Universal reference book for medicines
Name of the drug: PERFALGAN (PERFALGAN)

Active substance: paracetamol

Type: Analgesic-antipyretic

Manufacturer: BRISTOL-MYERS SQUIBB (France)
Composition, form of production and packaging
Solution for infusions is
transparent, colorless or slightly yellowish, without visible mechanical inclusions.

1 ml of 1 fl.

paracetamol 10 mg 500 mg

Excipients: mannitol, cysteine ​​hydrochloride monohydrate, disodium phosphate dihydrate, sodium hydroxide, hydrochloric acid concentrated, water d / and nitrogen.

50 ml - bottles (1) - cardboard boxes.

50 ml - bottles (12) - cardboard boxes.

Solution for infusions is transparent, colorless or slightly yellowish, without visible mechanical inclusions.

1 ml of 1 fl.

paracetamol 10 mg 1 g

Excipients: mannitol, cysteine ​​hydrochloride monohydrate, disodium phosphate dihydrate, sodium hydroxide, hydrochloric acid concentrated, water d / and nitrogen.

100 ml - bottles (1) - cardboard boxes.

100 ml - bottles (12) - cardboard boxes.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2008.

PHARMACHOLOGIC EFFECT

Analgetic-antipyretic for infusion.
Has an analgesic and antipyretic effect, the mechanism of which is due to the blocking of COX-1 and COG-2 in the central nervous system (mainly) and the impact on pain centers and thermoregulation. In areas of inflammation, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of anti-inflammatory effect.
The drug does not affect the synthesis of prostaglandins in peripheral tissues, which causes the absence of a negative effect on the water-electrolyte balance (does not cause delay of sodium and water) and the mucosa of the gastrointestinal tract.

PHARMACOKINETICS

Suction and distribution

C max in the blood plasma is achieved after 15 minutes and is 15-30 Ојg / ml.
V d is 1 l / kg. Penetrates through the BBB. Paracetamol weakly binds to plasma proteins.
Metabolism and excretion

Paracetamol is biotransformed in the liver to form glucuronides and sulfates.
A small part (about 4%) is metabolized with the participation of cytochrome P 450isozymes with the formation of an intermediate metabolite (N-acetylbenzoquinonimine), which under normal conditions is quickly neutralized by reduced glutathione and excreted in the urine after binding to cysteine ​​and mercaptopuric acid. However, with massive intoxication, the amount of this toxic metabolite increases.
T 1/2 is 2.7 hours, the total ground clearance is 18 l / h.

Paracetamol is excreted mainly in the urine;
90% of the dose is excreted by the kidneys within 24 hours mainly in the form of glucuronide (60-80%) and sulfate (20-30%), less than 5% is excreted unchanged.
Pharmacokinetics in special clinical cases

T 1/2 in children - 1.5-2 h, in newborns - 3.5 h.

With severe renal failure (CC 10-30 ml / min) excretion of paracetamol is somewhat slowed down, and T 1/2 is 2-5.3 hours. The rate of elimination of glucuronide and sulfate in patients with severe renal insufficiency is 3 times lower than in healthy patients.

INDICATIONS

- pain syndrome of moderate intensity, especially after surgical interventions;

- febrile syndrome on the background of infectious and inflammatory diseases.

The drug is indicated for rapid relief of pain and febrile syndrome (including if paracetamol can not be ingested).

DOSING MODE

The drug is used as an IV infusion for 15 minutes.
The minimum interval between administrations should be 4 hours.
Adolescents older than 12 years and adults with a body weight of more than 50 kg maximum single dose is 1 g of paracetamol, i.e.
1 bottle (100 ml). The maximum daily dose is 4 g.
Adolescents older than 12 years and adults with a body weight of 35 to 50 kg of the drug is prescribed at the rate of 15 mg / kg paracetamol for administration (ie, 1.5 ml of solution per 1 kg of body weight).
The maximum daily dose is 60 mg / kg.
Children aged 1 to 11 years with a body weight of 34 kg are prescribed 15 mg / kg paracetamol per infusion, i.e., 1.5 ml solution per kg, up to 4 times / day.
The minimum interval between administrations is 4 hours. The maximum daily dose is 60 mg / kt.
In patients with impaired liver or kidney function, with Gilbert's syndrome and in the elderly, the interval between injections should be at least 8 hours, with the daily dose to be reduced.

The drug contained in an open and unused completely vial should be destroyed.
Additional dilution of the preparation with 0.9% sodium chloride solution is possible by a factor of 10. The solution prepared in this way should be used within 1 hour after its preparation (including the infusion time).
SIDE EFFECT

From the digestive system: increased activity of liver enzymes (usually without the development of jaundice).

From the side of the cardiovascular system: arterial hypotension.

From the hemopoietic system: thrombocytopenia.

Dermatological reactions: itching, rash on the skin and mucous membranes (usually erythematous or urticaria).

Allergic reactions: angioedema.

CONTRAINDICATIONS

- pronounced violations of the liver function;

- Children's age up to 1 year;

- hypersensitivity to paracetamol or propacetamol hydrochloride (paracetamol prodrug) or any other component of the drug.

With caution, the drug is prescribed for renal insufficiency of a serious degree (QC less than 30 ml / min), benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, patients with chronic alcoholism (including alcoholic liver damage), The elderly, with a deficiency of glucose-6-phosphate dehydrogenase.

PREGNANCY AND LACTATION

With caution appoint the drug during pregnancy.

There were no adverse events in children with paracetamol during lactation (breastfeeding)

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution, the drug is prescribed for renal failure of severe degree (QC less than 30 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated the use of the drug in severe violations of liver function.

With caution, the drug is prescribed for benign hyperbilirubinemia (including Gilbert syndrome), viral hepatitis, patients with chronic alcoholism (including alcoholic liver damage).

SPECIAL INSTRUCTIONS

The risk of liver damage increases in patients with alcoholic hepatosis.

With the use of Perfalan, laboratory tests for the quantitative determination of uric acid in the plasma are distorted.

When the drug is used for a long time, it is necessary to monitor the pattern of peripheral blood and the functional state of the liver.

During the use of the drug should not drink alcohol.

OVERDOSE

The clinical picture of an acute overdose develops in the first 24 hours after taking paracetamol in a high dose.
Symptoms of chronic overdose appear after 2-4 days after increasing the dose of the drug.
Symptoms of acute overdose: diarrhea, decreased appetite, nausea, vomiting, discomfort and / or abdominal pain, pale skin.
With the simultaneous administration of paracetamol to adults at a dose of 7.5 g or more, and for children over 140 mg / kg, cytolysis of hepatocytes occurs with complete and irreversible necrosis of the liver, the development of hepatic insufficiency, metabolic acidosis and encephalopathy, which can lead to coma and death. After 12.8 hours after the introduction of paracetamol, an increase in liver transaminases, LDH and bilirubin levels and a decrease in the level of prothrombin are noted.
Symptoms of chronic overdose: a hepatotoxic effect develops, characterized by common symptoms (pain, weakness, adynamia, increased sweating) and specific, characterizing liver damage.
As a result, hepatonecrosis can develop. Hepatotoxic effect of paracetamol can be complicated by the development of hepatic encephalopathy (disorders of thinking, CNS depression, agitation and stupor), seizures, respiratory depression, coma, cerebral edema, blood clotting disorder, development of DIC syndrome, hypoglycemia, metabolic acidosis, arrhythmia, collapse. Rarely, liver function abnormalities develop with lightning speed and can be complicated by renal failure (tubular necrosis).
Treatment: the introduction of donors of SH-groups and precursors of the synthesis of glutathione methionine after 8-9 hours after an overdose and N-acetylcysteine ​​after 12 hours. The need for additional therapeutic measures (further introduction of methionine, intravenous injection of N-acetylcysteine) is determined by the concentration of paracetamol in the blood, as well as the time that has passed since its introduction.

DRUG INTERACTION

When combined, inducers of microsomal liver enzymes (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites of paracetamol, which allows the development of severe intoxication with a slight excess of the dose.

When combined with paracetamol, ethanol increases the likelihood of developing acute pancreatitis.

When combined, inhibitors of microsomal liver enzymes (including cimetidine) reduce the risk of hepatotoxic effects.

Long-term use of barbiturates reduces the effectiveness of paracetamol.

Long-term combined use of paracetamol and NSAIDs increases the risk of developing analgesic nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure.

Simultaneous long-term use of paracetamol in high doses and salicylates increases the risk of cancer of the kidney or bladder.

When combined, diflunisal increases the concentration of paracetamol in the blood plasma by 50% and increases the risk of developing hepatotoxic reactions.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children at a temperature of 15 В° to 30 В° C.
Shelf life - 2 years.
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