ACETILYN. 500 mg. 100 tablets
- Anti-inflammatory agent in rheumatoid arthritis, neuritis, polyneuritis .
ACETILYN. 500 mg. 100 tablets
- Symptomatic treatment of colds with fever and mild to moderate pain : neuralgia, toothache , headache, migraine;
- Anti-inflammatory agent in rheumatoid arthritis , neuritis, polyneuritis ;
- In low-dose antiplatelet agent such as for prophylaxis of infarction and post-myocardial infarction ;
- Prevention nasledoperativni thrombosis.
4.2 . Dosage and method of administration
Tablets should be taken during or after a meal , with more liquid.
- Having analgesic and antipyretic agent - 1-2 500 mg tablets , 3 times daily . DMD - 3 g.
- Having an anti-inflammatory agent - 2 tablets of 500 mg 3 times daily.
- As an antiplatelet agent - 1/2 tablet daily.
For children over 12 years:
- As an analgesic and antipyretic -1 / 2 to 1 tablet daily as needed.
- Having an anti-inflammatory agent - 1 500 mg 3 times daily.
4.3 . Contraindications
- Hypersensitivity to salicylates or to any component of the formulation ;
- Gastric and duodenal ulcers ;
- Bleeding diathesis , thrombocytopenia , hemophilia ;
- Renal failure and oxaluria ;
- Children under 12 years of age.
Caution should be used in :
- Known hypersensitivity to other NSAIDs ;
- Bronchial asthma , nasal polyps , allergic diseases, and atopy ;
- Genetically determined glucose- 6-phosphate dehydrogenase deficiency ( hemolytic anemia) ;
- Gastrointestinal disease (e.g., gastritis ) ;
- Liver and / or kidney disease.
4.4 . Special warnings and special precautions for use
Additional use of salicylates or other NSAIDs should be avoided . Administration of acetylsalicylic acid for many years can lead to kidney damage . It is necessary to regularly check kidney function.
Taking aspirin in children and adolescents up to 12 years with febrile illness associated with dangerous complications ( Reye's syndrome ) . Prolonged vomiting , dehydration, impaired consciousness , seizures requiring immediate intensive care . It is recommended to restrict the use of aspirin in children under 12 years. Acetylsalicylic acid in children can be used only on specific prescription.
There is a correlation between hypersensitivity to acetylsalicylic acid and natural penicillins . Chronic ingestion of alcohol increases the risk of stomach bleeding while taking aspirin . The composition of Atsetilin one of the ingredients is wheat starch. It may be dangerous for patients with celiac disease (gluten enteropathy ) .
4.5 . Interactions
Coadministration of Atsetilin with other drugs can lead to an increase or a decrease in their effects.
- The effect of anticoagulant and antithrombotic drugs (eg coumarin derivatives , heparin, dipyridamole and sulfinpyrazone ) ;
- The risk of bleeding from the gastrointestinal tract after coadministration of glucocorticoids or alcohol;
- Wanted and unwanted effects of NSAIDs ;
- Hypoglycaemic effect of sulphonylureas ;
- Desirable and undesirable effects of methotrexate.
Atsetilin weakened :
- The effect of spironolactone and furosemide ;
- The effect of uricosuric agents ( probenecid , sulfinpyrazone ) .
- In doses of 1-2 g per day of the antihypertensive effect of captopril, especially in patients with low-renin .
Concomitant use of antacids , H2 blockers and anticholinergics decrease the absorption of Atsetilin . Concurrent administration of tetracyclines may lead to the formation of complexes nonabsorbable . Therefore, it should be an interval of at least 1-3 hours between the various drugs.
4.6 . Pregnancy and lactation
Not recommended to Atsetilin in III- quarter of pregnancy because it may cause prolongation of bleeding time and maternal deteto.Prez first 6 months of pregnancy and during lactation Atsetilin should be administered in the lowest possible doses once daily and only after careful evaluation of the risk / benefit and under strict pokazaniya.Neobhodimo breastfeeding during the implementation of Atsetilin be discontinued.
4.7 . Effects on ability to drive and operate machinery.
No effect on ability to drive and use machines.
4.8 . Undesirable effects
- Hypersensitivity reactions (urticaria , angioedema followed by asthma) ;
- Stomach upset (nausea, vomiting , dyspepsia , abdominal pain) ;
- Occult bleeding from the gastrointestinal tract, which in rare cases can lead to anemia;
- Prolongation of bleeding time ;
- Provoking an asthma attack. In asthmatic patients sensitivnostta expressed with bronchoconstriction and is most frequently associated with nasal polyps . The correlation between hipersensitivnost aspirin , asthma and nasal polyps is known as aspirin triad ;
- Thrombocytopenia and aplastic anemia ;
- Reversible reduction in renal blood flow ;
- Prolonged high doses can be associated with kidney and liver damage - high doses can lead to dizziness , tinnitus or ulceration of the gastrointestinal tract with bleeding ;
- Reye's syndrome .
4.9 . overdose
An overdose of aspirin with symptoms of irritation of the gastrointestinal tract - nausea , vomiting , stomach pain, as well as dizziness , headache , confusion, tinnitus and hyperventilation with respiratory alkalosis . In long-standing cases observed CNS depression , pyrexia , respiratory and metabolic acidosis , toxic circulatory and renal failure , cerebral and pulmonary edema , coma . In children is possible and hypoglycemia.
Management of overdose
- Elimination of toxic substances ( careful gastric lavage )
- Monitoring of acid- base balance and electrolyte balance , correction of glucose - intensive medical care ( ventilation , introduction of liquids)
- Speeding up the release ( alkalinity of the urine , forced diuresis , hemodialysis)
- Implementation of diazepam in the presence of seizures.
5 . Pharmacological
ATC code NO2BA01. Other analgesics and antipyretics . Salicylic crab and derivatives.
5.1. Pharmacodynamic properties
Atsetilin analgesic effect occurs mainly against externa - proprioceptive and pain (from a skin oprno joints , teeth ) . There are anti-inflammatory ( anti-rheumatic ) and moderate antipyretic effect . At low doses (50-380 mg) inhibits platelet aggregation. There are a holekinetichen and hypoglycemic ( in diabetics ) effect.
At higher doses stimulate respiration lowers blood prothrombin ( competitive antagonism with vitamin K ) and increases the excretion of uric acid ( uricosuric effect). A major feature of the mechanism of action of a atsetilina inhibition of cyclooxygenase , which leads to blocking of the synthesis endoperoxide , thromboxanes and prostaglandins . The analgesic effect is mainly peripheral mechanism - the lack of prostaglandin endoperoxide reduces sensitivity of sensory nerve endings to Algogenic mediators and exogenous Knox. Furthermore, a role , and to the reduced levels of prostaglandins in the brain , thereby increasing the threshold of the pain sensitivity of the level of the thalamus .
The antiinflammatory effect of atsetilina is determined primarily by inhibiting the synthesis of prostaglandin endoperoxide and at the very site of infection . Also plays a role to stabilize the lysosomal membranes, inhibition of hyaluronidase , decoupling of oxidative phosphorylation and the like.
Its antipyretic action is related to lowering the level of prostaglandin E, and E in the central nervous system are thought to mediate the effects of exogenous and endogenous pyrogens on thermoregulatory center in the hypothalamus. Furthermore atsetilin inhibit the formation , the release and penetration into the CNS of pyrogens themselves , which are obtained from bacterial endotoxins . and neutrophil leukocytes. Impaired synthesis of prostaglandins and leukotrienes increase the amount of the underlying and the side effects of the preparation.
5.2 . pharmacokinetics
Rapidly absorbed from the gastrointestinal tract. The plasma protein is associated with 50-80 %. The plasma half-life ranged from 2 to 4 1/2 hours. Easily passes the blood-brain and placental barriers. Metabolized primarily in the liver. The elimination is carried out mainly via the kidneys in the form of free salicylic acid (85% in alkaline , acidic 10% retention) . Urine excreted 50% of the amount administered in the form of various conjugates and partly unchanged .
5.3 . Preclinical safety data
Acetylsalicylic acid is reacted with DNA in vitro . At low concentrations of interacting with the phosphate groups in the DNA structure and A-T bases . In high concentrations , and is reacted with G- C pairs .
Acetylsalicylic acid was not mutagenic in the Ames Salmonella test. With or without metabolic activation acetylsalicylic acid induces chromosomal aberrations in cultured fibroblasts.
6 . PHARMACEUTICAL PARTICULARS
6.1. List of excipients and their amounts
Microcrystalline cellulose (Cellulose microcrystalline) 47,0 mg
Wheat starch (Wheat starch) 37,0 mg
Stearic acid (Stearic acid) 6,0 mg
Colloidal silica (Silica colloidal anhydrous) 8,0 mg
Talc (Talc) 2,0 mg
6.2 . Incompatibilities
6.3. Expiration date
- Of container PVC / aluminum foil - 5 (five) years;
- Packaging polypropylene bottle tablets x 1000 - 3 (three) years.
The product should not be used after the expiry date stated on the packaging.
6.4 . Special precautions for storage
Store in original container in a dry place protected from light at temperatures below 25 ° C.
Keep out of reach children!
6.5. Packaging Data
6.5.1 . primary packaging
• 10 tablets in blister PVC but foil / aluminum foil.
6.5.2 . secondary packaging
• 2 blisters of 10 tablets per carton.
• 50 blisters of 10 tablets per carton (500 tablets) - for hospital use.
• 1000 tablets in a polypropylene - for hospital use.