Riboxin [Inosine]
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2019-09-19
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Clinical Pharmacology
Pharmacotherapeutic group:
metabolic agent.
KODATH: [С01ЕВ].
Pharmacological properties:
Riboxin is a derivative (nucleoside) of purine - the precursor of ATP adenosine triphosphate. It belongs to the group of drugs that stimulate metabolic processes. It has antihypoxic and antiarrhythmic effects. Increases the energy balance of the myocardium, improves coronary circulation, prevents the effects of intraoperative renal ischemia. He is directly involved in glucose metabolism and contributes to the activation of metabolism in hypoxic conditions and in the absence of ATP.
It activates the metabolism of pyruvic acid to ensure the normal process of tissue respiration, and also contributes to the activation of xanthine dehydrogenase. Stimulates the synthesis of nucleotides, enhances the activity of certain enzymes of the Krebs cycle. Penetrating into the cells, it has a positive effect on metabolic processes in the myocardium - it increases the strength of the heart contractions and contributes to a more complete relaxation of the myocardium in diastole, as a result of which the stroke volume increases. The mechanism of antiarrhythmic action is not fully understood.
Reduces platelet aggregation, activates tissue regeneration (especially the myocardium and gastrointestinal mucosa).
Pharmacokinetics
Metabolized in the liver with the formation of glucuronic acid and its subsequent oxidation. In small quantities excreted in the urine.
Indications
Comprehensive treatment of myocardial infarction, ischemic heart disease, cardiac arrhythmias caused by the use of cardiac glycosides, on the background of myocardial dystrophy after infectious diseases. Liver diseases (hepatitis, cirrhosis, fatty degeneration). Surgery on an isolated kidney (as a means of pharmacological protection when blood circulation is turned off).
Composition
1 ml of solution contains:
active ingredient: inosine (riboxin) 20 mg,
excipients: propylene glycol, sodium hydroxide, sodium sulfite anhydrous, water for injection.
Description:
Colorless or slightly colored clear liquid.
Inosine is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Riboxin-SOLOFARM | solution | ||
| Riboxin injection 2% | Grotex Ltd | Russia | solution |
| Riboxin | Dalkhimpharm | Russia | ampoules |
| Riboxin | BPMP | Belarus | pills |
| Riboxin injection 2% | BPMP | Belarus | ampoules |
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Dosage and Administration
The drug is administered intravenously in a stream slowly or drip (40-60 drops in 1 minute). Treatment begins with the introduction of 200 mg (10 ml of 2% solution) 1 time per day, then, with good endurance, the dose is increased to 400 mg (20 ml of 2% solution) 1-2 times a day.
Duration of treatment is 10-15 days.
Jet injection of the drug is possible with acute arrhythmias in a single dose of 200-400 mg.
For pharmacological protection of ischemic kidneys, riboxin is administered intravenously in a single dose, 1.2 g (60 ml of a 2% solution) 5–15 minutes before clamping the renal artery, and then another 0.8 g (40 ml of a 2% solution ) immediately after the restoration of blood circulation.
When drip into a vein, a 2% solution of the drug is diluted in 5% dextrose solution (glucose) or isotonic sodium chloride solution (up to 250 ml).
Adverse reactions
Allergic reactions: pruritus, skin flushing (the drug should be abolished). Rarely: an increase in the concentration of uric acid in the blood, exacerbation of gout (with prolonged use).
Contraindications
Hypersensitivity to the drug, gout, hyperuricemia, pregnancy, lactation, age up to 18 years (efficacy and safety have not been established). Use with caution in renal failure.
- Brand name: Riboxin-SOLOFARM
- Active ingredient: Inosine
- Dosage form: Solution for intravenous administration of 20 mg / ml.
- Manufacturer: Borisov plant
Studies and clinical trials of Inosine (Click to expand)
- Synthesis of a New N1-Pentyl Analogue of Cyclic Inosine Diphosphate Ribose (cIDPR) as a Stable Potential Mimic of Cyclic ADP Ribose (cADPR)
- Stabilities and Isomeric Equilibria in Solutions of Monomeric Metal-Ion Complexes of Guanosine 5′-Triphosphate (GTP4−) and Inosine 5′-Triphosphate (ITP4−) in Comparison with Those of Adenosine 5′-Triphosphate (ATP4−)
- Detection of Hydrogen Bridges between Inosine and Other Nucleosides by NMR Spectroscopy
- Molecular imprinting micropolymerbeads having cooperative effect of both surfactant and inosine template
- A rapid and simple chemiluminescence method for screening levels of inosine and hypoxanthine in non-traumatic chest pain patients
- Minor nucleosides in RNA: Optical studies of dinucleoside phosphates containing inosine
- A real-time and hands-on research course in protein purification and characterization: Purification and crystal growth of human inosine triphosphate pyrophosphatase
- Effect of diets containing adenosine, guanosine, inosine or xanthosine on the nucleotide content of Artemia. Influence of mycophenolic acid
- ChemInform Abstract: An Approach to a Carbocyclic Analogue of Cyclic Adenosine 5′- Diphosphate Ribose. The Synthesis and Bisphosphorylation of N1-((1S,3R) -3-(Hydroxymethyl)cyclopent-1-yl)inosine.
- ChemInform Abstract: Synthesis of Amide Linked Nucleosides at the 6 Position of Deoxy Inosine and Their Application to DNA Synthesis; Hybridization Studies.
- ChemInform Abstract: Lipase-Catalyzed Protection of the Hydroxy Groups of the Nucleosides Inosine and 2′-Deoxyinosine: A New Chemoenzymatic Synthesis of the Antiviral Drug 2′,3′-Dideoxyinosine.
- ChemInform Abstract: Mechanism-based Design of Inosine 5′-Monophosphate Dehydrogenase Inhibitors: Synthesis and Biological Activities of 5-Ethynyl-1-β-D-ribofuranosylimidazole-4-carboxamide (EICAR) and Its Derivatives
- ChemInform Abstract: Synthetic Studies on the Glycosylation of the Base Residues of Inosine and Uridine.
- ChemInform Abstract: C6 Substitution of Inosine Using Hexamethylphosphorous Triamide in Conjunction with Carbon Tetrahalide or N-Halosuccinimide.
- ChemInform Abstract: An Improved Synthesis of Inosine 3′-Phosphoramidite.
- ChemInform Abstract: Acid—Base Properties of the 5′-Triphosphates of Guanosine and Inosine (GTP4- and ITP4-) and of Several Related Nucleobase Derivatives.
- ChemInform Abstract: Regioselective BH3—Hydride Reduction of Inosine Derivatives.
- ChemInform Abstract: Glycosylations of Inosine and Uridine Nucleoside Bases and Synthesis of the New 1-(β-D-Glucopyranosyl)-inosine-5′,6′′-diphosphate.
- ChemInform Abstract: Rapid Synthesis of Triazine Inhibitors of Inosine Monophosphate Dehydrogenase.
- A Survey of Cyclic Replacements for the Central Diamide Moiety of Inhibitors of Inosine Monophosphate Dehydrogenase
- Novel Amide-Based Inhibitors of Inosine 5′-Monophosphate Dehydrogenase.
- Novel Guanidine-Based Inhibitors of Inosine Monophosphate Dehydrogenase.
- NAD Analogues 18 — The Chemistry of Nucleoside and Dinucleotide Inhibitors of Inosine Monophosphate Dehydrogenase (IMPDH)
- X-ray and Solution Structure of Inosine 5' -Monophosphate Coordinated to (Ethylenediamine)palladium(II). —the Importance of Intramolecular Hydrogen Bonding
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