Citramon P - instructions for use, dose, side effects, contraindications

Description:Round planocylindrical with a risk and facet of a tablet of light brown color with impregnations of white and brown color, with the smell of cocoa.

Pharmacotherapeutic group:Analgesic combined (NSAIDs + analgesic non-narcotic remedy + psychostimulant)

ATX: & nbsp

N.02.B.A.51 Acetylsalicylic acid in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined drug.

Acetylsalicylic acid has antipyretic and anti-inflammatory effect, relieves pain, especially caused by the inflammatory process,and also inhibits thrombus formation, improves microcirculation in the inflammatory focus.

Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, dilates the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation; reduces drowsiness, a feeling of fatigue, increases mental and physical performance. In this combination caffeine in a small dose practically does not have a stimulating effect on the central nervous system, it increases the tone of the vessels of the brain and promotes the acceleration of blood flow.

Paracetamol has analgeziruyuschim, antipyretic and weak anti-inflammatory effect, which is due to its influence on the center of thermoregulation in the hypothalamus and a weak ability to inhibit the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

After ingestion, all the components in the preparation of the preparation are absorbed quickly and completely. Wherein caffeine increases the bioavailability of paracetamol and acetylsalicylic acid. During absorption caffeine and acetylsalicylic acid are subjected to intensive biotransformation with the formation of active metabolites. From acetylsalicylic acid in the process of deacetylation in the wall of the intestine and liver is formed salicylic acid. Caffeine under the influence of cytochrome P450 isoform CYP1A2 the liver forms dimethylxanthines (theophylline, paraxanthin). The maximum concentration of all components in the blood plasma is achieved through 0.3-1.0 h. In plasma, about 80% of salicylic acid and 10-15% of paracetamol are in the albumin-bound state. The components of the drug easily penetrate into all tissues and body fluids. In the brain tissues, salicylates are found in small amounts, whereas paracetamol and caffeine levels are comparable to plasma. With the development of acidosis salicylic acid passes into a non-ionized form and its penetration into the tissues of the nervous system increases. All components quickly pass through the placenta, enter the breast milk. Metabolism of the components of the drug occurs in the liver. At the same time, 4 metabolites are formed from salicylic acid (salicylurate, salicyl-phenol glucuronide, gentisinic and gentisuronic acids); paracetamol forms 2 inactive metabolites of paracetamol-glucuronide and sulfate (80% of the total) and potentially toxic N-acetyl-benziminoquinone (N-ABI, about 17%). Caffeine forms dimethyl- and monomethylxanthines, dimethyl- and monomethyl-uric acids, trimethyl- and dimethylallantoin, derivatives of uridine. Under the influence of caffeine, the metabolism of paracetamol with the formation of N-ABI slightly increases (to 20-25%). Metabolism products are excreted by the kidneys in unchanged form 60% of salicylates, 10% of caffeine and 5% of paracetamol and in the form of metabolites. The rate of elimination of all components of the combination is approximately the same, the half-elimination period is 2-4.5 hours. With an increase in the dose of citramone II, a decrease in the elimination of acetylsalicylic acid is observed compared with other components up to 15 hours. In smokers, on the contrary, there is an acceleration in the elimination of caffeine and in comparison with other components of citramone P.

Indications:

Pain syndrome of mild and moderate severity (of various origins): headache, migraine, toothache, neuralgia, myalgia, arthralgia, algodismenorea. Feverish syndrome: with acute respiratory infections, influenza.

Contraindications:

- peptic ulcer of the stomach and duodenum in the phase of exacerbation;

- gastrointestinal hemorrhages (including in the anamnesis);

- expressed violations of the liver and / or kidney, gout;

- hemorrhagic diathesis, hemophilia, hypoprothrombinemia;

- surgical interventions, accompanied by heavy bleeding;

- deficiency of glucose-6-phosphate dehydrogenase;

- glaucoma;

- hypersensitivity to the components of the drug, bronchial asthma, urticaria or acute rhinitis, triggered by the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs;

- Children's age (under 15 years - the risk of developing Reye's syndrome in children with hyperthermia in the presence of viral diseases);

- increased excitability, sleep disturbance;

- organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis);

- arterial hypertension III degree;

- portal hypertension;

- avitaminosis K.

Carefully:

Renal and hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome, viral hepatitis, alcoholic liver damage), gout, alcoholism, epilepsy and propensity to convulsive seizures, elderly age.

Pregnancy and lactation:

Application during pregnancy and during lactation is contraindicated.

Dosing and Administration:

Inside (during or after a meal), 1 tablet every 4 hours, with a pain syndrome - 1-2 tablets; the average daily dose is 3-4 tablets, the maximum daily dose is 8 tablets. The course of treatment is no more than 5 days.

To reduce the irritant effect on the gastrointestinal tract, you should drink the tablet with milk or alkaline mineral water.

The drug should not be taken more than 5 days as an analgesic drug and more than 3 days - antipyretic (without appointment and supervision of a doctor).

Side effects:

There may be side effects that are typical of acetylsalicylic acid, paracetamol and caffeine: gastralgia, nausea, vomiting, hepatotoxicity, nephrotoxicity, anorexia, erosive and ulcerative lesions of the gastrointestinal tract and duodenal ulcers, gastrointestinal bleeding, allergic reactions (including syndrome Stevens-Johnson, Lyell), tachycardia, increased blood pressure, bronchospasm.

Overdose:

Symptoms (due to acetylsalicylic acid):

- with light intoxication: nausea, vomiting, gastralgia, dizziness, ringing in the ears;

- with severe intoxication: retardation, drowsiness, collapse, convulsions, bronchospasm, shortness of breath, anuria, bleeding. Initially, the central hyperventilation leads to respiratory alkalosis (shortness of breath, dyspnea, cyanosis, perspiration). With increasing intoxication, progressive paralysis of respiration and dissociation of oxidative phosphorylation cause respiratory acidosis.

Treatment: Continuous monitoring of the acid-base state and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Increased reserve alkalinity increases the excretion of acetylsalicylic acid due to alkalinization of urine.

Symptoms of overdose (due to paracetamol): in the first 24 hours - pallor, nausea, vomiting and pain in the abdominal region; through 12-48 h - kidney and liver damage with the development of hepatic insufficiency (encephalopathy, coma, death), cardiac arrhythmias and pancreatitis. Liver involvement is possible with 10 g or more (in adults).The risk of overdose increases in patients with alcoholic liver diseases of a non-cirrhotic nature.

Treatment: gastric lavage for the first 4 hours of poisoning, the appointment of methionine inside or to / in the introduction of acetylcysteine. With prolonged use - dizziness, headache, impaired vision. Tinnitus, platelet aggregation reduction, hypocoagulation, hemorrhagic syndrome (epistaxis, bleeding gums, purpura, etc.), renal failure with papillary necrosis, deafness syndrome Reye in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, impaired liver function).

Interaction:

Interaction caused by acetylsalicylic acid:

- increases the toxicity of methotrexate, reducing its renal clearance, valproic acid;

- It enhances the effects of other nonsteroidal anti-inflammatory drugs, narcotic analgesics, oral hypoglycemic drugs, heparin, anticoagulants, thrombolytics, and antiplatelet drugs, sulfonamides (including co-trimoxazole), triiodothyronine;

- reduces the effect of uricosuric medicines (benzbromarone, sulfinpyrazone), antihypertensive drugs, diuretics (spironolactone, furosemide);

- glucocorticosteroids, ethanol and ethanol-containing drugs increase the damaging effect on the mucous membrane of the gastrointestinal tract, increase the risk of developing gastrointestinal bleeding;

- increases the concentration of digoxin, barbiturates, lithium salts in plasma.

- antacids containing magnesium and / or aluminum slow down and worsen the absorption of acetylsalicylic acid.

- Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Interaction due to paracetamol:

- reduces the effectiveness of uricosuric medicines;

- concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (decreased synthesis of procoagulant factors in the liver);

- inducers of microsomal oxidation in the liver (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication even with a slight overdose;

- long-term use of barbiturates reduces the effectiveness of paracetamol;

- Ethanol promotes the development of acute pancreatitis;

- inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxic action;

- prolonged sharing of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure;

- simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer;

- diflunisal increases the plasma concentration of paracetamol by 50% - the risk of hepatotoxicity;

- Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Interaction with caffeine:

- caffeine is an adenosine antagonist (large doses of adenosine may be required);

- with the joint use of caffeine and barbiturates, primidone, anticonvulsant drugs (hydantoin derivatives, especially phenytoin) it is possible to increase metabolism and increase caffeine clearance; cimetidine, oral contraceptive drugs, disulfiram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increasing blood concentrations);

- caffeine-containing drinks and other medicines that stimulate the central nervous system - excessive stimulation of the central nervous system is possible;

- mexiletine - reduces the excretion of caffeine to 50%;

- nicotine - increases the rate of caffeine withdrawal;

- monoamine oxidase inhibitors, furazolidone, procarbazine and selegiline - large doses of caffeine can cause the development of dangerous cardiac arrhythmias or a marked increase in blood pressure;

- caffeine reduces the absorption of calcium in the gastrointestinal tract;

- reduces the effect of narcotic and hypnotic drugs;

- increases the excretion of lithium drugs with urine;

- accelerates absorption and enhances the action of cardiac glycosides, increases their toxicity;

- the joint use of caffeine with beta-blockers can lead to mutual suppression of therapeutic effects; with adrenergic bronchodilator drugs - to additional stimulation of the central nervous system and other additive toxic effects;

- caffeine can reduce the clearance of theophylline and possibly other xanthines, increasing the possibility of additive pharmacodynamic and toxic effects.

Special instructions:

Do not administer the drug to children under 15 years of age, especially with chickenpox, influenza, in the presence of acute respiratory viral infections, because of the high risk of the syndrome Reye. Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver. Because the acetylsalicylic acid slows the clotting of the blood, the patient, if he is to undergo surgery, must warn the doctor in advance about taking the drug.

A dose of 2-3 g / day of acetylsalicylic acid can lead to a delay in uric acid in the blood plasma due to a violation of the excretory function of the kidneys.

Since the use of acetylsalicylic acid decreases the excretion of uric acid salts, predisposing patients may have an exacerbation (attack) of gout.

During the intake should refrain from drinking alcohol (increased risk of gastrointestinal bleeding).

Effect on the ability to drive transp. cf. and fur:

Since when the drug is likely to cause bronchospasm and increase blood pressure, it is recommended during treatment to refrain from practicing potentially dangerous activities that require increased attention and speed of mental and motor reactions, including. management of vehicles.

Form release / dosage:

Pills.

Packaging:

For 10 tablets in a contour non-cellular package of paper with a polymer coating. 10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil or paper with a polymer coating.

For 100 contour packs, together with an equal number of instructions for use are placed in a group box - a box of cardboard.

Storage conditions:

In a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LS-002586

Date of registration:17.04.2012

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp05.04.2013

Illustrated instructions

Instructions

Citramon P (Citramon P)