Paracetamol | Paracetamol rectal suppositories for children 100 mg 10 pcs.
Special Price
$13.58
Regular Price
$21.00
In stock
SKU
BID497772
Release form
Rectal suppositories for children
Rectal suppositories for children
Release form
Rectal suppositories for children
Pharmacological action
Non-narcotic analgesic that blocks COX1 and COX2 mainly in the central nervous system, affecting pain and thermoregulation centers. 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 leads to the absence of a negative effect on the water-salt metabolism (delay of Na + and water) and the mucous membrane of the gastrointestinal tract.
Pharmacokinetics
Absorption - high, TCmax - 0.5-2 h Cmax - 5-20 μg / ml. Communication with plasma proteins - 15%. Penetrates through the BBB. Less than 1% of the dose of paracetamol taken by the nursing mother passes into breast milk. It is metabolized in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation with microsomal liver enzymes. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this metabolic pathway are the isoenzyme CYP2E1 (predominantly), CYP1A2 and CYP3A4 (secondary role). With glutathione deficiency, these metabolites can cause damage and necrosis of hepatocytes.
Additional metabolic pathways include hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.
In adults, glucuronidation predominates, in newborns (including premature babies) and young children - sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.
T1 / 2 - 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged.
Indications
Used in children from 3 months to 12 years of age as:
- antipyretic in acute respiratory diseases, flu, childhood infections, post-vaccination reactions and other conditions, accompanied by fever
- a painkiller for pain of mild to moderate intensity, including: headache and toothache, muscle pain, neuralgia, pain from injuries and burns.
Contraindications
Hypersensitivity, neonatal period (up to 1 month).
Caution. Renal and liver failure, benign hyperbilirubinemia (including Gilbert syndrome), viral hepatitis, blood diseases (leukopenia, thrombocytopenia), early chest age (up to 3 months).
Ingredients
1 supp. - paracetamol 100 mg
Excipients: solid fat base to obtain a suppository weighing 1.25 g
Dosage and administration
Rectally.
Multiplicity of administration 2-4 times a day interval - at least 4 hours.
Dose depends on the age and body weight of the child. The average single dose is 10-12 mg / kg body weight. The maximum daily dose of paracetamol should not exceed 60 mg / kg body weight.
Depending on age, the following single doses are recommended:
from 6 to 12 months - 0.5-1 suppository (50-100 mg)
from 1 year to 3 years - 1-1.5 suppository (100-150 mg)
from 3 to 5 years - 1.5-2 suppositories for (150-200 mg)
from 5 to 10 years - 2.5-3.5 suppositories (250-350 mg)
from 10 to 12 years - 3.5-5 suppositories (350-500 mg).
Do not take the drug for more than 3 days as an antipyretic and 5 days as an anesthetic without a doctor's prescription! In children younger than 3 months, it can be used at elevated temperatures caused by vaccination (vaccination). For all other indications, Paracetamol in children under 3 months of age is used only as directed by a doctor.
Side effects
Allergic reactions (including skin rash, itching, angioedema).
Rarely - hematopoiesis (anemia, thrombocytopenia, methemoglobinemia).
Drug Interactions
Stimulators of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which makes it possible to develop small hepatotoxic effects. Microsomal oxidation inhibitors (including cimetidine) reduce the risk of hepatotoxicity. When taken with salicylates, the nephrotoxic effect of paracetamol increases. The combination with chloramphenicol leads to an increase in the toxic properties of the latter. Enhances the effect of indirect anticoagulants and reduces the effectiveness of uricosuric drugs.
Overdose of
Symptoms: during the first 24 hours after taking gastrointestinal upsets (diarrhea, loss of appetite, nausea, vomiting, cramping, stomach pain), Symptoms of liver dysfunction may appear 12-48 hours after overdose (severity of necrosis directly depends on the degree of overdose) - an increase in the activity of “liver” transaminases, an increase in prothrombin time, a detailed clinical picture of liver damage appears after 1-6 days. In severe overdose - liver failure with progressive encephalopathy. Rarely, liver dysfunction develops at lightning speed and can be complicated by renal failure (tubular necrosis).
Treatment: administration of SH-group donors and precursors of glutathione-methionine synthesis within 8-9 hours after an overdose and N-acetylcysteine up to 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.
Storage conditions
In a dry, dark place at a temperature of no higher than 15 РC.
Terms and conditions otpuska IZ
pharmacies without a prescription
dosage form
rectal suppositories
Indications
Colds, Depression, Hypotension, Concussions5 kp Cold, Body fever, SARS, Toothache, Flu
Biochemist, Russia
Rectal suppositories for children
Pharmacological action
Non-narcotic analgesic that blocks COX1 and COX2 mainly in the central nervous system, affecting pain and thermoregulation centers. 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 leads to the absence of a negative effect on the water-salt metabolism (delay of Na + and water) and the mucous membrane of the gastrointestinal tract.
Pharmacokinetics
Absorption - high, TCmax - 0.5-2 h Cmax - 5-20 μg / ml. Communication with plasma proteins - 15%. Penetrates through the BBB. Less than 1% of the dose of paracetamol taken by the nursing mother passes into breast milk. It is metabolized in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation with microsomal liver enzymes. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this metabolic pathway are the isoenzyme CYP2E1 (predominantly), CYP1A2 and CYP3A4 (secondary role). With glutathione deficiency, these metabolites can cause damage and necrosis of hepatocytes.
Additional metabolic pathways include hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.
In adults, glucuronidation predominates, in newborns (including premature babies) and young children - sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.
T1 / 2 - 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged.
Indications
Used in children from 3 months to 12 years of age as:
- antipyretic in acute respiratory diseases, flu, childhood infections, post-vaccination reactions and other conditions, accompanied by fever
- a painkiller for pain of mild to moderate intensity, including: headache and toothache, muscle pain, neuralgia, pain from injuries and burns.
Contraindications
Hypersensitivity, neonatal period (up to 1 month).
Caution. Renal and liver failure, benign hyperbilirubinemia (including Gilbert syndrome), viral hepatitis, blood diseases (leukopenia, thrombocytopenia), early chest age (up to 3 months).
Ingredients
1 supp. - paracetamol 100 mg
Excipients: solid fat base to obtain a suppository weighing 1.25 g
Dosage and administration
Rectally.
Multiplicity of administration 2-4 times a day interval - at least 4 hours.
Dose depends on the age and body weight of the child. The average single dose is 10-12 mg / kg body weight. The maximum daily dose of paracetamol should not exceed 60 mg / kg body weight.
Depending on age, the following single doses are recommended:
from 6 to 12 months - 0.5-1 suppository (50-100 mg)
from 1 year to 3 years - 1-1.5 suppository (100-150 mg)
from 3 to 5 years - 1.5-2 suppositories for (150-200 mg)
from 5 to 10 years - 2.5-3.5 suppositories (250-350 mg)
from 10 to 12 years - 3.5-5 suppositories (350-500 mg).
Do not take the drug for more than 3 days as an antipyretic and 5 days as an anesthetic without a doctor's prescription! In children younger than 3 months, it can be used at elevated temperatures caused by vaccination (vaccination). For all other indications, Paracetamol in children under 3 months of age is used only as directed by a doctor.
Side effects
Allergic reactions (including skin rash, itching, angioedema).
Rarely - hematopoiesis (anemia, thrombocytopenia, methemoglobinemia).
Drug Interactions
Stimulators of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which makes it possible to develop small hepatotoxic effects. Microsomal oxidation inhibitors (including cimetidine) reduce the risk of hepatotoxicity. When taken with salicylates, the nephrotoxic effect of paracetamol increases. The combination with chloramphenicol leads to an increase in the toxic properties of the latter. Enhances the effect of indirect anticoagulants and reduces the effectiveness of uricosuric drugs.
Overdose of
Symptoms: during the first 24 hours after taking gastrointestinal upsets (diarrhea, loss of appetite, nausea, vomiting, cramping, stomach pain), Symptoms of liver dysfunction may appear 12-48 hours after overdose (severity of necrosis directly depends on the degree of overdose) - an increase in the activity of “liver” transaminases, an increase in prothrombin time, a detailed clinical picture of liver damage appears after 1-6 days. In severe overdose - liver failure with progressive encephalopathy. Rarely, liver dysfunction develops at lightning speed and can be complicated by renal failure (tubular necrosis).
Treatment: administration of SH-group donors and precursors of glutathione-methionine synthesis within 8-9 hours after an overdose and N-acetylcysteine up to 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.
Storage conditions
In a dry, dark place at a temperature of no higher than 15 РC.
Terms and conditions otpuska IZ
pharmacies without a prescription
dosage form
rectal suppositories
Indications
Colds, Depression, Hypotension, Concussions5 kp Cold, Body fever, SARS, Toothache, Flu
Biochemist, Russia
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