Instructions for use Paracetamol-S-hemofarm (effervescent tablets). Children's syrup Paracetamol - instructions for use
APPROVED
By order of the chairman
Committee for Control of Medical and
pharmaceutical activities
Ministry of Health
Republic of Kazakhstan
From "_____"______________2011
№ ______________
Instructions for medical use
Medicine
EFFERALGAN
Efferalgan
International generic name
Paracetamol
Effervescent tablets 500 mg
Compound
One tablet contains
active substance: paracetamol - 500 mg,
excipients: anhydrous citric acid, sodium bicarbonate, anhydrous sodium carbonate, sorbitol E 420, sodium docusate, povidone, sodium saccharin E 952, sodium benzoate.
Description
Pills white with beveled edges and scoring, soluble in water. When dissolved in water, the release of gas bubbles is observed.
Pharmacotherapeutic group
Analgesics and antipyretics.
PBX code N02BE01
Pharmacokinetics
At orally Paracetamol absorption occurs quickly and completely. Maximum plasma concentrations are reached 30-60 minutes after administration. Paracetamol is quickly and evenly distributed into all tissues. Plasma protein binding is weak. Paracetamol is metabolized primarily in the liver. The drug is excreted primarily in the urine. 90% dose taken excreted by the kidneys within 24 hours, mainly in the form of glucuronide conjugates (60-80%) and sulfate conjugates (20-30%). Less than 5% is excreted unchanged. The half-life is approximately 2 hours. Renal failure: in case of severe renal failure(creatinine clearance less than 10 ml/min.) the excretion of paracetamol and its metabolites slows down. In elderly people, the ability to conjugate does not change.
Pharmacodynamics
Analgesic effect effervescent tablets occurs faster than when taking regular tablets containing paracetamol. Efferalgan (paracetamol) has an analgesic and antipyretic effect, which is associated with its effect on the thermoregulation center in the hypothalamus and the ability to inhibit the synthesis of prostaglandins, eliminates headaches and other types of pain, and reduces fever.
Indications for use
Pain syndrome of mild or moderate intensity, including: headache and toothache, pain with radiculitis, muscle and rheumatic pain, neuralgia, algodismenorrhea, pain with injuries and burns, sore throat with “colds”.
"Colds" (acute respiratory diseases, influenza), and other infectious diseases accompanied by an increase in body temperature.
Directions for use and doses
Dissolve the tablet completely in a glass of water and drink.
This form release is intended for adults and children weighing more than 50 kg (15 years and older).
Maximum single dose is 2 tablets of 500 mg. Maximum daily dose is 8 tablets. You should always maintain an interval of 4 hours between doses.
In case of severe renal failure, the interval between doses should be at least 8 hours and daily dose should not exceed 3 g of paracetamol per day.
Duration of treatment without medical supervision should not exceed 3 days when prescribed as an antipyretic and 5 days when prescribed as an analgesic.
Nausea, vomiting, abdominal pain
Skin rash, urticaria, angioedema, Quincke's edema, Lyell's syndrome, Stevenson-Johnson syndrome
Anemia, agranulocytosis, thrombocytopenia, leukopenia, hemolytic and aplastic anemia
With long-term use in large doses Oh
Methemoglobinemia
Pancytopenia
Liver dysfunction
Interstitial nephritis, renal dysfunction, oliguria, anuria
Contraindications
Increased sensitivity to paracetamol and other components of the drug
Hepatocellular failure.
Blood diseases, including anemia
Glucose-6-phosphate dehydrogenase enzyme deficiency
Pregnancy, lactation period
Chronic alcoholism
Childhood up to 15 years.
Reduces the effectiveness of uricosuric drugs. 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, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxications even with a small overdose. Long term use Barbiturates reduce the effectiveness of paracetamol. Ethanol promotes development acute pancreatitis. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxicity. Long-term sharing paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing analgesic nephropathy and renal capillary necrosis, and the onset of end-stage renal failure. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney cancer or bladder. Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.
If the febrile syndrome continues during the use of paracetamol for more than 3 days, and pain syndrome- more than 5 days, consultation with a doctor is required.
The risk of developing liver damage increases in patients with alcoholic hepatosis. Distorts indicators laboratory research in the quantitative determination of glucose content and uric acid in plasma.
During long-term treatment painting control is required peripheral blood And functional state liver.
This drug contains 412.4 mg of sodium per tablet, which should be taken into account by people on a strict low-salt diet. Since the drug contains sorbitol, it should not be used in cases of fructose intolerance, poor absorption of glucose and galactose, or isomaltose deficiency.
Prescribe with caution to patients with Gilbert's syndrome, with benign hyperbilirubinemia, as well as elderly patients. Paracetamol is a methemoglobin former. If side effects occur, you should stop taking the medications.
Features of the drug's influence on the ability to drive vehicles and dangerous mechanisms
Considering the side effects of the drug, caution should be exercised when driving vehicles or potentially dangerous mechanisms.
Efferalgan
International nonproprietary name
Paracetamol
Dosage form
Effervescent tablets 500 mg
Compound
One tablet contains
active substance: paracetamol - 500 mg,
excipients: anhydrous citric acid, sodium bicarbonate, anhydrous sodium carbonate, sorbitol E 420, sodium docusate, povidone, sodium saccharin E 954, sodium benzoate.
Description
White tablets with beveled edges and scored lines, soluble in water. When dissolved in water, the release of gas bubbles is observed.
Pharmacotherapeutic group
Analgesics and antipyretics. Anilides. Paracetamol.
ATX code N02BE01
Pharmacological properties
Pharmacokinetics
When paracetamol is taken orally, absorption occurs quickly and completely. Maximum plasma concentrations are achieved 30-60 minutes after administration. Paracetamol is quickly and evenly distributed into all tissues. Plasma protein binding is weak. Paracetamol is metabolized primarily in the liver. The drug is excreted primarily in the urine. 90% of the dose taken is excreted by the kidneys within 24 hours, mainly in the form of glucuronic conjugates (60-80%) and sulfate conjugates (20-30%). Less than 5% is excreted unchanged. The half-life is approximately 2 hours.
Renal failure: in case of severe renal failure (creatinine clearance less than 10 ml/min.), the elimination of paracetamol and its metabolites is slowed down.
In elderly people, the ability to conjugate does not change.
Pharmacodynamics
The analgesic effect of effervescent tablets occurs faster than when taking regular tablets containing paracetamol. Efferalgan (paracetamol) has an analgesic and antipyretic effect, which is associated with its effect on the thermoregulation center in the hypothalamus and the ability to inhibit the synthesis of prostaglandins, eliminates headaches and other types of pain, and reduces fever.
Indications for use
Pain syndrome of mild or moderate intensity, including: headache and toothache, pain with radiculitis, muscle and rheumatic pain, neuralgia, algodismenorrhea, pain with injuries and burns, sore throat with “colds”.
“Colds” (acute respiratory diseases, flu), and other infectious diseases accompanied by an increase in body temperature.
Directions for use and doses
Dissolve the tablet completely in a glass of water and drink.
This release form is intended for adults and children weighing more than 50 kg (15 years and older).
The maximum single dose is 2 tablets of 500 mg. The maximum daily dose is 8 tablets. You should always maintain a 4 hour interval between doses.
In case of severe renal failure, the interval between doses should be at least 8 hours and the daily dose should not exceed 3 g of paracetamol per day.
The duration of treatment without medical supervision should not exceed 3 days when prescribed as an antipyretic and 5 days when prescribed as an analgesic.
Side effects
Nausea, vomiting, abdominal pain,
Skin rash, urticaria, angioedema, angioedema, Lyell's syndrome, Stevenson-Johnson syndrome.
With long-term use:
Anemia, agranulocytosis, thrombocytopenia, leukopenia, hemolytic and aplastic anemia.
With long-term use in large doses:
Methemoglobinemia,
Pancytopenia.
Anaphylactic shock,
Liver dysfunction
Interstitial nephritis, renal dysfunction, oliguria, anuria.
Contraindications
Hypersensitivity to paracetamol and other components of the drug,
Hepatocellular failure,
Blood diseases, including anemia,
Deficiency of the enzyme glucose-6-phosphate dehydrogenase,
Pregnancy, lactation period,
Chronic alcoholism,
Children's age up to 15 years.
Drug interactions
Reduces the effectiveness of uricosuric drugs. Concomitant use of paracetamol in high doses increases the effect of anticoagulant agents (decreased synthesis of procoagulant factors in the liver). Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxications even with a small overdose. Long-term use of barbiturates reduces the effectiveness of paracetamol. Ethanol contributes to the development of acute pancreatitis. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxicity. Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing analgesic nephropathy and renal capillary necrosis, and the onset of end-stage 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 developing hepatotoxicity.
Special instructions
If fever continues during the use of paracetamol for more than 3 days, and pain continues for more than 5 days, a doctor’s consultation is required.
The risk of developing liver damage increases in patients with alcoholic hepatosis. Distorts laboratory test results in the quantitative determination of glucose and uric acid in plasma.
During long-term treatment, monitoring of the peripheral blood picture and the functional state of the liver is necessary.
This drug contains 412.4 mg of sodium per tablet, which should be taken into account by people on a strict low-salt diet. Since the drug contains sorbitol, it should not be used in cases of fructose intolerance, poor absorption of glucose and galactose, or isomaltose deficiency.
Prescribe with caution to patients with Gilbert's syndrome, with benign hyperbilirubinemia, as well as elderly patients. Paracetamol is a methemoglobin former. If side effects occur, you should stop taking the medications.
Features of the drug's influence on the ability to drive vehicles and dangerous machinery
Considering the side effects of the drug, caution should be exercised when driving vehicles or potentially dangerous mechanisms.
Overdose
Symptoms: nausea, vomiting, anorexia, pallor, and abdominal pain usually appear within the first 24 hours.
An overdose of more than 10 g of paracetamol at one time in adults and 150 mg/kg of body weight at one time in children can cause cytolysis of hepatocytes, which can lead to complete and irreversible necrosis, with subsequent development of liver failure, metabolic acidosis, encephalopathy, which can lead to coma or death.
At the same time, there is an increase in the level of liver transaminases, lactate dehydrogenase, bilirubin and a decreased level of prothrombin within 12-48 hours after an overdose.
Treatment: gastric lavage, intake activated carbon, inducing vomiting, administration of SH-group donors and precursors for the synthesis of glutathione - methionine 8 - 9 hours after an overdose and N-acetylcysteine - after 12 hours.
Release form and packaging
4 tablets are placed in a contour-free packaging (strip) made of aluminum foil with a polyethylene coating.
Active substance or group name:
Paracetamol
Average price: 146 rub.
Registration number
P N011549/01
Trade name
Efferalgan ® (Efferalgan®)
International nonproprietary name
paracetamol (paracetamol)
Dosage form Efferalgan ®
effervescent tablets
Description of Efferalgan ® a
Round, flat, white tablets with beveled edges and a score on one side. When dissolved in water, intense release of gas bubbles is observed.
Composition of Efferalgan ®
1 effervescent tablet contains:
Active substance: paracetamol 500 mg.
Excipients: anhydrous citric acid 1114.00 mg, sodium bicarbonate 942.00 mg, anhydrous sodium carbonate 332.00 mg, sorbitol 300.00 mg, sodium saccharinate 7.00 mg, sodium docusate 0.227 mg, povidone 1.287 mg, sodium benzoate 60.606 mg.
Pharmacotherapeutic group
Analgesic non-narcotic drug.
CODE ATX
N02BE01
Pharmacological properties
Paracetamol (para-aminophenol derivative) has analgesic, antipyretic and weak anti-inflammatory effects.
The exact mechanism of the analgesic and antipyretic effect of paracetamol has not been established. Apparently, it includes central and peripheral components.
The drug blocks cyclooxygenase I and II mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains practically complete absence it has an anti-inflammatory effect. The drug does not have a negative effect on water-salt metabolism(sodium and water retention) and the gastrointestinal mucosa due to the lack of influence on the synthesis of prostaglandins in peripheral tissues.
Pharmacokinetics
Absorption.When taken orally, paracetamol is absorbed quickly and completely. Cmax (maximum plasma concentration of paracetamol)
is achieved 10-60 minutes after administration.
Distribution. Paracetamol is quickly distributed in all tissues. The concentration in blood, saliva and plasma is the same. Plasma protein binding is negligible.
Metabolism. Paracetamol is mainly metabolized in the liver. There are two main metabolic pathways producing glucuronides and sulfates. The latter is mainly
used if the dose of paracetamol exceeds the therapeutic dose.
A small amount of paracetamol is metabolized by the cytochrome P450 isoenzyme to form an intermediate compoundN-acetylbenzoquinoneimine, which in normal conditions undergoes rapid detoxification by glutathione and is excreted in the urine after binding to cysteine and mercaptopuric acid. However, with massive intoxication, the content of this toxic metabolite increases.
Excretion.It is carried out mainly with urine. 90% of the dose of paracetamol taken is excreted by the kidneys within 24 hours, mainly in the form of glucuronide (60 to 80%) and sulfate (20 to 30%). Less than 5% is excreted unchanged. The half-life is approximately 2 hours.Pharmacokinetics special groups patientsAt severe violations renal function (creatinine clearance less than 30 ml/min), the excretion of paracetamol and its metabolites is delayed.
Indications for useEfferalgan ® effervescent tablets
Moderate or mild pain syndrome (headache, toothache, migraine pain, neuralgia, muscle pain, lower back pain, pain from injuries and burns, sore throat, painful menstruation);
Increased body temperature with colds and other infectious inflammatory diseases.
Contraindications
Hypersensitivity to paracetamol, propacetamol hydrochloride (prodrug of paracetamol) or any other component of the drug;
Expressed liver failure or decompensated liver diseases in the acute stage;
Sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
Pregnancy (I andIIItrimester) and lactation period;
Children's age up to 12 years.
With caution
Severe renal failure (creatinine clearance< 30 мл/мин), печеночная недостаточность, хронический алкоголизм/дефицит питания, анорексия, булимия, кахексия, гиповолемия, обезвоживание, дефицит глюкозо-6-фосфатдегидрогеназы, врождённые гипербилирубинемии (синдромы Жильбера, Дубинина-Джонсона и Ротора), viral hepatitis; old age.
Directions for use and dosesEfferalgan ® a effervescent tablets
Inside. Dissolve the tablet in a glass of water (200 ml). Usually take 1-2 tablets 2-3 times a day at intervals of at least 4 hours. The maximum single dose is 2 tablets (1 g), the daily dose is 8 tablets (4 g).
In patients with severe renal impairment (creatinine clearance less than 30 ml/min), the interval between doses of the drug should be at least 6 hours.
In patients with chronic or compensated active liver diseases, especially those accompanied by liver failure, in patients with chronic alcoholism, eating disorders and dehydration, the daily dose should not exceed 3 g, i.e. 6 tablets.
The duration of use without consulting a doctor is no more than 5 days when prescribed as an analgesic and 3 days as an antipyretic.
Side effects
When using the drug, the following were noted: side effects(frequency not set):
Allergic reactions : hypersensitivity reactions, itchy skin, rash on the skin and mucous membranes (erythema or urticaria), Quincke's edema, multiform exudative erythema(including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactic shock.
Cocentral and peripheral sides nervous system(when taking high doses): dizziness, psychomotor agitation and disturbance of orientation in space and time.
Co sides of the digestive organs: nausea, diarrhea, epigastric pain, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (dose-dependent effect).
Co sides endocrine system: hypoglycemia, up to hypoglycemic coma.
Co sides of the hematopoietic organs: anemia (cyanosis), sulfohemaglobinemia, methemoglobinemia (shortness of breath, heart pain), hemolytic anemia(especially patients with glucose-6-phosphate dehydrogenase deficiency), thrombocytopenia, neutropenia, leukopenia.
Others:decline blood pressure(as a symptom of anaphylaxis), changes in prothrombin time and international normalized ratio (INR).
Overdose
In case of overdose, intoxication is possible, especially in children, patients with liver diseases (caused chronic alcoholism), in patients with nutritional disorders, as well as in patients taking enzyme inducers, in which fulminant hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis, in the above cases - sometimes with a fatal outcome. The clinical picture of acute overdose develops within 24 hours after taking paracetamol.
Symptoms: gastrointestinal disorders(nausea, vomiting, loss of appetite, feeling of discomfort in abdominal cavity and/or abdominal pain), pallor skin, sweating, malaise. When simultaneous administration of 7.5 g or more to adults or more than 140 mg/kg to children, cytolysis of hepatocytes occurs with complete and irreversible liver necrosis, the development of liver failure, metabolic acidosis and encephalopathy, which can lead to coma and fatal outcome. 12-48 hours after the administration of paracetamol, an increase in the activity of “liver” transaminases and lactate dehydrogenase is observed. bilirubin concentrations anddecrease in prothrombin concentration. Clinical symptoms liver damage appears 1 - 2 days after an overdose of the drug and reaches a maximum on day 3-4.
Treatment:
Immediate hospitalization;
Determination of the quantitative content of paracetamol in blood plasma before starting treatment as soon as possible early dates after an overdose;
Gastric lavage;
Introduction of donorsSH- groups and precursors for the synthesis of glutathione - methionine and acetylcysteine - within 8 hours after an overdose. The need for additional therapeutic measures (further administration of methionine, intravenous administration of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration;
Symptomatic treatment;
Liver tests should be performed at the beginning of treatment and then every 24 hours. In most cases, liver transaminase activity returns to normal within 1-2 weeks. In very severe cases, a liver transplant may be required.
Interaction with other drugs
Phenytoin reduces the effectiveness of paracetamol and increases the risk of hepatotoxicity. Patients taking phenytoin should avoid frequent use of paracetamol, especially in high doses. Probenecid almost halves the clearance of paracetamol, inhibiting the process of its conjugation with glucuronic acid. If administered concomitantly, consider reducing the dose of paracetamol. Caution should be exercised during the simultaneous use of paracetamol and inducers of microsomal liver enzymes (for example, ethanol, barbiturates, isoniazid, rifampicin, carbamazepine, anticoagulants, zidovudine, amoxicillin + clavulanic acid, phenylbutazone, tricyclic antidepressants).
Long-term simultaneous use Barbiturates reduce the effectiveness of paracetamol.
Salicylamide may increase the half-life of paracetamol.
Acetaminophen may enhance the effect of anticoagulants.
Special instructions
To avoid overdose, the content of paracetamol in other drugs that the patient takes simultaneously with Efferapgan should be taken into account. Taking paracetamol in doses higher than recommended can cause severe liver damage.
If the febrile syndrome continues during the use of paracetamol for more than 3 days, and the pain syndrome continues for more than 5 days, a doctor’s consultation is required.
Taking Efferalgan® may distort laboratory test results when quantifying uric acid levels in plasma.
To avoid toxic damage liver paracetamol should not be combined with taking alcoholic drinks, and also taken by persons prone to chronic alcohol consumption. The risk of developing liver damage increases in patients with alcoholic hepatosis.
With prolonged use of the drug, monitoring of the picture is necessaryperipheral blood and functional state of the liver The drug Efferalgan® contains 412.4 mg of sodium per tablet, which should be taken into account by patients on a strict low-salt diet.
Since the drug contains sorbitol, it should not be used in cases of sucrase/isomaltase deficiency, fructose intolerance, or glucose-galactose malabsorption.
Impact on the ability to drive vehicles and operate machinery.
The effect on the ability to drive vehicles and operate machinery has not been studied.
If the patient experiences dizziness, psychomotor agitation and disorientation in space and time, he is not recommended to drive a car or other machinery during treatment with the drug.
Release form Efferalgan ®
Effervescent tablets 500 mg. 4 tablets per strip (aluminum foil/polyethylene). 4 strips along with instructions for use in a cardboard box.
Availability and price in pharmacies Efferalgan effervescent tablets
Storage conditions
Store in a dry place at a temperature of 15-30 °C. Keep out of the reach of children!
Best before date
3 years. Do not use after expiration date.
Conditions for dispensing from pharmacies
Over the counter.
Manufacturer, packer (primary packaging),packer (secondary/tertiary packaging) issuing quality control
Bristol-Myers Squibb, France
47520 France, Le Passage, st. Avenue de Pirene, 979
47520 France, Le Passage, Avenue des Pyrenees, 979
Legal entity in whose name the registration certificate was issued
Bristol-Myers Squibb, France 92506 France, Cedex, Rueil-Mampaison, st. Rue Joseph Monnier, 3, post office box 325Bristol-Myers Squibb, France 92506 France, Cedex, Rueil Malmaison, rue Joseph Monier 3, BP 325
PARACETAMOL-C-HEMOFARM
Release form
effervescent tablets
Owner/Registrar
International Classification of Diseases (ICD-10)
J06.9 Acute infection upper respiratory tract unspecified J10 Influenza caused by an identified influenza virus K08.8 Other specified changes in teeth and their supporting apparatus M25.5 Joint pain M79.1 Myalgia M79.2 Neuralgia and neuritis, unspecified N94.4 Primary dysmenorrhea N94.5 Secondary dysmenorrhea R50 Fever of unknown origin R51 Headache R52.0 Acute pain R52.2 Other constant painPharmacological group
Analgesic-antipyretic
Pharmacological action
Paracetamol-S-Hemofarm is a combination of paracetamol and ascorbic acid(vitamin C).
Paracetamol - analgesic non-narcotic drug, the mechanism of action is associated with inhibition of prostaglandin synthesis and a predominant effect on the thermoregulation center in the hypothalamus.
Ascorbic acid (vitamin C) plays important role in the regulation of redox processes, carbohydrate metabolism, blood clotting, tissue regeneration; participates in the synthesis of glucocorticosteroids, collagen and procollagen; normalizes capillary permeability. Particularly important is the ability to increase the body's resistance, which is likely due to the antioxidant properties of ascorbic acid and stimulation of the immune system.
Pharmacokinetics
Paracetamol - characterized by high absorption, Tmax - 0.5-2 hours; C max - 5-20 mcg/ml. Communication with plasma proteins - 15%. Penetrates the blood-brain barrier. Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk. The therapeutically effective concentration of paracetamol in plasma is achieved when administered at a dose of 10-15 mg/kg. Metabolized in the liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The CYP2E1 isoenzyme is also involved in the metabolism of the drug. T 1/2 - 1-4 hours. Excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, drug clearance decreases and T1/2 increases.
Ascorbic acid is absorbed in the gastrointestinal tract, mainly in the jejunum. With an increase in dose to 200 mg, up to 140 mg (70%) is absorbed; with a further increase in dose, absorption decreases (50-20%). Communication with plasma proteins - 25%. Gastrointestinal diseases ( peptic ulcer stomach and duodenum, constipation or diarrhea, helminthic infestation, giardiasis), consumption of fresh fruit and vegetable juices, alkaline drinking reduce the absorption of ascorbate in the intestine.
The normal concentration of ascorbic acid in plasma is approximately 10-20 mcg/ml, body reserves are about 1.5 g when taking daily recommended doses and 2.5 g when taking 200 mg/day Tmax after oral administration is 4 hours.
Easily penetrates into leukocytes, platelets, and then into all tissues; the highest concentration is achieved in the glandular organs, leukocytes, liver and lens of the eye; deposited in the posterior lobe of the pituitary gland, adrenal cortex, ocular epithelium, interstitial cells of the seminal glands, ovaries, liver, spleen, pancreas, lungs, kidneys, intestinal wall, heart, muscles, thyroid gland; penetrates the placenta. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and plasma. At deficiency states leukocyte concentrations decline later and more slowly and are considered a better measure of deficiency than plasma concentrations. Metabolized primarily in the liver into deoxyascorbic acid and further into oxaloacetic and diketogulonic acids.
Excreted by the kidneys, through the intestines, with sweat, breast milk in the form of unchanged ascorbate and metabolites.
When high doses are prescribed, the rate of elimination increases sharply. Smoking and drinking ethanol accelerate the destruction of ascorbic acid (conversion into inactive metabolites), sharply reducing reserves in the body. Excreted during hemodialysis.
Indications
Pain syndrome of mild or moderate intensity ( headache, neuralgia, myalgia, arthralgia, algodismenorrhea, toothache);
To reduce elevated temperature body for infectious and inflammatory diseases (including colds) and flu.
Contraindications
Bronchoobstruction;
Urticaria, provoked by taking acetylsalicylic acid or other NSAIDs (including a history);
Severe renal failure (creatinine clearance (CC) less than 30 ml/min);
Acute liver disease or severe liver failure in the acute phase;
Condition after coronary artery bypass surgery, confirmed hyperkalemia;
Gastrointestinal bleeding;
Inflammatory bowel diseases;
Erosive and ulcerative changes in the mucous membrane of the stomach and duodenum in the acute phase;
Portal hypertension;
Pregnancy (I and III trimesters);
Lactation period;
Glucose-6-phosphate dehydrogenase deficiency;
Children under 6 years of age;
Hypersensitivity to the components of the drug.
WITH caution: erosive and ulcerative lesions of the gastrointestinal tract (history), presence Helicobacter pylori; hepatic lung failure and moderate severity, renal failure (creatinine clearance (CC) more than 30 ml/min, but less than 60 ml/min); IHD, chronic heart failure; cerebrovascular diseases; blood diseases (thrombocytopenia, leukopenia, agranulocytosis), constitutional hyperbilirubinemia (Gilbert's syndrome), congenital hyperbilirubinemia (Dubin-Johnson syndrome and Rotor syndrome), dyslipidemia/hyperlipidemia, diabetes mellitus, diseases peripheral arteries, heavy somatic diseases, long-term use of NSAIDs, simultaneous administration oral GCS (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidog-rel), selective inhibitors serotonin reuptake (including citalopram, fluoxetine, paroxetine, sertraline), smoking, alcoholism, old age.
Side effects
Allergic reactions: skin rash, itching, urticaria, Quincke's edema.
From the outside digestive system: nausea, epigastric pain.
From the hematopoietic system: anemia, thrombocytopenia, agranulocytosis.
With long-term use in large doses - hepatotoxic effect, irritation of the mucous membrane gastrointestinal tract, nephrotoxic effect ( renal colic, glucosuria, aseptic pyuria, interstitial nephritis, papillary necrosis), hyperprothrombinemia, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia.
Very rarely there is a decrease in blood pressure and dyspnea.
Long-term use of large doses of vitamin C can lead to the formation of oxalate kidney stones.
Overdose
Symptoms(due to paracetamol): pallor of the skin, loss of appetite, nausea, vomiting; hepatonecrosis (the severity of necrosis due to intoxication directly depends on the degree of overdose). Toxic effect in adults, it is possible after taking more than 10-15 g of paracetamol: increased activity of liver transaminases, increased prothrombin time (12-48 hours after administration); expanded clinical picture Liver damage appears after 1-6 days. Rarely, liver failure develops suddenly and can be complicated by renal failure (tubular necrosis).
Treatment: gastric lavage, intake of activated carbon, administration of SH-group donors and precursors for the synthesis of glutathione - methionine - 8-9 hours after an overdose and N-acetylcysteine - after 12 hours.
The need for additional therapeutic activities(further administration of methionine, intravenous administration of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.
Special instructions
Simultaneous use with others medicines must be agreed with a doctor.
After 5 days of using the drug, it is necessary to monitor the peripheral blood picture and the functional state of the liver.
To avoid toxic liver damage, paracetamol should not be combined with alcoholic beverages, or taken by persons prone to chronic alcohol consumption.
There is evidence that frequent use medications containing paracetamol lead to worsening of asthma symptoms.
For renal failure
At renal failure
WITH caution: renal failure (creatinine clearance (CC) more than 30 ml/min, but less than 60 ml/min).
In case of liver dysfunction
At liver failure the daily dose is reduced by reducing the single dose and/or frequency of administration.
WITH caution: liver failure of mild to moderate severity.
If gastric emptying is delayed (propantheline bromide), the onset of action of paracetamol may be delayed.
By accelerating gastric emptying (metoclopramide), the drug begins to work faster.
The toxicity of chloramphenicol increases.
Use caution with prolonged use of paracetamol and simultaneous therapy with oral drugs that inhibit blood clotting.
Directions for use
Effervescent tablet The drug Paracetamol-S-Hemofarm is completely dissolved in a glass of water, and the resulting solution is drunk immediately. It is better to take the medicine between meals.
Unless otherwise instructed by your doctor, the following dosages should be observed when using the drug.
Adults and teenagers over 14 years old the drug is prescribed 1-2 tablets. 1-3 times/day. The maximum daily dose of paracetamol is 4 g (12 effervescent tablets).
For younger children school age(6-9 years) the drug is prescribed 1/2 tablet. 1-3 times/day. The maximum single dose is 1 tablet, the maximum daily dose is 3 tablets.
For children 9-12 years old- 1 tab. 1-3 times/day. The maximum single dose is 2 tablets, the maximum daily dose is 6 tablets.
The interval between doses should be at least 4 hours. The maximum duration of treatment for children- 3 days. Maximum duration of treatment for adults- no more than 5 days when prescribed as an analgesic and no more than 3 days when prescribed as an antipyretic.
At renal and/or liver failure the daily dose is reduced by reducing the single dose and/or frequency of administration.
Storage conditions and shelf life
Store out of reach of children, in a dry place, protected from light, at a temperature of 15° to 25°C. Shelf life - 2 years.
Release from pharmacies
The drug is approved for use as an over-the-counter product.
Description:
Dosage form:
Capsules, effervescent powder for the preparation of solution for oral administration [for children], solution for infusion, solution for oral administration [for children], syrup, rectal suppositories, rectal suppositories [for children], suspension for oral administration, suspension
A non-narcotic analgesic, it blocks COX1 and COX2 mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the almost complete absence of anti-inflammatory effect. The absence of a blocking effect on the synthesis of Pg in peripheral tissues determines the absence of negative influence on water-salt metabolism (Na+ and water retention) and the gastrointestinal mucosa.
Indications:
Feverish syndrome in the background infectious diseases; pain syndrome (mild and moderate severity): arthralgia, myalgia, neuralgia, migraine, toothache and headache, algodismenorrhea.
Contraindications:
Hypersensitivity, neonatal period (up to 1 month). With caution. Renal and liver failure, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, alcoholic liver damage, alcoholism, pregnancy, lactation, old age, early infancy(up to 3 months), glucose-6-phosphate dehydrogenase deficiency; diabetes mellitus (for syrup).
Side effects:
From the skin: itching, rash on the skin and mucous membranes (usually erythematous, urticaria), angioedema, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). From the side of the central nervous system (usually develops when taking high doses): dizziness, psychomotor agitation and disorientation. From the digestive system: nausea, epigastric pain, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (dose-dependent effect). From the endocrine system: hypoglycemia, up to hypoglycemic coma. From the hematopoietic organs: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia (especially for patients with glucose-6-phosphate dehydrogenase deficiency). With long-term use in large doses - aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia. From the urinary system: (when taking large doses) - nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis). Overdose. Symptoms (acute overdose develops 6-14 hours after taking paracetamol, chronic - 2-4 days after exceeding the dose) of acute overdose: dysfunction of the gastrointestinal tract (diarrhea, loss of appetite, nausea and vomiting, abdominal discomfort and/or pain in stomach), increased sweating. Symptoms chronic overdose: a hepatotoxic effect develops, characterized by general symptoms(pain, weakness, adynamia, increased sweating) and specific, characterizing liver damage. As a result, hepatonecrosis may develop. The hepatotoxic effect of paracetamol can be complicated by the development of hepatic encephalopathy (thought disturbances, central nervous system depression, stupor), convulsions, respiratory depression, coma, cerebral edema, hypocoagulation, development of disseminated intravascular coagulation syndrome, hypoglycemia, metabolic acidosis, arrhythmia, collapse. Rarely, liver dysfunction develops at lightning speed and can be complicated by renal failure (renal tubular necrosis). Treatment: administration of SH-group donors and precursors of glutathione synthesis - methionine 8-9 hours after an overdose and N-acetylcysteine - after 12 hours. The need for additional therapeutic measures (further administration of methionine, intravenous administration of N-acetylcysteine) is determined in depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.
Directions for use and dosage:
Inside, with a large number liquids, 1-2 hours after eating (taking immediately after eating leads to a delay in the onset of action). For adults and adolescents over 12 years of age (body weight more than 40 kg), a single dose is 500 mg; the maximum single dose is 1 g. The frequency of administration is up to 4 times a day. The maximum daily dose is 4 g; The maximum duration of treatment is 5-7 days. In patients with impaired liver or kidney function, with Gilbert's syndrome, in elderly patients, the daily dose should be reduced and the interval between doses should be increased. Children: maximum daily dose for children up to 6 months (up to 7 kg) - 350 mg, up to 1 year (up to 10 kg) - 500 mg, up to 3 years (up to 15 kg) - 750 mg, up to 6 years (up to 22 kg ) - 1 g, up to 9 years (up to 30 kg) - 1.5 g, up to 12 years (up to 40 kg) - 2 g. In the form of a suspension: children 6-12 years old - 10-20 ml (in 5 ml - 120 mg), 1-6 years - 5-10 ml, 3-12 months - 2.5-5 ml. The dose for children aged 1 to 3 months is determined individually. Frequency of appointment - 4 times a day; the interval between each dose is at least 4 hours. The maximum duration of treatment without consulting a doctor is 3 days (when taken as an antipyretic drug) and 5 days (as an analgesic). Rectally. Adults - 500 mg 1-4 times a day; maximum single dose - 1 g; maximum daily dose - 4 g. Children 12-15 years old - 250-300 mg 3-4 times a day; 8-12 years - 250-300 mg 3 times a day; 6-8 years - 250-300 mg 2-3 times a day; 4-6 years - 150 mg 3-4 times a day; 2-4 years - 150 mg 2-3 times a day; 1-2 years - 80 mg 3-4 times a day; from 6 months to 1 year - 80 mg 2-3 times a day; from 3 months to 6 months - 80 mg 2 times a day.
Special instructions:
If the febrile syndrome continues during the use of paracetamol for more than 3 days and pain syndrome for more than 5 days, a doctor’s consultation is required. The risk of developing liver damage increases in patients with alcoholic hepatosis. Distorts laboratory test results in the quantitative determination of glucose and uric acid in plasma. During long-term treatment, monitoring of the peripheral blood picture and the functional state of the liver is necessary. The syrup contains 0.06 XE of sucrose per 5 ml, which should be taken into account when treating patients with diabetes.
Interaction:
Reduces the effectiveness of uricosuric drugs. 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, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxications even with a small overdose. Long-term use of barbiturates reduces the effectiveness of paracetamol. Ethanol contributes to the development of acute pancreatitis. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxicity. Long-term combined use of paracetamol and other NSAIDs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, and the onset of end-stage 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 developing hepatotoxicity. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
