Upsarin Upsa exhibits analgesic, anti-inflammatory, antipyretic, antiagregatnoe action. Acetylsalicylic acid is a non-negotiable due to inhibition of cyclooxygenase enzyme inhibits the biosynthesis of prostaglandins. At the site of inflammation reduces the permeability of the capillaries, reduces the activity of hyaluronidase, limits the energy security of inflammation by inhibiting the production of ATP. Reduces arousal centers of thermoregulation and pain sensitivity, reduces algogenov action of bradykinin. Furthermore, acetylsalicylic acid inhibits platelet aggregation by blocking the platelet thromboxane A2 synthesis.
The drug is available in the form of effervescent tablets buffering properties, which reduces the irritant effect of acetylsalicylic acid on the mucosa of the gastrointestinal tract.
Soluble effervescent tablets of the drug are absorbed faster than conventional tablets. Maximum concentration of acetylsalicylic acid in the blood plasma after 15-40 minutes after administration. Bioavailability acetylsalicylic acid varies depending on the dose: it is approximately 60% less than when receiving 500 mg and 90% - at receiving more than 1 g due to saturation of hydrolysis in the liver. Aspirin is rapidly hydrolyzed to form salicylic acid, which also has a pharmacological activity. Acetylsalicylic acid and salicylic acid is rapidly distributed throughout the body. These acids cross the placental barrier and get into the breast milk. Salicylic acid is extensively bound to plasma proteins (90%). Plasma half-life of aspirin is 15-20 minutes, and salicylic acid - 2-4 hours.
Acetylsalicylic acid is metabolized primarily in the liver and excreted primarily in the urine as salicylic, salitsilurovoy, gentesovoy acids and glucuronides.
Indications for use
• Pain weak and moderate intensity in infectious and inflammatory diseases (influenza, acute respiratory disease), as well as neurology, basic and toothache;
• hyperthermic response of different origins;
• rheumatic diseases;
• prevention of thrombosis, thromboembolism, myocardial infarction and ischemic stroke.
The method of use and dosage.
The tablet was dissolved in a glass of water immediately before use.
Adults: the recommended dosage by ½ - 1 tablet at the reception, where appropriate technique can be repeated, but the daily dose should not exceed 3 g (6 tablets), the interval between doses - at least 4 hours. When intense pain or hyperthermia for admission of two tablets every 4 hours but not more than 6 tablets per day.
Elderly: daily dose of 2g per day of acetylsalicylic acid, i.e. 4 tablets usually administered one tablet of 500 mg at intervals of at least 4 hours but not more than 4 tablets Upsarin Upsa 500 night.
Children: 9 years weighing 30 kg, the daily dose should not exceed 50 mg / kg body weight. The drug may be administered to children weighing at least 30 kg (usually 9 years), with an interval between doses of 6 to 4 hours.
Patients should know that without a doctor's advice to take acetylsalicylic acid can be no more than 3 days for treatment gipertermichnoy reaction and not more than 5 days for the treatment of pain.
On the part of the digestive system: in some cases - nausea, anorexia, abdominal pain, erosive and ulcerative changes of gastric mucosa and other parts of the gastrointestinal tract, gastro-intestinal bleeding.
On the part of the hemostatic system: possible hemorrhagic syndrome (nosebleeds, bleeding from the gums, hemorrhagic purpura), prolonged bleeding.
Hypersensitivity reactions: urticaria, bronchospasm, angioedema, anaphylaxis.
Intolerance to aspirin or other components of the drug;
phenylketonuria, as the drug comprises aspartame;
bronchial asthma, which is due to taking aspirin or other nonsteroidal anti-inflammatory agents;
the last three months of pregnancy;
aggravation of gastric ulcer and duodenal ulcer;
born or acquired bleeding diathesis;
increased risk of bleeding;
severe hepatic impairment;
severe renal insufficiency;
resistant to the treatment of severe heart failure;
compound with methotrexate at doses exceeding 15 mg / week;
compound with high doses indirect anticoagulants, particularly in the treatment of rheumatic diseases;
children weighing less than 30 kg (under 9 years).
There is a risk of the development of toxicity in the elderly, especially in young children (as in therapeutic applications, and in casual reception). Severe intoxication can cause death.
Symptoms: Intoxication middle stage: tinnitus, hearing loss, headache, dizziness - symptoms disappear when the dose.
Heavy intokcikatsiya: In children there is a threat to life while receiving 100 mg / kg or more, thus there is diarrhea, hyperventilation, respiratory alkalosis, metabolic acidosis, ketosis, hypoglycemia, coma, collapse, respiratory failure.
Treatment: Immediate hospitalization;
gastric lavage and administration of activated charcoal;
monitoring of acid-base balance;
leaching from urine to pH 7, 5 to 8, in severe poisoning may hemodialysis;
Features of use
To prevent overdose, make sure that other drugs that the patient uses do not contain aspirin.
Caution must be adhered to in the appointment of the drug to patients with a history of gastric or duodenal ulcer, as well as gastrointestinal bleeding, patients with bronchial asthma and kidney failure.
Caution must be adhered to in the appointment of the drug to patients who used hypoglycemic agents (required regular monitoring of blood sugar levels), glucocorticoids, antihypertensives, diuretics (to ensure adequate hydration of the patient and monitoring of kidney function), antacids that are not absorbed and contain magnesium hydroxide and / or aluminum (they must be taken no earlier than 2 hours after dosing).
Patients who are on sodium-free diet, it should be remembered that each tablet formulation contains 388 mg of sodium 5.
In children younger than 12 years with viral infections (chickenpox, flu-like infection) while taking aspirin and in rare cases may develop Reye's syndrome, which is unsafe for life, so acetylsalicylic acid should be used in children only a doctor when other means are not effective.
During pregnancy (in I and II trimesters) possible single dose of the drug.
Lactation. Aspirin passes into breast milk, so use the drug during lactation is inappropriate.
Interactions with other drugs. The combinations that are contraindicated.
Oral anticoagulants. Upon receipt of acetylsalicylic acid in a dose of 3 g / day anticoagulants extruded with compounds to plasma proteins.
Methotrexate at doses exceeding 15 mg / week. Increases myelotoxic effect.
Oral anticoagulants. Increased risk of bleeding, you need to monitor the performance of blood clotting, and especially the duration of bleeding.
Other non-steroidal anti-inflammatory drugs. Increases the risk of gastric and duodenal ulcers and gastrointestinal bleeding.
Heparin. Increased risk of bleeding (inhibition of platelet function and mucosal lesions of the gastrointestinal tract).
Urikozuricheskie means (benzbromarone, probenecid). Reduced urikozurichesky effect due to competition for the excretion of uric acid in the renal tubules.
Combinations that need to be cautious.
Antidiabetics (insulin). Strengthening the hypoglycemic action.
Diuretics and ACE inhibitors. When taken in large doses may develop acute renal failure in patients with dehydration (decreased glomerular filtration through inhibition of prostaglandin synthesis, also reduced the hypotensive effect).
Glucocorticoids (for systemic use) decrease in the concentration of salicylates in the blood during treatment with corticosteroids and the risk of an overdose of salicylates after their withdrawal (corticosteroids increase the excretion of salicylates).
Methotrexate at doses below 15 mg / week. Risk of myelotoxicity.
Combinations to be taken into account.
Intrauterine devices. Reduce the risk of contraceptive effect.
Gastrointestinal topical agents: oxides and hydroxides of magnesium, aluminum, calcium salt. Increased excretion of salicylates kidneys through urine leaching.