Nurofen Express Gel 5% 50g
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Active ingredients
Ibuprofen
Release form
Gel
Composition
Gel for external use is transparent or slightly opalescent, colorless, homogeneous, with a characteristic odor of isopropyl alcohol. 100 g ibuprofen 5 g. Excipients: gietellose - 1. 8 g, sodium hydroxide QS - 0. 93-1 g, benzyl alcohol - 1 g, isopropanol - 5 g, purified water - 86. 2 g
Pharmacological effect
Absorption - high, connection with plasma proteins (mainly albumin) - more than 90%. A high degree of protein binding results in a relatively low volume of distribution (0.1 L / kg). Although ibuprofen is actively associated with albumin, it does not affect drug interactions. The time to reach maximum plasma concentration Ttah - 1-2 hours. The half-life is 2 hours. In the elderly (over 65 years), the half-life of the drug is increased, the total clearance is reduced. According to some data, babies aged 6–18 months have a higher Tmax (3 hours). It is believed that in children the half-life of ibuprofen does not differ significantly from the value established for adults. Eating slows down the absorption of ibuprofen, but does not reduce its bioavailability. When taken with food, Tmax is increased by 30-60 minutes compared with fasting and is 1.5-3 hours. Ibuprofen slowly penetrates into the cavity of the joints, is retained in the synovial tissue, creating in it greater concentrations than in the plasma; The maximum concentration is observed after 5-6 hours after administration. Cerebrospinal fluid shows lower concentrations of ibuprofen compared to plasma. After absorption, about 60% of the pharmacologically inactive R-form slowly transforms into the active S-form in the gastrointestinal tract and liver. It is metabolized in the liver to form 4 metabolites. Excreted by the kidneys (70-90% of the administered dose in the form of ibuprofen and its metabolites; in unchanged form, no more than 1%) and, to a lesser extent, with bile (less than 2%). Excretion of metabolites with urine usually ends 24 hours after the last dose. The total excretion of ibuprofen and its metabolites in the urine is linearly dependent on the dosage. At the age of 2 months, the kidneys are well developed enough to cope with the elimination of ibuprofen by glomerular filtration. The study, which included 49 children aged 3 months to 12 years, showed no age-dependent differences in the rate of absorption and elimination of ibuprofen.
Pharmacokinetics
The drug belongs to nonsteroidal anti-inflammatory drugs (NSAIDs). Nurofen has anesthetic, antipyretic and anti-inflammatory effect. Indiscriminately blocks TsOG1 and TsOG2. The mechanism of action of ibuprofen is due to inhibition of the synthesis of prostaglandins - mediators of pain, inflammation and hyperthermic reaction. A decrease in temperature during fever begins 30 minutes after ingestion, its maximum effect is manifested after 3 hours. The leading analgesic mechanism is the reduction of prostaglandin production of classes E, F and I, biogenic amines, which leads to the prevention of the development of hyperalgesia at the level of changes in the sensitivity of nociceptors. The analgesic effect is most pronounced inflammatory in nature. The analgesic effect is felt within 15 minutes after taking ibuprofen. Anti-inflammatory effect due to inhibition of cyclooxygenase (COX) activity. As a result, the synthesis of prostaglandins in inflammatory foci. This leads to a decrease in the secretion of inflammatory mediators and a decrease in the activity of the exudative and proliferative phases of the inflammatory process.
Indications
Muscle pain, back pain, arthritis, ligament damage, sprains, sports injuries, inflammation and neuralgia.
Contraindications
Bronchial asthma, urticaria, rhinitis, triggered by the administration of acetylsalicylic acid (salicylates) or other NSAIDs. children's age up to 12 years. hypersensitivity to the components of the drug or to other NSAIDs. The drug is used with caution in case of concomitant diseases of the liver or kidneys, the gastrointestinal tract, as well as in the urticaria, rhinitis, or in the polyps of the mucous membrane of the nasal cavity, during pregnancy and during lactation.
Precautionary measures
Nurofen is prescribed with caution in patients with heart failure, arterial hypertension, blood clotting disorders, and renal and / or liver function disorders. Care should be taken when using the drug in patients with bronchial asthma and other obstructive pulmonary diseases due to the risk of bronchospasm. Patients with diseases of the gastrointestinal tract (ulcerative colitis, Crohn's disease) should be carefully prescribed NSAIDs due to the possible exacerbation of these diseases.With caution, the drug is prescribed for elderly patients, since they more often have adverse side effects on NSAIDs, mainly gastrointestinal bleeding and perforation, which can lead to a sharp deterioration. Patients with gastrointestinal toxicity in history, especially elderly patients, should report any unusual abdominal symptom (especially gastrointestinal bleeding), especially if the symptom is observed at the initial stage of taking the drug. If patients with gastrointestinal bleeding develop on the background of the drug, it is urgent to stop taking the drug. The simultaneous use of Nurofen and other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided. Systemic lupus erythematosus, as well as mixed connective tissue diseases contribute to an increased risk of aseptic meningitis. There is some evidence that drugs that inhibit the synthesis of cyclogenase / prostaglandins can cause impaired fertility in women, affecting ovulation. This phenomenon is reversible with drug withdrawal. The drug should not be administered to patients with fructose intolerance, with the syndrome of glucose-galactose malabsorption or sucrase-isomaltase deficiency. Two Nurofen pills contain 25.3 mg of sodium, which should be taken into account in patients who are on a controlled sodium diet. During long-term treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys. When symptoms of gastropathy appear, a careful monitoring is shown, including esophagogastroduodenoscopy, complete blood count (hemoglobin determination), fecal occult blood test. If necessary, determine the 17-ketosteroids drug should be canceled 48 hours before the study. Patients should refrain from all activities related to driving and working with moving machinery, as well as from other potentially dangerous activities related to concentration and increased speed of psychomotor reactions. During the period of treatment should refrain from the use of alcoholic beverages.When used in children aged 6 to 12 years, it should be borne in mind that pills can not be divided, and therefore can be used only in those children who have a single dose of at least 1 tablet.
Use during pregnancy and lactation
Use of the drug during pregnancy is possible only under the supervision of a physician. Use of the drug during the I and II trimesters is undesirable, but possible with caution. If Nurofen is used by a woman who is planning a pregnancy, or by a woman in the I and II trimester of pregnancy, then the smallest effective dose and short periods of treatment should be chosen. Use during the III trimester is contraindicated. The use of the drug during lactation is not recommended. In a number of studies, ibuprofen has been found in breast milk at very low concentrations, and its effect on infants is unlikely.
Dosage and administration
Outwardly. Adults and children over 12 years. On 4-10 cm of the drug (equivalent to 50-125 mg ibuprofen) apply to the skin and rub until completely absorbed.
Side effects
Slight redness of the skin, burning sensation or tingling at the site of application of the gel. Very rarely (in case of hypersensitivity to the components of the drug) - allergic reactions, bronchospasm. If you experience side effects, you should stop taking the drug and consult a doctor.
Overdose
Symptoms: abdominal pain, nausea, vomiting, lethargy, headache, tinnitus, metabolic acidosis, coma, acute renal and hepatic failure, gastrointestinal bleeding, low blood pressure (BP), bradycardia, tachycardia, atrial fibrillation, arrest respiration, increased prothrombin time, seizures are rarely possible. Treatment: during the first hour after taking the drug, gastric lavage and taking activated carbon. Alkaline drink, forced diuresis, and symptomatic therapy are also recommended. In the case of frequent or prolonged seizures, it is necessary to use anticonvulsant drugs (diazepam or lorazepam intravenously).
Interaction with other drugs
It is not recommended to take NUROFEN pills with acetylsalicylic acid (aspirin) at the same time, if taking low-dose aspirin (not exceeding 75 mg per day) is not recommended by the doctor, since it increases the risk of adverse side effects. When taken simultaneously, ibuprofen can inhibit the effects of low doses of aspirin on platelet aggregation.You should also avoid taking two or more NSAIDs at the same time, including selective cyclooxygenase-2 inhibitors, as this may increase the risk of side effects. When administered with anticoagulant and thrombolytic drugs (alteplazy, streptokinase, urokinase), the risk of bleeding increases at the same time. Cefamendol, cefaperazon, cefotetan, valproic acid, plicamycin, increase the incidence of hypoprothrombinemia. Cyclosporine and gold preparations increase the effect of ibuprofen on the synthesis of prostaglandins in the kidneys, which is manifested by an increased risk of nephrotoxicity. Ibuprofen increases the plasma concentration of cyclosporine and the likelihood of its hepatotoxic effects. Do not use NSAIDs for 8-12 days after taking mifepristone, as NSAIDs can reduce the effect of mifepristone. At the same time taking NSAIDs and tacrolimus may increase the risk of nephrotoxicity. At the same time taking NSAIDs and zidovudine increases the risk of hematological toxicity. Patients taking NSAIDs and quinolones, increases the risk of seizures. Drugs that block tubular secretion, reduce excretion and increase the plasma concentration of ibuprofen. Inductors of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of developing severe hepatotoxic reactions. Inhibitors of microsomal oxidation - reduce the risk of hepatotoxic action. Reduces the hypotensive activity of vasodilators, natriuretic in furosemide and hydrochlorothiazide. Reduces the effectiveness of uricosuric drugs, enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics. Strengthens the side effects of mineral corticosteroids, glucocorticosteroids, estrogens, ethanol. Enhances the effect of oral hypoglycemic drugs, sulfonylurea derivatives and insulin. Antacids and colestyramine reduce absorption. Increases blood concentration of digoxin, lithium preparations, methotrexate. Caffeine enhances the analgesic effect.