Kalpol - instructions for use, doses, side effects, contraindications

Component	Content in 5 ml
Active substance
Paracetamol	120.0000 mg
Excipients
Sugar syrup [sucrose, water]	2.8125 ml
Sorbitol	1.7450 ml
Glycerol	315.0000 mg
Xanthan gum	7,500 mg
Methylparahydroxybenzoate	5,0000 mg
Dye azorubin	0.0750 mg
Aromatic Strawberry	0.0125 ml
Purified water	up to 5,0000 ml

Description:

Suspension pink color with the smell of strawberry. On the surface of the suspension, a small foaming is permissible, which disappears when shaken.

Pharmacotherapeutic group:analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:

Mechanism of action

Paracetamol has antipyretic and analgesic effect. Because the paracetamol has an extremely small effect on the synthesis of prostaglandins in peripheral tissues, it does not change the water-electrolyte metabolism and does not damage the mucous membrane of the gastrointestinal tract. In this way, paracetamol particularly suitable for patients with a history of gastrointestinal disease (such as in patients with a history of gastrointestinal bleeding or in elderly patients) or patients taking concomitant medications, when inhibition of peripheral prostaglandins may be undesirable.

Pharmacokinetics:

Suction

Paracetamol is rapidly and almost completely absorbed in the gastrointestinal tract.

Absorption is high, the time to reach the maximum concentration in the blood plasma (TCmax) - 0,5-2 hours; the maximum concentration in the blood plasma (C_max) - 5-20 mcg / ml. Connection with blood plasma proteins - 15%. Paracetamol penetrates the blood-brain barrier. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk.

Distribution

At therapeutic concentrations, binding to plasma proteins is minimal.

Metabolism

Paracetamol is metabolized in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation with microsomal enzymes of the liver. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated to glutathione, and then to cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this pathway are isozymes CYP2E1 (predominantly), CYP1A2 and CYP3A4 (a secondary role). With a deficiency of glutathione, these metabolites can cause damage and necrosis of hepatocytes.

Additional metabolic pathways include hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacamol, which are subsequently conjugated to glucuronides or sulfates. In adults, glucuronation predominates, in newborns (including prematurity) and small children, sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

Excretion

The half-life (T1/2) -1-4 hours. Paracetamol is excreted by the kidneys in the form of metabolites, mainly conjugates, less than 5% - in unchanged form. In elderly patients, clearance of paracetamol decreases and T1/2.

Indications:

The drug Kalpol® is used in children from 3 months to 12 years as:

- antipyretics - to reduce high fever on the background of catarrhal diseases, influenza and childhood infectious diseases;

- anesthetic - with toothache, including with teething or after tooth extraction, headache, sore throat, earache in otitis media.

The preparation Kalpol® in children aged 2 to 3 months can be used once to reduce the temperature after vaccination. The use of the drug for other indications in this age group is possible only on the recommendation of a doctor.

Contraindications:

- Hypersensitivity to paracetamol or any other component of the drug in the anamnesis;

- age younger than 2 months;

- severe violations of the liver and kidneys;

- isomaltase and / or sucrose deficiency, fructose intolerance, glucose galactose malabsorption.

Carefully:

- Severe blood diseases (severe anemia, leukopenia, thrombocytopenia);

- deficiency of the enzyme glucose-6-phosphate dehydrogenase; impaired liver function (including Gilbert's syndrome), impaired renal function.

Before you start taking the drug, you should consult your doctor.

Pregnancy and lactation:

Fertility.

No information.

Pregnancy

In studies on animals and humans, there was no risk of using Kalpol® during pregnancy or the harmful effects of the drug on the development of the embryo and fetus.

Breastfeeding period.

Paracetamol penetrates the placental barrier, and also excretes in breast milk. In human studies, no adverse effect of paracetamol on the baby's body was found in breastfeeding.

Dosing and Administration:

Only for oral administration.

The drug Kalpol® apply inside with a lot of liquid after 1-2 hours after eating.

Suspension of the preparation Kalpol® should not be diluted. For convenience and accuracy of dosing, use a measuring spoon, measuring 2.5 and 5 ml of the suspension.

Children from 2 months to 3 months

For symptomatic relief of postvaccinal reactions, a single dose is 10-15 mg / kg. Apply 1-2 times a day, with an interval of at least 4 hours.If the fever persists after taking a second dose of the drug, you should consult a doctor. For all other indications, the use of the drug in patients of this age category only on the recommendation of a doctor!

Children aged 3 months to 12 years

The maximum daily dose is 60 mg / kg, which is divided into several doses of 10-15 mg / kg in a single dose. Apply one single dose 3-4 times a day with an interval of at least 4 hours. Take no more than four single doses per 24 hours. Do not exceed the indicated dose.

Body weight, kg	Age	Single dose		The maximum daily dose
Body weight, kg	Age	ml	mg	ml	mg
6-8	3-6 months	4,0	96	16,0	384
8-10	6-12 months	5,0	120	20,0	480
10-13	1-2 years	7,0	168	28,0	672
13-15	2-3 years	9,0	216	36,0	864
15-21	3-6 years old	10,0	240	40,0	960
21-29	6-9 years	14,0	336	56,0	1344
29-42	9-12 years old	20,0	480	80,0	1920

The maximum duration of the drug without a doctor's consultation is 3 days. If it is necessary to continue taking the drug for more than 3 days, a doctor's consultation is required.

The drug Kalpol® should not be taken concomitantly with other paracetamol-containing drugs.

Side effects:

Unwanted reactions, information about which was obtained in earlier clinical trials, were infrequent and were obtained from a smallnumber of patients taking the drug.Therefore, the frequency categories were formed on the basis of the experience of the post-marketing use of the drug in the therapeutic dosage and were evaluated as associated with its use. The undesirable reactions presented below are listed according to the body systems and in accordance with the frequency of occurrence. Frequency of occurrence is defined as follows: Often (≥ 1/10), often (≥1/100 and <1/10), infrequently (≥ 1/1 000 and <1/100), rarely (≥ 1/10 000 and <1/1 000), rarely (< 1/10 000), frequency unknown (the frequency can not be estimated from the available data).

The frequency of unwanted reactions was assessed by spontaneous reports obtained at the stage of post-registration observation.

Frequency of occurrence of undesirable reactions

Disorders from the blood and lymphatic system

Very rarely: thrombocytopenia.

Immune system disorders

Rarely: anaphylaxis, skin reactions sensitivity, in including rash on the skin, angioedema and Stevens-Johnson syndrome.

Disturbances from the respiratory system, chest and mediastinal organs

Very rarely: bronchospasm in patients with hypersensitivity to acetylsalicylic acid and intolerance to other non-steroidal anti-inflammatory drugs.

Disturbances from the liver and bile ducts

Rarely: violations of the liver.

Overdose:

Symptoms

During the first 24 hours after ingestion, the pallor of the skin, nausea, vomiting, anorexia, abdominal pain, impaired glucose metabolism (dizziness, unconsciousness, sweating), metabolic acidosis. Symptoms of liver dysfunction (tenderness in the liver, increased activity of "liver" enzymes) may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis, characteristic signs of which are pain in the lumbar region, hematonuria (an admixture of blood or erythrocytes in the urine), proteinuria (increased protein in the urine), with severe liver damage may be absent; arrhythmia, pancreatitis. Hepatotoxic effect in adults is manifested when taking 10 g or more, in children - more than 125 mg / kg. Whenthe presence of factors that affect the toxicity of paracetamol for the liver, it is possible to damage the liver after taking 5 g of paracetamol and more.

Treatment

In case of suspicion of an overdose, even in the absence of severe first symptoms, it is necessary to stop using the drug and immediately consult a doctor for medical assistance. It is recommended to wash the stomach no later than 4 hours after poisoning and taking enterosorbents (Activated carbon); introduction of donors of SH-groups and precursors of glutathione-methionine synthesis for 8-9 hours after overdose and N-acetylcysteine for 12 hours. The need for additional therapeutic measures (further introduction of methionine, intravenous injection of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its administration.

Treatment of children with severe impairment of liver function 24 hours after taking the drug should be carried out in conjunction with specialists from the toxicology center or specialized department of liver diseases.

Interaction:

If the child is already receiving other medications, prior to taking Kalpol®, consult a physician.

Zidovudine, flumecinol, butadione, preparations of St. John's wort increase the production of hydroxylated active metabolites, causing the possibility of developing severe liver damage in case of an overdose of paracetamol (5 g or more).

With the combined use of paracetamol and chloramphenicol, the time of chloramphenicol elimination is increased by a factor of 5, which increases the risk of chloramphenicol poisoning.

Metoclopramide and domperidone increase, and colestramine reduces the rate of absorption of paracetamol.

Paracetamol reduces the effectiveness of uricosuric medicines. The concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (a decrease in the synthesis of procoagulant factors in the liver). The anticoagulant effect of warfarin and other coumarins can be enhanced with prolonged regular daily use of paracetamol with an increased risk of bleeding; The occasional use of paracetamol has no significant effect on the effects of anticoagulants.

Inductors of microsomal oxidation in the liver (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), alcohol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop hepatotoxic effects even with a slight overdose.

Long-term use of barbiturates reduces the effectiveness of paracetamol. Alcohol contributes to the development of acute pancreatitis. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxic effects.

Long-term combined use of paracetamol and other NSAIDs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer.

Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

It should avoid the simultaneous use of the suspension for oral administration of Kalpol® with other paracetamol-containing drugs, as this can cause an overdose of paracetamol.

Patients with glutathione deficiency are overdose, precautions should be taken. The incidence of hepatic insufficiency / impaired liver function in patients with low glutathione levels, in particularly severely depleted patients with anorexia, chronic alcoholics or patients with low body mass index, has been reported.

The use of paracetamol in patients with low levels of glutathione, for example in sepsis, may increase the risk of metabolic acidosis.

When using the drug for more than 5-7 days, it is necessary to monitor the peripheral blood and the functional state of the liver.

The drug Kalpol® contains methyl parahydroxybenzoate, which can be the cause of delayed allergic reactions.

Suspension for oral administration® contains sugar syrup, which should be taken into account when treating patients with diabetes mellitus.

Paracetamol distorts the results of laboratory studies of glucose and uric acid in the blood plasma.

If the duration of fever and pain syndrome is more than 3 days, you should consult your doctor.

Suspension for oral administration® contains 0.20 bread units (XE) in 1 dose (in 5 ml of the suspension).

Effect on the ability to drive transp. cf. and fur:

It is unlikely to affect the ability to drive and use other vehicles.

Form release / dosage:

Suspension for oral administration, 120 mg / 5 ml.

Packaging:

For 70 ml or 100 ml of suspension in dark glass bottles, closed with a lid with plastic lock, or plastic or metal screw caps with the control of the first opening. 1 bottle together with a measuring spoon and instructions for medical use in a cardboard box.

Storage conditions:

Store at a temperature of no higher than 25 ° C in a dark place.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N015380 / 01

Date of registration:20.03.2009

The owner of the registration certificate:GlaxoSmithKline Trading, ZAO GlaxoSmithKline Trading, ZAO Russia

Manufacturer: & nbsp

ASPEN BAD OLDESLOE, GmbH Germany

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Kalpol® (Calpol®)