Xanthinol niacinate

Xanthinol niacinate More Info

Xanthinol niacinate is a synthetic vasoactive agent and a derivative of niacin (vitamin B3) and xanthine. It is clinically classified as a peripheral vasodilator and antiplatelet agent, widely used in the management of cardiovascular and cerebrovascular disorders characterized by impaired blood flow.

1. Chemical & Pharmacological Properties

Chemical Formula: C₁₉H₂₃N₅O₆

Molecular Weight: 429.42 g/mol

Mechanism of Action:

It exerts dual effects: as a niacin derivative, it promotes vasodilation by inhibiting phosphodiesterase and increasing cyclic adenosine monophosphate (cAMP) levels in vascular smooth muscle cells; as a xanthine derivative, it enhances cerebral and peripheral blood flow by reducing blood viscosity and improving red blood cell deformability.

Additionally, it exhibits mild antiplatelet activity, reducing the risk of thrombus formation in microcirculation.

2. Therapeutic Indications

Xanthinol niacinate is primarily indicated for:

Cerebrovascular diseases: Cerebral atherosclerosis, cerebral infarction sequelae, and vascular dementia, to improve cerebral blood perfusion and neurological function.

Peripheral vascular diseases: Intermittent claudication, Raynaud’s phenomenon, and diabetic peripheral neuropathy, to alleviate ischemia-related symptoms such as pain and numbness.

Ophthalmic disorders: Ischemic optic neuropathy and retinal vascular occlusion, to enhance ocular blood flow.

3. Dosage & Administration

It is available in oral formulations (tablets/capsules) and injectable preparations.

Oral dose: Typically 300–600 mg per day, divided into 2–3 doses, adjusted based on patient response and tolerance.

Injectable dose: Administered intravenously or intramuscularly under medical supervision, usually 300 mg once or twice daily.

4. Contraindications & Precautions

Contraindications: Hypersensitivity to xanthinol niacinate, niacin, or xanthine derivatives; severe hypotension; acute myocardial infarction; and peptic ulcer disease.

Precautions:

Monitor blood pressure during treatment, especially in patients with hypotension or taking antihypertensive drugs.

Avoid use in pregnant or lactating women unless clearly necessary, as safety data are limited.

Gastrointestinal side effects (e.g., nausea, vomiting) may occur; administration with food can reduce discomfort.

5. Adverse Reactions

Common: Flushing, pruritus, and gastrointestinal disturbances (mild and transient, related to niacin release).

Rare: Hypotension, headache, dizziness, and allergic reactions (rash, urticaria). Severe adverse events such as liver function abnormalities are extremely rare with standard doses.

6. Pharmaceutical & Industrial Notes

In the pharmaceutical industry, xanthinol niacinate is produced via the condensation reaction of niacin with xanthinol.

It is a prescription-only medication in most regions, requiring strict quality control to ensure purity and bioavailability.

For raw material suppliers, key specifications include assay (≥98.5%), related substances (≤1.0%), and loss on drying (≤0.5%).