Ambazone is an oral

antiseptic An antiseptic ( and ) is an antimicrobial substance or compound that is applied to living tissue to reduce the possibility of sepsis, infection, or putrefaction. Antiseptics are generally distinguished from ''antibiotics'' by the latter's abil ...

. Ambazone was patented in 1957 by

Bayer Bayer AG (English: , commonly pronounced ; ) is a German multinational pharmaceutical and biotechnology company and is one of the largest pharmaceutical companies and biomedical companies in the world. Headquartered in Leverkusen, Bayer' ...

under the trade name Iversal, and briefly used in Germany. It is still used in Russia, countries of the former Soviet Union, Poland and Romania. It has not been approved by the United States

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...

(FDA).

Synthesis

Ambazone can be obtained in a two step synthetic method, reacting 1,4-benzoquinone with aminoguanidine and thiosemicarbazide. Ambazone synthesis01

Obtaining a pharmaceutical grade material is difficult due to high amounts of by-products, synthetic intermediates and decomposition products.

Applications

Bacteriostatic A bacteriostatic agent or bacteriostat, abbreviated Bstatic, is a biological or chemical agent that stops bacteria from reproducing, while not necessarily killing them otherwise. Depending on their application, bacteriostatic antibiotics, disinfec ...

action on hemolytic streptococcus, ''

Streptococcus pneumoniae ''Streptococcus pneumoniae'', or pneumococcus, is a Gram-positive, spherical bacteria, hemolysis (microbiology), alpha-hemolytic member of the genus ''Streptococcus''. ''S. pneumoniae'' cells are usually found in pairs (diplococci) and do not f ...

'' and viridans streptococci.

Physical properties

Through experimental testing ambazone has shown

properties, along with anti-tumor properties. Ambazone has the following physical characteristics. Ambazone is prepared by way of solid based crystallization or grinding.

Mode of action

The mode of action for ambazone has been studied extensively and has been shown to react via different methods. Ambazone shows low

mutagenic In genetics, a mutagen is a physical or chemical agent that permanently changes genetic material, usually DNA, in an organism and thus increases the frequency of mutations above the natural background level. As many mutations can cause cancer in ...

activity and no cardiovascular, CNS, metabolic, or gastrointestinal

side-effects In medicine, a side effect is an effect of the use of a medicinal drug or other treatment, usually adverse but sometimes beneficial, that is unintended. Herbal and traditional medicines also have side effects. A drug or procedure usually used ...

with I.V. doses up to 10-5 mol/kg and oral doses up to 10-3 mol/kg. Ambazone can be administered via oral or I.V. administration, but the problem with oral administration is that one experimental study shows there is only a 35–50% absorption while another study shows 40% in the intestines; these results would tend to lead the reader to think that ambazone would not be the best choice for treatment, because with such a low absorbance, there is going to have to be a greater concentration ingested to gain a positive effect from the drug. The problem with a greater concentration is that ambazone has a half-life of 6–7 hours. It was stated above that ambazone possess no CNS side-effects due to the fact, that it will not cross the blood brain barrier. Although this is the body's way of protecting unwanted substances from attacking the brain, this also limits the treatment of brain tumors with ambazone.

Research

The therapeutic properties of ambazone were studied in lab rats and the therapeutic dose was determined to be 60–125 mg/kg of body weight. As stated above, ambazone possesses anti-septic properties shown by its increased activity against gram-positive cocci. Along with anti-septic properties, ambazone has also shown its ability to fight forms of leukemia in lab rats. When administered orally the results showed prolongation of life expectancy and curing of L1210 and P388

leukemia Leukemia ( also spelled leukaemia; pronounced ) is a group of blood cancers that usually begin in the bone marrow and produce high numbers of abnormal blood cells. These blood cells are not fully developed and are called ''blasts'' or '' ...

in lab rats. Scientists used different methods to determine the results, such as; mean survival time (MST), percent increase of life span, survival rates, percent change in body weights and number of peritoneal cells. When testing ambazone via AMES with no metabolic activation, it was found there are no mutagenic or carcinogenic properties. When the same test was performed with metabolic activation or when the C-Test was performed, it showed the potential for mutagenicity. The results show two different paths and until further testing has been performed it cannot be determined if the good outweighs the bad when it comes to using ambazone for treatment.

References

{{Stomatological preparations Antiseptics Antibiotics Guanidines Thioureas Thiosemicarbazones