OXIMOL [Paracetamol] 1000 mg IV solution

OXIMOL

instructions for medical use of the medicinal product

Tradename

Oxymol, Оксимол

International non-proprietary name

paracetamol, paracetamol

Composition

Each vial (100 ml solution) contains:

active ingredient: paracetamol 1000 mg

excipients: sodium bisulfate, mannitol, disodium edetate, water for injection Dosage form

Solution for infusion.

Pharmacotherapeutic group

Analgesics and antipyretics.

Pharmacological properties

Pharmacodynamics

Paracetamol has pain relief and antipyretic action.

The exact mechanism of the analgesic and antipyretic action of paracetamol has not been established. Apparently, it includes the central and peripheral components.

It is known that paracetamol inhibits cyclooxygenase I and II mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of its anti-inflammatory effect. The lack of influence on the synthesis of prostaglandins in peripheral tissues causes the absence of a negative effect on the water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract.

The analgesic effect of paracetamol occurs within 5-10 minutes after the start of the infusion and reaches a maximum after 1 hour; duration of action from 4 to 6 h.

The antipyretic effect of paracetamol occurs within 30 minutes after the start of the infusion; duration of action not less than 6 h.

Pharmacokinetics

The time of maximum plasma concentration is reached 15 minutes after
intravenous infusion and is 30 mcg / ml. The volume of distribution is 1 l/kg.
Paracetamol is weakly bound to plasma proteins. Penetrates through the blood-brain barrier, through 20 min after intravenous infusion 1 g in cerebrospinal fluid a significant concentration of paracetamol is found (about 1.5 microns / ml).
Metabolized in the liver with the formation of glucuronides and sulfates. Small part (4 %) of the drug is metabolized cytochrome 450 c education intermediate
metabolite ( N -acetylbenzoquinoneimine), which under normal conditions fast
rendered harmless by restored glutathione and output with urine after binding with
cysteine and mercaptopuric acid. However, with massive intoxication, the amount of this toxic metabolite increases. The half-life in adults is 2.7 hours, in children - 1.5 - 2 hours, in newborns - 3.5 hours, total clearance 18 l / h. Paracetamol is excreted mainly in the urine, 90% of the dose taken is excreted by the kidneys within 24 hours, in mainly in the form of glucuronide (60 - 80%) and sulfate (20 - 30%). Less than 5% is excreted in unchanged. In severe renal failure (creatinine clearance below 10-30 ml/min) the excretion of paracetamol is somewhat slowed down, and the half-life is 2 - 5.3 hours. The rate of excretion of glucuronide and sulfate in patients with severe renal failure is 3 times less than in healthy patients.

Indications for use

Oxymol for infusion is indicated for the short-term treatment of moderate pain, especially after

operations and for short-term treatment fever, when intravenous administration clinically

justified or there is an urgent need for pain medication treatment or in cupping

hyperthermia and/or when administered under using other routes of administration is not possible.

Contraindications

• hypersensitivity to paracetamol or proparacetamol hydrochloride (a prodrug of paracetamol) or one of the excipients;
• severe liver failure;

• neonatal period (up to 1 month).

Dosage and administration

Intravenous single infusion over 15 minutes.

The drug should not be mixed in the same infusion bottle with other drugs.

Infusion should be carried out immediately after opening the vial; the unused balance of the drug is destroyed. Before starting the infusion, the vial with the drug should be carefully examined for the absence of visible mechanical particles and a change in the color of the solution.

Unintentional excess of the recommended doses can lead to serious impairment of liver function, including fatal outcome. When determining the dose, one should also take into account the individual risk factors for hepatotoxicity present in the patient: liver failure, chronic alcoholism, chronic malnutrition, dehydration.

Doses are calculated based on the patient's body weight.

Patient's body weight	Dose of Oxymol per application (solution 10 mg/ml)	Minimum interval between doses	Maximum daily dose*
>50 kg	1 g, i.e. 1 bottle (100 ml) up to 4 times a day	4 hours	Not more than 4 g
>33 kg - <50 kg	15 mg/kg i.e. 1.5 ml/kg up to 4 times a day	4 hours	<60 mg/kg, but not more than 3 g
>10 kg - <33 kg	15 mg/kg i.e. 1.5 ml/kg up to 4 times a day	4 hours	<60 mg/kg, but not more than 2 g
<10 kg **	7.5 mg/kg i.e. 0.75 ml/kg up to 4 times a day	4 hours	<30 mg/kg, maximum daily dose - no more than 30 mg/kg

* The maximum daily dose, taking into account the intake of all drugs containing paracetamol or propacetamol.

** The safety and efficacy of the drug in premature infants has not been established.

In severe renal impairment (creatinine clearance <30 ml / min), the interval between injections of the drug should be at least 6 hours.

In patients with impaired liver function, the daily dose should be reduced or the interval between doses of the drug should be increased. The maximum daily dose should not exceed 60 mg/kg (no more than 2 g/day) in the following cases:

- in adults weighing less than 50 kg;

- with chronic liver diseases or compensated liver diseases in the active stage in adults, especially with mild or moderate liver failure;

- Gilbert's syndrome (familial hyperbilirubinemia);

- in patients with chronic alcoholism;

- with malnutrition (low stores of hepatic glutathione);

- in dehydrated patients.

Dose adjustment for elderly patients is not required.

Special instructions and precautions

It is recommended that the patient be switched to oral pain medication as soon as possible.

The risk of developing very serious liver damage increases when the recommended doses are exceeded (including with the simultaneous use of Oxymol and other drugs containing paracetamol and propacetamol), as well as in patients with chronic alcoholism. Clinical symptoms and signs of liver damage (including fulminant hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis) are usually observed 2 days after taking the drug and reach a maximum, usually after 4-6 days.

Patients should be informed of signs of serious skin reactions such as acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis. The drug should be discontinued at the first manifestations of skin reactions or any other signs of hypersensitivity.

In order to avoid the risk of overdose, the simultaneous administration of Oxymol and other drugs containing paracetamol or propacetamol is not recommended.

Distorts the results of the quantitative determination of the content of uric acid in plasma.

Influence on the ability to drive vehicles and mechanisms

Oxymol does not affect the ability to drive vehicles and mechanisms that require increased concentration.

Use during pregnancy and during breastfeeding

Clinical experience with the intravenous use of paracetamol in pregnant women is limited. However, oral epidemiological data have not revealed undesirable side effects in pregnant women and in the fetus / newborn. The expected data on the effect of paracetamol when used during pregnancy did not show an increase in the risk of fetal malformations.

However, Oxymol should be used during pregnancy only if the expected benefit outweighs the potential risk to the mother and fetus. Recommended doses and duration of administration should be strictly controlled.

During breastfeeding, the drug can be used, but care should be taken when taking the drug during this period.

Interaction with other drugs

Probenecid almost halves the clearance of paracetamol by inhibiting the process of its conjugation with glucuronic acid. With simultaneous use, consideration should be given to reducing the dose of paracetamol.

Phenytoin reduces the effectiveness of paracetamol and increases the risk of hepatotoxicity. Patients taking phenytoin should avoid the use of paracetamol in high doses and / or for a long time.

Ethanol contributes to the development of acute pancreatitis.

Inhibitors of microsomal liver enzymes (including cimetidine) reduce the risk of hepatotoxicity.

Prolonged use of barbiturates reduces the effectiveness of paracetamol.

Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs (salicylamide) increases the risk of developing analgesic nephropathy and renal papillary necrosis, the onset of end-stage renal failure.