Filariasis , drugs used

Diethylcarbamazine is an anthelmintic drug that does not resemble other antiparasitic compounds although it has some relationship with piperazine derivatives and it has been useful in the management of filariasis due to Wuchereria bancrofti or Brugia malayi and Loa loa and of tropical eosinophilia. It is a lipoxygenase inhibitor and alters the surface structure of the parasite making it more susceptible to destruction by the host. It is well absorbed and widely distributed. It is eliminated with an half-life of 5-13 hours both by metabolism and excretion unchanged in the urine. 

During the last four decades, microfilaricidal diethylcarbamazine [46] and macrofilaricidal suramin [47,48] have been used for the treatment of filariasis however, iboth of these drugs possess unwanted side-effects such as mazzotti reaction, toxicity, etc. Suramin is highly active against the adult worm of 0. volvulus [47] in humans, but it is very toxic to the kidney, liver and bone marrow and has other side-effects similar to DEC. DEC in the treatment of onchocerciasis produces severe mazzotti reaction (an allergic response due to rapid death of microfilariae) along with other side-effects such as pruritus and anaphylactic shock. However, the mass treatment of lymphatic filariasis with DEC was successful due to a lower and milder incidence of these adverse... 

Although a number of natural products have enjoyed wide usage in the treatment of various helminth diseases of man and domestic animals prior to 1960, with the advent of more effective and safer synthetic anthelmintics most of them were eventually abandoned and are now of historical value only [52]. For example, santonin was included in 25th edition of the United States Dispensary (1955), but was removed from the U.S. Medical Compendium of National Formulary (1960). Similarly, aspidium oleoresin was included in the U.S. Pharmacopeia of 1960 and the full clinical usage of this drug was available in the U.S. Dispensary only until 1973 [1]. This makes the description of SAR and synthesis of most of the anthelmintic natural products less meaningful and is, therefore, not discussed in the present text. However, the SAR profile of avermectins and milbemycins is discussed, of which the former have in recent years been used extensively in the treatment of onchocerciasis and lymphatic filariasis in humans [20]. 

Oinical use Diethylcarbamazine is the drug of choice for filariasis and an alternative... 

In the beginning, for the most part the metabolites of drugs could only be identified in urine when a spectrum of the isolated (or independently synthesized) substance was known. For example, oxpentifylline, extensively used in the treatment of vascular diseases, and its acidic metabolite l-(4 -carboxybutyl)-3,7-dimethylxanthine can be directly identified and quantified in a freeze-dried urine sample using a 250-MHz spectrometer [6], The medication of lymphatic filariasis with diethylcarbamazepine has to be monitored for several reasons [7]. Since the drug lacks an absorbing chromophore (HPLC/UV-detection) and GC needs a special detector and troublesome extraction method, H NMR spectroscopy appears to be suitable for the urine analysis the urine samples were mixed with 10% D2O and directly measured afterwards. 

Diethylcarbamazine (A,A-diethyl-4-methyl-l-piperazinecarboxamide Figure 12.13) a piperazine derivative, is an anthelmintic drug that in humans is used for the treatment of filariasis. In veterinary medicine it is used mainly, indeed almost exclusively for the prevention and treatment of heartworm (Dilofilaria immitis) in dogs. ... 

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