Xantinol nicotinate (Tablets, Solution) Instructions for Use

Instructions
Dosage forms

ATC Code

C04AD02 (Xantinol nicotinate)

Active Substance

Xantinol nicotinate (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Drug improving microcirculation. Angioprotector

Pharmacotherapeutic Group

Peripheral vasodilators; purine derivatives

Pharmacological Action

A microcirculation-improving agent; combines the properties of theophylline and nicotinic acid. It causes dilation of peripheral vessels, improves collateral circulation, improves microcirculation, and improves tissue oxygenation and nutrition.

It has an antiplatelet action, activates fibrinolysis processes, improves cerebral circulation, and reduces blood viscosity.

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

By reducing total peripheral vascular resistance (TPVR) and enhancing myocardial contractions, it contributes to an increase in minute volume of blood 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 the activity of lipoprotein lipase, reduces blood viscosity, and reduces platelet aggregation.

Pharmacokinetics

After oral administration, Xantinol nicotinate is rapidly absorbed from the gastrointestinal tract (GI 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 labeled 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 for 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 nicotinic acid is taken in low doses) and the second pathway is conjugation with glycine to form nicotinuric acid.

Nicotinic acid is excreted in the urine, mainly as metabolites; with repeated administration, up to 12% of the administered dose of nicotinic acid is excreted unchanged in the urine.

After intramuscular (IM) administration, 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

Open the list of ICD codes

ICD-10 code	Indication
E78.0	Pure hypercholesterolemia
E78.1	Pure hyperglyceridemia
E78.2	Mixed hyperlipidemia
G45	Transient cerebral ischemic attacks [TIAs] and related syndromes
H81.0	Ménière's disease
I25.1	Atherosclerotic heart disease
I63	Cerebral infarction
I67.2	Cerebral atherosclerosis
I73.0	Raynaud's syndrome
I73.1	Obliterative thromboangiitis [Buerger's disease]
I73.8	Other specified peripheral vascular diseases
I73.9	Peripheral vascular disease, unspecified (including intermittent claudication, arterial spasm)
I79.2	Peripheral angiopathy in diseases classified elsewhere (including diabetic angiopathy)
I80	Phlebitis and thrombophlebitis
I83.2	Varicose veins of lower extremities with ulcer and inflammation
L98.4	Chronic skin ulcer, not elsewhere classified

ICD-11 code	Indication
4A44.8	Thromboangiitis obliterans
5C80.00	Primary hypercholesterolemia
5C80.1	Hypertriglyceridemia
5C80.2	Mixed hyperlipidemia
8B10.Z	Transient ischemic attack, unspecified
8B11	Cerebral ischemic stroke
AB31.0	Ménière's disease
BA52.Z	Atherosclerosis of coronary arteries, site unspecified
BD42.0	Raynaud's disease
BD42.1	Raynaud's syndrome
BD42.Z	Raynaud's phenomenon, unspecified
BD4Z	Chronic obliterative arterial diseases, unspecified
BD53.Y	Other specified secondary involvement of arteries and arterioles
BD55	Asymptomatic stenosis of intracranial or extracranial artery
BD5Z	Diseases of arteries or arterioles, unspecified
BD70.0	Superficial thrombophlebitis of lower extremities
BD70.Z	Superficial thrombophlebitis, unspecified
BD71.4	Deep vein thrombosis of lower extremity
BD74.Z	Chronic venous insufficiency of lower extremities, unspecified
BD7Z	Diseases of veins, unspecified
EA40	Tropical phagedenic ulcer
EB90.21	Tuberous xanthoma
EB90.22	Eruptive xanthoma
EF60	Ischemic ulceration of the skin
EG00	Dilation of skin vessels of the extremities
EM0Z	Unspecified skin disorder
MB40.7	Acroparesthesia
ME60.2	Ulcerative skin lesion of unspecified nature

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Solution

For acute tissue blood supply disorders, the drug is administered intramuscularly (IM) at 0.3 g (2 ml of 15% solution) 1-3 times/day. Depending on the nature of the disease, the dose can be gradually increased to 0.6-0.9 g (4-6 ml of 15% solution) 2-3 times/day. The duration of treatment is 2-3 weeks.

For acute peripheral and cerebral circulation disorders, Xantinol nicotinate is administered intravenously (IV) by drip at a rate of 40-50 drops/min. For this, 1.5 g (10 ml of 15% solution) of the drug is diluted in 200-500 ml of 5% glucose solution or in 200 ml of isotonic sodium chloride solution; the resulting infusion mixture is administered by drip over 1.5-4 hours. The infusion can be repeated up to 4 times/day; the duration of treatment is 5-10 days.

Tablets

Administered orally, intramuscularly (IM), and intravenously (IV) (bolus or drip). The dose, method and regimen of administration, and duration of therapy are determined individually, depending on the indications, clinical situation, and the dosage form used.

Adverse Reactions

From the cardiovascular system: possible decrease in blood pressure (BP), 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 the level of transaminases and alkaline phosphatase (ALP) is possible.

From the nervous system: headache.

Allergic reactions:skin itching, urticaria, angioneurotic edema, anaphylactic shock.

Other: 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, changes in glucose tolerance, an increase in the level of uric acid in the blood serum are possible.

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

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, peptic ulcer of the stomach and duodenum 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 the lactation period, breastfeeding should 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 (no experience with use).

Special Precautions

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

Xantinol nicotinate causes a “nicotinic-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 distorted.

In patients with diabetes mellitus, glycemia should be carefully monitored.

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

Influence on the ability to drive vehicles and mechanisms

When using xantinol nicotinate, dizziness, weakness, and arterial hypotension are possible, in connection with this, 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 hypotensive agents (including beta-blockers, alpha-blockers, ganglioblockers). Do not use simultaneously with MAO inhibitors and strophanthin.

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

Simultaneous consumption of alcohol may enhance the severity of the side effects 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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Xantinol nicotinate [Armavir Biopharmaceutical Plant, FSE (Russia)]
Solution for intravenous and intramuscular injection 150 mg/ml: 10 ml amp. 20 pcs.

Marketing Authorization Holder

Armavir Biopharmaceutical Plant, FSE (Russia)

Dosage Form

Xantinol nicotinate

Solution for intravenous and intramuscular injection 150 mg/ml: 10 ml amp. 20 pcs.

Dosage Form, Packaging, and Composition

Solution for IV and IM injection	1 ml	1 amp.
Xantinol nicotinate	150 mg	1.5 g

10 ml – ampoules (10) – cardboard packs.

Xantinol nicotinate [Dalkhimpharm, JSC (Russia)]
Tablets 150 mg: 30 or 60 pcs.

Marketing Authorization Holder

Dalkhimpharm, JSC (Russia)

Dosage Form

Xantinol nicotinate

Tablets 150 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Tablets	1 tab.
Xantinol nicotinate	150 mg

10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.

Xantinol nicotinate [Dalkhimpharm, JSC (Russia)]
Solution for intramuscular administration 300 mg/2 ml: amp. 10 pcs.

Marketing Authorization Holder

Dalkhimpharm, JSC (Russia)

Dosage Form

Xantinol nicotinate

Solution for intramuscular administration 300 mg/2 ml: amp. 10 pcs.

Dosage Form, Packaging, and Composition

Solution for IM administration transparent, colorless.

	1 ml
Xantinol nicotinate	150 mg

Excipients : water for injections.

2 ml – ampoules (10) – cardboard packs.
2 ml – ampoules (5) – contour cell packs (2) – cardboard packs.

Xantinol nicotinate [Irbit Chemical Pharmaceutical Plant, JSC (Russia)]
Tablets 150 mg: 120 pcs.

Marketing Authorization Holder

Irbit Chemical Pharmaceutical Plant, JSC (Russia)

Manufactured By

Irbit Chemical Pharmaceutical Plant, JSC (Russia)

Dosage Form

Xantinol nicotinate

Tablets 150 mg: 120 pcs.

Dosage Form, Packaging, and Composition

Tablets	1 tab.
Xantinol nicotinate	150 mg

120 pcs. – polymer containers (1) – cardboard packs.

Xantinol nicotinate [N.A. Semashko Moscow Chemical Pharmaceutical Preparations, JSC (Russia)]
Solution for intravenous and intramuscular administration 150 mg/ml: 2 ml amp. 10 pcs.

Marketing Authorization Holder

N.A. Semashko Moscow Chemical Pharmaceutical Preparations, JSC (Russia)

Dosage Form

Xantinol nicotinate

Solution for intravenous and intramuscular administration 150 mg/ml: 2 ml amp. 10 pcs.

Dosage Form, Packaging, and Composition

Solution for IV and IM administration colorless, transparent.

	1 ml
Xantinol nicotinate	150 mg

Excipients : water for injections (up to 1 ml).

2 ml – ampoules (10) – cardboard boxes.

Xantinol nicotinate [Novosibkhimpharm, JSC (Russia)]
Solution for intravenous and intramuscular administration 150 mg/ml: 2 ml or 10 ml amp. 5, 10, or 20 pcs.

Marketing Authorization Holder

Novosibkhimpharm, JSC (Russia)

Dosage Form

Xantinol nicotinate

Solution for intravenous and intramuscular administration 150 mg/ml: 2 ml or 10 ml amp. 5, 10, or 20 pcs.

Dosage Form, Packaging, and Composition

Solution for IV and IM administration colorless transparent.

	1 ml
Xantinol nicotinate	150 mg

Excipients : water for injections up to 1 ml.

2 ml – ampoules (10) – cardboard boxes.
10 ml – ampoules (10) – cardboard boxes.
2 ml – ampoules (5) – contour cell packs (1) – cardboard packs.
2 ml – ampoules (5) – contour cell packs (2) – cardboard packs.
2 ml – ampoules (10) – contour cell packs (1) – cardboard packs.
2 ml – ampoules (10) – contour cell packs (2) – cardboard packs.
10 ml – ampoules (5) – contour cell packs (1) – cardboard packs.
10 ml – ampoules (5) – contour cell packs (2) – cardboard packs.
10 ml – ampoules (10) – contour cell packs (1) – cardboard packs.
10 ml – ampoules (10) – contour cell packs (2) – cardboard packs.

Xantinol nicotinate [Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)]
Tablets 150 mg: 60 pcs.

Marketing Authorization Holder

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

Dosage Form

Xantinol nicotinate

Tablets 150 mg: 60 pcs.

Dosage Form, Packaging, and Composition

Tablets white or almost white, flat-cylindrical, with a bevel and a score line.

	1 tab.
Xantinol nicotinate	150 mg

Excipients: lactose – 15.7 mg, potato starch – 51.3 mg, povidone (low molecular weight medical polyvinylpyrrolidone) – 10.7 mg.

10 pcs. – contour cell packs (6) – cardboard packs.
10 pcs. – contour non-cell packs (6) – cardboard packs.

Xantinol nicotinate [Ellara, LLC (Russia)]
Solution for intravenous and intramuscular administration 150 mg/ml: 2 ml amp. 5 or 10 pcs.

Marketing Authorization Holder

Ellara, LLC (Russia)

Dosage Form

Xantinol nicotinate

Solution for intravenous and intramuscular administration 150 mg/ml: 2 ml amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and intramuscular administration colorless transparent.

	1 ml
Xantinol nicotinate	150 mg

Excipients: water for injections – up to 1 ml.

2 ml – glass ampoules (5) – contour cell packs (1) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packs (2) – cardboard packs.
2 ml – glass ampoules (5) – cardboard packs.
2 ml – glass ampoules (10) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packs (4) – cardboard packs (for hospitals).
2 ml – glass ampoules (5) – contour cell packs (5) – cardboard packs (for hospitals).
2 ml – glass ampoules (5) – contour cell packs (10) – cardboard packs (for hospitals).
2 ml – glass ampoules (5) – contour cell packs (50) – cardboard packs (for hospitals).
2 ml – glass ampoules (5) – contour cell packs (100) – cardboard packs (for hospitals).

Xantinol nicotinate-N.S. [Shchelkovsky Vitamin Plant, JSC (Russia)]
Tablets 150 mg: 30 or 60 pcs.