Snake venom metalloproteinases (SVMPs) play an important role in local and systemic manifestations of viperid snakebite envenomations. The therapy available has been based on the intravenous administration of antivenoms; nevertheless, they have a limited efficacy against local effects provoked by SVMPs. For this reason, it is important to search for alternative venom inhibitors, either synthetic or natural, that would complement the action of antivenoms, particularly regarding neutralization of local tissue damage caused by SVMPs. In this review, information about low molecular mass synthetic and natural molecules that have been reported to be inhibitors of SVMPs is described, focusing on their ability to abrogate the activities of SVMPs and on the molecular mechanisms involved.