IVERMECTIN: AN ENDECTOCIDE

ABSTRACT

 

Ivermectin (IVM), a dihydro derivative of avermectin (AVM), originating solely from the fermentation products of Streptomyces avermitilis had an immeasurably beneficial impact in improving the lives and welfare of billions of people worldwide. Originally introduced as a veterinary drug, it was quickly discovered to be ideal in combating two of the world’s most devastating and disfiguring diseases; onchocerciasis and lymphatic filariasis (LF) which has plagued the world’s poor throughout the tropics for centuries. Following its approval for human use in 1987, Merck & Co. established a worldwide program to donate IVM as Mectizan® to treat onchocerciasis (river blindness). Building on the successful implementation of the river blindness program, in 1998 Merck & Co. expanded its commitment to include donating Mectizan® for LF. It is now being used as a tool in campaigns to eliminate both diseases globally and has also been used to successfully overcome several other human diseases. IVM is frequently used in veterinary and human medicine due to its broad spectrum of activity, high efficacy and wide margin of safety. In humans, IVM is used for the treatment of various endo- and ecto-parasitic diseases like strongyloidiasis, cutaneous larva migrans, filariasis, scabies and lice infestations. New uses for it are continually being found. Of particular interest is its potential as an additional vector control tool for malaria. This paper looks in-depth at IVM, a drug that is active against endo- and ecto-parasites of humans and animals.

TABLE OF CONTENTCERTIFICATION…………………………………………………………………iACKNOWLEDGEMENT…………………………………………………………iiDEDICATION…………………………………………………………………….iiiTABLE OF CONTENT…………………………………………………………...ivLIST OF ABREVIATIONS……………………………………………………….viABSTRACT……………………………………………………………………….viiiCHAPTER ONEINTRODUCTION………………………………………………………………...1CHAPTER TWODISCOVERY AND DEVELOPMENT OF IVERMECTIN…………………...52.1. History and Discovery of Ivermectin………………………………………….52.2. Development of Ivermectin…………………………………………………....82.2.1. Chemical Composition of Ivermectin………………………………..8 2.2.2. Production and Synthesis of Ivermectin…………………………….10CHAPTER THREEIVERMECTIN IN THE TREATMENT OF HUMAN DISEASES…………..133.1. Advent of Ivermectin for Human Use………………………………………...133.2. Dosage and Efficacy of Ivermectin in the Treatment of Human Diseases……203.3. Pharmacokinetics of Ivermectin………………………………………………30 3.4. Mode of Action of Ivermectin………………………………………………...373.5. Adverse Effects of Drug Use………………………………………………….41CHAPTER FOURTOXICITY AND DRUG RESISTANCE……………………………………….464.1. Toxicity of Ivermectin………………………………………………………...464.2. Drug Resistance……………………………………………………………….50iv CHAPTER FIVE NEW HORIZONS IN THE USE OF IVERMECTIN…………………………...545.1. Control of Malaria and Other Mosquito-Borne Parasitoses………………….....545.2. Control of Trypanosomiasis…………………………………………………….615.3. Control of Leishmaniasis………………………………………………………. 625.4. Control of other Parasitic Infections/Infestations……………………………….635.5. Antiviral Potency………………………………………………………………..655.6. Antibacterial Potency……………………………………………………………665.7. Anticancer Agent………………………………………………………………..675.8. Anti-inflammatory Agent………………………………………………………..685.9. Anti-Diabetic Agent……………………………………………………………..68CHAPTER SIXSUMMARY AND CONCLUSION………………………………………………....69REFERENCES……………………………………………………………………....71