Instructions for Askofen-L tablets No. 100
Composition
active ingredients: 1 tablet contains acetylsalicylic acid 200 mg, paracetamol 200 mg, caffeine 40 mg;
Excipients: citric acid monohydrate; potato starch; calcium stearate.
Dosage form
Pills.
Main physicochemical properties: solid, regular round cylinders, the upper and lower surfaces of which are flat, the edges of the surfaces are beveled, with a dividing line on one side, white in color. Marbling is allowed on the surface of the tablets.
Pharmacotherapeutic group
Analgesics. Other analgesics and antipyretics. Acetylsalicylic acid, combinations without psycholeptics. ATC code N02B A51.
Pharmacological properties
Pharmacodynamics.
The drug has analgesic, antipyretic and anti-inflammatory effects. The components that make up the drug enhance each other's effects.
The antipyretic effect of acetylsalicylic acid is realized through the central nervous system by inhibiting the synthesis of prostaglandins PGF2 in the hypothalamus in response to the influence of endogenous pyrogens. The analgesic effect has both peripheral and central origin: peripheral effect - inhibition of prostaglandin synthesis in inflamed tissues; central effect - effect on the hypothalamic centers. Acetylsalicylic acid also reduces platelet aggregation.
Paracetamol has analgesic, antipyretic and very weak anti-inflammatory effects, which is associated with its effect on the thermoregulation center in the hypothalamus and its weak ability to inhibit prostaglandin synthesis in peripheral tissues.
Caffeine stimulates the central nervous system. It also enhances positive conditioned reflexes, stimulates motor activity, weakens the effect of hypnotics and narcotics, and enhances the effect of analgesics and antipyretics.
Pharmacokinetics.
Not studied.
Indication
Treatment of mild to moderate pain syndrome: headache, toothache, neuralgia, myalgia, arthralgia, primary dysmenorrhea. As an antipyretic in diseases accompanied by fever.
Contraindication
Hypersensitivity to the components of the drug, hypersensitivity to other xanthine derivatives (theophylline, theobromine), other salicylates;
– history of bronchial asthma, urticaria or rhinitis caused by the use of salicylates or other non-steroidal anti-inflammatory drugs (NSAIDs);
– congenital hyperbilirubinemia, severe renal or hepatic insufficiency, congenital glucose-6-phosphate dehydrogenase deficiency, Gilbert's syndrome;
– blood diseases, hemorrhagic diathesis, hemophilia, hypoprothrombinemia, leukopenia, anemia, increased tendency to bleed, thrombosis, thrombophlebitis, hemorrhagic diseases;
– acute gastrointestinal ulcers; gastrointestinal bleeding; surgical interventions accompanied by significant bleeding;
– severe cardiovascular diseases, including rhythm disturbances, paroxysmal tachycardia, severe atherosclerosis, severe ischemic heart disease, severe heart failure, acute myocardial infarction, severe arterial hypertension, portal hypertension, tendency to vasospasm;
– states of increased arousal, sleep disorders, old age, glaucoma, alcoholism, hyperthyroidism, acute pancreatitis, prostatic hypertrophy, severe forms of diabetes mellitus.
Use simultaneously with monoamine oxidase inhibitors (MAOIs), as well as within 2 weeks after their discontinuation. Combination with methotrexate at a dosage of 15 mg per week or more.
Concomitant use with tricyclic antidepressants or β-blockers.
Interaction with other medicinal products and other types of interactions
Contraindicated combinations.
Methotrexate - when used in combination with salicylates at a dose of 15 mg/week or more, the hematological toxicity of methotrexate increases due to a decrease in the renal clearance of methotrexate by anti-inflammatory agents and its displacement from plasma protein binding, therefore this combination is contraindicated.
MAO inhibitors – when used in combination with caffeine, a dangerous increase in blood pressure is possible, so this combination is contraindicated.
Combinations that should be used with caution.
Paracetamol. Anticonvulsants (including phenytoin, barbiturates, carbamazepine), antidepressants and other microsomal oxidation stimulants - these drugs increase the production of hydroxylated active metabolites that affect liver function, leading to the possibility of severe intoxication with small overdoses of the drug.
With simultaneous use with hepatotoxic drugs, the toxic effect of drugs on the liver increases. Simultaneous use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome.
The rate of absorption of paracetamol may increase when used simultaneously with metoclopramide and domperidone and decrease when used with cholestyramine. Paracetamol reduces the effectiveness of diuretics. Coumarin derivatives (warfarin) increase the risk of bleeding with long-term use of paracetamol. Do not use simultaneously with alcohol.
Under the influence of paracetamol, the half-life of chloramphenicol increases 5 times.
Caffeine. Cimetidine, hormonal contraceptives, isoniazid enhance the effect of caffeine. Caffeine reduces the effect of opioid analgesics, anxiolytics, hypnotics and sedatives, is an antagonist of anesthetics and other drugs that depress the central nervous system (CNS), a competitive antagonist of drugs that depress the CNS, a competitive antagonist of drugs that depress adenosine, ATP. With simultaneous use of caffeine with ergotamine, the absorption of ergotamine from the digestive tract improves, with thyroid-stimulating drugs, the thyroid effect increases. Caffeine reduces the concentration of lithium in the blood. Caffeine increases the effect (improves bioavailability) of analgesics-antipyretics, potentiates the effects of xanthine derivatives, α- and β-adrenomimetics, psychostimulants.
Acetylsalicylic acid. Concomitant use with uricosuric agents such as benzobromarone, probenecid reduces the effect of uric acid excretion (due to competition for uric acid excretion by the renal tubules). With simultaneous use with digoxin, the concentration of the latter in the blood plasma increases due to a decrease in renal excretion. ACE inhibitors in combination with high doses of acetylsalicylic acid cause a decrease in glomerular filtration due to inhibition of vasodilator prostaglandins and a decrease in the hypotensive effect. Selective serotonin reuptake inhibitors: the risk of bleeding from the upper digestive tract increases due to the possibility of a synergistic effect. With simultaneous use with valproic acid, acetylsalicylic acid displaces it from its connection with plasma proteins, increasing toxicity.
The drug enhances the effect of agents that reduce blood clotting and platelet aggregation, the side effects of corticosteroids, sulfonylureas, and methotrexate.
Combination with barbiturates, anticonvulsants, salicylates, rifampicin, and alcohol should be avoided.
Application features
You should consult a doctor before using the medicine.
Do not use the drug with other products containing paracetamol or acetylsalicylic acid.
Do not exceed the indicated doses of the drug. For short-term use.
The drug should be used with caution in patients with a history of gastrointestinal ulcers, including chronic or recurrent peptic ulcer disease or a history of gastrointestinal bleeding; concomitant use of anticoagulants.
Patients with impaired kidney and liver function should consult a doctor regarding the possibility of using the drug.
Patients with liver and kidney dysfunction should reduce the dose of the drug or increase the interval between doses. In case of impaired kidney and liver function, the interval between doses should be at least 8 hours.
Since acetylsalicylic acid, like all non-selective non-steroidal anti-inflammatory drugs, causes irritation of the mucous membrane of the digestive tract, the drug should be taken only after meals, washed down with water, alkaline mineral waters, sodium bicarbonate solution (preferably milk).
With prolonged use of the drug, it is necessary to check for the presence of blood in the stool to detect ulcerogenic effects and perform blood tests (effect on platelet aggregation, some anticoagulant activity).
In case of hyperthermia, the drug should be prescribed only if other analgesics and antipyretics are ineffective, as there is a risk of developing Reye's syndrome. If vomiting occurs as a result of using the drug, Reye's syndrome should be suspected.
It should be noted that patients with alcoholic liver disease are at increased risk of hepatotoxicity from paracetamol. The drug may affect laboratory results for blood glucose and uric acid.
Liver disease increases the risk of liver damage from paracetamol. The risk of overdose is higher in patients with non-cirrhotic alcoholic liver disease.
Patients with severe infections such as sepsis, which are accompanied by a decrease in glutathione levels, are at increased risk of metabolic acidosis when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or difficult breathing, nausea, vomiting, loss of appetite. You should seek immediate medical attention if these symptoms occur.
During surgical operations (including dental), the use of drugs containing acetylsalicylic acid increases the likelihood of bleeding, which is due to the inhibition of platelet aggregation for some time after the use of acetylsalicylic acid. The use of the drug should be discontinued 5-7 days before surgery (to reduce the risk of increased bleeding).
The patient must inform the doctor in advance about taking Askofen L.
In patients with allergic complications, including bronchial asthma, allergic rhinitis, urticaria, skin itching, mucosal edema and nasal pollinosis, as well as in combination with chronic respiratory tract infections and in patients with hypersensitivity to nonsteroidal anti-inflammatory drugs, bronchospasm or an attack of bronchial asthma may develop, therefore the use of NSAIDs in this category of patients is contraindicated.
Acetylsalicylic acid, which is part of the drug, even in small doses can reduce the excretion of uric acid from the body, which can cause an acute attack of gout in sensitive patients.
Since acetylsalicylic acid causes irritation of the mucous membrane, the drug should not be used in children due to the risk of developing Reye's syndrome. In patients with bronchial asthma, allergic diseases, hypersensitivity to NSAIDs, an allergic reaction or exacerbation of the underlying disease is possible.
During treatment with the drug, it is not recommended to consume excessive amounts of beverages containing caffeine (e.g. coffee, tea). This may cause sleep disturbances, tremors, feelings of tension, irritability, and an unpleasant feeling behind the chest due to palpitations.
Do not drink alcoholic beverages during treatment (increased risk of gastrointestinal bleeding).
Patients should consult a doctor if they take analgesics every day for mild arthritis; if they use warfarin or similar drugs that have an anticoagulant effect, as well as when using Askofen L before starting to take ibuprofen as a painkiller.
Do not use in case of hypersensitivity to analgesics, anti-inflammatory, antirheumatic drugs. Use with caution in combination with anticoagulants, as well as in patients with circulatory disorders (e.g. renal vascular pathology, congestive heart failure, hypovolemia, major surgery, sepsis or severe bleeding), since acetylsalicylic acid also increases the risk of renal dysfunction and acute renal failure. Ibuprofen may reduce the inhibitory effect of acetylsalicylic acid on platelet aggregation.
The drug may affect the results of laboratory tests for blood glucose and uric acid.
It is not recommended to use Askofen L without consulting a doctor for more than 5 days as an analgesic and more than 3 days as an antipyretic.
If symptoms persist, consult a doctor.
If the headache becomes persistent, you should see a doctor.
It is contraindicated to prescribe to patients with bronchial asthma, with increased bleeding. The drug is used with extreme caution with simultaneous therapy with anticoagulants (coumarin and heparin), with impaired liver function and kidney diseases, as well as with simultaneous anti-inflammatory therapy.
Use during pregnancy or breastfeeding
Do not use the medicine during pregnancy or breastfeeding.
Acetylsalicylic acid has a teratogenic effect; when used during pregnancy in the first trimester, it causes cleft palate, in the third trimester - inhibition of labor activity (inhibition of prostaglandin synthesis), closure of the ductus arteriosus in the fetus, which causes pulmonary vascular hyperplasia and hypertension in the vessels of the small circulation, impaired renal function with the possible subsequent development of renal failure with oligohydramnios, prolongation of bleeding time, antiplatelet effect, which can occur even after the use of very low doses.
Caffeine increases the risk of spontaneous miscarriage.
The drug passes into breast milk, which increases the risk of bleeding in children due to impaired platelet function.
Ability to influence reaction speed when driving vehicles or other mechanisms
Since adverse reactions from the nervous system (dizziness, increased excitability, impaired orientation and attention) are possible, when using Askofen L, driving a car and work that requires increased attention and speed of psychomotor reactions should be avoided.
Method of administration and doses
The medicine is intended for oral administration.
Adults: 1 tablet 2-3 times a day after meals. The maximum daily dose of the drug is 6 tablets (in 3 doses).
The duration of the course of treatment depends on the course and severity of the disease and should not exceed 5 days when used as an analgesic and 3 days as an antipyretic.
Do not take with other medicines containing paracetamol.
The drug should not be used in children due to the risk of developing Reye's syndrome (hyperpyrexia, metabolic acidosis, nervous system and mental disorders, vomiting, liver dysfunction) in case of hyperthermia against the background of viral diseases.
Overdose
Symptoms of paracetamol overdose.
Liver damage is possible in adults who have taken 10 g or more of paracetamol, and in children who have taken the drug in a dose of more than 150 mg/kg of body weight. In patients with risk factors (long-term treatment with carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; regular use of excessive amounts of ethanol; glutathione cachexia (digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia)) the use of 5 g or more of paracetamol may lead to liver damage.
Liver damage may become apparent 12-48 hours after taking excessive doses of the drug. The following symptoms may occur in the first 24 hours: pallor, nausea, vomiting, anorexia, abdominal pain. In severe poisoning, liver failure may progress to encephalopathy, hypoglycemia, coma and death. Acute renal failure with acute tubular necrosis may manifest as severe lumbar pain, hematuria, proteinuria and develop even in the absence of severe kidney damage. Glucose metabolism disorders and metabolic acidosis may occur. Cardiac arrhythmia and pancreatitis have also been noted. With prolonged use of the drug in high doses, aplastic anemia, thrombocytopenia, pancytopenia, agranulocytosis, neutropenia, leukopenia may develop from the hematopoietic system. When taking large doses, from the side of the CNS - dizziness, psychomotor agitation and disorientation; from the side of the urinary system - nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis).
In case of overdose, urgent medical attention is required. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting or may not reflect the severity of the overdose or the risk of organ damage. Treatment with activated charcoal should be considered if an overdose of paracetamol has been taken within 1 hour. The concentration of paracetamol in the blood plasma should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine can be used within 24 hours of paracetamol ingestion, but the maximum protective effect occurs when it is used within 8 hours of ingestion. The effectiveness of the antidote decreases sharply after this time. If necessary, the patient should be given intravenous N-acetylcysteine in doses according to current recommendations. In the absence of vomiting, oral methionine can be used as a suitable alternative in remote areas outside the hospital. General supportive measures should also be applied.
Symptoms of acetylsalicylic acid overdose.
Salicylate overdose is possible due to chronic intoxication resulting from long-term therapy (administration of more than 100 mg/kg/day for more than 2 days may cause toxic effects), as well as acute intoxication, which is life-threatening (overdose) and may be caused by accidental use (children) or an unforeseen overdose.
Chronic salicylate poisoning may be latent because its symptoms are nonspecific. Moderate chronic salicylate intoxication, or salicylism, usually occurs only after repeated ingestion of large doses. The main symptoms are: balance disorders, dizziness, tinnitus, deafness, increased sweating, nausea and vomiting, headache, confusion. These symptoms can be controlled by reducing the dose. Tinnitus may occur at plasma salicylate concentrations above 150-300 μg/ml. More serious adverse reactions occur at plasma salicylate concentrations above 300 μg/ml.
Acute intoxication is indicated by a pronounced change in acid-base balance, which may vary depending on age and severity of intoxication. The severity of the condition cannot be determined solely on the basis of the concentration of salicylates in the blood plasma.
Treatment: intoxication caused by an overdose of acetylsalicylic acid is determined by the severity, clinical symptoms and is treated by standard methods used in poisoning. All measures should be aimed at accelerating the removal of the drug and restoring electrolyte and acid-base balance. Activated charcoal, forced alkaline diuresis are used. Depending on the state of acid-base balance and electrolyte balance, infusion of electrolyte solutions is carried out. In severe poisoning, hemodialysis is indicated. With long-term use of high doses, aplastic anemia, thrombocytopenia, pancytopenia, agranulocytosis, neutropenia, leukopenia are possible. When taking high doses, disorders of the central nervous system may occur (dizziness, psychomotor agitation, impaired orientation and attention, insomnia, tremor, nervousness, anxiety), and nephrotoxicity of the urinary system (renal colic, interstitial nephritis, papillary necrosis). In case of overdose, increased sweating, psychomotor agitation or CNS depression, drowsiness, impaired consciousness, cardiac arrhythmias, tachycardia, extrasystole, tremor, hyperreflexia, and convulsions may occur.
Symptoms of caffeine overdose.
Large doses of caffeine can cause epigastric pain, vomiting, diuresis, rapid breathing, extrasystole, tachycardia or cardiac arrhythmia, effects on the central nervous system (dizziness, insomnia, nervousness, nervous excitement, syndrome of increased neuro-reflex excitability, headache, irritability, state of affect, anxiety, restlessness, tremor, convulsions). Clinically significant symptoms of caffeine overdose are also associated with liver damage by paracetamol.
Treatment. In case of overdose, urgent medical attention is required, even if symptoms of overdose are absent. Administration of methionine orally or acetylcysteine intravenously may have a positive effect within 48 hours after overdose. It is also necessary to apply general supportive measures, symptomatic therapy, including the use of β-adrenoreceptor antagonists, which can eliminate cardiotoxic effects. There is no specific antidote.
Adverse reactions
When using the drug Askofen L, some patients may experience adverse reactions that are typical of acetylsalicylic acid, paracetamol, or caffeine.
On the part of the organs of vision: visual impairment, indicating overdose.
From the side of the organs of hearing and vestibular apparatus: ringing in the ears, tinnitus, disorientation.
Respiratory system: rhinitis, nasal congestion, bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs.
From the cardiovascular system: tachycardia, palpitations, arterial hypertension, arrhythmia.
From the blood and lymphatic system: anemia, sulfate hemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, pain in the heart area), hemolytic anemia, bruising or bleeding, with prolonged use in high doses - aplastic anemia, pancytopenia, neutropenia, thrombocytopenia, agranulocytosis. Due to the antiplatelet effect on platelets, acetylsalicylic acid increases the risk of bleeding. Bleeding such as intraoperative hemorrhages, hematomas, bleeding from the genitourinary system, nosebleeds, bleeding from the gums, gastrointestinal bleeding and cerebral hemorrhages (especially in patients with uncontrolled arterial hypertension and/or with simultaneous use of antihemostatic agents) has been observed, which in isolated cases were life-threatening.
From the nervous system: headache, nervousness, anxiety, dizziness, tremor, paresthesia, increased excitability, irritability, sleep disturbances, insomnia, general weakness, irritability.
On the part of the psyche: feeling of fear, anxiety, restlessness.
On the part of the digestive tract: dyspeptic disorders, including nausea, vomiting, epigastric discomfort and pain, heartburn, abdominal pain; inflammation of the digestive tract, erosive-ulcerative lesions of the digestive tract, which in rare cases can cause gastrointestinal bleeding and perforation with corresponding laboratory and clinical manifestations; ulcers on the mucous membrane of the oral cavity.
Immune system disorders: hypersensitivity reactions, including anaphylaxis, anaphylactic shock.
In patients with individual hypersensitivity to salicylates, allergic skin reactions may develop, including symptoms such as skin hyperemia, a feeling of heat, rash, urticaria, edema, itching, angioedema, rhinitis, nasal congestion. In patients with bronchial asthma, an increase in the frequency of bronchospasm is possible; allergic reactions of mild to moderate severity, which can affect the skin, respiratory tract, digestive tract, cardiovascular system and manifest themselves in the form of rashes, urticaria, edema, itching.
On the part of the endocrine system: hypoglycemia, up to hypoglycemic coma.
From the urinary system: nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis).
Skin and subcutaneous tissue disorders: pruritus, rash on the skin and mucous membranes (usually generalized rash, erythematous, urticaria), angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
General disorders: general weakness.
Others: Bleeding can lead to acute and chronic posthemorrhagic/iron deficiency anemia (due to so-called occult microbleeding) with corresponding laboratory manifestations and clinical symptoms such as asthenia, pallor of the skin, hypoperfusion, non-cardiogenic pulmonary edema.
Reporting of suspected adverse reactions.
Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
6 tablets in blisters;
6 tablets in a blister, 10 blisters in a pack;
10 tablets in blisters;
10 tablets in a blister, 10 blisters in a pack;
10 tablets in a blister, 1 blister in a pack.
Vacation category
Without a prescription: tablets No. 6, No. 10.
By prescription: tablets No. 60 (6×10), No. 100 (10×10).
Producer
JSC "Lubnypharm".
Location of the manufacturer and address of its place of business.
Ukraine, 37500, Poltava region, Lubny, Barvinkova st., 16.
