Xanthinol

Nicotinyl alcohol (3-pyridinylcarbinol, 3-pyridinemethanol) (27) has use as an antilipemic and peripheral vasodilator. It is available from either the reductions of nicotinic acid esters or preferably, the reduction of the nitrile to the amine followed by dia2otation and nucleophilic displacement. It is frequently adininistered in the form of the tartrate (Eig. 7). Nicotinic acid is frequently used as a salt in conjunction with basic dmgs such as the peripheral vasodilator xanthinol niacinate (28). Nicotinic acid and its derivatives have widespread use as antihyperlipidemic agents and peripheral vasodilators (1). 

Endomethylene-A -tetrahydro benzaldehyde Cyclothiazide Epibromohydrin Carteolol Epichlorohydrin Acebutolol Atenolol Befunolol Betaxolol HCI Bufetrol Bunitrolol Bupranolol Carazolol Carnitine Celiprolol Colestipol Cromolyn sodium I ndenolol Mazindol Mepindolol Metoprolol tartrate Nadolol Nifuratel Oxprenolol Penbutolol Practolol Propafenone HCI Propranolol HCI Viloxazine HCI Xanthinol niacinate Epinephrine... 

Loriaux SM, Deijen JB, Orlebeke JF and DeSwart JH (1985). The effect of niacin and xanthinol nicotinate on human memory in different age categories. Psychopharmacology,... 

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. 

Nicotinic acid derivatives include acipimox, aluminium nicotinate, nicotinyl alcohol, and xanthinol nicotinate. The adverse effects of these compounds appear to be identical to those of nicotinic acid. 

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. 

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