контрактне виробництво
свічки контактне виробництво
виробництво торгова марка
PARACETAMOL
Release form
Rectal suppositories.
For children
Not contraindicated
For pregnant women
Not contraindicated
For nursing mothers
Not contraindicated
For drivers
Not contraindicated
Storage temperature
Until 25 °C
INSTRUCTION
storage
active substance: paracetamol; 1 suppository contains paracetamol 80 mg or 170 mg or 330 mg; excipient: solid fat.
Medicinal form
Rectal suppositories. Main physico-chemical properties: suppositories are white or white with a creamy shade of color.
Pharmacotherapeutic group
Analgesics and antipyretics. Paracetamol. ATX code N02B E01.
Pharmacological properties
Pharmacodynamics. It has an analgesic, antipyretic and weak anti-inflammatory effect. The mechanism of action is due to inhibition of prostaglandin synthesis and a predominant effect on the thermoregulation center in the hypothalamus. Pharmacokinetics. Absorption of paracetamol with rectal administration is slower than with oral administration, but it is more complete. The peak concentration in blood plasma is reached within 2–3 hours after administration. Paracetamol is quickly distributed in all tissues. Concentrations in blood, saliva and plasma are comparable. Binding to plasma proteins is weak. Paracetamol is metabolized mainly in the liver with the formation of inactive compounds with glucuronic acid and sulfates. As a result of the metabolism catalyzed by cytochrome P450, an intermediate reagent (N-acetylbenzoquinoneimine) is formed, which, when using paracetamol, is quickly detoxified by reduced glutathione and excreted in the urine after conjugation with cysteine and mercaptopuric acid. However, with massive poisoning, the amount of this toxic metabolite increases. It is excreted mainly with urine. 90% of the dose of paracetamol taken is excreted by the kidneys within 24 hours, mainly in the form of glucuronide conjugates (from 60 to 80%) and sulfate conjugates (from 20 to 30%). Less than 5% of the substance is excreted unchanged. The half-life is from 4 to 5 hours. With severe renal failure (creatinine clearance below 10 ml/min), the excretion of paracetamol and its metabolites slows down.
Indication
Symptomatic treatment of diseases accompanied by pain of weak and moderate intensity and/or an increase in body temperature.
Contraindication
Hypersensitivity to paracetamol or other components of the drug. Liver failure. Severe disorders of kidney and/or liver function, congenital hyperbilirubinemia. Recently experienced proctitis, anusitis or rectal bleeding. Alcoholism. Deficiency of glucose-6-phosphate dehydrogenase, blood diseases, pronounced anemia, leukopenia. Inflammation of the mucous membrane of the rectum and dysfunction of the anus. Diarrhea.
Interaction with other medicinal products and other forms of interaction
Interactions that require caution when used together Oral anticoagulants When taking the maximum dose of paracetamol (4 g/day) for at least 4 days, it is possible to increase the effect of oral anticoagulants and increase the risk of bleeding. INR (International Normalized Ratio) should be monitored at regular intervals. If necessary, the dose of oral anticoagulant should be adjusted during treatment with paracetamol. The rate of absorption of paracetamol can increase when taken with metoclopramide and domperidone and decrease with cholestyramine. Barbiturates reduce the antipyretic effect of paracetamol. Anticonvulsant drugs (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of microsomal liver enzymes, can increase the toxic effect of paracetamol on the liver as a result of increasing the degree of transformation of the drug into hepatotoxic metabolites. With the simultaneous use of paracetamol with hepatotoxic agents, the hepatotoxic effect of the drug on the liver increases. Simultaneous use of high doses of paracetamol with isoniazid and rifampicin increases the risk of hepatotoxic syndrome. Paracetamol reduces the effectiveness of diuretics. Do not use simultaneously with alcohol. Effect on laboratory tests Administration of paracetamol can affect the determination of glucose in the blood, carried out by the method of glucose oxidase-peroxidase in the case of abnormally high concentrations. The introduction of paracetamol can affect the determination of uric acid in the blood, carried out by the phosphate-tungsten method.
Features of use
For suppositories, there is a risk of local toxicity, the frequency and intensity of which increases with long-term use, depending on the frequency of administration and the dosage level. Do not use the drug for children together with other products containing paracetamol. When treating with paracetamol at a dose of 60 mg/kg/day, the concomitant use of another antipyretic is justified only in case of ineffectiveness of paracetamol. Do not exceed recommended doses. The drug is contraindicated in diarrhea. If hyperthermia lasts more than 3 days of drug use or the state of health worsens, it is necessary to consult a doctor. Use during pregnancy or breastfeeding. The specified dosage form is used for children in these dosages. The ability to influence the speed of reaction when driving vehicles or other mechanisms. The drug is used in children.
Methods of application
The drug should be used under the close supervision of a doctor, with special caution for children under 1 year of age. Apply rectally. Suppositories are not subject to division to obtain the required dosage. If, when calculating the daily dose according to the child's body weight, the necessary single dose is less than that contained in one suppository, then after consulting a doctor, it is recommended to use other medicinal forms of paracetamol (for example, oral solution). When treating children, you should follow the dose calculation regime according to the child's body weight and choose the dosage form of the drug depending on this. The approximate age of children based on body weight is given only as a recommendation. A single dose is 15 mg/kg of the child's body weight. The drug is used in 4 doses with an interval of 6 hours. The recommended daily dose of paracetamol is about 60 mg/kg of body weight/day in 4 doses, i.e. 15 mg/kg of body weight every 6 hours. Rectal suppositories of 80 mg are used for children aged approximately 3 to 4 months, when the child's body weight is 4 to 6 kg. Apply from 3 to 4 suppositories per day with an interval between administrations of 6 hours depending on the child's body weight at the rate of 60 mg/kg/day. Sample calculation when the child's body weight is 4 kg: 4 kg x 60 mg = 3.80 mg where 4 kg is the child's body weight; 60 mg - daily dose of paracetamol per 1 kg of the child's body weight; 80 mg is the amount of paracetamol in 1 suppository. Rectal suppositories of 170 mg are used for children aged approximately 6 months to 2 years, when the child's body weight is on average from 8 to 12 kg. Apply from 3 to 4 suppositories per day with an interval between administrations of 6 hours depending on the child's body weight at the rate of 60 mg/kg/day. Sample calculation when the child's body weight is 12 kg: 12 kg x 60 mg = 4.170 mg where 12 kg is the child's body weight; 60 mg - daily dose of paracetamol per 1 kg of the child's body weight; 170 mg is the amount of paracetamol in 1 suppository. Rectal suppositories of 330 mg are used for children aged approximately 4 to 9 years, when the child's body weight is on average 15 to 24 kg. Apply from 3 to 4 suppositories per day with an interval between administrations of 6 hours depending on the child's body weight at the rate of 60 mg/kg/day. The daily dose of paracetamol is 60 mg/kg/body weight. Sample calculation when the child's body weight is 22 kg: 22 kg x 60 mg = 4.330 mg where 22 kg is the child's body weight; 60 mg - daily dose of paracetamol per 1 kg of the child's body weight; 330 mg is the amount of paracetamol in 1 suppository. If pain or fever lasts more than 3 days or new symptoms of the disease appear, a doctor's consultation is necessary regarding the feasibility of further use of the drug. The recommended daily dose of paracetamol is about 60 mg/kg of body weight/day in 4 doses, i.e. 15 mg/kg of body weight every 6 hours. In severe renal insufficiency (creatinine clearance less than 10 ml/min), the interval between doses should be at least 8 hours. Application involves rectal administration of one suppository of 80 mg or 170 mg or 330 mg, which is repeated if necessary at intervals of at least 6 hours, without exceeding the daily dose (no more than 4 suppositories per day). Due to the risk of local toxicity, it is not recommended to use suppositories more than 4 times a day, and the duration of treatment with the rectal method of administration should be as short as possible. Children. When treating children, you should adhere to the dosage regimen according to the child's body weight, and depending on this, choose the dosage form of the drug. Paracetamol, rectal suppositories of 80 mg, is intended for children with a body weight of 4 to 6 kg (age approximately 3 months to 4 months). Paracetamol, 170 mg rectal suppositories, is intended for children with a body weight of 8 to 12 kg (age approximately 6 months to 2 years). Paracetamol, 330 mg rectal suppositories, is intended for children with a body weight of 15 to 24 kg (age approximately 4 to 9 years).
Overdose
To avoid overdose, you should not use other medicines containing paracetamol. There is a risk of overdose in children (drug overdose and accidental poisoning are common). This can lead to death. For children with a body weight of less than 37 kg, the maximum daily dose of paracetamol should not exceed 80 mg/kg of body weight/day. For children with a body weight of 38 kg to 50 kg, the maximum daily dose of paracetamol should not exceed 3 g/day. For children with a body weight of more than 50 kg, the maximum daily dose of paracetamol should not exceed 4 g/day. At a single dose of paracetamol in a dose of 150 mg/kg of a child's body weight, it can cause hepatocellular failure, impaired glucose metabolism, metabolic acidosis, hemorrhages, hypoglycemia, encephalopathy, coma, and lead to death. At the same time, the level of liver transaminases, lactate dehydrogenase, and bilirubin increases, and within 12–48 hours, the level of prothrombin decreases. Acute renal failure with acute tubular necrosis can be manifested by severe pain in the lower back, hematuria, proteinuria and can 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, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia may develop on the part of hematopoietic organs. When taking large doses from the side of the central nervous system - dizziness, psychomotor agitation and disorientation; from the urinary system – nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis); from the side of the digestive system - hepatonecrosis. 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; insufficiency of the glutathione system, for example, malnutrition, AIDS, fasting, cystic fibrosis, cachexia) use of 5 g or more paracetamol can cause liver damage. Liver damage may become apparent 12 to 48 hours after an overdose. In case of overdose, the patient should be taken to the hospital immediately, even if there are no early symptoms of overdose. Overdose symptoms appear within the first 24 hours: nausea, vomiting, decreased appetite, pallor, abdominal pain - or may not reflect the severity of the overdose or the risk of injury. Emergency measures: - immediate hospitalization; - determination of the level of paracetamol in blood plasma; - gastric lavage; - administration of the antidote N-acetylcysteine intravenously or methionine orally during the first 10 hours; - symptomatic therapy.
Side effects
Very rarely: allergic reactions: anaphylaxis, anaphylactic shock, Quincke's edema, erythema, urticaria, skin itching, rash on the skin and mucous membranes, exudative erythema multiforme, toxic epidermal necrolysis; from the hematopoietic organs: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, thrombocytopenia, leukopenia, and neutropenia; from the respiratory system: bronchospasm in patients sensitive to aspirin and other NSAIDs; from the digestive system: nausea, pain in the epigastrium, impaired liver function, increased activity of liver enzymes, as a rule, without the development of jaundice, hepatonecrosis (dose-dependent effect); from the endocrine system: hypoglycemia, up to hypoglycemic coma. Associated with the dosage form: irritation of the rectum and anus. If any unwanted reactions occur, you should stop using the drug and consult a doctor.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not higher than 25 ºС. Keep out of the reach of children.
Packaging
5 suppositories in strips. 2 strips in a pack.
Leave category
Without a prescription.
Producer
Monfarm PJSC.
Address
Ukraine, 19161, Cherkasy region, Uman district, village Avramivka, str. Zavodska, 8.