Citramon-ExtraCap capsules 240mg+27.45mg +180mg, 10pcs

Composition

Active ingredients:

acetylsalicylic acid-240.0 mg,

paracetamol-180.0 mg,

caffeine-27.45 mg;

excipients:

citric acid (citric acid monohydrate) – 5.00 mg,

potato starch-20.95 mg,

talc-10.00 mg,

low-molecular povidone (polyvinylpyrrolidone low-molecular medical 12600±2700 or K-17) – 3.00 mg,

calcium stearate-1.00 mg,

colloidal silicon dioxide (aerosil) – 2.60 mg.

Solid gelatin capsules No. 00.

Capsule shell composition (body and cap):

titanium dioxide (E 171) – 2.6666%, quinoline yellow (E 104) – 1.8394%, dye sunset yellow (E 110) – 0.0088%, gelatin – up to 100%.

Pharmacological action

Pharmacotherapeutic group: combined analgesic (NSAID + non-narcotic analgesic + psychostimulant)

ATX code: [N02 BA 71]

Pharmacological properties

Pharmacodynamics

Combined drug.

Acetylsalicylic acid (ASA) has an antipyretic and anti-inflammatory effect, relieves pain, especially caused by the inflammatory process, and also inhibits blood clots, improves microcirculation in the focus of inflammation.

Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, expands the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation; reduces drowsiness, fatigue, increases mental and physical performance. In this combination, caffeine in a small dose has almost no stimulating effect on the central nervous system, increases the tone of the brain vessels and accelerates blood flow.

Paracetamol has analgesic, antipyretic and weak anti-inflammatory effects, which is associated with its effect on the thermoregulatory center in the hypothalamus and its weak ability to inhibit prostaglandin synthesis in peripheral tissues.

Pharmacokinetics

of ASA: oral absorption is complete. During absorption, it undergoes presystemic elimination in the intestinal wall and systemic elimination in the liver (deacetylated). The resorbed part is rapidly hydrolyzed by cholinesterases and albuminesterase, so the half-life is no more than 15-20 minutes. It circulates in the body (by 75-90% due to albumin) and is distributed in the tissues in the form of salicylic acid anion. The time to reach the maximum concentration is 2 hours. It is mainly metabolized in the liver with the formation of 4 metabolites found in many tissues and urine. It is excreted by active secretion in the renal tubules in the form of salicylate (60%) and its metabolites. The excretion of unchanged salicylate depends on the pH of the urine (when the urine is alkalinized, the ionization of salicylates increases, their reabsorption worsens, and the excretion increases significantly). The rate of elimination depends on the dose: when taking small doses, the half-life is 2-3 hours, with an increase in the dose it can increase to 15-30 hours. In newborns, salicylate elimination is much slower than in adults.

Paracetamol: the adsorption is high, the maximum concentration is reached in 0.5-2 hours and is 5-20 mcg / ml, the binding to plasma proteins is 15%. Penetrates the blood-brain barrier. Less than 1% of the dose taken by a nursing mother passes into breast milk. A therapeutically effective plasma concentration of paracetamol is achieved when administered at a dose of 10-15 mg / kg. It is metabolized in the liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form already inactive metabolites. When glutathione is deficient, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The SUR2 E1 isoenzyme is also involved in metabolism. The half-life is 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly in the form of conjugates. Only 3% are displayed unchanged. In elderly patients, the clearance of the drug decreases and the half-life increases.

Caffeine: when taken orally, absorption is good and occurs throughout the intestines. Absorption is mainly due to lipophilicity, rather than water solubility. The maximum concentration is reached in 50-75 minutes and is 1.58-1.76 mg/l. It is quickly distributed in all organs and tissues of the body: it easily penetrates the blood-brain barrier and the placenta. The volume of distribution in adults is 0.4-0.6 l / kg, in newborns-0.78-0.92 l/kg. The relationship with blood proteins (albumins) is 25-36%. Metabolism in the liver is exposed to more than 90, in children of the first years of life up to 10-15%. In adults, about 80% of the caffeine dose is metabolized to paraxanthin, about 10% to theobromine, and about 4% to theophylline, which are subsequently demethylated to monomethylxanthines and then to methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10 hours), in newborns-65-130 hours (by 4-7 months of life it decreases to the value as in adults). Elimination of caffeine and its metabolites is carried out by the kidneys (1-2% is excreted unchanged in adults, up to 85% in newborns).

Indications

Mild to moderate pain syndrome (of various origins): headache, migraine, toothache, neuralgia, myalgia, arthralgia, algodismenorrhea. Febrile syndrome: with acute respiratory diseases, flu.

Contraindications

-Peptic ulcer of the stomach and duodenum in the acute phase; – Gastrointestinal bleeding or perforation, peptic ulcer in the anamnesis;- Severe renal or hepatic insufficiency; – Hemorrhagic diathesis, hypocoagulation (including hemophilia, hypoprothrombinemia);- Surgical interventions accompanied by heavy bleeding;- Pregnancy, breast-feeding period;-Glucose-6-phosphate dehydrogenase deficiency;- Glaucoma; – Hypersensitivity to the components of the drug;- Complete and incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, and intolerance to ASA or other nonsteroidal anti-inflammatory drugs (including in the anamnesis);- Children under 15 years of age as an analgesic, for febrile syndrome-up to 18 years;- Increased excitability, sleep disorders; – Organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis);- Severe arterial hypertension;- Portal hypertension;- Chronic heart failure of NYHA functional class III-IV; – Concomitant use of methotrexate more than 15 mg per week; – Avitaminosis K; – Hypoproteinemia. With caution: Gout, hyperuricemia, gastric and duodenal ulcer, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergy, concomitant use of methotrexate at a dose of less than 15 mg / week, concomitant therapy with anticoagulants, nonsteroidal anti-inflammatory drugs, glucocorticosteroids, antiplatelet agents, selective serotonin reuptake inhibitors. Mild to moderate renal insufficiency, mild to moderate hepatic insufficiency with elevated transaminase levels, benign hyperbilirubinemia (including Gilbert’s syndrome, alcoholic liver damage), alcoholism, epilepsy and a tendency to convulsive seizures, old age, gout, arterial hypertension, chronic heart failure of NYHA functional class I-II, coronary heart disease, cerebrovascular diseases, peripheral artery diseases, smoking. If you have one of these diseases/If you have any serious medical conditions, be sure to consult your doctor before taking the drug.

Side effects

Gastralgia, nausea, vomiting, hepatotoxicity, nephrotoxicity, erosive and ulcerative lesions of the gastrointestinal tract, allergic reactions (including Stevens-Johnson syndrome, Lyell), tachycardia, increased blood pressure, bronchospasm.

Interaction

Increases the effect of heparin, indirect anticoagulants, reserpine, steroid hormones and hypoglycemic drugs. Concomitant use with other NSAIDs, methotrexate increases the risk of side effects. Reduces the effectiveness of spironolactone, furosemide, antihypertensive drugs, as well as anti-gouty drugs that promote uric acid excretion. Barbiturates, rifampicin, salicylamide, antiepileptic drugs, etc. stimulators of microsomal oxidation contribute to the formation of toxic metabolites of paracetamol that affect liver function.

How to take it, course of use and dosage

The drug should not be taken for more than 5 days as an analgesic drug and for more than 3 days as an antipyretic (without the appointment and supervision of a doctor). Inside (during or after a meal, with a sufficient amount of water at each dose). In case of headache, the recommended dose is 1-2 capsules, in case of severe headache, the next dose is taken in 4-6 hours. For migraines, the recommended dose is 2 capsules if symptoms appear, if necessary, repeat after 4-6 hours. For the treatment of headaches and migraines, the drug is used for no more than 4 days. For pain syndrome – 1-2 capsules; the average daily dose is 3-4 capsules, the maximum daily dose is 8 capsules. The course of treatment is no more than 3-5 days. Elderly (over 65 years old)Caution should be exercised in elderly patients, especially those with low body weight. Patients with hepatic and renal insufficiency The effect of impaired liver or kidney function on the pharmacokinetics of the drug has not been studied. Given the mechanism of action of acetylsalicylic acid and paracetamol, their use may worsen renal and hepatic insufficiency.In this regard, the drug is contraindicated in patients with severe hepatic or renal insufficiency (see section “Contraindications”), and in patients with mild to moderate hepatic and renal insufficiency, it should be used with caution (see section “With caution”).

Overdose

of Acetylsalicylic acid In mild intoxications – dizziness, tinnitus, deafness, increased sweating, nausea, vomiting, headache and confusion. Occurs at a plasma concentration of 150-300 mcg / ml. Treatment – reduction of the dose or discontinuation of therapy. At concentrations above 300 mcg / ml, more severe intoxication occurs, manifested by hyperventilation, fever, anxiety, ketoacidosis, respiratory alkalosis, and metabolic acidosis. Depression of the central nervous system can lead to coma, and cardiovascular collapse and respiratory failure can also occur. The greatest risk of developing chronic intoxication is observed in children and the elderly when taking more than 100 mg / kg / day for several days. Treatment If more than 120 mg/kg of salicylates are suspected of being ingested within the last hour, activated charcoal is repeatedly administered orally. When taking more than 120 mg/kg of salicylates, their plasma concentration should be determined, although it is impossible to predict its severity only on the basis of this indicator, it is also necessary to take into account clinical and biochemical parameters. If the plasma concentration exceeds 500 mcg / ml (350 mcg / ml for children under 5 years of age), intravenous sodium bicarbonate effectively removes salicylates from the plasma. If the plasma concentration exceeds 700 mcg/ml (lower concentrations in children and the elderly) or in severe metabolic acidosis, the therapy of choice is hemodialysis or hemoperfusion. Paracetamol overdose Intoxication is possible in overdose, especially in elderly patients, children, patients with liver diseases (caused by chronic alcoholism), in patients with nutritional disorders, as well as in patients taking inducers of microsomal liver enzymes, which can develop lightning – fast hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis, in the above cases-sometimes with a fatal outcome. The clinical picture of acute overdose develops within 24 hours after taking paracetamol. Symptoms: gastrointestinal disorders (nausea, vomiting, decreased appetite, abdominal discomfort and / or abdominal pain), pallor of the skin. With simultaneous use of 7.5 g or more to adults or more than 140 mg/kg to children, cytolysis of hepatocytes occurs with complete and irreversible liver necrosis, the development of liver failure, metabolic acidosis and encephalopathy, which can lead to coma and death. 12-48 hours after paracetamol use, there is an increase in the activity of microsomal liver enzymes, lactate dehydrogenase, bilirubin concentration, and a decrease in prothrombin content. Clinical symptoms of liver damage appear 2 days after an overdose of the drug and reach a maximum on day 4-6. Treatment: Slow hospitalization. Determination of the quantitative content of paracetamol in blood plasma before starting treatment as early as possible after an overdose; use of SH – group donors and glutathione synthesis precursors – methionine and acetylcysteine – is most effective in the first 8 hours. The need for additional therapeutic measures (further use of methionine, intravenous use of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its use. Symptomatic treatment. Laboratory tests of the activity of microsomal liver enzymes should be performed at the beginning of treatment and then every 24 hours. In most cases, the activity of microsomal liver enzymes normalizes within 1-2 weeks. In very severe cases, a liver transplant may be required. Common symptoms include gastralgia, agitation, delirium, anxiety, nervousness, restlessness, insomnia, mental agitation, muscle twitching, confusion, seizures, dehydration, frequent urination, hyperthermia, headache, increased tactile or pain sensitivity, nausea and vomiting (sometimes with blood), tinnitus. With severe overdose, hyperglycemia may occur. Cardiological disorders are manifested by tachycardia and arrhythmia. Treatment – reducing the dose or eliminating caffeine.

Special instructions

General This medicinal product should not be taken simultaneously with medicinal products containing ASA or paracetamol. Similar to other migraine medications, caution should be exercised before starting treatment for suspected migraines in patients who have not previously been diagnosed with migraines, or in patients who have atypical symptoms of migraines, to exclude other potentially serious neurological disorders. If patients experience vomiting in >20% of migraine attacks or require bed rest in >50% of migraine attacks, the drug should not be used. If migraines do not stop after taking the first two tablets of the drug, you should seek medical help. The drug should not be used if the patient has experienced more than 10 headache attacks per month for at least the last three months. In this case, you should suspect a headache due to excessive use of medications and cancel treatment. In addition, patients should seek medical attention. Caution should be exercised in patients with risk factors for dehydration, such as vomiting, diarrhea, or before or after major surgery. Due to its pharmacodynamic properties, the drug can mask the signs and symptoms of infection. Due to the content of acetylsalicylic acid in the preparation, the drug should be used with caution in patients with gout, impaired renal or liver function, dehydration, uncontrolled arterial hypertension, glucose-6-phosphate dehydrogenase deficiency and diabetes mellitus. Due to the inhibition of ASA platelet aggregation, the drug can lead to prolonged bleeding time during and after surgical interventions (including small ones, for example, tooth extraction). The drug should not be used simultaneously with anticoagulants and other drugs that interfere with blood clotting, without the supervision of a doctor (see the section “Interaction with other drugs”). Patients with blood clotting disorders should be carefully monitored. Caution should be exercised in case of metro-or menorrhagia. If the patient develops bleeding or ulceration of the gastrointestinal tract while taking the drug, it should be stopped immediately. Potentially fatal bleeding, ulceration, and perforation of the gastrointestinal tract may occur at any time during treatment with any NSAID, with or without a history of premonitory and severe gastrointestinal complications. These complications tend to be more severe in older patients. Alcohol, glucocorticosteroids, and NSAIDs may increase the risk of gastrointestinal bleeding (see section “Interactions with other medications”). The drug may contribute to the development of bronchospasm and the occurrence of exacerbation of bronchial asthma (including bronchial asthma caused by intolerance to analgesics) or other hypersensitivity reactions. Risk factors include bronchial asthma, seasonal allergic rhinitis, nasal polyposis, chronic obstructive pulmonary disease, and chronic respiratory tract infections (especially those associated with symptoms characteristic of allergic rhinitis). Such phenomena may also occur in patients with allergic reactions (for example, skin reactions, including pruritus and urticaria) to other substances. Special care is recommended in these patients. Children under 18 years of age should not be prescribed medications containing acetylsalicylic acid as an antipyretic, since in the case of a viral infection, they can increase the risk of Reye’s syndrome. Symptoms of Reye’s syndrome include hyperpyrexia, prolonged vomiting, metabolic acidosis, disorders of the nervous system and psyche, hepatomegaly and liver function disorders, acute encephalopathy, respiratory disorders, convulsions, coma. ASA can distort the results of laboratory tests of thyroid function due to false-positive low concentrations of levothyroxine (T%^%4) and triiodothyronine (T%^%3) (see the section “Interaction with other drugs”). Due to the content of paracetamol in the drug, caution should be exercised when prescribing the drug to patients with impaired renal or liver function or alcohol dependence. The risk of paracetamol poisoning is increased in patients taking other potentially hepatotoxic drugs or drugs that induce microsomal liver enzymes (for example, rifampicin, isoniazid, chloramphenicol, sleeping pills and anticonvulsants, including phenobarbital, phenytoin and carbamazepine). Patients with a history of alcoholism are particularly at risk for liver damage (see the section “Interaction with other drugs”). When using the drug, serious skin reactions can develop, such as acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, which can lead to death. Patients should be informed about signs of serious skin reactions. The drug should be discontinued at the first appearance of skin reactions or any other signs of hypersensitivity. Due to the caffeine content of the drug, the drug should be used with caution in patients with gout, hyperthyroidism and arrhythmia.When using the drug, you should limit the consumption of products containing caffeine, since excessive intake of caffeine can lead to nervousness, irritability, insomnia and, in some cases, palpitations. Influence on laboratory studieshigh doses of ASA can distort the results of a number of clinical and biochemical laboratory studies. The use of paracetamol may affect the results of uric acid determination by the phosphor-wolframic acid method and glycemia by the glucose oxidase/peroxidase method. Caffeine may reverse the effects of dipyridamole on myocardial blood flow, thus distorting the results of this study. During the study, it is necessary to refrain from taking caffeine for 8-12 hours. Influence on the ability to drive vehicles and mechanisms:During the use of the drug, you should refrain from driving vehicles and working with other mechanisms, because caffeine, which is part of the drug, can cause impaired concentration and reaction speed, and acetylsalicylic acid, which is also part of the drug, can in rare cases cause dizziness.

Storage conditions

Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years.

Active ingredients

: Acetylsalicylic acid, Caffeine, Paracetamol

Dosage form

Capsules

Purpose

For adults and Children over 15 years of age

Indications

Neuritis, Flu, Migraines, Colds