Anvimax capsules, No. 20
Expiration Date: 05/2027
Russian Pharmacy name:
Анвимакс капсулы, №20
Etiotropic treatment of influenza type A;
symptomatic treatment of colds, flu and acute respiratory viral infections, accompanied by fever, muscle pain, headache, chills in adults.
Inside.
Adults: 1 capsule P blue and 1 capsule P red (single dose) 2-3 times a day after meals with water for 3-5 days until the symptoms of the disease disappear.
If there is no improvement in well-being, the drug should be discontinued and a doctor should be consulted.
Capsule set
1 set
Blue P capsule
active substance:
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 hard gelatin capsule: gelatin - 94.795 mg; patented blue dye (E131) or brilliant blue dye (E133) - 0.265 mg; titanium dioxide (E171) - 1.94 mg
Red P capsule
active ingredients:
ascorbic acid 300 mg
calcium gluconate monohydrate 100 mg
rimantadine hydrochloride 50 mg
Rutoside trihydrate (calculated as Rutoside) 20 mg Loratadine 3 mg
excipients: potato starch - 2.2 mg; magnesium stearate - 4.8 mg hard gelatin capsule: gelatin - 94.064 mg; iron dye yellow oxide (E172) - 0.97 mg; iron dye red oxide (E172) - 0.485 mg; crimson dye (Ponso 4R) (E124) - 0.511 mg; titanium dioxide (E171) - 0.97 mg
Hypersensitivity to one or more of the components that make up the drug;
erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
gastrointestinal bleeding;
hemophilia;
hemorrhagic diathesis;
hypoprothrombinemia;
portal hypertension;
vitamin deficiency 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 intake of cardiac glycosides (risk of arrhythmias);
lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
phenylketonuria;
pregnancy;
breastfeeding period;
children under 18 years of age.
With care: epilepsy; cerebral atherosclerosis; diabetes; deficiency of glucose-6-phosphate dehydrogenase; hemochromatosis; sideroblastic anemia; thalassemia; hyperoxaluria; kidney stone disease; dehydration; electrolyte disturbances (risk of developing hypercalcemia); diarrhea; malabsorption syndrome; calcium nephrourolithiasis (history); hypercalciuria; elderly patients with arterial hypertension (the risk of developing hemorrhagic stroke increases due to rimantadine, which is part of the drug).
pharmachologic effect
The combined drug has antiviral, interferonogenic, antipyretic, analgesic, antihistamine and angioprotective effects.
Paracetamol has analgesic and antipyretic effects.
Ascorbic acid is involved in the regulation of redox processes, contributes to normal capillary permeability, blood clotting, tissue regeneration, plays a positive role in the development of the body's immune reactions, 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 A. By blocking the M2 channels of 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 alpha and gamma interferons. In influenza caused by the B virus, rimantadine has an antitoxic effect.
Rutoside is an angioprotective agent. Reduces capillary permeability, swelling and inflammation, strengthens the vascular wall. Inhibits aggregation and increases the degree of deformation of erythrocytes.
Loratadine - a blocker of histamine H1 receptors, prevents the development of tissue edema associated with the release of histamine.
Pharmacokinetics
Paracetamol
Absorption and distribution
Absorption is high. According to the results of clinical studies, the following pharmacokinetic parameters of paracetamol were established: when using capsules, Cmax of paracetamol in blood plasma is achieved after 1.20 ± 0.72 h and is 5.01 ± 1.70 ?g / ml, when powder is used - after 0.7 ± 0.39 h and is 4.79 ± 1.81 ?g / ml.
Plasma protein binding - 15%. Penetrates the BBB.
Metabolism and excretion
It is 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 metabolic pathway are the isoenzyme CYP2E1 (mainly), CYP1A2 and CYP3A4 (minor role). When glutathione is deficient, these metabolites can cause damage and necrosis of hepatocytes. Additional metabolic pathways are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated with glucuronides or sulfates. In adults, glucuronidation predominates. Conjugated paracetamol metabolites (glucuronides,sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.
It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. According to the results of clinical studies, T1 / 2 of paracetamol is 3.04 ± 1.01 hours when taking the drug in capsules, 2.73 ± 0.76 hours when taking the drug in powder form.
Pharmacokinetics in special clinical situations
In elderly patients, the clearance of the drug decreases and T1 / 2 increases.
Vitamin C
Absorption and distribution
Absorbed from the gastrointestinal tract (mainly in the jejunum). Diseases of the gastrointestinal tract (peptic ulcer and duodenal ulcer, constipation or diarrhea, helminthic invasion, giardiasis), the use of fresh fruit and vegetable juices, alkaline drinks reduce the absorption of ascorbic acid in the intestine. The concentration of ascorbic acid in plasma is normally approximately 10-20 ?g / ml. The time to reach Cmax in blood plasma after oral administration is 4 hours.
Plasma protein binding - 25%. Easily penetrates into leukocytes, platelets, and then into 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 deficient conditions, the concentration in leukocytes decreases later and more slowly and is considered as a better criterion for assessing deficiency than plasma concentration.
Metabolism and excretion
It is metabolized mainly 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 unchanged and in the form of metabolites.
Pharmacokinetics in special clinical situations
Smoking and consumption of ethanol accelerate the breakdown of ascorbic acid (conversion into inactive metabolites), dramatically reducing body stores.
It is excreted during hemodialysis.
Calcium gluconate
Approximately 1/5 to 1/3 part 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 rest (80%) - by the intestines.
Rimantadin
Absorption and distribution
After oral administration, it 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, Cmax in blood plasma is achieved after 4.53 ± 2.52 hours and is 68.2 ± 26.6 ng / ml, when using the drug in powder form - after 5.28 ± 2.54 hours and is 69 ± 19.7 ng / ml.
Plasma protein binding is about 40%. Vd - 17-25 l / kg. Concentration in nasal discharge is 50% higher than in plasma.
Metabolism and excretion
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. According to the results of clinical studies, the T1 / 2 of rimantadine is 30.51 ± 9.83 hours when using the drug in the form of capsules, 33.26 ± 12.76 hours when using the drug in powder form.
Pharmacokinetics in special clinical situations
In chronic renal failure, T1 / 2 doubles. In persons with renal insufficiency and in the elderly, rimantadine can accumulate in toxic concentrations if the dose is not adjusted in proportion to the decrease in CC. Hemodialysis has little effect on the clearance of rimantadine.
Rutoside
The time to reach Cmax in blood plasma after oral administration is 1-9 hours.
It is excreted mainly in the bile and to a lesser extent by the kidneys. T1 / 2 - 10-25 hours
Loratadin
Absorption and distribution
It is quickly and completely absorbed from the gastrointestinal 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, Cmax in blood plasma is reached after 2.92 ± 1.31 h and is 2.36 ± 1.53 ng / ml, when using the drug in powder form - after 3.28 ± 1.25 h and is 1.85 ± 0.95 ng / ml.
Plasma protein binding - 97%. Does not penetrate the BBB.
Metabolism and excretion
It is metabolized in the liver with the formation of an active metabolite of descarboethoxyloratadine with the participation of cytochrome isoenzymes CYP3A4 and, to a lesser extent, CYP2D6.
It is excreted by the kidneys and with bile. According to the results of clinical studies, T1 / 2 of loratadine when taking capsules is 12.36 ± 6.84 hours, when using the drug in powder form - 11.29 ± 5.52 hours.
Pharmacokinetics in special clinical situations
Cmax in the elderly increases by 50%.
In patients with chronic renal failure and during hemodialysis, the pharmacokinetics practically does not change.
Side effect
From the nervous system: increased excitability, drowsiness, tremors, hyperkinesia, dizziness, headache, flushes 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 pollakiuria.
From the side of the hematopoietic system: changes in blood parameters (control is required).
Allergic reactions: angioedema, anaphylactic shock, skin rash, itching, urticaria.
Skin disorders: Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), acute generalized exanthematous pustulosis.
Others: inhibition of the function of the insular apparatus of the pancreas (hyperglycemia, glucosuria).
Post-registration experience: during the use of AnviMaxЃ, cases of angioedema, light-headedness, fever, decreased blood pressure, urticaria, pruritus, erythema, hearing impairment, sore throat were described.
If any of the side effects indicated in the instructions are aggravated or any other side effects not indicated in the instructions are noted, the patient should immediately inform the doctor about it.
Application during pregnancy and lactation
Use during pregnancy and breastfeeding is contraindicated.
Application for violations of liver function
The use of the drug is contraindicated in portal hypertension, acute liver disease (acute hepatitis), or exacerbation of chronic liver disease.
Application for impaired renal function
The use of the drug is contraindicated in renal failure, acute kidney disease (acute glomerulonephritis, acute pyelonephritis), or exacerbation of chronic kidney disease, nephrourolithiasis.
The drug should be used with caution in case of calcium nephrourolithiasis (in history).
Application in children
The use of the drug is contraindicated in children and adolescents under 18 years of age.
Use in elderly patients
The drug should be used with caution in elderly patients with arterial hypertension (the risk of hemorrhagic stroke increases due to rimantadine, which is part of the drug).
special instructions
Duration of use - no more than 5 days.
The drug should not be used in the presence of metastatic tumors.
Patients who abuse alcohol 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 mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Overdose
—имптомы: в течение первых 24 ч после приема - бледность кожных покровов, тошнота, диаре¤, рвота, боль в эпигастральной области; нарушение метаболизма глюкозы, метаболический ацидоз, тахикарди¤, аритми¤, головна¤ боль, обострение сопутствующих хронических заболеваний. —имптомы нарушени¤ функции печени могут по¤витьс¤ через 12-48 ч после передозировки. ѕри т¤желой передозировке - печеночна¤ недостаточность с прогрессирующей энцефалопатией, кома; остра¤ почечна¤ недостаточность с тубул¤рным некрозом (в т.ч. при отсутствии т¤желого поражени¤ печени).
ѕорог передозировки может быть снижен у пациентов пожилого возраста, у пациентов, принимающих определенные препараты (например, индукторы микросомальных ферментов печени), алкоголь или страдающих истощением.
Ћечение: введение донаторов SH-групп и предшественников синтеза глутатиона-метионина в течение 8-9 ч после передозировки и ацетилцистеина - в течение 8 ч. ѕромывание желудка, симптоматическа¤ терапи¤. Ќеобходимость в проведении дополнительных терапевтических меропри¤тий (дальнейшее введение метионина, ацетилцистеина) определ¤етс¤ в зависимости от концентрации парацетамола в крови, а также от времени, прошедшего после его приема.
Ћекарственное взаимодействие
ѕарацетамол снижает эффективность урикозурических лекарственных средств.
—опутствующее применение парацетамола в высоких дозах повышает эффект антикоагул¤нтных лекарственных средств.
»ндукторы микросомального окислени¤ в печени (фенитоин, барбитураты, рифампицин, фенилбутазон, трициклические антидепрессанты), этанол и гепатотоксичные лекарственные средства увеличивают продукцию гидроксилированных активных метаболитов, что обусловливает возможность развити¤ т¤желых интоксикаций даже при небольшой передозировке.
ѕри одновременном применении с метоклопрамидом возможно увеличение скорости всасывани¤ парацетамола.
?лительное использование барбитуратов снижает эффективность парацетамола.
»нгибиторы микросомального окислени¤ снижают риск гепатотоксического действи¤.
–имантадин усиливает возбуждающий эффект кофеина.
?иметидин снижает клиренс римантадина на 18%.
јскорбинова¤ кислота повышает концентрацию в крови бензилпенициллина.
”лучшает всасывание в кишечнике препаратов железа (переводит трехвалентное железо в двухвалентное); может повышать выведение железа при одновременном применении с дефероксамином.
”величивает риск развити¤ кристаллурии при лечении салицилатами и сульфаниламидами короткого действи¤, замедл¤ет выведение почками кислот, увеличивает выведение лекарственных средств, имеющих щелочную реакцию (в т.ч. алкалоидов).
—нижает концентрацию в крови пероральных контрацептивов.
ѕовышает общий клиренс этанола, который в свою очередь снижает концентрацию аскорбиновой кислоты в организме.
ѕри одновременном применении уменьшает хронотропное действие изопреналина.
Ѕарбитураты и примидон повышают выведение аскорбиновой кислоты с мочой.
”меньшает терапевтическое действие антипсихотических лекарственных средств (нейролептиков) - производных фенотиазина.
Reduces tubular reabsorption of amphetamine and tricyclic antidepressants.
Loratadin
Inhibitors of CYP3A4 and CYP2D6 increase the concentration of loratadine in the blood.