Anopyrin

February 21, 2021 by No Comments

Indications for use

Anopyrin - Rheumatism, rheumatoid arthritis, infectious-allergic
Anopyrin – Rheumatism, rheumatoid arthritis, infectious-allergic

Anopyrin – Rheumatism, rheumatoid arthritis, infectious-allergic myocarditis, pericarditis, rheumatic chorea – not currently used.

Febrile syndrome in infectious-inflammatory diseases.

Pain syndrome (various genesis): headache (including those associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, lumbago, thoracic radicular syndrome, myalgia, arthralgia, algodysmenorrhea.

As an antiplatelet drug (doses up to 300 mg/day): CHD, presence of multiple risk factors for CHD, myocardial ischemia without pain, unstable angina pectoris, myocardial infarction (to reduce risk of recurrent myocardial infarction and death after myocardial infarction), recurrent transient brain ischemia and ischemic stroke in men, prosthetic heart valves (prevention and treatment of thromboemboli), Coronary balloon angioplasty and stent placement (reducing the risk of recurrent stenosis and treatment of secondary coronary artery dissection), in non-atherosclerotic coronary artery disease (Kawasaki disease), aortoarteritis (Takayasu disease), Valve mitral heart defects and atrial fibrillation, mitral valve prolapse (thromboembolism prevention), recurrent pulmonary embolism, pulmonary infarction, acute thrombophlebitis, Dressler syndrome.

In clinical immunology and allergology: in gradually increasing doses for long-term “aspirin” desensitization and formation of persistent tolerance to NSAIDs in patients with “aspirin” asthma and “aspirin triad”.

Active ingredient, group

Acetylsalicylic acid, Non-steroidal anti-inflammatory drug (NSAID)

Contraindications

Hypersensitivity; gastrointestinal erosive and ulcerative lesions (acute phase), gastrointestinal bleeding; “aspirin” triad (combination of bronchial asthma, recurrent polyposis of the nose and sinuses and intolerance of ASA and pyrazolone-containing drugs); hemorrhagic diathesis (hemophilia, Willebrand disease, telangiectasias, hypoprothrombinemia, thrombocytopenia, thrombocytopenic purpura); dissecting aortic aneurysm, portal hypertension, vitamin K deficiency, hepatic/renal insufficiency, pregnancy (I and III trimesters), lactation, glucose-6-phosphate dehydrogenase deficiency, childhood (under 15 years – risk of Reye syndrome in children with hyperthermia caused by viral diseases). With caution. Hyperuricemia, urate nephrourolithiasis, gout, liver disease, gastric and/or duodenal ulcer (history), decompensated CHF.

How to use: dosage and course of treatment

Soluble tablets: orally, pre-dissolved in a small amount of water – 400-800 mg 2-3 times a day (not more than 6 g). In acute rheumatism – 100 mg/kg/day in 5-6 doses.

Tablets containing ASK in doses over 325 mg (400-500 mg) are intended for use as an analgesic and anti-inflammatory drug; in doses of 50-75-100-300-325 mg – in adults, mainly as an antiplatelet drug.

Orally, with fever and pain syndrome in adults – 0.5-1 g/day (up to 3 g) divided into 3 doses. The duration of treatment should not exceed 2 weeks.

Effervescent tablets are dissolved in 100-200 ml of water and taken orally, after meals, a single dose of 0.25-1 g, taken 3-4 times a day. Duration of treatment – from a single dose to many months of the course.

To improve blood rheology 0.15-0.25 g / day for several months.

In myocardial infarction, as well as for secondary prevention in patients who have had a myocardial infarction, 40-325 mg once daily (more often 160 mg). As an inhibitor of platelet aggregation – 300-325 mg / day for a long time. In dynamic cerebral circulatory disorders in men, cerebral thromboembolism – 325 mg/day with a gradual increase to a maximum of 1 g/day, for the prevention of recurrences – 125-300 mg/day. For prevention of thrombosis or aortic shunt occlusion, 325 mg every 7 hours through an intranasally placed gastric tube, then orally 325 mg 3 times daily (usually in combination with dipyridamole, which is withdrawn after a week, continuing long-term ASA treatment).

In active rheumatism, a daily dose of 5-8 g was prescribed (not currently prescribed) for adults and 100-125 mg/kg for adolescents (15-18 years old); the frequency of use is 4-5 times a day. After 1-2 weeks of treatment, the dose for children is reduced to 60-70 mg/kg/day, while treatment of adults is continued in the same dose, and the duration of treatment is up to 6 weeks. Discontinuation is carried out gradually over 1-2 weeks.

Pharmacological action

Anopyrin - Rheumatism, rheumatoid arthritis, infectious-allergic
Anopyrin – Rheumatism, rheumatoid arthritis, infectious-allergic

NSAID; has anti-inflammatory, analgesic and antipyretic effects associated with indiscriminate inhibition of COX1 and COX2 activity that regulate Pg synthesis. As a result, Pg is not formed, providing formation of edema and hyperalgesia. Decrease of Pg (mainly E1) in the thermoregulation center results in decrease of body temperature due to dilation of skin vessels and increase of sweating.

The analgesic effect is due to both central and peripheral action.

Reduces aggregation, platelet adhesion and thrombosis by inhibiting the synthesis of thromboxane A2 in platelets. The antiplatelet effect lasts for 7 days after a single dose (more pronounced in men than in women). Reduces mortality and risk of myocardial infarction in unstable angina. Effective in primary prevention of cardiovascular diseases, especially myocardial infarction in men over 40 years old, and in secondary prevention of myocardial infarction.

At a daily dose of 6 g or more suppresses prothrombin synthesis in the liver and increases prothrombin time.

Increases plasma fibrinolytic activity and decreases the concentration of vitamin K-dependent clotting factors (II, VII, IX, X). Increases the frequency of hemorrhagic complications during surgical interventions, increases the risk of bleeding during anticoagulant therapy.

Stimulates excretion of uric acid (disrupts its reabsorption in the renal tubules), but in high doses.

COX1 blockade in the gastric mucosa leads to inhibition of gastroprotective Pg, which may cause mucosal ulceration and subsequent bleeding. Less irritating effect on the mucous membrane of the gastrointestinal tract have drug forms containing buffer substances, enteric coating, as well as special “effervescent” forms of tablets.

Side effects

Nausea, decreased appetite, gastralgia, diarrhea; allergic reactions (skin rash, angioneurotic edema, bronchospasm); impaired hepatic and/or renal function; thrombocytopenia, anemia, leukopenia, Reye syndrome (encephalopathy and acute fatty liver dystrophy with rapid development of liver failure), formation of “aspirin” asthma and “aspirin triad” (combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis and intolerance to ASA and drugs of pyrazolone series) on the basis of the hapten mechanism.

With long-term use – dizziness, headache, vomiting, erosive-ulcerative lesions of the gastrointestinal tract, hypocoagulation, bleeding (including vision disorders, decreased hearing acuity, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with increased blood creatinine and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased CHF symptoms, edema, increased activity of “liver” transaminases.Overdose. Symptoms (single dose of less than 150 mg/kg – acute poisoning is considered mild, 150-300 mg/kg – moderate, more than 300 mg/kg – severe): salicylitis syndrome (nausea, vomiting, tinnitus, visual disturbance, dizziness, severe headache, general malaise, fever – poor prognostic sign in adults). Severe poisoning – central pulmonary hyperventilation, respiratory alkalosis, metabolic acidosis, confusion, drowsiness, collapse, seizures, anuria, bleeding. Initially, central pulmonary hyperventilation leads to respiratory alkalosis – shortness of breath, choking, cyanosis, cold clammy sweat; as intoxication increases, respiratory paralysis and dissociation of oxidative phosphorylation increase, causing respiratory acidosis.

In chronic overdose, plasma concentrations determined correlate poorly with the severity of intoxication. The greatest risk of developing chronic intoxication is noted in elderly people when taking more than 100 mg/kg/day for several days. In children and elderly patients the initial signs of salicylation are not always noticeable, so it is advisable to periodically determine the concentration of salicylates in blood: levels above 70 mg% indicate moderate or severe intoxication; above 100 mg% – extremely severe, prognostically unfavorable. In moderate poisoning, hospitalization for 24 hours is necessary.

Treatment: provocation of vomiting, prescription of activated charcoal and laxatives, constant monitoring of COC and electrolyte balance; depending on the state of metabolism – administration of sodium hydrocarbonate, sodium citrate solution or sodium lactate. Increasing the reserve alkalinity enhances excretion of ASA through alkalinization of the urine. Urine alkalization is indicated when salicylate levels are above 40 mg% and is provided by IV infusion of sodium bicarbonate (88 mEq in 1 liter of 5% dextrose solution, at 10-15 ml/h/kg); restoration of BOD and induction of diuresis are achieved by sodium bicarbonate infusion in the same doses and dilutions, which are repeated 2-3 times. Caution should be exercised in elderly patients in whom intensive fluid infusion may lead to pulmonary edema. The use of acetazolamide to alkalize urine is not recommended (may cause acidemia and increase the toxic effects of salicylates). Hemodialysis is indicated for salicylate levels greater than 100-130 mg%, in patients with chronic poisoning – 40 mg% or lower if indicated (refractory acidosis, progressive deterioration, severe CNS damage, pulmonary edema and renal failure). In case of pulmonary edema – AVI with oxygen-enriched mixture.

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