Instructions for Gropivirine syrup 50 mg/ml bottle 100 ml
Composition
active ingredient: inosine pranobex;
1 ml of syrup contains 50 mg of inosine pranobex;
excipients: sucrose; sodium citrate monobasic anhydrous; methyl parahydroxybenzoate (E 218); propyl parahydroxybenzoate (E 216); sodium hydroxide; cherry flavoring; purified water.
Dosage form
Syrup.
Main physicochemical properties: clear liquid from colorless to light brown with a cherry odor.
Pharmacotherapeutic group
Antiviral drugs for systemic use.
ATX code J05A X05.
Pharmacological properties
Pharmacodynamics.
Gropivirin® is an antiviral agent with immunomodulatory properties. The drug normalizes (to an individual norm) the deficiency or dysfunction of cellular immunity, inducing the maturation and differentiation of T-lymphocytes and T1-helpers, potentiating the induction of a lymphoproliferative response in mitogenic or antigen-active cells.
Inosine pranobex simulates the cytotoxicity of T-lymphocytes and natural killer cells, the function of CD8 and CD4, and also increases the amount of immunoglobulin G and additional surface markers of complement. Inosine pranobex enhances the synthesis of interleukin-1 (IL-1) and the synthesis of interleukin-2 (IL-2), regulating the expression of IL-2 receptors. Inosine pranobex significantly increases the secretion of endogenous gamma interferon and reduces the production of interleukin-4 in the body. Inosine pranobex enhances the action of neutrophil granulocytes, chemotaxis and phagocytosis of monocytes and macrophages. Inosine pranobex inhibits virus synthesis by incorporating inosine-orotic acid into the polyribosomes of the virus-infected cell, inhibiting the attachment of adenylic acid to viral mRNA, and molecular reorganization of lymphocyte intramembrane plasma particles, which almost triples its density.
Pharmacokinetics.
Absorption: After oral administration of inosine pranobex, it is rapidly and completely absorbed (≥ 90%) from the gastrointestinal tract into the blood.
Distribution. When the drug and its components were administered to animals, radiolabeled material was detected in the following organs (in order of decreasing specific activity): kidneys, lungs, liver, heart, spleen, testes, pancreas, brain, and skeletal muscles.
Metabolism: Oral administration of 1 g of radiolabeled inosine pranobex in humans resulted in plasma levels of 1-dimethylamino-2-propanol and 4-acetylamidobenzoic acid of 3.7 μg/mL (2 h) and 9.4 μg/mL (1 h), respectively. In known clinical dose tolerance studies, the peak post-dose increase in uric acid concentration, an indicator of inosine metabolism, has been found to be non-linear and may vary by 10% over 1-3 hours.
Elimination. The daily urinary excretion of 4-acetylamidobenzoic acid and its main metabolite at steady state with daily administration of 4 g of the drug was approximately 85% of the administered dose. 95% of the radioactive 1-dimethylamino-2-propanol in the urine was detected as unchanged 1-dimethylamino-2-propanol and its metabolite (N-oxide). The half-life is 3.5 hours for 1-dimethylamino-2-propanol and 50 minutes for 4-acetylamidobenzoic acid. The main metabolites of inosine pranobex in humans are the N-oxide of 1-dimethylamino-2-propanol and the ortho-acylglucuronide of 4-acetylamidobenzoic acid. Since inosine is metabolized by purine degradation to uric acid, experimental studies with radiolabeled inosine pranobex in humans are uninformative. In animals, up to 70% of administered inosine pranobex can be excreted in the urine as uric acid after oral administration of the tablet form, with the remainder as the common metabolites xanthine and hypoxanthine.
Bioavailability. Steady-state urinary recovery of 4-acetamidobenzoic acid and its metabolite was > 90% of the expected solution values. Recovery of 1-dimethylamino-2-propanol and its metabolite was > 76%. Plasma AUC values for 1-dimethylamino-2-propanol were ≥ 88% and for 4-acetamidobenzoic acid were ≥ 77%.
Indication
Viral respiratory infections;
viral infections caused by herpes simplex virus types 1 and 2, varicella virus, cytomegalovirus, Epstein-Barr virus, measles virus, mumps virus, including in patients with immunodeficiency states;
papillomavirus infections of the skin and mucous membranes: genital warts, papillomavirus infection of the vulva, vagina and cervix (as part of complex therapy);
acute viral encephalitis (as part of complex therapy);
viral hepatitis (as part of complex therapy);
subacute sclerosing panencephalitis (as part of complex therapy).
Contraindication
Hypersensitivity to the active substance or to any of the excipients of the drug, exacerbation of gout, hyperuricemia.
Interaction with other medicinal products and other types of interactions
The drug should not be taken simultaneously with immunosuppressants. Caution should be exercised when prescribing the drug with xanthine oxidase inhibitors or agents that promote the excretion of uric acid, including diuretics, thiazide diuretics (such as hydrochlorothiazide, chlorthalidone, indapamide) or loop diuretics (such as furosemide, torasemide, ethacrynic acid).
Inosine pranobex should not be used during immunosuppressant therapy, as the simultaneous use of immunosuppressants may affect its expected therapeutic effect due to the peculiarities of pharmacokinetic mechanisms (use is possible only after completion of therapy).
When used simultaneously with azidothymidine, nucleotide formation is increased due to increased bioavailability of azidothymidine in blood plasma and increased intracellular phosphorylation in human blood monocytes.
Application features
During treatment with Gropivirine®, a temporary increase in serum and urine uric acid levels is possible, especially in men and elderly patients, but usually these values remain within the normal range (up to 8 mg/dL μmol/L, respectively).
The cause of the increase in uric acid levels is the catabolic metabolism of inosine in humans. This is not due to a fundamental change in enzyme function or renal clearance function caused by the drug. Therefore, the drug should be used with special caution in patients with gout, hyperuricemia, urolithiasis, and reduced renal function. During treatment, it is necessary to monitor the level of uric acid in these patients.
Some patients may experience acute hypersensitivity reactions (angioedema, anaphylactic shock, urticaria). In such cases, therapy with Gropivirine® should be discontinued.
With prolonged use of the drug, there is a risk of developing nephrolithiasis.
Excipients of the drug.
The drug Gropivirin®, syrup, contains methyl parahydroxybenzoate and propyl parahydroxybenzoate, which may cause allergic reactions (possibly delayed).
Gropivirine® syrup contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
Use during pregnancy or breastfeeding
Controlled studies of fetal health and fertility in humans are lacking. It is not known whether inosine pranobex is excreted in human milk. The drug should not be used during pregnancy or breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
The effect of the drug on the reaction rate when driving vehicles or operating other mechanisms has not been studied. However, patients should be aware that the drug may cause dizziness or other adverse reactions from the nervous system (see section "Adverse reactions").
Method of administration and doses
The drug should be administered orally.
The daily dose depends on body weight, the course and severity of the disease, and the patient's condition.
The daily dose should be divided evenly into doses throughout the day.
Adults, including elderly patients: the recommended daily dose is 50 mg/kg body weight (1 ml/kg), usually 3 g/day (20 ml of syrup 3-4 times a day). The maximum daily dose for adults is 80 ml of syrup (4 g of inosine pranobex).
Children over 1 year of age: the recommended daily dose is 50 mg/kg body weight (1 ml/kg), evenly divided into 3-4 doses according to the table below:
Body weight, kg
Dosage regimen, ml
10-14 kg
3 × 5 ml
15-20 kg
3 × 5-7.5 ml
21-30 kg
3 × 7.5-10 ml
31-40 kg
3 × 10-15 ml
41-50 kg
3 × 15-17.5 ml
*To measure the dose, use the dosing device with a measuring scale, which is included in the package.
Duration of treatment.
Acute diseases. In diseases with a short course, the course of treatment is 5-14 days. After the symptoms of the disease have subsided, treatment should be continued for another 1-2 days or longer, depending on the course of the disease and the patient's condition.
Viral diseases with a long course. Treatment should be continued for 1-2 weeks after the symptoms of the disease have subsided or longer, depending on the course of the disease and the patient's condition.
Recurrent diseases. At the initial stage of treatment, the same recommendations are followed as in the case of acute diseases. During maintenance therapy, the dose can be reduced to 500-1000 mg/day. At the first signs of relapse, it is necessary to resume taking the daily dose recommended in the case of acute diseases, and this dose should be continued for 1-2 days after the symptoms disappear. The course of treatment can be repeated several times if necessary, depending on the patient's condition, on the recommendation of a doctor.
Chronic diseases. The drug should be administered in a daily dose of 50 mg/kg of body weight according to the following regimens:
asymptomatic diseases – take for 30 days with a break of 60 days;
diseases with moderately severe symptoms – take for 60 days with a break of 30 days;
The course of treatment should be repeated as many times as necessary, with constant monitoring of the patient's condition and indications for extending therapy.
For infections caused by human papillomavirus (external genital warts (condyloma acuminatum) or papillomavirus infection of the cervical canal), use 3 g/day for 14-28 days as monotherapy or as an adjunct to local therapy or surgical treatment according to the following regimens:
for the treatment of low-risk patients (patients with normal immunity or patients with a low risk of relapse), the drug should be used for 14-28 days until maximum eradication of the virus is achieved, then a break of 2 months should be taken. The course of treatment can be repeated using the same dose, while it is necessary to constantly monitor the patient's condition and indications for continued therapy;
For the treatment of high-risk patients* (immunocompromised patients or those at high risk of relapse), the drug should be administered 5 days a week for 1-2 weeks per month for 3 months. The course of treatment should be repeated as many times as necessary, with constant monitoring of the patient's condition and indications for continued therapy.
*High-risk factors in patients with recurrent or recurrent cervical dysplasia or genital HPV infection, as with other similar conditions, include:
immunodeficiency caused by:
- a history of chronic or recurrent infections or sexually transmitted diseases;
- chemotherapy;
- chronic alcoholism;
long-term use of oral contraceptives (from 2 years);
folate level in erythrocytes less than 660 nmol/l;
multiple sexual partners or changing permanent sexual partner;
frequent vaginal intercourse (≥ 2-6 times per week) or anal sex;
atopy (hereditary predisposition to hypersensitivity);
poorly controlled diabetes;
smoking;
genital papillomavirus infection that lasts more than 2 years or has 3 or more recurrences in history;
negative history of skin warts in childhood.
In subacute sclerosing panencephalitis, the daily dose is 100 mg/kg of body weight, the maximum dose is 3-4 g/day, while it is necessary to constantly monitor the patient's condition and indications for continued therapy.
Children
The drug Gropivirin®, syrup, is used in children aged 1 year and older.
Overdose
No cases of overdose have been reported. Overdose may cause increased levels of uric acid in the blood serum and urine. Treatment is symptomatic.
Side effects
The only persistent adverse reaction during treatment with inosine pranobex in adults and children is a temporary increase in uric acid levels in the blood serum and urine, which return to their original normal values a few days after the end of treatment.
The frequency of adverse reactions is defined as follows: common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); very rare (≥1/10000); frequency unknown (cannot be estimated due to lack of data).
Very common: Laboratory tests: increased blood uric acid, increased urine uric acid.
Common: Laboratory tests: increased blood urea nitrogen, increased transaminases, increased blood alkaline phosphatase.
General disorders: increased fatigue, malaise.
Skin and subcutaneous tissue disorders: rash, itching.
On the part of the digestive tract: vomiting, nausea, feeling of discomfort in the epigastric region.
From the nervous system: headache, dizziness.
Musculoskeletal and musculoskeletal disorders: arthralgia.
Uncommon: Gastrointestinal disorders: diarrhea, constipation.
From the nervous system: drowsiness, sleep disorders.
Mental disorders: nervousness.
From the urinary system: polyuria.
During post-marketing surveillance, the following adverse reactions were reported, the frequency of which cannot be determined from the available data:
from the digestive tract: abdominal pain (upper part);
from the immune system: anaphylactic reactions, anaphylactic shock, angioedema, hypersensitivity, urticaria;
from the nervous system: dizziness;
Skin and subcutaneous tissue disorders: erythema.
Expiration date
2 years.
The shelf life after first opening is 6 months.
Do not use the drug after the expiration date indicated on the package.
Packaging
100 ml in a bottle. 1 bottle with a dosing syringe in a pack.
Vacation category
According to the recipe.
Storage conditions
According to the recipe.
Producer
JSC "Farmak".
Address
Ukraine, 04080, Kyiv, Kyrylivska St., 74.
