Citramon-Borimed

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Latin name: Citramon-Borimed

ATX code: N02BA51

Active ingredient: acetylsalicylic acid (Acetylsalicylic acid) + caffeine (Caffeine) + paracetamol (Paracetamol)

Manufacturer: JSC "Borisov Plant of Medical Products" (JSC "BZMP") (Republic of Belarus)

Description and photo update: 2019-09-07

Citramon-Borimed is a combined drug designed to relieve pain of moderate and mild severity.

Release form and composition

Dosage form - tablets: light brown with white blotches, flat, with a chamfer and a risk, have a mild cocoa smell (in blisters of 10 tablets, in a cardboard box 1 package and instructions for the use of Citramon-Borimed; in contour bezel-less packages according to 6 tablets).

Composition for 1 tablet:

active substances: acetylsalicylic acid - 220 mg; paracetamol - 200 mg; caffeine - 27 mg;
auxiliary components: stearic acid, cocoa, talc, potato starch, food citric acid monohydrate.

Pharmacological properties

Pharmacodynamics

Citramon-Borimed is one of the combined preparations, the action of which is due to the properties of the active ingredients:

acetylsalicylic acid: has antipyretic and anti-inflammatory effects; helps to relieve pain, especially caused by the inflammatory process; also, its effect is aimed at improving microcirculation in the focus of inflammation and suppressing thrombus formation;
caffeine: promotes an increase in reflex excitability of the spinal cord, dilation of blood vessels of skeletal muscles, kidneys, heart, brain, reduction of platelet aggregation, excitation of vasomotor and respiratory centers; also, its effect is aimed at reducing drowsiness, feelings of fatigue, accelerating blood flow, increasing the tone of the vessels of the brain;
paracetamol: has an analgesic, antipyretic and weak anti-inflammatory effect, it is based on the effect on the center of thermoregulation in the hypothalamus and a weak ability to inhibit the biosynthesis of prostaglandins that occurs in peripheral tissues.

Pharmacokinetics

All active ingredients that make up Citramon-Borimed are absorbed quickly and in full enough after oral administration. At the same time, caffeine increases the bioavailability of other active ingredients.

Caffeine and acetylsalicylic acid undergo intensive biotransformation during absorption, in the process of which active metabolites are formed. Salicylic acid is formed from acetylsalicylic acid in the intestinal wall and liver during deacetylation. Caffeine is metabolized in the liver to dimethylxanthines (paraxanthine, theophylline) under the influence of the cytochrome P ₄₅₀ isoform CYP1A2.

The maximum plasma concentration of all components in the blood is reached in 20-60 minutes. About 10-15% of paracetamol and about 80% of salicylic acid are in the plasma bound to albumin.

The components of Citramon-Borimed easily penetrate into all body fluids and tissues. Salicylates are found in small amounts in brain tissues, while levels of caffeine and paracetamol are comparable to plasma levels. With the development of acidosis, salicylic acid passes into a non-ionized form, while its penetration into the tissues of the nervous system increases.

All active ingredients of the drug quickly pass through the placenta and into breast milk.

The final metabolic process takes place in the liver. 4 metabolites are formed from salicylic acid (salicylovophenolic glucuronide, salicylurate, gentisuronic and gentisic acids), paracetamol forms two inactive metabolites (paracetamol-glucuronide and sulfate, the latter makes up 80% of the total amount) and the potentially toxic M-acetyl-benziminoquinone), accounting for about 17% of the total. Caffeine forms mono- and dimethylmethylxanthines, mono- and dimethylmethyl uric acids, trimethyl- and dimethylallantoin, uridine derivatives.

The metabolism of paracetamol with the formation of N-ABI under the influence of caffeine increases slightly (up to 20-25%).

Metabolic products are excreted by the kidneys unchanged (salicylates - 60%, caffeine - 10%, paracetamol - 5%) and as metabolites. The elimination rate of all active substances of the combination is approximately the same, T _1/2 (half-life) is in the range from 2 to 4.5 hours. With an increase in the dose of Citramon-Borimed, the excretion of acetylsalicylic acid slows down in comparison with the other components up to 15 hours, in smokers, the elimination of caffeine is accelerated in comparison with the other components.

Indications for use

pain syndrome of moderate and weak severity: headache and toothache, migraine, algomenorrhea, neuralgia, arthralgia, myalgia;
febrile syndrome of various etiologies (Citramon-Borimed is used as an antipyretic agent).

Contraindications

renal and hepatic impairment;
congenital hyperbilirubinemia;
bronchial asthma, acute rhinitis or urticaria associated with the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs in history;
benign hyperbilirubinemia (including viral hepatitis, Gilbert's syndrome, alcoholic liver damage);
blood diseases, anemia, leukopenia;
deficiency of glucose-6-phosphate dehydrogenase;
gastrointestinal bleeding (including a history);
exacerbation of gastric ulcer and duodenal ulcer;
hemophilia, hemorrhagic diathesis, hypoprothrombinemia;
vitamin K deficiency;
gout;
severe cardiovascular diseases, including rhythm disturbances, severe coronary heart disease, severe atherosclerosis, severe arterial hypertension and heart failure;
states of sleep disturbance, increased arousal;
portal hypertension;
alcoholism;
glaucoma;
epilepsy and tendency to seizures;
combined use with monoamine oxidase inhibitors (including 14 days after their withdrawal);
combined use with methotrexate at a dose of 15 mg per week or more;
surgical interventions that are accompanied by profuse bleeding;
age up to 18 years;
elderly age;
pregnancy and lactation;
individual intolerance to the components of Citramon-Borimed, other xanthine derivatives (theophylline, theobromine) and salicylates.

Citramon-Borimed, instructions for use: method and dosage

Citramon-Borimed tablets are taken orally, preferably immediately after a meal or between meals.

The recommended dosing regimen for adults: 2-3 times a day (with an interval of at least 6-8 hours), 1 tablet. The maximum single dose is 2 tablets. You can take no more than 4 tablets per day.

As an antipyretic agent, Citramon-Borimed is prescribed at a body temperature of 38.5 ° C (with a burdened history of febrile convulsions - at a temperature of 37.5 ° C) in a dose of 1-2 tablets.

Duration of use - up to 3 or 5 days (as an antipyretic and pain reliever, respectively).

Side effects

digestive system: dyspeptic disorders, including vomiting, nausea, pain and discomfort in the epigastrium, heartburn, abdominal pain, inflammation and erosive and ulcerative lesions of the gastrointestinal tract, which in some cases can cause gastrointestinal bleeding and perforation with corresponding clinical and laboratory manifestations;
immune system: hypersensitivity reactions, including anaphylaxis, rhinitis, anaphylactic shock, nasal congestion;
endocrine system: hypoglycemia, up to hypoglycemic coma;
skin and subcutaneous tissue: itching, rash on mucous membranes and skin (including urticaria and erythematous rashes), angioedema, exudative erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome;
hepatobiliary system: increased activity of hepatic enzymes, mainly without the development of jaundice, hepatonecrosis (is a dose-dependent effect);
cardiovascular system: palpitations, tachycardia, arterial hypertension;
neurological disorders: general weakness, anxiety, headache, dizziness, ringing in the ears, insomnia, sleep disturbance, anxiety, paresthesia, tremor, fear, agitation, irritability;
blood and lymphatic system: anemia, sulfate hemoglobinemia and methemoglobinemia (in the form of cyanosis, shortness of breath, pain in the heart), hemolytic anemia; increased risk of bleeding (associated with the antiplatelet effect of acetylsalicylic acid on platelets); during therapy, bleeding may occur such as hematomas, intraoperative and cerebral hemorrhages, nasal and gastrointestinal bleeding, bleeding from the organs of the genitourinary system, gums;
urinary system: nephrotic syndrome, papillary necrosis, interstitial nephritis, renal failure (with prolonged use);
others: noncardiogenic pulmonary edema, acute or chronic post-hemorrhagic anemia / iron deficiency anemia (associated with the so-called latent microbleeding) with corresponding clinical symptoms (in the form of asthenia, pallor of the skin, hypoperfusion) and laboratory manifestations.

Overdose

Signs of an overdose of Citramon-Borimed

The main symptoms of a drug overdose are determined by the active ingredient that caused it.

Paracetamol overdose

Liver damage can occur in adults and children who have taken from 10,000 mg and from 150 mg / kg of paracetamol, respectively.

In the first 24 hours, the following disorders are observed: pallor of the skin, vomiting, nausea, headache, anorexia, hepatonecrosis, an increase in the prothrombin index, an increase in the activity of hepatic transaminases. Liver damage can occur 12–48 hours after taking excessive doses of the substance. Possible metabolic acidosis and impaired glucose metabolism.

Liver failure against the background of severe poisoning can lead to consequences such as encephalopathy, coma and death. Acute renal failure in combination with acute tubular necrosis may occur even in patients without severe renal impairment.

There is also information about cardiac arrhythmias. With prolonged use of high doses, disorders may develop in the form of aplastic anemia, thrombocytopenia, pancytopenia, agranulocytosis, neutropenia, leukopenia.

Caffeine overdose

When taking large doses of caffeine, pain in the epigastric region, vomiting, rapid breathing, diuresis, extrasystole, tachycardia or cardiac arrhythmia are possible.

Overdose can affect the central nervous system, which is manifested by dizziness, insomnia, nervous excitement, irritability, passion, anxiety, tremors, convulsions.

Overdose of acetylsalicylic acid

An overdose of salicylates can lead to chronic intoxication resulting from long-term treatment (when using the drug at a dose of 100 mg / kg per day for more than 2 days, toxic effects are possible), as well as acute intoxication (as a result of accidental use by children or unintentional overdose).

Chronic poisoning can be latent, since there are no specific signs. Moderate chronic intoxication associated with the intake of salicylates, in most cases, occurs only after repeated administration of large doses of the drug.

An overdose of acetylsalicylic acid is manifested by imbalance, dizziness, ringing in the ears, deafness, increased sweating, nausea and vomiting, headache, confusion. These symptoms can be controlled by dose reduction.

At a plasma concentration of salicylates in the blood of 0.15–0.3 mg / ml, ringing in the ears may occur. The development of serious side effects occurs when the plasma concentration of salicylates in the blood is from 0.3 mg / ml.

A sign of acute intoxication is a pronounced change in the acid-base balance, which differs depending on the severity of intoxication and age. It is impossible to determine the severity of the condition only on the basis of the plasma concentration of salicylates in the blood.

Citramon-Borimed overdose therapy

At the first signs of intoxication, the abolition of Citramon-Borimed is indicated. To prevent absorption of the drug in the stomach and intestines, gastric lavage with activated charcoal is prescribed, and saline laxatives (magnesium sulfate) are taken. Alkalizing agents are introduced to maintain urine pH at 7.5–8.0. With a plasma level of salicylates of 300 and 500 mg / l (2.2 and 3.6 mmol / l) in children and adults, respectively, forced alkaline diuresis is required (intravenous infusion of sodium bicarbonate 88 mEq / l and 5% glucose solution at a rate of 10– 15 ml / kg / h with furosemide at a dose of 40-60 mg).

It is necessary to ensure the restoration of the volume of circulating blood and to correct the acid-base state.

Other possible measures depending on the indications:

cerebral edema: artificial ventilation of the lungs with an oxygen-enriched mixture in the mode of positive pressure at the end of exhalation; hyperventilation in combination with osmotic diuretics;
liver damage: N-acetylcysteine is introduced - a specific antidote to paracetamol. 20% N-acetylcysteine solution can be administered orally and intravenously. The first dose is 140 mg / kg (0.7 ml / kg), then it is halved. A total of 17 doses are shown. The best results are achieved if treatment is started in the first 10 hours after the development of intoxication. After 36 hours from the moment of intoxication, this method of therapy is considered ineffective;
an increase in the prothrombin index: if the value of the indicator exceeds 1.5, the use of 1-10 mg of vitamin K ₁ (phytomenadione) is indicated; when this value is increased to 3 or more, it is necessary to start the infusion of native plasma or a concentrate of coagulation factors (from 1 to 2 units).

Hemodialysis in the treatment of intoxication is contraindicated. The use of glucocorticosteroids and antihistamines is unacceptable. It is not recommended to use acetazolamide to alkalize urine, which is associated with the likelihood of acidemia and increased toxic effects of salicylate.

special instructions

The combined use of Citramon-Borimed with other drugs containing paracetamol and acetylsalicylic acid is not recommended. It is necessary to observe the prescribed doses and the duration of the course of use.

Citramon-Borimed should be used with caution in patients with a history of gastrointestinal ulcers, including those with a history of chronic / recurrent peptic ulcer disease or gastrointestinal bleeding and when combined with anticoagulants, in case of impaired renal and / or hepatic function …

The likelihood of damage to the hepatic function with paracetamol in the presence of liver disease increases. In patients with alcoholic liver damage, the risk of overdose is higher. You should refrain from drinking alcohol during the period of therapy, as this increases the risk of toxic liver damage and gastrointestinal bleeding.

It is not recommended to consume excessive amounts of caffeinated drinks (for example, coffee, tea) while taking Citramon-Borimed. This is due to the likelihood of developing sleep disorders, tremors, irritability, feeling of tension, palpitations.

Acetylsalicylic acid helps to reduce the excretion of uric acid from the body, which can lead to an acute attack of gout in predisposed patients.

The use of acetylsalicylic acid can cause the development of bronchospasm, an attack of bronchial asthma or other hypersensitivity reactions. Risk factors: aggravated history of bronchial asthma, hay fever, nasal polyposis, bronchopulmonary diseases, cases of allergies (skin rashes, allergic rhinitis).

Acetylsalicylic acid helps to slow down blood clotting. This effect persists for several days after administration, which must be taken into account if surgical interventions are necessary, including minor operations (for example, tooth extraction).

In patients with glucose-6-phosphate dehydrogenase deficiency, acetylsalicylic acid can cause hemolytic anemia or hemolysis. Contributing factors are acute infection or the use of high doses.

In hemochromatosis, thalassemia, as well as in the presence of a predisposition to recurrent nephrolithiasis or nephrolithiasis from calcium oxalate, when using Citramon-Borimed, care must be taken.

Influence on the ability to drive vehicles and complex mechanisms

While taking Citramon-Borimed in high doses, you should refrain from driving and performing other types of work with potentially dangerous consequences. This is due to the significant likelihood of developing side effects from the nervous system, such as increased excitability, dizziness, impaired attention and orientation.

Application during pregnancy and lactation

Citramon-Borimed is not prescribed during pregnancy / lactation.

Pediatric use

Due to the existing risk of Reye's syndrome with hyperthermia against the background of viral diseases (in the form of hyperpyrexia, metabolic acidosis, mental and nervous system disorders, vomiting, liver dysfunctions), Citramon-Borimed is not prescribed to patients under 18 years of age.

With impaired renal function

It is contraindicated to take Citramon-Borimed tablets for renal failure.

For violations of liver function

Citramon-Borimed is contraindicated in liver failure.

Use in the elderly

It is contraindicated to use Citramon-Borimed in elderly patients.

Drug interactions

Contraindicated combinations with Citramon-Borimed:

methotrexate (15 mg per week): in the case of combined use with salicylates, the hematological toxicity of methotrexate increases, which is associated with a decrease in its renal clearance by anti-inflammatory agents and its displacement from its bonds with plasma proteins;
monoamine oxidase inhibitors: in the case of combined use with caffeine, a dangerous increase in blood pressure can be noted.

Paracetamol in the composition of Citramon-Borimed requires caution in combined use with the following substances / preparations:

antidepressants and other stimulants of microsomal oxidation: there is an increase in the production of hydroxylated active metabolites that affect hepatic function, which, with small overdose of the drug, causes severe intoxication;
diuretics: against the background of combined use, their effectiveness decreases;
cholestyramine: the rate of absorption of paracetamol may be reduced;
metoclopramide, domperidone: the rate of absorption of paracetamol may increase;
coumarin derivatives (warfarin): with prolonged use of paracetamol, the risk of bleeding increases;
chloramphenicol: its half-life is increased by 5 times.

Caffeine in Citramon-Borimed requires caution when used in combination with the following substances / preparations:

hormonal contraceptives, cimetidine, isoniazid: enhance the effect of caffeine;
opioid analgesics, anxiolytics, drugs with hypnotics and sedatives: their effect is reduced;
drugs for anesthesia and other drugs that depress the central nervous system: caffeine, being an analeptic, antagonizes them;
drugs that depress the central nervous system, adenosine drugs, adenosine triphosphates: caffeine is their competitive antagonist;
ergotamine: its absorption in the gastrointestinal tract is improved;
thyroid-stimulating agents: the thyroid effect increases;
analgesics-antipyretics: their effectiveness is enhanced (due to improved bioavailability);
xanthine derivatives, α- and β-adrenomimetics, psychostimulants: caffeine potentiates their effects;
lithium preparations: against the background of the use of caffeine, the concentration of lithium in the blood decreases.

Acetylsalicylic acid in the composition of Citramon-Borimed requires caution in combined use with the following substances / preparations:

uricosuric agents (probenecid, benzbromarone): the effect of excretion of uric acid is reduced;
angiotensin-converting enzyme inhibitors (in combination with acetylsalicylic acid in high doses): there is a decrease in filtration in the glomeruli due to inhibition of the vasodilatory effect of prostaglandins and a decrease in the hypotensive effect;
digoxin: its plasma concentration in the blood will increase due to a decrease in renal excretion;
valproic acid: its toxicity increases, since it is displaced by acetylsalicylic acid from the connection with blood plasma proteins;
selective serotonin reuptake inhibitors: the risk of bleeding from the upper digestive tract increases (due to the possibility of a synergistic effect);
corticosteroids, sulfonylurea derivatives, methotrexate: their side effects are enhanced;
drugs that reduce platelet aggregation and blood clotting: acetylsalicylic acid potentiates their effectiveness;
barbiturates, anticonvulsants, salicylates, rifampicin, alcohol: combinations are recommended to be avoided.

Analogs

Citramon-Borimed analogs are Citramon P, Kofitsil-plus, Excedrin, Askofen-P, Aquacitramon, Acifein, Tsitramon-LekT, Citrapar, Citramarin, 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 4 years.

Terms of dispensing from pharmacies

Available without a prescription.

Reviews of Citramone-Borimed

On specialized sites, there are mainly positive reviews about Citramone-Borimed. Patients note that the drug has a quick effect, most often it is taken for headaches. Reports of the development of side effects are extremely rare.

Price for Citramon-Borimed in pharmacies

The price of Citramon-Borimed is unknown, since the drug is not available in pharmacies.

The approximate cost of analogs:

Citramon P (10 tablets) - 15 rubles;
Askofen-P (10 tablets) - 18 rubles;
Excedrin (10 coated tablets) - 159 rubles.

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!