Although the venom of the diamondback isn't particularly toxic, the size of the snake allows a larger capacity of venom which is released from its two prominent fangs. It's not uncommon that only one bite mark from one fang is visible after a strike. Fangs can break or bend, or the bite area may be small, causing a miss. All pit vipers have the ability to control the flow of venom through their fangs, allowing the diamondback to release most of its venom in a single strike (though often a pit viper will not release any of its venom).

Most of the toxin released is proteolytic like all other American pit vipers. Proteolytic venoms are, in fact, advanced and concentrated fluids that destroy tissues and other cells through intramolecular digestion. A few toxic effects include: cytotoxic (destroys cells), hemotoxic (destroys red blood cells), myotoxic (causes paralysis and muscle destruction), hemorrhagic (causes persistent bleeding). Smaller amounts of neurotoxins are also present. Unlike neurotoxins, hemotoxin envenomations becomes quickly apparent; the area around the wound swells at a rapid rate. Discoloration and pain are also experienced shortly after being bitten. Professional medical attention should be sought immediately, especially when the victim is a child. The smaller the victim the less time it takes for the venom to spread. Although it is commonly believed that baby or young rattlesnakes deliver more concentrated venom and are thus more dangerous, this idea is not supported by scientific evidence. The amount of venom delivered is a much more important indicator of the bite's danger than the venom's concentration, and since larger (older) snakes can deliver much more venom, larger rattlesnakes should always be considered more dangerous even though many bites from adult snakes are "dry"

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