suppressing the activity of COX, and reducing the production of prostaglandins; has a predominant effect on the center of thermoregulation in the hypothalamus.
Pharmacokinetics
Ibuprofen Absorption - 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. Communication with plasma proteins - more than 90%. The half-life (T1 / 2) is about 2 hours. It slowly penetrates into the cavity of the joints and accumulates in the synovial fluid, creating in it higher concentrations than in the blood plasma. After absorption, about 60% of the pharmacologically inactive R-form slowly transforms into the active S-form. Subjected to metabolism. More than 90% is excreted by the kidneys (in unchanged form, not more than 1%) and, to a lesser extent, with bile as metabolites and their conjugates. Paracetamol. Absorption is high, the bond with plasma proteins is less than 10% and slightly increases with overdose.Sulfate and glucuronide metabolites do not bind to plasma proteins even in relatively high concentrations. The value of Cmax - 5-20 mcg / ml, TCmax - 0.5-2 hours. It is fairly evenly distributed in body fluids. It penetrates the blood-brain barrier. About 90-95% of paracetamol is metabolized in the liver to form 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 drug is hydroxylated by microsomal enzymes to form highly active N-acetyl-n-benzoquinone imine, which binds to the sulfhydryl groups of glutathione. When glutathione is depleted in the liver (overdose), the hepatocyte enzyme systems can be blocked, leading to the development of their necrosis. T1 / 2 - 2-3 hours. It is excreted by the kidneys, mainly in the form of glucuronide and sulphate conjugates (less than 5% - unchanged). Less than 1% of the accepted dose of paracetamol penetrates into breast milk. In children, the ability to form conjugates with glucuronic acid is lower than in adults.
Indications
Feverish conditions (including influenza and colds), myalgia, neuralgia, back pain, joint pain, pain in inflammatory and degenerative diseases of the musculoskeletal system, pain in bruises, sprains, dislocations, fractures post-traumatic and postoperative pain, toothache, algomenorrhea (painful menstruation), the drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease,
Contraindications
Increased individual sensitivity to components of the drug (including other NSAIDs), gastric ulcer and duodenal ulcer in the acute phase, gastrointestinal bleeding, severe renal failure (creatinine clearance (CC) less than 30 mlmin), complete or incomplete combination of bronchial asthma , recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history), lesions of the optic nerve, the genetic absence of glucose-6-phosphate dehydrogen basics, diseases of the blood system, the period after coronary artery bypass surgery.progressive kidney disease, severe liver failure or active liver disease, confirmed hyperkalemia, active gastrointestinal bleeding, inflammatory bowel disease, pregnancy (III term), children under 12 years of age.
Precautionary measures
With caution, the drug is used in the elderly, in patients with impaired liver or kidney function, with chronic heart failure, with dyspeptic symptoms before treatment, a history of gastrointestinal bleeding and diseases of the digestive organs, immediately after surgery, with indications of a history of allergic reactions associated with the intake of nonsteroidal anti-inflammatory drugs, bronchial asthma, polyps of the mucous membrane of the cavity and nose, as well as in persons receiving anticoagulant drugs and hypoglycemic drugs for oral administration.
Use during pregnancy and lactation
During pregnancy and lactation use of the drug is not recommended. If necessary, receive during lactation is necessary to resolve the issue of transfer to artificial feeding.
Dosage and administration
Inside (before or after 2-3 hours after eating), without chewing, drinking plenty of water. Adults. 1 tablet 3 times a day. The maximum daily dose is 3 pills. Children over 12 years old (body weight over 40 kg). 1 tablet 2 times a day. The duration of treatment is not more than 3 days as an antipyretic and not more than 5 days as an anesthetic. Continuation of drug treatment is possible only after consulting a doctor.
Side effects
Coronary heart disease, chronic heart failure, cerebrovascular disease, dyslipidemia, hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, CC less than 60 mlmin, ulcerative lesions of the gastrointestinal tract in history, the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, alcoholism, severe somatic diseases, simultaneous administration of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid Ota, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).Viral hepatitis, hepatic or renal failure of moderate and mild severity, benign hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndrome), liver cirrhosis with portal hypertension, nephrotic syndrome.
Overdose
Symptoms of acute poisoning include nausea, vomiting, stomach pain, and in severe cases, liver failure and a coma. If you suspect poisoning, you should immediately seek medical help, if less than 4 hours have passed since the moment of poisoning, you can do a gastric lavage.
Interaction with other drugs
If you need to use Ibuclin while taking other drugs, be sure to consult with your doctor. Ibuklin's combination with other nonsteroidal anti-inflammatory drugs, barbiturates, anticonvulsants, rifampicin, hypoglycemic drugs, and hormonal contraceptives should be avoided. Part of ibuprofen may weaken the effect of furosemide, thiazide diuretics, antihypertensive drugs, increase the cytotoxicity of chloramphenicol (chloramphenicol). Combined use with anticoagulants can enhance their effect. Use with potassium-sparing diuretics can cause hyperkalemia. When used together, it is possible to increase the blood concentration of digoxin, phenytoin, methotrexate, lithium. When used with metoclopramide, it is possible to increase the concentration of paracetamol in the blood. Hepatotoxic effect of both components may be enhanced when taking alcohol.
special instructions
You should avoid the simultaneous use of the drug with other drugs containing paracetamol and / or NSAIDs. When using the drug for more than 5-7 days as prescribed by a doctor, it is necessary to monitor the indicators of peripheral blood and the functional state of the liver. With the simultaneous use of indirect anticoagulants, it is necessary to monitor the indicators of the blood coagulation system. Co-administration of the drug Ibuclin with other NSAIDs should be avoided. In order to avoid possible damaging effects on the liver during the period of taking the drug should not drink alcohol.The drug may distort the results of laboratory tests in the quantitative determination of serum uric acid glucose, 17-keto steroids (the drug must be removed 48 hours before the study). Influence on the ability to drive vehicles and control mechanisms. During the period of treatment, the patient should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.