Citramon Ultra
Citramon Ultra: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Citramon Ultra
ATX code: N02BA71
Active ingredient: acetylsalicylic acid (Acidum acetylsalicylicum) + caffeine (Caffeine) + paracetamol (Paracetamol)
Manufacturer: Obolenskoye - pharmaceutical company, JSC (Russia); PharmVILAR, NPO (Russia); Pharmproject JSC (Russia)
Description and photo update: 28.11.2018
Prices in pharmacies: from 53 rubles.
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Citramon Ultra is a combined analgesic drug.
Release form and composition
Dosage form - film-coated tablets: oblong biconvex, with rounded ends, with a line on one side; the shell is light brown, the core is almost white or white (in a cardboard box there are 1-6 blisters of 5, 6, 10, 15 or 20 tablets and instructions for the use of Citramon Ultra).
1 tablet contains:
- active substances: acetylsalicylic acid - 240 mg; paracetamol - 180 mg; caffeine - 27.3 mg (caffeine monohydrate - 30 mg);
- auxiliary components: hydroxypropyl methylcellulose, potato starch, colloidal silicon dioxide, microcrystalline cellulose, citric acid monohydrate, crospovidone, lactose monohydrate, polyethylene glycol 6000, stearic acid;
- film casing: Opadry II (85 series), polyvinyl alcohol, macrogol, titanium dioxide, talc, black, yellow and red iron oxide.
Pharmacological properties
Pharmacodynamics
Citramon Ultra is a combined drug, its effects are due to the properties of the active ingredients:
- acetylsalicylic acid: has an antipyretic and anti-inflammatory effect, helps to relieve pain, especially associated with the inflammatory process, as well as inhibit platelet aggregation, reduce thrombus formation and improve microcirculation in the focus of inflammation;
- paracetamol: has antipyretic, analgesic and very mild anti-inflammatory effects; this is due to the effect of a substance in the hypothalamus on the center of thermoregulation and a weakly expressed ability to quickly inhibit the biosynthesis of prostaglandins in peripheral tissues;
- caffeine: increases the reflex excitability of the spinal cord, excites the vasomotor and respiratory centers, reduces platelet aggregation, dilates the blood vessels of the brain, skeletal muscles, kidneys, heart; helps to reduce the feeling of fatigue, drowsiness, increase physical and mental performance, accelerate blood flow and normalize the tone of the cerebral vessels; in a small dose in this combination, caffeine has practically no stimulating effect on the central nervous system.
Pharmacokinetics
Acetylsalicylic acid
The substance is absorbed sufficiently after oral administration. During absorption, there is a presystemic elimination in the liver and intestinal wall (deacetylation process). The absorbed part of the dose is rapidly hydrolyzed by albumin esterase and plasma cholinesterases. In the body, the substance circulates in connection with proteins at a level of up to 90%. Salicylates penetrate into body fluids and tissues easily, including peritoneal and synovial fluids, joint cavities. TC max (time to reach maximum concentration) for medicinal forms with buffering properties - 2 hours.
Biotransformation occurs in the liver, while 4 metabolites are formed. Ascorbic acid is excreted mainly by active secretion in the kidney tubules: 60% - in the form of salicylic acid, the rest - as metabolites. With alkalization of urine, the reabsorption of ionized salicylates worsens, their excretion increases significantly. The rate of elimination is determined by the dose, T 1/2 (half-life) is for small doses - 2-3 hours, with their increase - up to 15-30 hours. The elimination of salicylates in newborns is much slower than in adults. Salicylates cross the placenta and are excreted in small quantities in breast milk.
Paracetamol
The substance is rapidly absorbed from the gastrointestinal tract. C max (maximum concentration) is 5–20 μg / ml, the time to reach it is from 30 minutes to 2 hours. Binds to plasma proteins at a level of up to 15%. Penetrates the blood-brain barrier.
Metabolism occurs in the liver by conjugation with sulfates and glucuronides. Also, paracetamol is partially oxidized by liver microsomal enzymes. In this case, toxic intermediate metabolites are formed, which are then conjugated with glutathione, and then with mercapturic acid and cysteine. The main isozymes of cytochrome P450 for this metabolic pathway are CYP2E1, CYP1A2, and to a lesser extent, CYP3A4. The metabolites formed in this way in the case of a deficiency of glutathione can lead to damage and necrosis of hepatocytes.
In newborns and young children, sulfation prevails, in adults - glucuronidation. Conjugated metabolites of paracetamol have low pharmacological (including toxic) activity.
Additional metabolic pathways are methoxylation to 3-methoxyparacetamol and hydroxylation to 3-hydroxyparacetamol, which are subsequently conjugated to sulfates or glucuronides.
Excretion is carried out by the kidneys mainly in the form of conjugation products; up to 5% of the dose is excreted unchanged. T 1/2 ranges from 1 to 4 hours. In elderly patients, the clearance of the substance decreases, and T 1/2 increases.
Less than 1% of the paracetamol dose taken by a nursing mother passes into breast milk.
Caffeine
The substance is well absorbed in the intestines. Absorption occurs mainly not due to water solubility, but due to lipophilicity. TC max is 50–75 minutes, C max is in the range from 1.58 to 1.76 mg / l. The substance is quickly distributed in all tissues and organs, easily penetrates the blood-brain barrier and the placenta. V d (volume of distribution) is: adults - 0.4-0.6 l / kg; newborns - 0.78-0.92 l / kg. Caffeine binds to blood proteins (albumin) at a level of 25–36%.
In adults, more than 90% of the dose is metabolized in the liver, of which about 80% is metabolized into paraxanthine, about 10% into theobromine, and about 4% into theophylline. Subsequently, these compounds are demethylated to monomethylxanthines, then to methylated uric acids. In children of the first years of life, from 10 to 15% of caffeine is biotransformed.
T 1/2: adults - 3.9-5.3 hours (in some cases - up to 10 hours); children under 4-7 months - up to 130 hours.
Excretion is carried out mainly in the form of metabolites by the kidneys. Excretion unchanged: adults - 1–2%, newborns - up to 85%.
Indications for use
Citramon Ultra is prescribed for the relief of the following pains of various origins of mild and moderate severity: headache, myalgia, algodismenorrhea, neuralgia, migraine, toothache, arthralgia, as well as for the treatment of fever in ARVI (including influenza).
Contraindications
Absolute:
- gastrointestinal bleeding, erosive and ulcerative lesions of the gastrointestinal tract, gastric ulcer and duodenal ulcer (with exacerbation);
- full or partial combination of bronchial asthma with nasal polyposis and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;
- severe arterial hypertension, severe ischemic heart disease;
- surgical interventions that are accompanied by bleeding;
- portal hypertension;
- hemorrhagic diathesis, hemophilia, hypocoagulation, hypoprothrombinemia;
- vitamin deficiency K;
- renal failure;
- glaucoma;
- lactose intolerance, deficiency of glucose-6-phosphate dehydrogenase and lactase, glucose-galactose malabsorption;
- anxiety disorders (agoraphobia, panic disorder), sleep disorders, hyperexcitability;
- I and III trimesters of pregnancy, lactation period;
- age up to 15 years (associated with the risk of developing Reye's syndrome with hyperthermia against the background of viral diseases);
- individual intolerance to the components in Citramon Ultra.
Relative (Citramon Ultra is prescribed under medical supervision):
- gout;
- liver failure, liver disease, alcoholic liver damage;
- benign hyperbilirubinemia (including Gilbert's syndrome);
- alcoholism;
- II trimester of pregnancy;
- elderly age.
Citramon Ultra, instructions for use: method and dosage
Citramon Ultra tablets are taken orally with or after meals.
Recommended dosage: 1-2 tablets 3-4 times a day. The break between doses of single doses is from 4 to 8 hours. The maximum is 8 tablets per day.
Without the appointment / supervision of a doctor, the duration of the course should not exceed 3 or 5 days as an antipyretic or analgesic agent, respectively.
Side effects
- blood coagulation system: thrombocytopenia, anemia, hypocoagulation, methemoglobinemia, decreased platelet aggregation, hemorrhagic syndrome (manifested in the form of nosebleeds, bleeding gums, purpura, etc.);
- digestive system: nausea, gastralgia, hepatotoxicity, vomiting, erosive and ulcerative lesions of the gastrointestinal tract;
- heart and blood vessels: increased blood pressure, tachycardia;
- urinary system: kidney damage with papillary necrosis, nephrotoxicity;
- sense organs: tinnitus, visual impairment, deafness;
- allergic reactions: bronchospasm, skin rash, itching, angioedema, skin flushing, Stevens-Johnson syndrome, Lyell's syndrome;
- nervous system: headache, dizziness.
Children may develop Reye's syndrome, which manifests itself in the form of hyperpyrexia, metabolic acidosis, vomiting, impaired liver function, psyche and nervous system.
Possible side effects associated with the properties of the active ingredients of Citramon Ultra:
- paracetamol: nausea, epigastric pain, allergic reactions (manifested as skin rash, itching, Quincke's edema, urticaria); rarely - anemia, methemoglobinemia, thrombocytopenia; when carrying out a long course with the use of high doses - hepatotoxic and nephrotoxic effects;
- acetylsalicylic acid; dyspepsia (manifested in the form of nausea, stomach pain); with prolonged therapy - gastritis, gastric bleeding, gastric ulcer and duodenal ulcer; sometimes - allergic reactions (in the form of bronchospasm, Quincke's edema, skin reactions);
- caffeine: sometimes - ringing in the ears, insomnia, trembling limbs, palpitations, vomiting, shortness of breath; in case of abuse - drug dependence.
Overdose
The main symptoms of an overdose of Citramon Ultra, depending on the degree of intoxication:
- mild: dizziness, pallor of the skin, ringing in the ears, vomiting, gastralgia, nausea;
- severe: metabolic acidosis, impaired glucose metabolism, anorexia, bronchospasm, lethargy, collapse, drowsiness, convulsions, shortness of breath, anuria, bleeding.
Symptoms of liver dysfunction following an overdose may appear 12–48 hours later. In severe cases, it is possible to develop liver failure with progressive encephalopathy, coma, death. Other probable disorders: acute renal failure with tubular necrosis (including in the absence of severe liver damage), pancreatitis, arrhythmia.
Central hyperventilation of the lungs initially leads to respiratory alkalosis (in the form of shortness of breath, suffocation, cyanosis, increased sweating). Uncoupling of oxidative phosphorylation and progressive respiratory depression as intoxication intensifies can cause respiratory acidosis.
Therapy: it is necessary to constantly monitor the acid-base and electrolyte balances; after assessing the state of metabolism, sodium bicarbonate, citrate or sodium lactate can be prescribed. Against the background of increasing reserve alkalinity due to alkalization of urine, the excretion of acetylsalicylic acid increases.
Donators of SH-groups and precursors of glutathione synthesis are introduced: within 8-9 hours after overdose - methionine, within 8 hours - acetylcysteine. Additional therapeutic measures are determined by the doctor depending on the time elapsed after taking paracetamol and its concentration in the blood.
special instructions
It is impossible to prescribe the drug to children under 15 years of age, since acetylsalicylic acid is a part of Citramon Ultra, which, in the case of a viral infection, increases the risk of Reye's syndrome. Its symptoms include acute encephalopathy, prolonged vomiting, and enlarged liver. With prolonged therapy, monitoring of the functional state of the liver and peripheral blood is required.
In the case of the appointment of Citramon Ultra to patients with hypersensitivity or the presence of asthmoid responses to salicylates or other derivatives of acetylsalicylic acid, special precautions should be taken (in an emergency room).
One of the properties of acetylsalicylic acid is to slow down blood coagulation, in this regard, when planning a surgical intervention, you need to warn your doctor in advance about taking Citramon Ultra. Low doses of acetylsalicylic acid reduce the excretion of uric acid. In some cases, in patients with a corresponding predisposition, this can provoke the development of a gout attack.
Due to the increased likelihood of gastrointestinal bleeding during the period of therapy, it is recommended to refrain from using ethanol.
Influence on the ability to drive vehicles and complex mechanisms
Patients taking Citramon Ultra tablets should be careful when driving.
Application during pregnancy and lactation
In the I and III trimesters of pregnancy and during lactation, drug therapy is contraindicated.
In the II trimester of pregnancy, Citramon Ultra should be used with caution.
Acetylsalicylic acid has teratogenic properties. In the case of taking the drug in the first trimester of pregnancy, the likelihood of a malformation increases - splitting of the upper palate. In the third trimester, inhibition of labor is possible, closure of the ductus arteriosus in the fetus, which leads to hyperplasia of the pulmonary vessels and hypertension in the vessels of the pulmonary circulation.
Acetylsalicylic acid is excreted in breast milk, and due to dysfunction of platelets, the likelihood of bleeding in a child increases.
Pediatric use
Citramon Ultra is not prescribed to patients under 15 years of age.
With impaired renal function
In case of renal failure, Citramon Ultra is contraindicated.
For violations of liver function
Citramon Ultra is prescribed with caution to patients with liver disease, alcoholic liver damage and liver failure.
Use in the elderly
Citramon Ultra in elderly patients should be used under medical supervision.
Drug interactions
- heparin, indirect anticoagulants, reserpine, steroid hormones and hypoglycemic drugs: their effect is enhanced;
- non-steroidal anti-inflammatory drugs, methotrexate: the risk of side effects increases; with prolonged combined use, there is an increase in the likelihood of renal papillary necrosis and analgesic nephropathy, the onset of end-stage renal failure;
- salicylates (with high doses of paracetamol): the risk of bladder / kidney cancer increases;
- spironolactone, furosemide, drugs with hypotensive action, uricosuric drugs that promote the excretion of uric acid: their effectiveness decreases;
- inducers of liver microsomal enzymes (phenylbutazone, phenytoin, rifampicin, barbiturates, tricyclic antidepressants), hepatotoxic drugs, ethanol: there is an increase in the production of hydroxylated active metabolites, which leads to the possibility of severe intoxication even in the case of a minor overdose;
- barbiturates (long-term therapy): the effectiveness of paracetamol decreases;
- inducers of microsomal liver enzymes (including cimetidine): the risk of hepatotoxic effects of paracetamol decreases;
- metoclopramide: paracetamol absorption is accelerated;
- chloramphenicol: its T 1/2 increases significantly (associated with paracetamol);
- anticoagulants (coumarin derivatives; with combined repeated use of paracetamol): their effect is enhanced, which is associated with a decrease in the biosynthesis of procoagulant factors in the liver;
- ethanol: the risk of developing acute pancreatitis increases (associated with paracetamol);
- Diflunisal: the concentration of paracetamol in plasma increases significantly, while the likelihood of developing hepatotoxicity increases;
- myelotoxic drugs: the hematotoxicity of Citramon Ultra is enhanced;
- ergotamine: its absorption is accelerated (associated with caffeine).
Analogs
The analogues of Citramon Ultra are AquaCitramon, Askofen-P, Kofitsil-plus, Migrenol Extra, Citramon P, Citramarine, Excedrin, Citrapar, etc.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews of Citramone Ultra
Reviews of Citramone Ultra characterize it as a fast-acting pain reliever. The advantage of the drug is the presence of a film shell, which reduces the likelihood of a negative effect on the digestive tract. At the same time, many patients note that the cost of Citramon Ultra is unjustifiably overstated in comparison with analogues.
Price for Citramon Ultra in pharmacies
Approximate price for Citramon Ultra, film-coated tablets, for 10 pcs. in the package is 60-90 rubles.
Citramon Ultra: prices in online pharmacies
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Drug name Price Pharmacy |
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Citramon Ultra film-coated tablets 20 pcs. RUB 53 Buy |
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Citramon Ultra tablets p.o. 20 pcs. RUB 59 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
