Effects of human exposure to selected pesticides on hematological profile, liver and kidney functions, as well as variations in butyrylcholinesterase (BChE) concentrations and BChE gene were investigated. Additionally, pesticides-related knowledge, attitude, pesticides-handling practices, and health-related symptoms, including depression in these subjects were studied. The study group consisted of 427 individuals of similar socio-economic status: 256 farmers and 61 pesticides vendors exposed to pesticides versus 83 non-exposed individuals and 27 non-exposed vendors (control). A structured questionnaire was used for evaluation of attitude, practices and selfreported health-related symptoms including depression. Blood samples were also collected from all the individuals for hematological and biochemical analyses. Depression was more prevalent among farmers with prolonged exposure duration to pesticides and poor pesticides handling practices (P = 0.001); farmers that smoked suffered more depression than the non-smokers. Farmers that did not use any protective measures showed significantly higher prevalence of health-related disorders, such as nervous system effects, eyes irritation, skin rashes, urinary, cardiac, gastro-intestinal, and respiratory problems compared to the subjects taking protective measures. Blood analyses of pesticides-exposed farmers and vendors showed significantly elevated values of urea, creatinine, aspartate transaminase (AST) and alanine transaminase (ALT), whereas significant decrease in levels of BChE, serum albumin and total proteins, erythrocytes, leucocytes, granulocytes numbers, hemoglobin, haemocrit number, mean corpuscular hemoglobin (MCH), platelet count (PLT), platelets distribution width count (PDWC) compared to the level of these parameters in control subjects. Of the study individuals, blood samples of the most affected farmers were selected for genetic analysis of Exon 1 of BChE gene. It was found that a single synonymous SNP A>G was observed at the locus 2417 when comparing with the (gb M32388.1) available in the NCBI. The mutation was observed in all the samples that related with person having pesticides exposure. The present study confirms that pesticide exposure may adversely affect human health and alter vital hematological and biochemical parameters; additionally, alterations at gene level may also occur. Based on the findings of this study, safer and improved agricultural practices are suggested to pesticides handlers (farmers as well as vendors and retailers) to avoid health hazards.