Inibisine^® (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmasintez, JSC (Russia)

ATC Code

J05AX05 (Inosine pranobex)

Active Substance

Inosine pranobex (BAN)

Dosage Form

Inibisine®

Tablets 500 mg: 5, 10, 15, 20, 25, 30, 40, 50, or 100 pcs.

Dosage Form, Packaging, and Composition

Tablets are white or almost white, capsule-shaped, biconvex, with a score on one side; the tablet can be divided into equal doses.

Excipients: potato starch, povidone K25, magnesium stearate.

5 pcs. – blister packs (1) – cardboard packs.
5 pcs. – blister packs (2) – cardboard packs.
5 pcs. – blister packs (3) – cardboard packs.
5 pcs. – blister packs (4) – cardboard packs.
5 pcs. – blister packs (5) – cardboard packs.
5 pcs. – blister packs (10) – cardboard packs.
10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.
10 pcs. – blister packs (5) – cardboard packs.
10 pcs. – blister packs (10) – cardboard packs.
30 pcs. – polymer jars (10) – cardboard packs.

Clinical-Pharmacological Group

Immunostimulant drug with antiviral activity

Pharmacotherapeutic Group

Systemic antiviral agents; direct-acting antiviral agents; other antiviral agents

Pharmacological Action

An immunostimulating agent with nonspecific antiviral action. It is a complex containing inosine and the salt of 4-acetamidobenzoic acid with N,N-dimethylamino-2-propanol in a molar ratio of 1:3. The efficacy of the complex is determined by the presence of inosine, the second component increases its availability for lymphocytes.

It restores lymphocyte functions under immunosuppression conditions, increases blastogenesis in the monocytic cell population, stimulates the expression of membrane receptors on the surface of T-helpers, prevents the decrease in lymphocyte activity under the influence of glucocorticoids, and normalizes thymidine incorporation into them.

Inosine pranobex has a stimulating effect on the activity of cytotoxic T-lymphocytes and natural killer cells, the functions of T-suppressors and T-helpers, increases the production of IgG, interferon gamma, interleukins (IL)-1 and IL-2, reduces the formation of proinflammatory cytokines – IL-4 and IL-10, and potentiates the chemotaxis of neutrophils, monocytes, and macrophages.

It exhibits antiviral activity in vivo against Herpes simplex viruses, cytomegalovirus, measles virus, human T-cell lymphoma virus type III, polioviruses, influenza A and B, ECHO virus (human enterocytopathic virus), encephalomyocarditis, and equine encephalitis virus.

The mechanism of antiviral action is associated with the inhibition of viral RNA and the enzyme dihydropteroate synthase, which is involved in the replication of some viruses.

It enhances the virus-suppressed synthesis of lymphocyte mRNA, which is accompanied by suppression of viral RNA biosynthesis and translation of viral proteins, and increases the production of interferons alpha and gamma by lymphocytes, which have antiviral properties.

It reduces the clinical manifestations of viral diseases, accelerates reconvalescence, and increases the body’s resistance.

When used as an auxiliary drug for infectious lesions of the mucous membranes and skin caused by the Herpes simplex virus, healing of the affected surface occurs faster than with traditional treatment. New blisters, edema, erosions, and disease relapses occur less frequently.

With timely use of inosine pranobex, the frequency of viral infections decreases, and the duration and severity of the disease are reduced.

Pharmacokinetics

After oral administration, it is rapidly and almost completely (> 90%) absorbed and has good bioavailability. When taken orally at a dose of 1500 mg, the C_max of inosine pranobex is reached after 1 hour and is 600 µg/ml. It is not detected in the blood 2 hours after administration.

Inosine pranobex consists of inosine and the salt of p-acetamidobenzoic acid with N,N-dimethylamino-2-propanol. Each of the components of inosine pranobex is rapidly metabolized. Almost 100% of metabolites are detected in the urine within 8 to 24 hours after administration.

Inosine is metabolized according to the cycle typical for purine nucleotides, with the formation of uric acid, the concentration of which in the blood serum may increase. As a result, the formation of uric acid crystals in the urinary tract is possible. The increase in uric acid concentration is non-linear and may change by ±10% within 1-3 hours after oral administration.

As a result of the metabolism of p-acetamidobenzoic acid, o-acylglucuronide is formed; N,N-dimethylamino-2-propanol is metabolized to N-oxide. The AUC of p-acetamidobenzoic acid is >88%, the AUC of N,N-dimethylamino-2-propanol is >77%. No accumulation in the body has been detected.

Inosine and its metabolites are excreted in the urine. When the equilibrium concentration is reached with a daily dose of 4 g, the daily urinary excretion of p-acetamidobenzoic acid and its metabolite is approximately 85% of the administered dose; T_1/2 is 50 min. The T_1/2 of N,N-dimethylamino-2-propanol is 3-5 hours.

Inosine pranobex and its metabolites are completely eliminated from the body within 48 hours.

Indications

Immunodeficiency conditions caused by viral infections in patients with normal and weakened immune systems, including diseases caused by Herpes simplex viruses types 1 and 2 (including genital herpes and herpes of other localizations), Varicella zoster (herpes zoster, chickenpox); subacute sclerosing panencephalitis. Treatment of influenza and other acute respiratory viral infections; infectious mononucleosis caused by the Epstein-Barr virus; cytomegalovirus infection; severe measles; papillomavirus infection: laryngeal/vocal cord papillomas (fibrous type), genital papillomavirus infection in men and women, warts; molluscum contagiosum.

ICD codes

Dosage Regimen

Take orally.

Adults: from 500 mg to 4 g/day.

Children aged 3 to 12 years: 50 mg/kg/day.

In both adults and children, in severe infectious diseases, the dose can be individually increased to 100 mg/kg of body weight/day, divided into 4-6 doses. Maximum daily dose for adults is 3-4 g, for children – 50 mg/kg.

The frequency of administration, course of treatment, frequency of repeated courses depends on the indications, course of the disease, treatment regimen.

Adverse Reactions

Nervous system disorders: frequently – headache, dizziness, fatigue, malaise; infrequently – nervousness, drowsiness, insomnia.

Gastrointestinal disorders: frequently – decreased appetite, nausea, vomiting, epigastric pain; infrequently – diarrhea, constipation.

Hepatobiliary system disorders: frequently – increased activity of liver enzymes, alkaline phosphatase.

Skin and subcutaneous tissue disorders: frequently – itching, rash.

Renal and urinary disorders: infrequently – polyuria.

Allergic reactions: infrequently – maculopapular rash, urticaria, angioedema.

Musculoskeletal and connective tissue disorders: frequently – joint pain, exacerbation of gout.

Other: frequently – increased blood urea nitrogen concentration.

Contraindications

Gout; urolithiasis; arrhythmia; chronic renal failure; children under 3 years of age (body weight under 15-20 kg); pregnancy; lactation period (breastfeeding); hypersensitivity to the drug components.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Special Precautions

Use with caution when prescribing the drug with xanthine oxidase inhibitors, diuretics, zidovudine, in acute renal failure.

Inosine pranobex, like other antiviral agents, is most effective in acute viral infections if treatment is started at an early stage of the disease (preferably from the first day).

Since inosine is excreted from the body in the form of uric acid, with long-term use, it is recommended to periodically monitor the concentration of uric acid in the blood serum and urine. Patients with a significantly increased concentration of uric acid in the body may simultaneously take drugs that lower its concentration.

It is necessary to monitor the concentration of uric acid in the blood serum when using inosine pranobex simultaneously with drugs that increase the concentration of uric acid or drugs that impair kidney function.

In elderly patients, an increase in the concentration of uric acid in the blood serum and urine occurs more often than in middle-aged patients.

Use with caution in patients with acute hepatic insufficiency, since the drug is metabolized in the liver. In patients with hepatic insufficiency, the content of uric acid in the blood serum and urine should be monitored every 2 weeks. Monitoring of liver enzyme activity is recommended every 4 weeks during long-term courses of treatment with the drug.

Effect on the ability to drive vehicles and mechanisms

When used in patients engaged in driving vehicles and other potentially hazardous activities, the possibility of dizziness and drowsiness should be considered.

Drug Interactions

Immunosuppressants weaken the immunostimulating effect of inosine pranobex.

With simultaneous use with xanthine oxidase inhibitors (allopurinol), or “loop” diuretics (furosemide, torasemide, ethacrynic acid), an increase in the concentration of uric acid in the blood serum is possible.

Concomitant use with zidovudine leads to an increase in the concentration of zidovudine in the blood plasma and prolongs its T_1/2. With this combination, dose adjustment of zidovudine may be required.

When used in combination, it enhances the action of interferon-alpha, the antiviral agents acyclovir and zidovudine.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.