Composition
Active ingredients:
paracetamol is 360 mg,
Gorbunova acid 300 mg,
calcium gluconate monohydrate 100 mg
of rimantadine hydrochloride — 50 mg
of rutin trihydrate (in terms of rutin) — 20 mg,
loratadine 3 mg;
excipients: citric acid — 716 mg, sodium bicarbonate — 584 mg, sorbitol — 97,85 mg, macrogol (polyethylene glycol 6000) — 75 mg, isoleucine — 75 mg, flavor raspberry (flavor food powdered “Raspberry 909”) — 75 mg Acesulfame potassium,20 mg, aspartame,20 mg, povidone (povidone K-30) — 3.75 mg, colorant beetroot red (E 162) — 0.4 mg.
Pharmacological properties
Pharmacotherapeutic group: ARI and “cold” symptoms remedy.
ATX Code: R05X
Pharmacological properties
Pharmacodynamics
The combined drug has antiviral, interferogenic, antipyretic, analgesic, antihistamine and angioprotective effects. Paracetamol has analgesic and antipyretic effects.
Ascorbic acid is involved in the regulation of redox processes, promotes normal capillary permeability, blood coagulation, tissue regeneration, and plays a positive role in the development of immune reactions in the body and replenishes the deficiency of vitamin C.
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 acute respiratory viral infections (ARVI), has anti-allergic action (mechanism unclear).
Rimantadine has antiviral activity against the influenza A virus. By blockingthe M2channels of the influenza A virus, it disrupts its ability to enter cells and release ribonucleoprotein, thereby inhibiting the most important stage of viral replication. Induces the production of interferons alpha and gamma. In influenza caused by the B virus, rimantadine has an antitoxic effect.
Rutoside is an angioprotector. Reduces capillary permeability, swelling and inflammation, and strengthens the vascular wall. Inhibits aggregation and increases the degree of deformation of red blood cells.
Loratadine is a blocker of H1-histamine receptors, prevents the development of tissue edema associated with the release of histamine.
Pharmacokinetics
Paracetamol. Absorption is high. Binding to plasma proteins is 15%. Penetrates the blood-brain barrier. It is metabolized in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, and oxidation by microsomal liver enzymes. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The main cytochrome P 450 isoenzymes for this pathway of metabolism are CYP2E1 (mainly), CYP1A2 and CYP3A4 (secondary role). When glutathione is deficient, these metabolites can cause hepatocyte damage and necrosis. Additional metabolic pathways are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxy-paracetamol, which are subsequently conjugated to glucuronides or sulfates. In adults, glucuronidation prevails. Conjugated metabolites of paracetamol (glucuronides, sulfates, and glutathione conjugates) have low pharmacological (including toxic) activity. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and the half-life increases.
Ascorbic acid is absorbed in the gastrointestinal tract (mainly in the jejunum). Binding to plasma proteins is 25%. Diseases of the gastrointestinal tract (peptic ulcer of the stomach and duodenum 12, constipation or diarrhea, helminthic invasion, giardiasis), the use of fresh fruit and vegetable juices, alkaline drinking reduce the absorption of ascorbic acid in the intestines. The normal concentration of ascorbic acid in plasma is approximately 10-20 micrograms / ml. The time of maximum concentration in blood plasma after oral use is 4 hours. It easily penetrates into white blood cells, platelets, and then into all tissues; the highest concentration is achieved in glandular organs, white blood cells, liver and lens of the eye; it penetrates through the placenta.
The concentration of ascorbic acid in white blood cells and platelets is higher than in red blood cells and in plasma. In deficient states, the concentration in white blood cells decreases later and more slowly and is considered as a better criterion for assessing the deficit than the concentration in plasma. It is mainly metabolized in the liver to deoxyascorbic acid and then to oxaloacetic acid and ascorbate-2-sulfate. It is excreted by the kidneys, through the intestines, with sweat in unchanged form and in the form of metabolites. Smoking and drinking ethanol accelerate the breakdown of ascorbic acid (conversion to inactive metabolites), dramatically reducing the body’s reserves. It is excreted during hemodialysis.
Calcium gluconate. Approximately 1/5-1/3 of orally administered calcium gluconate is absorbed in the small intestine; this process depends on the presence of ergocalciferol, pH, dietary characteristics, and the presence of factors that can bind calcium ions. The 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%) – by the intestines.
Rimantadine. After oral use, it is almost completely absorbed in the intestines. Absorption is slow. Binding to plasma proteins is about 40%. The volume of distribution is 17-25 l / kg. The concentration in the nasal secretions is 50% higher than the plasma one. It is metabolized in the liver. More than 90% is excreted by the kidneys within 72 hours, mainly in the form of metabolites,15% – unchanged. In chronic renal failure, the half-life is increased by 2 times. In patients with renal insufficiency and in the elderly, toxic concentrations may accumulate if the dose is not adjusted in proportion to the decrease in creatinine clearance. Hemodialysis has little effect on rimantadine clearance.
Rutoside. The time of maximum concentration in blood plasma after oral use is 1-9 hours. It is mainly excreted in the bile and to a lesser extent by the kidneys. The elimination half-life is 10-25 hours.
Loratadine. It is rapidly and completely absorbed in the gastrointestinal tract. The maximum concentration in the elderly increases by 50%. Binding to plasma proteins is 97%. It is metabolized in the liver to form the active metabolite descarboethoxyloratadine with the participation of cytochrome isoenzymes CYP3A4 and, to a lesser extent, CYP2D6. It does not cross the blood-brain barrier. It is excreted by the kidneys and bile. In patients with chronic renal failure and during hemodialysis, the pharmacokinetics practically do not change.
Indications
Etiotropic treatment of influenza type A, symptomatic treatment of “colds”, influenza and ARVI, accompanied by fever, muscle pain, headache, chills in adults.
Use during pregnancy and lactation
Use during pregnancy and lactation is contraindicated
Contraindications
Hypersensitivity to one or more components of the drug; erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; gastrointestinal bleeding; hemophilia; hemorrhagic diathesis; hypoprothrombinemia; portal hypertension; beriberi K; renal failure; pregnancy, breast-feeding; thyroid diseases, acute kidney diseases, liver diseases (acute glomerulonephritis, acute pyelonephritis acute hepatitis, or exacerbation of chronic diseases of these organs); chronic alcoholism; hypercalcemia, severe hypercalciuria, nephrourolithiasis, sarcoidosis, simultaneous use of cardiac glycosides (risk of arrhythmias); fructose intolerance; phenylketonuria.
Children under 18 years of age.
With caution
Restricted use in epilepsy, cerebral atherosclerosis, diabetes mellitus, glucose-6-phosphate dehydrogenase deficiency, hemochromatosis, sideroblastic anemia, thalassemia, hyperoxaluria, kidney stones, dehydration, electrolyte disorders (risk of hypercalcemia), diarrhea, malabsorption syndrome, calcium nephrourolithiasis (in the anamnesis), hypercalciuria; simultaneous or during the previous 2 weeks taking monoamine oxidase inhibitors, tricyclic antidepressants; while taking drugs that can negatively affect the liver (for example, inducers of microsomal liver enzymes). Caution should be exercised in the treatment of patients with recurrent formation of urate stones in the kidneys; progressive malignant diseases; bronchial asthma.
Elderly patients with arterial hypertension (increased risk of hemorrhagic stroke, due to the drug rimantadine).
Side effects
According to the components included in the product.
From the central nervous system: increased excitability, drowsiness, tremor, hyperkinesia, dizziness, headache, “flushes” of blood to the face.
From the digestive system: damage to the mucous membrane of the stomach and duodenum, dyspepsia, dry mouth, lack of appetite, bloating (flatulence), diarrhea (diarrhea).
From the urinary system: moderate pollakiuria.
From the side of hematopoietic organs: changes in blood parameters. Control is required.
Allergic reactions: angioedema, anaphylactic shock, skin rash, pruritus, urticaria.
Skin disorders: Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome) and acute generalized exanthematous pustulosis.
Other: inhibition of the function of the insular apparatus of the pancreas (hyperglycemia, glucosuria).
If any of the side effects listed in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor immediately.
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, which causes the possibility of severe intoxication even with a small overdose. When used concomitantly with metoclopramide, it is possible to increase the rate of absorption of paracetamol. Long-term use of barbiturates reduces the effectiveness of paracetamol. Microsomal oxidation inhibitors reduce the risk of hepatotoxic effects.
Rimantadine enhances the stimulating effect of caffeine. Cimetidine reduces rimantadine clearance by 18%.
Ascorbic acid increases the concentration of benzylpenicillin in the blood. Improves intestinal absorption of iron preparations (converts trivalent iron to bivalent); may increase iron excretion when used concomitantly with deferoxamine. Increases the risk of crystalluria during treatment with short-acting salicylates and sulfonamides, slows down the excretion of acids by the kidneys, increases the excretion of drugs that have an alkaline reaction (including alkaloids). Reduces the concentration of oral contraceptives in the blood. Increases the total clearance of ethanol, which in turn reduces the concentration of ascorbic acid in the body. When used concomitantly, it reduces the chronotropic effect of isoprenaline. Barbiturates and primidone increase the excretion of ascorbic acid in the urine. Reduces the therapeutic effect of antipsychotic drugs (neuroleptics) — phenothiazine derivatives, tubular reabsorption of amphetamine and tricyclic antidepressants.
Loratadine. Inhibitors of CYP3A4 and CYP2D6 increase the concentration of loratadine in the blood.
How to take, course of use and dosage
Inside.
Dissolve the tablet in half a cup of boiled warm water. Use immediately after dissolution. Stir the solution before use.
Adults: take 1 tablet 2-3 times a day after meals for 3-5 days (no more than 5 days) until symptoms disappear.
If you do not feel better, you should stop taking the drug and consult a doctor.
Overdose
Symptoms: during the first 24 hours after use — pallor of the skin, nausea, diarrhea, vomiting, epigastric pain; impaired glucose metabolism, metabolic acidosis (including lactic acidosis), hypokalemia, tachycardia, arrhythmia, headache, exacerbation of concomitant chronic diseases. Symptoms of impaired liver function may appear 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).
The overdose threshold may be lowered in elderly patients, in patients taking certain medications (for example, inducers of microsomal liver enzymes), alcohol, or those suffering from exhaustion.
Treatment: use of SH-group donors and glutathione — methionine synthesis precursors within 8-9 hours after overdose and acetylcysteine-within 8 hours. Gastric lavage, symptomatic therapy. The need for additional therapeutic measures (further use of methionine, acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after taking it.
Description
Round flat-cylindrical tablets with a rough surface from light pink to dark pink color with lighter and darker inclusions with a chamfer, with a characteristic smell. Greenish-yellow splashes are allowed. They are hygroscopic.
Special instructions
Duration of application-no more than 5 days.
Do not use in the presence of metastatic tumors.
People who are prone to using ethanol should consult a doctor before starting treatment with the drug, since paracetamol can have a damaging effect on the liver.
Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention
During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Form of production
Effervescent tablets [with raspberry flavor and aroma].10 tablets in a tube made of polypropylene complete with a lid made of polyethylene with a silica gel insert. 1 tube together with the instructions for use in a pack of cardboard.
Storage conditions
At a temperature not exceeding 25°C.
Keep out of reach of children.
Shelf
life is 2 years.
Do not use after the expiration date indicated on the package.
Active ingredient
Paracetamol, Ascorbic Acid, Rimantadine, Rutoside, Loratadine, Calcium Gluconate
Dosage form
soluble tablets
Purpose
For adults
Indications
Flu, Sore Throat, Runny Nose, Cold
Best price for AnviMax Raspberry effervescent pills, 10pcs in our online pharmacy!
Side effects of AnviMax Raspberry effervescent pills, 10pcs.
Reviews
There are no reviews yet