AnviMax, capsules, 20pcs

Composition

Capsule P.

Active ingredient: paracetamol-360 mg;

Excipients: pregelatinized starch-9 mg, colloidal silicon dioxide-3 mg, lactose monohydrate-1.2 mg, magnesium stearate-3.8 mg, polysorbate 80-3 mg.

The composition of the hard gelatin capsule: gelatin-94.795 mg, proprietary blue dye (E 131) or diamond blue dye (E 133) – 0.265 mg, titanium dioxide (E 171) – 1.94 mg.

Capsule R.

Active ingredients: ascorbic acid-300 mg, calcium gluconate monohydrate-100 mg, rimantadine hydrochloride-50 mg, rutoside trihydrate (based on rutoside) — 20 mg, loratadine-3 mg;

Excipients: potato starch-2.2 mg, magnesium stearate-4.8 mg.

Capsules hard gelatin: gelatin — 94,064 mg, dye iron oxide yellow (E 172) — 0,97 mg, dye iron oxide red (E 172) — appears to be 0.485 mg, dye crimson [Ponceau 4R] (E 124) — 0,511 mg, titanium dioxide (E 171) — 0,97 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 blocking_{the M2}channels 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-methoxyparacetamol, 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.

The maximum concentration (cmax) of paracetamol in blood plasma is reached when using capsules after 1.20±0.72 hours and is 5.01±1.70 mcg / ml, the half-life (T_1/2) is 3.04±1.01 hours.

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 concentration of ascorbic acid in the blood plasma is normally approximately 10-20 mcg / 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, through the sweat glands 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, T_1/2 increases 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.

_{Cmax of}rimantadine in blood plasma is reached with the use of capsules in 4.53±2.52 hours and is 68.2±26.6 ng / ml, T_1/2-30.51±9.83 hours.

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. T_1/2 — 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.

_{Cmax of}loratadine in blood plasma is reached in 2.92±1.31 hours and is 2.36±1.53 ng / ml, T_1/2-12.36±6.84 hours.

Indications

Treatment of influenza type A, symptomatic treatment of “colds”, flu and ARVI, accompanied by fever, chills, nasal congestion, sore throat, joint and muscle pain, headache.

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); lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

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.

Elderly patients with arterial hypertension (increased risk of hemorrhagic stroke, due to the drug rimantadine).

Side effects

Possible undesirable side effects are indicated according to the components included in the composition.

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.

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).

Post-registration experience

Cases of angioedema, pre-syncope, fever, low blood pressure, urticaria, pruritus, erythema, hearing disorders, and sore throat have been reported during the use of AnviMax®.

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.

For adults: 1 capsule P of blue color and 1 capsule P of red color (single dose) 2-3 times a

day after meals, washed down with water. The interval between doses of the drug is 4-6 hours. A course of therapy until the symptoms of the disease disappear. AnviMax® should not be taken for more than 5 days. If there is no relief of symptoms within 3 days after starting the drug, you should consult a doctor.

Overdose

Symptoms: during the first 24 hours after ingestion — pallor of the skin, nausea, diarrhea, vomiting, epigastric pain; impaired glucose metabolism, metabolic acidosis, 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).

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

Capsules P solid gelatin No. 0 blue color. The contents of capsules are a mixture of powder and granules of white or white with a creamy or pinkish tinge of color, the presence of lumps is allowed.

Capsules R solid gelatin No. 0 red color. The contents of capsules are a mixture of powder and granules from yellow to yellow with a greenish tinge and white in color, the presence of lumps is allowed.

Special instructions

Duration of application-no more than 5 days.

It is necessary to carry out laboratory monitoring of blood parameters.

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

Taking into account the possible development of side effects (dizziness, drowsiness) during treatment, it is not recommended to drive vehicles and engage in other activities that require increased concentration of attention and high speed of psychomotor reactions.

Form of production

Capsules.

Capsules of P. 10 capsules in a contour cell package.

Capsules: 10 capsules in a contour cell package.

2 contour cell packages (one with blue P capsules, the second with red P capsules) with instructions for use in a cardboard pack.

Storage conditions

Store in a dry place protected from light 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

Capsules

Purpose

For adults

Indications

Cold, Flu