Paralen extra - instructions for use, doses, side effects, contraindications

Similar drugsTo uncover

Dosage form: & nbspcoated tablets

Composition:

Each tablet contains:

active substances: paracetamol 500 mg, caffeine 65 mg;

Excipients: core: starch corn pregelatinized 35,520 mg, povidone-30 3,330 mg, croscarmellose sodium 13,375 mg, stearic acid 2,775 mg, microcrystalline cellulose 65,000 mg; film sheath: hypromellose 2910/5 16,600 mg, macrogol-6000 3,330 mg, talc 3,330 mg, titanium dioxide 1,550 mg, dimethicone emulsion SE 2 0,250 mg.

Description:

Round, from white to white with a yellowish shade of color, biconvex tablets covered with a film sheath, engraved "PARALEN EXTRA" on one of the parties.

Pharmacotherapeutic group:Analgesic combined (analgesic non-narcotic remedy + psychostimulating agent)

Pharmacodynamics:

Combined drug has an analgesic and antipyretic effect, due to its constituent active components: paracetamol and caffeine.

Paracetamol

Paracetamol is an analgesic and antipyretic agent without anti-inflammatory action with good tolerability in the gastrointestinal tract.The mechanism of action is similar to the action of acetylsalicylic acid and is determined by the process of inhibiting prostaglandins in the central nervous system (CNS). Inhibition is selective.

Paracetamol blocks cyclooxygenase (COX) only in CNS cells, affecting the centers of pain and thermoregulation (in cellular tissues, cellular peroxidases neutralize the effect of paracetamol on COX), which explains the almost complete absence of anti-inflammatory effect. The absence of influence on the synthesis of prostaglandins in peripheral tissues explains the absence of a negative influence on the water-salt metabolism (sodium and water retention) and gastrointestinal mucosa.

The drug has no effect on the glucose level in the blood plasma, so it can be used in patients with diabetes mellitus. Paracetamol can be taken in cases where the use of salicylates is contraindicated.

Caffeine

Caffeine stimulates the psychomotor centers of the brain, has an analytical effect, increases the analgesic effect of paracetamol, removes drowsiness and fatigue, increases physical and mental performance.

Pharmacokinetics:

Paracetamol

Paracetamol is absorbed from the gastrointestinal tract quickly and almost completely. Distribution in body fluids is relatively uniform. The maximum concentration in blood plasma (T_max) is achieved in the period from 15 to 60 minutes after ingestion.

The drug penetrates the blood-brain barrier, the placental barrier and into the milk of nursing mothers.

Breast milk penetrates less than 1% of the accepted dose of paracetamol. The therapeutically effective concentration of paracetamol in blood plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Paracetamol is metabolized in the liver: 80% enters the conjugation reaction with glucuronic acid and sulfates to form inactive metabolites, 17% is hydroxylated to form active metabolites that are conjugated to glutathione and form inactive metabolites. If there is a lack, call them necrosis.

Excretion of paracetamol occurs almost exclusively through the kidneys in the form of conjugated metabolites. About 5% of paracetamol is excreted unchanged. The half-life (T_1/2) is 2-3 hours after taking a therapeutic dose, and in case of severe hepatic insufficiency it can increase up to 5 hours. In case of renal failure due to a decrease in excretory function, the dose of paracetamol should be reduced.

Caffeine

Caffeine is rapidly absorbed from the gastrointestinal tract and distributed throughout the body. T_max caffeine - 1h; T_1/2- 4-9 hours Caffeine almost completely metabolized in the liver by oxidation and demethylation with the formation of 1-methylxanthine, 1-methyl uric acid and acetylated derivatives of uracil, a small amount is converted into theophylline and theobromine. 65-80% of the drug is excreted by the kidneys.

Indications:

Paralen® Extra is used for rapid relief of headache (including migraine pain), toothache, sore throat, back pain, neuralgia, muscular and rheumatic pain, as well as painful menstruation, pain with injuries, burns, and to reduce increased fever for colds and flu.

Contraindications:

- Hypersensitivity to paracetamol, caffeine or any auxiliary substance included in the preparation;

- severe renal and / or hepatic insufficiency;

- acute hepatitis;

- concomitant administration of medications that affect liver function;

- age up to 12 years;

- pregnancy, the period of breastfeeding;

- Do not take as part of complex therapy with other paracetamol-containing drugs.

Carefully:

Use with caution in patients with congenital benign hyperbilirubinemia (Gilbert's syndrome, Dabin-Johnson syndrome or syndrome Rotor); with hepatic and / or renal insufficiency; alcoholic liver damage; suffering from chronic alcoholism; with deficiency of glucose-6-phosphate dehydrogenase; with atopic bronchial asthma and / or pollinosis; hemolytic anemia; with hypersensitivity to aspirin or non-steroidal anti-inflammatory drugs (NSAIDs); when combined with some sleeping pills and antiepileptic drugs (glutetimide, phenobarbital, phenytoin, carbamazepine), with rifampicin, preparations of St. John's wort, tricyclic antidepressants and other inducers of microsomal liver enzymes; when combined with zidovudine andisoniazid; with simultaneous use with alcohol.

Pregnancy and lactation:

Pregnancy

Epidemiological studies conducted during pregnancy did not demonstrate the adverse effects of paracetamol and caffeine used in the recommended doses. It is not recommended to use this product during the first trimester of pregnancy. Regarding the admission during the second and third trimester of pregnancy, you should consult your doctor to decide the relationship between the expected benefit for the mother and the potential risk to the fetus.

Breast-feeding

Paracetamol enters the milk of a nursing mother, but a hundred of the amount has no clinical significance. Paracetamol and its metabolites were not found in the urine of a baby who was breast-fed. I do not report any adverse reactions in children who have breast milk, even after prolonged use of paracetamol, except for one case of maculopapular rash.

With short-term use and accompanying monitoring of the child's condition, there is no need to stop breastfeeding.

Dosing and Administration:

Inside, squeezed large amounts of liquid, 1-2 hours after eating (taking immediately after a meal leads to a delay in the onset of action of the drug).

Adults (including elderly patients):

1-2 tablets up to four times a day, as necessary, with an interval between doses of at least 4 hours. A single dose for persons with a body weight of up to 60 kg is 1 tablet, for individuals weighing more than 60 kg, the maximum single dose is 2 tablets . Do not take more than 8 tablets within 24 hours. The drug should not be used for more than 10 days.

Adolescents aged 12-15 years:

1 tablet 3 times a day with an interval of at least 6 hours.

The drug is not intended for use in children younger than 12 years.

Patients with renal insufficiency:

For patients with renal insufficiency, a dose adjustment is necessary: 500 mg can be taken every 6 hours at a glomerular filtration rate (GFR) of more than 10 ml / min; at GFR values below 10 ml / min, the drug is taken every 8 hours.

Do not exceed the recommended dose. If you have taken a dose that exceeds the recommended dose, seek medical help, even if you are feeling well. Overdose of paracetamol can cause hepatic insufficiency.

The drug is not recommended for more than five days as an anesthetic and for more than three days as an antipyretic agent without prescribing and monitoring the doctor. An increase in the daily dose of the drug or the duration of treatment is possible only under the supervision of a physician.

Side effects:

According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often (≥ 1/10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, < 1/100), rarely (≥1 / 10000, <1/1000) and very rarely (<1/10000); frequency is unknown (the frequency of occurrence of phenomena can not be determined on the basis of available data).

Paracetamol

Violations from the blood and lymphatic system: rarely - Thrombocytopenia, leukopenia, neutropenia, pancytopenia, agranulocytosis.

Immune system disorders: frequency unknown - angioedema (Quincke's edema); frequency unknown - anaphylactic shock.

Disturbances from the respiratory system, chest and mediastinal organs: very rarely - bronchospasm.

Disturbances from the liver and bile ducts: very rarely - jaundice; the frequency is unknown - cytolytic hepatitis, which can lead to acute hepatic insufficiency.

Disturbances from the skin and subcutaneous tissues: rarely - allergic skin reactions, rash; very rarely - acute generalized exanthematous pustulosis, toxic epidermal necrolysis, persistent drug erythema; unknown - Stevens-Johnson syndrome,

With prolonged use of the drug in high doses, the likelihood of hepatotoxic and nephrotoxic effects increases, as well as the development of pancytopenia, therefore in this case, patients need to monitor the parameters of the cellular composition of the blood.

Caffeine

Disorders of the psyche: often - increased excitability, sleep disturbance, insomnia due to CNS stimulation.

Disorders from the gastrointestinal tract: often - nausea caused by irritation of the gastrointestinal tract.

If any of the listed adverse reactions occur, Paralen® Extra should be discontinued and consult a doctor immediately.

Overdose:

Symptoms

Paracetamol

Overdose even with relatively small doses of paracetamol (8-15 g, depending on the patient's body weight) can lead to severe liver damage and sometimes acute tubular necrosis.

In case of an overdose of paracetamol during the first 24 hours, pallor of the skin, anorexia, nausea, vomiting and abdominal pain usually appear. Overdose can lead to hepatic cytolysis, which in turn can lead to hepatocellular insufficiency, metabolic acidosis, encephalopathy, coma and death.

The toxic effect of the drug in adults is possible after taking more than 10 g of paracetamol (12-48 hours after administration) and may be accompanied by pain in the liver, increased activity of liver transaminases, lactate dehydrogenase and bilirubin in blood plasma, while increasing prothrombin time. Rarely, liver function abnormalities develop rapidly. A more pronounced tendency to liver damage is noted in patients taking enzyme inducers (carbamazepine, phenytoin, barbiturates, rifampicin) or in patients who abuse alcohol.

Possible development of a violation of carbohydrate metabolism and metabolic acidosis. There was reported acute renal failure with acute tubular necrosis, characteristic signs of which are pain in the lumbar region, hematuria (an admixture of blood or erythrocytes in the urine), proteinuria (high protein in the urine).

Overdose may also lead to the development of acute pancreatitis and pancytopenia, there were cases of cardiac arrhythmias.

Caffeine

An overdose of caffeine can be accompanied by the following symptoms: epigastric pain, vomiting, frequent urination, tachycardia, arrhythmia, insomnia, anxiety, agitation, anxiety, increased neuro-reflex excitability, tremors and convulsions. Note that the appearance of clinically significant symptoms of caffeine overdose while taking this drug is always associated with severe liver disease on the background of paracetamol overdose.

Treatment

Paracetamol

If you suspect an overdose, even if there is no early symptoms, you should stop using the product and seek medical advice. Within an hour after taking paracetamol, gastric lavage and intake of enterosorbents (Activated carbon, hydrolysis lignin). Thereafter, administer 2.5 g methionine inwardly and intravenous antidote N-acetylcysteine (within 8-15 hours after the overdose), drugs have a positive effect over 48 hours after the overdose. Acetylcysteine usually administered to adults and children intravenously in a 5% glucose solution, the initial dose should be 150 mg / kg body weight and administered for 15 minutes. Then, at a dose of 50 mg / kg administered for 4 hours, then - at a dose of 100 mg / kg 16-20 hours after the start of therapy. Acetylcysteine can also be taken internally at a dose of 70-140 mg / kg 3 times a day for 10 hours after taking a toxic dose of paracetamol. It is necessary to ensure the holding of therapeutic measures aimed at maintaining vital body functions. In case of severe intoxication, hemodialysis may be used.

Caffeine

There is no specific antidote. Treatment is symptomatic, aimed at maintaining vital body functions. Within an hour after an overdose, it is recommended to take activated carbon and enterosorbents. To reduce the effects of caffeine on the central nervous system, intravenous sedation is recommended.

Interaction:

With regular intake for a long time, the drug enhances the effect of indirect coagulants (warfarin or other coumarin products), which increases the risk the occurrence of bleeding. In such patients, it is necessary to monitor the parameters of the blood coagulation system.

Increases the effect of monoamine oxidase inhibitors (MAO).

When combined with inducers of microsomal liver enzymes, for example, some hypnotic and antiepileptic drugs (glutetimide, phenobarbital, phenytoin, carbamazepine, topiramate), with rifampicin, barbiturates, preparations of St. John's wort, tricyclic antidepressants and others that increase the formation of hydroxylated active metabolites of paracetamol, the risk of toxic liver damage increases with minor overdoses of paracetamol (dose of 5 g or more). Inhibitors of microsomal liver enzymes (cimetidine) reduce the risk of hepatotoxic action of the drug.

With the simultaneous use of Paralen® Extra and liquids containing alcohol, the risk of toxic damage to the liver increases.

Co-administration of flucloxacillin with paracetamol can lead to metabolic acidosis, especially in patients with risk factors for glutathione depletion, such as sepsis, malnutrition or chronic alcoholism.

Hepatotoxic substances can increase potential cumulation and overdose of paracetamol.

The rate of absorption of paracetamol can be increased by metoclopramide or domperidone, while cholestyramine can lead to its decrease.

Paracetamol increases the amount of acetylsalicylic acid and chloramphenicol in the blood plasma. Under the influence of paracetamol, the time of chloramphenicol elimination is increased by 5 times.

Joint use of drugs that slow the emptying of the stomach, such as propanthelin, can reduce the absorption of paracetamol and delay its onset.

Probenecid and salicylamide have an effect on the excretion and concentration of paracetamol in the blood plasma.

With the simultaneous administration of paracetamol with lamotrigine, a decrease in the efficacy of lamotrigine was reported.

Simultaneous reception of paracetamol and isoniazid may lead to an increased risk of developing a hepatotoxic effect.

A predisposition to the development of neutropenia and hepatotoxicity was reported with simultaneous administration of paracetamol and zidovudine. Therefore, this drug can be used concomitantly with zidovudine only after a thorough evaluation of the relationshiptargetnd use / risk.

The drug Paralen® Extra can reduce the effectiveness of uricosuric medicines.

Simultaneous administration of clozapine and caffeine can lead to an increased risk of developing toxicity symptoms of clozapine.

Special instructions:

Without consulting a doctor, the Paralen® Extra drug should be taken no more than 3 days in the treatment of febrile syndrome and no more than 5 days - with pain syndrome.

If there is no improvement in the condition when taking the drug, or the headache becomes permanent, it is necessary to consult a doctor.

Patients with impaired liver function and patients receiving large doses of Paralen® Extra for a long period are recommended to regularly monitor liver function and monitor the pattern of peripheral blood.

When conducting tests to determine the content of uric acid or glucose in the blood plasma should inform the doctor about taking Paralen® Extra.

It is necessary to measure prothrombin time with concomitant therapy with indirect anticoagulants (warfarin and other coumarin products) and high doses of paracetamol.

Patients should be warned about the undesirability of concurrent intake of other paracetamol-containing products.

Deficiency of glutathione, caused by eating disorders, fasting, starvation, cystic fibrosis or HIV infection, can increase the risk of severe liver damage with small paracetamol overdoses (5 g or more). Liver damage can occur when lower doses of Paralen® Extra are used together with induction drugs of microsomal liver enzymes, alcohol, or other hepatotoxic drugs.

Avoid drinking alcohol during therapy. The highest risk of hepatotoxicity of paracetamol is noted in chronic alcoholics.

Patients with renal and hepatic insufficiency, Paralen® Extra drug should be used with caution and only after consulting a doctor.

The drug can change the results of doping control tests in athletes.

It is difficult to establish a diagnosis in the syndrome of "acute abdomen."

In patients suffering from atopic bronchial asthma, pollinosis, there is an increased risk of allergic reactions.

Excessive consumption of caffeinated products (coffee, tea) on the background of treatment can cause symptoms of caffeine overdose.

When taking the drug, serious skin reactions can develop, such as acute generalized exanthematous pustulosis; Stevens-Johnson syndrome; toxic epidermal necrolysis, which can lead to death. Patients should be informed of the signs of serious skin reactions. The drug should be discontinued at the first manifestations of skin reactions or any other signs of hypersensitivity.

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

The effects of Paralen® Extra on the ability to drive vehicles and mechanisms are not revealed.

Form release / dosage:

The tablets covered with a cover.

Packaging:

For 12 tablets in a blister of PVC / Al.

For 1 or 2 blisters are placed in a cardboard box along with instructions for use.

Storage conditions:

At temperatures up to 25 ° С.

Keep out of the reach of children.

Shelf life:

3 years.

He apply after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-005892/08

Date of registration:23.07.2008 / 08.10.2015

Date of cancellation:2017-12-19

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp19.12.2017

Illustrated instructions

Instructions

Paralen® extra (Paralen® extra)