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Instructions for medical use of
ASPIRIN® C
Trade name
Aspirin® C
International nonproprietary name
No
Dosage form
Effervescent tablets
Composition
1 effervescent tablet includes:
active substance: acetylsalicylic acid 400 mg, ascorbic acid (Vitamin C) 240 mg;
adjuvants: anhydrous sodium citrate, sodium carbonate, anhydrous acidum citricum, anhydrous sodium carbonate.
Description
White round flat tablets with intagliation in the form of Bayer’s firm cross on one side and even surface on the other side.
Pharmacotherapeutic group
Drugs for treatment of diseases of nervous system. Analgesics. Analgesics- alexipyretics other.Salicylic acid and its derivatives. Acetylsalicylic acid in combination with other drugs (except for neuroleptics).
Code АТХN02BA51
Pharmacological properties
Pharmacokinetics
In case of ingestion acetylsalicylic acid is quickly absorbed from gastrointestinal system. Food in stomach significantly changes absorption of acetylsalicylic acid. Acetylsalicylic acid is distributed in the most tissues and liquid fluids of body. It passes through hematoencephalic barrier (HEB).
Acetylsalicylic acid is metabolized in liver by means of hydrolysis with formation of salicylic acid with further conjugation with glycine or glucuronid. About 80% of salicylic acid is bounded with plasma protein.
Effective half-life (Т1/2) of acetylsalicylic acid is about 15 min, salicylic acid – about 3 h.
It is excreted by kidney mainly in the form of salicylic acid.
After ingestion ascorbic acid is absorbed in small intestine with participation of sodium-dependent transfer system; absorption is not proportional to given dose. Maximal concentration (Сmax) after ingestion is reached in 4 hours.
It easily penetrates in leucocytes, thrombocytes, then in all tissues; it is deposited in neural lobe of hypophysis, suprarenal cortex, liver, brain, lungs, kidneys, intestinal wall, heart, muscles, spleen, pancreatic gland. It is metabolized mainly in liver. Main metabolites of ascorbic acid are excreted with urine.
Pharmacodynamics
Acetylsalicylic acid (ASA) is referred to group of non-steroidal anti-inflammatory drugs (NAID) and has anaesthetic, antipyretic and antiphlogistic action as well as inhibits thrombocyte aggregation. Action mechanism is connected with inhibition of activity COX – the main ferment of metabolism of arachidonic acid being a precoursor of prostaglandins that take the main part in pathogenesis of inflammation, pain and fever.
Analgesic effect of acetylsalicylic acid is based on two mechanisms: peripheral (indirectly, through inhibition of prostaglandin synthesis) and central (based on inhibition of prostaglandin synthesis in central and peripheral nervous system). As a result of decrease in production of prostaglandins, their influence on heat regulating centers are decreased.
Irreversible damage of synthesis in thrombocytes of thromboxane А2 leads to antiplatelet action of acetylsalicylic acid. In case of use in increased doses ASA can inhibit synthesis of proserosyme in liver and increases prothrombin time.
Ascorbic acid is a water-soluble vitamin, it takes an important part in regulation of oxidation-reduction processes, carbohydrate metabolism, blood coagulability, tissue regeneration, supports increase in body resistance.
Ascorbic acid is a component part of system protecting body from harmful influence of free radicals and other oxidants of exogenous and endogenous nature that takes an important part in inflammatory processes and function of leucocytes.
Ascorbic acid takes an important part in process of synthesis of endocellular mucopolysaccharides that provide strength of capillar walls.
Dosage and methods of use
Ingest.
Effervescent tablet shall be dissolved in cup of water and drink.
In case of pain syndrome of weak and average intensity and febricity, single dose is 1-2 effervescent tablets with interval of 4-8 hours.
Maximal single dose – 2 effervescent tablet.
Maximal daily dose shall not exceed 10 effervescent tablets.’
Adverse reaction
Gastro-intestinal tract
Frequent: stomachache, nausea, vomit, hearburn.
Rare: obvious (black bowel movement, bloody vomit) or latent character of gastrointestinal hemorrhage that can lead to asiderotic anemia, erosive and ulcerous damages (including with perforation) of gastro-intestinal tract; compromised liver function (increased liver transaminase).
Blood circulatory system.
Rare: hemorrhagic syndrome (nasal hemorrhage, stomatorrhagia hemorrhage), increase of blood coagulability period, thrombocytopenia, anemia, leucocytopenia, prolonged bleeding time.
immune system.
Rare: skin rash, hypersensitivity of breathing passage (bronchismus), gastro-intestinal tract, heart-vascular system: pressure decrease, labored breathing, rhinitis, nasal congestion, acute anaphylaxis, Quincke's disease.
Central nervous system: headache, faintness, buzzing in ears, amblyacousia, clouding of consciousness.
Urinary condition.
Very rare: interstitial nephritis, prerenal azotemia with increased creatinine in blood and hypercalcemia, acute renal failure, nephrotic syndrome; formation of oxalate, cystine and/or urate calculi.
In case of any adverse reactions it is necessary immediately to stop using the drug and contact with a doctor.
Contraindications
Drug interaction
Due to the fact that anti-inflammatory drugs decrease renal clearance of methotrexate and inhibits binding of methotrexate with plasma protein, combined use of acetylsalicylic acid and methotrexate in dose ≥15 mg per week is contraindicated.
In case of combined use of ASA with anticoagulants (coumarine, heparin) there is an increased risk of bleeding due to dysfunction of thrombocytes and damage of mucous of gastro-intestinal tract.
Due to reciprocal gain of effect during use with large doses (3 ≥ g/day) of other NSAID including salycylates, there is an increased risk of ulcerous damages and gastrointestinal hemorrhage.
In case of combined use with uricosuric drugs (benzbromarone, probenecid), there can be marked decrease of uricosuric effect (in connection with certain excretion ofuric acid by kidney).
ASA increases concentration of digoxin in blood plasma.
High doses of ASA enhances hypoglycemic effect of antidiabetic medication (insulin, sulfonylurea medications). In case of combined use of acetylsalicylic acid in doses ≥ 3 g/days with diuretics there is marked decrease of glomerular filtration (in connection with decrease of synthesis of prostaglandin by kidneys).
System glucocorticoids (except forhydrocortisone used in replacement therapy during Addison disease) decreases concentration of salycylates in blood plasma that increases risk of overdosage of salycylates after termination of treatment by glucocorticosteroids.
During combined use of ASA in doses≥ 3 g/day and inhibitors of angiotensine transforming enzyme (ATE) there is a marked decrease of glomerular filtration of inhibitors of ATE that is accompanied by decrease of their antihypertensive action.
ASA increases poisonous effect of valproic acid.
Alcohol used with ASA increases bleeding time and damaging effect of acetylsalicylic acid on mucous membrane of gastrointestinal system.
Ascorbic acid increases blood concentration ofsalycylates (increases risk of crystalluria), ethinylestradiol, benzylpenicillin and tetracyclines, decreases effect of oral contraceptives.
It decreases anticoagulation effect of coumarin derivatives.
It improves absorption in ferrum drugs in intestine.
During long use quinolinic drugs, calcium chloride, salicylate, corticosteroids drain reserves of ascorbic acid.
Simultaneous use of vitamin C and deferoxamine increases tissue toxicity of ferrum, especially in myocard that can lead to circulatory decompensation.
Antacids containing magnesium hydroxide and/or aluminium hydroxide slow down and decrease ASA absorption.
Special indications
Acetylsalicylic acid should be used with care:
- in case of increased sensibility to analgesics, antiphlogistics and antirheumatic drugs, in case of other type hypersensitivity;
- in case of ulcer disease of stomach and/or duodenum, erosive gastritis and tendency to gastrointestinal hemorrhage;
- in case of concomitant treatment by anticlotting agents;
- in case of dysfunction of liver, kidney and heart-vascular system (peripheral vascular disease of liver, chronic cardiac failure, dehydration, sepsic or extensive hemorrhagic events), because ASA will lead to risk of renal disorder and development of acute renal failure.
- ASA can lead to bronchospasm, bronchial asthmatic attack or other reactions of increased sensibility. Risk factors: availability of bronchial asthma in anamnesis, hay fever, nasal polyps, chronic bronchopulmonary diseases, cases of allergy in anamnesis.
Possibility of acetylsalicylic acid to inhibit platelet aggregation can lead to increased bleeding during and after surgery (including small, for example tooth extraction). Bleeding risk is increased in case of use of high doses of ASA.
Low doses of ASA decrease extraction of uric acid that lead to development of gout of patients with low level of its extraction that can be reason of acute fit of gout of predisposed patients.
The drug should not be prescribed as febrifuge agent to children and teen-agers under 18 years with acute respiratory disease caused by virus infections due to risk of development of Reye's syndrome.
ASA can provoke hemolysis or hemolytic anemia of patients with deficit of glucose-6-phosphate dehydrogenase. Contributing factors: high dose, fever and acute infection.
Patients with aptitude to nephrolithiasis connected with calcium oxalate or recurrent nephrolithiasis should be care during use of vitamin C.
The drug includes sodium that should be taken into account by patients having low-salt diet.
Pregnancy and lactation period
Inhibition of synthesis of prostaglandins can exert negative influence on pregnancy and/or embryo/ fetal development.
Use of salycylates in the first 3 months of pregnancy can be connected with increased frequency of defects of fetal development (fissured palate, cardiac defect). However in case of use of the drug according to therapeutic dose, risk of birth defects of fetal development is low. In the last trimester of pregnancy, salycylates in high dose (above 300 mg/day) lead to slowdown of act of delivery, its prolongation, early closing of ductus arteriosis of fetus, increased bleeding of mother and fetus, and prescription before act of delivery can lead to intracerebral bleeding, especially for prematurely born children.
In II trimester of pregnancy salycylates can be prescribed only taking into account serious assessment of risks and benefits.
Some salycylates and its metabolites are excreted with breast milk. Accidental use of salycylates during lactation does not lead to adverse reaction of children and not require termination of breast feeding. However in case of long use of the drug and prescription of high doses it is required to stop breast feeding immediately.
Effects on ability to drive and use potentially dangerous machines
No effect.
Overdosage
Symptoms: singing in the ears, hearing decrease, headache, vertigo. Fever, hyperventilation, ketose, respiratory alkalosis, metabolic acidosis, coma,circulatory collapse, respiratory insufficiency, expressed hypoglycaemia can appear later.
Treatment: it is required to vomit or to have gastric lavage, to prescribe absorbent carbon and apocathartic. Further treatment shall be performed specialized department.
Form of output and packing
2 tablets in paper blister made of paper laminated by aluminium foil.
5 blisters with medical use instruction in Kazakh and Russian are placed in cardboard package.
Storage conditions
Do not store above 25 °C.
Keep out of the reach of children!
Shelf life
3 years.
Do not use after the expiration date indicated on the package.
Conditions for drug supply
Over the counter
Manufacturer/ Packager
Bayer Bitterfeld GmbH
OT Greppin, Salegaster Chaussee 1, 06803 Bitterfeld-Wolfen, Germany.
Name and country of the Registration Certificate holder
Bayer Consumer Care AG, Switzerland
Name, address and contact data of the organization receiving claims (offers) from consumers regarding the quality of products on the territory of the Republic of Kazakhstan
“Bayer KAZ” LLP.
Timiryazev Street, 42, Pav. 15, Off. 301
050057 Almaty, Republic of Kazakhstan
Tel: +7 727 258 80 40, fax: +7 727 258 80 39
e-mail: kz.claims@bayer.com
Name, address and contact data of the organization responsible for post approval supervision over drug safety on the territory of the Republic of Kazakhstan
“Bayer KAZ” LLP.
Timiryazev Street, 42, Pav. 15, office 301
050057 Almaty, Republic of Kazakhstan
Tel: +7 701 715 78 46(round the clock)
Tel.: +7 727 258 80 40 (ext. 106) (during working hours)
Fax: +7 727 2588 039
e-mail: pv.centralasia@bayer.com
