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

Excipients: ethyl cellulose, silicon dioxide colloid (silicon dioxide colloidal anhydrous), aspartame, citric acid (citric acid anhydrous), sucrose, lemon flavor.

Description:

Homogeneous powder from white to white with a yellowish hue of color with a characteristic, smell of lemon.

Pharmacotherapeutic group:An analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.51 Paracetamol in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined drug. Paracetamol has analgesic (analgesic) and antipyretic effect. Non-narcotic analgesic, blocks cyclooxygenase I and II types, mainly in the central nervous system, 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 anti-inflammatory effect. The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (retention of sodium and water ions) and the mucous membrane of the gastrointestinal tract.

Ascorbic acid participates in the regulation of redox processes, carbohydrate metabolism, blood coagulation, tissue regeneration (restoration), in the synthesis of steroid hormones; increases the body's resistance to infections, reduces vascular permeability, reduces the need for vitamins B1, B2, A, E, folic acid,pantothenic acid. It improves paracetamol tolerance and extends its action (slowing its excretion).

Pharmacokinetics:

When ingestion, paracetamol quickly and completely absorbed. The maximum concentration in the plasma is reached after 30-60 minutes after ingestion.

Paracetamol is quickly distributed across all tissues. Blood, plasma and saliva have comparable concentrations. The connection with plasma proteins is low.

Penetrates through the blood-brain barrier. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk.

Metabolised 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 of metabolism are isoenzyme CYP2E1 (predominantly), GYP1A2 and CYP3A4 (a secondary role). With a deficiency of glutathione, these metabolites can cause damage and necrosis of hepatocytes.

Additional ways of metabolism are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.

In adults, glucuronation predominates, in newborns (including premature infants) and small children, sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) possess low pharmacological (including toxic) activity.

Paracetamol is excreted mainly in the urine. 90% of the absorbed amount is excreted through the kidneys within 24 hours, mainly in the form of metabolites: glucuronides (60-80%) and sulfates (20-30%). Less than 5% is displayed unchanged. The half-life is 1-4 hours. The half-life can be prolonged in cases of liver and kidney disease, in overdose and in newborns. The maximum effect and average duration of action (4-6 hours) approximately correlates with the concentration in the plasma. In patients with severe renal failure (creatinine clearance less than 10 ml / min) excretion of paracetamol and its metabolites slows down.

Ascorbic acid is absorbed in the gastrointestinal tract (mainly in the jejunum). With an increase in the dose up to 200 mg, up to 140 mg (70%) is absorbed; with a further increase in the dose, the absorption decreases (50-20%). Connection with plasma proteins - 25%. The concentration of ascorbic acid in plasma is normally around 10-20 μg / ml, the body stores about 1.5 g when taking daily recommended doses and 2.5 g when taken at 200 mg per day. The time to reach the maximum concentration after ingestion is -4 hours.

Easily penetrates into leukocytes, platelets, and then into all tissues; the greatest concentration is achieved in glandular organs, leukocytes, liver and lens of the eye; penetrates the placenta. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and in plasma.

Metabolised mainly in the liver in desoxyascorbic and then in oxaloacetic and ascorbate-2-sulfate.

It is excreted by the kidneys, through the intestines, with sweat, breast milk in unchanged form and in the form of metabolites.

Indications:

Feverish syndrome in the background of catarrhal diseases. Pain syndrome of mild and moderate severity: arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea (painful menstruation).

Contraindications:

Hypersensitivity (hypersensitivity to the drug), gastric intestinal bleeding, portal hypertension (increased blood pressure in the portal vein), a deficiency of glucose-6-phosphate dehydrogenase deficiency, phenylketonuria, expressed human liver and kidney function, blood disease (anemia, thrombocytopenia, leukopenia) . Children under 12 years of age and patients with a body weight of less than 40 kg.

Carefully:

Disturbances of liver and kidney function, Gilbert syndrome, Dubin-Johnson and Rotor, viral hepatitis, alcohol (alcoholic liver disease), advanced age, simultaneous administration of other paracetamol-containing drugs.

Pregnancy and lactation:

Data on the efficacy and safety studies of the combination of paracetamol and ascorbic acid in pregnant and lactating women are not available. Thus, it is not possible to assess the possible relationship between risk and benefit, and therefore the use of the drug in these categories of patients is not recommended.

Dosing and Administration:

The dose of paracetamol depends on the age and body weight, generally 10-15 mg / kg body weight once, the maximum daily dose of 60 mg / kg body weight.

A single dose (1 sachet) is equivalent to 600 mg of paracetamol.

The weight	Maximum allowable single dose in bags	The maximum allowable daily dose in bags	The maximum allowable daily dose of paracetamol
More than 66 kg	1 sachet	4 sachets (equivalent to 2400 mg of paracetamol)	4000 mg
51-65 kg	1 sachet	4 sachets (equivalent to 2400 mg of paracetamol)	3000 mg
40-50 kg	1 sachet	3 sachets (equivalent to 1800 mg of paracetamol)	2000 mg

Reception of the drug can be repeated after 6-8 hours, i.e. 3-4 packets per day. The interval between taking each dose should be at least 6 hours.

Do not exceed a single dose of the drug.

If the patient simultaneously takes other paracetamol-containing drugs, the maximum daily allowable dose of paracetamol should not be exceeded (see table).

Patients with liver or kidney disease and Gilbert's syndrome: the dosage should be reduced or the interval between doses should be increased.

Patients with severe renal insufficiency: in such cases (creatinine clearance less than 10 ml / min), the interval between doses should be at least 8 hours.

Elderly patients: no special dose adjustment is required.

Mode of application: the contents of one sachet should be poured into a glass, pour the necessary amount of hot water, mix and immediately drink the resulting warm drink.

Application after eating can lead to a delay in the onset of action of the drug.

Duration of application

The drug should not be used for more than 3 days without a doctor's recommendation. It is necessary to consult a doctor if symptoms persist for more than 3 days.

Side effects:

Allergic reactions (skin rash, itching, hives, angioedema), nausea, epigastric pain; anemia, thrombocytopenia, agranulocytosis.

With prolonged use in large doses - hepatotoxic and nephrotoxic action; hematopoiesis.

Overdose:

Symptoms: during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, abdominal pain; disturbance of glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (incl.in the absence of severe liver damage); arrhythmia, pancreatitis. Hepatotoxic effect in adults is manifested when taking 10 g or more.

Treatment: introduction of donators SH-groups and precursors of glutathione-methionine-for 8-9 hours after overdose and acetylcysteine-for 8 hours. The need for additional therapeutic measures (continued methionine administration, intravenous acetylcysteine) is determined depending on the concentration of paracetamol in the blood, and from the time that has elapsed since it was received.

Interaction:

Do not use other medicines containing paracetamol, as well as other non-narcotic analgesics, non-steroidal anti-inflammatory drugs (metamizol sodium, acetylsalicylic acid, ibuprofen and the like), barbiturates, antiepileptic drugs, rifampicin, chloramphenicol.

Prolonged sharing of paracetamol and other non-steroidal anti-inflammatory drugs 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. Inductors of microsomal liver enzymes (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which determines the possibility of developing severe intoxication with small overdoses.

Inhibitors of microsomal liver enzymes (cimetidine) reduce the risk of hepatotoxic action of the drug.

Simultaneous use of paracetamol and ethanol can enhance hepatotoxicity of paracetamol, as well as promote the development of acute pancreatitis.

Reduces the effectiveness of uricosuric medicines.

Metoclopramide increases absorption, paracetamol. The use of drugs that slow the emptying of the stomach (eg, propanthelin bromide), contributes to a decrease in the absorption of paracetamol.

Increases the toxicity of chloramphenicol.

May enhance the effect of indirect anticoagulants.

Special instructions:

Patients with diabetes should take into account that in 1 packet of the drug contains almost 3.8 grams of sucrose (approximately 0.38 bread units). Acceptance of the drug distorts the indicators of laboratory studies in the quantitative determination of glucose and uric acid in the plasma.

Simultaneous reception with ethanol (including ethanol-containing beverages) is not recommended.

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

The intake of the drug does not affect the speed of mental and motor reactions, so there is no need to refrain from driving motor vehicles and taking other activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Powder for the preparation of solution for ingestion 600 mg + 50 mg.

Packaging:

5 grams of powder in bags. The edges of the sachets are covered with a sealing tape. Material of sachets - a composite film from aluminum, paper and polyethylene.

5 bags with instructions for use in a cardboard pack.

Storage conditions:

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 expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N012930 / 01

Date of registration:04.08.2010

Expiration Date:Unlimited

The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany

Manufacturer: & nbsp

STADA Arzneimittel, AG Germany

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp10.05.2017

Illustrated instructions

Instructions

Grippostad® (Grippostad®)