Cefecon D for children, rectal 50 mg 10 pcs

It has analgesic and antipyretic effect. It blocks cyclooxygenase in CNS, affecting the centers of pain and thermoregulation.

In the focus of inflammation, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the lack of significant anti-inflammatory action.

The drug has no negative effect on water-electrolyte metabolism (does not lead to sodium and water retention) and gastrointestinal mucosa.

Pharmacokinetics

Intake and distribution

It is quickly and highly absorbed from the gastrointestinal tract. Cmax is reached after 30-60 min. Binding to plasma proteins is 15%. It penetrates through the HEB.

Metabolism and excretion

Metabolized in the liver; 80% reacts with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form active metabolites, which then conjugate with glutathione to form inactive metabolites.

In glutathione deficiency these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. T1/2 is 2-3 h. Within 24 hours, 85-95% of paracetamol is excreted by the kidneys as glucuronides and sulfates, 3% is unchanged.

Pharmacokinetics in special clinical cases

Vd and bioavailability in children (including infants) are similar to those in adults. In infants of the first 2 days of life and in children aged 3-10 years, the main metabolite of paracetamol is paracetamol sulfate; in children 12 years and older – conjugated glucuronide.

There is no significant age difference in the elimination rate of paracetamol and in the total amount of the drug excreted in the urine.

Indications

The drug is intended for use in children aged 3 months to 12 years.

In children aged 1 to 3 months, a single use of the drug is possible to reduce fever after vaccination (the possibility of using the drug for other indications is decided by the doctor individually).

Used as:

antipyretic for acute respiratory viral infections, influenza, childhood infections, post-vaccination reactions and other conditions accompanied by an increase in body temperature;
an analgesic for pain of mild to moderate intensity, including: headache, toothache, muscle pain, neuralgia, pain from injuries and burns.

Pharmacological effect

Has an analgesic and antipyretic effect. Blocks cyclooxygenase in the central nervous system, affecting pain and thermoregulation centers.

At the site of inflammation, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the lack of significant anti-inflammatory effect.

The drug does not have a negative effect on water-electrolyte metabolism (does not lead to sodium and water retention) and the gastrointestinal mucosa.

Pharmacokinetics

Suction and distribution

Quickly and highly absorbed from the gastrointestinal tract. Cmax is reached within 30-60 minutes. Plasma protein binding – 15%. Penetrates through the BBB.

Metabolism and excretion

Metabolized in the liver; 80% reacts with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form active metabolites, which are then conjugated with glutathione to form inactive metabolites.

With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. T1/2 – 2-3 hours. Within 24 hours, 85-95% of paracetamol is excreted by the kidneys in the form of glucuronides and sulfates, unchanged – 3%.

Pharmacokinetics in special clinical situations

Vd and bioavailability in children (including newborns) are similar to those in adults. In newborns of the first 2 days of life and in children aged 3-10 years, the main metabolite of paracetamol is paracetamol sulfate, in children 12 years and older – conjugated glucuronide.

There is no significant age-related difference in the rate of elimination of paracetamol and in the total amount of the drug excreted in the urine.

Special instructions

The patient should be warned about the need to consult a doctor if fever persists for more than 3 days and pain persists for more than 5 days.

Concomitant use with other paracetamol-containing drugs should be avoided, because this may cause an overdose of paracetamol.

When using the drug for more than 5-7 days, peripheral blood counts and the functional state of the liver should be monitored. Paracetamol distorts laboratory results in the quantitative determination of glucose and uric acid in plasma.

For impaired renal function

Use the drug with caution in case of impaired renal function.

For liver dysfunction

Use the drug with caution in case of liver dysfunction.

Active ingredient

Paracetamol

Composition

One suppository contains:

Active substance:

Paracetamol – 50 mg, 100 mg or 250 mg;

Basics for suppositories:

Solid fat (vitepsol, supposir) – until a suppository weighing 1.25 g is obtained.

Pregnancy

Use with caution during pregnancy, breastfeeding and children under 3 months of age.

Contraindications

Hypersensitivity, neonatal period (up to 1 month).

With caution

Renal and liver failure, benign hyperbilirubinemia (including Gilbert’s syndrome), viral hepatitis, alcoholic liver damage, alcoholism, pregnancy, lactation, genetic absence of glucose-6-phosphate dehydrogenase, concomitant use of other paracetamol-containing drugs.

Side Effects

From the digestive system: nausea, vomiting, abdominal pain are possible.

Allergic reactions: rash on the skin and mucous membranes, itching, urticaria, Quincke’s edema.

From the hematopoietic system: rarely – anemia, thrombocytopenia, leukopenia, agranulocytosis.

With long-term use in high doses, the development of hepatotoxic and nephrotoxic (interstitial nephritis and papillary necrosis) effects, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia is possible.

Interaction

Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol, hepatotoxic drugs increase

production of hydroxylated active metabolites, which makes it possible to develop severe intoxication even with a slight overdose.

Microsomal oxidation inhibitors (cimetidine) reduce the risk of hepatotoxicity.

When taken simultaneously with salicylates, the likelihood of developing nephrotoxicity increases.

When used together with paracetamol, the toxic effects of chloramphenicol are enhanced.

When used together with paracetamol, the effect of indirect anticoagulants is enhanced and the effectiveness of uricosuric drugs is reduced.

Overdose

Symptoms:

during the first 24 hours after administration – pallor of the skin, nausea, vomiting, anorexia, abdominal pain; impaired glucose metabolism, metabolic acidosis.

Symptoms of liver dysfunction may appear 12-48 hours after an overdose.

In case of severe overdose – liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis. The hepatotoxic effect in adults occurs when taking 10 g or more.

Treatment:

administration of SH-group donors and precursors for the synthesis of glutathione – methionine 8-9 hours after an overdose and N-acetylcysteine ​​- after 12 hours.

The need for further therapeutic measures (further administration of methionine, intravenous administration of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its administration.

Storage conditions

In a dry place, at a temperature not exceeding 20 °C

Shelf life

3 years

Manufacturer

Nizhpharm JSC, Russia