Instructions Groprinosin tablets 500 mg blister No. 20
Composition
active ingredient: inosine pranobex;
1 tablet contains 500 mg of inosine pranobex;
Excipients: potato starch, povidone, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: oval, biconvex tablets, white to cream in color, with a score line on one side, 17 mm long, 7 mm wide.
Pharmacotherapeutic group
Antiviral drugs for systemic use.
ATX code J05A X05.
Pharmacological properties
Pharmacodynamics
Groprinosin 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 models the cytotoxicity of T-lymphocytes and natural killers, the function of T8-suppressors and T4-helpers, and also increases the amount of immunoglobulin G and additional surface markers of complement. The drug 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 and inhibits the addition of adenylic acid to viral mRNA.
Pharmacokinetics
Absorption: When inosine pranobex is administered orally, it is rapidly and completely absorbed (≥ 90%) in the gastrointestinal tract and enters the bloodstream.
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): kidney, lung, liver, heart, spleen, testes, pancreas, brain, and skeletal muscle.
Metabolism: After oral administration of 1 g of radiolabeled inosine pranobex in humans, the following plasma levels were found for 1-dimethylamino-2-propanol and 4-acetamidobenzoic acid, respectively: 3.7 μg/mL (2 hours) and 9.4 μg/mL (1 hour). In human tolerability studies, the maximum increase in uric acid levels after dosing, as a measure of inosine in the preparation, is not linear and can vary within 10% over 1-3 hours.
Elimination: The daily urinary excretion of 4-acetamidobenzoic acid and its major metabolite at steady state at a dose of 4 g/day was approximately 85% of the administered dose. 95% of the radioactivity from 1-dimethylamino-2-propanol in the urine was recovered as unchanged 1-dimethylamino-2-propanol and its metabolite (N-oxide). The elimination half-life is 3.5 hours for 1-dimethylamino-2-propanol and 50 minutes for 4-acetamidobenzoic acid. The major metabolites of inosine pranobex in humans are the N-oxide of 1-dimethylamino-2-propanol and the o-acylglucuronide of 4-acetamidobenzoic acid. Since the inosine molecule is metabolized by purine biodegradation to uric acid, experiments 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 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; viral respiratory infections; 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, gout, hyperuricemia.
Interaction with other medicinal products and other types of interactions
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
Since during treatment with Groprinosin®, a temporary increase in serum uric acid levels is possible, especially in men and elderly patients, the drug is contraindicated for use in patients suffering from gout, hyperuricemia, and should also be used with caution in patients with urolithiasis and reduced kidney function. When using the drug for more than 3 months, it is advisable to check laboratory indicators of liver and kidney function (transaminases, creatinine), serum uric acid levels, and perform a blood test every month.
Some patients may experience acute hypersensitivity reactions (angioedema, anaphylactic shock, urticaria). In such cases, therapy with Groprinosin® should be discontinued.
With prolonged use of the drug, there is a risk of developing nephrolithiasis.
Ability to influence reaction speed when driving vehicles or other mechanisms
The effect of the drug on the reaction rate when driving vehicles or working with other mechanisms has not been studied. However, patients should be aware that the drug Groprinosin® may cause dizziness or other adverse reactions from the nervous system.
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.
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.
Adults and children over 12 years of age: 50 mg/kg body weight (usually 6-8 tablets divided into 3-4 doses), maximum daily dose – 4 g.
Children aged 1 to 12 years – 50 mg/kg of body weight (usually 1 tablet per 10 kg of body weight for a child weighing 10-20 kg, with a body weight of more than 20 kg, prescribe the dose as for adults) in 3-4 doses per day, the maximum daily dose is 4 g. To facilitate administration, the tablet can be crushed and/or dissolved in a small amount of water immediately before use.
Duration of treatment.
Acute diseases: for diseases with a short course, the course of treatment is from 5 to 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 as for acute diseases apply. During maintenance therapy, the dose can be reduced to 500-1000 mg (1-2 tablets) per day. At the first signs of relapse, it is necessary to resume taking the daily dose recommended for acute diseases and continue taking this dose 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;
Diseases with severe symptoms – take for 90 days with a 30-day break.
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 (2 tablets 3 times a 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 patients from the high-risk group* (patients with immunodeficiency or with a high risk of relapse), the drug should be used 5 days a week, consecutively 1-2 weeks a month for 3 months. The course of treatment should be repeated as many times as necessary, while it is necessary to constantly monitor the patient's condition and indications for prolonging 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 change of permanent sexual partner; frequent vaginal intercourse (≥ 2-6 times a week) or anal sex; atopy (hereditary predisposition to increased sensitivity); poorly controlled diabetes; smoking; genital papillomavirus infection lasting more than 2 years or with 3 or more relapses 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 prolonging therapy.
Children
Use for children over 1 year of age.
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.
Adverse reactions
The only consistent adverse reaction during the use of inosine pranobex in adults and children is a temporary increase in serum and urinary uric acid levels, which return to baseline within a few days after the end of treatment.
The frequency of adverse reactions is defined as follows: common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); very rare (≥1/10000); 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 muscular disorders: arthralgia (joint pain).
Uncommon: Gastrointestinal disorders: diarrhea, constipation.
From the nervous system: drowsiness, sleep disorders.
Mental disorders: nervousness.
On the part of the urinary system: polyuria (increased urine volume).
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 (in the upper abdomen), lack of appetite;
from the immune system: anaphylactic reactions, anaphylactic shock, angioedema, hypersensitivity, urticaria;
Skin and subcutaneous tissue disorders: erythema.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
10 tablets in a blister; 2 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
LLC "Gedeon Richter Poland".
Location of the manufacturer and its business address
5, Kn. J. Ponyatowskiego Street, Grodzisk Mazowiecki, 05-825, Poland.
