Flushing xanthinol nicotinate

Nicotinic acid and its derivatives (pyridylcarbinol, xanthinol nicotinate, acipimox) activate endothelial lipoprotein lipase and thereby lower triglyceride levels. At the start of therapy, a prostaglandin-mediated vasodilation occurs (flushing and hypotension) that can be prevented by low doses of acetyl-salicylic acid. 

Nicotinic acid (5.18), and related derivatives such as pyridylcarbinol (5.19), xanthinol nicotinate (5.20), acipimox (5.21), given in large doses, influence the lipoprotein ratio, decreasing the concentrations of very low and low-density lipoprotein, but have no effect on HDL-cholesterol complexes. Acipimox (5.21) is a new pyrazine derivative that is 20 times more active than nicotinic acid. When first administered, the use of these agents is associated with flushing and hypotension. 

Severe toxicoderma has been reported with xanthinol nicotinate and confirmed by a provocation test (SEDA-1, 333). Flushing is claimed to be less frequent with xanthinol nicotinate than with nicotinic acid, but has nevertheless been repeatedly observed, and its other adverse effects are likely to be the same as those of nicotinic acid. 

---