Antigrippin maximum
Antigrippin-maximum: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Antigrippin-maximum
ATX code: J05AX
Active ingredient: paracetamol (Paracetamol), rimantadine hydrochloride (Rimantadine hydrochloride), ascorbic acid (Ascorbic acid), loratadine (Loratadine), rutoside (Rutoside), calcium gluconate monohydrate (Calcium gluconate monohydrate)
Manufacturer: JSC "Pharmproekt" (Russia), CJSC "ZiO-Zdorovie" (Russia), LLC "NPO FarmVILAR" (Russia)
Description and photo update: 2019-10-07
Antigrippin-maximum is a remedy for etiotropic and symptomatic therapy of respiratory viral diseases.
Release form and composition
Dosage forms:
- capsules of two types: capsules P - hard gelatinous, size No. 0, blue; content - a mixture of granules (of different sizes, irregular shape, may contain lumps) and / or powder of white or white with a pinkish or creamy shade; capsules R - hard gelatinous, size No. 0, red; content - a mixture of granules (of different sizes, irregular shapes, may contain lumps) and / or powder of white and yellow with a greenish tinge (in a cardboard box there are 2 separate blister packs, one contains 10 P capsules, the other contains 10 P capsules);
- powder for preparation of solution for oral administration (raspberry, lemon, lemon with honey or blackcurrant): a mixture of almost white granules and greenish-yellow powder, with a characteristic odor. Ready solution: slightly cloudy, colorless or with a yellowish tinge, has a characteristic odor (raspberry, lemon, lemon with honey or black currant, respectively), may contain undissolved yellow particles (5 g each in sachets made of a combined material, in a cardboard box 3, 6, 8, 12 or 24 sachets).
Each pack also contains instructions for the use of Antigrippin-maximum.
Composition of 1 capsule P:
- active substance: paracetamol - 360 mg;
- auxiliary components: colloidal silicon dioxide, pregelatinized starch, magnesium stearate, lactose monohydrate;
- capsule shell: gelatin, titanium dioxide (E171), patented blue dye (E131).
Composition of 1 capsule R:
- active substances: ascorbic acid - 300 mg, calcium gluconate monohydrate - 100 mg, rimantadine hydrochloride - 50 mg, rutoside (in the form of trihydrate) - 20 mg, loratadine - 3 mg;
- auxiliary components: magnesium stearate, potato starch;
- capsule shell: gelatin, titanium dioxide (E171), iron dye red oxide (E172), iron dye yellow oxide (E172), crimson dye (Ponso 4R) (E124).
Powder composition for oral solution in 1 sachet:
- active substances: paracetamol - 360 mg, ascorbic acid - 300 mg, calcium gluconate monohydrate - 100 mg, rimantadine hydrochloride - 50 mg, rutoside - 20 mg, loratadine - 3 mg;
- auxiliary components: lactose, colloidal silicon dioxide, hypromellose, aspartame, food flavoring (raspberry, lemon, lemon-honey or blackcurrant).
Pharmacological properties
Pharmacodynamics
Antigrippin-maximum is a combined drug that has antiviral, anti-inflammatory, interferonogenic, antipyretic, analgesic, antiallergic and angioprotective effect.
Properties of the active components of the drug:
- paracetamol is an analgesic-antipyretic with analgesic, anti-inflammatory and antipyretic effects;
- ascorbic acid - vitamin C, involved in the regulation of redox processes, normalizing blood clotting, capillary permeability and tissue regeneration, activating immunity;
- calcium gluconate monohydrate is an agent that prevents the development of increased permeability and fragility of blood vessels, causing hemorrhagic processes in acute respiratory viral infections (ARVI) and influenza. Restores capillary circulation. Has antiallergic activity (the mechanism of its action has not been established);
- rimantadine hydrochloride is an antiviral agent effective against influenza A. By blocking the M 2 channels of influenza A virus, it disrupts its ability to enter cells and release ribonucleoprotein, thereby inhibiting the most important stage of viral replication. Promotes the production of interferons alpha and gamma. Has antitoxic effect in influenza caused by the B virus;
- rutoside is an angioprotector that strengthens the vascular wall, reduces increased capillary permeability by reducing swelling and inflammation. Increases the degree of erythrocyte deformation. It has antiplatelet properties;
- loratadine is a blocker of H 1 -histamine receptors, which prevents the development of tissue edema caused by the release of histamine.
Pharmacokinetics
Paracetamol
After oral administration in the gastrointestinal tract (GIT) is absorbed to a high degree. According to clinical studies, when using Antigrippin-maximum in capsules, C max (maximum plasma concentration) of paracetamol is 5.01 ± 1.7 μg / ml and is achieved within 1.2 ± 0.72 hours.
Plasma proteins bind 15% of the dose. Penetrates the blood-brain barrier.
It is metabolized in the liver mainly by conjugation with sulfates and glucuronides, as well as by oxidation by liver microsomal enzymes, as a result of which toxic intermediate metabolites are formed - they are subsequently conjugated first with glutathione, then with mercaptopuric acid and cysteine. In this metabolic pathway, the cytochrome P 450 isoenzyme CYP2E1 is mainly involved, to a lesser extent - isoenzymes CYP3A4 and CYP1A2. In patients with glutathione deficiency, toxic metabolites can cause damage and necrosis of hepatocytes.
Additional metabolic pathways are methoxylation to 3-methoxyparacetamol and hydroxylation to 3-hydroxyparacetamol. These metabolites are subsequently conjugated to sulfates or glucuronides. In adult patients, glucuronidation predominates.
Conjugated paracetamol metabolites (sulfates, conjugates with glutathione, and glucuronides) have low pharmacological and toxic activity.
Paracetamol is excreted mainly by the kidneys in the form of metabolites (mainly conjugates). About 3% of the dose is excreted unchanged.
T ½ (half-life) is 3.04 ± 1.01 hours. In elderly patients, paracetamol clearance decreases and T ½ increases.
Vitamin C
In the gastrointestinal tract, ascorbic acid is absorbed mainly in the jejunum. About 25% of the dose taken is bound to plasma proteins.
The absorption of the drug in the intestine decreases with the use of alkaline drinks, fresh vegetable and fruit juices, as well as with diseases of the gastrointestinal tract, such as diarrhea, constipation, peptic ulcer of the duodenum and stomach, giardiasis, helminthic invasion.
Plasma concentration is normally about 10–20 µg / ml. C max is noted after about 4 hours. Vitamin C easily penetrates into platelets and leukocytes, then into all body tissues. The highest concentration reaches in the liver, leukocytes, glandular organs and the lens of the eye. In platelets and leukocytes, the concentration of ascorbic acid is higher than in plasma and erythrocytes. Penetrates the placental barrier.
In patients with deficient conditions, the level of ascorbic acid in leukocytes decreases later and more slowly. This criterion for assessing deficiency is considered to be superior compared to plasma concentration.
Vitamin C is biotransformed mainly in the liver into deoxyascorbic acid, then into oxaloacetic acid and ascorbate-2-sulfate. It is excreted in the form of metabolites and unchanged through the intestines, kidneys and sweat.
Alcohol consumption and smoking contribute to the rapid destruction of ascorbic acid, due to which its reserves in the body are sharply reduced.
The drug is excreted during hemodialysis.
Calcium gluconate
After oral administration, approximately ⅕ – of the calcium gluconate is absorbed in the small intestine. This process depends on the pH level, diet, the presence of ergocalciferol, and the presence of factors that can bind calcium ions.
Calcium ions are absorbed more intensively with a deficiency of this trace element in the body and adherence to a diet with reduced calcium intake.
It is excreted mainly through the intestines (80%), to a lesser extent (20%) - by the kidneys.
Rimantadin
When administered orally, the drug is slowly but completely absorbed in the intestine. According to the data of clinical studies, when using the drug in capsules, C max is 68.2 ± 26.6 ng / ml and is noted after 4.53 ± 2.52 hours.
About 40% of the dose is bound to plasma proteins. The volume of distribution (V d) is 17–25 l / kg. The concentration of the drug in the nasal secretion is 50% higher than in the plasma.
Rimantadine is metabolized in the liver. T ½ is 30.51 ± 9.83 hours.
It is excreted mainly (more than 90%) by the kidneys within 72 hours, mainly in the form of metabolites, about 15% of the dose is excreted unchanged.
In patients with chronic renal failure, T ½ increases by 2 times.
In the elderly and patients with renal failure, rimantadine can accumulate in toxic concentrations if the dose is not adjusted in accordance with the level of creatinine clearance (CC).
In patients receiving hemodialysis, there were no significant changes in rimantadine clearance.
Rutoside
After oral administration, C max is observed in the period from 1 to 9 hours.
Rutozid is excreted mainly in the bile, to a lesser extent in the urine.
T ½ varies in the range from 10 to 25 hours.
Loratadin
When taken orally from the gastrointestinal tract, loratadine is absorbed quickly and completely. According to the results of clinical studies, when using the drug in capsules, C max is 2.36 ± 1.53 ng / ml and is noted after 2.92 ± 1.31 hours.
About 97% of the dose binds to plasma proteins.
Loratadine is metabolized in the liver with the participation of predominantly cytochrome CYP3A4 isoenzymes, to a lesser extent - CYP2D6. The main active metabolite is descarboethoxyloratadine.
Loratadine does not cross the blood-brain barrier. It is excreted by the kidneys and through the intestines (with bile). T ½ is 12.36 ± 6.84 hours.
In elderly patients, C max increases by about 50%.
In chronic renal failure and hemodialysis, the pharmacokinetic characteristics of loratadine practically do not change.
Indications for use
- symptomatic therapy of ARVI, flu and other colds accompanied by fever, chills, headache and muscle pain;
- etiotropic treatment of influenza type A.
Contraindications
Absolute:
- vitamin K deficiency;
- hemorrhagic diathesis;
- hemophilia;
- severe hypercalciuria;
- hypercalcemia;
- nephrourolithiasis;
- renal failure;
- acute and exacerbation of chronic kidney disease (including acute pyelonephritis and acute glomerulonephritis);
- chronic alcoholism;
- acute and exacerbations of chronic liver diseases (including acute hepatitis);
- portal hypertension;
- hypoprothrombinemia;
- diseases of the thyroid gland;
- gastrointestinal bleeding;
- erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- sarcoidosis;
- age up to 12 years - for powder, up to 18 years - for capsules;
- period of pregnancy and lactation;
- simultaneous use of cardiac glycosides;
- hypersensitivity to drug components.
Relative (Antigrippin-maximum should be used with caution):
- deficiency of glucose-6-phosphate dehydrogenase, malabsorption syndrome;
- dehydration, electrolyte disturbances;
- hemochromatosis;
- hyperoxaluria;
- mild to moderate hypercalciuria;
- thalassemia;
- sideroblastic anemia;
- a history of calcium nephrourolithiasis;
- diarrhea;
- cerebral atherosclerosis;
- epilepsy;
- diabetes;
- arterial hypertension in elderly patients.
Antigrippin-maximum, instructions for use: method and dosage
The drug in both dosage forms is taken orally.
In capsules Antigrippin-maximum is prescribed for adults 1 capsule P (blue) and 1 capsule P (red) at a time 2 or 3 times a day. The duration of treatment is determined by the moment the symptoms of the disease disappear. The capsules should be swallowed whole and washed down with plenty of water.
In powder form, Antigrippin-maximum is prescribed for adults and adolescents from 12 years old, 1 sachet 2 or 3 times a day. Before taking the contents of 1 sachet dissolve in 1 glass of hot boiled water. The drug should be taken hot, after stirring well. The duration of treatment is determined by the moment the symptoms of the disease disappear.
Usually, the course of treatment is 3-5 days. If within 3 days there is no improvement in well-being, you need to stop taking the drug and consult your doctor. The maximum duration of use of Antigrippin-maximum is 5 days.
Side effects
- from the digestive system: with prolonged use of the drug (more than 7 days) - dry mouth, flatulence, dyspepsia, diarrhea, anorexia, damage to the mucous membrane of the stomach and duodenum;
- from the urinary system: moderate pollakiuria;
- on the part of the hematopoietic system: when taking Antigrippin, a maximum of more than 7 days - thrombocytopenia, agranulocytosis, anemia, neutropenia, leukopenia;
- from the side of the central nervous system: rarely - hyperkinesia, headache, flushing of the face, drowsiness, increased excitability, dizziness, tremor;
- allergic reactions: rarely - itching, skin rash, urticaria;
- others: inhibition of the function of the insular apparatus of the pancreas (which is manifested by glucosuria, hyperglycemia).
Overdose
On the first day after taking an excessive dose of Antigrippin-maximum, the following symptoms can be observed: pallor of the skin, pain in the epigastric region, vomiting, diarrhea, nausea, headache, arrhythmia, tachycardia, impaired glucose metabolism, metabolic acidosis, exacerbation of concomitant chronic diseases. 12–48 hours after an overdose, signs of impaired hepatic function may appear. With severe intoxication, the development of hepatic failure with progressive encephalopathy is possible. There is a risk of acute renal failure with tubular necrosis (including in patients without severe liver damage), coma.
First of all, it is recommended to do a gastric lavage and consult a doctor.
Within 8 hours after an overdose, the administration of acetylcysteine is recommended, within 8-9 hours - the introduction of SH-group donors and precursors of glutathione (methionine) synthesis. Treatment is symptomatic. The need for additional therapeutic measures is determined individually, depending on the concentration of paracetamol in the blood and the time elapsed since its intake.
special instructions
Antigrippin-maximum has no carcinogenic effect. However, the drug should not be administered to patients with metastatic tumors.
Alcohol abusers are advised to consult a doctor before taking Antigrippin-Maximum, since paracetamol has a potential hepatotoxic effect.
With prolonged use, the drug can exacerbate existing chronic diseases.
Influence on the ability to drive vehicles and complex mechanisms
Antigrippin-maximum in some patients causes drowsiness and dizziness, therefore, during the period of taking it, it is recommended to be careful when driving a car and performing work with potentially dangerous consequences.
Application during pregnancy and lactation
Antigrippin maximum during pregnancy and lactation is contraindicated.
Pediatric use
In powder form, the drug is contraindicated in children under 12 years of age. Antigrippin-maximum capsules are not prescribed to patients under 18 years of age.
With impaired renal function
Renal failure, acute diseases and exacerbation of chronic kidney disease (including acute glomerulonephritis) are contraindications to the appointment of Antigrippin-maximum.
For violations of liver function
Antigrippin-maximum is contraindicated in patients with portal hypertension, acute diseases and exacerbation of chronic liver diseases (including acute hepatitis).
Use in the elderly
Antigrippin-maximum should be used with caution in elderly patients with portal hypertension, since they have rimantadine, which is part of the drug, increases the risk of developing hemorrhagic stroke.
Drug interactions
Possible interactions of paracetamol:
- uricosuric drugs: their effectiveness decreases;
- inhibitors of microsomal oxidation: the risk of developing the hepatotoxic effect of paracetamol decreases;
- anticoagulants: while taking high doses of paracetamol, their effect is enhanced;
- metoclopramide: the rate of absorption of paracetamol may increase;
- hepatotoxic agents, ethanol, inducers of microsomal oxidation in the liver (barbiturates, phenylbutazone, rifampicin, phenytoin, tricyclic antidepressants): the production of hydroxylated active metabolites of paracetamol increases, which increases the risk of developing severe intoxication even with a small overdose;
- barbiturates (with prolonged use): the effectiveness of paracetamol decreases.
Possible interactions of ascorbic acid:
- benzylpenicillin: its plasma concentration increases;
- oral contraceptives: their content in the blood decreases;
- primidone, barbiturates: increased excretion of ascorbic acid in the urine;
- isoprenaline: its chronotropic effect decreases;
- amphetamine, tricyclic antidepressants: their tubular reabsorption decreases;
- drugs with an alkaline reaction (including alkaloids): their excretion increases;
- short-acting sulfonamides, salicylates: the risk of developing crystalluria increases;
- acids: their excretion by the kidneys decreases;
- antipsychotic drugs (neuroleptics), phenothiazine derivatives: their therapeutic effect decreases;
- iron supplements: their absorption in the intestine improves; with the combined use of deferoxamine, it is possible to increase the excretion of iron;
- ethanol: its total clearance increases, and the concentration of ascorbic acid in the body decreases.
Possible interactions of rimantadine:
- cimetidine: the clearance of rimantadine decreases by 18%;
- caffeine: its stimulating effect is enhanced.
Possible interactions of loratadine: its plasma concentration increases with the simultaneous use of CYP3A4 and CYP2D6 inhibitors.
If necessary, the simultaneous use of Antigrippin-maximum and any other drug, you should consult your doctor.
Analogs
Antigrippin-maximum analogs are: AnviMax, Angrippin Maxim, Antigrippin-Anvi, Antigrippin-ARVI, Kofanol, Kaffetin Cold, Kaffetin KOLDmax, Padeviks, etc.
Terms and conditions of storage
Keep out of the reach of children, protected from light and in a dry place at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Antigrippin-maximum
According to reviews, Antigrippin-maximum is a drug that quickly and effectively helps with the first symptoms of colds and flu: it reduces fever, eliminates headaches and weakness, and reduces the symptoms of a cold.
Separately, the pleasant taste of the solution prepared from the powder is noted.
The price of Antigrippin-maximum in pharmacies
The approximate price of Antigrippin-maximum in the form of a powder for the preparation of a solution for oral administration, depending on the number of sachets in the package: 3 pcs. - 130-150 rubles., 6 pcs. - 195-235 rubles., 12 pcs. - 360-390 rubles., 24 pcs. - 600-630 rubles. The cost of capsules (20 pieces per pack) is about 213 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!