Paracetamol altpharm 0 25 n10 supp rect. Medicinal reference book geotar

in a blister pack 5 pcs.; in a cardboard pack 2 packs.

Description of the dosage form

Suppositories are white or white with a creamy or yellowish tint, torpedo-shaped.

Pharmacodynamics

Paracetamol has analgesic and antipyretic effects. Blocks cyclooxygenase in the central nervous system, affecting pain and thermoregulation centers. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the lack of a significant anti-inflammatory effect.

The drug does not have negative influence on water-salt metabolism(sodium and water retention) and gastrointestinal mucosa.

Pharmacokinetics

Absorption is high, quickly absorbed from the gastrointestinal tract. The period to reach Cmax is 30–60 minutes, binding to plasma proteins is 15%. Penetrates through the BBB. The volume of distribution and bioavailability in children and neonates are similar to those in adults.

Metabolized in the liver: 80% - enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% - 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. In newborns in the first two days of life and in children 3–10 years of age, the main metabolite of paracetamol is paracetamol sulfate; in children 12 years of age and older, it is conjugated glucuronide.

T1/2 - 2–3 hours. Within 24 hours, 85–88% of paracetamol is excreted by the kidneys in the form of glucuronides and sulfates, unchanged - 3%. There is no significant age difference in the rate of elimination of paracetamol and in total number There is no drug that is excreted in the urine.

Paracetamol-Altpharm: Indications

Used in children from 3 months to 12 years as:

antipyretic for acute respiratory infections, influenza, childhood infections, post-vaccination reactions and other conditions accompanied by an increase in body temperature;

painkiller for pain syndrome weak and moderate intensity, incl. head and toothache, muscle pain, neuralgia, pain from injuries and burns.

In children from 1 to 3 months, a single dose of the drug can be taken to reduce fever after vaccination.

Paracetamol-Altpharm: Contraindications

hypersensitivity to the components of the drug;

age up to 1 month of life.

With caution:

liver and kidney dysfunction;

Gilbert's syndrome; Dubin-Johnson and Rotor;

diseases of the blood system (anemia, thrombocytopenia, leukopenia);

genetic absence of the enzyme glucose-6-phosphate dehydrogenase.

Directions for use and doses

Rectally, after a cleansing enema or spontaneous bowel movement. The dosage of the drug is calculated depending on age and body weight, in accordance with the table. A single dose is 10–15 mg/kg 2–3 times a day every 4–6 hours. Maximum daily dose paracetamol should not exceed 60 mg/kg.

Dosage of the drug for children of different ages

Paracetamol-Altpharm: Side effects

From the gastrointestinal tract: nausea, vomiting, abdominal pain.

Allergic reactions: itching, rash on the skin and mucous membranes, urticaria, Quincke's edema.

From the hematopoietic organs: anemia, leukopenia, agranulocytosis, thrombocytopenia.

At long-term use in large doses - hepatotoxic and nephrotoxic effects ( interstitial nephritis, papillary necrosis), hemolytic anemia.

Suppositories - 1 soup:

Active ingredient: paracetamol - 500 mg.

5 pieces each in a blister pack made of polyvinyl chloride film. Two contour packages along with instructions for use in a cardboard box.

Description of the dosage form

Suppositories are white to white with a creamy or yellowish tint, torpedo-shaped without visible inclusions on a longitudinal section.

Pharmacokinetics

Paracetamol, when taken orally, is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum level of concentration in the blood is reached after 30-60 minutes. At rectal administration paracetamol, the completeness of its absorption may be lower than after oral administration.

Paracetamol is quickly and evenly distributed throughout the tissues of the body. 10-15% of the dose taken is bound to plasma proteins. The volume of distribution and bioavailability in children and adults do not differ significantly. The drug penetrates the placental barrier. IN breast milk Feeding mothers receive less than 1% of the dose taken.

Paracetamol is metabolized by liver microsomal enzymes, about 80% forms conjugates with glucuronic acid and sulfates, up to 17% undergoes hydroxylation to form active metabolites that are conjugated with glutathione. With an overdose or deficiency of glutathione, these metabolites can cause necrosis of hepatocytes.

The half-life of paracetamol is 1.5-2.5 hours. It may increase in patients with pronounced violation liver function and elderly patients. 24 hours after administration, 85-90% of paracetamol is excreted in the urine in the form of glucoronides and sulfates, and 3% unchanged.

In children under 10-12 years of age, the formation of conjugates with sulfates is the main route of metabolism and excretion of paracetamol. The likelihood of hepatotoxicity in children is lower than in adults. Other pharmacokinetic parameters of adults and children do not differ.

Pharmacodynamics

Paracetamol contained in suppositories has antipyretic and analgesic effects. The drug blocks cyclooxygenase in the central nervous system, affecting the centers of pain and thermoregulation. Body heat loss during fever increases as a result of vasodilation and increased peripheral blood flow. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains practically complete absence anti-inflammatory effect of the drug.

Instructions

The drug is administered rectally (injected into the rectum). Before using the suppository, it is recommended to empty the intestines.

The duration of treatment is no more than 3 days when prescribed as an antipyretic and no more than 5 days when prescribed as an analgesic. Further treatment the drug is possible only after consultation with a doctor.

Indications for use Paracetamol-altpharm

Paracetamol-Altpharm suppositories are used in adults and children from 3 months of life (in children from 1 to 3 months of life - only as prescribed by a doctor):

  • As an antipyretic for acute respiratory diseases, influenza, childhood infections, post-vaccination reactions and other infectious and inflammatory diseases accompanied by an increase in body temperature;
  • as an analgesic for pain of mild or moderate intensity, including: headaches and toothaches, muscle pain, neuralgia, pain from injuries and burns.

Contraindications to the use of Paracetamol-altpharm

The drug should be used with caution in case of impaired liver or kidney function, in elderly patients, and in alcoholism.

The drug should not be used in patients with diarrhea.

Paracetamol-altpharm Use during pregnancy and children

Children under 3 one month old suppositories are prescribed only on the recommendation of a doctor.

Contraindicated during breastfeeding.

Paracetamol-altpharm Side effects

Possible nausea, epigastric pain, allergic reactions - skin rash, itching, urticaria, angioedema. In rare cases, dysfunction of the liver, kidneys, and hematopoietic system (anemia, agranulocytosis, thrombocytopenia) is observed. With long-term use in large doses - hepatotoxic effect, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia; nephrotoxicity (interstitial nephritis, papillary necrosis). Whenever side effects you should stop taking the drug and consult your doctor.

Drug interactions

When the patient simultaneously takes other medicines You should consult your doctor.

Taken together with salicylates significantly increases the risk of nephritis toxic effect.

When taking paracetamol and barbiturates, anticonvulsants (phenytoin), tricyclic antidepressants, rifampicin, butadione, and alcohol simultaneously, the risk of hepatotoxicity of the drug increases. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxicity.

Paracetamol enhances the effect of anticoagulants and reduces the effectiveness of uricosuric drugs.

When using the drug together with chloramphenicol, the toxicity of the latter increases.

Dosage Paracetamol-altpharm

Dosage for adults:

Average single dose 500 mg 2-4 times a day; maximum single dose - 1 g (2 suppositories of 500 mg each); maximum daily dose - 4 g.

The duration of treatment with paracetamol without consulting a doctor is 3-5 days.

Dosage for children:

Depends on the age and body weight of the child. The recommended single dose of paracetamol is 10-15 mg/kg of the child’s body weight. The drug is used 3-4 times a day with an interval of 4-6 hours. The maximum daily dose is no more than 60 mg/kg of the child’s body weight.

Overdose

Symptoms. In case of overdose or hypersensitivity to the drug, pallor, lack of appetite, nausea, vomiting, and epigastric pain are noted. Increased levels of liver enzymes, increased prothrombin time, and later pain in the liver area. In severe cases it develops liver failure, hepatonecrosis, coma and encephalopathy.

Treatment. In these cases, it is recommended to lavage the stomach during the first four hours, take energy sorbents, intravenous administration antidote - N-acetylcysteine, oral administration of methionine. If symptoms of poisoning appear, stop taking the drug and consult a doctor.

Precautions

When using the drug for more than 7 days, monitoring is necessary. functional state liver and peripheral blood picture.

If the patient's condition does not improve within 3-5 days, consult a doctor.

Dosage form:  rectal suppositories Compound:

Composition for 1 suppository:

Active substance: paracetamol - 0.05 g, 0.10 g, 0.25 g or 0.5 g. Excipient: fatty acids glycerides (solid fat) - 0.75 g, 0.90 g, 0.75 g or 0.60 g.

Description:

Suppositories are white to white with a creamy or yellowish tint, torpedo-shaped without visible inclusions on the longitudinal section.

Pharmacotherapeutic group:analgesic non-narcotic drug Pharmacodynamics:Paracetamol has antipyretic and analgesic effects. The drug blocks cyclooxygenase 1 and 2 in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular pyroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of the anti-inflammatory effect of the drug. The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (delay Na+ and water) and erosive and ulcerative lesions mucous membrane gastrointestinal tract. Pharmacokinetics:

Paracetamol is quickly and almost completely absorbed from the gastrointestinal tract. Maximum concentration paracetamol in the blood is achieved 1.6 - 2.8 hours after administration of the drug and is 2.6 - 5.6 mg/liter. When administered rectally, the complete absorption of paracetamol is lower than after oral administration.

Paracetamol is quickly and evenly distributed throughout the tissues of the body. 10 - 15% of the dose taken is bound to plasma proteins. The volume of distribution and bioavailability in children and adults do not differ significantly. The drug penetrates the blood-brain and placental barriers. Less than 1% of the dose taken enters the breast milk of nursing mothers.

Paracetamol is metabolized by microsomal liver enzymes. About 80% forms conjugates with glucuronic acid and sulfates, up to 17% undergoes hydroxylation to form active metabolites that are conjugated with glutathione. With an overdose or deficiency of glutathione, these metabolites can cause necrosis of hepatocytes.

The half-life of paracetamol is 2.0 - 4.0 hours. It may increase in patients with severe liver dysfunction and elderly patients. 24 hours after administration, 85-90% of paracetamol is excreted in the urine in the form of glucoronides and sulfates, and 3% unchanged.

In children under 10 - 12 years of age, the formation of conjugates with sulfates is the main route of metabolism and excretion of paracetamol. The likelihood of hepatotoxicity in children is lower than in adults. Other pharmacokinetic parameters of adults and children do not differ.

Indications:

As an antipyretic for acute respiratory diseasesdiseases, flu, childhood infections, post-vaccination reactions and othersinfectious and inflammatory diseases accompanied by increased body temperature.

As an analgesic for pain of mild or moderate intensity, including: headache and toothache, muscle pain, arthralgia, neuralgia, algodismenorrhea, pain from injuries and burns.

Contraindications:

Increased individual sensitivity to paracetamol or other components of the drug.

Severe liver and kidney dysfunction, blood diseases, deficiency of the enzyme glucose-6-phosphate dehydrogenase.

Childhood up to 1 month of life.

Acute inflammation or bleeding in the rectum.

With caution:

The drug should be taken with caution in case of impaired liver or kidney function (renal and hepatic failure, viral hepatitis, alcoholic liver damage);

During pregnancy;

During breastfeeding;

Children under 3 months;

Elderly patients;

For alcoholism;

At benign hyperbilirubinemia(including Gilbert's syndrome);

Directions for use and dosage:

The drug is administered rectally (injected into the rectum). Before using the suppository, it is recommended to empty the intestines.

Dosage for adults and adolescents over 15 years of age:

The average single dose is 500 mg 1 - 4 times a day; maximum single dose - 1 g; maximum daily dose - 4 g.

Dosage for children:

Depends on the age and body weight of the child. The recommended single dose of paracetamol is 10-15 mg/kg of the child’s body weight. The frequency of administration is 1 - 4 times a day with an interval of at least 4 hours. The maximum daily dose is not more than 60 mg/kg of the child’s body weight.

Approximate dosage scheme for suppositories for children depending on age:

Child's age

Single dose

Daily dose

1 - 3 months

3-6 months

50 mg

150 mg

6 -12 months

50 mg - 100 mg

150 mg-200 mg

1 - 2 years

50 mg -100 mg

200 mg - 300 mg

2-6 years

100 mg-250 mg

300 mg - 600 mg

6-8 years

250 mg

500 mg - 750 mg

8-12 years

250 mg

750 mg

12 - 15 years

250 mg

750 mg - 1000 mg

The dose for children from 1 month to 3 months is determined individually by the doctor. The duration of treatment without consulting a doctor is no more than 3 days when prescribed as an antipyretic and no more than 5 days when prescribed as an analgesic. Further treatment with the drug is possible only after consultation with a doctor.

Side effects:Possible allergic reactions - skin rash, itching, urticaria, angioedema. In rare cases, dysfunction of the liver, kidneys, and hematopoietic system (anemia, agranulocytosis, thrombocytopenia) is observed. With long-term use in large doses - hepatotoxic effect, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia; nephrotoxicity (interstitial nephritis, papillary necrosis). If anyside effects, you should stop taking the drug and consult your doctor. Overdose:

Symptoms: during the first 24 hours after administration - pallor skin, nausea, vomiting, anorexia, abdominal pain; disturbance of glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12 to 48 hours after an overdose. In case of severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis. The hepatotoxic effect in adults occurs when taking 10 g or more.

Treatment: administration of SH-group donors and precursors for the synthesis of glutathione - methionine within 8 - 9 hours after an overdose and acetylcysteine ​​- within 12 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 the time elapsed after its administration.

Interaction:

If the patient is taking other medications at the same time, consult a doctor.

Paracetamol can enhance the effect of indirect anticoagulants (coumarin derivatives), hypoglycemic drugs (sulfonylurea derivatives) by displacing these compounds from binding to plasma proteins.

Taken together with salicylates significantly increases the risk of nephrotoxicity. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney cancer or bladder.

Paracetamol enhances the effect of drugs that depress the central nervous system, ethanol.

Long-term use anticonvulsants causes an increase in the activity of liver enzymes, which increases the intensity of the “first pass” effect through the liver and increases the clearance of paracetamol. This may prevent paracetamol blood levels from reaching therapeutic levels. Barbiturates, antiepileptic drugs, anticonvulsants (phenytoin), tricyclic antidepressants, estrogen-containing contraceptives, butadione, as well as alcohol and other stimulants of microsomal oxidation promote the formation of hydroxylated active metabolites of paracetamol, which makes it possible to develop severe intoxications even with a small overdose. promotes development acute pancreatitis.

Barbiturates, tricyclic antidepressants, increase the half-life of paracetamol. Long-term use of barbiturates reduces the effectiveness of paracetamol.

Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.

Inhibitors of microsomal oxidation (including) reduce the risk of hepatotoxicity.

Corticosteroids may increase the risk of side effects in gastrointestinal tract.

Myelotoxic medicines increase the manifestations of hematotoxicity of the drug.

Long-term combined use of paracetamol and non-steroidal anti-inflammatory drugs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, the onset of terminal stage renal failure.

Paracetamol reduces effectiveness antihypertensive drugs, diuretics, anti-gout drugs that promote excretion uric acid. inhibits the renal excretion of lithium, methotrexate, aminoglycosides, digoxin in case of impaired renal function (especially in young childrenschool age and the elderly), increases the concentration of these compounds in the blood and increases their toxicity.

For children under 3 months of age and women during pregnancy, suppositories are prescribed only on the recommendation of a doctor.

If the patient's condition does not improve within 3-5 days, consult a doctor.

When using the drug for more than 7 days, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

The drug distorts the indicators laboratory research at quantification glucose and uric acid in plasma.

The risk of developing liver damage increases in patients with alcoholic illness liver.

The drug should not be used in patients with diarrhea.

Impact on the ability to drive vehicles. Wed and fur.:Effect of the drug on the ability to drive vehicles and no mechanisms were observed. Release form/dosage:Rectal suppositories 50 mg; 100 mg; 250 mg; 500 mg. Package: 5 suppositories each in a blister pack made of polyvinyl chloride film. Two contour packages along with instructions for use in a cardboard box. Storage conditions:

Store in a place protected from light at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Best before date:

2 years. Do not use after the expiration date indicated on the package.

Instructions

Analgesic-antipyretic. It has analgesic, antipyretic and weak anti-inflammatory effects. The mechanism of action is associated with inhibition of prostaglandin synthesis, with a predominant effect on the thermoregulation center in the hypothalamus.

Pharmacokinetics

After oral administration, paracetamol is rapidly absorbed from the gastrointestinal tract, mainly in small intestine, mainly by passive transport. After a single dose of 500 mg, Cmax in blood plasma is reached after 10-60 minutes and is about 6 μg/ml, then gradually decreases and after 6 hours it is 11-12 μg/ml.

Widely distributed in tissues and mainly in body fluids, with the exception of adipose tissue and cerebrospinal fluid.

Protein binding is less than 10% and increases slightly with overdose. Sulfate and glucuronide metabolites do not bind to plasma proteins even at relatively high concentrations.

Paracetamol is metabolized primarily in the liver by conjugation with glucuronide, conjugation with sulfate and oxidation with the participation of mixed liver oxidases and cytochrome P450.

The negatively acting hydroxylated metabolite N-acetyl-p-benzoquinoneimine, which is formed in very small quantities in the liver and kidneys by mixed oxidases and is usually detoxified by binding to glutathione, can escalate with paracetamol overdose and cause tissue damage.

In adults, most paracetamol is bound to glucuronic acid and to a lesser extent to sulfuric acid. These conjugated metabolites do not have biological activity. In premature infants, newborns and in the first year of life, the sulfate metabolite predominates.

T1/2 is 1-3 hours. In patients with liver cirrhosis, T1/2 is slightly longer. The renal clearance of paracetamol is 5%.

It is excreted in the urine mainly in the form of glucuronide and sulfate conjugates. Less than 5% is excreted as unchanged paracetamol.

Release form

5 pcs. - contour cell packaging (2) - cardboard packs.

Dosage

Orally or rectally in adults and adolescents weighing more than 60 kg, use a single dose of 500 mg, frequency of administration - up to 4 times a day. The maximum duration of treatment is 5-7 days.

Maximum doses: single - 1 g, daily - 4 g.

Single oral doses for children aged 6-12 years - 250-500 mg, 1-5 years - 120-250 mg, from 3 months to 1 year - 60-120 mg, up to 3 months - 10 mg/kg. Single doses at rectal use in children aged 6-12 years - 250-500 mg, 1-5 years - 125-250 mg.

The frequency of use is 4 times a day with an interval of at least 4 hours. The maximum duration of treatment is 3 days.

Maximum dose: 4 single doses per day.

Interaction

When used simultaneously with inducers of microsomal liver enzymes and drugs with hepatotoxic effects, there is a risk of increasing the hepatotoxic effect of paracetamol.

When used simultaneously with anticoagulants, a slight or moderate increase in prothrombin time is possible.

When used simultaneously with anticholinergic drugs, the absorption of paracetamol may be reduced.

When used simultaneously with oral contraceptives, the elimination of paracetamol from the body is accelerated and its analgesic effect may be reduced.

When used simultaneously with uricosuric drugs, their effectiveness decreases.

When used simultaneously activated carbon The bioavailability of paracetamol decreases.

When used simultaneously with diazepam, the excretion of diazepam may be reduced.

There are reports of the possibility of enhancing the myelosuppressive effect of zidovudine when used simultaneously with paracetamol. A case of severe toxic liver damage has been described.

Cases of toxic effects of paracetamol have been described when used simultaneously with isoniazid.

When used simultaneously with carbamazepine, phenytoin, phenobarbital, primidone, the effectiveness of paracetamol decreases, which is due to an increase in its metabolism (glucuronidation and oxidation processes) and excretion from the body. Cases of hepatotoxicity have been described with the simultaneous use of paracetamol and phenobarbital.

When using cholestyramine for a period of less than 1 hour after taking paracetamol, the absorption of the latter may be reduced.

When used simultaneously with lamotrigine, the excretion of lamotrigine from the body moderately increases.

When used simultaneously with metoclopramide, it is possible to increase the absorption of paracetamol and increase its concentration in the blood plasma.

When used simultaneously with probenecid, the clearance of paracetamol may be reduced; with rifampicin, sulfinpyrazone - it is possible to increase the clearance of paracetamol due to an increase in its metabolism in the liver.

When used simultaneously with ethinyl estradiol, the absorption of paracetamol from the intestine increases.

Side effects

From the outside digestive system: rarely - dyspeptic effects, with long-term use in high doses - hepatotoxic effect.

From the hematopoietic system: rarely - thrombocytopenia, leukopenia, pancytopenia, neutropenia, agranulocytosis.

Allergic reactions: rarely - skin rash, itching, urticaria.

Indications

Pain syndrome of mild to moderate intensity of various origins(incl. headache, migraine, toothache, neuralgia, myalgia, algodismenorrhea; pain from injuries, burns). Fever in infectious and inflammatory diseases.

Contraindications

Chronic alcoholism, increased sensitivity to paracetamol.

Features of application

Use during pregnancy and breastfeeding

Paracetamol penetrates the placental barrier. To date, there have been no negative effects of paracetamol on the fetus in humans.

Paracetamol is excreted in breast milk: the content in milk is 0.04-0.23% of the dose taken by the mother.

If necessary, use paracetamol during pregnancy and lactation ( breastfeeding) the expected benefit of therapy for the mother and the potential risk to the fetus or child should be carefully weighed.

Experimental studies have not established the embryotoxic, teratogenic and mutagenic effects of paracetamol.

Use for liver dysfunction

Use with caution in patients with impaired liver function.

Use for renal impairment

Use with caution in patients with impaired renal function.

Use in children

Application is possible according to the dosage regimen.

Use in elderly patients

Use with caution in elderly patients.

Special instructions

Use with caution in patients with impaired liver and kidney function, with benign hyperbilirubinemia, as well as in elderly patients.

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

It is used to treat premenstrual tension syndrome in combination with pamabrom (a diuretic, a xanthine derivative) and mepiramine (a histamine H1 receptor blocker).

Release form: Solid dosage forms. Rectal suppositories.



General characteristics. Compound:

Active substance: paracetamol - 0.05 g, 0.1 g, 0.25 g or 0.5 g.

Excipient: fatty acid glycerides (solid fat) - 0.75 g, 0.90 g, 0.75 g or 0.60 g.

Suppositories are white to white with a creamy or yellowish tint, torpedo-shaped without visible inclusions on a longitudinal section.


Pharmacological properties:

Pharmacodynamics.

Paracetamol contained in suppositories has antipyretic and analgesic effects. The drug blocks cyclooxygenase in the central nervous system, affecting the centers of pain and thermoregulation. Body heat loss during fever increases as a result of vasodilation and increased peripheral blood flow. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of the anti-inflammatory effect of the drug.

The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (retention of Na+ and water) and erosive and ulcerative lesions of the mucous membrane of the gastrointestinal tract.

Pharmacokinetics.

Paracetamol, when taken orally, is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum level of concentration in the blood is reached after 30-60 minutes. When paracetamol is administered rectally, the completeness of its absorption may be lower than after oral administration.
Paracetamol is quickly and evenly distributed throughout the tissues of the body. 10-15% of the dose taken is bound to plasma proteins. The volume of distribution and bioavailability values ​​in children and adults do not differ significantly. The drug penetrates the placental barrier. Less than 1% of the administered dose enters the breast milk of nursing mothers.
Paracetamol is metabolized by liver microsomal enzymes, about 80% forms conjugates with glucuronic acid and sulfates, up to 17% undergoes hydroxylation to form active metabolites that are conjugated with glutathione. With an overdose or deficiency of glutathione, these metabolites can cause hepatocytes.
The half-life of paracetamol is 1.5-2.5 hours. It may increase in patients with severe liver dysfunction and elderly patients. 24 hours after administration, 85-90% of paracetamol is excreted in the urine in the form of glucoronides and sulfates, and 3% unchanged.
In children under 10-12 years of age, the formation of conjugates with sulfates is the main route of metabolism and excretion of paracetamol. The likelihood of hepatotoxicity in children is lower than in adults. Other pharmacokinetic parameters of adults and children do not differ.

Indications for use:

The drug is recommended for adults and children from 1 month of life (for children from 1 to 3 months of life - as prescribed by a doctor):
- as an antipyretic for acute respiratory diseases, influenza, childhood infections, post-vaccination reactions and other infectious and inflammatory diseases accompanied by an increase in body temperature.
- as an analgesic for pain of mild or moderate intensity, including: headaches, muscle pain, algodismenorrhea, pain from injuries and burns.


Important! Get to know the treatment

Directions for use and dosage:

The drug is administered rectally (injected into the rectum). Before using the suppository, it is recommended to empty the intestines.

Dosage for adults:
The average single dose is 500 mg 2-4 times a day; maximum single dose - 1 g (2 suppositories of 500 mg each); maximum daily dose - 4 g.
The duration of treatment with paracetamol without consulting a doctor is 3-5 days.

Dosage for children:
Depends on the age and body weight of the child. The recommended single dose of paracetamol is 10-15 mg/kg of the child’s body weight. The drug is used 3-4 times a day with an interval of 4-6 hours. The maximum daily dose is no more than 60 mg/kg of the child’s body weight.

Approximate dosage scheme for suppositories in children depending on age:

Child's age Single dose
mg suppositories
1-3 months 50 mg 1 soup 50 mg (as recommended by a doctor)
3-5 months 75 mg 1.5 soup. 50 mg each
5-12 months 100 mg 1 soup 100 mg each
1-3 years 100-150 mg 1-1.5 soup. 100 mg each
3 years - 6 years 150-250 mg 1.5 soup. 100 mg - 1 soup. 250 mg each
6 years - 11 years 250-375 mg 1-1.5 soup. 250 mg each
11 years - 14 years 375-500 mg 1.5 soup. 250 mg - 1 soup. 500 mg each

The duration of treatment is no more than 3 days when prescribed as an antipyretic and no more than 5 days when prescribed as an analgesic. Further treatment with the drug is possible only after consultation with a doctor.

Features of application:

With caution
The drug should be taken with caution in case of impaired liver or kidney function (renal, viral, alcoholic liver damage); during pregnancy; during breastfeeding; children under 3 months; elderly patients; with alcoholism; with benign hyperbilirubinemia (including Gilbert's syndrome).

The drug "Paracetamol-Altpharm" rectal suppositories should not be prescribed simultaneously with other drugs containing paracetamol.
When using the drug for more than 7 days, monitoring the functional state of the liver and the picture of peripheral blood is necessary.
If the patient's condition does not improve within 3-5 days, consult a doctor.

Side effects:

Allergic reactions are possible - itching, angioedema. In rare cases, dysfunctions of the liver, kidneys, and hematopoietic system are observed (anemia,). With long-term use in large doses - hepatotoxic effect, aplastic anemia, pancytopenia; nephrotoxicity (interstitial, papillary necrosis). If side effects occur, you should stop taking the drug and consult your doctor.

Interaction with other drugs:

If the patient is taking other medications at the same time, consult a doctor.
Combination with hepatotoxic drugs, anticoagulants, sleeping pills, tranquilizers, and antidepressants is not recommended.
Paracetamol can enhance the effect of indirect anticoagulants (coumarin derivatives), hypoglycemic drugs (sulfonylurea derivatives) by displacing these compounds from binding to plasma proteins.
Taken together with salicylates significantly increases the risk of nephrotoxicity. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer.
Paracetamol enhances the effect of drugs that depress the central nervous system, ethanol.
Long-term use of anticonvulsants causes an increase in the activity of liver enzymes, which increases the intensity of the “first pass” effect through the liver and increases the clearance of paracetamol. This may prevent paracetamol blood levels from reaching therapeutic levels. Barbiturates, rifampicin, salicylamide, antiepileptic drugs, anticonvulsants (phenytoin), tricyclic antidepressants, estrogen-containing contraceptives, butadione, as well as alcohol and other stimulants of microsomal oxidation contribute to the formation of hydroxylated active metabolites of paracetamol, which makes it possible to develop severe intoxications even with a small overdose. Ethanol contributes to the development of acute pancreatitis.
Barbiturates, tricyclic antidepressants, rifampicin increase the half-life of paracetamol. Long-term use of barbiturates reduces the effectiveness of paracetamol.
Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.
Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxicity.
Corticosteroids may increase the risk of gastrointestinal side effects.
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
Long-term combined use of paracetamol and nonsteroidal anti-inflammatory drugs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, and the onset of end-stage renal failure.
Paracetamol reduces the effectiveness of antihypertensive drugs, diuretics, and anti-gout drugs that promote the elimination of uric acid.
Paracetamol inhibits the renal excretion of lithium, methotrexate, aminoglycosides, digoxin in case of impaired renal function (especially in children of primary school age and the elderly), increases the concentration of these compounds in the blood and increases their toxicity.
Caffeine, codeine, acetylsalicylic acid can reduce toxicity and enhance the analgesic effect of paracetamol.
Metoclopramide and domperidone accelerate absorption, and cholesterol reduces the rate of absorption of paracetamol. Atropine, pethidine and other antispasmodics cause a delay in the action of the drug.
Under the influence of paracetamol, the elimination time of chloramphenicol increases 5 times.. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In case of severe overdose - liver failure with progressive encephalopathy, coma, death; with tubular necrosis (including in the absence of severe liver damage); , .


The hepatotoxic effect in adults occurs when taking 10 g or more.

Treatment: administration of SH-group donors and precursors for the synthesis of glutathione - methionine within 8-9 hours after an overdose and acetylcysteine ​​- within 12 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 the time elapsed after its administration.

Storage conditions:

In a dry place, protected from light, at a temperature not exceeding 25 C. Keep out of the reach of children.

Shelf life: 2 years. After the expiration date, do not use the drug.

Vacation conditions:

Over the counter

Package:

Suppositories of 50 mg, 100 mg, 250 mg and 500 mg, 5 pieces each in a blister pack made of polyvinyl chloride film.

Two contour packages along with instructions for use in a cardboard pack.