Anvimax powder for internal use blackcurrant №12

pharmachologic effect

The combined drug has antiviral, interferonogenic, antipyretic, analgesic, antihistamine and angioprotective effects.

Paracetamol possesses analgesic and antipyretic effects.

Vitamin C participates in the regulation of redox processes, contributes to the normal permeability of capillaries, blood clotting, tissue regeneration, plays a positive role in the development of immune reactions of the body, compensates for vitamin C deficiency

Calcium gluconateas a source of Calcium ions, prevents the development of increased permeability and fragility of blood vessels, causing hemorrhagic processes in case of influenza and ARVI, has antiallergic effect (mechanism is unclear).

Rimantadine possesses antiviral activity against influenza A virus. Blocking M₂Channels of influenza A virus, violates its ability to penetrate cells and release ribonucleoprotein, thereby inhibiting the most important stage of viral replication. Induces the production of Interferon alpha and gamma. With influenza B virus, Rimantadine has an antitoxic effect.

Rutoside is an angioprotector.Reduces capillary permeability, swelling and inflammation, strengthens the vascular wall. It inhibits aggregation and increases the degree of red blood cell deformation.

Loratadine - histamine H blocker₁-receptors, prevents the development of tissue edema associated with the release of histamine.

Pharmacokinetics

Paracetamol

Suction and distribution

Absorption is high. According to the results of clinical studies, the following pharmacokinetic parameters of Paracetamol were established: when using capsules C_max plasma paracetamol is reached in 1.20 ± 0.72 h and amounts to 5.01 ± 1.70 mcg / ml, with the use of powder in 0.7 ± 0.39 h and amounts to 4.79 ± 1.81 mcg / ml.

Plasma protein binding - 15%. Penetrates the BBB.

Metabolism and excretion

Metabolized in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, 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 isoenzymes of cytochrome P450 for this pathway are the isoenzyme CYP2E1 (predominantly), CYP1A2, and CYP3A4 (secondary role). When glutathione is deficient, these metabolites can cause damage and necrosis of hepatocytes. Additional metabolic pathways are hydroxylation to 3-hydroxy paracetamol and methoxylation to 3-methoxy paracetamol, which are subsequently conjugated with glucuronides or sulfates.In adults, glucuronidation prevails. Conjugated paracetamol metabolites (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

Excreted by the kidneys as metabolites, mainly conjugates, only 3% unchanged. According to the results of clinical studies T_1/2 paracetamol is 3.04 ± 1.01 h when taking the drug in capsules, 2.73 ± 0.76 h - when taking the drug in powder form.

Pharmacokinetics in special clinical situations

Elderly patients decrease drug clearance and increase T_1/2.

Vitamin C

Suction and distribution

Absorbed from the gastrointestinal tract (mainly in the jejunum). Diseases of the gastrointestinal tract (gastric ulcer and duodenal ulcer, constipation or diarrhea, worm infestation, giardiasis), the use of fresh fruit and vegetable juices, alkaline drink reduces the absorption of Ascorbic acid in the intestine. The plasma ascorbic acid concentration is normally around 10-20 μg / ml. Time to reach C_max in blood plasma after ingestion - 4 hours

Plasma protein binding - 25%. It penetrates easily into leukocytes, platelets, and then into all tissues; the greatest concentration is reached 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 in plasma. In deficient states, 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 excretion

Metabolized predominantly in the liver to deoxyascorbic and then to oxaloacetic acid and ascorbate 2-sulfate.

Excreted by the kidneys, through the intestines, with then unchanged and in the form of metabolites.

Pharmacokinetics in special clinical situations

Smoking and the use of ethanol accelerate the destruction of ascorbic acid (turning into inactive metabolites), sharply reducing reserves in the body.

It is derived 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, the pH, dietary patterns 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 rest (80%) - by the intestines.

Rimantadine

Suction and distribution

After ingestion is almost completely absorbed in the intestine. Absorption is slow. According to the results of clinical studies, the following pharmacokinetic parameters of rimantadine were established: when using capsules C_max in blood plasma, it is achieved in 4.53 ± 2.52 h and amounts to 68.2 ± 26.6 ng / ml, when using the drug in powder form - in 5.28 ± 2.54 h and is 69 ± 19.7 ng / ml.

Plasma protein binding is about 40%. V_d - 17-25 l / kg. Concentration in the discharge from the nose is 50% higher than in plasma.

Metabolism and excretion

Metabolized in the liver.More than 90% is excreted by the kidneys within 72 hours, mainly in the form of metabolites, 15% - unchanged. According to the results of clinical studies T_1/2 rimantadine is 30.51 ± 9.83 h when using the drug in the form of capsules, 33.26 ± 12.76 h - when using the drug in the form of powder.

Pharmacokinetics in special clinical situations

In chronic renal failure T_1/2 increases by 2 times. In patients with renal insufficiency and in elderly people, rimantadine can accumulate in toxic concentrations if the dose is not adjusted in proportion to the decrease in CC. Hemodialysis has a minor effect on the clearance of rimantadine.

Rutoside

Time to reach C_max in blood plasma after oral administration - 1-9 hours

It is excreted mainly with bile and to a lesser extent by the kidneys. T_1/2 - 10-25 h.

Loratadine

Suction and distribution

Quickly and completely absorbed from the digestive tract. According to the results of clinical studies, the following pharmacokinetic parameters of loratadine were established: when using the drug in the form of capsules C_max in blood plasma, it is reached after 2.92 ± 1.31 h and amounts to 2.36 ± 1.53 ng / ml, when using the drug in powder form - after 3.28 ± 1.25 h and amounts to 1.85 ± 0.95 ng / ml.

Plasma protein binding - 97%. Does not penetrate the BBB.

Metabolism and excretion

Metabolized in the liver to form the active metabolite of descarboethoxyloratadine with the participation of cytochrome CYP3A4 isoenzymes and to a lesser extent CYP2D6.

Excreted by the kidneys and with bile.According to the results of clinical studies T_1/2 loratadine when taking capsules is equal to 12.36 ± 6.84 h, when using the drug in powder form - 11.29 ± 5.52 h.

Pharmacokinetics in special clinical situations

C_max in the elderly increases by 50%.

In patients with chronic renal failure and during hemodialysis, the pharmacokinetics are virtually unchanged.

Indications

- etiotropic treatment of influenza type A;

- symptomatic treatment of "colds" diseases, influenza and ARVI, accompanied by fever, muscle pain, headache, chills in adults.

Dosing regimen

The drug is taken orally after a meal. Capsules should be washed down with water. The powder (contents of 1 sachet) must be dissolved in 1/2 cup of warm boiled water and stirred. The resulting solution should be consumed immediately after preparation.

For adults appoint 1 capsule P blue and 1 capsule P red (single dose) or 1 sachet of powder 2-3 times / day.

The drug should be taken within 3-5 days (no more than 5 days) until the symptoms of the disease disappear. In the absence of improvement in well-being, the patient should stop using the drug and consult a doctor.

Side effect

From the nervous system: irritability, 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 mucous membranes in the mouth, lack of appetite, flatulence, diarrhea.

From the urinary system: moderate pollakiuria.

From the hemopoietic system: changes in blood counts (control required).

On the part of the endocrine system: inhibition of the function of the insular apparatus of the pancreas (hyperglycemia, glycosuria).

Allergic reactions: skin rash, itching, urticaria.

If any of the side effects indicated in the instructions are aggravated or any other side effects that are not indicated in the instructions are noted, the patient should immediately inform the doctor.

Contraindications

- Hypersensitivity to one or several components of the drug;

- erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;

- Gastrointestinal bleeding ;

- hemophilia;

- hemorrhagic diathesis;

- hypoprothrombinemia;

- portal hypertension;

- avitaminosis K;

- renal failure;

- diseases of the thyroid gland;

- acute diseases of the kidneys, liver (acute glomerulonephritis, acute pyelonephritis, acute hepatitis), or exacerbation of chronic diseases of these organs;

- chronic alcoholism;

- hypercalcemia, severe hypercalciuria;

- Nephrourolithiasis;

- sarcoidosis;

- simultaneous reception of cardiac glycosides (risk of arrhythmias);

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

- Phenylketonuria (for powder);

- pregnancy;

- breastfeeding period;

- children's and teenage age up to 18 years;

WITH caution the drug should be used and its use should be limited in case of epilepsy, cerebral atherosclerosis, diabetes mellitus, deficit cells, hemochromatosis, sideroblastic anemia, thalassemia, hyperoxaluria, urolithiasis, dehydration, electrolyte disturbances (risk of developing anemia, hyperoxaluria, urolithiasis, dehydration, electrolyte disorders (risk of developing anemia, hyperoxaluria, urolithiasis, dehydration, electrolyte disorders). calcium nephrourolithiasis (in history), hypercalciuria; as well as in elderly patients with arterial hypertension (the risk of hemorrhagic stroke increases, due to rimantadine, which is part of the drug).

Use during pregnancy and lactation

Use during pregnancy and during breastfeeding is contraindicated.

Application for violations of the liver

The use of the drug is contraindicated in portal hypertension, acute liver disease (acute g