Xanthinol nicotinate Review Article |
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 Complamin, or xanthinol nicotinate is a vasodilating agent from two compounds, xanthinol and nicotinic/niacinic acid, which both acts as vasodilator.
It is a drug available only in select countries. Its approved use is for the management of cerebral and peripheral vascular disorders, as well as for the management of hyperlipidemias (Sweetman, 2009). It is also used for short term memory disorders and other cognitive disorders such as dementia.
Mechanism of Action
Complamin’s activity is based on its two components – xanthinol and nicotinic acid. Complamin is slowly metabolised in the body to release the two drugs. Nicotinic acid is a known vasodilating agent, which most studies say is the main active component of the drug. Xanthinol, a theopylline derivative, enhances the effects of nicotinic acid (Bieron et al., 1998).
In a study made by Seidel and Endell (1977), they determined the possible mechanism of action of Complamin. In their study, they found that Complamin acts by inhibition of collagen induced platelet aggregation, which is opposed to an earlier theory that it inhibits adenosine diphosphate-induced aggregation. Continue reading...
Xanthinol nicotinate generic (generic - what is it?)
| Dosage |
Packing |
Price |
Add to basket |
| 150 mg |
50 tab ($0.18 per tab) |
USD 9.00 |
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| 150 mg |
100 tab ($0.15 per tab) |
USD 15.00 |
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| 150 mg |
200 tab ($0.12 per tab) |
USD 23.00 |
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| 500 mg |
100 tab ($0.45 per tab) |
USD 45.00 |
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In a more recent study by Cheng et al. (2005), they stated that the vasodilating effect of nicotinic acid may be due to increased synthesis and secretion of prostaglandin D2 (PGD2), a type of prostacylcin in the serum. PGD2 directly stimulates vasodilation. Bieron and colleagues (1998) supports these findings, and that nicotinic acid also increases the release of nitric oxide, another endogenous vasodilator. They further stated that xanthinol enhances the physiological response to these two mediators, increasing their secondary messengers’ actions.
Its molecular formula is C13H21N5O4•C6H5NO2 and its structural formula is:
Xanthinol (left) and Nicotinic acid (right)
 
Clinical studies
Little studies have been available for this drug though it has been used for more than 40 years. This may be due to the fact that it is available only in select countries. However, these studies have a lot to say regarding the possible impact of this drug in several disorders, such as lipid problems, vascular problems (platelet aggregation hypertension) and cognitive functioning.
In a study made by Gaevyĭ and colleagues (1984), they found that Complamin is able to provide a vasodilating effect both on cerebral and peripheral vascular systems decreasing blood pressure in highly perfused organs in animal models. These findings were further supported by Mungiu et al. (1991) and Hegde (1991).Aside from its antiplatelet activities, it was also found to have fibrinolytic (Beiron et al., 1998) by two mechanisms, reduction of fibrinogen levels and increase in tissue plasminogen activators, which dissolves clot.
Nicotinic acid is a proven antihyperlipidemic agent, which affects all lipid parameters (Knopp et al., 1985). Nicotinic acid inhibits very low density lipoprotein (VLDL) secretions, leading to a decreased low density lipoprotein (LDL) levels. Nicoitinic acid may also inhibit the rate limiting enzyme of triglyceride synthesis, diacylglycerol acetyltransferase 2 (Ganji et al., 2004). In a study by Machalke and colleagues, 1982, they have proven that Complamin, in which consists of nicotinic acid lowers serum lipid levels.
High lipid foods
   
Due to its antiplatelet, fibrinolytic and lipid lowering activities, Complamin is a useful drug with multi-targeted effect, targeting lipids, platelets and fibrin plugs for a total protection from more serious vascular problems.
In a study made by Mfifi and colleagues (1979), they found that upon Complamin promotes the healing of leg ulcers associated with blood abnormalities like thalassaemia.
Complamin has also found its use as a cognitive drug, improving sensory register, short-term as well long-term memory. In a study by Loriaux et al. (1985), they found that Complamin possibly enhances cell glucose metabolism and improves oxygen supply in the brain. In a study by Brenner (1983), he reported that Complamin increases glucose concentration in the brain of animal models. This mechanism may very well be the reason for improvement of cognitive function - more energy source, better functioning for brain cells.
In a study by Lehmann and Grobe-Einsler (1993), they monitored the use of Complamin. They found the drug provided significant results for the management of cerbrovascular insufficiency. Aside from that, the study was able to find that 87% of the patients did not experience adverse drug effects.
Side Effects, Precautions
Low incidence of general itching and flushing was found, as well as reddening of the skin, which varies per patient.
Caution is advised to patients with diabetes and gout, because it increases glucose levels and uric levels in the blood, respectively. Liver problems may also occur, which is seen with an increase in liver enzymes up to twice of normal values. Liver toxicity must be monitored. Complamin is contraindicated to patients with severe peptic disease.
Bibliography
Afifi, A. M., Adnan, M., Taha, M., and Amasha, M. E., 1979, Xanthinol nicotinate in the management of leg ulcers associated with haemoglobinopathies
Bieroń, K., Swies, J., Kostka-Trabka, E., and Gryglewski, R.J., 1998, Thrombolytic and antiplatelet action of xanthinol nicotinate (Sadamin): possible mechanisms
Brenner. G., 1983, Effect of xanthinol nicotinate on brain metabolism in rats
Cheng, K., Wu, T., Wu, K. K., et al., 2005, Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans
Gaevyĭ, M. D., Sankina, T. V., Nagornaia, G.V., 1984, Effect of pentoxyfylline and xanthinol nicotinate on the overall blood pressure and tonus of cerebral and peripheral vessels
Ganji, H., Tavintharan, S., Zhu, D., et al., 2004, Niacin noncompetitively inhibits DGAT2 but not DGAT1 activity in HepG2 cells
Hegde, K. S., Selvamurthy, W., Ray, U. S., and Patil, S. K., 1991, Role of xanthinol
nicotinate in the revival of monkeys subjected to acute haemorrhagic shock
Knopp, R. H., Ginsberg, J., Albers, J. J., et al. Contrasting effects of unmodified and time-release forms of niacin on lipoproteins in hyperlipidemic subjects: Clues to mechanism of action of niacin
Loriaux, S. M., Deijen, J. B., Orlebeke, J. F., De Swart, J. H., 1985, The effects of nicotinic acid and xanthinol nicotinate on human memory in different categories of age. A double blind study
Machalke, K., Djaja, S., and Richter, E., 1982, Lipid-lowering effect of etofibrate, bezafibrate and xanthinol nicotinate in patients with hyperlipoproteinemias, Ther Ggw.
121(5):301-311
Mungiu, O. C., Topoliceanu, F., Ionescu G.D., The action of xanthinol nicotinate on the central and peripheral arterial pressure and on respiration in dogs
Seidel G., and Endell, W., 1977, Effect of xanthinol nicotinate treatment on platelet aggregation
Sweetman, S. C. ed., 2009, Martindale, The complete drug reference 36th ed, London: Pharmaceutical Press, 1433
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