Infulgan

Infulgan belongs to the group of antipyretics and analgesics.

The paracetamol contained in the medication demonstrates antipyretic and analgesic activity. Due to the fact that the drug does not affect the processes of PG binding inside the peripheral tissues, it does not lead to the development of a negative effect relative to EBV indicators (fluid and sodium retention), as well as the mucous membrane inside the digestive system. [1]

Indications Infulgan

It is used for short -term therapy for moderate pain (especially after surgery), as well as for short-term therapy of hyperthermic signs (in situations where there is a clinical justification for intravenous administration of drugs or when it is impossible to use other methods of application).

Release form

The release of the medication is realized in the form of an infusion liquid - inside bottles with a capacity of 20, 50 or 100 ml. There is 1 such bottle inside the box.

Pharmacodynamics

Paracetamol has a blocking effect on the activity of COX-1 and COX-2 exclusively within the central nervous system - it acts on pain and thermoregulatory centers.

Inside the inflamed tissues, cell peroxidases neutralize the effect that paracetamol has on COX, which explains the almost complete absence of anti-inflammatory activity. [2]

Pharmacokinetics

Relief of pain is observed after 5-10 minutes from the moment of application of Infulgan. The maximum analgesic effect develops after 60 minutes, and the duration of this effect is usually 4-6 hours.

The medication reduces the temperature within half an hour after application, and its antipyretic effect lasts for at least 6 hours.

Absorption.

With a single administration of up to 2 g of drugs and with repeated use in the next 24 hours, the pharmacokinetic characteristics of paracetamol remain linear.

The level of bioavailability when using an infusion of 0.5 and 1 g of the drug is similar to those observed in the case of using 1 and 2 g of propacetamol (it contains 0.5 and 1 g of paracetamol, respectively). Plasma level Cmax is noted at the end of the infusion, which for 0.5 or 1 g of the substance lasts 15 minutes and is equal to 15 or 30 μg / ml, respectively.

Distribution processes.

The distribution volume of the drug is approximately 1 l / kg. Paracetamol has poor protein synthesis. When using 1 g of Infulgan, most of it (approximately 1.5 μg / ml) is determined inside the cerebrospinal fluid after 20 minutes from the moment of infusion. 

Exchange processes.

Most of paracetamol is involved in intrahepatic metabolism, going through 2 main phases: conjugation with the participation of glucuronic and sulfuric acid. The last phase has a fast saturation in the case of using portions exceeding the medicinal value.

A small amount (less than 4%) of drugs is involved in metabolism with the help of hemoprotein P450, in which an intermediate metabolic element (N-acetylbenzoquinone imine) is formed, which is rapidly neutralized under stable conditions under the action of reduced glutathione. Further, it is excreted in the urine, synthesized with mercaptopuric acid and cysteine. But in the case of massive intoxication, the volumes of this toxic metabolic element increase.

Excretion.

The metabolic components of paracetamol are mainly excreted in the urine. Over a period of 24 hours, 90% of the administered portion is excreted - most in the form of glucuronide (by 60-80%), as well as sulfate (by 20-30%). Less than 5% of drugs are excreted unchanged. The half-life is 2.7 hours, and the systemic clearance is 18 l / h.

Dosing and administration

It is necessary to inject the medication in / in the way.

Adults, adolescents, as well as children weighing over 33 kg use liquid from bottles with a volume of 0.1 liters.

Children weighing less than 33 kg are prescribed medicine from bottles of 20 or 50 ml.

Serving size is based on the patient's weight:

• weight ≤10 kg: portion is 7.5 mg / kg (volume at the 1st injection - 0.75 ml / kg). For 1 injection, no more than 7.5 ml of the drug can be used. No more than 30 mg / kg is administered per day;
• weight in the range> 10 / ≤3.3 kg: dosage size 15 mg / kg (volume 1.5 ml / kg). For 1 injection, you can use 49.5 ml. Per day - maximum 60 mg / kg (no more than 2 g);
• weight in the range> 33 / ≤50 kg: dosage is 15 mg / kg (volume 1.5 ml / kg). For 1 injection, a maximum of 75 ml is allowed. No more than 60 mg / kg is used per day (maximum 3 g);
• weight> 50 kg (with risk of hepatotoxicity): serving size - 1 g (volume 0.1 l). For 1-well infusion, you can enter no more than 0.1 ml. A maximum of 3 g is used per day;
• weight> 50 kg (no risk of hepatotoxicity): dosage size - 1 g (volume 0.1 l). For 1 injection, apply no more than 0.1 liters. No more than 4 g is introduced per day.

A minimum of 4-hour interval must be observed between procedures. Often no more than 4 infusions are administered per day.

In persons with kidney failure (severe), a minimum 6-hour interval between infusions must be observed.

The maximum daily portions are assigned to persons who do not use other medicines, which contain paracetamol, therefore, if they need to use such drugs, they need to change the dosage of Infulgan in accordance with this.

Persons with severe renal failure.

When using paracetamol in people with CC values of ≤30 ml per minute, it is necessary to increase the minimum interval between procedures to 6 hours.

People with chronic alcoholism, hepatocellular insufficiency, and people with dehydration or chronic malnutrition (low levels of intrahepatic glutathione reserves).

A maximum of 3 g of medication can be used per day. Paracetamol is given through an infusion that lasts 15 minutes.

Children weighing ≤10 kg.

Due to the small volume of the substance used, the medicine bottle is not suspended for the infusion. The required amount of drugs is drawn through a syringe from a bottle, and then injected undissolved (or dissolved in 5% glucose or 0.9% NaCl (in a proportion of 1k9)) over a 15-minute interval.

The diluted medicinal liquid must be applied within 60 minutes from the moment of its preparation (this segment also includes the time of the infusion).

A syringe with a volume of 5 or 10 ml is used to select the required dosage (taking into account the weight of the child). In this case, the serving size should be no more than 7.5 ml.

• Application for children

It can be used from the moment the child is born. Cannot be administered only to premature infants.

Use Infulgan during pregnancy

There is only limited information regarding the clinical use of drugs. Epidemiological information regarding the administration of therapeutic portions of paracetamol shows no negative impact on the course of pregnancy or fetal development.

Prospective data on drug poisoning during pregnancy did not show an increase in the likelihood of developing anomalies.

During pregnancy, Infulgan is used only after a careful assessment of all possible risks and benefits, and during the selection of the dosage and duration of therapy, the instructions must be strictly followed.

Taken orally, paracetamol is excreted in small quantities in mother's milk. In infants, the development of negative symptoms was not found in the case of using paracetamol for hepatitis B.

Contraindications

It is contraindicated to appoint people with severe intolerance to paracetamol, propacetamol hydrochloride (which is a precursor of paracetamol) or other elements of the drug. In addition, it is not used for severe hepatocellular insufficiency.

Side effects Infulgan

The main side effects:

• systemic disorders: occasionally malaise appears. Signs of intolerance are singly noted;
• cardiac disorders: occasionally there is a decrease in blood pressure values;
• problems with digestive function: occasionally there is an increase in liver transaminases;
• lesions of the blood system and lymph: leuko-, thrombocyto- or neutropenia is observed singly.

Clinical tests led to frequent occurrence of negative symptoms in the area of the injection (burning and pain).

Signs of severe intolerance appeared occasionally: from rashes or urticaria, to the development of anaphylaxis, in which it was necessary to cancel therapy.

In addition, there is information about the appearance of redness, erythema, itching or tachycardia.

Overdose

The likelihood of hepatic damage (among those hepatitis cholestatic, fulminant or cytolytic forms, as well as liver failure) increases in young children, the elderly, people with chronic alcoholism, hepatic pathologies, alimentary dystrophy and with reduced enzyme activity. With such violations, poisoning with Infulgan can be fatal.

Manifestations develop during the first 24 hours - among them anorexia, abdominal pain, vomiting, pallor and nausea.

Intoxication develops with a single use of a portion of 7.5+ g (for an adult) and 0.14 g / kg (for a child). In such cases, there is a failure of liver function, hepatic cytolysis, and in addition, metabolic acidosis and encephalopathy, which can provoke coma and death. Over a period of 12-48 hours, the indices of intrahepatic transaminases (AST and ALT) and bilirubin with LDH increase, and the values of prothrombin also decrease.

Clinical signs of liver damage are noted after 2 days, reaching their maximum after 4-6 days.

Among the urgent measures required:

• urgent hospitalization;
• identification of plasma parameters of paracetamol (must be carried out before starting therapy, as quickly as possible after poisoning);
• ingestion or intravenous injection of antidote - NAC substances. It is recommended to carry out this procedure within 10 hours after intoxication. You can use NAC later, but the therapy will last longer;
• symptomatic actions.

Before starting therapy, liver function tests should be performed (they must be repeated at 24-hour intervals). Often, the values of intrahepatic transaminases return to normal after 1-2 weeks; while the hepatic activity is fully restored. But sometimes patients may need a liver transplant.

Interactions with other drugs

When combined with probenecid, the level of paracetamol clearance decreases by half - due to blocking the synthesis of the latter with glucuronic acid. In this regard, with the simultaneous introduction of these drugs, a decrease in the portion of paracetamol is required.

Salicylates are able to prolong the half-life of paracetamol.

Substances that induce intrahepatic oxidation of microsomes (this includes barbiturates, phenylbutazone with phenytoin, tricyclics, ethyl alcohol and rifampicin) can lead to the development of severe poisoning even in the case of a slight excess of the dosage.

The combination of paracetamol (4 g per day for a period of at least 4 days) and anticoagulants taken orally can provoke small changes in INR values. With such combinations, it is required to monitor the INR level during therapy and for 7 days after stopping the use of Infulgan.

Storage conditions

Infulgan is required to be kept in a place out of the reach of children. Do not freeze the medicine. Temperature values - maximum 25 ° С.

Shelf life

Infulgan can be used within 24 months from the date of manufacture of the therapeutic.

Analogs

The analogs of the drug are the substances Elgan, Panadol with Grippocitron, Anapiron, Piaron and Efferalgan with Paracetamol, Tsefekon D and Ifimol with Rodapap DC 90 HSP.