Paracetamol-Darnitsa: reviews, analogues, instructions, where to buy. Paracetamol-darnitsa - instructions, indications, composition, method of application Doses and method of application

general characteristics:

international and chemical names: paracetamol; N-(4-hydroxyphenyl)acetamide;

Basic physical and chemical properties: tablets of white or almost white color, flat-cylindrical shape with a chamfer and a score;

Compound: 1 tablet contains paracetamol 200 mg based on 100% dry matter;

excipients: potato starch, povidone, calcium stearate, aerosil.

Release form. Pills.

Pharmacotherapeutic group. Analgesics-antipyretics.

ATS code N02B E01.

Pharmacological properties.

Pharmacodynamics. Non-narcotic analgesic. Non-selectively inhibits COX, affecting pain and thermoregulation centers. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the insignificant anti-inflammatory effect. There is no effect on the synthesis of prostaglandins in peripheral tissues, which means that paracetamol does not have a negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa. The possibility of formation of methemoglobin and sulfhemoglobin is unlikely.

Pharmacokinetics. Absorption is high, almost 100%. In the systemic circulation, 15% of the drug that is absorbed binds to plasma proteins. The time to reach maximum concentration in the blood (TCmax) is 20 – 30 minutes. The therapeutically effective concentration of paracetamol in plasma is achieved when administered at a dose of 10–15 mg/kg. Penetrates the blood-brain barrier. Passes into breast milk. The amount of the drug in breast milk is less than 1% of the dose of paracetamol taken by the mother. Metabolized in the liver: 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites. 17% of the drug undergoes hydroxylation to form active metabolites, which conjugate with glutathione and form inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The half-life (T1/2) of paracetamol is 2 – 3 hours. In elderly patients, drug clearance decreases and T1/2 increases. Excreted by the kidneys - 3% unchanged.

Indications for use. Pain syndrome of weak and moderate intensity of various origins (headache, migraine, toothache, neuralgia, myalgia, algodismenorrhea, pain from injuries, burns). Fever in infectious and inflammatory diseases.

Directions for use and doses. Orally, with a large amount of liquid, 1–2 hours after a meal (taken immediately after a meal leads to a longer absorption time). For adults and adolescents over 12 years of age (body weight more than 40 kg), a single dose is 400 mg (2 tablets); maximum single dose – 1 g; frequency of administration – up to 4 times a day. The maximum daily dose for adults 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 are prescribed at the rate of 10 - 15 mg/kg - a single dose. The dose can be repeated after 6 hours (up to 4 times a day).

The maximum daily dose for children from 3 years to 6 years (up to 22 kg) is 1 g, from 6 years to 9 years (up to 30 kg) – 1.5 g, from 9 years to 12 years (up to 40 kg) – 2 d. The maximum duration of treatment without consulting a doctor is 3 days (when taken as an antipyretic drug) and 5 days (as an analgesic drug).

Side effect. Some patients may experience side effects of the drug, namely:

Allergic reactions: 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). Long-term use of paracetamol, more than 1 tablet per day (1000 or more tablets in a lifetime), doubles the risk of developing severe analgesic nephropathy, leading to end-stage renal failure.

Contraindications. Hypersensitivity to the components of the drug. Children under 3 years of age in this dosage form. Glucose-6-phosphate dehydrogenase deficiency; blood diseases (anemia, leukopenia). Severe liver and kidney failure.

Overdose. Acute overdose develops 6–14 hours after taking paracetamol, chronic overdose develops 2–4 days after exceeding the dose.

Symptoms of acute overdose: dysfunction of the gastrointestinal tract, diarrhea, loss of appetite, nausea and vomiting, abdominal discomfort and/or abdominal pain, increased sweating.

Symptoms of chronic overdose: a hepatotoxic effect develops, characterized by general symptoms such as pain, weakness, adynamia, increased sweating and specific ones characterizing liver damage. As a result, hepatonecrosis may develop. The hepatotoxic effect of paracetamol can be complicated by the development of hepatic encephalopathy with impaired thinking, depression of central nervous system functions, and stupor. Possible convulsions, respiratory depression, coma, cerebral edema. In severe cases, hypocoagulation and disseminated intravascular coagulation develop. Hypoglycemia, metabolic acidosis, arrhythmia, collapse. Sometimes liver dysfunction develops at lightning speed and can be complicated by renal failure (renal tubular necrosis).

Treatment: 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 measures (further administration of methionine, intravenous administration of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its administration.

Features of application. Use with caution in renal failure, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), during pregnancy, and lactation; elderly patients. Taking paracetamol during pregnancy may increase the baby's risk of developing the following breathing problems.

With long-term use of paracetamol, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

For children under 3 years of age, the drug is prescribed in the form of syrup.

Interaction with other drugs. Widely used in various combinations with acetylsalicylic acid, codeine, caffeine, while the dose of paracetamol is reduced and its therapeutic effect is enhanced.

In recent years, data have emerged on the hepatotoxic effect of paracetamol in moderate overdose, with the simultaneous administration of paracetamol in high therapeutic doses with inducers of the microsomal liver enzyme system P-450 (antihistamines, glucocorticoids, phenobarbital, ethacrynic acid, rifampicin), as well as in patients with alcoholism . Even when taken in therapeutic doses (2.5 - 4 g/day), paracetamol can cause serious liver damage in alcoholics, as well as in people who regularly drink alcohol, especially if paracetamol was taken a short period of time after drinking alcohol.

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%, resulting in an increased risk of hepatotoxicity. Myelotoxic drugs enhance the hematotoxicity of the drug.

Storage conditions. Store out of the reach of children, in the original packaging, at a temperature not exceeding 25 ºС.

Shelf life – 4 years.

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Date of publication: 03/30/17

PARACETAMOL-DARNITSA

COMPOSITION OF THE DRUG

active ingredient: paracetamol;

1 tablet contains paracetamol 200 mg;

excipients: corn starch, povidone, microcrystalline cellulose, sodium starch, calcium stearate.

DOSAGE FORM

Pills.

Tablets are white or almost white with a grayish tint, flat-cylindrical in shape, with a bevel and a score.

NAME AND LOCATION OF MANUFACTURER:

CJSC "Pharmaceutical Firm "Darnitsa". Ukraine, 02093, Kyiv, Borispolskaya str., 13.

Pharmacotherapeutic group. Analgesics-antipyretics.

ATC code N02B E01.

Non-narcotic analgesic. Non-selectively inhibits COX, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the insignificant anti-inflammatory effect. There is no effect on the synthesis of prostaglandins in peripheral tissues, which means paracetamol has no negative effect on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract. The possibility of the formation of methemoglobin and sulfhemoglobin is unlikely.

Absorption is high, almost 100%. In the systemic circulation, 15% of the drug Absorbed binds to plasma proteins. The time to reach maximum concentration in the blood (TCmax) is 20-30 minutes. The therapeutically effective concentration of paracetamol in blood plasma is achieved when administered at a dose of 10-15 mg/kg. Penetrates through the blood-brain barrier and into breast milk. The amount of the drug in breast milk is less than 1% of the dose of paracetamol taken by the mother. Metabolized in the liver: 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites. 17% of the drug undergoes hydroxylation to form active metabolites, conjugates with glutathione and forms inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The half-life (T1/2) of paracetamol is 2-3 hours. In elderly patients, clearance decreases and T1/2 increases. Excreted by the kidneys - 3% unchanged.

INDICATIONS FOR USE

Pain syndrome of weak and moderate intensity of various origins (headache, including migraine and tension headache, back pain, rheumatic pain, muscle pain, periodic pain in women, neuralgia, toothache). Relief of cold and flu symptoms such as fever, aches and pains.

CONTRAINDICATIONS

Hypersensitivity to the components of the drug, severe dysfunction of the liver and / or kidneys, congenital hyperbilirubinemia, deficiency of glucose-6-phosphate dehydrogenase, alcoholism, blood diseases, severe anemia, leukopenia.

APPLICATION FEATURES

It is necessary to consult a doctor regarding the possibility of using the drug in patients with impaired renal and liver function.

Keep in mind that in patients with alcoholic liver damage the risk of hepatotoxic action of paracetamol increases; the drug may affect the results of laboratory tests on the content of glucose and uric acid in the blood.

Exceed the indicated doses.

Do not take the drug with other products containing paracetamol.

With long-term use of paracetamol, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

Do not drink alcohol during treatment with paracetamol.

USE DURING PREGNANCY OR BREAST-FEEDING

Pregnancy. Prescribing the drug during these periods is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or child.

Breastfeeding period. Paracetamol passes into breast milk, but in clinically insignificant quantities. Available published data do not contain any contraindications for breastfeeding.

ABILITY TO INFLUENCE REACTION SPEED WHEN DRIVING VEHICLES OR WORKING WITH OTHER MECHANISMS

METHOD OF APPLICATION AND DOSES

Use internally. Take with plenty of liquid, 1-2 hours after meals (taken immediately after meals leads to a longer absorption time).

For adults and children over 12 years of age (body weight more than 40 kg), a single dose is 400-1000 mg, frequency of administration is up to 4 times a day. The maximum daily dose for adults is 4000 mg. The maximum duration of treatment is 5-7 days. For patients with impaired liver or kidney function, in elderly patients, the dose should be reduced and the interval between doses increased.

Children are prescribed at the rate of 10-15 mg/kg - a single dose. The dose can be repeated after 6 hours (up to 4 times a day).

The maximum daily dose for children from 3 to 6 years (up to 22 kg) is 1000 mg, from 6 to 9 years (up to 30 kg) - 1500 mg, from 9 to 12 years (up to 40 kg) - 2000 mg. The maximum duration of treatment without consulting a doctor is 3 days (when taken as an antipyretic drug) and 5 days (as an analgesic drug).

OVERDOSE

Symptoms of paracetamol overdose.

With long-term use of high doses, aplastic anemia, thrombocytopenia, pancytopenia, agranulocytosis, neutropenia, leukopenia are possible. When taking high doses, disturbances may occur from the central nervous system (dizziness, psychomotor agitation, impaired orientation and attention, insomnia, tremor, nervousness, anxiety), from the urinary system - nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis). When using paracetamol more than 1 tablet per day (1000 or more tablets in a lifetime), the risk of developing severe analgesic nephropathy leading to end-stage renal failure doubles.

In case of overdose, increased sweating, psychomotor agitation or depression of the central nervous system, drowsiness, impaired consciousness, cardiac arrhythmia, tachycardia, extrasystole, tremor, hyperreflexia, and convulsions may be observed.

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 patients with risk factors (long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; regular intake of excessive amounts of ethanol; glutathione cachexia (digestive disorders, cystic fibrosis, HIV infection, hunger, cachexia) Taking 5g or more of paracetamol may cause liver damage.

In the first 24 hours: pallor, nausea, vomiting, anorexia, abdominal pain, hepatonecrosis, increased activity of liver transaminases, increased prothrombin index. Liver damage may become apparent 12-48 hours after taking excessive doses of the drug. Impaired glucose metabolism and metabolic acidosis may occur. In severe poisoning, liver failure can progress to encephalopathy, hemorrhage, hypoglycemia, coma and death. Acute renal failure with acute tubular necrosis can manifest as severe lumbar pain, hematuria, proteinuria and develop even in the absence of severe kidney damage. Cardiac arrhythmia and pancreatitis were also noted.

Treatment. In case of overdose, emergency medical care is required. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting, or may not reflect the severity of overdose or the risk of organ damage. Activated charcoal treatment should be considered if an excessive dose of paracetamol has been taken within 1:00. Plasma concentrations of paracetamol should be measured 4 hours or later after administration (earlier concentrations are not reliable). Treatment with N-acetylcysteine is applicable within 24 hours after taking paracetamol, but the maximum protective effect is obtained when it is used within 8 hours after taking it. The effectiveness of the antidote decreases sharply after this time. If necessary, the patient is administered N-acetylcysteine according to the established list of doses. In the absence of vomiting, oral methionine may be used as an appropriate alternative in remote areas outside the hospital.

Side effects

Some patients may experience side effects of the drug, namely:

from the blood and lymphatic system: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia (especially for patients with glucose-6-phosphate dehydrogenase deficiency).

from the respiratory system: bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs;

From the digestive system: nausea, epigastric pain, increased activity of liver enzymes, usually without the development of jaundice;

from the endocrine system: hypoglycemia, up to hypoglycemic coma;

from the immune system: anaphylaxis, skin itching, rash on the skin and mucous membranes (usually generalized rash, skin rash, urticaria), angioedema, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (syndrome) Lyell).

Interaction with other drugs and other types of interactions

The rate of absorption of paracetamol may be increased when used simultaneously with metoclopramide and domperidone and decreased when used with cholestyramine.

The anticoagulant effect of warfarin and other coumarins may be enhanced by long-term regular use of paracetamol with an increased risk of bleeding. Periodic use does not have a significant effect.

Barbiturates reduce the antipyretic effect of paracetamol.

Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of microsomal liver enzymes, may increase the toxic effects of paracetamol on the liver due to an increase in the degree of conversion of the drug to hepatotoxic metabolites. With the simultaneous use of paracetamol with hepatotoxic drugs, the toxic effect of the drugs on the liver increases. The simultaneous use of large doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome.

Paracetamol reduces the effectiveness of diuretics.

BEST BEFORE DATE

STORAGE CONDITIONS

Store out of the reach of children in the original packaging at a temperature not exceeding 25 ° C.

PACKAGE

10 tablets in a blister pack; 1 or 10 blister packs per pack; 10 tablets in blister packs.

VACATION CATEGORY

Without a prescription - tablets No. 10.

Prescription - tablets (No. 10x10).

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

Pharmachologic effect: 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 a negative effect on water-salt metabolism (retention of Na+ and water) and the mucous membrane of the gastrointestinal tract.

Indications: Feverish syndrome due to 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 of chronic overdose: a hepatotoxic effect develops, characterized by general symptoms (pain, weakness, adynamia, increased sweating) and specific ones characterizing liver damage. As a result, hepatonecrosis may develop. The hepatotoxic effect of paracetamol may 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 suddenly 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: Paracetamol-Darnitsa is taken orally, with plenty of liquid, 1-2 hours after a meal (taking immediately after a meal results in a delay in the onset of action). For adults and adolescents over 12 years of age (body weight over 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 indications: 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 with other drugs: 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.

Paracetamol, a drug from the group of analgesics-antipyretics, is the main metabolite of phenacetin, which is quickly converted in the body and causes an analgesic effect.

This drug was synthesized by Harmon Northrop Morse in 1873 and used as an antipyretic by Hinsberg O. and Treupel G. in 1894, and entered clinical practice in 1950. It was registered as a separate drug in the USA in 1955.

Used for dental, rheumatoid, pain, migraine and tension headaches, to relieve symptoms of fever and muscle pain due to colds and flu.

Paracetamol is excellently tolerated and the risk of developing dangerous complications is minimal. And the existence of various dosage forms - tablets, effervescent tablets, capsules, oral suspension, syrup, suppositories, solution for infusion - allow the drug to be used for all age categories of patients.

The unique mechanism of action of paracetamol is the main distinguishing feature from NSAIDs and opioids. Paracetamol affects the activity of the cyclooxygenase enzyme, but more so on one of its variations - COX-3, the activity of which is found in the central nervous system. Due to this, the analgesic and antipyretic effect is central. Since the mechanisms of action are different, there is the possibility of combined use of NSAIDs and paracetamol, which significantly increases the expected pharmacotherapeutic effect and allows the use of NSAIDs in lower doses.

It is worth noting the relative safety of long-term use of paracetamol in the treatment of osteoarthritis of large joints and hands; this ensures proper pain control and improves the quality of life of patients with this pathology.

So, the benefits of paracetamol are:

distinctive mechanism of action on COX-3;
low risk of complications from the gastrointestinal tract and cardiovascular system;
high efficiency and safety;
possibility of use in combination with non-steroidal anti-inflammatory drugs;
long-term use for chronic diseases of the musculoskeletal system;
availability of various dosage forms on the pharmaceutical market;
has a sufficient clinical evidence base.

Based on its characteristics, paracetamol is a “first-line” drug for the relief of moderate pain in outpatient practice. In addition, paracetamol is on the list of vital drugs.

Compound

Dosage form

Pills.

Basic physical and chemical properties: tablets are white or almost white, flat-cylindrical in shape, with a chamfer and a score. A grayish tint is allowed.

Pharmacological group

Analgesics-antipyretics. ATX code N02B E01.

Pharmacological properties

Pharmacodynamics.

Non-narcotic analgesic. Non-selectively inhibits COX, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the insignificant anti-inflammatory effect. There is no effect on the synthesis of prostaglandins in peripheral tissues, which means that paracetamol does not have a negative effect on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract. The possibility of the formation of methemoglobin and sulfhemoglobin is unlikely.

Pharmacokinetics.

Absorption is high, almost 100%. In the systemic circulation, 15% of the absorbed drug binds to blood plasma proteins. The time to reach maximum concentration in the blood (T Cmax) is 20-30 minutes. The therapeutically effective concentration of paracetamol in blood plasma is achieved when administered at a dose of 10-15 mg/kg. Penetrates through the blood-brain barrier and into breast milk. The amount of the drug in breast milk is less than 1% of the dose of paracetamol taken by a nursing mother. Metabolized in the liver: 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites. 17% of the drug undergoes hydroxylation to form active metabolites, which conjugate with glutathione and form inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The half-life (T 1/2) of paracetamol is 2-3 hours. In elderly patients, drug clearance decreases and T1/2 increases. Excreted by the kidneys - 3% unchanged.

Indications

Headache, including migraine and tension headache;
toothache;
backache;
rheumatic pain;
muscle pain;
periodic pain in women;
moderate pain with arthritis;
Relieving symptoms of fever and pain from colds and flu.

Contraindications

Hypersensitivity to the components of the drug,
severe impairment of liver and/or kidney function;
congenital hyperbilirubinemia;
deficiency of glucose-6-phosphate dehydrogenase;
alcoholism;
blood diseases;
Gilbert's syndrome;
severe anemia;
leukopenia.

Interaction with other drugs and other types of interactions

The rate of absorption of paracetamol may increase when used metoclopramide And domperidone and decrease with use cholestyramine.

Anticoagulant effect warfarin and others coumarins with an increased risk of bleeding may increase with simultaneous long-term use of paracetamol. Periodic use does not have a significant effect.

Barbiturates reduce the antipyretic effect of paracetamol.

Anticonvulsants (including phenytoin, barbiturates, carbamazepine), stimulating the activity of microsomal liver enzymes, can increase the toxic effect of paracetamol on the liver as a result of increasing the degree of conversion of the drug into hepatotoxic metabolites. With the simultaneous use of paracetamol with hepatotoxic drugs, the toxic effect of the drugs on the liver increases.

Concomitant use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome.

Paracetamol reduces effectiveness diuretics.

Do not use simultaneously with alcohol.

Application Features

If you have liver or kidney diseases, you should consult your doctor before using the drug. Before using the drug, you should consult your doctor if the patient is using warfarin or similar drugs that have an anticoagulant effect.

It should be taken into account that in patients with alcoholic non-cirrhotic liver damage, the risk of hepatotoxic action of paracetamol increases.

The drug may affect the results of laboratory tests of blood glucose and uric acid levels.

In patients with severe infections such as sepsis, which are accompanied by a decrease in glutathione levels, the risk of metabolic acidosis increases when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or labored breathing, nausea, vomiting, and loss of appetite. If these symptoms occur, you should consult a doctor immediately.

Do not exceed the indicated doses.

Do not take the drug with other products containing paracetamol.

Patients should consult a physician if they experience mild arthritis pain and need to take analgesics daily.

If symptoms do not go away, you should consult a doctor. If the headache becomes persistent, you should consult a doctor.

Use during pregnancy or breastfeeding

Prescribing the drug during these periods is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or child.

Paracetamol passes into breast milk, but in clinically insignificant quantities. Available published data do not contain any contraindications for breastfeeding.

The ability to influence the reaction rate when driving vehicles or other mechanisms

Does not affect.

Directions for use and doses

The drug is intended for oral administration.

Adults and children over 12 years of age: 1-2 tablets 4 times a day if necessary. Do not take more than 8 tablets (4000 mg) within 24 hours.

Children (6-12 years old):½-1 tablet 3-4 times a day if necessary.

A single dose of paracetamol is 10-15 mg/kg body weight, the maximum daily dose is 60 mg/kg body weight. Do not take more than 4 doses in 24 hours. The maximum period of use for children without consulting a doctor is 3 days.

The interval between doses is at least 4 hours.

Do not take with other medicines containing paracetamol.

Children

Do not use in children under 6 years of age.

Overdose

Liver damage is possible in adults who took 10 g or more of paracetamol, and in children who took more than 150 mg/kg body weight. In patients with risk factors (long-term use of carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; alcohol abuse; deficiency of the glutathione system, for example: digestive disorders, cystic fibrosis, HIV infection, fasting, cachexia) Taking 5g or more of paracetamol may cause liver damage.

Symptoms of overdose in the first 24 hours: pallor, nausea, vomiting, loss of appetite and abdominal pain. Liver damage may become apparent 12-48 hours after overdose. Impaired glucose metabolism and metabolic acidosis may occur. In severe poisoning, liver failure can progress to encephalopathy, hemorrhage, hypoglycemia, coma and death. Acute renal failure with acute tubular necrosis can manifest as severe lumbar pain, hematuria, proteinuria and develop even in the absence of severe liver damage. Cardiac arrhythmia and pancreatitis were also noted.

With long-term use of the drug in large doses, the hematopoietic organs may develop aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia. When taking large doses, the central nervous system may experience dizziness, psychomotor agitation, and disorientation; from the urinary system - nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis).

Treatment: In case of overdose, emergency medical care is required. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting, or may not reflect the severity of overdose or the risk of organ damage. Treatment with activated charcoal should be considered if an excessive dose of paracetamol has been taken within 1 hour. Plasma concentrations of paracetamol should be measured 4 hours or later after administration (earlier concentrations are not reliable). Treatment with N-acetylcysteine can be given within 24 hours of taking paracetamol, but the maximum protective effect is obtained when given within 8 hours of taking it. The effectiveness of the antidote decreases sharply after this time. If necessary, the patient should be administered N-acetylcysteine intravenously according to current recommendations. In the absence of vomiting, oral methionine may be used as an appropriate alternative in remote areas outside the hospital.

Side effects

If adverse reactions occur, you must stop using the drug and immediately consult a doctor.

The following adverse reactions may develop:

from the immune system:	anaphylaxis, hypersensitivity reactions, including pruritus, rash on the skin and mucous membranes (usually generalized rashes, erythematous rashes, urticaria), angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome );
from the digestive system:	nausea, epigastric pain;
from the endocrine system:	hypoglycemia, up to hypoglycemic coma;
from the blood and lymphatic system:	thrombocytopenia, agranulocytosis, anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, bruising or bleeding;
from the respiratory system:	bronchospasm in patients sensitive to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;
from the hepatobiliary system:	impaired liver function, increased activity of liver enzymes, usually without the development of jaundice.

Best before date

Storage conditions

Store in original packaging at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Package

10 tablets in a blister pack; 1 blister pack per pack; 10 tablets in blister packs.

Paracetamol, a drug from the group of analgesics-antipyretics, is the main metabolite of phenacetin, which is quickly converted in the body and causes an analgesic effect.

Used for dental, rheumatoid, pain, migraine and tension headaches, to relieve symptoms of fever and muscle pain due to colds and flu.

So, the benefits of paracetamol are:

distinctive mechanism of action on COX-3;
low risk of complications from the gastrointestinal tract and cardiovascular system;
high efficiency and safety;
possibility of use in combination with non-steroidal anti-inflammatory drugs;
long-term use for chronic diseases of the musculoskeletal system;
availability of various dosage forms on the pharmaceutical market;
has a sufficient clinical evidence base.

Based on its characteristics, paracetamol is a “first-line” drug for the relief of moderate pain in outpatient practice. In addition, paracetamol is on the list of vital drugs.

Compound

Dosage form

Pills.

Basic physical and chemical properties: tablets are white or almost white, flat-cylindrical in shape, with a chamfer and a score. A grayish tint is allowed.

Pharmacological group

Analgesics-antipyretics. ATX code N02B E01.

Pharmacological properties

Pharmacodynamics.

Non-narcotic analgesic. Non-selectively inhibits COX, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the insignificant anti-inflammatory effect. There is no effect on the synthesis of prostaglandins in peripheral tissues, which means that paracetamol does not have a negative effect on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract. The possibility of the formation of methemoglobin and sulfhemoglobin is unlikely.

Pharmacokinetics.

Indications

Headache, including migraine and tension headache;
toothache;
backache;
rheumatic pain;
muscle pain;
periodic pain in women;
moderate pain with arthritis;
Relieving symptoms of fever and pain from colds and flu.

Contraindications

Hypersensitivity to the components of the drug,
severe impairment of liver and/or kidney function;
congenital hyperbilirubinemia;
deficiency of glucose-6-phosphate dehydrogenase;
alcoholism;
blood diseases;
Gilbert's syndrome;
severe anemia;
leukopenia.

Interaction with other drugs and other types of interactions

The rate of absorption of paracetamol may increase when used metoclopramide And domperidone and decrease with use cholestyramine.

Anticoagulant effect warfarin and others coumarins with an increased risk of bleeding may increase with simultaneous long-term use of paracetamol. Periodic use does not have a significant effect.

Barbiturates reduce the antipyretic effect of paracetamol.

Concomitant use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome.

Paracetamol reduces effectiveness diuretics.

Do not use simultaneously with alcohol.

Application Features

It should be taken into account that in patients with alcoholic non-cirrhotic liver damage, the risk of hepatotoxic action of paracetamol increases.

The drug may affect the results of laboratory tests of blood glucose and uric acid levels.

Do not exceed the indicated doses.

Do not take the drug with other products containing paracetamol.

Patients should consult a physician if they experience mild arthritis pain and need to take analgesics daily.

If symptoms do not go away, you should consult a doctor. If the headache becomes persistent, you should consult a doctor.

Use during pregnancy or breastfeeding

Prescribing the drug during these periods is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or child.

Paracetamol passes into breast milk, but in clinically insignificant quantities. Available published data do not contain any contraindications for breastfeeding.

The ability to influence the reaction rate when driving vehicles or other mechanisms

Does not affect.

Directions for use and doses

The drug is intended for oral administration.

Adults and children over 12 years of age: 1-2 tablets 4 times a day if necessary. Do not take more than 8 tablets (4000 mg) within 24 hours.

Children (6-12 years old):½-1 tablet 3-4 times a day if necessary.

The interval between doses is at least 4 hours.

Do not take with other medicines containing paracetamol.

Children

Do not use in children under 6 years of age.

Overdose

Side effects

If adverse reactions occur, you must stop using the drug and immediately consult a doctor.

The following adverse reactions may develop:

from the immune system:	anaphylaxis, hypersensitivity reactions, including pruritus, rash on the skin and mucous membranes (usually generalized rashes, erythematous rashes, urticaria), angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome );
from the digestive system:	nausea, epigastric pain;
from the endocrine system:	hypoglycemia, up to hypoglycemic coma;
from the blood and lymphatic system:	thrombocytopenia, agranulocytosis, anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, bruising or bleeding;
from the respiratory system:	bronchospasm in patients sensitive to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;
from the hepatobiliary system:	impaired liver function, increased activity of liver enzymes, usually without the development of jaundice.

Best before date

Storage conditions

Store in original packaging at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Package

10 tablets in a blister pack; 1 blister pack per pack; 10 tablets in blister packs.