Expiration date: 12/2026
Clinical and pharmacological group
(Preparation for etiotropic and symptomatic treatment of respiratory viral infections)
Form of production, composition and packaging
Powder for preparation of oral solution [lemon, lemon with honey, raspberry, blackcurrant] in the form of a mixture of powder and granules from almost white to yellow with a greenish tinge of color, with a characteristic smell (lemon, lemon with honey, raspberry, black currant), allowed the presence of single granules of pink color, the prepared solution is colorless or with a yellowish tinge, slightly cloudy, with a characteristic smell (lemon, lemon with honey, raspberry, black, the presence of undissolved particles of yellow color is allowed.
1 sachet contains:
paracetamol 360 mg
ascorbic acid 300 mg
calcium gluconate monohydrate 100 mg
rimantadine hydrochloride 50 mg
rutoside (in the form of trihydrate) 20 mg
loratadine 3 mg
Excipients: aspartame 30 mg hypromellose 10 mg, silica colloidal anhydrous 20 mg, lactose monohydrate - 4086 mg, flavor food (lemon or honey-lemon or raspberry, or black currant) - 21 mg. 5 g - heat sealable bags (3) - packs cardboard.
Pharmacological action
Combined preparation has antiviral, interferonogenic, antipyretic, analgesic, antihistamine and angioprotective action.
Paracetamol has analgesic and antipyretic effect.
Ascorbic acid is involved in the regulation of oxidation-reduction processes, promotes normal capillary permeability, blood coagulation, tissue regeneration, plays a positive role in the development of immune responses, replenishes vitamin C deficiency.
Calcium gluconate, as a source of calcium ions, prevents the development of increased permeability and fragility of blood vessels, causing hemorrhagic processes in influenza and SARS, has an anti-allergic effect (the mechanism is unclear).
Rimantadine has antiviral activity against influenza virus A. by Blocking the M2 channels of influenza A, disrupts its ability to penetrate into cells and release ribonucleoprotein, thereby inhibiting a crucial stage of replication of viruses. Induces the production of interferon alpha and gamma. In influenza caused by the b virus, rimantadine has an antitoxic effect.
Rutin is a angioprotectors. It reduces capillary permeability, swelling and inflammation, strengthens the vascular wall. Inhibits aggregation and increases the degree of deformation of red blood cells.
Loratadin - blocker of histamine H1-receptors, prevents the development of tissue edema associated with the release of histamine.
Pharmacokinetics
Paracetamol
Suction and distribution - high. According to the results of clinical studies, the following pharmacokinetic parameters of paracetamol were established: Cmax in blood plasma is achieved by applying the powder through 0.7±0.39 h and is 4.79±1.81 µg/ml.plasma protein - 15%. Penetrates the GAB.Metabolism and wavegenerated in the liver by three main pathways: conjugation with glucuronide, conjugation with sulfate, and oxidation by liver microsomal enzymes. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The major isoenzymes of cytochrome P450 in this pathway is the CYP2E1 isozyme (predominantly), CYP3A4, and CYP1A2 (minor role). With glutathione deficiency, these metabolites can cause damage and necrosis of hepatocytes. Additional routes of metabolism are hydroxylation to 3-hydroxypentanal and methoxylamine to 3-methoxypyrazine, which subsequently conjugium with glucuronide or sulfate. In adults, glucuronidation prevails. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.It is excreted by the kidneys as metabolites, mainly conjugates, only 3% unchanged. According to the results of clinical studies of the T1/2 of paracetamol is equal to 2.73±0.76 h. Pharmacokinetics in special clinical slucaju elderly patients have reduced clearance of the drug and increases T1/2.
Ascorbic acid
Absorption and distribution is absorbed in the gastrointestinal tract (mainly in the jejunum). Gastrointestinal diseases (stomach and duodenal ulcer, constipation or diarrhea, worm infestation, giardiasis), the use of fresh fruit and vegetable juices, alkaline drink reduce the absorption of ascorbic acid in the intestine. The concentration of ascorbic acid in the plasma of normal is approximately 10-20 µg/ml. the Time to reach Cmax in plasma after oral administration - 4 hours Connection with the plasma protein - 25%. Easily penetrates into leukocytes, platelets, and then-in all tissues, the highest concentration is achieved in the glandular organs, leukocytes, liver and lens of the eye, penetrates the placental barrier. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and plasma. In deficit conditions, the concentration in leukocytes decreases later and more slowly and is considered as a better criterion for assessing the deficit than the concentration in plasma.Metabolism and excretionetaboliziruetsya mainly in the liver in deoxyascorbic and further in oxaleacetic acid and ascorbate-2-sulfate.It is excreted by the kidneys, through the intestine, then unchanged and in the form of metabolites.Pharmacokinetics in special clinical cases, the use of ethanol accelerates the destruction of ascorbic acid (conversion to inactive metabolites), sharply reducing the reserves in the body.It is excreted in hemodialysis.
Calcium gluconate
Approximately 1/5-1/3 of the orally administered calcium gluconate is absorbed in the small intestine, this process depends on the presence of ergocalciferol, pH, diet features and the presence of factors capable of binding calcium ions. Absorption of calcium ions increases with its deficiency and the use of a diet with a reduced content of calcium ions.About 20% is excreted by the kidneys, the remaining amount (80%) - the intestine.
Rimantadine
Absorption and distribution after ingestion is almost completely absorbed in the intestine. Absorption is slow. According to the results of clinical studies established the following pharmacokinetic parameters of rimantadine: Cmax in blood plasma is achieved when using the powder through 5.28±2.54 h and is 69.0±19.7 ng/ml. Relationship to plasma proteins - about 40%. Vd - 17-25 l/kg. Concentration in the discharge from the nose 50% higher than in plasma.Metabolism and wavegenerated in the liver. More than 90% is excreted by the kidneys for 72 hours, mainly in the form of metabolites, 15% - in unchanged form. According to the results of clinical studies of the T1/2 of rimantadine is 33.26± 12.76 h. Pharmacokinetics in special clinical slucajni chronic renal failure T1/2 increases in 2 times. In persons with renal insufficiency and in elderly people, rimantadine may accumulate in toxic concentrations, if the dose is not adjusted in proportion to a decrease in creatinine clearance. Hemodialysis has a slight effect on the clearance of rimantadine.
Rutoside
Time to reach Cmax in plasma after oral administration-1-9 no. it is Excreted mainly with bile and to a lesser extent kidneys. T1/2 of 10-25 h.
Loratadine
Suction and RASPREDELENIYa and completely absorbed in the digestive tract. According to the results of clinical studies, the following pharmacokinetic parameters of loratadine were established: Cmax in blood plasma is achieved through 3.28±1.25 h and is 1.85±0.95 ng/ml.plasma protein - 97%. It permeates through the GEB.Metabolism and excretion is metabolized in the liver to form an active metabolite of descarboethoxyloratadine with the participation of cytochrome CYP3A4 isoenzymes and to a lesser extent CYP2D6.It is excreted by the kidneys and bile. According to the results of clinical studies of T1/2 loratadine is equal to 11.29±5.52 h. Pharmacokinetics in special clinical sluchajnyh in the elderly increases by 50%.In patients with chronic renal insufficiency and during hemodialysis pharmacokinetics virtually unchanged.
Dosage
Adults are prescribed inside 1 sachet 2-3 times / day after meals for 3-5 days (no more than 5 days) until the symptoms of the disease disappear.If there is no improvement in the state of health, the drug should be stopped and consult a doctor.The contents of 1 bag should be dissolved in half a glass of boiled warm water and drink immediately after dissolution. Before use, the solution must be stirred.
Overdose
Symptoms: during the first 24 hours after administration - pale skin, nausea, diarrhea, vomiting, epigastric pain, glucose metabolism, metabolic acidosis, tachycardia, arrhythmia, headache, exacerbation of concomitant chronic diseases. Symptoms of liver dysfunction may appear after 12-48 hours after an overdose. In severe overdose-liver failure with progressive encephalopathy, coma, acute renal failure with tubular necrosis (including in the absence of severe liver damage).
Treatment: the introduction of aid donors SH-groups and precursor to the synthesis of glutathione-methionine for 8-9 hours after the overdose and acetylcysteine within 8 h. gastric Lavage, symptomatic therapy. The need for additional therapeutic measures (further administration of methionine, acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its reception.
Drug interaction
Paracetamol
reduces the effectiveness of uricosuric drugs.Concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs.Inducers of microsomal oxidation in the liver (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, that makes the possibility of development of heavy intoxications even at small overdose.While the use of metoclopramide may increase the rate of absorption of paracetamol.Prolonged use of barbiturates reduces the effectiveness of paracetamol.Inhibitors of microsomal oxidation reduce the risk of hepatotoxic action.
Rimantadine
enhances the stimulating effect of caffeine.Cimetidine reduces the clearance of rimantadine by 18%.
Ascorbic acid
increases the concentration of benzylpenicillin in the blood.It improves the absorption of iron in the intestine (translates trivalent iron into bivalent), can increase the excretion of iron while using deferoxamine.Increases the risk of crystalluria in the treatment of salicylates and sulfonamides of short-acting, inhibits the excretion of kidney acids, increases the excretion of drugs with an alkaline reaction (including alkaloids'.)Reduces the concentration of oral contraceptives in the blood.It increases the overall clearance of ethanol, which in turn reduces the concentration of ascorbic acid in the body.With simultaneous use reduces the chronotropic effect of isoprenaline.Barbiturates and primidone increase excretion of ascorbic acid in the urine.Reduces the therapeutic effect of antipsychotic drugs (neuroleptics) - phenothiazine derivatives.Reduces tubular reabsorption of amphetamine and tricyclic antidepressants.
Loratadine
CYP3A4 and CYP2D6 inhibitors increase the concentration of loratadine in the blood.
Pregnancy and lactation
Use during pregnancy and breastfeeding is contraindicated.
Side effect
From the Central nervous system: increased excitability, drowsiness, tremor, hyperkinesia, dizziness, headache, "tides" of blood to the face.From the digestive system: damage to the mucous membrane of the stomach and duodenum, dyspepsia, dryness of the mucous membrane in the mouth, lack of appetite, flatulence, diarrhea.
From the urinary system: moderate pollakiuriya.
From the hematopoietic organs: changes in blood parameters (need control).
From the endocrine system: inhibition of the function of the insulin apparatus of the pancreas (hyperglycemia, glucosuria).Allergic reactions: skin rash, itching, urticaria.If any of the side effects listed in the instructions are aggravated, or you notice any other side effects not listed in the instructions, notify your doctor immediately.
Storage conditions and terms
The drug should be stored in a dry place, out of reach of children at a temperature not exceeding 25°C.
Shelf life-2 years.
Indications
- etiotropic treatment of influenza a, - symptomatic treatment of colds, influenza and SARS, accompanied by fever, muscle pain, headache, chills, in adults.
Contraindications
— erosivno-azwenne shock syndrome in acute phase, gastro — intestinal bleeding, hemophilia, hemorrhagic diathesis, hypoprothrombinemia, — portal hypertension, beriberi K, — kidney failure, thyroid disease, acute kidney disease, the liver (acute glomerulonephritis, acute pyelonephritis, acute hepatitis), or exacerbation of chronic diseases of these organs, — alcoholism, — hypercalcemia, hypercalciuria expression, nefrourolitiaz, — sarcoidosis, — concomitant use of cardiac glycosides (risk of arrhythmias), — lactose intolerance, lactase deficiency, glucose-galactose malabsorption, - phenylketonuria, - pregnancy, — the period of breastfeeding, — children up to 18 years, - increased sensitivity to one or more components of the drug.
With caution the drug should be used and to restrict its use in epilepsy, cerebral arteriosclerosis, diabetes, deficiency of glucose-6-phosphate dehydrogenase, hemochromatosis, sideroblastnoj anemia, thalassemia, hyperoxaluria, kidney stones, dehydration, electrolyte disorders (risk of hypercalcaemia), diarrhea, malabsorption syndrome, calcium nefrourolitiaz (history), hypercalciuria, and in elderly patients with arterial hypertension (increases the risk of hemorrhagic stroke, by a member of the drug rimantadine).
Special instruction
Duration of application-no more than 5 days.Do not use the drug in the presence of metastatic tumors.Patients who abuse alcohol should consult a doctor before treatment with the drug, since paracetamol can have a damaging effect on the liver.
Impact on the ability to drive and operate machinery
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.
Application in violation of renal function
Contraindicated in renal failure, acute kidney disease (acute glomerulonephritis, acute pyelonephritis), or exacerbation of chronic kidney diseases
Application in violation of liver function
Contraindicated in acute liver diseases( acute hepatitis), or exacerbation of chronic liver diseases
