Daleron - instructions for use, dose, side effects, contraindications

Excipients: corn starch, povidone, talc, silicon dioxide colloid, anhydrous, magnesium stearate, casein, processed with formaldehyde, potassium sorbate.

Description:

Round, slightly biconvex white tablets with bevelled edges and risk on one side.

Pharmacotherapeutic group:Analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:

Paracetamol has an analgesic and antipyretic effect. The drug blocks cyclooxygenase 1 and 2 mainly in the central nervous system (CNS), affecting the centers of pain and thermoregulation.In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of its anti-inflammatory effect. The drug has no adverse effect on water-salt metabolism (sodium and water retention) and gastrointestinal mucosa (GI tract), due to lack of influence on the synthesis of prostaglandins in peripheral tissues. The possibility of methaemoglobin formation is unlikely.

Pharmacokinetics:

Absorption is high. The time required to reach the maximum concentration (TCmah) - 0.5-2 hours; the maximum concentration (Cmax) is 5-20 μg / ml. Connection with plasma proteins - 15%. Penetrates through the blood-brain barrier. The volume of distribution varies from 0.8 to 1.36 l / kg body weight. Breast milk penetrates less than 1% of the accepted dose of paracetamol. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Metabolised in the liver (90-95%): 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione with the formation of already inactive metabolites.With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. In the metabolism of the drug is also involved isoenzyme CYP2E1. The half-life (T1 / 2) is 1.5-3 hours (the mean T1 / 2 is 2.3 hours). It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% - in unchanged form. In elderly patients, the clearance of the drug decreases and T1/2.

Indications:

Daleron tablets are used as:

- antipyretic agents for infectious-inflammatory (bacterial, viral) diseases;

- anesthetic for pain in muscles and joints;

- anesthetic for mild to moderate pain syndrome (headache, toothache) of non-inflammatory origin; with neuralgia, algodismenorea;

- an anesthetic for trauma, medical interventions.

Contraindications:

- Hypersensitivity to paracetamol or other components of the drug;

- Children under the age of 9 years and / or with a body weight of less than 35 kg;

- congenital insufficiency of glucose-6-phosphate dehydrogenase;

- expressed violations of the liver or kidney function (creatinine clearance (CK) less than 30 ml / min), viral hepatitis;

- congenital intolerance to fructose.

Carefully:Renal and hepatic insufficiency, congenital hyperbilirubinemia, alcoholic liver damage, elderly patients, pregnancy and lactation period

Pregnancy and lactation:

Preclinical studies in animals have not revealed any adverse effect of paracetamol on pregnancy or fetal development. However, the risk can not be ruled out completely. During pregnancy, especially in the first trimester, and during lactation, the drug can be used only on the recommendation of a doctor, for a short period of time, preferably once.

Dosing and Administration:

Inside, with a lot of fluid. Adults and children over 12 years 1-2 tablets 2-3 times a day at intervals of not less than 4 hours.

The maximum single dose for adults and adolescents over 12 years is 2 tablets (1 g), daily - 8 tablets (4 g).

Children aged 9 to 12 years: to ½ -1 tablet up to 4 times a day. The maximum single dose for children aged 9 to 12 years is 1 tablet (0.5 g), daily - 4 tablets (2 g), with mandatory intervals between taking at least 4 hours.

Do not exceed recommended daily doses.

In patients with impaired liver or kidney function, in elderly patients, the interval between doses should be at least 8 hours and the daily dose should be reduced.

Duration of admission (without consultation with a doctor) no more than 5 days with an appointment as an anesthetic, and no more than 3 days - as an antipyretic agent.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10

often from> 1/100 to <1/10

infrequently from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000

very rarely from <1/10000, including individual messages.

When taking the drug in recommended doses, adverse reactions develop rarely and are poorly expressed.

From the digestive system: rarely - nausea; very rarely - vomiting, diarrhea, jaundice, pancreatitis and increased activity of "liver" enzymes.

Allergic reactions: rarely - skin rash, itching, hives, swelling of Quincke.

From the organs of hematopoiesis and lymphatic system: very rarely - leukopenia, thrombocytopenia.

Other: rarely - weakness.

Overdose:

Symptoms Acute paracetamol poisoning develops within 24 hours and is manifested: pallor of the integument, sweating, abdominal pain, anorexia, nausea, vomiting,hepatonecrosis (the severity of necrosis directly depends on the degree of overdose). Symptoms of liver dysfunction in adults are possible after 1-6 days after taking more than 10-15 g of paracetamol: increased activity of "liver" transaminases, an increase in prothrombin time. In rare cases, impaired liver function develops at a lightning speed and can be complicated by renal insufficiency (tubular necrosis).

Treatment: recommended discontinuation of the drug, gastric lavage, reception of enterosorbents (Activated carbon, Polyphepan (hydrolysis lignin)). Further therapeutic measures should be carried out in the setting of a medical institution: the introduction of donators SH-groups and precursors of glutathione-methionine synthesis for 8-9 hours after overdose and acetylcysteine for 12 hours. The need for additional therapeutic measures (further introduction of methionine, intravenous acetylcysteine) is determined by the concentration of paracetamol in the blood, as well as by the time elapsed after its reception.

Interaction:

Inhibitors of microsomal oxidation (incl. cimetidine) reduce the risk of hepatotoxic action.

Reduces efficiency uricosuric drugs.

For prolonged and regular use paracetamol potentiates the action warfarin and other coumarin derivatives, increases the risk of bleeding.

Simultaneous reception colestyramine leads to a decrease in the absorption of paracetamol (and weakening effects of paracetamol).

Metoclopramide and domperidone increase the absorption of paracetamol.

Simultaneous application of paracetamol and non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the terminal stage of renal failure.

Simultaneous application of paracetamol and chloramphenicol may be accompanied by an increase in T1 / 2 chloramphenicol up to 5 times.

Stimulants of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which causes the possibility of severe intoxication even with small overdoses.

Salicylamide increases paracetamol, which leads to the accumulation of paracetamol and, accordingly,increased formation of its toxic metabolites.

Simultaneous application of paracetamol and ethanol can enhance hepatotoxicity of paracetamol, and also promote the development of acute pancreatitis.

Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.

Special instructions:

Do not use Daleron tablets at the same time as other drugs containing paracetamol (risk of increased side effects).

Patients with congenital hyperbilirubinemia drug should be used in lower doses and with a longer interval between doses.

If there are signs of liver damage (skin itching, jaundice of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increasing the level of "liver" transaminases), stop taking the drug and consult a doctor.

With caution and under the supervision of a doctor, the drug should be administered to patients with impaired liver or kidney function, concomitantly with anticoagulants and drugs affecting the central nervous system. When taking metoclopramide, domperidone, or colestyramine, it is also necessary to consult a doctor.

Distorts the indicators of laboratory tests in quantitative determination of uric acid in the plasma.

To avoid toxic damage to the liver paracetamol should not be combined with the reception of alcoholic beverages, but also to people prone to chronic alcohol consumption. The risk of liver damage increases in patients with alcoholic hepatosis.

With continued use of the drug, it is necessary to monitor the parameters of peripheral blood and the functional state of the liver.

Duration of admission (without consulting a doctor) is no more than 5 days when prescribed as an anesthetic and no more than 3 days - as an antipyretic. Further treatment with the drug is possible only after consulting a doctor.

Casein, treated with formaldehyde, contained in tablets of Daleron, can cause diarrhea.

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

Daleron does not affect the ability to drive a car and to work with technical means.

Form release / dosage:

Tablets of 500 mg.

Packaging:

6 tablets per blister. 2 blisters per pack of cardboard along with instructions for use.

Storage conditions:

Store in a dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:П N011471 / 01

Date of registration:16.09.2009

Expiration Date:Unlimited

Date of cancellation:2016-12-07

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp07.12.2016

Illustrated instructions

Instructions

Daleron (Daleron®)