Instructions for Citramon Extra tablets No. 10
Composition
active ingredients: paracetamol, coffee;
1 tablet contains: paracetamol 500 mg; caffeine 50 mg;
excipients: microcrystalline cellulose, methylcellulose, croscarmellose sodium, povidone, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: white or almost white tablets, round in shape with a flat surface, a bevel and a score.
Pharmacotherapeutic group
Analgesics and antipyretics. Paracetamol, combinations without psycholeptics. ATX code N02B E51.
Pharmacological properties
Pharmacodynamics.
Combined drug.
Paracetamol has analgesic, antipyretic and weak anti-inflammatory effects, which are associated with its effect on the thermoregulation center in the hypothalamus and a less pronounced ability to inhibit prostaglandin synthesis in tissues.
Caffeine increases the reflex excitability of the spinal cord, stimulates the respiratory and hemodynamic centers, dilates 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 practically no stimulating effect on the central nervous system, but contributes to the normalization of the tone of brain vessels and the acceleration of blood flow.
Pharmacokinetics.
Paracetamol and caffeine are rapidly absorbed from the gastrointestinal tract and distributed to most body tissues. Binding of paracetamol to plasma proteins is minimal at therapeutic doses.
Paracetamol and caffeine are metabolized mainly in the liver and excreted in the urine as transformation products. The average half-life in blood plasma after oral administration is: for paracetamol - about 2.3 hours, for caffeine - about 4.9 hours.
Indication
The drug has a moderate analgesic and antipyretic effect. Indications for use are headache, including migraine, toothache, neuralgia, rheumatic pain, periodic pain in women; to relieve symptoms of colds and flu, sore throat.
Contraindication
Hypersensitivity to paracetamol, caffeine or any other component of the drug in history; severe liver and/or kidney disorders; congenital hyperbilirubinemia; glucose-6-phosphate dehydrogenase deficiency; alcoholism; blood diseases, severe anemia, leukopenia; states of increased excitement, sleep disorders, epilepsy; severe increased blood pressure, organic diseases of the cardiovascular system, including severe atherosclerosis, severe hypertension; decompensated heart failure, acute myocardial infarction, paroxysmal tachycardia, hyperthyroidism, acute pancreatitis, Gilbert's syndrome, severe forms of diabetes mellitus, glaucoma; age over 60 years.
Do not use with monoamine oxidase inhibitors (MAOIs) and within 2 weeks of discontinuing MAOIs.
Contraindicated in patients taking tricyclic antidepressants or beta-blockers.
Interaction with other medicinal products and other types of interactions
Paracetamol
With the simultaneous use of paracetamol with hepatotoxic agents, the toxic effect of the drug on the liver increases.
Barbiturates, rifampicin, salicylamide, antiepileptic drugs, carbamazepine, phenytoin, ethanol, phenylbutazone, tricyclic antidepressants and other microsomal oxidation stimulants - these drugs increase the production of hydroxylated active metabolites that affect liver function, causing the possibility of developing severe intoxications with small overdoses of the drug.
Barbiturates – reduce the antipyretic effect of paracetamol.
Paracetamol may reduce the bioavailability of lamotrigine, reducing its effect due to the possible induction of its metabolism in the liver.
The risk of developing neutropenia increases with the simultaneous use of paracetamol and zidovudine.
Microsomal oxidation inhibitors (cimetidine) - reduce the risk of hepatotoxic effects of Citramon Extra.
Concomitant use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome.
Metoclopramide and domperidone – increase the absorption of paracetamol.
Ethanol – simultaneous administration of paracetamol and ethanol increases the risk of developing hepatotoxic effects and acute pancreatitis.
Do not use simultaneously with alcohol.
Long-term simultaneous use of the drug with acetylsalicylic acid or other non-steroidal anti-inflammatory drugs may lead to kidney damage.
Flucloxacillin - caution should be exercised when using paracetamol with flucloxacillin, as such concomitant use is associated with high anion gap metabolic acidosis, especially in patients with risk factors (see section "Special warnings and precautions for use").
Coumarin derivatives (warfarin) – long-term use of paracetamol increases the risk of bleeding. Taking single doses does not have a significant effect.
Cholestyramine – reduces the absorption of paracetamol.
Probenecid affects the concentration of paracetamol in blood plasma and its excretion.
Paracetamol reduces the effectiveness of diuretics.
Caffeine
Concomitant use of caffeine with MAO inhibitors can cause a dangerous increase in blood pressure.
Caffeine enhances the effect (improves bioavailability) of analgesics-antipyretics, potentiates the effects of xanthine derivatives, α- and β-adrenomimetics, and psychostimulants.
Cimetidine, hormonal contraceptives, isoniazid - enhance the effects 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, and a competitive antagonist of adenosine and adenosine triphosphate (ATP) drugs.
The simultaneous use of caffeine with thyroid-stimulating agents increases the thyroid effect.
Caffeine reduces the concentration of lithium in the blood.
Caffeine accelerates the absorption of ergotamine.
Application features
It is necessary to consult a doctor regarding the possibility of using the drug in patients with impaired kidney and liver function.
It should be taken into account that patients with liver disease have an increased risk of hepatotoxic effects of paracetamol.
Alcoholic beverages should not be consumed during treatment. Paracetamol may be toxic to the liver at doses greater than 6–8 g per day, but adverse effects on the liver may occur at much lower doses in the case of alcohol, liver enzyme inducers, or other substances that have a toxic effect on the liver, and this effect is higher in patients with non-cirrhotic alcoholic liver disease. Long-term alcohol consumption significantly increases the risk of developing hepatotoxic effects of paracetamol. Regular liver function tests are recommended in patients with impaired liver function, as well as in those taking large doses of paracetamol for a long time.
Before using the drug, it is necessary to consult a doctor if the patient is taking warfarin or similar drugs that have an anticoagulant effect. Restrictions on the use of the drug in such patients are primarily due to the content of paracetamol.
When treating with oral anticoagulants with simultaneous administration of large doses of paracetamol, monitoring of prothrombin time is necessary.
The drug may affect the results of laboratory tests for blood glucose and uric acid.
Cases of liver dysfunction/hepatic failure have been reported in patients with reduced glutathione levels, e.g. in severe wasting, anorexia, low body mass index, chronic alcoholism or sepsis. Patients with reduced glutathione levels are at increased risk of metabolic acidosis when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or labored breathing, nausea, vomiting, loss of appetite. You should seek medical attention immediately if these symptoms occur.
Caution should be exercised when using paracetamol with flucloxacillin due to the increased risk of high anion gap metabolic acidosis, especially in patients with severe renal insufficiency, sepsis, malnutrition or other causes of glutathione deficiency (e.g. chronic alcoholism), and when maximum daily doses of paracetamol are used. Close monitoring, including measurement of urinary 5-oxoproline, is recommended.
During treatment with the drug, it is not recommended to consume excessive amounts of beverages containing caffeine (such as coffee, tea and some other drinks). This may lead to sleep problems, tremors, chest discomfort due to palpitations, tension and irritability.
Do not exceed the indicated doses.
Do not take the medicine with other medicines containing paracetamol.
If symptoms persist, you should consult a doctor.
If the headache becomes persistent, you should see a doctor.
Keep the medicine out of the sight and reach of children.
Use during pregnancy or breastfeeding
It is not recommended to use the drug during pregnancy, as the risk of spontaneous miscarriage associated with the use of caffeine is increased.
Paracetamol and caffeine pass into breast milk, but in clinically insignificant amounts when taken in recommended doses. It is not recommended to use the drug during breastfeeding. Caffeine in breast milk may have a stimulating effect on infants during breastfeeding, but no significant toxicity has been observed.
Ability to influence reaction speed when driving vehicles or other mechanisms
Has no significant impact.
Method of administration and doses
The medicine is intended for oral use.
Adults and children over 12 years of age: 1–2 tablets 4 times a day. The interval between doses is at least 4 hours. Do not take more than 8 tablets (4000 mg paracetamol/400 mg caffeine) in 24 hours. Do not exceed the recommended dose.
Do not use together with other medicines containing paracetamol.
The duration of treatment is determined by the doctor.
The medicine is not recommended for use in children under 12 years of age.
Overdose
Liver damage is possible in adults after using 10 g or more of paracetamol, and in children after using more than 150 mg/kg of body weight.
Paracetamol overdose can cause liver failure, which may require a liver transplant or be fatal.
In patients with risk factors (long-term treatment with carbamazepine, phenobarbital, 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) taking 5 g or more of paracetamol can lead to liver damage.
Symptoms of overdose in the first 24 hours: pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may occur 12–48 hours after overdose and reach a maximum after 4–6 days. Glucose metabolism disorders and metabolic acidosis may occur. In severe poisoning, liver failure may progress to encephalopathy, hemorrhage, hypoglycemia, coma and be fatal. Acute renal failure with acute tubular necrosis may manifest as severe lumbar pain, hematuria, proteinuria and develop even in the absence of severe liver damage. Cardiac arrhythmia and pancreatitis have also been reported.
With prolonged use of the drug in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia may develop from the hematopoietic system. When taking large doses, dizziness, psychomotor agitation and disorientation may occur from the central nervous system; nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis) may occur from the urinary system.
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. If an overdose is confirmed or only suspected, the patient should be taken to the nearest medical facility where they can receive emergency medical care and qualified treatment. This should be done even if there are no symptoms of overdose, because of the risk of delayed liver damage.
Activated charcoal should be considered if paracetamol overdose has been taken within 1 hour. Plasma paracetamol concentrations should be measured 4 hours or later after ingestion (earlier concentrations are not reliable). N-acetylcysteine treatment can be used up to 24 hours after paracetamol ingestion, but maximum protection is obtained when administered within 8 hours of ingestion. The efficacy of the antidote decreases sharply after this time. If necessary, the patient should be given N-acetylcysteine intravenously at the recommended dosage. In the absence of vomiting, oral methionine may be used as a suitable alternative in remote areas outside the hospital.
Caffeine overdose can cause epigastric pain, vomiting, diuresis, rapid breathing, extrasystole, tachycardia or cardiac arrhythmia, effects on the central nervous system (dizziness, insomnia, nervous excitement, irritability, affective state, anxiety, tremor, convulsions). Clinically important symptoms of caffeine overdose are also associated with liver damage by paracetamol, which can be observed when taking such an amount of the drug that causes a caffeine overdose. There is no specific antidote, but supportive measures, such as the use of β-adrenoreceptor antagonists, can alleviate the cardiotoxic effect. Gastric lavage is necessary, oxygen therapy is recommended, and diazepam is recommended for convulsions. Symptomatic therapy.
Side effects
The following adverse reactions have been identified during post-marketing surveillance. Since adverse reactions were reported voluntarily and the patient population is unknown, the frequency of these adverse reactions cannot be estimated, but they are likely to be rare (< 1/10,000).
Respiratory, thoracic and mediastinal disorders: rhinitis, nasal congestion, bronchospasm in patients sensitive to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.
Gastrointestinal: nausea, vomiting, heartburn, epigastric pain, slight laxative effect.
From the liver and biliary tract: increased activity of liver enzymes, usually without the development of jaundice, hepatotoxic effect, impaired liver function, liver failure, hepatonecrosis (dose-dependent effect), jaundice.
From the kidneys and urinary system: nephrotoxic effect (including interstitial nephritis, papillary necrosis), aseptic pyuria.
On the part of the endocrine system: hypoglycemia, up to hypoglycemic coma.
From the nervous system: headache, nervousness, dizziness.
Psychiatric: insomnia, restlessness, anxiety, and irritability.
Blood and lymphatic system disorders: thrombocytopenia, leukopenia, neutropenia, agranulocytosis, pancytopenia, anemia, aplastic anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, bruising or bleeding.
Immune system disorders: hypersensitivity reactions, including skin and mucous membrane rashes (usually generalized rash, erythematous rash), Stevens-Johnson syndrome, angioedema, anaphylaxis, anaphylactic shock, erythema multiforme exudative, toxic epidermal necrolysis (Lyell's syndrome), acute generalized exanthematous pustulosis.
Skin and subcutaneous tissue disorders: itching, rash, sweating, purpura, urticaria.
Concomitant use of the drug in recommended doses with products containing caffeine may increase side effects caused by caffeine, such as dizziness, increased excitability, insomnia, restlessness, anxiety, irritability, headache, gastrointestinal disorders and rapid heartbeat.
Reporting of suspected adverse reactions.
Reporting suspected adverse reactions after the marketing authorisation of a medicinal product is an important procedure. It allows for continued monitoring of the benefit-risk balance of the medicinal product in question. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
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
10 tablets in a contour blister pack; 1 contour blister pack in a pack.
Vacation category
Without a prescription.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and address of its place of business
Ukraine, 02093, Kyiv, Boryspilska St., 13.
