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Riboxine (Inosine) ampoules - Instructions for Use, Dosage, Side Effects, Reviews

18 Jan 2017

Pharmacological group: Anabolics.

Synonyms: An Jie Di Lin, An Qi Mi Rui, Ba Quan, Bioxin, Catacol, Correctol, Dan Ze, De Yi Mei, Di Li, En Li Ke, Fu Li Ding, Fu Li Xin, Gan Ke, Gan Quan, Hu Yue, Inosie F, Inosine Towa, Inosine-Hua Nan Pharm, Lai Mei Kang, Lan Xu, Li Fu - Binhu Shuanghe Pharm, PiDi Gan, Pu Fu, Qi Fang Neng, Quan Zhu, Riboxins, Riboxin, Riboxine, Riboxine-Darnitsa, Tonarsyl (veterinary use), WeiMeiJia, Xin Feng, Yan Luo Qi, Yi Rong Xin, Ying Di Te (Inosine and Citicoline), Yong Rui Neng, Ze Bei, Zhu Lu, Zuo He, Antikataraktikum N, Catacol, Correctol, Lumiclar.

Active substance: Inosine.

Inosine is a nucleoside that is formed when hypoxanthine is attached to a ribose ring (also known as a ribofuranose) via a β-N9-glycosidic bond.

Inosine is commonly found in tRNAs and is essential for proper translation of the genetic code in wobble base pairs.

Knowledge of inosine metabolism has led to advances in immunotherapy in recent decades. Inosine monophosphate is oxidised by the enzyme inosine monophosphate dehydrogenase, yielding xanthosine monophosphate, a key precursor in purine metabolism. Mycophenolate mofetil is an anti-metabolite, anti-proliferative drug that acts as an inhibitor of inosine monophosphate dehydrogenase. It is used in the treatment of a variety of autoimmune diseases including granulomatosis with polyangiitis because the uptake of purine by actively dividing B cells can exceed 8 times that of normal body cells, and, therefore, this set of white cells (which cannot operate purine salvage pathways) is selectively targeted by the purine deficiency resulting from inherited metabolic diseases (IMD) inhibition.

Inosine Reactions

Adenine is converted to adenosine or inosine monophosphate (IMP), either of which, in turn, is converted into inosine (I), which pairs with adenine (A), cytosine (C), and uracil (U).

Purine nucleoside phosphorylase intraconverts inosine and hypoxanthine.

Inosine is also an intermediate in a chain of purine nucleotides reactions required for muscle movements.

Inosine was tried in the 1970s in Eastern countries for improving athletic performance. Nevertheless, the clinical trials for this purpose showed no improvement.It has been shown that inosine has neuroprotective properties. It has been proposed for spinal cord injury; because it improves axonal rewiring, and for administration after stroke, because observation has shown that axonal rewiring is encouraged. You can buy Riboxin.

After ingestion, inosine produces uric acid that is suggested to be a natural antioxidant and a peroxynitrite scavenger with potential benefits to patients with multiple sclerosis (MS). Peroxynitrite has been correlated with axon degeneration. In 2003, a study was initiated at the University of Pennsylvania MS Center to determine whether raising the levels of uric acid by the administration of inosine would slow the progression of MS. The study was completed in 2006 but the results were not reported to NIH. A subsequent publication hinted at potential benefits but the sample size (16 patients) was too small for a definitive conclusion. In addition, the side effect of the treatment was the development of kidney stones in four of 16 patients. Thus, additional studies are necessary to prove the treatment's efficacy.

Inosine (Riboxin) is classified as an antiviral.

Riboxin (Inosine ) at Fitness

Despite lack of clinical evidence that it improves muscle development, inosine remains an ingredient in some fitness supplements.

Feeding Stimulant

Inosine has also been found to be an important feed stimulant by itself or in combination with certain amino acids in some species of farmed fish. For example, inosine and inosine-5-monophosphate have been reported as specific feeding stimulants for turbot fry, (Scophthalmus maximus) and Japanese amberjack, (Seriola quinqueradiata). The main problem of using inosine and/or inosine-5-monophosphate as feeding attractants is their high cost. However, their use may be economically justified within larval feeds for marine fish larvae during the early weaning period, since the total quantity of feed consumed is relatively low.

Inosine monophosphate dehydrogenase (IMP)

IMP dehydrogenase (Inosine-5'-monophosphate dehydrogenase) (Inosinic acid dehydrogenaseis) (IMPDH) an enzyme that converts inosine monophosphate to xanthosine monophosphate:

inosine 5'-phosphate + NAD+ + H2O ⇌ {\displaystyle \rightleftharpoons } \rightleftharpoons xanthosine 5'-phosphate + NADH + H+

Inosine monophosphate dehydrogenase catalyzes the rate-limiting reaction of de novo GTP biosynthesis.

IMP dehydrogenase is associated with cell proliferation and is a possible target for cancer chemotherapy. Mammalian and bacterial IMPDHs are tetramers of identical chains. There are two IMP dehydrogenase isozymes in humans. IMP dehydrogenase nearly always contains a long insertion that has two CBS domains within it.

The structure of this enzyme is composed of a TIM barrel domain with two CBS domains inserted within a loop.

It is inhibited by Mycophenolic acid, ribavirin, and 6TGMP (6-thioguanine monophosphate). 6TGMP inhibition prevents purine interconversion and thus the synthesis of purine nucleotides.

ATC C01EB Drugs for treatment of other diseases of the heart.

Nosological classification (ICD–10)

E80 Disorders of porphyrin and bilirubin;

I20 Angina [ angina ];

I21 Acute myocardial infarction;

I25 Chronic ischemic heart disease;

I42 Cardiomyopathy;

I49.9 Heart rhythm disturbances, unspecified;

K73 Chronic hepatitis, not elsewhere classified;

K74 Fibrosis and cirrhosis;

R07.2 Pain in the Heart;

T46.0 Poisoning by cardiac glycosides and drugs of similar action.

Pharmacological action

Riboxinum - derivative (nucleoside) purine - predecessor. Adenosine triphosphate (ATP). Refers to a group of drugs that stimulate the metabolic processes.

Riboxin has antihypoxia and antiarrhythmic effect. Increases the energy balance of the myocardium, improves coronary circulation, prevents the effects of intraoperative renal ischemia. Directly involved in the metabolism of glucose and promotes activation of metabolism in hypoxic conditions and in the absence of ATP. Activates the metabolism of pyruvic acid necessary to ensure the normal process of cell respiration and promotes activation of xanthine dehydrogenase. Stimulates the synthesis of nucleotides, enhances the activity of certain enzymes of the Krebs cycle. Penetrating into cells, has a positive effect on metabolism in the myocardium increases the force of heart contractions and promotes more complete relaxation of the myocardium in diastole, resulting in increased stroke volume. The mechanism of antiarrhythmic action until the end is unclear. Reduces platelet aggregation, activates the regeneration of tissues (particularly infarction and gastrointestinal mucosa).

Pharmacokinetics

Metabolized in the liver to form glucuronic acid and its subsequent oxidation. In small amounts excreted through the kidneys.

Riboxin Dosage

The drug is used IV jet slowly drip (40–60 drops/min). Treatment is initiated by introducing 200 mg (10 ml solution of 20 mg/ml), 1 time/day, and then, if tolerated, the dose was increased to 400 mg (20 ml solution of 20 mg/ml) 1–2 times/day. Duration of treatment - 10–15 days.

Bolus drug may acute when arrhythmias in a single dose of 200–400 mg (10–20 ml of 20 mg/ml).

In order to protect renal pharmacological subjected ischemia Riboxinum introducing IV single bolus dose of 1200 mg (60 ml solution of 20 mg/ml) for 5–15 min before the renal artery clamping, and then another 800 mg (40 ml solution of 20 mg/ml) immediately after the restoration of blood flow.

For IV drip a solution of 20 mg/ml diluted in 5% dextrose (glucose) solution or 0.9% sodium chloride (250 mL).

Riboxin Overdose

Currently, the cases of overdose have been reported.

Riboxin Drug Interactions

Reduce the effectiveness of immunosuppressants Riboxinum.

In a joint application with cardiac glycosides drug can prevent the occurrence of arrhythmias, amplify positive inotropic effect.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Riboxin (Inosine) Side effects

Allergic reactions: itching, redness of the skin (the drug should be discontinued.)

Rare: increased concentration of uric acid in the blood, increase gout (with prolonged use).

Indications for Riboxin

Comprehensive treatment of myocardial infarction, coronary heart disease, heart rhythm disorders associated with the use of cardiac glycosides, amid myocardiodystrophy after infectious diseases;

Liver disease (hepatitis, cirrhosis, fatty degeneration);

Operations in the isolated kidney (as a means of pharmacological protection when you turn off blood circulation).

Contraindications for Riboxin (Inosine)

Gout;

Hyperuricemia;

Pregnancy;

Lactation;

Age 18 (efficacy and safety have not been established);

Hypersensitivity to the drug.

Precautions: renal failure.

Cautions

Riboxinum not applicable for emergency correction of disorders of cardiac activity.

When the itching and redness of the skin drug treatment should be discontinued.

During prolonged treatment is desirable to control the concentration of uric acid in the blood and urine.

Riboxin Reviews

Riboxinum drug used in bodybuilding to support the heart muscle during the "dry", and for the anabolic properties. The latter, however, are greatly exaggerated - no 10 kg of muscle per course with him not to increase. In medicine, it is known as a means to increase coronary blood flow, and the treatment of various heart diseases.

Application Riboxinum bodybuilding
The effect of receiving Riboxinum Inositol used in sport as the iron in the form of conventional tablets and injections pharmacy, and as a component of some fat burners. There it is necessary to support the work of the heart, which is experiencing higher loads during the "drying". There are some drugs Riboxinum of sports nutrition lines, usually called Inosine.

The drug has anabolic properties and affects the metabolism, but the gain in muscle mass and strength can not be expected from him.

In the 70s of the last century Riboxinum widely used in bodybuilding and sports of force, it was later proven that his influence on the processes in the Krebs cycle and metabolism has nothing to do with the growth indicators of strength in athletes. Not reflected in its reception and the structure and muscle density.

There is a belief that the drug affects the recovery of muscle tissue, and can be used in the process of weight loss, as the anti-catabolic. Indeed, such properties are not expressed in the preparation, and wishing to lose weight only take it to protect cardiac muscle overload, and further its power.

How to take Riboxinum bodybuilding
As riboksin bodybuilding answer to the question of how to take Riboxinum bodybuilding depends on indication for use. For the purpose of improving the performance of the cardiovascular bodibildera system applied dosage of 1.5 - 2.5 g of substance in the form of tablets, half an hour before meals, three times a day. Start using tablets with half the dosage - 0.6 grams 3 times per day. If well tolerated, the amount of the substance increases.

Need to track inositol as a component in sports foods, and adjust the dosage. The injectable form is considered less hepatotoxicity, but in the practice of body building is used little.
Side effects

Common side effects Riboxinum arising Propafenone - allergic reaction, possible aggravation of pre-existing gout. When poor tolerability noted bradycardia and flushing. Then the drug overturned. Contraindications: acute renal failure

Reviews Riboxinum
Analyzing feedback on Riboxinum in bodybuilding, it may be noted that the taking is not only wishing to gain muscle mass, but also slimming. And most of the information of such a plan comes from them. Of course, to lose 5-10 kg inositol without diet yet it failed anyone yet, because there is a certain amount of disappointment, however.

Not happy Riboxinum and striving for muscle gain, especially if the latter are engaged in too little. The drug is quite specific, and keep track of a healthy person is difficult to real work.

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