Xatinate (Tablets) Instructions for Use

Marketing Authorization Holder

Bryntsalov-A, JSC (Russia)

ATC Code

C04AD02 (Xantinol nicotinate)

Active Substance

Xantinol nicotinate (Rec.INN registered by WHO)

Dosage Form

Xatinate

Tablets 150 mg: 20, 30 or 40 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.

Clinical-Pharmacological Group

Drug improving microcirculation. Angioprotector

Pharmacotherapeutic Group

Vasodilating agent

Pharmacological Action

A microcirculation-improving agent; combines the properties of theophylline and nicotinic acid. Causes dilation of peripheral vessels, improves collateral circulation, improves microcirculation, improves tissue oxygenation and nutrition. It has an antiplatelet effect, activates fibrinolysis processes, improves cerebral circulation, and reduces blood viscosity.

It enhances oxidative phosphorylation and ATP synthesis. By blocking adenosine receptors and PDE, it increases the cAMP content in the cell and substrate-stimulates the synthesis of NAD and NADP.

By reducing total peripheral vascular resistance and enhancing myocardial contractions, it contributes to an increase in minute blood volume and enhancement of cerebral circulation, reducing the severity of the consequences of cerebral hypoxia.

With prolonged use, it has an antiatherosclerotic effect, activates fibrinolysis processes, reduces the concentration of cholesterol and atherogenic lipids, increases lipoprotein lipase activity, reduces blood viscosity, and reduces platelet aggregation.

Pharmacokinetics

After oral administration, Xantinol nicotinate is rapidly absorbed from the gastrointestinal tract. In the body, it dissociates to form xantinol and nicotinic acid. Nicotinic acid binds to blood proteins by less than 20%. Preclinical studies in mice have shown that nicotinic acid combined with a radioactive isotope accumulates in the liver, kidneys, and adipose tissue.

The metabolism of nicotinic acid occurs in the liver. There are two pathways of nicotinic acid metabolism: the first pathway is the formation of nicotinamide adenine dinucleotide (NAD) with subsequent conversion to N-methylnicotinamide and N-methyl-2-pyridone-5-carboxamide (the main metabolic pathway when taking nicotinic acid in low doses) and the second pathway is conjugation with glycine to form nicotinuric acid. Nicotinic acid is excreted in the urine, mainly in the form of metabolites; with repeated administration, up to 12% of the administered dose of nicotinic acid is excreted in the urine unchanged.

After intramuscular injection, Xantinol nicotinate is absorbed quickly and completely. With repeated use, its pharmacokinetics do not change. No accumulation is noted.

After administration, it undergoes intensive metabolism in the liver.

Indications

As part of complex therapy: obliterating atherosclerosis of limb vessels, Raynaud’s disease, obliterating endarteritis, diabetic angiopathy, acute thrombophlebitis (superficial and deep veins), trophic ulcers of the legs, cerebrovascular insufficiency, Ménière’s syndrome, cerebral vascular atherosclerosis, cerebrovascular accident, coronary artery atherosclerosis, hypercholesterolemia, hypertriglyceridemia.

ICD codes

Dosage Regimen

Administer Xatinate orally, intramuscularly, or intravenously as a bolus or drip infusion.

Determine the dose, route of administration, and treatment duration individually based on the indication and clinical situation.

For oral administration, the typical adult dose is 150 mg to 300 mg taken two to three times daily.

For intramuscular injection, administer 300 mg to 600 mg once or twice daily.

For intravenous administration, inject 300 mg to 600 mg slowly or administer as an infusion diluted in a suitable solution.

Initiate therapy with a lower dose and gradually increase it to minimize potential adverse effects.

For long-term management of chronic conditions, continue treatment for several weeks or months as clinically indicated.

Do not exceed the maximum daily dose as determined by the prescribing physician.

Monitor blood pressure during and after parenteral administration due to the risk of hypotension.

Adjust the regimen for elderly patients or those with labile blood pressure, using caution.

Adverse Reactions

From the cardiovascular system: possible decrease in blood pressure, transient sensation of heat, redness of the skin.

From the digestive system: rarely – nausea, diarrhea, anorexia, gastralgia; with long-term use in high doses, an increase in transaminase and alkaline phosphatase levels is possible.

From the nervous system: headache.

Allergic reactions: skin itching, urticaria, angioedema, anaphylactic shock.

Others: weakness, chills, tingling of the skin, especially in the head and neck area (these symptoms usually disappear within 10-20 minutes, do not require special treatment and discontinuation of this medication); with long-term use in high doses, a change in glucose tolerance, an increase in serum uric acid levels is possible.

When using nicotinic acid preparations, a false increase in the concentration of catecholamines in blood plasma and urine may be noted, and a false-positive result in the determination of urine glucose using Benedict’s test may also be noted.

Contraindications

Hypersensitivity to xantinol nicotinate; acute bleeding, acute myocardial infarction, mitral stenosis, acute heart failure, chronic heart failure in the stage of decompensation, arterial hypotension, gastric and duodenal ulcer in the acute phase, acute renal failure, glaucoma; first trimester of pregnancy, lactation period (breastfeeding); childhood.

Use in Pregnancy and Lactation

Contraindicated for use in the first trimester of pregnancy. In the second and third trimester of pregnancy, the use of xantinol nicotinate is permissible only in the presence of absolute indications, in the case where the intended benefit to the mother outweighs the potential risk to the fetus. Xantinol nicotinate in this case is used under the careful supervision of a physician.

If it is necessary to use xantinol nicotinate during lactation, breastfeeding must be discontinued, because nicotinic acid is excreted in breast milk.

Use in Renal Impairment

Contraindicated for use in acute renal failure.

Pediatric Use

The use of xantinol nicotinate in children is contraindicated (experience of use is absent).

Special Precautions

Xantinol nicotinate should be used with caution in case of labile blood pressure.

Xantinol nicotinate causes a “nicotine-like” syndrome, accompanied by hyperesthesia of the mucous membrane of the nasal and oral cavities (exacerbates the sensitivity of olfactory and taste receptors). In this regard, the smell and taste of alcoholic beverages consumed during therapy is perceived as more sharp and perverted.

In patients with diabetes mellitus, it is necessary to carefully monitor glycemia.

Avoid getting xantinol nicotinate into the eyes or on mucous membranes.

Influence on the ability to drive vehicles and mechanisms

When using xantinol nicotinate, dizziness, weakness, and arterial hypotension are possible, in this regard, during the treatment period, patients should avoid driving vehicles and other activities requiring high concentration and speed of psychomotor reactions.

Drug Interactions

To avoid a sharp decrease in blood pressure, Xantinol nicotinate should not be used simultaneously with antihypertensive agents (including beta-blockers, alpha-blockers, ganglion blockers). Do not use simultaneously with MAO inhibitors and strophanthin.

Simultaneous use of nicotinic acid preparations in combination with HMG-CoA reductase inhibitors (statins) may increase the risk of myopathy and rhabdomyolysis.

Simultaneous consumption of alcohol may enhance the severity of the side effect of xantinol nicotinate (sensation of heat, redness of the skin).

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.