Perfalgan - Instructions For Use, Price, Reviews, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Perfalgan

Perfalgan: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Perfalgan

ATX code: N02BE01

Active ingredient: paracetamol (paracetamol)

Producer: Bristol-Myers Squibb (France), Bristol-Myers Squibb, SrL Italy

Description and photo updated: 22.11.2018

Perfalgan is a non-narcotic drug with a pronounced analgesic and antipyretic effect.

Release form and composition

Dosage form of Perfalgan - solution for infusion: clear liquid, slightly yellowish or colorless, without visible mechanical impurities [in a bottle of colorless transparent glass 50 or 100 ml, in a cardboard box 1 or 12 (for hospitals) bottles].

Composition of 1 ml solution:

• active substance: paracetamol - 10 mg;
• auxiliary components: mannitol, cysteine hydrochloride monohydrate, disodium phosphate dihydrate, sodium hydroxide, concentrated hydrochloric acid, nitrogen, water for injection.

Pharmacological properties

Pharmacodynamics

Paracetamol, the active ingredient of Perfalgan, has an analgesic, antipyretic and weak anti-inflammatory effect. The mechanism of its influence consists in blocking the activity of cyclooxygenase 1 and 2 in the central nervous system, inhibition of prostaglandin synthesis, predominantly affecting the centers of pain and thermoregulation in the hypothalamus. The practical absence of an anti-inflammatory effect is explained by the neutralization of the effect of paracetamol on cyclooxygenase in inflamed tissues by cellular peroxidases. Paracetamol does not adversely affect the mucous membrane of the gastrointestinal tract and water-electrolyte metabolism (water and sodium retention), since it does not participate in the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics

The maximum concentration (C _max) of paracetamol in blood plasma after intravenous infusion of the drug at a dose of 500 or 1000 mg is, respectively, 15 or 30 μg / ml and is reached after 15 minutes. The volume of distribution (V _d) is 1 l / kg. Paracetamol weakly binds to plasma proteins. It has the ability to penetrate the blood-brain barrier. After intravenous infusion of a dose of 1000 mg after 20 minutes, a significant content of paracetamol is noted in the cerebrospinal fluid - approximately 1.5 μm / ml.

The active substance is metabolized in the liver, forming glucuronides and sulfates. A small part (4%) of the dose is biotransformed with the participation of the cytochrome P450 enzyme into the active intermediate metabolite N-acetylbenzoquinone imine, which under normal conditions undergoes rapid neutralization by reduced glutathione and, after binding with mercaptopuric acid and cysteine, is excreted in the urine. However, under conditions of massive intoxication, the concentration of this toxic metabolite increases.

The half-life (T _1/2) of paracetamol is: in adults - 2.7 hours; in children - 1.5–2 hours. The total ground clearance is 18 l / h. The drug is excreted mainly by the kidneys: about 90% of the dose taken - during the day with urine, mainly in the form of glucuronide (60 to 80%) and sulfate (20 to 30%); unchanged - less than 5% of the dose taken.

In patients with severe renal insufficiency (with creatinine clearance less than 10-30 ml / min), drug excretion slows down somewhat, T _1/2 is in the range from 2 to 5.3 hours. The rate of excretion of glucuronide and sulfate in such patients is 3 times lower than in healthy people.

Indications for use

• pain syndrome of moderate and low intensity of various origins (including headache, toothache, migraine, neuralgia, algodismenorrhea, myalgia, pain in burns, injuries, and also after surgical interventions);
• febrile syndrome in infectious and inflammatory diseases.

According to the instructions, Perfalgan is also used to quickly relieve pain and fever, including in cases of difficulty in taking the medicine orally.

Contraindications

Absolute:

• severe liver dysfunction;
• children's age up to 1 year;
• increased individual sensitivity to paracetamol or propacetamol hydrochloride (paracetamol prodrug) or any of the auxiliary ingredients of the drug.

Relative (using Perfalgan requires caution):

• severe renal failure (with creatinine clearance less than 30 ml / min);
• benign hyperbilirubinemia (including viral hepatitis, Gilbert's syndrome, alcoholic liver damage);
• chronic alcoholism;
• deficiency of glucose-6-phosphate dehydrogenase;
• pregnancy, lactation period;
• elderly age.

Instructions for use of Perfalgan: method and dosage

Perfalgan is administered intravenously as an infusion over 15 minutes once.

Additional dilution of the drug with 0.9% sodium chloride solution is allowed, maximum 10 times. The diluted solution must be used within one hour of preparation, including the time of infusion.

Unused solution in an open bottle must be destroyed.

Recommended dosage regimens of Perfalgan:

• children from 1 to 11 years old (weighing up to 34 kg): 15 mg / kg body weight of paracetamol per infusion (1.5 ml of solution per 1 kg of body weight) up to 4 times a day. The maximum daily dose is 60 mg / kg. The interval between injections should be at least 4 hours;
• adults and adolescents over 12 years old weighing from 35 to 50 kg: 15 mg / kg of body weight per infusion (1.5 ml / kg). The maximum daily dose is 60 mg / kg. The minimum interval between injections is 4 hours;
• adults and adolescents over 12 years of age weighing more than 50 kg: the maximum single dose is 1000 mg (1 bottle of 100 ml), the daily dose is 4000 mg. The interval between injections should be at least 4 hours.

For patients with impaired renal and / or liver function, with Gilbert's syndrome and elderly patients, it is recommended to reduce the daily dose of Perfalgan and administer it at intervals of at least 8 hours.

Side effects

Possible side reactions from systems and organs:

• organs of the gastrointestinal tract: an increase in the enzymatic activity of hepatic transaminases (without the development of jaundice, as a rule);
• hematopoietic organs: thrombocytopenia;
• cardiovascular system: arterial hypotension;
• skin: itching, rash on the skin and / or mucous membranes (usually urticarial or erythematous), Quincke's edema.

Overdose

In case of an acute overdose of paracetamol within 24 hours after administration, the following symptoms may develop: pallor of the skin, gastrointestinal disturbances (decreased appetite, nausea / vomiting, diarrhea, abdominal discomfort, abdominal pain). 12-13 hours after the administration of Perfalgan, there is an increase in the activity of liver enzymes, lactate dehydrogenase and bilirubin levels, as well as a decrease in prothrombin levels. In the case of simultaneous administration of paracetamol to adults over 7.5 g or children over 140 mg / kg, cytolysis of hepatocytes develops with irreversible and complete liver necrosis, the onset of liver failure, encephalopathy and metabolic acidosis, which can lead to coma, as well as death.

In the case of chronic overdose, 2-4 days after exceeding the dose of paracetamol, a hepatotoxic effect may develop, which is characterized by general (weakness, pain, increased sweating, weakness) and specific liver symptoms. The hepatotoxic effect can cause the development of hepatonecrosis, hepatic encephalopathy (suppression of higher nervous activity, impaired thinking, agitation and stupor), respiratory depression, hypoglycemia, seizures, arrhythmias, blood clotting disorders, metabolic acidosis, cerebral edema, coma, thrombohemorrhagic syndrome.

In rare cases, impaired liver function develops with lightning speed and can be complicated by renal failure (acute tubular necrosis).

For the treatment of acute overdose, it is recommended to administer SH-group donors and precursors of the synthesis of glutathione - methionine 8–9 hours after it, and after 12 hours - the introduction of N-acetylcysteine. Further administration of methionine and N-acetylcysteine depends on the content of paracetamol in the blood, and on the time elapsed after the administration of its increased dose.

special instructions

During the period of prolonged use of Perfalgan, it is necessary to monitor the functioning of the liver and the picture of peripheral blood.

In patients with alcoholic liver hepatosis during treatment with paracetamol, the risk of developing hepatic disorders increases.

When determining the amount of uric acid and glucose in the blood plasma, it should be borne in mind that Perfalgan can distort laboratory tests.

An open and unused vial with the drug must be destroyed.

Application during pregnancy and lactation

Paracetamol has the ability to penetrate the placental barrier. However, the negative effect of the drug on the human fetus has not yet been recorded. Experimental studies have not established the embryotoxic, mutagenic and teratogenic effects of Perfalgan.

Partial release of paracetamol occurs with breast milk - 0.04–0.23% of the dose of the drug taken by the mother is found in milk.

If it is necessary to use Perfalgan during pregnancy and breastfeeding, it is necessary to carefully analyze the ratio of the expected benefits of therapy to the mother and the potential risk to the fetus or child.

Pediatric use

Perfalgan is contraindicated for children under 1 year old.

Children from 1 year old can enter the drug, subject to the dosing regimen.

With impaired renal function

When using Perfalgan in patients with severe renal failure (creatinine clearance below 30 ml / min), caution should be exercised.

For violations of liver function

In severe liver dysfunction, it is not recommended to prescribe the drug.

Patients with alcoholic liver damage should be administered Perfalgan with caution.

Use in the elderly

Older age is a relative contraindication to the use of paracetamol.

Drug interactions

The use of paracetamol at the same time as some drugs can lead to the development of the following effects:

• barbiturates, ethyl alcohol, phenytoin, phenylbutazone, rifampicin, tricyclic antidepressants and other inducers of microsomal oxidation in the liver: an increase in the production of hydroxylated active metabolites, which increases the risk of severe intoxication even in the case of a small overdose of paracetamol. Prolonged use of barbiturates reduces the effectiveness of paracetamol;
• inhibitors of microsomal oxidation (including cimetidine): reduce the likelihood of a hepatotoxic effect;
• non-steroidal anti-inflammatory drugs: with long-term joint use - an increase in the risk of developing nephropathy, papillary renal necrosis and end-stage chronic renal failure;
• salicylates: with long-term simultaneous use with high doses of paracetamol - an increase in the risk of bladder cancer or kidney cancer;
• Diflunisal: 50% increase in the concentration of paracetamol in the blood plasma, which increases the likelihood of developing hepatotoxicity.

Analogs

Perfalgan's analogues are Ifimol, Paracetamol, Paracetamol Kabi, Paracetamol Routek and others.

Terms and conditions of storage

Store at temperatures between 15 and 30 ° C.

Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Perfalgan

There are very few reviews about Perfalgan. Based on the available data, it can be concluded that its effectiveness is beyond doubt, but the drug is not suitable for all patients. Therefore, you should carefully apply Perfalgan in each case, and if negative manifestations occur, immediately inform your doctor about them.

Price for Perfalgan in pharmacies

The price of Perfalgan for a package of 12 100 ml bottles is approximately 1,080 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!