Citramon: side effects, instructions

"Citramon": composition and other characteristics

"Citramon" is an anesthetic that prevents inflammatory processes and also has an antipyretic effect. The only form of release is tablets. They are packaged in cardboard packages, each containing 10 or 6 pieces.

The active ingredient is acetylsalicylic acid (240 mg per tablet). The following are used as auxiliary components:

citric acid (20 mg);
phenacetin (180 mg);
caffeine (20 mg).

The composition and dosage of components may vary significantly, as determined by manufacturers. The features of the tablet may also differ. For example, “Citramon Ultra”, unlike the classic “Citramon”, is a drug with film-coated tablets. This makes oral administration easier.

The effect on the body is complex:

Acetylsalicylic acid reduces temperature and resists inflammatory processes.
Caffeine stimulates excitation processes in the central nervous system and activates the brain.
In combination with acetylsalicylic acid and paracetamol, the drug has a pronounced analgesic effect.

The product is available freely and does not require a prescription. Stored at normal room temperature up to 25 degrees. The shelf life is 2 years from the date of production.

For reference

One of the common types of the drug is Citramon P. Along with the main components, it contains paracetamol, which enhances the analgesic and antipyretic effect.

Citramon Ultra, 20 pcs., film-coated tablets

Acetylsalicylic acid: after oral administration it is absorbed quite completely. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated).

The absorbed part is quickly hydrolyzed by plasma cholinesterases and albuminesterase. In the body, acetylsalicylic acid circulates in association with proteins up to 90%. Salicylates easily penetrate into tissues and body fluids, including joint cavities, synovial and peritoneal fluids. TCmax - 2 hours for dosage forms with buffering properties.

Biotransforms in the liver to form 4 metabolites. Removal of acetylsalicylic acid is carried out mainly by active secretion in the renal tubules in the form of salicylic acid itself (60%) and its metabolites. When urine becomes alkalized, the reabsorption of ionized salicylates worsens, and their excretion increases significantly. The rate of elimination depends on the dose: when taking small doses, T1/2 is 2-3 hours, with increasing doses it can increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults. Salicylates cross the placenta and are excreted in small quantities in breast milk.

Paracetamol: quickly absorbed from the gastrointestinal tract. TCmax - 0.5-2 hours; Cmax - 5-20 mcg/ml. Communication with plasma proteins is up to 15%. Penetrates the blood-tencephalic barrier (BBB).

In adults, glucuronidation predominates, in newborns and small children - sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

Additional metabolic pathways for paracetamol are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates. Excreted by the kidneys mainly in the form of conjugation products, less than 5% is excreted unchanged. T1/2 -1-4 hours. In elderly patients, drug clearance decreases and T1/2 increases.

Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk.

Caffeine: well absorbed in the intestines. Absorption occurs primarily due to lipophilicity rather than water solubility. Tmax - 50-75 minutes after oral administration, Cmax - 1.58-1.76

mg/l. It is quickly distributed in all organs and tissues of the body, easily penetrates the BBB and the placenta. The volume of distribution in adults is 0.4-0.6 l/kg, in newborns - 0.78-0.92 l/kg. Communication with blood proteins (albumin) - 25-36%.

More than 90% is metabolized in the liver, in children of the first years of life up to 10-15%. In adults, about 80% of a caffeine dose is metabolized to paraxanthine, about 10% to theobromine, and about 4% to theophylline. These compounds are subsequently demethylated into monomethylxanthines and then into methylated uric acids.

T1/2 in adults - 3.9-5.3 hours (sometimes - up to 10 hours), in newborns (up to 4-7 months of life) - up to 130 hours.

It is excreted primarily by the kidneys in the form of metabolites. Excretion of 1-2% of caffeine in adults and up to 85% in newborns occurs unchanged.

What do Citramon tablets help with?

The main purpose of the drug is to relieve moderate and mild pain in the presence of concomitant diseases:

ARVI;
flu;
general malaise;
febrile syndrome;
neuralgia;
arthralgia;
algodysmenorrhea;
migraine;
myalgia;

The drug is used to treat headaches, muscle pain, dental pain, and joint pain. "Citramon" is effective in relieving any pain that is associated with inflammatory processes. It contains several active components that mutually enhance each other's actions.

Contraindications for use

Restrictions associated with the use of the product contain a fairly large list of disorders and diseases:

nasal polyposis;
bronchial asthma;
hypersensitivity to one or more components;
bleeding of the gastrointestinal tract;
diathesis of hemorrhagic type;
erosion, ulcer of the gastrointestinal tract (in the acute stage);
portal hypertension"
severe course of coronary heart disease;
hemophilia;
renal failure;
increased nervous excitability;
kidney failure;
sleep problems;
bleeding during operations;
severe hypertension;
glaucoma;
simultaneous use of anticoagulant drugs;
aortic aneurysm;
pregnancy period (especially during the 1st and 3rd trimesters);
feeding period (any stage);
children up to 15 years old inclusive.

There are also relative contraindications in which Citramon should be taken with caution. These are liver dysfunctions, as well as gout.

Citramon Ultra

Acetylsalicylic acid: after oral administration it is absorbed quite completely. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is quickly hydrolyzed by plasma cholinesterases and albuminesterase. In the body, acetylsalicylic acid circulates in association with proteins up to 90%. Salicylates easily penetrate into tissues and body fluids, including joint cavities, synovial and peritoneal fluids.

TCmax - 2 hours for dosage forms with buffering properties.

Biotransforms in the liver to form 4 metabolites.

Removal of acetylsalicylic acid is carried out mainly by active secretion in the renal tubules in the form of salicylic acid itself (60%) and its metabolites. When urine becomes alkalized, the reabsorption of ionized salicylates worsens, and their excretion increases significantly.

The rate of elimination depends on the dose: when taking small doses, T1/2 is 2-3 hours, with increasing doses it can increase to 15-30 hours.

In newborns, the elimination of salicylates is much slower than in adults.

Salicylates cross the placenta and are excreted in small quantities in breast milk.

Metabolized in the liver by conjugation with glucuronides and sulfates, and is also partially oxidized by microsomal liver enzymes. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this metabolic pathway are the isoenzyme CYP2E1, CYP1A2 and, to a lesser extent, CYP3A4. With glutathione deficiency, these metabolites can cause damage and necrosis of hepatocytes. In adults, glucuronidation predominates; in newborns, sulfation predominates. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

Additional metabolic pathways for paracetamol are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.

Excreted by the kidneys mainly in the form of conjugation products, less than 5% is excreted unchanged. T1/2 - 1-4 hours.

In elderly patients, drug clearance decreases and T1/2 increases.

Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk.

Caffeine: well absorbed in the intestines. Absorption occurs primarily due to lipophilicity rather than water solubility. Tmax - 50-75 minutes after oral administration, Cmax - 1.58-1.76 mg/l. It is quickly distributed in all organs and tissues of the body, easily penetrates the BBB and the placenta.

The volume of distribution in adults is 0.4-0.6 l/kg, in newborns - 0.78-0.92 l/kg. Communication with blood proteins (albumin) - 25-36%.

T1/2 in adults - 3.9-5.3 hours (sometimes - up to 10 hours), in newborns (up to 4-7 months of life) - up to 130 hours.

It is excreted primarily by the kidneys in the form of metabolites. Excretion of 1-2% of caffeine in adults and up to 85% in newborns occurs unchanged.

Side effects

In case of overdose, long-term use, chronic diseases, as well as individual intolerance to the components, side effects are possible:

anorexia;
nausea;
bleeding of the gastrointestinal tract;
the appearance of ulcers on the mucous membranes of the gastrointestinal tract;
liver failure;
hypersensitivity;
nephrotic syndrome;
kidney failure;
anemia;
fatty hepatosis in acute form;
complications associated with heart failure;
sleep disorders, insomnia;
headaches;
tinnitus;
dizziness;
increased anxiety;
heart rhythm disturbances;
high blood pressure;
psychological dependence (only in case of long-term use of high doses).

Cases of overdose

In small quantities, an overdose leads to ringing in the ears, nausea, vomiting, dizziness, and pale skin. In case of severe overdose, more serious disorders are observed:

breathing problems;
circulatory disorders;
increased anxiety;
feeling dazed;
headache;
nausea;
bleeding;
sweating;
fatigue, increased drowsiness;
convulsions;
extremely rarely - coma.

In these cases, you must immediately stop taking the drug and its analogues with the same active ingredients. If the symptoms are severe, you will need to seek emergency medical help.

Instructions for use CITRAMONUM-BORIMED

Symptoms.

Symptoms of paracetamol overdose. Liver damage is possible in adults who took 10 g or more of paracetamol, and in children who took the drug more than 150 mg/kg body weight. In the first 24 hours:

pallor, nausea, vomiting, anorexia and headache, hepatonecrosis, increased activity of “liver” transaminases, increased prothrombin index. Liver damage may appear 12-48 hours after taking excess doses of the drug. Impaired glucose metabolism and metabolic acidosis may occur. In severe poisoning, liver failure can lead to encephalopathy, coma and death. Acute renal failure with acute tubular necrosis can develop even in the absence of severe kidney damage. Cardiac arrhythmia was also noted. With long-term use of high doses, aplastic anemia, thrombocytopenia, pancytopenia, agranulocytosis, neutropenia, leukopenia are possible.

Symptoms of caffeine overdose. Large doses of caffeine can cause pain in the epigastric region, vomiting, diuresis, rapid breathing, extrasystole, tachycardia or cardiac arrhythmia, and affect the central nervous system (dizziness, insomnia, nervous agitation, irritability, state of passion, anxiety, tremor, convulsions).

Symptoms of an overdose of acetylsalicylic acid. In case of an overdose of salicylates, chronic intoxication resulting from long-term therapy is possible (use of the drug more than 100 mg/kg/day for more than 2 days can lead to toxic effects), as well as acute intoxication, the causes of which may be accidental use by children or an unintentional overdose.

Chronic poisoning with salicylates can be hidden, since its symptoms are nonspecific. Moderate chronic intoxication caused by salicylates occurs, as a rule, only after repeated doses of large doses.

Symptoms Impaired balance, dizziness, ringing in the ears, deafness, increased sweating, nausea and vomiting, headache, confusion. These symptoms can be controlled by reducing the dose. Tinnitus can occur when the concentration of salicylates in the blood plasma is more than 150-300 mcg/ml. Serious adverse reactions occur when the concentration of salicylates in the blood plasma is more than 300 mcg/ml. Acute intoxication is indicated by a pronounced change in the acid-base balance, which may differ depending on the age and severity of intoxication. The severity of the condition cannot be determined solely on the basis of the concentration of salicylates in the blood plasma.

Treatment:

discontinuation of the drug, gastric lavage with activated charcoal and administration of saline laxatives (magnesium sulfate) to prevent absorption of the drug in the stomach and intestines. Introduction of alkalizing agents to maintain urine pH values at 7.5-8.0. When the level of salicylates in plasma exceeds 300 mg/l (2.2 mmol/l) in children and 500 mg/l (3.6 mmol/l) in adults, forced alkaline diuresis is indicated (provided by intravenous infusion of sodium bicarbonate 88 mEq/l and 5% glucose at a rate of 10-15 ml/kg/h with furosemide 40-60 mg). The volume of circulating blood is restored and the acid-base state is corrected. In case of cerebral edema, artificial ventilation of the lungs with an oxygen-enriched mixture in positive end-expiratory pressure mode is indicated. For cerebral edema, hyperventilation is performed in combination with the administration of osmotic diuretics.

In the presence of liver damage, a specific antidote of paracetamol, N-acetylcysteine, is administered. A 20% solution of N-acetylcysteine is used intravenously and orally:

first dose 140 mg/kg (0.7 ml/kg), then 70 mg/kg (0.35 ml/kg). A total of 17 doses are administered. The most effective treatment is started in the first 10 hours after the development of intoxication. If more than 36 hours have passed since intoxication, treatment is ineffective.

If the prothrombin index increases by more than 1.5, vitamin K1 (phytomenadione) 1-10 mg is used; if the prothrombin index increases to more than 3.0, it is necessary to begin infusion of native plasma or a concentrate of coagulation factors (1-2 units).

When treating intoxication, hemodialysis is contraindicated. It is unacceptable to use antihistamines and glucocorticosteroids. It is not recommended to use acetazolamide to alkalinize urine in the treatment of intoxication due to the possibility of developing acidemia and increasing the toxic effect of salicylate on the patient's body.